PE20110575A1 - INHIBIDORES DE mTOR CINASA PARA INDICADORES DE ONCOLOGIA Y ENFERMEDADES ASOCIADAS CON LA TRAYECTORIA mTOR/PI3K/AKT - Google Patents

INHIBIDORES DE mTOR CINASA PARA INDICADORES DE ONCOLOGIA Y ENFERMEDADES ASOCIADAS CON LA TRAYECTORIA mTOR/PI3K/AKT

Info

Publication number
PE20110575A1
PE20110575A1 PE2011000936A PE2011000936A PE20110575A1 PE 20110575 A1 PE20110575 A1 PE 20110575A1 PE 2011000936 A PE2011000936 A PE 2011000936A PE 2011000936 A PE2011000936 A PE 2011000936A PE 20110575 A1 PE20110575 A1 PE 20110575A1
Authority
PE
Peru
Prior art keywords
mtor
pirazin
methyl
pi3k
akt
Prior art date
Application number
PE2011000936A
Other languages
English (en)
Inventor
Jan Elsner
Roy L Harris
Branden Lee
Deborah Mortensen
Garrick Packard
Patrick Papa
Sophie Perrin-Ninkovic
Jennifer Riggs
Sabita Sankar
John Sapienza
Graziella Shevlin
Lida Tehrani
Weiming Xu
Jingjing Zhao
Janson Parnes
Loui Madakamutil
Kimberly Fultz
Rama K Narla
Original Assignee
Signal Pharm Llc
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=41490345&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20110575(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Signal Pharm Llc filed Critical Signal Pharm Llc
Publication of PE20110575A1 publication Critical patent/PE20110575A1/es

Links

Classifications

    • 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
    • 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
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • 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
    • 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
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • 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
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • 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
    • 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
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/20Nitrogen atoms
    • 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
    • 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/14Ortho-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
    • C07D487/10Spiro-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
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/14Ortho-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
    • 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
    • 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 Table
    • C07F5/02Boron compounds
    • C07F5/025Boronic and borinic acid compounds

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Otolaryngology (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE 3,4-DIHIDROPIRAZINO[2,3-b]PIRAZIN-2(1H)-ONA DE FORMULA (I) DONDE R1 ES ALQUILO(C1-C8), ARILO(C6-C14), CICLOALQUILO(C3-C10), ENTRE OTROS; R2 ES H, ALQUILO(C1-C8), CICLOALQUILO(C3-C10), ENTRE OTROS; R3 Y R4 SON CADA UNO H, ALQUILO(C1-C8), ARILO(C6-C14), CICLOALQUILO(C3-C10), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 6-(1H-PIRROLO[2,3-b]PIRIDIN-3-IL)-4-(2-(TETRAHIDRO-2H-PIRAN-4-IL)ETIL)-3,4-DIHIDROPIRAZINO[2,3-b]PIRAZIN-2(1H)-ONA; 6-(4-METIL-6-(1H-1,2,4-TRIAZOL-3-IL)PIRIDIN-3-IL)-4-((TETRAHIDRO-2H-PIRAN-4-IL)METIL)-3,4-DIHIDROPIRAZINO[2,3-b]PIRAZIN-2(1H)-ONA; 6-(5-FLUORO-2-METIL-4-(1H-1,2,4-TRIAZOL-3-IL)FENIL)-4-((TRANS-4-METOXICICLOHEXIL)METIL)-3,4-DIHIDROPIRAZINO[2,3-b]PIRAZIN-2(1H)-ONA; ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LAS CINASAS mTOR, ADN-PK O PI3K SIENDO UTILES EN EL TRATAMIENTO DE CANCER, PSORIASIS, ASMA, ARTRITIS REUMATOIDE, DIABETES MELLITUS TIPO II
PE2011000936A 2008-10-27 2009-10-27 INHIBIDORES DE mTOR CINASA PARA INDICADORES DE ONCOLOGIA Y ENFERMEDADES ASOCIADAS CON LA TRAYECTORIA mTOR/PI3K/AKT PE20110575A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US10862708P 2008-10-27 2008-10-27

Publications (1)

Publication Number Publication Date
PE20110575A1 true PE20110575A1 (es) 2011-08-11

Family

ID=41490345

Family Applications (3)

Application Number Title Priority Date Filing Date
PE2012002515A PE20130457A1 (es) 2008-10-27 2009-10-27 INHIBIDORES DE mTOR CINASA PARA INDICADORES DE ONCOLOGIA Y ENFERMEDADES ASOCIADAS CON LA TRAYECTORIA mTOR/PI3K/AKT
PE2011000936A PE20110575A1 (es) 2008-10-27 2009-10-27 INHIBIDORES DE mTOR CINASA PARA INDICADORES DE ONCOLOGIA Y ENFERMEDADES ASOCIADAS CON LA TRAYECTORIA mTOR/PI3K/AKT
PE2014000555A PE20141197A1 (es) 2008-10-27 2009-10-27 INHIBIDORES DE mTOR CINASA PARA INDICADORES DE ONCOLOGIA Y ENFERMEDADES ASOCIADAS CON LA TRAYECTORIA mTOR/PI3K/AKT

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PE2012002515A PE20130457A1 (es) 2008-10-27 2009-10-27 INHIBIDORES DE mTOR CINASA PARA INDICADORES DE ONCOLOGIA Y ENFERMEDADES ASOCIADAS CON LA TRAYECTORIA mTOR/PI3K/AKT

