JP2013541561A5 - - Google Patents

Download PDF

Info

Publication number
JP2013541561A5
JP2013541561A5 JP2013536908A JP2013536908A JP2013541561A5 JP 2013541561 A5 JP2013541561 A5 JP 2013541561A5 JP 2013536908 A JP2013536908 A JP 2013536908A JP 2013536908 A JP2013536908 A JP 2013536908A JP 2013541561 A5 JP2013541561 A5 JP 2013541561A5
Authority
JP
Japan
Prior art keywords
item
composition
compound
compound according
pharmaceutically acceptable
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.)
Granted
Application number
JP2013536908A
Other languages
English (en)
Japanese (ja)
Other versions
JP5957460B2 (ja
JP2013541561A (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/US2011/058610 external-priority patent/WO2012061299A1/en
Publication of JP2013541561A publication Critical patent/JP2013541561A/ja
Publication of JP2013541561A5 publication Critical patent/JP2013541561A5/ja
Application granted granted Critical
Publication of JP5957460B2 publication Critical patent/JP5957460B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

JP2013536908A 2010-11-01 2011-10-31 複素環式化合物またはその使用 Expired - Fee Related JP5957460B2 (ja)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US40908010P 2010-11-01 2010-11-01
US61/409,080 2010-11-01
US41182910P 2010-11-09 2010-11-09
US61/411,829 2010-11-09
US41233010P 2010-11-10 2010-11-10
US61/412,330 2010-11-10
US201161534323P 2011-09-13 2011-09-13
US61/534,323 2011-09-13
PCT/US2011/058610 WO2012061299A1 (en) 2010-11-01 2011-10-31 Heterocyclic compounds and uses thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2016121575A Division JP6778512B2 (ja) 2010-11-01 2016-06-20 複素環式化合物またはその使用

Publications (3)

Publication Number Publication Date
JP2013541561A JP2013541561A (ja) 2013-11-14
JP2013541561A5 true JP2013541561A5 (enExample) 2014-11-27
JP5957460B2 JP5957460B2 (ja) 2016-07-27

Family

ID=46024790

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2013536908A Expired - Fee Related JP5957460B2 (ja) 2010-11-01 2011-10-31 複素環式化合物またはその使用
JP2016121575A Expired - Fee Related JP6778512B2 (ja) 2010-11-01 2016-06-20 複素環式化合物またはその使用

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2016121575A Expired - Fee Related JP6778512B2 (ja) 2010-11-01 2016-06-20 複素環式化合物またはその使用

Country Status (19)

Country Link
US (6) US8975249B2 (enExample)
EP (1) EP2635284B1 (enExample)
JP (2) JP5957460B2 (enExample)
KR (1) KR101954593B1 (enExample)
CN (1) CN103269704B (enExample)
AR (1) AR083676A1 (enExample)
BR (1) BR112013010564B1 (enExample)
CA (1) CA2815858C (enExample)
ES (1) ES2776002T3 (enExample)
IL (2) IL225883A (enExample)
MX (2) MX382354B (enExample)
MY (1) MY181898A (enExample)
NZ (2) NZ609957A (enExample)
PH (2) PH12013500870A1 (enExample)
RU (1) RU2644151C2 (enExample)
SG (2) SG190116A1 (enExample)
TW (2) TWI632134B (enExample)
WO (1) WO2012061299A1 (enExample)
ZA (1) ZA201304009B (enExample)

