[go: up one dir, main page]

PE20091384A1 - Compuestos tienopirimidina y pirazolopirimidina como inhibidores de quinasa mtor y quinasa p13 - Google Patents

Compuestos tienopirimidina y pirazolopirimidina como inhibidores de quinasa mtor y quinasa p13

Info

Publication number
PE20091384A1
PE20091384A1 PE2008001780A PE2008001780A PE20091384A1 PE 20091384 A1 PE20091384 A1 PE 20091384A1 PE 2008001780 A PE2008001780 A PE 2008001780A PE 2008001780 A PE2008001780 A PE 2008001780A PE 20091384 A1 PE20091384 A1 PE 20091384A1
Authority
PE
Peru
Prior art keywords
kinase
halo
oxa
pyrimidin
oct
Prior art date
Application number
PE2008001780A
Other languages
English (en)
Inventor
Arie Zask
Joshua Aaron Kaplan
Jeroen Cunera Verheijen
Kevin J Curran
David James Richard
Semiramis Ayral-Kaloustian
Original Assignee
Wyeth Corp
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 Wyeth Corp filed Critical Wyeth Corp
Publication of PE20091384A1 publication Critical patent/PE20091384A1/es

Links

Classifications

    • 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
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P17/06Antipsoriatics
    • 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
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • 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
    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

REFERIDA A COMPUESTOS DERIVADOS DE TIENOPIRIMIDINA Y PIRAZOLOPIRIMIDINA DE FORMULAS (Ia) Y (IIa), DONDE Het ES UN HETEROBICICLILO DE 5 A 10 MIEMBROS QUE CONTIENE POR LO MENOS UN ATOMO DE O Y N; Y OPCIONALMENTE HETEROATOMOS ADICIONALES DE O, S Y N; R20 ES OH, HALO, ALCOXI(C1-C2), ENTRE OTROS; R1 ES HALO, ALQUILO(C1-C6), ENTRE OTROS; R2 ES H, HALO, ACILO(C1-C8), ENTRE OTROS; R3 ES H, ALQUILO(C1-C6), ENTRE OTROS; R8 ES H, HALO, ALQUILO(C1-C6), ENTRE OTROS; Ar ES FENILO, NAFTILO, ENTRE OTROS; t ES DE 0 A 16; m ES DE 0 A 4; r ES 0 O 1. SON COMPUESTOS PREFERIDOS: 3-[4-(8-OXA-3-AZABICICLO[3.2.1]OCT-3-1L)-1-FENIL-1H-PIRAZOLO[3,4-d]PIRIMIDIN-6-IL]FENOL, 1-METIL-3-{4-[4-(8-OXA-3-AZABICILO[3.2.1]OCT-3-IL)-1-(2,2,2-TRIFLUOROETIL)-1H-PIRAZOLO[3,4-d]PIRIMIDIN-6-IL]FENIL}UREA, {4-[4-(8-OXA-3-AZABICICLO[3.2.1]OCT-3-IL)-1-(2,2,2-TRIFLUOROETIL)-1H-PIRAZOLO[2,3-d]PIRIMIDIN-6-IL]FENIL}CARBAMATO DE METILO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON INHIBIDORES DE QUINASA mTOR Y DE QUINASA PI3K, SIENDO UTILES PARA EL TRATAMIENTO DE TRASTORNOS OSEOS, CANCER DE PROSTATA, ANGIOGENIA, ENTRE OTROS
PE2008001780A 2007-10-16 2008-10-16 Compuestos tienopirimidina y pirazolopirimidina como inhibidores de quinasa mtor y quinasa p13 PE20091384A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US98033207P 2007-10-16 2007-10-16
US2759508P 2008-02-11 2008-02-11

Publications (1)

Publication Number Publication Date
PE20091384A1 true PE20091384A1 (es) 2009-09-09

Family

ID=40345078

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008001780A PE20091384A1 (es) 2007-10-16 2008-10-16 Compuestos tienopirimidina y pirazolopirimidina como inhibidores de quinasa mtor y quinasa p13

Country Status (26)

