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PE20200795A1 - 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) - Google Patents

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)

Info

Publication number
PE20200795A1
PE20200795A1 PE2020000234A PE2020000234A PE20200795A1 PE 20200795 A1 PE20200795 A1 PE 20200795A1 PE 2020000234 A PE2020000234 A PE 2020000234A PE 2020000234 A PE2020000234 A PE 2020000234A PE 20200795 A1 PE20200795 A1 PE 20200795A1
Authority
PE
Peru
Prior art keywords
androgen receptor
diazaspiro
methylbenzamide
thioxo
oxo
Prior art date
Application number
PE2020000234A
Other languages
English (en)
Inventor
Nicholas D Smith
Mark R Herbert
Ouathek Ouerfelli
Anna Dilhas
Original Assignee
Aragon Pharmaceuticals Inc
Sloan Kettering Inst Cancer Res
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=PE20200795(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 Res filed Critical Aragon Pharmaceuticals Inc
Publication of PE20200795A1 publication Critical patent/PE20200795A1/es

Links

Classifications

    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Tropical Medicine & Parasitology (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)

Abstract

La presente invencion hace referencia a formas amorfas y cristalinas del compuesto 4-[7-(6-ciano-5-trifluorometilpiridin-3-il)-8-oxo-6-tioxo-5,7-diazaspiro[3.4]oct-5-il]-2-fluoro-N-metilbenzamida, el cual es modulador del receptor androgenico. Tambien se refiere a composiciones que comprenden este compuesto y que se emplean en el tratamiento de enfermedades o afecciones asociadas con la actividad del receptor androgenico. Este compuesto se emplea en el tratamiento de diversos estados del cancer prostatico.
PE2020000234A 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) PE20200795A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261656888P 2012-06-07 2012-06-07
PCT/US2013/044116 WO2013184681A1 (en) 2012-06-07 2013-06-04 Crystalline forms of an androgen receptor modulator

Publications (1)

Publication Number Publication Date
PE20200795A1 true PE20200795A1 (es) 2020-08-10

Family

ID=49712550

Family Applications (3)

Application Number Title Priority Date Filing Date
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)
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)
PE2014002383A PE20150631A1 (es) 2012-06-07 2013-06-04 Formas cristalinas de un modulador del receptor androgenico

Family Applications Before (1)

Application Number Title Priority Date Filing Date
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 (1)

Application Number Title Priority Date Filing Date
PE2014002383A PE20150631A1 (es) 2012-06-07 2013-06-04 Formas cristalinas de un modulador del receptor androgenico

Country Status (45)

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US (9) US9481663B2 (es)
EP (4) EP3533792B1 (es)
JP (3) JP6182209B2 (es)
KR (2) KR102062024B1 (es)
CN (3) CN105693692A (es)
AU (3) AU2013271751B2 (es)
BR (1) BR112014030678A2 (es)
CA (4) CA3008345C (es)
CL (1) CL2014003331A1 (es)
CO (1) CO7240407A2 (es)
CR (2) CR20190331A (es)
CY (4) CY1120393T1 (es)
DK (3) DK3348553T3 (es)
EA (3) EA028791B1 (es)
EC (1) ECSP14030098A (es)
ES (3) ES2875932T3 (es)
FR (1) FR21C1050I2 (es)
GT (1) GT201400283A (es)
HK (2) HK1210175A1 (es)
HR (3) HRP20180902T1 (es)
HU (4) HUE038082T2 (es)
IL (5) IL320522A (es)
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LU (1) LUC00236I2 (es)
ME (2) ME03081B (es)
MX (1) MX356754B (es)
MY (1) MY187500A (es)
NI (1) NI201400142A (es)
NL (1) NL301144I2 (es)
NO (1) NO2021046I1 (es)
NZ (2) NZ702203A (es)
PE (3) PE20200725A1 (es)
PH (2) PH12014502714A1 (es)
PL (3) PL3533792T3 (es)
PT (3) PT2858985T (es)
RS (3) RS60617B1 (es)
SG (3) SG10201610249TA (es)
SI (3) SI2858985T1 (es)
SM (3) SMT202000496T1 (es)
TR (1) TR201808939T4 (es)
TW (1) TWI532732B (es)
UA (2) UA115665C2 (es)
WO (1) WO2013184681A1 (es)
ZA (1) ZA201500076B (es)

