CN104812757B - 二螺吡咯烷衍生物的晶体 - Google Patents
二螺吡咯烷衍生物的晶体 Download PDFInfo
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- CN104812757B CN104812757B CN201380057995.9A CN201380057995A CN104812757B CN 104812757 B CN104812757 B CN 104812757B CN 201380057995 A CN201380057995 A CN 201380057995A CN 104812757 B CN104812757 B CN 104812757B
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/10—Spiro-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2012-195761 | 2012-09-06 | ||
| JP2012195761 | 2012-09-06 | ||
| PCT/JP2013/073865 WO2014038606A1 (ja) | 2012-09-06 | 2013-09-05 | ジスピロピロリジン誘導体の結晶 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104812757A CN104812757A (zh) | 2015-07-29 |
| CN104812757B true CN104812757B (zh) | 2016-11-09 |
Family
ID=50237214
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380057995.9A Active CN104812757B (zh) | 2012-09-06 | 2013-09-05 | 二螺吡咯烷衍生物的晶体 |
Country Status (12)
| Country | Link |
|---|---|
| US (8) | US9359368B2 (enExample) |
| EP (1) | EP2894156B1 (enExample) |
| JP (1) | JP6016284B2 (enExample) |
| KR (1) | KR102217410B1 (enExample) |
| CN (1) | CN104812757B (enExample) |
| BR (1) | BR112015004816B1 (enExample) |
| CA (1) | CA2884238C (enExample) |
| ES (1) | ES2637150T3 (enExample) |
| IN (1) | IN2015MN00464A (enExample) |
| RU (1) | RU2647840C2 (enExample) |
| TW (1) | TWI586668B (enExample) |
| WO (1) | WO2014038606A1 (enExample) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI586668B (zh) | 2012-09-06 | 2017-06-11 | 第一三共股份有限公司 | 二螺吡咯啶衍生物之結晶 |
| BR112015013611A2 (pt) | 2012-12-20 | 2017-11-14 | Merck Sharp & Dohme | composto, e, composição farmacêutica |
| 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 |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| 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 |
| EP3260119B1 (en) | 2015-02-20 | 2023-11-15 | Daiichi Sankyo Company, Limited | Combination method for treating cancer |
| TWI697329B (zh) * | 2015-04-13 | 2020-07-01 | 日商第一三共股份有限公司 | 血液癌症治療用之醫藥及其用途 |
| 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 |
| WO2017069288A1 (en) | 2015-10-23 | 2017-04-27 | Daiichi Sankyo Company, Limited | Pharmaceutical composition for use in treating aml and method of treating aml in a subject in need thereof |
| CN113521069A (zh) * | 2015-10-23 | 2021-10-22 | 第一三共株式会社 | 用于治疗癌症的mdm2抑制剂的给药方案 |
| CN109152843A (zh) | 2016-05-20 | 2019-01-04 | 豪夫迈·罗氏有限公司 | Protac抗体缀合物及其使用方法 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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. |
| 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 |
| WO2023056069A1 (en) | 2021-09-30 | 2023-04-06 | Angiex, Inc. | Degrader-antibody conjugates and methods of using same |
| 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 |
| WO2024240858A1 (en) | 2023-05-23 | 2024-11-28 | Valerio Therapeutics | Protac molecules directed against dna damage repair system and uses thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006091646A2 (en) * | 2005-02-22 | 2006-08-31 | The Regents Of The University Of Michigan | Small molecule inhibitors of mdm2 and uses thereof |
| WO2012038307A1 (en) * | 2010-09-20 | 2012-03-29 | F. Hoffmann-La Roche Ag | Spiro substituted pyrrolo[1,2-c]imidazole derivatives useful as mdm2 inhibitors |
| CN103635473A (zh) * | 2011-03-10 | 2014-03-12 | 第一三共株式会社 | 二螺吡咯烷衍生物 |
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| US6740495B1 (en) | 2000-04-03 | 2004-05-25 | Rigel Pharmaceuticals, Inc. | Ubiquitin ligase assay |
| US6979551B2 (en) | 2000-04-03 | 2005-12-27 | Rigel Pharmaceuticals, Inc. | Assays for identifying ubiquitin agents and for identifying agents that modify the activity of ubiquitin agents |
