MX392906B - Derivados de bisfenol y su uso como moduladores de la actividad del receptor de androgeno. - Google Patents

Derivados de bisfenol y su uso como moduladores de la actividad del receptor de androgeno.

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Publication number
MX392906B
MX392906B MX2018012619A MX2018012619A MX392906B MX 392906 B MX392906 B MX 392906B MX 2018012619 A MX2018012619 A MX 2018012619A MX 2018012619 A MX2018012619 A MX 2018012619A MX 392906 B MX392906 B MX 392906B
Authority
MX
Mexico
Prior art keywords
sup
androgen receptor
receptor activity
modulators
bisphenol derivatives
Prior art date
Application number
MX2018012619A
Other languages
English (en)
Other versions
MX2018012619A (es
Inventor
Carmen Adriana Banuelos
Jun Wang
Kunzhong Jian
Marianne Dorothy Sadar
Nasrin R Mawil
Raymond Andersen
Yu- Chi Yang
Original Assignee
British Columbia Cancer Agency Branch
Univ British Columbia
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 British Columbia Cancer Agency Branch, Univ British Columbia filed Critical British Columbia Cancer Agency Branch
Publication of MX2018012619A publication Critical patent/MX2018012619A/es
Publication of MX392906B publication Critical patent/MX392906B/es

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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
    • A61K31/075—Ethers or acetals
    • A61K31/085—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon
    • A61K31/09—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon having two or more such linkages
    • 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
    • A61K31/095—Sulfur, selenium, or tellurium compounds, e.g. thiols
    • A61K31/10—Sulfides; Sulfoxides; Sulfones
    • 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
    • A61K31/13—Amines
    • A61K31/145—Amines having sulfur, e.g. thiurams (>N—C(S)—S—C(S)—N< and >N—C(S)—S—S—C(S)—N<), Sulfinylamines (—N=SO), Sulfonylamines (—N=SO2)
    • A—HUMAN NECESSITIES
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    • 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
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/222—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
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    • 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
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
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    • C07C217/02—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C217/04—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C217/28—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having one amino group and at least two singly-bound oxygen atoms, with at least one being part of an etherified hydroxy group, bound to the carbon skeleton, e.g. ethers of polyhydroxy amines
    • C07C217/30—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having one amino group and at least two singly-bound oxygen atoms, with at least one being part of an etherified hydroxy group, bound to the carbon skeleton, e.g. ethers of polyhydroxy amines having the oxygen atom of at least one of the etherified hydroxy groups further bound to a carbon atom of a six-membered aromatic ring
    • C07C217/32—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having one amino group and at least two singly-bound oxygen atoms, with at least one being part of an etherified hydroxy group, bound to the carbon skeleton, e.g. ethers of polyhydroxy amines having the oxygen atom of at least one of the etherified hydroxy groups further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted
    • C07C217/36—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having one amino group and at least two singly-bound oxygen atoms, with at least one being part of an etherified hydroxy group, bound to the carbon skeleton, e.g. ethers of polyhydroxy amines having the oxygen atom of at least one of the etherified hydroxy groups further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted by carbon atoms having at least two bonds to oxygen atoms
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    • C07C233/17—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/18—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
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    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/03—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
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    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
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    • C07C311/05—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms to acyclic carbon atoms of hydrocarbon radicals substituted by nitrogen atoms, not being part of nitro or nitroso groups
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    • C07C43/20—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
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    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
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    • C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain

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  • Chemical & Material Sciences (AREA)
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  • Health & Medical Sciences (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Medicinal Chemistry (AREA)
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  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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Abstract

Se proporcionan los compuestos que tienen una estructura de la Fórmula I: (ver Fórmula) o una sal, tautómero o estereoisómero farmacéuticamente aceptable de estos, donde R1, R2, R3, R11a, R11b, R11c, R11d, y X, son tal como se definen en la. También se proporcionan usos de tales compuestos para modular la actividad del receptor de andrógeno, diagnósticos por imaginología de cáncer y terapéutica, y métodos para el tratamiento de sujetos que lo necesitan, que incluye el cáncer de próstata.
MX2018012619A 2016-04-15 2017-04-18 Derivados de bisfenol y su uso como moduladores de la actividad del receptor de androgeno. MX392906B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662323196P 2016-04-15 2016-04-15
PCT/CA2017/000083 WO2017177307A1 (en) 2016-04-15 2017-04-18 Bisphenol derivatives and their use as androgen receptor activity modulators

