[go: up one dir, main page]

CO2018013015A2 - Procesos para la preparación de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidin-1-carboxamida y sales del mismo - Google Patents

Procesos para la preparación de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidin-1-carboxamida y sales del mismo

Info

Publication number
CO2018013015A2
CO2018013015A2 CONC2018/0013015A CO2018013015A CO2018013015A2 CO 2018013015 A2 CO2018013015 A2 CO 2018013015A2 CO 2018013015 A CO2018013015 A CO 2018013015A CO 2018013015 A2 CO2018013015 A2 CO 2018013015A2
Authority
CO
Colombia
Prior art keywords
hydroxypyrrolidin
pyrazolo
difluorophenyl
pyrrolidin
pyrimidin
Prior art date
Application number
CONC2018/0013015A
Other languages
English (en)
Inventor
Charles Todd Eary
Mark Reynolds
Stacey Spencer
Derrick Juengst
Bruno Hache
Yutong Jiang
Julia Haas
Steven W Andrews
Original Assignee
Loxo Oncology Inc
Array Biopharma Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=58794189&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CO2018013015(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Loxo Oncology Inc, Array Biopharma Inc filed Critical Loxo Oncology Inc
Publication of CO2018013015A2 publication Critical patent/CO2018013015A2/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

La presente invención se refiere a un proceso para preparar un compuesto de Fórmula I Fórmula I o una sal del mismo, como se describe en la presente.
CONC2018/0013015A 2016-05-18 2018-11-30 Procesos para la preparación de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidin-1-carboxamida y sales del mismo CO2018013015A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662338359P 2016-05-18 2016-05-18
PCT/US2017/033257 WO2017201241A1 (en) 2016-05-18 2017-05-18 Preparation of (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-y l)-3-hydroxypyrrolidine-1-carboxamide

Publications (1)

Publication Number Publication Date
CO2018013015A2 true CO2018013015A2 (es) 2019-08-20

Family

ID=58794189

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2018/0013015A CO2018013015A2 (es) 2016-05-18 2018-11-30 Procesos para la preparación de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidin-1-carboxamida y sales del mismo

Country Status (28)

Country Link
US (1) US11214571B2 (es)
EP (2) EP3458456B1 (es)
JP (1) JP7443057B2 (es)
KR (1) KR102566858B1 (es)
CN (1) CN110049987B (es)
AU (1) AU2017268371B2 (es)
CA (1) CA3024603A1 (es)
CL (1) CL2018003264A1 (es)
CO (1) CO2018013015A2 (es)
DK (2) DK3458456T3 (es)
ES (2) ES2836222T3 (es)
FI (1) FI3800189T3 (es)
HR (2) HRP20201984T1 (es)
HU (2) HUE053643T2 (es)
IL (1) IL262964B (es)
LT (2) LT3458456T (es)
MX (1) MX392604B (es)
NZ (1) NZ748520A (es)
PE (1) PE20190437A1 (es)
PL (2) PL3458456T3 (es)
PT (2) PT3458456T (es)
RS (2) RS64698B1 (es)
RU (1) RU2745953C2 (es)
SG (1) SG11201810245WA (es)
SI (2) SI3800189T1 (es)
UA (1) UA127826C2 (es)
WO (1) WO2017201241A1 (es)
ZA (1) ZA201808534B (es)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103965200B (zh) 2008-09-22 2016-06-08 阵列生物制药公司 作为trk激酶抑制剂的取代的咪唑并[1,2-b]哒嗪化合物
CN102264736B (zh) 2008-10-22 2013-08-14 阵列生物制药公司 作为TRK激酶抑制剂的取代的吡唑并[1,5-a]嘧啶化合物
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
EP3521291A1 (en) 2010-05-20 2019-08-07 Array Biopharma, Inc. Macrocyclic compounds as trk kinase inhibitors
BR112017010141A2 (pt) 2014-11-16 2018-03-06 Array Biopharma, Inc. Forma cristalina de hidrogenossulfato de (s)-n-(5- ((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5- a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida
AU2016344058A1 (en) 2015-10-26 2018-05-17 Array Biopharma Inc. Point mutations in Trk inhibitor-resistant cancer and methods relating to the same
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
CN109414442B (zh) 2016-04-04 2024-03-29 洛克索肿瘤学股份有限公司 一种化合物的液体制剂
US11214571B2 (en) 2016-05-18 2022-01-04 Array Biopharma Inc. Process for the preparation of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide and salts thereof
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
ES2930081T3 (es) * 2017-08-11 2022-12-07 Teligene Ltd Pirazolopirimidinas sustituidas útiles como inhibidores de quinasas
CN109232582B (zh) * 2018-11-28 2021-02-05 安礼特（上海）医药科技有限公司 拉洛替尼硫酸氢盐晶型及其制备和应用
CN112457231A (zh) * 2019-09-09 2021-03-09 上海医药工业研究院 一种拉罗替尼（Larotrectinib）中间体的消旋化方法
CN110804059B (zh) * 2019-09-30 2024-03-12 郑州泰基鸿诺医药股份有限公司 氨基甲酸酯类化合物、药物组合物及其应用
CN111138437B (zh) * 2019-12-04 2021-03-05 杭州华东医药集团新药研究院有限公司 取代的吡唑并[1,5-a]嘧啶氨基酸衍生物及其用途
CN112624950A (zh) * 2020-12-10 2021-04-09 北京蓝博特科技有限公司 一种(r)-2-(2,5-二氟苯基)吡咯烷的合成方法
WO2022168115A1 (en) 2021-02-05 2022-08-11 Mylan Laboratories Limited A process for the preparation of larotrectinib or its salts
CN113444070A (zh) * 2021-07-28 2021-09-28 深圳市真味生物科技有限公司 一种由手性叔丁基亚磺酰胺合成手性尼古丁的制备方法
CN115872905B (zh) * 2021-09-29 2024-08-09 凯特立斯（深圳）科技有限公司 一种拉罗替尼中间体的制备方法
WO2024023836A1 (en) 2022-07-27 2024-02-01 Mylan Laboratories Limited Polymorphic form of larotrectinib sulfate
EP4382529A1 (en) 2022-12-07 2024-06-12 Bayer Consumer Care AG A process for preparing pure (3s)-pyrrolidin-3-ol and pure (3s)-pyrrolidin-3-ol hydrochloride

