JP2011525915A5 - - Google Patents
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- Publication number
- JP2011525915A5 JP2011525915A5 JP2011516311A JP2011516311A JP2011525915A5 JP 2011525915 A5 JP2011525915 A5 JP 2011525915A5 JP 2011516311 A JP2011516311 A JP 2011516311A JP 2011516311 A JP2011516311 A JP 2011516311A JP 2011525915 A5 JP2011525915 A5 JP 2011525915A5
- Authority
- JP
- Japan
- Prior art keywords
- alkylene
- balance
- substituted
- alkyl
- allowed
- 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- Withdrawn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
- 150000001875 compounds Chemical class 0.000 claims 25
- 125000000217 alkyl group Chemical group 0.000 claims 23
- 125000002947 alkylene group Chemical group 0.000 claims 20
- 229910052799 carbon Inorganic materials 0.000 claims 14
- 125000004432 carbon atom Chemical group C* 0.000 claims 14
- 125000003118 aryl group Chemical group 0.000 claims 12
- 125000003342 alkenyl group Chemical group 0.000 claims 11
- 125000000304 alkynyl group Chemical group 0.000 claims 11
- 125000000623 heterocyclic group Chemical group 0.000 claims 11
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 8
- 125000001188 haloalkyl group Chemical group 0.000 claims 8
- 125000003710 aryl alkyl group Chemical group 0.000 claims 7
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 7
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 7
- -1 pyrrolopyrimidyl Chemical group 0.000 claims 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000001475 halogen functional group Chemical group 0.000 claims 6
- 125000001786 isothiazolyl group Chemical group 0.000 claims 6
- 125000000842 isoxazolyl group Chemical group 0.000 claims 6
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 6
- 125000002971 oxazolyl group Chemical group 0.000 claims 6
- 125000003373 pyrazinyl group Chemical group 0.000 claims 6
- 125000004076 pyridyl group Chemical group 0.000 claims 6
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 6
- 125000000335 thiazolyl group Chemical group 0.000 claims 6
- 125000002541 furyl group Chemical group 0.000 claims 5
- 125000002883 imidazolyl group Chemical group 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 125000003226 pyrazolyl group Chemical group 0.000 claims 5
- 125000000168 pyrrolyl group Chemical group 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 125000001544 thienyl group Chemical group 0.000 claims 5
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 4
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000004429 atom Chemical group 0.000 claims 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 2
- 230000004968 inflammatory condition Effects 0.000 claims 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 125000005343 heterocyclic alkyl group Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 206010039083 rhinitis Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 125000004306 triazinyl group Chemical group 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 0 CC([U]=CN=*)=C Chemical compound CC([U]=CN=*)=C 0.000 description 15
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13324908P | 2008-06-26 | 2008-06-26 | |
| US61/133,249 | 2008-06-26 | ||
| PCT/US2009/003803 WO2009158011A1 (en) | 2008-06-26 | 2009-06-26 | Alkynyl alcohols as kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011525915A JP2011525915A (ja) | 2011-09-29 |
| JP2011525915A5 true JP2011525915A5 (OSRAM) | 2012-06-07 |
Family
ID=41090264
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011516311A Withdrawn JP2011525915A (ja) | 2008-06-26 | 2009-06-26 | キナーゼ阻害薬としてのアルキニルアルコール類 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20110086834A1 (OSRAM) |
| EP (1) | EP2315751A1 (OSRAM) |
| JP (1) | JP2011525915A (OSRAM) |
| AU (1) | AU2009263037B2 (OSRAM) |
| CA (1) | CA2728767A1 (OSRAM) |