Families Citing this family (75)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011523646A (ja) 2008-05-21 2011-08-18 アリアド・ファーマシューティカルズ・インコーポレイテッド キナーゼ阻害剤としてのリン誘導体
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
AU2009262068C1 (en) 2008-06-27 2015-07-02 Celgene Car Llc Heteroaryl compounds and uses thereof
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
KR101705158B1 (ko) 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Ｅｇｆｒ 억제제 및 질환 치료방법
PH12013500246A1 (en) 2010-08-10 2019-10-11 Celgene Avilomics Res Inc Besylate salt of a btk inhibitor
BR112013010564B1 (pt) * 2010-11-01 2021-09-21 Celgene Car Llc Compostos heterocíclicos e composições compreendendo os mesmos
JP5956999B2 (ja) * 2010-11-01 2016-07-27 セルジーン アヴィロミクス リサーチ， インコーポレイテッド ヘテロアリール化合物およびその使用
EP2637502B1 (en) 2010-11-10 2018-01-10 Celgene CAR LLC Mutant-selective egfr inhibitors and uses thereof
AU2012250517B2 (en) 2011-05-04 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
JP2014532658A (ja) 2011-10-28 2014-12-08 セルジーン アヴィロミクス リサーチ， インコーポレイテッド ブルトン型チロシンキナーゼ疾患または障害を治療する方法
US9586965B2 (en) 2012-01-13 2017-03-07 Acea Biosciences Inc. Pyrrolo[2,3-d]pyrimidine compounds as inhibitors of protein kinases
US9034885B2 (en) 2012-01-13 2015-05-19 Acea Biosciences Inc. EGFR modulators and uses thereof
CA2861010A1 (en) 2012-01-13 2013-07-18 Xiao Xu Heterocyclic compounds and uses as anticancer agents
US9464089B2 (en) 2012-01-13 2016-10-11 Acea Biosciences Inc. Heterocyclic compounds and uses thereof
US8889666B2 (en) * 2012-02-23 2014-11-18 Taiho Pharmaceutical Co., Ltd. Quinolyl pyrrolo pyrimidyl condensed-ring compound and salt thereof
JP6317320B2 (ja) 2012-03-15 2018-04-25 セルジーン シーエーアール エルエルシー 上皮成長因子受容体キナーゼ阻害剤の塩
ES2880109T3 (es) * 2012-03-15 2021-11-23 Celgene Car Llc Formas sólidas de un inhibidor de la cinasa del receptor del factor de crecimiento epidérmico
JP6469567B2 (ja) 2012-05-05 2019-02-13 アリアド・ファーマシューティカルズ・インコーポレイテッド Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物
US9126950B2 (en) 2012-12-21 2015-09-08 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
CN105188371A (zh) 2013-02-08 2015-12-23 西建阿维拉米斯研究公司 Erk抑制剂及其用途
KR20150119401A (ko) 2013-02-22 2015-10-23 다이호야쿠힌고교 가부시키가이샤 3환성 화합물의 제조 방법 및 상기 제조 방법에 의해 얻을 수 있는 3환성 화합물
US9346801B2 (en) 2013-03-01 2016-05-24 Amgen Inc. Substituted 7-oxo-pyrido[2,3-d]pyrimidines and methods of use
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
EP2994456A4 (en) * 2013-05-06 2017-01-04 Clovis Oncology, Inc. Salts of an epidermal growth factor receptor kinase inhibitor
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
BR112016000195A8 (pt) * 2013-07-11 2019-12-31 Acea Biosciences Inc compostos heterocíclicos, composição farmacêutica, combinação, seu uso, e método para inibir uma atividade da tirosina quinase btk ou jak, egfr, alk, pdgfr, blk, bmx/etk, flt3(d835y), itk, tec, txk, e suas respectivas vias
US9492471B2 (en) 2013-08-27 2016-11-15 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase
US9415049B2 (en) 2013-12-20 2016-08-16 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
NO2718543T3 (enExample) * 2014-02-04 2018-01-06
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
US9879008B2 (en) 2014-04-14 2018-01-30 Shanghai Haiyan Pharmaceutical Technology Co., Ltd. 2,3,4,6-tetra-substituted benzene-1,5-diamine derivatives, preparation method therefor and medicinal use thereof
CN106536503B (zh) * 2014-04-18 2019-09-06 北京澳合药物研究院有限公司 一种酪氨酸激酶抑制剂及其用途
CN104130265B (zh) * 2014-04-29 2017-01-25 苏州景泓生物技术有限公司 一种含有螺环或桥环的嘧啶类化合物
CN105315259B (zh) 2014-07-29 2018-03-09 上海艾力斯医药科技有限公司 吡啶胺基嘧啶衍生物、其制备方法及应用
WO2016025561A1 (en) 2014-08-13 2016-02-18 Celgene Avilomics Research, Inc. Forms and compositions of an erk inhibitor
CN105384694B (zh) * 2014-08-22 2020-09-04 四川海思科制药有限公司 一种取代的氨基嘧啶衍生物及其制备方法和药物用途
CN105384695B (zh) * 2014-08-22 2019-12-20 四川海思科制药有限公司 嘧啶衍生物及其制备方法和在医药上的应用
