CA2884238C - Crystals of dispiropyrrolidine derivatives - Google Patents
Crystals of dispiropyrrolidine derivatives Download PDFInfo
- Publication number
- CA2884238C CA2884238C CA2884238A CA2884238A CA2884238C CA 2884238 C CA2884238 C CA 2884238C CA 2884238 A CA2884238 A CA 2884238A CA 2884238 A CA2884238 A CA 2884238A CA 2884238 C CA2884238 C CA 2884238C
- Authority
- CA
- Canada
- Prior art keywords
- crystal
- ray powder
- powder diffraction
- diffraction pattern
- angstroms
- 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.)
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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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (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 |
|---|---|---|---|
| JP2012195761 | 2012-09-06 | ||
| JP2012-195761 | 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 |
|---|---|
| CA2884238A1 CA2884238A1 (en) | 2014-03-13 |
| CA2884238C true CA2884238C (en) | 2017-10-03 |
Family
ID=50237214
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2884238A Active CA2884238C (en) | 2012-09-06 | 2013-09-05 | Crystals of dispiropyrrolidine derivatives |
Country Status (12)
| Country | Link |
|---|---|
| US (8) | US9359368B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2894156B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP6016284B2 (cg-RX-API-DMAC7.html) |
| KR (1) | KR102217410B1 (cg-RX-API-DMAC7.html) |
| CN (1) | CN104812757B (cg-RX-API-DMAC7.html) |
| BR (1) | BR112015004816B1 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2884238C (cg-RX-API-DMAC7.html) |
| ES (1) | ES2637150T3 (cg-RX-API-DMAC7.html) |
| IN (1) | IN2015MN00464A (cg-RX-API-DMAC7.html) |
| RU (1) | RU2647840C2 (cg-RX-API-DMAC7.html) |
| TW (1) | TWI586668B (cg-RX-API-DMAC7.html) |
| WO (1) | WO2014038606A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
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| 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 |
| RU2690663C2 (ru) | 2012-12-20 | 2019-06-05 | Мерк Шарп И Доум Корп. | Замещенные имидазопиридины в качестве ингибиторов hdm2 |
| 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 |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| AU2016209349B2 (en) | 2015-01-20 | 2020-05-07 | Arvinas, Inc. | Compounds and methods for the targeted degradation of the Androgen Receptor |
| US12312316B2 (en) | 2015-01-20 | 2025-05-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| KR102595395B1 (ko) | 2015-02-20 | 2023-10-27 | 다이이찌 산쿄 가부시키가이샤 | 암의 병용 치료법 |
| EP3284466A4 (en) * | 2015-04-13 | 2018-12-05 | Daiichi Sankyo Company, Limited | Treatment method combining mdm2 inhibitor and btk inhibitor |
| US20180147202A1 (en) | 2015-06-05 | 2018-05-31 | 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 |
| EP3364972A1 (en) * | 2015-10-23 | 2018-08-29 | Daiichi Sankyo Company, Limited | Dosage regimen of mdm2 inhibitor for treating cancers |
| CN108135884A (zh) * | 2015-10-23 | 2018-06-08 | 第三共株式会社 | 用于治疗aml的药物组合物和治疗有此需要的对象中的aml的方法 |
| JP2019522633A (ja) | 2016-05-20 | 2019-08-15 | ジェネンテック, インコーポレイテッド | Protac抗体コンジュゲート及び使用方法 |
| IL290809B2 (en) | 2016-11-01 | 2024-01-01 | Arvinas Operations Inc | Tau-protein targeting protacs and associated methods of use |
| WO2018102725A1 (en) | 2016-12-01 | 2018-06-07 | Arvinas, Inc. | Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders |
| WO2018118598A1 (en) | 2016-12-23 | 2018-06-28 | Arvinas, Inc. | Compounds and methods for the targeted degradation of fetal liver kinase polypeptides |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| WO2018119448A1 (en) | 2016-12-23 | 2018-06-28 | Arvinas, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides |
| CA3047586A1 (en) | 2016-12-23 | 2018-06-28 | Arvinas Operations, Inc. | Egfr proteolysis targeting chimeric molecules and associated methods of use |
| 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 |
| EP3573977A4 (en) | 2017-01-26 | 2020-12-23 | Arvinas Operations, Inc. | Modulators of estrogen receptor proteolysis and associated methods of use |
| 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 |
| BR112020020307A2 (pt) | 2018-04-04 | 2021-01-12 | Arvinas Operations, Inc. | Moduladores de proteólise e métodos de uso associados |
| EP3841100A1 (en) | 2018-08-20 | 2021-06-30 | Arvinas Operations, Inc. | Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases |
| AU2020336309A1 (en) | 2019-08-26 | 2022-03-17 | Arvinas Operations, Inc. | Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders |
| 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 |
| TW202214236A (zh) | 2020-09-14 | 2022-04-16 | 美商亞文納營運公司 | 用於靶向降解雌激素受體之化合物之結晶及非晶形形式 |
| WO2023056069A1 (en) | 2021-09-30 | 2023-04-06 | Angiex, Inc. | Degrader-antibody conjugates and methods of using same |
| EP4584258A1 (en) | 2022-09-07 | 2025-07-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use |
| KR20250151412A (ko) | 2023-01-26 | 2025-10-21 | 아비나스 오퍼레이션스, 인코포레이티드 | 세레블론계 kras 분해 단백질 및 이와 관련된 용도 |
| WO2024240858A1 (en) | 2023-05-23 | 2024-11-28 | Valerio Therapeutics | Protac molecules directed against dna damage repair system and uses thereof |
Family Cites Families (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CA2469187C (en) | 2001-12-18 | 2012-07-17 | F. Hoffmann-La Roche Ag | Cis-2,4,5-triphenyl-imidazolines and their use in the treatment of tumors |
| US7132421B2 (en) | 2003-06-17 | 2006-11-07 | Hoffmann-La Roche Inc. | CIS-imidazoles |
| US7425638B2 (en) | 2003-06-17 | 2008-09-16 | Hoffmann-La Roche Inc. | Cis-imidazolines |
| 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 |
| EA014445B1 (ru) * | 2005-02-22 | 2010-12-30 | Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган | Низкомолекулярные ингибиторы mdm2 и их применения |
| US7576082B2 (en) | 2005-06-24 | 2009-08-18 | Hoffman-La Roche Inc. | Oxindole derivatives |
| AR059265A1 (es) * | 2006-02-07 | 2008-03-19 | Astrazeneca Ab | Compuestos espiro condensados con actividad inhibitoria en el receptor vaniloide1 (vr1) |
| US20070213341A1 (en) | 2006-03-13 | 2007-09-13 | Li Chen | Spiroindolinone derivatives |
| CA2644758A1 (en) | 2006-03-13 | 2007-09-20 | F. Hoffmann-La Roche Ag | Spiroindolinone derivatives |
| ZA200901224B (en) | 2006-08-30 | 2010-05-26 | Univ Michigan | New small molecule inhibitors of MDM2 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 |
| BRPI0810082A2 (pt) | 2007-03-29 | 2014-10-21 | Novartis Ag | 3-imidazolil-indóis para o tratamento de doenças proliferativas |
| US7553833B2 (en) | 2007-05-17 | 2009-06-30 | Hoffmann-La Roche Inc. | 3,3-spiroindolinone derivatives |
| US7834179B2 (en) | 2007-05-23 | 2010-11-16 | Hoffmann-La Roche Inc. | Spiroindolinone derivatives |
| US8134001B2 (en) | 2007-12-14 | 2012-03-13 | Hoffmann-La Roche Inc. | Spiroindolinone derivatives |
| US7776875B2 (en) | 2007-12-19 | 2010-08-17 | Hoffman-La Roche Inc. | Spiroindolinone derivatives |
