JP2018519343A5 - - Google Patents
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- JP2018519343A5 JP2018519343A5 JP2018500297A JP2018500297A JP2018519343A5 JP 2018519343 A5 JP2018519343 A5 JP 2018519343A5 JP 2018500297 A JP2018500297 A JP 2018500297A JP 2018500297 A JP2018500297 A JP 2018500297A JP 2018519343 A5 JP2018519343 A5 JP 2018519343A5
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- JP
- Japan
- Prior art keywords
- alkyl
- nhs
- nhc
- cycloalkyl
- independently
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 claims 144
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 56
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 53
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 43
- 150000003839 salts Chemical class 0.000 claims 41
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 40
- 125000003118 aryl group Chemical group 0.000 claims 40
- 229910052805 deuterium Inorganic materials 0.000 claims 40
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 38
- 150000001875 compounds Chemical class 0.000 claims 38
- 229910052736 halogen Inorganic materials 0.000 claims 30
- 150000002367 halogens Chemical class 0.000 claims 30
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 25
- 125000002950 monocyclic group Chemical group 0.000 claims 21
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims 15
- 229910052717 sulfur Inorganic materials 0.000 claims 14
- 229910052757 nitrogen Inorganic materials 0.000 claims 11
- 229910052799 carbon Inorganic materials 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 8
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 7
- 125000001246 bromo group Chemical group Br* 0.000 claims 7
- 125000001309 chloro group Chemical group Cl* 0.000 claims 7
- 125000001153 fluoro group Chemical group F* 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- -1 C 1 -C 6 alkyl Chemical group 0.000 claims 6
- 125000003342 alkenyl group Chemical group 0.000 claims 5
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 206010061218 Inflammation Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 102000001253 Protein Kinase Human genes 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 2
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000004777 2-fluoroethyl group Chemical group [H]C([H])(F)C([H])([H])* 0.000 claims 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- BTBUEUYNUDRHOZ-UHFFFAOYSA-N Borate Chemical compound [O-]B([O-])[O-] BTBUEUYNUDRHOZ-UHFFFAOYSA-N 0.000 claims 1
- 101000686031 Homo sapiens Proto-oncogene tyrosine-protein kinase ROS Proteins 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 1
- 102100023347 Proto-oncogene tyrosine-protein kinase ROS Human genes 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 108060006633 protein kinase Proteins 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562188043P | 2015-07-02 | 2015-07-02 | |
| US62/188,043 | 2015-07-02 | ||
| US201662353728P | 2016-06-23 | 2016-06-23 | |
| US62/353,728 | 2016-06-23 | ||
| PCT/US2016/040329 WO2017004342A1 (en) | 2015-07-02 | 2016-06-30 | Chiral diaryl macrocycles as modulators of protein kinases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018519343A JP2018519343A (ja) | 2018-07-19 |
| JP2018519343A5 true JP2018519343A5 (https=) | 2019-07-25 |
| JP6871903B2 JP6871903B2 (ja) | 2021-05-19 |
