PE20200725A1 - Formas cristalinas del modulador receptor de androgeno: 4-[7-(6-ciano-5-trifluorometilpiridin-3-il)-8-oxo-6-tioxo-5,7-diazaespiro[3,4]oct-5-il]-2-fluoro-n-metilbenzamida) (apalutamida) - Google Patents
Formas cristalinas del modulador receptor de androgeno: 4-[7-(6-ciano-5-trifluorometilpiridin-3-il)-8-oxo-6-tioxo-5,7-diazaespiro[3,4]oct-5-il]-2-fluoro-n-metilbenzamida) (apalutamida)Info
- Publication number
- PE20200725A1 PE20200725A1 PE2019002096A PE2019002096A PE20200725A1 PE 20200725 A1 PE20200725 A1 PE 20200725A1 PE 2019002096 A PE2019002096 A PE 2019002096A PE 2019002096 A PE2019002096 A PE 2019002096A PE 20200725 A1 PE20200725 A1 PE 20200725A1
- Authority
- PE
- Peru
- Prior art keywords
- theta
- crystalline forms
- trifluoromethylpyridin
- methylbenzamide
- thioxo
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- 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
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- 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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/28—Antiandrogens
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Tropical Medicine & Parasitology (AREA)
- Urology & Nephrology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261656888P | 2012-06-07 | 2012-06-07 | |
| PCT/US2013/044116 WO2013184681A1 (en) | 2012-06-07 | 2013-06-04 | Crystalline forms of an androgen receptor modulator |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20200725A1 true PE20200725A1 (es) | 2020-07-21 |
Family
ID=49712550
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2019002096A PE20200725A1 (es) | 2012-06-07 | 2013-06-04 | Formas cristalinas del modulador receptor de androgeno: 4-[7-(6-ciano-5-trifluorometilpiridin-3-il)-8-oxo-6-tioxo-5,7-diazaespiro[3,4]oct-5-il]-2-fluoro-n-metilbenzamida) (apalutamida) |
| PE2014002383A PE20150631A1 (es) | 2012-06-07 | 2013-06-04 | Formas cristalinas de un modulador del receptor androgenico |
| PE2020000234A PE20200795A1 (es) | 2012-06-07 | 2013-06-04 | Composicion que comprende una forma cristalina del modulador receptor de androgeno: 4-[7-(6-ciano-5-trifluometilpiridin-3-il)-8-oxo-6-tioxo-5,7-diazaespiro [3.4]oct-5-il]-2-fluoro-n-metilbenzamida (apalutamida) |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2014002383A PE20150631A1 (es) | 2012-06-07 | 2013-06-04 | Formas cristalinas de un modulador del receptor androgenico |
| PE2020000234A PE20200795A1 (es) | 2012-06-07 | 2013-06-04 | Composicion que comprende una forma cristalina del modulador receptor de androgeno: 4-[7-(6-ciano-5-trifluometilpiridin-3-il)-8-oxo-6-tioxo-5,7-diazaespiro [3.4]oct-5-il]-2-fluoro-n-metilbenzamida (apalutamida) |
Country Status (45)
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008119015A2 (en) | 2007-03-27 | 2008-10-02 | Sloan-Kettering Institute For Cancer Research | Synthesis of thiohydantoins |
| PE20150099A1 (es) | 2011-12-16 | 2015-01-30 | Olema Pharmaceuticals Inc | Compuestos novedosos de benzopirano, composiciones y usos de los mismos |
| ES2809738T3 (es) | 2012-06-07 | 2021-03-05 | Aragon Pharmaceuticals Inc | Formas cristalinas de un modulador de receptor de andrógenos |
| WO2014043208A1 (en) | 2012-09-11 | 2014-03-20 | Medivation Prostate Therapeutics, Inc. | Formulations of enzalutamide |
| PT3305285T (pt) | 2012-09-26 | 2020-11-24 | Aragon Pharmaceuticals Inc | Antiandrogénios para o tratamento de cancro da próstata resistente à castração não metastático |
| JOP20200097A1 (ar) | 2013-01-15 | 2017-06-16 | Aragon Pharmaceuticals Inc | معدل مستقبل أندروجين واستخداماته |
| CN106795152B (zh) * | 2014-08-26 | 2020-01-31 | 安斯达尔生物技术有限责任公司 | 蛋白激酶抑制剂 |
| CR20170217A (es) | 2014-12-05 | 2017-08-30 | Aragon Pharmaceuticals Inc | Composiciones anticancerígenas |