| US7723372B2 (en) | 2008-03-19 | 2010-05-25 | Hoffman-La Roche Inc. | Spiroindolinone derivatives |
| AR073578A1 (es) | 2008-09-15 | 2010-11-17 | Priaxon Ag | Pirrolidin-2-onas |
| US8354444B2 (en) | 2008-09-18 | 2013-01-15 | Hoffmann-La Roche Inc. | Substituted pyrrolidine-2-carboxamides |
| RS52660B (sr) | 2008-09-18 | 2013-06-28 | F. Hoffmann-La Roche Ag | Supstituisani pirolidin-2-karboksamidi |
| JP5520236B2 (ja) | 2009-01-16 | 2014-06-11 | 第一三共株式会社 | プロリン環構造を有するイミダゾチアゾール誘導体 |
| US20100190814A1 (en) | 2009-01-26 | 2010-07-29 | Li Chen | Spiroindolinone derivative prodrugs |
| US7928233B2 (en) | 2009-02-10 | 2011-04-19 | Hoffmann-La Roche Inc. | Spiroindolinone pyridine derivatives |
| US8217051B2 (en) | 2009-02-17 | 2012-07-10 | Hoffmann-La Roche Inc. | Spiroindolinone derivatives |
| US8076482B2 (en) * | 2009-04-23 | 2011-12-13 | Hoffmann-La Roche Inc. | 3,3′-spiroindolinone derivatives |
| US8017607B2 (en) | 2009-10-14 | 2011-09-13 | Hoffmann-La Roche Inc. | N-substituted-pyrrolidines as inhibitors of MDM2-P-53 interactions |
| UA107814C2 (uk) | 2009-11-12 | 2015-02-25 | Дзе Ріджентс Оф Дзе Юніверсіті Оф Мічіган | Спірооксіндольні антагоністи мdм2 |
| US20110118283A1 (en) | 2009-11-17 | 2011-05-19 | Qingjie Ding | Substituted Pyrrolidine-2-Carboxamides |
| US8088815B2 (en) | 2009-12-02 | 2012-01-03 | Hoffman-La Roche Inc. | Spiroindolinone pyrrolidines |
| US8288431B2 (en) | 2010-02-17 | 2012-10-16 | Hoffmann-La Roche Inc. | Substituted spiroindolinones |
| KR20130050938A (ko) | 2010-04-09 | 2013-05-16 | 더 리젠츠 오브 더 유니버시티 오브 미시건 | 질환 치료시 사용하기 위한 mdm2 억제제에 대한 바이오마커 |
| US8217044B2 (en) | 2010-04-28 | 2012-07-10 | Hoffmann-La Roche Inc. | Spiroindolinone pyrrolidines |
| US20120010235A1 (en) | 2010-07-12 | 2012-01-12 | Xin-Jie Chu | N-substituted pyrrolidines |
| US20120046306A1 (en) | 2010-08-18 | 2012-02-23 | David Joseph Bartkovitz | Substituted Heteroaryl Spiropyrrolidine MDM2 Antagonists |
| US20130200039A1 (en) | 2010-09-08 | 2013-08-08 | 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 |
| US20120071499A1 (en) | 2010-09-20 | 2012-03-22 | Xin-Jie Chu | Substituted Spiro[3H-Indole-3,6'(5'H)-[1H]Pyrrolo[1,2c]Imidazole-1',2(1H,2'H)-diones |
| 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 |
| MY172862A (en) * | 2011-03-10 | 2019-12-13 | Daiichi Sankyo Co Ltd | Dispiropyrrolidine derivatives |
| CN103717605B (zh) * | 2011-05-11 | 2016-05-18 | 密执安州立大学董事会 | 螺-羟吲哚mdm2拮抗剂 |
| 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 BR BR112015004816-1A patent/BR112015004816B1/pt active IP Right Grant
- 2013-09-05 ES ES13835941.9T patent/ES2637150T3/es active Active
- 2013-09-05 JP JP2014534398A patent/JP6016284B2/ja active Active
- 2013-09-05 IN IN464MUN2015 patent/IN2015MN00464A/en unknown
- 2013-09-05 KR KR1020157005386A patent/KR102217410B1/ko active Active
- 2013-09-05 WO PCT/JP2013/073865 patent/WO2014038606A1/ja not_active Ceased
- 2013-09-05 EP EP13835941.9A patent/EP2894156B1/en 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 CA CA2884238A patent/CA2884238C/en active Active
- 2013-09-05 CN CN201380057995.9A patent/CN104812757B/zh active Active
-
2016
- 2016-05-02 US US15/144,485 patent/US9540386B2/en active Active
- 2016-12-06 US US15/370,160 patent/US9884871B2/en active Active
- 2016-12-06 US US15/370,292 patent/US9718830B2/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
-
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
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20150306 |