CN101883774A - 噻吩并嘧啶和吡唑并嘧啶化合物及其用作mtor激酶和pi3激酶抑制剂的用途 - Google Patents

噻吩并嘧啶和吡唑并嘧啶化合物及其用作mtor激酶和pi3激酶抑制剂的用途 Download PDF

Info

Publication number
CN101883774A
CN101883774A CN2008801190434A CN200880119043A CN101883774A CN 101883774 A CN101883774 A CN 101883774A CN 2008801190434 A CN2008801190434 A CN 2008801190434A CN 200880119043 A CN200880119043 A CN 200880119043A CN 101883774 A CN101883774 A CN 101883774A
Authority
CN
China
Prior art keywords
phenyl
oxa
pyrimidine
azabicyclo
pyrazolo
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CN2008801190434A
Other languages
English (en)
Chinese (zh)
Inventor
A·扎斯克
J·A·卡普兰
J·C·维海珍
K·J·柯伦
D·J·理查德
S·艾罗尔-卡劳斯申
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Wyeth LLC
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 CN101883774A publication Critical patent/CN101883774A/zh
Pending legal-status Critical Current

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)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Obesity (AREA)
  • Endocrinology (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)
CN2008801190434A 2007-10-16 2008-10-15 噻吩并嘧啶和吡唑并嘧啶化合物及其用作mtor激酶和pi3激酶抑制剂的用途 Pending CN101883774A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US98033207P 2007-10-16 2007-10-16
US60/980,332 2007-10-16
US2759508P 2008-02-11 2008-02-11
US61/027,595 2008-02-11
PCT/US2008/079940 WO2009052145A1 (en) 2007-10-16 2008-10-15 Thienopyrimidine and pyrazolopyrimidine compounds and their use as mtor kinase and pi3 kinase inhibitors

Publications (1)

Publication Number Publication Date
CN101883774A true CN101883774A (zh) 2010-11-10

Family

ID=40345078

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2008801190434A Pending CN101883774A (zh) 2007-10-16 2008-10-15 噻吩并嘧啶和吡唑并嘧啶化合物及其用作mtor激酶和pi3激酶抑制剂的用途

Country Status (26)

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

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013152717A1 (zh) * 2012-04-10 2013-10-17 上海昀怡健康管理咨询有限公司 稠合嘧啶类化合物,其制备方法,中间体,组合物和应用
CN104080789A (zh) * 2012-01-31 2014-10-01 南京奥昭生物科技有限公司 作为布鲁顿酪氨酸激酶抑制剂的环状分子
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
CN109824701A (zh) * 2019-03-26 2019-05-31 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
CN110850012A (zh) * 2018-08-21 2020-02-28 成都弘达药业有限公司 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
CN111646995A (zh) * 2019-03-04 2020-09-11 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
CN113278015A (zh) * 2021-05-31 2021-08-20 云南大学 一种荧光探针及其制备方法和应用
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

