JP2010502751A - キナーゼ阻害物質、およびキナーゼ阻害物質の使用および同定方法 - Google Patents

キナーゼ阻害物質、およびキナーゼ阻害物質の使用および同定方法 Download PDF

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JP2010502751A
JP2010502751A JP2009527627A JP2009527627A JP2010502751A JP 2010502751 A JP2010502751 A JP 2010502751A JP 2009527627 A JP2009527627 A JP 2009527627A JP 2009527627 A JP2009527627 A JP 2009527627A JP 2010502751 A JP2010502751 A JP 2010502751A
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btk
methyl
optionally substituted
less
phenyl
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JP2010502751A5 (enExample
Inventor
エー. ホイットニー,ジェイムズ
パオロ,ジュリー ディ
エー. ベレカ,マーク
アール. ブリッテリ,デイビッド
エス. カリー,ケビン
ダブリュ. ダロウ,ジェイムズ
イー. クロプフ,ジェフリー
エイチ. リー,ソン
エル. ガリオン,スティーブン
エー. ミッチェル,スコット
エー.アイ. ピッペン,ダグラス
エー. ブロムグレン,ピーター
グレゴリー スタッフォード,ダグラス
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シージーアイ ファーマシューティカルズ,インコーポレイティド
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JP2009527627A 2006-09-11 2007-09-11 キナーゼ阻害物質、およびキナーゼ阻害物質の使用および同定方法 Pending JP2010502751A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US84385306P 2006-09-11 2006-09-11
PCT/US2007/078186 WO2008033858A2 (en) 2006-09-11 2007-09-11 Kinase inhibitors, and methods of using and identifying kinase inhibitors

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JP2010502751A true JP2010502751A (ja) 2010-01-28
JP2010502751A5 JP2010502751A5 (enExample) 2010-10-21

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US (1) US20100160292A1 (enExample)
EP (2) EP2068849A2 (enExample)
JP (1) JP2010502751A (enExample)
WO (1) WO2008033858A2 (enExample)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013161848A1 (ja) * 2012-04-27 2013-10-31 カルナバイオサイエンス株式会社 新規1,2,4-トリアジン誘導体
JP2015518903A (ja) * 2012-06-08 2015-07-06 バイオジェン・エムエイ・インコーポレイテッドBiogen MA Inc. ピリミジニルチロシンキナーゼ阻害剤
JP2017502933A (ja) * 2013-12-05 2017-01-26 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト 求電子性官能基を有するヘテロアリールピリドン及びアザ−ピリドン化合物
US10577374B2 (en) 2009-09-04 2020-03-03 Sunesis Pharmaceuticals, Inc. Bruton's tyrosine kinase inhibitors
US11174243B2 (en) 2016-07-21 2021-11-16 Sunesis Pharmaceuticals, Inc. Succinate forms and compositions of Bruton's tyrosine kinase inhibitors

