JP2017527578A5 - - Google Patents
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- Publication number
- JP2017527578A5 JP2017527578A5 JP2017513450A JP2017513450A JP2017527578A5 JP 2017527578 A5 JP2017527578 A5 JP 2017527578A5 JP 2017513450 A JP2017513450 A JP 2017513450A JP 2017513450 A JP2017513450 A JP 2017513450A JP 2017527578 A5 JP2017527578 A5 JP 2017527578A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- compound
- irritable bowel
- bowel syndrome
- 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
- 150000003839 salts Chemical class 0.000 claims 8
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- -1 2- (dimethylamino) ethyl Chemical group 0.000 claims 4
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 4
- 108091000080 Phosphotransferase Proteins 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 4
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 4
- 230000001404 mediated effect Effects 0.000 claims 4
- 102000020233 phosphotransferase Human genes 0.000 claims 4
- 238000000634 powder X-ray diffraction Methods 0.000 claims 4
- 206010010774 Constipation Diseases 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 230000005855 radiation Effects 0.000 claims 2
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 1
- 208000004998 Abdominal Pain Diseases 0.000 claims 1
- 206010012735 Diarrhoea Diseases 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims 1
- QIAFMBKCNZACKA-UHFFFAOYSA-N N-benzoylglycine Chemical compound OC(=O)CNC(=O)C1=CC=CC=C1 QIAFMBKCNZACKA-UHFFFAOYSA-N 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- 206010036772 Proctalgia Diseases 0.000 claims 1
- 229940009098 aspartate Drugs 0.000 claims 1
- 239000013078 crystal Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 201000000117 functional diarrhea Diseases 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 238000001890 transfection Methods 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2014086197 | 2014-09-10 | ||
| CNPCT/CN2014/086197 | 2014-09-10 | ||
| CN2015086995 | 2015-08-14 | ||
| CNPCT/CN2015/086995 | 2015-08-14 | ||
| PCT/IB2015/056905 WO2016038552A1 (en) | 2014-09-10 | 2015-09-09 | Pyridone derivatives as rearranged during transfection (ret) kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019102776A Division JP6728447B2 (ja) | 2014-09-10 | 2019-05-31 | Ｒｅｔ（ｒｅａｒｒａｎｇｅｄ ｄｕｒｉｎｇ ｔｒａｎｓｆｅｃｔｉｏｎ）キナーゼ阻害剤としてのピリジン誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017527578A JP2017527578A (ja) | 2017-09-21 |
| JP2017527578A5 true JP2017527578A5 (2) | 2018-10-25 |
| JP6538154B2 JP6538154B2 (ja) | 2019-07-03 |
Family
ID=54186249
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017513450A Expired - Fee Related JP6538154B2 (ja) | 2014-09-10 | 2015-09-09 | Ｒｅｔ（ｒｅａｒｒａｎｇｅｄ ｄｕｒｉｎｇ ｔｒａｎｓｆｅｃｔｉｏｎ）キナーゼ阻害剤としてのピリジン誘導体 |
| JP2019102776A Expired - Fee Related JP6728447B2 (ja) | 2014-09-10 | 2019-05-31 | Ｒｅｔ（ｒｅａｒｒａｎｇｅｄ ｄｕｒｉｎｇ ｔｒａｎｓｆｅｃｔｉｏｎ）キナーゼ阻害剤としてのピリジン誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019102776A Expired - Fee Related JP6728447B2 (ja) | 2014-09-10 | 2019-05-31 | Ｒｅｔ（ｒｅａｒｒａｎｇｅｄ ｄｕｒｉｎｇ ｔｒａｎｓｆｅｃｔｉｏｎ）キナーゼ阻害剤としてのピリジン誘導体 |
Country Status (36)
| Country | Link |
|---|---|
| US (4) | US9918974B2 (2) |
| EP (2) | EP3517526B1 (2) |
| JP (2) | JP6538154B2 (2) |
| KR (1) | KR20170045350A (2) |
| CN (1) | CN107074768B (2) |