| CA2969675C (en) | 2014-12-05 | 2023-06-06 | Aragon Pharmaceuticals, Inc. | Anticancer compositions |
| BR112017011788A2 (pt) | 2014-12-05 | 2017-12-26 | Aragon Pharmaceuticals Inc | composições anticâncer |
| WO2016100905A1 (en) | 2014-12-19 | 2016-06-23 | Lutron Electronics Co., Inc. | Multi-channel lighting fixture having multiple light-emitting diode drivers |
| TW201808287A (zh) | 2016-06-03 | 2018-03-16 | 美商艾瑞岡醫藥公司 | 抗癌組成物 |
| ES2952770T3 (es) | 2016-12-13 | 2023-11-06 | Watson Lab Inc | Formas de estado sólido de apalutamida |
| EP4438126A3 (en) | 2017-10-16 | 2025-01-01 | Aragon Pharmaceuticals, Inc. | Anti-androgens for the treatment of non-metastatic castration-resistant prostate cancer |
| WO2019135254A1 (en) | 2018-01-02 | 2019-07-11 | Mylan Laboratories Limited | Apalutamide polymorphs and their preparation thereof |
| WO2019242439A1 (zh) * | 2018-06-20 | 2019-12-26 | 苏州科睿思制药有限公司 | Arn-509的晶型及其制备方法和用途 |
| WO2020049598A2 (en) | 2018-09-08 | 2020-03-12 | Cipla Limited | Apalutamide polymorphs |
| IT201900003839A1 (it) | 2019-03-15 | 2020-09-15 | Olon Spa | Sintesi di apalutamide amorfa stabile |
| WO2020234817A1 (en) * | 2019-05-21 | 2020-11-26 | Laurus Labs Limited | Polymorphic forms of apalutamide and its preparation thereof |
| IT201900010593A1 (it) | 2019-07-01 | 2021-01-01 | Dipharma Francis Srl | Forma cristallina di un inibitore di recettori degli androgeni |
| EP4017848A1 (en) * | 2019-08-22 | 2022-06-29 | Dr. Reddy's Laboratories Ltd. | Process for the preparation of apalutamide |
| IT201900015974A1 (it) | 2019-09-10 | 2021-03-10 | Olon Spa | Apalutamide cristallina stabile in forma pura e processo per la sua preparazione |
| CN110590740A (zh) * | 2019-09-20 | 2019-12-20 | 武汉大学 | 一种阿帕鲁胺化合物及其药物制剂 |
| WO2022049265A1 (en) | 2020-09-04 | 2022-03-10 | Synthon B.V. | Improved process for preparation of apalutamide |
| CN112679468A (zh) * | 2021-01-05 | 2021-04-20 | 四川科伦药物研究院有限公司 | 阿帕他胺的晶体形式、制备方法和用途 |
| WO2023143090A1 (zh) * | 2022-01-25 | 2023-08-03 | 成都苑东生物制药股份有限公司 | 一种阿帕他胺溶剂化物新晶型及其制备方法 |
| CN115536634B (zh) * | 2022-10-17 | 2024-06-11 | 上海博悦生物科技有限公司 | 一种阿帕他胺的合成方法 |
| CN116332907A (zh) * | 2023-03-16 | 2023-06-27 | 奥锐特药业股份有限公司 | 一种无定形阿帕他胺的制备方法 |
| WO2025153768A1 (en) * | 2024-01-18 | 2025-07-24 | Nanoform Finland Oyj | Composition comprising crystalline nanosized apalutamide |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5323907A (en) | 1992-06-23 | 1994-06-28 | Multi-Comp, Inc. | Child resistant package assembly for dispensing pharmaceutical medications |
| US7709517B2 (en) | 2005-05-13 | 2010-05-04 | The Regents Of The University Of California | Diarylhydantoin compounds |
| CN101032483B (zh) * | 2006-03-09 | 2011-05-04 | 陈德桂 | 调节雄激素受体活性的乙内酰脲衍生物及其应用 |
| PL3412290T3 (pl) | 2006-03-27 | 2021-09-06 | The Regents Of The University Of California | Modulator receptora androgenowego do leczenia raka gruczołu krokowego i chorób związanych z receptorem androgenowym |
| CA2648139A1 (en) * | 2006-03-29 | 2007-11-08 | The Regents Of The University Of California | Diaryl thiohydantoin compounds and their use in the treatment of hyperproliferative disorders |
| WO2008119015A2 (en) * | 2007-03-27 | 2008-10-02 | Sloan-Kettering Institute For Cancer Research | Synthesis of thiohydantoins |
| EA028869B1 (ru) | 2010-02-16 | 2018-01-31 | Арагон Фармасьютикалс, Инк. | Модуляторы рецептора андрогенов и их применение |
| ES2809738T3 (es) | 2012-06-07 | 2021-03-05 | Aragon Pharmaceuticals Inc | Formas cristalinas de un modulador de receptor de andrógenos |
| WO2019242439A1 (zh) | 2018-06-20 | 2019-12-26 | 苏州科睿思制药有限公司 | Arn-509的晶型及其制备方法和用途 |
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2013
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2024
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