MX350010B - Inhibidores syk de imidazopiridinas. - Google Patents

Inhibidores syk de imidazopiridinas.

Info

Publication number
MX350010B
MX350010B MX2012010418A MX2012010418A MX350010B MX 350010 B MX350010 B MX 350010B MX 2012010418 A MX2012010418 A MX 2012010418A MX 2012010418 A MX2012010418 A MX 2012010418A MX 350010 B MX350010 B MX 350010B
Authority
MX
Mexico
Prior art keywords
imidazopyridines
methods
syk inhibitors
syk
certain
Prior art date
Application number
MX2012010418A
Other languages
English (en)
Other versions
MX2012010418A (es
Inventor
Peter Blomgren
Kevin S Currie
E Jeffrey
Seung H Lee
Scott A Mitchell
Aaron C Schmitt
Jianjun Xu
Zhongdong Zhao
Original Assignee
Gilead Connecticut 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
Application filed by Gilead Connecticut Inc filed Critical Gilead Connecticut Inc
Publication of MX2012010418A publication Critical patent/MX2012010418A/es
Publication of MX350010B publication Critical patent/MX350010B/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/69Boron compounds
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/4985Pyrazines or piperazines 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
    • A61K31/495Heterocyclic 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/04Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-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
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12QMEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/48Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase
    • C12Q1/485Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase involving kinase

Abstract

Se proporcionan en la presente ciertas imidazopiridinas (I) y composiciones farmacéuticas de las mismas. Se proporcionan métodos para tratar pacientes que sufren de ciertas enfermedades y trastornos que responden a la inhibición de la actividad de Syk, los cuales comprenden administrar a tales pacientes una cantidad de al menos una entidad química efectiva para reducir los signos o síntomas de la enfermedad o trastorno. También se proporcionan métodos para determina la presencia o ausencia de la Syk quinasa en una muestra.
MX2012010418A 2010-03-11 2011-03-11 Inhibidores syk de imidazopiridinas. MX350010B (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US31277110P 2010-03-11 2010-03-11
US31322310P 2010-03-12 2010-03-12
PCT/US2011/028194 WO2011112995A1 (en) 2010-03-11 2011-03-11 Imidazopyridines syk inhibitors

Publications (2)

Publication Number Publication Date
MX2012010418A MX2012010418A (es) 2013-01-14
MX350010B true MX350010B (es) 2017-08-23

Family

ID=43828318

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2012010418A MX350010B (es) 2010-03-11 2011-03-11 Inhibidores syk de imidazopiridinas.

Country Status (14)

Country Link
US (3) US9562056B2 (es)
EP (1) EP2545052B1 (es)
JP (3) JP5938352B2 (es)
KR (1) KR101717809B1 (es)
CN (1) CN103168039B (es)
AU (3) AU2011226689B2 (es)
BR (1) BR112012022943A2 (es)
CA (1) CA2792769C (es)
ES (1) ES2530449T3 (es)
HK (1) HK1180689A1 (es)
MX (1) MX350010B (es)
NZ (1) NZ602362A (es)
PT (1) PT2545052E (es)
WO (1) WO2011112995A1 (es)