Country Link
US (1) US8129371B2 (es)
EP (1) EP2212333A1 (es)
JP (1) JP2011500702A (es)
KR (1) KR20100083170A (es)
CN (1) CN101883774A (es)
AP (1) AP2010005234A0 (es)
AR (1) AR068898A1 (es)
AU (1) AU2008312631A1 (es)
BR (1) BRPI0817681A2 (es)
CA (1) CA2702838A1 (es)
CL (1) CL2008003061A1 (es)
CO (1) CO6321257A2 (es)
CR (1) CR11373A (es)
DO (1) DOP2010000118A (es)
EA (1) EA201000484A1 (es)
EC (1) ECSP10010112A (es)
IL (1) IL205109A0 (es)
MA (1) MA31884B1 (es)
MX (1) MX2010004260A (es)
NI (1) NI201000060A (es)
PA (1) PA8799101A1 (es)
PE (1) PE20091384A1 (es)
TN (1) TN2010000171A1 (es)
TW (1) TW200922593A (es)
WO (1) WO2009052145A1 (es)
ZA (1) ZA201003430B (es)

Families Citing this family (94)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0974129B1 (en) * 1996-09-04 2006-08-16 Intertrust Technologies Corp. Trusted infrastructure support systems, methods and techniques for secure electronic commerce, electronic transactions, commerce process control and automation, distributed computing, and rights management
US7754208B2 (en) 2001-01-17 2010-07-13 Trubion Pharmaceuticals, Inc. Binding domain-immunoglobulin fusion proteins
US20030133939A1 (en) 2001-01-17 2003-07-17 Genecraft, Inc. Binding domain-immunoglobulin fusion proteins
WO2007014278A2 (en) 2005-07-25 2007-02-01 Trubion Pharmaceuticals, Inc. B-cell reduction using cd37-specific and cd20-specific binding molecules
EP2418223A3 (en) 2006-06-12 2013-01-16 Emergent Product Development Seattle, LLC Single-chain multivalent binding proteins with effector function
CL2008003798A1 (es) 2007-12-19 2009-10-09 Amgen Inc Compuestos derivados de heterobiciclos aromaticos sustituidos, inhibidores de pi3 quinasa; composicion farmaceutica; utiles en el tratamiento de cancer, melanomas, glioblastomas, entre otras enfermedades.
BRPI0911377A8 (pt) 2008-04-11 2017-12-05 Trubion Pharmaceuticals Inc Imunoterápico de cd7 e combinação com quimioterápico bifuncional deste
TW201004963A (en) * 2008-07-03 2010-02-01 Targacept Inc Derivatives of oxabispidine as neuronal nicotinic acetylcholine receptor ligands
EP2318377B1 (en) * 2008-07-31 2013-08-21 Genentech, Inc. Pyrimidine compounds, compositions and methods of use
US8450322B2 (en) 2008-09-22 2013-05-28 Array Biopharma Inc. Substituted imidazo[1,2b]pyridazine compounds as Trk kinase inhibitors
TWI378933B (en) 2008-10-14 2012-12-11 Daiichi Sankyo Co Ltd Morpholinopurine derivatives
KR102037619B1 (ko) 2008-10-22 2019-10-28 어레이 바이오파마 인크. TRK 키나아제 억제제로서 치환된 피라졸로[1,5­a] 피리미딘 화합물
PL2385832T3 (pl) 2009-01-08 2016-01-29 Curis Inc Inhibitory 3-kinazy fosfoinozytydowej z grupą wiążącą cynk
WO2010120998A1 (en) * 2009-04-17 2010-10-21 Wyeth Llc Pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses
EP2435438A1 (en) * 2009-05-27 2012-04-04 Genentech, Inc. Bicyclic pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use
EP2445346A4 (en) * 2009-06-24 2012-12-05 Genentech Inc OXOHETEROCYCLIC FUSIONED PYRIMIDINE COMPOUNDS AND COMPOSITIONS AND METHOD FOR THEIR USE
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
US20110021515A1 (en) * 2009-07-24 2011-01-27 Takeda Pharmaceutical Company Limited Dihyrofuropyrmindine compounds
KR101147550B1 (ko) 2009-10-22 2012-05-17 한국과학기술연구원 단백질 키나아제 저해활성을 가지는 2,7-치환된 티에노[3,2-d]피리미딘 화합물
BR112012011147A2 (pt) 2009-11-12 2021-09-08 F.Hoffmann-La Roche Ag Composto, composição farmacêutica e uso de um composto.
