AR043085A1 - Un metodo para tratar una enfermedad asociada con el receptor-beta del estrogeno - Google Patents

Un metodo para tratar una enfermedad asociada con el receptor-beta del estrogeno

Info

Publication number
AR043085A1
AR043085A1 ARP000101771A ARP000101771A AR043085A1 AR 043085 A1 AR043085 A1 AR 043085A1 AR P000101771 A ARP000101771 A AR P000101771A AR P000101771 A ARP000101771 A AR P000101771A AR 043085 A1 AR043085 A1 AR 043085A1
Authority
AR
Argentina
Prior art keywords
nra
hydrogen
value
beta
estrogen
Prior art date
Application number
ARP000101771A
Other languages
English (en)
Original Assignee
Astra Zeneca Uk Ltd
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 Astra Zeneca Uk Ltd filed Critical Astra Zeneca Uk Ltd
Publication of AR043085A1 publication Critical patent/AR043085A1/es

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Classifications

    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
    • A61K31/37—Coumarins, e.g. psoralen
    • 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
    • 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
    • A61K31/12—Ketones
    • A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system

Landscapes

  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pyrane Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Un método para tratar una enfermedad asociada con el receptor-beta del estrógeno que comprende el paso de administrar una cantidad terapéuticamente efectiva de un compuesto que satisface la ecuación: (KialfaA/kibeta)/KialfaE/kibetaE) > 1, donde: KialfaA es el valor de Ki para el agonista en ER-alfa; KibetaA es el valor de Ki para el agonista en ER-beta; KialfaE es el valor Ki para el estrógeno en ER-alfa; y KibetaA es el valor de Ki para el estrógeno en ER-beta. El método es útil en el tratamiento de enfermedades relacionadas con el receptor-beta del estrógeno tales como enfermedad de Alzheimer, afecciones por ansiedad, afecciones depresivas, osteoporosis, enfermedad cardiovascular, artritis reumatoidea y cáncer de próstata. Preferiblemente los compuestos tienen la fórmula (1), donde L1 es -C(=O)-, =C(R6)-, -CH(R6)-, O, S, o NRa; L2 es =C- o -CH-; L3 es =C(R6)-, -CH(R6)- o -C(=O)-; y L4 es -C(=O)-, CH2, O, S, o NRa; donde: cuando L1 es -C(=O)-, L4 es CH2, O, S, o NRa; cuando L3 es -C(=O), L1 es =C(R6)- o -CH(R6)-, y L4 es O o NRa, cuando L1 es =C(R6)-, L2 es =C-; cuando L1 es -CH(R6)-, L2 es -CH-; cuando L3 es =C(R6)-, L2 es =C-; y cuando L3 es -CH(R6)-, L2 es -CH-; Ra es, independientemente, en cada caso, H ó alquilo (C1-5); R1 es fenilo, fenilo sustituido o heterociclo; R2, R3, R4, y R5 son cada uno, independientemente, -Ra, -ORa, -SRa, -NRaRa, -NC(=O)Ra, -NS(=O)Ra, -NS(=O)2Ra, halógeno, ciano, -CF3, -CO2Ra, -C(=O)Ra, -C(=O)NHRa, nitro, -S(=O)Ra, o -S(=O)2Ra; R6 es H, alquilo (C1-5), fenilo o CF3; y donde, cuando L1 es -C(=O)-, y R2 es hidroxi o hidrógeno, y R3 es hidrógeno, y R4 es hidroxi, y R5 es hidrógeno, y R6 es hidrógeno, entonces R1 no es para-fenol; y una sal del mismo aceptable para uso farmacéutico.
ARP000101771A 1999-04-16 2000-04-14 Un metodo para tratar una enfermedad asociada con el receptor-beta del estrogeno AR043085A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US12990199P 1999-04-16 1999-04-16

Publications (1)

Publication Number Publication Date
AR043085A1 true AR043085A1 (es) 2005-07-20

Family

ID=22442124

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP000101771A AR043085A1 (es) 1999-04-16 2000-04-14 Un metodo para tratar una enfermedad asociada con el receptor-beta del estrogeno

Country Status (22)

Country Link
US (1) US6518301B1 (es)
EP (1) EP1173164A2 (es)
JP (1) JP2002542187A (es)
KR (1) KR20010108509A (es)
CN (1) CN1358091A (es)
AR (1) AR043085A1 (es)
AU (1) AU4128800A (es)
BG (1) BG106103A (es)
BR (1) BR0009814A (es)
CA (1) CA2370126A1 (es)
CZ (1) CZ20013714A3 (es)
EE (1) EE200100526A (es)
HU (1) HUP0200740A3 (es)
IL (1) IL145839A0 (es)
IS (1) IS6108A (es)
MX (1) MXPA01010423A (es)
NO (1) NO20015015L (es)
PL (1) PL351314A1 (es)
SK (1) SK14762001A3 (es)
TR (2) TR200201762T2 (es)
WO (1) WO2000062765A2 (es)
ZA (1) ZA200108409B (es)

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AU2003286781B2 (en) 2002-10-29 2009-05-21 Brigham Young University Use of equol for treating androgen mediated diseases
US8580846B2 (en) * 2002-10-29 2013-11-12 Brigham Young University Use of equol for ameliorating or preventing neuropsychiatric and neurodegenerative diseases or disorders
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TWI492943B (zh) 2008-12-05 2015-07-21 大塚製藥股份有限公司 喹啉酮化合物及藥學組成物（二）
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Also Published As

Publication number Publication date
KR20010108509A (ko) 2001-12-07
IS6108A (is) 2001-10-15
HUP0200740A2 (hu) 2002-07-29
TR200201762T2 (tr) 2002-10-21
US6518301B1 (en) 2003-02-11
TR200102992T2 (tr) 2004-12-21
BR0009814A (pt) 2002-01-08
CZ20013714A3 (cs) 2002-08-14
NO20015015L (no) 2001-12-17
HUP0200740A3 (en) 2004-08-30
CA2370126A1 (en) 2000-10-26
PL351314A1 (en) 2003-04-07
NO20015015D0 (no) 2001-10-15
AU4128800A (en) 2000-11-02
CN1358091A (zh) 2002-07-10
BG106103A (en) 2002-05-31
JP2002542187A (ja) 2002-12-10
WO2000062765A3 (en) 2001-09-07
IL145839A0 (en) 2002-07-25
WO2000062765A2 (en) 2000-10-26
ZA200108409B (en) 2003-03-26
EP1173164A2 (en) 2002-01-23
SK14762001A3 (sk) 2002-10-08
EE200100526A (et) 2002-12-16
MXPA01010423A (es) 2002-03-27

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