Family Applications After (1)

Application Number Title Priority Date Filing Date
PE2014000555A PE20141197A1 (es) 2008-10-27 2009-10-27 INHIBIDORES DE mTOR CINASA PARA INDICADORES DE ONCOLOGIA Y ENFERMEDADES ASOCIADAS CON LA TRAYECTORIA mTOR/PI3K/AKT

Country Status (35)

Country Link
US (10) US8110578B2 (es)
EP (5) EP2740733B1 (es)
JP (3) JP5689420B2 (es)
KR (2) KR101815604B1 (es)
CN (3) CN102245611B (es)
AR (2) AR073995A1 (es)
AU (1) AU2009320137C1 (es)
BR (1) BRPI0920254A2 (es)
CA (1) CA2740975C (es)
CO (1) CO6501147A2 (es)
CR (1) CR20110223A (es)
CY (2) CY1117272T1 (es)
DK (2) DK2740732T3 (es)
EC (1) ECSP11011084A (es)
ES (4) ES2794012T3 (es)
HK (3) HK1154858A1 (es)
HR (2) HRP20160084T1 (es)
HU (1) HUE026834T2 (es)
IL (1) IL212440A (es)
LT (1) LT2740732T (es)
MX (2) MX2011004401A (es)
MY (1) MY159235A (es)
NI (1) NI201100080A (es)
NZ (4) NZ592278A (es)
PE (3) PE20130457A1 (es)
PL (2) PL2740733T3 (es)
PT (1) PT2740732T (es)
RU (2) RU2692796C2 (es)
SG (3) SG2014006852A (es)
SI (2) SI2740732T1 (es)
SM (1) SMT201600089B (es)
TW (3) TWI605047B (es)
UA (1) UA108601C2 (es)
WO (1) WO2010062571A1 (es)
ZA (1) ZA201102813B (es)

