JP2017526711A5 - - Google Patents
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- Publication number
- JP2017526711A5 JP2017526711A5 JP2017513448A JP2017513448A JP2017526711A5 JP 2017526711 A5 JP2017526711 A5 JP 2017526711A5 JP 2017513448 A JP2017513448 A JP 2017513448A JP 2017513448 A JP2017513448 A JP 2017513448A JP 2017526711 A5 JP2017526711 A5 JP 2017526711A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- pharmaceutically acceptable
- hydrogen
- acceptable salt
- dihydropyridin
- 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
- 150000001875 compounds Chemical class 0.000 claims 15
- 239000001257 hydrogen Substances 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- -1 methoxy, isopropoxy Chemical group 0.000 claims 8
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 4
- 230000001404 mediated effect Effects 0.000 claims 4
- 238000000634 powder X-ray diffraction Methods 0.000 claims 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 3
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 3
- 239000004202 carbamide Substances 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- QXALUNHYJJONQH-UHFFFAOYSA-N 1,1,1-trifluoro-2-methylpropane Chemical compound CC(C)C(F)(F)F QXALUNHYJJONQH-UHFFFAOYSA-N 0.000 claims 2
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 2
- 206010010774 Constipation Diseases 0.000 claims 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 239000000460 chlorine Substances 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 239000013078 crystal Substances 0.000 claims 2
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 125000004284 isoxazol-3-yl group Chemical group [H]C1=C([H])C(*)=NO1 0.000 claims 2
- DFRZDZKDAVMTGG-UHFFFAOYSA-N 1-(5-tert-butyl-2-phenylpyrazol-3-yl)-3-[4-(6-oxo-1H-pyridin-3-yl)phenyl]urea Chemical compound C(C)(C)(C)C1=NN(C(=C1)NC(=O)NC1=CC=C(C=C1)C1=CNC(C=C1)=O)C1=CC=CC=C1 DFRZDZKDAVMTGG-UHFFFAOYSA-N 0.000 claims 1
- LSWAQEYWXBLMIN-UHFFFAOYSA-N 1-[2-(4-ethoxy-6-oxo-1H-pyridin-3-yl)-4-methylpyrimidin-5-yl]-3-[5-(1,1,1-trifluoro-2-methylpropan-2-yl)-1,2-oxazol-3-yl]urea Chemical compound C(C)OC=1C(=CNC(C=1)=O)C1=NC=C(C(=N1)C)NC(=O)NC1=NOC(=C1)C(C(F)(F)F)(C)C LSWAQEYWXBLMIN-UHFFFAOYSA-N 0.000 claims 1
- KFZDJMBSOJDTIX-UHFFFAOYSA-N 1-[2-(5-ethoxy-6-oxo-1H-pyridin-3-yl)-4-methylpyrimidin-5-yl]-3-[5-(1,1,1-trifluoro-2-methylpropan-2-yl)-1,2-oxazol-3-yl]urea Chemical compound C(C)OC1=CC(=CNC1=O)C1=NC=C(C(=N1)C)NC(=O)NC1=NOC(=C1)C(C(F)(F)F)(C)C KFZDJMBSOJDTIX-UHFFFAOYSA-N 0.000 claims 1
- JIJPTBPAIKXAHQ-UHFFFAOYSA-N 1-[5-(5-ethoxy-6-oxo-1H-pyridin-3-yl)-3-methylpyrazin-2-yl]-3-[5-(1,1,1-trifluoro-2-methylpropan-2-yl)-1,2-oxazol-3-yl]urea Chemical compound C(C)OC1=CC(=CNC1=O)C=1N=C(C(=NC=1)NC(=O)NC1=NOC(=C1)C(C(F)(F)F)(C)C)C JIJPTBPAIKXAHQ-UHFFFAOYSA-N 0.000 claims 1
- 208000004998 Abdominal Pain Diseases 0.000 claims 1
- 206010012735 Diarrhoea Diseases 0.000 claims 1
- 206010036772 Proctalgia Diseases 0.000 claims 1
- 201000000117 functional diarrhea Diseases 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 230000005855 radiation Effects 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2014000834 | 2014-09-10 | ||
| CNPCT/CN2014/000834 | 2014-09-10 | ||
| PCT/CN2015/089332 WO2016037578A1 (en) | 2014-09-10 | 2015-09-10 | Novel compounds as rearranged during transfection (ret) inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017526711A JP2017526711A (ja) | 2017-09-14 |
