ECSP055530A - Estratrienos 9-alfa-sustituidos como estrógenos de eficacia selectiva - Google Patents

Estratrienos 9-alfa-sustituidos como estrógenos de eficacia selectiva

Info

Publication number
ECSP055530A
ECSP055530A EC2005005530A ECSP055530A ECSP055530A EC SP055530 A ECSP055530 A EC SP055530A EC 2005005530 A EC2005005530 A EC 2005005530A EC SP055530 A ECSP055530 A EC SP055530A EC SP055530 A ECSP055530 A EC SP055530A
Authority
EC
Ecuador
Prior art keywords
preparations
relates
substituted
stratriens
strateges
Prior art date
Application number
EC2005005530A
Other languages
English (en)
Inventor
Dirk Kosemund
Gerd Mueller
Alexander Hillisch
Karl-Heinrich Fritzemeier
Peter Muhn
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
Application filed by Schering Ag filed Critical Schering Ag
Publication of ECSP055530A publication Critical patent/ECSP055530A/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0055Estrane derivatives not substituted in position 17
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30Oestrogens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0066Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0072Normal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J63/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/008Expansion 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)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Transplantation (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La invención se relaciona con nuevos estratrienos 9 -sustituidos de la fórmula general I, 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 estró-geno 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. El invento también se refiere a la prepara-ción de estos estratrienos, a su aplicación terapéutica y a formas de administra-ción farmacéuticas que contienen los nuevos compuestos. La invención se refie-re, además, al uso de estos compuestos para el tratamiento de enfermedades y estados originados por deficiencia de estrógenos.
EC2005005530A 2002-06-11 2005-01-10 Estratrienos 9-alfa-sustituidos como estrógenos de eficacia selectiva ECSP055530A (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
ECSP055530A true ECSP055530A (es) 2005-03-10

Family

ID=29723144

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2005005530A ECSP055530A (es) 2002-06-11 2005-01-10 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
WO2005051401A2 (en) * 2003-11-26 2005-06-09 Schering Aktiengesellschaft Prevention and treatment of hypertensive heart diseases by the selective estrogens 8beta-vinyl-estra-1,3,5(10)-trien-3,17beta-diol and 17beta-fluor-9alpha-vinyl-estra-1,3,5(10)-trien-3,16alpha-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
CA2714598A1 (en) * 2008-02-13 2009-08-20 Bayer Schering Pharma Aktiengesellschaft 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
EP2358351A1 (en) * 2008-11-21 2011-08-24 Bayer Pharma Aktiengesellschaft Drug delivery system
EP3185881B1 (en) 2014-08-26 2022-03-09 Betanien Hospital Methods, agents and compositions for treatment of inflammatory conditions
CN113056473A (zh) * 2018-09-07 2021-06-29 达特茅斯学院托管理事会 C19支架和甾体及其使用和制造方法

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
PT1226155E (pt) * 1999-11-02 2007-07-26 Bayer Schering Pharma Ag 18-nor-esteróides como estrogénios selectivamente activos
IL152248A0 (en) * 2000-04-12 2003-05-29 Schering Ag 8beta-HYDROCARBYL-SUBSTITUTED ESTRATRIENES FOR USE AS SELECTIVE ESTROGENS

Also Published As

Publication number Publication date
DE10226326A1 (de) 2004-01-15
IL165321A (en) 2009-08-03
TWI286140B (en) 2007-09-01
PL209910B1 (pl) 2011-11-30
HRP20050009A2 (en) 2005-04-30
ATE303397T1 (de) 2005-09-15
MXPA04012491A (es) 2005-06-08
ZA200500217B (en) 2006-03-29
RS107004A (sr) 2006-10-27
RS50878B (sr) 2010-08-31
AU2003242683B9 (en) 2009-08-27
NO20050127D0 (no) 2005-01-10
CU23414B7 (es) 2009-09-08
UA78062C2 (en) 2007-02-15
AU2003242683A1 (en) 2003-12-22
TW200407331A (en) 2004-05-16
WO2003104253A2 (de) 2003-12-18
DE50301116D1 (de) 2005-10-06
EA008442B1 (ru) 2007-06-29
HK1081203A1 (en) 2006-05-12
NO20050127L (no) 2005-03-11
CA2486495A1 (en) 2003-12-18
KR101006612B1 (ko) 2011-01-10
EP1517914A2 (de) 2005-03-30
CN1293090C (zh) 2007-01-03
AR040188A1 (es) 2005-03-16
CR10289A (es) 2008-11-26
PL373090A1 (en) 2005-08-08
ES2248770T3 (es) 2006-03-16
KR20050009745A (ko) 2005-01-25
UY27844A1 (es) 2003-12-31
DK1517914T3 (da) 2006-01-16
HRP20050009B1 (hr) 2013-07-31
NO329563B1 (no) 2010-11-15
AU2003242683B2 (en) 2009-07-02
JP2005533053A (ja) 2005-11-04
EP1517914B1 (de) 2005-08-31
EA200401544A1 (ru) 2005-06-30
CN1659181A (zh) 2005-08-24
BR0312140A (pt) 2005-04-05
CA2486495C (en) 2011-04-19
WO2003104253A3 (de) 2004-09-16
PE20040613A1 (es) 2004-12-01
JP4615998B2 (ja) 2011-01-19

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