CN114502539A - 包含雄激素受体的抑制剂的药物组合物和组合及其用途 - Google Patents

包含雄激素受体的抑制剂的药物组合物和组合及其用途 Download PDF

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CN114502539A
CN114502539A CN202080039623.3A CN202080039623A CN114502539A CN 114502539 A CN114502539 A CN 114502539A CN 202080039623 A CN202080039623 A CN 202080039623A CN 114502539 A CN114502539 A CN 114502539A
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China
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alkyl
optionally substituted
independently
cancer
androgen receptor
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CN202080039623.3A
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English (en)
Chinese (zh)
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H-J·周
R·勒莫伊涅
P·维尔斯克
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University of British Columbia
Provincial Health Services Authority
ESSA Pharma Inc
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University of British Columbia
Provincial Health Services Authority
ESSA Pharma Inc
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    • 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
    • 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
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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
    • A61K31/415—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
    • 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
    • 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
    • A61K31/42—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
    • 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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/4245—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
    • 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
    • A61K31/63—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
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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)
CN202080039623.3A 2019-03-28 2020-03-27 包含雄激素受体的抑制剂的药物组合物和组合及其用途 Pending CN114502539A (zh)

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

Publications (1)

Publication Number Publication Date
CN114502539A true CN114502539A (zh) 2022-05-13

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

Cited By (2)

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WO2023222011A1 (zh) * 2022-05-17 2023-11-23 海创药业股份有限公司 一种治疗三阴乳腺癌的联合用药物
WO2026056655A1 (zh) * 2024-09-12 2026-03-19 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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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
US12030875B2 (en) 2018-09-07 2024-07-09 PIC Therapeutics, Inc. EIF4E inhibitors and uses thereof
WO2020198712A1 (en) 2019-03-28 2020-10-01 Essa Pharma, Inc. Pharmaceutical compositions and combinations comprising inhibitors of the androgen receptor and uses thereof
AU2020348675B2 (en) 2019-09-16 2025-11-20 Takeda Pharmaceutical Company Limited Azole-fused pyridazin-3(2H)-one derivatives
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
AU2021230289A1 (en) 2020-03-03 2022-09-29 PIC Therapeutics, Inc. eIF4E inhibitors and uses thereof
AU2021255723A1 (en) 2020-04-17 2022-12-08 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
KR20220111673A (ko) * 2021-02-02 2022-08-09 주식회사 엘지화학 단백질 키나아제 억제제로서의 신규한 화합물
WO2022221661A1 (en) * 2021-04-16 2022-10-20 Essa Pharma, Inc. 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
JP2024534127A (ja) 2021-08-25 2024-09-18 ピク セラピューティクス， インコーポレイテッド ｅＩＦ４Ｅ阻害剤及びその使用
US12157732B2 (en) 2021-08-25 2024-12-03 PIC Therapeutics, Inc. eIF4E inhibitors and uses thereof
WO2023031371A1 (en) * 2021-09-01 2023-03-09 Janssen Pharmaceutica Nv Combination therapies for metastatic castration-resistant prostate cancer
US20240358701A1 (en) * 2021-09-01 2024-10-31 Essa Pharma Inc. Pharmaceutical compositions and combinations comprising inhibitors of the androgen receptor and uses thereof
CN118715210A (zh) * 2022-02-10 2024-09-27 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
WO2024006207A1 (en) * 2022-06-26 2024-01-04 Essa Pharma Inc. An n-terminal domain androgen receptor inhibitor and uses thereof
US11993580B1 (en) 2022-12-02 2024-05-28 Neumora Therapeutics, Inc. Methods of treating neurological disorders

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US20130045204A1 (en) * 2011-08-19 2013-02-21 The University Of British Columbia Fluorinated bisphenol ether compounds and methods for their use
US20170298033A1 (en) * 2016-04-15 2017-10-19 The University Of British Columbia Bisphenol derivatives and their use as androgen receptor activity modulators
US20180327368A1 (en) * 2015-01-13 2018-11-15 The University Of British Columbia University-Industry Liaison Office Heterocyclic compounds for cancer imaging and treatment and methods for their use
CN113195441A (zh) * 2018-10-18 2021-07-30 埃萨制药股份有限公司 雄激素受体调节剂及其使用方法

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LT2656842T (lt) * 2006-03-27 2016-09-26 The Regents Of The University Of California Androgeno receptoriaus moduliatorius, skirtas prostatos vėžio ir su androgeno receptoriumi susijusių ligų gydymui
PT2872482T (pt) * 2012-07-13 2020-09-22 Oncternal Therapeutics Inc Método de tratamento de cancro de mama com modulador seletivo do recetor de andrógeno (sarm)
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
LT3474841T (lt) * 2016-06-22 2022-06-10 Ellipses Pharma Ltd Ar+ krūties vėžio gydymo būdai

Patent Citations (4)

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US20130045204A1 (en) * 2011-08-19 2013-02-21 The University Of British Columbia Fluorinated bisphenol ether compounds and methods for their use
US20180327368A1 (en) * 2015-01-13 2018-11-15 The University Of British Columbia University-Industry Liaison Office Heterocyclic compounds for cancer imaging and treatment and methods for their use
US20170298033A1 (en) * 2016-04-15 2017-10-19 The University Of British Columbia Bisphenol derivatives and their use as androgen receptor activity modulators
CN113195441A (zh) * 2018-10-18 2021-07-30 埃萨制药股份有限公司 雄激素受体调节剂及其使用方法

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023222011A1 (zh) * 2022-05-17 2023-11-23 海创药业股份有限公司 一种治疗三阴乳腺癌的联合用药物
WO2026056655A1 (zh) * 2024-09-12 2026-03-19 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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JP2022521824A (ja) 2022-04-12
AU2020248105A1 (en) 2021-11-11
KR20210144827A (ko) 2021-11-30
CA3134545A1 (en) 2020-10-01
WO2020198710A1 (en) 2020-10-01
IL286726A (en) 2021-12-01
MX2021011826A (es) 2021-12-10
US20220202780A1 (en) 2022-06-30
EP3947353A4 (en) 2023-07-05
EP3947353A1 (en) 2022-02-09

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