HRP20040684B1 - Spojevi 2,4-pirimidindiamina i njihova upotreba - Google Patents

Spojevi 2,4-pirimidindiamina i njihova upotreba

Info

Publication number
HRP20040684B1
HRP20040684B1 HRP20040684AA HRP20040684A HRP20040684B1 HR P20040684 B1 HRP20040684 B1 HR P20040684B1 HR P20040684A A HRP20040684A A HR P20040684AA HR P20040684 A HRP20040684 A HR P20040684A HR P20040684 B1 HRP20040684 B1 HR P20040684B1
Authority
HR
Croatia
Prior art keywords
compounds
release
methods
pyrimidinediamine compounds
receptor signaling
Prior art date
Application number
HRP20040684AA
Other languages
English (en)
Inventor
Rajinder Singh
Ankush Argade
Donald G. Payan
Susan Molineux
Sacha J. Holland
Jeffrey Clough
Holger Keim
Somasekhar Bhamidipati
Catherine Sylvain
Hui Li
Alexander B. Rossi
Original Assignee
Rigel Pharmaceuticals, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=32996332&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20040684(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Rigel Pharmaceuticals, Inc. filed Critical Rigel Pharmaceuticals, Inc.
Publication of HRP20040684A2 publication Critical patent/HRP20040684A2/hr
Publication of HRP20040684B1 publication Critical patent/HRP20040684B1/hr

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/5381,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines having two or more nitrogen atoms in the same ring, e.g. oxadiazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/14Decongestants or antiallergics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/341,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/361,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic System
    • C07F5/02Boron compounds
    • C07F5/027Organoboranes and organoborohydrides

Abstract

Ovaj izum omogućuje spojeve 2,4-pirimidindiamina koji inhibiraju IgE i/ili IgG receptor signalizirajuće kaskade koji vode oslobađanju kemijskih posrednika, međuproizvode i metode sinteziranja spojeva i metode korištenja spojeva u različitim kontekstima, uključujući i liječenje i prevenciju bolesti karakteriziranih, prouzročenih ili vezanih za oslobađanje kemijskih posrednika putem degranulacije i drugih procesa na koje utječe aktiviranje IgE i/ili IgG receptora signalizirajućih kaskada.
HRP20040684AA 2002-02-01 2004-07-23 Spojevi 2,4-pirimidindiamina i njihova upotreba HRP20040684B1 (hr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US35326702P 2002-02-01 2002-02-01
US35333302P 2002-02-01 2002-02-01
US39967302P 2002-07-29 2002-07-29
US43427702P 2002-12-17 2002-12-17
PCT/US2003/003022 WO2003063794A2 (en) 2002-02-01 2003-01-31 2,4-pyrimidinediamine compounds and their uses

Publications (2)

Publication Number Publication Date
HRP20040684A2 HRP20040684A2 (hr) 2008-12-31
HRP20040684B1 true HRP20040684B1 (hr) 2014-07-04

Family

ID=32996332

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20040684AA HRP20040684B1 (hr) 2002-02-01 2004-07-23 Spojevi 2,4-pirimidindiamina i njihova upotreba

Country Status (25)

Country Link
US (41) US7557210B2 (hr)
EP (2) EP1471915B1 (hr)
JP (2) JP4658477B2 (hr)
KR (1) KR101037856B1 (hr)
CN (2) CN102174024B (hr)
AT (1) ATE524184T1 (hr)
AU (2) AU2003208931C1 (hr)
BR (1) BRPI0307355C1 (hr)
CA (1) CA2474277C (hr)
CY (1) CY1112516T1 (hr)
DK (2) DK1471915T3 (hr)
ES (2) ES2440283T3 (hr)
HK (2) HK1154216A1 (hr)
HR (1) HRP20040684B1 (hr)
IL (1) IL221381A (hr)
MX (2) MXPA04007386A (hr)
NO (1) NO328071B1 (hr)
NZ (1) NZ534361A (hr)
PL (1) PL214988B1 (hr)
PT (2) PT1471915E (hr)
RS (2) RS54105B1 (hr)
SG (1) SG167664A1 (hr)
SI (2) SI1471915T1 (hr)
TW (1) TWI329105B (hr)
WO (1) WO2003063794A2 (hr)

