JP2011529073A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2011529073A5 JP2011529073A5 JP2011520196A JP2011520196A JP2011529073A5 JP 2011529073 A5 JP2011529073 A5 JP 2011529073A5 JP 2011520196 A JP2011520196 A JP 2011520196A JP 2011520196 A JP2011520196 A JP 2011520196A JP 2011529073 A5 JP2011529073 A5 JP 2011529073A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- heterocyclyl
- heteroaryl
- alkenyl
- 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.)
- Withdrawn
Links
- 125000000217 alkyl group Chemical group 0.000 claims 45
- 125000000623 heterocyclic group Chemical group 0.000 claims 33
- 229910052739 hydrogen Inorganic materials 0.000 claims 25
- 239000001257 hydrogen Substances 0.000 claims 25
- 125000001072 heteroaryl group Chemical group 0.000 claims 24
- 125000004452 carbocyclyl group Chemical group 0.000 claims 16
- 229910052736 halogen Inorganic materials 0.000 claims 16
- 150000002367 halogens Chemical class 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 15
- -1 amino, substituted amino, amide Chemical class 0.000 claims 13
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 12
- 150000002431 hydrogen Chemical class 0.000 claims 12
- 125000003545 alkoxy group Chemical group 0.000 claims 11
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 11
- 125000000547 substituted alkyl group Chemical group 0.000 claims 11
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 10
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 8
- 125000003342 alkenyl group Chemical group 0.000 claims 7
- 125000003118 aryl group Chemical group 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 7
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 6
- 125000004093 cyano group Chemical class *C#N 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- RGICCULPCWNRAB-UHFFFAOYSA-N 2-[2-(2-hexoxyethoxy)ethoxy]ethanol Chemical compound CCCCCCOCCOCCOCCO RGICCULPCWNRAB-UHFFFAOYSA-N 0.000 claims 4
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 150000001408 amides Chemical class 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000002950 monocyclic group Chemical group 0.000 claims 3
- 125000005415 substituted alkoxy group Chemical group 0.000 claims 3
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- NMPVEAUIHMEAQP-UHFFFAOYSA-N 2-Bromoacetaldehyde Chemical compound BrCC=O NMPVEAUIHMEAQP-UHFFFAOYSA-N 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 125000003282 alkyl amino group Chemical group 0.000 claims 2
- 208000026935 allergic disease Diseases 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 125000003107 substituted aryl group Chemical group 0.000 claims 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- FUSFWUFSEJXMRQ-UHFFFAOYSA-N 2-bromo-1,1-dimethoxyethane Chemical compound COC(CBr)OC FUSFWUFSEJXMRQ-UHFFFAOYSA-N 0.000 claims 1
- CRZJPEIBPQWDGJ-UHFFFAOYSA-N 2-chloro-1,1-dimethoxyethane Chemical compound COC(CCl)OC CRZJPEIBPQWDGJ-UHFFFAOYSA-N 0.000 claims 1
- QSKPIOLLBIHNAC-UHFFFAOYSA-N 2-chloro-acetaldehyde Chemical compound ClCC=O QSKPIOLLBIHNAC-UHFFFAOYSA-N 0.000 claims 1
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 208000037979 autoimmune inflammatory disease Diseases 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 239000003153 chemical reaction reagent Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000000286 phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 0 C*1*CCC1 Chemical compound C*1*CCC1 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8327108P | 2008-07-24 | 2008-07-24 | |
| US61/083,271 | 2008-07-24 | ||