BR112012011188A2 (pt) * 2009-11-12 2021-06-29 F.Hoffmann - La Roche Ag ''composto,composição farmacêutica e uso de um composto"
WO2011078795A1 (en) * 2009-12-21 2011-06-30 S*Bio Pte Ltd Bridged morpholino substituted purines
WO2011090935A1 (en) * 2010-01-19 2011-07-28 Merck Sharp & Dohme Corp. PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS mTOR INHIBITORS
KR101942212B1 (ko) 2010-02-03 2019-01-24 시그날 파마소티칼 엘엘씨 Tor 키나제 억제자에 대한 민감성 예측 바이오마커로서 lkb1 돌연변이의 동정
CA2793778A1 (en) 2010-04-05 2011-11-13 Wyeth Llc Biomarkers for p13k-driven cancer
ES2628418T3 (es) 2010-05-20 2017-08-02 Array Biopharma, Inc. Compuestos macrocíclicos como inhibidores de la TRK cinasa
ES2685171T3 (es) 2010-06-14 2018-10-05 The Scripps Research Institute Reprogramación de células a un nuevo destino
EA201390766A1 (ru) * 2010-11-24 2013-11-29 Экселиксис, Инк. БЕНЗОКСАЗЕПИНЫ КАК ИНГИБИТОРЫ PI3K/mTOR И СПОСОБЫ ИХ ИСПОЛЬЗОВАНИЯ И ПОЛУЧЕНИЯ
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
WO2012099581A1 (en) 2011-01-19 2012-07-26 Takeda Pharmaceutical Company Limited Dihydrofuropyrimidine compounds
WO2013019927A1 (en) 2011-08-03 2013-02-07 Signal Pharmaceuticals, Llc Identification of gene expression profile as a predictive biomarker for lkb1 status
FR2985257B1 (fr) * 2011-12-28 2014-02-14 Sanofi Sa Composes dimeres agonistes des recepteurs des fgfs (fgfrs), leur procede de preparation et leur application en therapeutique
JP5985658B2 (ja) * 2012-01-31 2016-09-06 ナンジン アルゲン ファルマ カンパニー リミテッドNanjing Allgen Pharma Co. Ltd. ブルトンチロシンキナーゼ阻害薬としての環状分子
US9499561B2 (en) 2012-04-10 2016-11-22 Shanghai Yingli Pharmaceutical Co., Ltd. Fused pyrimidine compound, and preparation method, intermediate, composition, and uses thereof
CN103374021B (zh) * 2012-04-21 2015-10-28 通化济达医药有限公司 含有锌结合基的吡啶并嘧啶类HDAC和mTOR抑制剂
KR20160027217A (ko) 2012-05-23 2016-03-09 에프. 호프만-라 로슈 아게 내배엽 및 간세포를 수득하고 사용하는 조성물 및 방법
CN103450204B (zh) * 2012-05-31 2016-08-17 中国科学院上海药物研究所 吡咯[2,1-f][1,2,4]并三嗪类化合物,其制备方法及用途
NZ702747A (en) 2012-06-13 2017-03-31 Incyte Holdings Corp Substituted tricyclic compounds as fgfr inhibitors
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr 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
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
KR102240356B1 (ko) 2013-04-17 2021-04-14 시그날 파마소티칼 엘엘씨 Tor 키나제 억제제와 5-치환된 퀴나졸리논 화합물을 포함하는 암 치료용 조합 요법
US9359364B2 (en) 2013-04-17 2016-06-07 Signal Pharmaceuticals, 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
HK1221144A1 (zh) 2013-04-17 2017-05-26 西格诺药品有限公司 用於治疗癌症的包含tor激酶抑制剂和胞苷类似物的组合疗法
SG10201801965RA (en) 2013-04-17 2018-04-27 Signal Pharm Llc Treatment of cancer with dihydropyrazino-pyrazines
SG11201508302PA (en) 2013-04-17 2015-11-27 Signal Pharm Llc Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer
CA2909579A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and n-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide for treating cancer
EP2986298A1 (en) 2013-04-17 2016-02-24 Signal Pharmaceuticals, LLC Treatment of cancer with dihydropyrazino-pyrazines
LT2986610T (lt) 2013-04-19 2018-04-10 Incyte Holdings Corporation Bicikliniai heterociklai, kaip fgfr inhibitoriai
CN105407892B (zh) 2013-05-29 2019-05-07 西格诺药品有限公司 一种化合物的药物组合物、其固体形式及它们的使用方法
WO2015013579A1 (en) 2013-07-26 2015-01-29 Update Pharma Inc. Compositions to improve the therapeutic benefit of bisantrene