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2009215191A1 (en) 2008-02-13 2009-08-20 Gilead Connecticut, Inc. 6-aryl-imidaz0[l, 2-a] pyrazine derivatives, method of making, and method of use thereof
PT2716157T (pt) 2008-12-08 2016-08-23 Gilead Connecticut Inc Imidazopirazinas ¿ inibidores de syc
JP5696052B2 (ja) 2008-12-08 2015-04-08 ギリアード コネチカット, インコーポレイテッド イミダゾピラジンsyk阻害剤
US9562056B2 (en) 2010-03-11 2017-02-07 Gilead Connecticut, Inc. Imidazopyridines Syk inhibitors
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
BR112014010391A2 (pt) * 2011-11-03 2017-04-18 Hoffmann La Roche composto, composição farmacêutica, processo de produção de uma composição farmacêutica, método de tratamento, kit e uso de uma composição farmacêutica
LT3495367T (lt) 2012-06-13 2021-02-25 Incyte Holdings Corporation Pakeistieji tricikliniai junginiai, kaip fgfr inhibitoriai
US20130338142A1 (en) * 2012-06-14 2013-12-19 Gilead Connecticut, Inc. Imidazopyrazine syk inhibitors
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
CN102898426B (zh) * 2012-11-15 2015-04-22 江苏先声药业有限公司 抑制igf-1r酪氨酸激酶活性的吡啶并吡唑类衍生物
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
MY181497A (en) 2013-04-19 2020-12-23 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
JP6153667B2 (ja) 2013-07-30 2017-06-28 ギリアード コネチカット, インコーポレイテッド Sky阻害剤の製剤
PL3027618T3 (pl) 2013-07-30 2021-04-19 Kronos Bio, Inc. Polimorf inhibitorów syk
SG11201600373YA (en) 2013-07-31 2016-02-26 Gilead Sciences Inc Syk inhibitors
SG11201603050TA (en) 2013-12-04 2016-05-30 Gilead Sciences Inc Methods for treating cancers
TWI735853B (zh) 2013-12-23 2021-08-11 美商克洛諾斯生技有限公司 脾酪胺酸激酶抑制劑
US9290505B2 (en) 2013-12-23 2016-03-22 Gilead Sciences, Inc. Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
WO2015157955A1 (en) * 2014-04-17 2015-10-22 Abbvie Inc. Heterocyclic btk inhibit ors
MA40075A (fr) 2014-07-14 2016-01-21 Gilead Sciences Inc Combinaisons pour traiter des cancers
TW201617074A (zh) * 2014-07-14 2016-05-16 吉李德科學股份有限公司 Syk(脾酪胺酸激酶)抑制劑
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
WO2016134320A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
CN108699084A (zh) * 2015-12-10 2018-10-23 拜耳制药股份公司 取代全氢吡咯并[3,4-c]吡咯衍生物及其用途
US10111882B2 (en) 2016-09-14 2018-10-30 Gilead Sciences, Inc. SYK inhibitors
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
CN110678461B (zh) * 2017-06-14 2021-08-10 正大天晴药业集团股份有限公司 Syk抑制剂及其使用方法
US11384082B2 (en) 2017-08-25 2022-07-12 Kronos Bio, Inc. Hydrates of polymorphs of 6-(1H-indazol-6-YL)-N-(4-morpholinophenyl)-2,3-dihydroimidazo[1,2-A]pyrazin-8-amine bisemsylate as Syk inhibitors
EP3788046A1 (en) 2018-05-04 2021-03-10 Incyte Corporation Salts of an fgfr inhibitor
MA52494A (fr) 2018-05-04 2021-03-10 Incyte Corp Formes solides d'un inhibiteur de fgfr et leurs procédés de préparation
WO2020113094A1 (en) 2018-11-30 2020-06-04 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
CN113950479A (zh) 2019-02-22 2022-01-18 克洛诺斯生物股份有限公司 作为syk抑制剂的缩合吡嗪的固体形式
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
WO2020188015A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
CN110183471B (zh) * 2019-05-21 2022-02-15 江苏大学 一种哌嗪类衍生物及制备方法及应用
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
EP4045151A1 (en) 2019-10-14 2022-08-24 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021089791A1 (en) 2019-11-08 2021-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021113479A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CA3162010A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Derivatives of an fgfr inhibitor
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN112010879B (zh) * 2020-09-15 2021-07-02 山西大学 一种Zn功能配合物及其制备方法和应用
TW202313611A (zh) 2021-06-09 2023-04-01 美商英塞特公司 作為fgfr抑制劑之三環雜環
CN113636973B (zh) * 2021-09-07 2023-04-07 山东铂源药业股份有限公司 一种4-(6-氨基吡啶-3-基)哌嗪-1-羧酸叔丁酯的工业化制备方法

