CU23414B7 - Estratrienos 9-alfa-sustituidos como estrógenos de eficacia selectiva - Google Patents

Estratrienos 9-alfa-sustituidos como estrógenos de eficacia selectiva

Info

Publication number
CU23414B7
CU23414B7 CU20040282A CU20040282A CU23414B7 CU 23414 B7 CU23414 B7 CU 23414B7 CU 20040282 A CU20040282 A CU 20040282A CU 20040282 A CU20040282 A CU 20040282A CU 23414 B7 CU23414 B7 CU 23414B7
Authority
CU
Cuba
Prior art keywords
substituted
preparations
stratriens
strateges
alpha
Prior art date
Application number
CU20040282A
Other languages
English (en)
Inventor
Karl-Heinrich Fritzemeier
Alexander Hillisch
Gerd Mueller
Dirk Kosemund
Peter Muhn
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 CU23414B7 publication Critical patent/CU23414B7/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0055—Estrane derivatives not substituted in position 17
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P19/08—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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0072—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the A ring of the steroid being aromatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/008—Expansion of ring D by one atom, e.g. D homo steroids

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Gynecology & Obstetrics (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Nuevos estratrienos 9 alfa-sustituidos de fórmula general (I), ESPACIO PARA FÓRMULA donde R3, R7, R7', R13, R16 y R17 y R17' tienen los significados indicados en la descripción, así como R9 es un radical alquenilo de cadena lineal o ramificada, opcionalmente halogenado de modo parcial o total con 2 a 6 átomos de carbono, un radical etinilo o prop-1-inilo, como ingredientes activos farmacéuticos, que presentan in vitro una mayor afinidad en preparaciones de receptores de estrógeno de próstata de rata que en preparaciones de receptores de estrógeno de útero de rata y que presentan in vivo, con preferencia, un efecto preferencial en el ovario en comparación con el útero, a su preparación, su aplicación terapéutica y a formas farmacéuticas que contienen los nuevos compuestos. La invención describe, además, el uso de estos compuestos para el tratamiento de enfermedades y estados originados por deficiencia de estrógenos.
CU20040282A 2002-06-11 2004-12-10 Estratrienos 9-alfa-sustituidos como estrógenos de eficacia selectiva CU23414B7 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10226326A DE10226326A1 (de) 2002-06-11 2002-06-11 9-alpha-substiuierte Estratriene als selektiv wirksame Estrogene

Publications (1)

Publication Number Publication Date
CU23414B7 true CU23414B7 (es) 2009-09-08

Family

ID=29723144

Family Applications (1)

Application Number Title Priority Date Filing Date
CU20040282A CU23414B7 (es) 2002-06-11 2004-12-10 Estratrienos 9-alfa-sustituidos como estrógenos de eficacia selectiva

Country Status (28)

Country Link
EP (1) EP1517914B1 (es)
JP (1) JP4615998B2 (es)
KR (1) KR101006612B1 (es)
CN (1) CN1293090C (es)
AR (1) AR040188A1 (es)
AT (1) ATE303397T1 (es)
AU (1) AU2003242683B9 (es)
BR (1) BR0312140A (es)
CA (1) CA2486495C (es)
CR (1) CR10289A (es)
CU (1) CU23414B7 (es)
DE (2) DE10226326A1 (es)
DK (1) DK1517914T3 (es)
EA (1) EA008442B1 (es)
EC (1) ECSP055530A (es)
ES (1) ES2248770T3 (es)
HR (1) HRP20050009B1 (es)
IL (1) IL165321A (es)
MX (1) MXPA04012491A (es)
NO (1) NO329563B1 (es)
PE (1) PE20040613A1 (es)
PL (1) PL209910B1 (es)
RS (1) RS50878B (es)
TW (1) TWI286140B (es)
UA (1) UA78062C2 (es)
UY (1) UY27844A1 (es)
WO (1) WO2003104253A2 (es)
ZA (1) ZA200500217B (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10027887A1 (de) 2000-05-31 2001-12-13 Jenapharm Gmbh Verbindungen mit einer Sulfonamidgruppe und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen
PT1689410E (pt) * 2003-11-26 2008-08-18 Bayer Schering Pharma Ag Prevenção e tratamento de doenças cardíacas hipertensivas pelos estrogénios selectivos 8beta-vinil-estra-1,3,5(10)-trieno-3,17beta-diol e 17beta-fluoro-9alfa-vinil-estra-1,3,5(10)-trieno-3,16alfa-diol
US7534780B2 (en) 2004-05-21 2009-05-19 Bayer Schering Pharma Aktiengesellschaft Estradiol prodrugs
DE102005057224A1 (de) * 2005-11-29 2007-05-31 Bayer Schering Pharma Ag Prodrugs ERß-selektiver Substanzen, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen
US20110052699A1 (en) * 2008-02-13 2011-03-03 Adrian Funke Drug delivery system with stabilising effect
EP2143432A1 (en) 2008-07-11 2010-01-13 Bayer Schering Pharma AG 9-alpha estratriene derivatives as ER-beta selective ligands for the prevention and treatment of intestinal cancer
JP2012509286A (ja) * 2008-11-21 2012-04-19 バイエル ファーマ アクチエンゲゼルシャフト 薬物送達システム
EP3185881B1 (en) 2014-08-26 2022-03-09 Betanien Hospital Methods, agents and compositions for treatment of inflammatory conditions
WO2020051329A1 (en) * 2018-09-07 2020-03-12 Trustees Of Dartmouth College C19 scaffolds and steroids and methods of use and manufacture thereof

