[go: up one dir, main page]

PE20121470A1 - Compuestos de diarilhidantoina como antagonistas del receptor de androgeno - Google Patents

Compuestos de diarilhidantoina como antagonistas del receptor de androgeno

Info

Publication number
PE20121470A1
PE20121470A1 PE2012000638A PE2012000638A PE20121470A1 PE 20121470 A1 PE20121470 A1 PE 20121470A1 PE 2012000638 A PE2012000638 A PE 2012000638A PE 2012000638 A PE2012000638 A PE 2012000638A PE 20121470 A1 PE20121470 A1 PE 20121470A1
Authority
PE
Peru
Prior art keywords
thioxo
oxo
trifluoromethyl
phenyl
androgen receptor
Prior art date
Application number
PE2012000638A
Other languages
English (en)
Inventor
Michael E Jung
Dongwon Yoo
Charles L Sawyers
Chris Tran
Original Assignee
Univ California
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 Univ California filed Critical Univ California
Publication of PE20121470A1 publication Critical patent/PE20121470A1/es

Links

Classifications

    • 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
    • C07D403/10—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 carbon chain containing aromatic 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
    • A61K31/4164—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
    • 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
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/86—Oxygen and sulfur atoms, e.g. thiohydantoin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Investigating Or Analysing Biological Materials (AREA)

Abstract

SE REFIERE A UN COMPUESTO DERIVADO DE DIARILHIDANTOINA DE FORMULA (I) DONDE: R1 Y R2 JUNTOS COMPRENDEN DE 2-8 ATOMOS DE CARBONO Y SON INDEPENDIENTEMENTE UN GRUPO ALQUILO C1-8 O UN GRUPO ALQUILO C1-8 SUSTITUIDO CON UN SUSTIUYENTE SELECCIONADO DE HIDROXI, BROMO, FLUORO, CLORO, ENTRE OTROS; R3 ES H Y FORMILO; R4 ES H, F, Cl, Br Y I.; R11 Y R12 SON INDEPENDIENTEMENTE H Y METILO. SON COMPUESTOS PREFERIDOS: 4-(3-(4-(3-CIANOPROPIL)FENIL)-4,4-DIMETIL-5-OXO-2-TIOXO-IMIDAZOLIN-1-IL)-2-(TRIFLUOROMETIL)BENZONITRILO; 4-(8-OXO-5-(4-(4-OXOBUTIL)FENIL)-6-TIOXO-5,7-DIAZASPIRO[3.4]OCTAN-7-IL)-2-(TRIFLUOROMETIL)BENZONITRILO; 4-(4-(7-(4-CIANO-3-(TRIFLUOROMETIL)FENIL)-8-OXO-6-TIOXO-5,7-DIAZASPIRO[3.4]OCT-AN-5-IL)-2-FLUOROFENIL)-2,2-DIMETIL-N-METIBUTANAMIDA; ENTRE OTROS. REFERIDA ADEMAS A UNA COMPOSICION FARMACEUTICA. DICHO COMPUESTO ES UN ANTAGONISTA DEL RECEPTOR DE ANDROGENO SIENDO UTIL EN EL TRATAMIENTO DE CANCER DE PROSTATA REFRACTARIO A LA HORMONA
PE2012000638A 2007-10-26 2008-10-24 Compuestos de diarilhidantoina como antagonistas del receptor de androgeno PE20121470A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US99607607P 2007-10-26 2007-10-26

Publications (1)

Publication Number Publication Date
PE20121470A1 true PE20121470A1 (es) 2012-11-18

Family

ID=40278902

Family Applications (3)

Application Number Title Priority Date Filing Date
PE2012000638A PE20121470A1 (es) 2007-10-26 2008-10-24 Compuestos de diarilhidantoina como antagonistas del receptor de androgeno
PE2017000081A PE20170428A1 (es) 2007-10-26 2008-10-24 Compuestos de diarilhidantoina
PE2008001821A PE20091262A1 (es) 2007-10-26 2008-10-24 Compuestos de diarilhidantoina como antagonistas del receptor de androgeno

Family Applications After (2)

Application Number Title Priority Date Filing Date
PE2017000081A PE20170428A1 (es) 2007-10-26 2008-10-24 Compuestos de diarilhidantoina
PE2008001821A PE20091262A1 (es) 2007-10-26 2008-10-24 Compuestos de diarilhidantoina como antagonistas del receptor de androgeno

Country Status (10)

