JP2017537886A5 - - Google Patents
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- Publication number
- JP2017537886A5 JP2017537886A5 JP2017522375A JP2017522375A JP2017537886A5 JP 2017537886 A5 JP2017537886 A5 JP 2017537886A5 JP 2017522375 A JP2017522375 A JP 2017522375A JP 2017522375 A JP2017522375 A JP 2017522375A JP 2017537886 A5 JP2017537886 A5 JP 2017537886A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- alkyl
- optionally substituted
- hydrogen
- 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
- 125000000217 alkyl group Chemical group 0.000 claims description 91
- 125000000623 heterocyclic group Chemical group 0.000 claims description 48
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 38
- 125000001072 heteroaryl group Chemical group 0.000 claims description 34
- 229910052739 hydrogen Inorganic materials 0.000 claims description 30
- 239000001257 hydrogen Substances 0.000 claims description 30
- 125000003118 aryl group Chemical group 0.000 claims description 28
- 125000000304 alkynyl group Chemical group 0.000 claims description 27
- 150000002431 hydrogen Chemical class 0.000 claims description 27
- 125000003342 alkenyl group Chemical group 0.000 claims description 25
- 229910052736 halogen Inorganic materials 0.000 claims description 20
- 150000002367 halogens Chemical class 0.000 claims description 20
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 2
- 239000013078 crystal Substances 0.000 claims 23
- 239000000651 prodrug Substances 0.000 claims 23
- 229940002612 prodrug Drugs 0.000 claims 23
- 150000003839 salts Chemical class 0.000 claims 23
- 239000012453 solvate Substances 0.000 claims 23
- 150000001875 compounds Chemical class 0.000 claims 21
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 13
- 125000000547 substituted alkyl group Chemical group 0.000 claims 8
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 7
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 7
- 125000003107 substituted aryl group Chemical group 0.000 claims 7
- 238000000034 method Methods 0.000 claims 6
- 150000004677 hydrates Chemical class 0.000 claims 5
- 230000000155 isotopic effect Effects 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 102000001253 Protein Kinase Human genes 0.000 claims 3
- 125000002252 acyl group Chemical group 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 125000004430 oxygen atom Chemical group O* 0.000 claims 3
- 108060006633 protein kinase Proteins 0.000 claims 3
- 125000004434 sulfur atom Chemical group 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- JGLMVXWAHNTPRF-CMDGGOBGSA-N CCN1N=C(C)C=C1C(=O)NC1=NC2=CC(=CC(OC)=C2N1C\C=C\CN1C(NC(=O)C2=CC(C)=NN2CC)=NC2=CC(=CC(OCCCN3CCOCC3)=C12)C(N)=O)C(N)=O Chemical compound CCN1N=C(C)C=C1C(=O)NC1=NC2=CC(=CC(OC)=C2N1C\C=C\CN1C(NC(=O)C2=CC(C)=NN2CC)=NC2=CC(=CC(OCCCN3CCOCC3)=C12)C(N)=O)C(N)=O JGLMVXWAHNTPRF-CMDGGOBGSA-N 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 230000006907 apoptotic process Effects 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 230000001939 inductive effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 238000002372 labelling Methods 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000005415 substituted alkoxy group Chemical group 0.000 claims 1
- 239000011593 sulfur Substances 0.000 claims 1
- 238000003419 tautomerization reaction Methods 0.000 claims 1
- 125000006708 (C5-C14) heteroaryl group Chemical group 0.000 description 6
- -1 C 1-10 perhaloalkyl Chemical group 0.000 description 4
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 description 3
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 description 3
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- 125000004432 carbon atom Chemical group C* 0.000 description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 125000001424 substituent group Chemical group 0.000 description 2
- 229910052799 carbon Inorganic materials 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462067178P | 2014-10-22 | 2014-10-22 | |
| US62/067,178 | 2014-10-22 | ||
