EA032467B1 - Нестероидные антиандрогены и селективные модуляторы андрогеновых рецепторов с пиридильной группой - Google Patents

Нестероидные антиандрогены и селективные модуляторы андрогеновых рецепторов с пиридильной группой Download PDF

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Publication number
EA032467B1
EA032467B1 EA201691267A EA201691267A EA032467B1 EA 032467 B1 EA032467 B1 EA 032467B1 EA 201691267 A EA201691267 A EA 201691267A EA 201691267 A EA201691267 A EA 201691267A EA 032467 B1 EA032467 B1 EA 032467B1
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EA
Eurasian Patent Office
Prior art keywords
rug
compound
group
acetone
rat
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EA201691267A
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English (en)
Russian (ru)
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EA201691267A1 (ru
Inventor
Фернанд Лабри
Шанкар Мохан Сингх
Ричард Лабрек
Ливиу Константин Чобану
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Эндорешерш, Инк.
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Publication of EA201691267A1 publication Critical patent/EA201691267A1/ru
Publication of EA032467B1 publication Critical patent/EA032467B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
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    • A61K38/08—Peptides having 5 to 11 amino acids
    • A61K38/09—Luteinising hormone-releasing hormone [LHRH], i.e. Gonadotropin-releasing hormone [GnRH]; Related peptides
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    • 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
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

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  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
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  • Hematology (AREA)
  • Rheumatology (AREA)
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  • Gynecology & Obstetrics (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
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  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Emergency Medicine (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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EA201691267A 2013-12-19 2014-12-16 Нестероидные антиандрогены и селективные модуляторы андрогеновых рецепторов с пиридильной группой EA032467B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361918133P 2013-12-19 2013-12-19
US14/567,970 US9682960B2 (en) 2013-12-19 2014-12-11 Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety
PCT/CA2014/000894 WO2015089634A1 (en) 2013-12-19 2014-12-16 Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety

Publications (2)

Publication Number Publication Date
EA201691267A1 EA201691267A1 (ru) 2017-01-30
EA032467B1 true EA032467B1 (ru) 2019-05-31

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EA201691267A EA032467B1 (ru) 2013-12-19 2014-12-16 Нестероидные антиандрогены и селективные модуляторы андрогеновых рецепторов с пиридильной группой

Country Status (14)

Country Link
US (1) US9682960B2 (https=)
EP (1) EP3083590B1 (https=)
JP (2) JP6698022B2 (https=)
CN (1) CN105873917B (https=)
AR (1) AR098887A1 (https=)
AU (1) AU2014366802B2 (https=)
BR (1) BR112016014326B1 (https=)
CA (1) CA2933693C (https=)
DK (1) DK3083590T3 (https=)
EA (1) EA032467B1 (https=)
ES (1) ES2771748T3 (https=)
HU (1) HUE047975T2 (https=)
TW (1) TWI639585B (https=)
WO (1) WO2015089634A1 (https=)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9682960B2 (en) * 2013-12-19 2017-06-20 Endorecherche, Inc. Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety
AR103990A1 (es) 2015-01-09 2017-06-21 Bristol Myers Squibb Co Ureas cíclicas como inhibidoras de rock
TWI726969B (zh) 2016-01-11 2021-05-11 比利時商健生藥品公司 用作雄性激素受體拮抗劑之經取代之硫尿囊素衍生物
WO2018005533A1 (en) 2016-07-01 2018-01-04 G1 Therapeutics, Inc. Antiproliferative pyrimidine-based compounds
BR112020018094A2 (pt) 2018-03-08 2020-12-22 Incyte Corporation Compostos de aminopirazina diol como inibidores de pi3k-¿
CN108329236B (zh) * 2018-04-04 2020-12-29 盐城师范学院 一种恩杂鲁胺中间体的制备方法
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
JP2022547777A (ja) * 2019-09-06 2022-11-16 小野薬品工業株式会社 ヒダントイン誘導体
WO2025103470A1 (zh) * 2023-11-17 2025-05-22 中国药科大学 作为雄激素受体(ar)拮抗剂的化合物及其应用

