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) | CN110003217B (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) | HUE059041T2 (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) | PT3057969T (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 (84)
| Publication number | Priority date | Publication date | Assignee | Title |
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| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| NZ703495A (en) | 2012-07-11 | 2018-02-23 | Blueprint Medicines Corp | Inhibitors of the fibroblast growth factor receptor |
| WO2014160521A1 (en) | 2013-03-15 | 2014-10-02 | Blueprint Medicines Corporation | Piperazine derivatives and their use as kit modulators |
| MY181020A (en) | 2013-03-15 | 2020-12-16 | Sanofi Sa | Heteroaryl compounds and uses thereof |
| TWI647220B (zh) | 2013-03-15 | 2019-01-11 | 美商西建卡爾有限責任公司 | 雜芳基化合物及其用途 |
| 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 |
| MX365614B (es) * | 2013-10-17 | 2019-06-07 | Blueprint Medicines Corp | Composiciones utiles para tratar trastornos relacionados con kit. |
| PT3395814T (pt) | 2013-10-25 | 2022-07-27 | Blueprint Medicines Corp | Inibidores do recetor do fator de crescimento de fibroblastos |
| WO2015108992A1 (en) | 2014-01-15 | 2015-07-23 | Blueprint Medicines Corporation | Heterobicyclic compounds and their use as fgfr4 receptor inhibitors |
| 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 |
| US9688680B2 (en) | 2014-08-04 | 2017-06-27 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| US10202365B2 (en) | 2015-02-06 | 2019-02-12 | 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 |
| CA2992586A1 (en) | 2015-07-16 | 2017-01-19 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
| BR112018001190A2 (pt) | 2015-07-24 | 2018-09-11 | Blueprint Medicines Corp | composições úteis para tratar distúrbios relacionados a kit e pdfgr |
| WO2017035354A1 (en) | 2015-08-26 | 2017-03-02 | Blueprint Medicines Corporation | Compounds and compositions useful for treating disorders related to 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 |
| RS65069B1 (sr) | 2015-11-02 | 2024-02-29 | Blueprint Medicines Corp | Inhibitori ret-a |
| SG10201912607SA (en) | 2015-11-19 | 2020-02-27 | Blueprint Medicines Corp | Compounds and compositions useful for treating disorders related to ntrk |
| AR107912A1 (es) | 2016-03-17 | 2018-06-28 | Blueprint Medicines Corp | Inhibidores de ret |
| 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 |
| FI3442977T3 (fi) | 2016-04-15 | 2023-09-26 | Blueprint Medicines Corp | Aktiviinireseptorin kaltaisen kinaasin estäjät |
| 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. |
| WO2018017983A1 (en) | 2016-07-22 | 2018-01-25 | 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 |
| 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 |
| 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 |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| 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 |
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