JP2018519343A5 - - Google Patents
Download PDFInfo
- Publication number
- 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
- Authority
- 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.)
- Granted
Links
- 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 (enExample) | 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 (enExample) |
| EP (1) | EP3317285B1 (enExample) |
| JP (1) | JP6871903B2 (enExample) |
| KR (1) | KR102599788B1 (enExample) |
| CN (1) | CN107735399B (enExample) |
| AU (2) | AU2016287568B2 (enExample) |
| CA (1) | CA2989327A1 (enExample) |
| ES (1) | ES2864839T3 (enExample) |
| IL (1) | IL256377A (enExample) |
| MX (1) | MX2017017097A (enExample) |
| RU (1) | RU2732405C2 (enExample) |
| TW (1) | TW201716415A (enExample) |
| WO (1) | WO2017004342A1 (enExample) |
Families Citing this family (66)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI2350075T1 (sl) | 2008-09-22 | 2014-06-30 | Array Biopharma, Inc. | Substituirane imidazo (1,2b)piridazinske spojine kot Trk kinazni inhibitorji |
| CN102264736B (zh) | 2008-10-22 | 2013-08-14 | 阵列生物制药公司 | 作为TRK激酶抑制剂的取代的吡唑并[1,5-a]嘧啶化合物 |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| BR122019024201B1 (pt) | 2010-05-20 | 2021-08-03 | Array Biopharma Inc | Composto macrocíclico como inibidores de trk quinase, seu uso, e composição farmacêutica |
| WO2015112806A2 (en) | 2014-01-24 | 2015-07-30 | Tp Therapeutics, Inc. | Diaryl macrocycles as modulators of protein kinases |
| 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 |
| RU2732405C2 (ru) | 2015-07-02 | 2020-09-16 | Тёрнинг Поинт Терапьютикс, Инк. | Хиральные диарильные макроциклы в качестве модуляторов протеинкиназ |
| BR112018000297A2 (pt) | 2015-07-06 | 2018-09-04 | Tp Therapeutics Inc | polimorfo de macrociclo de diarila |
| WO2017015367A1 (en) * | 2015-07-21 | 2017-01-26 | Tp Therapeutics, Inc. | Chiral diaryl macrocycles and uses thereof |
| 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 |
| UA125025C2 (uk) | 2016-04-04 | 2021-12-29 | Локсо Онколоджі, Інк. | Способи лікування дитячих ракових захворювань |
| UA125026C2 (uk) | 2016-04-04 | 2021-12-29 | Локсо Онколоджі, Інк. | РІДКІ КОМПОЗИЦІЇ (S)-N-(5-((R)-2-(2,5-ДИФТОРФЕНІЛ)ПІРОЛІДИН-1-ІЛ)ПІРАЗОЛО[1,5-a]ПІРИМІДИН-3-ІЛ)-3-ГІДРОКСИПІРОЛІДИН-1-КАРБОКСАМІДУ |
| MX392604B (es) | 2016-05-18 | 2025-03-24 | Array Biopharma Inc | Procesos para la preparacion de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidin-1-carboxamida y sales del mismo. |
| AU2017292646A1 (en) * | 2016-07-05 | 2019-02-07 | Blade Therapeutics, Inc. | Calpain modulators and therapeutic uses thereof |
| AU2017302019A1 (en) * | 2016-07-28 | 2019-02-07 | Turning Point Therapeutics, Inc. | Macrocycle kinase inhibitors |
| US10934261B2 (en) | 2016-09-28 | 2021-03-02 | 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 |
| PT3658148T (pt) | 2017-07-28 | 2024-08-26 | Turning Point Therapeutics Inc | Compostos macrocíclicos e utilizações dos mesmos |
| KR102619444B1 (ko) | 2017-08-23 | 2023-12-29 | 치아타이 티안큉 파마수티컬 그룹 주식회사 | 아미노피라졸 및 피리미딘을 함유하는 마크로사이클 및 그의 약학적 조성물 및 용도 |
| 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 |
| CA3081790C (en) * | 2017-11-10 | 2023-03-07 | Angex Pharmaceutical, Inc. | Macrocyclic compounds as trk kinase inhibitors and uses thereof |
| RS63787B1 (sr) | 2017-12-19 | 2022-12-30 | Turning Point Therapeutics Inc | Makrociklična jedinjenja za lečenje bolesti |
| CN109456331B (zh) | 2017-12-22 | 2020-06-05 | 深圳市塔吉瑞生物医药有限公司 | 一种取代的吡唑并[1,5-a]嘧啶化合物及其药物组合物及用途 |
| WO2019144885A1 (zh) * | 2018-01-23 | 2019-08-01 | 深圳市塔吉瑞生物医药有限公司 | 取代的吡唑并[1,5-a]嘧啶类的大环化合物 |