Family
ID=57609146
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018500297A Active JP6871903B2 (ja) | 2015-07-02 | 2016-06-30 | プロテインキナーゼのモジュレーターとしてのキラルジアリール大環状分子 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US10316044B2 (https=) |
| EP (1) | EP3317285B1 (https=) |
| JP (1) | JP6871903B2 (https=) |
| KR (1) | KR102599788B1 (https=) |
| CN (1) | CN107735399B (https=) |
| AU (2) | AU2016287568B2 (https=) |
| CA (1) | CA2989327A1 (https=) |
| ES (1) | ES2864839T3 (https=) |
| IL (1) | IL256377A (https=) |
| MX (1) | MX2017017097A (https=) |
| RU (1) | RU2732405C2 (https=) |
| TW (1) | TW201716415A (https=) |
| WO (1) | WO2017004342A1 (https=) |
Families Citing this family (66)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010033941A1 (en) | 2008-09-22 | 2010-03-25 | Array Biopharma Inc. | Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors |
| MY169791A (en) | 2008-10-22 | 2019-05-15 | Array Biopharma Inc | Substituted pyrazolo [1,5-a] pyrimidine compounds as trk 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 |
| ME03376B (me) | 2010-05-20 | 2020-01-20 | Array Biopharma Inc | Makrociklička jedinjenja kао inhibiтori trk kinaze |
| ES2933350T3 (es) | 2014-01-24 | 2023-02-06 | Turning Point Therapeutics Inc | Macrociclos de diarilo como moduladores de proteína quinasas |
| CN113354649B (zh) | 2014-11-16 | 2024-12-10 | 阵列生物制药公司 | 一种新的晶型 |
| AU2016287568B2 (en) | 2015-07-02 | 2020-08-20 | Turning Point Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
| RU2765181C2 (ru) * | 2015-07-06 | 2022-01-26 | Тёрнинг Поинт Терапьютикс, Инк. | Полиморфная форма диарильного макроцикла |
| PT3733187T (pt) | 2015-07-21 | 2024-11-08 | Turning Point Therapeutics Inc | Macrociclo de diarilo quiral e utilização do mesmo no tratamento do cancro |
| 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 |
| FI3439662T3 (fi) | 2016-04-04 | 2024-09-04 | Loxo Oncology Inc | (s)-n-(5-((r)-2-(2,5-difluorifenyyli)pyrrolidin-1-yyli)pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidin nesteformulaatioita |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| EP3458456B1 (en) | 2016-05-18 | 2020-11-25 | 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 |
| AU2017292646A1 (en) * | 2016-07-05 | 2019-02-07 | Blade Therapeutics, Inc. | Calpain modulators and therapeutic uses thereof |
| US10689400B2 (en) * | 2016-07-28 | 2020-06-23 | Turning Point Therapeutics, Inc. | Macrocycle kinase inhibitors |
| WO2018064119A1 (en) | 2016-09-28 | 2018-04-05 | Blade Therapeutics, Inc. | Calpain modulators and therapeutic uses thereof |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| TWI808958B (zh) * | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| CN107586796B (zh) * | 2017-07-20 | 2021-08-06 | 暨明医药科技（苏州）有限公司 | (r)-2-(1-氨基乙基)-4-氟苯酚的合成方法 |
| CN111182903A (zh) * | 2017-07-28 | 2020-05-19 | 特普医药公司 | 巨环化合物及其用途 |
| CA3071032A1 (en) | 2017-08-23 | 2019-02-28 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Macrocycle containing aminopyrazole and pyrimidine and pharmaceutical composition and use thereof |
| CN109516999B (zh) * | 2017-11-01 | 2021-08-17 | 郑州泰基鸿诺医药股份有限公司 | 用作蛋白质激酶调节剂的化合物及其应用 |
| AU2018364938B2 (en) * | 2017-11-10 | 2021-11-11 | Angex Pharmaceutical, Inc. | Macrocyclic compounds as TRK kinase inhibitors and uses thereof |