Families Citing this family (115)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
HUE035029T2 (en) 2008-05-21 2018-03-28 Ariad Pharma Inc Kinase inhibitor phosphorus derivatives
US8110578B2 (en) * 2008-10-27 2012-02-07 Signal Pharmaceuticals, Llc Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway
WO2010056311A1 (en) 2008-11-12 2010-05-20 Ariad Pharmaceuticals, Inc. Pyrazinopyrazines and derivatives as kinase inhibitors
DE102009043260A1 (de) 2009-09-28 2011-04-28 Merck Patent Gmbh Pyridinyl-imidazolonderivate
WO2011053518A1 (en) * 2009-10-26 2011-05-05 Signal Pharmaceuticals, Llc Methods of synthesis and purification of heteroaryl compounds
EP2531194B1 (en) * 2010-02-03 2018-04-18 Signal Pharmaceuticals, LLC Identification of lkb1 mutation as a predictive biomarker for sensitivity to tor kinase inhibitors
US20110275699A1 (en) * 2010-03-16 2011-11-10 University Of California Treatment For Obesity And Diabetes
US20120028972A1 (en) * 2010-07-30 2012-02-02 Lilly Wong Biomarker assays for detecting or measuring inhibition of tor kinase activity
KR102024948B1 (ko) * 2011-02-18 2019-11-04 노파르티스 파르마 아게 mTOR/JAK 저해제 병용 요법
WO2012122405A2 (en) * 2011-03-08 2012-09-13 The Trustees Of Columbia University In The City Of New York Screening assays using stem cells and stem cell-derived neurons from mouse models of alzheimer's disease
EA201391626A1 (ru) 2011-05-04 2014-03-31 Ариад Фармасьютикалз, Инк. Соединения для ингибирования клеточной пролиферации в egfr-стимулированных типах рака
WO2013019927A1 (en) * 2011-08-03 2013-02-07 Signal Pharmaceuticals, Llc Identification of gene expression profile as a predictive biomarker for lkb1 status
EP3466423B1 (en) 2011-10-19 2021-07-28 Signal Pharmaceuticals, LLC Treatment of cancer with tor kinase inhibitors
AU2015200318B2 (en) * 2011-10-19 2016-10-20 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
AU2015201807B2 (en) * 2011-12-02 2016-12-08 Signal Pharmaceuticals, Llc Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methocyclohexyl)-3,4-dihydropyrazino[2,3-b] pyrazin-2(1H)-one, a solid form thereof and methods of their use
SG10201604558SA (en) * 2011-12-02 2016-07-28 Signal Pharm Llc Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4 methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use
US10272068B2 (en) 2012-01-17 2019-04-30 Tyme, Inc. Pharmaceutical compositions and methods
US10646552B2 (en) 2012-01-17 2020-05-12 Tyme, Inc. Pharmaceutical compositions and methods
US8481498B1 (en) 2012-01-17 2013-07-09 Steven Hoffman Pharmaceutical compositions and methods
US20130183263A1 (en) 2012-01-17 2013-07-18 Steven Hoffman Pharmaceutical compositions and methods
CN104220057B (zh) * 2012-01-17 2017-11-03 迪美公司 药物组合物和方法
FR2986230B1 (fr) * 2012-01-30 2014-03-07 Univ Paris Diderot Paris 7 Nouveaux composes et compositions utilises comme anticancereux
MX358303B (es) 2012-02-24 2018-08-14 Signal Pharm Llc Uso de 7-(6-(2-hidroxipropan-2il) piridin-3-il)-1-((1r,4r)4-metoxi ciclohexil)-3, 4-dihidropirazin-[2,3-b] pirazin-2(1h)-ona o una sal, estereoisómero o tautómero aceptable farmaceuticamente del mismo, en combinación con una cantidad efectiva de erlotinib o azacitidina para preparar un composición farmacéutica en el tratamiento de cáncer de pulmón de cédula no pequeña, avanzado.
EP2825171B1 (en) * 2012-03-15 2018-03-14 Signal Pharmaceuticals, LLC Treatment of cancer with tor kinase inhibitors
US20130245029A1 (en) * 2012-03-15 2013-09-19 Signal Pharmaceuticals, Llc Treatment of cancer with tor kinase inhibitors
CN104271139A (zh) 2012-03-15 2015-01-07 西格诺药品有限公司 用tor激酶抑制剂治疗癌症
AU2013203153B2 (en) * 2012-03-15 2015-09-03 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
AU2015213400B2 (en) * 2012-03-15 2017-07-27 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
AU2015201138B2 (en) * 2012-03-15 2016-06-23 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
US20150166591A1 (en) 2012-05-05 2015-06-18 Ariad Pharmaceuticals, Inc. Methods and compositions for raf kinase mediated diseases
PT3176170T (pt) 2012-06-13 2019-02-05 Incyte Holdings Corp Compostos tricíclicos substituídos como inibidores de fgfr
AU2015213397B2 (en) * 2012-10-18 2017-07-27 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
EA039396B1 (ru) * 2012-10-18 2022-01-24 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Лечение рака молочной железы с тройным негативным фенотипом ингибиторами tor-киназы
AU2013202768B2 (en) * 2012-10-18 2015-11-05 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