| JP4361798B2 (ja) | 2001-12-18 | 2009-11-11 | エフ.ホフマン−ラ ロシュ アーゲー | Mdm2インヒビターとしてのシス−イミダゾリン |
| RU2305095C2 (ru) | 2001-12-18 | 2007-08-27 | Ф.Хоффманн-Ля Рош Аг | Цис-2,4,5-трифенилимидазолины и фармацевтическая композиция на их основе |
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| US7132421B2 (en) | 2003-06-17 | 2006-11-07 | Hoffmann-La Roche Inc. | CIS-imidazoles |
| CN1953965B (zh) | 2004-05-18 | 2012-07-04 | 霍夫曼-拉罗奇有限公司 | 新型顺式咪唑啉类化合物 |
| GB0419481D0 (en) | 2004-09-02 | 2004-10-06 | Cancer Rec Tech Ltd | Isoindolin-1-one derivatives |
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| US20070213341A1 (en) | 2006-03-13 | 2007-09-13 | Li Chen | Spiroindolinone derivatives |
| CA2661354C (en) | 2006-08-30 | 2012-12-18 | The Regents Of The University Of Michigan | New small molecule inhibitors of mdm2 and the uses thereof |
| JP2010504298A (ja) | 2006-09-21 | 2010-02-12 | エフ.ホフマン−ラ ロシュ アーゲー | オキシンドール誘導体 |
| US7638548B2 (en) | 2006-11-09 | 2009-12-29 | Hoffmann-La Roche Inc. | Spiroindolinone derivatives |
| AR065860A1 (es) | 2007-03-29 | 2009-07-08 | Novartis Ag | 3-imidazolil-indoles para el tratamiento de enfermedades proliferativas |
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| WO2012032466A1 (en) | 2010-09-08 | 2012-03-15 | Basf Se | Aqueous polishing compositions containing n-substituted diazenium dioxides and/or n'-hydroxy-diazenium oxide salts |
| US20120065210A1 (en) | 2010-09-15 | 2012-03-15 | Xin-Jie Chu | Substituted hexahydropyrrolo[1,2-c]imidazolones |
| WO2012076513A1 (en) | 2010-12-09 | 2012-06-14 | F. Hoffmann-La Roche Ag | 3-cyano-1-hydroxymethyl-2-phenylpyrrolidine derivatives as inhibitors of mdm2-p53 interactions useful for the treatment of cancer |
| SG194873A1 (en) * | 2011-05-11 | 2013-12-30 | Sanofi Sa | Spiro-oxindole mdm2 antagonists |
| TWI586668B (zh) | 2012-09-06 | 2017-06-11 | 第一三共股份有限公司 | 二螺吡咯啶衍生物之結晶 |
-
2013
- 2013-09-04 TW TW102131754A patent/TWI586668B/zh active
- 2013-09-05 WO PCT/JP2013/073865 patent/WO2014038606A1/ja not_active Ceased
- 2013-09-05 CA CA2884238A patent/CA2884238C/en active Active
- 2013-09-05 IN IN464MUN2015 patent/IN2015MN00464A/en unknown
- 2013-09-05 BR BR112015004816-1A patent/BR112015004816B1/pt active IP Right Grant
- 2013-09-05 EP EP13835941.9A patent/EP2894156B1/en active Active
- 2013-09-05 ES ES13835941.9T patent/ES2637150T3/es active Active
- 2013-09-05 JP JP2014534398A patent/JP6016284B2/ja active Active
- 2013-09-05 CN CN201380057995.9A patent/CN104812757B/zh active Active
- 2013-09-05 RU RU2015112098A patent/RU2647840C2/ru active
- 2013-09-05 US US14/426,630 patent/US9359368B2/en active Active
- 2013-09-05 KR KR1020157005386A patent/KR102217410B1/ko active Active
-
2016
- 2016-05-02 US US15/144,485 patent/US9540386B2/en active Active
- 2016-12-06 US US15/370,380 patent/US9718831B2/en active Active
- 2016-12-06 US US15/370,618 patent/US9745315B2/en active Active
- 2016-12-06 US US15/370,292 patent/US9718830B2/en active Active
- 2016-12-06 US US15/370,160 patent/US9884871B2/en active Active
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2018
- 2018-02-02 US US15/887,444 patent/US10023578B2/en active Active
- 2018-02-02 US US15/887,648 patent/US10030030B2/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006091646A2 (en) * | 2005-02-22 | 2006-08-31 | The Regents Of The University Of Michigan | Small molecule inhibitors of mdm2 and uses thereof |
| WO2012038307A1 (en) * | 2010-09-20 | 2012-03-29 | F. Hoffmann-La Roche Ag | Spiro substituted pyrrolo[1,2-c]imidazole derivatives useful as mdm2 inhibitors |
| CN103635473A (zh) * | 2011-03-10 | 2014-03-12 | 第一三共株式会社 | 二螺吡咯烷衍生物 |
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