JP2013509429A5 - - Google Patents
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- JP2013509429A5 JP2013509429A5 JP2012537075A JP2012537075A JP2013509429A5 JP 2013509429 A5 JP2013509429 A5 JP 2013509429A5 JP 2012537075 A JP2012537075 A JP 2012537075A JP 2012537075 A JP2012537075 A JP 2012537075A JP 2013509429 A5 JP2013509429 A5 JP 2013509429A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- following structure
- following
- pharmaceutically acceptable
- pharmaceutical composition
- 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 22
- 108700012411 TNFSF10 Proteins 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 230000030833 cell death Effects 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 239000012458 free base Substances 0.000 claims 1
- 230000001939 inductive effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 0 C*[C@@](C)C(N[C@@](C(C)(C)C)C(N(CCC1)[C@@]1C(N[C@](CNC(C(CCCC1)C1C(NC[C@](C1=CCCCC1)N*([C@](CCC1)N1C([C@](C(C)(C)C)NC([C@](C)NC)=O)=O)=O)=O)=O)C1CCCCC1)=*)=O)=O Chemical compound C*[C@@](C)C(N[C@@](C(C)(C)C)C(N(CCC1)[C@@]1C(N[C@](CNC(C(CCCC1)C1C(NC[C@](C1=CCCCC1)N*([C@](CCC1)N1C([C@](C(C)(C)C)NC([C@](C)NC)=O)=O)=O)=O)=O)C1CCCCC1)=*)=O)=O 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25578809P | 2009-10-28 | 2009-10-28 | |
| US61/255,788 | 2009-10-28 | ||
| PCT/US2010/054546 WO2011059763A2 (en) | 2009-10-28 | 2010-10-28 | Dimeric smac mimetics |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014084316A Division JP2014167006A (ja) | 2009-10-28 | 2014-04-16 | 二量体Ｓｍａｃ模倣薬 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013509429A JP2013509429A (ja) | 2013-03-14 |
| JP2013509429A5 true JP2013509429A5 (enExample) | 2013-12-05 |
| JP5529282B2 JP5529282B2 (ja) | 2014-06-25 |
Family
ID=43992315
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012537075A Expired - Fee Related JP5529282B2 (ja) | 2009-10-28 | 2010-10-28 | 二量体Ｓｍａｃ模倣薬 |
| JP2014084316A Pending JP2014167006A (ja) | 2009-10-28 | 2014-04-16 | 二量体Ｓｍａｃ模倣薬 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014084316A Pending JP2014167006A (ja) | 2009-10-28 | 2014-04-16 | 二量体Ｓｍａｃ模倣薬 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US8551955B2 (enExample) |
| EP (2) | EP2784076A1 (enExample) |
| JP (2) | JP5529282B2 (enExample) |
| CN (1) | CN102958928B (enExample) |
| CA (1) | CA2789879A1 (enExample) |
| WO (1) | WO2011059763A2 (enExample) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2882740B1 (en) * | 2012-08-09 | 2017-03-01 | Bristol-Myers Squibb Company | Iap antagonists |
| MX2015001905A (es) | 2012-08-15 | 2015-06-05 | Hoffmann La Roche | Azaheterociclos como inhibidores de bir2 y/o bir3. |
| US9603889B2 (en) * | 2012-10-02 | 2017-03-28 | Bristol-Myers Squibb Company | IAP antagonists |
| CA2879870A1 (en) * | 2012-10-11 | 2014-04-17 | F. Hoffmann-La Roche Ag | Azaindolines |
| CA2880324A1 (en) * | 2012-10-11 | 2014-04-17 | F. Hoffmann-La Roche Ag | Azaindolines |
| JP6309536B2 (ja) * | 2012-12-11 | 2018-04-11 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | 二量体化合物 |
| GB201311888D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| US9637518B2 (en) | 2013-07-12 | 2017-05-02 | Bristol-Myers Squibb Company | IAP antagonists |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| EP3143026B1 (en) | 2014-05-13 | 2024-07-10 | Novartis AG | Compounds and compositions for inducing chondrogenesis |
| WO2016079527A1 (en) | 2014-11-19 | 2016-05-26 | Tetralogic Birinapant Uk Ltd | Combination therapy |
| WO2016097773A1 (en) | 2014-12-19 | 2016-06-23 | Children's Cancer Institute | Therapeutic iap antagonists for treating proliferative disorders |
