JP2010523722A5 - - Google Patents
Download PDFInfo
- Publication number
- 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
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- compound
- group
- trail
- apoptosis
- 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
- 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 (en:Method) | 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 (en:Method) |
| EP (1) | EP2139490B1 (en:Method) |
| JP (1) | JP5416089B2 (en:Method) |
| KR (1) | KR101081685B1 (en:Method) |
| CN (1) | CN101686981B (en:Method) |
| AU (1) | AU2008240119B2 (en:Method) |
| BR (1) | BRPI0810522B8 (en:Method) |
| CA (1) | CA2683318C (en:Method) |
| CY (1) | CY1115735T1 (en:Method) |
| DK (1) | DK2139490T3 (en:Method) |
| EA (1) | EA017797B1 (en:Method) |
| ES (1) | ES2504216T3 (en:Method) |
| HR (1) | HRP20140885T1 (en:Method) |
| HU (1) | HUE024142T2 (en:Method) |
| IL (1) | IL201474A (en:Method) |
| MX (1) | MX2009011069A (en:Method) |
| NZ (1) | NZ580468A (en:Method) |
| PL (1) | PL2139490T3 (en:Method) |
| PT (1) | PT2139490E (en:Method) |
| SI (1) | SI2139490T1 (en:Method) |
| WO (1) | WO2008128171A2 (en:Method) |
| ZA (1) | ZA200907055B (en:Method) |
Families Citing this family (64)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| RU2418807C2 (ru) | 2005-10-25 | 2011-05-20 | Аегера Терапьютикс Инк. | Соединения, связывающие bir домены iap |
| TWI543988B (zh) | 2006-03-16 | 2016-08-01 | 科學製藥股份有限公司 | 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 |
| US9527915B2 (en) | 2009-11-05 | 2016-12-27 | The Uab Research Foundation | Treating basal-like genotype cancers |
| KR20120140658A (ko) | 2010-02-12 | 2012-12-31 | 파마사이언스 인크. | Ｉａｐ ｂｉｒ 도메인 결합 화합물 |
| 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 |
| HK1211030A1 (en) * | 2012-08-23 | 2016-05-13 | The Regents Of The University Of Michigan | Bivalent inhibitors of iap proteins and therapeutic methods using the same |
| CA2896577C (en) | 2012-11-30 | 2024-01-23 | Sanford-Burnham Medical Research Institute | Inhibitor of apoptosis protein (iap) antagonists |
| 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 |
| CA2920466C (en) | 2013-09-09 | 2018-10-02 | Halliburton Energy Services, Inc. | Activation of set-delayed cement compositions by retarder exchange |
| 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 |
| KR20230119040A (ko) | 2015-01-20 | 2023-08-14 | 아비나스 오퍼레이션스, 인코포레이티드 | 안드로겐 수용체의 표적화된 분해를 위한 화합물 및방법 |
| US12312316B2 (en) | 2015-01-20 | 2025-05-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| 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 |
| EP3302482A4 (en) | 2015-06-05 | 2018-12-19 | Arvinas, Inc. | Tank-binding kinase-1 protacs 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 |
| CN109311867A (zh) | 2016-04-20 | 2019-02-05 | 葛兰素史克知识产权开发有限公司 | 包含ripk2抑制剂的共轭物 |
| GB201610147D0 (en) | 2016-06-10 | 2016-07-27 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| EP3535265A4 (en) | 2016-11-01 | 2020-07-08 | Arvinas, Inc. | PROTACS TARGETING ON TAU PROTEIN AND RELATED METHODS FOR USE |
| HUE064609T2 (hu) | 2016-12-01 | 2024-04-28 | Arvinas Operations Inc | Tetrahidronaftalin és tetrahidroizokinolin származékok mint ösztrogénreceptor-lebontó anyagok |
| EP3559002A4 (en) | 2016-12-23 | 2021-02-17 | Arvinas Operations, Inc. | CHEMERICAL MOLECULES TARGETING EGFR PROTEOLYSIS AND RELATED METHODS OF USE |
| US10723717B2 (en) | 2016-12-23 | 2020-07-28 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | 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 |
| 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 |
| BR112020007046A2 (pt) | 2017-10-19 | 2020-11-17 | Debiopharm International S.A. | produto de combinação para o tratamento do câncer |
| 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 |
