JP2010506847A5 - - Google Patents
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- Publication number
- JP2010506847A5 JP2010506847A5 JP2009532544A JP2009532544A JP2010506847A5 JP 2010506847 A5 JP2010506847 A5 JP 2010506847A5 JP 2009532544 A JP2009532544 A JP 2009532544A JP 2009532544 A JP2009532544 A JP 2009532544A JP 2010506847 A5 JP2010506847 A5 JP 2010506847A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- pyrrolidin
- pyridin
- cyclohexyl
- methylamino
- 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
Links
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 10
- -1 2,3-dihydroindolyl Chemical group 0.000 claims 9
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 125000001475 halogen functional group Chemical group 0.000 claims 3
- 125000001041 indolyl group Chemical group 0.000 claims 3
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 150000001875 compounds Chemical class 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
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- FLBAYUMRQUHISI-UHFFFAOYSA-N 1,8-naphthyridine Chemical compound N1=CC=CC2=CC=CN=C21 FLBAYUMRQUHISI-UHFFFAOYSA-N 0.000 claims 1
- PDQRQJVPEFGVRK-UHFFFAOYSA-N 2,1,3-benzothiadiazole Chemical compound C1=CC=CC2=NSN=C21 PDQRQJVPEFGVRK-UHFFFAOYSA-N 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000005956 isoquinolyl group Chemical group 0.000 claims 1
- FUQJVCQDMIKMLZ-UHFFFAOYSA-N n-[1-[2-[2-(benzimidazol-1-yl)pyridin-4-yl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]-2-(methylamino)propanamide Chemical compound CNC(C)C(=O)NC(C(C)C)C(=O)N1CCCC1C1=CC=NC(N2C3=CC=CC=C3N=C2)=C1 FUQJVCQDMIKMLZ-UHFFFAOYSA-N 0.000 claims 1
- XGAQLJAHEOQJEK-UHFFFAOYSA-N n-[1-cyclohexyl-2-[2-(5-indazol-1-ylpyridin-3-yl)pyrrolidin-1-yl]-2-oxoethyl]-2-(methylamino)propanamide Chemical compound C1CCC(C=2C=C(C=NC=2)N2C3=CC=CC=C3C=N2)N1C(=O)C(NC(=O)C(C)NC)C1CCCCC1 XGAQLJAHEOQJEK-UHFFFAOYSA-N 0.000 claims 1
- NPQDDJGXKMNGIB-UHFFFAOYSA-N n-[1-cyclohexyl-2-[2-(5-naphthalen-2-ylpyridin-3-yl)pyrrolidin-1-yl]-2-oxoethyl]-2-(methylamino)propanamide Chemical compound C1CCC(C=2C=C(C=NC=2)C=2C=C3C=CC=CC3=CC=2)N1C(=O)C(NC(=O)C(C)NC)C1CCCCC1 NPQDDJGXKMNGIB-UHFFFAOYSA-N 0.000 claims 1
- CMBQZNRFGUADIY-UHFFFAOYSA-N n-[1-cyclohexyl-2-[2-[2-(2,3-dihydroindol-1-yl)pyridin-4-yl]pyrrolidin-1-yl]-2-oxoethyl]-2-(methylamino)propanamide Chemical compound C1CCC(C=2C=C(N=CC=2)N2C3=CC=CC=C3CC2)N1C(=O)C(NC(=O)C(C)NC)C1CCCCC1 CMBQZNRFGUADIY-UHFFFAOYSA-N 0.000 claims 1
- GAPYLLQYZGTWHG-UHFFFAOYSA-N n-[1-cyclohexyl-2-[2-[2-(5-fluoroindol-1-yl)pyridin-4-yl]pyrrolidin-1-yl]-2-oxoethyl]-2-(methylamino)propanamide Chemical compound C1CCC(C=2C=C(N=CC=2)N2C3=CC=C(F)C=C3C=C2)N1C(=O)C(NC(=O)C(C)NC)C1CCCCC1 GAPYLLQYZGTWHG-UHFFFAOYSA-N 0.000 claims 1
- HZJHWCJCYNSURC-UHFFFAOYSA-N n-[1-cyclohexyl-2-[2-[5-(3,5-dimethylphenyl)pyridin-3-yl]pyrrolidin-1-yl]-2-oxoethyl]-2-(methylamino)propanamide Chemical compound C1CCC(C=2C=C(C=NC=2)C=2C=C(C)C=C(C)C=2)N1C(=O)C(NC(=O)C(C)NC)C1CCCCC1 HZJHWCJCYNSURC-UHFFFAOYSA-N 0.000 claims 1
