CL2008003158A1 - Compuestos derivados de diariltiohidantoina con actividad antagonista fuerte y con actividad agonista minima sobre el receptor de androgeno (ar); procedimiento de preparacion; composicion farmaceutica que los comprende; uso en el tratamiento de un desorden proliferativo tal como cancer de prostata. - Google Patents

Compuestos derivados de diariltiohidantoina con actividad antagonista fuerte y con actividad agonista minima sobre el receptor de androgeno (ar); procedimiento de preparacion; composicion farmaceutica que los comprende; uso en el tratamiento de un desorden proliferativo tal como cancer de prostata.

Info

Publication number
CL2008003158A1
CL2008003158A1 CL2008003158A CL2008003158A CL2008003158A1 CL 2008003158 A1 CL2008003158 A1 CL 2008003158A1 CL 2008003158 A CL2008003158 A CL 2008003158A CL 2008003158 A CL2008003158 A CL 2008003158A CL 2008003158 A1 CL2008003158 A1 CL 2008003158A1
Authority
CL
Chile
Prior art keywords
pharmaceutical composition
prostate cancer
androgen receptor
diarylthiohydantoin
activity
Prior art date
Application number
CL2008003158A
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 CL2008003158A1 publication Critical patent/CL2008003158A1/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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

LA PRESENTE INVENCIÓN SE REFIERE A COMPUESTOS DERIVADOS DE DIARILHIDANTOINA DE FÓRMULA: DONDE R1 R2 R3, R4  R11 Y R12 SE DEFINEN TAL COMO EN EL PLIEGO DE REIVINDICACIONES. LA INVENCIÓN ADEMÁS DESCRIBE LA COMPOSICIÓN FARMACÉUTICA QUE COMPRENDE A LOS COMPUESTOS DE LA CLÁUSULA PRINCIPAL Y UN PORTADOR O DILUYENTE FARMACÉUTICAMENTE ACEPTABLE; Y EL PROCEDIMIENTO DE PREPARACIÓN DE DICHOS COMPUESTOS. LOS COMPUESTOS REVELADOS PRESENTAN ACTIVIDAD SOBRE EL RECEPTOR DE ANDRÓGENO (AR) E INHIBEN EL CRECIMIENTO DEL CÁNCER DE PRÓSTATA REFRACTARIO A LA HORMONA.  
CL2008003158A 2007-10-26 2008-10-24 Compuestos derivados de diariltiohidantoina con actividad antagonista fuerte y con actividad agonista minima sobre el receptor de androgeno (ar); procedimiento de preparacion; composicion farmaceutica que los comprende; uso en el tratamiento de un desorden proliferativo tal como cancer de prostata. CL2008003158A1 (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
CL2008003158A1 true CL2008003158A1 (es) 2009-05-29

Family

ID=40278902

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2008003158A CL2008003158A1 (es) 2007-10-26 2008-10-24 Compuestos derivados de diariltiohidantoina con actividad antagonista fuerte y con actividad agonista minima sobre el receptor de androgeno (ar); procedimiento de preparacion; composicion farmaceutica que los comprende; uso en el tratamiento de un desorden proliferativo tal como cancer de prostata.

Country Status (11)