Families Citing this family (86)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1679668B1 (en) * 1996-09-04 2010-01-27 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
US20030133939A1 (en) 2001-01-17 2003-07-17 Genecraft, Inc. Binding domain-immunoglobulin fusion proteins
US7754208B2 (en) 2001-01-17 2010-07-13 Trubion Pharmaceuticals, Inc. Binding domain-immunoglobulin fusion proteins
PT1912675E (pt) 2005-07-25 2014-05-09 Emergent Product Dev Seattle Moléculas de ligaçao especificas para cd37 e especificas para cd20
MX380352B (es) 2006-06-12 2025-03-12 Aptevo Res & Development Llc Proteinas de union multivalentes monocatenarias con funcion efectora.
US7820665B2 (en) 2007-12-19 2010-10-26 Amgen Inc. Imidazopyridazine inhibitors of PI3 kinase for cancer treatment
RS51975B (sr) 2008-04-11 2012-02-29 Emergent Product Development Seattle Llc. Cd37 imunoterapeutski proizvod i njegova kombinacija sa bifunkcionalnim hemoterapeutskim sredstvom
TW201004963A (en) * 2008-07-03 2010-02-01 Targacept Inc Derivatives of oxabispidine as neuronal nicotinic acetylcholine receptor ligands
PE20110403A1 (es) * 2008-07-31 2011-07-04 Genentech Inc Compuestos biciclicos fusionados de pirimidina en el tratamiento del cancer
RS53350B (sr) 2008-09-22 2014-10-31 Array Biopharma, Inc. Supstituisana jedinjenja imidazo[1,2-b]piridazina kao inhibitori trk kinaze
TWI378933B (en) 2008-10-14 2012-12-11 Daiichi Sankyo Co Ltd Morpholinopurine derivatives
PT2725028T (pt) 2008-10-22 2016-08-31 Array Biopharma Inc Compostos de pirazolo[1,5-]pirimidina substituídos como intermediários na síntese de inibidores de cinase trk
DK2385832T3 (en) 2009-01-08 2015-09-21 Curis Inc Phosphoinositid-3-kinase-inhibitorer med en zink-bindingsdel
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
AU2010254161A1 (en) * 2009-05-27 2011-11-10 F. Hoffmann-La Roche Ag Bicyclic pyrimidine PI3K inhibitor compounds selective for p110 delta, and methods of use
US20100331305A1 (en) * 2009-06-24 2010-12-30 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
KR101447789B1 (ko) * 2009-11-12 2014-10-06 에프. 호프만-라 로슈 아게 N-7 치환된 퓨린 및 피라졸로피리미딘 화합물, 조성물 및 사용 방법
RU2607635C2 (ru) * 2009-11-12 2017-01-10 Ф.Хоффманн-Ля Рош Аг N-9-замещенные пуриновые соединения, композиции и способы применения
WO2011078795A1 (en) * 2009-12-21 2011-06-30 S*Bio Pte Ltd Bridged morpholino substituted purines
EP2525659B1 (en) 2010-01-19 2019-02-27 Merck Sharp & Dohme Corp. PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS mTOR INHIBITORS
EP2992878A1 (en) 2010-02-03 2016-03-09 Signal Pharmaceuticals, LLC Identification of lkb1 mutation as a predictive biomarker for sensitivity to tor kinase inhibitors
JP2013523807A (ja) 2010-04-05 2013-06-17 ワイス・エルエルシー Pi3kにより誘発される癌のためのバイオマーカー
HUE044025T2 (hu) 2010-05-20 2019-09-30 Array Biopharma Inc Makrociklusos vegyületek mint TRK-kináz inhibitorok
ES2986590T3 (es) 2010-06-14 2024-11-12 Scripps Research Inst Reprogramación de células hacia un nuevo destino
WO2012071519A1 (en) * 2010-11-24 2012-05-31 Exelixis, Inc. Benzoxazepines as inhibitors of p13k/mtor and methods of their use and manufacture
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
AU2012290056B2 (en) 2011-08-03 2015-03-19 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
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
