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. |
| EP2903998B1 (en) * | 2012-10-02 | 2017-03-15 | Bristol-Myers Squibb Company | Iap antagonists |
| US9309248B2 (en) * | 2012-10-11 | 2016-04-12 | Hoffmann-La Roche Inc. | Azaindolines |
| JP6333267B2 (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 |
| MA38240B1 (fr) * | 2012-12-11 | 2018-09-28 | Hoffmann La Roche | Nouveaux composes dimeres substitues antagonistes de l'iap utiles pour le traitement du cancer, de preference des tumeurs solides |
| 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 |
| EP3019517A1 (en) * | 2013-07-12 | 2016-05-18 | Bristol-Myers Squibb Company | Iap antagonists |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| MX377796B (es) | 2014-05-13 | 2025-03-11 | Novartis Ag | Compuestos y composiciones para inducir condrogenesis. |
| 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 |
| KR102564925B1 (ko) | 2015-01-20 | 2023-08-07 | 아비나스 오퍼레이션스, 인코포레이티드 | 안드로겐 수용체의 표적화된 분해를 위한 화합물 및 방법 |
| US12312316B2 (en) | 2015-01-20 | 2025-05-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| EP3302482A4 (en) | 2015-06-05 | 2018-12-19 | 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 |
| EP3337476A4 (en) | 2015-08-19 | 2019-09-04 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| EP3535265A4 (en) | 2016-11-01 | 2020-07-08 | Arvinas, Inc. | PROTACS TARGETING ON TAU PROTEIN AND RELATED METHODS FOR USE |
| PL3689868T3 (pl) | 2016-12-01 | 2024-03-11 | Arvinas Operations, Inc. | Pochodne tetrahydronaftalenu i tetrahydroizochinoliny jako degradery receptorów estrogenowych |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| WO2018118598A1 (en) | 2016-12-23 | 2018-06-28 | Arvinas, Inc. | Compounds and methods for the targeted degradation of fetal liver kinase polypeptides |
| 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 |
| CN117510491A (zh) | 2016-12-23 | 2024-02-06 | 阿尔维纳斯运营股份有限公司 | 用于迅速加速性纤维肉瘤多肽的靶向降解的化合物和方法 |
| 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 |
| 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 |
| WO2019099926A1 (en) | 2017-11-17 | 2019-05-23 | Arvinas, 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. |
| CN112912376A (zh) | 2018-08-20 | 2021-06-04 | 阿尔维纳斯运营股份有限公司 | 用于治疗神经变性疾病的具有E3泛素连接酶结合活性并靶向α-突触核蛋白的蛋白水解靶向嵌合(PROTAC)化合物 |
| 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 |
| KR20220012844A (ko) * | 2019-04-05 | 2022-02-04 | 헤파진 테라퓨틱스 (에이치케이) 리미티드 | 아포토시스 단백질 억제제의 2가 길항제 |
| CN119954801A (zh) | 2019-07-17 | 2025-05-09 | 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 |
| MX2022002415A (es) | 2019-08-26 | 2022-03-22 | Arvinas Operations Inc | Metodos de tratamiento del cancer de mama con derivados de tetrahidronaftaleno como degradadores del receptor de estrogenos. |
| US20250268863A1 (en) | 2019-09-25 | 2025-08-28 | Debiopharm International Sa | Dosing regimens for treatment of patients with locally advanced squamous cell carcinoma |
| JP7659553B2 (ja) * | 2019-11-08 | 2025-04-09 | サンフォード バーンハム プレビス メディカル ディスカバリー インスティテュート | アポトーシス阻害（ｉａｐ）タンパク質アンタゴニスト |
| JP2023539663A (ja) | 2020-08-28 | 2023-09-15 | アルビナス・オペレーションズ・インコーポレイテッド | 急速進行性線維肉腫タンパク質分解化合物及び関連する使用方法 |
| BR112023004656A2 (pt) | 2020-09-14 | 2023-05-09 | Arvinas Operations Inc | Formas cristalinas e amorfas de um composto para a degradação direcionada do receptor de estrogênio |
| CA3179181A1 (en) | 2021-03-15 | 2022-09-22 | Maze Therapeutics, Inc. | Inhibitors of glycogen synthase 1 (gys1) and methods of use thereof |
| EP4190452B1 (de) | 2021-12-01 | 2024-07-24 | 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 |
| US12448399B2 (en) | 2023-01-26 | 2025-10-21 | Arvinas Operations, Inc. | Cereblon-based KRAS degrading PROTACs and 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 |
| US7138401B2 (en) | 2003-09-18 | 2006-11-21 | Conforma Therapeutics Corporation | 2-aminopurine analogs having HSP90-inhibiting activity |
| 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 |
| ES2394441T3 (es) | 2004-04-07 | 2013-01-31 | Novartis Ag | Inhibidores de IAP |
| DK1778718T3 (da) | 2004-07-02 | 2014-11-10 | Genentech Inc | Iap-inhibitorer |
| 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 |
| ES2349110T5 (es) | 2004-12-20 | 2013-11-27 | Genentech, Inc. | Inhibidores de IAP derivados de pirrolidina |
| 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 |
| EP1883627B1 (en) * | 2005-05-18 | 2018-04-18 | Pharmascience Inc. | Bir domain binding compounds |
| CA2617642A1 (en) * | 2005-08-09 | 2007-02-22 | Tetralogic Pharmaceuticals Corporation | Treatment of proliferative disorders |
| CA2564872C (en) | 2005-10-25 | 2010-12-21 | Aegera Therapeutics 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. |
| SG171682A1 (en) * | 2006-05-16 | 2011-06-29 | Aegera Therapeutics Inc | Iap bir domain binding compounds |
| 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 WO PCT/US2010/054546 patent/WO2011059763A2/en not_active Ceased
- 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 US US12/914,840 patent/US8551955B2/en not_active Expired - Fee Related
- 2010-10-28 EP EP10830467.6A patent/EP2493879B1/en not_active Not-in-force
- 2010-10-28 EP EP14167843.3A patent/EP2784076A1/en not_active Withdrawn
- 2010-10-28 CA CA2789879A patent/CA2789879A1/en not_active Abandoned
-
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