AU2013203714B2 (en) * 2012-10-18 2015-12-03 Signal Pharmaceuticals, Llc Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity
EP2945636B1 (en) 2013-01-16 2017-06-28 Signal Pharmaceuticals, LLC Substituted pyrrolopyrimidine compounds, compositions thereof, and methods of treatment therewith
EP2948134B1 (en) 2013-01-24 2020-03-04 Palvella Therapeutics, Inc. Compositions for transdermal delivery of mtor inhibitors
WO2014134240A1 (en) 2013-02-28 2014-09-04 Signal Pharmaceuticals, Llc Treatment of cancer with tor kinase inhibitors
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
TW201526894A (zh) * 2013-04-17 2015-07-16 Signal Pharm Llc 藉二氫吡并吡治療癌症
KR102271344B1 (ko) 2013-04-17 2021-07-01 시그날 파마소티칼 엘엘씨 디하이드로피라지노-피라진을 사용한 암의 치료
KR102240356B1 (ko) * 2013-04-17 2021-04-14 시그날 파마소티칼 엘엘씨 Tor 키나제 억제제와 5-치환된 퀴나졸리논 화합물을 포함하는 암 치료용 조합 요법
AU2014254053B2 (en) 2013-04-17 2019-06-06 Signal Pharmaceuticals, Llc Treatment of cancer with Dihydropyrazino-Pyrazines
NZ730189A (en) * 2013-04-17 2018-09-28 Signal Pharm Llc Pharmaceutical formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one
JP6389241B2 (ja) 2013-04-17 2018-09-12 シグナル ファーマシューティカルズ,エルエルシー 癌を治療するためのTORキナーゼ阻害剤及びIMiD化合物を含む組合せ療法
JP6382948B2 (ja) * 2013-04-17 2018-08-29 シグナル ファーマシューティカルズ,エルエルシー 癌を治療するためのtorキナーゼ阻害剤及びシチジン類似体を含む組合せ療法
KR102221005B1 (ko) * 2013-04-17 2021-02-26 시그날 파마소티칼 엘엘씨 전립선암 치료를 위한 디하이드로피라지노-피라진 화합물 및 안드로겐 수용체 길항제를 포함하는 조합 요법
BR112015026021A2 (pt) 2013-04-17 2017-07-25 Signal Pharm Llc terapia de combinação compreendendo um inibidor de tor quinase e n-(3-(5-flúor-2-(4-(2-met-oxietoxi)fenilamino)pirimidin-4-ilamino)fenil)acrilamida para o tratamento de câncer
SG10201708520YA (en) 2013-04-19 2017-12-28 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2014193912A1 (en) * 2013-05-29 2014-12-04 Signal Pharmaceuticals, Llc Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use
EP3052093A1 (en) 2013-10-04 2016-08-10 Signal Pharmaceuticals, LLC A tor kinase inhibitor in the prevention or treatment of cancer characterized by gene mutations
US9326962B2 (en) 2013-10-22 2016-05-03 Steven Hoffman Compositions and methods for treating intestinal hyperpermeability
US9585841B2 (en) 2013-10-22 2017-03-07 Tyme, Inc. Tyrosine derivatives and compositions comprising them
US10813901B2 (en) 2013-10-22 2020-10-27 Yamo Pharmaceuticals Llc Compositions and methods for treating autism
US9763903B2 (en) 2013-10-22 2017-09-19 Steven Hoffman Compositions and methods for treating intestinal hyperpermeability
US10751313B2 (en) 2013-10-22 2020-08-25 Yamo Pharmaceuticals Llc Compositions and methods for treating autism
WO2015069217A1 (en) * 2013-11-05 2015-05-14 Baylor College Of Medicine Src kinase inhibition as treatment for lympangioleiomyomatosis and tuberous sclerosis
WO2015160868A1 (en) 2014-04-16 2015-10-22 Signal Pharmaceuticals, Llc Methods for treating cancer using tor kinase inhibitor combination therapy
ES2881863T3 (es) 2014-04-16 2021-11-30 Signal Pharm Llc Métodos para tratar cáncer usando terapia de combinación de inhibidor de quinasa TOR con un inhibidor de histona desacetilasa
NZ714742A (en) 2014-04-16 2017-04-28 Signal Pharm Llc Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use
US9512129B2 (en) 2014-04-16 2016-12-06 Signal Pharmaceuticals, Llc Solid forms comprising 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one and a coformer
US9718824B2 (en) 2014-04-16 2017-08-01 Signal Pharmaceuticals, Llc Solid forms comprising 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, and a coformer, compositions and methods of use thereof
KR20170024120A (ko) 2014-07-14 2017-03-06 시그날 파마소티칼 엘엘씨 치환된 피롤로피리미딘 화합물을 사용한 암의 치료방법, 이의 조성물
NZ629796A (en) 2014-07-14 2015-12-24 Signal Pharm Llc Amorphous form of 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d]oxazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use
EP3193902A4 (en) 2014-09-11 2018-03-28 The Regents of The University of California mTORC1 INHIBITORS
US9987241B2 (en) 2014-09-25 2018-06-05 The Board Of Regents Of The University Of Oklahoma Enzyme conjugate and prodrug cancer therapy
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
TWI712601B (zh) 2015-02-20 2020-12-11 美商英塞特公司 作為fgfr抑制劑之雙環雜環
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
US10722484B2 (en) 2016-03-09 2020-07-28 K-Gen, Inc. Methods of cancer treatment
US20180078539A1 (en) 2016-03-23 2018-03-22 Louis Habash T-cell regulation in t-cell mediated diseases by reducing pathogenic function of th17 in a human subject through treatment with a nitroxide