Family Cites Families (272)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ234143A (en) 1989-06-28 1991-10-25 Mcneil Ppc Inc Aqueous pharmaceutical suspension formulation for administering substantially insoluble pharmaceutical agents
GB9212308D0 (en) * 1992-06-10 1992-07-22 Ici Plc Therapeutic compositions
ATE233245T1 (de) 1993-11-30 2003-03-15 Searle & Co Substituierte pyrazolyl-benzolsulfonamide und ihre verwendung als cyclooxygenaseii inhibitoren
US5844092A (en) 1994-03-18 1998-12-01 Genentech, Inc. Human TRK receptors and neurotrophic factor inhibitors
US5430021A (en) 1994-03-18 1995-07-04 Pharmavene, Inc. Hydrophobic drug delivery systems
US5877016A (en) 1994-03-18 1999-03-02 Genentech, Inc. Human trk receptors and neurotrophic factor inhibitors
US6458811B1 (en) 1996-03-26 2002-10-01 Eli Lilly And Company Benzothiophenes formulations containing same and methods
CA2206201A1 (en) 1996-05-29 1997-11-29 Yoshiaki Isobe Pyrazole derivatives and their pharmaceutical use
JP3898296B2 (ja) 1996-08-28 2007-03-28 ポーラ化成工業株式会社 ピロロピラゾロピリミジン化合物及びこれを有効成分とする医薬
DE69827786T2 (de) 1997-04-25 2005-11-24 Takeda Pharmaceutical Co. Ltd. Condensierte pyridazine derivate,deren herstellung und verwendung
PL195280B1 (pl) 1999-01-21 2007-08-31 Bristol Myers Squibb Co Kompleks inhibitora RAS-farnezylotransferazy o ulepszonej rozpuszczalności w wodzie i trwałości oraz kompozycja inhibitora RAS-farnezylotransferazy
UA74546C2 (en) 1999-04-06 2006-01-16 Boehringer Ingelheim Ca Ltd Macrocyclic peptides having activity relative to hepatitis c virus, a pharmaceutical composition and use of the pharmaceutical composition
US6534085B1 (en) 1999-09-23 2003-03-18 Bioresponse L.L.C. Phytochemicals for promoting weight loss
KR100823764B1 (ko) 2000-06-22 2008-04-21 제넨테크, 인크. 아고니스트 안티-티알케이-씨 모노클로날 항체
GB0028575D0 (en) 2000-11-23 2001-01-10 Elan Corp Plc Oral pharmaceutical compositions containing cyclodextrins
GB0121919D0 (en) * 2001-09-11 2001-10-31 Astrazeneca Ab Chemical compounds
BR0116388A (pt) 2000-12-22 2003-09-30 Astrazeneca Ab Composto, processo para preparar um composto, composição farmacêutica e método para tratar, em um animal de sangue quente, distúrbios de alimentação e uso de um composto
TWI312347B (en) 2001-02-08 2009-07-21 Eisai R&D Man Co Ltd Bicyclic nitrogen-containing condensed ring compounds
BR0210231A (pt) 2001-05-30 2004-09-14 Genentech Inc Método de controle de uma disfunção relacionada ao fator de crescimento dos nervos (ngf), composição farmacêutica, artigo manufaturado e uso de anticorpo monoclonal anti-ngf
US7101572B2 (en) 2001-12-07 2006-09-05 Unilab Pharmatech, Ltd. Taste masked aqueous liquid pharmaceutical composition
US20030199525A1 (en) 2002-03-21 2003-10-23 Hirst Gavin C. Kinase inhibitors
WO2003091256A1 (en) 2002-04-23 2003-11-06 Shionogi & Co., Ltd. PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVE AND NAD(P)H OXIDASE INHIBITOR CONTAINING THE SAME
US7449488B2 (en) 2002-06-04 2008-11-11 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
US6982253B2 (en) 2002-06-05 2006-01-03 Supergen, Inc. Liquid formulation of decitabine and use of the same
ITMI20021620A1 (it) 2002-07-23 2004-01-23 Novuspharma Spa Composto ad ativita' antitumorale
JP4024624B2 (ja) 2002-08-26 2007-12-19 富士通株式会社 半導体装置の製造方法及び製造装置
US8580782B2 (en) 2002-09-04 2013-11-12 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
US7119200B2 (en) 2002-09-04 2006-10-10 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
CA2497440C (en) 2002-09-04 2011-03-22 Schering Corporation Pyrazolopyrimidines as cyclin-dependent kinase inhibitors
US7196078B2 (en) 2002-09-04 2007-03-27 Schering Corpoartion Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors
AU2003299651A1 (en) 2002-12-11 2004-06-30 Merck And Co., Inc. Tyrosine kinase inhibitors
WO2004052286A2 (en) 2002-12-11 2004-06-24 Merck & Co., Inc. Tyrosine kinase inhibitors
JP4634367B2 (ja) 2003-02-20 2011-02-16 スミスクライン ビーチャム コーポレーション ピリミジン化合物
GB0303910D0 (en) 2003-02-20 2003-03-26 Merck Sharp & Dohme Therapeutic agents
WO2004082458A2 (en) 2003-02-21 2004-09-30 The Johns Hopkins University Tyrosine kinome
JP2004277337A (ja) 2003-03-14 2004-10-07 Sumitomo Pharmaceut Co Ltd ピラゾロ［１，５−ａ］ピリミジン誘導体
WO2004087707A1 (en) 2003-03-31 2004-10-14 Vernalis (Cambridge) Limited Pyrazolopyrimidine compounds and their use in medicine
WO2004089471A2 (en) 2003-04-11 2004-10-21 Novo Nordisk A/S NEW PYRAZOLO[1,5-a] PYRIMIDINES DERIVATIVES AND PHARMACEUTICAL USE THEREOF
US20060094699A1 (en) 2003-04-11 2006-05-04 Kampen Gita Camilla T Combination therapy using an 11beta-hydroxysteroid dehydrogenase type 1 inhibitor and a glucocorticoid receptor agonist to minimize the side effects associated with glucocorticoid receptor agonist therapy
JP2006522744A (ja) 2003-04-11 2006-10-05 ノボ　ノルディスク　アクティーゼルスカブ グルココルチコイド受容体アゴニスト療法に伴う副作用を最小化するための、１１β−ヒドロキシステロイドデヒドロゲナーゼ１型阻害剤およびグルココルチコイド受容体アゴニストを使用する併用療法
JPWO2004096851A1 (ja) 2003-04-28 2006-10-12 株式会社ガルファーマ ガレクチン９誘導因子
PA8603801A1 (es) 2003-05-27 2004-12-16 Janssen Pharmaceutica Nv Derivados de la quinazolina
JP2005008581A (ja) 2003-06-20 2005-01-13 Kissei Pharmaceut Co Ltd 新規なピラゾロ［１，５−ａ］ピリミジン誘導体、それを含有する医薬組成物およびそれらの用途
EA009517B1 (ru) 2003-06-27 2008-02-28 Байер Кропсайенс Аг Пиразолопиримидины