Country Link
US (2) US8680291B2 (es)
EP (3) EP2220050A2 (es)
JP (4) JP5535925B2 (es)
AR (1) AR069039A1 (es)
CA (2) CA2703635C (es)
CL (1) CL2008003158A1 (es)
PE (3) PE20121470A1 (es)
TW (3) TW201716385A (es)
UY (1) UY31432A1 (es)
WO (1) WO2009055053A2 (es)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7709517B2 (en) 2005-05-13 2010-05-04 The Regents Of The University Of California Diarylhydantoin compounds
CN101460467B (zh) 2006-03-29 2012-09-19 加利福尼亚大学董事会 二芳基硫代乙内酰脲化合物
UY31432A1 (es) 2007-10-26 2009-05-29 Compuestos de diarilhidantoina
CA2753425A1 (en) 2009-02-24 2010-09-02 Medivation Prostate Therapeutics, Inc. Specific diarylhydantoin and diarylthiohydantoin compounds
EP2416657A4 (en) * 2009-04-09 2012-09-05 Medivation Prostate Therapeutics Inc COMPOUNDS COMPRISING SUBSTITUTED DI-ARYLHYDANTOIDS AND DI-ARYLTHIOHYDANTOINES AND METHODS OF USE THEREOF
CA2772579C (en) * 2009-09-10 2015-12-08 Youzhi Tong Thioimidazolidinone androgen receptor antagonists and uses thereof
TW201111378A (en) 2009-09-11 2011-04-01 Bayer Schering Pharma Ag Substituted (heteroarylmethyl) thiohydantoins
WO2011044327A1 (en) * 2009-10-07 2011-04-14 Medivation Prostate Therapeutics, Inc. Substituted phenylcarbamoyl alkylamino arene compounds and n,n'-bis-arylurea compounds
AR078793A1 (es) 2009-10-27 2011-12-07 Orion Corp Derivados de carboxamidas no esteroidales y acil hidrazona moduladores de receptores androgenicos de tejido selectivo (sarm), composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del cancer de prostata entre otros
EA028869B1 (ru) * 2010-02-16 2018-01-31 Арагон Фармасьютикалс, Инк. Модуляторы рецептора андрогенов и их применение
SI2538785T1 (en) 2010-02-24 2018-05-31 Medivation Prostate Therapeutics Llc Methods for the synthesis of diarylthiohidantoin and diarylhydantoin compounds
MX2012013855A (es) * 2010-05-28 2013-04-08 Univ Texas Compuestos de oligobenzamida y su uso.
EP2646553A4 (en) * 2010-11-12 2015-01-07 Santaris Pharma As COMPOSITIONS AND METHODS OF TREATING ANDROGEN RECEPTOR DEPENDENT DISORDERS INCLUDING CANCER
RU2598854C2 (ru) * 2011-03-10 2016-09-27 Сучжоу Кинтор Фармасьютикалз, Инк. Производные тиогидантоина, полезные в качестве антагонистов рецептора андрогена
ES2541295T3 (es) 2011-04-21 2015-07-17 Orion Corporation Carboxamidas que modulan el receptor de andrógenos
CN103997894B (zh) 2011-07-29 2016-08-24 麦迪韦逊前列腺治疗股份有限公司 乳癌的治疗
UY34646A (es) 2012-03-02 2013-10-31 Novartis Ag Compuestos de espirohidantoína y su uso como moduladores selectivos del receptor de andrógenos
HUE032306T2 (en) 2012-06-26 2017-09-28 Bayer Pharma AG N- [4- (quinolin-4-yloxy) cyclohexyl (methyl)] (hetero) arylcarboxamides as androgen receptor antagonists, their production and use as pharmaceutical products
MY180834A (en) 2012-09-26 2020-12-10 Aragon Pharmaceuticals Inc Anti-androgens for the treatment of non-metastatic castrate-resistant prostate cancer
JOP20200097A1 (ar) 2013-01-15 2017-06-16 Aragon Pharmaceuticals Inc معدل مستقبل أندروجين واستخداماته
US9682960B2 (en) 2013-12-19 2017-06-20 Endorecherche, Inc. Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety
BR112017012142A2 (pt) 2014-12-12 2018-01-02 Medivation Prostate Therapeutics Inc método para predição da resposta a agentes terapêuticos para o câncer de mama e método de tratamento de câncer de mama
CN106146403B (zh) * 2015-04-02 2018-11-20 正大天晴药业集团股份有限公司 一种恩杂鲁胺的纯化方法
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
MX2020003845A (es) 2017-10-16 2020-11-06 Aragon Pharmaceuticals Inc Antiandrógenos para el tratamiento de cáncer de próstata no metastásico resistente a la castración.
US20210386826A1 (en) 2018-11-05 2021-12-16 Pfizer Inc. Combination for Treating Cancer
EP4313034A1 (en) 2021-03-24 2024-02-07 Pfizer Inc. Combination of talazoparib and an anti-androgen for the treatment of ddr gene mutated metastatic castration-sensitive prostate cancer
CN115181043B (zh) * 2022-07-27 2024-05-07 爱斯特（成都）生物制药股份有限公司 一种连续流制备4-异硫氰基-2-(三氟甲基)苯甲腈的方法