Families Citing this family (353)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100480242C (zh) * 2001-05-29 2009-04-22 舍林股份公司 Cdk抑制性嘧啶化合物、其制备方法以及作为药物的应用
JP4510442B2 (ja) * 2001-06-26 2010-07-21 ブリストル−マイヤーズ スクイブ カンパニー TNF−α発現のN−ヘテロ環インヒビター
US7638522B2 (en) * 2001-08-13 2009-12-29 Janssen Pharmaceutica N.V. Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino] benzonitrile
US8101629B2 (en) * 2001-08-13 2012-01-24 Janssen Pharmaceutica N.V. Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile
JO3429B1 (ar) * 2001-08-13 2019-10-20 Janssen Pharmaceutica Nv مشتقات برميدينات مثبطة فيروس الايدز
EP2332924A1 (de) * 2001-10-17 2011-06-15 Boehringer Ingelheim Pharma GmbH & Co. KG Pyrimidinderivate, Arzneimittel enthaltend diese Verbindungen, deren Verwendung und Verfahren zu ihrer Herstellung
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
CA2476281A1 (en) * 2002-02-08 2003-08-14 Smithkline Beecham Corporation Pyrimidine compounds
GB0206215D0 (en) 2002-03-15 2002-05-01 Novartis Ag Organic compounds
CA2489648A1 (en) * 2002-06-17 2003-12-24 Smithkline Beecham Corporation Chemical process
NZ537752A (en) 2002-07-29 2006-12-22 Rigel Pharmaceuticals Inc Use of 2,4-pyrimidinediamine compounds in the preparation of medicaments for treating autoimmune diseases
EP2130541A3 (en) * 2002-07-29 2013-12-18 Rigel Pharmaceuticals, Inc. Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
KR101140785B1 (ko) * 2002-08-09 2012-05-03 얀센 파마슈티카 엔.브이. 4-〔〔4-〔〔4-(2-시아노에테닐)-2,6-디메틸페닐〕아미노〕-2-피리미디닐〕아미노〕벤조니트릴의 제조방법
RS20050363A (en) * 2002-11-28 2007-11-15 Schering Aktiengesellschaft, Chk-,pdk-and akt-inhibitory pyrimidines,their production an use as pharmaceutical agents
US7109337B2 (en) 2002-12-20 2006-09-19 Pfizer Inc Pyrimidine derivatives for the treatment of abnormal cell growth
SI1625121T1 (sl) 2002-12-20 2010-04-30 Pfizer Prod Inc Derivati pirimidina za zdravljenje abnormalne rasti celic
UA80767C2 (en) * 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
CA2514612A1 (en) * 2003-01-30 2004-08-12 Boehringer Ingelheim Pharmaceuticals, Inc. 2,4-diaminopyrimidine derivatives useful as inhibitors of pkc-theta
ES2325440T3 (es) * 2003-02-20 2009-09-04 Smithkline Beecham Corporation Compuestos de pirimidina.
CL2004000303A1 (es) * 2003-02-20 2005-04-08 Tibotec Pharm Ltd Compuestos derivados de pirimidinas y triazinas; proceso de preparacion; composicion farmaceutica; y su uso para inhibir la replicacion del vih.
GB0305929D0 (en) * 2003-03-14 2003-04-23 Novartis Ag Organic compounds
US7504396B2 (en) 2003-06-24 2009-03-17 Amgen Inc. Substituted heterocyclic compounds and methods of use
ES2351603T3 (es) 2003-07-25 2011-02-08 Idenix Pharmaceuticals, Inc. Análogos de nucleósidos de purina para el tratamiento de enfermedades causadas por flaviridae incluyendo hepatitis c.
ES2421139T3 (es) * 2003-07-30 2013-08-29 Rigel Pharmaceuticals, Inc. Compuestos de 2,4-pirimidindiamina para su uso en el tratamiento o la prevención de enfermedades autoinmunitarias
EP1648875A1 (en) * 2003-07-30 2006-04-26 Cyclacel Limited 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors
WO2005016894A1 (en) * 2003-08-15 2005-02-24 Novartis Ag 2, 4-pyrimidinediamines useful in the treatment of neoplastic diseases, inflammatory and immune system disorders
GB0321710D0 (en) * 2003-09-16 2003-10-15 Novartis Ag Organic compounds
CA2543249C (en) 2003-11-05 2012-08-07 F. Hoffmann-La Roche Ag Phenyl derivatives as ppar agonists
JP2007511641A (ja) * 2003-11-14 2007-05-10 アシュランド・ライセンシング・アンド・インテレクチュアル・プロパティー・エルエルシー 自己光開始性多官能アクリレートと脂環族エポキシ化合物との二元硬化反応生成物
EP1749827A4 (en) 2004-03-30 2010-04-21 Kyowa Hakko Kirin Co Ltd ANTITUMOR AGENTS
JP2007537238A (ja) 2004-05-14 2007-12-20 ファイザー・プロダクツ・インク 異常細胞増殖の治療のためのピリミジン誘導体
WO2005111024A1 (en) 2004-05-14 2005-11-24 Pfizer Products Inc. Pyrimidine derivatives for the treatment of abnormal cell growth
MXPA06013164A (es) 2004-05-14 2007-02-13 Pfizer Prod Inc Derivados de pirimidina para el tratamiento de crecimiento de celulas anormal.
WO2005118544A2 (en) * 2004-05-18 2005-12-15 Rigel Pharmaceuticals, Inc. Cycloalkyl substituted pyrimidinediamine compounds and their uses
EP1598343A1 (de) * 2004-05-19 2005-11-23 Boehringer Ingelheim International GmbH 2-Arylaminopyrimidine als PLK Inhibitoren
WO2006004776A1 (en) * 2004-06-29 2006-01-12 Rigel Pharmaceuticals, Inc. 4-pyrimidineamine compounds and their uses as anti-proliferative agents
US20060051406A1 (en) * 2004-07-23 2006-03-09 Manjeet Parmar Formulation of insoluble small molecule therapeutics in lipid-based carriers
GB0419160D0 (en) * 2004-08-27 2004-09-29 Novartis Ag Organic compounds
US20060058525A1 (en) * 2004-09-01 2006-03-16 Rajinder Singh Synthesis of 2,4-pyrimidinediamine compounds
WO2006027378A1 (en) * 2004-09-10 2006-03-16 Altana Pharma Ag Roflumilast and syk inhibitor combination and methods of use thereof
AU2005281735A1 (en) * 2004-09-10 2006-03-16 Nycomed Gmbh Ciclesonide and syk inhibitor combination and methods of use thereof
CA2579143A1 (en) 2004-09-13 2006-03-23 Amgen Inc. Vanilloid receptor ligands and their use in treatments
JP2008538544A (ja) 2004-09-23 2008-10-30 レディ ユーエス セラピューティックス, インコーポレイテッド 新規ピリミジン化合物、それらの調製のためのプロセスおよびそれらを含む組成物
AU2005289426A1 (en) * 2004-09-27 2006-04-06 Amgen Inc. Substituted heterocyclic compounds and methods of use
AU2005288866B2 (en) 2004-09-30 2012-07-26 Janssen Sciences Ireland Uc HIV inhibiting 5-substituted pyrimidines
CN101031558B (zh) 2004-09-30 2011-10-05 泰博特克药品有限公司 抑制人类免疫缺陷病毒的5-杂环基嘧啶
WO2006050476A2 (en) * 2004-11-03 2006-05-11 Vertex Pharmaceuticals Incorporated Pyrimidine derivatives as ion channel modulators and methods of use
GB2420559B (en) * 2004-11-15 2008-08-06 Rigel Pharmaceuticals Inc Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
US7557207B2 (en) 2004-11-24 2009-07-07 Rigel Pharmaceuticals, Inc. Spiro 2,4-pyrimidinediamine compounds and their uses
MY169441A (en) * 2004-12-08 2019-04-11 Janssen Pharmaceutica Nv 2,4, (4,6) pyrimidine derivatives
US7555655B2 (en) * 2004-12-22 2009-06-30 5th Fleet, L.L.C. Apparatus, system, and method for generating and authenticating a computer password
ES2337496T3 (es) 2005-01-19 2010-04-26 Rigel Pharmaceuticals, Inc. Profarmacos de compuestos de 2,4-pirimidindiamina y sus usos.
WO2007027238A2 (en) * 2005-05-03 2007-03-08 Rigel Pharmaceuticals, Inc. Jak kinase inhibitors and their uses
JP5225079B2 (ja) 2005-06-08 2013-07-03 ライジェル ファーマシューティカルズ, インコーポレイテッド Jak経路の阻害のための組成物および方法
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US7576053B2 (en) * 2005-06-13 2009-08-18 Rigel Pharmaceuticals, Inc. Methods and compositions for treating degenerative bone disorders
PL1734251T3 (pl) * 2005-06-17 2007-05-31 Magneti Marelli Powertrain Spa Wtryskiwacz paliwa
WO2007028445A1 (en) * 2005-07-15 2007-03-15 Glaxo Group Limited 6-indolyl-4-yl-amino-5-halogeno-2-pyrimidinyl-amino derivatives
PE20070362A1 (es) * 2005-07-15 2007-04-23 Glaxo Group Ltd COMPUESTOS DERIVADOS DE INDAZOL-4-IL-2,4-PIRIMIDINDIAMINA COMO INHIBIDORES DE TIROSINA QUINASA (QUINASA Syk)
EP1746096A1 (en) * 2005-07-15 2007-01-24 4Sc Ag 2-Arylbenzothiazole analogues and uses thereof in the treatment of cancer
EP1924565B1 (en) 2005-09-01 2016-09-14 F.Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p3x2/3 modulators
JP2009511548A (ja) 2005-10-14 2009-03-19 ノイロサーチ アクティーゼルスカブ 新規ピリミジン−2,4−ジアミン誘導体及び小コンダクタンスのカルシウム依存性カリウムチャネルのモジュレーターとしてのこれらの使用
AU2006309013B2 (en) * 2005-11-01 2012-06-28 Impact Biomedicines, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
US8133900B2 (en) * 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
US8604042B2 (en) * 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
US7713987B2 (en) * 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
US8246984B2 (en) * 2005-12-06 2012-08-21 Rigel Pharmaceuticals, Inc. Formulation of insoluble small molecule therapeutics in lipid-based carriers
US7601713B2 (en) 2005-12-15 2009-10-13 Rigel Pharmaceuticals, Inc. Kinase inhibitors and their uses
JP2007186507A (ja) * 2005-12-15 2007-07-26 Nippon Nohyaku Co Ltd フタルアミド誘導体及び農園芸用殺虫剤並びにその使用方法
JP4332590B2 (ja) * 2005-12-21 2009-09-16 ファイザー・プロダクツ・インク 異常細胞増殖を治療するためのピリミジン誘導体
WO2007085540A1 (en) * 2006-01-27 2007-08-02 Glaxo Group Limited 1h-indaz0l-4-yl-2 , 4-pyrimidinediamine derivatives
WO2007120980A2 (en) 2006-02-17 2007-10-25 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for treating or preventing autoimmune diseases
ES2622493T3 (es) * 2006-02-24 2017-07-06 Rigel Pharmaceuticals, Inc. Composiciones y métodos para la inhibición de la ruta de JAK
MX2008012576A (es) 2006-03-30 2008-10-10 Tibotec Pharm Ltd Pirimidinas 5-amido sustituidas inhibidoras del virus de inmunodeficiencia humana.
JP2009544592A (ja) * 2006-07-21 2009-12-17 ノバルティス アクチエンゲゼルシャフト Jakキナーゼ阻害剤としての2,4−ジ(アリールアミノ)−ピリミジン−5−カルボキサミド化合物
US8445437B2 (en) * 2006-07-27 2013-05-21 The Brigham And Women's Hospital, Inc. Treatment and prevention of cardiovascular disease using mast cell stabilizers
AR063946A1 (es) * 2006-09-11 2009-03-04 Cgi Pharmaceuticals Inc Determinadas pirimidinas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden.
CA2673125C (en) 2006-10-19 2015-04-21 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2008051547A1 (en) 2006-10-23 2008-05-02 Cephalon, Inc. Fused bicyclic derivatives of 2,4-diaminopyrimidine as alk and c-met inhibitors
EP2097378B1 (en) * 2006-11-03 2012-09-12 GlaxoSmithKline LLC Novel seh inhibitors and their use
EP2420505A1 (en) 2006-11-21 2012-02-22 Rigel Pharmaceuticals, Inc. Prodrug salts of 2, 4- pyrimidinediamine compounds and their uses
NZ577197A (en) 2006-12-08 2011-02-25 Irm Llc Pyrimidine compounds especially 4-phenylamino-2-arylamino-pyrimidine derivatives and compositions as protein kinase inhibitors
CN101611035A (zh) 2006-12-28 2009-12-23 大正制药株式会社 吡唑并嘧啶化合物
JP5283633B2 (ja) 2006-12-29 2013-09-04 テイボテク・フアーマシユーチカルズ Hiv阻害性5,6−置換ピリミジン
DK2114901T3 (da) 2006-12-29 2014-06-30 Janssen R & D Ireland Hiv-inhiberende 6-substituerede pyrimidiner
US7947698B2 (en) 2007-03-23 2011-05-24 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
US7834024B2 (en) 2007-03-26 2010-11-16 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
TWI484960B (zh) 2007-04-16 2015-05-21 Hutchison Medipharma Entpr Ltd 嘧啶衍生物
CA2684447C (en) 2007-04-18 2012-01-24 Pfizer Products Inc. Sulfonyl amide derivatives for the treatment of abnormal cell growth
CA2693594A1 (en) 2007-07-17 2009-01-22 Rigel Pharmaceuticals, Inc. Cyclic amine substituted pyrimidinediamines as pkc inhibitors
NZ583582A (en) 2007-09-05 2012-02-24 Rigel Pharmaceuticals Inc Xinafoate salt of n4-(2, 2-difluoro-4h-benzo [1,4] oxazin-3-one) -6-yl] -5-fluoro-n2- [3- (methylaminocarbonylmethyleneoxy) phenyl] 2, 4-pyrimidinediamine
CN101808642B (zh) 2007-09-28 2012-05-02 布里格海姆妇女医院公司 肥大细胞稳定剂治疗肥胖症
PT2214487E (pt) * 2007-10-11 2014-02-20 Glaxosmithkline Llc Novos inibidores de seh e sua utilização
WO2009049165A1 (en) * 2007-10-11 2009-04-16 Smithkline Beecham Corporation Novel seh inhibitors and their use
WO2009049154A1 (en) * 2007-10-11 2009-04-16 Smithkline Beecham Corporation NOVEL sEH INHIBITORS AND THEIR USE
TR201807879T4 (tr) * 2007-11-07 2018-06-21 Rigel Pharmaceuticals Inc Bir su ayırma maddesi kullanılarak ıslak granülasyon.
EP2231620A1 (en) * 2007-12-03 2010-09-29 Boehringer Ingelheim International GmbH Diaminopyridines for the treatment of diseases which are characterised by excessive or anomal cell proliferation
JP2011506333A (ja) * 2007-12-06 2011-03-03 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー 新規sEH阻害剤およびその使用
EP2240021A4 (en) * 2008-01-30 2011-08-17 Glaxosmithkline Llc NEW SEH-HEMMER AND ITS USE
WO2009097476A1 (en) * 2008-01-30 2009-08-06 Smithkline Beecham Corporation NOVEL sEH INHIBITORS AND THEIR USE
KR101700454B1 (ko) 2008-02-15 2017-01-26 리겔 파마슈티칼스, 인크. 피리미딘-2-아민 화합물 및 jak 키나제 억제제로서의 그의 용도
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
US8063058B2 (en) 2008-04-16 2011-11-22 Portola Pharmaceuticals, Inc. Inhibitors of syk and JAK protein kinases
KR20100132550A (ko) 2008-04-16 2010-12-17 포톨라 파마슈티컬스, 인코포레이티드 syk 또는 JAK 키나제 억제제로서의 2,6-디아미노-피리미딘-5-일-카르복스아미드
WO2009145856A1 (en) * 2008-04-16 2009-12-03 Portola Pharmaceuticals, Inc. 2, 6-diamino-pyrimidin- 5-yl-carboxamides as syk or jak kinases inhibitors
NZ588830A (en) 2008-04-22 2012-11-30 Portola Pharm Inc Inhibitors of protein kinases
US7829574B2 (en) 2008-05-09 2010-11-09 Hutchison Medipharma Enterprises Limited Substituted quinazoline compounds and their use in treating angiogenesis-related diseases
KR20110025915A (ko) 2008-06-16 2011-03-14 에프. 호프만-라 로슈 아게 오렉시닌 수용체 길항제로서 헤테로방향족 모노아마이드
CA2986640C (en) 2008-06-27 2019-03-26 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
AU2013202496B2 (en) * 2008-06-27 2016-08-04 Celgene Car Llc Heteroaryl compounds and uses thereof
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
US8426430B2 (en) 2008-06-30 2013-04-23 Hutchison Medipharma Enterprises Limited Quinazoline derivatives
TW201008933A (en) 2008-08-29 2010-03-01 Hutchison Medipharma Entpr Ltd Pyrimidine compounds
CA2736258C (en) 2008-09-23 2016-11-29 Rigel Pharmaceuticals, Inc. Tricyclic carbamate jak inhibitors
US20100137313A1 (en) * 2008-10-03 2010-06-03 Astrazeneca Ab Heterocyclic derivatives and methods of use thereof
CA2746810C (en) 2008-12-30 2017-03-14 Rigel Pharmaceuticals, Inc. Pyrimidinediamine kinase inhibitors
ES2555982T3 (es) * 2009-01-15 2016-01-12 Rigel Pharmaceuticals, Inc. Inhibidores de la proteína quinasa C y usos de los mismos
JP5781943B2 (ja) 2009-01-21 2015-09-24 ライジェル ファーマシューティカルズ, インコーポレイテッド 炎症性疾患、自己免疫疾患または増殖性疾患の治療に有用なn2−(3−ピリジルまたはフェニル)−n4−(4−ピペリジル)−2,4−ピリミジンジアミン誘導体
EP2389372B1 (en) 2009-01-23 2015-09-09 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US8592415B2 (en) * 2009-02-11 2013-11-26 Reaction Biology Corp. Selective kinase inhibitors
CA2760794C (en) 2009-05-05 2017-07-25 Dana Farber Cancer Institute Egfr inhibitors and methods of treating disorders
US8367689B2 (en) 2009-05-06 2013-02-05 Portola Pharmaceuticals, Inc. Inhibitors of JAK
WO2010143733A1 (en) 2009-06-09 2010-12-16 Takeda Pharmaceutical Company Limited Novel fused cyclic compound and use thereof
UA108077C2 (xx) 2009-07-02 2015-03-25 Синтез динатрієвої солі n4-(2,2-диметил-4-$(дигідрофосфонокси)метил]-3-оксо-5-піридо$1,4]оксазин-6-іл)-5-фтор-n2-(3,4,5-триметоксифеніл)-2,4-піримідиндіаміну
US20110015155A1 (en) 2009-07-17 2011-01-20 Rigel Pharmaceuticals, Inc. Deuterated 2, 4-Pyrimidinediamine Compounds and Prodrugs Thereof and Their Uses
BR112012002001A2 (pt) * 2009-07-28 2016-05-10 Rigel Pharmaceuticals Inc método para tratar uma doença e/ou distúrbio do olho, formulação farmacêutica, e, kit
EP2490536A4 (en) * 2009-10-23 2013-04-17 Glaxo Wellcome Mfg Pte Ltd COMPOSITION AND METHOD
WO2011063241A1 (en) 2009-11-20 2011-05-26 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses
CA2780759A1 (en) 2009-12-01 2011-06-09 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
GEP20146125B (en) 2009-12-17 2014-07-25 Merck Canada Aminopyrimidines as syk inhibitors
WO2011075560A1 (en) 2009-12-17 2011-06-23 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
MX2012007402A (es) 2009-12-23 2012-08-23 Takeda Pharmaceutical Pirrolidinonas heteroaromaticas fusionadas como inhibidores de tirosina cinasa esplenica (syk).
AT509266B1 (de) * 2009-12-28 2014-07-15 Tech Universität Wien Substituierte pyridine und pyrimidine
US8367315B2 (en) * 2010-03-05 2013-02-05 Adan Rios Inactivation of reverse transcriptases by azido-diarylpyrimidines
MX355697B (es) 2010-04-12 2018-04-27 Supernus Pharmaceuticals Inc Métodos para producir sales de viloxazina y polimorfos novedosos de las mismas.
JP6067550B2 (ja) 2010-04-13 2017-01-25 ライジェル ファーマシューティカルズ, インコーポレイテッド 2,4−ピリミジンジアミン化合物およびそのプロドラッグならびにそれらの使用
MX2012013274A (es) 2010-05-21 2013-05-28 Chemilia Ab Novedosos derivados de la pirimidina.
EP2395001A1 (en) 2010-05-21 2011-12-14 Chemilia AB Novel pyrimidine derivatives
JP5713367B2 (ja) 2010-06-04 2015-05-07 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Lrrk2モジュレーターとしてのアミノピリミジン誘導体
EP2595982B1 (en) 2010-07-21 2018-06-13 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
BR112013001632B1 (pt) 2010-07-28 2021-05-25 Rigel Pharmaceuticals composto, composição farmacêutica, e, método de fabricar um composto
KR20130099040A (ko) 2010-08-10 2013-09-05 셀진 아빌로믹스 리서치, 인코포레이티드 Btk 억제제의 베실레이트 염
WO2012061428A2 (en) 2010-11-01 2012-05-10 Portola Pharmaceuticals, Inc. Nicotinamides as jak kinase modulators
US8975249B2 (en) 2010-11-01 2015-03-10 Celgene Avilomics Research, Inc. Heterocyclic compounds and uses thereof
US20130317029A1 (en) 2010-11-01 2013-11-28 Portola Pharmaceuticals, Inc. Oxypyrimidines as syk modulators
TW201238938A (en) 2010-11-01 2012-10-01 Portola Pharm Inc Benzamides and nicotinamides as Syk modulators
EP2635285B1 (en) 2010-11-01 2017-05-03 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
WO2012060847A1 (en) 2010-11-07 2012-05-10 Targegen, Inc. Compositions and methods for treating myelofibrosis
US8796255B2 (en) 2010-11-10 2014-08-05 Celgene Avilomics Research, Inc Mutant-selective EGFR inhibitors and uses thereof
BR112013011600B1 (pt) 2010-11-10 2022-01-11 Genentech, Inc Derivados de pirazol aminopirimidina, seu uso e composição que os compreende
WO2012097207A2 (en) * 2011-01-13 2012-07-19 The Johns Hopkins University Cytokine profiles as methods for diagnosis and prognosis of irritable bowel syndrome
EP2489663A1 (en) 2011-02-16 2012-08-22 Almirall, S.A. Compounds as syk kinase inhibitors
EP2502924A1 (en) 2011-03-24 2012-09-26 Chemilia AB Novel pyrimidine derivatives
US9006241B2 (en) 2011-03-24 2015-04-14 Noviga Research Ab Pyrimidine derivatives
US9249124B2 (en) * 2011-03-30 2016-02-02 H. Lee Moffitt Cancer Center And Research Institute, Inc. Aurora kinase inhibitors and methods of making and using thereof
AU2016244228B2 (en) * 2011-04-22 2019-02-21 Signal Pharmaceuticals, Llc Substituted diaminocarboxamide and diaminocarbonitrile pyrimidines, compositions thereof, and methods of treatment therewith
KR102055532B1 (ko) 2011-04-22 2019-12-12 시그날 파마소티칼 엘엘씨 치환된 디아미노카르복스아미드 및 디아미노카르보니트릴 피리미딘, 그의 조성물, 및 그를 사용하는 치료 방법
WO2012154520A1 (en) 2011-05-10 2012-11-15 Merck Sharp & Dohme Corp. Pyridyl aminopyridines as syk inhibitors
WO2012154518A1 (en) 2011-05-10 2012-11-15 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as syk inhibitors
EP2706853B1 (en) 2011-05-10 2017-06-14 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
WO2012167423A1 (en) 2011-06-08 2012-12-13 Hutchison Medipharma Limited Substituted pyridopyrazines as novel syk inhibitors
US9056873B2 (en) 2011-06-22 2015-06-16 Takeda Pharmaceutical Company Limited Substituted 6-aza-isoindolin-1-one derivatives
AU2012288632B2 (en) 2011-07-28 2017-08-17 Rigel Pharmaceuticals, Inc. New (trimethoxyphenylamino)pyrimidinyl formulations
ES2643235T3 (es) 2011-09-02 2017-11-21 Purdue Pharma Lp Pirimidinas como bloqueantes del canal de sodio
WO2013037705A2 (en) 2011-09-16 2013-03-21 Fovea Pharmaceuticals Aniline derivatives,their preparation and their therapeutic application
US9216173B2 (en) 2011-10-05 2015-12-22 Merck Sharp & Dohme Corp. 2-Pyridyl carboxamide-containing spleen tyrosine kinase (SYK) inhibitors
EP2763975B1 (en) 2011-10-05 2016-04-06 Merck Sharp & Dohme Corp. 3-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
US9006444B2 (en) 2011-10-05 2015-04-14 Merck Sharp & Dohme Corp. Phenyl carboxamide-containing spleen tyrosine kinase (SYK) inhibitors
EP2768480A1 (en) 2011-10-21 2014-08-27 Rigel Pharmaceuticals, Inc. Method and device for administering xinafoate salt of n4-(2,2-difluoro-4h-benzo [1,4]oxazin-3-one) -6-yl]-5-fluoro-n2- [3- (methylaminocarbonylmethyleneoxy) phenyl]2,4-pyrimidinediamine