RS52332B (sr) 2003-07-15 2012-12-31 Amgen Inc. Humana anti-ngf neutrališuća antitela kao selektivni inhibitori ngf signalnog puta
US7491794B2 (en) 2003-10-14 2009-02-17 Intermune, Inc. Macrocyclic compounds as inhibitors of viral replication
US7169918B2 (en) 2003-10-27 2007-01-30 Genelabs Technologies, Inc. Methods for preparing 7-(2′-substituted-β-D-ribofuranosyl)-4-(NR2R3)-5-(substituted ethyn-1-yl)-pyrrolo[2,3-d]pyrimidine derivatives
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
AU2004292773A1 (en) 2003-11-28 2005-06-09 Novartis Ag Diaryl urea derivatives in the treatment of protein kinase dependent diseases
ES2305887T3 (es) 2003-12-18 2008-11-01 Janssen Pharmaceutica Nv Derivados de pirido y pirimidopirimidinas como agentes antiproliferativos.
JP5138938B2 (ja) 2003-12-19 2013-02-06 プレキシコン インコーポレーテッド Ｒｅｔ調節剤の開発のための化合物および方法
WO2005068424A1 (en) 2004-01-20 2005-07-28 Cell Therapeutics Europe S.R.L. Indolinone derivatives as receptor tyrosine kinase ihibitors
US20050222171A1 (en) 2004-01-22 2005-10-06 Guido Bold Organic compounds
WO2005099363A2 (en) 2004-03-26 2005-10-27 Whitehead Institute For Biomedical Research Methods of diagnosing, preventing and treating cancer metastasis
CN1938311A (zh) 2004-03-30 2007-03-28 因特蒙公司 作为病毒复制抑制剂的大环化合物
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
PE20060664A1 (es) 2004-09-15 2006-08-04 Novartis Ag Amidas biciclicas como inhibidores de cinasa
MX337817B (es) 2004-11-04 2011-11-04 Vertex Pharma Pirazolo [1,5-a] pirimidinas de utilidad como inhibidores de proteina quinasas.
JO3088B1 (ar) 2004-12-08 2017-03-15 Janssen Pharmaceutica Nv مشتقات كوينازولين كبيرة الحلقات و استعمالها بصفتها موانع كينيز متعددة الاهداف
DE102005003687A1 (de) 2005-01-26 2006-07-27 Sphingo Tec Gmbh Immunoassay zur Bestimmung der Freisetzung von Neurotensin in die Zirkulation
NZ561526A (en) 2005-02-16 2010-11-26 Astrazeneca Ab Pyrazole derivatives as Trk kinase inhibitors
CN101119996A (zh) 2005-02-16 2008-02-06 阿斯利康(瑞典)有限公司 化学化合物
WO2006102194A1 (en) 2005-03-21 2006-09-28 Eli Lilly And Company Imidazopyridazine compounds
WO2006115452A1 (en) 2005-04-27 2006-11-02 Astrazeneca Ab Use of pyrazolyl-pyrimidine derivatives in the treatment of pain
US20080287437A1 (en) 2005-05-16 2008-11-20 Astrazeneca Ab Pyrazolylaminopyrimidine Derivatives Useful as Tyrosine Kinase Inhibitors
CN100406650C (zh) 2005-06-05 2008-07-30 徐斌 一种抗特大变位的模块式梳型桥梁伸缩缝装置
ITRM20050290A1 (it) 2005-06-07 2006-12-08 Lay Line Genomics Spa Uso di molecole in grado di inibire il legame tra ngf e il suo recettore trka come analgesici ad effetto prolungato.
DK2395004T3 (en) 2005-06-22 2016-03-21 Plexxikon Inc Pyrrolo [2,3-b] pyridine derivatives as protein kinase inhibitors
US20070025540A1 (en) 2005-07-07 2007-02-01 Roger Travis Call center routing based on talkativeness
CN101263156A (zh) 2005-07-25 2008-09-10 因特蒙公司 C型肝炎病毒复制的新颖大环抑制剂
JP2009502734A (ja) 2005-07-29 2009-01-29 アステラス製薬株式会社 Ｌｃｋ阻害剤としての縮合複素環
CN101232871A (zh) 2005-08-03 2008-07-30 伊士曼化工公司 生育酚聚乙二醇琥珀酸酯粉末及其制备方法
US20070191306A1 (en) 2005-08-17 2007-08-16 Bristol-Myers Squibb Company FACTOR Xa INHIBITOR FORMULATION AND METHOD
CA2619365A1 (en) 2005-08-22 2007-03-01 Amgen Inc. Pyrazolopyridine and pyrazolopyrimidine compounds useful as kinase enzymes modulators
WO2007025090A2 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase
PT1919979E (pt) 2005-08-25 2014-03-07 Creabilis Therapeutics Spa Polímeros conjugados de k-252a e seus derivados
DE102005042742A1 (de) 2005-09-02 2007-03-08 Schering Ag Substituierte Imidazo[1,2b]pyridazine als Kinase-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
US20070078136A1 (en) 2005-09-22 2007-04-05 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
BRPI0616985B1 (pt) 2005-10-06 2021-10-26 Merck Sharp & Dohme Corp. Composto de pirazolo[1,5-a]pirimidina, e, uso de um composto
JP5102212B2 (ja) 2005-10-06 2012-12-19 メルク・シャープ・アンド・ドーム・コーポレーション プロテインキナーゼインヒビターとしてのピラゾロピリミジン
NZ568135A (en) 2005-10-11 2011-06-30 Array Biopharma Inc Macrocyclic compounds and methods for inhibiting hepatitis C viral replication
WO2007057782A2 (en) 2005-10-11 2007-05-24 Centre National De La Recherche Scientifique (Cnrs) 3 -hydroxyflavone derivatives for the detection and the quantification of cell apoptosis
WO2007048066A2 (en) 2005-10-21 2007-04-26 Exelixis, Inc. Pyrazolo-pyrimidines as casein kinase ii (ck2) modulators
WO2007057399A2 (en) 2005-11-15 2007-05-24 Boehringer Ingelheim International Gmbh Treatment of cancer with indole derivatives
GB0524436D0 (en) 2005-11-30 2006-01-11 Novartis Ag Organic compounds
WO2007070504A2 (en) 2005-12-13 2007-06-21 Morton Grove Pharmaceuticals, Inc. Stable and palatable oral liquid sumatriptan compositions
US8399442B2 (en) 2005-12-30 2013-03-19 Astex Therapeutics Limited Pharmaceutical compounds
US20080108611A1 (en) 2006-01-19 2008-05-08 Battista Kathleen A Substituted thienopyrimidine kinase inhibitors
WO2007087245A2 (en) 2006-01-24 2007-08-02 Merck & Co., Inc. Ret tyrosine kinase inhibition
KR100846988B1 (ko) 2006-03-06 2008-07-16 제일약품주식회사 신규한 티에노피리미딘 유도체 또는 이의 약학적으로허용가능한 염, 이의 제조방법 및 이를 함유하는 약학조성물
JP2009529047A (ja) * 2006-03-07 2009-08-13 アレイ バイオファーマ、インコーポレイテッド ヘテロ二環系ピラゾール化合物およびその使用