| PCT/US2009/051536 WO2010011837A1 (en) | 2008-07-24 | 2009-07-23 | Fused heterocyclic compounds useful as kinase modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011529073A JP2011529073A (ja) | 2011-12-01 |
| JP2011529073A5 true JP2011529073A5 (US07714131-20100511-C00001.png) | 2012-07-26 |
Family
ID=41119904
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011520196A Withdrawn JP2011529073A (ja) | 2008-07-24 | 2009-07-23 | キナーゼ調節因子として有用な縮合ヘテロ環化合物 |
Country Status (5)
Families Citing this family (57)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8389527B2 (en) | 2008-02-06 | 2013-03-05 | Bristol-Myers Squibb Company | Substituted imidazopyridazines useful as kinase inhibitors |
| MX2012004990A (es) | 2009-10-30 | 2012-06-12 | Janssen Pharmaceutica Nv | Deribados de imidazo [1,2-b] pirimideazina y su uso como inhibidores de la enzima fosfodiesterasa 10. |
| AR080754A1 (es) | 2010-03-09 | 2012-05-09 | Janssen Pharmaceutica Nv | Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10 |
| WO2013000924A1 (en) | 2011-06-27 | 2013-01-03 | Janssen Pharmaceutica Nv | 1-ARYL-4-METHYL-[1,2,4]TRIAZOLO[4,3-a]QUINOXALINE DERIVATIVES |
| CA2852964A1 (en) * | 2011-11-03 | 2013-05-10 | F. Hoffmann-La Roche Ag | Bicyclic piperazine compounds |
| WO2013133367A1 (ja) * | 2012-03-09 | 2013-09-12 | カルナバイオサイエンス株式会社 | 新規トリアジン誘導体 |
| US8461179B1 (en) | 2012-06-07 | 2013-06-11 | Deciphera Pharmaceuticals, Llc | Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
| US9669035B2 (en) | 2012-06-26 | 2017-06-06 | Janssen Pharmaceutica Nv | Combinations comprising PDE 2 inhibitors such as 1-aryl-4-methyl-[1,2,4]triazolo-[4,3-A]]quinoxaline compounds and PDE 10 inhibitors for use in the treatment of neurological of metabolic disorders |
| RU2667058C2 (ru) | 2012-07-09 | 2018-09-14 | Янссен Фармацевтика Нв | Ингибиторы фермента фосфодиэстеразы 10 |
| TW201414737A (zh) | 2012-07-13 | 2014-04-16 | 必治妥美雅史谷比公司 | 作爲激酶抑制劑之咪唑并三□甲腈 |
| HUE031980T2 (en) | 2013-04-25 | 2017-08-28 | Beigene Ltd | Condensed heterocyclic compounds as protein kinase inhibitors |
| MX2016003292A (es) | 2013-09-13 | 2016-06-24 | Beigene Ltd | Anticuerpos anti-muerte programada 1 y su uso como terapeuticos y diagnosticos. |
| CN104086551B (zh) * | 2014-06-06 | 2016-09-21 | 人福医药集团股份公司 | 化合物及其制备方法和用途 |
| CN106604742B (zh) | 2014-07-03 | 2019-01-11 | 百济神州有限公司 | 抗pd-l1抗体及其作为治疗剂及诊断剂的用途 |
| US10844064B2 (en) | 2014-09-17 | 2020-11-24 | Cyclerion Therapeutics, Inc. | sGC stimulators |
| ME03807B (me) | 2014-10-24 | 2021-04-20 | Bristol Myers Squibb Co | Jedinjenja indol karboksamida korisna kao inhibitori kinaze |
| EP3294737A4 (en) * | 2015-05-12 | 2018-10-03 | Kalyra Pharmaceuticals, Inc. | Bicyclic compounds |
| WO2017070089A1 (en) | 2015-10-19 | 2017-04-27 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| MD3377488T2 (ro) | 2015-11-19 | 2023-02-28 | Incyte Corp | Compuși heterociclici ca imunomodulatori |
| TW201726623A (zh) * | 2015-12-17 | 2017-08-01 | 英塞特公司 | 作為免疫調節劑之雜環化合物 |
| MX2018007774A (es) | 2015-12-22 | 2018-11-09 | Incyte Corp | Compuestos heterociclicos como inmunomoduladores. |
| AR108396A1 (es) | 2016-05-06 | 2018-08-15 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
| ES2905980T3 (es) | 2016-05-26 | 2022-04-12 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
| CN109890819B (zh) | 2016-06-20 | 2022-11-22 | 因赛特公司 | 作为免疫调节剂的杂环化合物 |
| AU2017293423B2 (en) | 2016-07-05 | 2023-05-25 | Beigene, Ltd. | Combination of a PD-1 antagonist and a RAF inhibitor for treating cancer |
| EP3484866B1 (en) | 2016-07-14 | 2022-09-07 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| US10927117B2 (en) | 2016-08-16 | 2021-02-23 | Beigene Switzerland Gmbh | Crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof |
