EA033956B1 - 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 - Google Patents

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 Download PDF

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Publication number
EA033956B1
EA033956B1 EA201791592A EA201791592A EA033956B1 EA 033956 B1 EA033956 B1 EA 033956B1 EA 201791592 A EA201791592 A EA 201791592A EA 201791592 A EA201791592 A EA 201791592A EA 033956 B1 EA033956 B1 EA 033956B1
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Eurasian Patent Office
Prior art keywords
crystalline form
prostate cancer
methylbenzamide
oct
cyano
Prior art date
Application number
EA201791592A
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English (en)
Russian (ru)
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EA201791592A1 (ru
Inventor
Николас Д. Смит
Марк Р. Херберт
Оуатек Оуерфелли
Анна Дилхас
Original Assignee
Арагон Фармасьютикалз, Инк.
Слоан-Кеттеринг Инститьют Фор Кэнсер Рисерч
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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=EA033956(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Арагон Фармасьютикалз, Инк., Слоан-Кеттеринг Инститьют Фор Кэнсер Рисерч filed Critical Арагон Фармасьютикалз, Инк.
Publication of EA201791592A1 publication Critical patent/EA201791592A1/ru
Publication of EA033956B1 publication Critical patent/EA033956B1/ru

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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)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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)
EA201791592A 2012-06-07 2013-06-04 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 EA033956B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261656888P 2012-06-07 2012-06-07
US61/656,888 2012-06-07

Publications (2)

Publication Number Publication Date
EA201791592A1 EA201791592A1 (ru) 2018-01-31
EA033956B1 true EA033956B1 (ru) 2019-12-13

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Application Number Title Priority Date Filing Date
EA201791592A EA033956B1 (ru) 2012-06-07 2013-06-04 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
EA201992010A EA201992010A1 (ru) 2012-06-07 2013-06-04 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
EA201492272A EA028791B1 (ru) 2012-06-07 2013-06-04 Кристаллическая форма модулятора андрогенных рецепторов

Family Applications After (2)

Application Number Title Priority Date Filing Date
EA201992010A EA201992010A1 (ru) 2012-06-07 2013-06-04 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
EA201492272A EA028791B1 (ru) 2012-06-07 2013-06-04 Кристаллическая форма модулятора андрогенных рецепторов

