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
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- JP
- Japan
- Prior art keywords
- compound
- following structure
- following
- pharmaceutically acceptable
- pharmaceutical composition
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- 150000001875 compounds Chemical class 0.000 claims 22
- 239000003814 drug Substances 0.000 claims 2
- 230000001939 inductive effect Effects 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 206010059512 Apoptosis Diseases 0.000 claims 1
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 claims 1
- 108010001801 Tumor Necrosis Factor-alpha Proteins 0.000 claims 1
- 230000006907 apoptotic process Effects 0.000 claims 1
- 230000027455 binding Effects 0.000 claims 1
- 230000030833 cell death Effects 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 239000012458 free base Substances 0.000 claims 1
- 239000003446 ligand Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000546 pharmaceutic aid Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 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 (US07981874-20110719-C00313.png) | 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)
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014025759A1 (en) * | 2012-08-09 | 2014-02-13 | Bristol-Myers Squibb Company | Iap antagonists |
| BR112015003201A2 (pt) | 2012-08-15 | 2017-07-04 | Hoffmann La Roche | composto, composição farmacêutica, uso de um composto e método para tratar ou melhorar o cãncer |
| US9603889B2 (en) * | 2012-10-02 | 2017-03-28 | Bristol-Myers Squibb Company | IAP antagonists |
| CN104640860B (zh) * | 2012-10-11 | 2017-05-31 | 霍夫曼-拉罗奇有限公司 | 氮杂二氢吲哚 |
| US9309248B2 (en) * | 2012-10-11 | 2016-04-12 | Hoffmann-La Roche Inc. | Azaindolines |
| MX2015007053A (es) * | 2012-12-11 | 2015-09-28 | Hoffmann La Roche | Compuestos dimericos. |
| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| GB201311888D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| EP3019517A1 (en) | 2013-07-12 | 2016-05-18 | Bristol-Myers Squibb Company | Iap antagonists |
| TWI662039B (zh) | 2014-05-13 | 2019-06-11 | 瑞士商諾華公司 | 用於誘發軟骨生成之化合物及組合物 |
| 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 |
| US20170327469A1 (en) | 2015-01-20 | 2017-11-16 | Arvinas, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| EP3247708A4 (en) | 2015-01-20 | 2018-09-12 | Arvinas, Inc. | Compounds and methods for the targeted degradation of the androgen receptor |
| US20180147202A1 (en) | 2015-06-05 | 2018-05-31 | Arvinas, Inc. | TANK-BINDING KINASE-1 PROTACs AND ASSOCIATED METHODS OF USE |
| AU2016294450A1 (en) * | 2015-07-13 | 2017-12-07 | Arvinas Operations, 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 |
| KR102173464B1 (ko) | 2016-12-01 | 2020-11-04 | 아비나스 오퍼레이션스, 인코포레이티드 | 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체 |
| WO2018118598A1 (en) | 2016-12-23 | 2018-06-28 | Arvinas, Inc. | Compounds and methods for the targeted degradation of fetal liver kinase polypeptides |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| WO2018119448A1 (en) | 2016-12-23 | 2018-06-28 | Arvinas, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides |
| WO2018119441A1 (en) | 2016-12-23 | 2018-06-28 | Arvinas, Inc. | Egfr proteolysis targeting chimeric molecules and associated methods of use |
| 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 |
| MX2019008934A (es) | 2017-01-26 | 2019-11-05 | Arvinas Operations Inc | Moduladores de la proteolisis del receptor de estrogeno y métodos asociados de uso,. |
| WO2019059687A1 (ko) * | 2017-09-22 | 2019-03-28 | 서울대학교 산학협력단 | 플루오렌 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 hcv 관련 질환의 예방 또는 치료용 약학적 조성물 |
