EA008442B1 - 9α-ЗАМЕЩЁННЫЕ ЭСТРАТРИЕНЫ В КАЧЕСТВЕ ЭСТРОГЕНОВ ИЗБИРАТЕЛЬНОГО ДЕЙСТВИЯ - Google Patents

9α-ЗАМЕЩЁННЫЕ ЭСТРАТРИЕНЫ В КАЧЕСТВЕ ЭСТРОГЕНОВ ИЗБИРАТЕЛЬНОГО ДЕЙСТВИЯ Download PDF

Info

Publication number
EA008442B1
EA008442B1 EA200401544A EA200401544A EA008442B1 EA 008442 B1 EA008442 B1 EA 008442B1 EA 200401544 A EA200401544 A EA 200401544A EA 200401544 A EA200401544 A EA 200401544A EA 008442 B1 EA008442 B1 EA 008442B1
Authority
EA
Eurasian Patent Office
Prior art keywords
trien
diol
estra
compounds
homo
Prior art date
Application number
EA200401544A
Other languages
English (en)
Russian (ru)
Other versions
EA200401544A1 (ru
Inventor
Дирк Коземунд
Герд Мюллер
Александер Хиллиш
Карл-Генрих Фритцемайер
Петер Мун
Original Assignee
Шеринг Акциенгезельшафт
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 Шеринг Акциенгезельшафт filed Critical Шеринг Акциенгезельшафт
Publication of EA200401544A1 publication Critical patent/EA200401544A1/ru
Publication of EA008442B1 publication Critical patent/EA008442B1/ru

Links

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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Transplantation (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (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)
EA200401544A 2002-06-11 2003-06-11 9α-ЗАМЕЩЁННЫЕ ЭСТРАТРИЕНЫ В КАЧЕСТВЕ ЭСТРОГЕНОВ ИЗБИРАТЕЛЬНОГО ДЕЙСТВИЯ EA008442B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10226326A DE10226326A1 (de) 2002-06-11 2002-06-11 9-alpha-substiuierte Estratriene als selektiv wirksame Estrogene
PCT/EP2003/006172 WO2003104253A2 (de) 2002-06-11 2003-06-11 9-alpha-substituierte estratriene als selektiv wirksame estrogene

Publications (2)

Publication Number Publication Date
EA200401544A1 EA200401544A1 (ru) 2005-06-30
EA008442B1 true EA008442B1 (ru) 2007-06-29

Family

ID=29723144

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200401544A EA008442B1 (ru) 2002-06-11 2003-06-11 9α-ЗАМЕЩЁННЫЕ ЭСТРАТРИЕНЫ В КАЧЕСТВЕ ЭСТРОГЕНОВ ИЗБИРАТЕЛЬНОГО ДЕЙСТВИЯ

Country Status (28)

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

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
EP1689410B1 (en) * 2003-11-26 2008-05-21 Bayer Schering Pharma 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
EP2252261A2 (en) * 2008-02-13 2010-11-24 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
WO2010057594A1 (en) * 2008-11-21 2010-05-27 Bayer Schering Pharma Aktiengesellschaft Drug delivery system
EP3185881B1 (en) 2014-08-26 2022-03-09 Betanien Hospital Methods, agents and compositions for treatment of inflammatory conditions
CA3109978A1 (en) * 2018-09-07 2020-03-12 Trustees Of Dartmouth College C19 scaffolds and steroids and methods of use and manufacture thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3960841A (en) * 1973-07-13 1976-06-01 Schering Aktiengesellschaft 3,17,18-Trihydroxy-1,3,5(10)-estratrienes
DE19906159A1 (de) * 1999-02-09 2000-08-10 Schering Ag 16-Hydroxyestratriene als selektiv wirksame Estrogene

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6154158A (en) * 1998-06-30 2000-11-28 Qualcomm Incorporated Digital-to-analog converter D.C. offset correction comparing converter input and output signals
EP1226155B1 (de) * 1999-11-02 2007-05-02 Bayer Schering Pharma AG 18-nor-steroide als selektiv wirksame estrogene
AU5834101A (en) * 2000-04-12 2001-10-23 Schering Ag 8ss-hydrocarbyl-substituted estratrienes for use as selective estrogens

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3960841A (en) * 1973-07-13 1976-06-01 Schering Aktiengesellschaft 3,17,18-Trihydroxy-1,3,5(10)-estratrienes
DE19906159A1 (de) * 1999-02-09 2000-08-10 Schering Ag 16-Hydroxyestratriene als selektiv wirksame Estrogene

