JP2010523722A5 - - Google Patents
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- JP2010523722A5 JP2010523722A5 JP2010503269A JP2010503269A JP2010523722A5 JP 2010523722 A5 JP2010523722 A5 JP 2010523722A5 JP 2010503269 A JP2010503269 A JP 2010503269A JP 2010503269 A JP2010503269 A JP 2010503269A JP 2010523722 A5 JP2010523722 A5 JP 2010523722A5
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- 150000001875 compounds Chemical class 0.000 claims description 109
- 238000000034 method Methods 0.000 claims description 64
- 239000003446 ligand Substances 0.000 claims description 40
- 230000006907 apoptotic process Effects 0.000 claims description 38
- 229910052739 hydrogen Inorganic materials 0.000 claims description 38
- 239000000411 inducer Substances 0.000 claims description 36
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 35
- 108060008682 Tumor Necrosis Factor Proteins 0.000 claims description 34
- 125000001072 heteroaryl group Chemical group 0.000 claims description 34
- 102000003390 tumor necrosis factor Human genes 0.000 claims description 34
- 239000001257 hydrogen Substances 0.000 claims description 32
- 229910052760 oxygen Inorganic materials 0.000 claims description 28
- 125000003107 substituted aryl group Chemical group 0.000 claims description 28
- 229910052717 sulfur Inorganic materials 0.000 claims description 28
- 150000001717 carbocyclic compounds Chemical class 0.000 claims description 26
- 239000002246 antineoplastic agent Substances 0.000 claims description 24
- 229910052799 carbon Inorganic materials 0.000 claims description 20
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 20
- 150000001420 substituted heterocyclic compounds Chemical class 0.000 claims description 20
- 150000002431 hydrogen Chemical class 0.000 claims description 18
- 101000610604 Homo sapiens Tumor necrosis factor receptor superfamily member 10B Proteins 0.000 claims description 16
- 102100031988 Tumor necrosis factor ligand superfamily member 6 Human genes 0.000 claims description 16
- 102100040112 Tumor necrosis factor receptor superfamily member 10B Human genes 0.000 claims description 16
- 239000000556 agonist Substances 0.000 claims description 16
- 241001465754 Metazoa Species 0.000 claims description 15
- 101000610605 Homo sapiens Tumor necrosis factor receptor superfamily member 10A Proteins 0.000 claims description 14
- 102100040113 Tumor necrosis factor receptor superfamily member 10A Human genes 0.000 claims description 14
- 125000003118 aryl group Chemical group 0.000 claims description 14
- 201000010099 disease Diseases 0.000 claims description 14
- 125000000217 alkyl group Chemical group 0.000 claims description 12
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims description 12
- 230000003463 hyperproliferative effect Effects 0.000 claims description 12
- 150000003839 salts Chemical class 0.000 claims description 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 9
- 108010039471 Fas Ligand Protein Proteins 0.000 claims description 8
- 101150009046 Tnfrsf1a gene Proteins 0.000 claims description 8
- 108050002568 Tumor necrosis factor ligand superfamily member 6 Proteins 0.000 claims description 8
- 229940127089 cytotoxic agent Drugs 0.000 claims description 8
- 239000000651 prodrug Substances 0.000 claims description 8
- 229940002612 prodrug Drugs 0.000 claims description 8
- 206010028980 Neoplasm Diseases 0.000 claims description 6
- 125000006242 amine protecting group Chemical group 0.000 claims description 6
- 201000011510 cancer Diseases 0.000 claims description 6
- 208000035475 disorder Diseases 0.000 claims description 6
- 230000006882 induction of apoptosis Effects 0.000 claims description 6
- 229910052757 nitrogen Inorganic materials 0.000 claims description 6
- 230000005855 radiation Effects 0.000 claims description 6
- 206010029113 Neovascularisation Diseases 0.000 claims description 4
- 125000005466 alkylenyl group Chemical group 0.000 claims description 4