| LT3728271T (lt) | 2017-12-19 | 2022-12-12 | Turning Point Therapeutics, Inc. | Makrocikliniai junginiai, skirti ligų gydymui |
| EP3730492A4 (en) | 2017-12-22 | 2021-08-11 | Shenzhen TargetRx, Inc. | SUBSTITUTED PYRAZOLO [1,5-A] PYRIMIDINE COMPOUND AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US11345703B2 (en) | 2018-01-23 | 2022-05-31 | Shenzhen Targetrx, Inc. | Substituted pyrazolo[1,5-a]pyrimidine macrocyclic compound |
| TW201932472A (zh) * | 2018-01-30 | 2019-08-16 | 大陸商上海吉倍生物技術有限公司 | 具有大環分子結構的化合物及其用途 |
| WO2019184955A1 (en) * | 2018-03-28 | 2019-10-03 | Fochon Pharmaceuticals, Ltd. | Macrocyclic compounds as trk kinases inhibitors |
| US11584759B2 (en) | 2018-04-18 | 2023-02-21 | Hitgen Inc. | Macrocyclic kinase inhibitor |
| WO2019210835A1 (zh) * | 2018-05-04 | 2019-11-07 | 正大天晴药业集团股份有限公司 | 作为蛋白激酶调节剂的二芳基大环化合物 |
| WO2019233461A1 (zh) * | 2018-06-08 | 2019-12-12 | 江苏威凯尔医药科技有限公司 | 原肌球蛋白受体激酶抑制剂及其制备方法和应用 |
| CN110577532B (zh) * | 2018-06-08 | 2022-06-03 | 江苏威凯尔医药科技有限公司 | 原肌球蛋白受体激酶抑制剂及其制备方法和应用 |
| CN110950889B (zh) * | 2018-09-27 | 2022-04-05 | 北京赛林泰医药技术有限公司 | 一种多靶点激酶抑制剂及其制备方法和用途 |
| EP3858834A4 (en) * | 2018-09-29 | 2022-06-22 | Shandong Luye Pharmaceutical Co., Ltd. | PYRAZOLOPYRIMIDE DERIVATIVES AS SELECTIVE TRK INHIBITORS |
| JP7631193B2 (ja) | 2018-10-22 | 2025-02-18 | アルミス インコーポレイテッド | Ｔｙｋ２阻害剤およびその使用 |
| CN111171049B (zh) * | 2018-11-09 | 2021-06-04 | 山东轩竹医药科技有限公司 | 酪氨酸激酶抑制剂及其用途 |
| CN111171020A (zh) | 2018-11-13 | 2020-05-19 | 上海轶诺药业有限公司 | 一类六元并六元杂环化合物及其作为蛋白受体激酶抑制剂的用途 |
| CN111171019A (zh) | 2018-11-13 | 2020-05-19 | 上海轶诺药业有限公司 | 一类五元并六元杂环化合物及其作为蛋白受体激酶抑制剂的用途 |
| CA3132632A1 (en) * | 2019-03-11 | 2020-09-17 | Esker Therapeutics, Inc. | Tyk2 inhibitors and uses thereof |
| CA3134814A1 (en) * | 2019-03-26 | 2020-10-01 | Ventyx Biosciences, Inc. | Tyk2 pseudokinase ligands |
| WO2020233645A1 (zh) * | 2019-05-21 | 2020-11-26 | 浙江海正药业股份有限公司 | 大环类衍生物、及其制备方法和用途 |
| WO2020257189A1 (en) * | 2019-06-19 | 2020-12-24 | Turning Point Therapeutics, Inc. | Macrocycles for treating disease |
| WO2020257165A1 (en) * | 2019-06-19 | 2020-12-24 | Turning Point Therapeutics, Inc. | Macrocycles for use in treating disease |
| WO2020257169A1 (en) * | 2019-06-19 | 2020-12-24 | Turning Point Therapeutics, Inc. | Polymorphs of a macrocyclic kinase inhibitor |
| WO2021027503A1 (zh) * | 2019-08-12 | 2021-02-18 | 罗欣药业(上海)有限公司 | 三环类化合物、其制备方法、中间体及应用 |
| CN114761407B (zh) * | 2019-11-18 | 2024-06-18 | 广州嘉越医药科技有限公司 | 作为高选择性ros1抑制剂的化合物及其应用 |
| BR112022010278A2 (pt) | 2019-11-27 | 2022-10-04 | Turning Point Therapeutics Inc | Terapia combinada que envolve compostos macrocíclicos de diarila |
| MX2022006366A (es) * | 2019-11-27 | 2022-06-22 | Turning Point Therapeutics Inc | Terapia de combinacion que implica compuestos de diarilo macrociclico. |
| US11634433B2 (en) * | 2019-12-03 | 2023-04-25 | Turning Point Therapeutics, Inc. | Macrocycles for use in treating disease |
| AU2020402942B2 (en) * | 2019-12-13 | 2023-05-11 | Scinnohub Pharmaceutical Co., Ltd | Fluorine-containing heterocyclic derivatives with macrocyclic structure and use thereof |
| CN113045575B (zh) * | 2019-12-27 | 2022-06-17 | 成都倍特药业股份有限公司 | 一种化合物的制备方法及其中间体和中间体的制备方法 |
| CN113527298B (zh) * | 2020-04-17 | 2025-01-03 | 浙江海正药业股份有限公司 | 大环内酰胺类衍生物、及其制备方法和用途 |