| EP3710443A1 (en) | 2017-11-17 | 2020-09-23 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides |
| MX2020010420A (es) | 2018-04-04 | 2020-12-11 | Arvinas Operations Inc | Moduladores de la proteólisis y métodos asociados de uso. |
| 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 |
| TWI824069B (zh) * | 2018-11-30 | 2023-12-01 | 英商葛蘭素史密斯克藍智慧財產發展有限公司 | 用於hiv治療之化合物 |
| US20220096436A1 (en) | 2019-01-17 | 2022-03-31 | Debiopharm International S.A. | Combination product for the treatment of cancer |
| EP3946607A1 (en) | 2019-04-05 | 2022-02-09 | Hepagene Therapeutics (HK) Limited | Bivalent antagonists of inhibitors of apoptosis proteins |
| EP3999182A1 (en) | 2019-07-17 | 2022-05-25 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated methods of use |
| CA3151770A1 (en) | 2019-09-25 | 2021-04-01 | Silvano BRIENZA | Dosing regimens for treatment of patients with locally advanced squamous cell carcinoma |
| JP2024511979A (ja) | 2021-03-15 | 2024-03-18 | メイズ セラピューティクス， インコーポレイテッド | グリコーゲンシンターゼ１（ｇｙｓ１）の阻害剤及びその使用方法 |
| EP4190452A1 (de) | 2021-12-01 | 2023-06-07 | Eppendorf SE | Abstandshalter zum halten von übereinandergestapelten pipettenspitzenträgern auf abstand voneinander |
| WO2024054591A1 (en) | 2022-09-07 | 2024-03-14 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use |
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 |
| US7138401B2 (en) | 2003-09-18 | 2006-11-21 | Conforma Therapeutics Corporation | 2-aminopurine analogs having HSP90-inhibiting activity |
| AU2005218555B2 (en) * | 2004-03-01 | 2008-01-03 | 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 |
| AR048927A1 (es) | 2004-04-07 | 2006-06-14 | Novartis Ag | Compuestos heterociclicos como inhibidores de proteinas de apoptosis (iap); composiciones farmaceuticas que los contienen y su uso en el tratamiento de una enfermedad proliferativa |
| CA2570321C (en) | 2004-07-02 | 2013-10-08 | Genentech, Inc. | Inhibitors of iap |
| CA2574040C (en) | 2004-07-15 | 2014-05-06 | Tetralogic Pharmaceuticals Corporation | Iap binding compounds |
| EA019420B1 (ru) | 2004-12-20 | 2014-03-31 | Дженентех, Инк. | Пирролидиновые ингибиторы иап (ингибиторов апоптоза) |
| CN103083644B (zh) * | 2005-02-25 | 2014-05-28 | 泰特拉洛吉克药业公司 | Iap二聚体抑制剂 |
| 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 |
| US20070042428A1 (en) * | 2005-08-09 | 2007-02-22 | Stacy Springs | 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 |
| BRPI0708942A2 (pt) | 2006-03-21 | 2011-06-14 | Joyant Pharmaceuticals Inc | composto promotor de apoptose, uso e mÉtodo de produÇço do mesmo e composiÇço farmacÊutica |
| BRPI0711591A2 (pt) * | 2006-05-16 | 2011-11-16 | Aegera Therapeutics Inc | composto de ligação de domìnio bir da iap |
| AU2008240153B2 (en) * | 2007-04-12 | 2013-01-31 | Joyant Pharmaceuticals, Inc. | SMAC mimetic dimers and trimers useful as anti-cancer agents |
| US20110117081A1 (en) * | 2008-05-05 | 2011-05-19 | Aegera Therapeutics, Inc. | Functionalized pyrrolidines and use thereof as iap inhibitors |
-
2010
- 2010-10-28 EP EP14167843.3A patent/EP2784076A1/en not_active Withdrawn
- 2010-10-28 JP JP2012537075A patent/JP5529282B2/ja not_active Expired - Fee Related
- 2010-10-28 CN CN201080058719.0A patent/CN102958928B/zh not_active Expired - Fee Related
- 2010-10-28 WO PCT/US2010/054546 patent/WO2011059763A2/en active Application Filing
- 2010-10-28 EP EP10830467.6A patent/EP2493879B1/en not_active Not-in-force
- 2010-10-28 CA CA2789879A patent/CA2789879A1/en not_active Abandoned
- 2010-10-28 US US12/914,840 patent/US8551955B2/en 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
