CO5180552A1 - Ent-esteroides en calidad de estrogenos con efecto selectivo - Google Patents

Ent-esteroides en calidad de estrogenos con efecto selectivo

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Publication number
CO5180552A1
CO5180552A1 CO00027851A CO00027851A CO5180552A1 CO 5180552 A1 CO5180552 A1 CO 5180552A1 CO 00027851 A CO00027851 A CO 00027851A CO 00027851 A CO00027851 A CO 00027851A CO 5180552 A1 CO5180552 A1 CO 5180552A1
Authority
CO
Colombia
Prior art keywords
group
hydrogen atom
atom
r13so2
moiety
Prior art date
Application number
CO00027851A
Other languages
English (en)
Inventor
Schwarz Sigfrid
Dirk Kosemund
Gerd Muller
Margit Richter
Peters Olaf
Peter Droescher
Walter Elger
Alexander Hillisch
Bomer Ulf
Karl Heinz Fritzemeier
Christa Hegeke-Hartu
Original Assignee
Bayer Schering Pharma 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
Application filed by Bayer Schering Pharma Ag filed Critical Bayer Schering Pharma Ag
Publication of CO5180552A1 publication Critical patent/CO5180552A1/es

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    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/566—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol having an oxo group in position 17, e.g. estrone
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/567—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • 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
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric 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
    • A61P19/08—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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • 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
    • A61P5/30—Oestrogens
    • 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
    • A61P5/32—Antioestrogens
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

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  • Health & Medical Sciences (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)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Pregnancy & Childbirth (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

Ent-Esteroides de fórmula I<EMI FILE="00027851_1" ID="1" IMF=JPEG >en dondeun grupo R12-O-, en el cual R12 representa un átomo de hidrógeno o un resto hidrocarbonado de hasta 5 átomos de carbono que puede contener un enlace doble C-C o un enlace triple C-C; un grupo R13SO2-O-, en el cual R13 representa un grupo R14R15N, en donde R14 y R15 representan independientemente un átomo de hidrógeno, un resto alquilo(C1-5), un grupo C(O)R16, siendo R16 un resto hidrocarbonado de hasta 12 átomos de carbono que puede contener adicionalmente hasta tres enlaces dobles y/o triples, un resto cicloalquilo (C3-7), un resto arilo o una combinación de estas características estructurales, o junto con el átomo de N representan un radical de polimetilenimino de 4 a 6 átomos de C o un radical de morfolino;R2 representa un grupo R12-O-, R13SO2-O- o -O-C(O)R16, en donde R12, R13 y R16 tienen en cada caso el significado indicado para R1; R3, R4, R5, R8 y R9 representan independientemente un átomo de hidrógeno,un átomo de halógeno, un grupoR12-O-, R13SO2-O- o -R16, en donde R12, R13 y R16 tienen en cada casoel significado indicado para R1;R6 representa un átomo de hidrógeno ubicado en yR7 representa un átomo de hidrógenooR6 y R7 representa juntos un grupo a - o ß metileno;R10 representa dos átomos de hidrógeno; dos átomos de halógeno; un átomo de hidrógeno y un átomo de halógeno; un grupo =CR17R18, en donde R17 y R18 representan independientemente un átomo de hidrógeno y un átomo de halógeno; un átomo de hidrógeno y un grupo R12-O-; un átomo de hidrógeno y un grupo R13SO2-O-; un grupo R12 y un grupo -O-C(O)R16; un grupo R12 y un grupo hidroxilo; en donde R12, R13 y R16 tienen en cada caso el significado indicado para R1; un átomo de oxígeno;R11 representa un átomo de hidrógeno, un grupo metilo o etilo;R19 representa un átomo de hidrógeno o un resto hidrocarbonado de hasta cinco átomos de carbono que puede estar parcialmente o totalmente fluorado y puede contener un enlace doble C-C o un enlace tripleC-C; ...
CO00027851A 1999-04-15 2000-04-14 Ent-esteroides en calidad de estrogenos con efecto selectivo CO5180552A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE19917930A DE19917930A1 (de) 1999-04-15 1999-04-15 Ent-Steroide als selektiv wirksame Estrogene

Publications (1)

Publication Number Publication Date
CO5180552A1 true CO5180552A1 (es) 2002-07-30

Family

ID=7905255

Family Applications (1)

Application Number Title Priority Date Filing Date
CO00027851A CO5180552A1 (es) 1999-04-15 2000-04-14 Ent-esteroides en calidad de estrogenos con efecto selectivo

Country Status (11)