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005049580A1 (en) * 2003-11-13 2005-06-02 Bristol-Myers Squibb Company Monocyclic n-aryl hydantoin modulators of androgen receptor function
WO2006133567A1 (en) * 2005-06-17 2006-12-21 Endorecherche, Inc. Helix 12 directed non-steroidal antiandrogens
CA2677295A1 (fr) * 2007-02-05 2008-09-18 Aventis Pharma S.A. Procede de preparation de sulfanylamides et sulfinamidines fluores et leurs utilisations
CA2773591A1 (en) * 2009-09-11 2011-03-17 Ulrich Luecking Substituted (heteroarylmethyl) thiohydantoins as anticancer drugs
WO2013067142A1 (en) * 2011-11-02 2013-05-10 Medivation Technologies, Inc. Compounds and treatment methods
WO2015018356A1 (zh) * 2013-08-08 2015-02-12 上海医药集团股份有限公司 二芳基乙内酰脲衍生物、其制备方法、药物组合物和应用

Family Cites Families (68)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3797494A (en) 1969-04-01 1974-03-19 Alza Corp Bandage for the administration of drug by controlled metering through microporous materials
US3742951A (en) 1971-08-09 1973-07-03 Alza Corp Bandage for controlled release of vasodilators
US4191775A (en) 1977-12-15 1980-03-04 Imperial Chemical Industries Limited Amide derivatives
ATE28864T1 (de) 1982-07-23 1987-08-15 Ici Plc Amide-derivate.
DE3333240A1 (de) 1983-09-12 1985-03-28 Schering AG, 1000 Berlin und 4709 Bergkamen Mittel zur transdermalen applikation von arzneimittelwirkstoffen
US4568343A (en) 1984-10-09 1986-02-04 Alza Corporation Skin permeation enhancer compositions
US4816258A (en) 1987-02-26 1989-03-28 Alza Corporation Transdermal contraceptive formulations
US5064654A (en) 1989-01-11 1991-11-12 Ciba-Geigy Corporation Mixed solvent mutually enhanced transdermal therapeutic system
US5071644A (en) 1990-08-07 1991-12-10 Mediventures, Inc. Topical drug delivery with thermo-irreversible gels
FR2671348B1 (fr) 1991-01-09 1993-03-26 Roussel Uclaf Nouvelles phenylimidazolidines, leur procede de preparation, leur application comme medicaments et les compositions pharmaceutiques les renfermant.
FR2693461B1 (fr) 1992-07-08 1994-09-02 Roussel Uclaf Nouvelles phénylimidazolidines substituées, leur procédé de préparation, leur application comme médicaments et les compositions pharmaceutiques les renfermant.
US5411981A (en) 1991-01-09 1995-05-02 Roussel Uclaf Phenylimidazolidines having antiandrogenic activity
FR2694290B1 (fr) 1992-07-08 1994-09-02 Roussel Uclaf Nouvelles phénylimidazolidines éventuellement substituées, leur procédé de préparation, leur application comme médicaments et les compositions pharmaceutiques les renfermant.
TW521073B (en) 1994-01-05 2003-02-21 Hoechst Marion Roussel Inc New optionally substituted phenylimidazolidines, their preparation process, their use as anti-androgenic agent and the pharmaceutical compositions containing them
EP1043325B1 (en) 1994-12-22 2004-06-16 Ligand Pharmaceuticals Incorporated Steroid receptor modulator compounds and methods
US5656651A (en) 1995-06-16 1997-08-12 Biophysica Inc. Androgenic directed compositions
FR2741342B1 (fr) 1995-11-22 1998-02-06 Roussel Uclaf Nouvelles phenylimidazolidines fluorees ou hydroxylees, procede, intermediaires de preparation, application comme medicaments, nouvelle utilisation et compositions pharmaceutiques
FR2742749B1 (fr) 1995-12-22 1998-02-06 Roussel Uclaf Nouvelles phenylimidazolidines comportant notamment un radical nitrooxy ou carbonyloxy, procede et intermediaires de preparation, application comme medicaments, nouvelles utilisations et compositions pharmaceutiques
US6071957A (en) 1996-11-27 2000-06-06 The University Of Tennessee Research Corporation Irreversible non-steroidal antagonist compound and its use in the treatment of prostate cancer
