ATE365707T1 - 3,4-disubstituierte acylanilidderivate und deren verwendung als androgen rezeptor suppressoren - Google Patents

3,4-disubstituierte acylanilidderivate und deren verwendung als androgen rezeptor suppressoren

Info

Publication number
ATE365707T1
ATE365707T1 AT99958948T AT99958948T ATE365707T1 AT E365707 T1 ATE365707 T1 AT E365707T1 AT 99958948 T AT99958948 T AT 99958948T AT 99958948 T AT99958948 T AT 99958948T AT E365707 T1 ATE365707 T1 AT E365707T1
Authority
AT
Austria
Prior art keywords
androgen receptor
derivatives
disubstituted
therapy
suppressors
Prior art date
Application number
AT99958948T
Other languages
English (en)
Inventor
Milos Sovak
Allen Seligson
James Douglas
Brian Campion
Jason Brown
Original Assignee
Biophysica Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Biophysica Inc filed Critical Biophysica Inc
Application granted granted Critical
Publication of ATE365707T1 publication Critical patent/ATE365707T1/de

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D207/36—Oxygen or sulfur atoms
    • C07D207/40—2,5-Pyrrolidine-diones
    • C07D207/404—2,5-Pyrrolidine-diones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. succinimide
    • C07D207/408—Radicals containing only hydrogen and carbon atoms attached to ring carbon atoms
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/56—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and doubly-bound oxygen atoms bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • C07C255/60—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/30—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by halogen atoms, or by nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C07C317/46—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/60—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C335/00—Thioureas, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C335/04—Derivatives of thiourea
    • C07C335/06—Derivatives of thiourea having nitrogen atoms of thiourea groups bound to acyclic carbon atoms
    • C07C335/08—Derivatives of thiourea having nitrogen atoms of thiourea groups bound to acyclic carbon atoms of a saturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C335/00—Thioureas, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C335/04—Derivatives of thiourea
    • C07C335/16—Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C335/00—Thioureas, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C335/04—Derivatives of thiourea
    • C07C335/16—Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C335/22—Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
    • 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
    • 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
    • C07D233/88—Nitrogen atoms, e.g. allantoin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyrrole Compounds (AREA)
AT99958948T 1998-12-18 1999-11-12 3,4-disubstituierte acylanilidderivate und deren verwendung als androgen rezeptor suppressoren ATE365707T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US09/215,351 US6184249B1 (en) 1998-12-18 1998-12-18 Androgen receptor suppressors in the therapy and diagnosis of prostate cancer, alopecia and other hyper-androgenic syndromes

Publications (1)

Publication Number Publication Date
ATE365707T1 true ATE365707T1 (de) 2007-07-15

Family

ID=22802642

Family Applications (1)

Application Number Title Priority Date Filing Date
AT99958948T ATE365707T1 (de) 1998-12-18 1999-11-12 3,4-disubstituierte acylanilidderivate und deren verwendung als androgen rezeptor suppressoren

Country Status (8)

