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

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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
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phenyl
oxa
pyrimidine
azabicyclo
pyrazolo
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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
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Wyeth LLC
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  • 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)
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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)

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CN101883774A true CN101883774A (zh) 2010-11-10

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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

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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
EP0974129B1 (en) * 1996-09-04 2006-08-16 Intertrust Technologies Corp. Trusted infrastructure support systems, methods and techniques for secure electronic commerce, electronic transactions, commerce process control and automation, distributed computing, and rights management
US7754208B2 (en) 2001-01-17 2010-07-13 Trubion Pharmaceuticals, Inc. Binding domain-immunoglobulin fusion proteins
US20030133939A1 (en) 2001-01-17 2003-07-17 Genecraft, Inc. Binding domain-immunoglobulin fusion proteins
SI1912675T1 (sl) 2005-07-25 2014-07-31 Emergent Product Development Seattle, Llc zmanjšanje števila celic B z uporabo molekul, ki se specifično vežejo na CD37 in CD20
EP2418223A3 (en) 2006-06-12 2013-01-16 Emergent Product Development Seattle, LLC Single-chain multivalent binding proteins with effector function
WO2009085230A1 (en) 2007-12-19 2009-07-09 Amgen Inc. Inhibitors of pi3 kinase
SG189772A1 (en) 2008-04-11 2013-05-31 Trubion Pharmaceuticals Inc Cd37 immunotherapeutic and combination with bifunctional chemotherapeutic thereof
TW201004963A (en) * 2008-07-03 2010-02-01 Targacept Inc Derivatives of oxabispidine as neuronal nicotinic acetylcholine receptor ligands
EP2318377B1 (en) * 2008-07-31 2013-08-21 Genentech, Inc. Pyrimidine compounds, compositions and methods of use
EP2350075B1 (en) 2008-09-22 2014-03-05 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
KR101853026B1 (ko) 2008-10-22 2018-04-27 어레이 바이오파마 인크. ＴＲＫ 키나아제 억제제로서 치환된 피라졸로［１,５­ａ］ 피리미딘 화합물
EA024252B1 (ru) 2009-01-08 2016-08-31 Кьюрис, Инк. Ингибиторы фосфоинозитид-3-киназ с цинксвязывающей группой
US8835429B2 (en) * 2009-04-17 2014-09-16 Wyeth Llc Pyrimidine compounds, their use as mTOR kinase and Pl3 kinase inhibitors, and their syntheses
SG175708A1 (en) * 2009-05-27 2011-12-29 Genentech Inc 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
BR112012011188A2 (pt) * 2009-11-12 2021-06-29 F.Hoffmann - La Roche Ag ''composto,composição farmacêutica e uso de um composto"
US8828990B2 (en) 2009-11-12 2014-09-09 Genentech, Inc. N-7 substituted purine and pyrazolopyrimine compounds, compositions and methods of use
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
MX2012009030A (es) 2010-02-03 2012-09-12 Signal Pharm Llc Identificacion de mutacion lkb1 como biomarcador predictivo para sensibilidad a inhibidores de tor cinasa.
WO2011125012A1 (en) 2010-04-05 2011-10-13 Wyeth Llc Biomarkers for p13k-driven cancer
CN105693720B (zh) 2010-05-20 2019-01-18 阵列生物制药公司 作为trk激酶抑制剂的大环化合物
EP3399026B1 (en) 2010-06-14 2024-06-26 The Scripps Research Institute Reprogramming of cells to a new fate
EA201390766A1 (ru) * 2010-11-24 2013-11-29 Экселиксис, Инк. БЕНЗОКСАЗЕПИНЫ КАК ИНГИБИТОРЫ PI3K/mTOR И СПОСОБЫ ИХ ИСПОЛЬЗОВАНИЯ И ПОЛУЧЕНИЯ
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
WO2012099581A1 (en) 2011-01-19 2012-07-26 Takeda Pharmaceutical Company Limited Dihydrofuropyrimidine compounds
MX2014001246A (es) 2011-08-03 2014-06-11 Signal Pharm Llc Identificación del perfil de la expresión génica como biomarcador predictivo del estatus de lkb1.
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
RU2014149145A (ru) 2012-05-23 2016-07-20 Ф. Хоффманн-Ля Рош Аг Композиции и способы получения и применения эндодермальных клеток и гепатоцитов
