JP2016538257A5 - - Google Patents
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- JP2016538257A5 JP2016538257A5 JP2016523939A JP2016523939A JP2016538257A5 JP 2016538257 A5 JP2016538257 A5 JP 2016538257A5 JP 2016523939 A JP2016523939 A JP 2016523939A JP 2016523939 A JP2016523939 A JP 2016523939A JP 2016538257 A5 JP2016538257 A5 JP 2016538257A5
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- JP
- Japan
- Prior art keywords
- monocyclic
- compound
- bicyclic
- pharmaceutically acceptable
- pharmaceutical composition
- 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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- 150000001875 compounds Chemical class 0.000 claims description 62
- 125000002950 monocyclic group Chemical group 0.000 claims description 44
- 239000008194 pharmaceutical composition Substances 0.000 claims description 34
- 150000003839 salts Chemical class 0.000 claims description 25
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 24
- 230000035772 mutation Effects 0.000 claims description 22
- 125000000217 alkyl group Chemical group 0.000 claims description 17
- 229910052739 hydrogen Inorganic materials 0.000 claims description 14
- 239000001257 hydrogen Substances 0.000 claims description 14
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 14
- 125000000623 heterocyclic group Chemical group 0.000 claims description 13
- 125000005843 halogen group Chemical group 0.000 claims description 12
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 10
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims description 10
- 239000003795 chemical substances by application Substances 0.000 claims description 10
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 7
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims description 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 6
- -1 C 1 -C 6 alkoxy Chemical group 0.000 claims description 5
- 125000002947 alkylene group Chemical group 0.000 claims description 5
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 229940079593 drug Drugs 0.000 claims description 4
- 125000001188 haloalkyl group Chemical group 0.000 claims description 4
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 4
- 208000008585 mastocytosis Diseases 0.000 claims description 4
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 3
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 claims description 3
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 3
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims description 3
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 3
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims description 2
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 2
- 125000000304 alkynyl group Chemical group 0.000 claims description 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 2
- 125000003118 aryl group Chemical group 0.000 claims description 2
- 125000004104 aryloxy group Chemical group 0.000 claims description 2
- 125000004429 atom Chemical group 0.000 claims description 2
- 229910052799 carbon Inorganic materials 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 125000000335 thiazolyl group Chemical group 0.000 claims description 2
