CN115916170A - 固体形式的n-末端结构域雄激素受体抑制剂及其用途 - Google Patents

固体形式的n-末端结构域雄激素受体抑制剂及其用途 Download PDF

Info

Publication number
CN115916170A
CN115916170A CN202180028377.6A CN202180028377A CN115916170A CN 115916170 A CN115916170 A CN 115916170A CN 202180028377 A CN202180028377 A CN 202180028377A CN 115916170 A CN115916170 A CN 115916170A
Authority
CN
China
Prior art keywords
compound
cancer
solvate
sdd
amorphous form
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CN202180028377.6A
Other languages
English (en)
Chinese (zh)
Inventor
H-J·周
P·维希克
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.)
ESSA Pharma Inc
Original Assignee
ESSA Pharma Inc
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
Application filed by ESSA Pharma Inc filed Critical ESSA Pharma Inc
Publication of CN115916170A publication Critical patent/CN115916170A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/69—Benzenesulfonamido-pyrimidines
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
CN202180028377.6A 2020-04-17 2021-04-16 固体形式的n-末端结构域雄激素受体抑制剂及其用途 Pending CN115916170A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063011671P 2020-04-17 2020-04-17
US63/011,671 2020-04-17
PCT/US2021/027771 WO2021212032A1 (en) 2020-04-17 2021-04-16 Solid forms of an n-terminal domain androgen receptor inhibitor and uses thereof

Publications (1)

Publication Number Publication Date
CN115916170A true CN115916170A (zh) 2023-04-04

Family

ID=78081437

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202180028377.6A Pending CN115916170A (zh) 2020-04-17 2021-04-16 固体形式的n-末端结构域雄激素受体抑制剂及其用途

Country Status (8)

Country Link
US (6) US20210323931A1 (https=)
EP (1) EP4135675A4 (https=)
JP (2) JP2023522040A (https=)
KR (1) KR20230004498A (https=)
CN (1) CN115916170A (https=)
AU (1) AU2021255723A1 (https=)
CA (1) CA3174422A1 (https=)
WO (1) WO2021212032A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN118706889A (zh) * 2024-05-31 2024-09-27 瀚晖制药有限公司 一种阿帕他胺固体制剂结晶度的检测方法

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016141458A1 (en) 2015-03-12 2016-09-15 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
US11485713B2 (en) 2018-05-25 2022-11-01 Essa Pharma, Inc. Androgen receptor modulators and methods for their use
WO2020198712A1 (en) 2019-03-28 2020-10-01 Essa Pharma, Inc. Pharmaceutical compositions and combinations comprising inhibitors of the androgen receptor and uses thereof
CN115916170A (zh) 2020-04-17 2023-04-04 埃萨制药股份有限公司 固体形式的n-末端结构域雄激素受体抑制剂及其用途
WO2022060969A1 (en) * 2020-09-16 2022-03-24 Essa Pharma, Inc. Pharmaceutical compositions and combinations comprising inhibitors of the androgen receptor and uses thereof
US20240207264A1 (en) * 2021-04-16 2024-06-27 Essa Pharma Inc. Pharmaceutical compositions comprising inhibitors of the androgen receptor and uses thereof
WO2023031371A1 (en) * 2021-09-01 2023-03-09 Janssen Pharmaceutica Nv Combination therapies for metastatic castration-resistant prostate cancer
WO2024006207A1 (en) * 2022-06-26 2024-01-04 Essa Pharma Inc. An n-terminal domain androgen receptor inhibitor and uses thereof

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1856461A (zh) * 2003-07-28 2006-11-01 史密丝克莱恩比彻姆公司 作为雌激素受体调节剂的亚环烷基化合物
US20080058383A1 (en) * 2003-10-21 2008-03-06 Henrik Jernstedt Androgen Receptor Modulators
CN101146531A (zh) * 2005-01-21 2008-03-19 阿斯泰克斯治疗有限公司 药物化合物
CN101945853A (zh) * 2007-12-21 2011-01-12 配体药物公司 选择性雄激素受体调节剂(sarm)及其应用
US20120172406A1 (en) * 2009-09-10 2012-07-05 Youzhi Tong Androgen receptor antagonists and uses thereof
WO2018045450A1 (en) * 2016-09-09 2018-03-15 British Columbia Cancer Agency Branch Bisphenol a compounds and methods for treating drug-resistant androgen receptor mediated cancers
US20180271849A1 (en) * 2015-09-29 2018-09-27 Kangpu Biopharmaceuticals, Ltd. Pharmaceutical composition and application thereof
CN109311807A (zh) * 2016-04-15 2019-02-05 不列颠哥伦比亚癌症局分支机构 双酚衍生物和其作为雄激素受体活性调节剂的用途
WO2019226991A1 (en) * 2018-05-25 2019-11-28 Essa Pharma, Inc. Androgen receptor modulators and methods for their use

