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 (https=) | 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 (https=) |
| EP (1) | EP2102229B1 (https=) |
| JP (1) | JP5190062B2 (https=) |
| KR (1) | KR20090065548A (https=) |
| CN (1) | CN101595121A (https=) |
| AU (1) | AU2007307763A1 (https=) |
| BR (1) | BRPI0719221A2 (https=) |
| CA (1) | CA2666112A1 (https=) |
| MX (1) | MX2009003834A (https=) |
| RU (1) | RU2009117701A (https=) |
| WO (1) | WO2008045905A1 (https=) |
Families Citing this family (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK1836201T4 (da) | 2004-12-20 | 2013-11-11 | Genentech Inc | Pyrrolidininhibitorer af IAP. |
| 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 |
| WO2007048224A1 (en) | 2005-10-25 | 2007-05-03 | Aegera Therapeutics Inc. | Iap bir domain binding compounds |
| CN101374829A (zh) | 2005-12-19 | 2009-02-25 | 健泰科生物技术公司 | Iap的抑制剂 |
| TWI504597B (zh) | 2006-03-16 | 2015-10-21 | Pharmascience Inc | 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 |
| CN101535300B (zh) | 2006-05-16 | 2014-05-28 | 埃格拉医疗公司 | Iap bir域结合化合物 |
| PE20110220A1 (es) * | 2006-08-02 | 2011-04-11 | 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 |
| NZ577150A (en) * | 2006-12-19 | 2012-04-27 | Genentech Inc | Imidazopyridine inhibitors of iap |
| WO2008134679A1 (en) | 2007-04-30 | 2008-11-06 | Genentech, Inc. | Inhibitors of iap |
| CN102099035A (zh) | 2008-05-16 | 2011-06-15 | 诺瓦提斯公司 | Iap抑制剂的免疫调节 |
| JP2011529962A (ja) | 2008-08-02 | 2011-12-15 | ジェネンテック， インコーポレイテッド | Ｉａｐのインヒビター |
| JP5693452B2 (ja) * | 2008-08-04 | 2015-04-01 | 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、医薬組成物およびそれらの使用方法 |
| US20110218211A1 (en) * | 2008-08-16 | 2011-09-08 | Genentech, Inc. | Azaindole inhibitors of iap |
| US9643922B2 (en) | 2008-08-18 | 2017-05-09 | Yale University | MIF modulators |
| US20120040974A1 (en) * | 2008-08-18 | 2012-02-16 | Yale University | Mif modulators |
| US9540322B2 (en) | 2008-08-18 | 2017-01-10 | Yale University | MIF modulators |
| US20100317593A1 (en) * | 2009-06-12 | 2010-12-16 | Astrazeneca Ab | 2,3-dihydro-1h-indene compounds |
| US20110034469A1 (en) | 2009-08-04 | 2011-02-10 | Takeda Pharmaceutical Company Limited | Heterocyclic Compound |
| MX2012006877A (es) | 2009-12-18 | 2012-08-31 | Idenix Pharmaceuticals Inc | Inhibidores de virus de hepatitis c de arileno o heteroarileno 5, 5 - fusionado. |
| US9284350B2 (en) | 2010-02-12 | 2016-03-15 | Pharmascience Inc. | IAP BIR domain binding compounds |
| 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 |
| EP2651917A1 (en) * | 2010-12-13 | 2013-10-23 | Novartis AG | Dimeric iap inhibitors |
| UY33794A (es) * | 2010-12-13 | 2012-07-31 | Novartis Ag | Inhibidores diméricos de las iap |
| 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 |
| MX2014001088A (es) * | 2011-07-28 | 2015-03-19 | Chdi Foundation Inc | Ciertos inhibidores de quinurenina-3-monooxigenasa, composiciones farmaceuticas, y metodos de uso de las mismas. |
| SI2750677T1 (sl) | 2011-08-30 | 2017-10-30 | Chdi Foundation, Inc. | Inhibitorji kinurenin-3-monooksigenaze, farmacevtski sestavki in postopki njihove uporabe |