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MX2018012619A MX2018012619A (es) 2019-06-24
MX392906B true MX392906B (es) 2025-03-24

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US (4) US20170298033A1 (es)
EP (1) EP3442942B1 (es)
JP (2) JP7142577B2 (es)
KR (1) KR102409651B1 (es)
CN (2) CN119143585A (es)
AU (1) AU2017250025B2 (es)
BR (1) BR112018071183B1 (es)
CA (1) CA3021008A1 (es)
ES (1) ES2969445T3 (es)
IL (1) IL262338B (es)
MX (1) MX392906B (es)
NZ (1) NZ748200A (es)
RU (1) RU2767257C2 (es)
WO (1) WO2017177307A1 (es)

Families Citing this family (15)

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Publication number Priority date Publication date Assignee Title
HUE057962T2 (hu) 2015-01-13 2022-06-28 British Columbia Cancer Agency Branch Heterociklusos vegyületek rák képalkotására és kezelésére és eljárás ezek alkalamzására
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
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
US11485713B2 (en) 2018-05-25 2022-11-01 Essa Pharma, Inc. Androgen receptor modulators and methods for their use
US20200123117A1 (en) * 2018-10-18 2020-04-23 Essa Pharma, Inc. Androgen receptor modulators and methods for their use
CA3134545A1 (en) * 2019-03-28 2020-10-01 Essa Pharma, Inc. Pharmaceutical compositions and combinations comprising inhibitors of the androgen receptor and uses thereof
US12109179B2 (en) 2019-03-28 2024-10-08 Essa Pharma Inc. Pharmaceutical compositions and combinations comprising inhibitors of the androgen receptor and uses thereof
CN112457366B (zh) * 2019-09-06 2024-03-19 江西济民可信集团有限公司 作为蛋白降解剂的并环类化合物及其制备方法和应用
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
US12152035B2 (en) 2020-12-30 2024-11-26 Industrial Technology Research Institute Androgen receptor binding molecule and use thereof
CN113648418B (zh) * 2021-05-08 2022-08-05 南方医科大学 Apelin-APJ抑制剂在制备治疗血睾屏障损伤药物中的应用
KR20220157096A (ko) * 2021-05-20 2022-11-29 연세대학교 산학협력단 암의 예방, 개선 또는 치료용 조성물
KR20220157089A (ko) * 2021-05-20 2022-11-29 연세대학교 산학협력단 암의 예방, 개선 또는 치료용 조성물
WO2023046283A1 (en) 2021-09-22 2023-03-30 Fundació Institut De Recerca Biomèdica (Irb Barcelona) Compounds and their use in a method for modulating ar (androgen receptor) transcriptional activity

Family Cites Families (99)

