MX378282B - Forma cristalina del inhibidor del receptor androgenico y metodo de preparacion de la misma. - Google Patents
Forma cristalina del inhibidor del receptor androgenico y metodo de preparacion de la misma.Info
- Publication number
- MX378282B MX378282B MX2018002759A MX2018002759A MX378282B MX 378282 B MX378282 B MX 378282B MX 2018002759 A MX2018002759 A MX 2018002759A MX 2018002759 A MX2018002759 A MX 2018002759A MX 378282 B MX378282 B MX 378282B
- Authority
- MX
- Mexico
- Prior art keywords
- crystal
- compound
- formula
- androgen receptor
- receptor inhibitor
- Prior art date
Links
- 102000001307 androgen receptors Human genes 0.000 title abstract 2
- 108010080146 androgen receptors Proteins 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 239000013078 crystal Substances 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 3
- 239000003960 organic solvent Substances 0.000 abstract 2
- 238000002360 preparation method Methods 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 238000002425 crystallisation Methods 0.000 abstract 1
- 230000008025 crystallization Effects 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 150000002170 ethers Chemical class 0.000 abstract 1
- 150000002576 ketones Chemical class 0.000 abstract 1
- 231100000053 low toxicity Toxicity 0.000 abstract 1
- 239000012046 mixed solvent Substances 0.000 abstract 1
- 150000002825 nitriles Chemical class 0.000 abstract 1
- 239000002904 solvent Substances 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
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
Se proporcionan una forma cristalina de un inhibidor del receptor androgénico, y un método de preparación de la misma. En términos particulares, se proporcionan un cristal tipo I de (S)-4-(3-(4-(2,3-dihidroxipropoxi)fenil)-4,4-dimetil-5-carbonil-2-tioimidazolin-1-il)-2-(trifluorometil)benzonitrilo (un compuesto de la fórmula (I)) y un método de preparación del mismo, en donde el método comprende: 1) se agrega cualquier forma cristalina o forma amorfa del compuesto como se muestra por la fórmula (I), a una cantidad adecuada de un solvente orgánico, se calienta y se disuelve hasta que esté transparente, seguido por enfriamiento y cristalización, en donde el solvente orgánico se selecciona a partir de cualquiera de ésteres, cetonas, nitrilos y éteres que tienen 5 o menos átomos de carbono, o un solvente mixto del mismo; y 2) el cristal se filtra, lava y seca. El cristal tipo I obtenido del compuesto de la fórmula (I) tiene una buena estabilidad química y estabilidad de su forma cristalina, y el solvente de cristalización utilizado tiene una baja toxicidad y poca formación de residuos, y se puede utilizar mejor en tratamientos clínicos.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510574141 | 2015-09-10 | ||
| CN201610073458 | 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 (2)
| Publication Number | Publication Date |
|---|---|
| MX2018002759A MX2018002759A (es) | 2018-08-01 |
| MX378282B true MX378282B (es) | 2025-03-10 |
Family
ID=58240573
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2018002759A MX378282B (es) | 2015-09-10 | 2016-08-23 | Forma cristalina del inhibidor del receptor androgenico y metodo de preparacion de la misma. |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US10150739B2 (es) |
| EP (1) | EP3348546B1 (es) |
| JP (1) | JP6843116B2 (es) |
| KR (1) | KR20180048939A (es) |
| CN (1) | CN107001284B (es) |
| AU (1) | AU2016318700B2 (es) |
| BR (1) | BR112018003258A2 (es) |
| CA (1) | CA2996674A1 (es) |
| CY (1) | CY1123027T1 (es) |
| DK (1) | DK3348546T3 (es) |
| ES (1) | ES2794568T3 (es) |
| HR (1) | HRP20200852T1 (es) |
| HU (1) | HUE050459T2 (es) |
| LT (1) | LT3348546T (es) |
| MX (1) | MX378282B (es) |
| PL (1) | PL3348546T3 (es) |
| PT (1) | PT3348546T (es) |
| RS (1) | RS60448B1 (es) |
| RU (1) | RU2018109121A (es) |
| SI (1) | SI3348546T1 (es) |
| SM (1) | SMT202000258T1 (es) |
| TW (1) | TWI708764B (es) |