Family Cites Families (74)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US4326525A (en) 1980-10-14 1982-04-27 Alza Corporation Osmotic device that improves delivery properties of agent in situ
US5364620A (en) 1983-12-22 1994-11-15 Elan Corporation, Plc Controlled absorption diltiazem formulation for once daily administration
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
FR2607813B1 (fr) 1986-12-05 1989-03-31 Montpellier I Universite Alkylamino-8 imidazo (1,2-a) pyrazines et derives, leur preparation et leur application en therapeutique
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
US4902514A (en) 1988-07-21 1990-02-20 Alza Corporation Dosage form for administering nilvadipine for treating cardiovascular symptoms
US5137876A (en) 1990-10-12 1992-08-11 Merck & Co., Inc. Nucleoside antiviral and anti-inflammatory compounds and compositions and methods for using same
DE4327027A1 (de) 1993-02-15 1994-08-18 Bayer Ag Imidazoazine
DE4337609A1 (de) 1993-11-04 1995-05-11 Boehringer Ingelheim Kg Neue Pyrazincarboxamidderivate, ihre Herstellung und ihre Verwendung in Arzneimitteln
DE4337611A1 (de) 1993-11-04 1995-05-11 Boehringer Ingelheim Kg Neue Benzoylguanidine, ihre Herstellung und ihre Verwendung in Arzneimitteln
FR2711993B1 (fr) 1993-11-05 1995-12-01 Rhone Poulenc Rorer Sa Médicaments contenant des dérivés de 7H-imidazol[1,2-a]pyrazine-8-one, les nouveaux composés et leur préparation.
US6334997B1 (en) 1994-03-25 2002-01-01 Isotechnika, Inc. Method of using deuterated calcium channel blockers
WO1995026325A2 (en) 1994-03-25 1995-10-05 Isotechnika Inc. Enhancement of the efficacy of drugs by deuteration
FR2723373B1 (fr) 1994-08-02 1996-09-13 Rhone Poulenc Rorer Sa Forme purifiee de streptogramines, sa preparation et les compositions pharmaceutiques qui la contiennent
WO1996034866A1 (en) 1995-05-01 1996-11-07 Fujisawa Pharmaceutical Co., Ltd. Imidazo 1,2-a pyridine and imidazo 1,2-a pyridezine derivatives and their use as bone resorption inhibitors
US5593997A (en) 1995-05-23 1997-01-14 Pfizer Inc. 4-aminopyrazolo(3-,4-D)pyrimidine and 4-aminopyrazolo-(3,4-D)pyridine tyrosine kinase inhibitors
SE9704404D0 (sv) 1997-11-28 1997-11-28 Astra Ab New compounds
EE05699B1 (et) * 1999-01-25 2014-02-17 Biogen, Inc. BAFF, sellega seonduvad blokeerivad ained ja nende kasutamine B-rakkude ja immunoglobuliinide stimuleerimisel ja p„rssimisel immuunsusreaktsioonides
DE19948434A1 (de) 1999-10-08 2001-06-07 Gruenenthal Gmbh Substanzbibliothek enthaltend bicyclische Imidazo-5-amine und/oder bicyclische Imidazo-3-amine
JP2001302667A (ja) 2000-04-28 2001-10-31 Bayer Ag イミダゾピリミジン誘導体およびトリアゾロピリミジン誘導体
GB0018473D0 (en) 2000-07-27 2000-09-13 Merck Sharp & Dohme Therapeutic agents
DE10050663A1 (de) 2000-10-13 2002-04-18 Gruenenthal Gmbh Verwendung von substituierten Imidazo[1,2-a]pyridin-, -pyrimidin- und pyrazin-3-yl-amin-Derivaten zur Herstellung von Medikamenten zur NOS-Inhibierung
WO2002060492A1 (en) 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
GB0103926D0 (en) 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
WO2002076985A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
AU2003219690A1 (en) 2002-02-19 2003-09-09 Pharmacia And Upjohn Company Fused bicyclic-n-bridged-heteroaromatic carboxamides for the treatment of disease
CA2482991A1 (en) 2002-04-19 2003-10-30 Cellular Genomics, Inc. Imidazo[1,2-a]pyrazin-8-ylamines method of making and method of use thereof
WO2004022562A1 (en) 2002-09-09 2004-03-18 Cellular Genomics, Inc. 6-ARYL-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINES, METHOD OF MAKING, AND METHOD OF USE THEREOF
US6992080B2 (en) * 2002-09-19 2006-01-31 Schering Corporation Imidazopyridines as cyclin dependent kinase inhibitors
KR20060010709A (ko) 2002-09-23 2006-02-02 쉐링 코포레이션 사이클린 의존성 키나제 억제제로서의 신규한 이미다조피라진
NZ538685A (en) 2002-09-23 2008-02-29 Schering Corp Imidazopyrazines as cyclin dependent kinase inhibitors
WO2004072081A1 (en) 2003-02-10 2004-08-26 Cellular Genomics, Inc. Certain 8-heteroaryl-6-phenyl-imidazo[1,2-a]pyrazines as modulators of kinase activity