* 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
EP0056175B1 (en) 1981-01-13 1985-05-02 Teijin Limited Ion-permeable composite membrane and its use in selective separation
IN169231B (es) * 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
EP0290860B1 (en) 1987-04-27 1995-01-25 Mitsubishi Gas Chemical Company, Inc. Thermosetting resin composition
US5155196A (en) 1987-06-01 1992-10-13 The Dow Chemical Company Polymer resulting from the cure of a preformed chromene-containing mixture
WO1988009782A1 (en) 1987-06-01 1988-12-15 The Dow Chemical Company Process for making propargyl ethers of hydroxyaromatic compounds
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
FI972235A7 (fi) 1994-11-29 1997-05-27 Hoechst Marion Roussel Inc Inc Menetelmä triaryylietyleenijohdannaisten käyttämiseksi osteoporoosin h oidossa ja ehkäisyssä
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
WO2000001813A2 (en) 1998-06-30 2000-01-13 The University Of British Columbia Peptide 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
JP2003511467A (ja) 1999-10-14 2003-03-25 ブリストル−マイヤーズ スクイブ カンパニー アンドロゲンレセプターリガンド結合ドメインの結晶構造
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
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
HRP20050038A2 (en) 2002-06-17 2005-08-31 University Of Tennessee Research Foundation N-bridged selective androgen receptor modulators and methods of use thereof
GB0324551D0 (en) 2003-10-21 2003-11-26 Karobio Ab Novel compounds
JP4589337B2 (ja) 2003-11-20 2010-12-01 イーライ リリー アンド カンパニー ビタミン受容体調節剤
WO2005077967A1 (en) 2004-02-13 2005-08-25 The University Of British Columbia Radiolabeled compounds and compositions, their precursors and methods for their production
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
BRPI0514405A (pt) 2004-08-18 2008-06-10 Warner Lambert Co moduladores de androgênio
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
PT1861365E (pt) 2005-03-15 2009-09-22 4Sc Ag N-sulfonilpirroles e a sua utilização como inibidores de histona-desacetilase
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
DK1976828T3 (en) 2005-12-29 2017-03-06 Celtaxsys Inc DIAMINE DERIVATIVES AS INhibitors of Leukotriene A4 HYDROLASE
LT2656841T (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
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
EP2139878A2 (en) 2007-02-20 2010-01-06 Basf Se High refractive index monomers, compositions and uses thereof
KR20110044216A (ko) 2008-07-02 2011-04-28 브리티쉬 콜롬비아 캔써 에이전시 브랜치 디글리시드 에테르 유도체 치료법 및 이의 사용 방법
US8455477B2 (en) 2008-08-05 2013-06-04 Merck Sharp & Dohme Corp. Therapeutic compounds
CA2786319C (en) 2010-01-06 2019-03-12 British Columbia Cancer Agency Branch 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
WO2012145330A1 (en) 2011-04-18 2012-10-26 The University Of British Columbia Fluorene-9-bisphenol compounds and methods for their use
WO2012145328A1 (en) 2011-04-18 2012-10-26 The University Of British Columbia Dibenzylphenyl compounds and methods for their use
ES2613098T3 (es) 2011-08-19 2017-05-22 British Columbia Cancer Agency Branch Compuestos de éter de bisfenol fluorado y métodos para su uso
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
PL2872482T3 (pl) 2012-07-13 2021-03-08 Oncternal Therapeutics, Inc. Sposób leczenia raków sutka z użyciem selektywnego modulatora receptora androgenowego (sarm)
JOP20130273B1 (ar) 2012-09-11 2021-08-17 Genzyme Corp مثبطات انزيم (سينثاز) غلوكوسيل سيراميد
MX347705B (es) 2013-05-10 2017-05-09 British Columbia Cancer Agency Branch Derivados de ester moduladores del receptor de androgeno y metodos para su uso.
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
US9375496B2 (en) * 2013-09-09 2016-06-28 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
WO2016058080A1 (en) 2014-10-14 2016-04-21 British Columbia Cancer Agency Branch Fluoro-chloro bisphenol ether compounds and methods for their use
WO2016058082A1 (en) 2014-10-14 2016-04-21 British Columbia Cancer Agency Branch 18f compounds for cancer imaging and methods for their use
HUE057962T2 (hu) 2015-01-13 2022-06-28 British Columbia Cancer Agency Branch Heterociklusos vegyületek rák képalkotására és kezelésére és eljárás ezek alkalamzására
US10471023B2 (en) 2015-03-12 2019-11-12 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
US20170298033A1 (en) 2016-04-15 2017-10-19 The University Of British Columbia Bisphenol derivatives and their use as androgen receptor activity modulators
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
SMT202200199T1 (it) 2016-06-22 2022-07-21 Ellipses Pharma Ltd Metodi di trattamento del cancro del seno 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
US11485713B2 (en) 2018-05-25 2022-11-01 Essa Pharma, Inc. Androgen receptor modulators and methods for their use
US20200123117A1 (en) 2018-10-18 2020-04-23 Essa Pharma, Inc. Androgen receptor modulators and methods for their use
JP2022510410A (ja) 2018-12-07 2022-01-26 スミトモ ダイニッポン ファーマ オンコロジー， インコーポレイテッド 去勢抵抗性および去勢感受性前立腺がんを処置するための方法
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
US12109179B2 (en) 2019-03-28 2024-10-08 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

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