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) | EP2493879B1 (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 |
| JP6333826B2 (ja) | 2012-10-11 | 2018-05-30 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | アザインドリン |
| BR112015005627A2 (pt) * | 2012-10-11 | 2017-08-08 | Hoffmann La Roche | composto, composição farmacêutica, uso de composto, método de tratamento e invenção. |
| CN104854100B (zh) * | 2012-12-11 | 2017-05-24 | 霍夫曼-拉罗奇有限公司 | 二聚化合物 |
| 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 |
| WO2015006524A1 (en) * | 2013-07-12 | 2015-01-15 | Bristol-Myers Squibb Company | Iap antagonists |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| HRP20241236T1 (hr) | 2014-05-13 | 2024-12-06 | Novartis Ag | Spojevi i pripravci za induciranje hondrogeneze |
| 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 |
| JP6817962B2 (ja) | 2015-01-20 | 2021-01-20 | アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． | ターゲティングされたアンドロゲン受容体分解のための化合物および方法 |
| 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 |
| CA2988436A1 (en) * | 2015-07-13 | 2017-01-19 | Arvinas, Inc. | Alanine-based modulators of proteolysis and associated methods of use |
| EP3337476A4 (en) | 2015-08-19 | 2019-09-04 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| MX2019005007A (es) | 2016-11-01 | 2019-07-18 | Arvinas Inc | Protac dirigidos a la proteína tau y métodos asociados de uso. |
| IL266842B (en) | 2016-12-01 | 2022-09-01 | Arvinas Operations Inc | History of tetrahydronaphthalene and tetrahydroisoquinoline as estrogen receptor antagonists |
| CN110753693A (zh) | 2016-12-23 | 2020-02-04 | 阿尔维纳斯运营股份有限公司 | Egfr蛋白水解靶向嵌合分子和相关使用方法 |
| IL325835A (en) | 2016-12-23 | 2026-03-01 | Univ Yale | Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides |
| US10806737B2 (en) | 2016-12-23 | 2020-10-20 | Arvinas Operations, 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 |
| 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 |
| IL300417A (en) | 2017-01-26 | 2023-04-01 | Arvinas Operations Inc | Bifunctional benzothiophene compounds, preparations containing them and their use in therapy |
| EP3686185B1 (en) * | 2017-09-22 | 2023-12-13 | 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 |
| US11707452B2 (en) | 2018-08-20 | 2023-07-25 | Arvinas Operations, Inc. | Modulators of alpha-synuclein proteolysis and associated methods of use |
| CN113613724B (zh) * | 2018-11-30 | 2024-11-08 | 葛兰素史克知识产权开发有限公司 | 可用于hiv疗法的化合物 |
| EP3911316A1 (en) | 2019-01-17 | 2021-11-24 | Debiopharm International SA | 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 |
| EP3999182A1 (en) | 2019-07-17 | 2022-05-25 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated methods of use |
| WO2021041348A1 (en) | 2019-08-26 | 2021-03-04 | Arvinas Operations, Inc. | Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders |
| AU2020356356A1 (en) | 2019-09-25 | 2022-05-12 | Debiopharm International S.A. | Dosing regimens for treatment of patients with locally advanced squamous cell carcinoma |
| US12678509B2 (en) | 2019-11-08 | 2026-07-14 | Sanford Burnham Prebys Medical Discovery Institute | Inhibitor of apoptosis (IAP) protein antagonists |
| WO2022047145A1 (en) | 2020-08-28 | 2022-03-03 | Arvinas Operations, Inc. | Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use |
| AU2021342287A1 (en) | 2020-09-14 | 2023-04-13 | Arvinas Operations, Inc. | Crystalline forms of a compound for the targeted degradation of estrogen receptor |
| EP4308095A4 (en) | 2021-03-15 | 2025-02-19 | Maze Therapeutics, Inc. | GLYCOGEN SYNTHASE 1 (GYS1) INHIBITORS AND METHODS OF USE THEREOF |
| 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 |
| PE20260006A1 (es) | 2023-01-26 | 2026-01-06 | Arvinas Operations Inc | Protacs degradadores de kras basados en cereblon y usos relacionados con los mismos |
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 |
| NZ546611A (en) | 2003-09-18 | 2010-02-26 | Conforma Therapeutics Corp | Novel heterocyclic compounds as HSP90-inhibitors |
| EP1723122B1 (en) * | 2004-03-01 | 2014-11-19 | Board of Regents, The University of Texas System | Dimeric small molecule potentiators of apoptosis |
| US7345081B2 (en) | 2004-03-23 | 2008-03-18 | Genentech, Inc. | Azabicyclo-octane inhibitors of IAP |
| PL2253614T3 (pl) | 2004-04-07 | 2013-03-29 | Novartis Ag | Inhibitory IAP |
| KR100926203B1 (ko) | 2004-07-02 | 2009-11-09 | 제넨테크, 인크. | Ｉａｐ의 억제제 |
| JP5230865B2 (ja) | 2004-07-15 | 2013-07-10 | テトラロジック ファーマシューティカルズ コーポレーション | Ｉａｐ結合性化合物 |
| MX2007007195A (es) | 2004-12-20 | 2007-10-08 | Genentech Inc | Inhibidores de pirrolidina de iap. |
| EA012810B1 (ru) * | 2005-02-25 | 2009-12-30 | Тетралоджик Фармасеутикалс | Димерные ингибиторы ингибиторов белков апоптоза (iap) |
| WO2006122408A1 (en) * | 2005-05-18 | 2006-11-23 | Aegera Therapeutics Inc. | Bir domain binding compounds |
| CA2617642A1 (en) * | 2005-08-09 | 2007-02-22 | Tetralogic Pharmaceuticals Corporation | Treatment of proliferative disorders |
| AU2006308453B9 (en) | 2005-10-25 | 2011-12-01 | Pharmascience Inc. | IAP BIR domain binding compounds |
| 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 |
| MX2008012053A (es) | 2006-03-21 | 2008-12-17 | Joyant Pharmaceuticals Inc | Promotores de apoptosis de molecula pequeña. |
| BRPI0711591A2 (pt) * | 2006-05-16 | 2011-11-16 | Aegera Therapeutics, Inc. | composto de ligação de domìnio bir da iap |
| CA2684169C (en) | 2007-04-12 | 2012-06-19 | 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 EP10830467.6A patent/EP2493879B1/en not_active Not-in-force
- 2010-10-28 CN CN201080058719.0A patent/CN102958928B/zh not_active Expired - Fee Related
- 2010-10-28 US US12/914,840 patent/US8551955B2/en not_active Expired - Fee Related
- 2010-10-28 CA CA2789879A patent/CA2789879A1/en not_active Abandoned
- 2010-10-28 EP EP14167843.3A patent/EP2784076A1/en not_active Withdrawn
- 2010-10-28 WO PCT/US2010/054546 patent/WO2011059763A2/en not_active Ceased
- 2010-10-28 JP JP2012537075A patent/JP5529282B2/ja 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