| MX (1) | MX2010013920A (OSRAM) |
| WO (1) | WO2009158011A1 (OSRAM) |
Families Citing this family (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20120117905A (ko) | 2010-01-28 | 2012-10-24 | 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 | 프로테아좀 활성을 향상시키는 조성물 및 방법 |
| US9090593B2 (en) | 2010-12-09 | 2015-07-28 | Amgen Inc. | Bicyclic compounds as Pim inhibitors |
| TW201247650A (en) | 2011-03-16 | 2012-12-01 | Hoffmann La Roche | 6,5-heterocyclic propargylic alcohol compounds and uses therefor |
| EP2688886A1 (en) | 2011-03-22 | 2014-01-29 | Amgen Inc. | Azole compounds as pim inhibitors |
| WO2012135697A2 (en) * | 2011-03-30 | 2012-10-04 | H. Lee Moffitt Cancer Center & Research Institute Inc. | Novel rho kinase inhibitors and methods of use |
| PT2707101T (pt) | 2011-05-12 | 2019-05-30 | Proteostasis Therapeutics Inc | Reguladores da proteostase |
| EP2551670A1 (en) | 2011-07-27 | 2013-01-30 | Merck Patent GmbH | NIK inhibitors cell-based assay |
| JP6050238B2 (ja) | 2011-10-19 | 2016-12-21 | 興和株式会社 | 新規なスピロインドリン化合物、及びそれを含有する医薬 |
| HK1206024A1 (en) * | 2012-02-17 | 2015-12-31 | F. Hoffmann-La Roche Ag | Tricyclic compounds and methods of use therefor |
| WO2014116228A1 (en) | 2013-01-25 | 2014-07-31 | President And Fellows Of Harvard College | Usp14 inhibitors for treating or preventing viral infections |
| TWI663166B (zh) * | 2013-04-24 | 2019-06-21 | 健生藥品公司 | 新化合物 |
| CN105658639A (zh) * | 2013-08-22 | 2016-06-08 | 豪夫迈·罗氏有限公司 | 炔基醇和应用方法 |
| EP3036230A1 (en) * | 2013-08-22 | 2016-06-29 | F. Hoffmann-La Roche AG | Alkynyl alcohols and methods of use |
| TWI704146B (zh) * | 2013-09-26 | 2020-09-11 | 比利時商健生藥品公司 | 用作ＮＩＫ抑制劑之新的1-(４-嘧啶基)-１Ｈ-吡唑並[３,２-ｃ]吡啶衍生物 |
| TWI627173B (zh) * | 2013-09-26 | 2018-06-21 | 比利時商健生藥品公司 | 作為ＮＩＫ抑制劑的新穎３－（１Ｈ－吡唑－４－基）－１Ｈ－吡咯并［２，３－ｃ］吡啶衍生物 |
| WO2015073528A1 (en) | 2013-11-12 | 2015-05-21 | Proteostasis Therapeutics, Inc. | Proteasome activity enhancing compounds |
| WO2015150097A1 (en) | 2014-04-04 | 2015-10-08 | Iomet Pharma Ltd | Indole derivatives for use in medicine |
| KR101551313B1 (ko) * | 2014-07-28 | 2015-09-09 | 충남대학교산학협력단 | 신규한 인덴 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 망막 질환의 예방 또는 치료용 약학적 조성물 |
| ES2704749T3 (es) * | 2014-10-23 | 2019-03-19 | Janssen Pharmaceutica Nv | Nuevos derivados de pirazol en calidad de inhibidores de nik |
| CN107074882B (zh) * | 2014-10-23 | 2019-07-30 | 詹森药业有限公司 | 作为nik抑制剂的新的吡唑并嘧啶衍生物 |
| EA033238B1 (ru) * | 2014-10-23 | 2019-09-30 | Янссен Фармацевтика Нв | Новые производные тиенопиримидина в качестве ингибиторов nik |
| KR102500071B1 (ko) | 2014-10-23 | 2023-02-14 | 얀센 파마슈티카 엔.브이. | Ｎｉｋ 억제제로서의 신규 화합물 |
| JP2018510140A (ja) * | 2015-02-25 | 2018-04-12 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | アルキニルアルコール及び使用方法 |
| CA2984586C (en) * | 2015-04-29 | 2021-02-16 | Guangdong Zhongsheng Pharmaceutical Co., Ltd. | Fused-ring or tricyclic aryl pyrimidine compound used as kinase inhibitor |
| US11001569B2 (en) | 2016-01-22 | 2021-05-11 | Janssen Pharmaceutica Nv | 6-membered heteroaromatic substituted cyanoindoline derivatives as NIK inhibitors |
| TWI739783B (zh) * | 2016-01-22 | 2021-09-21 | 比利時商健生藥品公司 | 作為nik抑制劑的新穎的經取代氰基吲哚啉衍生物 |
| CN105769871A (zh) * | 2016-03-03 | 2016-07-20 | 东北师范大学 | Nik蛋白激酶抑制剂作为制备治疗肝病的药物的应用 |
| EA037358B1 (ru) * | 2016-03-10 | 2021-03-17 | Янссен Фармасьютика Нв | Новые замещённые производные цианиндолина в качестве nik-ингибиторов |
| KR102587619B1 (ko) * | 2016-06-30 | 2023-10-11 | 잔센파마슈티카엔.브이. | Nik 억제제로서의 시아노인돌린 유도체 |
| CN109641882B (zh) * | 2016-06-30 | 2022-10-28 | 杨森制药有限公司 | 作为nik抑制剂的杂芳族衍生物 |
| CN109641894B (zh) * | 2016-08-24 | 2022-09-09 | 豪夫迈·罗氏有限公司 | 2-氮杂双环[3.1.0]己烷-3-酮衍生物及使用方法 |
| EP3504192B1 (en) * | 2016-08-24 | 2022-04-06 | F. Hoffmann-La Roche AG | 2-azabicyclo[3.1.0]hexan-3-one derivatives and methods of use |