US10231959B2 (en) 2016-03-23 2019-03-19 Louis Habash Increasing expression level of apoptosis-related genes by treating a human subject with a nitroxide
JP2019509352A (ja) * 2016-03-23 2019-04-04 ルイス ハバシュ, ヒトの被験物質をニトロキシドで処理することによってapoptosis関連遺伝子の発現レベルを増加させる
US10159665B2 (en) 2016-03-23 2018-12-25 Louis Habash Preventing amyloid plaque formation by treating a human subject with a nitroxide
US10818331B2 (en) 2016-09-27 2020-10-27 Spin Memory, Inc. Multi-chip module for MRAM devices with levels of dynamic redundancy registers
EP3565520A4 (en) 2017-01-06 2020-08-19 Palvella Therapeutics, Inc. Anhydrous compositions of MTOR inhibitors and method of use
WO2018183868A1 (en) * 2017-03-31 2018-10-04 Bioventures, Llc Inhibitors of dna pk and uses thereof
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
SG11201912403SA (en) 2017-06-22 2020-01-30 Celgene Corp Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection
WO2020032951A1 (en) 2018-08-09 2020-02-13 The Board Of Regents Of The University Of Oklahoma Antimalarial enzyme conjugates, kits containing same, and methods of producing and using same
KR102133794B1 (ko) * 2017-08-24 2020-07-15 주식회사 셀투인 세포 소기관 내 글루타치온 측정용 실시간 형광 이미징 센서 및 이의 제조 방법
US10656994B2 (en) 2017-10-24 2020-05-19 Spin Memory, Inc. Over-voltage write operation of tunnel magnet-resistance (“TMR”) memory device and correcting failure bits therefrom by using on-the-fly bit failure detection and bit redundancy remapping techniques
AU2018360801A1 (en) 2017-11-01 2020-05-14 Celgene Corporation Process for producing a T cell composition
KR102083916B1 (ko) 2017-11-23 2020-03-03 서울대학교산학협력단 대장암 진단을 위한 tcf7 돌연변이의 용도 및 게다토리십 약물내성을 갖는 대장암 치료용 조성물
US11434242B2 (en) * 2017-12-04 2022-09-06 Bial—Portela & Ca, S.A. Dopamine-b-hydroxylase inhibitors
US10886330B2 (en) 2017-12-29 2021-01-05 Spin Memory, Inc. Memory device having overlapping magnetic tunnel junctions in compliance with a reference pitch
US10840439B2 (en) 2017-12-29 2020-11-17 Spin Memory, Inc. Magnetic tunnel junction (MTJ) fabrication methods and systems
WO2019157516A1 (en) 2018-02-12 2019-08-15 resTORbio, Inc. Combination therapies
CR20200578A (es) 2018-05-01 2021-02-22 Revolution Medicines Inc Análogos de rapamicina a c40, c28 y c32 como inhibidores de mtor
CN112368289B (zh) 2018-05-01 2024-02-20 锐新医药公司 作为mtor抑制剂的c26-连接的雷帕霉素类似物
MA52493A (fr) 2018-05-04 2021-03-10 Incyte Corp Sels d'un inhibiteur de fgfr
US11466004B2 (en) 2018-05-04 2022-10-11 Incyte Corporation Solid forms of an FGFR inhibitor and processes for preparing the same
US10411185B1 (en) 2018-05-30 2019-09-10 Spin Memory, Inc. Process for creating a high density magnetic tunnel junction array test platform
WO2019241789A1 (en) 2018-06-15 2019-12-19 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
JP2021530463A (ja) 2018-07-02 2021-11-11 パルヴェラ セラピューティクス、インク. mTOR阻害剤の無水組成物および使用方法
US10650875B2 (en) 2018-08-21 2020-05-12 Spin Memory, Inc. System for a wide temperature range nonvolatile memory
US10971680B2 (en) 2018-10-01 2021-04-06 Spin Memory, Inc. Multi terminal device stack formation methods
US11621293B2 (en) 2018-10-01 2023-04-04 Integrated Silicon Solution, (Cayman) Inc. Multi terminal device stack systems and methods
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
UY38806A (es) 2019-08-01 2021-02-26 Novartis Ag Compuestos inhibidores tricíclicos de kars dependientes de akr1c3, composiciones y sus usos
CA3157361A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
JP2023505258A (ja) 2019-12-04 2023-02-08 インサイト・コーポレイション Fgfr阻害剤としての三環式複素環
BR112022010664A2 (pt) 2019-12-04 2022-08-16 Incyte Corp Derivados de um inibidor de fgfr
TW202134234A (zh) 2019-12-05 2021-09-16 美商奈維特製藥公司 雷帕黴素類似物及其用途
WO2021219091A2 (zh) * 2020-04-29 2021-11-04 北京泰德制药股份有限公司 喹喔啉酮衍生物作为kras g12c突变蛋白的不可逆抑制剂
US20230321108A1 (en) * 2020-07-22 2023-10-12 Nanjing Chia Tai Tianqing Pharmaceutical Co., Ltd. Unit dosage composition of akt inhibitor
WO2022166866A1 (zh) * 2021-02-08 2022-08-11 南京明德新药研发有限公司 二氢吡嗪并吡嗪类大环化合物
JP2024506381A (ja) 2021-02-16 2024-02-13 ヴァクシテック ノース アメリカ, インコーポレイテッド 両親媒性ペプチドに基づく自己集合ナノ粒子
EP4352059A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2022266251A1 (en) * 2021-06-16 2022-12-22 The Board Of Trustees Of The Leland Stanford Junior University Compositions for treatment of psoriasis
WO2023170107A1 (en) 2022-03-07 2023-09-14 Centre Hospitalier Universitaire Vaudois (Chuv) Pi3k/akt/mtor inhibitor for improving the cellular uptake of a radiopharmaceutical
WO2024092030A1 (en) 2022-10-25 2024-05-02 Vaccitech North America, Inc. Self-assembling nanoparticles

