JP2012529535A5 - - Google Patents
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- JP2012529535A5 JP2012529535A5 JP2012515123A JP2012515123A JP2012529535A5 JP 2012529535 A5 JP2012529535 A5 JP 2012529535A5 JP 2012515123 A JP2012515123 A JP 2012515123A JP 2012515123 A JP2012515123 A JP 2012515123A JP 2012529535 A5 JP2012529535 A5 JP 2012529535A5
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- JP
- Japan
- Prior art keywords
- alkyl
- phenyl
- alkoxy
- substituted
- halo
- 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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- 125000000217 alkyl group Chemical group 0.000 claims 264
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 131
- -1 —OH Chemical group 0.000 claims 74
- 125000003545 alkoxy group Chemical group 0.000 claims 56
- 125000005843 halogen group Chemical group 0.000 claims 50
- 125000001424 substituent group Chemical group 0.000 claims 47
- 125000000623 heterocyclic group Chemical group 0.000 claims 30
- 125000004093 cyano group Chemical group *C#N 0.000 claims 28
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 22
- 125000001072 heteroaryl group Chemical group 0.000 claims 21
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 17
- 229910052799 carbon Inorganic materials 0.000 claims 17
- 125000000753 cycloalkyl group Chemical group 0.000 claims 17
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 15
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 15
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 14
- 125000004076 pyridyl group Chemical group 0.000 claims 14
- 125000003118 aryl group Chemical group 0.000 claims 12
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 12
- 125000001624 naphthyl group Chemical group 0.000 claims 11
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 11
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims 10
- KZNICNPSHKQLFF-UHFFFAOYSA-N succinimide Chemical compound O=C1CCC(=O)N1 KZNICNPSHKQLFF-UHFFFAOYSA-N 0.000 claims 10
- 125000005037 alkyl phenyl group Chemical group 0.000 claims 9
- 125000004122 cyclic group Chemical group 0.000 claims 9
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 9
- 150000001875 compounds Chemical class 0.000 claims 8
- 125000001188 haloalkyl group Chemical group 0.000 claims 8
- 125000001041 indolyl group Chemical group 0.000 claims 8
- 229910052760 oxygen Inorganic materials 0.000 claims 8
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 7
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 7
- 125000002541 furyl group Chemical group 0.000 claims 7
- 125000002883 imidazolyl group Chemical group 0.000 claims 7
- 125000002757 morpholinyl group Chemical group 0.000 claims 7
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 6
- 125000000335 thiazolyl group Chemical group 0.000 claims 6
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims 5
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 5
- 235000010290 biphenyl Nutrition 0.000 claims 5
- 239000004305 biphenyl Substances 0.000 claims 5
- 125000004432 carbon atom Chemical group C* 0.000 claims 5
- 125000001207 fluorophenyl group Chemical group 0.000 claims 5
- 125000005842 heteroatom Chemical group 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 125000003386 piperidinyl group Chemical group 0.000 claims 5
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 4
- 125000004103 aminoalkyl group Chemical group 0.000 claims 4
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 4
- 125000001544 thienyl group Chemical group 0.000 claims 4
- 125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 claims 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 3
- 150000001204 N-oxides Chemical class 0.000 claims 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- 125000003226 pyrazolyl group Chemical group 0.000 claims 3
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 claims 2
- 125000006705 (C5-C7) cycloalkyl group Chemical group 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 230000000172 allergic effect Effects 0.000 claims 2