| US10858319B2 (en) | 2016-10-03 | 2020-12-08 | Iomet Pharma Ltd. | Indole derivatives for use in medicine |
| WO2018206820A1 (en) | 2017-05-12 | 2018-11-15 | Mavalon Therapeutics Limited | Substituted heterocyclic compounds as allosteric modulators of group ii metabotropic glutamate receptors |
| CN109810110B (zh) * | 2017-11-22 | 2023-01-24 | 中国科学院上海药物研究所 | 一种具有2-氨基嘧啶结构的化合物，其制备方法和用途 |
| EP3768666A1 (en) | 2018-03-20 | 2021-01-27 | Plexxikon Inc. | Compounds and methods for ido and tdo modulation, and indications therefor |
| MA56038B1 (fr) | 2019-05-31 | 2024-11-29 | Janssen Pharmaceutica Nv | Inhibiteurs à petite molécule de kinase induisant nf-kb |
| EP3782702A1 (en) * | 2019-08-21 | 2021-02-24 | AC BioScience SA | Compounds and use thereof for the treatment of infectious diseases and cancer |
| CN116157393A (zh) * | 2020-06-12 | 2023-05-23 | 弗特克斯药品有限公司 | Apol1的抑制剂及其用途 |
| CN113831325A (zh) * | 2020-06-23 | 2021-12-24 | 沈阳药科大学 | 新型吲哚类衍生物及其制备方法和应用 |
| CN111960983A (zh) * | 2020-08-31 | 2020-11-20 | 南通大学 | 一种n-甲基-3-(1-甲基吡咯烷-3-基)丙-1-胺及其合成方法 |
| CN112194609B (zh) * | 2020-10-22 | 2022-11-04 | 西北农林科技大学 | 3,3-二取代氧化吲哚类化合物及其制备方法与用途 |
| CN112174938A (zh) * | 2020-10-27 | 2021-01-05 | 浙江工业大学 | 4-吲哚-2-氨基嘧啶类化合物及其应用 |
| CN115215861B (zh) * | 2021-04-16 | 2024-03-15 | 上海翊石医药科技有限公司 | 一种芳杂环取代的炔烃类化合物及其制备方法和用途 |
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| DK429884A (da) * | 1983-10-07 | 1985-04-08 | Hoffmann La Roche | Heterocycliske forbindelser |
| GB8714537D0 (en) * | 1987-06-22 | 1987-07-29 | Ici Plc | Pyrazine derivatives |
| GB2208860B (en) * | 1987-08-20 | 1991-10-09 | Ici Plc | Pyrimidine derivatives |
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| GB0123589D0 (en) * | 2001-10-01 | 2001-11-21 | Syngenta Participations Ag | Organic compounds |
| CN1313450C (zh) * | 2002-04-26 | 2007-05-02 | 伊莱利利公司 | 速激肽受体拮抗剂 |
| ATE384053T1 (de) * | 2002-04-26 | 2008-02-15 | Lilly Co Eli | Triazolderivate als tachykininrezeptor- antagonisten |
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| DE10229762A1 (de) * | 2002-07-03 | 2004-01-22 | Aventis Pharma Deutschland Gmbh | Pyrazoloisoquinolinenderivaten zur Inhibierung von NFkappaB-induzierende Kinase |
| US20050035498A1 (en) * | 2003-08-13 | 2005-02-17 | Stevens Randal Alan | Methods of making a negative hearing aid mold |
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| US20070167426A1 (en) * | 2004-06-02 | 2007-07-19 | Schering Corporation | Compounds for the treatment of inflammatory disorders and microbial diseases |
| US7829727B2 (en) * | 2005-11-16 | 2010-11-09 | Xerox Corporation | Device containing compound having indolocarbazole moiety and divalent linkage |
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| US20060174937A1 (en) * | 2005-02-09 | 2006-08-10 | Zhang-Lin Zhou | High performance organic materials for solar cells |
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| WO2007058879A2 (en) * | 2005-11-10 | 2007-05-24 | Smithkline Beecham Corporation | Inhibitors of akt activity |
| JP2009517342A (ja) * | 2005-11-10 | 2009-04-30 | スミスクライン・ビーチャム・コーポレイション | Ａｋｔ活性の阻害剤 |
| JP2010518014A (ja) * | 2007-01-31 | 2010-05-27 | バーテックス ファーマシューティカルズ インコーポレイテッド | キナーゼ阻害剤として有用な２−アミノピリジン誘導体 |
| US8343966B2 (en) * | 2008-01-11 | 2013-01-01 | Novartis Ag | Organic compounds |
-
2009
- 2009-06-26 JP JP2011516311A patent/JP2011525915A/ja not_active Withdrawn
- 2009-06-26 MX MX2010013920A patent/MX2010013920A/es not_active Application Discontinuation
- 2009-06-26 US US12/997,868 patent/US20110086834A1/en not_active Abandoned
- 2009-06-26 AU AU2009263037A patent/AU2009263037B2/en not_active Ceased
- 2009-06-26 WO PCT/US2009/003803 patent/WO2009158011A1/en not_active Ceased
- 2009-06-26 CA CA2728767A patent/CA2728767A1/en not_active Abandoned
- 2009-06-26 EP EP09770549A patent/EP2315751A1/en not_active Withdrawn
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