| CN113735856A (zh) * | 2020-05-29 | 2021-12-03 | 百极弘烨(南通)医药科技有限公司 | 大环jak抑制剂及其应用 |
| EP4163283A1 (en) * | 2020-06-04 | 2023-04-12 | Scinnohub Pharmaceutical Co., Ltd | Compound having macrocyclic structure and use thereof |
| CN114073704B (zh) * | 2020-08-14 | 2023-08-11 | 赛诺哈勃药业（成都）有限公司 | 具有大环结构的含氟并杂环衍生物的应用 |
| EP4214215A1 (en) * | 2020-09-16 | 2023-07-26 | Alumis Inc. | Tyk2 inhibitors and uses thereof |
| CN114591351B (zh) * | 2020-12-03 | 2023-12-05 | 成都科岭源医药技术有限公司 | 一种多环化合物及其制备方法和用途 |
| CN114763360A (zh) * | 2021-01-15 | 2022-07-19 | 广州百霆医药科技有限公司 | 手性大环化合物作为蛋白激酶抑制剂及其用途 |
| WO2022218276A1 (zh) * | 2021-04-12 | 2022-10-20 | 成都倍特药业股份有限公司 | 含氟大环结构化合物的固体形态、制备方法和应用 |
| CN117597128A (zh) * | 2021-08-23 | 2024-02-23 | 正大天晴药业集团股份有限公司 | 含有氨基的大环化合物在治疗trk激酶介导的肿瘤中的用途 |
| CN113582994B (zh) * | 2021-09-28 | 2022-02-11 | 北京鑫开元医药科技有限公司 | 具有trk激酶抑制活性的化合物、制备方法、组合物及其用途 |
| CN116063326B (zh) * | 2021-11-02 | 2025-08-05 | 赛诺哈勃药业（成都）有限公司 | 作为蛋白激酶调节剂的含氨基大环化合物 |
| WO2023208244A1 (zh) * | 2022-04-29 | 2023-11-02 | 南京明德新药研发有限公司 | 大环类化合物及其应用 |
| WO2024051631A1 (zh) | 2022-09-07 | 2024-03-14 | 苏州朗睿生物医药有限公司 | 一种大环咪唑并[1,2-b]哒嗪衍生物及其制备方法和用途 |
| CN115746023B (zh) * | 2022-10-27 | 2024-08-09 | 复旦大学 | 一种作为蛋白激酶抑制剂的含吲唑结构的杂环大环化合物及其制备方法 |
Family Cites Families (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4838925A (en) | 1986-04-25 | 1989-06-13 | E. I. Du Pont De Nemours And Company | Heterocyclic acyl sulfonamides |
| EP0281841B1 (de) | 1987-03-07 | 1990-11-14 | Bayer Ag | Verfahren zur Herstellung von 5-Amino-4,6-dihalogenpyridinen |
| ATE195935T1 (de) | 1993-03-25 | 2000-09-15 | Upjohn Co | Formyl- oder cyano- substituierte indolderivate mit dopaminergischer wirkung |
| PT657458E (pt) | 1993-12-07 | 2002-02-28 | Lilly Co Eli | Inibidores de proteina cinase c |
| FR2746309B1 (fr) | 1996-03-22 | 1998-04-17 | Oreal | Composition de teinture des fibres keratiniques contenant des pyrazolopyrimidineoxo ; leur utilisation pour la teinture comme coupleurs, procedes de teinture |
| RS49779B (sr) | 1998-01-12 | 2008-06-05 | Glaxo Group Limited, | Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze |
| FR2793791B1 (fr) | 1999-05-19 | 2002-01-25 | Univ Paris 7 Denis Diderot | Nouveaux composes inhibiteurs specifiques de phospholipases a2 |
| JP4180365B2 (ja) | 2000-07-31 | 2008-11-12 | エフ．ホフマン−ラ ロシュ アーゲー | ピペラジン誘導体 |
| ATE301661T1 (de) | 2000-12-08 | 2005-08-15 | Ortho Mcneil Pharm Inc | Makroheterocyclische verbindungen als kinase inhibitoren |
| JP2004532834A (ja) | 2001-03-23 | 2004-10-28 | イーライ・リリー・アンド・カンパニー | ヒスタミンｈ３受容体アンタゴニストである非イミダゾール系アリールアルキルアミン化合物、その製造および治療的使用 |
| US7550470B2 (en) | 2002-12-11 | 2009-06-23 | Merck & Co. Inc. | Substituted pyrazolo[1,5-A]pyrimidines as tyrosine kinase inhibitors |
| KR20110073500A (ko) | 2008-09-08 | 2011-06-29 | 메르크 파텐트 게엠베하 | 오로라 키나아제 억제제로서 마크로사이클릭 피리미딘 |
| WO2010033941A1 (en) * | 2008-09-22 | 2010-03-25 | Array Biopharma Inc. | Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors |
| MY169791A (en) * | 2008-10-22 | 2019-05-15 | Array Biopharma Inc | Substituted pyrazolo [1,5-a] pyrimidine compounds as trk kinase inhibitors |
| EP2348860B1 (en) | 2008-10-31 | 2015-05-27 | Genentech, Inc. | Pyrazolopyrimidine jak inhibitor compounds and methods |
| WO2010063487A1 (en) | 2008-12-05 | 2010-06-10 | Merz Pharma Gmbh & Co. Kgaa | Pyrazolopyrimidines, a process for their preparation and their use as medicine |