UA120108C2 (uk) * 2014-12-12 2019-10-10 Мерк Патент Гмбх Комбінація похідної 6-оксо-1,6-дигідропіридазину, що має протиракову активність, з інгібітором рефр
CN104961688A (zh) * 2014-12-25 2015-10-07 苏州晶云药物科技有限公司 一种表皮生长因子受体激酶抑制剂的磷酸盐及其制备方法
CN105884695B (zh) * 2015-02-13 2019-02-26 山东轩竹医药科技有限公司 杂环衍生物类酪氨酸激酶抑制剂
CN105985318A (zh) * 2015-02-15 2016-10-05 宁波文达医药科技有限公司 作为t790变异抑制剂的嘧啶衍生物
CN104860890B (zh) * 2015-04-29 2018-03-13 上海泓博智源医药股份有限公司 T790m突变型egfr的抑制剂及其在制备抗肿瘤药物中的应用
WO2016185333A1 (en) 2015-05-15 2016-11-24 Novartis Ag Methods for treating egfr mutant cancers
CN106554347B (zh) 2015-09-25 2020-10-30 浙江博生医药有限公司 Egfr激酶抑制剂及其制备方法和应用
EP3359159B1 (en) 2015-10-09 2023-06-07 ACEA Therapeutics, Inc. Pharmaceutical compositions of a pyrrolopyrimidine kinase inhibitor, and methods of making same
CN106608868A (zh) * 2015-10-21 2017-05-03 复旦大学 5-(硫醚基)嘧啶类化合物及其药用组合物和应用
CN105198821B (zh) 2015-10-26 2017-12-05 苏州明锐医药科技有限公司 洛昔替尼的制备方法
CN105461640B (zh) * 2015-12-02 2017-11-21 芷威（上海）化学科技有限公司 一种酪氨酸激酶抑制剂的制备方法
CN105481779B (zh) * 2015-12-24 2019-01-25 南京华威医药科技集团有限公司 抗癌药物Rociletinib及其中间体制备
CN106146406A (zh) * 2016-02-23 2016-11-23 深圳市塔吉瑞生物医药有限公司 一种取代的二氨基嘧啶类化合物及包含该化合物的组合物及其用途
CN107540661A (zh) * 2016-06-24 2018-01-05 正大天晴药业集团股份有限公司 作为egfr抑制剂的苯胺嘧啶化合物的结晶
IL263815B (en) 2016-06-29 2022-07-01 Principia Biopharma Inc Modified release formulations of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[4,3-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4 -Methyl-4-[4-(Oxtan-3-yl)piperazin-1-yl)pent-2-ananitrile
CN106243044A (zh) * 2016-06-30 2016-12-21 浙江大学 含卤代丙烯酰胺侧链的嘧啶类衍生物及制备和应用
CN106565612B (zh) * 2016-10-25 2018-10-16 大连医科大学 二苯乙烯基嘧啶类化合物，组合物及其用途
CN110753693A (zh) 2016-12-23 2020-02-04 阿尔维纳斯运营股份有限公司 Egfr蛋白水解靶向嵌合分子和相关使用方法
CN106916112B (zh) * 2017-03-02 2019-12-20 四川海思科制药有限公司 嘧啶衍生物及其制备方法和在医药上的应用
EP3596086A4 (en) * 2017-03-16 2020-12-16 Celgene CAR LLC MK2 INHIBITORS, THEIR SYNTHESIS AND THEIR INTERMEDIARIES
AU2017408099A1 (en) 2017-04-07 2019-11-07 ACEA Therapeutics, Inc. Pharmaceutical salts, physical forms, and compositions of pyrrolopyrimidine kinase inhibitors, and methods of making same
KR101936054B1 (ko) 2017-06-23 2019-01-11 한국과학기술연구원 항염증 활성을 가지는 6-페녹시피리미딘 유도체, 이의 제조방법 및 이를 활성성분으로 하는 약학 조성물
UA127380C2 (uk) * 2017-11-02 2023-08-02 Ле Лаборатуар Сервье Співкристали, фармацевтичні композиції на їх основі та способи лікування, які передбачають їх застосування
CN108530450B (zh) * 2018-05-03 2021-03-30 赖建智 具有egfr抑制活性的化合物、制备方法及其在疾病治疗中的应用
ES2980434T3 (es) 2018-07-21 2024-10-01 Linnaeus Therapeutics Inc Agonista de GPER enantioméricamente purificado para su uso en el tratamiento de estados patológicos y afecciones
WO2020051571A1 (en) * 2018-09-07 2020-03-12 H. Lee Moffitt Cancer Center And Research Institute, Inc. Brd4-jak2 inhibitors
WO2020051572A1 (en) * 2018-09-07 2020-03-12 H. Lee Moffitt Cancer Center And Research Institute, Inc. Brd4-jak2 inhibitors
AU2020365951B2 (en) 2019-10-14 2026-07-16 Principia Biopharma Inc. Methods for treating immune thrombocytopenia by administering (R)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
KR102993352B1 (ko) 2019-12-20 2026-07-22 프린시피아 바이오파마, 인코퍼레이티드 2-[3-[4-아미노-3-(2-플루오로-4-페녹시-페닐)피라졸로[3,4-d]피리미딘-1-일]피페리딘-1-카르보닐]-4-메틸-4-[4-(옥세탄-3-일)피페라진-1-일]펜트-2-에네니트릴의 고체 형태
WO2021150723A1 (en) 2020-01-22 2021-07-29 Principia Biopharma Inc. Crystalline forms of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-1h-pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
CN116490201A (zh) 2020-07-02 2023-07-25 布里奇恩生物科学公司 Yap/taz-tead肿瘤蛋白的抑制剂，其合成和用途
CN116685583A (zh) * 2020-10-30 2023-09-01 缆图药品公司 嘧啶化合物、组合物及其医药应用
EP4237418B1 (en) 2020-10-30 2026-02-11 Blueprint Medicines Corporation Pyrimidine compounds, compositions, and medicinal applications thereof
JP2024523861A (ja) 2021-06-15 2024-07-02 ジェネンテック， インコーポレイテッド がんを処置するための併用療法におけるｅｇｆｒ阻害剤およびｐｅｒｋ活性化剤、ならびにこれらの使用
CN114213339B (zh) * 2021-12-20 2023-10-31 苏州康纯医药科技有限公司 一种表皮细胞生长因子受体突变抑制剂的制备方法