| DK3500299T3 (da) | 2016-08-19 | 2024-01-29 | Beigene Switzerland Gmbh | Kombination af zanubrutinib med et anti-CD20- eller et anti-PD-1-antistof til anvendelse i behandling af cancer |
| EP3504198B1 (en) | 2016-08-29 | 2023-01-25 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| AU2017326558B2 (en) | 2016-09-19 | 2022-01-06 | Mei Pharma, Inc. | Combination therapy |
| PE20191532A1 (es) | 2016-12-22 | 2019-10-23 | Incyte Corp | Compuestos heterociclicos como inmunomoduladores |
| WO2018119236A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Triazolo[1,5-a]pyridine derivatives as immunomodulators |
| LT3558990T (lt) | 2016-12-22 | 2022-12-27 | Incyte Corporation | Tetrahidroimidazo[4,5-c]piridino dariniai kaip pd-l1 internalizavimo induktoriai |
| ES2899402T3 (es) | 2016-12-22 | 2022-03-11 | Incyte Corp | Derivados de piridina como inmunomoduladores |
| CN110461847B (zh) | 2017-01-25 | 2022-06-07 | 百济神州有限公司 | (S)-7-(1-(丁-2-炔酰基)哌啶-4-基)-2-(4-苯氧基苯基)-4,5,6,7-四氢吡唑并[1,5-a]嘧啶-3-甲酰胺的结晶形式、其制备及用途 |
| CA3066518A1 (en) | 2017-06-26 | 2019-01-03 | Beigene, Ltd. | Immunotherapy for hepatocellular carcinoma |
| US11377449B2 (en) | 2017-08-12 | 2022-07-05 | Beigene, Ltd. | BTK inhibitors with improved dual selectivity |
| CN111801334B (zh) | 2017-11-29 | 2023-06-09 | 百济神州瑞士有限责任公司 | 使用包含btk抑制剂的组合治疗惰性或侵袭性b-细胞淋巴瘤 |
| SG11202007198WA (en) | 2018-01-31 | 2020-08-28 | Deciphera Pharmaceuticals Llc | Combination therapy for the treatment of gastrointestinal stromal tumors |
| JP2021515767A (ja) | 2018-03-07 | 2021-06-24 | バイエル・アクチエンゲゼルシヤフト | Ｅｒｋ５阻害剤の同定及び使用 |
| MX2020010321A (es) | 2018-03-30 | 2021-01-08 | Incyte Corp | Compuestos heterociclicos como inmunomoduladores. |
| MX2020012045A (es) | 2018-05-11 | 2021-03-29 | Incyte Corp | Derivados de tetrahidro-imidazo[4,5-c]piridina como inmunomoduladores de ligando 1 de muerte programada (pd-l1). |
| CN111825675B (zh) * | 2019-04-15 | 2023-08-01 | 武汉朗来科技发展有限公司 | Rock抑制剂及其制备方法和用途 |
| WO2020234103A1 (en) | 2019-05-21 | 2020-11-26 | Bayer Aktiengesellschaft | Identification and use of kras inhibitors |
| MX2022001671A (es) | 2019-08-09 | 2022-05-13 | Incyte Corp | Sales de un inhibidor de pd-1/pd-l1. |
| BR112022002609A2 (pt) | 2019-08-12 | 2022-08-09 | Deciphera Pharmaceuticals Llc | Métodos de tratamento de tumores estromais gastrointestinais |
| TW202122082A (zh) | 2019-08-12 | 2021-06-16 | 美商迪賽孚爾製藥有限公司 | 治療胃腸道基質瘤方法 |
| AR120109A1 (es) | 2019-09-30 | 2022-02-02 | Incyte Corp | Compuestos de pirido[3,2-d]pirimidina como inmunomoduladores |
| CN114829366A (zh) | 2019-11-11 | 2022-07-29 | 因赛特公司 | Pd-1/pd-l1抑制剂的盐及结晶形式 |
| KR20220123058A (ko) | 2019-12-30 | 2022-09-05 | 데시페라 파마슈티칼스, 엘엘씨. | 1-(4-브로모-5-(1-에틸-7-(메틸아미노)-2-옥소-1,2-디히드로-1,6-나프티리딘-3-일)-2-플루오로페닐)-3-페닐우레아의 조성물 |
| IL293866A (en) | 2019-12-30 | 2022-08-01 | Deciphera Pharmaceuticals Llc | Compositions of amorphous kinase inhibitors and methods of using them |
| US11760756B2 (en) | 2020-11-06 | 2023-09-19 | Incyte Corporation | Crystalline form of a PD-1/PD-L1 inhibitor |
| WO2022099071A1 (en) | 2020-11-06 | 2022-05-12 | Incyte Corporation | Process for making a pd-1/pd-l1 inhibitor and salts and crystalline forms thereof |
| US11780836B2 (en) | 2020-11-06 | 2023-10-10 | Incyte Corporation | Process of preparing a PD-1/PD-L1 inhibitor |
| WO2023139164A1 (en) * | 2022-01-20 | 2023-07-27 | Origenis Gmbh | Cdk9 inhibitors |
| US11786531B1 (en) | 2022-06-08 | 2023-10-17 | Beigene Switzerland Gmbh | Methods of treating B-cell proliferative disorder |