| WO2019177902A1 (en) | 2018-03-10 | 2019-09-19 | Yale University | Modulators of btk proteolysis and methods of use |
| CN112218859B (zh) | 2018-04-04 | 2024-10-29 | 阿尔维纳斯运营股份有限公司 | 蛋白水解调节剂及相关使用方法 |
| WO2020023851A1 (en) | 2018-07-26 | 2020-01-30 | Yale University | Bifunctional substitued pyrimidines as modulators of fak proteolyse |
| CN112533898A (zh) | 2018-07-31 | 2021-03-19 | 日商泛美克斯股份有限公司 | 杂环化合物 |
| US11707452B2 (en) | 2018-08-20 | 2023-07-25 | Arvinas Operations, Inc. | Modulators of alpha-synuclein proteolysis and associated methods of use |
| CN113164775B (zh) | 2018-09-07 | 2025-03-18 | 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多环化合物和方法 |
| CN112888460A (zh) | 2018-10-16 | 2021-06-01 | 达纳-法伯癌症研究所有限公司 | Lrkk2的野生型及突变型的降解剂 |
| JP2022511437A (ja) | 2018-11-26 | 2022-01-31 | デバイオファーム インターナショナル エス．エー． | Ｈｉｖ感染の組み合わせ治療 |
| US10870663B2 (en) | 2018-11-30 | 2020-12-22 | Glaxosmithkline Intellectual Property Development Limited | Compounds useful in HIV therapy |
| JP7504106B2 (ja) | 2019-01-17 | 2024-06-21 | デビオファーム・インターナショナル・エス・アー | がんの処置のための組合せ物 |
| WO2020206137A1 (en) | 2019-04-04 | 2020-10-08 | Dana-Farber Cancer Institute, Inc. | Cdk2/5 degraders and uses thereof |
| 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 |
| EP3999182A1 (en) | 2019-07-17 | 2022-05-25 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated methods of use |
| JP7764027B2 (ja) | 2019-07-31 | 2025-11-05 | ファイメクス株式会社 | 複素環化合物 |
| BR112022003490A2 (pt) | 2019-08-26 | 2022-05-24 | Arvinas Operations Inc | Método de tratamento do câncer de mama e mama metastático, método para degradação seletiva, método para inibir uma quinase, kit, composição líquida, e, método de produção de uma composição líquida |
| MX2022003628A (es) * | 2019-09-25 | 2022-07-21 | Debiopharm Int Sa | Regímenes de dosificación para el tratamiento de pacientes con carcinoma de células escamosas avanzado localmente. |
| MX2022008874A (es) * | 2020-01-20 | 2022-08-11 | Astrazeneca Ab | Inhibidores de la tirosina cinasa del receptor del factor de creciminto epidermico para el tratamiento del cancer. |
| 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 |
| IL301155A (en) | 2020-09-14 | 2023-05-01 | Arvinas Operations Inc | Crystalline forms of a compound for the targeted degradation of estrogen receptor |
| US11814367B2 (en) | 2021-03-15 | 2023-11-14 | Maze Therapeutics, Inc. | Inhibitors of glycogen synthase 1 (GYS1) and methods of use thereof |
| 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 |
| US11957759B1 (en) | 2022-09-07 | 2024-04-16 | 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 |
| WO2024159164A2 (en) | 2023-01-26 | 2024-08-02 | 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 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3989816A (en) | 1975-06-19 | 1976-11-02 | Nelson Research & Development Company | Vehicle composition containing 1-substituted azacycloheptan-2-ones |
| US4444762A (en) | 1980-04-04 | 1984-04-24 | Nelson Research & Development Company | Vehicle composition containing 1-substituted azacyclopentan-2-ones |
| CA2462200A1 (en) * | 2001-08-10 | 2003-02-20 | Palatin Technologies, Inc. | Peptidomimetics of biologically active metallopeptides |
| CN1960728A (zh) * | 2004-01-16 | 2007-05-09 | 密歇根大学董事会 | 构象受限的smac模拟物及其应用 |
| WO2006010119A2 (en) | 2004-07-09 | 2006-01-26 | Michael Norris | Cargo retaining device for use in vehicle cargo storage areas |
| US7674787B2 (en) * | 2004-07-09 | 2010-03-09 | The Regents Of The University Of Michigan | Conformationally constrained Smac mimetics and the uses thereof |
| US8202902B2 (en) * | 2006-05-05 | 2012-06-19 | The Regents Of The University Of Michigan | Bivalent SMAC mimetics and the uses thereof |
