DOP2010000118A - Compuestos de tienopirimidina y pirazolopirimidina como inhibidores de mtor cinasa y p13 cinasa - Google Patents

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

Info

Publication number
DOP2010000118A
DOP2010000118A DO2010000118A DO2010000118A DOP2010000118A DO P2010000118 A DOP2010000118 A DO P2010000118A DO 2010000118 A DO2010000118 A DO 2010000118A DO 2010000118 A DO2010000118 A DO 2010000118A DO P2010000118 A DOP2010000118 A DO P2010000118A
Authority
DO
Dominican Republic
Prior art keywords
cinasa
compounds
tienopirimidine
pirazolopirimidine
mtor
Prior art date
Application number
DO2010000118A
Other languages
English (en)
Inventor
Semiramis Ayral-Kaloustian
Kevin Joseph
Joshua Aaron Kaplan
David James Richard
Jeroen Cunera Verheijen
Arie Zask
Original Assignee
Wyeth 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
Application filed by Wyeth Llc filed Critical Wyeth Llc
Publication of DOP2010000118A publication Critical patent/DOP2010000118A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Transplantation (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

La invencion se refiere a compuestos de tienopirimidina y pirazolopirimidina de las Formulas (Ia) y (IIa), o una de sus sales farmaceuticamente aceptables, en Las que las variables constituyentes son como se definen en el presente documento, a composiciones que comprenden los compuestos y a procedimientos de preparacion y use de los compuestos.
DO2010000118A 2007-10-16 2010-04-16 Compuestos de tienopirimidina y pirazolopirimidina como inhibidores de mtor cinasa y p13 cinasa DOP2010000118A (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
DOP2010000118A true DOP2010000118A (es) 2010-06-30

Family

ID=40345078

Family Applications (1)

Application Number Title Priority Date Filing Date
DO2010000118A DOP2010000118A (es) 2007-10-16 2010-04-16 Compuestos de tienopirimidina y pirazolopirimidina como inhibidores de mtor cinasa y p13 cinasa