CA2853498A1 (en) 2011-10-28 2013-05-02 Celgene Avilomics Research, Inc. Methods of treating a bruton's tyrosine kinase disease or disorder
KR102019530B1 (ko) 2011-11-23 2019-09-06 포톨라 파마슈티컬스, 인코포레이티드 피라진 키나아제 저해제
EP2802577B1 (en) * 2012-01-13 2017-03-01 Bristol-Myers Squibb Company Triazolyl-substituted pyridyl compounds useful as kinase inhibitors
EP2825041B1 (en) 2012-03-15 2021-04-21 Celgene CAR LLC Solid forms of an epidermal growth factor receptor kinase inhibitor
RS57901B1 (sr) 2012-03-15 2019-01-31 Celgene Car Llc Soli inhibitora kinaze receptora epidermalnog faktora rasta
EP2827890B1 (en) 2012-03-23 2019-08-28 The University Of Queensland Immunomodulatory agent and uses therefor
EP2833889B1 (en) 2012-04-04 2017-11-01 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
WO2013166413A2 (en) * 2012-05-03 2013-11-07 Saint Louis College Of Pharmacy Compositions and methods for increasing neurotrophic peptides
US20130310340A1 (en) 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
WO2013192128A1 (en) 2012-06-20 2013-12-27 Merck Sharp & Dohme Corp. Imidazolyl analogs as syk inhibitors
EP2863914B1 (en) 2012-06-20 2018-10-03 Merck Sharp & Dohme Corp. Pyrazolyl derivatives as syk inhibitors
US9416111B2 (en) 2012-06-22 2016-08-16 Merck Sharp & Dohme Corp. Substituted diazine and triazine spleen tyrosine kinease (Syk) inhibitors
EP2863916B1 (en) 2012-06-22 2018-07-18 Merck Sharp & Dohme Corp. Substituted pyridine spleen tyrosine kinase (syk) inhibitors
KR101446742B1 (ko) 2012-08-10 2014-10-01 한국화학연구원 N2,n4-비스(4-(피페라진-1-일)페닐)피리미딘-2,4-디아민 유도체 또는 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
US9353066B2 (en) 2012-08-20 2016-05-31 Merck Sharp & Dohme Corp. Substituted phenyl-Spleen Tyrosine Kinase (Syk) inhibitors
EP2711365A1 (en) 2012-09-21 2014-03-26 Chemilia AB 4-Indazolylamino-2-(2-(indol-3-yl)ethyl)aminopyrimidines useful for the treatment of cancer
EP2711364A1 (en) 2012-09-21 2014-03-26 Chemilia AB 4-(Indolyl or benzimidazolyl)amino-2-(2-(indol-3-yl)ethyl)aminopyrimidines useful for the treatment of cancer
WO2014048065A1 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Triazolyl derivatives as syk inhibitors
EP2903970A4 (en) 2012-10-08 2016-11-30 Portola Pharm Inc SUBSTITUTED PYRIMIDINYL KINASE INHIBITORS
CA2892677A1 (en) 2012-12-04 2014-06-12 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
EP2931281B1 (en) 2012-12-12 2018-01-17 Merck Sharp & Dohme Corp. Amino-pyrimidine-containing spleen tyrosine kinase inhibitors
EP2935226A4 (en) 2012-12-21 2016-11-02 Celgene Avilomics Res Inc HETEROARYL COMPOUNDS AND USES THEREOF
WO2014100314A1 (en) 2012-12-21 2014-06-26 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors
EP2948150A1 (en) 2013-01-25 2015-12-02 Rigel Pharmaceuticals, Inc. Compounds and methods for treating inflammatory bowel diseases
PE20151274A1 (es) 2013-02-08 2015-09-12 Celgene Avilomics Res Inc Inhibidores de erk y sus usos
CA2905993C (en) * 2013-03-14 2022-12-06 Tolero Pharmaceuticals, Inc. Substituted 4-amino-pyrimidinyl-2-amino-phenyl derivatives and pharmaceutical compositions thereof for use as jak2 and alk2 inhibitors
US9169249B2 (en) 2013-03-14 2015-10-27 Rigel Pharmaceuticals, Inc. Protein kinase C inhibitors and uses thereof
US10150742B2 (en) * 2013-03-15 2018-12-11 President And Fellows Of Harvard College Substituted heterocyclic compounds for treating or preventing viral infections
WO2014176216A1 (en) 2013-04-26 2014-10-30 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyrimidines as spleen tyrosine kinase inhibitors
EP2988744A4 (en) 2013-04-26 2016-11-02 Merck Sharp & Dohme THIAZOLE SUBSTITUTED AMINOHETEROARYL COMPOUNDS TYLOSINE KINASE SPLENIC INHIBITORS
CN105658650B (zh) * 2013-06-24 2019-01-08 默克专利有限公司 用作***受体调节剂的咪唑化合物及其用途
CN105592850B (zh) 2013-08-06 2019-11-15 H·李·莫菲特癌症中心研究所公司 Ack1/tnk2酪氨酸激酶的抑制剂
US9492471B2 (en) 2013-08-27 2016-11-15 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase
US9415049B2 (en) 2013-12-20 2016-08-16 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
WO2015095444A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
WO2015094997A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
EP3083559B1 (en) 2013-12-20 2021-03-10 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
NZ715903A (en) 2014-01-30 2017-06-30 Signal Pharm Llc Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use
EP3653207A1 (en) 2014-02-10 2020-05-20 Respivant Sciences GmbH Mast cell stabilizers treatment for systemic disorders
JP2017505348A (ja) 2014-02-10 2017-02-16 パタラ ファーマ リミテッド ライアビリティ カンパニー 肺疾患治療のための肥満細胞安定剤
US9340540B2 (en) 2014-02-28 2016-05-17 Nimbus Lakshmi, Inc. TYK2 inhibitors and uses thereof
US9775839B2 (en) 2014-03-13 2017-10-03 Merck Sharp & Dohme Corp. 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors
MX2016012574A (es) 2014-03-28 2017-09-26 Calitor Sciences Llc Compuestos heteroarilo sustituidos y metodos de uso.
CN112430250A (zh) 2014-08-12 2021-03-02 莫纳什大学 定向淋巴的前药
ES2741785T3 (es) 2014-08-13 2020-02-12 Celgene Car Llc Formas y composiciones de un inhibidor de ERK
WO2016060963A1 (en) 2014-10-14 2016-04-21 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use
ES2882954T3 (es) 2014-12-16 2021-12-03 Signal Pharm Llc Usos médicos que comprenden métodos para la medición de la inhibición de la quinasa c-Jun N-terminal en la piel
US9796685B2 (en) 2014-12-16 2017-10-24 Signal Pharmaceuticals, Llc Formulations of 2-(tert-butylamino)-4-((1R,3R,4R)-3-hydroxy-4-Methylcyclohexylamino)-pyrimidine-5-carboxamide
EP3250557A4 (en) 2015-01-29 2018-06-20 Signal Pharmaceuticals, LLC Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide
WO2016138352A1 (en) 2015-02-27 2016-09-01 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
WO2017004134A1 (en) 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
US10045985B2 (en) * 2015-07-09 2018-08-14 Merck Patent Gmbh Heteroaryl compounds as BTK inhibitors and uses thereof
WO2017019487A1 (en) 2015-07-24 2017-02-02 Celgene Corporation Methods of synthesis of (1r,2r,5r)-5-amino-2-methylcyclohexanol hydrochloride and intermediates useful therein
WO2017027402A1 (en) 2015-08-07 2017-02-16 Patara Pharma, LLC Methods for the treatment of systemic disorders treatable with mast cell stabilizers, including mast cell related disorders
EP3331522A1 (en) 2015-08-07 2018-06-13 Patara Pharma LLC Methods for the treatment of mast cell related disorders with mast cell stabilizers
JP6802263B2 (ja) 2015-09-02 2020-12-16 ニンバス ラクシュミ, インコーポレイテッド Tyk2阻害剤およびその使用
WO2017041139A1 (en) 2015-09-08 2017-03-16 Monash University Lymph directing prodrugs
US10683308B2 (en) 2015-09-11 2020-06-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
EP3347097B1 (en) 2015-09-11 2021-02-24 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine derivatives as modulators of the kinases jak, flt3 and aurora
PT3364958T (pt) 2015-10-23 2023-04-10 Navitor Pharm Inc Moduladores de interação sestrina-gator2 e utilizações dos mesmos
CN108472298B (zh) 2015-11-24 2021-04-20 深圳阿拉丁医疗科技有限公司 选择性激酶抑制剂
AU2016363005A1 (en) 2015-12-04 2018-07-05 Portola Pharmaceuticals, Inc. Cerdulatinib for treating hematological cancers
US11370792B2 (en) 2015-12-14 2022-06-28 Raze Therapeutics, Inc. Caffeine inhibitors of MTHFD2 and uses thereof
CN105646371B (zh) * 2016-01-19 2019-10-01 浙江大学 含异羟肟酸片段的2,4-二芳胺基嘧啶类衍生物及制备和应用
ES2949357T3 (es) * 2016-03-09 2023-09-28 Raze Therapeutics Inc Inhibidores de 3-fosfoglicerato deshidrogenasa y usos de los mismos
PL3426243T3 (pl) 2016-03-09 2021-10-04 Raze Therapeutics, Inc. Inhibitory dehydrogenazy 3-fosfoglicerynianowej i ich zastosowania
WO2017156527A1 (en) * 2016-03-11 2017-09-14 H. Lee Moffitt Cancer Center And Research Institute, Inc. Aurora kinase and janus kinase inhibitors for prevention of graft versus host disease
WO2017177230A1 (en) 2016-04-08 2017-10-12 X4 Pharmaceuticals, Inc. Methods for treating cancer
CN109641838A (zh) 2016-06-21 2019-04-16 X4 制药有限公司 Cxcr4抑制剂及其用途
WO2017223239A1 (en) 2016-06-21 2017-12-28 X4 Pharmaceuticals, Inc. Cxcr4 inhibitors and uses thereof
EP3471726A4 (en) 2016-06-21 2019-10-09 X4 Pharmaceuticals, Inc. CXCR4 INHIBITORS AND USES THEREOF
WO2018044942A1 (en) 2016-08-31 2018-03-08 Patara Pharma, LLC Cromolyn compositions for treatment of chronic cough due to idiopathic pulmonary fibrosis
TW201822764A (zh) 2016-09-14 2018-07-01 美商基利科學股份有限公司 Syk抑制劑
AU2017325844A1 (en) 2016-09-14 2019-03-07 Gilead Sciences, Inc. SYK inhibitors
AU2017339366A1 (en) 2016-10-07 2019-04-11 Respivant Sciences Gmbh Cromolyn compositions for treatment of pulmonary fibrosis
CN109952303B (zh) 2016-10-14 2022-10-21 林伯士拉克许米公司 Tyk2抑制剂及其用途
EP3528816A4 (en) 2016-10-21 2020-04-08 Nimbus Lakshmi, Inc. TYK2 INHIBITORS AND USES THEREOF
US10414727B2 (en) 2016-11-08 2019-09-17 Navitor Pharmaceuticals, Inc. Phenyl amino piperidine mTORC inhibitors and uses thereof
AU2017368050A1 (en) 2016-11-29 2019-06-20 Puretech Lyt, Inc. Exosomes for delivery of therapeutic agents
US11091451B2 (en) 2016-12-05 2021-08-17 Raze Therapeutics, Inc. SHMT inhibitors and uses thereof
CN110603261A (zh) 2016-12-23 2019-12-20 拜斯科阿迪有限公司 具有新型键结构的肽衍生物
EP3565638B8 (en) 2017-01-06 2024-04-10 BicycleRD Limited Bicycle conjugate for treating cancer
CN108341835B (zh) * 2017-01-22 2021-01-15 正大天晴药业集团股份有限公司 用作酪氨酸激酶抑制剂的含硼化合物
TWI783978B (zh) 2017-03-08 2022-11-21 美商林伯士拉克許米公司 Tyk2抑制劑、其用途及生產方法
EP3375784A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aza-dihydro-acridone derivatives
EP3375778A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aryl-piperidine derivatives
BR112018075312A2 (pt) 2017-03-20 2019-10-01 Forma Therapeutics Inc composições de pirrolopirrol como ativadores da piruvato quinase (pkr)
WO2018191146A1 (en) 2017-04-10 2018-10-18 Navitor Pharmaceuticals, Inc. Heteroaryl rheb inhibitors and uses thereof
WO2018195471A1 (en) 2017-04-21 2018-10-25 Gilead Sciences, Inc. Syk inhibitors in combination with hypomethylating agents
EP3615019A4 (en) 2017-04-26 2021-01-27 Navitor Pharmaceuticals, Inc. MODULATORS OF SESTRIN-GATOR2 INTERACTION AND USES THEREOF
US10857196B2 (en) 2017-04-27 2020-12-08 Bicycletx Limited Bicyclic peptide ligands and uses thereof
US10899798B2 (en) 2017-06-26 2021-01-26 Bicyclerd Limited Bicyclic peptide ligands with detectable moieties and uses thereof
US11390609B2 (en) * 2017-06-30 2022-07-19 Beijing Tide Pharmaceutical Co., Ltd. Rho-associated protein kinase inhibitor, pharmaceutical composition comprising same, and preparation method and use thereof
CA3070621A1 (en) 2017-07-28 2019-01-31 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
EP3659307A4 (en) * 2017-07-28 2021-09-22 Yale University ANTI-CANCER MEDICINAL PRODUCTS AND THEIR MANUFACTURING AND USE PROCEDURES
EP3668887A1 (en) 2017-08-14 2020-06-24 Bicyclerd Limited Bicyclic peptide ligand sting conjugates and uses thereof
US20200283482A1 (en) 2017-08-14 2020-09-10 Bicyclerd Limited Bicyclic peptide ligand prr-a conjugates and uses thereof
US11883497B2 (en) 2017-08-29 2024-01-30 Puretech Lyt, Inc. Lymphatic system-directing lipid prodrugs
EP4306524A2 (en) 2017-08-29 2024-01-17 PureTech LYT, Inc. Lymphatic system-directing lipid prodrugs
WO2019060693A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES THEREOF
US11623932B2 (en) 2017-09-22 2023-04-11 Kymera Therapeutics, Inc. Protein degraders and uses thereof
US10052326B1 (en) 2017-10-12 2018-08-21 King Saud University Antihepatotoxic agents
MX2020004155A (es) 2017-10-19 2020-08-03 Bayer Animal Health Gmbh Uso de pirrolidonas heteroaromaticas fusionadas para el tratamiento y prevencion de enfermedades en animales.
US11166959B2 (en) 2017-11-06 2021-11-09 Bristol-Myers Squibb Company Isofuranone compounds useful as HPK1 inhibitors
WO2019099311A1 (en) 2017-11-19 2019-05-23 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use
EP3727362A4 (en) 2017-12-19 2021-10-06 PureTech LYT, Inc. MYCOPHENOLIC ACID LIPID MEDICINAL PRODUCTS AND THEIR USES
TWI825046B (zh) 2017-12-19 2023-12-11 英商拜西可泰克斯有限公司 Epha2特用之雙環胜肽配位基
US11608345B1 (en) 2017-12-19 2023-03-21 Puretech Lyt, Inc. Lipid prodrugs of rapamycin and its analogs and uses thereof
GB201721265D0 (en) 2017-12-19 2018-01-31 Bicyclerd Ltd Bicyclic peptide ligands specific for EphA2
US11304954B2 (en) 2017-12-19 2022-04-19 Puretech Lyt, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
EP3731869A4 (en) 2017-12-26 2021-09-22 Kymera Therapeutics, Inc. KINASES IRAQ DEGRADATION AGENTS AND THEIR USES
US11485743B2 (en) 2018-01-12 2022-11-01 Kymera Therapeutics, Inc. Protein degraders and uses thereof
US11512080B2 (en) 2018-01-12 2022-11-29 Kymera Therapeutics, Inc. CRBN ligands and uses thereof
MX2020007799A (es) 2018-01-29 2020-09-18 Merck Patent Gmbh Inhibidores de cinasa no derrepresible de control de aminoacido general 2 (gcn2) y sus usos.
EP3746071A4 (en) 2018-01-29 2021-09-01 Merck Patent GmbH GCN2 INHIBITORS AND THEIR USES
AU2019229258B2 (en) 2018-02-27 2023-09-14 Artax Biopharma Inc. Chromene derivatives as inhibitors of TCR-Nck interaction
US11013741B1 (en) 2018-04-05 2021-05-25 Sumitomo Dainippon Pharma Oncology, Inc. AXL kinase inhibitors and use of the same
PL3784666T3 (pl) 2018-04-24 2022-07-18 Merck Patent Gmbh Związki przeciwproliferacyjne i ich zastosowania
US11059826B2 (en) 2018-04-24 2021-07-13 Vertex Pharmaceuticals Incorporated Pteridinone compounds and uses thereof
JP7324778B2 (ja) 2018-05-04 2023-08-10 ポートラ ファーマシューティカルズ, エルエルシー セルデュラチニブ(cerdulatinib)の固体形態
KR20210021534A (ko) 2018-06-15 2021-02-26 나비토르 파마슈티칼스 인코포레이티드 라파마이신 유사체 및 이의 용도
US11180531B2 (en) 2018-06-22 2021-11-23 Bicycletx Limited Bicyclic peptide ligands specific for Nectin-4
GB201810316D0 (en) 2018-06-22 2018-08-08 Bicyclerd Ltd Peptide ligands for binding to EphA2
US10487057B1 (en) * 2018-07-05 2019-11-26 Landos Biopharma, Inc. NLRX1 ligands
US11292792B2 (en) 2018-07-06 2022-04-05 Kymera Therapeutics, Inc. Tricyclic CRBN ligands and uses thereof
CN112512597A (zh) 2018-07-26 2021-03-16 大日本住友制药肿瘤公司 用于治疗与acvr1表达异常相关的疾病的方法以及用于此的acvr1抑制剂
US10548889B1 (en) 2018-08-31 2020-02-04 X4 Pharmaceuticals, Inc. Compositions of CXCR4 inhibitors and methods of preparation and use
CN113164419A (zh) 2018-09-07 2021-07-23 皮克医疗公司 Eif4e抑制剂和其用途
US20200129485A1 (en) 2018-09-19 2020-04-30 Forma Therapeutics, Inc. Treating sickle cell disease with a pyruvate kinase r activating compound
EP3852791A4 (en) 2018-09-19 2022-06-15 Forma Therapeutics, Inc. ACTIVATION OF PYRUVATE KINASE R
WO2020081508A1 (en) 2018-10-15 2020-04-23 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
CN112955459A (zh) 2018-10-23 2021-06-11 拜斯科技术开发有限公司 双环肽配体和其用途
CA3117336A1 (en) 2018-10-24 2020-04-30 Navitor Pharmaceuticals, Inc. Polymorphs of (s)-2-amino-5,5-difluoro-4,4-dimethylpentanoic acid for use in modulating mtorc1
MX2021006154A (es) 2018-11-30 2021-08-24 Kymera Therapeutics Inc Degradadores de cinasas asociadas al receptor de interleucina 1 (irak) y usos de los mismos.
US11053241B2 (en) 2018-11-30 2021-07-06 Nimbus Lakshmi, Inc. TYK2 inhibitors and uses thereof
EP3670659A1 (en) 2018-12-20 2020-06-24 Abivax Biomarkers, and uses in treatment of viral infections, inflammations, or cancer
CA3126034A1 (en) 2019-01-23 2020-07-30 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
WO2020165600A1 (en) 2019-02-14 2020-08-20 Bicycletx Limited Bicyclic peptide ligand sting conjugates and uses thereof
CN114364798A (zh) 2019-03-21 2022-04-15 欧恩科斯欧公司 用于治疗癌症的Dbait分子与激酶抑制剂的组合
AU2020253990A1 (en) 2019-04-02 2021-10-28 Bicycletx Limited Bicycle toxin conjugates and uses thereof
CA3135802A1 (en) 2019-04-05 2020-10-08 Kymera Therapeutics, Inc. Stat degraders and uses thereof
CN114502540A (zh) 2019-05-31 2022-05-13 医肯纳肿瘤学公司 Tead抑制剂和其用途
CN114302878A (zh) 2019-07-03 2022-04-08 大日本住友制药肿瘤公司 酪氨酸激酶非受体1(tnk1)抑制剂及其用途
JP2022543843A (ja) 2019-08-08 2022-10-14 ライジェル ファーマシューティカルズ, インコーポレイテッド サイトカイン放出症候群を治療するための化合物及び方法
CA3150492A1 (en) 2019-09-11 2021-03-18 Donna L. Romero USP30 INHIBITORS AND USES THEREOF
BR112022004451A2 (pt) 2019-09-13 2022-06-21 Nimbus Saturn Inc Antagonistas de hpk1 e usos dos mesmos
IL292612A (en) 2019-11-01 2022-07-01 Navitor Pharm Inc Treatment methods using mtorc1 modulator
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
WO2021094296A1 (en) 2019-11-12 2021-05-20 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of mast cell stabilizer for the treatment of heart failure with preserved ejection fraction
WO2021113665A1 (en) 2019-12-05 2021-06-10 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
EP4076520A4 (en) 2019-12-17 2024-03-27 Kymera Therapeutics Inc IRAQ DEGRADERS AND USES THEREOF
EP4076524A4 (en) 2019-12-17 2023-11-29 Kymera Therapeutics, Inc. IRAQ DEGRADERS AND USES THEREOF
JP2023509394A (ja) 2019-12-23 2023-03-08 カイメラ セラピューティクス, インコーポレイテッド Smarca分解剤およびそれらの使用
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2021155185A1 (en) * 2020-01-30 2021-08-05 Sumitomo Dainippon Pharma Oncology, Inc. Aminopyrimidinylaminobenzonitrile derivatives as nek2 inhibitors
AR121506A1 (es) 2020-03-03 2022-06-08 Pic Therapeutics Inc Inhibidores del eif4e y sus usos
CN115768474A (zh) * 2020-03-12 2023-03-07 里格尔药品股份有限公司 用于治疗covid-19相关病症的方法
MX2022011602A (es) 2020-03-19 2023-01-04 Kymera Therapeutics Inc Degradadores de la proteína de homólogo de ratón de minuto 2 (mdm2) y usos de los mismos.
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
WO2022038158A1 (en) 2020-08-17 2022-02-24 Bicycletx Limited Bicycle conjugates specific for nectin-4 and uses thereof
WO2022120353A1 (en) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead inhibitors and uses thereof
CN117015531A (zh) 2020-12-02 2023-11-07 医肯纳肿瘤学公司 Tead抑制剂及其用途
CN112920124B (zh) * 2021-01-29 2024-03-01 安徽医科大学 一种嘧啶-2,4-二胺类化合物及其制备方法与应用
US20230113202A1 (en) 2021-02-02 2023-04-13 Liminal Biosciences Limited Gpr84 antagonists and uses thereof
BR112023015584A2 (pt) 2021-02-02 2023-10-24 Liminal Biosciences Ltd Antagonistas de gpr84 e usos dos mesmos
KR20230145446A (ko) 2021-02-15 2023-10-17 카이메라 쎄라퓨틱스 인코포레이티드 Irak4 분해제 및 이의 용도
JP2024509192A (ja) 2021-03-05 2024-02-29 ニンバス サターン, インコーポレイテッド Hpk1アンタゴニスト及びその使用
CA3215081A1 (en) 2021-04-16 2022-10-20 Alfredo C. Castro Mek inhibitors and uses thereof
IL310924A (en) 2021-08-25 2024-04-01 Pic Therapeutics Inc EIF4E inhibitors and their uses
WO2023028238A1 (en) 2021-08-25 2023-03-02 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
WO2023108536A1 (en) * 2021-12-16 2023-06-22 Lynk Pharmaceuticals Co. Ltd. Tyk2 inhibitors and compositions and methods thereof
WO2023114984A1 (en) 2021-12-17 2023-06-22 Ikena Oncology, Inc. Tead inhibitors and uses thereof
US11478464B1 (en) 2022-02-06 2022-10-25 King Faisal University Method for treating inflammation
WO2023173057A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023173053A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023211889A1 (en) 2022-04-25 2023-11-02 Ikena Oncology, Inc. Polymorphic compounds and uses thereof
KR20230155351A (ko) * 2022-05-03 2023-11-10 한국화학연구원 5-클로로-2,4-다이아미노피리미딘을 포함하는 키나아제 억제 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
US20230357125A1 (en) * 2022-05-06 2023-11-09 AMPAC Fine Chemicals Process for Catalytic Reduction of Nitro Compounds to Amines
WO2023230205A1 (en) 2022-05-25 2023-11-30 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2024028363A1 (en) 2022-08-02 2024-02-08 Liminal Biosciences Limited Heteroaryl carboxamide and related gpr84 antagonists and uses thereof
WO2024028365A1 (en) 2022-08-02 2024-02-08 Liminal Biosciences Limited Substituted pyridone gpr84 antagonists and uses thereof
WO2024028364A1 (en) 2022-08-02 2024-02-08 Liminal Biosciences Limited Aryl-triazolyl and related gpr84 antagonists and uses thereof
WO2024042361A1 (en) * 2022-08-24 2024-02-29 Sudo Biosciences Limited Tyk2 inhibitors and uses thereof

Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1991018887A1 (en) * 1990-06-06 1991-12-12 Smithkline Beecham Intercredit B.V. Diaminopyrimidine compounds
WO1999031073A1 (fr) * 1997-12-15 1999-06-24 Yamanouchi Pharmaceutical Co., Ltd. Nouveaux derives de pyrimidine-5-carboxamide
US5958935A (en) * 1995-11-20 1999-09-28 Celltech Therapeutics Limited Substituted 2-anilinopyrimidines useful as protein kinase inhibitors
WO1999050250A1 (en) * 1998-03-27 1999-10-07 Janssen Pharmaceutica N.V. Hiv inhibiting pyrimidine derivatives
WO2000027825A1 (en) * 1998-11-10 2000-05-18 Janssen Pharmaceutica N.V. Hiv replication inhibiting pyrimidines
WO2000039101A1 (en) * 1998-12-24 2000-07-06 Astrazeneca Ab Pyrimidine compounds
WO2001022938A1 (en) * 1999-09-24 2001-04-05 Janssen Pharmaceutica N.V. Antiviral compositions
WO2001023362A2 (en) * 1999-09-24 2001-04-05 Abbott Gmbh & Co. Kg Rate-controlled particles
WO2001060816A1 (en) * 2000-02-17 2001-08-23 Amgen Inc. Kinase inhibitors
WO2001064656A1 (en) * 2000-03-01 2001-09-07 Astrazeneca Ab 2,4,di(hetero-)arylamino(-oxy)-5-substituted pyrimidines as antineoplastic agents
WO2001085699A2 (en) * 2000-05-08 2001-11-15 Janssen Pharmaceutica N.V. Prodrugs of hiv replication inhibiting pyrimidines
WO2002004429A1 (en) * 2000-07-11 2002-01-17 Astrazeneca Ab Pyrimidine derivatives