| WO2019149131A1 (zh) * | 2018-01-30 | 2019-08-08 | 上海吉倍生物技术有限公司 | 具有大环分子结构的化合物及其用途 |
| JP2021519297A (ja) * | 2018-03-28 | 2021-08-10 | フォチョン・ファーマシューティカルズ・リミテッドＦｏｃｈｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｌｔｄ． | Ｔｒｋキナーゼ阻害剤としての大環状化合物 |
| US11584759B2 (en) | 2018-04-18 | 2023-02-21 | Hitgen Inc. | Macrocyclic kinase inhibitor |
| CN111918868B (zh) * | 2018-05-04 | 2022-12-30 | 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 |
| 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 |
| 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 |
| 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 |
| RS66346B1 (sr) | 2018-10-22 | 2025-01-31 | Alumis Inc | Inhibitori tyk2 i njihova upotreba |
| 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 |
| 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 |
| 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 |
| US20220177486A1 (en) * | 2019-03-11 | 2022-06-09 | Esker Therapeutics, Inc. | Tyk2 inhibitors and uses thereof |
| SG11202110523XA (en) * | 2019-03-26 | 2021-10-28 | Ventyx Biosciences Inc | Tyk2 pseudokinase ligands |
| US12410191B2 (en) | 2019-05-21 | 2025-09-09 | Zhejiang Hisun Pharmaceutical Co., Ltd. | Macrolide derivatives, preparation method and application thereof |
| 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 |
| US12497412B2 (en) | 2019-11-18 | 2025-12-16 | Guangzhou Joyo Pharmatech Co., Ltd. | Compound as highly selective ROS1 inhibitor and use thereof |
| WO2021108682A1 (en) | 2019-11-27 | 2021-06-03 | Turning Point Therapeutics, Inc. | Combination therapy involving diaryl macrocyclic compounds |
| KR20220134522A (ko) * | 2019-11-27 | 2022-10-05 | 터닝 포인트 테라퓨틱스, 인크. | 디아릴 매크로시클릭 화합물을 수반하는 병용 요법 |
| TW202134249A (zh) | 2019-12-03 | 2021-09-16 | 美商特普醫葯公司 | 用於治療疾病的巨環 |
| US12428433B2 (en) | 2019-12-13 | 2025-09-30 | 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 |
| WO2021244609A1 (zh) * | 2020-06-04 | 2021-12-09 | 成都倍特药业股份有限公司 | 具有大环结构的化合物及其用途 |
| 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 |
| IL301385A (en) * | 2020-09-16 | 2023-05-01 | Alumis Inc | TYK2 inhibitors and their use |
| WO2022117090A1 (zh) * | 2020-12-03 | 2022-06-09 | 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 |
| CN117412970B (zh) * | 2021-04-12 | 2025-12-30 | 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 |
| WO2023025141A1 (zh) * | 2021-08-23 | 2023-03-02 | 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 |
| AU2023339247A1 (en) | 2022-09-07 | 2025-03-27 | Suzhou Langrui Biopharmaceutical Co., Ltd. | Macrocyclic imidazo[1,2-b]pyridazine derivative, preparation method therefor, and use thereof |
| 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 |
| ES2021105B3 (es) | 1987-03-07 | 1991-10-16 | Bayer Ag | Procedimiento para la obtencion de 5-amino-4,6-dihalogeno piridinas. |
| ES2149869T3 (es) | 1993-03-25 | 2000-11-16 | Upjohn Co | Derivados de indol sustituidos por formil o ciano con actividad dopominergica. |
| KR100340159B1 (ko) | 1993-12-07 | 2002-11-23 | 일라이 릴리 앤드 캄파니 | 단백질키나제c억제제 |
| 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 |
| WO2002010169A1 (en) | 2000-07-31 | 2002-02-07 | F. Hoffmann-La Roche Ag | Piperazine derivatives |
| RU2275373C2 (ru) | 2000-12-08 | 2006-04-27 | Орто-Макнейл Фармасьютикал, Инк. | Макрогетероциклические соединения |
| 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 |
| ES2668834T3 (es) | 2008-09-08 | 2018-05-22 | Merck Serono Sa | Pirimidinas macrociclicas como inhibidores de proteína quinasas |
| SI2350075T1 (sl) * | 2008-09-22 | 2014-06-30 | Array Biopharma, Inc. | Substituirane imidazo (1,2b)piridazinske spojine kot Trk kinazni inhibitorji |