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 (91)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69638122D1 (de) * 1996-09-04 2010-03-18 Intertrust Tech Corp Zuverlässige Infrastrukturhilfssysteme, Verfahren und Techniken für sicheren elektronischen Handel, elektronische Transaktionen, Handelsablaufsteuerung und Automatisierung, verteilte Verarbeitung und Rechteverwaltung
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
ES2539250T3 (es) 2005-07-25 2015-06-29 Emergent Product Development Seattle, Llc Reducción de células B mediante el uso de moléculas de unión específica a CD37 y de unión específica a CD20
SG172698A1 (en) 2006-06-12 2011-07-28 Trubion Pharmaceuticals Inc Single-chain multivalent binding proteins with effector function
EP2231661A1 (en) 2007-12-19 2010-09-29 Amgen, Inc. Inhibitors of pi3 kinase
SI2132228T1 (sl) 2008-04-11 2011-10-28 Emergent Product Dev Seatle CD37 imunoterapevtik in kombinacija z njegovim bifunkcionalnim kemoterapevtikom
TW201004963A (en) * 2008-07-03 2010-02-01 Targacept Inc Derivatives of oxabispidine as neuronal nicotinic acetylcholine receptor ligands
NZ590777A (en) * 2008-07-31 2012-11-30 Genentech Inc PYRIMIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE FOR INHIBITING mTOR
WO2010033941A1 (en) 2008-09-22 2010-03-25 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
US8513263B2 (en) 2008-10-22 2013-08-20 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyrimidine compounds as Trk kinase inhibitors
PT2385832E (pt) 2009-01-08 2015-11-02 Curis Inc Inibidores de fosfoinoritide 3-quinase com uma fração de ligação ao zinco
JP5649643B2 (ja) * 2009-04-17 2015-01-07 ワイス・エルエルシー ピリミジン化合物、ｍＴＯＲキナーゼおよびＰＩ３キナーゼ阻害剤としてのそれらの使用、ならびにそれらの合成
WO2010138589A1 (en) * 2009-05-27 2010-12-02 Genentech, Inc. Bicyclic pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use
SG176959A1 (en) * 2009-06-24 2012-01-30 Genentech Inc Oxo-heterocycle fused pyrimidine compounds, compositions and methods of 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
KR101469334B1 (ko) * 2009-11-12 2014-12-04 에프. 호프만-라 로슈 아게 Ｎ-9-치환된 퓨린 화합물, 조성물 및 사용 방법
RU2515541C2 (ru) 2009-11-12 2014-05-10 Ф.Хоффманн-Ля Рош Аг N-7 замещенные пурины и пиразолопиримидины, их композиции и способы применения
WO2011078795A1 (en) * 2009-12-21 2011-06-30 S*Bio Pte Ltd Bridged morpholino substituted purines
US9227971B2 (en) 2010-01-19 2016-01-05 Merck Sharp & Dohme Corp. Pyrazolo[1,5-a]pyrimidine compounds as mTOR inhibitors
WO2011097333A1 (en) 2010-02-03 2011-08-11 Signal Pharmaceuticals, Llc Identification of lkb1 mutation as a predictive biomarker for sensitivity to tor kinase inhibitors
WO2011125012A1 (en) 2010-04-05 2011-10-13 Wyeth Llc Biomarkers for p13k-driven cancer
CN102971322B (zh) 2010-05-20 2016-02-17 阵列生物制药公司 作为trk激酶抑制剂的大环化合物
US9376664B2 (en) 2010-06-14 2016-06-28 The Scripps Research Institute Reprogramming of cells to a new fate
CN103459384A (zh) * 2010-11-24 2013-12-18 埃克塞里艾克西斯公司 作为PI3K/mTOR抑制剂的苯并氧氮杂环庚三烯以及它们使用和制造方法
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
WO2012099581A1 (en) 2011-01-19 2012-07-26 Takeda Pharmaceutical Company Limited Dihydrofuropyrimidine compounds
CN103857804A (zh) 2011-08-03 2014-06-11 西格诺药品有限公司 作为lkb1状态的预测性生物标志物的基因表达谱的鉴定
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
WO2013113097A1 (en) * 2012-01-31 2013-08-08 Beta Pharma Canada Inc. Cyclic molecules as bruton's tyrosine kinase inhibitors
JP6077642B2 (ja) * 2012-04-10 2017-02-08 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、その調製法、中間体、組成物、及び使用
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
JP6301316B2 (ja) 2012-05-23 2018-03-28 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 内胚葉細胞および肝実質細胞の組成物ならびにそれらの細胞を入手および使用する方法
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
RS58514B1 (sr) 2012-06-13 2019-04-30 Incyte Holdings Corp Supstituisana triciklična jedinjenja kao inhibitori fgfr
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines 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
