KR20210144827A - 안드로겐 수용체의 억제제를 포함하는 약제학적 조성물 및 조합물 및 그의 용도 - Google Patents

안드로겐 수용체의 억제제를 포함하는 약제학적 조성물 및 조합물 및 그의 용도 Download PDF

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KR20210144827A
KR20210144827A KR1020217034804A KR20217034804A KR20210144827A KR 20210144827 A KR20210144827 A KR 20210144827A KR 1020217034804 A KR1020217034804 A KR 1020217034804A KR 20217034804 A KR20217034804 A KR 20217034804A KR 20210144827 A KR20210144827 A KR 20210144827A
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alkyl
optionally substituted
halogen
androgen receptor
cancer
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Korean (ko)
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한-지에 주
모인 로난 레
피터 비르시크
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에싸 파마 아이엔씨.
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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
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • 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
    • A61K31/275—Nitriles; Isonitriles
    • A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
    • 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
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
    • A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/42—Oxazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
    • A61K31/4245—Oxadiazoles
    • 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
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • 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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
KR1020217034804A 2019-03-28 2020-03-27 안드로겐 수용체의 억제제를 포함하는 약제학적 조성물 및 조합물 및 그의 용도 Ceased KR20210144827A (ko)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201962825450P 2019-03-28 2019-03-28
US62/825,450 2019-03-28
US201962842980P 2019-05-03 2019-05-03
US62/842,980 2019-05-03
US201962857519P 2019-06-05 2019-06-05
US62/857,519 2019-06-05
PCT/US2020/025539 WO2020198710A1 (en) 2019-03-28 2020-03-27 Pharmaceutical compositions and combinations comprising inhibitors of the androgen receptor and uses thereof

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KR20210144827A true KR20210144827A (ko) 2021-11-30

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US (1) US20220202780A1 (enExample)
EP (1) EP3947353A4 (enExample)
JP (1) JP2022521824A (enExample)
KR (1) KR20210144827A (enExample)
CN (1) CN114502539A (enExample)
AU (1) AU2020248105A1 (enExample)
CA (1) CA3134545A1 (enExample)
IL (1) IL286726A (enExample)
MX (1) MX2021011826A (enExample)
WO (1) WO2020198710A1 (enExample)