- ACQFZFNGNCKJHL-UHFFFAOYSA-N n-[2-[2-[5-(1,3-benzodioxol-5-yl)pyridin-3-yl]pyrrolidin-1-yl]-1-cyclohexyl-2-oxoethyl]-2-(methylamino)propanamide Chemical compound C1CCC(C=2C=C(C=NC=2)C=2C=C3OCOC3=CC=2)N1C(=O)C(NC(=O)C(C)NC)C1CCCCC1 ACQFZFNGNCKJHL-UHFFFAOYSA-N 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 0 CC(C(N(CC*(*)C1)C1*(*)*)=O)NC(C(*)(*)N(C)*)=O Chemical compound CC(C(N(CC*(*)C1)C1*(*)*)=O)NC(C(*)(*)N(C)*)=O 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US82923406P | 2006-10-12 | 2006-10-12 | |
| US60/829,234 | 2006-10-12 | ||
| PCT/US2007/080875 WO2008045905A1 (en) | 2006-10-12 | 2007-10-10 | Pyrrolydine derivatives as iap inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010506847A JP2010506847A (ja) | 2010-03-04 |
| JP2010506847A5 true JP2010506847A5 (enExample) | 2010-12-16 |
| JP5190062B2 JP5190062B2 (ja) | 2013-04-24 |
Family
ID=38984426
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009532544A Expired - Fee Related JP5190062B2 (ja) | 2006-10-12 | 2007-10-10 | Ｉａｐ阻害剤としてのピロリジン誘導体 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US8044209B2 (enExample) |
| EP (1) | EP2102229B1 (enExample) |
| JP (1) | JP5190062B2 (enExample) |
| KR (1) | KR20090065548A (enExample) |
| CN (1) | CN101595121A (enExample) |
| AU (1) | AU2007307763A1 (enExample) |
| BR (1) | BRPI0719221A2 (enExample) |
| CA (1) | CA2666112A1 (enExample) |
| MX (1) | MX2009003834A (enExample) |
| RU (1) | RU2009117701A (enExample) |
| WO (1) | WO2008045905A1 (enExample) |
Families Citing this family (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20120127754A (ko) | 2004-12-20 | 2012-11-23 | 제넨테크, 인크. | Ｉａｐ의 피롤리딘 억제제 |
| JP4954983B2 (ja) | 2005-05-18 | 2012-06-20 | ファーマサイエンス・インコーポレイテッド | Ｂｉｒドメイン結合化合物 |
| RU2418807C2 (ru) | 2005-10-25 | 2011-05-20 | Аегера Терапьютикс Инк. | Соединения, связывающие bir домены iap |
| RU2451025C2 (ru) | 2005-12-19 | 2012-05-20 | Дженентек, Инк. | Ингибиторы iap |
| TWI543988B (zh) | 2006-03-16 | 2016-08-01 | 科學製藥股份有限公司 | 結合於細胞凋亡抑制蛋白（ｉａｐ）之桿狀病毒ｉａｐ重複序列（ｂｉｒ）區域之化合物 |
| US8110681B2 (en) | 2006-03-17 | 2012-02-07 | The United States Of America As Represented By The Secretary, Department Of Health And Human Services | Compounds for the treatment of spinal muscular atrophy and other uses |
| SG10201407457UA (en) | 2006-05-16 | 2014-12-30 | Pharmascience Inc | Iap bir domain binding compounds |
| PE20110218A1 (es) * | 2006-08-02 | 2011-04-01 | Novartis Ag | DERIVADOS DE 2-OXO-ETIL-AMINO-PROPIONAMIDA-PIRROLIDIN-2-IL-SUSTITUIDOS COMO INHIBIDORES DEL ENLACE DE LA PROTEINA Smac AL INHIBIDOR DE LA PROTEINA DE APOPTOSIS |
| RU2466131C2 (ru) * | 2006-12-19 | 2012-11-10 | Дженентек, Инк. | Имидазопиридиновые ингибиторы iap |
| NZ598890A (en) | 2007-04-30 | 2013-10-25 | Genentech Inc | Inhibitors of iap |
| WO2009140447A1 (en) * | 2008-05-16 | 2009-11-19 | Novartis Ag | Immunomodulation by iap inhibitors |