Family Cites Families (137)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US750351A (en) * 1904-01-26 Smoke-purifier
US756552A (en) * 1898-04-14 1904-04-05 Robert Adams Window-sash.
US680835A (en) * 1900-07-05 1901-08-20 Joseph A Beamisderfer Nut-lock.
US2004100A (en) 1934-05-25 1935-06-11 Carter Loran Everett Brush and stubble cutter
JPS4916937B1 (es) 1970-01-21 1974-04-25
JPS4920973B1 (es) 1970-05-28 1974-05-29
US3823240A (en) 1970-10-06 1974-07-09 Rhone Poulenc Sa Fungicidal hydantoin derivatives
JPS4887030U (es) 1972-01-27 1973-10-22
US3923994A (en) 1973-07-13 1975-12-02 Smithkline Corp Anti-arthritic compositions comprising a 3-aryl 2-thiohydantoin and methods of producing anti-arthritic acitvity
GB1472467A (en) 1974-04-19 1977-05-04 Wyeth John & Brother Ltd Thiohydantoins
FR2329276A1 (fr) 1975-10-29 1977-05-27 Roussel Uclaf Nouvelles imidazolidines substituees, procede de preparation, application comme medicament et compositions les renfermant
US3970662A (en) 1975-06-19 1976-07-20 Sterling Drug Inc. 4-(3-Nitrophenyl)-2,3,5,6-pyridinetetracarboxylic acid and intermediates
DE2614831A1 (de) 1976-04-06 1977-10-20 Bayer Ag 1,3,4-thiadiazolylderivate, verfahren zu ihrer herstellung sowie ihre verwendung als herbizide
MC1220A1 (fr) 1977-10-28 1979-07-20 Hoffmann La Roche Nouveaux derives d'imidazolidine
CA1138334A (en) 1977-10-28 1982-12-28 Karl Bernauer Pharmaceutical preparations containing certain urea derivatives
AU531493B2 (en) 1977-12-01 1983-08-25 The Wellcome Foundation Limited Thiohydantion derivatives
EP0004723A1 (en) 1978-03-30 1979-10-17 Beecham Group Plc Deoxyhydantoins, processes for their preparation and pharmaceutical compositions containing them
FR2449448B1 (fr) 1979-02-20 1983-05-27 Inst Nat Radio Elements Composition pharmaceutique comprenant un derive de phenylhydantoine, derives mis en oeuvre et leur preparation
FI801184A7 (fi) 1979-04-24 1981-01-01 F Hoffmann La Roche & Co Menetelmä imidatsolidiini-johdannaisten valmistamiseksi.
US4399216A (en) 1980-02-25 1983-08-16 The Trustees Of Columbia University Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials
NZ197008A (en) 1980-05-22 1984-10-19 Ici Ltd Acylanilide derivatives and pharmaceutical compositions
JPS57197268A (en) 1981-05-29 1982-12-03 Sumitomo Chem Co Ltd Substituted phenylhydantoin derivative, its preparation, and herbicide containing the same as active ingredient
US4753957A (en) 1981-09-28 1988-06-28 Rohm And Haas Company Substituted 2,4-imidazolidinediones and fungicidal compositions
EP0091596B1 (de) 1982-04-08 1991-09-11 Shell Internationale Researchmaatschappij B.V. Neue Hydantoine, ihre Herstellung und Verwendung
US4432987A (en) 1982-04-23 1984-02-21 Pfizer Inc. Crystalline benzenesulfonate salts of sultamicillin
EP0100172B1 (en) 1982-07-23 1987-08-12 Imperial Chemical Industries Plc Amide derivatives
US4473393A (en) 1982-08-06 1984-09-25 Buffalo Color Corporation Pesticidal thiohydantoin compositions
US4559157A (en) 1983-04-21 1985-12-17 Creative Products Resource Associates, Ltd. Cosmetic applicator useful for skin moisturizing
JPS59210083A (ja) 1983-05-13 1984-11-28 Otsuka Chem Co Ltd １，３，４−チアジアゾ−ル−５−オン誘導体、その製造法及び該誘導体を有効成分とする除草剤
LU84979A1 (fr) 1983-08-30 1985-04-24 Oreal Composition cosmetique ou pharmaceutique sous forme aqueuse ou anhydre dont la phase grasse contient un polyether oligomere et polyethers oligomeres nouveaux