| JP2017526711A5 true JP2017526711A5 (enExample) | 2018-10-18 |
| JP6538153B2 JP6538153B2 (ja) | 2019-07-03 |
Family
ID=55458357
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017513448A Expired - Fee Related JP6538153B2 (ja) | 2014-09-10 | 2015-09-10 | Ｒｅａｒｒａｎｇｅｄ ｄｕｒｉｎｇ ｔｒａｎｓｆｅｃｔｉｏｎ（ｒｅｔ）阻害剤としての新規な化合物 |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US9879021B2 (enExample) |
| EP (1) | EP3191449B1 (enExample) |
| JP (1) | JP6538153B2 (enExample) |
| KR (1) | KR20170046180A (enExample) |
| CN (1) | CN107250110B (enExample) |
| AU (1) | AU2015316438B2 (enExample) |
| BR (1) | BR112017004897A2 (enExample) |
| CA (1) | CA2960730A1 (enExample) |
| CL (1) | CL2017000589A1 (enExample) |
| CO (1) | CO2017002378A2 (enExample) |
| CR (1) | CR20170094A (enExample) |
| DK (1) | DK3191449T3 (enExample) |
| DO (1) | DOP2017000067A (enExample) |
| EA (1) | EA032030B1 (enExample) |
| ES (1) | ES2819871T3 (enExample) |
| IL (1) | IL250923B (enExample) |
| MX (1) | MX381233B (enExample) |
| MY (1) | MY187169A (enExample) |
| PE (1) | PE20170677A1 (enExample) |
| PH (1) | PH12017500454A1 (enExample) |
| SG (1) | SG11201701695UA (enExample) |
| UA (1) | UA123084C2 (enExample) |
| WO (1) | WO2016037578A1 (enExample) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102971322B (zh) | 2010-05-20 | 2016-02-17 | 阵列生物制药公司 | 作为trk激酶抑制剂的大环化合物 |
| KR20170046180A (ko) * | 2014-09-10 | 2017-04-28 | 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 | 형질감염 중 재배열 (ret) 억제제로서의 신규 화합물 |
| PT3191450T (pt) | 2014-09-10 | 2019-05-29 | Glaxosmithkline Ip Dev Ltd | Derivados de piridona como inibidores da quinase rearranjada durante a transfecção (ret) |
| WO2016127074A1 (en) | 2015-02-06 | 2016-08-11 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as ret inhibitors |
| CN108349969B (zh) | 2015-07-16 | 2022-05-10 | 阵列生物制药公司 | 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡啶化合物 |
| RS65069B1 (sr) | 2015-11-02 | 2024-02-29 | Blueprint Medicines Corp | Inhibitori ret-a |
| WO2017145050A1 (en) * | 2016-02-23 | 2017-08-31 | Glaxosmithkline Intellectual Property Development Limited | Pyridylpyridone derivative useful as a ret kinase inhibitor in the treatment of ibs and cancer |
| US20170252350A1 (en) * | 2016-03-03 | 2017-09-07 | Cornell University | Small molecule ire1-alpha inhibitors |
| US10183928B2 (en) | 2016-03-17 | 2019-01-22 | Blueprint Medicines Corporation | Inhibitors of RET |
| WO2018017983A1 (en) | 2016-07-22 | 2018-01-25 | 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 |
| 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 |
| TWI795381B (zh) | 2016-12-21 | 2023-03-11 | 比利時商健生藥品公司 | 作為ｍａｌｔ１抑制劑之吡唑衍生物 |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| ES2948194T3 (es) | 2017-01-18 | 2023-09-01 | Array Biopharma Inc | Compuestos de pirazolo[1,5-a]pirazina sustituida como inhibidores de la cinasa RET |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| WO2018213329A1 (en) | 2017-05-15 | 2018-11-22 | Blueprint Medicines Corporation | Combinations of ret inhibitors and mtorc1 inhibitors and uses thereof for the treatment of cancer mediated by aberrant ret activity |
| 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 |
| CN111971286B (zh) | 2018-01-18 | 2023-04-14 | 阿雷生物药品公司 | 作为RET激酶抑制剂的取代的吡咯并[2,3-d]嘧啶化合物 |