Family Cites Families (282)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US113398A (en) * 1871-04-04 Improvement in towel-brackets and sponge-holders
US80858A (en) * 1868-08-11 Ensmore
US192301A (en) * 1877-06-19 Improvement in lemon-squeezers
US38243A (en) * 1863-04-21 Improvement in flasks for founders
US3159547A (en) 1963-06-28 1964-12-01 Abbott Lab Method of lowering blood pressure with 4-(2-amino-4-pyrimidylamino)-benzene-sulfonamide
US3320256A (en) 1965-04-09 1967-05-16 Hoffmann La Roche Fluorinated imidazoo[1, 2-c]pyrimidines and pyrimido[1, 2-c]pyrimidines
US4166452A (en) 1976-05-03 1979-09-04 Generales Constantine D J Jr Apparatus for testing human responses to stimuli
US4256108A (en) 1977-04-07 1981-03-17 Alza Corporation Microporous-semipermeable laminated osmotic system
US4265874A (en) 1980-04-25 1981-05-05 Alza Corporation Method of delivering drug with aid of effervescent activity generated in environment of use
JPS59122899U (ja) 1983-02-08 1984-08-18 松下電器産業株式会社 アイロン
US5087240A (en) 1983-08-18 1992-02-11 Drug Delivery Systems Inc. Transdermal drug patch with conductive fibers
US4921475A (en) 1983-08-18 1990-05-01 Drug Delivery Systems Inc. Transdermal drug patch with microtubes
EP0139613A1 (de) 1983-08-29 1985-05-02 Ciba-Geigy Ag N-(2-Nitrophenyl)-4-aminopyrimidin-Derivate, deren Herstellung und Verwendung
HU192875B (en) 1984-10-05 1987-07-28 Richter Gedeon Vegyeszet Process for preparing 2-pyridinethiol derivatives
DE3666587D1 (en) 1985-08-02 1989-11-30 Leo Pharm Prod Ltd Novel vitamin d analogues
US4738851A (en) 1985-09-27 1988-04-19 University Of Iowa Research Foundation, Inc. Controlled release ophthalmic gel formulation
DE3618353A1 (de) * 1986-05-31 1987-12-03 Hoechst Ag Schaedlingsbekaempfungsmittel auf der basis von aminopyrimidin-derivaten sowie neue aminopyrimidin-verbindungen
JPS638387A (ja) 1986-06-27 1988-01-14 Yoshitomi Pharmaceut Ind Ltd セフエム化合物
JPH0696592B2 (ja) * 1986-06-30 1994-11-30 株式会社クラレ 17β−ヒドロキシ−17α−(3−ヒドロキシプロピル)アンドロスタ−4,6−ジエン−3−オンの製造方法
US5163899A (en) 1987-03-20 1992-11-17 Drug Delivery Systems Inc. Transdermal drug delivery system
DE3868287D1 (de) 1987-04-02 1992-03-19 Ciba Geigy Ag Reaktivfarbstoffe, deren herstellung und verwendung.
US5312325A (en) 1987-05-28 1994-05-17 Drug Delivery Systems Inc Pulsating transdermal drug delivery system
SU1499883A1 (ru) 1987-11-24 1991-10-23 Научно-исследовательский институт фармакологии АМН СССР Дихлоргидрат 2,4-бис-(п-трет-бутиланилино)-5-окси-6-метилпиримидина, обладающий анальгетической и противовоспалительной активностью
GB8804164D0 (en) 1988-02-23 1988-03-23 Tucker J M Bandage for administering physiologically active compound
JP2711161B2 (ja) 1988-04-21 1998-02-10 レオ・ファーマシューティカル・プロダクツ・リミテッド・エイ/エス(レーベンス・ケミスケ・ファブリック・プロデュクチオンスアクチーセルスカブ) 新規ビタミンd類似体
US4882150A (en) 1988-06-03 1989-11-21 Kaufman Herbert E Drug delivery system
US5008110A (en) 1988-11-10 1991-04-16 The Procter & Gamble Company Storage-stable transdermal patch
US5088977A (en) 1988-12-21 1992-02-18 Drug Delivery Systems Inc. Electrical transdermal drug applicator with counteractor and method of drug delivery
HU206337B (en) 1988-12-29 1992-10-28 Mitsui Petrochemical Ind Process for producing pyrimidine derivatives and pharmaceutical compositions
IE63502B1 (en) 1989-04-21 1995-05-03 Zeneca Ltd Aminopyrimidine derivatives useful for treating cardiovascular disorders
US5179204A (en) 1989-09-05 1993-01-12 Hoechst-Roussel Pharmaceuticals Incorporated N-substituted-4-pyrimidinamines and pyrimidinediamines
US4983608A (en) 1989-09-05 1991-01-08 Hoechst-Roussell Pharmaceuticals, Inc. N-substituted-4-pyrimidinamines and pyrimidinediamines
US5521222A (en) 1989-09-28 1996-05-28 Alcon Laboratories, Inc. Topical ophthalmic pharmaceutical vehicles
JPH03127790A (ja) * 1989-10-11 1991-05-30 Morishita Pharmaceut Co Ltd N―(1h―テトラゾール―5―イル)―2―アニリノ―5―ピリミジンカルボキシアミド類及びその合成中間体
TW224941B (hr) 1989-11-08 1994-06-11 Yamanouchi Pharma Co Ltd
PT96059B (pt) 1989-12-04 1998-07-31 Searle & Co Sistema de camada unica para a administracao de um medicamento por via transdermica
US5532228A (en) 1990-02-06 1996-07-02 Schering Aktiengesellschaft Side-chain homologous vitamin D derivatives, process for their production, pharmaceutical preparations containing these derivatives and their use as pharmaceutical agents
DE4011682A1 (de) 1990-04-06 1991-10-10 Schering Ag 24-oxa-derivate in der vitamin d-reihe
JPH03127790U (hr) 1990-04-06 1991-12-24
US5077033A (en) 1990-08-07 1991-12-31 Mediventures Inc. Ophthalmic drug delivery with thermo-irreversible gels of polxoxyalkylene polymer and ionic polysaccharide
DE4029650A1 (de) * 1990-09-19 1992-03-26 Hoechst Ag 2-anilino-pyrimidine, verfahren zu ihrer herstellung, sie enthaltene mittel und ihre verwendung als fungizide
JPH04178385A (ja) 1990-11-09 1992-06-25 Yamanouchi Pharmaceut Co Ltd ジケトピリドピラジン誘導体
DK0495421T3 (da) 1991-01-15 1996-12-09 Alcon Lab Inc Anvendelse af carragenaner i topiske ophthalmiske sammensætninger
US5246948A (en) 1991-05-10 1993-09-21 Takeda Chemical Industries, Ltd. Pyridine derivatives, their production and use
US5200400A (en) 1991-07-12 1993-04-06 New England Deaconess Hospital Corporation Method for inhibiting allograft rejection using photoactivatable nucleotides or nucleosides
CA2074864A1 (en) 1991-07-30 1993-01-31 Carmen Almansa Tetralones with pharmacological activity
US5352456A (en) 1991-10-10 1994-10-04 Cygnus Therapeutic Systems Device for administering drug transdermally which provides an initial pulse of drug
US5728536A (en) 1993-07-29 1998-03-17 St. Jude Children's Research Hospital Jak kinases and regulation of Cytokine signal transduction
DE4141746A1 (de) 1991-12-13 1993-06-17 Schering Ag 20-methyl-substituierte vitamin d-derivate
WO1993011938A1 (en) 1991-12-18 1993-06-24 Minnesota Mining And Manufacturing Company Multilayered barrier structures
EP0553769B1 (de) 1992-01-29 1996-01-03 FRANZ VÖLKL GmbH & CO. SKI UND TENNIS SPORTARTIKELFABRIK KG Ballspielschläger, insbesondere Tennisschläger
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
US5194431A (en) 1992-07-08 1993-03-16 Wisconsin Alumni Research Foundation 24-cyclopropane vitamin D derivatives
DE69329136T2 (de) * 1992-10-14 2001-06-07 Mitsubishi Chem Corp Verfahren zur Herstellung einer thermoplastischen Harzzusammensetzung
US5335501A (en) 1992-11-16 1994-08-09 General Electric Company Flow spreading diffuser
TW287160B (hr) 1992-12-10 1996-10-01 Hoffmann La Roche
DE4308034A1 (de) * 1993-03-13 1994-09-15 Cassella Ag Neue Heterocyclen, ihre Herstellung und ihre Verwendung
HUT74464A (en) 1993-10-12 1996-12-30 Du Pont Merck Pharma 1n-alkyl-n-arylpyrimidinamines and derivatives thereof, and pharmaceutical compositions containing them
IL112290A (en) 1994-01-12 1999-01-26 Novartis Ag Transformed aryl and the troiryl pyrimidines and herbicides containing them
CA2150609C (en) 1994-06-01 1998-12-08 Mikiro Yanaka Pyrimidine derivatives and pharmaceutical composition
IL114193A (en) 1994-06-20 2000-02-29 Teva Pharma Ophthalmic pharmaceutical compositions based on sodium alginate
ES2094688B1 (es) 1994-08-08 1997-08-01 Cusi Lab Manoemulsion del tipo de aceite en agua, util como vehiculo oftalmico y procedimiento para su preparacion.
US5733932A (en) 1995-01-06 1998-03-31 The Picower Institute For Medical Research Compounds and methods of use to derivatize neighboring lysine residues in proteins under physiological conditions
US6242434B1 (en) 1997-08-08 2001-06-05 Bone Care International, Inc. 24-hydroxyvitamin D, analogs and uses thereof
US5700904A (en) 1995-06-07 1997-12-23 Eli Lilly And Company Preparation of an acylated protein powder
US6316635B1 (en) 1995-06-07 2001-11-13 Sugen, Inc. 2-indolinone derivatives as modulators of protein kinase activity
GB9516121D0 (en) 1995-08-05 1995-10-04 Pfizer Ltd Organometallic addition to ketones
IT1283911B1 (it) 1996-02-05 1998-05-07 Farmigea Spa Soluzioni oftalmiche viscosizzate con polisaccaridi della gomma di tamarindo
JP4058129B2 (ja) 1996-03-18 2008-03-05 株式会社資生堂 ピリジン誘導体及び抗潰瘍剤、抗菌剤
TW440563B (en) 1996-05-23 2001-06-16 Hoffmann La Roche Aryl pyrimidine derivatives and a pharmaceutical composition thereof
US6696448B2 (en) 1996-06-05 2004-02-24 Sugen, Inc. 3-(piperazinylbenzylidenyl)-2-indolinone compounds and derivatives as protein tyrosine kinase inhibitors
GB9619284D0 (en) 1996-09-16 1996-10-30 Celltech Therapeutics Ltd Chemical compounds
US6004985A (en) 1996-10-09 1999-12-21 Berlex Laboratories, Inc. Thio acid derived monocylic N-heterocyclics as anticoagulants
US5800807A (en) 1997-01-29 1998-09-01 Bausch & Lomb Incorporated Ophthalmic compositions including glycerin and propylene glycol
GB9705361D0 (en) 1997-03-14 1997-04-30 Celltech Therapeutics Ltd Chemical compounds
US6316429B1 (en) 1997-05-07 2001-11-13 Sugen, Inc. Bicyclic protein kinase inhibitors
US6486185B1 (en) 1997-05-07 2002-11-26 Sugen, Inc. 3-heteroarylidene-2-indolinone protein kinase inhibitors
US6987113B2 (en) 1997-06-11 2006-01-17 Sugen, Inc. Tyrosine kinase inhibitors
SE9702401D0 (sv) 1997-06-19 1997-06-19 Astra Ab Pharmaceutical use
GB9718913D0 (en) 1997-09-05 1997-11-12 Glaxo Group Ltd Substituted oxindole derivatives
US6133305A (en) * 1997-09-26 2000-10-17 Sugen, Inc. 3-(substituted)-2-indolinones compounds and use thereof as inhibitors of protein kinase activity
US6093820A (en) 1997-10-02 2000-07-25 Taro Pharmaceutical Industries Ltd. Method and reagents for N-alkylating ureides
US6022884A (en) 1997-11-07 2000-02-08 Amgen Inc. Substituted pyridine compounds and methods of use
GB9723859D0 (en) 1997-11-12 1998-01-07 Zeneca Ltd Compound,composition and use
DE19750701A1 (de) 1997-11-15 1999-05-20 Dystar Textilfarben Gmbh & Co Verfahren zur Umsetzung von fluorsubstituierten Heterocyclen mit Aminen in Gegenwart von Phasentransfer-Katalysatoren
EP1051181B1 (en) 1997-12-31 2004-03-17 The University Of Kansas Water soluble prodrugs of tertiary amine containing drugs and methods of making thereof
US6355683B1 (en) * 1998-09-11 2002-03-12 Ilexus Pty Limited Fc receptor modulators and uses thereof
WO1999041244A1 (en) 1998-02-13 1999-08-19 Pharmacia & Upjohn Company Substituted aminophenyl isoxazoline derivatives useful as antimicrobials
AU748087B2 (en) 1998-02-17 2002-05-30 Tularik Inc. Anti-viral pyrimidine derivatives
DE69943247D1 (de) 1998-03-27 2011-04-14 Janssen Pharmaceutica Nv HIV hemmende Pyrimidin Derivate
GB9806739D0 (en) 1998-03-28 1998-05-27 Univ Newcastle Ventures Ltd Cyclin dependent kinase inhibitors
EP1054871A2 (en) 1998-04-01 2000-11-29 Du Pont Pharmaceuticals Company Pyrimidines and triazines as integrin antagonists
US6261547B1 (en) 1998-04-07 2001-07-17 Alcon Manufacturing, Ltd. Gelling ophthalmic compositions containing xanthan gum
DE69933661T3 (de) 1998-04-15 2012-01-26 Merck Serono Biodevelopment Genomische sequenz des 5-lipoxygenase-aktivierenden proteins (flap), polymorphische marker und ihre anwendung in der diagnose von asthma
US6197934B1 (en) 1998-05-22 2001-03-06 Collagenesis, Inc. Compound delivery using rapidly dissolving collagen film
NZ508180A (en) 1998-05-22 2003-09-26 Smithkline Beecham Corp 2(alkyl)-, 5(4-pyridinyl)- substituted imidazole derivatives and pharmaceuticals thereof
AU4851599A (en) 1998-06-30 2000-01-17 Parker Hughes Institute Method for inhibiting c-jun expression using jak-3 inhibitors
HUP0103386A3 (en) 1998-08-21 2002-07-29 Parker Hughes Inst St Paul Use of quinazoline derivatives for producing pharmaceutical compositions having jak 3-inhibitor effect
JP2002523497A (ja) 1998-08-29 2002-07-30 アストラゼネカ・アクチエボラーグ ピリミジン化合物
DE19851421A1 (de) 1998-11-07 2000-05-11 Boehringer Ingelheim Pharma Neue Pyrimidine, deren Herstellung und Verwendung
WO2000027802A1 (en) 1998-11-12 2000-05-18 Ariad Pharmaceuticals, Inc. Bicyclic signal transduction inhibitors, compositions containing them & uses thereof
US6127376A (en) 1998-12-04 2000-10-03 Berlex Laboratories, Inc. Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants
US6841567B1 (en) 1999-02-12 2005-01-11 Cephalon, Inc. Cyclic substituted fused pyrrolocarbazoles and isoindolones
US6673908B1 (en) 1999-02-22 2004-01-06 Nuvelo, Inc. Tumor necrosis factor receptor 2
GB9904995D0 (en) 1999-03-04 1999-04-28 Glaxo Group Ltd Substituted aza-oxindole derivatives
US6624171B1 (en) 1999-03-04 2003-09-23 Smithkline Beecham Corporation Substituted aza-oxindole derivatives
US6080747A (en) 1999-03-05 2000-06-27 Hughes Institute JAK-3 inhibitors for treating allergic disorders
CZ20013451A3 (cs) * 1999-03-26 2002-04-17 Astrazeneca Ab Nové sloučeniny
AU4198400A (en) 1999-04-06 2000-10-23 Krenitsky Pharmaceuticals Inc. Neurotrophic thio substituted pyrimidines
DE19917785A1 (de) 1999-04-20 2000-10-26 Bayer Ag 2,4-Diamino-pyrimidin-Derivate
AU5108000A (en) 1999-06-10 2001-01-02 Yamanouchi Pharmaceutical Co., Ltd. Novel nitrogen-contaiing heterocyclic derivatives or salts thereof
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
TWI262914B (en) 1999-07-02 2006-10-01 Agouron Pharma Compounds and pharmaceutical compositions for inhibiting protein kinases
GB9918035D0 (en) 1999-07-30 1999-09-29 Novartis Ag Organic compounds
ATE318267T1 (de) 1999-09-30 2006-03-15 Neurogen Corp Einige alkylendiamin-substituierte heterocyclen
KR100317935B1 (ko) 1999-10-20 2001-12-22 유승필 대사성 골질환 치료용 약제조성물 및 이의 제조방법
AU1026901A (en) 1999-10-29 2001-05-08 Syngenta Participations Ag Novel herbicides
AU4903201A (en) 1999-11-30 2001-07-03 Parker Hughes Institute Inhibitors of thrombin induced platelet aggregation
EP1382339B1 (en) 1999-12-10 2007-12-05 Pfizer Products Inc. Compositions containing pyrrolo ¬2,3-d pyrimidine derivatives
EP1244672B1 (en) 1999-12-21 2005-07-20 Sugen, Inc. 4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors
US20020065270A1 (en) 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
AU2735201A (en) * 1999-12-28 2001-07-09 Pharmacopeia, Inc. Pyrimidine and triazine kinase inhibitors
US6362172B2 (en) 2000-01-20 2002-03-26 Bristol-Myers Squibb Company Water soluble prodrugs of azole compounds
AU2968701A (en) 2000-01-24 2001-07-31 Genzyme Corporation Jak/stat pathway inhibitors and the uses thereof
CZ20013540A3 (cs) 2000-02-05 2002-03-13 Vertex Pharmaceuticals Incorporated Deriváty pyrazolu jako inhibitory ERK a farmaceutický prostředek, který je obsahuje
AU782878B2 (en) 2000-02-05 2005-09-08 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of erk
GB0004888D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004886D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US6525051B2 (en) 2000-03-27 2003-02-25 Schering Aktiengesellschaft N-heterocyclic derivatives as NOS inhibitors
US6608048B2 (en) 2000-03-28 2003-08-19 Wyeth Holdings Tricyclic protein kinase inhibitors
AR028261A1 (es) 2000-03-28 2003-04-30 Wyeth Corp Inhibidores triciclicos de la proteina quinasa
WO2001085700A2 (en) 2000-05-08 2001-11-15 Janssen Pharmaceutica N.V. Hiv replication inhibiting pyrimidines and triazines
NZ522364A (en) 2000-06-26 2004-09-24 Pfizer Prod Inc Pyrrolo[2,3-d]pyrimidine compounds as immunosuppressive agents
US20050009876A1 (en) * 2000-07-31 2005-01-13 Bhagwat Shripad S. Indazole compounds, compositions thereof and methods of treatment therewith
CA2422354C (en) 2000-09-15 2009-12-08 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
WO2002028862A2 (en) 2000-10-02 2002-04-11 Emory University Triptolide analogs for the treatment of autoimmune and inflammatory disorders
US6448401B1 (en) 2000-11-20 2002-09-10 Bristol-Myers Squibb Company Process for water soluble azole compounds
WO2002043735A1 (en) 2000-11-29 2002-06-06 Parker Hughes Institute Inhibitors of thrombin induced platelet aggregation
US20020137755A1 (en) 2000-12-04 2002-09-26 Bilodeau Mark T. Tyrosine kinase inhibitors
US20020115173A1 (en) 2000-12-11 2002-08-22 Children's Medical Center Corporation Short peptides from the 'A-region' of protein kinases which selectively modulate protein kinase activity
EP1349852A2 (en) 2000-12-20 2003-10-08 Sugen, Inc. 4-(hetero)aryl substituted indolinones
CN1307173C (zh) * 2000-12-21 2007-03-28 葛兰素集团有限公司 作为血管生成调节剂的嘧啶胺
NZ526469A (en) 2000-12-21 2005-10-28 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors
WO2002060492A1 (en) 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
AUPR279101A0 (en) * 2001-01-30 2001-02-22 Cytopia Pty Ltd Protein kinase signalling