EP2004623B1 (en) 2006-03-27 2013-10-09 Nerviano Medical Sciences S.r.l. Pyridyl- and pyrimidinyl-substituted pyrrole-, thiophene- and furane-derivatives as kinase inhibitors
GB0606805D0 (en) 2006-04-04 2006-05-17 Novartis Ag Organic compounds
ATE471940T1 (de) 2006-04-26 2010-07-15 Hoffmann La Roche Thienoä3,2-düpyrimidin-derivat geeignet als pi3k inhibitor
ES2556173T3 (es) 2006-05-18 2016-01-13 Eisai R&D Management Co., Ltd. Agente antitumoral para un cáncer de tiroides
EP1873157A1 (en) 2006-06-21 2008-01-02 Bayer Schering Pharma Aktiengesellschaft Pyrazolopyrimidines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same
TWI419889B (zh) 2006-07-05 2013-12-21 Mitsubishi Tanabe Pharma Corp 吡唑并〔１，５-ａ〕嘧啶化合物
EP2058309A4 (en) 2006-08-04 2010-12-22 Takeda Pharmaceutical CONDENSED HETEROCYCLIC COMPOUND
PE20080538A1 (es) 2006-08-04 2008-06-18 Takeda Pharmaceutical Derivado heterociclico fusionado y su uso
US7531539B2 (en) 2006-08-09 2009-05-12 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
US20110021513A1 (en) 2006-09-07 2011-01-27 Biogen Idec Ma Inc. Modulators of interleukin-1 receptor-associated kinase
EP2067039A2 (en) 2006-09-12 2009-06-10 Novartis Forschungsstiftung, Zweigniederlassung Friedrich Miescher Institute for Biomedical Research Non-neuroendocrine cancer therapy
JP2010504933A (ja) 2006-09-29 2010-02-18 ノバルティス アーゲー Ｐｉ３ｋ脂質キナーゼ阻害剤としてのピラゾロピリミジン
CA2667962A1 (en) 2006-10-30 2008-05-08 Novartis Ag Heterocyclic compounds as antiinflammatory agents
AU2007316417B2 (en) 2006-11-06 2013-08-22 Tolero Pharmaceuticals, Inc. Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors
CN101641351A (zh) 2006-12-21 2010-02-03 普莱希科公司 用于激酶调节的化合物和方法及其适应症
PE20081581A1 (es) 2006-12-21 2008-11-12 Plexxikon Inc COMPUESTOS PIRROLO[2,3-b]PIRIDINAS COMO MODULADORES DE QUINASA
WO2008079909A1 (en) 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
US7820684B2 (en) 2007-03-01 2010-10-26 Supergen, Inc. Pharmaceutical formulations comprising salts of a protein kinase inhibitor and methods of using same
US20080234267A1 (en) 2007-03-20 2008-09-25 Karen Elizabeth Lackey Compounds and Methods of Treatment
US20080234262A1 (en) 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
EP2137187A1 (en) 2007-03-28 2009-12-30 Inovacia AB Pyrazolo [1,5-a]pyrimidines as inhibitors of stearoyl-coa desaturase
CN103214482B (zh) 2007-04-03 2016-06-29 阵列生物制药公司 作为受体酪氨酸激酶抑制剂的咪唑并[1,2-a]吡啶化合物
BRPI0811516A2 (pt) 2007-05-04 2014-11-18 Irm Llc Compostos e composições como inibidores de c-kit e pdgfr cinase
CA2687909C (en) 2007-06-21 2015-09-15 Janssen Pharmaceutica Nv Indolin-2-ones and aza-indolin-2-ones
CN101801962A (zh) 2007-07-09 2010-08-11 阿斯利康(瑞典)有限公司 用于治疗增殖疾病的三取代嘧啶衍生物
SG183036A1 (en) 2007-07-17 2012-08-30 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
AR067585A1 (es) 2007-07-19 2009-10-14 Schering Corp Compuestos heterociclicos de amidas como inhibidores de la proteincinasa
SI2176231T1 (sl) 2007-07-20 2017-01-31 Nerviano Medical Sciences S.R.L. Substituirani indazolni derivati, aktivni kot kinazni inhibitorji
WO2009017838A2 (en) 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
EP2187964B1 (en) 2007-08-10 2014-10-08 Regeneron Pharmaceuticals, Inc. High affinity human antibodies to human nerve growth factor
CA2702838A1 (en) 2007-10-16 2009-04-23 Wyeth Llc Thienopyrimidine and pyrazolopyrimidine compounds and their use as mtor kinase and pi3 kinase inhibitors
KR20100089851A (ko) 2007-10-23 2010-08-12 노파르티스 아게 호흡기 질환의 치료를 위한 ｔｒｋｂ 항체의 용도
US20110046127A1 (en) 2007-11-08 2011-02-24 Paolo Pevarello Imidazopyridazines for Use as Protein Kinase Inhibitors
CN101970440A (zh) 2007-11-28 2011-02-09 先灵公司 作为蛋白激酶抑制剂的2-氟吡唑并[1，5-a]嘧啶类
WO2009071480A2 (en) 2007-12-04 2009-06-11 Nerviano Medical Sciences S.R.L. Substituted dihydropteridin-6-one derivatives, process for their preparation and their use as kinase inhibitors
US8642035B2 (en) 2008-01-17 2014-02-04 Irm Llc Anti-TrkB antibodies
JP2009203226A (ja) 2008-01-31 2009-09-10 Eisai R & D Management Co Ltd ピリジン誘導体およびピリミジン誘導体を含有するレセプターチロシンキナーゼ阻害剤
AU2009221177B2 (en) 2008-03-03 2013-05-30 Ucb Biopharma Sprl Pharmaceutical solutions, process of preparation and therapeutic uses
KR100963051B1 (ko) 2008-03-14 2010-06-09 광동제약 주식회사 입자크기가 조절된 술포데히드로아비에트산을 함유한쓴맛이 저감된 경구용 액상 조성물
ES2588193T3 (es) 2008-03-28 2016-10-31 Nerviano Medical Sciences S.R.L. Derivados de 3,4-dihidro-2H-pirazino[1,2-a]indol-1-ona activos como inhibidores de cinasa, proceso para su preparación y composiciones farmacéuticas que los comprenden
US20090275622A1 (en) 2008-04-30 2009-11-05 Prasoona Linga Nizatidine formulations
CN102056927B (zh) 2008-05-13 2014-06-25 Irm责任有限公司 作为激酶抑制剂的稠合含氮杂环及其组合物
WO2009143018A2 (en) 2008-05-19 2009-11-26 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
PE20091846A1 (es) 2008-05-19 2009-12-16 Plexxikon Inc DERIVADOS DE PIRROLO[2,3-d]-PIRIMIDINA COMO MODULADORES DE CINASAS
KR101257158B1 (ko) 2008-05-23 2013-04-23 노파르티스 아게 단백질 티로신 키나제 억제제로서의 퀴놀린 및 퀴녹살린의 유도체
CA2727389A1 (en) 2008-06-10 2009-12-17 Prabha N. Ibrahim 5h-pyrrolo [2,3-b] pyrazine derivatives for kinase modulation, and indications therefor
EP2323664B1 (en) 2008-07-29 2015-01-07 Nerviano Medical Sciences S.r.l. Use of a cdk inhibitor for the treatment of glioma