UA125503C2 (uk) 2012-06-13 2022-04-13 Інсайт Холдинґс Корпорейшн Заміщені трициклічні сполуки як інгібітори 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
TWI654979B (zh) 2013-04-17 2019-04-01 美商標誌製藥公司 使用tor激酶抑制劑組合療法以治療癌症之方法
WO2014172431A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, 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
KR102221029B1 (ko) 2013-04-17 2021-02-26 시그날 파마소티칼 엘엘씨 디하이드로피라지노-피라진을 사용한 암의 치료
JP6382945B2 (ja) 2013-04-17 2018-08-29 シグナル ファーマシューティカルズ,エルエルシー ジヒドロピラジノ−ピラジンによる癌治療
WO2014172432A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer
KR102459285B1 (ko) 2013-04-17 2022-10-27 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
MY181497A (en) 2013-04-19 2020-12-23 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
CN113831345A (zh) 2013-05-29 2021-12-24 西格诺药品有限公司 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途
CN105764502A (zh) 2013-07-26 2016-07-13 现代化制药公司 改善比生群及其类似物及衍生物的治疗益处的组合方法
CN104513254B (zh) 2013-09-30 2019-07-26 上海璎黎药业有限公司 稠合嘧啶类化合物、中间体、其制备方法、组合物和应用
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
FI3699181T3 (fi) 2014-11-16 2023-03-28 Array Biopharma Inc Kiteinen muoto (s)-n-(5-((r)-2-(2,5-diluorifenyyli)-pyrrolidin-1-yyli)-pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidivetyysulfaatista
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
CR20170390A (es) 2015-02-20 2017-10-23 Incyte Holdings Corp Heterociclos biciclicos como inhibidores de fgfr
BR112018005573A2 (pt) 2015-09-21 2019-01-22 Aptevo Research And Development Llc ?polipeptídeos de ligação a cd3?
EP3368039A1 (en) 2015-10-26 2018-09-05 The Regents of The University of Colorado, A Body Corporate Point mutations in trk inhibitor-resistant cancer and methods relating to the same
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
RS65987B1 (sr) 2016-04-04 2024-10-31 Loxo Oncology Inc Tečne formulacije (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirolidin-1-il)-pirazolo[1,5-]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamida
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
EP3800189B1 (en) 2016-05-18 2023-06-28 Loxo Oncology, Inc. Preparation of (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
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
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
BR112020022392A2 (pt) 2018-05-04 2021-02-02 Incyte Corporation formas sólidas de um inibidor de fgfr e processos para preparação das mesmas
PE20210919A1 (es) 2018-05-04 2021-05-19 Incyte Corp Sales de un inhibidor de fgfr
MA54907A (fr) * 2019-02-06 2022-05-11 Venthera Inc Inhibiteurs de phosphoinositide 3-kinase topiques
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
EP3800188A1 (en) 2019-10-02 2021-04-07 Bayer AG Substituted pyrazolopyrimidines as irak4 inhibitors
GEP20247679B (en) 2019-10-14 2024-10-10 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JP7720840B2 (ja) 2019-12-04 2025-08-08 インサイト・コーポレイション Fgfr阻害剤としての三環式複素環
PE20221504A1 (es) 2019-12-04 2022-09-30 Incyte Corp Derivados de un inhibidor de fgfr
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
TW202304459A (zh) 2021-04-12 2023-02-01 美商英塞特公司 包含fgfr抑制劑及nectin-4靶向劑之組合療法
TW202313611A (zh) 2021-06-09 2023-04-01 美商英塞特公司 作為fgfr抑制劑之三環雜環
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3649395B2 (ja) 2000-04-27 2005-05-18 山之内製薬株式会社 縮合ヘテロアリール誘導体