Also Published As

Publication number Publication date
CA2486495C (en) 2011-04-19
TWI286140B (en) 2007-09-01
PL373090A1 (en) 2005-08-08
HRP20050009B1 (hr) 2013-07-31
ES2248770T3 (es) 2006-03-16
AU2003242683A1 (en) 2003-12-22
NO20050127L (no) 2005-03-11
WO2003104253A2 (de) 2003-12-18
ZA200500217B (en) 2006-03-29
DE10226326A1 (de) 2004-01-15
CN1659181A (zh) 2005-08-24
JP4615998B2 (ja) 2011-01-19
CN1293090C (zh) 2007-01-03
KR20050009745A (ko) 2005-01-25
DK1517914T3 (da) 2006-01-16
AU2003242683B2 (en) 2009-07-02
NO20050127D0 (no) 2005-01-10
NO329563B1 (no) 2010-11-15
ECSP055530A (es) 2005-03-10
HRP20050009A2 (en) 2005-04-30
PE20040613A1 (es) 2004-12-01
KR101006612B1 (ko) 2011-01-10
HK1081203A1 (en) 2006-05-12
PL209910B1 (pl) 2011-11-30
TW200407331A (en) 2004-05-16
UA78062C2 (en) 2007-02-15
IL165321A (en) 2009-08-03
CR10289A (es) 2008-11-26
EP1517914A2 (de) 2005-03-30
CU23414B7 (es) 2009-09-08
UY27844A1 (es) 2003-12-31
CA2486495A1 (en) 2003-12-18
DE50301116D1 (de) 2005-10-06
MXPA04012491A (es) 2005-06-08
RS50878B (sr) 2010-08-31
RS107004A (sr) 2006-10-27
AU2003242683B9 (en) 2009-08-27
AR040188A1 (es) 2005-03-16
JP2005533053A (ja) 2005-11-04
EP1517914B1 (de) 2005-08-31
BR0312140A (pt) 2005-04-05
WO2003104253A3 (de) 2004-09-16
EA200401544A1 (ru) 2005-06-30
ATE303397T1 (de) 2005-09-15

Similar Documents

Publication Publication Date Title
US7414043B2 (en) 9-α-substituted estratrienes as selectively active estrogens
US6958327B1 (en) 18 Norsteroids as selectively active estrogens
EA006299B1 (ru) 8β-ГИДРОКАРБИЛЗАМЕЩЕННЫЕ ЭСТРАТРИЕНЫ В КАЧЕСТВЕ ЭСТРОГЕНОВ ИЗБИРАТЕЛЬНОГО ДЕЙСТВИЯ
CA2371972A1 (en) Ent-steroids as selectively active estrogens
KR20010101822A (ko) 선택적 에스트로겐으로서 16-히드록시에스트라트리엔
EA008442B1 (ru) 9α-ЗАМЕЩЁННЫЕ ЭСТРАТРИЕНЫ В КАЧЕСТВЕ ЭСТРОГЕНОВ ИЗБИРАТЕЛЬНОГО ДЕЙСТВИЯ
ES2286042T3 (es) 18-nor-esteroides como estrogenos eficaces selectivamente.
ES2393942T3 (es) 16,ALFA-FLUORO-ESTRATIENOS 8-BETA- sustituidos en calidad de estrógenos selectivamente activos
US20060270845A1 (en) 16-Hydroxyestratrienes as selectively active estrogens
NZ524485A (en) 4-halogenated 17-methylene steroids, method for the production thereof and pharmaceutical compositions containing these compounds
NZ536882A (en) 9-Alpha-substituted estratrienes as selectively active estrogens
JP2007532688A (ja) 17α−フルオロ−17β−ヒドロキシイミノメチルステロイド、それらを製造する方法および前記化合物を含んでなる医薬組成物
HK1142612A (en) 8-beta-substituted estratrienes as selectively active estrogens
US20050282791A1 (en) 18-nor steroids as selectively active estrogens
AU2004201405A1 (en) Ent-Steroids as selectively active estrogens

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ KZ KG MD TJ TM

PD4A Registration of transfer of a eurasian patent in accordance with the succession in title
TC4A Change in name of a patent proprietor in a eurasian patent
PC4A Registration of transfer of a eurasian patent by assignment
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): BY RU