CN104619692A - 雄激素受体调节剂的晶形 - Google Patents

雄激素受体调节剂的晶形 Download PDF

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Publication number
CN104619692A
CN104619692A CN201380041652.3A CN201380041652A CN104619692A CN 104619692 A CN104619692 A CN 104619692A CN 201380041652 A CN201380041652 A CN 201380041652A CN 104619692 A CN104619692 A CN 104619692A
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China
Prior art keywords
crystalline form
property
xrpd
ray powder
powder diffraction
Prior art date
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Pending
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CN201380041652.3A
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English (en)
Chinese (zh)
Inventor
N.D.史密斯
M.R.赫伯特
O.奥尔费里
A.迪哈斯
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Memorial Sloan Kettering Cancer Center
Aragon Pharmaceuticals Inc
Original Assignee
Memorial Sloan Kettering Cancer Center
Aragon Pharmaceuticals Inc
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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=CN104619692(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Memorial Sloan Kettering Cancer Center, Aragon Pharmaceuticals Inc filed Critical Memorial Sloan Kettering Cancer Center
Priority to CN202110417935.XA priority Critical patent/CN113135892A/zh
Priority to CN201610202980.2A priority patent/CN105693692A/zh
Publication of CN104619692A publication Critical patent/CN104619692A/zh
Pending legal-status Critical Current

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    • 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

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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)
  • Reproductive Health (AREA)
  • Urology & Nephrology (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)
CN201380041652.3A 2012-06-07 2013-06-04 雄激素受体调节剂的晶形 Pending CN104619692A (zh)

Priority Applications (2)

Application Number Priority Date Filing Date Title
CN202110417935.XA CN113135892A (zh) 2012-06-07 2013-06-04 雄激素受体调节剂的晶形
CN201610202980.2A CN105693692A (zh) 2012-06-07 2013-06-04 雄激素受体调节剂的晶形

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261656888P 2012-06-07 2012-06-07
US61/656888 2012-06-07
PCT/US2013/044116 WO2013184681A1 (en) 2012-06-07 2013-06-04 Crystalline forms of an androgen receptor modulator

Related Child Applications (2)

Application Number Title Priority Date Filing Date
CN202110417935.XA Division CN113135892A (zh) 2012-06-07 2013-06-04 雄激素受体调节剂的晶形
CN201610202980.2A Division CN105693692A (zh) 2012-06-07 2013-06-04 雄激素受体调节剂的晶形

Publications (1)

Publication Number Publication Date
CN104619692A true CN104619692A (zh) 2015-05-13

Family

ID=49712550

Family Applications (3)

Application Number Title Priority Date Filing Date
CN201380041652.3A Pending CN104619692A (zh) 2012-06-07 2013-06-04 雄激素受体调节剂的晶形
CN201610202980.2A Pending CN105693692A (zh) 2012-06-07 2013-06-04 雄激素受体调节剂的晶形
CN202110417935.XA Pending CN113135892A (zh) 2012-06-07 2013-06-04 雄激素受体调节剂的晶形

Family Applications After (2)

Application Number Title Priority Date Filing Date
CN201610202980.2A Pending CN105693692A (zh) 2012-06-07 2013-06-04 雄激素受体调节剂的晶形
CN202110417935.XA Pending CN113135892A (zh) 2012-06-07 2013-06-04 雄激素受体调节剂的晶形

