KR102062024B1 - 안드로겐 수용체 조절제의 결정 형태 - Google Patents

안드로겐 수용체 조절제의 결정 형태 Download PDF

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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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delete delete
theta
methylbenzamide
oct
oxo
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KR20150021993A (ko
Inventor
니콜라스 디. 스미스
마크 알. 허버트
오아텍 아우어펠리
안나 딜라
Original Assignee
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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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28Antiandrogens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline 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)
KR1020157000266A 2012-06-07 2013-06-04 안드로겐 수용체 조절제의 결정 형태 Active KR102062024B1 (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 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

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ID=49712550

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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

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

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EP (4) EP3348553B1 (enExample)
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ME (2) ME03815B (enExample)
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TW (1) TWI532732B (enExample)
UA (2) UA115665C2 (enExample)
WO (1) WO2013184681A1 (enExample)
ZA (1) ZA201500076B (enExample)

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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

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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

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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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HUE054595T2 (hu) 2021-09-28
MY187500A (en) 2021-09-24
TW201402561A (zh) 2014-01-16
SI3348553T1 (sl) 2020-11-30
CA2875767A1 (en) 2013-12-12
RS61988B1 (sr) 2021-07-30
EA201492272A1 (ru) 2015-05-29
US20190241539A1 (en) 2019-08-08
IL267608A (en) 2019-08-29
PE20200795A1 (es) 2020-08-10
HUE038082T2 (hu) 2018-09-28
US12018008B2 (en) 2024-06-25
RS60617B1 (sr) 2020-09-30
MX356754B (es) 2018-06-11
EP3533792A1 (en) 2019-09-04
PE20200725A1 (es) 2020-07-21
KR102195916B1 (ko) 2020-12-30
MX2014015005A (es) 2015-09-04
KR20150021993A (ko) 2015-03-03
PL3348553T3 (pl) 2021-02-08
TWI532732B (zh) 2016-05-11
LUC00236I2 (enExample) 2025-02-03
LT3533792T (lt) 2021-07-26
LT2858985T (lt) 2018-09-25
AU2013271751B2 (en) 2017-02-23
CN104619692A (zh) 2015-05-13
EP3348553B1 (en) 2020-07-08
SI2858985T1 (sl) 2018-12-31
ZA201500076B (en) 2016-10-26
CY1120393T1 (el) 2019-07-10
CR20140549A (es) 2015-04-06
FR21C1050I1 (fr) 2021-12-10
IL259738A (en) 2018-07-31
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CA3055660A1 (en) 2013-12-12
HK1210175A1 (en) 2016-04-15
US20210163441A1 (en) 2021-06-03
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US20190330182A1 (en) 2019-10-31
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US20170001977A1 (en) 2017-01-05
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CA3008345A1 (en) 2013-12-12
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UA123142C2 (uk) 2021-02-24
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CR20190331A (es) 2019-11-12
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AU2017200298B2 (en) 2017-09-28
GT201400283A (es) 2017-07-03
SI3533792T1 (sl) 2021-11-30
PT3348553T (pt) 2020-09-28
WO2013184681A1 (en) 2013-12-12
LTPA2021525I1 (enExample) 2021-11-25
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US10526310B2 (en) 2020-01-07
EP2858985B1 (en) 2018-04-18
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US10934271B2 (en) 2021-03-02
CN113135892A (zh) 2021-07-20
EA028791B1 (ru) 2017-12-29
JP2015518890A (ja) 2015-07-06
US20200354335A1 (en) 2020-11-12
HRP20180902T1 (hr) 2018-08-24
US20180258067A1 (en) 2018-09-13
CA2875767C (en) 2018-08-14
AU2017279807B2 (en) 2018-11-08
AU2017279807A1 (en) 2018-01-25
KR20190132543A (ko) 2019-11-27
ECSP14030098A (es) 2016-01-29
NZ717683A (en) 2018-04-27
AU2013271751A1 (en) 2014-12-18
ME03081B (me) 2019-01-20
CL2014003331A1 (es) 2016-03-04
JP6182209B2 (ja) 2017-08-16
IL236055A0 (en) 2015-02-01
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JP6345821B2 (ja) 2018-06-20
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US10556882B2 (en) 2020-02-11
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PH12016501470B1 (en) 2021-12-10
BR112014030678A2 (pt) 2017-06-27
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IL267608B1 (en) 2025-06-01
CN105693692A (zh) 2016-06-22
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US10766875B2 (en) 2020-09-08
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US9994545B2 (en) 2018-06-12
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US10308630B2 (en) 2019-06-04
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US9481663B2 (en) 2016-11-01
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EP3533792B1 (en) 2021-05-05
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