JP2017522273A5 - - Google Patents
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- Publication number
- JP2017522273A5 JP2017522273A5 JP2016570242A JP2016570242A JP2017522273A5 JP 2017522273 A5 JP2017522273 A5 JP 2017522273A5 JP 2016570242 A JP2016570242 A JP 2016570242A JP 2016570242 A JP2016570242 A JP 2016570242A JP 2017522273 A5 JP2017522273 A5 JP 2017522273A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- alkyl
- heteroaryl
- aryl
- 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
- 241000725303 Human immunodeficiency virus Species 0.000 claims description 52
- 229940083346 IAP antagonist Drugs 0.000 claims description 22
- 239000003814 drug Substances 0.000 claims description 19
- 229940124597 therapeutic agent Drugs 0.000 claims description 19
- 239000005557 antagonist Substances 0.000 claims description 13
- 238000011225 antiretroviral therapy Methods 0.000 claims description 12
- 239000012268 protein inhibitor Substances 0.000 claims description 12
- 229940121649 protein inhibitor Drugs 0.000 claims description 12
- 230000001640 apoptogenic effect Effects 0.000 claims description 9
- 230000010076 replication Effects 0.000 claims description 7
- 230000035897 transcription Effects 0.000 claims description 6
- 238000013518 transcription Methods 0.000 claims description 6
- 210000000987 immune system Anatomy 0.000 claims description 5
- 230000000694 effects Effects 0.000 claims description 4
- 230000007774 longterm Effects 0.000 claims description 4
- 230000035755 proliferation Effects 0.000 claims description 4
- 230000006907 apoptotic process Effects 0.000 claims description 3
- 125000000217 alkyl group Chemical group 0.000 claims 55
- 125000003118 aryl group Chemical group 0.000 claims 35
- 125000001072 heteroaryl group Chemical group 0.000 claims 31
- 229910052799 carbon Inorganic materials 0.000 claims 15
- 229920006395 saturated elastomer Polymers 0.000 claims 15
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 13
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 13
- 229910052717 sulfur Inorganic materials 0.000 claims 13
- 125000000753 cycloalkyl group Chemical group 0.000 claims 12
- 229910052760 oxygen Inorganic materials 0.000 claims 11
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 150000001204 N-oxides Chemical class 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 9
- 150000001875 compounds Chemical class 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- -1 aromatic lactam Chemical class 0.000 claims 6
- 125000004429 atom Chemical group 0.000 claims 6
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 6
- 125000006747 (C2-C10) heterocycloalkyl group Chemical group 0.000 claims 5
- 125000004404 heteroalkyl group Chemical group 0.000 claims 5
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 150000003384 small molecules Chemical class 0.000 claims 3
- 125000003003 spiro group Chemical group 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 125000006584 (C3-C10) heterocycloalkyl group Chemical group 0.000 claims 2
- 125000002619 bicyclic group Chemical group 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 125000000547 substituted alkyl group Chemical group 0.000 claims 2
- 125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 230000003247 decreasing effect Effects 0.000 claims 1
- 229940121372 histone deacetylase inhibitor Drugs 0.000 claims 1
- 239000003276 histone deacetylase inhibitor Substances 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 238000000034 method Methods 0.000 description 15
- 210000004027 cell Anatomy 0.000 description 7
- 230000003313 weakening effect Effects 0.000 description 4
- 210000001744 T-lymphocyte Anatomy 0.000 description 1
- 230000003213 activating effect Effects 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462007702P | 2014-06-04 | 2014-06-04 | |
| US62/007,702 | 2014-06-04 | ||