| MX390189B (es) | 2015-01-20 | 2025-03-20 | Arvinas Operations Inc | COMPUESTOS Y METODOS PARA LA DEGRADACION DIRIGIDA DE RECEPTOR DE ANDROGENOs. |
| US12312316B2 (en) | 2015-01-20 | 2025-05-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| WO2016197114A1 (en) | 2015-06-05 | 2016-12-08 | Arvinas, Inc. | Tank-binding kinase-1 protacs and associated methods of use |
| WO2017011590A1 (en) * | 2015-07-13 | 2017-01-19 | Arvinas, Inc. | Alanine-based modulators of proteolysis and associated methods of use |
| WO2017030814A1 (en) | 2015-08-19 | 2017-02-23 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| AU2017367872B2 (en) | 2016-11-01 | 2022-03-31 | Arvinas, Inc. | Tau-protein targeting protacs and associated methods of use |
| CN118834201A (zh) | 2016-12-01 | 2024-10-25 | 阿尔维纳斯运营股份有限公司 | 作为雌激素受体降解剂的四氢萘和四氢异喹啉衍生物 |
| KR20190101406A (ko) | 2016-12-23 | 2019-08-30 | 아비나스 오퍼레이션스, 인코포레이티드 | Egfr 단백질분해 표적화 키메라 분자 및 관련 사용 방법 |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| KR102839545B1 (ko) | 2016-12-23 | 2025-07-29 | 아비나스 오퍼레이션스, 인코포레이티드 | 급속 진행성 섬유육종 폴리펩티드의 표적화 분해를 위한 화합물 및 방법 |
| WO2018118598A1 (en) | 2016-12-23 | 2018-06-28 | Arvinas, Inc. | Compounds and methods for the targeted degradation of fetal liver kinase polypeptides |
| US11191741B2 (en) | 2016-12-24 | 2021-12-07 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide |
| CA3049912A1 (en) | 2017-01-26 | 2018-08-02 | Arvinas Operations, Inc. | Modulators of estrogen receptor proteolysis and associated methods of use |
| US11261175B2 (en) | 2017-09-22 | 2022-03-01 | Seoul National University R&Db Foundation | Fluorene derivative or pharmaceutically acceptable salt thereof, preparation method therefor, and pharmaceutical composition comprising same as effective ingredient for preventing or treating HCV-related disease |
| US11065231B2 (en) | 2017-11-17 | 2021-07-20 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides |
| BR112020020307A2 (pt) | 2018-04-04 | 2021-01-12 | Arvinas Operations, Inc. | Moduladores de proteólise e métodos de uso associados |
| JP7297053B2 (ja) | 2018-08-20 | 2023-06-23 | アルビナス・オペレーションズ・インコーポレイテッド | 神経変性疾患を治療するためのｅ３ユビキチンリガーゼ結合活性を有するキメラ（ｐｒｏｔａｃ）化合物を標的とし、アルファ－シヌクレインタンパク質を標的とするタンパク質分解 |
| EP4342473A3 (en) * | 2018-11-30 | 2024-05-15 | GlaxoSmithKline Intellectual Property Development Limited | Compounds useful in hiv therapy |
| WO2020148447A1 (en) | 2019-01-17 | 2020-07-23 | Debiopharm International S.A. | Combination product for the treatment of cancer |
| AU2020252216B2 (en) * | 2019-04-05 | 2026-02-26 | Hepagene Therapeutics (HK) Limited | Bivalent antagonists of inhibitors of apoptosis proteins |
| CN114867727B (zh) | 2019-07-17 | 2025-02-21 | 阿尔维纳斯运营股份有限公司 | Tau蛋白靶向化合物及相关使用方法 |
| IL290789B2 (en) | 2019-08-26 | 2025-09-01 | Arvinas Operations Inc | Methods for treating breast cancer with a history of tetrahydronaphthalene as estrogen receptor-disrupting agents |
| WO2021058794A1 (en) | 2019-09-25 | 2021-04-01 | Debiopharm International S.A. | Dosing regimens for treatment of patients with locally advanced squamous cell carcinoma |
| US20230115837A1 (en) * | 2019-11-08 | 2023-04-13 | Sanford Burnham Prebys Medical Discovery Institute | Inhibitor of apoptosis (iap) protein antagonists |
| US12180193B2 (en) | 2020-08-28 | 2024-12-31 | Arvinas Operations, Inc. | Accelerating fibrosarcoma protein degrading compounds and associated methods of use |
| KR20230069144A (ko) | 2020-09-14 | 2023-05-18 | 아비나스 오퍼레이션스, 인코포레이티드 | 에스트로겐 수용체의 표적화된 분해를 위한 화합물의 결정질 형태 |
| MX2023009857A (es) | 2021-03-15 | 2024-01-03 | Maze Therapeutics Inc | Inhibidores de la glucogeno sintasa 1 (gys1) y metodos de uso de los mismos. |
| EP4190452B1 (de) | 2021-12-01 | 2024-07-24 | Eppendorf SE | Abstandshalter zum halten von übereinandergestapelten pipettenspitzenträgern auf abstand voneinander |