- 125000001544 thienyl group Chemical group 0.000 claims description 2
- 150000003573 thiols Chemical class 0.000 claims description 2
- 201000008736 Systemic mastocytosis Diseases 0.000 claims 7
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 208000006343 Cutaneous Mastocytosis Diseases 0.000 claims 2
- 208000000516 mast-cell leukemia Diseases 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 101000692455 Homo sapiens Platelet-derived growth factor receptor beta Proteins 0.000 claims 1
- 102100026547 Platelet-derived growth factor receptor beta Human genes 0.000 claims 1
- 201000008213 SM-AHNMD Diseases 0.000 claims 1
- 208000032391 Smoldering systemic mastocytosis Diseases 0.000 claims 1
- 208000032488 Systemic mastocytosis with associated hematologic neoplasm Diseases 0.000 claims 1
- 208000014951 hematologic disease Diseases 0.000 claims 1
- 210000003630 histaminocyte Anatomy 0.000 claims 1
- 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 1
- 208000026901 systemic mastocytosis with an associated clonal hematologic non-mast cell lineage disease Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 description 3
- 125000006728 (C1-C6) alkynyl group Chemical group 0.000 description 1
- 0 C*c1cnc(N(CC2)CCN2c2ncn[n]3c2cc(*)c3)nc1 Chemical compound C*c1cnc(N(CC2)CCN2c2ncn[n]3c2cc(*)c3)nc1 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 description 1
- 125000004001 thioalkyl group Chemical group 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361892086P | 2013-10-17 | 2013-10-17 | |
| US61/892,086 | 2013-10-17 | ||
| US201461931204P | 2014-01-24 | 2014-01-24 | |
| US61/931,204 | 2014-01-24 | ||
| US201461975229P | 2014-04-04 | 2014-04-04 | |
| US61/975,229 | 2014-04-04 | ||
| PCT/US2014/060746 WO2015057873A1 (en) | 2013-10-17 | 2014-10-15 | Compositions useful for treating disorders related to kit |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018224481A Division JP6782756B2 (ja) | 2013-10-17 | 2018-11-30 | Kitに関連する疾患を治療するために有用な化合物の製法と中間体化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016538257A JP2016538257A (ja) | 2016-12-08 |
| JP2016538257A5 true JP2016538257A5 (https=) | 2017-11-24 |
| JP6446040B2 JP6446040B2 (ja) | 2018-12-26 |
Family
ID=51904226
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016523939A Active JP6446040B2 (ja) | 2013-10-17 | 2014-10-15 | Kitに関連する疾患を治療するために有用な組成物 |
| JP2018224481A Active JP6782756B2 (ja) | 2013-10-17 | 2018-11-30 | Kitに関連する疾患を治療するために有用な化合物の製法と中間体化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018224481A Active JP6782756B2 (ja) | 2013-10-17 | 2018-11-30 | Kitに関連する疾患を治療するために有用な化合物の製法と中間体化合物 |
Country Status (30)
| Country | Link |
|---|---|
| US (7) | US9200002B2 (https=) |
| EP (2) | EP3057969B1 (https=) |
| JP (2) | JP6446040B2 (https=) |
| KR (1) | KR102378689B1 (https=) |
| CN (2) | CN110003217B (https=) |
| AU (1) | AU2014337314B2 (https=) |
| BR (1) | BR112016008541B1 (https=) |
| CA (1) | CA2926999C (https=) |
| CY (2) | CY1121182T1 (https=) |
| DK (1) | DK3057969T3 (https=) |
| ES (2) | ES2923888T3 (https=) |
| HR (1) | HRP20181388T1 (https=) |
| HU (3) | HUE059041T2 (https=) |
| IL (1) | IL244677B (https=) |
| LT (2) | LT3057969T (https=) |
| MX (1) | MX365614B (https=) |
