KR102062024B1 - 안드로겐 수용체 조절제의 결정 형태 - Google Patents
안드로겐 수용체 조절제의 결정 형태 Download PDFInfo
- Publication number
- KR102062024B1 KR102062024B1 KR1020157000266A KR20157000266A KR102062024B1 KR 102062024 B1 KR102062024 B1 KR 102062024B1 KR 1020157000266 A KR1020157000266 A KR 1020157000266A KR 20157000266 A KR20157000266 A KR 20157000266A KR 102062024 B1 KR102062024 B1 KR 102062024B1
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- South Korea
- Prior art keywords
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- theta
- methylbenzamide
- oct
- oxo
- 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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- 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
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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
- A61K31/435—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
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- 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
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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
-
- 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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- 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)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261656888P | 2012-06-07 | 2012-06-07 | |
| US61/656,888 | 2012-06-07 | ||
| PCT/US2013/044116 WO2013184681A1 (en) | 2012-06-07 | 2013-06-04 | Crystalline forms of an androgen receptor modulator |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020197033592A Division KR102195916B1 (ko) | 2012-06-07 | 2013-06-04 | 안드로겐 수용체 조절제의 결정 형태 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20150021993A KR20150021993A (ko) | 2015-03-03 |
| KR102062024B1 true KR102062024B1 (ko) | 2020-01-03 |
Family
ID=49712550
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020157000266A Active KR102062024B1 (ko) | 2012-06-07 | 2013-06-04 | 안드로겐 수용체 조절제의 결정 형태 |
| KR1020197033592A Active KR102195916B1 (ko) | 2012-06-07 | 2013-06-04 | 안드로겐 수용체 조절제의 결정 형태 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020197033592A Active KR102195916B1 (ko) | 2012-06-07 | 2013-06-04 | 안드로겐 수용체 조절제의 결정 형태 |
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 |
| EA201992010A1 (ru) | 2012-06-07 | 2020-01-24 | Арагон Фармасьютикалз, Инк. | Кристаллическая форма а 4-[7-(6-циано-5-трифторметилпиридин-3-ил)-8-оксо-6-тиоксо-5,7-диазаспиро[3.4]окт-5-ил]-2-фтор-n-метилбензамида для лечения заболевания или состояния, связанного с активностью андрогенных рецепторов, включая рак простаты |
| WO2014043208A1 (en) | 2012-09-11 | 2014-03-20 | Medivation Prostate Therapeutics, Inc. | Formulations of enzalutamide |
| SG11201501870RA (en) | 2012-09-26 | 2015-04-29 | Aragon Pharmaceuticals Inc | Anti-androgens for the treatment of non-metastatic castrate-resistant prostate cancer |
| SG10201907684PA (en) * | 2013-01-15 | 2019-10-30 | Aragon Pharmaceuticals Inc | Androgen receptor modulator and uses thereof |
| 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 |
| ES3019912T3 (en) | 2014-12-05 | 2025-05-21 | Aragon Pharmaceuticals Inc | Anticancer compositions |
| WO2016090098A1 (en) | 2014-12-05 | 2016-06-09 | Aragon Pharmaceuticals, Inc. | Anticancer compositions |
| ES2839128T3 (es) | 2014-12-05 | 2021-07-05 | Aragon Pharmaceuticals Inc | Composiciones anticancerosas |
| CA2971443C (en) | 2014-12-19 | 2020-10-27 | Lutron Electronics Co., Inc. | Multi-channel lighting fixture having multiple light-emitting diode drivers |
| TN2018000366A1 (en) | 2016-06-03 | 2020-06-15 | Aragon Pharmaceuticals Inc | Anticancer compositions. |
| US11149017B2 (en) | 2016-12-13 | 2021-10-19 | Watson Laboratories Inc. | Solid state forms of apalutamide |
| AU2018351714A1 (en) | 2017-10-16 | 2020-04-30 | 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 |
| JP2021527680A (ja) * | 2018-06-20 | 2021-10-14 | クリスタル ファーマシューティカル（スーチョウ）カンパニー，リミテッド | Ａｒｎ−５０９の結晶形、その製造方法及びその用途 |
| 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 |
| EP4541786A3 (en) | 2020-09-04 | 2025-08-06 | 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 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070004753A1 (en) | 2005-05-13 | 2007-01-04 | The Regents Of The University Of California | Diarylhydantoin compounds |
| WO2007127010A2 (en) | 2006-03-29 | 2007-11-08 | The Regents Of The University Of California | Diarylthiohydantoin compounds |
| WO2008119015A2 (en) * | 2007-03-27 | 2008-10-02 | Sloan-Kettering Institute For Cancer Research | Synthesis of thiohydantoins |
Family Cites Families (6)
| 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 |
| 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 |
| LT2656842T (lt) | 2006-03-27 | 2016-09-26 | The Regents Of The University Of California | Androgeno receptoriaus moduliatorius, skirtas prostatos vėžio ir su androgeno receptoriumi susijusių ligų gydymui |
| WO2011103202A2 (en) * | 2010-02-16 | 2011-08-25 | Aragon Pharmaceuticals, Inc. | Androgen receptor modulators and uses thereof |
| EA201992010A1 (ru) | 2012-06-07 | 2020-01-24 | Арагон Фармасьютикалз, Инк. | Кристаллическая форма а 4-[7-(6-циано-5-трифторметилпиридин-3-ил)-8-оксо-6-тиоксо-5,7-диазаспиро[3.4]окт-5-ил]-2-фтор-n-метилбензамида для лечения заболевания или состояния, связанного с активностью андрогенных рецепторов, включая рак простаты |
| JP2021527680A (ja) | 2018-06-20 | 2021-10-14 | クリスタル ファーマシューティカル（スーチョウ）カンパニー，リミテッド | Ａｒｎ−５０９の結晶形、その製造方法及びその用途 |
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2013
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- 2013-06-04 WO PCT/US2013/044116 patent/WO2013184681A1/en not_active Ceased
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2016
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2017
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2018
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2019
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2020
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2021
- 2021-01-26 US US17/158,806 patent/US12018008B2/en active Active
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- 2021-11-02 NO NO2021046C patent/NO2021046I1/no unknown
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- 2021-11-03 LT LTPA2021525C patent/LTC3533792I2/lt unknown
- 2021-11-03 FR FR21C1050C patent/FR21C1050I2/fr active Active
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2024
- 2024-05-13 US US18/662,345 patent/US20250092011A1/en not_active Abandoned
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2025
- 2025-04-18 US US19/183,276 patent/US20260109683A1/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070004753A1 (en) | 2005-05-13 | 2007-01-04 | The Regents Of The University Of California | Diarylhydantoin compounds |
| WO2007127010A2 (en) | 2006-03-29 | 2007-11-08 | The Regents Of The University Of California | Diarylthiohydantoin compounds |
| WO2008119015A2 (en) * | 2007-03-27 | 2008-10-02 | Sloan-Kettering Institute For Cancer Research | Synthesis of thiohydantoins |
Also Published As
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| Publication | Publication Date | Title |
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