| PCT/US2015/056899 WO2016065138A1 (en) | 2014-10-22 | 2015-10-22 | Thiazolyl-containing compounds for treating proliferative diseases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017537886A JP2017537886A (ja) | 2017-12-21 |
| JP2017537886A5 true JP2017537886A5 (OSRAM) | 2018-11-29 |
| JP6788583B2 JP6788583B2 (ja) | 2020-11-25 |
Family
ID=55761545
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017522375A Active JP6788583B2 (ja) | 2014-10-22 | 2015-10-22 | 増殖性疾患を処置するためのチアゾリル含有化合物 |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US10112957B2 (OSRAM) |
| EP (2) | EP3715346B1 (OSRAM) |
| JP (1) | JP6788583B2 (OSRAM) |
| AU (1) | AU2015335788B2 (OSRAM) |
| CA (1) | CA2965178C (OSRAM) |
| IL (1) | IL251790B (OSRAM) |
| WO (1) | WO2016065138A1 (OSRAM) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9908872B2 (en) | 2013-12-13 | 2018-03-06 | Dana-Farber Cancer Institute, Inc. | Methods to treat lymphoplasmacytic lymphoma |
| AU2014361798B2 (en) | 2013-12-13 | 2020-06-11 | Dana-Farber Cancer Institute, Inc. | Methods to treat lymphoplasmacytic lymphoma |
| EP3715346B1 (en) | 2014-10-22 | 2024-01-03 | Dana-Farber Cancer Institute, Inc. | Thiazolyl-containing compounds for treating proliferative diseases |
| BR112018075086B1 (pt) * | 2016-07-14 | 2024-02-27 | Eli Lilly And Company | Derivados de pirazolilaminobenzimidazol, seu uso, e composição farmacêutica |
| EP3534899B1 (en) | 2016-11-03 | 2022-06-01 | Corvus Pharmaceuticals, Inc. | Compounds and methods for modulating interleukin-2-inducible t-cell kinase |
| KR102328682B1 (ko) * | 2018-08-27 | 2021-11-18 | 주식회사 대웅제약 | 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물 |
| CN109265455B (zh) * | 2018-11-09 | 2020-08-18 | 新发药业有限公司 | 一种达沙替尼的制备方法 |
| EP4112617A4 (en) * | 2020-02-26 | 2024-03-13 | Daewoong Pharmaceutical Co., Ltd. | PROCESS FOR PREPARING HETEROCYCLIC AMINE DERIVATIVES |
| JP7691991B2 (ja) * | 2020-03-06 | 2025-06-12 | ナショナル・ヘルス・リサーチ・インスティテューツ | ピリミジン化合物及びその薬学的使用 |
| WO2024111626A1 (ja) * | 2022-11-25 | 2024-05-30 | カルナバイオサイエンス株式会社 | 新規チアゾール誘導体 |
Family Cites Families (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9816837D0 (en) | 1998-08-04 | 1998-09-30 | Zeneca Ltd | Amide derivatives |
| ATE269295T1 (de) | 1998-04-17 | 2004-07-15 | Parker Hughes Inst | Btk inhibitoren und verfahren zur identifizierung und verwendung |
| BR9912729A (pt) | 1998-08-04 | 2001-05-02 | Astrazeneca Ab | Derivado de amida, processo para prepará-lo, e, uso do mesmo |
| AU761361B2 (en) | 1998-09-25 | 2003-06-05 | Astrazeneca Ab | Benzamide derivatives and their use as cytokine inhibitors |
| US6306897B1 (en) | 1999-03-19 | 2001-10-23 | Parker Hughes Institute | Calanolides for inhibiting BTK |
| ATE511840T1 (de) | 2001-10-09 | 2011-06-15 | Amgen Inc | Imidazolderivate als entzündungshemmende mittel |
| RU2005106871A (ru) | 2002-08-14 | 2005-10-10 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Ингибиторы протеинкиназ и их применение |
| ES2571779T3 (es) | 2002-12-13 | 2016-05-26 | Ym Biosciences Australia Pty | Inhibidores de cinasa a base de nicotinamida |
| WO2006067445A2 (en) | 2004-12-22 | 2006-06-29 | Astrazeneca Ab | Csf-1r kinase inhibitors |
| CA2589773A1 (en) | 2004-12-22 | 2006-06-29 | Astrazeneca Ab | Pyridine carboxamide derivatives for use as anticancer agents |
| CA2593803A1 (en) * | 2005-01-26 | 2006-08-03 | Irm Llc | Thiazole-amide compounds and compsitions as protein kinase inhibitors |
| US7375951B2 (en) * | 2006-07-07 | 2008-05-20 | Lutron Electronics Co., Inc. | Load control device having a split enclosure |
| US7605154B2 (en) | 2005-08-08 | 2009-10-20 | Janssen Pharmaceutica N.V. | Substituted Thiazolo [4,5-d]pyrimidines as protein kinase inhibitors |
| US7754717B2 (en) | 2005-08-15 | 2010-07-13 | Amgen Inc. | Bis-aryl amide compounds and methods of use |
| JP5225857B2 (ja) | 2005-11-14 | 2013-07-03 | ジェネンテック，インコーポレイティド | ヘッジホッグシグナル伝達のビスアミド阻害剤 |
| US20070155746A1 (en) | 2005-12-23 | 2007-07-05 | Kalypsys, Inc. | Novel substituted pyridinyloxy and pyrimidinyloxy amides useful as inhibitors of protein kinases |
| US20090312396A1 (en) | 2006-07-10 | 2009-12-17 | Astrazeneca Ab | Methods for cancer treatment using tak1 inhibitors |