Country Link
US (2) US8680291B2 (es)
EP (3) EP2620432A3 (es)
JP (4) JP5535925B2 (es)
AR (1) AR069039A1 (es)
CA (2) CA2703635C (es)
CL (1) CL2008003158A1 (es)
HK (1) HK1165198A1 (es)
PE (3) PE20121470A1 (es)
TW (3) TWI469971B (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
SG10201408699TA (en) * 2006-03-29 2015-02-27 Univ California Diarylthiohydantoin compounds
EP2620432A3 (en) 2007-10-26 2013-12-18 The Regents Of the University of California Diarylhydantoin compounds
BRPI1007990A2 (pt) 2009-02-24 2015-09-01 Medivation Prostate Therapeutics Inc Compostos específicos de diaril-hidantoína e diariltioidantoína.
US8710086B2 (en) * 2009-04-09 2014-04-29 Medivation Technologies, Inc. Substituted di-arylhydantoin and di-arylthiohydantoin compounds and methods of use thereof
CN102482230B (zh) * 2009-09-10 2016-01-06 苏州开拓药业有限公司 雄激素受体拮抗剂及其用途
TW201111378A (en) 2009-09-11 2011-04-01 Bayer Schering Pharma Ag Substituted (heteroarylmethyl) thiohydantoins
EP2485804A4 (en) * 2009-10-07 2015-07-29 Medivation Technologies Inc SUBSTITUTED PHENYLCARBAMOYL ALKYLAMINOAREN COMPOUNDS AND N, N'-BIS-ARYL UREA 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
EP3124481B1 (en) * 2010-02-16 2018-03-28 Aragon Pharmaceuticals, Inc. Androgen receptor modulators and uses thereof
DK3329775T3 (da) 2010-02-24 2021-07-26 Medivation Prostate Therapeutics Llc Fremgangsmåder til syntese af diarylthiohydantoin- og diarylhydantoinforbindelser
AU2011258009B2 (en) * 2010-05-28 2016-04-21 The Board Of Regents Of The University Of Texas System Oligo-benzamide compounds and their use
WO2012065051A1 (en) 2010-11-12 2012-05-18 Enzon Pharmaceuticals, Inc. Compositions and methods for treating androgen receptor dependent disorders including cancers
DK2683694T3 (en) 2011-03-10 2016-07-18 Suzhou Kintor Pharmaceuticals Inc ANDROGEN RECEPTOR ANTAGONISTS AND APPLICATIONS THEREOF
WO2012143599A1 (en) 2011-04-21 2012-10-26 Orion Corporation Androgen receptor modulating carboxamides
MX359664B (es) * 2011-07-29 2018-10-05 Univ Colorado Regents Tratamiento de cáncer de mama.
UY34646A (es) 2012-03-02 2013-10-31 Novartis Ag Compuestos de espirohidantoína y su uso como moduladores selectivos del receptor de andrógenos
US9428460B2 (en) * 2012-06-26 2016-08-30 Bayer Pharma Aktiengesellschaft N-[4-(quinolin-4-yloxy)cyclohexyl(methyl)](hetero)arylcarboxamides as androgen receptor antagonists, production and use thereof as medicinal products
SG10201912719TA (en) 2012-09-26 2020-02-27 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
EP3230471B1 (en) 2014-12-12 2019-08-28 Medivation Prostate Therapeutics LLC Method for predicting response to breast cancer therapeutic agents and method of treatment of breast cancer
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
AU2018351714A1 (en) 2017-10-16 2020-04-30 Aragon Pharmaceuticals, Inc. Anti-androgens for the treatment of non-metastatic castration-resistant prostate cancer
JP2022509917A (ja) 2018-11-05 2022-01-25 ファイザー・インク がんを処置するための組合せ
CA3214316A1 (en) 2021-03-24 2022-09-29 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
IL55774A (en) 1977-10-28 1982-04-30 Sparamedica Ag Pharmaceutical compositions containing urea derivatives,certain such novel derivatives and their manufacture
JPS5492962A (en) 1977-12-01 1979-07-23 Wellcome Found Thiohydantoin compound
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
FI801184A (fi) 1979-04-24 1980-10-25 Hoffmann La Roche Foerfarande foer framstaellning av imidazolidinderivat
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
DE3372965D1 (en) * 1982-07-23 1987-09-17 Ici 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.
US5411981A (en) 1991-01-09 1995-05-02 Roussel Uclaf Phenylimidazolidines having antiandrogenic activity
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.
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.
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.
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
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.
JPH09508125A (ja) 1994-01-21 1997-08-19 セプラコー，インコーポレイテッド 光学的純正ｒ−（−）−カソデックスを使用した男性ホルモン依存疾患治療のための方法と組成
EP0721944B1 (en) 1994-07-29 2001-01-17 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
DE69638137D1 (de) * 1995-09-07 2010-04-15 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
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
EP0876354A1 (en) 1995-11-28 1998-11-11 American Home Products Corporation 2-(substituted sulfanyl)-3,5-dihydro-imidazol-4-one derivatives
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
EP1087770A4 (en) * 1998-06-15 2001-11-14 Merck & Co Inc INHIBITORS OF PRENYL PROTEIN TRANSFERASE
DE59905623D1 (de) 1998-09-22 2003-06-26 Degussa Verfahren zur Herstellung von Imidazolidin-2,4-dionen
ATE384048T1 (de) 1998-09-22 2008-02-15 Astellas Pharma Inc Cyanophenyl-derivate