JPS6092285A (ja) 1983-10-26 1985-05-23 Shionogi & Co Ltd イソオキサゾ−ル系環状尿素類
GB8513754D0 (en) 1985-05-31 1985-07-03 Jones T R Anti-cancer quinazoline derivatives
DE3604042A1 (de) 1986-02-08 1987-08-13 Hoechst Ag Imidazolidin(thi)on-derivate, verfahren zu ihrer herstellung sowie ihre verwendung im pflanzenschutz
US5071773A (en) 1986-10-24 1991-12-10 The Salk Institute For Biological Studies Hormone receptor-related bioassays
US5084472A (en) 1986-11-04 1992-01-28 Roussel Application of 1-(3'-trifluoromethyl-4'-nitrophenyl)-4,4'-dimethylimidazoline 2,5-dione in the treatment of hormone-dependent cancers other than that of the prostate
US4820508A (en) 1987-06-23 1989-04-11 Neutrogena Corporation Skin protective composition
US4859228A (en) 1987-07-16 1989-08-22 Ici Americas Inc Novel 5-aminomethylene-2,4-imidazolidinediones and 5-aminomethylene-2-thionoimidazolidine-4-ones
US5010182A (en) 1987-07-28 1991-04-23 Chiron Corporation DNA constructs containing a Kluyveromyces alpha factor leader sequence for directing secretion of heterologous polypeptides
FR2619381B1 (fr) 1987-08-13 1989-12-08 Roussel Uclaf Nouvelles imidazolidines substituees par un radical hydroxymethyle et un radical phenyl substitue, leur procede de preparation, leur application comme medicaments, les compositions pharmaceutiques les renfermant et un intermediaire pour leur preparation
CA1331757C (en) 1988-02-29 1994-08-30 Janssen Pharmaceutica Naamloze Vennootschap 5-lipoxygenase inhibiting 4-(4-phenyl-1-piperazinyl)phenols
US5614620A (en) 1988-03-30 1997-03-25 Arch Development Corporation DNA binding proteins including androgen receptor
US4992478A (en) 1988-04-04 1991-02-12 Warner-Lambert Company Antiinflammatory skin moisturizing composition and method of preparing same
US6307030B1 (en) 1988-04-15 2001-10-23 The University Of North Carolina At Chapel Hill Androgen receptor proteins, recombinant DNA molecules coding for such, and use of such compositions
JPH0219363A (ja) 1988-07-06 1990-01-23 Fujisawa Pharmaceut Co Ltd イミダゾリジン誘導体
AU4005289A (en) 1988-08-25 1990-03-01 Smithkline Beecham Corporation Recombinant saccharomyces
US4938949A (en) 1988-09-12 1990-07-03 University Of New York Treatment of damaged bone marrow and dosage units therefor
DE3835168A1 (de) 1988-10-15 1990-04-19 Bayer Ag N-aryl-stickstoffheterocyclen, mehrere verfahren zu ihrer herstellung und ihre verwendung als herbizide
FR2646437B1 (fr) 1989-04-28 1991-08-30 Transgene Sa Nouvelles sequences d'adn, leur application en tant que sequence codant pour un peptide signal pour la secretion de proteines matures par des levures recombinantes, cassettes d'expression, levures transformees et procede de preparation de proteines correspondant
FR2656302B1 (fr) 1989-12-22 1992-05-07 Roussel Uclaf Nouveau procede de preparation de l'anandron et derives de l'anandron.
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.
USRE35956E (en) 1991-01-09 1998-11-10 Roussel Uclaf Phenylimidazolidines having antiandrogenic activity
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.
US5411981A (en) 1991-01-09 1995-05-02 Roussel Uclaf Phenylimidazolidines having antiandrogenic activity
US5346913A (en) 1992-05-26 1994-09-13 Rohm And Haas Company N-iodopropargyl hydantoin compounds, compositions, preparation, and use as antimicrobial agents
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.