| EP2526934B1 (en) | 2006-09-22 | 2015-12-09 | Pharmacyclics LLC | Inhibitors of bruton's tyrosine kinase |
| WO2008144253A1 (en) | 2007-05-14 | 2008-11-27 | Irm Llc | Protein kinase inhibitors and methods for using thereof |
| TW200906825A (en) * | 2007-05-30 | 2009-02-16 | Scripps Research Inst | Inhibitors of protein kinases |
| TW200911798A (en) | 2007-08-02 | 2009-03-16 | Amgen Inc | PI3 kinase modulators and methods of use |
| KR20120033357A (ko) | 2007-10-23 | 2012-04-06 | 테바 파마슈티컬 인더스트리즈 리미티드 | 다사티닙 다형체 및 이의 제조 방법 |
| WO2009076373A1 (en) | 2007-12-10 | 2009-06-18 | Concert Pharmaceuticals Inc. | Heterocyclic kinase inhibitors |
| WO2009137596A1 (en) | 2008-05-06 | 2009-11-12 | Cgi Pharmaceuticals, Inc. | Substituted amides, method of making, and use as btk inhibitors |
| CA2735208A1 (en) | 2008-09-02 | 2010-03-11 | Boehringer Ingelheim International Gmbh | Novel benzamides, production thereof, and use thereof as medicaments |
| WO2010056875A1 (en) | 2008-11-12 | 2010-05-20 | Cgi Pharmaceuticals, Inc. | Pyridazinones and their use as btk inhibitors |
| IN2012DN02493A (OSRAM) | 2009-09-03 | 2015-08-28 | Allergan Inc | |
| EP2485589A4 (en) | 2009-09-04 | 2013-02-06 | Biogen Idec Inc | HETEROARYL-BTK INHIBITORS |
| CA2784807C (en) * | 2009-12-29 | 2021-12-14 | Dana-Farber Cancer Institute, Inc. | Type ii raf kinase inhibitors |
| KR101995013B1 (ko) | 2010-07-13 | 2019-07-02 | 에프. 호프만-라 로슈 아게 | Irak4 조절제로서 피라졸로[1,5a]피리미딘 및 티에노[3,2b]피리미딘 유도체 |
| WO2012062704A1 (en) | 2010-11-09 | 2012-05-18 | Cellzome Limited | Pyridine compounds and aza analogues thereof as tyk2 inhibitors |
| WO2012068096A2 (en) | 2010-11-15 | 2012-05-24 | Exelixis, Inc. | Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture |
| PL2714677T3 (pl) | 2011-05-23 | 2019-02-28 | Merck Patent Gmbh | Pochodne pirydynowe i pirazynowe |
| KR20180084153A (ko) * | 2011-06-10 | 2018-07-24 | 메르크 파텐트 게엠베하 | Btk 억제 활성을 갖는 피리미딘 및 피리딘 화합물의 조성물 및 제조방법 |
| EP2548877A1 (en) | 2011-07-19 | 2013-01-23 | MSD Oss B.V. | 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors |
| EP2763966B1 (en) | 2011-10-03 | 2018-04-04 | Syngenta Participations AG | Insecticidal 2-methoxybenzamide derivatives |
| CA2850763A1 (en) | 2011-10-04 | 2013-04-11 | Gilead Calistoga Llc | Novel quinoxaline inhibitors of pi3k |
| SG11201401993RA (en) | 2011-11-03 | 2014-05-29 | Hoffmann La Roche | Alkylated piperazine compounds as inhibitors of btk activity |
| WO2013074986A1 (en) | 2011-11-17 | 2013-05-23 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-jun-n-terminal kinase (jnk) |
| CA2857302C (en) | 2011-12-15 | 2020-08-25 | Novartis Ag | Use of inhibitors of the activity or function of pi3k |
| CN103405429A (zh) | 2013-08-22 | 2013-11-27 | 中国药科大学 | 一类vegfr-2抑制剂及其用途 |
| WO2015069287A1 (en) | 2013-11-08 | 2015-05-14 | Allergan, Inc. | Compounds as tyrosine kinase modulators |
| US9908872B2 (en) | 2013-12-13 | 2018-03-06 | Dana-Farber Cancer Institute, Inc. | Methods to treat lymphoplasmacytic lymphoma |
| AU2014361798B2 (en) | 2013-12-13 | 2020-06-11 | Dana-Farber Cancer Institute, Inc. | Methods to treat lymphoplasmacytic lymphoma |
| EP3715346B1 (en) | 2014-10-22 | 2024-01-03 | Dana-Farber Cancer Institute, Inc. | Thiazolyl-containing compounds for treating proliferative diseases |
-
2015
- 2015-10-22 EP EP20161511.9A patent/EP3715346B1/en active Active
- 2015-10-22 JP JP2017522375A patent/JP6788583B2/ja active Active
- 2015-10-22 CA CA2965178A patent/CA2965178C/en active Active
- 2015-10-22 US US15/518,541 patent/US10112957B2/en active Active
- 2015-10-22 AU AU2015335788A patent/AU2015335788B2/en active Active
- 2015-10-22 EP EP15852450.4A patent/EP3209648B1/en active Active
- 2015-10-22 WO PCT/US2015/056899 patent/WO2016065138A1/en not_active Ceased
-
2017
- 2017-04-19 IL IL251790A patent/IL251790B/en active IP Right Grant
-
2018
- 2018-10-24 US US16/169,972 patent/US10464949B2/en not_active Expired - Fee Related
-
2019
- 2019-11-01 US US16/672,198 patent/US10844077B2/en active Active
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