WO2002064096A2 (en) 2001-02-16 2002-08-22 Tularik Inc. Methods of using pyrimidine-based antiviral agents
GB0103926D0 (en) 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
EP1423388B1 (en) 2001-02-20 2008-12-03 AstraZeneca AB 2-arylamino-pyrimidines for the treatment of gsk3-related disorders
GB2373186A (en) * 2001-02-23 2002-09-18 Astrazeneca Ab Pharmaceutical combinations of a CCR3 antagonist and a compound which is usefulreatment of asthma, allergic disease or inflammation
US7053089B2 (en) * 2001-02-23 2006-05-30 Merck & Co., Inc. N-substituted nonaryl-heterocyclic NMDA/NR2B antagonists
US20030165873A1 (en) 2001-03-02 2003-09-04 Come Jon H. Three hybrid assay system
CN100480242C (zh) * 2001-05-29 2009-04-22 舍林股份公司 Cdk抑制性嘧啶化合物、其制备方法以及作为药物的应用
US6762179B2 (en) 2001-05-31 2004-07-13 Vertex Pharmaceuticals Incorporated Thiazole compounds useful as inhibitors of protein kinase
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
JP4523271B2 (ja) * 2001-06-01 2010-08-11 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼのインヒビターとして有用なチアゾール化合物
JP4541695B2 (ja) 2001-06-15 2010-09-08 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼインヒビターとしての5−(2−アミノピリミジン−4−イル)ベンズイソキサゾール
JP2005500294A (ja) 2001-06-19 2005-01-06 ブリストル−マイヤーズ スクイブ カンパニー ホスホジエステラーゼ7に対するピリミジン阻害剤
WO2003000186A2 (en) 2001-06-21 2003-01-03 Ariad Pharmaceuticals, Inc. Novel phenylamino-pyrimidines and uses thereof
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
AP2003002929A0 (en) * 2001-06-23 2003-12-31 Aventis Pharma Inc Pyrrolopyrimidines as protein kinase inhibitors
JP4510442B2 (ja) * 2001-06-26 2010-07-21 ブリストル−マイヤーズ スクイブ カンパニー TNF−α発現のN−ヘテロ環インヒビター
CZ294535B6 (cs) 2001-08-02 2005-01-12 Ústav Experimentální Botaniky Avčr Heterocyklické sloučeniny na bázi N6-substituovaného adeninu, způsoby jejich přípravy, jejich použití pro přípravu léčiv, kosmetických přípravků a růstových regulátorů, farmaceutické přípravky, kosmetické přípravky a růstové regulátory tyto sloučeniny obsahující
JO3429B1 (ar) 2001-08-13 2019-10-20 Janssen Pharmaceutica Nv مشتقات برميدينات مثبطة فيروس الايدز
US7115617B2 (en) 2001-08-22 2006-10-03 Amgen Inc. Amino-substituted pyrimidinyl derivatives and methods of use
US6939874B2 (en) 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
US7070996B2 (en) 2001-08-31 2006-07-04 Rigel Pharmaceuticals, Inc. Production of cultured human mast cells and basophils for high throughput small molecule drug discovery
US6952284B2 (en) * 2001-08-31 2005-10-04 International Business Machines Corporation Manually operated digital printing device
US6433018B1 (en) 2001-08-31 2002-08-13 The Research Foundation Of State University Of New York Method for reducing hypertrophy and ischemia
JP2005506982A (ja) 2001-09-10 2005-03-10 スージェン・インコーポレーテッド キナーゼ阻害剤としての3−(4,5,6,7−テトラヒドロインドール−2−イルメチリデン)−2−インドリノン誘導体
WO2003030909A1 (en) * 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
WO2003026664A1 (en) 2001-09-26 2003-04-03 Bayer Corporation 2-phenylamino-4- (5-pyrazolylamino) -pyramidine derivatives as kinase inhibitors, in particular, src kinase inhibitors
WO2003040141A1 (en) 2001-09-28 2003-05-15 Bayer Pharmaceuticals Corporation Oxazolyl-phenyl-2,4-diamino-pyrimidine compounds and methods for treating hyperproliferative disorders
EP2332924A1 (de) 2001-10-17 2011-06-15 Boehringer Ingelheim Pharma GmbH & Co. KG Pyrimidinderivate, Arzneimittel enthaltend diese Verbindungen, deren Verwendung und Verfahren zu ihrer Herstellung
EP1453516A2 (de) * 2001-10-17 2004-09-08 Boehringer Ingelheim Pharma GmbH & Co.KG 5-substituierte 4-amino-2-phenylamino-pyrimdinderivate und ihre verwendung als beta-amyloid modulatoren
US6897208B2 (en) 2001-10-26 2005-05-24 Aventis Pharmaceuticals Inc. Benzimidazoles
NZ533147A (en) 2001-11-28 2006-12-22 Btg Int Ltd Preventives or remedies for alzheimer's disease, or amyloid protein fibril-formation inhibitors, which include a nitrogen-containing heteroaryl compound
GT200200234A (es) 2001-12-06 2003-06-27 Compuestos cristalinos novedosos
SE0104140D0 (sv) 2001-12-07 2001-12-07 Astrazeneca Ab Novel Compounds
AU2002367172A1 (en) 2001-12-21 2003-07-15 Bayer Pharmaceuticals Corporation 2,4-diamino-pyrimidine derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents
CA2473510A1 (en) 2002-01-23 2003-07-31 Bayer Pharmaceuticals Corporation Pyrimidine derivatives as rho-kinase inhibitors
TWI329105B (en) * 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
US6998391B2 (en) 2002-02-07 2006-02-14 Supergen.Inc. Method for treating diseases associated with abnormal kinase activity
CA2476281A1 (en) 2002-02-08 2003-08-14 Smithkline Beecham Corporation Pyrimidine compounds
US7153245B2 (en) * 2002-02-14 2006-12-26 Kellion Corporation Golf exerciser
CA2477505A1 (en) 2002-03-01 2003-09-12 Smithkline Beecham Corporation Diamino-pyrimidines and their use as angiogenesis inhibitors
EP1483260A1 (de) 2002-03-11 2004-12-08 Schering Aktiengesellschaft Cdk inhibitorische 2-heteroaryl-pyrimidine, deren herstellung und verwendung als arzneimittel
US7288547B2 (en) * 2002-03-11 2007-10-30 Schering Ag CDK-inhibitory 2-heteroaryl-pyrimidines, their production and use as pharmaceutical agents
GB0206215D0 (en) 2002-03-15 2002-05-01 Novartis Ag Organic compounds
PL372413A1 (en) 2002-03-20 2005-07-25 Bristol-Myers Squibb Company Phosphate prodrugs of fluorooxindoles
WO2004039359A2 (en) 2002-05-06 2004-05-13 Bayer Pharmaceuticals Corporation Use of pyrimidine derivates for the manifacture of a medicament for the treatment of hyper-proliferative disorders
AU2003231231A1 (en) 2002-05-06 2003-11-11 Bayer Pharmaceuticals Corporation Pyridinyl amino pyrimidine derivatives useful for treating hyper-proliferative disorders
AR039540A1 (es) 2002-05-13 2005-02-23 Tibotec Pharm Ltd Compuestos microbicidas con contenido de pirimidina o triazina
WO2003101989A1 (en) 2002-05-30 2003-12-11 Vertex Pharmaceuticals Incorporated Inhibitors of jak and cdk2 protein kinases
CA2489648A1 (en) 2002-06-17 2003-12-24 Smithkline Beecham Corporation Chemical process
WO2004002964A1 (ja) 2002-06-28 2004-01-08 Yamanouchi Pharmaceutical Co., Ltd. ジアミノピリミジンカルボキサミド誘導体
NZ537752A (en) 2002-07-29 2006-12-22 Rigel Pharmaceuticals Inc Use of 2,4-pyrimidinediamine compounds in the preparation of medicaments for treating autoimmune diseases
WO2004014384A2 (en) 2002-08-13 2004-02-19 Warner-Lambert Company Llc Cyclic compounds containing zinc binding groups as matrix metalloproteinase inhibitors
RU2005106871A (ru) * 2002-08-14 2005-10-10 Вертекс Фармасьютикалз Инкорпорейтед (Us) Ингибиторы протеинкиназ и их применение
JP2006512314A (ja) 2002-11-01 2006-04-13 バーテックス ファーマシューティカルズ インコーポレイテッド Jakインヒビターおよび他のプロテインキナーゼインヒビターとしての組成物の使用
DE60316013T2 (de) 2002-11-04 2008-05-29 Vertex Pharmaceuticals Inc., Cambridge Heteroaryl-pyrimidinderivate als jak-inhibitoren
CA2507406A1 (en) 2002-11-05 2004-05-21 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of jak and other protein kinases
GB0226583D0 (en) 2002-11-14 2002-12-18 Cyclacel Ltd Compounds
GB0226582D0 (en) 2002-11-14 2002-12-18 Cyclacel Ltd Anti-viral compounds
AR042052A1 (es) 2002-11-15 2005-06-08 Vertex Pharma Diaminotriazoles utiles como inhibidores de proteinquinasas
CN101353321A (zh) 2002-11-21 2009-01-28 辉瑞产品公司 3-氨基-哌啶衍生物及其制备方法
BR0316487A (pt) 2002-11-26 2005-10-11 Pfizer Prod Inc Método todo de tratamento da rejeição de transplantes
RS20050363A (en) 2002-11-28 2007-11-15 Schering Aktiengesellschaft, Chk-,pdk-and akt-inhibitory pyrimidines,their production an use as pharmaceutical agents
WO2004050068A1 (en) 2002-11-29 2004-06-17 Janssen Pharmaceutica N.V. Pharmaceutical compositions comprising a basic respectively acidic drug compound, a surfactant and a physiologically tolerable water-soluble acid respectively base
WO2004054617A1 (ja) 2002-12-13 2004-07-01 Kyowa Hakko Kogyo Co., Ltd. 中枢疾患の予防および/または治療剤
WO2004058749A1 (en) 2002-12-18 2004-07-15 Vertex Pharmaceuticals Incorporated Benzisoxazole derivatives useful as inhibitors of protein kinases
US7098332B2 (en) * 2002-12-20 2006-08-29 Hoffmann-La Roche Inc. 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
PL227577B1 (pl) 2003-02-07 2017-12-29 Janssen Pharmaceutica Nv Zastosowanie pochodnych pirymidyny do wytwarzania leku do zapobiegania zakażeniu wirusem HIV oraz kompozycja farmaceutyczna
CL2004000303A1 (es) 2003-02-20 2005-04-08 Tibotec Pharm Ltd Compuestos derivados de pirimidinas y triazinas; proceso de preparacion; composicion farmaceutica; y su uso para inhibir la replicacion del vih.
ES2325440T3 (es) 2003-02-20 2009-09-04 Smithkline Beecham Corporation Compuestos de pirimidina.
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
AU2004230841A1 (en) 2003-04-03 2004-10-28 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
AU2004236239A1 (en) 2003-04-30 2004-11-18 The Institutes For Pharmaceutical Discovery, Llc Substituted heteroaryls as inhibitors of protein tyrosine phosphatases
GB0311276D0 (en) 2003-05-16 2003-06-18 Astrazeneca Ab Chemical compounds
GB0311274D0 (en) 2003-05-16 2003-06-18 Astrazeneca Ab Chemical compounds
US7915293B2 (en) 2003-05-30 2011-03-29 Rigel Pharmaceuticals, Inc. Ubiquitin ligase inhibitors
CA2531401A1 (en) 2003-07-10 2005-01-27 Neurogen Corporation Substituted heterocyclic diarylamine analogues
CA2531232A1 (en) 2003-07-16 2005-02-10 Janssen Pharmaceutica N.V. Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors
DK1658292T3 (da) 2003-07-16 2007-11-12 Janssen Pharmaceutica Nv Triazologyrimidinderivater som glycogensynthasekinase 3 - inhibitorer
US20070161637A1 (en) 2003-07-22 2007-07-12 Neurogen Corporation Substituted pyridin-2-ylamine analogues
US7442698B2 (en) * 2003-07-24 2008-10-28 Amgen Inc. Substituted heterocyclic compounds and methods of use
EP1651599A4 (en) 2003-07-24 2008-09-24 Merck & Co Inc TYROSINE KINASE INHIBITORS
ES2421139T3 (es) 2003-07-30 2013-08-29 Rigel Pharmaceuticals, Inc. Compuestos de 2,4-pirimidindiamina para su uso en el tratamiento o la prevención de enfermedades autoinmunitarias
EP1648875A1 (en) 2003-07-30 2006-04-26 Cyclacel Limited 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors
DE602004032446D1 (de) 2003-08-07 2011-06-09 Rigel Pharmaceuticals Inc 2,4-pyrimidindiamin-verbindungen und verwendungen als antiproliferative mittel
AU2004264724A1 (en) 2003-08-14 2005-02-24 Pfizer Inc. Piperazine derivatives for the treatment of HIV infections
WO2005016894A1 (en) 2003-08-15 2005-02-24 Novartis Ag 2, 4-pyrimidinediamines useful in the treatment of neoplastic diseases, inflammatory and immune system disorders
TWI339206B (en) 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
WO2005028467A1 (en) 2003-09-15 2005-03-31 Anadys Pharmaceuticals, Inc. Antibacterial 3,5-diaminopiperidine-substitute aromatic and heteroaromatic compounds
GB0321710D0 (en) 2003-09-16 2003-10-15 Novartis Ag Organic compounds
US20070105839A1 (en) 2003-09-18 2007-05-10 Patricia Imbach 2, 4-Di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
WO2005027848A2 (en) 2003-09-19 2005-03-31 Barnes-Jewish Hospital Methods for screening osteogenic compounds targeting syk kinase and/or vav3 and uses of syk modulators and/or vav modulators
US8026245B2 (en) 2003-09-25 2011-09-27 Janssen Pharmaceutica N.V. HIV replication inhibiting purine derivatives
KR100777885B1 (ko) 2003-10-03 2007-11-28 화이자 인코포레이티드 Hiv 및 염증 치료를 위한 ccr5 수용체 길항제 활성을갖는 이미다조피리딘 치환된 트로판 유도체
DE10349423A1 (de) 2003-10-16 2005-06-16 Schering Ag Sulfoximinsubstituierte Parimidine als CDK- und/oder VEGF-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
US7235161B2 (en) * 2003-11-19 2007-06-26 Alcoa Inc. Stable anodes including iron oxide and use of such anodes in metal production cells
US20080312192A1 (en) 2003-11-28 2008-12-18 Guido Bold Diaryl Urea Derivatives in the Treatment of Protein Kinase Dependent Diseases
MY141255A (en) 2003-12-11 2010-03-31 Memory Pharm Corp Phosphodiesterase 4 inhibitors, including n-substituted diarylamine analogs
EP1694652A1 (en) 2003-12-19 2006-08-30 Rigel Pharmaceuticals, Inc. Stereoisomers and stereoisomeric mixtures of 1-(2,4-pyrimidinediamino)-2-cyclopentanecarboxamide synthetic intermediates
ZA200602666B (en) 2004-01-12 2007-09-26 Cytopia Res Pty Ltd Selective kinase inhibitors
GB0402653D0 (en) 2004-02-06 2004-03-10 Cyclacel Ltd Compounds
CN1918158B (zh) 2004-02-14 2011-03-02 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
US7745625B2 (en) 2004-03-15 2010-06-29 Bristol-Myers Squibb Company Prodrugs of piperazine and substituted piperidine antiviral agents
WO2005107760A1 (en) 2004-04-30 2005-11-17 Irm Llc Compounds and compositions as inducers of keratinocyte differentiation
WO2005118544A2 (en) * 2004-05-18 2005-12-15 Rigel Pharmaceuticals, Inc. Cycloalkyl substituted pyrimidinediamine compounds and their uses
GB0419161D0 (en) 2004-08-27 2004-09-29 Novartis Ag Organic compounds
US20060047135A1 (en) 2004-08-30 2006-03-02 Chadwick Scott T Process for preparing chloromethyl di-tert-butylphosphate
US20060058525A1 (en) * 2004-09-01 2006-03-16 Rajinder Singh Synthesis of 2,4-pyrimidinediamine compounds
WO2006034872A1 (de) * 2004-09-29 2006-04-06 Bayer Schering Pharma Aktiengesellschaft Substituierte 2-anilinopyrimidine als zellzyklus -kinase oder rezeptortyrosin-kinase inhibitoren, deren herstellung und verwendung als arzneimittel
EP1817303A2 (en) 2004-10-29 2007-08-15 Rigel Pharmaceuticals, Inc. Substituted pyridines with activity on syk kinase
US7557207B2 (en) * 2004-11-24 2009-07-07 Rigel Pharmaceuticals, Inc. Spiro 2,4-pyrimidinediamine compounds and their uses
US7442716B2 (en) 2004-12-17 2008-10-28 Merck Frosst Canada Ltd. 2-(phenyl or heterocyclic)-1H-phenantrho[9,10-d]imidazoles as mPGES-1 inhibitors
AU2005322855B2 (en) 2004-12-30 2012-09-20 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
ES2337496T3 (es) 2005-01-19 2010-04-26 Rigel Pharmaceuticals, Inc. Profarmacos de compuestos de 2,4-pirimidindiamina y sus usos.
WO2007027238A2 (en) 2005-05-03 2007-03-08 Rigel Pharmaceuticals, Inc. Jak kinase inhibitors and their uses
JP5225079B2 (ja) 2005-06-08 2013-07-03 ライジェル ファーマシューティカルズ, インコーポレイテッド Jak経路の阻害のための組成物および方法
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US7576053B2 (en) * 2005-06-13 2009-08-18 Rigel Pharmaceuticals, Inc. Methods and compositions for treating degenerative bone disorders
KR20080027832A (ko) 2005-07-11 2008-03-28 사노피-아벤티스 신규의 2,4-디아닐리노피리미딘 유도체, 그의 제법, 및의약으로서, 제약 조성물로서, 특히 ikk 억제제로서의그의 용도
CA2616512A1 (en) 2005-07-28 2007-02-08 Intervet International B.V. Novel benzimidazole (thio) carbamates with antiparasitic activity and the synthesis thereof
WO2007032263A1 (ja) 2005-09-13 2007-03-22 Eisai R & D Management Co., Ltd. 安定性が改善されたクロロメチルフォスフェイト誘導体を含む組成物およびその製造方法
EP1951261A4 (en) 2005-10-31 2009-06-24 Rigel Pharmaceuticals Inc PREPARATIONS AND METHODS FOR THE TREATMENT OF INFLAMMATORY DISORDERS
AU2006309013B2 (en) 2005-11-01 2012-06-28 Impact Biomedicines, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
US7713987B2 (en) * 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
US7962290B1 (en) * 2006-01-09 2011-06-14 Rigel Pharmaceuticals, Inc. Identification of pharmacophores from co-crystals of spleen tyrosine kinase (SYK) and SYK ligands
TW200736232A (en) 2006-01-26 2007-10-01 Astrazeneca Ab Pyrimidine derivatives
WO2007085540A1 (en) 2006-01-27 2007-08-02 Glaxo Group Limited 1h-indaz0l-4-yl-2 , 4-pyrimidinediamine derivatives
WO2007120980A2 (en) 2006-02-17 2007-10-25 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for treating or preventing autoimmune diseases
ES2622493T3 (es) 2006-02-24 2017-07-06 Rigel Pharmaceuticals, Inc. Composiciones y métodos para la inhibición de la ruta de JAK
US20090192158A1 (en) 2006-05-02 2009-07-30 Stacia Kargman Methods for Treating or Preventing Neoplasias
US7776855B2 (en) 2006-07-27 2010-08-17 Janssen Pharmaceutica N.V. Antimicrobial oxazolidinone prodrugs
CA2673125C (en) 2006-10-19 2015-04-21 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US7947698B2 (en) 2007-03-23 2011-05-24 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
US7834024B2 (en) 2007-03-26 2010-11-16 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
CA2693594A1 (en) 2007-07-17 2009-01-22 Rigel Pharmaceuticals, Inc. Cyclic amine substituted pyrimidinediamines as pkc inhibitors
DK2683385T3 (en) * 2011-03-10 2018-09-17 Rigel Pharmaceuticals Inc 2,4-SUBSTITUTED PYRIMIDINE DIAMINES FOR DISKOID LUPUS USE