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US10471023B2 (en) 2015-03-12 2019-11-12 British Columbia Cancer Agency Branch Bisphenol ether derivatives and methods for using the same
US20170298033A1 (en) 2016-04-15 2017-10-19 The University Of British Columbia Bisphenol derivatives and their use as androgen receptor activity modulators
WO2019226991A1 (en) 2018-05-25 2019-11-28 Essa Pharma, Inc. Androgen receptor modulators and methods for their use
EP3846793B1 (en) 2018-09-07 2024-01-24 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
US12637418B2 (en) 2019-01-24 2026-05-26 Takeda Pharmaceutical Company Limited Heterocyclic compounds as antagonist of NMDA
US12109179B2 (en) 2019-03-28 2024-10-08 Essa Pharma Inc. Pharmaceutical compositions and combinations comprising inhibitors of the androgen receptor and uses thereof
TWI873185B (zh) 2019-09-16 2025-02-21 日商武田藥品工業股份有限公司 唑稠合之嗒-3(2h)-酮衍生物
JP2021050161A (ja) 2019-09-25 2021-04-01 武田薬品工業株式会社 複素環化合物及びその用途
JP2021080177A (ja) 2019-11-14 2021-05-27 武田薬品工業株式会社 複素環化合物及びその用途
AR121506A1 (es) 2020-03-03 2022-06-08 Pic Therapeutics Inc Inhibidores del eif4e y sus usos
EP4135675A4 (en) * 2020-04-17 2024-04-10 Essa Pharma, Inc. SOLID FORMS OF AN N-TERMINAL DOMAIN ANDROGEN RECEPTOR INHIBITOR AND USES THEREOF
WO2022060969A1 (en) * 2020-09-16 2022-03-24 Essa Pharma, Inc. Pharmaceutical compositions and combinations comprising inhibitors of the androgen receptor and uses thereof
WO2022169248A1 (ko) * 2021-02-02 2022-08-11 주식회사 엘지화학 단백질 키나아제 억제제로서의 신규한 화합물
CA3215182A1 (en) * 2021-04-16 2022-10-20 Han-Jie Zhou Pharmaceutical compositions comprising inhibitors of the androgen receptor and uses thereof
CN115340527B (zh) * 2021-05-13 2023-09-15 成都先导药物开发股份有限公司 一种bcl-xl抑制剂及其制备方法和用途
CN113603695B (zh) * 2021-08-05 2022-06-14 青岛恒宁生物科技有限公司 一种取代的嘧啶胺类化合物或其作为农药可接受的盐、组合物及其用途
IL310924A (en) 2021-08-25 2024-04-01 Pic Therapeutics Inc Eif4e inhibitors and uses thereof
US12157732B2 (en) 2021-08-25 2024-12-03 PIC Therapeutics, Inc. eIF4E inhibitors and uses thereof
AU2022340817A1 (en) * 2021-09-01 2024-03-14 Essa Pharma Inc. Pharmaceutical compositions and combinations comprising inhibitors of the androgen receptor and uses thereof
US20240398797A1 (en) * 2021-09-01 2024-12-05 Janssen Pharmaceutica Nv Combination therapies for metastatic castration-resistant prostate cancer
WO2023151662A1 (zh) * 2022-02-10 2023-08-17 上海奕拓医药科技有限责任公司 雄激素受体活性调节剂及其应用
CN117065022A (zh) * 2022-05-17 2023-11-17 海创药业股份有限公司 一种治疗三阴乳腺癌的药物
WO2024006207A1 (en) * 2022-06-26 2024-01-04 Essa Pharma Inc. An n-terminal domain androgen receptor inhibitor and uses thereof
EP4626878A1 (en) 2022-12-02 2025-10-08 Neumora Therapeutics, Inc. Methods of treating neurological disorders
CN118255693A (zh) * 2024-03-28 2024-06-28 大连理工大学 联苯类化合物及其在制备治疗白血病、肺癌以及乳腺癌药物中的应用
CN121698845A (zh) * 2024-09-12 2026-03-20 青岛普泰科生物医药科技有限公司 一种四氢喹啉类ntd抑制剂及其应用

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BRPI0709771B1 (pt) * 2006-03-27 2022-01-25 The Regents Of The University Of California Composto e composição farmacêutica
ES2613098T3 (es) * 2011-08-19 2017-05-22 British Columbia Cancer Agency Branch Compuestos de éter de bisfenol fluorado y métodos para su uso
EP3733170A1 (en) * 2012-07-13 2020-11-04 Oncternal Therapeutics, Inc. A method of treating androgen receptor (ar) -positive breast cancers with selective androgen receptor modulator (sarms)
FI3988541T3 (fi) * 2015-01-13 2024-09-17 British Columbia Cancer Agency Branch Heterosyklisiä yhdisteitä syövän kuvantamiseksi ja hoitamiseksi ja menetelmiä niiden käyttämiseksi
US10980806B2 (en) * 2016-03-24 2021-04-20 University of Pittsburgh—of the Commonwealth System of Higher Education Small molecule inhibitors of the nuclear translocation of androgen receptor for the treatment of castration-resistant prostate cancer
US20170298033A1 (en) * 2016-04-15 2017-10-19 The University Of British Columbia Bisphenol derivatives and their use as androgen receptor activity modulators
WO2017223115A1 (en) * 2016-06-22 2017-12-28 Radius Health, Inc. Ar+ breast cancer treatment methods
AU2019362061B2 (en) * 2018-10-18 2024-09-26 Essa Pharma Inc Androgen receptor modulators and methods for their use

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JP2022521824A (ja) 2022-04-12
EP3947353A1 (en) 2022-02-09
IL286726A (en) 2021-12-01
US20220202780A1 (en) 2022-06-30
NZ781283A (en) 2024-09-27
EP3947353A4 (en) 2023-07-05
WO2020198710A1 (en) 2020-10-01
CA3134545A1 (en) 2020-10-01
AU2020248105A1 (en) 2021-11-11
MX2021011826A (es) 2021-12-10
CN114502539A (zh) 2022-05-13

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