Family Cites Families (98)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2571217A (en) 1951-10-16 Horace s
US2890189A (en) 1954-06-14 1959-06-09 Johnson & Son Inc S C Alkali soluble resins and compositions containing the same
US3074974A (en) 1957-12-06 1963-01-22 Monsanto Chemicals Method for the preparation of diglycidyl ether of tetrachlorobisphenol-a
US3162615A (en) 1961-01-03 1964-12-22 Dow Chemical Co Polyesters from cyclic polyhaloalkane polyols and unsaturated dicarboxylic acids
FR1389005A (fr) 1963-01-09 1965-02-12 Bayer Ag Procédé perfectionné pour durcir des polyépoxydes
SU638596A1 (ru) 1975-09-01 1978-12-25 Государственный Научно-Исследовательский И Проектный Институт Полимерных Клеев Им. Э.Л.Тер-Газаряна Хлоргидриднное производное диаллилизоциануровой кислоты в качестве пластификатора поливинилацетатной эмульсии
US4284574A (en) 1979-06-15 1981-08-18 Ciba-Geigy Corporation Diglycidyl ethers of di-secondary alcohols, their preparation, and curable compositions containing them
SU929630A1 (ru) 1980-02-06 1982-05-23 Научно-Исследовательский Институт Биологии При Иркутском Государственном Университете Им.А.А.Жданова Способ получени ди-или триоксидифенил-сульфонов
US4369298A (en) 1980-05-27 1983-01-18 Tokuyama Soda Kabushiki Kaisha Novel cured resin, process for production thereof, and lens composed of said resin from bis(alkyleneoxyphenyl)-diacrylate, bis(alkyleneoxyphenyl)diallyl ether, bis(alkyleneoxyphenyl)diallyl carbonate monomers
DE3170223D1 (en) 1981-01-13 1985-06-05 Teijin Ltd Ion-permeable composite membrane and its use in selective separation
JPS6049473A (ja) 1983-08-29 1985-03-18 Nec Corp カラ−コ−ドリ−ダ
IN169231B (https=) 1984-03-15 1991-09-14 Ciba Geigy Ag
PL141793B1 (en) 1984-10-08 1987-08-31 Politechnika Warszawska Method of obtaining bisphenolic resins
US5753730A (en) 1986-12-15 1998-05-19 Mitsui Toatsu Chemicals, Inc. Plastic lenses having a high-refractive index, process for the preparation thereof and casting polymerization process for preparing sulfur-containing urethane resin lens and lens prepared thereby
JPH0832844B2 (ja) 1987-02-09 1996-03-29 パイロツトインキ株式会社 筆記板用不透明性インキ
DE3852839T2 (de) 1987-04-27 1995-06-22 Mitsubishi Gas Chemical Co Hitzehärtbare Harzzusammensetzung.
KR910003821B1 (ko) 1987-06-01 1991-06-12 더 다우 케미칼 캄파니 하이드록시방향족 화합물의 프로파르길 에테르를 제조하는 방법
US5155196A (en) 1987-06-01 1992-10-13 The Dow Chemical Company Polymer resulting from the cure of a preformed chromene-containing mixture
JP2572020B2 (ja) 1987-06-19 1997-01-16 竹本油脂株式会社 熱硬化性樹脂用難燃剤
DE3821585A1 (de) 1987-09-13 1989-03-23 Hoechst Ag Positiv arbeitendes strahlungsempfindliches gemisch und daraus hergestelltes strahlungsempfindliches aufzeichnungsmaterial fuer hochenergetische strahlung
US4855184A (en) 1988-02-02 1989-08-08 Minnesota Mining And Manufacturing Company Radiation-curable protective coating composition
DE3939760A1 (de) 1989-12-01 1991-06-06 Bayer Ag Verfahren zur lackierung von kunststoffen, lackierte kunststoffe und die verwendung von hierzu geeigneten haftvermittlern
EP0515128A1 (en) 1991-05-23 1992-11-25 Konica Corporation Silver halide color photographic light-sensitive material
JPH0649473A (ja) 1992-08-04 1994-02-22 Asahi Chem Ind Co Ltd 冷媒組成物
DE4323512A1 (de) 1992-09-01 1994-04-28 Agfa Gevaert Ag Fotografisches Aufzeichnungsmaterial
JPH07117349A (ja) 1993-10-27 1995-05-09 Asahi Denka Kogyo Kk 感熱記録材料
CN1167437A (zh) 1994-11-29 1997-12-10 赫彻斯特马里恩鲁斯公司 用三芳基-乙烯衍生物治疗和预防骨质疏松的方法
DE19526146A1 (de) 1995-07-07 1997-01-09 Schering Ag Triphenylethylene, Verfahren zu deren Herstellung, diese Triphenylethylene enthaltene pharmazeutische Präparate sowie deren Verwendung zur Herstellung von Arzneimitteln
JPH09176240A (ja) 1995-12-27 1997-07-08 Mitsubishi Chem Corp 光重合性組成物
JPH10133427A (ja) 1996-11-05 1998-05-22 Fuji Xerox Co Ltd 静電潜像現像用キャリア、静電潜像現像剤及び画像形成方法
AR011626A1 (es) 1997-02-07 2000-08-30 Shell Int Research Un procedimiento para la elaboracion de compuestos epoxidos, resinas epoxidas obtenidas mediante dicho procedimiento y un procedimiento para laelaboracion de compuestos intermedios para la elaboracion de compuestos epoxidos
JPH10316803A (ja) 1997-05-16 1998-12-02 Teijin Chem Ltd 難燃性樹脂組成物
