PE20150631A1 - Formas cristalinas de un modulador del receptor androgenico - Google Patents

Formas cristalinas de un modulador del receptor androgenico

Info

Publication number
PE20150631A1
PE20150631A1 PE2014002383A PE2014002383A PE20150631A1 PE 20150631 A1 PE20150631 A1 PE 20150631A1 PE 2014002383 A PE2014002383 A PE 2014002383A PE 2014002383 A PE2014002383 A PE 2014002383A PE 20150631 A1 PE20150631 A1 PE 20150631A1
Authority
PE
Peru
Prior art keywords
androgen receptor
receptor modulator
crystalline forms
modulator
trifluoromethylpyridin
Prior art date
Application number
PE2014002383A
Other languages
English (en)
Spanish (es)
Inventor
Nicholas D Smith
Mark R Herbert
Ouathek Ouerfelli
Anna Dilhas
Original Assignee
Aragon Pharmaceuticals Inc
Sloan Kettering Inst Cancer
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
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=PE20150631(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Aragon Pharmaceuticals Inc, Sloan Kettering Inst Cancer filed Critical Aragon Pharmaceuticals Inc
Publication of PE20150631A1 publication Critical patent/PE20150631A1/es

Links

Classifications

    • 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

Landscapes

  • 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)
PE2014002383A 2012-06-07 2013-06-04 Formas cristalinas de un modulador del receptor androgenico PE20150631A1 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
PE20150631A1 true PE20150631A1 (es) 2015-05-11

Family

ID=49712550

Family Applications (3)

Application Number Title Priority Date Filing Date
PE2014002383A PE20150631A1 (es) 2012-06-07 2013-06-04 Formas cristalinas de un modulador del receptor androgenico
PE2020000234A PE20200795A1 (es) 2012-06-07 2013-06-04 Composicion que comprende una forma cristalina del modulador receptor de androgeno: 4-[7-(6-ciano-5-trifluometilpiridin-3-il)-8-oxo-6-tioxo-5,7-diazaespiro [3.4]oct-5-il]-2-fluoro-n-metilbenzamida (apalutamida)
PE2019002096A PE20200725A1 (es) 2012-06-07 2013-06-04 Formas cristalinas del modulador receptor de androgeno: 4-[7-(6-ciano-5-trifluorometilpiridin-3-il)-8-oxo-6-tioxo-5,7-diazaespiro[3,4]oct-5-il]-2-fluoro-n-metilbenzamida) (apalutamida)

Family Applications After (2)

Application Number Title Priority Date Filing Date
PE2020000234A PE20200795A1 (es) 2012-06-07 2013-06-04 Composicion que comprende una forma cristalina del modulador receptor de androgeno: 4-[7-(6-ciano-5-trifluometilpiridin-3-il)-8-oxo-6-tioxo-5,7-diazaespiro [3.4]oct-5-il]-2-fluoro-n-metilbenzamida (apalutamida)
PE2019002096A PE20200725A1 (es) 2012-06-07 2013-06-04 Formas cristalinas del modulador receptor de androgeno: 4-[7-(6-ciano-5-trifluorometilpiridin-3-il)-8-oxo-6-tioxo-5,7-diazaespiro[3,4]oct-5-il]-2-fluoro-n-metilbenzamida) (apalutamida)

Country Status (45)

Country Link
US (9) US9481663B2 (enExample)
EP (4) EP3348553B1 (enExample)
JP (3) JP6182209B2 (enExample)
KR (2) KR102062024B1 (enExample)
CN (3) CN113135892A (enExample)
AU (3) AU2013271751B2 (enExample)
BR (1) BR112014030678A2 (enExample)
CA (4) CA2875767C (enExample)
CL (1) CL2014003331A1 (enExample)
CO (1) CO7240407A2 (enExample)
CR (2) CR20190331A (enExample)
CY (4) CY1120393T1 (enExample)
DK (3) DK2858985T3 (enExample)
EA (3) EA033956B1 (enExample)
EC (1) ECSP14030098A (enExample)
ES (3) ES2809738T3 (enExample)
FR (1) FR21C1050I2 (enExample)
GT (1) GT201400283A (enExample)
HK (2) HK1210175A1 (enExample)
HR (3) HRP20180902T1 (enExample)
HU (4) HUE038082T2 (enExample)
IL (5) IL267608B2 (enExample)
IN (1) IN2014DN10084A (enExample)
LT (4) LT3348553T (enExample)
LU (1) LUC00236I2 (enExample)
ME (2) ME03081B (enExample)
MX (1) MX356754B (enExample)
MY (1) MY187500A (enExample)
NI (1) NI201400142A (enExample)
NL (1) NL301144I2 (enExample)
NO (1) NO2021046I1 (enExample)
NZ (2) NZ717683A (enExample)
PE (3) PE20150631A1 (enExample)
PH (2) PH12014502714A1 (enExample)
PL (3) PL3533792T3 (enExample)
PT (3) PT3348553T (enExample)
RS (3) RS60617B1 (enExample)
SG (3) SG11201408140QA (enExample)
SI (3) SI3348553T1 (enExample)
SM (3) SMT201800311T1 (enExample)
TR (1) TR201808939T4 (enExample)
TW (1) TWI532732B (enExample)
UA (2) UA115665C2 (enExample)
WO (1) WO2013184681A1 (enExample)
ZA (1) ZA201500076B (enExample)