Family Cites Families (169)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4032637A (en) 1972-09-26 1977-06-28 Sandoz Ltd. Method of promoting sleep
GB8608335D0 (en) 1986-04-04 1986-05-08 Pfizer Ltd Pharmaceutically acceptable salts
US5453510A (en) 1990-07-13 1995-09-26 Burroughs Wellcome Co. Neuromuscular blocking agents
JPH0741461A (ja) 1993-05-27 1995-02-10 Eisai Co Ltd スルホン酸エステル誘導体
EP0813525B9 (en) 1995-03-10 2004-02-04 Berlex Laboratories, Inc. Benzamidine derivatives their preparation and their use as anti-coagulants
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
GB9619284D0 (en) 1996-09-16 1996-10-30 Celltech Therapeutics Ltd Chemical compounds
GB9622363D0 (en) 1996-10-28 1997-01-08 Celltech Therapeutics Ltd Chemical compounds
ATE401312T1 (de) 1997-12-15 2008-08-15 Astellas Pharma Inc Pyrimidin-5-carboxamid-derivate
US6303652B1 (en) 1998-08-21 2001-10-16 Hughes Institute BTK inhibitors and methods for their identification and use
AU5438299A (en) 1998-08-29 2000-03-21 Astrazeneca Ab Pyrimidine compounds
ID28376A (id) 1998-11-10 2001-05-17 Janssen Pharmaceutica Nv Pirimidina yang menghambat replikasi hiv
US6262088B1 (en) 1998-11-19 2001-07-17 Berlex Laboratories, Inc. Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants
US6127376A (en) 1998-12-04 2000-10-03 Berlex Laboratories, Inc. Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants
GB9828511D0 (en) 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
US6495558B1 (en) 1999-01-22 2002-12-17 Amgen Inc. Kinase inhibitors
EP1150955A2 (en) 1999-02-04 2001-11-07 Millennium Pharmaceuticals, Inc. G-protein coupled heptahelical receptor binding compounds and methods of use thereof
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
AU5835400A (en) 1999-06-29 2001-01-31 Egis Gyogyszergyar Rt. Novel piperazinylalkylthiopyrimidine derivatives, pharmaceutical compositions containing the same, and process for the preparation of the active substance
CA2396693A1 (en) 1999-12-28 2001-07-05 Stephen T. Wrobleski Cytokine, especially tnf-alpha, inhibitors
KR20030024659A (ko) 2000-02-17 2003-03-26 암겐 인코포레이티드 키나제 억제제
GB0004887D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004888D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US7034019B2 (en) 2000-05-08 2006-04-25 Janssen Pharmaceutica N.V. Prodrugs of HIV replication inhibiting pyrimidines
GB0016877D0 (en) 2000-07-11 2000-08-30 Astrazeneca Ab Chemical compounds
CA2417500C (en) 2000-07-28 2008-11-18 Georgetown University Medical Center Erbb-2 selective small molecule kinase inhibitors
US6881737B2 (en) 2001-04-11 2005-04-19 Amgen Inc. Substituted triazinyl acrylamide derivatives and methods of use
JO3429B1 (ar) 2001-08-13 2019-10-20 Janssen Pharmaceutica Nv مشتقات برميدينات مثبطة فيروس الايدز
US6939874B2 (en) 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
WO2003030909A1 (en) 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
IL161662A0 (en) 2001-11-01 2004-09-27 Janssen Pharmaceutica Nv Heteroaryl amines as glycogen synthase kinase 3 beta inhibitors (gsk3 inhibitors)
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
US7459455B2 (en) 2002-02-08 2008-12-02 Smithkline Beecham Corporation Pyrimidine compounds
GB0206215D0 (en) 2002-03-15 2002-05-01 Novartis Ag Organic compounds
WO2003081210A2 (en) 2002-03-21 2003-10-02 Sunesis Pharmaceuticals, Inc. Identification of kinase inhibitors
US20040002395A1 (en) 2002-06-27 2004-01-01 Poynor Raymond L. Bridge weight for metal wood golf club
IL166241A0 (en) 2002-07-29 2006-01-15 Rigel Pharmaceuticals Inc Method of treating or preventing autoimmune diseases with 2,4-pyrimidinedinediamine compounds
CA2439440A1 (en) 2002-09-05 2004-03-05 Emory University Treatment of tuberous sclerosis associated neoplasms
AU2002951853A0 (en) 2002-10-04 2002-10-24 Commonwealth Scientific And Industrial Research Organisation Crystal structure of erbb2 and uses thereof
AU2002350719A1 (en) 2002-11-29 2004-06-23 Janssen Pharmaceutica N.V. Pharmaceutical compositions comprising a basic respectively acidic drug compound, a surfactant and a physiologically tolerable water-soluble acid respectively base
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
EP1597237B1 (en) 2003-02-07 2016-07-27 Janssen Pharmaceutica NV Pyrimidine derivatives for the prevention of HIV infection
ES2325440T3 (es) 2003-02-20 2009-09-04 Smithkline Beecham Corporation Compuestos de pirimidina.
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