FR2715402B1 (fr) 1994-01-05 1996-10-04 Roussel Uclaf Nouvelles phénylimidazolines éventuellement substituées, leur procédé et des intermédiaires 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
WO1995019770A1 (en) 1994-01-21 1995-07-27 Sepracor, Inc. Methods and compositions for treating androgen-dependent diseases using optically pure r-(-)-casodex
WO1996004248A1 (en) 1994-07-29 1996-02-15 Suntory Limited Imidazolidine derivative and use thereof
FR2725206B1 (fr) 1994-09-29 1996-12-06 Roussel Uclaf Nouvelles imidazolidines substituees par un heterocycle, leur procede et des intermediaires de preparation, leur application comme medicaments et les compositions pharmaceutiques les renfermant
US5656651A (en) 1995-06-16 1997-08-12 Biophysica Inc. Androgenic directed compositions
ATE459361T1 (de) 1995-09-07 2010-03-15 Univ Georgia Therapeutische azidverbindungen
DE19540027A1 (de) 1995-10-27 1997-04-30 Gruenenthal Gmbh Substituierte Imidazolidin-2,4-dion-Verbindungen als pharmazeutische Wirkstoffe
FR2741346B1 (fr) 1995-11-16 1997-12-19 Roussel Uclaf Nouveau procede de preparation de derives phenylimidazolidine
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
EP0876354A1 (en) 1995-11-28 1998-11-11 American Home Products Corporation 2-(substituted sulfanyl)-3,5-dihydro-imidazol-4-one derivatives
TW418195B (en) 1995-11-28 2001-01-11 American Home Prod 2-thioxo-imidazolidin-4-one derivatives
US5554607A (en) 1995-11-28 1996-09-10 American Home Products Corporation Use of 2-thioxo-imidazolin-4-one derivatives in the treatment of atherosclerosis
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
US6489163B1 (en) 1996-05-08 2002-12-03 Board Of Regents, The University Of Texas System Ribozyme mediated inactivation of the androgen receptor
JP3697320B2 (ja) 1996-06-20 2005-09-21 株式会社日立製作所 光ファイバセンサ
US5726061A (en) 1996-10-08 1998-03-10 Smithkline Beechum Corporation Method of diagnosing and monitoring colorectal cancer
US7053263B2 (en) 1996-10-15 2006-05-30 The Regents Of The University Of California Mouse models of human prostate cancer progression
US7205437B2 (en) 1996-11-27 2007-04-17 University Of Tennessee Research Foundation Selective androgen receptor modulators
ATE274707T1 (de) 1997-06-27 2004-09-15 Eads Deutschland Gmbh Füllstandmessradargerät
US6506607B1 (en) 1997-12-24 2003-01-14 Millennium Pharmaceuticals, Inc. Methods and compositions for the identification and assessment of prostate cancer therapies and the diagnosis of prostate cancer
WO1999065494A1 (en) 1998-06-15 1999-12-23 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
BR9914018A (pt) 1998-09-22 2001-07-03 Yamanouchi Pharmaceuticals Co Derivado de cianofenila
ATE240944T1 (de) 1998-09-22 2003-06-15 Degussa Verfahren zur herstellung von imidazolidin-2,4- dionen
WO2000026195A1 (en) 1998-10-30 2000-05-11 G.D. Searle & Co. Novel amino acid heterocyclic amide derivatives useful as nitric oxide synthase inhibitors
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
US6472415B1 (en) 1998-12-18 2002-10-29 Biophysica, Inc. Androgen receptor suppressors in the therapy and diagnosis of prostate cancer, alopecia and other hyper-androgenic syndromes
WO2000044731A1 (en) 1999-01-27 2000-08-03 G.D. Searle & Co. Novel hydroxyamidino carboxylate derivatives useful as nitric oxide synthase inhibitors
WO2001007048A1 (en) 1999-07-21 2001-02-01 Boehringer Ingelheim Pharmaceuticals, Inc. Small molecules useful in the treatment of inflammatory disease