- 208000010668 atopic eczema Diseases 0.000 claims 2
- 208000037979 autoimmune inflammatory disease Diseases 0.000 claims 2
- 125000002393 azetidinyl group Chemical group 0.000 claims 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000004965 chloroalkyl group Chemical group 0.000 claims 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 2
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 238000006467 substitution reaction Methods 0.000 claims 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 1
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 1
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 claims 1
- 125000006704 (C5-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000004605 1,2,3,4-tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims 1
- 125000002178 anthracenyl group Chemical group C1(=CC=CC2=CC3=CC=CC=C3C=C12)* 0.000 claims 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 125000002603 chloroethyl group Chemical group [H]C([*])([H])C([H])([H])Cl 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 125000005059 halophenyl group Chemical group 0.000 claims 1
- 125000004464 hydroxyphenyl group Chemical group 0.000 claims 1
- 125000004594 isoindolinyl group Chemical group C1(NCC2=CC=CC=C12)* 0.000 claims 1
- 125000003566 oxetanyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000000069 prophylactic effect Effects 0.000 claims 1
- 125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 0 C*(C(*=C(C)N)=C(C(*)=C)C(*(C)(C)*)=O)c1ccc(C)c(C)c1 Chemical compound C*(C(*=C(C)N)=C(C(*)=C)C(*(C)(C)*)=O)c1ccc(C)c(C)c1 0.000 description 4
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US18641709P | 2009-06-12 | 2009-06-12 | |
| US61/186,417 | 2009-06-12 | ||
| PCT/US2010/038079 WO2010144647A1 (en) | 2009-06-12 | 2010-06-10 | Nicotinamide compounds useful as kinase modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012529535A JP2012529535A (ja) | 2012-11-22 |
| JP2012529535A5 true JP2012529535A5 (OSRAM) | 2013-06-27 |
Family
ID=42543320
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012515123A Pending JP2012529535A (ja) | 2009-06-12 | 2010-06-10 | キナーゼモジュレーターとして有用なニコチンアミド化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8586751B2 (OSRAM) |
| EP (1) | EP2440204B1 (OSRAM) |
| JP (1) | JP2012529535A (OSRAM) |
| CN (1) | CN102458402B (OSRAM) |
| ES (1) | ES2444777T3 (OSRAM) |
| WO (1) | WO2010144647A1 (OSRAM) |
Families Citing this family (60)
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| US8110581B2 (en) | 2004-11-10 | 2012-02-07 | Incyte Corporation | Lactam compounds and their use as pharmaceuticals |
| AU2011272198B2 (en) * | 2010-06-30 | 2016-09-22 | Fujifilm Corporation | Novel nicotinamide derivatives or salts thereof |
| CA2816219C (en) * | 2010-11-01 | 2019-10-29 | Portola Pharmaceuticals, Inc. | Nicotinamides as syk modulators |
| LT2718270T (lt) * | 2011-06-10 | 2022-08-10 | Merck Patent Gmbh | Pirimidino ir piridino junginių, turinčių btk inhibitorinį aktyvumą, kompozicijos ir gamybos būdai |
| US9782406B2 (en) | 2011-10-25 | 2017-10-10 | Peking University Shenzhen Graduate School | Kinase inhibitor and method for treatment of related diseases |
| CN103073508B (zh) * | 2011-10-25 | 2016-06-01 | 北京大学深圳研究生院 | 激酶抑制剂及治疗相关疾病的方法 |
| ES2661444T3 (es) * | 2011-12-28 | 2018-04-02 | Fujifilm Corporation | Nuevo derivado de nicotinamida o sal del mismo |
| CN104169275B (zh) | 2012-01-13 | 2017-06-09 | 百时美施贵宝公司 | 用作激酶抑制剂的三唑取代的吡啶化合物 |
| WO2013106641A1 (en) | 2012-01-13 | 2013-07-18 | Bristol-Myers Squibb Company | Thiazolyl- or thiadiazolyl-substituted pyridyl compounds useful as kinase inhibitors |
| EP2802576B1 (en) | 2012-01-13 | 2018-06-27 | Bristol-Myers Squibb Company | Heterocyclic-substituted pyridyl compounds useful as kinase inhibitors |
| JP6120941B2 (ja) * | 2012-03-16 | 2017-04-26 | アクシキン ファーマシューティカルズ インコーポレーテッド | ３，５−ジアミノピラゾールキナーゼ阻害剤 |
| WO2013157021A1 (en) | 2012-04-20 | 2013-10-24 | Advinus Therapeutics Limited | Bicyclic compounds, compositions and medicinal applications thereof |