Patent Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1991018887A1 (en) * 1990-06-06 1991-12-12 Smithkline Beecham Intercredit B.V. Diaminopyrimidine compounds
US5958935A (en) * 1995-11-20 1999-09-28 Celltech Therapeutics Limited Substituted 2-anilinopyrimidines useful as protein kinase inhibitors
WO1999031073A1 (fr) * 1997-12-15 1999-06-24 Yamanouchi Pharmaceutical Co., Ltd. Nouveaux derives de pyrimidine-5-carboxamide
WO1999050250A1 (en) * 1998-03-27 1999-10-07 Janssen Pharmaceutica N.V. Hiv inhibiting pyrimidine derivatives
WO2000027825A1 (en) * 1998-11-10 2000-05-18 Janssen Pharmaceutica N.V. Hiv replication inhibiting pyrimidines
WO2000039101A1 (en) * 1998-12-24 2000-07-06 Astrazeneca Ab Pyrimidine compounds
WO2001022938A1 (en) * 1999-09-24 2001-04-05 Janssen Pharmaceutica N.V. Antiviral compositions
WO2001023362A2 (en) * 1999-09-24 2001-04-05 Abbott Gmbh & Co. Kg Rate-controlled particles
WO2001060816A1 (en) * 2000-02-17 2001-08-23 Amgen Inc. Kinase inhibitors
WO2001064656A1 (en) * 2000-03-01 2001-09-07 Astrazeneca Ab 2,4,di(hetero-)arylamino(-oxy)-5-substituted pyrimidines as antineoplastic agents
WO2001085699A2 (en) * 2000-05-08 2001-11-15 Janssen Pharmaceutica N.V. Prodrugs of hiv replication inhibiting pyrimidines
WO2002004429A1 (en) * 2000-07-11 2002-01-17 Astrazeneca Ab Pyrimidine derivatives