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 125000001188 haloalkyl group Chemical group 0.000 claims description 4
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 4
- 150000002391 heterocyclic compounds Chemical class 0.000 claims description 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 125000001424 substituent group Chemical group 0.000 claims description 4
- 150000001336 alkenes Chemical class 0.000 claims description 3
- 125000002485 formyl group Chemical class [H]C(*)=O 0.000 claims description 3
- 238000002360 preparation method Methods 0.000 claims description 3
- 206010000050 Abdominal adhesions Diseases 0.000 claims description 2
- 201000001320 Atherosclerosis Diseases 0.000 claims description 2
- 206010012689 Diabetic retinopathy Diseases 0.000 claims description 2
- 208000010412 Glaucoma Diseases 0.000 claims description 2
- 239000002136 L01XE07 - Lapatinib Substances 0.000 claims description 2
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims description 2
- 201000004681 Psoriasis Diseases 0.000 claims description 2
- 206010038933 Retinopathy of prematurity Diseases 0.000 claims description 2
- 206010039710 Scleroderma Diseases 0.000 claims description 2
- 206010043189 Telangiectasia Diseases 0.000 claims description 2
- 206010052779 Transplant rejections Diseases 0.000 claims description 2
- 208000013058 Weber syndrome Diseases 0.000 claims description 2
- 208000027418 Wounds and injury Diseases 0.000 claims description 2
- 230000033115 angiogenesis Effects 0.000 claims description 2
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 claims description 2
- 201000007293 brain stem infarction Diseases 0.000 claims description 2
- 150000001735 carboxylic acids Chemical group 0.000 claims description 2
- 238000006243 chemical reaction Methods 0.000 claims description 2
- 238000009833 condensation Methods 0.000 claims description 2
- 230000005494 condensation Effects 0.000 claims description 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 2
- 239000012458 free base Substances 0.000 claims description 2
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims description 2
- 229960005277 gemcitabine Drugs 0.000 claims description 2
- 238000005469 granulation Methods 0.000 claims description 2
- 230000003179 granulation Effects 0.000 claims description 2
- 125000001475 halogen functional group Chemical group 0.000 claims description 2
- 125000005843 halogen group Chemical group 0.000 claims description 2
- 125000000623 heterocyclic group Chemical group 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
- 230000001969 hypertrophic effect Effects 0.000 claims description 2
- 230000001939 inductive effect Effects 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- BCFGMOOMADDAQU-UHFFFAOYSA-N lapatinib Chemical compound O1C(CNCCS(=O)(=O)C)=CC=C1C1=CC=C(N=CN=C2NC=3C=C(Cl)C(OCC=4C=C(F)C=CC=4)=CC=3)C2=C1 BCFGMOOMADDAQU-UHFFFAOYSA-N 0.000 claims description 2
- 229960004891 lapatinib Drugs 0.000 claims description 2
- 208000002780 macular degeneration Diseases 0.000 claims description 2
- 230000002107 myocardial effect Effects 0.000 claims description 2
- 201000003142 neovascular glaucoma Diseases 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 231100000241 scar Toxicity 0.000 claims description 2
- 229940063683 taxotere Drugs 0.000 claims description 2
- 208000009056 telangiectasis Diseases 0.000 claims description 2
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims 29
- -1 hydrogen compound Chemical class 0.000 claims 2
- 239000012190 activator Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 230000001235 sensitizing effect Effects 0.000 claims 1
- 0 CC(*)C*(*)C(*[C@@](C*(*)CC[C@@](CC1)*2[C@]1IC)C2=O)=O Chemical compound CC(*)C*(*)C(*[C@@](C*(*)CC[C@@](CC1)*2[C@]1IC)C2=O)=O 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 2
- 230000003213 activating effect Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 238000009877 rendering Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US92334807P | 2007-04-13 | 2007-04-13 | |