WO2000026195A1 (en) 1998-10-30 2000-05-11 G.D. Searle & Co. Novel amino acid heterocyclic amide derivatives useful as nitric oxide synthase inhibitors
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
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
AU2847200A (en) 1999-01-27 2000-08-18 G.D. Searle & Co. Novel hydroxyamidino carboxylate derivatives useful as nitric oxide synthase inhibitors
US6350763B1 (en) * 1999-07-21 2002-02-26 Boehringer Ingelheim Pharmaceuticals, Inc. Small molecules useful in the treatment of inflammation disease
DE60027034T2 (de) * 1999-10-22 2006-11-09 Takeda Pharmaceutical Co. Ltd. 1-substituierte-phenyl-1-(1h-imidazol-4-yl)alkohole, verfahren zu deren herstellung sowie deren verwendung
US6479063B2 (en) 1999-12-27 2002-11-12 Kenneth Weisman Therapeutic uses of hormonal manipulation using combinations of various agents to treat atherosclerosis
CN1209358C (zh) * 2000-05-31 2005-07-06 田边制药株式会社 αLβ2介导细胞粘连的抑制剂
US6482829B2 (en) 2000-06-08 2002-11-19 Hoffmann-La Roche Inc. Substituted heterocyclic siprodecane compound active as an antagonist of neurokinin 1 receptor
JP4125955B2 (ja) 2000-11-24 2008-07-30 オスメテック パブリック リミテッド カンパニー 液体試料に関連するヘッドスペース内に存在する脂肪酸の検出による液体試料の感染検出方法
CA2431171A1 (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
RS26604A (en) 2001-10-01 2006-12-15 Bristol Myers Squibb Company Spiro-hydantoin compounds useful as anti-inflamatory agents
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
DE60303441T2 (de) 2002-02-08 2006-09-21 Merck & Co., Inc. N-biphenylmethylaminocycloalkancarboxamid-derivative
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
US20060127902A1 (en) 2002-08-15 2006-06-15 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
WO2004031160A2 (fr) 2002-10-04 2004-04-15 Laboratoires Fournier S.A. Composes derives de la 2-thiohydantoïne et leur utilisation pour le traitement du diabete
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
CA2526204A1 (en) 2003-06-12 2004-12-23 Novo Nordisk A/S Pyridinyl carbamates as hormone-sensitive lipase inhibitors
US7271188B2 (en) 2003-06-12 2007-09-18 Chugai Seikayu Kabushiki Kaisha Imidazolidine derivatives
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
AU2004305075A1 (en) 2003-12-19 2005-07-07 The Regents Of The University Of California Methods and materials for assessing prostate cancer therapies
US7173044B2 (en) 2004-02-19 2007-02-06 Solvay Pharmaceuticals B.V. Imidazoline derivatives having CB1-antagonistic activity
NZ550102A (en) 2004-02-24 2010-10-29 Univ California Methods and materials for assessing prostate cancer therapies and compounds (thiohydantoine derivatives)
US8940896B2 (en) 2004-03-15 2015-01-27 Ptc Therapeutics, Inc. Tetra-cyclic carboline derivatives useful in the inhibition of 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
WO2006013887A1 (ja) 2004-08-03 2006-02-09 Chugai Seiyaku Kabushiki Kaisha 新規イミダゾリジン誘導体
WO2006028226A1 (ja) * 2004-09-09 2006-03-16 Chugai Seiyaku Kabushiki Kaisha 新規イミダゾリジン誘導体およびその用途
US7709517B2 (en) 2005-05-13 2010-05-04 The Regents Of The University Of California Diarylhydantoin compounds
KR101332924B1 (ko) * 2005-05-13 2013-11-26 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
HUE027894T2 (en) 2006-03-27 2016-11-28 Univ California An androgen receptor modulator for the treatment of prostate cancer and androgen receptor related diseases
SG10201408699TA (en) * 2006-03-29 2015-02-27 Univ California Diarylthiohydantoin compounds
US8461343B2 (en) 2007-03-27 2013-06-11 Sloan-Kettering Institute For Cancer Research Synthesis of thiohydantoins
EP2620432A3 (en) * 2007-10-26 2013-12-18 The Regents Of the University of California Diarylhydantoin compounds
US8450290B2 (en) 2007-11-26 2013-05-28 Enzon Pharmaceuticals, Inc. Methods for treating androgen receptor dependent disorders including cancers
ES2402749T3 (es) 2007-12-11 2013-05-08 Theravance, Inc. Derivados de 3-carboxipropil-aminotetralina como antagonistas del receptor de opioide mu
US20110130296A1 (en) 2008-03-14 2011-06-02 The Regents Of The University Of California Multi-gene classifiers and prognostic indicators for cancers
BRPI1007990A2 (pt) 2009-02-24 2015-09-01 Medivation Prostate Therapeutics Inc Compostos específicos de diaril-hidantoína e diariltioidantoína.
US8710086B2 (en) 2009-04-09 2014-04-29 Medivation Technologies, Inc. Substituted di-arylhydantoin and di-arylthiohydantoin compounds 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
EP2485804A4 (en) 2009-10-07 2015-07-29 Medivation Technologies Inc SUBSTITUTED PHENYLCARBAMOYL ALKYLAMINOAREN COMPOUNDS AND N, N'-BIS-ARYL UREA COMPOUNDS
DK3329775T3 (da) 2010-02-24 2021-07-26 Medivation Prostate Therapeutics Llc Fremgangsmåder til syntese af diarylthiohydantoin- og diarylhydantoinforbindelser

