JP2012508274A5 - - Google Patents
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- Publication number
- JP2012508274A5 JP2012508274A5 JP2011536383A JP2011536383A JP2012508274A5 JP 2012508274 A5 JP2012508274 A5 JP 2012508274A5 JP 2011536383 A JP2011536383 A JP 2011536383A JP 2011536383 A JP2011536383 A JP 2011536383A JP 2012508274 A5 JP2012508274 A5 JP 2012508274A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- compound according
- independently
- nitrogen atom
- 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
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- 150000001875 compounds Chemical class 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- -1 2-thiazolyl Chemical group 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical group C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000003006 2-dimethylaminoethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- CWDWFSXUQODZGW-UHFFFAOYSA-N 5-thiazolyl Chemical group [C]1=CN=CS1 CWDWFSXUQODZGW-UHFFFAOYSA-N 0.000 claims 1
- 201000010915 Glioblastoma multiforme Diseases 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 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
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical compound C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11327308P | 2008-11-11 | 2008-11-11 | |
| US61/113,273 | 2008-11-11 | ||
| PCT/US2009/063020 WO2010056563A1 (en) | 2008-11-11 | 2009-11-03 | Akt and p70 s6 kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012508274A JP2012508274A (ja) | 2012-04-05 |
| JP2012508274A5 true JP2012508274A5 (enExample) | 2012-07-12 |
| JP5432275B2 JP5432275B2 (ja) | 2014-03-05 |
Family
ID=41402451
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011536383A Active JP5432275B2 (ja) | 2008-11-11 | 2009-11-03 | Ａｋｔおよびｐ７０ｓ６キナーゼ阻害剤 |
Country Status (36)
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2464125T3 (es) | 2009-07-02 | 2014-05-30 | Sanofi | Nuevos derivados de (6-oxo-1,6-dihidro-pirimidin-2-il)-amida, su preparación y su utilización farmacéutica como inhibidores de fosforilación de AKT |
| MX2012004780A (es) * | 2009-10-23 | 2012-08-23 | Lilly Co Eli | Inhibidores de akt. |
| JP5906303B2 (ja) | 2011-04-07 | 2016-04-20 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ | Ａｋｔキナーゼ阻害剤としてのイミダゾピリダジン類 |
| EP2730575B1 (en) * | 2011-07-09 | 2015-09-16 | Xuanzhu Pharma Co., Ltd. | Crystal form i of salt of dipeptidyl peptidase-iv inhibitor and preparation method and use thereof |
| KR101992505B1 (ko) | 2011-09-12 | 2019-06-24 | 메르크 파텐트 게엠베하 | 키나아제 활성의 조절제로서 용도를 위한 아미노피리미딘 유도체 |
| LT2755965T (lt) * | 2011-09-12 | 2017-11-10 | Merck Patent Gmbh | Naujieji imidazolo aminai kaip kinazės aktyvumo moduliatoriai |
| US9580443B2 (en) | 2012-11-16 | 2017-02-28 | Merck Patent Gmbh | Heterocyclic derivatives as modulators of kinase activity |
| CN110078743A (zh) * | 2012-11-16 | 2019-08-02 | 默克专利有限公司 | 用作激酶活性调节剂的新颖的咪唑-哌啶基衍生物 |
| EP2970201B1 (en) * | 2013-03-11 | 2019-06-19 | Merck Patent GmbH | 6-[4-(1h-imidazol-2-yl)piperidin-1-yl]pyrimidin-4-amine derivatives as modulators of kinase activity |
| US9434714B2 (en) * | 2014-02-11 | 2016-09-06 | Merck Patent Gmbh | Pyrimidine imidazole amines as modulators of kinase activity |
| TW201718574A (zh) | 2015-08-12 | 2017-06-01 | 美國禮來大藥廠 | Ｃｇｒｐ受體拮抗劑 |
| PT3459953T (pt) * | 2016-05-20 | 2021-07-29 | Taiho Pharmaceutical Co Ltd | Novo derivado de 5h-pirrolo[2,3-d]pirimidin-6(7h)-ona |
| WO2021185238A1 (zh) | 2020-03-17 | 2021-09-23 | 江苏恒瑞医药股份有限公司 | 稠合二环类衍生物、其制备方法及其在医药上的应用 |
| CN113444110B (zh) * | 2020-03-25 | 2023-05-12 | 江苏恒瑞医药股份有限公司 | 四氢吡咯并吡唑类衍生物、其制备方法及其在医药上的应用 |
| US20250145641A1 (en) | 2021-09-17 | 2025-05-08 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Fused bicyclic derivative, pharmaceutically acceptable salt, crystal form thereof and preparation method therefor |
