BG105804A - 16-hydroxyestratrienes as selective acting estrogens - Google Patents

16-hydroxyestratrienes as selective acting estrogens

Info

Publication number
BG105804A
BG105804A BG105804A BG10580401A BG105804A BG 105804 A BG105804 A BG 105804A BG 105804 A BG105804 A BG 105804A BG 10580401 A BG10580401 A BG 10580401A BG 105804 A BG105804 A BG 105804A
Authority
BG
Bulgaria
Prior art keywords
estrogens
5ht2a
hydroxyestratrienes
uterus
effect
Prior art date
Application number
BG105804A
Other languages
Bulgarian (bg)
Inventor
Hermann Kunzer
Rudolf Knauthe
Monika Lessl
Karl-Heinrich Fritzemeier
Christa Hegele-Hartung
Ulf Bomer
Gerd Muller
Dirk Kosemund
Original Assignee
Schering Aktiengesellschaft
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 Aktiengesellschaft filed Critical Schering Aktiengesellschaft
Publication of BG105804A publication Critical patent/BG105804A/en

Links

Classifications

    • 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
    • C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • 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
    • A61P19/02—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
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • 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
    • 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
    • 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
    • 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
    • C07J15/00—Stereochemically pure steroids containing carbon, hydrogen, halogen or oxygen having a partially or totally inverted skeleton, e.g. retrosteroids, L-isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J33/00—Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J33/002—Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J53/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by condensation with a carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms, including carboxyclic rings fused to the cyclopenta(a)hydrophenanthrene skeleton are included in this class
    • C07J53/002—Carbocyclic rings fused
    • C07J53/004—3 membered carbocyclic rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Toxicology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

The invention relates to new 3,16-dihydroxyestra-1,3,5/10-triene derivatives with the general formula wherein the meanings of the substituents are given in the description. The compounds are a novel type of steroid estrogens with selective effect on tissues and are used as pharmaceutical substances. In vitro they have a higher affinity to estrogen receptor preparations of the rat prostate of rats and of rat uterus, and in vivo they have a preferential effect basically on the bones as compared to the uterus and/or a marked effect with regard to the stimulation of the expansion of the 5HT2a-receptor and a 5HT2a-transporter. The invention also relates to methods for their production and their use in therapy, and to pharmaceutical forms containing said novel compounds. 52 claims
BG105804A 1999-02-09 2001-08-09 16-hydroxyestratrienes as selective acting estrogens BG105804A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19906159A DE19906159A1 (en) 1999-02-09 1999-02-09 16-hydroxyestratrienes as selectively active estrogens
PCT/EP2000/001073 WO2000047603A2 (en) 1999-02-09 2000-02-09 16-hydroxyestratrienes as selective estrogens

Publications (1)

Publication Number Publication Date
BG105804A true BG105804A (en) 2002-03-29

Family

ID=7897485

Family Applications (1)

Application Number Title Priority Date Filing Date
BG105804A BG105804A (en) 1999-02-09 2001-08-09 16-hydroxyestratrienes as selective acting estrogens

Country Status (30)

Country Link
EP (2) EP1144431B1 (en)
JP (1) JP2002536455A (en)
KR (1) KR20010101822A (en)
CN (1) CN1346364A (en)
AR (1) AR034392A1 (en)
AT (1) ATE313553T1 (en)
AU (1) AU2909500A (en)
BG (1) BG105804A (en)
BR (1) BR0008076A (en)
CA (1) CA2359660A1 (en)
CO (1) CO5150223A1 (en)
CZ (1) CZ20012843A3 (en)
DE (2) DE19906159A1 (en)
DK (1) DK1144431T3 (en)
EA (1) EA200100828A1 (en)
EE (1) EE200100412A (en)
ES (1) ES2255983T3 (en)
HK (1) HK1046145A1 (en)
HU (1) HUP0200055A3 (en)
IL (1) IL144455A0 (en)
MX (1) MXPA01008065A (en)
NO (1) NO20013860L (en)
NZ (1) NZ513409A (en)
PE (1) PE20001461A1 (en)
PL (1) PL350360A1 (en)
PT (1) PT1144431E (en)
SK (1) SK11302001A3 (en)
WO (1) WO2000047603A2 (en)
YU (1) YU57201A (en)
ZA (1) ZA200107388B (en)

Families Citing this family (15)

