UY27844A1 - Estratrienos 9-alfa-sustituidos como estrógenos de eficacia selectiva. - Google Patents

Estratrienos 9-alfa-sustituidos como estrógenos de eficacia selectiva.

Info

Publication number
UY27844A1
UY27844A1 UY27844A UY27844A UY27844A1 UY 27844 A1 UY27844 A1 UY 27844A1 UY 27844 A UY27844 A UY 27844A UY 27844 A UY27844 A UY 27844A UY 27844 A1 UY27844 A1 UY 27844A1
Authority
UY
Uruguay
Prior art keywords
substituted
preparations
stratriens
alfa
strategies
Prior art date
Application number
UY27844A
Other languages
English (en)
Inventor
Dirk Kosemund
Gerd Muller
Alexander Hillisch
Peter Muhn
Karl-Heinrich Fritzemeier
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 UY27844A1 publication Critical patent/UY27844A1/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)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (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)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Transplantation (AREA)
  • Gynecology & Obstetrics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Urology & Nephrology (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

La presente invención describe nuevos estratrienos 9a-sustituidos de la fórmula general I donde R3, R7, R13, R16, y R17 y R17` tienen los significados indicados en la descripción, 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.
UY27844A 2002-06-11 2003-06-11 Estratrienos 9-alfa-sustituidos como estrógenos de eficacia selectiva. UY27844A1 (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
UY27844A1 true UY27844A1 (es) 2003-12-31

Family

ID=29723144

Family Applications (1)

Application Number Title Priority Date Filing Date
UY27844A UY27844A1 (es) 2002-06-11 2003-06-11 Estratrienos 9-alfa-sustituidos como estrógenos de eficacia selectiva.

Country Status (29)

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)
HK (1) HK1081203A1 (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 (8)

* 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
KR20100117603A (ko) * 2008-02-13 2010-11-03 바이엘 쉐링 파마 악티엔게젤샤프트 안정화 효과를 갖는 약물 전달 시스템
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

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
AU1855201A (en) * 1999-11-02 2001-05-14 Schering Aktiengesellschaft 18-nor-steroids as selectively active estrogens
JP3828423B2 (ja) * 2000-04-12 2006-10-04 シエーリング アクチエンゲゼルシャフト 8β−置換された11β−ペンチル−及び11β−ヘキシル−エストラ−1,3,5(10)−トリエン誘導体類

Also Published As

Publication number Publication date
TW200407331A (en) 2004-05-16
CA2486495A1 (en) 2003-12-18
DE50301116D1 (de) 2005-10-06
HRP20050009B1 (hr) 2013-07-31
NO20050127L (no) 2005-03-11
KR20050009745A (ko) 2005-01-25
AR040188A1 (es) 2005-03-16
RS50878B (sr) 2010-08-31
WO2003104253A2 (de) 2003-12-18
ECSP055530A (es) 2005-03-10
IL165321A (en) 2009-08-03
AU2003242683B9 (en) 2009-08-27
HRP20050009A2 (en) 2005-04-30
EP1517914A2 (de) 2005-03-30
UA78062C2 (en) 2007-02-15
KR101006612B1 (ko) 2011-01-10
ES2248770T3 (es) 2006-03-16
NO329563B1 (no) 2010-11-15
EA008442B1 (ru) 2007-06-29
TWI286140B (en) 2007-09-01
BR0312140A (pt) 2005-04-05
PL373090A1 (en) 2005-08-08
CU23414B7 (es) 2009-09-08
CR10289A (es) 2008-11-26
AU2003242683A1 (en) 2003-12-22
EA200401544A1 (ru) 2005-06-30
NO20050127D0 (no) 2005-01-10
PE20040613A1 (es) 2004-12-01
WO2003104253A3 (de) 2004-09-16
DE10226326A1 (de) 2004-01-15
AU2003242683B2 (en) 2009-07-02
CN1659181A (zh) 2005-08-24
CA2486495C (en) 2011-04-19
ZA200500217B (en) 2006-03-29
HK1081203A1 (en) 2006-05-12
EP1517914B1 (de) 2005-08-31
CN1293090C (zh) 2007-01-03
DK1517914T3 (da) 2006-01-16
JP2005533053A (ja) 2005-11-04
JP4615998B2 (ja) 2011-01-19
PL209910B1 (pl) 2011-11-30
MXPA04012491A (es) 2005-06-08
RS107004A (en) 2006-10-27
ATE303397T1 (de) 2005-09-15

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Legal Events

Date Code Title Description
109 Application deemed to be withdrawn

Effective date: 20150427