BR112018003258A2 - forma cristalina de inibidor de receptor de androgênio e método de preparação do mesmo - Google Patents
forma cristalina de inibidor de receptor de androgênio e método de preparação do mesmoInfo
- Publication number
- BR112018003258A2 BR112018003258A2 BR112018003258-1A BR112018003258A BR112018003258A2 BR 112018003258 A2 BR112018003258 A2 BR 112018003258A2 BR 112018003258 A BR112018003258 A BR 112018003258A BR 112018003258 A2 BR112018003258 A2 BR 112018003258A2
- Authority
- BR
- Brazil
- Prior art keywords
- crystal
- compound
- formula
- receptor inhibitor
- crystalline form
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D233/86—Oxygen and sulfur atoms, e.g. thiohydantoin
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
é fornecida uma forma cristalina de um inibidor de receptor de androgênio e um método de preparação da mesma. em particular, é fornecido o cristal do tipo i de (s)-4-(3-(4-(2,3-di-hidróxipropóxi)fenil)-4,4-dimetil-5-carbonil-2-tioimidazolin-1-il)-2-(trifluorometil)benzonitrila (um composto de fórmula (i)) e um método de preparação do mesmo, em que o método compreende: 1) qualquer forma cristalina ou forma amorfa do composto como mostrado pela fórmula (i) é adicionada a uma quantidade apropriada de um solvente orgânico, aquecido e dis-solvido até que fique transparente, após isso é esfriado e cristalizado, em que o solvente orgânico é selecionado de qualquer um de ésteres, cetonas, nitrilas e éteres que possuem 5 ou menos átomos de carbo-no, ou um solvente misturado dos mesmos; e 2) o cristal é filtrado, la-vado e secado. o cristal do tipo i obtido do composto de fórmula (i) possui uma boa estabilidade química e estabilidade da forma de cris-tal, e o solvente de cristalização utilizado possui baixa toxicidade e re-síduo, e pode ser melhor utilizado para tratamento clínico.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510574141 | 2015-09-10 | ||
| CN201510574141.9 | 2015-09-10 | ||
| CN201610073458 | 2016-02-02 | ||
| CN201610073458.9 | 2016-02-02 | ||
| PCT/CN2016/096381 WO2017041622A1 (zh) | 2015-09-10 | 2016-08-23 | 一种雄性激素受体抑制剂的结晶形式及其制备方法 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112018003258A2 true BR112018003258A2 (pt) | 2018-09-25 |
Family
ID=58240573
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112018003258-1A BR112018003258A2 (pt) | 2015-09-10 | 2016-08-23 | forma cristalina de inibidor de receptor de androgênio e método de preparação do mesmo |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US10150739B2 (pt) |
| EP (1) | EP3348546B1 (pt) |
| JP (1) | JP6843116B2 (pt) |
| KR (1) | KR20180048939A (pt) |
| CN (1) | CN107001284B (pt) |
| AU (1) | AU2016318700B2 (pt) |
| BR (1) | BR112018003258A2 (pt) |
| CA (1) | CA2996674A1 (pt) |
| CY (1) | CY1123027T1 (pt) |
| DK (1) | DK3348546T3 (pt) |
| ES (1) | ES2794568T3 (pt) |
| HR (1) | HRP20200852T1 (pt) |
| HU (1) | HUE050459T2 (pt) |
| LT (1) | LT3348546T (pt) |
| MX (1) | MX2018002759A (pt) |
| PL (1) | PL3348546T3 (pt) |
| PT (1) | PT3348546T (pt) |
| RS (1) | RS60448B1 (pt) |
| RU (1) | RU2018109121A (pt) |
| SI (1) | SI3348546T1 (pt) |
| TW (1) | TWI708764B (pt) |
| WO (1) | WO2017041622A1 (pt) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107001284B (zh) | 2015-09-10 | 2019-11-22 | 江苏恒瑞医药股份有限公司 | 一种雄性激素受体抑制剂的结晶形式及其制备方法 |
| CN112300076B (zh) * | 2017-12-13 | 2022-10-25 | 江苏恒瑞医药股份有限公司 | 一种雄性激素受体抑制剂的晶型及其制备方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006028226A1 (ja) * | 2004-09-09 | 2006-03-16 | Chugai Seiyaku Kabushiki Kaisha | 新規イミダゾリジン誘導体およびその用途 |
| PT2444085E (pt) | 2005-05-13 | 2015-06-11 | Univ California | Compostos de diaril-hidantoínas como antagonistas do recetor androgénio para tratamento de cancro |