Also Published As

Publication number Publication date
TWI469971B (zh) 2015-01-21
PE20121470A1 (es) 2012-11-18
EP2397469A1 (en) 2011-12-21
UY31432A1 (es) 2009-05-29
TW201716385A (zh) 2017-05-16
CA2703635C (en) 2017-06-27
US8680291B2 (en) 2014-03-25
TWI557111B (zh) 2016-11-11
WO2009055053A2 (en) 2009-04-30
EP2220050A2 (en) 2010-08-25
JP2015180672A (ja) 2015-10-15
EP2397469B1 (en) 2014-12-31
EP2620432A3 (en) 2013-12-18
TW201522315A (zh) 2015-06-16
EP2620432A2 (en) 2013-07-31
PE20170428A1 (es) 2017-05-14
JP2011500813A (ja) 2011-01-06
CA2703635A1 (en) 2009-04-30
AR069039A1 (es) 2009-12-23
WO2009055053A3 (en) 2009-06-11
US9896437B2 (en) 2018-02-20
US20090111864A1 (en) 2009-04-30
TW200934762A (en) 2009-08-16
PE20091262A1 (es) 2009-09-09
JP2017052796A (ja) 2017-03-16
HK1165198A1 (en) 2012-09-28
JP5535925B2 (ja) 2014-07-02
JP2014074070A (ja) 2014-04-24
CA2966280A1 (en) 2009-04-30
JP5914538B2 (ja) 2016-05-11
US20150065546A1 (en) 2015-03-05

Similar Documents

Publication Publication Date Title
CL2008003158A1 (es) Compuestos derivados de diariltiohidantoina con actividad antagonista fuerte y con actividad agonista minima sobre el receptor de androgeno (ar); procedimiento de preparacion; composicion farmaceutica que los comprende; uso en el tratamiento de un desorden proliferativo tal como cancer de prostata.
CL2008002521A1 (es) Compuestos derivados de pirazol sustituidos, antagonista del receptor de androgeno; composicion farmaceutica que comprende a dichos compuestos; y uso del compusto para el tratamiento de cancer.
BR112016011949A8 (pt) composto, composição farmacêutica, e, uso dos mesmos”
BR112014014909A2 (pt) agonistas de tgr5 não sistêmicos
CL2008003846A1 (es) Uso de compuestos derivados de 1,2,4-triazolo condensado con heterociclos, los cuales actuan como ligados del receptor de androgeno (ar); compuestos; proceso de preparacion; composicion farmaceutica y el uso de dichos compuestos para el tratamiento del cancer de prostata.
CL2008001213A1 (es) Uso de compuestos derivados de piridin-4-il-benceno-1,4-diamino sustituidos por alquindol para preparar un medicamento para el tratamiento de un trastorno proliferativo tal como el cancer.
PE20191710A1 (es) Modulador del receptor de androgeno y usos de este
GT200900328A (es) Derivados de bencimidazol
PA8777101A1 (es) Derivados de sulfonil amida para el tratamiento del crecimiento celular anormal
MX345928B (es) Composiciones terapeuticamente activas y metodos de uso de las mismas.
HN2011000629A (es) Derivados de picolinamida como inhibidores de cinasa
CO6390101A2 (es) Compuestos purina
ECSP109935A (es) Derivados de morfolino pirimidina utilizados en enfermedades relacionadas con mtor quinasa y/o pi3k
PA8740901A1 (es) Compuestos organicos
CL2011000504A1 (es) Compuestos derivados de piridin-4-il-tiazol-2il-amida 2-amida-pirrolidin-1,2-dicarboxilico, inhibidores de quinasa de fosfatidil-inositol-3; composicion farmaceutica que comprende a uno de los compuestos; y uso de los compuestos en la preparacion de un medicamento para el tratamiento del cancer.
NI200800060A (es) Bencimidazoles sustituidos como inhibidores de cinasa.
UY32462A (es) Derivados de bifenilo novedosos para el tratamiento de infección por virus de hepatitis c 644
EA201300869A1 (ru) Морфинановые соединения
NZ719079A (en) Parasiticidal oral veterinary compositions comprising systemically-acting active agents, methods and uses thereof
UY31009A1 (es) Antagonistas del receptor de la hormona liberadora de gonadotropina y procedimientos relacionados con los mismos
NI200900184A (es) Uso de compuestos inhibidores de quinaxolina de pi3k-alfa para el tratamiento del cáncer.
SV2011003993A (es) Derivados de triazolo [4, 3-b] piridazina y sus usos para el cancer de prostata
GB0607954D0 (en) Organic compounds
CO6331308A2 (es) Derivados de carboxamidaindazol con actividad sobre el receptor cb1 y composiciones farmaceuticas que los comprenden
UY32731A (es) Nuevos derivados de piperidin-ilidenaminooxi-piperidin, composiciones farmacéuticas y métodos relacionados con ellos