CA2388508A1 (en) 1999-10-22 2001-05-03 Takeda Chemical Industries, Ltd. 1-substituted phenyl-1-(1h-imidazol-4-yl) alcohols, process for producing the same and use thereof
US6479063B2 (en) 1999-12-27 2002-11-12 Kenneth Weisman Therapeutic uses of hormonal manipulation using combinations of various agents to treat atherosclerosis
ES2284641T3 (es) 2000-05-31 2007-11-16 Tanabe Seiyaku Co., Ltd. Inhibidores de la adhesion celular mediada por alfa-l-beta-2.
US6482829B2 (en) 2000-06-08 2002-11-19 Hoffmann-La Roche Inc. Substituted heterocyclic siprodecane compound active as an antagonist of neurokinin 1 receptor
WO2002042488A1 (en) 2000-11-24 2002-05-30 Osmetech Plc Detection of infections in liquid samples by detecting fatty acids present in the headspace associated with the liquid sample
WO2002046186A1 (en) 2000-12-08 2002-06-13 Takeda Chemical Industries, Ltd. Substituted thiazole derivatives bearing 3-pyridyl groups, process for preparing the same and use thereof
WO2002053155A1 (en) 2000-12-30 2002-07-11 Geron Corporation Telomerase inhibitor
FR2823209B1 (fr) 2001-04-04 2003-12-12 Fournier Lab Sa Nouvelles thiohydantoines et leur utilisation en therapeutique
CN1596253A (zh) 2001-10-01 2005-03-16 布里斯托尔-迈尔斯斯奎布公司 用作抗炎药的螺－乙内酰脲化合物
EP1453516A2 (de) 2001-10-17 2004-09-08 Boehringer Ingelheim Pharma GmbH & Co.KG 5-substituierte 4-amino-2-phenylamino-pyrimdinderivate und ihre verwendung als beta-amyloid modulatoren
US6861432B2 (en) 2001-11-23 2005-03-01 Schering Aktiengesellschaft Piperazine derivatives that destabilize androgen receptors
GB0200283D0 (en) 2002-01-08 2002-02-20 Smithkline Beecham Plc Compounds
CA2473778A1 (en) 2002-02-08 2003-08-14 Merck & Co., Inc. N-biphenylmethyl aminocycloalkanecarboxamide derivatives
DE10218963A1 (de) 2002-04-27 2003-11-20 Aventis Pharma Gmbh Zubereitungen zur topischen Applikation von antiandrogen wirksamen Substanzen
TW200407324A (en) 2002-05-17 2004-05-16 Bristol Myers Squibb Co Bicyclic modulators of androgen receptor function
TW200401638A (en) 2002-06-20 2004-02-01 Bristol Myers Squibb Co Heterocyclic inhibitors of kinases
WO2004016758A2 (en) 2002-08-15 2004-02-26 Genzyme Corporation Brain endothelial cell expression patterns
AU2002951247A0 (en) 2002-09-06 2002-09-19 Alchemia Limited Compounds that interact with kinases
FR2845384B1 (fr) 2002-10-04 2004-12-31 Fournier Lab Sa Composes derives de la 2-thiohydantoine et leur utilisation en therapeutique
CA2500977A1 (en) 2002-10-04 2004-04-15 Laboratoires Fournier S.A. 2-thiohydantoine derivative compounds and use thereof in therapeutics
FR2850652B1 (fr) 2003-01-31 2008-05-30 Aventis Pharma Sa Nouveaux derives d'uree cyclique, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de kinases
DE10322108B4 (de) 2003-05-09 2008-12-11 Bayer Schering Pharma Aktiengesellschaft Antiandrogene Pyrrolidine mit tumorhemmender Wirksamkeit
EP1636205A1 (en) 2003-06-12 2006-03-22 Novo Nordisk A/S Pyridinyl carbamates as hormone-sensitive lipase inhibitors
EP1634874A4 (en) 2003-06-12 2008-04-02 Chugai Pharmaceutical Co Ltd imidazolidine
WO2005037797A1 (en) 2003-10-21 2005-04-28 Pharmacia Corporation Substituted pyrazole urea compounds for the treatment of inflammation
TW200523252A (en) 2003-10-31 2005-07-16 Takeda Pharmaceutical Pyridine compounds
