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
- Authority
- 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 (enExample) | 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 (enExample) |
| EP (2) | EP3409674B1 (enExample) |
| JP (2) | JP6446040B2 (enExample) |
| KR (1) | KR102378689B1 (enExample) |
| CN (2) | CN105658652B (enExample) |
| AU (1) | AU2014337314B2 (enExample) |
| BR (1) | BR112016008541B1 (enExample) |
| CA (1) | CA2926999C (enExample) |
| CY (2) | CY1121182T1 (enExample) |
| DK (1) | DK3057969T3 (enExample) |
| ES (2) | ES2923888T3 (enExample) |
| HR (1) | HRP20181388T1 (enExample) |
| HU (3) | HUE039687T2 (enExample) |
| IL (1) | IL244677B (enExample) |
| LT (2) | LT3057969T (enExample) |
| MX (1) | MX365614B (enExample) |
| NL (1) | NL301094I2 (enExample) |
| NO (1) | NO2021012I1 (enExample) |
| PH (1) | PH12016500611A1 (enExample) |
| PL (2) | PL3057969T3 (enExample) |
| PT (2) | PT3409674T (enExample) |
| RS (1) | RS57542B1 (enExample) |
| RU (1) | RU2706235C2 (enExample) |
| SG (1) | SG11201602937UA (enExample) |
| SI (1) | SI3057969T1 (enExample) |
| SM (1) | SMT201800448T1 (enExample) |
| TW (1) | TWI683814B (enExample) |
| UY (1) | UY35787A (enExample) |
| WO (1) | WO2015057873A1 (enExample) |
| ZA (1) | ZA201601970B (enExample) |
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 |
| DK2872491T3 (da) | 2012-07-11 | 2021-08-09 | Blueprint Medicines Corp | Inhibitorer af fibroblastvækstfaktorreceptoren |
| WO2014160521A1 (en) | 2013-03-15 | 2014-10-02 | Blueprint Medicines Corporation | Piperazine derivatives and their use as kit modulators |
| US9321786B2 (en) | 2013-03-15 | 2016-04-26 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| EP3943087A1 (en) | 2013-03-15 | 2022-01-26 | Celgene CAR LLC | Heteroaryl compounds and uses thereof |
| FR3008779B1 (fr) | 2013-07-19 | 2018-01-26 | Areva Np | Barre antivibratoire pour faisceau de tubes d'un generateur de vapeur |
| US9334263B2 (en) | 2013-10-17 | 2016-05-10 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| PT3409674T (pt) | 2013-10-17 | 2022-07-18 | Blueprint Medicines Corp | Processo para preparar composições úteis para tratar distúrbios relacionados com kit |
| BR112016008849B8 (pt) | 2013-10-25 | 2022-09-06 | Blueprint Medicines Corp | Compostos ou sais farmaceuticamente aceitáveis dos mesmos, uso dos referidos compostos e composições farmacêuticas |
| US9695165B2 (en) | 2014-01-15 | 2017-07-04 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| MA38393B1 (fr) | 2014-03-13 | 2018-11-30 | Sanofi Sa | Composés hétéroaryle et utilisations associées |
| CA2945674A1 (en) * | 2014-04-15 | 2015-10-22 | Dow Agrosciences Llc | Metalloenzyme inhibitor compounds as fungicides |
| WO2016022569A1 (en) | 2014-08-04 | 2016-02-11 | 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 |
| PT3322706T (pt) | 2015-07-16 | 2021-03-08 | Array Biopharma Inc | Compostos de pirazolo[1,5-a]piridina substituídos como inibidores da quinase do ret |
| RU2018106483A (ru) | 2015-07-24 | 2019-08-26 | Блюпринт Медсинс Корпорейшн | Соединения, подходящие для лечения расстройств, связанных с kit и pdgfr |
| BR112018003588A2 (pt) | 2015-08-26 | 2018-09-25 | Blueprint Medicines Corp | compostos e composições úteis para tratamento de distúrbios relacionados ao ntrk |