IL125840A (en) 1997-08-22 2002-12-01 Teijin Chemicals Ltd Bromine compound production method
JPH11166087A (ja) 1997-12-04 1999-06-22 Teijin Chem Ltd 難燃性樹脂組成物
CA2302169A1 (en) 1998-06-30 2000-01-13 The University Of British Columbia Inhibitors of androgen-independent activation of androgen receptor
US6245117B1 (en) 1998-08-07 2001-06-12 Ipposha Oil Industries Co., Ltd. Modifier of cellulose fibers and modification method of cellulose fibers
US6218430B1 (en) 1998-08-24 2001-04-17 Ligand Pharmaceuticals Incorporated Vitamin D3 mimics
JP3795679B2 (ja) 1998-09-01 2006-07-12 帝人化成株式会社 臭素化合物の製造方法
AU775928B2 (en) 1999-10-14 2004-08-19 Bristol-Myers Squibb Company Crystallographic structure of the androgen receptor ligand binding domain
US6534621B2 (en) 2000-05-18 2003-03-18 Dow Global Technologies Inc. Process for manufacturing a hydroxyester derivative intermediate and epoxy resins prepared therefrom
US6472436B1 (en) 2000-07-17 2002-10-29 The Salk Institute For Biological Studies Methods for protecting cells from amyloid toxicity and for inhibiting amyloid protein production
AU2001286965A1 (en) 2000-08-31 2002-03-13 Advanced Medicine, Inc. Sodium channel modulators
DE10102322A1 (de) 2001-01-19 2002-07-25 Merck Patent Gmbh Phenylderivate
US6646102B2 (en) 2001-07-05 2003-11-11 Dow Global Technologies Inc. Process for manufacturing an alpha-dihydroxy derivative and epoxy resins prepared therefrom
US20030092724A1 (en) 2001-09-18 2003-05-15 Huaihung Kao Combination sustained release-immediate release oral dosage forms with an opioid analgesic and a non-opioid analgesic
AU2003217304A1 (en) 2002-02-28 2003-09-16 The University Of Tennessee Research Corporation Radiolabeled selective androgen receptor modulators and their use in prostate cancer imaging and therapy
JP2005529952A (ja) 2002-06-17 2005-10-06 ユニバーシティ・オブ・テネシー・リサーチ・ファウンデーション Ｎ架橋選択的アンドロゲン受容体修飾物質及びその使用方法
US7595345B2 (en) 2003-11-20 2009-09-29 Eli Lilly And Company Vitamin D receptor modulators
JP2007524677A (ja) 2004-02-13 2007-08-30 ザ ユニバーシティ オブ ブリティッシュ コロンビア 放射性標識化合物及び組成物、それらの前駆体及びそれらの製造方法
JP2005325301A (ja) 2004-05-17 2005-11-24 Fuji Photo Film Co Ltd セルロースアシレートドープ組成物、およびセルロースアシレートフィルム
US20090105349A1 (en) 2004-08-18 2009-04-23 Warner-Lambert Company Llc Androgen modulators
JP2006208607A (ja) 2005-01-26 2006-08-10 Fuji Photo Film Co Ltd パターン形成材料、並びにパターン形成装置及び永久パターン形成方法
CN101137623B (zh) 2005-03-15 2013-03-27 奈科明有限责任公司 N-磺酰基吡咯及其作为组蛋白脱乙酰酶抑制剂的用途
JP4753601B2 (ja) 2005-03-23 2011-08-24 旭化成イーマテリアルズ株式会社 感光性組成物
EP1717235A3 (en) 2005-04-29 2007-02-28 Bioprojet Phenoxypropylpiperidines and -pyrrolidines and their use as histamine H3-receptor ligands
FR2885904B1 (fr) 2005-05-19 2007-07-06 Aventis Pharma Sa Nouveaux derives du fluorene, compositions les contenant et utilisation
EP1792622A1 (en) 2005-11-11 2007-06-06 GPC Biotech AG Anti-proliferative combination therapy comprising a platinum-based chemotherapeutic agent and EGFR inhibitors or pyrimidine analogues
LT1976828T (lt) 2005-12-29 2017-04-25 Celtaxsys, Inc. Diamino dariniai, kaip leukotrieno a4 hidrolazės inhibitoriai
SI2656842T1 (sl) 2006-03-27 2016-10-28 The Regents Of The University Of California Modulator androgenih receptorjev za zdravljenje raka prostate in bolezni, povezanih z androgenimi receptorji
JP2007290980A (ja) 2006-04-21 2007-11-08 Shin Etsu Chem Co Ltd 含フッ素（メタ）アクリル酸エステル
DE102006019044A1 (de) 2006-04-25 2007-10-31 Merck Patent Gmbh Antioxidantien
TW200819421A (en) 2006-10-31 2008-05-01 Univ Nat Chunghsing The method of synthesizing biphenol A, BPA having di-alkoxyl group by using polycarbonate or its waste
KR20090115797A (ko) 2007-02-20 2009-11-06 바스프 에스이 고굴절률 단량체, 이의 조성물 및 용도
HUE034458T2 (en) 2008-07-02 2018-02-28 British Columbia Cancer Agency Branch Diglycidyl ether derivatives, therapeutics and methods for their use
JP2011530511A (ja) 2008-08-05 2011-12-22 メルク・シャープ・エンド・ドーム・コーポレイション 治療用化合物
US9388112B2 (en) 2010-01-06 2016-07-12 The University Of British Columbia Bisphenol derivatives and their use as androgen receptor activity modulators
US20130109758A1 (en) 2010-01-06 2013-05-02 The University Of British Columbia Bisphenol derivative therapeutics and methods for their use