| NL (1) | NL301094I2 (https=) |
| NO (1) | NO2021012I1 (https=) |
| PH (1) | PH12016500611A1 (https=) |
| PL (2) | PL3057969T3 (https=) |
| PT (2) | PT3409674T (https=) |
| RS (1) | RS57542B1 (https=) |
| RU (1) | RU2706235C2 (https=) |
| SG (1) | SG11201602937UA (https=) |
| SI (1) | SI3057969T1 (https=) |
| SM (1) | SMT201800448T1 (https=) |
| TW (1) | TWI683814B (https=) |
| UY (1) | UY35787A (https=) |
| WO (1) | WO2015057873A1 (https=) |
| ZA (1) | ZA201601970B (https=) |
Families Citing this family (83)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| SG11201500125QA (en) | 2012-07-11 | 2015-02-27 | Blueprint Medicines Corp | Inhibitors of the fibroblast growth factor receptor |
| EP3943087A1 (en) | 2013-03-15 | 2022-01-26 | Celgene CAR LLC | Heteroaryl compounds and uses thereof |
| CN105307657B (zh) | 2013-03-15 | 2020-07-10 | 西建卡尔有限责任公司 | 杂芳基化合物和其用途 |
| US9321786B2 (en) | 2013-03-15 | 2016-04-26 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| WO2014160521A1 (en) | 2013-03-15 | 2014-10-02 | Blueprint Medicines Corporation | Piperazine derivatives and their use as kit modulators |
| FR3008779B1 (fr) | 2013-07-19 | 2018-01-26 | Areva Np | Barre antivibratoire pour faisceau de tubes d'un generateur de vapeur |
| SI3057969T1 (sl) | 2013-10-17 | 2018-10-30 | Blueprint Medicines Corporation | Sestavki, uporabni za zdravljenje motenj, povezanih s KIT |
| WO2015058129A1 (en) | 2013-10-17 | 2015-04-23 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| RS63405B1 (sr) | 2013-10-25 | 2022-08-31 | Blueprint Medicines Corp | Inhibitori receptora faktora rasta fibroblasta |
| US9695165B2 (en) | 2014-01-15 | 2017-07-04 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| WO2015160665A1 (en) | 2014-04-15 | 2015-10-22 | Dow Agrosciences Llc | Metalloenzyme inhibitor compounds as fungicides |
| US9688680B2 (en) | 2014-08-04 | 2017-06-27 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| WO2016127074A1 (en) | 2015-02-06 | 2016-08-11 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as ret inhibitors |
| WO2017004134A1 (en) * | 2015-06-29 | 2017-01-05 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| BR112018000808A2 (pt) | 2015-07-16 | 2018-09-04 | Array Biopharma Inc | compostos de pirazolo[1,5-a]piridina substituída como inibidores de ret cinase |
| CN108026102A (zh) | 2015-07-24 | 2018-05-11 | 蓝印药品公司 | 可用于治疗与kit和pdgfr相关的病症的化合物 |
| BR112018003588A2 (pt) | 2015-08-26 | 2018-09-25 | Blueprint Medicines Corp | compostos e composições úteis para tratamento de distúrbios relacionados ao ntrk |
| 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 |
| SI3371171T1 (sl) | 2015-11-02 | 2024-03-29 | Blueprint Medicines Corporation | Inhibitorji ret |
| SG10201912607SA (en) | 2015-11-19 | 2020-02-27 | Blueprint Medicines Corp | Compounds and compositions useful for treating disorders related to ntrk |
| US10183928B2 (en) | 2016-03-17 | 2019-01-22 | Blueprint Medicines Corporation | Inhibitors of RET |
| 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 |
| AU2017246547B2 (en) | 2016-04-04 | 2023-02-23 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| CN109311889B (zh) * | 2016-04-15 | 2021-11-16 | 缆图药品公司 | 激活素受体样激酶抑制剂 |