| PCT/US2015/034281 WO2015187998A2 (en) | 2014-06-04 | 2015-06-04 | Use of inhibitor of apoptosis protein (iap) antagonists in hiv therapy |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020066803A Division JP2020125302A (ja) | 2014-06-04 | 2020-04-02 | Ｈｉｖ治療におけるアポトーシスタンパク質阻害剤（ｉａｐ）のアンタゴニストの使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017522273A JP2017522273A (ja) | 2017-08-10 |
| JP2017522273A5 true JP2017522273A5 (enExample) | 2018-07-12 |
| JP6768522B2 JP6768522B2 (ja) | 2020-10-14 |
Family
ID=54767596
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016570242A Active JP6768522B2 (ja) | 2014-06-04 | 2015-06-04 | Ｈｉｖ治療におけるアポトーシスタンパク質阻害剤（ｉａｐ）のアンタゴニストの使用 |
| JP2020066803A Pending JP2020125302A (ja) | 2014-06-04 | 2020-04-02 | Ｈｉｖ治療におけるアポトーシスタンパク質阻害剤（ｉａｐ）のアンタゴニストの使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020066803A Pending JP2020125302A (ja) | 2014-06-04 | 2020-04-02 | Ｈｉｖ治療におけるアポトーシスタンパク質阻害剤（ｉａｐ）のアンタゴニストの使用 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US10300074B2 (enExample) |
| EP (1) | EP3151920B1 (enExample) |
| JP (2) | JP6768522B2 (enExample) |
| CA (1) | CA2950911C (enExample) |
| WO (1) | WO2015187998A2 (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2925764B1 (en) | 2012-11-30 | 2023-03-01 | Sanford-Burnham Medical Research Institute | Inhibitor of apoptosis protein (iap) antagonists |
| MX381320B (es) * | 2013-06-25 | 2025-03-12 | Walter & Eliza Hall Inst Medical Res | Usos de antagonistas de iap en infecciones intracelulares. |
| 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 |
| EP3151920B1 (en) | 2014-06-04 | 2025-08-06 | Sanford-Burnham Medical Research Institute | Use of inhibitor of apoptosis protein (iap) antagonists in hiv therapy |
| CN118436801A (zh) | 2016-05-20 | 2024-08-06 | 豪夫迈·罗氏有限公司 | Protac抗体缀合物及其使用方法 |
| CN113453678A (zh) * | 2018-11-26 | 2021-09-28 | 德彪药业国际股份公司 | Hiv感染的联合治疗 |
| BR112021010353A2 (pt) * | 2018-11-30 | 2021-08-31 | Glaxosmithkline Intellectual Property Development Limited | Compostos úteis em terapia hiv |
| US10870663B2 (en) | 2018-11-30 | 2020-12-22 | Glaxosmithkline Intellectual Property Development Limited | Compounds useful in HIV therapy |
| CN110028508B (zh) * | 2019-05-16 | 2021-05-28 | 南京华威医药科技集团有限公司 | 一种抗肿瘤的重氮双环类细胞凋亡蛋白抑制剂 |
| US20230011378A1 (en) | 2019-08-08 | 2023-01-12 | Institute For Cancer Research D/B/A The Research Institute Of Fox Chase Cancer Center | Combination Therapy For Treatment Of Cancer |
| EP4036570B1 (en) * | 2019-09-26 | 2025-03-05 | FUJIFILM Corporation | Reagent for measuring skin sensitization, method for measuring skin sensitization, and compound |
| 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 |
| EP4143198A4 (en) * | 2020-04-30 | 2024-05-01 | Sanford Burnham Prebys Medical Discovery Institute | Inhibitor of apoptosis (iap) protein antagonists |
| WO2023056069A1 (en) | 2021-09-30 | 2023-04-06 | Angiex, Inc. | Degrader-antibody conjugates and methods of using same |
| AR131299A1 (es) | 2022-12-09 | 2025-03-05 | Debiopharm Int Sa | Nuevos inhibidores de iap, métodos para fabricarlos y usos de los mismos |
| WO2024238598A2 (en) * | 2023-05-15 | 2024-11-21 | Recludix Pharma, Inc. | Stat degraders and uses thereof |
Family Cites Families (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4107288A (en) | 1974-09-18 | 1978-08-15 | Pharmaceutical Society Of Victoria | Injectable compositions, nanoparticles useful therein, and process of manufacturing same |
| US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
| US5455242A (en) | 1991-09-27 | 1995-10-03 | Merrell Dow Pharmaceuticals Inc. | Carboxyalkyl tricyclic derivatives useful as inhibitors of enkephalinase and ace |
| US5457196A (en) | 1991-09-27 | 1995-10-10 | Merrell Dow Pharmaceuticals Inc. | 2-substituted indane-2-carboxyalkyl derivatives useful as inhibitors of enkephalinase and ACE |
| DE69329701T2 (de) | 1992-10-30 | 2001-05-10 | Merrell Pharmaceuticals Inc., Cincinnati | Mercaptoacetylamid substituiertes bizyclisches laktam zur verwendung als enkephalinase und ace-hemmer |