JP5746032B2 (ja) 2008-09-19 2015-07-08 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ ３，４−ジヒドロ−２Ｈ−ピロロ［１，２−ａ］ピラジン−１−オン誘導体
CN103965200B (zh) 2008-09-22 2016-06-08 阵列生物制药公司 作为trk激酶抑制剂的取代的咪唑并[1,2-b]哒嗪化合物
CN102264736B (zh) 2008-10-22 2013-08-14 阵列生物制药公司 作为TRK激酶抑制剂的取代的吡唑并[1,5-a]嘧啶化合物
WO2010051549A1 (en) 2008-10-31 2010-05-06 Genentech, Inc. Pyrazolopyrimidine jak inhibitor compounds and methods
WO2010058006A1 (en) 2008-11-24 2010-05-27 Nerviano Medical Sciences S.R.L. Cdk inhibitor for the treatment of mesothelioma
JO3265B1 (ar) 2008-12-09 2018-09-16 Novartis Ag مثبطات بيريديلوكسى اندولات vegf-r2 واستخدامها لعلاج المرض
JP5979877B2 (ja) 2009-02-12 2016-08-31 セル・シグナリング・テクノロジー・インコーポレイテツド ヒト癌における変異ｒｏｓ発現
WO2010111527A1 (en) 2009-03-26 2010-09-30 Plexxikon, Inc. Pyrazolo [ 3, 4 -b] pyridines as kinase inhibitors and their medical use
US8546413B2 (en) 2009-06-15 2013-10-01 Nerviano Medical Sciences S.R.L. Substituted pyrimidinylpyrrolopyridinone derivatives, process for their preparation and their use as kinase inhibitors
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
RS56669B1 (sr) 2009-12-21 2018-03-30 Samumed Llc 1h-pirazolo[3,4-b]piridini i njihove terapeutske primene
WO2011092120A1 (en) 2010-01-29 2011-08-04 Nerviano Medical Sciences S.R.L. 6,7- dihydroimidazo [1,5-a] pyrazin-8 (5h) - one derivatives as protein kinase modulators
JP2013519706A (ja) 2010-02-18 2013-05-30 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル 癌転移を予防するための方法
WO2011127219A1 (en) 2010-04-06 2011-10-13 Caris Life Sciences Luxembourg Holdings Circulating biomarkers for disease
US8383793B2 (en) 2010-04-15 2013-02-26 St. Jude Children's Research Hospital Methods and compositions for the diagnosis and treatment of cancer resistant to anaplastic lymphoma kinase (ALK) kinase inhibitors
TWI619713B (zh) 2010-04-21 2018-04-01 普雷辛肯公司 用於激酶調節的化合物和方法及其適應症
EP3521291A1 (en) 2010-05-20 2019-08-07 Array Biopharma, Inc. Macrocyclic compounds as trk kinase inhibitors
EA028080B1 (ru) 2010-06-09 2017-10-31 Дана-Фарбер Кэнсер Инститьют, Инк. Мутация в mek1, придающая устойчивость к ингибиторам raf и mek
JP6121903B2 (ja) 2010-08-19 2017-04-26 ゾエティス・ベルジャム・エス・アー 抗ｎｇｆ抗体およびその使用
US8637516B2 (en) 2010-09-09 2014-01-28 Irm Llc Compounds and compositions as TRK inhibitors
WO2012034095A1 (en) 2010-09-09 2012-03-15 Irm Llc Compounds and compositions as trk inhibitors
JP2014005206A (ja) 2010-10-22 2014-01-16 Astellas Pharma Inc アリールアミノヘテロ環カルボキサミド化合物
AU2011336470B8 (en) 2010-12-01 2017-09-14 Alderbio Holdings Llc Anti-NGF compositions and use thereof
EP2668190B1 (en) 2011-01-26 2016-08-17 Nerviano Medical Sciences S.r.l. Tricyclic pyrrolo derivatives, process for their preparation and their use as kinase inhibitors
JP5925808B2 (ja) 2011-01-26 2016-05-25 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ 三環式誘導体、これらの調製方法およびこれらのキナーゼ阻害剤としての使用
JP5941069B2 (ja) 2011-02-07 2016-06-29 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． キナーゼ調節のための化合物および方法、ならびにそれに対する適応症
RU2606497C2 (ru) 2011-02-24 2017-01-10 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Тиазолилфенилбензолсульфонамидопроизводные в качестве ингибиторов киназ
US9102671B2 (en) 2011-02-25 2015-08-11 Novartis Ag Compounds and compositions as TRK inhibitors
JP5976778B2 (ja) 2011-04-11 2016-08-24 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤としてのピラゾリル−ピリミジン誘導体
EP2699564B1 (en) 2011-04-19 2016-12-14 Nerviano Medical Sciences S.r.l. Substituted pyrimidinyl-pyrroles active as kinase inhibitors
SI2707359T1 (sl) 2011-05-12 2017-02-28 Nerviano Medical Sciences S.R.L. Substituirani indazolni derivati, aktivni kot kinazni zaviralci
CN105130967B (zh) 2011-05-13 2018-04-17 阵列生物制药公司 作为trka激酶抑制剂的吡咯烷基脲和吡咯烷基硫脲化合物
US8912200B2 (en) 2011-07-28 2014-12-16 Nerviano Medical Sciences S.R.L. Alkynyl substituted pyrimidinyl-pyrroles active as kinases inhibitors
EP2788350B1 (en) 2011-10-07 2017-12-06 Nerviano Medical Sciences S.r.l. 4-ALKYL SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS
WO2013050446A1 (en) 2011-10-07 2013-04-11 Nerviano Medical Sciences S.R.L. SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS
WO2013059740A1 (en) 2011-10-21 2013-04-25 Foundation Medicine, Inc. Novel alk and ntrk1 fusion molecules and uses thereof
WO2013074518A1 (en) 2011-11-14 2013-05-23 Tesaro, Inc. Modulating certain tyrosine kinases
US9045478B2 (en) 2011-12-12 2015-06-02 Dr. Reddy's Laboratories Ltd. Substituted pyrazolo[1,5-a] pyridine as tropomyosin receptor kinase (Trk) inhibitors
US8377946B1 (en) 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
EP2842955B1 (en) 2012-04-26 2016-10-05 ONO Pharmaceutical Co., Ltd. Trk-inhibiting compound
JP2013226108A (ja) 2012-04-27 2013-11-07 Astellas Pharma Inc 新規ｎｔｒｋ２活性化変異の検出法
CN104395308B (zh) 2012-05-23 2016-08-24 内尔维阿诺医学科学有限公司 N-[5-(3,5-二氟-苄基)-1h-吲唑-3-基]-4-(4-甲基-哌嗪-1-基)-2-(四氢-吡喃-4-基氨基)-苯甲酰胺的制备方法
TWI585088B (zh) 2012-06-04 2017-06-01 第一三共股份有限公司 作爲激酶抑制劑之咪唑并［１，２－ｂ］嗒衍生物
SG11201408565VA (en) 2012-06-28 2015-02-27 Mcneil Ppc Inc Racecadotril liquid compositions
KR102163776B1 (ko) 2012-07-11 2020-10-12 블루프린트 메디신즈 코포레이션 섬유아세포 성장인자 수용체의 저해제
BR112015001690A2 (pt) 2012-07-24 2017-11-07 Pharmacyclics Inc mutações associadas com a resistência a inibidores da tirosina quinase de bruton (btk)