AR043002A1 (es) 2003-02-18 2005-07-13 Altana Pharma Ag Imidazopirazinas 6-substituidos
US7157460B2 (en) 2003-02-20 2007-01-02 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
US7186832B2 (en) 2003-02-20 2007-03-06 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
US7405295B2 (en) 2003-06-04 2008-07-29 Cgi Pharmaceuticals, Inc. Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
US20060183746A1 (en) 2003-06-04 2006-08-17 Currie Kevin S Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
US7393848B2 (en) 2003-06-30 2008-07-01 Cgi Pharmaceuticals, Inc. Certain heterocyclic substituted imidazo[1,2-A]pyrazin-8-ylamines and methods of inhibition of Bruton's tyrosine kinase by such compounds
WO2005019220A2 (en) 2003-08-11 2005-03-03 Cellular Genomics Inc. Substituted imidazo[1,2-a]pyrazines as modulators of kinase activity
US7144907B2 (en) 2003-09-03 2006-12-05 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
WO2005047290A2 (en) * 2003-11-11 2005-05-26 Cellular Genomics Inc. Imidazo[1,2-a] pyrazin-8-ylamines as kinase inhibitors
WO2005085252A1 (en) 2004-03-04 2005-09-15 Biofocus Discovery Limited Imidazo ‘1,2-a’ pyrazine compounds which interact with protein kinases
DE602005023333D1 (de) 2004-10-15 2010-10-14 Takeda Pharmaceutical Kinaseinhibitoren
EP1812442A2 (en) * 2004-11-10 2007-08-01 CGI Pharmaceuticals, Inc. Imidazo[1,2-a]pyrazin-8-ylamines useful as modulators of kinase activity
WO2007008541A2 (en) 2005-07-08 2007-01-18 Kalypsys, Inc. Cellular cholesterol absorption modifiers
WO2007056468A1 (en) 2005-11-10 2007-05-18 Schering Corporation Methods for inhibiting protein kinases
AU2006315718B2 (en) 2005-11-10 2012-10-04 Merck Sharp & Dohme Corp. Imidazopyrazines as protein kinase inhibitors
CA2662074A1 (en) * 2006-08-30 2008-03-06 Cellzome Limited Triazole derivatives as kinase inhibitors
JP2010511019A (ja) * 2006-12-01 2010-04-08 ガラパゴス・ナムローゼ・フェンノートシャップ 変性疾患及び炎症性疾患の治療に有用なイミダゾロピリジン化合物
CN101952283B (zh) * 2007-12-14 2013-04-17 霍夫曼-拉罗奇有限公司 咪唑并[1,2-a]吡啶和咪唑并[1,2-b]哒嗪衍生物
AU2009215191A1 (en) 2008-02-13 2009-08-20 Gilead Connecticut, Inc. 6-aryl-imidaz0[l, 2-a] pyrazine derivatives, method of making, and method of use thereof
WO2009155388A1 (en) * 2008-06-20 2009-12-23 Bristol-Myers Squibb Company Imidazopyridine and imidazopyrazine compounds useful as kinase inhibitors
EP2307413B1 (en) 2008-07-15 2015-09-09 F. Hoffmann-La Roche AG Novel phenyl-imidazopyridines and pyridazines
TWI453207B (zh) 2008-09-08 2014-09-21 Signal Pharm Llc 胺基***并吡啶,其組合物及使用其之治療方法
WO2010038257A1 (ja) * 2008-09-30 2010-04-08 株式会社アドバンテスト プログラマブルデバイス、およびデータ書込方法
JP5696052B2 (ja) * 2008-12-08 2015-04-08 ギリアード コネチカット, インコーポレイテッド イミダゾピラジンsyk阻害剤
PT2716157T (pt) 2008-12-08 2016-08-23 Gilead Connecticut Inc Imidazopirazinas ¿ inibidores de syc
US8450321B2 (en) 2008-12-08 2013-05-28 Gilead Connecticut, Inc. 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor
US9562056B2 (en) 2010-03-11 2017-02-07 Gilead Connecticut, Inc. Imidazopyridines Syk inhibitors
US20140148430A1 (en) 2012-11-26 2014-05-29 Gilead Connecticut, Inc. Imidazopyridines syk inhibitors
PL3027618T3 (pl) 2013-07-30 2021-04-19 Kronos Bio, Inc. Polimorf inhibitorów syk
JP6153667B2 (ja) 2013-07-30 2017-06-28 ギリアード コネチカット, インコーポレイテッド Sky阻害剤の製剤
SG11201600373YA (en) 2013-07-31 2016-02-26 Gilead Sciences Inc Syk inhibitors
SG11201603050TA (en) 2013-12-04 2016-05-30 Gilead Sciences Inc Methods for treating cancers
TWI735853B (zh) 2013-12-23 2021-08-11 美商克洛諾斯生技有限公司 脾酪胺酸激酶抑制劑
US9290505B2 (en) 2013-12-23 2016-03-22 Gilead Sciences, Inc. Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
MA40075A (fr) 2014-07-14 2016-01-21 Gilead Sciences Inc Combinaisons pour traiter des cancers
TW201617074A (zh) 2014-07-14 2016-05-16 吉李德科學股份有限公司 Syk(脾酪胺酸激酶)抑制劑
TW201639573A (zh) 2015-02-03 2016-11-16 吉李德科學股份有限公司 有關治療癌症之合併治療
AU2016252387A1 (en) 2015-04-21 2017-10-19 Gilead Sciences, Inc. Treatment of chronic graft versus host disease with Syk inhibitors
US10111882B2 (en) 2016-09-14 2018-10-30 Gilead Sciences, Inc. SYK inhibitors
TW201822764A (zh) 2016-09-14 2018-07-01 美商基利科學股份有限公司 Syk抑制劑

