KR102195916B1 - 안드로겐 수용체 조절제의 결정 형태 - Google Patents

안드로겐 수용체 조절제의 결정 형태 Download PDF

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KR102195916B1
KR102195916B1 KR1020197033592A KR20197033592A KR102195916B1 KR 102195916 B1 KR102195916 B1 KR 102195916B1 KR 1020197033592 A KR1020197033592 A KR 1020197033592A KR 20197033592 A KR20197033592 A KR 20197033592A KR 102195916 B1 KR102195916 B1 KR 102195916B1
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theta
methylbenzamide
thioxo
oct
oxo
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KR20190132543A (ko
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니콜라스 디. 스미스
마크 알. 허버트
오아텍 아우어펠리
안나 딜라
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아라곤 파마슈티컬스, 인코포레이티드
슬로안-케테링인스티튜트퍼캔서리서치
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Application filed by 아라곤 파마슈티컬스, 인코포레이티드, 슬로안-케테링인스티튜트퍼캔서리서치 filed Critical 아라곤 파마슈티컬스, 인코포레이티드
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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
    • 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

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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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
KR1020197033592A 2012-06-07 2013-06-04 안드로겐 수용체 조절제의 결정 형태 Active KR102195916B1 (ko)

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 Parent Applications (1)

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KR1020157000266A Division KR102062024B1 (ko) 2012-06-07 2013-06-04 안드로겐 수용체 조절제의 결정 형태

Publications (2)

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KR20190132543A KR20190132543A (ko) 2019-11-27
KR102195916B1 true KR102195916B1 (ko) 2020-12-30

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ID=49712550

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KR1020197033592A Active KR102195916B1 (ko) 2012-06-07 2013-06-04 안드로겐 수용체 조절제의 결정 형태
KR1020157000266A Active KR102062024B1 (ko) 2012-06-07 2013-06-04 안드로겐 수용체 조절제의 결정 형태

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KR1020157000266A Active KR102062024B1 (ko) 2012-06-07 2013-06-04 안드로겐 수용체 조절제의 결정 형태

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US (10) US9481663B2 (https=)
EP (4) EP2858985B1 (https=)
JP (3) JP6182209B2 (https=)
KR (2) KR102195916B1 (https=)
CN (3) CN105693692A (https=)
AU (3) AU2013271751B2 (https=)
BR (1) BR112014030678A2 (https=)
CA (4) CA3055660A1 (https=)
CL (1) CL2014003331A1 (https=)
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CR (2) CR20190331A (https=)
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DK (3) DK3533792T3 (https=)
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ES (3) ES2875932T3 (https=)
FR (1) FR21C1050I2 (https=)
GT (1) GT201400283A (https=)
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HR (3) HRP20180902T1 (https=)
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TW (1) TWI532732B (https=)
UA (2) UA115665C2 (https=)
WO (1) WO2013184681A1 (https=)
ZA (1) ZA201500076B (https=)

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EP2791128A4 (en) 2011-12-16 2015-04-22 Olema Pharmaceuticals Inc NOVEL BENZOPYRAN COMPOUNDS, COMPOSITIONS AND USES THEREOF
EP2858985B1 (en) 2012-06-07 2018-04-18 Aragon Pharmaceuticals, Inc. Crystalline forms of an androgen receptor modulator
JP6404217B2 (ja) 2012-09-11 2018-10-10 メディベイション プロステイト セラピューティクス エルエルシー エンザルタミドの製剤
NZ744456A (en) 2012-09-26 2019-09-27 Aragon Pharmaceuticals Inc Anti-androgens for the treatment of non-metastatic castrate-resistant prostate cancer
PL2945628T3 (pl) * 2013-01-15 2020-09-21 Aragon Pharmaceuticals, Inc. Modulator receptorów androgenowych w skojarzeniu z octanem abirateronu i prednizonem do leczenia nowotworu stercza
JP2017525727A (ja) * 2014-08-26 2017-09-07 アスター バイオテック リミテッド ライアビリティ カンパニー プロテインキナーゼ阻害剤
HUE054935T2 (hu) * 2014-12-05 2021-10-28 Aragon Pharmaceuticals Inc Rákellenes készítmények
SG11201704267VA (en) 2014-12-05 2017-06-29 Aragon Pharmaceuticals Inc Anticancer compositions
LT3226842T (lt) 2014-12-05 2021-03-25 Aragon Pharmaceuticals, Inc. Priešvėžinės kompozicijos
WO2016100905A1 (en) 2014-12-19 2016-06-23 Lutron Electronics Co., Inc. Multi-channel lighting fixture having multiple light-emitting diode drivers
CA3024872A1 (en) 2016-06-03 2017-12-07 Aragon Pharmaceuticals, Inc. Anticancer compositions
US11149017B2 (en) 2016-12-13 2021-10-19 Watson Laboratories Inc. Solid state forms of apalutamide
US10702508B2 (en) 2017-10-16 2020-07-07 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
EP3812378A4 (en) * 2018-06-20 2021-04-28 Crystal Pharmaceutical (Suzhou) Co., Ltd. CRYSTALLINE FORMS OF RNA-509, CORRESPONDING METHOD OF PREPARATION AND ASSOCIATED USE
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
US20220281836A1 (en) * 2019-08-22 2022-09-08 Dr. Reddy's Laboratories Limited 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
CN116034101B (zh) 2020-09-04 2026-04-03 斯索恩有限公司 制备阿帕鲁胺的改进方法
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

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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

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AU2011218173C1 (en) * 2010-02-16 2015-04-16 Aragon Pharmaceuticals, Inc. Androgen receptor modulators and uses thereof
EP2858985B1 (en) 2012-06-07 2018-04-18 Aragon Pharmaceuticals, Inc. Crystalline forms of an androgen receptor modulator
EP3812378A4 (en) 2018-06-20 2021-04-28 Crystal Pharmaceutical (Suzhou) Co., Ltd. CRYSTALLINE FORMS OF RNA-509, CORRESPONDING METHOD OF PREPARATION AND ASSOCIATED USE

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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

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MX2014015005A (es) 2015-09-04
US12018008B2 (en) 2024-06-25
US20190330182A1 (en) 2019-10-31
HRP20180902T1 (hr) 2018-08-24
WO2013184681A1 (en) 2013-12-12
RS57370B1 (sr) 2018-08-31
CL2014003331A1 (es) 2016-03-04
CY1120393T1 (el) 2019-07-10
AU2017200298A1 (en) 2017-02-02
FR21C1050I2 (fr) 2024-05-24
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US10308630B2 (en) 2019-06-04
MY187500A (en) 2021-09-24
PT3348553T (pt) 2020-09-28
IL267608B1 (en) 2025-06-01
HK1226066A1 (zh) 2017-09-22
US20250092011A1 (en) 2025-03-20
IL236055A0 (en) 2015-02-01
DK2858985T3 (en) 2018-05-28
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SMT202100355T1 (it) 2021-07-12
NI201400142A (es) 2016-12-02
US10934271B2 (en) 2021-03-02
KR20150021993A (ko) 2015-03-03
HUE038082T2 (hu) 2018-09-28
LT2858985T (lt) 2018-09-25
CA3008345C (en) 2019-10-22
KR20190132543A (ko) 2019-11-27
CY1123427T1 (el) 2021-12-31
CR20140549A (es) 2015-04-06
US20170001977A1 (en) 2017-01-05
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