| AU2013250726B2 (en) | 2012-04-20 | 2017-01-05 | Advinus Therapeutics Limited | Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof |
| EP3550031A1 (en) | 2012-07-24 | 2019-10-09 | Pharmacyclics, LLC | Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk) |
| RU2015116532A (ru) * | 2012-10-19 | 2016-12-10 | Ф. Хоффманн-Ля Рош Аг | Ингибиторы тирозинкиназы syk |
| JP6266639B2 (ja) * | 2012-11-08 | 2018-01-24 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | ＩＬ−１２、ＩＬ−２３および／またはＩＦＮαの調節に有用なアルキルアミド置換ピリミジン化合物 |
| TW201422606A (zh) | 2012-11-08 | 2014-06-16 | 必治妥美雅史谷比公司 | 可作爲激酶調節劑之經雙環雜環取代之吡啶化合物 |
| CA2890983A1 (en) | 2012-11-08 | 2014-05-15 | Bristol-Myers Squibb Company | Heteroaryl substituted pyridyl compounds useful as kinase modulators |
| CN104109127B (zh) * | 2013-04-19 | 2019-11-05 | 北京大学深圳研究生院 | 激酶抑制剂及治疗相关疾病的方法 |
| EA028756B1 (ru) | 2013-04-25 | 2017-12-29 | Бэйджин, Лтд. | Конденсированные гетероциклические соединения в качестве ингибиторов протеинкиназы |
| PT3702373T (pt) | 2013-09-13 | 2022-09-27 | Beigene Switzerland Gmbh | Anticorpos anti-pd1 e a sua utilização como agentes terapêuticos e de diagnóstico |
| PL3052476T3 (pl) * | 2013-09-30 | 2021-01-11 | Guangzhou Innocare Pharma Tech Co., Ltd. | Podstawione nikotynoimidowe inhibitory btk oraz sposób ich wytwarzania i zastosowanie w leczeniu raka, stanu zapalnego i chorób automunnologicznych |
| EP3060550B1 (en) * | 2013-10-21 | 2019-05-15 | Merck Patent GmbH | Heteroaryl compounds as btk inhibitors and uses thereof |
| GB201319277D0 (en) * | 2013-10-31 | 2013-12-18 | Akthelia Pharmaceuticals | A new class of inducers of antimicrobial compounds |
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| KR101772836B1 (ko) * | 2014-03-17 | 2017-08-29 | 화이자 인코포레이티드 | 대사 및 관련 장애의 치료에 사용하기 위한 디아실글리세롤 아실트랜스퍼라제 2 억제제 |
| JP6526189B2 (ja) | 2014-07-03 | 2019-06-05 | ベイジーン リミテッド | 抗ｐｄ−ｌ１抗体並びにその治療及び診断のための使用 |
| DK3461821T3 (da) | 2014-10-24 | 2020-08-17 | Bristol Myers Squibb Co | Indolcarboxamidforbindelser, der er brugbar som kinasehæmmere |
| EP3042903B1 (en) | 2015-01-06 | 2019-08-14 | Impetis Biosciences Ltd. | Substituted hetero-bicyclic compounds, compositions and medicinal applications thereof |
| CN104672219A (zh) * | 2015-02-13 | 2015-06-03 | 佛山市赛维斯医药科技有限公司 | 一类含葡萄糖酰胺结构的葡萄糖激酶活化剂及其用途 |
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| AR105112A1 (es) | 2015-06-24 | 2017-09-06 | Bristol Myers Squibb Co | Compuestos de aminopiridina sustituida con heteroarilo |
| TW201718571A (zh) | 2015-06-24 | 2017-06-01 | 必治妥美雅史谷比公司 | 經雜芳基取代之胺基吡啶化合物 |
| UY36747A (es) | 2015-06-24 | 2016-12-30 | Bristol Myers Squibb Company Una Corporación Del Estado De Delaware | Compuestos de aminopiridina sustituida con heteroarilo como inhibidores de quinasa y modulantes de irak-4 y composiciones farmacéuticas que los contienen |
| CN109475536B (zh) | 2016-07-05 | 2022-05-27 | 百济神州有限公司 | 用于治疗癌症的PD-l拮抗剂和RAF抑制剂的组合 |
| SG11201901141WA (en) | 2016-08-16 | 2019-03-28 | Beigene Ltd | 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 |
| CN118252927A (zh) | 2016-08-19 | 2024-06-28 | 百济神州有限公司 | 使用包含btk抑制剂的组合产品治疗癌症 |
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| EA039189B1 (ru) | 2017-05-11 | 2021-12-15 | Бристол-Маерс Сквибб Компани | Тиенопиридины и бензотиофены в качестве ингибиторов irak4 |
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| CN114174279B (zh) | 2019-08-06 | 2024-07-02 | 百时美施贵宝公司 | 可用作irak4抑制剂的双环杂环化合物 |
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| CN111909053B (zh) * | 2020-08-06 | 2022-12-06 | 湖北省生物农药工程研究中心 | 基于二芳胺单元的酰胺类衍生物及其制备方法和应用 |
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-
2010
- 2010-06-10 EP EP10724657.1A patent/EP2440204B1/en not_active Not-in-force
- 2010-06-10 US US13/377,157 patent/US8586751B2/en active Active
- 2010-06-10 JP JP2012515123A patent/JP2012529535A/ja active Pending
- 2010-06-10 WO PCT/US2010/038079 patent/WO2010144647A1/en not_active Ceased
- 2010-06-10 ES ES10724657.1T patent/ES2444777T3/es active Active
- 2010-06-10 CN CN2010800346423A patent/CN102458402B/zh not_active Expired - Fee Related
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