| EP2416657A4 (en) * | 2009-04-09 | 2012-09-05 | Medivation Prostate Therapeutics Inc | COMPOUNDS COMPRISING SUBSTITUTED DI-ARYLHYDANTOIDS AND DI-ARYLTHIOHYDANTOINES AND METHODS OF USE THEREOF |
| DK2894151T3 (da) * | 2012-09-04 | 2021-01-11 | Shanghai hengrui pharmaceutical co ltd | Imidazolinderivater, fremgangsmåder til fremstilling deraf og anvendelse deraf i medicin |
| CA2884640A1 (en) * | 2012-09-11 | 2014-03-20 | Dr. Reddy's Laboratories Limited | Enzalutamide polymorphic forms and its preparation |
| CN104356068A (zh) * | 2014-10-30 | 2015-02-18 | 杭州新博思生物医药有限公司 | 恩杂鲁胺新晶型及其制备方法 |
| CN107001284B (zh) | 2015-09-10 | 2019-11-22 | 江苏恒瑞医药股份有限公司 | 一种雄性激素受体抑制剂的结晶形式及其制备方法 |
-
2016
- 2016-08-23 CN CN201680003850.4A patent/CN107001284B/zh active Active
- 2016-08-23 SI SI201630801T patent/SI3348546T1/sl unknown
- 2016-08-23 WO PCT/CN2016/096381 patent/WO2017041622A1/zh active Application Filing
- 2016-08-23 KR KR1020187009184A patent/KR20180048939A/ko not_active Application Discontinuation
- 2016-08-23 LT LTEP16843560.0T patent/LT3348546T/lt unknown
- 2016-08-23 CA CA2996674A patent/CA2996674A1/en active Pending
- 2016-08-23 JP JP2018508712A patent/JP6843116B2/ja active Active
- 2016-08-23 EP EP16843560.0A patent/EP3348546B1/en active Active
- 2016-08-23 PT PT168435600T patent/PT3348546T/pt unknown
- 2016-08-23 PL PL16843560T patent/PL3348546T3/pl unknown
- 2016-08-23 RS RS20200617A patent/RS60448B1/sr unknown
- 2016-08-23 MX MX2018002759A patent/MX2018002759A/es unknown
- 2016-08-23 ES ES16843560T patent/ES2794568T3/es active Active
- 2016-08-23 AU AU2016318700A patent/AU2016318700B2/en not_active Ceased
- 2016-08-23 US US15/757,652 patent/US10150739B2/en active Active
- 2016-08-23 RU RU2018109121A patent/RU2018109121A/ru unknown
- 2016-08-23 BR BR112018003258-1A patent/BR112018003258A2/pt not_active Application Discontinuation
- 2016-08-23 HU HUE16843560A patent/HUE050459T2/hu unknown
- 2016-08-23 DK DK16843560.0T patent/DK3348546T3/da active
- 2016-09-07 TW TW105128891A patent/TWI708764B/zh active
-
2020
- 2020-05-26 HR HRP20200852TT patent/HRP20200852T1/hr unknown
- 2020-06-09 CY CY20201100522T patent/CY1123027T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| RU2018109121A3 (pt) | 2019-12-04 |
| SI3348546T1 (sl) | 2020-09-30 |
| EP3348546A1 (en) | 2018-07-18 |
| RU2018109121A (ru) | 2019-10-10 |
| LT3348546T (lt) | 2020-07-27 |
| TW201713628A (zh) | 2017-04-16 |
| US20180244628A1 (en) | 2018-08-30 |
| JP2018526364A (ja) | 2018-09-13 |
| CA2996674A1 (en) | 2017-03-16 |
| US10150739B2 (en) | 2018-12-11 |
| KR20180048939A (ko) | 2018-05-10 |
| WO2017041622A1 (zh) | 2017-03-16 |
| PL3348546T3 (pl) | 2020-09-21 |
| PT3348546T (pt) | 2020-05-29 |
| MX2018002759A (es) | 2018-08-01 |
| HRP20200852T1 (hr) | 2020-08-21 |
| CY1123027T1 (el) | 2021-10-29 |
| TWI708764B (zh) | 2020-11-01 |
| CN107001284B (zh) | 2019-11-22 |
| ES2794568T3 (es) | 2020-11-18 |
| EP3348546A4 (en) | 2019-03-27 |
| AU2016318700A1 (en) | 2018-04-05 |
| DK3348546T3 (da) | 2020-07-06 |
| HUE050459T2 (hu) | 2020-12-28 |
| AU2016318700B2 (en) | 2020-05-07 |
| RS60448B1 (sr) | 2020-07-31 |
| CN107001284A (zh) | 2017-08-01 |
| JP6843116B2 (ja) | 2021-03-17 |
| EP3348546B1 (en) | 2020-04-29 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] |
Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS. |
|
| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] | ||
| B06U | Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette] | ||
| B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
| B09B | Patent application refused [chapter 9.2 patent gazette] |