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2336432A1 (de) * 1973-07-13 1975-01-30 Schering Ag 3.17.18-trihydroxy-1.3.5(10)-oestratriene
US6154158A (en) * 1998-06-30 2000-11-28 Qualcomm Incorporated Digital-to-analog converter D.C. offset correction comparing converter input and output signals
DE19906159A1 (de) * 1999-02-09 2000-08-10 Schering Ag 16-Hydroxyestratriene als selektiv wirksame Estrogene
EP1226155B1 (de) * 1999-11-02 2007-05-02 Bayer Schering Pharma AG 18-nor-steroide als selektiv wirksame estrogene
SK14632002A3 (sk) * 2000-04-12 2003-03-04 Schering Aktiengesellschaft Substituované estratriény a ich použitie ako selektívne účinných estrogénov

Also Published As

Publication number Publication date
ATE303397T1 (de) 2005-09-15
HRP20050009A2 (en) 2005-04-30
ECSP055530A (es) 2005-03-10
UA78062C2 (en) 2007-02-15
CA2486495A1 (en) 2003-12-18
HRP20050009B1 (hr) 2013-07-31
WO2003104253A2 (de) 2003-12-18
EA008442B1 (ru) 2007-06-29
WO2003104253A3 (de) 2004-09-16
NO20050127D0 (no) 2005-01-10
EP1517914B1 (de) 2005-08-31
DE50301116D1 (de) 2005-10-06
MXPA04012491A (es) 2005-06-08
BR0312140A (pt) 2005-04-05
JP4615998B2 (ja) 2011-01-19
RS50878B (sr) 2010-08-31
KR20050009745A (ko) 2005-01-25
CA2486495C (en) 2011-04-19
PL373090A1 (en) 2005-08-08
AU2003242683A1 (en) 2003-12-22
AR040188A1 (es) 2005-03-16
PL209910B1 (pl) 2011-11-30
JP2005533053A (ja) 2005-11-04
AU2003242683B9 (en) 2009-08-27
EA200401544A1 (ru) 2005-06-30
KR101006612B1 (ko) 2011-01-10
HK1081203A1 (en) 2006-05-12
CR10289A (es) 2008-11-26
TWI286140B (en) 2007-09-01
CN1659181A (zh) 2005-08-24
CN1293090C (zh) 2007-01-03
EP1517914A2 (de) 2005-03-30
PE20040613A1 (es) 2004-12-01
RS107004A (sr) 2006-10-27
UY27844A1 (es) 2003-12-31
NO20050127L (no) 2005-03-11
IL165321A (en) 2009-08-03
TW200407331A (en) 2004-05-16
ZA200500217B (en) 2006-03-29
DK1517914T3 (da) 2006-01-16
ES2248770T3 (es) 2006-03-16
NO329563B1 (no) 2010-11-15
DE10226326A1 (de) 2004-01-15
AU2003242683B2 (en) 2009-07-02

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