US7759520B2 (en) 1996-11-27 2010-07-20 University Of Tennessee Research Foundation Synthesis of selective androgen receptor modulators
US6160011A (en) 1997-05-30 2000-12-12 The University Of Tennessee Research Corporation Non-steroidal agonist compounds and their use in male hormone therapy
HUP0101809A3 (en) 1998-03-11 2002-07-29 Endorech Inc Sainte Foy Inhibitors of type 5 and type 3 17betha-hydroxysteroid dehydrogenase and methods for their use
US6184249B1 (en) 1998-12-18 2001-02-06 Biophysica, Inc. Androgen receptor suppressors in the therapy and diagnosis of prostate cancer, alopecia and other hyper-androgenic syndromes
US6566372B1 (en) 1999-08-27 2003-05-20 Ligand Pharmaceuticals Incorporated Bicyclic androgen and progesterone receptor modulator compounds and methods
JP2003508397A (ja) 1999-08-27 2003-03-04 リガンド・ファーマシューティカルズ・インコーポレイテッド アンドロゲンレセプターモジュレーターとしての８−置換−６−トリフルオロメチル−９−ピリド［３，２−ｇ］キノリン化合物
US20040077605A1 (en) 2001-06-20 2004-04-22 Salvati Mark E. Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
MXPA02012605A (es) 2000-06-28 2003-05-14 Squibb Bristol Myers Co Moduladores selectivos del receptor androgeno y metodo para su identificacion, dise°o y uso.
US7001911B2 (en) 2000-06-28 2006-02-21 Bristol-Myers Squibb Company Fused cyclic modulators of nuclear hormone receptor function
JP2002088073A (ja) 2000-09-08 2002-03-27 Yamanouchi Pharmaceut Co Ltd 抗アンドロゲン剤
WO2002024702A1 (en) 2000-09-19 2002-03-28 Bristol-Myers Squibb Company Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
US7803970B2 (en) 2002-02-28 2010-09-28 University Of Tennessee Research Foundation Multi-substitued selective androgen receptor modulators and methods of use thereof
US7405234B2 (en) 2002-05-17 2008-07-29 Bristol-Myers Squibb Company Bicyclic modulators of androgen receptor function
DE10322108B4 (de) 2003-05-09 2008-12-11 Bayer Schering Pharma Aktiengesellschaft Antiandrogene Pyrrolidine mit tumorhemmender Wirksamkeit
JP4664814B2 (ja) 2003-06-12 2011-04-06 中外製薬株式会社 イミダゾリジン誘導体
CN1835937B (zh) 2003-06-13 2012-07-18 詹森药业有限公司 作为选择性雄激素受体调节剂(sarms)的噻唑啉衍生物
US20050124625A1 (en) 2003-10-21 2005-06-09 Salvati Mark E. Piperazine derivatives and their use as modulators of nuclear hormone receptor function
RU2397176C2 (ru) 2004-01-07 2010-08-20 Эндорешерш, Инк. Стероидные фармацевтические продукты, направленные на спираль 12
CA2564953A1 (en) 2004-05-03 2005-11-24 Janssen Pharmaceutica N.V. Novel indole derivatives as selective androgen receptor modulators (sarms)
EP1756101A2 (en) 2004-05-17 2007-02-28 Acadia Pharmaceuticals Inc. Androgen receptor modulators and method of treating disease using the same
PL1753417T3 (pl) 2004-06-07 2012-09-28 Univ Tennessee Res Found Selektywny modulator receptora androgenowego i jego zastosowania medyczne
NZ564223A (en) 2005-05-13 2011-03-31 Univ California Diarylhydantoin compounds for treating hormone refractory prostate cancer
AR057656A1 (es) 2005-07-01 2007-12-12 Ligand Pharm Inc Compuestos moduladores de receptores de androgeno y metodods relacionados
WO2007127010A2 (en) 2006-03-29 2007-11-08 The Regents Of The University Of California Diarylthiohydantoin compounds
EP2061767B1 (de) * 2006-08-08 2014-12-17 Sanofi Arylaminoaryl-alkyl-substituierte Imidazolidin-2,4-dione, Verfahren zu ihrer Herstellung, diese Verbindungen enthaltende Arzneimittel und ihre Verwendung
CN101501005A (zh) * 2006-08-08 2009-08-05 塞诺菲-安万特股份有限公司 芳基氨基芳基-烷基-取代的咪唑烷-2,4-二酮类、其制备方法、包含这些化合物的药物以及其用途
WO2008044033A1 (en) 2006-10-11 2008-04-17 Astrazeneca Ab Amide derivatives