| 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 |
| US10227329B2 (en) | 2016-07-22 | 2019-03-12 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to RET |
| WO2018022761A1 (en) * | 2016-07-27 | 2018-02-01 | Blueprint Medicines Corporation | Substituted cyclopentane-amides for treating disorders related to ret |
| TWI752098B (zh) | 2016-10-10 | 2022-01-11 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| WO2018136661A1 (en) | 2017-01-18 | 2018-07-26 | Andrews Steven W | SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| US11040979B2 (en) | 2017-03-31 | 2021-06-22 | Blueprint Medicines Corporation | Substituted pyrrolo[1,2-b]pyridazines for treating disorders related to KIT and PDGFR |
| TWI876442B (zh) | 2017-10-10 | 2025-03-11 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
| EP3697786B1 (en) | 2017-10-18 | 2022-08-31 | Blueprint Medicines Corporation | Substituted pyrrolopyridines as inhibitors of activin receptor-like kinase |
| CN108191874B (zh) * | 2018-01-16 | 2019-11-29 | 成都施贝康生物医药科技有限公司 | 一种C-Kit抑制剂及其应用 |
| EP3740490A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| JP7060694B2 (ja) | 2018-01-18 | 2022-04-26 | アレイ バイオファーマ インコーポレイテッド | Retキナーゼ阻害剤としての置換ピロロ[2,3-d]ピリミジン化合物 |
| US11472802B2 (en) | 2018-01-18 | 2022-10-18 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors |
| PE20210096A1 (es) | 2018-04-03 | 2021-01-12 | Blueprint Medicines Corp | Inhibidor de ret para uso en tratar cancer que tiene una alteracion de ret |
| CN109970745B (zh) * | 2018-04-16 | 2020-12-08 | 深圳市塔吉瑞生物医药有限公司 | 取代的吡咯并三嗪类化合物及其药物组合物及其用途 |
| US20210205782A1 (en) | 2018-06-22 | 2021-07-08 | Comercializadora Innvento S.A. | Multilayer absorbent filtering item comprising a first layer of a porous activated carbon support disposed on a nonwoven polyester-fibre felt, a second layer of a polymer film and a third layer of an active ingredient; method for obtaining said item; and use of same |
| CN117285467A (zh) | 2018-07-31 | 2023-12-26 | 罗索肿瘤学公司 | 喷雾干燥的分散体和制剂 |
| CN112996794A (zh) | 2018-09-10 | 2021-06-18 | 阿雷生物药品公司 | 作为ret激酶抑制剂的稠合杂环化合物 |
| US20220010382A1 (en) | 2018-11-12 | 2022-01-13 | Blueprint Medicines Corporation | Avapritinib resistance of kit mutants |
| CN109232583A (zh) * | 2018-11-29 | 2019-01-18 | 尚科生物医药(上海)有限公司 | 一种6-溴-3H-吡咯并[2,1-f][1,2,4]三嗪-4-酮的制备方法 |
| US12351571B2 (en) | 2018-12-19 | 2025-07-08 | Array Biopharma Inc. | Substituted quinoxaline compounds as inhibitors of FGFR tyrosine kinases |
| EP3898626A1 (en) | 2018-12-19 | 2021-10-27 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases |
| CN111410648B (zh) * | 2019-01-07 | 2024-03-29 | 浙江海正药业股份有限公司 | 一种手性c-KIT抑制剂药物关键中间体及其制备方法 |
| ES2966512T3 (es) | 2019-04-12 | 2024-04-22 | Blueprint Medicines Corp | Formas cristalinas de (S)-1-(4-fluorofenil)-1-(2-(4-(6-(1-metil-1H-pirazol-4-il)pirrolo[2,1-f][1,2,4]triazin-4-il)piperazinil)-pirimidin-5-il)etan-1-amina y métodos de elaboración |
| BR112021020441A2 (pt) | 2019-04-12 | 2021-12-14 | Blueprint Medicines Corp | Derivados de pirrolotriazina para tratar doenças mediadas por kit e pdgfra |
| WO2020234381A1 (en) | 2019-05-21 | 2020-11-26 | Janssen Pharmaceutica Nv | Processes and intermediates for preparing a btk inhibitor |