| AU (1) | AU2015313841B2 (2) |
| BR (1) | BR112017004900A2 (2) |
| CA (1) | CA2960768A1 (2) |
| CL (1) | CL2017000588A1 (2) |
| CO (1) | CO2017002273A2 (2) |
| CR (1) | CR20170093A (2) |
| CY (1) | CY1121661T1 (2) |
| DK (1) | DK3191450T3 (2) |
| DO (1) | DOP2017000059A (2) |
| EA (1) | EA033544B1 (2) |
| ES (2) | ES2816453T3 (2) |
| HR (1) | HRP20190815T1 (2) |
| HU (1) | HUE044604T2 (2) |
| IL (1) | IL250908B (2) |
| LT (1) | LT3191450T (2) |
| MA (1) | MA40581A (2) |
| ME (1) | ME03432B (2) |
| MX (1) | MX373863B (2) |
| MY (1) | MY181913A (2) |
| PE (1) | PE20170705A1 (2) |
| PH (1) | PH12017500425A1 (2) |
| PL (1) | PL3191450T3 (2) |
| PT (1) | PT3191450T (2) |
| RS (1) | RS58813B1 (2) |
| SG (1) | SG11201701694QA (2) |
| SI (1) | SI3191450T1 (2) |
| SM (1) | SMT201900304T1 (2) |
| TW (1) | TWI683807B (2) |
| UA (1) | UA122213C2 (2) |
| UY (1) | UY36293A (2) |
| WO (1) | WO2016038552A1 (2) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ604708A (en) | 2010-05-20 | 2015-05-29 | Array Biopharma Inc | Macrocyclic compounds as trk kinase inhibitors |
| PE20170705A1 (es) | 2014-09-10 | 2017-05-21 | Glaxosmithkline Ip Dev Ltd | Nuevos compuestos como inhibidores de ret (reorganizado durante la transfeccion) |
| EA032030B1 (ru) | 2014-09-10 | 2019-03-29 | Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед | Соединения в качестве ингибиторов реаранжированной во время трансфекции (ret) киназы |
| US10202365B2 (en) | 2015-02-06 | 2019-02-12 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors |
| BR112018000808A2 (pt) | 2015-07-16 | 2018-09-04 | Array Biopharma Inc | compostos de pirazolo[1,5-a]piridina substituída como inibidores de ret cinase |
| PL3371171T3 (pl) | 2015-11-02 | 2024-03-25 | Blueprint Medicines Corporation | Inhibitory RET |
| TW201738228A (zh) | 2016-03-17 | 2017-11-01 | 藍圖醫藥公司 | Ｒｅｔ之抑制劑 |
| US10227329B2 (en) | 2016-07-22 | 2019-03-12 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to RET |
| JP2018052878A (ja) * | 2016-09-29 | 2018-04-05 | 第一三共株式会社 | ピリジン化合物 |
| 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 |
| US11168090B2 (en) | 2017-01-18 | 2021-11-09 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors |
| 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 |
| JP2020519672A (ja) | 2017-05-15 | 2020-07-02 | ブループリント メディシンズ コーポレイション | ＲＥＴ阻害剤とｍＴＯＲＣ１阻害剤との組合せ及び異常なＲＥＴ活性によって媒介されるがんを処置するためのその使用 |
| TWI812649B (zh) | 2017-10-10 | 2023-08-21 | 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 |
| WO2019143991A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | SUBSTITUTED PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS AS RET KINASE INHIBITORS |
| EP3740491A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| CN111615514B (zh) | 2018-01-18 | 2022-10-11 | 奥瑞生物药品公司 | 作为ret激酶抑制剂的取代的吡唑并[4,3-c]吡啶化合物 |
| SI3773589T1 (sl) | 2018-04-03 | 2024-03-29 | Blueprint Medicines Corporation | Inhibitor RET za uporabo pri zdravljenju raka, ki ima RET spremembo |
| EP3849986B1 (en) | 2018-09-10 | 2022-06-08 | Array Biopharma, Inc. | Fused heterocyclic compounds as ret kinase inhibitors |
| JP2023527412A (ja) | 2020-05-29 | 2023-06-28 | ブループリント メディシンズ コーポレイション | プラルセチニブの固体形態 |
| CN115803316B (zh) * | 2020-07-23 | 2024-12-06 | 深圳晶泰科技有限公司 | 吡啶酮类化合物及其制备方法和应用 |