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104080789A (zh) * 2012-01-31 2014-10-01 南京奥昭生物科技有限公司 作为布鲁顿酪氨酸激酶抑制剂的环状分子
CN104080789B (zh) * 2012-01-31 2016-05-11 南京奥昭生物科技有限公司 作为布鲁顿酪氨酸激酶抑制剂的环状分子
WO2013152717A1 (zh) * 2012-04-10 2013-10-17 上海昀怡健康管理咨询有限公司 稠合嘧啶类化合物,其制备方法,中间体,组合物和应用
US9499561B2 (en) 2012-04-10 2016-11-22 Shanghai Yingli Pharmaceutical Co., Ltd. Fused pyrimidine compound, and preparation method, intermediate, composition, and uses thereof
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
CN110850012A (zh) * 2018-08-21 2020-02-28 成都弘达药业有限公司 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
CN111646995A (zh) * 2019-03-04 2020-09-11 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
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
CN109824701A (zh) * 2019-03-26 2019-05-31 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
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
CN113278015A (zh) * 2021-05-31 2021-08-20 云南大学 一种荧光探针及其制备方法和应用
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

Also Published As

Publication number Publication date
EA201000484A1 (ru) 2010-12-30
CR11373A (es) 2010-05-03
AP2010005234A0 (en) 2010-04-30
AR068898A1 (es) 2009-12-16
BRPI0817681A2 (pt) 2015-04-14
IL205109A0 (en) 2010-11-30
WO2009052145A1 (en) 2009-04-23
JP2011500702A (ja) 2011-01-06
KR20100083170A (ko) 2010-07-21
CO6321257A2 (es) 2011-09-20
ZA201003430B (en) 2011-02-23
US8129371B2 (en) 2012-03-06
MX2010004260A (es) 2010-04-30
ECSP10010112A (es) 2010-08-31
CL2008003061A1 (es) 2009-01-09
AU2008312631A1 (en) 2009-04-23
TN2010000171A1 (fr) 2011-11-11
NI201000060A (es) 2010-10-04
PE20091384A1 (es) 2009-09-09
TW200922593A (en) 2009-06-01
EP2212333A1 (en) 2010-08-04
DOP2010000118A (es) 2010-06-30
MA31884B1 (fr) 2010-12-01
US20090098086A1 (en) 2009-04-16
PA8799101A1 (es) 2009-05-15
CA2702838A1 (en) 2009-04-23

Similar Documents

Publication Publication Date Title
CN101883774A (zh) 噻吩并嘧啶和吡唑并嘧啶化合物及其用作mtor激酶和pi3激酶抑制剂的用途
CN112638380B (zh) 小脑蛋白(crbn)配体
TWI657079B (zh) 苯并咪唑及咪唑并吡啶甲脒化合物
TWI710558B (zh) 二雜芳基化合物及其用途
ES2834027T3 (es) Compuestos de N-pirrolidinil, N'-pirazolil-urea como inhibidores de TrkA quinasa
CN101594871B (zh) 吡咯并嘧啶化合物及其用途
RU2537945C2 (ru) Триазиновые, пиримидиновые и пиридиновые аналоги и их применение в качестве терапевтических агентов и диагностических проб
CN104230831B (zh) 作为PI3激酶和mTOR抑制剂的三嗪化合物
CN103261167B (zh) 取代的6,6-稠合含氮杂环化合物及其用途
CN105452257B (zh) 新型稠合嘧啶化合物或其盐
TWI480282B (zh) 稠合雜環衍生物及其用途
CN102014914A (zh) 3h-[1,2,3]三唑并[4,5-d]嘧啶化合物、其作为mtor激酶和pi3激酶抑制剂的用途、以及它们的合成
TW202144345A (zh) Kras突變蛋白抑制劑
TW202024060A (zh) 稠環化合物
WO2020253862A1 (zh) 含氮芳基磷氧化物类衍生物、其制备方法和应用
WO2019037678A1 (zh) 吡唑并[3,4-d]嘧啶-3-酮衍生物、其药物组合物及应用
CN102762208A (zh) 作为ck2抑制剂的吡唑嘧啶和相关杂环
CN101687822A (zh) 二(芳基氨基)芳基化合物
KR20130086520A (ko) 스피로시클릭 화합물 및 이들의 치료제 및 진단 프로브로서 용도
CN110818724A (zh) 吡啶酮和氮杂吡啶酮化合物及使用方法
JP2018515612A (ja) 置換キノキサリン誘導体
CN108884097B (zh) 嘧啶类衍生物、其制备方法和其在医药上的用途
CN102711766A (zh) N-9-取代的嘌呤化合物、组合物和使用方法
CN104177363A (zh) 双环杂环胺类Hedgehog信号通路抑制剂
RU2809631C2 (ru) Пиразиновые соединения и их применения

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20101110