Country Link
EP (1) EP1169336B1 (es)
JP (1) JP2002542255A (es)
AR (1) AR023497A1 (es)
AT (1) ATE316978T1 (es)
AU (1) AU4401100A (es)
CA (1) CA2371972A1 (es)
CO (1) CO5180552A1 (es)
DE (2) DE19917930A1 (es)
ES (1) ES2258005T3 (es)
PE (1) PE20010042A1 (es)
WO (1) WO2000063228A1 (es)

Families Citing this family (32)

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US6350739B1 (en) 1999-08-11 2002-02-26 University Of Florida Resarch Foundation, Inc. Methods of prevention and treatment of ischemic damage
PT1226155E (pt) * 1999-11-02 2007-07-26 Bayer Schering Pharma Ag 18-nor-esteróides como estrogénios selectivamente activos
US6958327B1 (en) 1999-11-02 2005-10-25 Schering, Ag 18 Norsteroids as selectively active estrogens
DE10039199A1 (de) * 2000-08-10 2002-02-21 Schering Ag Kombinationspräparate aus einem ERß selektiven Estrogen und einem SERM oder Antiestrogen
GB0020498D0 (en) * 2000-08-18 2000-10-11 Sterix Ltd Compound
DE10048634A1 (de) * 2000-09-27 2002-04-18 Jenapharm Gmbh 19-Nor-17alpha-pregna-1,3,5(10)-trien-17beta-ole mit einem 21, 16alpha-Laktonring
CA2427817C (en) 2000-11-03 2009-04-14 Washington University Estrone-derivatives having cytoprotective activity
AU2002228891A1 (en) * 2000-11-17 2002-05-27 Washington University Cytoprotective estrogen derivatives
WO2002068548A1 (en) * 2001-02-27 2002-09-06 Schering Ag Use of erss-selective ligands for regulating fertility and compounds useful therefore
DE10151365A1 (de) 2001-10-17 2003-04-30 Schering Ag 17-Chlor-D-Homosteroide als selektive Estrogenrezeptorantagonisten
DK1390040T3 (da) 2001-05-18 2007-04-23 Pantarhei Bioscience Bv Farmaceutisk præparat til anvendelse i hormonerstatningsterapi
US7732430B2 (en) 2001-05-23 2010-06-08 Pantarhei Bioscience B.V. Drug delivery system comprising a tetrahydroxilated estrogen for use in hormonal contraception
EP1390041B1 (en) 2001-05-23 2009-11-25 Pantarhei Bioscience B.V. Drug delivery system comprising a tetrahydroxylated estrogen for use in hormonal contraception
DE10151363A1 (de) * 2001-10-17 2003-05-08 Schering Ag Somatotrope Therapie
EP1446128B1 (en) 2001-11-15 2006-12-06 Pantarhei Bioscience B.V. Use of estrogenic compounds in combination with progestogenic compounds in hormone-replacement therapy
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WO2003103685A1 (en) 2002-06-11 2003-12-18 Pantarhei Bioscience B.V. A method of treating human skin and a skin care composition for use in such a method
ATE340579T1 (de) * 2002-06-11 2006-10-15 Pantarhei Bioscience Bv Methode zur behandlung oder prävention immunologischer erkrankungen und pharmazeutische zusammensetzung zur solchen anwendung
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ATE410170T1 (de) * 2003-03-27 2008-10-15 Pantarhei Bioscience Bv Verwendung von estrogenen zur behandlung von männerunfruchtbarkeit
DE10317922B4 (de) * 2003-04-17 2009-11-26 Presearch Gmbh Verwendung eines Kombinationspräparates aus oralem Kontrazeptivum und Calcium/Vitamin D
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CN104926916B (zh) * 2015-06-05 2016-08-24 郑祖兰 甾体化合物，含其药物组合物及其制备方法和应用
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RS62222B1 (sr) 2016-07-07 2021-09-30 Sage Therapeutics Inc 24-hidroksisteroli supstituisani na poziciji 11 za upotrebu u lečenju stanja povezanih sa nmda
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Also Published As

Publication number Publication date
AR023497A1 (es) 2002-09-04
EP1169336A1 (en) 2002-01-09
ATE316978T1 (de) 2006-02-15
ES2258005T3 (es) 2006-08-16
WO2000063228A1 (en) 2000-10-26
DE60025817D1 (de) 2006-04-13
AU4401100A (en) 2000-11-02
CA2371972A1 (en) 2000-10-26
DE60025817T2 (de) 2006-11-02
EP1169336B1 (en) 2006-02-01
DE19917930A1 (de) 2000-10-19
PE20010042A1 (es) 2001-02-15
JP2002542255A (ja) 2002-12-10

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