Country Link
US (1) US6184249B1 (de)
EP (1) EP1144366B1 (de)
AT (1) ATE365707T1 (de)
AU (1) AU1621500A (de)
CZ (1) CZ300149B6 (de)
DE (1) DE69936397T2 (de)
IL (2) IL143709A0 (de)
WO (1) WO2000037430A2 (de)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US6828458B2 (en) * 2000-05-25 2004-12-07 Biophysica, Inc. Topical antiandrogen for hair loss and other hyperandrogenic conditions
US20040077605A1 (en) 2001-06-20 2004-04-22 Salvati Mark E. Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
US7001911B2 (en) 2000-06-28 2006-02-21 Bristol-Myers Squibb Company Fused cyclic modulators of nuclear hormone receptor function
BR0111298A (pt) * 2000-06-28 2005-05-10 Bristol Myers Squibb Co Moduladores seletivos dos receptores de andrógenos e métodos para identificação, projeto e uso dos mesmos
US6953679B2 (en) 2000-09-19 2005-10-11 Bristol-Myers Squibb Company Method for the preparation of fused heterocyclic succinimide compounds and analogs thereof
US7102026B2 (en) * 2001-06-13 2006-09-05 Teva Gyógyszergyár Zártkörüen Müködö Részvénytársaság Process for preparing and isolating rac-bicalutamide and its intermediates
WO2002100339A2 (en) * 2001-06-13 2002-12-19 Biogal Gyogyszergyar Rt. Novel process for preparing rac-bicalutamide and its intermediates
DE60228330D1 (de) 2001-12-19 2008-09-25 Bristol Myers Squibb Co Kondensierte heterocyclische verbindungen und deren analoga; modulatoren der funktion von nukleären hormonrezeptoren
DE10322108B4 (de) 2003-05-09 2008-12-11 Bayer Schering Pharma Aktiengesellschaft Antiandrogene Pyrrolidine mit tumorhemmender Wirksamkeit
KR100783255B1 (ko) 2004-02-13 2007-12-06 워너-램버트 캄파니 엘엘씨 안드로젠 수용체 조절제
JP2007532621A (ja) 2004-04-13 2007-11-15 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー アンドロゲンモジュレータ
WO2005102990A1 (en) 2004-04-22 2005-11-03 Warner-Lambert Company Llc Androgen modulators
US20060009430A1 (en) * 2004-07-01 2006-01-12 Kelly Gregory J Composition for the prevention and treatment of the detrimental effects of dihydrotestosterone
EP1781598A1 (de) 2004-07-08 2007-05-09 Warner-Lambert Company LLC Androgenmodulatoren
WO2006037468A1 (en) * 2004-09-30 2006-04-13 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa Hiv reverse transcriptase inhibitors
TW200724139A (en) 2005-05-05 2007-07-01 Warner Lambert Co Androgen modulators
US7709516B2 (en) 2005-06-17 2010-05-04 Endorecherche, Inc. Helix 12 directed non-steroidal antiandrogens
US20070048246A1 (en) * 2005-09-01 2007-03-01 Biophysica Research, Inc. Novel skin care compositions
WO2008044033A1 (en) * 2006-10-11 2008-04-17 Astrazeneca Ab Amide derivatives
US9284345B2 (en) 2007-04-12 2016-03-15 Endorecherche, Inc. 17alpha-substituted steroids as systemic antiandrogens and selective androgen receptor modulators
TWI469971B (zh) 2007-10-26 2015-01-21 Univ California 二芳基乙內醯脲類化合物
BRPI0821676A2 (pt) 2007-12-21 2015-06-16 Astrazeneca Ab Composto, composição farmacêutica, e, processo para a preparação dos compostos.
US9682960B2 (en) 2013-12-19 2017-06-20 Endorecherche, Inc. Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety
WO2016049774A1 (en) * 2014-10-03 2016-04-07 The Royal Institution For The Advancement Of Learning/Mcgill University Urea and bis-urea based compounds and analogues thereof useful in the treatment of androgen receptor mediated diseases or disorders
US11292782B2 (en) 2018-11-30 2022-04-05 Nuvation Bio Inc. Diarylhydantoin compounds and methods of use thereof

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DE2059872A1 (de) * 1970-12-05 1972-06-15 Merck Patent Gmbh Thioharnstoffe,Verfahren zu ihrer Herstellung und ihre Verwendung zur Schaedlingsbekaempfung
US4191775A (en) * 1977-12-15 1980-03-04 Imperial Chemical Industries Limited Amide derivatives
AU8961382A (en) * 1981-11-06 1983-05-12 Imperial Chemical Industries Plc Amide derivatives
EP0100172B1 (de) 1982-07-23 1987-08-12 Imperial Chemical Industries Plc Amide-Derivate
GB8617652D0 (en) 1986-07-18 1986-08-28 Ici Plc Acylanilide derivatives
US5411981A (en) * 1991-01-09 1995-05-02 Roussel Uclaf Phenylimidazolidines having antiandrogenic activity
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
US5656651A (en) 1995-06-16 1997-08-12 Biophysica Inc. Androgenic directed compositions
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
WO1998055153A1 (en) * 1997-06-04 1998-12-10 The University Of Tennessee Research Corporation Non-steroidal radiolabeled agonist/antagonist compounds and their use in prostate cancer imaging

Also Published As

Publication number Publication date
EP1144366A2 (de) 2001-10-17
CZ300149B6 (cs) 2009-02-25
IL143709A0 (en) 2002-04-21
CZ20012141A3 (cs) 2002-02-13
EP1144366A3 (de) 2003-06-04
WO2000037430A2 (en) 2000-06-29
EP1144366B1 (de) 2007-06-27
DE69936397D1 (de) 2007-08-09
DE69936397T2 (de) 2008-03-06
IL143709A (en) 2007-06-03
WO2000037430A3 (en) 2003-04-17
US6184249B1 (en) 2001-02-06
AU1621500A (en) 2000-07-12

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