US20050014753A1 (en) 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
US20050043233A1 (en) 2003-04-29 2005-02-24 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis
US7504396B2 (en) 2003-06-24 2009-03-17 Amgen Inc. Substituted heterocyclic compounds and methods of use
ES2421139T3 (es) 2003-07-30 2013-08-29 Rigel Pharmaceuticals, Inc. Compuestos de 2,4-pirimidindiamina para su uso en el tratamiento o la prevención de enfermedades autoinmunitarias
DK1663242T3 (da) 2003-08-07 2011-08-01 Rigel Pharmaceuticals Inc 2,4-Pyrimidindiamin-forbindelser og anvendelse som antiproliferative midler
ATE542801T1 (de) 2003-08-15 2012-02-15 Novartis Ag Zur behandlung von neoplastischen krankheiten, entzündlichen erkrankungen und erkrankungen des immunsystems geeignete 2,4-pyrimidindiamine
GB0321710D0 (en) 2003-09-16 2003-10-15 Novartis Ag Organic compounds
AU2004272288B2 (en) 2003-09-18 2008-11-13 Novartis Ag 2,4-di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
EP1694652A1 (en) 2003-12-19 2006-08-30 Rigel Pharmaceuticals, Inc. Stereoisomers and stereoisomeric mixtures of 1-(2,4-pyrimidinediamino)-2-cyclopentanecarboxamide synthetic intermediates
ES2389203T3 (es) 2004-01-12 2012-10-24 Ym Biosciences Australia Pty Ltd Inhibidores de quinasa selectivos
CN1930128A (zh) 2004-01-16 2007-03-14 惠氏公司 受体酪氨酸激酶抑制剂的喹啉中间体及其合成
US7378448B2 (en) 2004-03-15 2008-05-27 Eli Lilly And Company Diphenylether amide derivatives as opioid receptor antagonists
WO2005105988A2 (en) 2004-04-28 2005-11-10 Vertex Pharmaceuticals Incorporated Crystal structure of human jak3 kinase domain complex and binding pockets thereof
JP4812763B2 (ja) 2004-05-18 2011-11-09 ライジェル ファーマシューティカルズ， インコーポレイテッド シクロアルキル置換ピリミジンジアミン化合物およびそれらの用途
EP1598343A1 (de) 2004-05-19 2005-11-23 Boehringer Ingelheim International GmbH 2-Arylaminopyrimidine als PLK Inhibitoren
AU2005250484B2 (en) 2004-06-04 2011-08-11 Genentech, Inc. EGFR mutations
US7521457B2 (en) 2004-08-20 2009-04-21 Boehringer Ingelheim International Gmbh Pyrimidines as PLK inhibitors
GB0419161D0 (en) 2004-08-27 2004-09-29 Novartis Ag Organic compounds
EP1805142A4 (en) 2004-09-23 2009-06-10 Reddy Us Therapeutics Inc PYRIDINE-BASED COMPOUNDS, PROCESS FOR THEIR PREPARATION AND COMPOSITIONS CONTAINING SAME
ATE520672T1 (de) 2004-09-30 2011-09-15 Tibotec Pharm Ltd Hiv-hemmende 5-carbo- oder heterozyklisch substituierte pyrimidine
US7799915B2 (en) 2004-10-13 2010-09-21 Wyeth Llc Anilino-pyrimidine analogs
EP2100899A3 (en) 2004-10-20 2009-09-30 Proteolix, Inc. Compounds for proteasome enzyme inhibition
WO2006053109A1 (en) 2004-11-10 2006-05-18 Synta Pharmaceuticals Corp. Heteroaryl compounds
GB2420559B (en) 2004-11-15 2008-08-06 Rigel Pharmaceuticals Inc Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
ATE540035T1 (de) 2004-11-24 2012-01-15 Rigel Pharmaceuticals Inc Spiro-2,4-pyrimidindiamin-verbindungen und ihre verwendungen
MY169441A (en) 2004-12-08 2019-04-11 Janssen Pharmaceutica Nv 2,4, (4,6) pyrimidine derivatives
US8211929B2 (en) 2004-12-30 2012-07-03 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
AU2006204724A1 (en) 2005-01-14 2006-07-20 Millennium Pharmaceuticals, Inc. Cinnamide and hydrocinnamide derivatives with raf-kinase inhibitory activity
US7449458B2 (en) 2005-01-19 2008-11-11 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
WO2006086777A2 (en) 2005-02-11 2006-08-17 Memorial Sloan Kettering Cancer Center Methods and compositions for detecting a drug resistant egfr mutant
WO2006101977A2 (en) 2005-03-16 2006-09-28 Targegen, Inc. Pyrimidine compounds and methods of use
DE102005016634A1 (de) 2005-04-12 2006-10-19 Merck Patent Gmbh Neuartige Aza-Hetercyclen als Kinase-Inhibitoren
JP2008540436A (ja) 2005-05-03 2008-11-20 ライジェル ファーマシューティカルズ， インコーポレイテッド Ｊａｋキナーゼインヒビターおよびそれらの使用
WO2006124874A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
WO2006128172A2 (en) 2005-05-26 2006-11-30 Synta Pharmaceuticals Corp. Method for treating b cell regulated autoimmune disorders
WO2006128129A2 (en) 2005-05-26 2006-11-30 Synta Pharmaceuticals Corp. Method for treating cancer
WO2006129100A1 (en) 2005-06-03 2006-12-07 Glaxo Group Limited Novel compounds
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2006133426A2 (en) 2005-06-08 2006-12-14 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
TWI377198B (en) * 2005-08-24 2012-11-21 Eisai R&D Man Co Ltd Novel pyridine derivatives and pyrimidine derivatives (3)