US7256208B2 (en) 2003-11-13 2007-08-14 Bristol-Myers Squibb Company Monocyclic N-Aryl hydantoin modulators of androgen receptor function
EP1709152A4 (en) 2003-12-15 2007-11-07 Univ California MOLECULAR SIGNATURE OF PTEN TUMOR SUPPRESSOR
DE602004031881D1 (de) 2003-12-19 2011-04-28 Univ California Verfahren und materialien zur beurteilung von prostatakrebstherapien
US7173044B2 (en) 2004-02-19 2007-02-06 Solvay Pharmaceuticals B.V. Imidazoline derivatives having CB1-antagonistic activity
WO2005099693A2 (en) 2004-02-24 2005-10-27 The Regents Of The University Of California Methods and materials for assessing prostate cancer therapies and compounds
WO2005089752A2 (en) 2004-03-15 2005-09-29 Ptc Therapeutics, Inc. Tetra-cyclic carboline derivatives for inhibiting angiogenesis
EP1598343A1 (de) 2004-05-19 2005-11-23 Boehringer Ingelheim International GmbH 2-Arylaminopyrimidine als PLK Inhibitoren
EP1621539A1 (en) 2004-07-27 2006-02-01 Aventis Pharma S.A. Heterocycle -substituted cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors
JP4912148B2 (ja) 2004-08-03 2012-04-11 中外製薬株式会社 新規イミダゾリジン誘導体
EP1790640A4 (en) * 2004-09-09 2009-07-29 Chugai Pharmaceutical Co Ltd NEW IMIDAZOLIDINE DERIVATIVE AND APPLICATION THEREOF
US7709517B2 (en) 2005-05-13 2010-05-04 The Regents Of The University Of California Diarylhydantoin compounds
KR101782236B1 (ko) * 2005-05-13 2017-09-26 더 리전트 오브 더 유니버시티 오브 캘리포니아 디아릴히단토인 화합물
GB0521373D0 (en) 2005-10-20 2005-11-30 Kudos Pharm Ltd Pthalazinone derivatives
JP4887030B2 (ja) 2005-11-18 2012-02-29 株式会社日立ハイテクノロジーズ 荷電粒子線装置
CN101032483B (zh) 2006-03-09 2011-05-04 陈德桂 调节雄激素受体活性的乙内酰脲衍生物及其应用
PT2368550E (pt) 2006-03-27 2013-12-03 Univ California Modulador do receptor de androgénios para o tratamento de cancro da próstata e doenças associadas ao receptor de androgénios
CN101460467B (zh) 2006-03-29 2012-09-19 加利福尼亚大学董事会 二芳基硫代乙内酰脲化合物
US8461343B2 (en) 2007-03-27 2013-06-11 Sloan-Kettering Institute For Cancer Research Synthesis of thiohydantoins
UY31432A1 (es) * 2007-10-26 2009-05-29 Compuestos de diarilhidantoina
US8450290B2 (en) 2007-11-26 2013-05-28 Enzon Pharmaceuticals, Inc. Methods for treating androgen receptor dependent disorders including cancers
CL2008003672A1 (es) 2007-12-11 2009-05-29 Theravance Biopharma R&D Ip Llc Compuestos derivados de 3-carbopropil-aminotetralina; procedimiento de preparación; composición farmacéutica que los comprende; y sus usos para tratar disfunciones intestinales inducidas por opioides.
US20110130296A1 (en) 2008-03-14 2011-06-02 The Regents Of The University Of California Multi-gene classifiers and prognostic indicators for cancers
CA2753425A1 (en) 2009-02-24 2010-09-02 Medivation Prostate Therapeutics, Inc. Specific diarylhydantoin and diarylthiohydantoin compounds
EP2416657A4 (en) 2009-04-09 2012-09-05 Medivation Prostate Therapeutics Inc COMPOUNDS COMPRISING SUBSTITUTED DI-ARYLHYDANTOIDS AND DI-ARYLTHIOHYDANTOINES AND METHODS OF USE THEREOF
WO2011022316A1 (en) 2009-08-20 2011-02-24 The Regents Of The University Of Colorado, A Body Corporate Mirnas dysregulated in triple-negative breast cancer
WO2011044327A1 (en) 2009-10-07 2011-04-14 Medivation Prostate Therapeutics, Inc. Substituted phenylcarbamoyl alkylamino arene compounds and n,n'-bis-arylurea compounds
SI2538785T1 (en) 2010-02-24 2018-05-31 Medivation Prostate Therapeutics Llc Methods for the synthesis of diarylthiohidantoin and diarylhydantoin compounds