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
ES2984771T3 (es) 2012-06-13 2024-10-31 Incyte Holdings Corp Compuestos tricíclicos sustituidos como inhibidores de FGFR
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
AU2013203714B2 (en) 2012-10-18 2015-12-03 Signal Pharmaceuticals, Llc Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
MX374749B (es) 2013-04-17 2025-03-06 Signal Pharm Llc Terapia de combinacion que comprende un inhibidor de tor cinasa y un analogo de citidina para tratar cancer.
NZ629469A (en) 2013-04-17 2017-05-26 Signal Pharm Llc Methods for treating cancer using dihydropyrazino-pyrazine compound combination therapy
EP2986322A1 (en) 2013-04-17 2016-02-24 Signal Pharmaceuticals, LLC Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating 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
NZ629411A (en) 2013-04-17 2017-06-30 Signal Pharm Llc Treatment of cancer with dihydropyrazino-pyrazines
NZ629230A (en) 2013-04-17 2017-05-26 Signal Pharm Llc Pharmaceutical formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one
NZ629332A (en) 2013-04-17 2017-05-26 Signal Pharm Llc Treatment of cancer with dihydropyrazino-pyrazines
EA035095B1 (ru) 2013-04-19 2020-04-27 Инсайт Холдингс Корпорейшн Бициклические гетероциклы в качестве ингибиторов fgfr
HK1223286A1 (zh) 2013-05-29 2017-07-28 西格诺药品有限公司 7-(6-(2-羟基丙-2-基)吡啶-3-基)-1-((反式)-4-甲氧基环己基)-3，4-二氢吡嗪并[2，3-b]吡嗪-2(1h)-酮的药物组合物、其固体形式及它们的使用方法
KR20160099081A (ko) 2013-07-26 2016-08-19 업데이트 파마 인코포레이트 비산트렌의 치료 효과 개선용 조합 방법
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
PE20161475A1 (es) * 2014-05-14 2017-01-08 Pfizer Pirazolopiridinas y pirazolopirimidinas
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
TWI746426B (zh) 2014-11-16 2021-11-21 美商亞雷生物製藥股份有限公司 (S)-N-(5-((R)-2-(2,5-二氟苯基)-吡咯啶-1-基)-吡唑并[1,5-a]嘧啶-3-基)-3-羥基吡咯啶-1-甲醯胺硫酸氫鹽結晶型
EA038045B1 (ru) 2015-02-20 2021-06-28 Инсайт Корпорейшн Бициклические гетероциклы в качестве ингибиторов fgfr
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
UA126278C2 (uk) 2015-09-21 2022-09-14 Аптево Рісьорч Енд Девелопмент Ллс Поліпептиди, які зв'язують cd3
TN2018000138A1 (en) 2015-10-26 2019-10-04 Array Biopharma Inc 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
HUE068971T2 (hu) 2016-04-04 2025-02-28 Loxo Oncology Inc (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-A]pirimidin-3-il) -3-hidroxipirrolidin-1-karboxamid folyékony készítményei
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
SI3458456T1 (sl) 2016-05-18 2021-04-30 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
MY198676A (en) 2017-06-22 2023-09-15 Celgene Corp Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection
US11666888B2 (en) 2018-02-05 2023-06-06 Bio-Rad Laboratories, Inc. Chromatography resin having an anionic exchange-hydrophobic mixed mode ligand
US11174257B2 (en) 2018-05-04 2021-11-16 Incyte Corporation Salts of an FGFR inhibitor
RS66310B1 (sr) 2018-05-04 2025-01-31 Incyte Corp Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu
MX2021009142A (es) * 2019-02-06 2021-10-13 Venthera Inc Inhibidores topicos de fosfoinositol 3-cinasas.
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
EP3800188A1 (en) 2019-10-02 2021-04-07 Bayer AG Substituted pyrazolopyrimidines as irak4 inhibitors
PH12022550892A1 (en) 2019-10-14 2023-05-03 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
JP2024513575A (ja) 2021-04-12 2024-03-26 インサイト・コーポレイション Ｆｇｆｒ阻害剤及びネクチン－４標的化剤を含む併用療法
WO2022261160A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
TW202313610A (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

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001083456A1 (en) 2000-04-27 2001-11-08 Yamanouchi Pharmaceutical Co., Ltd. Condensed heteroaryl derivatives

Cited By (12)

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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
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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
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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

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