CA2626789A1 (en) 2005-10-21 2007-04-26 Exelixis, Inc. Pyrimidinones as casein kinase ii (ck2) modulators
WO2007053452A1 (en) 2005-11-01 2007-05-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
CA2626479A1 (en) 2005-11-03 2007-05-18 Irm Llc Protein kinase inhibitors
US7713987B2 (en) 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
JP2009520038A (ja) 2005-12-19 2009-05-21 ジェネンテック・インコーポレーテッド ピリミジンキナーゼインヒビター
TW200736232A (en) 2006-01-26 2007-10-01 Astrazeneca Ab Pyrimidine derivatives
EA200870217A1 (ru) 2006-01-30 2009-02-27 Экселиксис, Инк. 4-арил-2-аминопиримидины или 4-арил-2-аминоалкилпиримидины в качестве модуляторов jak-2 и содержащие их фармацевтические композиции
KR101411695B1 (ko) 2006-02-17 2014-07-03 리겔 파마슈티칼스, 인크. 자가면역 질환의 치료 또는 예방을 위한 2,4-피리미딘디아민 화합물
WO2007098507A2 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
ES2353725T3 (es) 2006-03-30 2011-03-04 Tibotec Pharmaceuticals Pirimidinas sustituidas con 5-(hidroximetileno y aminometileno) que inhiben el vih.
AU2007233737B2 (en) 2006-03-30 2012-11-29 Janssen Sciences Ireland Uc HIV inhibiting 5-amido substituted pyrimidines
GB0608386D0 (en) 2006-04-27 2006-06-07 Senexis Ltd Compounds
US7560588B2 (en) 2006-04-27 2009-07-14 Intezyne Technologies, Inc. Poly(ethylene glycol) containing chemically disparate endgroups
US8604031B2 (en) 2006-05-18 2013-12-10 Mannkind Corporation Intracellular kinase inhibitors
DE102006027156A1 (de) 2006-06-08 2007-12-13 Bayer Schering Pharma Ag Sulfimide als Proteinkinaseinhibitoren
AU2007269540B2 (en) 2006-07-05 2013-06-27 Exelixis, Inc. Methods of using IGF1R and Abl kinase modulators
WO2008009458A1 (en) 2006-07-21 2008-01-24 Novartis Ag 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors
DE102006041382A1 (de) 2006-08-29 2008-03-20 Bayer Schering Pharma Ag Carbamoyl-Sulfoximide als Proteinkinaseinhibitoren
EP2529621B1 (en) 2006-09-22 2016-10-05 Pharmacyclics LLC Inhibitors of bruton's tyrosine kinase
DK2089369T3 (da) 2006-10-19 2011-05-09 Rigel Pharmaceuticals Inc 2,4-pyrimidindiaminderivater som hæmmere af JAK-kinaser til behandling af autoimmune sygdomme
WO2008054827A2 (en) 2006-11-03 2008-05-08 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
WO2008064274A1 (en) 2006-11-21 2008-05-29 Rigel Pharmaceuticals, Inc. Prodrug salts of 2, 4-pyrimidinediamine compounds and their uses
JP5208123B2 (ja) 2006-12-08 2013-06-12 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤としての化合物および組成物
CA2670645A1 (en) 2006-12-19 2008-07-03 Genentech, Inc. Pyrimidine kinase inhibitors
EP1939185A1 (de) 2006-12-20 2008-07-02 Bayer Schering Pharma Aktiengesellschaft Neuartige Hetaryl-Phenylendiamin-Pyrimidine als Proteinkinaseinhibitoren zur Behandlung von Krebs
US9006243B2 (en) 2006-12-29 2015-04-14 Janssen R&D Ireland HIV inhibiting 6-substituted pyrimidines
US8318736B2 (en) 2006-12-29 2012-11-27 Janssen R&D Ireland HIV inhibiting 5,6-substituted pyrimidines
PE20081636A1 (es) 2007-01-26 2009-01-10 Smithkline Beecham Corp Inhibidores de antranilamida para aurora quinasa
CA2702647C (en) 2007-01-31 2016-03-22 Ym Biosciences Australia Pty Ltd Thiopyrimidine-based compounds and uses thereof
DE102007010801A1 (de) 2007-03-02 2008-09-04 Bayer Cropscience Ag Diaminopyrimidine als Fungizide
CA2681250A1 (en) 2007-03-20 2008-09-25 Smithkline Beecham Corporation Chemical compounds
US20100105674A1 (en) 2007-03-20 2010-04-29 Deanda Jr Felix Chemical Compounds
US7947698B2 (en) 2007-03-23 2011-05-24 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
WO2008118823A2 (en) 2007-03-26 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US8809273B2 (en) 2007-03-28 2014-08-19 Pharmacyclics, Inc. Inhibitors of Bruton's tyrosine kinase
US20120065201A1 (en) 2007-03-28 2012-03-15 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
US8242271B2 (en) 2007-06-04 2012-08-14 Avila Therapeutics, Inc. Heterocyclic compounds and uses thereof
CN101903357A (zh) 2007-07-17 2010-12-01 里格尔药品股份有限公司 作为pkc抑制剂的环状胺取代的嘧啶二胺
WO2009017838A2 (en) 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
BRPI0815979A2 (pt) 2007-08-28 2017-06-13 Irm Llc compostos e composições com inibidores de quinase, bem como uso dos mesmos
WO2009032703A1 (en) 2007-08-28 2009-03-12 Irm Llc 2- (het) arylamino-6-aminopyridine derivatives and fused forms thereof as anaplastic lymphoma kinase inhibitors
US20090088371A1 (en) 2007-08-28 2009-04-02 Rigel Pharmaceuticals, Inc. Combination therapy with syk kinase inhibitor
US7989465B2 (en) * 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
