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- Withdrawn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 (https=) | 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 (https=) |
| EP (1) | EP2315751A1 (https=) |
| JP (1) | JP2011525915A (https=) |
| AU (1) | AU2009263037B2 (https=) |
| CA (1) | CA2728767A1 (https=) |
| MX (1) | MX2010013920A (https=) |
| WO (1) | WO2009158011A1 (https=) |
Families Citing this family (44)
| Publication number | Priority date | Publication date | Assignee | Title |
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| MX336731B (es) | 2010-01-28 | 2016-01-28 | Harvard College | Composiciones y metodos para potenciar la actividad de proteasoma. |
| CA2819373A1 (en) * | 2010-12-09 | 2012-06-14 | Amgen Inc. | Bicyclic compounds as pim inhibitors |
| MX2013010513A (es) | 2011-03-16 | 2013-10-07 | Hoffmann La Roche | Compuestos de alcohol 6,5-heterociclil-propargilico y usos de los mismos. |
| 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 |
| DK2707101T3 (da) | 2011-05-12 | 2019-05-13 | Proteostasis Therapeutics Inc | Proteostaseregulatorer |
| EP2551670A1 (en) | 2011-07-27 | 2013-01-30 | Merck Patent GmbH | NIK inhibitors cell-based assay |
| US8921576B2 (en) | 2011-10-19 | 2014-12-30 | Kowa Company, Ltd. | Spiroindoline compound, and medicinal agent comprising same |
| JP2015507001A (ja) * | 2012-02-17 | 2015-03-05 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | 三環式化合物及びその使用方法 |
| US9849135B2 (en) | 2013-01-25 | 2017-12-26 | 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 |
| US20150057260A1 (en) * | 2013-08-22 | 2015-02-26 | Genentech, Inc. | Alkynyl alcohols and methods of use |
| US20160096850A9 (en) * | 2013-08-22 | 2016-04-07 | Genentech, Inc. | 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 |
| NZ725860A (en) | 2014-04-04 | 2019-08-30 | 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 |
| BR112017008039B1 (pt) * | 2014-10-23 | 2023-04-11 | Janssen Pharmaceutica N.V. | Derivados de pirazol como inibidores de nik, seu uso no tratamento ou prevenção de câncer e composição farmacêutica que os compreende |
| AU2015334917B2 (en) * | 2014-10-23 | 2019-08-29 | Janssen Pharmaceutica Nv | New compounds as NIK inhibitors |
| MX371151B (es) * | 2014-10-23 | 2020-01-20 | Janssen Pharmaceutica Nv | NUEVOS DERIVADOS DE TIENOPIRIMIDINA EN CALIDAD DE INHIBIDORES DE LA CINASA INDUCTORA DE NF-kB (NIK). |
| JP6616412B2 (ja) * | 2014-10-23 | 2019-12-04 | ヤンセン ファーマシューティカ エヌ．ベー． | Ｎｉｋ阻害剤としての新規のピラゾロピリミジン誘導体 |
| 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 |
| WO2016173438A1 (zh) * | 2015-04-29 | 2016-11-03 | 南京明德新药研发股份有限公司 | 稠环或三环芳基嘧啶化合物用作激酶抑制剂 |
| ES2775449T3 (es) | 2016-01-22 | 2020-07-27 | Janssen Pharmaceutica Nv | Nuevos derivados de cianoindolina sustituida como inhibidores de nik |
| EP3405464B1 (en) | 2016-01-22 | 2019-12-04 | Janssen Pharmaceutica NV | New 6-membered heteroaromatic substituted cyanoindoline derivatives as nik inhibitors |
| 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 |
| WO2018002217A1 (en) * | 2016-06-30 | 2018-01-04 | Janssen Pharmaceutica Nv | Heteroaromatic derivatives as nik inhibitors |
| ES2837157T3 (es) | 2016-06-30 | 2021-06-29 | Janssen Pharmaceutica Nv | Derivados de cianoindolina como inhibidores de NIK |
| WO2018037059A1 (en) * | 2016-08-24 | 2018-03-01 | F. Hoffmann-La Roche Ag | 2-azabicyclo[3.1.0]hexan-3-one derivatives and methods of use |
| WO2018037058A1 (en) * | 2016-08-24 | 2018-03-01 | 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 |
| CN110769830A (zh) | 2017-05-12 | 2020-02-07 | 马瓦隆治疗有限公司 | 作为ii组代谢型谷氨酸受体的别构调节剂的取代的杂环化合物 |
| 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 |
| AU2019239952A1 (en) | 2018-03-20 | 2020-10-08 | Plexxikon Inc. | Compounds and methods for IDO and TDO modulation, and indications therefor |
| CN114222737B (zh) * | 2019-05-31 | 2024-07-26 | 詹森药业有限公司 | NF-κB诱导激酶的小分子抑制剂 |
| EP3782702A1 (en) * | 2019-08-21 | 2021-02-24 | AC BioScience SA | Compounds and use thereof for the treatment of infectious diseases and cancer |
| CA3185604A1 (en) * | 2020-06-12 | 2021-12-16 | Vertex Pharmaceuticals Incorporated | Inhibitors of apol1 and use of the same |
| 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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| GB0123589D0 (en) * | 2001-10-01 | 2001-11-21 | Syngenta Participations Ag | Organic compounds |
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| US20060174937A1 (en) * | 2005-02-09 | 2006-08-10 | Zhang-Lin Zhou | High performance organic materials for solar cells |
| US20090227616A1 (en) * | 2005-11-10 | 2009-09-10 | Smithkline Beecham Corporation, A Corporation | Inhibitors of akt activity |
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| TW200736260A (en) * | 2005-11-10 | 2007-10-01 | Smithkline Beecham Corp | Inhibitors of Akt activity |
| AU2008210455A1 (en) * | 2007-01-31 | 2008-08-07 | Vertex Pharmaceuticals Incorporated | 2-aminopyridine derivatives useful as kinase inhibitors |
| US8343966B2 (en) * | 2008-01-11 | 2013-01-01 | Novartis Ag | Organic compounds |
-
2009
- 2009-06-26 AU AU2009263037A patent/AU2009263037B2/en not_active Ceased
- 2009-06-26 JP JP2011516311A patent/JP2011525915A/ja not_active Withdrawn
- 2009-06-26 EP EP09770549A patent/EP2315751A1/en not_active Withdrawn
- 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 US US12/997,868 patent/US20110086834A1/en not_active Abandoned
- 2009-06-26 MX MX2010013920A patent/MX2010013920A/es not_active Application Discontinuation
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