AU2011218173C1 (en) 2010-02-16 2015-04-16 Aragon Pharmaceuticals, Inc. Androgen receptor modulators and uses thereof
EP2693875A4 (en) 2011-04-08 2014-10-22 British Columbia Cancer Agency BISPHENOL COMPOUNDS AND METHOD FOR THEIR USE
WO2012145328A1 (en) 2011-04-18 2012-10-26 The University Of British Columbia Dibenzylphenyl compounds and methods for their use
WO2012145330A1 (en) 2011-04-18 2012-10-26 The University Of British Columbia Fluorene-9-bisphenol compounds and methods for their use
US20130045204A1 (en) * 2011-08-19 2013-02-21 The University Of British Columbia Fluorinated bisphenol ether compounds and methods for their use
WO2013028791A1 (en) 2011-08-22 2013-02-28 British Columbia Cancer Agency Branch 18f compounds for cancer imaging and methods for their use
US9365510B2 (en) 2012-04-16 2016-06-14 British Columbia Cancer Agency Branch Aziridine bisphenol ethers and related compounds and methods for their use
LT2872482T (lt) 2012-07-13 2020-12-28 Oncternal Therapeutics, Inc. Krūties vėžių gydymo būdas selektyviu androgeno receptoriaus moduliatoriumi
MA37975B2 (fr) 2012-09-11 2021-03-31 Genzyme Corp Inhibiteurs de synthase de glucosylcéramide
AU2014262333B2 (en) 2013-05-10 2016-06-16 British Columbia Cancer Agency Branch Ester derivatives of androgen receptor modulators and methods for their use
CN103342892A (zh) 2013-06-06 2013-10-09 西安交通大学 一种双马来酰亚胺树脂的增韧改性剂及其制备方法
US20150010469A1 (en) 2013-07-03 2015-01-08 British Columbia Cancer Agency Branch Bisphenol ether compounds with novel bridging groups and methods for their use
WO2015031984A1 (en) 2013-09-09 2015-03-12 British Columbia Cancer Agency Branch Halogenated compounds for cancer imaging and treatment and methods for their use
TW201600499A (zh) 2014-05-15 2016-01-01 巴斯夫歐洲公司 用於製備石墨烯奈米帶的鄰三聯苯
WO2016058082A1 (en) 2014-10-14 2016-04-21 British Columbia Cancer Agency Branch 18f compounds for cancer imaging and methods for their use
WO2016058080A1 (en) 2014-10-14 2016-04-21 British Columbia Cancer Agency Branch Fluoro-chloro bisphenol ether compounds and methods for their use
DK3988541T3 (da) 2015-01-13 2024-09-16 British Columbia Cancer Agency Branch Heterocycliske forbindelser til billedscanning og behandling af cancer samt fremgangsmåder til anvendelse af disse
WO2016141458A1 (en) 2015-03-12 2016-09-15 British Columbia Cancer Agency Branch Bisphenol ether derivatives and methods for using the same
CA2929345A1 (en) 2015-09-02 2017-03-02 British Columbia Cancer Agency Branch Co-targeting androgen receptor splice variants and mtor signaling pathway for the treatment of castration-resistant prostate cancer
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
WO2017210771A1 (en) 2016-06-06 2017-12-14 British Columbia Cancer Agency Branch Compounds and compositions for radiation therapy and methods of using the same
MX389702B (es) 2016-06-22 2025-03-20 Ellipses Pharma Ltd Compuestos para usarse en el tratamiento de cancer de mama que expresa el receptor de androgenos (ar+).
WO2018157232A1 (en) 2017-02-28 2018-09-07 British Columbia Cancer Agency Branch Pharmaceutical compositions 'and combinations comprising inhibitors of the androgen receptor a1wd uses thereof
WO2019023651A2 (en) 2017-07-28 2019-01-31 Massachusetts Institute Of Technology MODULATORS OF THE SMALL MOLECULE ANDROGEN RECEPTOR
WO2020081999A1 (en) * 2018-10-18 2020-04-23 Essa Pharma, Inc. Androgen receptor modulators and methods for their use
CA3120850A1 (en) 2018-12-07 2020-06-11 Sumitomo Dainippon Pharma Oncology, Inc. Methods for treating castration-resistant and castration- sensitive prostate cancer
CN114269331A (zh) * 2019-03-28 2022-04-01 埃萨制药股份有限公司 雄激素受体调节剂和用作蛋白水解靶向嵌合体配体的方法
CA3134545A1 (en) * 2019-03-28 2020-10-01 Essa Pharma, Inc. Pharmaceutical compositions and combinations comprising inhibitors of the androgen receptor 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
CN115916170A (zh) 2020-04-17 2023-04-04 埃萨制药股份有限公司 固体形式的n-末端结构域雄激素受体抑制剂及其用途
WO2022060969A1 (en) 2020-09-16 2022-03-24 Essa Pharma, Inc. Pharmaceutical compositions and combinations comprising inhibitors of the androgen receptor and uses thereof