JP5600063B2 (ja) 2007-10-19 2014-10-01 セルジーン アビロミクス リサーチ， インコーポレイテッド ヘテロアリール化合物およびその使用
CA2710118A1 (en) 2007-12-20 2009-07-02 Cellzome Limited Sulfamides as zap-70 inhibitors
RU2490015C2 (ru) 2008-02-22 2013-08-20 Райджел Фармасьютикалз, Инк. Применение 2,4-пиримидиндиаминов для лечения атеросклероза
US20110098288A1 (en) 2008-03-11 2011-04-28 Jeremy Major Sulfonamides as zap-70 inhibitors
US8205348B2 (en) 2008-03-19 2012-06-26 Zashiki-Warashi Manufacturing Inc. Tile spacer and holder therefor
CL2009000600A1 (es) 2008-03-20 2010-05-07 Bayer Cropscience Ag Uso de compuestos de diaminopirimidina como agentes fitosanitarios; compuestos de diaminopirimidina; su procedimiento de preparacion; agente que los contiene; procedimiento para la preparacion de dicho agente; y procedimiento para combatir plagas de animales y/u hongos dañinos patogenos de plantas.
WO2009127642A2 (en) 2008-04-15 2009-10-22 Cellzome Limited Use of lrrk2 inhibitors for neurodegenerative diseases
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
KR20100132550A (ko) 2008-04-16 2010-12-17 포톨라 파마슈티컬스, 인코포레이티드 ｓｙｋ 또는 ＪＡＫ 키나제 억제제로서의 ２,６－디아미노-피리미딘－５－일－카르복스아미드
CA2722326A1 (en) 2008-04-24 2009-10-29 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
JP2011523646A (ja) 2008-05-21 2011-08-18 アリアド・ファーマシューティカルズ・インコーポレイテッド キナーゼ阻害剤としてのリン誘導体
AU2009262068C1 (en) * 2008-06-27 2015-07-02 Celgene Car Llc Heteroaryl compounds and uses thereof
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
CN102159214A (zh) 2008-07-16 2011-08-17 药品循环公司 用于实体肿瘤的治疗的布鲁顿酪氨酸激酶的抑制剂
WO2010025833A1 (de) 2008-09-03 2010-03-11 Bayer Cropscience Ag Alkoxy- und alkylthio-substituierte anilinopyrimidine
WO2010077740A2 (en) 2008-12-09 2010-07-08 Cytokine Pharmasciences, Inc. Novel antiviral compounds, compositions, and methods of use
CA2748758C (en) 2009-01-15 2017-06-13 F. Hoffmann-La Roche Ag Antibodies against phosphorylated tyrosines on erythropoietin receptor (epor)
US20120270237A9 (en) 2009-04-03 2012-10-25 Cellzone AG Methods for the identification of kinase interacting molecules and for the purification of kinase proteins
KR101705158B1 (ko) * 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Ｅｇｆｒ 억제제 및 질환 치료방법
MX2011011875A (es) 2009-05-08 2011-12-08 Astellas Pharma Inc Compuesto de carboxamida heterociclica diamino.
WO2010146132A1 (en) 2009-06-18 2010-12-23 Cellzome Limited Sulfonamides and sulfamides as zap-70 inhibitors
US7741330B1 (en) 2009-10-12 2010-06-22 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of Bruton's tyrosine kinase
WO2011079231A1 (en) 2009-12-23 2011-06-30 Gatekeeper Pharmaceutical, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
WO2011140338A1 (en) 2010-05-05 2011-11-10 Gatekeeper Pharmaceuticals, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
MX380504B (es) 2010-06-03 2025-03-12 Pharmacyclics Llc El uso de inhibidores de la tirosina quinasa de bruton (btk).
US20120071497A1 (en) 2010-06-03 2012-03-22 Pharmacyclics, Inc. Methods of treating abc-dlbcl using inhibitors of bruton's tyrosine kinase
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
PH12013500246A1 (en) 2010-08-10 2019-10-11 Celgene Avilomics Res Inc Besylate salt of a btk inhibitor
JP5956999B2 (ja) 2010-11-01 2016-07-27 セルジーン アヴィロミクス リサーチ， インコーポレイテッド ヘテロアリール化合物およびその使用
WO2012061415A1 (en) 2010-11-01 2012-05-10 Portola Pharmaceuticals, Inc. Oxypyrimidines as syk modulators
BR112013010564B1 (pt) 2010-11-01 2021-09-21 Celgene Car Llc Compostos heterocíclicos e composições compreendendo os mesmos
EP2637502B1 (en) 2010-11-10 2018-01-10 Celgene CAR LLC Mutant-selective egfr inhibitors and uses thereof
CN102558149A (zh) 2010-12-29 2012-07-11 中国医学科学院药物研究所 嘧啶衍生物、及其制法和药物组合物与用途
AU2012250517B2 (en) 2011-05-04 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
DK2710007T3 (da) 2011-05-17 2020-01-27 Principia Biopharma Inc Kinasehæmmere
US20140303191A1 (en) 2011-10-19 2014-10-09 Pharmacyclics, Inc. Use of inhibitors of bruton's tyrosine kinase (btk)
CN103159742B (zh) 2011-12-16 2015-08-12 北京韩美药品有限公司 5-氯嘧啶类化合物及其作为egfr酪氨酸激酶抑制剂的应用
JP6317320B2 (ja) * 2012-03-15 2018-04-25 セルジーン シーエーアール エルエルシー 上皮成長因子受容体キナーゼ阻害剤の塩
ES2880109T3 (es) 2012-03-15 2021-11-23 Celgene Car Llc Formas sólidas de un inhibidor de la cinasa del receptor del factor de crecimiento epidérmico
SG11201503459SA (en) 2012-11-02 2015-06-29 Pharmacyclics Inc Tec family kinase inhibitor adjuvant therapy
JP6800750B2 (ja) 2013-08-02 2020-12-16 ファーマサイクリックス エルエルシー 固形腫瘍の処置方法