| US11779572B1 (en) | 2022-09-02 | 2023-10-10 | Deciphera Pharmaceuticals, Llc | Methods of treating gastrointestinal stromal tumors |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4200750A (en) | 1977-01-07 | 1980-04-29 | Westwood Pharmaceuticals Inc. | 4-Substituted imidazo [1,2-a]quinoxalines |
| US4327027A (en) * | 1979-06-15 | 1982-04-27 | Vertac Chemical Corporation | Chemical detoxification of toxic chlorinated aromatic compounds |
| DE4327027A1 (de) | 1993-02-15 | 1994-08-18 | Bayer Ag | Imidazoazine |
| DE19912636A1 (de) | 1999-03-20 | 2000-09-21 | Aventis Cropscience Gmbh | Bicyclische Heterocyclen, Verfahren zu ihrer Herstellung und ihre Verwendung als Herbizide und pharmazeutische Mittel |
| TWI312347B (en) | 2001-02-08 | 2009-07-21 | Eisai R&D Man Co Ltd | Bicyclic nitrogen-containing condensed ring compounds |
| UA80296C2 (en) | 2002-09-06 | 2007-09-10 | Biogen Inc | Imidazolopyridines and methods of making and using the same |
| EP1460077B1 (en) | 2003-03-18 | 2007-08-01 | The Jordanian Pharmaceutical Manufacturing Co. Ltd. | Novel pyrazolopyrimidones and their use as PDE inhibitors |
| US7405295B2 (en) | 2003-06-04 | 2008-07-29 | Cgi Pharmaceuticals, Inc. | Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds |
| US20060183746A1 (en) | 2003-06-04 | 2006-08-17 | Currie Kevin S | Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds |
| US7393848B2 (en) | 2003-06-30 | 2008-07-01 | Cgi Pharmaceuticals, Inc. | Certain heterocyclic substituted imidazo[1,2-A]pyrazin-8-ylamines and methods of inhibition of Bruton's tyrosine kinase by such compounds |
| WO2005047290A2 (en) | 2003-11-11 | 2005-05-26 | Cellular Genomics Inc. | Imidazo[1,2-a] pyrazin-8-ylamines as kinase inhibitors |
| EP1812439B2 (en) | 2004-10-15 | 2017-12-06 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| NZ555681A (en) | 2004-11-10 | 2009-08-28 | Cgi Pharmaceuticals Inc | Imidazo[1, 2-a] pyrazin-8-ylamines useful as modulators of kinase activity |
| WO2006065788A2 (en) | 2004-12-13 | 2006-06-22 | Glaxo Group Limited | Novel muscarinic acetylcholine receptor antagonists |
| BRPI0608252A2 (pt) | 2005-03-10 | 2010-04-06 | Cgi Pharmaceuticals Inc | entidades quìmicas, composições farmacêuticas compreendendo as mesmas, métodos utilizando as referidas entidades quìmicas e uso das referidas entidades quìmicas |
| US7470693B2 (en) * | 2005-04-21 | 2008-12-30 | Bristol-Myers Squibb Company | Oxalamide derivatives as kinase inhibitors |
| US20070078136A1 (en) * | 2005-09-22 | 2007-04-05 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful as kinase modulators |
| US7547782B2 (en) * | 2005-09-30 | 2009-06-16 | Bristol-Myers Squibb Company | Met kinase inhibitors |
| US20100160292A1 (en) | 2006-09-11 | 2010-06-24 | Cgi Pharmaceuticals, Inc | Kinase Inhibitors, and Methods of Using and Identifying Kinase Inhibitors |
| WO2008037607A1 (de) | 2006-09-25 | 2008-04-03 | Basf Se | Carbonylgruppen-enthaltende heterocyclische verbindungen und deren verwendung zur bekämpfung von phytopathogenen pilzen |
| US7492329B2 (en) | 2006-10-12 | 2009-02-17 | Hewlett-Packard Development Company, L.P. | Composite material with chirped resonant cells |
| EP2125819B1 (en) * | 2007-03-21 | 2014-10-22 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful for the treatment of proliferative, allergic, autoimmune or inflammatory diseases |
-
2009
- 2009-07-23 WO PCT/US2009/051536 patent/WO2010011837A1/en active Application Filing
- 2009-07-23 US US13/055,601 patent/US8476430B2/en active Active
- 2009-07-23 JP JP2011520196A patent/JP2011529073A/ja not_active Withdrawn
- 2009-07-23 EP EP09790767.9A patent/EP2323665B1/en not_active Not-in-force
- 2009-07-23 CN CN2009801373694A patent/CN102164604A/zh active Pending
