UA123142C2 - Кристалічні форми модулятора андрогенного рецептора - Google Patents

Кристалічні форми модулятора андрогенного рецептора Download PDF

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Publication number
UA123142C2
UA123142C2 UAA201702779A UAA201702779A UA123142C2 UA 123142 C2 UA123142 C2 UA 123142C2 UA A201702779 A UAA201702779 A UA A201702779A UA A201702779 A UAA201702779 A UA A201702779A UA 123142 C2 UA123142 C2 UA 123142C2
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UA
Ukraine
Prior art keywords
theta
methylbenzamide
thioxo
fluoro
oxo
Prior art date
Application number
UAA201702779A
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English (en)
Ukrainian (uk)
Inventor
Ніколас Д. Сміт
Николас Д. Смит
Марк Р. Херберт
Оуатек Оуерфеллі
Оуатек Оуэрфелли
Анна Ділхас
Анна Дилхас
Original Assignee
Арагон Фармасьютікалз, Інк.
Слоан-Кеттерінг Інстітьют Фор Кенсер Рісерч
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=49712550&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=UA123142(C2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Арагон Фармасьютікалз, Інк., Слоан-Кеттерінг Інстітьют Фор Кенсер Рісерч filed Critical Арагон Фармасьютікалз, Інк.
Publication of UA123142C2 publication Critical patent/UA123142C2/uk

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    • 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
    • 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
    • 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)
UAA201702779A 2012-06-07 2013-06-04 Кристалічні форми модулятора андрогенного рецептора UA123142C2 (uk)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261656888P 2012-06-07 2012-06-07

Publications (1)

Publication Number Publication Date
UA123142C2 true UA123142C2 (uk) 2021-02-24

Family

ID=49712550

Family Applications (2)

Application Number Title Priority Date Filing Date
UAA201702779A UA123142C2 (uk) 2012-06-07 2013-06-04 Кристалічні форми модулятора андрогенного рецептора
UAA201500086A UA115665C2 (uk) 2012-06-07 2013-06-04 Кристалічні форми модулятора андрогенного рецептора

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UAA201500086A UA115665C2 (uk) 2012-06-07 2013-06-04 Кристалічні форми модулятора андрогенного рецептора