| TN2019000271A1 (en) | 2015-10-26 | 2021-01-07 | Univ Colorado Regents | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| EP3371171B1 (en) | 2015-11-02 | 2023-10-25 | Blueprint Medicines Corporation | Inhibitors of ret |
| RU2018122089A (ru) | 2015-11-19 | 2019-12-25 | Блюпринт Медсинс Корпорейшн | Соединения и композиции, подходящие для лечения расстройств, связанных с ntrk |
| WO2017161269A1 (en) | 2016-03-17 | 2017-09-21 | Blueprint Medicines Corporation | Inhibitors of ret receptor tyrosine kinases |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| IL304018A (en) | 2016-04-04 | 2023-08-01 | Loxo Oncology Inc | Liquid formulations of (S)-N-(5-((R)-2-(5,2-difluorophenyl)-pyrrolidine-1-yl)-pyrazolo[5,1-A]pyrimidin-3-yl)-3 -hydroxypyrrolidine-1-carboxamide |
| TN2019000332A1 (en) | 2016-04-04 | 2021-05-07 | Loxo Oncology Inc | Methods of treating pediatric cancers |
| FI3442977T3 (fi) * | 2016-04-15 | 2023-09-26 | Blueprint Medicines Corp | Aktiviinireseptorin kaltaisen kinaasin estäjät |
| ES2952056T3 (es) | 2016-05-18 | 2023-10-26 | Loxo Oncology Inc | Preparación de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida |
| US10227329B2 (en) | 2016-07-22 | 2019-03-12 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to RET |
| US10035789B2 (en) * | 2016-07-27 | 2018-07-31 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to RET |
| 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 |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| 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 |
| JP6888101B2 (ja) | 2017-01-18 | 2021-06-16 | 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ラゾロ［１，５−ａ］ピラジン化合物 |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| WO2018183712A1 (en) * | 2017-03-31 | 2018-10-04 | Blueprint Medicines Corporation | Pyrrolo[1,2-b]pyridazine compounds and compositions useful 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 |
| WO2019143991A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | SUBSTITUTED PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS AS RET KINASE INHIBITORS |
| WO2019143977A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| JP6997876B2 (ja) | 2018-01-18 | 2022-02-04 | 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ラゾリル［４，３－ｃ］ピリジン化合物 |
| BR112020020273A2 (pt) | 2018-04-03 | 2021-04-06 | Blueprint Medicines Corporation | Inibidor de ret para uso no tratamento de câncer tendo uma alteração de ret |
| JP7710223B2 (ja) * | 2018-04-16 | 2025-07-18 | 深▲チェン▼市塔吉瑞生物医薬有限公司 | 置換ピロロトリアジン系化合物およびその医薬組成物並びにそれらの使用 |
| WO2019165566A1 (es) | 2018-06-22 | 2019-09-06 | Comercializadora Innvento S.A. | Artículo filtrante-absorbente multicapa que comprende una primera capa de un soporte poroso de carbón activado dispuesto sobre un fieltro no tejido de fibras de poliéster, una segunda capa de una película de polímero y una tercera capa de un agente activo; proceso para obtener dicho artículo; y uso del mismo |
| JP7286755B2 (ja) | 2018-07-31 | 2023-06-05 | ロクソ オンコロジー， インコーポレイテッド | （ｓ）－５－アミノ－３－（４－（（５－フルオロ－２－メトキシベンズアミド）メチル）フェニル）－１－（１，１，１－トリフルオロプロパン－２－イル）－１ｈ－ピラゾール－４－カルボキサミドの噴霧乾燥分散体および製剤 |
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| 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 |
| CN113474337A (zh) | 2018-12-19 | 2021-10-01 | 奥瑞生物药品公司 | 作为fgfr抑制剂用于治疗癌症的7-((3，5-二甲氧基苯基)氨基)喹喔啉衍生物 |
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| 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 |
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