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AR036812A1 - Inhibidores de la 17beta-hidroxiesteroide deshidrogenasa tipo 3, composiciones farmaceuticas y el uso de dichos compuestos para la fabricacion de medicamentos para el tratamiento de enfermedades androgeno-dependientes - Google Patents

Inhibidores de la 17beta-hidroxiesteroide deshidrogenasa tipo 3, composiciones farmaceuticas y el uso de dichos compuestos para la fabricacion de medicamentos para el tratamiento de enfermedades androgeno-dependientes

Info

Publication number
AR036812A1
AR036812A1 ARP020103851A ARP020103851A AR036812A1 AR 036812 A1 AR036812 A1 AR 036812A1 AR P020103851 A ARP020103851 A AR P020103851A AR P020103851 A ARP020103851 A AR P020103851A AR 036812 A1 AR036812 A1 AR 036812A1
Authority
AR
Argentina
Prior art keywords
group
alkyl
aryl
heteroaryl
heteroarylalkyl
Prior art date
Application number
ARP020103851A
Other languages
English (en)
Original Assignee
Schering Corp
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 Schering Corp filed Critical Schering Corp
Publication of AR036812A1 publication Critical patent/AR036812A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28—Antiandrogens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/34—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (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)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Inhibidores de la 17beta-hidroxiesteroide deshidrogenasa tipo 3 de la fórmula (1), una de sus prodrogas, o una de las sales o solvatos aceptables para uso farmacéutico del compuesto o de la prodroga, en la cual, R1 se selecciona del grupo conformado por arilo, heteroarilo, arilalquilo, heteroarilalquilo y difenilalquilo, cada uno sustituido en forma opcional con 1 a 6 grupos seleccionados del grupo conformado por: halógeno, -OCF3 u -OCHF2, -CF3, -CN, alquilo o R18-alquilo, heteroalquilo o R18-heteroalquilo, arilo o R18-arilo, heteroarilo o R18-heteroarilo, arilalquilo o R18-arilalquilo, heteroarilalquilo o R18-heteroarilalquilo, hidroxi, alcoxi, ariloxi, -SO2-alquilo, -NR11R12, -N(R11)C(O)R13, metilendioxi, difluorometilendioxi, trifluoroalcoxi, -SCH3 ó -SCF3, y -SO2CF3 ó -NHSO2CF3; R2 y R3 se seleccionan, cada uno en forma independiente, del grupo conformado por: H, -OH, alcoxi, alquilo, cicloalquilo, heterocicloalquilo, cicloalquilalquilo, trifluoroalquilo, heteroalquilo, arilalquilo, heteroarilalquilo, arilalcoxi, heteroarilalcoxi, -(CH2)n-NR11R12 y -(CH2)n-SR11, con la salvedad de que cuando X es N, entonces R2 y R3 no sean, cada uno, -OH, alcoxi, arilalcoxi ó heteroarilalcoxi; R4, R5, R7 y R8 se seleccionan, cada uno en forma independiente, del grupo conformado por: H, -OR14, -NR11R12, -N(R11)C(O)R13, alquilo, arilo, cicloalquilo, arilalquilo, heteroalquilo, heteroarilo, heteroarilalquilo, heterocicloalquilo, fórmulas (2), (3) y (4), con la salvedad de que cuando Z y/o X son N, entonces R4, R5, R7 y R8 no sean, cada uno, -OR14, -NR11R12, ó -N(R11)C(O)R13; R6 se selecciona del grupo conformado por -C(O)R15 y -SO2R15; R9 y R10 se seleccionan, cada uno en forma independiente, del grupo conformado por: H, F, -CF3, -CHF2, alquilo, cicloalquilo, arilalquilo, heteroalquilo, heteroarilalquilo, heterocicloalquilo, hidroxi, alcoxi, ariloxi, -NR11R12 y -N(R11)C(O)R13 con la salvedad de que cuando Z es N, entonces R9 y R10 no sean, cada uno, F, hidroxi, alcoxi, ariloxi, -NR11R12 ó -N(R11)C(O)R13; R11 se selecciona del grupo conformado por H, alquilo, arilo y heteroarilo; R12 se selecciona del grupo conformado por H, alquilo, arilo y heteroarilo; R13 se selecciona del grupo conformado por alquilo, alcoxi y ariloxi; R14 se selecciona del grupo conformado por H, alquilo, arilo y heteroarilo; R15 se selecciona del grupo conformado por: -NR16R17, -OR16, alquilo, cicloalquilo, heterocicloalquilo, arilo, arilalquilo y heteroarilalquilo, cada uno sustituido en forma opcional con R18; R16 y R17 se seleccionan, cada uno en forma independiente, del grupo conformado por: alquilo, arilo, arilalquilo, heteroalquilo, y heteroarilo, cada uno sustituido en forma opcional con R18, y H, con la salvedad de que cuando R15 es -OR16, entonces R16 no sea H; R18 tiene de 1 a 4 sustituyentes cada uno seleccionado en forma independiente del grupo conformado por: alquilo inferior, halo, ciano, nitro, haloalquilo, hidroxi, alcoxi, carboxi, carboxialquilo, carboxamida, mercapto, amino, alquilamino, dialquilamino, sulfonilo, sulfonamido, arilo y heteroarilo; X y Z se seleccionan, cada uno en forma independiente del grupo conformado por C y N; y n es 1-4; que son útiles como inhibidores de 17beta-hidroxiesteroide deshidrogenasa tipo 3: Se describen, además, composiciones farmacéuticas que contienen dichos compuestos y uso para la fabricación de medicamentos para el tratamiento o la prevención de enfermedades andrógeno-dependientes.
ARP020103851A 2001-10-17 2002-10-15 Inhibidores de la 17beta-hidroxiesteroide deshidrogenasa tipo 3, composiciones farmaceuticas y el uso de dichos compuestos para la fabricacion de medicamentos para el tratamiento de enfermedades androgeno-dependientes AR036812A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US33006601P 2001-10-17 2001-10-17