| KR20250052364A (ko) | 2022-08-24 | 2025-04-18 | 도레이 카부시키가이샤 | 암의 치료 및/또는 예방을 위한 의약품 |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20120046290A1 (en) | 1997-12-22 | 2012-02-23 | Jacques Dumas | Inhibition of p38 kinase activity using substituted heterocyclic ureas |
| US20070244120A1 (en) | 2000-08-18 | 2007-10-18 | Jacques Dumas | Inhibition of raf kinase using substituted heterocyclic ureas |
| SK286213B6 (sk) * | 1997-12-22 | 2008-05-06 | Bayer Corporation | Substituované heterocyklické močoviny, farmaceutický prípravok ich obsahujúci a ich použitie |
| MXPA00006233A (es) | 1997-12-22 | 2002-09-18 | Bayer Ag | Inhibicion de la actividad de la cinasa p38 utilizando ureas heterociclicas sustituidas. |
| KR20020060160A (ko) | 1999-08-12 | 2002-07-16 | 파마시아 이탈리아 에스.피.에이. | 3(5)-아미노-피라졸 유도체, 이의 제조 방법 및항종양제로서의 이의 용도 |
| AU2002215053A1 (en) * | 2000-11-27 | 2002-06-24 | Pharmacia Italia S.P.A. | Phenylacetamido- pyrazole derivatives and their use as antitumor agents |
| DE10201764A1 (de) | 2002-01-18 | 2003-07-31 | Bayer Cropscience Ag | Substituierte 4-Aminopyridin-Derivate |
| TW200406374A (en) | 2002-05-29 | 2004-05-01 | Novartis Ag | Diaryl urea derivatives useful for the treatment of protein kinase dependent diseases |
| AU2003264386A1 (en) | 2002-09-10 | 2004-04-30 | Kyorin Pharmaceutical Co., Ltd. | 4-(substituted aryl)-5-hydroxyisoquinolinone derivative |
| CA2536293A1 (en) | 2003-08-22 | 2005-03-03 | Boehringer Ingelheim Pharmaceuticals, Inc. | Methods of treating copd and pulmonary hypertension |
| TW200530236A (en) * | 2004-02-23 | 2005-09-16 | Chugai Pharmaceutical Co Ltd | Heteroaryl phenylurea |
| BRPI0519424B8 (pt) * | 2004-12-28 | 2021-05-25 | Athenex Inc | compostos, composição e uso dos ditos compostos para a preparação de um medicamento para prevenção ou tratamento de um distúrbio de proliferação celular ou infecção microbiana |
| US7968574B2 (en) | 2004-12-28 | 2011-06-28 | Kinex Pharmaceuticals, Llc | Biaryl compositions and methods for modulating a kinase cascade |
| GB0507575D0 (en) * | 2005-04-14 | 2005-05-18 | Novartis Ag | Organic compounds |
| US8247556B2 (en) * | 2005-10-21 | 2012-08-21 | Amgen Inc. | Method for preparing 6-substituted-7-aza-indoles |
| TW200804349A (en) * | 2005-12-23 | 2008-01-16 | Kalypsys Inc | Novel substituted pyrimidinyloxy ureas as inhibitors of protein kinases |
| WO2008002676A2 (en) | 2006-06-29 | 2008-01-03 | Kinex Pharmaceuticals, Llc | Biaryl compositions and methods for modulating a kinase cascade |
| KR101507375B1 (ko) * | 2006-09-15 | 2015-04-07 | 엑스커버리 홀딩 컴퍼니 엘엘씨 | 키나아제 억제제 화합물 |
| CA2666116A1 (en) | 2006-10-16 | 2008-04-24 | Novartis Ag | Phenylacetamides useful as protein kinase inhibitors |
| DK2848610T3 (da) * | 2006-11-15 | 2017-11-06 | Ym Biosciences Australia Pty | Hæmmere af kinaseaktivitet |
| JP2013502429A (ja) | 2009-08-19 | 2013-01-24 | アムビト ビオスシエンセス コルポラチオン | ビアリール化合物及びその使用方法 |
| US9073895B2 (en) | 2010-12-16 | 2015-07-07 | Boehringer Ingelheim International Gmbh | Biarylamide inhibitors of leukotriene production |
| BR112015023618A2 (pt) | 2013-03-15 | 2017-07-18 | Glaxosmithkline Ip Dev Ltd | derivados de piridina como inibidores de quinase reorganizada durante a transfecção (ret) |
| MA38394B1 (fr) | 2013-03-15 | 2018-04-30 | Glaxosmithkline Ip Dev Ltd | Dérivés pyridine utilisés comme inhibiteurs de la kinase réarrangée au cours de la transfection (ret) |