| CN114341138A (zh) * | 2019-07-09 | 2022-04-12 | 桑多斯股份公司 | 口服可用的选择性kit和pdgfr激酶抑制剂的晶型 |
| TW202126306A (zh) * | 2019-10-04 | 2021-07-16 | 美商纜圖藥品公司 | 嗜酸性球性病症之治療 |
| GB201915447D0 (en) | 2019-10-24 | 2019-12-11 | Johnson Matthey Plc | Polymorphs of avapritinib and methods of preparing the polymorphs |
| TW202122089A (zh) * | 2019-11-04 | 2021-06-16 | 美商纜圖藥品公司 | 肥大細胞疾病及嗜酸性病症之治療 |
| US20230101747A1 (en) | 2019-12-06 | 2023-03-30 | Schrödinger, Inc. | Cyclic compounds and methods of using same |
| CN110950872A (zh) * | 2019-12-25 | 2020-04-03 | 武汉九州钰民医药科技有限公司 | 制备靶向抗癌药avapritinib的方法 |
| CN110938077B (zh) * | 2019-12-25 | 2021-04-27 | 武汉九州钰民医药科技有限公司 | 合成Avapritinib的方法 |
| IL294214B2 (en) | 2019-12-27 | 2026-04-01 | Schrodinger Inc | Cyclic compounds and methods for using them |
| WO2021183709A1 (en) | 2020-03-11 | 2021-09-16 | Teva Czech Industries S.R.O | Solid state forms of avapritinib and process for preparation thereof |
| EP4157829A1 (en) | 2020-05-29 | 2023-04-05 | Blueprint Medicines Corporation | Solid forms of pralsetinib |
| WO2021257522A1 (en) | 2020-06-17 | 2021-12-23 | Teva Czech Industries S.R.O | Solid state forms of avapritinib salts |
| JP2023537470A (ja) | 2020-08-03 | 2023-09-01 | ヤンセン バイオテツク,インコーポレーテツド | ウイルス治療における多方向バイオ輸送のための材料及び方法 |
| CN116490507A (zh) | 2020-09-10 | 2023-07-25 | 薛定谔公司 | 用于治疗癌症的杂环包缩合cdc7激酶抑制剂 |
| US20230391780A1 (en) | 2020-10-14 | 2023-12-07 | Blueprint Medicines Corporation | Compositions and methods for treating kit- and pdgfra-mediated diseases |
| US20240010652A1 (en) * | 2020-10-14 | 2024-01-11 | Blueprint Medicines Corporation | Compositions and methods for treating kit- and pdgfra-mediated diseases |
| CN112552339A (zh) * | 2020-12-10 | 2021-03-26 | 安徽昊帆生物有限公司 | 一种o-二苯基磷酰羟胺的制备方法 |
| EP4284804A1 (en) | 2021-01-26 | 2023-12-06 | Schrödinger, Inc. | Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disorders |
| HU231413B1 (hu) | 2021-02-26 | 2023-08-28 | Egis Gyógyszergyár Zrt. | Eljárás avapritinib és intermedierek előállítására |
| TW202300150A (zh) | 2021-03-18 | 2023-01-01 | 美商薛定諤公司 | 環狀化合物及其使用方法 |
| CN113278023B (zh) * | 2021-07-22 | 2021-10-15 | 上海睿跃生物科技有限公司 | 含氮杂环化合物及其制备方法和应用 |
| CN113686987B (zh) * | 2021-08-19 | 2022-04-26 | 海南医学院 | 一种用于检测Avapritinib中间体中对映异构体的方法 |
| AU2022379973A1 (en) | 2021-11-08 | 2024-06-27 | Progentos Therapeutics, Inc. | Platelet-derived growth factor receptor (pdgfr) alpha inhibitors and uses thereof |
| TW202404949A (zh) * | 2022-04-19 | 2024-02-01 | 美商纜圖藥品公司 | Kit抑制劑 |
| US20240382493A1 (en) * | 2023-05-18 | 2024-11-21 | Blueprint Medicines Corporation | Methods for treating systemic mastocytosis and gastrointestinal stromal tumors |
| EP4719421A1 (en) * | 2023-06-02 | 2026-04-08 | Idrx, Inc. | Combination therapy comprising kit inhibitors for use in the treatment of cancer |
| WO2025059027A1 (en) | 2023-09-11 | 2025-03-20 | Schrödinger, Inc. | Cyclopenta[e]pyrazolo[1,5-a]pyrimidine derivatives as malt1 inhibitors |
| WO2025170989A1 (en) | 2024-02-05 | 2025-08-14 | Blueprint Medicines Corporation | High-risk disease features of indolent systemic mastocytosis and methods for treating |
Family Cites Families (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS61238784A (ja) | 1985-04-17 | 1986-10-24 | Sumitomo Seiyaku Kk | コハク酸イミド誘導体及びその酸付加塩 |