| WO2010086040A1 (en) | 2009-01-29 | 2010-08-05 | Biomarin Iga, Ltd. | Pyrazolo-pyrimidines for treatment of duchenne muscular dystrophy |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| ES2446720T3 (es) * | 2009-10-13 | 2014-03-10 | Elanco Animal Health Ireland Limited | Inhibidores de la integrasa macrocíclica |
| WO2011071725A1 (en) | 2009-12-07 | 2011-06-16 | Boehringer Ingelheim International Gmbh | Heterocyclic compounds containing a pyrrolopyridine or benzimidazole core |
| WO2011071716A1 (en) | 2009-12-07 | 2011-06-16 | Boehringer Ingelheim International Gmbh | Heterocyclic compounds containing an indole core |
| SA111320200B1 (ar) | 2010-02-17 | 2014-02-16 | ديبيوفارم اس ايه | مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة |
| ME03376B (me) * | 2010-05-20 | 2020-01-20 | Array Biopharma Inc | Makrociklička jedinjenja kао inhibiтori trk kinaze |
| UY33597A (es) * | 2010-09-09 | 2012-04-30 | Irm Llc | Compuestos y composiciones como inhibidores de la trk |
| WO2012034095A1 (en) | 2010-09-09 | 2012-03-15 | Irm Llc | Compounds and compositions as trk inhibitors |
| WO2012075393A2 (en) | 2010-12-02 | 2012-06-07 | President And Fellows Of Harvard College | Activators of proteasomal degradation and uses thereof |
| EP2508607A1 (en) | 2011-04-07 | 2012-10-10 | Helmholtz-Zentrum für Infektionsforschung GmbH | Medicament for liver regeneration and for treatment of liver failure |
| WO2013001310A1 (en) | 2011-06-30 | 2013-01-03 | Centro Nacional De Investigaciones Oncológicas (Cnio) | Macrocyclic compounds and their use as cdk8 inhibitors |
| BR112014003802A2 (pt) | 2011-08-19 | 2017-06-13 | Merck Sharp & Dohme | composto, composto composição farmacêutica, uso de um composto, método para fabricar um composto, e, preparação de um medicamento |
| WO2013045702A2 (en) | 2011-09-29 | 2013-04-04 | L'oreal | Dye composition comprising a non-glycosyl iridoid compound and a specific nucleophile or an amino or thio polymer, dyeing process, and device therefor |
| WO2013045701A2 (en) | 2011-09-29 | 2013-04-04 | L'oreal | Dyeing process using a composition comprising a glycosyl iridoid compound and a nucleophile or an amino or thio polymer, composition and devices therefor |
| BR112014007622A2 (pt) | 2011-09-30 | 2017-04-04 | Oncodesign Sa | inibidores de flt3 cinase macrocíclicos |
| JP6073343B2 (ja) | 2011-10-20 | 2017-02-01 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ | サーチュイン調節因子としての置換された二環式アザ複素環およびアナログ |
| DK2822953T5 (en) * | 2012-03-06 | 2017-09-11 | Pfizer | Macrocyclic derivatives for the treatment of proliferative diseases |
| CN104302649B (zh) | 2012-03-09 | 2017-06-23 | 莱西肯医药有限公司 | 基于吡唑并[1,5‑a]嘧啶的化合物、包含它们的组合物及其使用方法 |
| WO2013134219A1 (en) | 2012-03-09 | 2013-09-12 | Lexicon Pharmaceuticals, Inc. | Imidazo [1, 2 - b] pyridazine - based compounds, compositions comprising them, and uses thereof |
| GB201205669D0 (en) | 2012-03-30 | 2012-05-16 | Agency Science Tech & Res | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
| JP2016506921A (ja) | 2013-01-30 | 2016-03-07 | バイエル ファーマ アクチエンゲゼルシャフト | アミノ置換イソチアゾール |
| WO2014173928A1 (en) | 2013-04-23 | 2014-10-30 | Lek Pharmaceuticals D.D. | Novel synthetic process to 8-chloro-1-methyl-benzo[d]azepine, novel intermediates and the production thereof |