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
D. GHOSH: "2,4-bis(arylamino)-5-methylpyrimidines as antimicrobial agent" JOURNAL OF MEDICINAL CHEMISTRY., vol. 10, no. 5, 1967, pages 974-975 *
D. LUDOVICI ET AL.: "evolution of anti-hiv drug candidates.Part 3:diarylpyrimidine analogues." BIOORGANIC & MEDICINAL CHEMISTRY LETTERS., vol. 11, 2001, strane 2235-2239 *
DOLLY GHOSH: "2,4-bis(arylamino)-6-methyl pyrimidines as antimicrobial agents." J. INDIAN CHEM. SOC., vol. LVIII, May 1981 (1981-05), strane 512-513 *
M.M. EL-KERDAWY: "2,4-bis(substituted)-5-nitropyrimidines of expected diuretic action." EGYPT J. CHEM., vol. 29, no. 2, 1986, strane 247-251 *

Also Published As

Publication number Publication date
BRPI0307355C1 (pt) 2021-05-25
JP2005516046A (ja) 2005-06-02
US9499493B2 (en) 2016-11-22
US8853397B2 (en) 2014-10-07
US20150126504A1 (en) 2015-05-07
US20150005297A1 (en) 2015-01-01
US20060058292A1 (en) 2006-03-16
US10369148B2 (en) 2019-08-06
US9913842B2 (en) 2018-03-13
US20070293522A1 (en) 2007-12-20
EP1471915A2 (en) 2004-11-03
US20200085820A1 (en) 2020-03-19
US9162989B2 (en) 2015-10-20
US10314840B2 (en) 2019-06-11
BRPI0307355B1 (pt) 2018-11-13
US8748597B2 (en) 2014-06-10
SI1471915T1 (sl) 2012-03-30
US20070293521A1 (en) 2007-12-20
BRPI0307355B8 (pt) 2019-08-06
US20090082567A1 (en) 2009-03-26
US20150329532A1 (en) 2015-11-19
HRP20040684A2 (hr) 2008-12-31
RS54105B1 (en) 2015-10-30
US20130324524A1 (en) 2013-12-05
US8822685B2 (en) 2014-09-02
NZ534361A (en) 2008-04-30
EP2281563A1 (en) 2011-02-09
SI2281563T1 (sl) 2014-02-28
TW200307547A (en) 2003-12-16
US20060135543A1 (en) 2006-06-22
SG167664A1 (en) 2011-01-28
US20070293524A1 (en) 2007-12-20
DK1471915T3 (da) 2012-01-09
US20060035916A1 (en) 2006-02-16
NO328071B1 (no) 2009-11-23
KR101037856B1 (ko) 2011-06-01
PL214988B1 (pl) 2013-10-31
MX341239B (es) 2016-08-12
AU2003208931B2 (en) 2008-09-04
US20130317216A1 (en) 2013-11-28
WO2003063794A3 (en) 2003-12-04
US10682350B2 (en) 2020-06-16
CY1112516T1 (el) 2015-12-09
US7557210B2 (en) 2009-07-07
US7498435B2 (en) 2009-03-03
US20150158823A1 (en) 2015-06-11
CN1625400B (zh) 2011-04-13
US10828301B2 (en) 2020-11-10
US9416112B2 (en) 2016-08-16
NO20043632L (no) 2004-10-26
PL373530A1 (en) 2005-09-05
YU67404A (sh) 2006-08-17
US11007193B2 (en) 2021-05-18
CN102174024B (zh) 2015-02-11
US20170151239A1 (en) 2017-06-01
US20150266828A1 (en) 2015-09-24
JP5357116B2 (ja) 2013-12-04
US8148525B2 (en) 2012-04-03
US7803939B2 (en) 2010-09-28
ATE524184T1 (de) 2011-09-15
CN1625400A (zh) 2005-06-08
US7550460B2 (en) 2009-06-23
US20070293520A1 (en) 2007-12-20
US10709703B2 (en) 2020-07-14
IL221381A (en) 2015-05-31
US7329672B2 (en) 2008-02-12
US20170246167A1 (en) 2017-08-31
US20190358228A1 (en) 2019-11-28
US8188276B2 (en) 2012-05-29
JP2010285441A (ja) 2010-12-24
US20160009660A1 (en) 2016-01-14
CA2474277C (en) 2013-09-24
PT2281563E (pt) 2013-12-09
US20190255047A1 (en) 2019-08-22
RS53367B (en) 2014-10-31
US9018204B1 (en) 2015-04-28
US7642351B2 (en) 2010-01-05
TWI329105B (en) 2010-08-21
IL221381A0 (en) 2012-09-24
JP4658477B2 (ja) 2011-03-23
RS20120098A1 (en) 2012-08-31
EP1471915B1 (en) 2011-09-14
US20070225321A1 (en) 2007-09-27
EP2281563B1 (en) 2013-09-18
KR20040101216A (ko) 2004-12-02
US7435814B2 (en) 2008-10-14
PT1471915E (pt) 2011-12-26
US20050038243A1 (en) 2005-02-17
US8334296B2 (en) 2012-12-18
US20140330007A1 (en) 2014-11-06
US8410266B2 (en) 2013-04-02
US20210267971A1 (en) 2021-09-02
ES2440283T3 (es) 2014-01-28
US9346765B2 (en) 2016-05-24
US20070293523A1 (en) 2007-12-20
US20050209230A1 (en) 2005-09-22
ES2373646T3 (es) 2012-02-07
HK1154216A1 (hr) 2012-04-13
US8835430B2 (en) 2014-09-16
US7820819B2 (en) 2010-10-26
US9586908B2 (en) 2017-03-07
BR0307355A (pt) 2006-04-11
US20040029902A1 (en) 2004-02-12
US20090171085A1 (en) 2009-07-02
EP1471915A4 (en) 2006-02-15
AU2003208931C1 (en) 2009-04-02
HK1069538A1 (hr) 2005-05-27
US7060827B2 (en) 2006-06-13
US20110144330A1 (en) 2011-06-16
US7655797B2 (en) 2010-02-02
US9133133B2 (en) 2015-09-15
US7485724B2 (en) 2009-02-03
US7332484B2 (en) 2008-02-19
US9540334B2 (en) 2017-01-10
US20130150349A1 (en) 2013-06-13
US20170081290A1 (en) 2017-03-23
WO2003063794A2 (en) 2003-08-07
US20160009661A1 (en) 2016-01-14
CA2474277A1 (en) 2003-08-07
US20140303154A1 (en) 2014-10-09
US20120045454A1 (en) 2012-02-23
US20100197918A1 (en) 2010-08-05
US20090156622A1 (en) 2009-06-18
US7589200B2 (en) 2009-09-15
US20060025410A1 (en) 2006-02-02
US7329671B2 (en) 2008-02-12
DK2281563T3 (da) 2014-01-13
US20080039622A1 (en) 2008-02-14
US20090171086A1 (en) 2009-07-02
US9040550B2 (en) 2015-05-26
CN102174024A (zh) 2011-09-07
US20140031350A1 (en) 2014-01-30
MXPA04007386A (es) 2006-04-27
US7906644B2 (en) 2011-03-15
AU2008252053A1 (en) 2009-01-08

Similar Documents

Publication Publication Date Title
HRP20040684B1 (hr) Spojevi 2,4-pirimidindiamina i njihova upotreba
ATE399165T1 (de) Chinolinverbindungen und deren verwendungen
NL300933I2 (nl) Letermovir
TNSN05272A1 (fr) Ligands de recepteurs de cannabinoides et leurs utilisations
DK1556021T3 (da) Farmaceutiske sammensætninger omfattende flavonoider og menthol samt fremgangsmåder til behandling med brug af nævnte sammensætninger
DK1594833T3 (da) 1-phenylalkancarboxylsyrederivater til behandling af neurodegenerative sygdomme
MA31767B1 (fr) Composes organiques et leurs utilisations
BG66080B1 (bg) Заместени тиоацетамиди
DOP2002000429A (es) Imidazotriazinas
BRPI0411900A (pt) compostos antivirais e métodos
EA200401341A1 (ru) Применение остеопротегерина для лечения и/или профилактики фиброзного заболевания
MA30485B1 (fr) Aminothiazoles et leurs utilisations
GT200400231A (es) Compuestos de sulfoniltetrahidro-3h-benzo(e)indol-8-amina como ligandos de la 5-hidroxitriptamina-6.
DE69936774D1 (de) Strukturproteine des virus, welches die pankreas-krankheit bei fischen verursacht, und ihre verwendungen
CY1115243T1 (el) Ενωσεις 2,4-πυριμιδινοδιαμινης και οι χρησεις τους
DE602004012759D1 (de) Behandlung von fibrosen
DE60326348D1 (de) Makrozyclen zur behandlung von krebserkrankungen
ATE286390T1 (de) Felabamat-derivate zur behandlung von neuropathischem schmerz
DOP2003000728A (es) Compuestos de tiazol para el tratamiento de trastornos neurodegenetivos

Legal Events

Date Code Title Description
A1OB Publication of a patent application
AIPI Request for the grant of a patent on the basis of a substantive examination of a patent application
B1PR Patent granted
ODRP Renewal fee for the maintenance of a patent

Payment date: 20190107

Year of fee payment: 17

ODRP Renewal fee for the maintenance of a patent

Payment date: 20200108

Year of fee payment: 18

ODRP Renewal fee for the maintenance of a patent

Payment date: 20210120

Year of fee payment: 19

ODRP Renewal fee for the maintenance of a patent

Payment date: 20220104

Year of fee payment: 20

PB20 Patent expired after termination of 20 years

Effective date: 20230131