| CA2730448A1 (en) | 2008-08-02 | 2010-02-11 | Genentech, Inc. | Inhibitors of iap |
| NZ601483A (en) * | 2008-08-04 | 2013-10-25 | Chdi Foundation Inc | Certain kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof |
| JP2012500272A (ja) * | 2008-08-16 | 2012-01-05 | ジェネンテック， インコーポレイテッド | Ｉａｐのアザインドールインヒビター |
| US9643922B2 (en) | 2008-08-18 | 2017-05-09 | Yale University | MIF modulators |
| US9540322B2 (en) | 2008-08-18 | 2017-01-10 | Yale University | MIF modulators |
| PE20110368A1 (es) * | 2008-08-18 | 2011-06-13 | Univ Yale | Moduladores de mif |
| US20100317593A1 (en) * | 2009-06-12 | 2010-12-16 | Astrazeneca Ab | 2,3-dihydro-1h-indene compounds |
| AR077688A1 (es) | 2009-08-04 | 2011-09-14 | Takeda Pharmaceutical | Compuestos heterociclicos, utiles en el tratamiento de cancer |
| SG181797A1 (en) | 2009-12-18 | 2012-07-30 | Idenix Pharmaceuticals Inc | 5,5-fused arylene or heteroarylene hepatitis c virus inhibitors |
| MX340870B (es) | 2010-02-12 | 2016-07-27 | Pharmascience Inc | Compuestos de unión del dominio de repetición de inhibidores de proteínas de apoptosis de baculovirus. |
| PT2611797T (pt) * | 2010-08-31 | 2017-02-07 | Hanmi Science Co Ltd | Derivados de quinolina ou de quinazolina com atividade indutora de apoptose nas células |
| UY33794A (es) * | 2010-12-13 | 2012-07-31 | Novartis Ag | Inhibidores diméricos de las iap |
| CN103261186A (zh) * | 2010-12-13 | 2013-08-21 | 诺瓦提斯公司 | 二聚化iap抑制剂 |
| JP2014094886A (ja) * | 2011-02-28 | 2014-05-22 | Nippon Chemiphar Co Ltd | Ｇｐｒ１１９作動薬 |
| GB201106817D0 (en) | 2011-04-21 | 2011-06-01 | Astex Therapeutics Ltd | New compound |
| JP2014521651A (ja) * | 2011-07-28 | 2014-08-28 | シーエイチディーアイ ファウンデーション，インコーポレーテッド | 特定のキヌレニン−３−モノオキシゲナーゼインヒビターおよびその医薬組成物ならびにこれらの使用方法 |
| BR112014004741B1 (pt) | 2011-08-30 | 2021-10-13 | Chdi Foundation, Inc | Entidade química, seu uso e composição farmacêutica compreendendo a mesma |
| AU2012300246A1 (en) | 2011-08-30 | 2014-03-06 | Chdi Foundation, Inc. | Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof |
| NO2755614T3 (enExample) * | 2012-01-03 | 2018-03-31 | ||
| GB201218864D0 (en) | 2012-10-19 | 2012-12-05 | Astex Therapeutics Ltd | Bicyclic heterocycle compounds and their uses in therapy |
| US9980973B2 (en) | 2012-10-19 | 2018-05-29 | Astex Therapeutics Limited | Bicyclic heterocycle compounds and their uses in therapy |
| JP6321020B2 (ja) * | 2012-10-19 | 2018-05-09 | アステックス、セラピューティックス、リミテッドＡｓｔｅｘ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｌｉｍｉｔｅｄ | 二環式複素環化合物およびそれらの治療での使用 |
| GB201218850D0 (en) | 2012-10-19 | 2012-12-05 | Astex Therapeutics Ltd | Bicyclic heterocycle compounds and their uses in therapy |
| GB201218862D0 (en) * | 2012-10-19 | 2012-12-05 | Astex Therapeutics Ltd | Bicyclic heterocycle compounds and their uses in therapy |
| WO2015092420A1 (en) | 2013-12-20 | 2015-06-25 | Astex Therapeutics Limited | Bicyclic heterocycle compounds and their uses in therapy |