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1856461A (zh) * 2003-07-28 2006-11-01 史密丝克莱恩比彻姆公司 作为雌激素受体调节剂的亚环烷基化合物
US20080058383A1 (en) * 2003-10-21 2008-03-06 Henrik Jernstedt Androgen Receptor Modulators
CN101146531A (zh) * 2005-01-21 2008-03-19 阿斯泰克斯治疗有限公司 药物化合物
CN101945853A (zh) * 2007-12-21 2011-01-12 配体药物公司 选择性雄激素受体调节剂(sarm)及其应用
US20120172406A1 (en) * 2009-09-10 2012-07-05 Youzhi Tong Androgen receptor antagonists and uses thereof
US20180271849A1 (en) * 2015-09-29 2018-09-27 Kangpu Biopharmaceuticals, Ltd. Pharmaceutical composition and application thereof
CN109311807A (zh) * 2016-04-15 2019-02-05 不列颠哥伦比亚癌症局分支机构 双酚衍生物和其作为雄激素受体活性调节剂的用途
WO2018045450A1 (en) * 2016-09-09 2018-03-15 British Columbia Cancer Agency Branch Bisphenol a compounds and methods for treating drug-resistant androgen receptor mediated cancers
WO2019226991A1 (en) * 2018-05-25 2019-11-28 Essa Pharma, Inc. Androgen receptor modulators and methods for their use