Families Citing this family (97)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HRP20100378T1 (hr) 2006-05-31 2010-08-31 Galapagos N.V. Spojevi triazolopirazina učinkoviti za tretman degenerativnih i upalnih bolesti
AR063706A1 (es) * 2006-09-11 2009-02-11 Cgi Pharmaceuticals Inc Determinadas amidas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmaceuticas que las comprenden.
CL2008002793A1 (es) 2007-09-20 2009-09-04 Cgi Pharmaceuticals Inc Compuestos derivados de amidas sustituidas, inhibidores de la actividad de btk; composicion farmaceutica que los comprende; utiles en el tratamiento del cancer, trastornos oseos, enfermedades autoinmunes, entre otras
JP5587193B2 (ja) * 2007-10-23 2014-09-10 エフ.ホフマン−ラ ロシュ アーゲー 新規なキナーゼ阻害剤
US7683064B2 (en) 2008-02-05 2010-03-23 Roche Palo Alto Llc Inhibitors of Bruton's tyrosine kinase
CA2723237A1 (en) * 2008-05-06 2009-11-12 Peter A. Blomgren Substituted amides, method of making, and use as btk inhibitors
PE20100851A1 (es) 2008-06-24 2011-01-31 Hoffmann La Roche PIRIDIN-2-ONAS Y PIRIDAZIN-3-ONAS SUSTITUIDAS COMO INHIBIDORES DE Btk
PL2300459T3 (pl) * 2008-07-02 2013-10-31 Hoffmann La Roche Nowe fenylopirazynony jako inhibitory kinazy
CA2726460C (en) * 2008-07-15 2017-02-21 F. Hoffmann-La Roche Ag Novel phenyl-imidazopyridines and pyridazines
EP2307418B1 (en) * 2008-07-18 2014-03-12 F.Hoffmann-La Roche Ag Novel phenylimidazopyrazines
WO2010011837A1 (en) 2008-07-24 2010-01-28 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
WO2010068806A1 (en) * 2008-12-10 2010-06-17 Cgi Pharmaceuticals, Inc. Amide derivatives as btk inhibitors in the treatment of allergic, autoimmune and inflammatory disorders as well as cancer
ES2443948T3 (es) 2008-12-19 2014-02-21 Bristol-Myers Squibb Company Compuestos de carbazol carboxamida útiles como inhibidores de quinasas
CN102458402B (zh) 2009-06-12 2013-10-02 百时美施贵宝公司 用作激酶调节剂的烟酰胺化合物
WO2011019780A1 (en) 2009-08-11 2011-02-17 Bristol-Myers Squibb Company Azaindazoles as btk kinase modulators and use thereof
US8685969B2 (en) 2010-06-16 2014-04-01 Bristol-Myers Squibb Company Carboline carboxamide compounds useful as kinase inhibitors
AR082590A1 (es) 2010-08-12 2012-12-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
WO2012135631A1 (en) 2011-03-30 2012-10-04 Arrien Pharmaeuticals Llc Substituted 5-(pyrazin-2-yl)-1h-pyrazolo [3, 4-b] pyridine and pyrazolo [3, 4-b] pyridine derivatives as protein kinase inhibitors
ES2548414T3 (es) 2011-07-08 2015-10-16 Novartis Ag Novedosos derivados de pirrolo pirimidina
US8461179B1 (en) 2012-06-07 2013-06-11 Deciphera Pharmaceuticals, Llc Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
HK1208681A1 (en) 2012-06-12 2016-03-11 Abbvie Inc. Pyridinone and pyridazinone derivatives
CA2876689C (en) 2012-06-13 2022-04-26 Incyte Corporation Substituted tricyclic compounds as fgfr inhibitors
HK1206073A1 (en) 2012-07-24 2015-12-31 药品循环有限责任公司 Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk)
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
WO2014108820A1 (en) * 2013-01-08 2014-07-17 Aurigene Discovery Technologies Limited Substituted 2-pyrazinone derivatives as kinase inhibitors
WO2014125410A1 (en) * 2013-02-12 2014-08-21 Aurigene Discovery Technologies Limited N-substituted heterocyclic derivatives as kinase inhibitors
PH12015502383B1 (en) 2013-04-19 2023-02-03 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
PL2989106T3 (pl) 2013-04-25 2017-08-31 Beigene, Ltd. Połączone związki heterocykliczne jako inhibitory kinazy białkowej
AR096721A1 (es) 2013-06-25 2016-01-27 Bristol Myers Squibb Co Compuestos de tetrahidrocarbazol y carbazol carboxamida sustituidos
KR102345381B1 (ko) 2013-06-25 2021-12-29 브리스톨-마이어스 스큅 컴퍼니 키나제 억제제로서 유용한 카르바졸 카르복스아미드 화합물
SMT202300039T1 (it) 2013-09-13 2023-03-17 Beigene Switzerland Gmbh Anticorpi anti-pd1 e loro uso come terapia e per diagnostica
JP2016535764A (ja) * 2013-10-04 2016-11-17 ビヨンド オンコロジー ファーマシューティカル エルエルシー ブルトンのチロシンキナーゼの阻害剤
US9512084B2 (en) 2013-11-29 2016-12-06 Novartis Ag Amino pyrimidine derivatives
AU2014360446A1 (en) 2013-12-05 2016-06-09 Pharmacyclics, Llc Inhibitors of Bruton's tyrosine kinase
TWI726608B (zh) 2014-07-03 2021-05-01 英屬開曼群島商百濟神州有限公司 抗pd-l1抗體及其作為治療及診斷之用途
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
TWI676618B (zh) 2014-10-24 2019-11-11 美商必治妥美雅史谷比公司 三環化合物
CN107108555B (zh) 2014-10-24 2020-12-01 百时美施贵宝公司 三环阻转异构体化合物
MX393057B (es) 2014-10-24 2025-03-24 Bristol Myers Squibb Co Compuestos de indol carboxamida útiles como inhibidores de cinasas.
CA2976790C (en) 2015-02-20 2024-02-27 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
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
US20170107216A1 (en) 2015-10-19 2017-04-20 Incyte Corporation Heterocyclic compounds as immunomodulators
MD3377488T2 (ro) 2015-11-19 2023-02-28 Incyte Corp Compuși heterociclici ca imunomodulatori
ES2916874T3 (es) 2015-12-17 2022-07-06 Incyte Corp Derivados de N-fenil-piridina-2-carboxamida y su uso como moduladores de la interacción proteína/proteína PD-1/PD-L1