EP2689778A1 (en) 2012-07-27 2014-01-29 Pierre Fabre Medicament Derivatives of azaindoles or diazaindoles for treating pain
DK2880025T3 (en) 2012-08-02 2019-03-18 Nerviano Medical Sciences Srl SUBSTITUTED PYROLES ACTIVE AS KINase INHIBITORS
WO2014036387A2 (en) 2012-08-31 2014-03-06 The Regents Of The University Of Colorado Methods for diagnosis and treatment of cancer
CN104703600A (zh) 2012-09-07 2015-06-10 埃克塞里艾克西斯公司 用于治疗肺腺癌的met、vegfr和ret的抑制剂
US20140084039A1 (en) 2012-09-24 2014-03-27 Electro Scientific Industries, Inc. Method and apparatus for separating workpieces
JP2014082984A (ja) 2012-10-23 2014-05-12 Astellas Pharma Inc 新規ｎｔｒｋ２活性化変異の検出法
EP4223770A3 (en) 2012-11-05 2023-10-18 Foundation Medicine, Inc. Novel fusion molecules and uses thereof
WO2014071358A2 (en) 2012-11-05 2014-05-08 Foundation Medicine, Inc. Novel ntrk1 fusion molecules and uses thereof
WO2014072220A1 (en) 2012-11-07 2014-05-15 Nerviano Medical Sciences S.R.L. Substituted pyrimidinyl and pyridinyl-pyrrolopyridinones, process for their preparation and their use as kinase inhibitors
US9790210B2 (en) 2012-11-13 2017-10-17 Array Biopharma Inc. N-(monocyclic aryl),N'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
ES2610975T3 (es) 2012-11-13 2017-05-04 Array Biopharma, Inc. Compuestos bicíclicos de urea, tiourea, guanidina y cianoguanidina útiles para el tratamiento del dolor
US9828360B2 (en) 2012-11-13 2017-11-28 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
WO2014078328A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-bicyclic aryl,n'-pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
US9790178B2 (en) 2012-11-13 2017-10-17 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
MX365733B (es) 2012-11-13 2019-06-12 Array Biopharma Inc Compuestos de n-pirrolidinil, n' -pirazolil-urea, tiourea, guanidina y cianoguanidina como inhibidores de trka cinasa.
US9981959B2 (en) 2012-11-13 2018-05-29 Array Biopharma Inc. Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
US9822118B2 (en) 2012-11-13 2017-11-21 Array Biopharma Inc. Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
WO2014078417A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
US9969694B2 (en) 2012-11-13 2018-05-15 Array Biopharma Inc. N-(arylalkyl)-N′-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
CA2877847A1 (en) 2012-11-29 2014-06-05 Yeda Research And Development Co. Ltd. Methods of preventing tumor metastasis, treating and prognosing cancer and identifying agents which are putative metastasis inhibitors
US9447135B2 (en) 2012-12-14 2016-09-20 University Of Kentucky Research Foundation Semi-synthetic mithramycin derivatives with anti-cancer activity
US9127055B2 (en) 2013-02-08 2015-09-08 Astellas Pharma Inc. Method of treating pain with anti-human NGF antibody
TWI567068B (zh) 2013-02-19 2017-01-21 小野藥品工業股份有限公司 Ｔｒｋ抑制化合物
US20160010068A1 (en) 2013-02-22 2016-01-14 Boris C. Bastian Fusion polynucleotides and fusion polypeptides associated with cancer and particularly melanoma and their uses as therapeutic and diagnostic targets
WO2014134096A1 (en) 2013-02-27 2014-09-04 Oregon Health & Science University Methods of treating cancers characterized by aberrent ros1 activity
WO2014150751A2 (en) 2013-03-15 2014-09-25 Novartis Ag Biomarkers associated with brm inhibition
US9499522B2 (en) 2013-03-15 2016-11-22 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
WO2014151734A1 (en) 2013-03-15 2014-09-25 The Trustees Of Columbia University In The City Of New York Fusion proteins and methods thereof
WO2014152777A2 (en) 2013-03-15 2014-09-25 Insight Genetics, Inc. Methods and compositions for the diagnosis and treatment of cancers resistant to ros1 inhibitors
EP4253558B1 (en) 2013-03-15 2025-07-02 The Board of Trustees of the Leland Stanford Junior University Identification and use of circulating nucleic acid tumor markers
MA38394B1 (fr) 2013-03-15 2018-04-30 Glaxosmithkline Ip Dev Ltd Dérivés pyridine utilisés comme inhibiteurs de la kinase réarrangée au cours de la transfection (ret)
AU2014254394B2 (en) 2013-04-17 2020-06-18 Life Technologies Corporation Gene fusions and gene variants associated with cancer
US10072298B2 (en) 2013-04-17 2018-09-11 Life Technologies Corporation Gene fusions and gene variants associated with cancer
EP2997030B1 (en) 2013-05-14 2017-08-09 Nerviano Medical Sciences S.R.L. Pyrrolo[2,3-d]pyrimidine derivatives, process for their preparation and their use as kinase inhibitors
RU2015149937A (ru) 2013-05-30 2017-07-06 Плексксикон Инк. Соединения для модулирования киназы и показания к их применению
TWI610923B (zh) 2013-07-11 2018-01-11 Betta Pharmaceuticals Co Ltd 酪氨酸蛋白激酶調節劑及其應用方法
US10705087B2 (en) 2013-07-26 2020-07-07 Japanese Foundation For Cancer Research Detection method for NTRK3 fusion
EP3027655B1 (en) 2013-07-30 2019-08-21 Blueprint Medicines Corporation Ntrk2 fusions
WO2015017528A1 (en) 2013-07-30 2015-02-05 Blueprint Medicines Corporation Pik3c2g fusions
WO2015039006A1 (en) 2013-09-16 2015-03-19 The General Hospital Corporation Methods of treating cancer
HUE059041T2 (hu) 2013-10-17 2022-10-28 Blueprint Medicines Corp Eljárás KIT-tel összefüggõ rendellenességek kezelésére alkalmas kompozíciók elõállítására