| CN102264736B (zh) * | 2008-10-22 | 2013-08-14 | 阵列生物制药公司 | 作为TRK激酶抑制剂的取代的吡唑并[1,5-a]嘧啶化合物 |
| BRPI0914404A2 (pt) | 2008-10-31 | 2019-03-06 | Genentech Inc | "compostos, composição farmacêutica e método para tratar ou atenuar a gravidade de uma doença ou condição responsiva à inibição da atividade jak quinase em um paciente" |
| 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 |
| WO2011045330A1 (en) | 2009-10-13 | 2011-04-21 | Tibotec Pharmaceuticals | Macrocyclic integrase inhibitors |
| WO2011071725A1 (en) | 2009-12-07 | 2011-06-16 | Boehringer Ingelheim International Gmbh | Heterocyclic compounds containing a pyrrolopyridine or benzimidazole core |
| US9150577B2 (en) | 2009-12-07 | 2015-10-06 | 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 |
| BR122019024201B1 (pt) | 2010-05-20 | 2021-08-03 | Array Biopharma Inc | Composto macrocíclico como inibidores de trk quinase, seu uso, e composição farmacêutica |
| 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 |
| MX2014001945A (es) | 2011-08-19 | 2014-03-27 | Merck Sharp & Dohme | Procedimiento e intermedios para la preparacion de macrolactamas. |
| 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 |
| MX347765B (es) | 2011-09-30 | 2017-05-12 | Oncodesign Sa | Inhibidores macrociclicos de la quinasa flt3. |
| KR20140077963A (ko) | 2011-10-20 | 2014-06-24 | 글락소스미스클라인 엘엘씨 | 시르투인 조절제로서의 치환된 비시클릭 아자-헤테로사이클 및 유사체 |
| CA2863892C (en) * | 2012-03-06 | 2016-08-30 | Pfizer Inc. | Macrocyclic derivatives for the treatment of proliferative diseases |
| DK2834243T3 (en) | 2012-03-09 | 2018-07-23 | Lexicon Pharmaceuticals Inc | Pyrazole [1,5-a] pyrimidine-based compounds, compositions comprising them and methods for their use |
| RU2014140739A (ru) | 2012-03-09 | 2016-04-27 | Лексикон Фармасьютикалз, Инк. | Соединения на основе имидазо[1, 2-b]пиридазина, композиции таких соединений и способы их применения |
| GB201205669D0 (en) | 2012-03-30 | 2012-05-16 | Agency Science Tech & Res | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
| EP2951174B1 (en) | 2013-01-30 | 2017-04-26 | Bayer Pharma Aktiengesellschaft | Amino-substituted isothiazoles |
| CN105358534A (zh) | 2013-04-23 | 2016-02-24 | 斯洛文尼亚莱柯制药股份有限公司 | 8-氯-1-甲基-苯并[d]吖庚因的新合成方法、新的中间体及其生产方法 |
| 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 |
| WO2015112806A2 (en) * | 2014-01-24 | 2015-07-30 | Tp Therapeutics, Inc. | Diaryl macrocycles as modulators of protein kinases |
| WO2016070241A1 (en) | 2014-11-03 | 2016-05-12 | Ctxt Pty Ltd | Triazine compounds, compositions and synthesis |
| HUE067779T2 (hu) | 2014-12-15 | 2024-11-28 | Cmg Pharmaceutical Co Ltd | Kondenzált gyûrûs heteroaril vegyületek és azok felhasználása TRK inhibitorokként |
| EP3259264B1 (en) | 2015-02-20 | 2022-07-27 | Rigel Pharmaceuticals, Inc. | Gdf-8 inhibitors |
| 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 |
| JP2018520992A (ja) | 2015-05-05 | 2018-08-02 | バイエル ファーマ アクチエンゲゼルシャフト | アミドで置換されているシクロヘキサン誘導体 |
| RU2732405C2 (ru) | 2015-07-02 | 2020-09-16 | Тёрнинг Поинт Терапьютикс, Инк. | Хиральные диарильные макроциклы в качестве модуляторов протеинкиназ |
| BR112018000297A2 (pt) | 2015-07-06 | 2018-09-04 | Tp Therapeutics Inc | polimorfo de macrociclo de diarila |
| WO2017015367A1 (en) | 2015-07-21 | 2017-01-26 | Tp Therapeutics, Inc. | Chiral diaryl macrocycles and uses thereof |
| 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 |
| JP7086395B2 (ja) | 2016-03-04 | 2022-06-20 | ヴァンダービルト ユニバーシティー | 置換インドールＭｃｌ－１阻害剤 |
| AU2017302019A1 (en) | 2016-07-28 | 2019-02-07 | Turning Point Therapeutics, Inc. | Macrocycle kinase inhibitors |