| US5508272A (en) | 1993-06-15 | 1996-04-16 | Bristol-Myers Squibb Company | Compounds containing a fused bicycle ring and processes therefor |
| US7718600B2 (en) | 2000-09-29 | 2010-05-18 | The Trustees Of Princeton University | IAP binding compounds |
| MXPA06008095A (es) | 2004-01-16 | 2007-03-28 | Univ Michigan | Mimeticos de smac conformacionalmente restringidos y sus usos. |
| JP4674231B2 (ja) | 2004-03-01 | 2011-04-20 | ボード・オブ・リージエンツ，ザ・ユニバーシテイ・オブ・テキサス・システム | ２量体小分子アポトーシス増強剤 |
| CA2558615C (en) | 2004-03-23 | 2013-10-29 | Genentech, Inc. | Azabicyclo-octane inhibitors of iap |
| AU2005231956B2 (en) | 2004-04-07 | 2009-11-05 | Novartis Ag | Inhibitors of IAP |
| PL1778718T3 (pl) | 2004-07-02 | 2015-03-31 | Genentech Inc | Inhibitory IAP |
| US7674787B2 (en) | 2004-07-09 | 2010-03-09 | The Regents Of The University Of Michigan | Conformationally constrained Smac mimetics and the uses thereof |
| EA200700225A1 (ru) | 2004-07-12 | 2008-02-28 | Айдан Фармасьютикалз, Инк. | Аналоги тетрапептида |
| 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 |
| AU2005319305B2 (en) | 2004-12-20 | 2012-08-23 | Genentech, Inc. | Pyrrolidine inhibitors of IAP |
| PL1851200T3 (pl) | 2005-02-25 | 2014-06-30 | Tetralogic Pharm Corp | Dimeryczne inhibitory IAP |
| WO2006133147A2 (en) | 2005-06-08 | 2006-12-14 | Novartis Ag | Organic compounds |
| WO2007041775A1 (en) * | 2005-10-10 | 2007-04-19 | The University Of Queensland | Cysteine protease inhibitors incorporating azide groups |
| WO2007048224A1 (en) | 2005-10-25 | 2007-05-03 | Aegera Therapeutics Inc. | Iap bir domain binding compounds |
| WO2007101347A1 (en) | 2006-03-07 | 2007-09-13 | Aegera Therapeutics Inc. | Bir domain binding compounds |
| EP2019671B1 (en) | 2006-05-05 | 2014-09-24 | The Regents Of The University Of Michigan | Intermediates for the preparation of bivalent smac mimetics |
| ATE517873T1 (de) | 2006-12-07 | 2011-08-15 | Novartis Ag | 6-oxo-1,6-dihydropyrimidin-2-yle bei der behandlung proliferativer krankheiten |
| US20090010941A1 (en) | 2007-04-09 | 2009-01-08 | University Of Massachusetts | Methods for treating HIV |
| EP2079309B1 (en) | 2007-04-12 | 2015-11-11 | Joyant Pharmaceuticals Inc | SMAC MIMEE DIMERS AND TRIMERS USEFUL AS ANTICANCER AGENTS |
| DK2139490T3 (da) | 2007-04-13 | 2014-09-08 | Univ Michigan | Diazo-bicykliske smac-mimetiske stoffer og anvendelser deraf |
| US8907092B2 (en) | 2007-04-30 | 2014-12-09 | Genentech, Inc. | Inhibitors of IAP |
| EP2058312A1 (en) | 2007-11-09 | 2009-05-13 | Universita' degli Studi di Milano | SMAC mimetic compounds as apoptosis inducers |
| WO2009126947A2 (en) | 2008-04-11 | 2009-10-15 | The Regents Of The University Of Michigan | Heteroaryl-substituted bicyclic smac mimetics and the uses thereof |
| BR112012015721A2 (pt) * | 2009-12-30 | 2017-09-26 | Avila Therapeutics Inc | modificação covalente de proteínas dirigida por ligante |
| DK2932970T3 (en) * | 2010-01-27 | 2018-05-28 | Viiv Healthcare Co | ANTIVIRAL THERAPY |
| WO2012125622A1 (en) | 2011-03-14 | 2012-09-20 | Bristol-Myers Squibb Company | Substituted adipic acid amides and uses thereof |
| EA201492260A1 (ru) * | 2012-06-06 | 2015-08-31 | Бионор Иммуно Ас | Вакцина |
| EP2925764B1 (en) * | 2012-11-30 | 2023-03-01 | Sanford-Burnham Medical Research Institute | Inhibitor of apoptosis protein (iap) antagonists |
| EP3151920B1 (en) | 2014-06-04 | 2025-08-06 | Sanford-Burnham Medical Research Institute | Use of inhibitor of apoptosis protein (iap) antagonists in hiv therapy |
-
2015
- 2015-06-04 EP EP15803740.8A patent/EP3151920B1/en active Active
- 2015-06-04 JP JP2016570242A patent/JP6768522B2/ja active Active
- 2015-06-04 US US15/313,286 patent/US10300074B2/en active Active
- 2015-06-04 CA CA2950911A patent/CA2950911C/en active Active
- 2015-06-04 WO PCT/US2015/034281 patent/WO2015187998A2/en not_active Ceased
-
2019
- 2019-05-24 US US16/421,966 patent/US10864217B2/en active Active
-
2020
- 2020-04-02 JP JP2020066803A patent/JP2020125302A/ja active Pending