CA3009474A1 (en) 2015-12-22 2017-06-29 Incyte Corporation Heterocyclic compounds as immunomodulators
CN107033069B (zh) * 2016-02-04 2022-03-04 中国科学院合肥物质科学研究院 一种新型布鲁顿酪氨酸激酶不可逆抑制剂
ES2906460T3 (es) 2016-05-06 2022-04-18 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
EP3464279B1 (en) 2016-05-26 2021-11-24 Incyte Corporation Heterocyclic compounds as immunomodulators
SG11201811414TA (en) 2016-06-20 2019-01-30 Incyte Corp Heterocyclic compounds as immunomodulators
WO2018007885A1 (en) 2016-07-05 2018-01-11 Beigene, Ltd. COMBINATION OF A PD-l ANTAGONIST AND A RAF INHIBITOR FOR TREATING CANCER
MA45669A (fr) 2016-07-14 2019-05-22 Incyte Corp Composés hétérocycliques utilisés comme immunomodulateurs
IL293319B1 (en) 2016-08-16 2026-01-01 Beone Medicines Ltd Crystal structure of s)–7–(1–acryloylpiperidin–4–yl)–2–(4–)phenoxyphenyl)–4,5,6,7–tetra–hydropyrazolo(1,5–a)pyrimidine–3–carboxamide, methods of preparation and uses thereof
CN110087680B (zh) 2016-08-19 2024-03-19 百济神州有限公司 使用包含btk抑制剂的组合产品治疗癌症
US20180057486A1 (en) 2016-08-29 2018-03-01 Incyte Corporation Heterocyclic compounds as immunomodulators
CN109982687A (zh) 2016-09-19 2019-07-05 梅制药公司 联合疗法
WO2018119236A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Triazolo[1,5-a]pyridine derivatives as immunomodulators
WO2018119286A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Bicyclic heteroaromatic compounds as immunomodulators
US10308644B2 (en) 2016-12-22 2019-06-04 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2018119221A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Pyridine derivatives as immunomodulators
EP4223369A1 (en) 2016-12-22 2023-08-09 Incyte Corporation Immunomodulator compounds and methods of use
EP3573989A4 (en) 2017-01-25 2020-11-18 Beigene, Ltd. CRYSTALLINE FORMS OF (S) -7- (1- (BUT-2-YNOYL) PIPERIDIN-4-YL) -2- (4-PHENOXYPHENYL) -4, 5, 6, 7-TETRAHY DROPYRAZOLO [1, 5-A ] PYRIMIDINE-3-CARBOXAMIDE, PREPARATION AND ASSOCIATED USES
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
EP3645569A4 (en) 2017-06-26 2021-03-24 BeiGene, Ltd. IMMUNOTHERAPY FOR LIVER CELL CARCINOMA
WO2019034009A1 (en) 2017-08-12 2019-02-21 Beigene, Ltd. BTK INHIBITOR WITH ENHANCED DOUBLE SELECTIVITY
US11786529B2 (en) 2017-11-29 2023-10-17 Beigene Switzerland Gmbh Treatment of indolent or aggressive B-cell lymphomas using a combination comprising BTK inhibitors
KR102708177B1 (ko) 2018-01-31 2024-09-23 데시페라 파마슈티칼스, 엘엘씨. 위장관 기질 종양의 치료를 위한 병용 요법
CN118903436A (zh) 2018-01-31 2024-11-08 德西费拉制药有限责任公司 治疗肥大细胞增多症的组合疗法
SMT202300065T1 (it) 2018-03-30 2023-05-12 Incyte Corp Composti eterociclici come immunomodulatori
KR102956194B1 (ko) 2018-05-04 2026-04-23 인사이트 코포레이션 Fgfr 억제제의 염
RS66310B1 (sr) 2018-05-04 2025-01-31 Incyte Corp Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu
CN112752756B (zh) 2018-05-11 2024-06-25 因赛特公司 作为PD-L1免疫调节剂的四氢-咪唑并[4,5-c]吡啶衍生物
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
IL330104A (en) 2019-03-11 2026-08-01 Deciphera Pharmaceuticals Llc Crystalline forms of rifatinib
EP3981399A4 (en) 2019-06-10 2023-05-31 BeiGene Switzerland GmbH ORAL SOLID TABLET WITH A TYROSINE KINAS INHIBITOR AND METHOD OF MANUFACTURE THEREOF
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
TW202115059A (zh) 2019-08-09 2021-04-16 美商英塞特公司 Pd—1/pd—l1抑制劑之鹽
HRP20260411T1 (hr) 2019-08-12 2026-05-08 Deciphera Pharmaceuticals, Llc Ripretinib za liječenje gastrointestinalnih stromalnih tumora
JP7559059B2 (ja) 2019-09-30 2024-10-01 インサイト・コーポレイション 免疫調節剤としてのピリド[3,2-d]ピリミジン化合物
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
GEP20247679B (en) 2019-10-14 2024-10-10 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
EP4058461A1 (en) 2019-11-11 2022-09-21 Incyte Corporation Salts and crystalline forms of a pd-1/pd-l1 inhibitor
WO2021113479A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
MX2022006691A (es) 2019-12-04 2022-09-19 Incyte Corp Derivados de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr).
FI4084779T3 (fi) 2019-12-30 2024-12-16 Deciphera Pharmaceuticals Llc 1-(4-bromi-5-(1-etyyli-7-(metyyliamino)-2-okso-1,2-dihydro-1,6-naftyridin-3-yyli)-2-fluorifenyyli)-3-fenyyliurean koostumuksia
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11780836B2 (en) 2020-11-06 2023-10-10 Incyte Corporation Process of preparing a PD-1/PD-L1 inhibitor
US11760756B2 (en) 2020-11-06 2023-09-19 Incyte Corporation Crystalline form of a PD-1/PD-L1 inhibitor
IL302590A (en) 2020-11-06 2023-07-01 Incyte Corp Process for preparing PD-1/PD-L1 inhibitor and salts and crystalline forms thereof
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
CA3220274A1 (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
US11786531B1 (en) 2022-06-08 2023-10-17 Beigene Switzerland Gmbh Methods of treating B-cell proliferative disorder
US11779572B1 (en) 2022-09-02 2023-10-10 Deciphera Pharmaceuticals, Llc Methods of treating gastrointestinal stromal tumors