| WO (1) | WO2017041622A1 (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10150739B2 (en) | 2015-09-10 | 2018-12-11 | Jiangsu Hengrui Medicine Co., Ltd. | Crystalline form of androgen receptor inhibitor and preparation method thereof |
| 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 |
|---|---|---|---|---|
| AU2005280908A1 (en) | 2004-09-09 | 2006-03-16 | Chugai Seiyaku Kabushiki Kaisha | Novel imidazolidine derivative and use thereof |
| EP3106162A1 (en) * | 2005-05-13 | 2016-12-21 | The Regents of the University of California | Diarylhydantoin compounds as androgen receptor antagonists for treatment of cancer |
| 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 |
| JP6262733B2 (ja) | 2012-09-04 | 2018-01-17 | シャンハイ ヘンルイ ファーマスーティカル カンパニー リミテッドＳｈａｎｇｈａｉ Ｈｅｎｇｒｕｉ Ｐｈａｒｍａｃｅｕｔｉｃａｌ Ｃｏ．， Ｌｔｄ． | イミダゾリン誘導体、その製造法、およびそれらの医薬への適用 |
| BR112015005404A2 (pt) * | 2012-09-11 | 2017-08-22 | Dr Reddys Laboratories Ltd | Formas polimórficas de enzalutamida e sua preparação |
| 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 |
| US10150739B2 (en) | 2015-09-10 | 2018-12-11 | Jiangsu Hengrui Medicine Co., Ltd. | Crystalline form of androgen receptor inhibitor and preparation method thereof |
-
2016
- 2016-08-23 US US15/757,652 patent/US10150739B2/en active Active
- 2016-08-23 SI SI201630801T patent/SI3348546T1/sl unknown
- 2016-08-23 RU RU2018109121A patent/RU2018109121A/ru unknown
- 2016-08-23 DK DK16843560.0T patent/DK3348546T3/da active
- 2016-08-23 WO PCT/CN2016/096381 patent/WO2017041622A1/zh not_active Ceased
- 2016-08-23 PL PL16843560T patent/PL3348546T3/pl unknown
- 2016-08-23 JP JP2018508712A patent/JP6843116B2/ja not_active Expired - Fee Related
- 2016-08-23 SM SM20200258T patent/SMT202000258T1/it unknown
- 2016-08-23 KR KR1020187009184A patent/KR20180048939A/ko not_active Ceased
- 2016-08-23 AU AU2016318700A patent/AU2016318700B2/en not_active Ceased
- 2016-08-23 CA CA2996674A patent/CA2996674A1/en active Pending
- 2016-08-23 BR BR112018003258-1A patent/BR112018003258A2/pt not_active Application Discontinuation
- 2016-08-23 HR HRP20200852TT patent/HRP20200852T1/hr unknown
- 2016-08-23 EP EP16843560.0A patent/EP3348546B1/en active Active
- 2016-08-23 RS RS20200617A patent/RS60448B1/sr unknown
- 2016-08-23 PT PT168435600T patent/PT3348546T/pt unknown
- 2016-08-23 CN CN201680003850.4A patent/CN107001284B/zh active Active
- 2016-08-23 ES ES16843560T patent/ES2794568T3/es active Active
- 2016-08-23 LT LTEP16843560.0T patent/LT3348546T/lt unknown
- 2016-08-23 MX MX2018002759A patent/MX378282B/es unknown
- 2016-08-23 HU HUE16843560A patent/HUE050459T2/hu unknown
- 2016-09-07 TW TW105128891A patent/TWI708764B/zh not_active IP Right Cessation
-
2020
- 2020-06-09 CY CY20201100522T patent/CY1123027T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP3348546A1 (en) | 2018-07-18 |
| AU2016318700A1 (en) | 2018-04-05 |
| CY1123027T1 (el) | 2021-10-29 |
| CA2996674A1 (en) | 2017-03-16 |
| US10150739B2 (en) | 2018-12-11 |
| PL3348546T3 (pl) | 2020-09-21 |
| JP2018526364A (ja) | 2018-09-13 |
| LT3348546T (lt) | 2020-07-27 |
| DK3348546T3 (da) | 2020-07-06 |
| KR20180048939A (ko) | 2018-05-10 |
| TWI708764B (zh) | 2020-11-01 |
| EP3348546B1 (en) | 2020-04-29 |
| HUE050459T2 (hu) | 2020-12-28 |
| CN107001284B (zh) | 2019-11-22 |
| SMT202000258T1 (it) | 2020-07-08 |
| RS60448B1 (sr) | 2020-07-31 |
| ES2794568T3 (es) | 2020-11-18 |
| CN107001284A (zh) | 2017-08-01 |
| HRP20200852T1 (hr) | 2020-08-21 |
| WO2017041622A1 (zh) | 2017-03-16 |
| SI3348546T1 (sl) | 2020-09-30 |
| PT3348546T (pt) | 2020-05-29 |
| AU2016318700B2 (en) | 2020-05-07 |
| TW201713628A (zh) | 2017-04-16 |
| MX2018002759A (es) | 2018-08-01 |
| US20180244628A1 (en) | 2018-08-30 |
| EP3348546A4 (en) | 2019-03-27 |
| JP6843116B2 (ja) | 2021-03-17 |
| RU2018109121A (ru) | 2019-10-10 |
| RU2018109121A3 (es) | 2019-12-04 |
| BR112018003258A2 (pt) | 2018-09-25 |
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