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
MONAGHAN, AMY E, AND IAIN J MCEWAN: "A sting in the tail: the N-terminal domain of the androgen receptor as a drug target", 《ASIAN JOURNAL OF ANDROLOGY 》, vol. 18, no. 5, 31 October 2016 (2016-10-31), pages 687 - 694 *
江军: "雄激素受体反义RNA抑制前列腺癌细胞LNCaP致瘤性的研究", 《第三军医大学学报》, vol. 25, no. 15, 14 November 2003 (2003-11-14), pages 1336 - 1338 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN118706889A (zh) * 2024-05-31 2024-09-27 瀚晖制药有限公司 一种阿帕他胺固体制剂结晶度的检测方法

Also Published As

Publication number Publication date
KR20230004498A (ko) 2023-01-06
US20210323931A1 (en) 2021-10-21
US11518747B2 (en) 2022-12-06
JP2023522040A (ja) 2023-05-26
EP4135675A1 (en) 2023-02-22
EP4135675A4 (en) 2024-04-10
US11814357B2 (en) 2023-11-14
US20210332016A1 (en) 2021-10-28
CA3174422A1 (en) 2021-10-21
WO2021212032A1 (en) 2021-10-21
US20220259158A1 (en) 2022-08-18
US20220073472A1 (en) 2022-03-10
JP2024110992A (ja) 2024-08-16
US11358938B2 (en) 2022-06-14
US20230104598A1 (en) 2023-04-06
US11242324B2 (en) 2022-02-08
AU2021255723A1 (en) 2022-12-08
US20240051926A1 (en) 2024-02-15

Similar Documents

Publication Publication Date Title
CN115916170A (zh) 固体形式的n-末端结构域雄激素受体抑制剂及其用途
US20240261282A1 (en) Pharmaceutical compositions and combinations comprising inhibitors of the androgen receptor and uses thereof
JP2022521824A (ja) アンドロゲン受容体の阻害剤を含む薬学的組成物及びその組み合わせならびにその使用
EA032596B1 (ru) Соли, способ их получения и их применение для лечения воспалительных заболеваний
CN101801381A (zh) 新型氨基甲酰基-环己烷衍生物的溶剂合物和结晶形式
US12509450B2 (en) Solid forms of a dual RAF/MEK inhibitor
BR112019018418A2 (pt) formas cristalinas do ácido obeticólico
TW201920160A (zh) ２－（５－（４－（２－嗎啉乙氧基）苯基）吡啶－２－基）－ｎ－芐乙醯胺之固態形式
JP7448541B2 (ja) 選択的エストロゲン受容体分解剤の新規な塩
US20240207264A1 (en) Pharmaceutical compositions comprising inhibitors of the androgen receptor and uses thereof
BR112017002449B1 (pt) Usos de isopropil éster de ácido (s)-(7-ciano-4-piridin-2-ilmetil-1,2,3,4-tetra-hidro-cilopenta [b]indol-2-i)-carbâmico, ou de um sal farmaceuticamente aceitável do mesmo
US12030886B2 (en) Form of ponatinib
JP2022524741A (ja) セリネクソールの共結晶形態
US20250188043A1 (en) Leflutrozole compositions of matter and processes for preparation
RU2802964C2 (ru) Твердые формы 2-(5-(4-(2-морфолиноэтокси)фенил)пиридин-2-ил)-n-бензилацетамида
RU2652377C2 (ru) Кристаллические формы (S)-4-амино-N-(1-(4-хлорфенил)-3-гидроксипропил)-1-(7Н-пирроло[2,3-d]пиримидин-4-ил)пиперидин-4-карбоксамида
JP2021522341A (ja) イソキノリノンの多形及びアモルファス形態ならびにその使用方法
HK1145148B (en) Solvate and crystalline forms of carbamoyl-cyclohexane derivatives

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
AD01 Patent right deemed abandoned
AD01 Patent right deemed abandoned

Effective date of abandoning: 20250829