| US10441654B2 (en) | 2014-01-24 | 2019-10-15 | Children's Hospital Of Eastern Ontario Research Institute Inc. | SMC combination therapy for the treatment of cancer |
| AU2015289492B2 (en) | 2014-07-17 | 2020-02-20 | Chdi Foundation, Inc. | Methods and compositions for treating HIV-related disorders |
| KR20170004160A (ko) * | 2015-07-01 | 2017-01-11 | 엘지전자 주식회사 | 이동단말기 및 그 제어방법 |
| TWI773657B (zh) | 2015-12-18 | 2022-08-11 | 美商亞德利克斯公司 | 作爲非全身ｔｇｒ５促效劑之經取代之4-苯基吡啶化合物 |
| US12084472B2 (en) | 2015-12-18 | 2024-09-10 | Ardelyx, Inc. | Substituted 4-phenyl pyridine compounds as non-systemic TGR5 agonists |
| IL274598B2 (en) | 2017-11-13 | 2025-01-01 | Chia Tai Tianqing Pharmaceutical Group Co Ltd | SMAC mimetics used as IAP inhibitors and their use |
| CN112533898A (zh) | 2018-07-31 | 2021-03-19 | 日商泛美克斯股份有限公司 | 杂环化合物 |
| WO2020177765A1 (zh) * | 2019-03-07 | 2020-09-10 | 正大天晴药业集团股份有限公司 | Iap抑制剂与免疫检查点抑制剂的组合 |
| JP7587526B2 (ja) * | 2019-05-10 | 2024-11-20 | チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッド | Ｉａｐ阻害剤としてのｓｍａｃ模倣物の結晶及びその製造方法 |
| US20220402935A1 (en) | 2019-07-31 | 2022-12-22 | Fimecs, Inc. | Heterocyclic compound |
| CN112521372B (zh) * | 2019-09-18 | 2022-07-08 | 南京华威医药科技集团有限公司 | 一种细胞凋亡蛋白抑制剂及其制备方法和用途 |
| EP4093394A1 (en) | 2020-01-20 | 2022-11-30 | Astrazeneca AB | Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1283827A2 (en) | 2000-05-23 | 2003-02-19 | Vertex Pharmaceuticals Incorporated | Caspase inhibitors and uses thereof |
| US7718600B2 (en) * | 2000-09-29 | 2010-05-18 | The Trustees Of Princeton University | IAP binding compounds |
| CN100384819C (zh) | 2002-07-02 | 2008-04-30 | 诺瓦提斯公司 | 与细胞凋亡蛋白抑制剂结合的smac蛋白的肽抑制剂 |
| RS52545B (sr) * | 2004-04-07 | 2013-04-30 | Novartis Ag | Inhibitori protein apoptoze (iap) |
| CA2570321C (en) | 2004-07-02 | 2013-10-08 | Genentech, Inc. | Inhibitors of iap |
| KR20120127754A (ko) | 2004-12-20 | 2012-11-23 | 제넨테크, 인크. | Ｉａｐ의 피롤리딘 억제제 |
| RU2451025C2 (ru) * | 2005-12-19 | 2012-05-20 | Дженентек, Инк. | Ингибиторы iap |
-
2007
- 2007-10-10 US US12/445,435 patent/US8044209B2/en not_active Expired - Fee Related
- 2007-10-10 EP EP07844058.3A patent/EP2102229B1/en not_active Not-in-force
- 2007-10-10 JP JP2009532544A patent/JP5190062B2/ja not_active Expired - Fee Related
- 2007-10-10 WO PCT/US2007/080875 patent/WO2008045905A1/en not_active Ceased
- 2007-10-10 RU RU2009117701/04A patent/RU2009117701A/ru not_active Application Discontinuation
- 2007-10-10 CN CNA2007800458268A patent/CN101595121A/zh active Pending
- 2007-10-10 KR KR1020097009617A patent/KR20090065548A/ko not_active Withdrawn
- 2007-10-10 AU AU2007307763A patent/AU2007307763A1/en not_active Abandoned
- 2007-10-10 BR BRPI0719221-5A patent/BRPI0719221A2/pt not_active Application Discontinuation
- 2007-10-10 MX MX2009003834A patent/MX2009003834A/es unknown
- 2007-10-10 CA CA002666112A patent/CA2666112A1/en not_active Abandoned
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