Also Published As

Publication number Publication date
AU2018203210A1 (en) 2018-05-31
AU2016219585B2 (en) 2018-02-08
KR101717809B1 (ko) 2017-03-17
US20190117679A1 (en) 2019-04-25
WO2011112995A1 (en) 2011-09-15
US10842803B2 (en) 2020-11-24
JP2013522238A (ja) 2013-06-13
AU2016219585A1 (en) 2016-09-08
JP2015164938A (ja) 2015-09-17
MX2012010418A (es) 2013-01-14
JP6177828B2 (ja) 2017-08-09
PT2545052E (pt) 2015-02-18
CN103168039B (zh) 2016-08-03
ES2530449T3 (es) 2015-03-02
US20170095490A1 (en) 2017-04-06
CN103168039A (zh) 2013-06-19
KR20130038239A (ko) 2013-04-17
US20130210802A1 (en) 2013-08-15
EP2545052B1 (en) 2014-11-12
HK1180689A1 (en) 2013-10-25
BR112012022943A2 (pt) 2018-06-05
CA2792769A1 (en) 2011-09-15
US10092583B2 (en) 2018-10-09
JP2017222685A (ja) 2017-12-21
NZ602362A (en) 2014-11-28
AU2011226689A1 (en) 2012-09-27
JP5938352B2 (ja) 2016-06-22
AU2011226689B2 (en) 2016-09-01
CA2792769C (en) 2018-05-22
EP2545052A1 (en) 2013-01-16
US9562056B2 (en) 2017-02-07

Similar Documents

Publication Publication Date Title
MX2012010418A (es) Inhibidores syk de imidazopiridinas.
MX2011006091A (es) Inhibidores de imidazopirazina syk.
CO6390109A2 (es) Inhibidores de syk de imidazopirazina
CY1124307T1 (el) Φαρμακευτικη συνθεση, μεθοδοι θεραπειας και χρησεις αυτων
MY166890A (en) Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
PH12015502575B1 (en) Piperidin-4-yl azetidine derivatives as jak1 inhibitors
MX2014002459A (es) Inhibidores de quinurenina-3-monooxigenasa, composiciones farmaceuticas y metodos de uso de los mismos.
MX2013011908A (es) Composiciones y usos terapeuticos de inhibidores de cinasa epsilon relacionados con cinasa i-kappa b (ikk) y cinasa 1 de union tank.
BR112014026703A2 (pt) inibidores de dna-pk
BR112014004560A2 (pt) compostos e composições como inibidores de c-kit quinase
BR112013008140A2 (pt) "compostos imidazotriazinona".
AU2012286851A8 (en) Certain kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
IN2015DN00376A (es)
BR112014004319A2 (pt) compostos e composições como inibidores de c-kit cinase
IN2012DN02471A (es)
WO2013112950A3 (en) Certain chemical entities, compositions, and methods
JO2645B1 (en) Vehicles
MX2012013879A (es) Derivados de hidroxipiridona, composiciones farmceuticas de los mismos y su uso terapeutico para tratar enfermedades proliferativas.
BR112015000808A2 (pt) regime de dosagem para inibidores de janus quinase (jak)
MX2014000204A (es) Metodo de administracion y tratamiento.
MX357770B (es) Ácidos nucleicos de enlace sdf-1 y el uso de los mismos en el tratamiento de cáncer.
UA106971C2 (uk) Похідне імідазопіразину та фармацевтична композиція на його основі
BR112014019274A2 (pt) métodos relacionados ao tratamento de doenças e distúrbios inflamatórios
WO2013068993A3 (en) Tyrosine isomers as therapeutic agents
UA110108C2 (xx) Азетидинові похідні піперидин-4-ілу як інгібітори jak1

Legal Events

Date Code Title Description
FG Grant or registration