Similar Documents

Publication Publication Date Title
JP2013544807A5 (enExample)
JP2013542256A5 (enExample)
AR076550A1 (es) Inhibidores de la janus tirosina kinasa (jak)
JP2020502049A5 (enExample)
UY33587A (es) Nuevos compuestos como inhibidores de quinasas syk y jak
RU2013118648A (ru) Гетероциклические соединения и их применение
AR077975A1 (es) Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina
JP2012504628A5 (enExample)
UY32251A (es) Compuestos quimicos
JP2014520898A5 (enExample)
SI3009431T1 (en) 2- (2,4,5-substituted-anilino) pyrimidine derivatives, as EGFR modulators useful for the treatment of cancer
CU24265B1 (es) Compuestos derivados de benzamida para inhibir la actividad de abl1, abl2 y bcr-abl1, útiles en el tratamiento del cáncer
RU2007127849A (ru) Аналоги тетрагидрохинолина в качестве мускариновых агонистов
JP2018519343A5 (enExample)
PE20141938A1 (es) Nuevos compuestos inhibidores de la fosfodiesterasa del tipo 10a
JP2017509689A5 (enExample)
JP2015524457A5 (enExample)
AU2014295538A1 (en) Substituted quinazolin-4-one derivatives
JP2008524328A5 (enExample)
AR088235A1 (es) Derivados de pirazoloquinolina
EA021854B1 (ru) Дисахариновая, дифумаровокислая, ди-1-гидрокси-2-нафтойнокислая и монобензойнокислая соли 4-(диметиламино)бутил-2-(4-((2-амино-4-метил-6-(пентиламино)пиримидин-5-ил)метил)фенил)ацетата
CO2017001603A2 (es) Compuestos aminopirimidinilo inhibidores de jak
JP2016514717A5 (enExample)
JOP20190113A1 (ar) مثبطات بروتون تيروزين كيناز
MX2009009121A (es) Aminoamidas como antagonistas de orexina.