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050090499A1 (en) * 2003-06-04 2005-04-28 Currie Kevin S. Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of bruton's tyrosine kinase by such compounds
US20050196851A1 (en) * 2001-08-15 2005-09-08 Parker Hughes Institute Crystal structure of the BTK kinase domain

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU3653099A (en) * 1998-04-17 1999-11-08 Parker Hughes Institute Btk inhibitors and methods for their identification and use
US6303652B1 (en) * 1998-08-21 2001-10-16 Hughes Institute BTK inhibitors and methods for their identification and use
EP1373554A2 (en) * 2000-10-23 2004-01-02 Bristol-Myers Squibb Company Modulators of bruton's tyronsine kinase, their identification and use
US7188992B2 (en) * 2003-07-30 2007-03-13 Americhem, Inc. Kneading element and related articles
WO2005047290A2 (en) * 2003-11-11 2005-05-26 Cellular Genomics Inc. Imidazo[1,2-a] pyrazin-8-ylamines as kinase inhibitors
JP2008519843A (ja) * 2004-11-10 2008-06-12 シージーアイ ファーマスーティカル インコーポレーテッド 特定のイミダゾ[1,2−a]ビラジン−8−イラミンズ、その生成方法及びそれに関する使用方法
AU2006223409B2 (en) * 2005-03-10 2011-07-21 Gilead Connecticut, Inc. Certain substituted amides, method of making, and method of use thereof

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050196851A1 (en) * 2001-08-15 2005-09-08 Parker Hughes Institute Crystal structure of the BTK kinase domain
US20050090499A1 (en) * 2003-06-04 2005-04-28 Currie Kevin S. Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of bruton's tyrosine kinase by such compounds

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10577374B2 (en) 2009-09-04 2020-03-03 Sunesis Pharmaceuticals, Inc. Bruton's tyrosine kinase inhibitors
WO2013161848A1 (ja) * 2012-04-27 2013-10-31 カルナバイオサイエンス株式会社 新規1,2,4-トリアジン誘導体
JP2015518903A (ja) * 2012-06-08 2015-07-06 バイオジェン・エムエイ・インコーポレイテッドBiogen MA Inc. ピリミジニルチロシンキナーゼ阻害剤
US9944622B2 (en) 2012-06-08 2018-04-17 Biogen Ma Inc. Pyrimidinyl tyrosine kinase inhibitors
US10618887B2 (en) 2012-06-08 2020-04-14 Sunesis Pharmaceuticals, Inc. Pyrimidinyl tyrosine kinase inhibitors
JP2017502933A (ja) * 2013-12-05 2017-01-26 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト 求電子性官能基を有するヘテロアリールピリドン及びアザ−ピリドン化合物
US11174243B2 (en) 2016-07-21 2021-11-16 Sunesis Pharmaceuticals, Inc. Succinate forms and compositions of Bruton's tyrosine kinase inhibitors

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