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UA (2) UA123142C2 (enExample)
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CA3008345C (en) 2012-06-07 2019-10-22 Aragon Pharmaceuticals, Inc. Crystalline forms of an androgen receptor modulator
CN105358535B (zh) 2012-09-11 2019-01-04 麦迪威森前列腺医疗有限责任公司 恩杂鲁胺制剂
EA030128B1 (ru) 2012-09-26 2018-06-29 Арагон Фармасьютикалз, Инк. Способ лечения неметастатического кастрационно-резистентного рака простаты
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
KR20200141533A (ko) 2014-12-05 2020-12-18 아라곤 파마슈티컬스, 인코포레이티드 항암 조성물
PT3226843T (pt) 2014-12-05 2021-07-07 Aragon Pharmaceuticals Inc Composições anticancro
ES3021508T3 (en) 2014-12-05 2025-05-27 Aragon Pharmaceuticals Inc Anticancer compositions
US9888543B2 (en) 2014-12-19 2018-02-06 Lutron Electronics Co, Inc. Multi-channel lighting fixture having multiple light-emitting diode drivers
MA45090A (fr) 2016-06-03 2021-04-28 Aragon Pharmaceuticals Inc Compositions anticancéreuses
EP3555061B1 (en) 2016-12-13 2023-06-07 Watson Laboratories Inc. Solid state forms of apalutamide
KR20240096623A (ko) 2017-10-16 2024-06-26 아라곤 파마슈티컬스, 인코포레이티드 비-전이성 거세-저항성 전립선암의 치료를 위한 항-안드로겐
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
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
EP4208451A1 (en) 2020-09-04 2023-07-12 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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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
CN102755318B (zh) * 2006-03-29 2014-09-10 加利福尼亚大学董事会 二芳基硫代乙内酰脲化合物
US8461343B2 (en) 2007-03-27 2013-06-11 Sloan-Kettering Institute For Cancer Research Synthesis of thiohydantoins
KR101819199B1 (ko) * 2010-02-16 2018-01-16 아라곤 파마슈티컬스, 인코포레이티드 안드로겐 수용체 조절제 및 이의 용도
CA3008345C (en) 2012-06-07 2019-10-22 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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LT3533792T (lt) 2021-07-26
ES2670683T3 (es) 2018-05-31
HUE050357T2 (hu) 2020-11-30
CA2875767A1 (en) 2013-12-12
LTPA2021525I1 (enExample) 2021-11-25
JP2015518890A (ja) 2015-07-06
US9994545B2 (en) 2018-06-12
US10526310B2 (en) 2020-01-07
IN2014DN10084A (enExample) 2015-08-21
TWI532732B (zh) 2016-05-11
DK3348553T3 (da) 2020-07-27
CA3008345C (en) 2019-10-22
CN105693692A (zh) 2016-06-22
EA201791592A1 (ru) 2018-01-31
AU2017279807B2 (en) 2018-11-08
IL275413A (en) 2020-07-30
CL2014003331A1 (es) 2016-03-04
MY187500A (en) 2021-09-24
NI201400142A (es) 2016-12-02
US10934271B2 (en) 2021-03-02
CY1123427T1 (el) 2021-12-31
PL2858985T3 (pl) 2018-09-28
BR112014030678A2 (pt) 2017-06-27
LUC00236I2 (enExample) 2025-02-03
US10556882B2 (en) 2020-02-11
EP3533792B1 (en) 2021-05-05
EP3348553A1 (en) 2018-07-18
IL267608A (en) 2019-08-29
IL320522A (en) 2025-06-01
FR21C1050I1 (fr) 2021-12-10
EP2858985A4 (en) 2016-05-25
HUE054595T2 (hu) 2021-09-28
KR20190132543A (ko) 2019-11-27
DK2858985T3 (en) 2018-05-28
ES2875932T3 (es) 2021-11-11
JP2018141009A (ja) 2018-09-13
UA115665C2 (uk) 2017-12-11
EP2858985A1 (en) 2015-04-15
CY1120393T1 (el) 2019-07-10
CA3008345A1 (en) 2013-12-12
SI3533792T1 (sl) 2021-11-30
CR20140549A (es) 2015-04-06
RS57370B1 (sr) 2018-08-31
CO7240407A2 (es) 2015-04-17
EA201992010A1 (ru) 2020-01-24
US20170001977A1 (en) 2017-01-05
IL259738A (en) 2018-07-31
IL236055A0 (en) 2015-02-01
RS60617B1 (sr) 2020-09-30
CA3055660A1 (en) 2013-12-12
EP3348553B1 (en) 2020-07-08
ZA201500076B (en) 2016-10-26
SI2858985T1 (sl) 2018-12-31
KR102062024B1 (ko) 2020-01-03
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PL3533792T3 (pl) 2021-11-29
MX2014015005A (es) 2015-09-04
JP6182209B2 (ja) 2017-08-16
US12018008B2 (en) 2024-06-25
US20180258067A1 (en) 2018-09-13
KR20150021993A (ko) 2015-03-03
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EA028791B1 (ru) 2017-12-29
US20190241539A1 (en) 2019-08-08
DK3533792T3 (da) 2021-06-28
SMT201800311T1 (it) 2018-07-17
PT3533792T (pt) 2021-06-07
PE20150631A1 (es) 2015-05-11
NL301144I2 (nl) 2025-03-20
PH12014502714A1 (en) 2015-02-02
KR102195916B1 (ko) 2020-12-30
PL3348553T3 (pl) 2021-02-08
FR21C1050I2 (fr) 2024-05-24
HRP20210909T1 (hr) 2021-09-03
LT2858985T (lt) 2018-09-25
IL259738B (en) 2021-06-30
EA033956B1 (ru) 2019-12-13
CY1124831T1 (el) 2022-03-24
AU2013271751A1 (en) 2014-12-18
AU2013271751B2 (en) 2017-02-23
PE20200795A1 (es) 2020-08-10
WO2013184681A1 (en) 2013-12-12
EP3533792A1 (en) 2019-09-04
CY2021032I2 (el) 2022-03-24
HRP20201387T1 (hr) 2020-11-27
US20150133481A1 (en) 2015-05-14
CA2875767C (en) 2018-08-14
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EP2858985B1 (en) 2018-04-18
CA3114726A1 (en) 2013-12-12
SG10201610249TA (en) 2017-02-27
PH12014502714B1 (en) 2015-02-02
AU2017279807A1 (en) 2018-01-25
US20190330182A1 (en) 2019-10-31
PH12016501470A1 (en) 2017-07-10
US10766875B2 (en) 2020-09-08
TW201402561A (zh) 2014-01-16
ES2809738T3 (es) 2021-03-05
ECSP14030098A (es) 2016-01-29
JP6345821B2 (ja) 2018-06-20
PT2858985T (pt) 2018-07-10
ME03815B (me) 2021-04-20
IL267608B2 (en) 2025-10-01
AU2017200298B2 (en) 2017-09-28
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US20200115361A1 (en) 2020-04-16
HUS2100047I1 (hu) 2021-11-29
CR20190331A (es) 2019-11-12
NO2021046I1 (no) 2021-11-02
US9481663B2 (en) 2016-11-01
LTC3533792I2 (enExample) 2024-07-10
US10308630B2 (en) 2019-06-04
IL267608B1 (en) 2025-06-01
SG11201408140QA (en) 2015-01-29
TR201808939T4 (tr) 2018-07-23
CN113135892A (zh) 2021-07-20
EA201492272A1 (ru) 2015-05-29
PT3348553T (pt) 2020-09-28
ME03081B (me) 2019-01-20
RS61988B1 (sr) 2021-07-30
SG10201610248SA (en) 2017-02-27
US20210163441A1 (en) 2021-06-03
HK1210175A1 (en) 2016-04-15
SMT202100355T1 (it) 2021-07-12
AU2017200298A1 (en) 2017-02-02
SI3348553T1 (sl) 2020-11-30
US20200354335A1 (en) 2020-11-12
JP2017178923A (ja) 2017-10-05
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HK1226066A1 (zh) 2017-09-22
GT201400283A (es) 2017-07-03
EP3922629A1 (en) 2021-12-15
NZ717683A (en) 2018-04-27
PE20200725A1 (es) 2020-07-21
LT3348553T (lt) 2020-09-25
CN104619692A (zh) 2015-05-13
HRP20180902T1 (hr) 2018-08-24
US20250092011A1 (en) 2025-03-20

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