| US60/923,348 | 2007-04-13 | ||
| PCT/US2008/060215 WO2008128171A2 (en) | 2007-04-13 | 2008-04-14 | Diazo bicyclic smac mimetics and the uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010523722A JP2010523722A (ja) | 2010-07-15 |
| JP2010523722A5 true JP2010523722A5 (enExample) | 2012-04-19 |
| JP5416089B2 JP5416089B2 (ja) | 2014-02-12 |
Family
ID=39864640
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010503269A Active JP5416089B2 (ja) | 2007-04-13 | 2008-04-14 | ジアゾ二環式ｓｍａｃ模倣物およびその使用 |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US8278293B2 (enExample) |
| EP (1) | EP2139490B1 (enExample) |
| JP (1) | JP5416089B2 (enExample) |
| KR (1) | KR101081685B1 (enExample) |
| CN (1) | CN101686981B (enExample) |
| AU (1) | AU2008240119B2 (enExample) |
| BR (1) | BRPI0810522B8 (enExample) |
| CA (1) | CA2683318C (enExample) |
| CY (1) | CY1115735T1 (enExample) |
| DK (1) | DK2139490T3 (enExample) |
| EA (1) | EA017797B1 (enExample) |
| ES (1) | ES2504216T3 (enExample) |
| HR (1) | HRP20140885T1 (enExample) |
| HU (1) | HUE024142T2 (enExample) |
| IL (1) | IL201474A (enExample) |
| MX (1) | MX2009011069A (enExample) |
| NZ (1) | NZ580468A (enExample) |
| PL (1) | PL2139490T3 (enExample) |
| PT (1) | PT2139490E (enExample) |
| SI (1) | SI2139490T1 (enExample) |
| WO (1) | WO2008128171A2 (enExample) |
| ZA (1) | ZA200907055B (enExample) |
Families Citing this family (64)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1883627B1 (en) | 2005-05-18 | 2018-04-18 | Pharmascience Inc. | Bir domain binding compounds |
| 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 |
| EP2139490B1 (en) * | 2007-04-13 | 2014-07-02 | The Regents of the University of Michigan | Diazo bicyclic smac mimetics and the uses thereof |
| EP2491041B1 (en) | 2009-10-23 | 2017-08-09 | The Regents of the University of Michigan | Bivalent diazo bicyclic smac mimetics and the uses thereof |
| BR112012010698A2 (pt) | 2009-11-05 | 2016-11-29 | Uab Research Foundation | método para tratamento de um sujeito com câncer, método de triagem de uma célula de câncer de mama, e , anticorpo |
| SG182724A1 (en) | 2010-02-12 | 2012-08-30 | Pharmascience Inc | Iap bir domain binding compounds |
| WO2012052758A1 (en) | 2010-10-22 | 2012-04-26 | Astrazeneca Ab | Response biomarkers for iap antagonists in human cancers |
| GB201106817D0 (en) * | 2011-04-21 | 2011-06-01 | Astex Therapeutics Ltd | New compound |
| RU2649975C2 (ru) * | 2012-08-23 | 2018-04-06 | Дзе Реджентс Оф Дзе Юнивёрсити Оф Мичиган | Бивалентные ингибиторы ингибиторов белков апоптоза и терапевтические способы их применения |
| JP6382831B2 (ja) | 2012-11-30 | 2018-08-29 | サンフォード−バーンハム メディカル リサーチ インスティテュート | アポトーシス阻害タンパク質（ｉａｐ）のアンタゴニスト |
| 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 |
| BR112016002613A2 (pt) | 2013-09-09 | 2017-08-01 | Halliburton Energy Services Inc | método de cimentação, composição de cimento de pega lenta e sistema para a cimentação |
| US10441654B2 (en) | 2014-01-24 | 2019-10-15 | Children's Hospital Of Eastern Ontario Research Institute Inc. | SMC combination therapy for the treatment of cancer |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| CA2950911C (en) | 2014-06-04 | 2023-10-10 | Sanford-Burnham Medical Research Institute | Use of inhibitor of apoptosis protein (iap) antagonists in hiv therapy |
| 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 |
| US12312316B2 (en) | 2015-01-20 | 2025-05-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| MX390189B (es) | 2015-01-20 | 2025-03-20 | Arvinas Operations Inc | COMPUESTOS Y METODOS PARA LA DEGRADACION DIRIGIDA DE RECEPTOR DE ANDROGENOs. |
| GB201506871D0 (en) | 2015-04-22 | 2015-06-03 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201506872D0 (en) | 2015-04-22 | 2015-06-03 | Ge Oil & Gas Uk Ltd | Novel compounds |
| WO2016197114A1 (en) | 2015-06-05 | 2016-12-08 | Arvinas, Inc. | Tank-binding kinase-1 protacs 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 |