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US (9) US9481663B2 (enExample)
EP (4) EP3533792B1 (enExample)
JP (3) JP6182209B2 (enExample)
KR (2) KR102062024B1 (enExample)
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TW (1) TWI532732B (enExample)
UA (2) UA115665C2 (enExample)
WO (1) WO2013184681A1 (enExample)
ZA (1) ZA201500076B (enExample)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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
CN115536634A (zh) * 2022-10-17 2022-12-30 上海博悦生物科技有限公司 一种阿帕他胺的合成方法
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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WO2008119015A2 (en) 2007-03-27 2008-10-02 Sloan-Kettering Institute For Cancer Research Synthesis of thiohydantoins
AP2014007657A0 (en) 2011-12-16 2014-05-31 Olema Pharmaceuticals Inc Novel benzopyran compounds, compositions and uses thereof
US9481663B2 (en) 2012-06-07 2016-11-01 Aragon Pharmaceuticals, Inc. Crystalline forms of an androgen receptor modulator
ES2892029T3 (es) 2012-09-11 2022-02-01 Medivation Prostate Therapeutics Llc Formulaciones de enzalutamida
UA117663C2 (uk) 2012-09-26 2018-09-10 Арагон Фармасьютікалз, Інк. Антиандроген для лікування неметастатичного кастраційно-резистентного раку передміхурової залози
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
MA41107B1 (fr) * 2014-12-05 2025-01-31 Aragon Pharmaceuticals, Inc. Compositions anti-cancéreuses
LT3226843T (lt) 2014-12-05 2021-08-10 Aragon Pharmaceuticals, Inc. Priešvėžinės kompozicijos
PT3226842T (pt) 2014-12-05 2020-12-23 Aragon Pharmaceuticals Inc Composições anticancerígenas
MX2017008050A (es) 2014-12-19 2018-01-18 Lutron Electronics Co Accesorio de iluminacion multicanal que tiene controladores de diodo emisor de luz.
AR108489A1 (es) 2016-06-03 2018-08-29 Aragon Pharmaceuticals Inc Composiciones antineoplásicas
WO2018112001A1 (en) 2016-12-13 2018-06-21 Watson Laboratories Inc. Solid state forms of apalutamide
US10702508B2 (en) 2017-10-16 2020-07-07 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
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
CN116034101A (zh) 2020-09-04 2023-04-28 斯索恩有限公司 制备阿帕鲁胺的改进方法
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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CN101032483A (zh) * 2006-03-09 2007-09-12 陈德桂 调节雄激素受体活性的乙内酰脲衍生物的组成及其应用
WO2008119015A2 (en) * 2007-03-27 2008-10-02 Sloan-Kettering Institute For Cancer Research Synthesis of thiohydantoins
CN101454002A (zh) * 2006-03-27 2009-06-10 加利福尼亚大学董事会 用于治疗前列腺癌和与雄激素受体相关的疾病的雄激素受体调节剂
WO2011103202A2 (en) * 2010-02-16 2011-08-25 Aragon Pharmaceuticals, Inc. Androgen receptor modulators and uses thereof

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US9481663B2 (en) 2012-06-07 2016-11-01 Aragon Pharmaceuticals, Inc. Crystalline forms of an androgen receptor modulator
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

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101032483A (zh) * 2006-03-09 2007-09-12 陈德桂 调节雄激素受体活性的乙内酰脲衍生物的组成及其应用
CN101454002A (zh) * 2006-03-27 2009-06-10 加利福尼亚大学董事会 用于治疗前列腺癌和与雄激素受体相关的疾病的雄激素受体调节剂
WO2008119015A2 (en) * 2007-03-27 2008-10-02 Sloan-Kettering Institute For Cancer Research Synthesis of thiohydantoins
WO2011103202A2 (en) * 2010-02-16 2011-08-25 Aragon Pharmaceuticals, Inc. Androgen receptor modulators and uses thereof

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN111344283A (zh) * 2018-06-20 2020-06-26 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
US11066384B2 (en) 2018-06-20 2021-07-20 Crystal Pharmaceutical (Suzhou) Co., Ltd. Crystalline forms of ARN-509, preparation method and use thereof
CN111344283B (zh) * 2018-06-20 2022-08-12 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
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
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
CN115536634A (zh) * 2022-10-17 2022-12-30 上海博悦生物科技有限公司 一种阿帕他胺的合成方法
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

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KR102195916B1 (ko) 2020-12-30
AU2017279807A1 (en) 2018-01-25
AU2017200298B2 (en) 2017-09-28
JP6182209B2 (ja) 2017-08-16
US20170001977A1 (en) 2017-01-05
US20200354335A1 (en) 2020-11-12
CN113135892A (zh) 2021-07-20
RS61988B1 (sr) 2021-07-30
WO2013184681A1 (en) 2013-12-12
FR21C1050I2 (fr) 2024-05-24
KR20150021993A (ko) 2015-03-03
LTPA2021525I1 (enExample) 2021-11-25
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EA201492272A1 (ru) 2015-05-29
DK2858985T3 (en) 2018-05-28
CA3055660A1 (en) 2013-12-12
SI2858985T1 (sl) 2018-12-31
PH12014502714B1 (en) 2015-02-02
EA033956B1 (ru) 2019-12-13
ES2809738T3 (es) 2021-03-05
ES2670683T3 (es) 2018-05-31
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SG10201610248SA (en) 2017-02-27
US10766875B2 (en) 2020-09-08
EP2858985A4 (en) 2016-05-25
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ME03081B (me) 2019-01-20
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KR20190132543A (ko) 2019-11-27
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CA3114726A1 (en) 2013-12-12
US10934271B2 (en) 2021-03-02
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US12018008B2 (en) 2024-06-25
UA115665C2 (uk) 2017-12-11
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US10526310B2 (en) 2020-01-07
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