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US8461343B2 (en) 2007-03-27 2013-06-11 Sloan-Kettering Institute For Cancer Research Synthesis of thiohydantoins
CN104169266A (zh) 2011-12-16 2014-11-26 奥乐玛药物股份有限公司 新的苯并吡喃化合物、其组合物和用途
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
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

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US5323907A (en) 1992-06-23 1994-06-28 Multi-Comp, Inc. Child resistant package assembly for dispensing pharmaceutical medications
US7709517B2 (en) * 2005-05-13 2010-05-04 The Regents Of The University Of California Diarylhydantoin compounds
AU2007245022A1 (en) 2006-03-29 2007-11-08 The Regents Of The University Of California Diarylthiohydantoin compounds
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
EP4385574A3 (en) 2006-03-27 2024-10-02 The Regents of the University of California Androgen receptor modulator for the treatment of prostate cancer and androgen receptor-associated diseases
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
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
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

Also Published As

Publication number Publication date
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
ES2809738T3 (es) 2021-03-05
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
CY2021032I1 (enExample) 2022-03-24
JP2015518890A (ja) 2015-07-06
SI2858985T1 (sl) 2018-12-31
SI3348553T1 (sl) 2020-11-30
PL2858985T3 (pl) 2018-09-28
US20200115361A1 (en) 2020-04-16
WO2013184681A1 (en) 2013-12-12
MX356754B (es) 2018-06-11
US12018008B2 (en) 2024-06-25
PH12014502714B1 (en) 2015-02-02
US10556882B2 (en) 2020-02-11
PT3348553T (pt) 2020-09-28
UA123142C2 (uk) 2021-02-24
CO7240407A2 (es) 2015-04-17
CA3055660A1 (en) 2013-12-12
PH12016501470B1 (en) 2021-12-10
CN105693692A (zh) 2016-06-22
SG10201610249TA (en) 2017-02-27
JP6345821B2 (ja) 2018-06-20
LUC00236I2 (enExample) 2025-02-03
US20250092011A1 (en) 2025-03-20
EA028791B1 (ru) 2017-12-29
BR112014030678A2 (pt) 2017-06-27
LT3348553T (lt) 2020-09-25
PE20200725A1 (es) 2020-07-21
ME03815B (me) 2021-04-20
CY1120393T1 (el) 2019-07-10
HK1226066A1 (zh) 2017-09-22
EA201492272A1 (ru) 2015-05-29
ECSP14030098A (es) 2016-01-29
AU2017279807A1 (en) 2018-01-25
FR21C1050I1 (fr) 2021-12-10
EP3348553A1 (en) 2018-07-18
HK1210175A1 (en) 2016-04-15
CL2014003331A1 (es) 2016-03-04
MX2014015005A (es) 2015-09-04
ES2670683T3 (es) 2018-05-31
HUE050357T2 (hu) 2020-11-30
IL236055A0 (en) 2015-02-01
KR102062024B1 (ko) 2020-01-03
SMT202000496T1 (it) 2020-11-10
IL259738A (en) 2018-07-31
CY1124831T1 (el) 2022-03-24
EA201992010A1 (ru) 2020-01-24
EP2858985A4 (en) 2016-05-25
PE20200795A1 (es) 2020-08-10
LT3533792T (lt) 2021-07-26
US20190241539A1 (en) 2019-08-08
CA2875767C (en) 2018-08-14
PT2858985T (pt) 2018-07-10
CR20140549A (es) 2015-04-06
AU2013271751A1 (en) 2014-12-18
US10766875B2 (en) 2020-09-08
IL275413A (en) 2020-07-30
IL259738B (en) 2021-06-30
SMT202100355T1 (it) 2021-07-12
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
EA033956B1 (ru) 2019-12-13
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
JP2017178923A (ja) 2017-10-05
PH12014502714A1 (en) 2015-02-02
TWI532732B (zh) 2016-05-11
PT3533792T (pt) 2021-06-07
US20150133481A1 (en) 2015-05-14
CA3008345A1 (en) 2013-12-12
CA3114726A1 (en) 2013-12-12
US20190330182A1 (en) 2019-10-31
HUS2100047I1 (hu) 2021-11-29

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