WO2015058129A1 (en) 2013-10-17 2015-04-23 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
CN105848654B (zh) 2013-10-24 2018-10-02 乔治城大学 用于治疗癌症的方法和组合物
BR112016008849B8 (pt) 2013-10-25 2022-09-06 Blueprint Medicines Corp Compostos ou sais farmaceuticamente aceitáveis dos mesmos, uso dos referidos compostos e composições farmacêuticas
WO2015064621A1 (ja) 2013-10-29 2015-05-07 公益財団法人がん研究会 新規融合体及びその検出法
WO2015108992A1 (en) 2014-01-15 2015-07-23 Blueprint Medicines Corporation Heterobicyclic compounds and their use as fgfr4 receptor inhibitors
RS65417B1 (sr) 2014-01-24 2024-05-31 Turning Point Therapeutics Inc Diaril makrocikli kao modulatori protein kinaza
KR101723997B1 (ko) 2014-02-05 2017-04-06 브이엠 온콜로지 엘엘씨 화합물의 조성물 및 이의 용도
US10231965B2 (en) 2014-02-20 2019-03-19 Ignyta, Inc. Molecules for administration to ROS1 mutant cancer cells
US20170044621A1 (en) 2014-04-18 2017-02-16 Blueprint Medicines Corporation Met fusions
EP3132056B1 (en) 2014-04-18 2021-11-24 Blueprint Medicines Corporation Pik3ca fusions
MX2016014945A (es) 2014-05-15 2017-03-27 Array Biopharma Inc 1- ((3s,4r) -4- (3-fluorofenil) -1- (2-metoxietil) pirrolidin-3-il) -3- (4-metil-3- (2-metilpirimidin-5-il) -1-fenil-1h-pirazol-5-il) urea como inhibidor de trka cinasa.
WO2015183836A1 (en) 2014-05-27 2015-12-03 Brian Haynes Compositions, methods, and uses related to ntrk2-tert fusions
WO2015183837A1 (en) 2014-05-27 2015-12-03 Brian Haynes Compositions, methods, and uses related to ntrk2-tert fusions
WO2015184443A1 (en) 2014-05-30 2015-12-03 The Regents Of The University Of Colorado Activating ntrk1 gene fusions predictive of kinase inhibitor therapy
US10378063B2 (en) 2014-06-10 2019-08-13 Blueprint Medicines Corporation RAF1 fusions
EP3155118A1 (en) 2014-06-10 2017-04-19 Blueprint Medicines Corporation Pkn1 fusions
WO2016011147A1 (en) 2014-07-17 2016-01-21 Blueprint Medicines Corporation Prkc fusions
US10370725B2 (en) 2014-07-17 2019-08-06 Blueprint Medicines Corporation FGR fusions
US10370723B2 (en) 2014-07-17 2019-08-06 Blueprint Medicines Corporation TERT fusions
EP3185870A4 (en) 2014-08-01 2018-06-20 Pharmacyclics LLC Biomarkers for predicting response of dlbcl to treatment with a btk inhibitor
WO2016022569A1 (en) 2014-08-04 2016-02-11 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
WO2016027754A1 (ja) 2014-08-18 2016-02-25 小野薬品工業株式会社 Ｔｒｋ阻害化合物の酸付加塩
EP3206711B1 (en) 2014-10-14 2023-05-31 Novartis AG Antibody molecules to pd-l1 and uses thereof
EA039885B1 (ru) 2014-11-14 2022-03-23 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Производные 6-амино-7-бицикло-7-деазапурина в качестве ингибиторов протеинкиназы
BR112017010141A2 (pt) 2014-11-16 2018-03-06 Array Biopharma, Inc. Forma cristalina de hidrogenossulfato de (s)-n-(5- ((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5- a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida
EP3221700B1 (en) 2014-11-18 2022-06-22 Blueprint Medicines Corporation Prkacb fusions
JP6609631B2 (ja) 2014-12-15 2019-11-20 シーエムジー ファーマシューティカル カンパニー，リミテッド 縮合環ヘテロアリール化合物及びｔｒｋ抑制剤としての用途
PE20180670A1 (es) 2015-05-20 2018-04-19 Broad Inst Inc Neoantigenos compartidos
EP3303382A4 (en) 2015-05-29 2018-12-19 Ignyta, Inc. Compositions and methods for treating patients with rtk mutant cells
BR112017025773A2 (pt) 2015-06-01 2018-08-14 Loxo Oncology Inc métodos de diagnóstico e tratamento de câncer
AU2015101722A4 (en) 2015-06-19 2016-05-19 Macau University Of Science And Technology Oncogenic ros1 and alk kinase inhibitor
US9782400B2 (en) 2015-06-19 2017-10-10 Macau University Of Science And Technology Oncogenic ROS1 and ALK kinase inhibitor
GB201511546D0 (en) 2015-07-01 2015-08-12 Immatics Biotechnologies Gmbh Novel peptides and combination of peptides for use in immunotherapy against ovarian cancer and other cancers
ES2864839T3 (es) 2015-07-02 2021-10-14 Turning Point Therapeutics Inc Macrociclos de diarilo quirales como moduladores de proteína quinasas
AU2016344058A1 (en) 2015-10-26 2018-05-17 Array Biopharma Inc. Point mutations in Trk inhibitor-resistant cancer and methods relating to the same
WO2017127835A2 (en) 2016-01-22 2017-07-27 The Medicines Company Aqueous formulations and methods of preparation and use thereof
WO2017155018A1 (ja) 2016-03-11 2017-09-14 小野薬品工業株式会社 Ｔｒｋ阻害剤抵抗性の癌治療剤
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
SG11201808676RA (en) 2016-04-04 2018-11-29 Loxo Oncology Inc Methods of treating pediatric cancers
CN109414442B (zh) 2016-04-04 2024-03-29 洛克索肿瘤学股份有限公司 一种化合物的液体制剂
WO2017184597A1 (en) 2016-04-19 2017-10-26 Exelixis, Inc. Triple negative breast cancer treatment method
US11214571B2 (en) 2016-05-18 2022-01-04 Array Biopharma Inc. Process for the preparation of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide and salts thereof
WO2017201156A1 (en) 2016-05-18 2017-11-23 Duke University Method of treating kras wild-type metastatic colorectal cell carcinoma using cabozantinib plus panitumumab
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
CA3080157A1 (en) 2017-10-26 2019-05-02 Array Biopharma Inc. Formulations of a macrocyclic trk kinase inhibitor
CA3095366A1 (en) 2018-03-29 2019-10-03 Loxo Oncology, Inc. Treatment of trk-associated cancers