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE262026C (es)
US3507866A (en) * 1967-08-08 1970-04-21 Merck & Co Inc 1h - imidazo(4,5-b)pyrazin - 2 - one and processes for their preparation
US3567725A (en) * 1968-11-20 1971-03-02 Merck & Co Inc Process for preparation of 1h-imidazo-(4,5-b)pyrazin-2-ones
US4294837A (en) * 1980-03-28 1981-10-13 Sterling Drug Inc. 1,3-Dihydro-6-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones and -imidazo[4,5-b]pyridine-2-thiones and their cardiotonic use
US4294836A (en) * 1980-03-24 1981-10-13 Sterling Drug Inc. 1,3-Dihydro-6-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones and -imidazo[4,5-b]-pyridine-2-thiones and their cardiotonic use
US4317909A (en) * 1980-03-24 1982-03-02 Sterling Drug Inc. Preparation of 1,3-dihydro-5-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones
US4309537A (en) * 1980-03-28 1982-01-05 Sterling Drug Inc. Production of imidazo[4,5-b]pyridin-2-ones or thiones
GB8709448D0 (en) * 1987-04-21 1987-05-28 Pfizer Ltd Heterobicyclic quinoline derivatives
JPS63275582A (ja) 1987-05-02 1988-11-14 Naade Kenkyusho:Kk 2−アミノイミダゾ〔4,5−b〕ピリジン誘導体の製造方法
DD262026A1 (de) 1987-07-10 1988-11-16 Akad Wissenschaften Ddr Verfahren zur herstellung von 4-substituierten 6-(pyrid-4-yl)-2,4-dihydro-1h-imidazo[4,5-b]pyrid-2-onen
FR2643903A1 (fr) 1989-03-03 1990-09-07 Union Pharma Scient Appl Nouveaux derives de benzimidazole, leurs procedes de preparation, intermediaires de synthese, compositions pharmaceutiques les contenant, utiles notamment pour le traitement des maladies cardiovasculaires, et des ulceres duodenaux
US4963561A (en) * 1990-02-28 1990-10-16 Sterling Drug Inc. Imidazopyridines, their preparation and use
TW274550B (es) * 1992-09-26 1996-04-21 Hoechst Ag
WO1995003009A1 (en) 1993-07-22 1995-02-02 Oculex Pharmaceuticals, Inc. Method of treatment of macular degeneration
US5770589A (en) 1993-07-27 1998-06-23 The University Of Sydney Treatment of macular degeneration
DK0790997T3 (da) * 1994-11-14 2000-08-21 Warner Lambert Co 6-Aryl-pyrido[2,3-d]pyrimidiner og napthyridiner til hæmning af protein-tyrosin-kinase-fremkaldt celleproliferation
IT1274549B (it) 1995-05-23 1997-07-17 Indena Spa Uso di flavanolignani per la preparazione di medicamenti ad attivita' antiproliferativa nei tumori dell'utero,dell'ovaio e del seno
DE19601627A1 (de) * 1996-01-18 1997-07-24 Bayer Ag Heteroatomhaltige Cyclopentanopyridyl-Oxazolidinone
US5800819A (en) 1996-01-25 1998-09-01 National Institute For Pharmaceutical Research And Development Federal Ministry Of Science And Technology Piper guineense, pterocarpus osun, eugenia caryophyllata, and sorghum bicolor extracts for treating sickle cell disease
US6281230B1 (en) 1996-07-24 2001-08-28 Celgene Corporation Isoindolines, method of use, and pharmaceutical compositions
US5635517B1 (en) 1996-07-24 1999-06-29 Celgene Corp Method of reducing TNFalpha levels with amino substituted 2-(2,6-dioxopiperidin-3-YL)-1-oxo-and 1,3-dioxoisoindolines
DK1017384T3 (da) * 1997-09-26 2005-01-31 Zentaris Gmbh Azabenzimidazolbaserede forbindelser til modulation af serin/threoninproteinkinasefunktion
ZA9810490B (en) 1997-12-03 1999-05-20 Dainippon Pharmaceutical Co 2-Aryl-8-oxodihydropurine derivative process for the preparation thereof pharmaceutical composition containing the same and intermediate therefor
US6015803A (en) 1998-05-04 2000-01-18 Wirostko; Emil Antibiotic treatment of age-related macular degeneration
US6225348B1 (en) 1998-08-20 2001-05-01 Alfred W. Paulsen Method of treating macular degeneration with a prostaglandin derivative
US6001368A (en) 1998-09-03 1999-12-14 Protein Technologies International, Inc. Method for inhibiting or reducing the risk of macular degeneration
JP2003146987A (ja) 1999-05-31 2003-05-21 Dainippon Pharmaceut Co Ltd 2−アリールプリン−9−アセトアミド誘導体
JP3814125B2 (ja) 1999-06-02 2006-08-23 大日本住友製薬株式会社 2−アリール−8−オキソジヒドロプリン誘導体からなる医薬
EP1257537B1 (en) * 2000-01-24 2007-05-30 AstraZeneca AB Therapeutic morpholino-substituted compounds
JP2002167387A (ja) 2000-11-29 2002-06-11 Dainippon Pharmaceut Co Ltd 2−(7,8−ジヒドロ−8−オキソ−9h−プリン−9−イル)酢酸誘導体
ES2249384T3 (es) * 2000-12-12 2006-04-01 Neurogen Corporation Espiro(isobenzofuran-1,4'-piperadin)-3-onas y 3h-espirobenzofuran-1,4-piperidinas.
US7451335B2 (en) 2001-04-24 2008-11-11 Broadcom Corporation Selectively disabling a portion of ASF operations when ASF device is powered by auxiliary power
UY27427A1 (es) 2001-09-04 2003-03-31 Boehringer Ingelheim Pharma Nuevas dihidro-pteridinonas, procedimientos para su preparación y su utilización como medicamentos
JP2005506350A (ja) * 2001-10-18 2005-03-03 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド サイトカイン阻害薬としての1,4−二置換ベンゾ−縮合尿素化合物
US7968569B2 (en) 2002-05-17 2011-06-28 Celgene Corporation Methods for treatment of multiple myeloma using 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione
US20040204420A1 (en) 2002-08-05 2004-10-14 Rana Tariq M. Compounds for modulating RNA interference
US7189740B2 (en) 2002-10-15 2007-03-13 Celgene Corporation Methods of using 3-(4-amino-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione for the treatment and management of myelodysplastic syndromes
US20040091455A1 (en) 2002-10-31 2004-05-13 Zeldis Jerome B. Methods of using and compositions comprising immunomodulatory compounds for treatment and management of macular degeneration
US7563810B2 (en) 2002-11-06 2009-07-21 Celgene Corporation Methods of using 3-(4-amino-1-oxo-1,3-dihydroisoindol-2-yl)-piperidine-2,6-dione for the treatment and management of myeloproliferative diseases
BRPI0406809A (pt) 2003-01-17 2005-12-27 Warner Lambert Co Heterociclos substituìdos de 2-aminopiridina como inibidores da proliferação celular
PT1599478E (pt) 2003-02-26 2007-05-31 Boehringer Ingelheim Pharma Di-hidropteridinonas, proceso para a sua preparação e a sua utilização como medicamento
GB2400101A (en) 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
US20050100529A1 (en) 2003-11-06 2005-05-12 Zeldis Jerome B. Methods of using and compositions comprising immunomodulatory compounds for the treatment and management of asbestos-related diseases and disorders
CN102786482A (zh) * 2003-11-21 2012-11-21 阿雷生物药品公司 Akt蛋白激酶抑制剂
ZA200607799B (en) 2004-03-22 2008-06-25 Celgene Corp Methods of using and compositions comprising immuno-modulatory compounds for the treatment and management of skin diseases or disorders
KR20060130781A (ko) * 2004-04-08 2006-12-19 토포타겟 에이/에스 다이페닐 인돌-2-온 화합물 및 암 치료에 있어서의 그의용도
WO2005105088A2 (en) 2004-04-23 2005-11-10 Celgene Corporation Methods of using and compositions comprising immunomodulatory compounds for the treatment and management of pulmonary hypertension
WO2005120511A1 (en) 2004-06-04 2005-12-22 Icos Corporation Methods for treating mast cell disorders
DE102004029784A1 (de) * 2004-06-21 2006-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 2-Benzylaminodihydropteridinone, Verfahren zur deren Herstellung und deren Verwendung als Arzneimittel
WO2006001266A1 (ja) 2004-06-23 2006-01-05 Banyu Pharmaceutical Co., Ltd. 2-アリールプリン誘導体の製造方法
WO2006020755A2 (en) 2004-08-10 2006-02-23 Beth Israel Deaconess Medical Center, Inc. Methods for identifying inhibitors of the mtor pathway as diabetes therapeutics
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
US7608622B2 (en) * 2004-09-24 2009-10-27 Janssen Pharmaceutica Nv Imidazo[4,5-b]pyrazinone inhibitors of protein kinases
MX2007005159A (es) 2004-10-29 2007-06-26 Tibotec Pharm Ltd Derivados de pirimidina biciclicos inhibidores del vih.
BRPI0517481A (pt) 2004-11-12 2008-10-14 Celgene Corp método para tratar, controlar ou evitar uma doença ou distúrbio parasìtico protozoário, e, composição farmacêutica
WO2006058008A1 (en) 2004-11-23 2006-06-01 Celgene Corporation Methods and compositions using immunomodulatory compounds for treatment and management of central nervous system injury
CA2588990A1 (en) 2004-12-01 2006-06-08 Celgene Corporation Compositions comprising immunomodulatory compounds and the use thereof for the treatment of immunodeficiency disorders
AU2005316668B2 (en) 2004-12-13 2012-09-06 Millennium Pharmaceuticals, Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors
WO2006091737A1 (en) 2005-02-24 2006-08-31 Kemia, Inc. Modulators of gsk-3 activity
CA2599212A1 (en) * 2005-02-25 2006-08-31 Kudos Pharmaceuticals Limited 2,4-diamino-pyridopyrimidine derivatives and their use as mtor inhibitors
RU2007140903A (ru) 2005-04-05 2009-05-20 Фармакопия, Инк. (Us) Производные пурина и имидазопиридина для иммуносупрессии
SI1951724T1 (sl) * 2005-11-17 2011-09-30 Osi Pharmaceuticals Llc Kondenzirani biciklični mTOR inhibitorji
ES2558517T3 (es) 2006-08-02 2016-02-04 Cytokinetics, Inc. Ciertas entidades químicas, composiciones y métodos que comprenden imidazopirimidinas
ES2381215T3 (es) 2006-10-19 2012-05-24 Signal Pharmaceuticals Llc Compuestos heteroarilo, sus composiciones y métodos de tratamiento con ellos
CN101679266B (zh) 2007-03-01 2015-05-06 诺华股份有限公司 Pim激酶抑制剂及其应用方法
US8110578B2 (en) 2008-10-27 2012-02-07 Signal Pharmaceuticals, Llc Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway
WO2011053518A1 (en) * 2009-10-26 2011-05-05 Signal Pharmaceuticals, Llc Methods of synthesis and purification of heteroaryl compounds