WO2008124000A2 (en) 2007-04-02 2008-10-16 Ligand Pharmaceuticals Incorporated Thiazole derivatives as androgen receptor modulator compounds
US9284345B2 (en) 2007-04-12 2016-03-15 Endorecherche, Inc. 17alpha-substituted steroids as systemic antiandrogens and selective androgen receptor modulators
EP2620432A3 (en) 2007-10-26 2013-12-18 The Regents Of the University of California Diarylhydantoin compounds
ES2389752T3 (es) 2007-12-14 2012-10-31 Ardea Biosciences, Inc. Inhibidores de la transcriptasa inversa
PE20091653A1 (es) 2008-03-26 2009-11-14 Takeda Pharmaceutical Derivados sustituidos de pirazol y su uso
US8710086B2 (en) 2009-04-09 2014-04-29 Medivation Technologies, Inc. Substituted di-arylhydantoin and di-arylthiohydantoin compounds and methods of use thereof
WO2010116342A2 (en) 2009-04-10 2010-10-14 Consiglio Nazionale Delle Ricerche Non-steroidal compounds for androgen receptor modulation
WO2010143803A2 (en) 2009-06-08 2010-12-16 Industry Foundation Of Chonnam National University New nicotinamide derivatives with anti-androgen effects, processes of preparing, and antiandrogens comprising the same
US8450374B2 (en) 2009-06-29 2013-05-28 University Of Delaware Pan-antagonists for the androgen receptor and androgen receptor mutants associated with anti-androgen withdrawal
AU2011212813B2 (en) 2010-02-04 2014-10-23 Radius Health, Inc. Selective androgen receptor modulators
AU2011218173C1 (en) * 2010-02-16 2015-04-16 Aragon Pharmaceuticals, Inc. Androgen receptor modulators and uses thereof
US8642632B2 (en) 2010-07-02 2014-02-04 Radius Health, Inc. Selective androgen receptor modulators
US9133182B2 (en) 2010-09-28 2015-09-15 Radius Health, Inc. Selective androgen receptor modulators
WO2012050868A1 (en) 2010-09-28 2012-04-19 Georgia Tech Research Corporation Histone deacetylase (hdac) inhibitors targeting prostate tumors and methods of making and using thereof
EA201390598A1 (ru) 2010-10-22 2013-08-30 Астеллас Фарма Инк. Антагонист мутантного андрогенного рецептора
WO2012143599A1 (en) 2011-04-21 2012-10-26 Orion Corporation Androgen receptor modulating carboxamides
AU2012288457B2 (en) 2011-07-27 2016-03-24 Novartis Ag Pyrazoline derivatives and their use as selective androgen receptor modulators
AR088082A1 (es) 2011-10-13 2014-05-07 Lilly Co Eli Moduladores selectivos del receptor androgeno
FI20116033A7 (fi) 2011-10-18 2013-04-19 Juha Pulkkinen Uudet ei-steroidiset yhdisteet androgeenireseptorin muuntelijoina
UY34646A (es) 2012-03-02 2013-10-31 Novartis Ag Compuestos de espirohidantoína y su uso como moduladores selectivos del receptor de andrógenos
EP2834216A1 (en) 2012-04-04 2015-02-11 Catylix Inc. Selective androgen receptor modulators
US9682960B2 (en) * 2013-12-19 2017-06-20 Endorecherche, Inc. Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005049580A1 (en) * 2003-11-13 2005-06-02 Bristol-Myers Squibb Company Monocyclic n-aryl hydantoin modulators of androgen receptor function
WO2006133567A1 (en) * 2005-06-17 2006-12-21 Endorecherche, Inc. Helix 12 directed non-steroidal antiandrogens
CA2677295A1 (fr) * 2007-02-05 2008-09-18 Aventis Pharma S.A. Procede de preparation de sulfanylamides et sulfinamidines fluores et leurs utilisations
CA2773591A1 (en) * 2009-09-11 2011-03-17 Ulrich Luecking Substituted (heteroarylmethyl) thiohydantoins as anticancer drugs
WO2013067142A1 (en) * 2011-11-02 2013-05-10 Medivation Technologies, Inc. Compounds and treatment methods
WO2015018356A1 (zh) * 2013-08-08 2015-02-12 上海医药集团股份有限公司 二芳基乙内酰脲衍生物、其制备方法、药物组合物和应用

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
D. Lesuisse et al., Bioorg. Med. Lett., 21 (2011), p. 2224-2228 *

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