Also Published As

Publication number Publication date
FI3800189T3 (fi) 2023-07-31
RS64698B1 (sr) 2023-11-30
RU2745953C2 (ru) 2021-04-05
PT3800189T (pt) 2023-07-27
HRP20201984T1 (hr) 2021-04-16
IL262964B (en) 2021-06-30
MX2018014116A (es) 2019-12-11
ES2952056T3 (es) 2023-10-26
AU2017268371A1 (en) 2018-12-06
RU2018144557A (ru) 2020-06-18
BR112018073504A2 (pt) 2019-03-26
ZA201808534B (en) 2024-04-24
JP2019516795A (ja) 2019-06-20
UA127826C2 (uk) 2024-01-17
KR102566858B1 (ko) 2023-08-11
HUE053643T2 (hu) 2021-07-28
AU2017268371B2 (en) 2020-11-19
EP3458456B1 (en) 2020-11-25
WO2017201241A1 (en) 2017-11-23
EP3800189B1 (en) 2023-06-28
PL3458456T3 (pl) 2021-04-19
US11214571B2 (en) 2022-01-04
LT3458456T (lt) 2021-02-25
CN110049987B (zh) 2022-02-18
PL3800189T3 (pl) 2023-10-23
JP7443057B2 (ja) 2024-03-05
HUE063877T2 (hu) 2024-02-28
RS61463B1 (sr) 2021-03-31
CL2018003264A1 (es) 2019-06-21
PT3458456T (pt) 2020-12-07
IL262964A (en) 2018-12-31
CN110049987A (zh) 2019-07-23
DK3800189T3 (da) 2023-07-31
SI3800189T1 (sl) 2023-11-30
RU2018144557A3 (es) 2020-06-18
EP3800189A1 (en) 2021-04-07
KR20190039474A (ko) 2019-04-12
PE20190437A1 (es) 2019-03-27
SI3458456T1 (sl) 2021-04-30
US20190218222A1 (en) 2019-07-18
EP3458456A1 (en) 2019-03-27
LT3800189T (lt) 2023-10-10
DK3458456T3 (da) 2020-12-14
HRP20230704T1 (hr) 2023-10-27
NZ748520A (en) 2025-06-27
CA3024603A1 (en) 2017-11-23
SG11201810245WA (en) 2018-12-28
MX392604B (es) 2025-03-24
ES2836222T3 (es) 2021-06-24

Similar Documents

Publication Publication Date Title
CO2018013015A2 (es) Procesos para la preparación de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidin-1-carboxamida y sales del mismo
UY37781A (es) Proceso para la preparación de pirazolo[1,5-a] pirimidinas y sales de las mismas
IL290905B1 (en) Crystal form of (s)–n-(5–)–2–(r))5,2-difluorophenyl)-pyrrolidine-1-yl)-pyrazolo[5,1-a]pyrimidine-3-yl)-3 -Hydroxypyrrolidine-1-carboxamide hydrogen sulfate
UY37927A (es) Proceso para la preparación de 6-(2-hidroxi-2-metilpropoxi)-4-(6-(6-((6-metoxipiridin-3-il)metil)-3,6-diazabiciclo[3.1.1]heptan-3-il)piridin-3-il)pirazolo[1,5-a]piridina-3-carbonitrilo
PH12018502102A1 (en) Pyrrolotriazine compounds as tam inhibitors
PH12017502407B1 (en) Fused pyrimidine compound or salt thereof
PH12017501016A1 (en) Triazolopyrimidine compounds and uses thereof
CL2017002179A1 (es) Sales de inhibidor de pi3k y procesos de preparación
MY188447A (en) Indazole compounds as fger kinase inhibitor, preparation and use thereof
WO2016130920A3 (en) Lrrk2 inhibitors and methods of making and using the same
AR100818A1 (es) N-(cianometil)-4-(2-(4-morfolinofenilamino)pirimidin-4-il)benzamida
CO6700837A2 (es) Proceso de elaboración para derivados de prrimidina
AR103680A1 (es) Inhibidores selectivos de bace1
BR112017015852A2 (pt) forma de cristal, sal hemicálcico, sal hemicálcico di-hidratado, sal monossódico hidratado, sal bissódico monoidratado, sal monossódico anidro e método para preparar o composto 1
MX2018009503A (es) Sal de trifluoroacetato de agonista de tlr7 y forma cristalina b de la misma, metodos de preparacion y usos.
MX2018008966A (es) Procesos mejorados para la preparacion de osimertinib (azd9291) o una sal del mismo y "azd9291 anilina" o una sal del mismo.
MX394038B (es) Derivados de pirrolotriazina como inhibidores de cinasas.
MX381037B (es) Formas cristalinas y formas de sal de compuestos de 7h-pirrolo [2,3-d]pirimidina y método de preparación de las mismas.
PH12017501335A1 (en) Novel salt of fused pyrimidine compound and crystal thereof
MX2017003415A (es) Un derivado de tetrahidropirrolo [3,4-d] [1,3]tiazina como inhibidor de bace.
JOP20180105A1 (ar) عملية لتحضير (s)-n-(5-((r)-2-(2,5-داي فلورو فينيل)بيريوليدين-1-يل)-بيرازولو [1,5-a]بيريميدين -3-يل)-3-هيدروكسي بيروليدين-1-كربوكساميد وأملاح منه
TH1601003657A (th) อนุพันธ์ [1,2,4] ไตรอะโซโล [1,5-a]ไพริมิดีน ดังสารยับยั้งโปรเตียโซมของ โปรโตซัวสำหรับการรักษาของโรคที่เกิดจากปรสิต เช่น โรคลิชมาเนียซิส