KR102242505B1 (ko) 2013-04-17 2021-04-20 시그날 파마소티칼 엘엘씨 암 치료용 tor 키나제 억제제 및 시티딘 유사체를 포함하는 병용 요법
KR20160004273A (ko) 2013-04-17 2016-01-12 시그날 파마소티칼 엘엘씨 1-에틸-7-(2-메틸-6-(1H-1,2,4-트리아졸-3-일)피리딘-3-일)-3,4-디하이드로피라지노[2,3-b]피라진-2(1H)-온에 관한 약학 제제, 제조방법, 고체 형태 및 사용 방법
JP2016516818A (ja) 2013-04-17 2016-06-09 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ｎ−（３−（５−フルオロ−２−（４−（２−メトキシエトキシ）フェニルアミノ）ピリミジン−４−イルアミノ）フェニル）アクリルアミドを含む組合せ療法
CN105377260B (zh) 2013-04-17 2020-06-12 西格诺药品有限公司 二氢吡嗪并-吡嗪类化合物在制备治疗癌症的药物中的应用
BR112015026257B1 (pt) 2013-04-17 2022-12-20 Signal Pharmaceuticals, Llc Uso de um composto dihidropirazino-pirazina e enzalutamida, composição farmacêutica que os compreende, e kit
TWI631950B (zh) 2013-04-17 2018-08-11 標誌製藥公司 藉二氫吡𠯤并吡𠯤治療癌症
AU2014253978B2 (en) 2013-04-17 2019-06-06 Signal Pharmaceuticals, Llc Combination therapy comprising a TOR kinase inhibitor and a 5-Substituted Quinazolinone Compound for treating cancer
AU2014253798C1 (en) 2013-04-19 2019-02-07 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
JP6401250B2 (ja) 2013-05-29 2018-10-10 シグナル ファーマシューティカルズ，エルエルシー ７−（６−（２−ヒドロキシプロパン−２−イル）ピリジン−３−イル）−１−（（ｔｒａｎｓ）−４−メトキシシクロヘキシル）−３，４−ジヒドロピラジノ［２，３−ｂ］ピラジン−２（１Ｈ）−オン、その固体形態の医薬組成物、及びその使用方法
KR20160099081A (ko) 2013-07-26 2016-08-19 업데이트 파마 인코포레이트 비산트렌의 치료 효과 개선용 조합 방법
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
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
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
SG11201609139WA (en) * 2014-05-14 2016-11-29 Pfizer Pyrazolopyridines and pyrazolopyrimidines
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
HRP20230271T1 (hr) 2014-11-16 2023-06-09 Array Biopharma, Inc. Kristalni oblik (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamid hidrogen sulfata
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
ES2751669T3 (es) 2015-02-20 2020-04-01 Incyte Corp Heterociclos bicíclicos como inhibidores FGFR
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
KR20180053322A (ko) 2015-09-21 2018-05-21 압테보 리서치 앤드 디벨롭먼트 엘엘씨 Cd3 결합 폴리펩타이드
RU2744852C2 (ru) 2015-10-26 2021-03-16 Локсо Онколоджи, Инк. Точечные мутации в устойчивых к ингибитору trk злокачественных опухолях и связанные с ними способы
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
SG11201808559PA (en) 2016-04-04 2018-10-30 Loxo Oncology Inc Liquid formulations of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
SI3800189T1 (sl) 2016-05-18 2023-11-30 Loxo Oncology, Inc. Priprava (s)-n-(5-((r)-2-(2,5-difluorofenil)pirolidin-1-il)pirazolo (1,5-a)pirimidin-3-il)-3-hidroksipirolidin-1-karboksamida
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
BR112019027402A2 (pt) 2017-06-22 2020-07-07 Celgene Corporation tratamento de carcinoma hepatocelular caracterizado por infecção pelo vírus da hepatite b
CN111683976B (zh) 2018-02-05 2022-11-18 生物辐射实验室股份有限公司 具有阴离子交换-疏水混合模式配体的色谱树脂
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
BR112020022373A2 (pt) 2018-05-04 2021-02-02 Incyte Corporation sais de um inibidor de fgfr
EP3788047B1 (en) 2018-05-04 2024-09-04 Incyte Corporation Solid forms of an fgfr inhibitor and processes for preparing the same
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
CA3127686A1 (en) * 2019-02-06 2020-08-13 Venthera, Inc. Topical phosphoinositide 3-kinase inhibitors
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
WO2020185532A1 (en) 2019-03-08 2020-09-17 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
EP3800188A1 (en) 2019-10-02 2021-04-07 Bayer AG Substituted pyrazolopyrimidines as irak4 inhibitors
WO2021076602A1 (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
BR112022010664A2 (pt) 2019-12-04 2022-08-16 Incyte Corp Derivados de um inibidor de fgfr
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
EP4323405A1 (en) 2021-04-12 2024-02-21 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
JP2024522189A (ja) 2021-06-09 2024-06-11 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式ヘテロ環