| EA032030B1 (ru) | 2014-09-10 | 2019-03-29 | Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед | Соединения в качестве ингибиторов реаранжированной во время трансфекции (ret) киназы |
| PE20170705A1 (es) * | 2014-09-10 | 2017-05-21 | Glaxosmithkline Ip Dev Ltd | Nuevos compuestos como inhibidores de ret (reorganizado durante la transfeccion) |
-
2015
- 2015-09-09 PE PE2017000417A patent/PE20170705A1/es unknown
- 2015-09-09 HR HRP20190815TT patent/HRP20190815T1/hr unknown
- 2015-09-09 LT LTEP15767599.2T patent/LT3191450T/lt unknown
- 2015-09-09 JP JP2017513450A patent/JP6538154B2/ja not_active Expired - Fee Related
- 2015-09-09 CA CA2960768A patent/CA2960768A1/en not_active Abandoned
- 2015-09-09 EP EP19160650.8A patent/EP3517526B1/en active Active
- 2015-09-09 SM SM20190304T patent/SMT201900304T1/it unknown
- 2015-09-09 EA EA201790546A patent/EA033544B1/ru not_active IP Right Cessation
- 2015-09-09 PL PL15767599T patent/PL3191450T3/pl unknown
- 2015-09-09 MX MX2017003114A patent/MX373863B/es active IP Right Grant
- 2015-09-09 UA UAA201703478A patent/UA122213C2/uk unknown
- 2015-09-09 AU AU2015313841A patent/AU2015313841B2/en not_active Ceased
- 2015-09-09 BR BR112017004900A patent/BR112017004900A2/pt not_active IP Right Cessation
- 2015-09-09 WO PCT/IB2015/056905 patent/WO2016038552A1/en not_active Ceased
- 2015-09-09 ME MEP-2019-136A patent/ME03432B/me unknown
- 2015-09-09 ES ES19160650T patent/ES2816453T3/es active Active
- 2015-09-09 MY MYPI2017700782A patent/MY181913A/en unknown
- 2015-09-09 SI SI201530720T patent/SI3191450T1/sl unknown
- 2015-09-09 SG SG11201701694QA patent/SG11201701694QA/en unknown
- 2015-09-09 CR CR20170093A patent/CR20170093A/es unknown
- 2015-09-09 US US15/509,613 patent/US9918974B2/en not_active Expired - Fee Related
- 2015-09-09 HU HUE15767599 patent/HUE044604T2/hu unknown
- 2015-09-09 MA MA040581A patent/MA40581A/fr unknown
- 2015-09-09 RS RS20190559A patent/RS58813B1/sr unknown
- 2015-09-09 EP EP15767599.2A patent/EP3191450B1/en active Active
- 2015-09-09 ES ES15767599T patent/ES2725704T3/es active Active
- 2015-09-09 PT PT15767599T patent/PT3191450T/pt unknown
- 2015-09-09 CN CN201580058320.5A patent/CN107074768B/zh not_active Expired - Fee Related
- 2015-09-09 DK DK15767599.2T patent/DK3191450T3/da active
- 2015-09-09 KR KR1020177009237A patent/KR20170045350A/ko not_active Ceased
- 2015-09-10 UY UY0001036293A patent/UY36293A/es unknown
- 2015-09-10 TW TW104129876A patent/TWI683807B/zh not_active IP Right Cessation
-
2017
- 2017-03-02 IL IL250908A patent/IL250908B/en active IP Right Grant
- 2017-03-07 PH PH12017500425A patent/PH12017500425A1/en unknown
- 2017-03-07 DO DO2017000059A patent/DOP2017000059A/es unknown
- 2017-03-07 CO CONC2017/0002273A patent/CO2017002273A2/es unknown
- 2017-03-09 CL CL2017000588A patent/CL2017000588A1/es unknown
-
2018
- 2018-01-23 US US15/877,524 patent/US10111866B2/en not_active Expired - Fee Related
- 2018-09-28 US US16/145,271 patent/US10292975B2/en not_active Expired - Fee Related
-
2019
- 2019-04-05 US US16/376,858 patent/US10709695B2/en not_active Expired - Fee Related
- 2019-05-09 CY CY20191100502T patent/CY1121661T1/el unknown
- 2019-05-31 JP JP2019102776A patent/JP6728447B2/ja not_active Expired - Fee Related
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