| WO2018112027A1 (en) | 2016-12-14 | 2018-06-21 | Development Center For Biotechnology | Antibody-drug conjugates and uses thereof |
| 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 |
| PT3658148T (pt) | 2017-07-28 | 2024-08-26 | Turning Point Therapeutics Inc | Compostos macrocíclicos e utilizações dos mesmos |
-
2016
- 2016-06-30 RU RU2018103907A patent/RU2732405C2/ru active
- 2016-06-30 EP EP16818768.0A patent/EP3317285B1/en active Active
- 2016-06-30 CA CA2989327A patent/CA2989327A1/en active Pending
- 2016-06-30 WO PCT/US2016/040329 patent/WO2017004342A1/en not_active Ceased
- 2016-06-30 JP JP2018500297A patent/JP6871903B2/ja active Active
- 2016-06-30 KR KR1020187002777A patent/KR102599788B1/ko active Active
- 2016-06-30 US US15/740,462 patent/US10316044B2/en active Active
- 2016-06-30 ES ES16818768T patent/ES2864839T3/es active Active
- 2016-06-30 AU AU2016287568A patent/AU2016287568B2/en not_active Ceased
- 2016-06-30 CN CN201680038613.1A patent/CN107735399B/zh active Active
- 2016-06-30 MX MX2017017097A patent/MX2017017097A/es unknown
- 2016-07-01 TW TW105121035A patent/TW201716415A/zh unknown
-
2017
- 2017-12-18 IL IL256377A patent/IL256377A/en unknown
-
2019
- 2019-05-29 US US16/425,407 patent/US11008337B2/en active Active
-
2020
- 2020-08-11 AU AU2020217336A patent/AU2020217336A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CY1120248T1 (el) | Ενωσεις ιμιδαζο[4,5-c]κινολιν-2-ονης και η χρηση τους στη θεραπευτικη αντιμετωπιση του καρκινου | |
| CY1124239T1 (el) | Ενωσεις αμινο-τριαζολοπυριδινης και χρηση αυτων στην αγωγη του καρκινου | |
| CY1124680T1 (el) | Παραγωγα 8-[6-[3-(αμινο)προποξυ]-3-πυριδυλο]-1-ισοπροπυλο-ιμιδαζο[4,5-c]κινολιν-2-ονης ως εκλεκτiκοι ρυθμιστες κινασης μεταλλαγμενης αταξιας τελαγγειεκτασιας (atm) για τη θεραπευτικη αγωγη του καρκινου | |
| MX375323B (es) | Inhibidores de cinasa de interacción con proteína cinasa activada por mitógeno (mnk) y métodos relacionados con los mismos. | |
| RU2018103907A (ru) | Хиральные диарильные макроциклы в качестве модуляторов протеинкиназ | |
| JP2021523221A5 (enExample) | ||
| CY1118572T1 (el) | Παραγωγο κυκλοαλκανιου | |
| EA201992126A1 (ru) | Ингибиторы jak, содержащие 4-членный гетероциклический амид | |
| JP2016527217A5 (enExample) | ||
| SI3009431T1 (en) | 2- (2,4,5-substituted-anilino) pyrimidine derivatives, as EGFR modulators useful for the treatment of cancer | |
| UA110259C2 (uk) | Похідні піролопіримідину і пурину | |
| CY1118135T1 (el) | Παραγωγα 2-(φαινυλο ή πυριδ-3-υλο) αμινοπυριμιδινης ως ρυθμιστες κινασης lrrk2 για τη θεραπευτικη αντιμετωπιση της νοσου του parkinson | |
| AR054127A1 (es) | Imidazoquinolinas como inhibidores de quinasa de lipido | |
| JP2017523152A5 (enExample) | ||
| AR106041A1 (es) | Moduladores de la proteína core de la hepatitis b | |
| JP2014521688A5 (enExample) | ||
| EA201291220A1 (ru) | Производные аминопиримидина в качестве модуляторов lrrk2 | |
| AR117189A1 (es) | Derivados de 6,7-dihidro-4h-pirazolo[1,5-a]pirazin indol-2-carboxamidas activos contra el virus de la hepatitis b (vhb) | |
| EA201001126A1 (ru) | Пирролопиримидины и пирролопиридины | |
| MY184433A (en) | 2,6-substituted purine derivatives and their use in the treatment of proliferative disorders | |
| JP2016529324A5 (enExample) | ||
| JP2016514719A5 (enExample) | ||
| RU2017111200A (ru) | Циклогексилэтилзамещенные диаза- и триаза-трициклические соединения в качестве антагонистов индоламин-2,3-диоксигеназы для лечения рака | |
| AR101177A1 (es) | Inhibidores de la syk | |
| JP2016537382A5 (enExample) |