| JP4649046B2 (ja) * | 1999-05-21 | 2011-03-09 | ブリストル−マイヤーズ スクイブ カンパニー | キナーゼのピロロトリアジン阻害剤 |
| US6982265B1 (en) | 1999-05-21 | 2006-01-03 | Bristol Myers Squibb Company | Pyrrolotriazine inhibitors of kinases |
| MXPA02003436A (es) | 1999-10-07 | 2002-08-20 | Amgen Inc | Inhibidores de triazina cinasa. |
| US6784603B2 (en) * | 2001-07-20 | 2004-08-31 | Teledyne Lighting And Display Products, Inc. | Fluorescent lighting apparatus |
| SE0102616D0 (sv) | 2001-07-25 | 2001-07-25 | Astrazeneca Ab | Novel compounds |
| PT1497019E (pt) | 2002-04-23 | 2015-09-10 | Bristol Myers Squibb Co | Compostos de pirrolotriazina anilina úteis como inibidores de quinase |
| TW200508224A (en) * | 2003-02-12 | 2005-03-01 | Bristol Myers Squibb Co | Cyclic derivatives as modulators of chemokine receptor activity |
| US7468376B2 (en) * | 2003-02-27 | 2008-12-23 | Palau Pharma, S.A. | Pyrazolopyridine derivates |
| WO2005117909A2 (en) | 2004-04-23 | 2005-12-15 | Exelixis, Inc. | Kinase modulators and methods of use |
| WO2006028524A2 (en) | 2004-04-29 | 2006-03-16 | Pharmix Corporation | Compositions and treatments for inhibiting kinase and/or hmg-coa reductase |
| US7439246B2 (en) * | 2004-06-28 | 2008-10-21 | Bristol-Myers Squibb Company | Fused heterocyclic kinase inhibitors |
| US7173031B2 (en) | 2004-06-28 | 2007-02-06 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| JP5116687B2 (ja) * | 2005-11-02 | 2013-01-09 | バイエル・ファルマ・アクチェンゲゼルシャフト | がんおよび他の過剰増殖性疾患の処置のためのピロロ[2,1−f][1,2,4]トリアジン−4−イルアミンIGF−1Rキナーゼ阻害剤 |
| US7348325B2 (en) * | 2005-11-30 | 2008-03-25 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| CN101007814A (zh) * | 2006-01-27 | 2007-08-01 | 上海恒瑞医药有限公司 | 吡咯并六元杂环化合物及其在医药上的用途 |
| DK1973910T3 (da) * | 2006-01-27 | 2013-08-12 | Shanghai Hengrui Pharm Co Ltd | Pyrrolo[3,2-c]pyridin-4-on-2-indolinon-proteinkinaseinhibitorer |
| HRP20140688T1 (hr) * | 2006-07-07 | 2014-10-24 | Bristol-Myers Squibb Company | Inhibitori piroltriazin kinaze |
| US8415340B2 (en) | 2007-07-25 | 2013-04-09 | Bristol-Myers Squibb Company | Triazine kinase inhibitors |
| CA2716856C (en) | 2008-03-20 | 2013-02-19 | Amgen Inc. | Aurora kinase modulators and method of use |
| KR20100003912A (ko) | 2008-07-02 | 2010-01-12 | 삼성전자주식회사 | 동일 포맷의 미디어 파일 간에 미디어 정보 호환이 가능한미디어 파일을 생성하는 방법 및 장치와 미디어 파일을실행하는 방법 및 장치 |
| WO2010022055A2 (en) | 2008-08-20 | 2010-02-25 | Amgen Inc. | Inhibitors of voltage-gated sodium channels |
| JP2012529512A (ja) | 2009-06-08 | 2012-11-22 | アブラクシス バイオサイエンス リミテッド ライアビリティー カンパニー | トリアジン誘導体類及びそれらの治療応用 |
| CA2767008C (en) | 2009-07-07 | 2018-01-30 | Pathway Therapeutics, Inc. | Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy |
| WO2011103196A1 (en) | 2010-02-17 | 2011-08-25 | Amgen Inc. | Aryl carboxamide derivatives as sodium channel inhibitors for treatment of pain |
| US8609672B2 (en) | 2010-08-27 | 2013-12-17 | University Of The Pacific | Piperazinylpyrimidine analogues as protein kinase inhibitors |
| CN102040494A (zh) | 2010-11-12 | 2011-05-04 | 西北师范大学 | 对氟苯甲醛的制备方法 |
| NZ611529A (en) * | 2010-12-23 | 2015-06-26 | Pfizer | Glucagon receptor modulators |
| SG11201500125QA (en) | 2012-07-11 | 2015-02-27 | Blueprint Medicines Corp | Inhibitors of the fibroblast growth factor receptor |