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JP2021527680A (ja) * 2018-06-20 2021-10-14 クリスタル ファーマシューティカル（スーチョウ）カンパニー，リミテッド Ａｒｎ−５０９の結晶形、その製造方法及びその用途
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IT201900003839A1 (it) 2019-03-15 2020-09-15 Olon Spa Sintesi di apalutamide amorfa stabile
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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
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
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JP2021527680A (ja) 2018-06-20 2021-10-14 クリスタル ファーマシューティカル（スーチョウ）カンパニー，リミテッド Ａｒｎ−５０９の結晶形、その製造方法及びその用途

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LT3533792T (lt) 2021-07-26
MX2014015005A (es) 2015-09-04
HUE038082T2 (hu) 2018-09-28
CA3114726A1 (en) 2013-12-12
IL320522A (en) 2025-06-01
JP2018141009A (ja) 2018-09-13
FR21C1050I2 (fr) 2024-05-24
DK3533792T3 (da) 2021-06-28
CY1123427T1 (el) 2021-12-31
CA3055660A1 (en) 2013-12-12
AU2017200298B2 (en) 2017-09-28
LTC3533792I2 (es) 2024-07-10
PH12014502714B1 (en) 2015-02-02
TW201402561A (zh) 2014-01-16
CR20190331A (es) 2019-11-12
KR20150021993A (ko) 2015-03-03
US10308630B2 (en) 2019-06-04
CA2875767C (en) 2018-08-14
HRP20210909T1 (hr) 2021-09-03
PH12016501470B1 (en) 2021-12-10
US10526310B2 (en) 2020-01-07
NI201400142A (es) 2016-12-02
US10934271B2 (en) 2021-03-02
TWI532732B (zh) 2016-05-11
CN104619692A (zh) 2015-05-13
AU2013271751B2 (en) 2017-02-23
UA123142C2 (uk) 2021-02-24
RS60617B1 (sr) 2020-09-30
US20200354335A1 (en) 2020-11-12
SG10201610249TA (en) 2017-02-27
NL301144I2 (nl) 2025-03-20
HUE050357T2 (hu) 2020-11-30
US20210163441A1 (en) 2021-06-03
ME03081B (me) 2019-01-20
IN2014DN10084A (es) 2015-08-21
LTPA2021525I1 (es) 2021-11-25
PE20200725A1 (es) 2020-07-21
SG11201408140QA (en) 2015-01-29
EA201791592A1 (ru) 2018-01-31
EP3922629A1 (en) 2021-12-15
ECSP14030098A (es) 2016-01-29
ES2670683T3 (es) 2018-05-31
US20200115361A1 (en) 2020-04-16
PL3533792T3 (pl) 2021-11-29
PT2858985T (pt) 2018-07-10
SMT202100355T1 (it) 2021-07-12
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RS61988B1 (sr) 2021-07-30
US20190330182A1 (en) 2019-10-31
PL2858985T3 (pl) 2018-09-28
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SMT201800311T1 (it) 2018-07-17
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CO7240407A2 (es) 2015-04-17
AU2017279807A1 (en) 2018-01-25
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ES2875932T3 (es) 2021-11-11
US9481663B2 (en) 2016-11-01
KR102195916B1 (ko) 2020-12-30
MX356754B (es) 2018-06-11
SI3348553T1 (sl) 2020-11-30
RS57370B1 (sr) 2018-08-31
US20180258067A1 (en) 2018-09-13
EP3348553B1 (en) 2020-07-08
US20190241539A1 (en) 2019-08-08
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BR112014030678A2 (pt) 2017-06-27
NZ717683A (en) 2018-04-27
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CY2021032I1 (es) 2022-03-24
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GT201400283A (es) 2017-07-03
CL2014003331A1 (es) 2016-03-04
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