| JPWO2015012328A1 (ja) | 2013-07-24 | 2017-03-02 | 武田薬品工業株式会社 | 複素環化合物 |
| CN104513253A (zh) * | 2013-10-01 | 2015-04-15 | 南京波尔泰药业科技有限公司 | 用于治疗增殖性疾病的大环化合物 |
| WO2015073267A1 (en) | 2013-11-15 | 2015-05-21 | Calitor Sciences, Llc | Substituted heteroaryl compounds and methods of use |
| ES2933350T3 (es) * | 2014-01-24 | 2023-02-06 | Turning Point Therapeutics Inc | Macrociclos de diarilo como moduladores de proteína quinasas |
| WO2016070241A1 (en) | 2014-11-03 | 2016-05-12 | Ctxt Pty Ltd | Triazine compounds, compositions and synthesis |
| CA2971024C (en) | 2014-12-15 | 2023-09-26 | Handok Inc. | Fused ring heteroaryl compounds and their use as trk inhibitors |
| JP6800158B2 (ja) | 2015-02-20 | 2020-12-16 | 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 | Ｇｄｆ−８阻害剤 |
| US10329294B2 (en) | 2015-03-12 | 2019-06-25 | Merck Sharp & Dohme Corp. | Pyrazolopyrimidine inhibitors of IRAK4 activity |
| US10155765B2 (en) | 2015-03-12 | 2018-12-18 | Merck Sharp & Dohme Corp. | Carboxamide inhibitors of IRAK4 activity |
| BR112017023764A2 (pt) | 2015-05-05 | 2018-07-31 | Bayer Pharma AG | derivados de ciclohexano substituído por amido |
| AU2016287568B2 (en) | 2015-07-02 | 2020-08-20 | Turning Point Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
| RU2765181C2 (ru) | 2015-07-06 | 2022-01-26 | Тёрнинг Поинт Терапьютикс, Инк. | Полиморфная форма диарильного макроцикла |
| PT3733187T (pt) | 2015-07-21 | 2024-11-08 | Turning Point Therapeutics Inc | Macrociclo de diarilo quiral e utilização do mesmo no tratamento do cancro |
| 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 |
| US11596639B2 (en) | 2016-03-04 | 2023-03-07 | Vanderbilt University | Substituted indole Mcl-1 inhibitors |
| US10689400B2 (en) | 2016-07-28 | 2020-06-23 | Turning Point Therapeutics, Inc. | Macrocycle kinase inhibitors |
| JP2020533269A (ja) | 2016-12-14 | 2020-11-19 | デベロップメント センター フォー バイオテクノロジー | 抗体−薬物複合体およびその使用 |
| TWI808958B (zh) | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| CN111182903A (zh) | 2017-07-28 | 2020-05-19 | 特普医药公司 | 巨环化合物及其用途 |
-
2016
- 2016-06-30 AU AU2016287568A patent/AU2016287568B2/en not_active Ceased
- 2016-06-30 ES ES16818768T patent/ES2864839T3/es active Active
- 2016-06-30 MX MX2017017097A patent/MX2017017097A/es unknown
- 2016-06-30 RU RU2018103907A patent/RU2732405C2/ru active
- 2016-06-30 KR KR1020187002777A patent/KR102599788B1/ko active Active
- 2016-06-30 CN CN201680038613.1A patent/CN107735399B/zh active Active
- 2016-06-30 WO PCT/US2016/040329 patent/WO2017004342A1/en not_active Ceased
- 2016-06-30 EP EP16818768.0A patent/EP3317285B1/en active Active
- 2016-06-30 CA CA2989327A patent/CA2989327A1/en active Pending
- 2016-06-30 US US15/740,462 patent/US10316044B2/en active Active
- 2016-06-30 JP JP2018500297A patent/JP6871903B2/ja active Active
- 2016-07-01 TW TW105121035A patent/TW201716415A/zh unknown
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2017
- 2017-12-18 IL IL256377A patent/IL256377A/en unknown
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2019
- 2019-05-29 US US16/425,407 patent/US11008337B2/en active Active
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2020
- 2020-08-11 AU AU2020217336A patent/AU2020217336A1/en not_active Abandoned
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