Also Published As

Publication number Publication date
EP3103803B1 (en) 2020-03-11
US20120071658A1 (en) 2012-03-22
EP2740733B1 (en) 2015-12-30
SI2740732T1 (sl) 2017-09-29
US20200262840A1 (en) 2020-08-20
CN102245611B (zh) 2016-10-26
HK1199020A1 (zh) 2015-06-19
EP2740732B1 (en) 2017-05-17
HK1154858A1 (zh) 2012-05-04
US20100216781A1 (en) 2010-08-26
AU2009320137A1 (en) 2010-06-03
AU2009320137C1 (en) 2014-11-06
US20230119470A1 (en) 2023-04-20
US9771371B2 (en) 2017-09-26
TW201531475A (zh) 2015-08-16
CN104744475A (zh) 2015-07-01
US9193692B2 (en) 2015-11-24
CA2740975A1 (en) 2010-06-03
RU2015105249A3 (es) 2018-08-16
ECSP11011084A (es) 2011-07-29
PE20141197A1 (es) 2014-09-22
US20120059164A1 (en) 2012-03-08
US8110578B2 (en) 2012-02-07
AU2009320137B2 (en) 2014-06-26
JP2015091839A (ja) 2015-05-14
RU2546658C2 (ru) 2015-04-10
CN102245611A (zh) 2011-11-16
US10683298B2 (en) 2020-06-16
NZ708183A (en) 2016-08-26
EP3660020A1 (en) 2020-06-03
HRP20171069T1 (hr) 2017-10-06
KR101896855B1 (ko) 2018-09-07
AR073995A1 (es) 2010-12-15
US20130289271A1 (en) 2013-10-31
US20150051397A1 (en) 2015-02-19
PL2740733T3 (pl) 2016-06-30
ES2794012T3 (es) 2020-11-17
NI201100080A (es) 2011-10-21
SG10201402267VA (en) 2014-07-30
PT2740732T (pt) 2017-07-18
US20160024101A1 (en) 2016-01-28
HK1200442A1 (en) 2015-08-07
ZA201102813B (en) 2012-07-25
TWI527817B (zh) 2016-04-01
JP5689420B2 (ja) 2015-03-25
TW201531474A (zh) 2015-08-16
TWI605047B (zh) 2017-11-11
HUE026834T2 (en) 2016-07-28
CR20110223A (es) 2011-08-12
NZ592278A (en) 2013-01-25
CN104725384B (zh) 2019-09-06
KR101815604B1 (ko) 2018-01-05
KR20110079761A (ko) 2011-07-07
US11292796B2 (en) 2022-04-05
CY1119075T1 (el) 2018-01-10
PL2740732T3 (pl) 2017-09-29
US8907087B2 (en) 2014-12-09
SMT201600089B (it) 2016-04-29
DK2740732T3 (en) 2017-08-07
RU2015105249A (ru) 2015-06-27
TW201026702A (en) 2010-07-16
US20170342080A1 (en) 2017-11-30
US10167290B2 (en) 2019-01-01
ES2633194T3 (es) 2017-09-19
EP2740733A1 (en) 2014-06-11
KR20170081743A (ko) 2017-07-12
MX2011004401A (es) 2011-06-16
NZ603831A (en) 2014-05-30
RU2692796C2 (ru) 2019-06-27
MY159235A (en) 2016-12-30
LT2740732T (lt) 2017-10-25
UA108601C2 (uk) 2015-05-25
IL212440A (en) 2017-03-30
JP2017014256A (ja) 2017-01-19
EP2740732A1 (en) 2014-06-11
MX361916B (es) 2018-12-19
EP2358718B1 (en) 2017-01-18
US8507492B2 (en) 2013-08-13
SI2740733T1 (sl) 2016-03-31
RU2011121353A (ru) 2012-12-10
AR110388A2 (es) 2019-03-27
DK2740733T3 (en) 2016-03-29
CN104725384A (zh) 2015-06-24
SG10201402273RA (en) 2014-10-30
HRP20160084T1 (hr) 2016-02-26
PE20130457A1 (es) 2013-04-17
US20190077806A1 (en) 2019-03-14
SG2014006852A (en) 2014-04-28
ES2620774T3 (es) 2017-06-29
US8492381B2 (en) 2013-07-23
EP2358718A1 (en) 2011-08-24
CO6501147A2 (es) 2012-08-15
EP3103803A1 (en) 2016-12-14
WO2010062571A1 (en) 2010-06-03
EP3660020B1 (en) 2023-07-05
CN104744475B (zh) 2018-01-12
IL212440A0 (en) 2011-06-30
CA2740975C (en) 2018-03-20
TWI535722B (zh) 2016-06-01
ES2562803T3 (es) 2016-03-08
JP6110358B2 (ja) 2017-04-05
CY1117272T1 (el) 2017-04-26
JP2012506875A (ja) 2012-03-22
BRPI0920254A2 (pt) 2020-06-23
NZ619458A (en) 2015-07-31