JP6441910B2 (ja) * 2013-09-30 2018-12-19 シャンハイ インリ ファーマシューティカル カンパニー リミティド 縮合ピリミジン化合物、中間体、その調製方法、組成物及び使用
FR3015483B1 (fr) * 2013-12-23 2016-01-01 Servier Lab Nouveaux derives de thienopyrimidine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US9763992B2 (en) 2014-02-13 2017-09-19 Father Flanagan's Boys' Home Treatment of noise induced hearing loss
EP3131551A4 (en) 2014-04-16 2017-09-20 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, COMPOSITIONS AND METHODS OF USE THEREOF
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
CR20160525A (es) 2014-05-14 2016-12-20 Pfizer Pirazolopiridinas y pirazolopirimidinas
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
CA2967951C (en) 2014-11-16 2023-11-07 Array Biopharma, Inc. Crystalline form of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
SG10201913036RA (en) 2015-02-20 2020-02-27 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US11352426B2 (en) 2015-09-21 2022-06-07 Aptevo Research And Development Llc CD3 binding polypeptides
CN108697708A (zh) 2015-10-26 2018-10-23 洛克索肿瘤学股份有限公司 Trk抑制剂抗性癌症中的点突变以及与此相关的方法
FR3046792B1 (fr) * 2016-01-19 2018-02-02 Les Laboratoires Servier Nouveaux derives d'ammonium, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
SI3439662T1 (sl) 2016-04-04 2024-11-29 Loxo Oncology, Inc. Tekoče formulacije (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirolidin -1-il)-pirazološ1,5-aćpirimidin-3-il)-3-hidroksipirolidin-1-karboksamida
DK3458456T3 (da) 2016-05-18 2020-12-14 Array Biopharma Inc Fremstilling af (s)-n-(5-((r)-2-(2,5-difluorphenyl)pyrrolidin-1-yl)pyrazol[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidin-1-carboxamid
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
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
US11666888B2 (en) 2018-02-05 2023-06-06 Bio-Rad Laboratories, Inc. Chromatography resin having an anionic exchange-hydrophobic mixed mode ligand
CN108358949A (zh) * 2018-03-01 2018-08-03 南京法恩化学有限公司 一种2,4-二氯噻吩并[3,2-d]嘧啶的制备方法
EP4309737A3 (en) 2018-05-04 2024-03-27 Incyte Corporation Solid forms of an fgfr inhibitor and processes for preparing the same
EP3788046B1 (en) 2018-05-04 2025-12-10 Incyte Corporation Salts of an fgfr inhibitor
CN110850012B (zh) * 2018-08-21 2022-07-08 四川弘远药业有限公司 一种1-(2,3-二氯苯基)哌嗪盐酸盐及其有关物质的检测方法
CN114072144A (zh) 2019-02-06 2022-02-18 维瑟拉有限公司 外用磷酸肌醇3-激酶抑制剂
CN111646995B (zh) * 2019-03-04 2023-03-21 四川大学 4-氨基-嘧啶并氮杂环-苯基脲类衍生物及其制备方法和用途
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
CN109824701B (zh) * 2019-03-26 2021-08-13 武汉工程大学 一种吡啶并噻唑类化合物及其制备方法和应用
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
EP3800188A1 (en) 2019-10-02 2021-04-07 Bayer AG Substituted pyrazolopyrimidines as irak4 inhibitors
CR20220169A (es) 2019-10-14 2022-10-27 Incyte Corp Heterociclos bicíclicos como inhibidores de fgfr
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
KR20220131900A (ko) 2019-12-04 2022-09-29 인사이트 코포레이션 Fgfr 억제제의 유도체
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US12065494B2 (en) 2021-04-12 2024-08-20 Incyte Corporation Combination therapy comprising an FGFR inhibitor and a Nectin-4 targeting agent
CN113278015B (zh) * 2021-05-31 2022-05-13 云南大学 一种荧光探针及其制备方法和应用
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
AR126101A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
WO2025201469A1 (zh) * 2024-03-28 2025-10-02 励缔(杭州)医药科技有限公司 具有mTOR抑制活性的有机化合物及其用途