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DE10039199A1 (en) * 2000-08-10 2002-02-21 Schering Ag Combination preparations from an ERß selective estrogen and a SERM or antiestrogen
DE10048634A1 (en) * 2000-09-27 2002-04-18 Jenapharm Gmbh 19-Nor-17alpha-pregna-1,3,5 (10) -trien-17beta-ole with a 21, 16alpha lactone ring
DE10151365A1 (en) 2001-10-17 2003-04-30 Schering Ag New 17-chloro-D-homosteroids, useful as estrogen receptor ligands for female or male contraception or treating benign or malignant proliferative diseases of the ovary
WO2002068548A1 (en) * 2001-02-27 2002-09-06 Schering Ag Use of erss-selective ligands for regulating fertility and compounds useful therefore
DE10151114A1 (en) * 2001-10-15 2003-04-17 Schering Ag New 8 beta-substituted-11 beta-aryl-estra-2,3,5(10)-triene derivatives, are tissue-selective estrogens useful e.g. as female or male contraceptives or for treating ovarian carcinoma
DE10151363A1 (en) * 2001-10-17 2003-05-08 Schering Ag Use of estrogen receptor beta agonists to prepare medicaments for producing somatotropic and organotropic effects on the CNS, circulatory, skeletal and immune system in aging men and women
US7414043B2 (en) 2002-06-11 2008-08-19 Schering Ag 9-α-substituted estratrienes as selectively active estrogens
DE10226326A1 (en) * 2002-06-11 2004-01-15 Schering Ag 9-alpha-substituted estratrienes as selective estrogens
TWI389917B (en) * 2006-04-13 2013-03-21 Sigma Tau Ind Farmaceuti Azaheterocyclyl derivatives of androstanes and androstenes as medicaments for cardiovascular disorders
TWI392682B (en) * 2006-04-13 2013-04-11 Sigma Tau Ind Farmaceuti Amino derivatives of androstanes and androstenes as medicaments for cardiovascular disorders
SE536263C2 (en) * 2011-12-21 2013-07-23 Airqone Building Scandinavia Ab Gas medium purifier including means for controlled supply of ionized air
WO2018039110A1 (en) * 2016-08-22 2018-03-01 Or-Genix Therapeutics, Inc. Estrogen receptor beta selective ligands
WO2019041078A1 (en) * 2017-08-28 2019-03-07 Zhejiang Jiachi Pharmaceutical Development Ltd. Asymmetric synthesis and uses of compounds in disease treatments
AU2019335005A1 (en) 2018-09-07 2021-03-18 Trustees Of Dartmouth College C19 scaffolds and steroids and methods of use and manufacture thereof
CN115154474A (en) * 2021-04-01 2022-10-11 中国人民解放军总医院 Application of cycloartane type triterpenoid saponin compound in preparation of T cell immunosuppressive agent

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Also Published As

Publication number Publication date
EP1144431A3 (en) 2002-06-12
KR20010101822A (en) 2001-11-14
BR0008076A (en) 2002-02-05
HK1046145A1 (en) 2002-12-27
IL144455A0 (en) 2002-05-23
CA2359660A1 (en) 2000-08-17
ES2255983T3 (en) 2006-07-16
HUP0200055A2 (en) 2002-05-29
EA200100828A1 (en) 2002-04-25
EP1144431A2 (en) 2001-10-17
ZA200107388B (en) 2005-01-25
HUP0200055A3 (en) 2002-10-28
AU2909500A (en) 2000-08-29
WO2000047603A3 (en) 2001-08-02
PT1144431E (en) 2006-05-31
DK1144431T3 (en) 2006-05-08
CZ20012843A3 (en) 2002-01-16
CN1346364A (en) 2002-04-24
DE19906159A1 (en) 2000-08-10
NZ513409A (en) 2004-02-27
YU57201A (en) 2005-06-10
WO2000047603A2 (en) 2000-08-17
JP2002536455A (en) 2002-10-29
MXPA01008065A (en) 2002-04-24
EE200100412A (en) 2002-12-16
DE50011908D1 (en) 2006-01-26
EP1144431B1 (en) 2005-12-21
PL350360A1 (en) 2002-12-02
AR034392A1 (en) 2004-02-25
CO5150223A1 (en) 2002-04-29
SK11302001A3 (en) 2002-01-07
NO20013860D0 (en) 2001-08-08
EP1580192A2 (en) 2005-09-28
ATE313553T1 (en) 2006-01-15
NO20013860L (en) 2001-10-08
WO2000047603A9 (en) 2001-09-07
PE20001461A1 (en) 2000-12-18

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