Publications (1)

Publication Number Publication Date
AR036812A1 true AR036812A1 (es) 2004-10-06

Family

ID=23288179

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP020103851A AR036812A1 (es) 2001-10-17 2002-10-15 Inhibidores de la 17beta-hidroxiesteroide deshidrogenasa tipo 3, composiciones farmaceuticas y el uso de dichos compuestos para la fabricacion de medicamentos para el tratamiento de enfermedades androgeno-dependientes

Country Status (12)

Country Link
US (1) US6969718B2 (es)
EP (1) EP1436281B1 (es)
JP (1) JP4309761B2 (es)
CN (1) CN1571782A (es)
AR (1) AR036812A1 (es)
AT (1) ATE471315T1 (es)
CA (1) CA2463626C (es)
DE (1) DE60236743D1 (es)
ES (1) ES2347643T3 (es)
MX (1) MXPA04003611A (es)
PE (1) PE20030705A1 (es)
WO (1) WO2003033487A1 (es)

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Also Published As

Publication number Publication date
ES2347643T3 (es) 2010-11-03
US20030232837A1 (en) 2003-12-18
JP4309761B2 (ja) 2009-08-05
EP1436281A1 (en) 2004-07-14
EP1436281B1 (en) 2010-06-16
PE20030705A1 (es) 2003-08-21
ATE471315T1 (de) 2010-07-15
CA2463626A1 (en) 2003-04-24
MXPA04003611A (es) 2004-07-30
US6969718B2 (en) 2005-11-29
CN1571782A (zh) 2005-01-26
CA2463626C (en) 2011-05-24
DE60236743D1 (de) 2010-07-29
JP2005506356A (ja) 2005-03-03
WO2003033487A1 (en) 2003-04-24

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