| CN111630054B (zh) | 2018-01-18 | 2023-05-09 | 奥瑞生物药品公司 | 作为RET激酶抑制剂的取代的吡唑并[3,4-d]嘧啶化合物 |
| US11472802B2 (en) | 2018-01-18 | 2022-10-18 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors |
| PT3773589T (pt) | 2018-04-03 | 2024-02-06 | Blueprint Medicines Corp | Inibidor de ret para utilização no tratamento de cancro com alteração de ret |
| CN109096264B (zh) * | 2018-08-28 | 2019-08-23 | 山东理工职业学院 | Ret抑制剂及其制备方法、组合物和用途 |
| WO2020055672A1 (en) | 2018-09-10 | 2020-03-19 | Array Biopharma Inc. | Fused heterocyclic compounds as ret kinase inhibitors |
| WO2020083311A1 (zh) * | 2018-10-24 | 2020-04-30 | 南京明德新药研发有限公司 | 作为ret抑制剂的吡嗪衍生物 |
| CN109678724A (zh) * | 2018-12-18 | 2019-04-26 | 常州大学 | 一种2-甲基-1-取代苯基-2-丙胺类化合物的新合成方法 |
| MX2021012417A (es) * | 2019-04-11 | 2021-11-12 | Janssen Pharmaceutica Nv | Anillos de piridina que contienen derivados como inhibidores de malt1. |
| US12433876B2 (en) | 2019-08-30 | 2025-10-07 | University Of Rochester | Septin inhibitors for treatment of cancers |
| CN110950898B (zh) * | 2019-12-12 | 2022-11-11 | 江苏华益科技有限公司 | 一种含氮的氘代甲基化合物的合成方法 |
| CN111187257B (zh) * | 2020-02-17 | 2021-03-16 | 山东理工职业学院 | Ret受体酪氨酸激酶抑制剂 |
| EP4157829A1 (en) | 2020-05-29 | 2023-04-05 | Blueprint Medicines Corporation | Solid forms of pralsetinib |
| 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 |
| CA3197220A1 (en) | 2020-11-06 | 2022-05-12 | David Craig Mcgowan | 2-pyridones as thyroid hormone receptor modulators |
| CN114539065B (zh) * | 2020-11-25 | 2023-07-25 | 帕潘纳(北京)科技有限公司 | 制备4-硝基-2-三氟甲基苯乙酮的方法 |
| EP4347587A1 (en) | 2021-06-02 | 2024-04-10 | FMC Corporation | Fused pyridines for controlling invertebrate pests |
| CN113896650A (zh) * | 2021-10-27 | 2022-01-07 | 成都科圣原医药科技有限公司 | 一种辛波莫德中间体的合成方法 |
| EP4524129A1 (en) | 2022-05-09 | 2025-03-19 | Maxunitech Inc. | Method for preparing 2-substituted aryl acetonitrile compound and use thereof |
| CN116283748A (zh) * | 2023-02-21 | 2023-06-23 | 康化（上海）新药研发有限公司 | 2,5-二氯-3-甲氧基吡啶的合成方法 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070244120A1 (en) * | 2000-08-18 | 2007-10-18 | Jacques Dumas | Inhibition of raf kinase using substituted heterocyclic ureas |
| EP1041982B1 (en) | 1997-12-22 | 2011-10-19 | Bayer HealthCare LLC | INHIBITION OF p38 KINASE ACTIVITY USING SUBSTITUTED HETEROCYCLIC UREAS |
| US20120046290A1 (en) | 1997-12-22 | 2012-02-23 | Jacques Dumas | Inhibition of p38 kinase activity using substituted heterocyclic ureas |
| PL205321B1 (pl) * | 1997-12-22 | 2010-04-30 | Bayer Corp | Zastosowanie podstawionych heterocyklicznych moczników do wytwarzania leku do hamowania kinazy raf, podstawione heterocykliczne moczniki oraz kompozycja farmaceutyczna je zawierająca |
| PL353455A1 (en) | 1999-08-12 | 2003-11-17 | Pharmacia Italia S.P.A. | 3(5)-amino-pyrazole derivatives, process for their preparation and their use as antitumor agents |
| JP2004517840A (ja) | 2000-11-27 | 2004-06-17 | フアルマシア・イタリア・エツセ・ピー・アー | フェニルアセトアミド−ピラゾール誘導体およびそれの抗腫瘍薬としての使用 |
| DE10201764A1 (de) | 2002-01-18 | 2003-07-31 | Bayer Cropscience Ag | Substituierte 4-Aminopyridin-Derivate |
| AR037647A1 (es) | 2002-05-29 | 2004-12-01 | Novartis Ag | Derivados de diarilurea utiles para el tratamiento de enfermedades dependientes de la cinasa de proteina |
| AU2003264386A1 (en) * | 2002-09-10 | 2004-04-30 | Kyorin Pharmaceutical Co., Ltd. | 4-(substituted aryl)-5-hydroxyisoquinolinone derivative |