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1277738B1 (en) 2000-04-27 2011-03-30 Astellas Pharma Inc. Condensed heteroaryl derivatives

Also Published As

Publication number Publication date
JP2011500702A (ja) 2011-01-06
AU2008312631A1 (en) 2009-04-23
CR11373A (es) 2010-05-03
AP2010005234A0 (en) 2010-04-30
MA31884B1 (fr) 2010-12-01
EP2212333A1 (en) 2010-08-04
KR20100083170A (ko) 2010-07-21
TW200922593A (en) 2009-06-01
PA8799101A1 (es) 2009-05-15
CN101883774A (zh) 2010-11-10
IL205109A0 (en) 2010-11-30
CO6321257A2 (es) 2011-09-20
EA201000484A1 (ru) 2010-12-30
DOP2010000118A (es) 2010-06-30
BRPI0817681A2 (pt) 2015-04-14
NI201000060A (es) 2010-10-04
ZA201003430B (en) 2011-02-23
MX2010004260A (es) 2010-04-30
US8129371B2 (en) 2012-03-06
WO2009052145A1 (en) 2009-04-23
AR068898A1 (es) 2009-12-16
CL2008003061A1 (es) 2009-01-09
US20090098086A1 (en) 2009-04-16
CA2702838A1 (en) 2009-04-23
ECSP10010112A (es) 2010-08-31
TN2010000171A1 (fr) 2011-11-11

Similar Documents

Publication Publication Date Title
PE20091384A1 (es) Compuestos tienopirimidina y pirazolopirimidina como inhibidores de quinasa mtor y quinasa p13
NZ592880A (en) Combinations of purine derivatives and proteasome inhibitors such as bortezomib for the treatment of hematological malignancy
GEP20125589B (en) TRIAZINE COMPOUNDS AS P13 KINASE AND mTOR INHIBITORS
PE20140100A1 (es) Combinaciones de compuestos inhibidores de fosfoinositida 3-quinasa y agentes quimioterapeuticos
EA201001017A1 (ru) 3h-[1,2,3]триазоло[4,5-d]пиримидиновые соединения, их применение в качестве ингибиторов киназы mtor и киназы pi3 и их синтезы
PE20081341A1 (es) Inhibidores de la actividad de la akt
PE20081888A1 (es) ANALOGOS DE PIRAZOLOPIRIMIDINA Y SU USO COMO INHIBIDORES DE CINASA mTOR Y CINASA PI3
PE20151249A1 (es) Derivados de pirazolopirimidina como inhibidores de jak quinasas
PE20091068A1 (es) Compuestos pirrolo[3,2-d]pirimidina y su uso como inhibidores de quinasa pi3 y quinasa mtor
NO20090631L (no) Morpholin pyrimidin derivativer anvendelige i behandlingen av proliferative lidelser
SV2006002110A (es) Compuestos terapeuticos ref. pc32293a
ECSP105253A (es) Derivados de 5-feniltiazol y uso como inhibidores de pi3 cinasa
CL2009000241A1 (es) Compuestos derivados de 5-(2-morfolin-4-il-7h-pirrolo[2,3-d]pirimidin-4-il)pirimidin-2-ilamina; proceso de preparacion; composicion farmaceutica; y uso de los compuestos para tratar o prevenir una enfermedad proliferativa tal como el cancer.
PE20140918A1 (es) Compuestos de benzoxepina inhibidores de la pi3k
PE20090887A1 (es) DERIVADOS DE 1H-PIRAZOL-[3,4-d]-PIRIMIDINA, 9H-PURINA Y 7H-PIRROL-[2,3-d]-PIRIMIDINA COMO INHIBIDORES DE CINASA P70 S6
PE20090210A1 (es) Compuestos derivados de pirazolo pirimidina como inhibidores de jak quinasa
ECSP066976A (es) 4-fenilamino-quinazolin-6-il-amidas
ECSP109937A (es) Pirimidil ciclopentanos como inhibidores de la proteína quinasa akt.
PE20110828A1 (es) Compuestos de pirazolopirimidina como inhibidores de jak
CL2012000708A1 (es) Compuestos derivados de imidazopiridina o imidazopirimidina, inhibidores de pde10a; proceso de preparacion de dichos compuestos; composiciones farmaceuticas; y su uso para el tratamiento terapeutico y/o preventivo de trastornos psicoticos, esquizofrenia, enfermedad de alzheimer, tumores solidos, entre otras enfermedades.
ATE457988T1 (de) A2a-adenosin-rezeptor-antagonisten
UY30051A1 (es) Derivados de pirimidina para el tratamiento del crecimiento celular anormal
MX2010002584A (es) Derivados de piperidina como agonistas de receptores muscarinicos.
ATE493418T1 (de) Dihydrofuropyrimidine als akt- proteinkinaseinhibitoren
RU2013147736A (ru) Хроменоновые соединения в качестве ингибиторов рi3-киназы для лечения рака

Legal Events

Date Code Title Description
FD Application declared void or lapsed