| EP4584258A1 (en) | 2022-09-07 | 2025-07-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use |
| AU2024212035A1 (en) | 2023-01-26 | 2025-08-14 | Arvinas Operations, Inc. | Cereblon-based kras degrading protacs ans uses related thereto |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4261989A (en) | 1979-02-19 | 1981-04-14 | Kaken Chemical Co. Ltd. | Geldanamycin derivatives and antitumor drug |
| GB9213215D0 (en) * | 1992-06-20 | 1992-08-05 | Wellcome Found | Peptides |
| US5387584A (en) | 1993-04-07 | 1995-02-07 | Pfizer Inc. | Bicyclic ansamycins |
| US5932566A (en) | 1994-06-16 | 1999-08-03 | Pfizer Inc. | Ansamycin derivatives as antioncogene and anticancer agents |
| US5624677A (en) | 1995-06-13 | 1997-04-29 | Pentech Pharmaceuticals, Inc. | Controlled release of drugs delivered by sublingual or buccal administration |
| US6790785B1 (en) | 2000-09-15 | 2004-09-14 | The Board Of Trustees Of The University Of Illinois | Metal-assisted chemical etch porous silicon formation method |
| WO2003086470A2 (en) | 2002-04-17 | 2003-10-23 | Deutsches Krebsforschungszentrum | Smac-peptides as therapeutics against cancer and autoimmune diseases |
| EP2145888A1 (en) | 2003-09-18 | 2010-01-20 | Conforma Therapeutics Corporation | Deazapurine derivatives as HSP90-Inhibitors |
| US7309792B2 (en) | 2004-03-01 | 2007-12-18 | Board Of Regents, The University Of Texas System | Dimeric small molecule potentiators of apoptosis |
| AU2005228950B2 (en) | 2004-03-23 | 2012-02-02 | Genentech, Inc. | Azabicyclo-octane inhibitors of IAP |
| RS52545B (sr) | 2004-04-07 | 2013-04-30 | Novartis Ag | Inhibitori protein apoptoze (iap) |
| NZ588799A (en) | 2004-07-02 | 2012-06-29 | Genentech Inc | Inhibitors of iap |
| ES2475207T3 (es) | 2004-07-15 | 2014-07-10 | Tetralogic Pharmaceuticals Corporation | Compuestos de unión a IAP |
| DK1836201T4 (da) | 2004-12-20 | 2013-11-11 | Genentech Inc | Pyrrolidininhibitorer af IAP. |
| PL1851200T3 (pl) | 2005-02-25 | 2014-06-30 | Tetralogic Pharm Corp | Dimeryczne inhibitory IAP |
| EP1883627B1 (en) * | 2005-05-18 | 2018-04-18 | Pharmascience Inc. | Bir domain binding compounds |
| WO2007021825A2 (en) * | 2005-08-09 | 2007-02-22 | Tetralogic Pharmaceuticals Corporation | Treatment of proliferative disorders |
| KR20080067357A (ko) | 2005-10-25 | 2008-07-18 | 에게라 쎄라퓨틱스 인코포레이티드 | Ｉａｐ ｂｉｒ 도메인 결합 화합물 |
| 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 |
| EP1996184A4 (en) | 2006-03-21 | 2010-09-22 | Joyant Pharmaceuticals Inc | SMALL MOLECULAR APOPTOSIS PROMOTERS |
| WO2007131366A1 (en) | 2006-05-16 | 2007-11-22 | Aegera Therapeutics Inc. | Iap bir domain binding compounds |
| EP2079309B1 (en) | 2007-04-12 | 2015-11-11 | Joyant Pharmaceuticals Inc | SMAC MIMEE DIMERS AND TRIMERS USEFUL AS ANTICANCER AGENTS |
| WO2009136290A1 (en) * | 2008-05-05 | 2009-11-12 | Aegera Therapeutics, Inc. | Functionalized pyrrolidines and use thereof as iap inhibitors |
-
2010
- 2010-10-28 JP JP2012537075A patent/JP5529282B2/ja not_active Expired - Fee Related
- 2010-10-28 WO PCT/US2010/054546 patent/WO2011059763A2/en not_active Ceased
- 2010-10-28 EP EP14167843.3A patent/EP2784076A1/en not_active Withdrawn
- 2010-10-28 CA CA2789879A patent/CA2789879A1/en not_active Abandoned
- 2010-10-28 EP EP10830467.6A patent/EP2493879B1/en not_active Not-in-force
- 2010-10-28 US US12/914,840 patent/US8551955B2/en not_active Expired - Fee Related
- 2010-10-28 CN CN201080058719.0A patent/CN102958928B/zh not_active Expired - Fee Related
-
2013
- 2013-08-22 US US13/973,979 patent/US20130344026A1/en not_active Abandoned
-
2014
- 2014-04-16 JP JP2014084316A patent/JP2014167006A/ja active Pending