| EP2892534B8 (en) | 2012-09-06 | 2021-09-15 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| MX365640B (es) | 2012-12-21 | 2019-06-10 | Plexxikon Inc | Compuestos y metodos para la modulacion de quinasas y sus indicaciones. |
| TWI629266B (zh) | 2012-12-28 | 2018-07-11 | 藍印藥品公司 | 纖維母細胞生長因子受體之抑制劑 |
| WO2014160521A1 (en) | 2013-03-15 | 2014-10-02 | Blueprint Medicines Corporation | Piperazine derivatives and their use as kit modulators |
| SI3057969T1 (sl) * | 2013-10-17 | 2018-10-30 | Blueprint Medicines Corporation | Sestavki, uporabni za zdravljenje motenj, povezanih s KIT |
| WO2015058129A1 (en) | 2013-10-17 | 2015-04-23 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| RS63405B1 (sr) | 2013-10-25 | 2022-08-31 | Blueprint Medicines Corp | Inhibitori receptora faktora rasta fibroblasta |
| US9695165B2 (en) | 2014-01-15 | 2017-07-04 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| US9688680B2 (en) | 2014-08-04 | 2017-06-27 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| WO2016127074A1 (en) | 2015-02-06 | 2016-08-11 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as ret inhibitors |
| CN108026102A (zh) | 2015-07-24 | 2018-05-11 | 蓝印药品公司 | 可用于治疗与kit和pdgfr相关的病症的化合物 |
| BR112018003588A2 (pt) | 2015-08-26 | 2018-09-25 | Blueprint Medicines Corp | compostos e composições úteis para tratamento de distúrbios relacionados ao ntrk |
| SI3371171T1 (sl) | 2015-11-02 | 2024-03-29 | Blueprint Medicines Corporation | Inhibitorji ret |
| SG10201912607SA (en) | 2015-11-19 | 2020-02-27 | Blueprint Medicines Corp | Compounds and compositions useful for treating disorders related to ntrk |
| US10183928B2 (en) | 2016-03-17 | 2019-01-22 | Blueprint Medicines Corporation | Inhibitors of RET |
| CN109311889B (zh) | 2016-04-15 | 2021-11-16 | 缆图药品公司 | 激活素受体样激酶抑制剂 |
| US10227329B2 (en) | 2016-07-22 | 2019-03-12 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to RET |
| WO2018022761A1 (en) | 2016-07-27 | 2018-02-01 | Blueprint Medicines Corporation | Substituted cyclopentane-amides for treating disorders related to ret |
| WO2018049233A1 (en) | 2016-09-08 | 2018-03-15 | Nicolas Stransky | Inhibitors of the fibroblast growth factor receptor in combination with cyclin-dependent kinase inhibitors |
| US11040979B2 (en) | 2017-03-31 | 2021-06-22 | Blueprint Medicines Corporation | Substituted pyrrolo[1,2-b]pyridazines for treating disorders related to KIT and PDGFR |
| CN109400610A (zh) | 2017-08-18 | 2019-03-01 | 浙江海正药业股份有限公司 | 吡咯并三嗪类衍生物、其制备方法及其在医药上的用途 |
| CN108191874B (zh) | 2018-01-16 | 2019-11-29 | 成都施贝康生物医药科技有限公司 | 一种C-Kit抑制剂及其应用 |
| US20220010382A1 (en) | 2018-11-12 | 2022-01-13 | Blueprint Medicines Corporation | Avapritinib resistance of kit mutants |
| ES2966512T3 (es) | 2019-04-12 | 2024-04-22 | Blueprint Medicines Corp | Formas cristalinas de (S)-1-(4-fluorofenil)-1-(2-(4-(6-(1-metil-1H-pirazol-4-il)pirrolo[2,1-f][1,2,4]triazin-4-il)piperazinil)-pirimidin-5-il)etan-1-amina y métodos de elaboración |
| CN110950872A (zh) | 2019-12-25 | 2020-04-03 | 武汉九州钰民医药科技有限公司 | 制备靶向抗癌药avapritinib的方法 |
| CN110938077B (zh) | 2019-12-25 | 2021-04-27 | 武汉九州钰民医药科技有限公司 | 合成Avapritinib的方法 |
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