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CN113135892A (zh) 2012-06-07 2021-07-20 阿拉贡药品公司 雄激素受体调节剂的晶形
EA033374B9 (ru) 2012-09-11 2019-12-18 Медивейшн Простейт Терапьютикс Ллк Твердые фармацевтические композиции, содержащие энзалутамид, и способ лечения
ES2836424T3 (es) 2012-09-26 2021-06-25 Aragon Pharmaceuticals Inc Antiandrógenos para tratar el cáncer de próstata no metastásico y resistente a la castración
JOP20200097A1 (ar) * 2013-01-15 2017-06-16 Aragon Pharmaceuticals Inc معدل مستقبل أندروجين واستخداماته
WO2016029776A1 (en) * 2014-08-26 2016-03-03 Astar Biotech Llc Protein kinase inhibitors
CN106999430A (zh) 2014-12-05 2017-08-01 阿拉贡药品公司 抗癌组合物
RS66323B1 (sr) 2014-12-05 2025-01-31 Aragon Pharmaceuticals Inc Sastavi protiv raka
MA41111B1 (fr) 2014-12-05 2021-09-30 Aragon Pharmaceuticals Inc Compositions anticancéreuses
WO2016100905A1 (en) 2014-12-19 2016-06-23 Lutron Electronics Co., Inc. Multi-channel lighting fixture having multiple light-emitting diode drivers
SG11201809680QA (en) 2016-06-03 2018-11-29 Aragon Pharmaceuticals Inc Anticancer compositions
ES2952770T3 (es) 2016-12-13 2023-11-06 Watson Lab Inc Formas de estado sólido de apalutamida
UA129105C2 (uk) 2017-10-16 2025-01-15 Арагон Фармасьютикалз, Інк. Антиандрогени для лікування неметастатичного резистентного до кастрації раку передміхурової залози
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
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
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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
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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
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KR102195916B1 (ko) 2020-12-30
US9994545B2 (en) 2018-06-12
DK2858985T3 (en) 2018-05-28
ES2875932T3 (es) 2021-11-11
CA3008345C (en) 2019-10-22
NZ717683A (en) 2018-04-27
PL3533792T3 (pl) 2021-11-29
US20210163441A1 (en) 2021-06-03
TW201402561A (zh) 2014-01-16
CR20190331A (es) 2019-11-12
PH12016501470A1 (en) 2017-07-10
SG10201610248SA (en) 2017-02-27
KR20150021993A (ko) 2015-03-03
EA201791592A1 (ru) 2018-01-31
HUE038082T2 (hu) 2018-09-28
MY187500A (en) 2021-09-24
SMT201800311T1 (it) 2018-07-17
JP6182209B2 (ja) 2017-08-16
ZA201500076B (en) 2016-10-26
IL267608B1 (en) 2025-06-01
GT201400283A (es) 2017-07-03
SI3533792T1 (sl) 2021-11-30
US20180258067A1 (en) 2018-09-13
AU2013271751B2 (en) 2017-02-23
LT2858985T (lt) 2018-09-25
NL301144I2 (nl) 2025-03-20
LTC3533792I2 (enExample) 2024-07-10
US10308630B2 (en) 2019-06-04
RS61988B1 (sr) 2021-07-30
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IN2014DN10084A (enExample) 2015-08-21
HRP20180902T1 (hr) 2018-08-24
EP3533792A1 (en) 2019-09-04
IL320522A (en) 2025-06-01
DK3348553T3 (da) 2020-07-27
NZ702203A (en) 2016-09-30
CY1123427T1 (el) 2021-12-31
CN113135892A (zh) 2021-07-20
RS57370B1 (sr) 2018-08-31
HRP20210909T1 (hr) 2021-09-03
US20200354335A1 (en) 2020-11-12
AU2017200298A1 (en) 2017-02-02
RS60617B1 (sr) 2020-09-30
EP2858985B1 (en) 2018-04-18
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JP2015518890A (ja) 2015-07-06
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SI3348553T1 (sl) 2020-11-30
PL2858985T3 (pl) 2018-09-28
US20200115361A1 (en) 2020-04-16
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US10556882B2 (en) 2020-02-11
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UA123142C2 (uk) 2021-02-24
CO7240407A2 (es) 2015-04-17
CA3055660A1 (en) 2013-12-12
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CN105693692A (zh) 2016-06-22
SG10201610249TA (en) 2017-02-27
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US20250092011A1 (en) 2025-03-20
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CY1120393T1 (el) 2019-07-10
HK1226066A1 (zh) 2017-09-22
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US20190241539A1 (en) 2019-08-08
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US10526310B2 (en) 2020-01-07
KR20190132543A (ko) 2019-11-27
PL3348553T3 (pl) 2021-02-08
IL267608B2 (en) 2025-10-01
HUE054595T2 (hu) 2021-09-28
UA115665C2 (uk) 2017-12-11
AU2017279807B2 (en) 2018-11-08
EP3348553B1 (en) 2020-07-08
EP3533792B1 (en) 2021-05-05
LTPA2021525I1 (enExample) 2021-11-25
CA2875767A1 (en) 2013-12-12
EP2858985A1 (en) 2015-04-15
US9481663B2 (en) 2016-11-01
HRP20201387T1 (hr) 2020-11-27
ME03081B (me) 2019-01-20
DK3533792T3 (da) 2021-06-28
AU2017200298B2 (en) 2017-09-28
NI201400142A (es) 2016-12-02
US10934271B2 (en) 2021-03-02
NO2021046I1 (no) 2021-11-02
SG11201408140QA (en) 2015-01-29
FR21C1050I2 (fr) 2024-05-24
EP3922629A1 (en) 2021-12-15
US20170001977A1 (en) 2017-01-05
TR201808939T4 (tr) 2018-07-23
JP2018141009A (ja) 2018-09-13
CN104619692A (zh) 2015-05-13
CY2021032I2 (el) 2022-03-24
IL267608A (en) 2019-08-29
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PH12014502714A1 (en) 2015-02-02
PE20150631A1 (es) 2015-05-11
TWI532732B (zh) 2016-05-11
PT3533792T (pt) 2021-06-07
US20150133481A1 (en) 2015-05-14
CA3008345A1 (en) 2013-12-12
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US20190330182A1 (en) 2019-10-31
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