| TW202421127A (zh) * | 2022-07-05 | 2024-06-01 | 日商大鵬藥品工業股份有限公司 | ５Ｈ－吡咯并〔２，３－ｄ〕嘧啶－６（７Ｈ）－酮及其鹽體之結晶 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005117909A2 (en) | 2004-04-23 | 2005-12-15 | Exelixis, Inc. | Kinase modulators and methods of use |
| MY179032A (en) | 2004-10-25 | 2020-10-26 | Cancer Research Tech Ltd | Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors |
| WO2006071819A1 (en) | 2004-12-28 | 2006-07-06 | Exelixis, Inc. | [1h-pyrazolo[3, 4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases |
| US7423043B2 (en) * | 2005-02-18 | 2008-09-09 | Lexicon Pharmaceuticals, Inc. | 4-Piperidin-1-yl-7H-pyrrolo[2,3-d]pyrimidine compounds |
| JP5114395B2 (ja) | 2005-06-30 | 2013-01-09 | プロシディオン・リミテッド | Ｇｐｃｒアゴニスト |
| WO2007125310A2 (en) | 2006-04-25 | 2007-11-08 | Astex Therapeutics Limited | Pharmaceutical combinations of pk inhibitors and other active agents |
| ES2878130T3 (es) | 2006-04-25 | 2021-11-18 | Astex Therapeutics Ltd | Derivados de purina y deazapurina como compuestos farmacéuticos |
| WO2008012635A2 (en) | 2006-07-26 | 2008-01-31 | Pfizer Products Inc. | Amine derivatives useful as anticancer agents |
| AR064416A1 (es) * | 2006-12-21 | 2009-04-01 | Cancer Rec Tech Ltd | Derivados de purina, piridina y pirimidina condensadas con heterociclos, moduladores de pka y/o pkb, composiciones farmaceuticas que los contienen, y usos para el tratamiento de enfermedades hiperproliferativas. |
| UA99284C2 (ru) | 2007-05-11 | 2012-08-10 | Елі Ліллі Енд Компані | ИНГИБИТОРЫ р70 S6-КИНАЗЫ |
-
2009
- 2009-10-28 AR ARP090104158A patent/AR074072A1/es unknown
- 2009-10-29 PA PA20098846901A patent/PA8846901A1/es unknown
- 2009-10-29 JO JO2009400A patent/JO2822B1/en active
- 2009-10-29 TW TW098136731A patent/TWI422587B/zh not_active IP Right Cessation
- 2009-11-03 UA UAA201105367A patent/UA100190C2/ru unknown
- 2009-11-03 CN CN2009801449532A patent/CN102216302B/zh active Active
- 2009-11-03 PL PL09744896T patent/PL2358710T3/pl unknown
- 2009-11-03 EP EP09744896A patent/EP2358710B1/en active Active
- 2009-11-03 RS RS20120443A patent/RS52520B/sr unknown
- 2009-11-03 US US12/611,139 patent/US8148387B2/en active Active
- 2009-11-03 MX MX2011005000A patent/MX2011005000A/es active IP Right Grant
- 2009-11-03 JP JP2011536383A patent/JP5432275B2/ja active Active
- 2009-11-03 ES ES09744896T patent/ES2391704T3/es active Active
- 2009-11-03 WO PCT/US2009/063020 patent/WO2010056563A1/en not_active Ceased
- 2009-11-03 KR KR1020117010569A patent/KR101334460B1/ko not_active Expired - Fee Related
- 2009-11-03 AU AU2009314324A patent/AU2009314324B2/en not_active Ceased
- 2009-11-03 HR HRP20120738AT patent/HRP20120738T1/hr unknown
- 2009-11-03 SI SI200930348T patent/SI2358710T1/sl unknown
- 2009-11-03 NZ NZ592062A patent/NZ592062A/xx not_active IP Right Cessation
- 2009-11-03 MY MYPI2011002030A patent/MY161461A/en unknown
- 2009-11-03 CA CA2743019A patent/CA2743019C/en not_active Expired - Fee Related
- 2009-11-03 DK DK09744896.3T patent/DK2358710T3/da active
- 2009-11-03 EA EA201170680A patent/EA018947B1/ru not_active IP Right Cessation
- 2009-11-03 PT PT09744896T patent/PT2358710E/pt unknown
- 2009-11-03 PE PE2011001018A patent/PE20110807A1/es not_active Application Discontinuation
- 2009-11-03 BR BRPI0921916A patent/BRPI0921916A2/pt not_active IP Right Cessation
-
2011
- 2011-03-24 IL IL211940A patent/IL211940A/en not_active IP Right Cessation
- 2011-04-06 ZA ZA2011/02549A patent/ZA201102549B/en unknown
- 2011-04-25 TN TN2011000207A patent/TN2011000207A1/fr unknown
- 2011-05-03 HN HN2011001247A patent/HN2011001247A/es unknown
- 2011-05-06 CR CR20110240A patent/CR20110240A/es unknown
- 2011-05-09 MA MA33822A patent/MA32776B1/fr unknown
- 2011-05-09 DO DO2011000129A patent/DOP2011000129A/es unknown
- 2011-05-11 EC EC2011011048A patent/ECSP11011048A/es unknown
- 2011-05-12 CO CO11058555A patent/CO6382114A2/es active IP Right Grant
-
2012
- 2012-10-05 CY CY20121100928T patent/CY1113409T1/el unknown
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