| HRP20141253T1 (en) * | 2006-05-05 | 2015-03-13 | The Regents Of The Universitiy Of Michigan | Intermediates for the preparation of bivalent smac mimetics |
| EP2139490B1 (en) * | 2007-04-13 | 2014-07-02 | The Regents of the University of Michigan | Diazo bicyclic smac mimetics and the uses thereof |
| CA2725398A1 (en) * | 2008-04-11 | 2009-10-15 | The Regents Of The University Of Michigan | Heteroaryl-substituted bicyclic smac mimetics and the uses thereof |
| US8625740B2 (en) * | 2011-04-14 | 2014-01-07 | Morpho Detection, Inc. | System and method for correcting X-ray diffraction profiles |
-
2008
- 2008-04-14 EP EP08745750.3A patent/EP2139490B1/en active Active
- 2008-04-14 WO PCT/US2008/060215 patent/WO2008128171A2/en not_active Ceased
- 2008-04-14 ES ES08745750.3T patent/ES2504216T3/es active Active
- 2008-04-14 HU HUE08745750A patent/HUE024142T2/en unknown
- 2008-04-14 DK DK08745750.3T patent/DK2139490T3/da active
- 2008-04-14 AU AU2008240119A patent/AU2008240119B2/en not_active Ceased
- 2008-04-14 KR KR1020097023384A patent/KR101081685B1/ko active Active
- 2008-04-14 EA EA200901400A patent/EA017797B1/ru unknown
- 2008-04-14 MX MX2009011069A patent/MX2009011069A/es active IP Right Grant
- 2008-04-14 CA CA2683318A patent/CA2683318C/en active Active
- 2008-04-14 CN CN2008800186484A patent/CN101686981B/zh active Active
- 2008-04-14 PL PL08745750T patent/PL2139490T3/pl unknown
- 2008-04-14 US US12/159,249 patent/US8278293B2/en active Active
- 2008-04-14 BR BRPI0810522A patent/BRPI0810522B8/pt not_active IP Right Cessation
- 2008-04-14 JP JP2010503269A patent/JP5416089B2/ja active Active
- 2008-04-14 NZ NZ580468A patent/NZ580468A/en not_active IP Right Cessation
- 2008-04-14 PT PT87457503T patent/PT2139490E/pt unknown
- 2008-04-14 HR HRP20140885AT patent/HRP20140885T1/hr unknown
- 2008-04-14 SI SI200831285T patent/SI2139490T1/sl unknown
-
2009
- 2009-10-09 ZA ZA2009/07055A patent/ZA200907055B/en unknown
- 2009-10-12 IL IL201474A patent/IL201474A/en active IP Right Grant
-
2012
- 2012-07-25 US US13/557,804 patent/US8664212B2/en active Active
-
2014
- 2014-09-29 CY CY20141100792T patent/CY1115735T1/el unknown
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2010523722A5 (en:Method) | ||
| CA2683318A1 (en) | Diazo bicyclic smac mimetics and the uses thereof | |
| EP1838320B1 (en) | Cxcr4 antagonists for the treatment of medical disorders | |
| US7026491B2 (en) | Coumarin derivatives useful as TNFα inhibitors | |
| JP2012504133A5 (en:Method) | ||
| RU2014110623A (ru) | Пирролопиразиновые ингибиторы киназы | |
| TW201818937A (zh) | 治療癌症之方法 | |
| JP2020506951A5 (en:Method) | ||
| JP2011509259A5 (en:Method) | ||
| KR102598246B1 (ko) | Jak 저해제로서 헤테로사이클릭 화합물, 및 이의 염 및 치료학적 용도 | |
| CA2854836C (en) | Tricyclic amino containing compounds for treatment or prevention of symptoms associated with endocrine dysfunction | |
| JP2011500638A5 (en:Method) | ||
| CN1312810A (zh) | 作为磷酸二酯酶4抑制剂的取代1,8－二氮杂萘－4(1h)－酮类化合物 | |
| JP2020517598A5 (en:Method) | ||
| RU2014100744A (ru) | Лечение респираторных нарушений с помощью trpa1 антагонистов | |
| RU2671195C2 (ru) | СПОСОБ ПОЛУЧЕНИЯ АРОМАТИЧЕСКОГО ГЕТЕРОЦИКЛИЧЕСКОГО СОЕДИНЕНИЯ, ПРИМЕНЯЕМОГО В КАЧЕСТВЕ СЕЛЕКТИВНОГО ИНГИБИТОРА КИНАЗ JAK3 и/или JAK1, И ПРИМЕНЕНИЕ АРОМАТИЧЕСКОГО ГЕТЕРОЦИКЛИЧЕСКОГО СОЕДИНЕНИЯ | |
| JP7768880B2 (ja) | Ｅｚｈ２を阻害するためのキノリン化合物および組成物 | |
| WO2012047630A2 (en) | N-alkyl or n-aryl substituted guanide and biguanide compounds and methods of their use | |
| CA2505874A1 (en) | Ccr1 antagonists for the treatment of i.a. demyelinating inflammatory disease | |
| JP2010540649A5 (en:Method) | ||
| KR20240012513A (ko) | 세스퀴테르펜 유도체, 그의 약학적 조성물 및 그의 제조 방법과 용도 | |
| JP2004536079A5 (en:Method) | ||
| JP6982716B2 (ja) | 複素環式化合物及びその使用 | |
| JP2006522039A5 (en:Method) | ||
| CN1838951A (zh) | 作为人类orl1受体激动剂的双环[3.1.1]庚烷取代的苯并咪唑酮和喹唑啉酮衍生物 |