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001083456A1 (fr) 2000-04-27 2001-11-08 Yamanouchi Pharmaceutical Co., Ltd. Derives d'heteroaryle condenses

Also Published As

Publication number Publication date
NI201000060A (es) 2010-10-04
CO6321257A2 (es) 2011-09-20
US20090098086A1 (en) 2009-04-16
TW200922593A (en) 2009-06-01
EA201000484A1 (ru) 2010-12-30
PA8799101A1 (es) 2009-05-15
TN2010000171A1 (fr) 2011-11-11
US8129371B2 (en) 2012-03-06
AP2010005234A0 (en) 2010-04-30
BRPI0817681A2 (pt) 2015-04-14
WO2009052145A1 (en) 2009-04-23
CA2702838A1 (en) 2009-04-23
CN101883774A (zh) 2010-11-10
CR11373A (es) 2010-05-03
MX2010004260A (es) 2010-04-30
CL2008003061A1 (es) 2009-01-09
AR068898A1 (es) 2009-12-16
MA31884B1 (fr) 2010-12-01
ECSP10010112A (es) 2010-08-31
IL205109A0 (en) 2010-11-30
AU2008312631A1 (en) 2009-04-23
EP2212333A1 (en) 2010-08-04
JP2011500702A (ja) 2011-01-06
ZA201003430B (en) 2011-02-23
PE20091384A1 (es) 2009-09-09
KR20100083170A (ko) 2010-07-21

Similar Documents

Publication Publication Date Title
DOP2010000118A (es) Compuestos de tienopirimidina y pirazolopirimidina como inhibidores de mtor cinasa y p13 cinasa
CR11568A (es) Compuestos de 3h-[1,2,3]triazolo[4,5-d]pirimidina, su uso como inhibidores de mtor quinasa y pi3 quinasa y su sintesis
CR20160014A (es) Compuestos de éster boronato y composiciones farmacéuticas de los mismos
ECSP10010015A (es) Inhibidores de proteasoma
CR20160475A (es) Derivados de ácido 1-amino-2-ciclobutiletilborónico
CO6620055A2 (es) Ciertas amino-pirimidinas, composiciones de las mismas y métodos para el uso de los mismos
UY33314A (es) Derivados de acido 1-amino-2-ciclopropiletilboronico
UY31299A1 (es) Nuevos inhibidores de catepsina y su uso
CO6321282A2 (es) Derivados de piperidinilindol como inhibidores de aldosterona sintasa
PA8828201A1 (es) Compuestos triazina como inhibidores mtor y quinasa p13
CR10304A (es) Compuestos de tetrahidropiridotienopirimidina y procedimientos de uso de los mismos
UY32049A (es) Inhibidores de cmet
UY30291A1 (es) Piridin(3,4-b)pirazinonas
CU20110235A7 (es) Derivados de imidazolidin-2-ona 1,3-disustituida como inhibidores de cyp17
CO6630154A2 (es) Ciertas amino-piridazinas, composiciones de las mismas y métodos de uso de los mimos
DOP2010000013A (es) Derivados de pirimidina trisustituida para el tratamiento de enfermedades proliferativas
UY29343A1 (es) Pirazolopiridinas y sales de las mismas, una composición farmacéutica que comprende dichos compuestos, un método para prepararlos y su uso.
GT200500310A (es) Compuestos organicos
ECSP10010389A (es) Pirimidil ciclopentanos hidroxilados en forma de inhibidores de akt proteina quinasa
CR11759A (es) Nueva clase de espiro piperidinas para el tratamiento de enfermedades neurodegenerativas
ECSP10010532A (es) Tiazolil-dihidro-indazoles
UY31000A1 (es) Oxoisoxazoles como inhibidores de lipasas y fosfolipasas
CO6551751A2 (es) Derivados de sulfonamida heterociíclicos
CO6460760A2 (es) Tia-triaza-ciclopentazulenos
UY30849A1 (es) S-nitrosotioles estables, procedimeinto de sintesis y uso