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PE20030708A1 - Derivados de piperazina desestabilizantes del receptor de androgenos - Google Patents

Derivados de piperazina desestabilizantes del receptor de androgenos

Info

Publication number
PE20030708A1
PE20030708A1 PE2002001124A PE2002001124A PE20030708A1 PE 20030708 A1 PE20030708 A1 PE 20030708A1 PE 2002001124 A PE2002001124 A PE 2002001124A PE 2002001124 A PE2002001124 A PE 2002001124A PE 20030708 A1 PE20030708 A1 PE 20030708A1
Authority
PE
Peru
Prior art keywords
trifluoromethyl
pentil
pyrrol
dihydro
phenyl
Prior art date
Application number
PE2002001124A
Other languages
English (en)
Inventor
Jens Hoffmann
Dieter Zopf
Christoph Huwe
Volker Schulze
Andreas Reicher
Helmut Morack
Arwed Cleve
Original Assignee
Schering Ag
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
Priority claimed from DE2001159035 external-priority patent/DE10159035A1/de
Priority claimed from DE2002138742 external-priority patent/DE10238742A1/de
Application filed by Schering Ag filed Critical Schering Ag
Publication of PE20030708A1 publication Critical patent/PE20030708A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/44Heterocyclic 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 three double bonds between ring members or between ring members and non-ring members
    • C07D207/444Heterocyclic 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 three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5
    • C07D207/448Heterocyclic 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 three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide
    • C07D207/452Heterocyclic 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 three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide with hydrocarbon radicals, substituted by hetero atoms, directly attached to the ring nitrogen atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic 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
    • C07D233/66Heterocyclic 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
    • C07D233/86Oxygen and sulfur atoms, e.g. thiohydantoin
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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 only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A DERIVADOS DE PIPERAZINA DE FORMULA I DONDE V ES UN RADICAL AROMATICO DE FORMULA II DONDE A ES ACETILO, ACETILAMINO, CIANO, NITRO, TRIFLUOROMETILO, ENTRE OTROS; B ES H, HALOGENO, TRIFLUOROMETILO; A Y B JUNTOS FORMAN UN GRUPO CICLICO; W ES UN HETEROCICLO DE FORMULA III DONDE T ES C, N; i Y j SON 1-2; R Y R' SON O, METILO; Y EQUIVALE A UNA UNION ENTRE EL N Y HETEROCICLICO Y Z A UN GRUPO CARBONILO, SULFONILO, IMINOCARBONILO, IMINOSULFONILO, ENTRE OTROS; Z Y Z' SON ALQUILO C1-C8, CICLOALQUILO C3-C6, FENILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS 4-[5-[1-[4-CIANO-3-(TRIFLUOROMETILO)FENIL]-2,5-DIHIDRO-4-METIL-2,5-DIOXI-1H-PIRROL-3-IL]PENTIL]PIPERAZINI-1-CARBOXILATO DE 1,1-DIMETILETILO, 4-[2,5-DIHIDRO-3-METL-4-[5-[4-[2-(METILSULFANIL)FENIL]-PIPERAZIN-1-IL]PENTIL]-2,5-DIOXI-1H-PIRROL-1-IL]-2-(TRIFLUOROMETIL)BENZONITRILO, 4-[3-[5-[4-(4-CIANOBENZOIL)PIPERAZIN-1-IL]PENTIL]-2,5-DIHIDRO-4-METIL-2,5DIOXO-1H-PIRROL-1-IL]-2-(TRIFLUOROMETIL)BENZONITRILO, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO PARA LA PREPARACION Y PRODUCTOS INTERMEDIOS. LOS COMPUESTOS MENCIONADOS SON DESESTABILIZANTES DEL RECEPTOR DE ANDROGENOS Y SON UTILES PARA EL TRATAMIENTO DE HIPERPLASIA PROSTATICA BENIGNA, ALOPECIA, ACNE
PE2002001124A 2001-11-23 2002-11-22 Derivados de piperazina desestabilizantes del receptor de androgenos PE20030708A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE2001159035 DE10159035A1 (de) 2001-11-23 2001-11-23 Androgenrezeptor destabilisierende Piperazinderivate
DE2002138742 DE10238742A1 (de) 2002-08-19 2002-08-19 Androgenrezeptor destabilisierende Piperazinderivate

Publications (1)

Publication Number Publication Date
PE20030708A1 true PE20030708A1 (es) 2003-08-28

Family

ID=26010698

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2002001124A PE20030708A1 (es) 2001-11-23 2002-11-22 Derivados de piperazina desestabilizantes del receptor de androgenos

Country Status (5)

Country Link
AU (1) AU2002360932A1 (es)
PE (1) PE20030708A1 (es)
TW (1) TW200301117A (es)
UY (1) UY27544A1 (es)
WO (1) WO2003043983A1 (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030195192A1 (en) * 2002-04-05 2003-10-16 Fortuna Haviv Nicotinamides having antiangiogenic activity
JP2006519755A (ja) * 2002-11-20 2006-08-31 ロレアル ピラゾール−カルボキシアミドを含有する毛髪の手入れ用又は睫毛用の組成物、毛髪及び睫毛の成長を刺激し、及び/又は抜毛を防止するためのそれらの使用
FR2847160A1 (fr) * 2002-11-20 2004-05-21 Oreal Composition capillaire contenant un compose pyrasol-carboxamide, son utilisation pour stimuler la pousse des cheveux et/ou freiner leur chute
US7592466B2 (en) 2003-10-09 2009-09-22 Abbott Laboratories Ureas having antiangiogenic activity
AU2005216200A1 (en) * 2004-02-22 2005-09-09 Government Of The United States Of America, As Represented By The Secretary Department Of Health And Human Services Maleiimide anti-tumor phosphatase inhibitors
CN101039927A (zh) * 2004-09-09 2007-09-19 财团法人乙卯研究所 5-羟色胺5-ht3受体激动剂
CN102464631B (zh) * 2010-11-08 2016-08-10 中国科学院上海药物研究所 哌嗪取代的1,3-二取代脲类化合物及哌嗪取代的酰胺类化合物及其制备方法和用途
BR102012000187A2 (pt) * 2012-01-05 2018-04-10 Univ Rio De Janeiro Derivados n-fenilpiperazínicos antagonistas de adrenoceptores a1a, a1d e de receptores 5-ht1a no tratamento da hiperplasia prostática benigna, composições farmacêuticas contendo os mesmos
US12152035B2 (en) 2020-12-30 2024-11-26 Industrial Technology Research Institute Androgen receptor binding molecule and use thereof

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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.
US5859014A (en) * 1995-06-09 1999-01-12 Syntex (U.S.A.) Inc. Pyrimidinedione, pyrimidinetrione, triazinedione and tetrahydroquinazolinedione derivatives as α1 -adrenergic receptor antagonists
US5656651A (en) * 1995-06-16 1997-08-12 Biophysica Inc. Androgenic directed compositions
US6673799B1 (en) * 1998-09-22 2004-01-06 Yamanouchi Pharmaceutical Co. Ltd. Cyanophenyl derivative

Also Published As

Publication number Publication date
AU2002360932A1 (en) 2003-06-10
UY27544A1 (es) 2003-06-30
WO2003043983A1 (de) 2003-05-30
TW200301117A (en) 2003-07-01

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