Similar Documents

Publication Publication Date Title
PE20110575A1 (es) INHIBIDORES DE mTOR CINASA PARA INDICADORES DE ONCOLOGIA Y ENFERMEDADES ASOCIADAS CON LA TRAYECTORIA mTOR/PI3K/AKT
PE20110545A1 (es) Compuestos de triazolopiridina como inhibidores de jak
CL2008003506A1 (es) Compuestos derivados de pirrolo[3,2-d]pirimidina, inhibidores de quinasa pi3 y quinasa mtor; metodo de preparacion; composicion farmaceutica, util para el tratamiento de enfermedades tales como aterosclerosis, artritis, psoriasis y cancer.
PE20110387A1 (es) Aminotriazolo-piridinas como inhibidores de cinasa
PE20141974A1 (es) Compuestos de heterociclilo
CO6612267A2 (es) Nuevos derivados de 1,1 dióxido- 5 fenil- 2,3,4-5tetrahidro- 1,4-benzotiazepina y composiciones farmaceúticas que los comprenden
PE20130306A1 (es) Morfolinopirimidinas y su uso en terapia
AR077977A1 (es) Compuestos y composiciones como inhibidores de cinasa de proteina
CR11757A (es) Compuestos de triazina como inhibidores mtor y quinasa pi3
PE20141167A1 (es) Piridopirazinas sustituidas como inhibidores novedosos de ptk
PE20120575A1 (es) Derivados de pirazolopirimidina como inhibidores de jak quinasas
EA201070395A1 (ru) Ингибиторы polo-подобных киназ
PE20141938A1 (es) Nuevos compuestos inhibidores de la fosfodiesterasa del tipo 10a
BRPI0911035B8 (pt) ativadores de pirrolidinona glicoquinase
PL415078A1 (pl) Podstawione aminotriazole przydatne jako inhibitory kwaśnej chitynazy ssaków
BR122013028005B8 (pt) compostos de ciclopentanos de pirimidila hidroxilados e metoxilados, composição farmacêutica, kit e forma de dosagem oral compreendendo os referidos compostos, uso das referidas composições, bem como processo de preparação dos referidos compostos
EA201100450A1 (ru) Макроциклические пирамидины в качестве ингибиторов протеинкиназы
TN2014000128A1 (en) 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh
NO20092657L (no) Bicyclic heterocyclic compounds as FGFR inhibitors
TN2011000244A1 (en) Organic compounds
BR112014005226A2 (pt) derivados de benzonitrila como inibidores de cinase
UY29414A1 (es) Derivados de pirimidina para el tratamiento de trastornos hiperproliferativos
PA8783501A1 (es) Derivados de quinaxolina como inhibidores de la actividad de cinasa de tirosina de las cinasas janus
PE20141380A1 (es) Imidazopiridazinas como inhibidores de quinasa akt
PE20080931A1 (es) Imidazopirazinas como inhibidores de proteina quinasa

Legal Events

Date Code Title Description
FC Refusal