Also Published As

Publication number Publication date
JP2015180672A (ja) 2015-10-15
US9896437B2 (en) 2018-02-20
TW201716385A (zh) 2017-05-16
JP5535925B2 (ja) 2014-07-02
JP5914538B2 (ja) 2016-05-11
AR069039A1 (es) 2009-12-23
JP2017052796A (ja) 2017-03-16
EP2620432A2 (en) 2013-07-31
CA2703635A1 (en) 2009-04-30
CA2703635C (en) 2017-06-27
TWI469971B (zh) 2015-01-21
EP2620432A3 (en) 2013-12-18
TW201522315A (zh) 2015-06-16
WO2009055053A3 (en) 2009-06-11
US8680291B2 (en) 2014-03-25
JP2011500813A (ja) 2011-01-06
EP2397469B1 (en) 2014-12-31
UY31432A1 (es) 2009-05-29
CA2966280A1 (en) 2009-04-30
TWI557111B (zh) 2016-11-11
CL2008003158A1 (es) 2009-05-29
PE20170428A1 (es) 2017-05-14
US20090111864A1 (en) 2009-04-30
JP2014074070A (ja) 2014-04-24
WO2009055053A2 (en) 2009-04-30
TW200934762A (en) 2009-08-16
EP2397469A1 (en) 2011-12-21
US20150065546A1 (en) 2015-03-05
PE20091262A1 (es) 2009-09-09
EP2220050A2 (en) 2010-08-25
HK1165198A1 (en) 2012-09-28

Similar Documents

Publication Publication Date Title
PE20121470A1 (es) Compuestos de diarilhidantoina como antagonistas del receptor de androgeno
PE20121050A1 (es) Compuestos de n-(1-(4-(1h-pirazol-5-il)ftalazin-1-il)piperidin-4-il)-benzamida sustituidos como antagonistas de la trayectoria hedgehog
PE20121180A1 (es) (heteroarilmetil) tiohidantoinas sustituidas como drogas anticancer
PE20140868A1 (es) Antagonistas trpm8 y su uso en tratamientos
PE20090596A1 (es) Imidazoles biciclicos fusionados
PE20130152A1 (es) Derivados de heterociclo biciclicos como inhibidores de proteina quinasa b
PE20080948A1 (es) Derivados de imidazol como moduladores de la senda de hedgehog
SI2614058T1 (sl) Polimorfi in soli N-(5-(4-(5-(((2R,6S)-2,6-dimetil-4-morfolinil)metil)-1,3-oksazol-2-il)- 1H-indazol-6-il)-2-(metiloksi)-3-piridinil)metansulfonamida
PE20110854A1 (es) DERIVADOS DE 1-FENIL-1H-PIRAZOLO[3,4-c]PIRIDINA-4-CARBONILAMINA COMO ANTAGONISTAS DE LOS RECEPTORES CCR1
PE20142293A1 (es) Pirimidinas y triazinas fusionadas sustituidas y su uso
PE20090678A1 (es) Combinaciones de compuestos inhibidores de fosfoinositida 3-quinasa y agentes quimioterapeuticos y los metodos de uso
PE20141050A1 (es) Inhibidores de quinasa relacionados con pirrolo (2,3-d) pirimidina tropomiosina
PE20081888A1 (es) ANALOGOS DE PIRAZOLOPIRIMIDINA Y SU USO COMO INHIBIDORES DE CINASA mTOR Y CINASA PI3
PE20080552A1 (es) Derivados de alcoholes 1-fenil-2-piridinil alquilenicos como inhibidores de fosfodiesterasa
PE20091653A1 (es) Derivados sustituidos de pirazol y su uso
PE20142019A1 (es) Nuevos derivados de acidos indaniloxidihidrobenzofuranilaceticos y sus usos como agonistas del receptor gpr40
PE20141361A1 (es) Compuesto heterociclico dihidroxi aromatico
PE20091321A1 (es) Derivados biciclicos de carboxamidas aza-biciclicas, su preparacion y su aplicacion en terapeutica
JP2013538802A5 (es)
AR067090A1 (es) Espiriciclos como inhibidores de la 11- beta hidroxiesteroide deshidrogenasa de tipo 1
PE20141203A1 (es) Benzilindazoles sustituidos para uso como inhibidores de la quinasa bub1 en el tratamiento de enfermedades hiperproliferativas
PE20110433A1 (es) Antagonistas de la via hedgehog de ftalazina disustituida
PE20081378A1 (es) Derivados de 1,2,4-triazol como moduladores de mglur5
PE20160691A1 (es) Nuevos derivados de triazolo[4,5-d]pirimidina
PE20120900A1 (es) Compuestos heterociclicos de fenoximetilo

Legal Events

Date Code Title Description
FC Refusal