| CN1838958A (zh) | 2003-08-22 | 2006-09-27 | 贝林格尔·英格海姆药物公司 | 治疗慢性阻塞性肺病和肺动脉高血压的方法 |
| US7968574B2 (en) | 2004-12-28 | 2011-06-28 | Kinex Pharmaceuticals, Llc | Biaryl compositions and methods for modulating a kinase cascade |
| MX2008011684A (es) * | 2006-03-17 | 2008-12-12 | Ambit Biosciences Corp | Compuestos de imidazolotiazol para el tratamiento de enfermedad. |
| ES2500165T3 (es) | 2006-06-29 | 2014-09-30 | Kinex Pharmaceuticals, Llc | Composiciones de biarilo y métodos para modular una cascada de quinasas |
| WO2008046802A1 (en) | 2006-10-16 | 2008-04-24 | Novartis Ag | Phenylacetamides useful as protein kinase inhibitors |
| PL2848610T3 (pl) | 2006-11-15 | 2018-01-31 | Ym Biosciences Australia Pty | Inhibitory aktywności kinazy |
| KR20120059558A (ko) | 2009-08-19 | 2012-06-08 | 암비트 바이오사이언시즈 코포레이션 | 바이아릴 화합물 및 이의 사용 방법 |
| EP2651930B1 (en) | 2010-12-16 | 2015-10-28 | Boehringer Ingelheim International GmbH | Biarylamide inhibitors of leukotriene production |
| HUE033423T2 (en) | 2013-03-15 | 2017-11-28 | Glaxosmithkline Ip Dev Ltd | Pyridine derivatives as rearranged during transfection (ret) kinase inhibitors |
| US8937071B2 (en) | 2013-03-15 | 2015-01-20 | Glaxosmithkline Intellectual Property Development Limited | Compounds as rearranged during transfection (RET) inhibitors |
| KR20170046180A (ko) | 2014-09-10 | 2017-04-28 | 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 | 형질감염 중 재배열 (ret) 억제제로서의 신규 화합물 |
| PT3191450T (pt) * | 2014-09-10 | 2019-05-29 | Glaxosmithkline Ip Dev Ltd | Derivados de piridona como inibidores da quinase rearranjada durante a transfecção (ret) |
-
2015
- 2015-09-10 KR KR1020177009244A patent/KR20170046180A/ko not_active Ceased
- 2015-09-10 SG SG11201701695UA patent/SG11201701695UA/en unknown
- 2015-09-10 AU AU2015316438A patent/AU2015316438B2/en not_active Ceased
- 2015-09-10 CA CA2960730A patent/CA2960730A1/en not_active Abandoned
- 2015-09-10 WO PCT/CN2015/089332 patent/WO2016037578A1/en not_active Ceased
- 2015-09-10 MY MYPI2017700792A patent/MY187169A/en unknown
- 2015-09-10 CR CR20170094A patent/CR20170094A/es unknown
- 2015-09-10 EA EA201790547A patent/EA032030B1/ru not_active IP Right Cessation
- 2015-09-10 JP JP2017513448A patent/JP6538153B2/ja not_active Expired - Fee Related
- 2015-09-10 CN CN201580060784.XA patent/CN107250110B/zh not_active Expired - Fee Related
- 2015-09-10 PE PE2017000446A patent/PE20170677A1/es unknown
- 2015-09-10 MX MX2017003118A patent/MX381233B/es unknown
- 2015-09-10 BR BR112017004897A patent/BR112017004897A2/pt not_active IP Right Cessation
- 2015-09-10 EP EP15840612.4A patent/EP3191449B1/en active Active
- 2015-09-10 UA UAA201703477A patent/UA123084C2/uk unknown
- 2015-09-10 US US15/509,569 patent/US9879021B2/en active Active
- 2015-09-10 DK DK15840612.4T patent/DK3191449T3/da active
- 2015-09-10 ES ES15840612T patent/ES2819871T3/es active Active
-
2017
- 2017-03-05 IL IL250923A patent/IL250923B/en active IP Right Grant
- 2017-03-09 CL CL2017000589A patent/CL2017000589A1/es unknown
- 2017-03-10 DO DO2017000067A patent/DOP2017000067A/es unknown
- 2017-03-10 CO CONC2017/0002378A patent/CO2017002378A2/es unknown
- 2017-03-10 PH PH12017500454A patent/PH12017500454A1/en unknown
- 2017-12-11 US US15/837,048 patent/US10294236B2/en not_active Expired - Fee Related
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