| JP2019514878A (ja) | 2016-04-20 | 2019-06-06 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ | Ｒｉｐｋ２阻害剤を含むコンジュゲート |
| GB201610147D0 (en) | 2016-06-10 | 2016-07-27 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| 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 |
| WO2018118598A1 (en) | 2016-12-23 | 2018-06-28 | Arvinas, Inc. | Compounds and methods for the targeted degradation of fetal liver kinase polypeptides |
| KR20190101406A (ko) | 2016-12-23 | 2019-08-30 | 아비나스 오퍼레이션스, 인코포레이티드 | Egfr 단백질분해 표적화 키메라 분자 및 관련 사용 방법 |
| KR102839545B1 (ko) | 2016-12-23 | 2025-07-29 | 아비나스 오퍼레이션스, 인코포레이티드 | 급속 진행성 섬유육종 폴리펩티드의 표적화 분해를 위한 화합물 및 방법 |
| 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 |
| CA3049912A1 (en) | 2017-01-26 | 2018-08-02 | Arvinas Operations, Inc. | Modulators of estrogen receptor proteolysis and associated methods of use |
| CA3078155A1 (en) | 2017-10-19 | 2019-04-25 | Debiopharm International S.A. | Combination product for the treatment of cancer |
| 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 |
| US11028088B2 (en) | 2018-03-10 | 2021-06-08 | Yale University | Modulators of BTK proteolysis and methods of use |
| BR112020020307A2 (pt) | 2018-04-04 | 2021-01-12 | Arvinas Operations, Inc. | Moduladores de proteólise e métodos de uso associados |
| WO2020023851A1 (en) | 2018-07-26 | 2020-01-30 | Yale University | Bifunctional substitued pyrimidines as modulators of fak proteolyse |
| WO2020027225A1 (ja) | 2018-07-31 | 2020-02-06 | ファイメクス株式会社 | 複素環化合物 |
| 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 |
| IL281188B2 (en) | 2018-09-07 | 2025-08-01 | Arvinas Operations Inc | Polycyclic compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides |
| US20210361774A1 (en) | 2018-10-16 | 2021-11-25 | Dana-Farber Cancer Institute, Inc. | Degraders of wild-type and mutant forms of lrrk2 |
| 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 |
| US10870663B2 (en) | 2018-11-30 | 2020-12-22 | Glaxosmithkline Intellectual Property Development Limited | Compounds useful in HIV therapy |
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| 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. |
| WO2024022275A1 (zh) * | 2022-07-29 | 2024-02-01 | 苏州科睿思制药有限公司 | Xevinapant的晶型及其制备方法和用途 |
| EP4584258A1 (en) | 2022-09-07 | 2025-07-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use |
| CN118027138A (zh) * | 2022-11-07 | 2024-05-14 | 南京中澳转化医学研究院有限公司 | 吡啶酮类化合物及其制备方法、药物组合物和应用 |
| AR131299A1 (es) * | 2022-12-09 | 2025-03-05 | Debiopharm Int Sa | Nuevos inhibidores de iap, métodos para fabricarlos y usos de los mismos |
| AU2024212035A1 (en) | 2023-01-26 | 2025-08-14 | Arvinas Operations, Inc. | Cereblon-based kras degrading protacs ans uses related thereto |
| WO2024240858A1 (en) | 2023-05-23 | 2024-11-28 | Valerio Therapeutics | Protac molecules directed against dna damage repair system and uses thereof |
| WO2026006700A1 (en) * | 2024-06-28 | 2026-01-02 | Regents Of The University Of Michigan | Pyrrolo[1,2-a]-azocine analogues as iap antagonists |
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| US7932382B2 (en) * | 2004-01-16 | 2011-04-26 | The Regents Of The University Of Michigan | Conformationally constrained Smac mimetics and the uses thereof |
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| US8202902B2 (en) * | 2006-05-05 | 2012-06-19 | The Regents Of The University Of Michigan | Bivalent SMAC mimetics and the uses thereof |
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| US8445473B2 (en) * | 2008-04-11 | 2013-05-21 | The Regents Of The University Of Michigan | Heteroaryl-substituted bicyclic Smac mimetics and the uses thereof |
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-
2008
- 2008-04-14 EP EP08745750.3A patent/EP2139490B1/en active Active
- 2008-04-14 SI SI200831285T patent/SI2139490T1/sl unknown
- 2008-04-14 MX MX2009011069A patent/MX2009011069A/es active IP Right Grant
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