| KR20140072037A (ko) | 2011-08-30 | 2014-06-12 | 씨에이치디아이 파운데이션, 인코포레이티드 | 키뉴레닌-3-모노옥시게나제 억제제, 약학적 조성물 및 이의 사용 방법 |
| NO2755614T3 (https=) | 2012-01-03 | 2018-03-31 | ||
| US9980973B2 (en) | 2012-10-19 | 2018-05-29 | Astex Therapeutics Limited | 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 |
| GB201218850D0 (en) * | 2012-10-19 | 2012-12-05 | Astex Therapeutics Ltd | 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 |
| GB201218864D0 (en) * | 2012-10-19 | 2012-12-05 | Astex Therapeutics Ltd | Bicyclic heterocycle compounds and their uses in therapy |
| BR122022015241B1 (pt) | 2013-12-20 | 2023-09-26 | Astex Therapeutics Limited | Compostos heterocíclicos bicíclicos intermediários para a preparação de um composto de fórmula (i) |
| WO2015109391A1 (en) | 2014-01-24 | 2015-07-30 | 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 |
| BR112020009369A2 (pt) | 2017-11-13 | 2020-10-13 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd | miméticos de smac usados como inibidores de iap e seus usos |
| WO2020027225A1 (ja) | 2018-07-31 | 2020-02-06 | ファイメクス株式会社 | 複素環化合物 |
| EP3936126A4 (en) * | 2019-03-07 | 2022-12-21 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | COMBINATION OF IAP INHIBITOR AND IMMUNOCHECK POINT INHIBITOR |
| KR20220006611A (ko) * | 2019-05-10 | 2022-01-17 | 치아타이 티안큉 파마수티컬 그룹 주식회사 | Iap 억제제로서의 smac 모방물의 결정 및 그 제조방법 |
| JP7764027B2 (ja) | 2019-07-31 | 2025-11-05 | ファイメクス株式会社 | 複素環化合物 |
| 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 |
| WO2021148396A1 (en) | 2020-01-20 | 2021-07-29 | 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 |
|---|---|---|---|---|
| KR20020025959A (ko) | 2000-05-23 | 2002-04-04 | 버텍스 파마슈티칼스 인코포레이티드 | 카스파제 억제제 및 이의 용도 |
| WO2004007529A2 (en) * | 2002-07-15 | 2004-01-22 | The Trustees Of Princeton University | Iap binding compounds |
| WO2004005248A1 (en) | 2002-07-02 | 2004-01-15 | Novartis Ag | Peptide inhibitors of smac protein binding to inhibitor of apoptosis proteins (iap) |
| DK2253614T3 (da) | 2004-04-07 | 2013-01-07 | Novartis Ag | IAP-inhibitorer |
| KR100984459B1 (ko) * | 2004-07-02 | 2010-09-29 | 제넨테크, 인크. | Ｉａｐ의 억제제 |
| DK1836201T4 (da) | 2004-12-20 | 2013-11-11 | Genentech Inc | Pyrrolidininhibitorer af IAP. |
| CN101374829A (zh) | 2005-12-19 | 2009-02-25 | 健泰科生物技术公司 | Iap的抑制剂 |
-
2007
- 2007-10-10 WO PCT/US2007/080875 patent/WO2008045905A1/en not_active Ceased
- 2007-10-10 JP JP2009532544A patent/JP5190062B2/ja not_active Expired - Fee Related
- 2007-10-10 RU RU2009117701/04A patent/RU2009117701A/ru not_active Application Discontinuation
- 2007-10-10 AU AU2007307763A patent/AU2007307763A1/en not_active Abandoned
- 2007-10-10 KR KR1020097009617A patent/KR20090065548A/ko not_active Withdrawn
- 2007-10-10 CA CA002666112A patent/CA2666112A1/en not_active Abandoned
- 2007-10-10 EP EP07844058.3A patent/EP2102229B1/en not_active Not-in-force
- 2007-10-10 US US12/445,435 patent/US8044209B2/en not_active Expired - Fee Related
- 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 CN CNA2007800458268A patent/CN101595121A/zh active Pending
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