BR0312140A - Estratrienos 9-alfa-substituìdos como estrogênios seletivamente eficazes - Google Patents

Estratrienos 9-alfa-substituìdos como estrogênios seletivamente eficazes

Info

Publication number
BR0312140A
BR0312140A BR0312140-2A BR0312140A BR0312140A BR 0312140 A BR0312140 A BR 0312140A BR 0312140 A BR0312140 A BR 0312140A BR 0312140 A BR0312140 A BR 0312140A
Authority
BR
Brazil
Prior art keywords
substituted
alpha
estrogen
well
selectively effective
Prior art date
Application number
BR0312140-2A
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 BR0312140A publication Critical patent/BR0312140A/pt

Links

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)
  • 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)
  • Transplantation (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

"ESTRATRIENOS 9-ALFA-SUBSTITUìDOS COMO ESTROGêNIOS SELETIVAMENTE EFICAZES". A presente invenção refere-se a novos estratrienos 9a-substituídos da fórmula geral (I), na qual R3, R7, R7<39>, R13, R16 bem como R17 e R17<198> têm os significados indicados na descrição bem como R9 representa um radical alquenila em cadeia linear ou ramificada, eventualmente parcial ou totalmente halogenado com 2 até 6 átomos de carbono, um radical etinila ou prop-1-inila, como substâncias ativas farmacêuticas, que in vitro apresentam uma maior afinidade corn preparações do receptor de estrogênio de próstata de rato do que com preparações do receptor de estrogênio de útero de rato fêmea e in vivo apresenta de preferência, um efeito preferencial no ovário em comparação com o útero, sua preparação, sua aplicação terapêutica e formas de administração farmacêuticas, que contêm os novos compostos. A invenção descreve além disso, a aplicação destes compostos para o tratamento de doenças e estados devido a deficiência de estrogênio.
BR0312140-2A 2002-06-11 2003-06-11 Estratrienos 9-alfa-substituìdos como estrogênios seletivamente eficazes BR0312140A (pt)

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 (1)

Publication Number Publication Date
BR0312140A true BR0312140A (pt) 2005-04-05

Family

ID=29723144

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0312140-2A BR0312140A (pt) 2002-06-11 2003-06-11 Estratrienos 9-alfa-substituìdos como estrogênios seletivamente eficazes

Country Status (29)

Country Link
EP (1) EP1517914B1 (pt)
JP (1) JP4615998B2 (pt)
KR (1) KR101006612B1 (pt)
CN (1) CN1293090C (pt)
AR (1) AR040188A1 (pt)
AT (1) ATE303397T1 (pt)
AU (1) AU2003242683B9 (pt)
BR (1) BR0312140A (pt)
CA (1) CA2486495C (pt)
CR (1) CR10289A (pt)
CU (1) CU23414B7 (pt)
DE (2) DE10226326A1 (pt)
DK (1) DK1517914T3 (pt)
EA (1) EA008442B1 (pt)
EC (1) ECSP055530A (pt)
ES (1) ES2248770T3 (pt)
HK (1) HK1081203A1 (pt)
HR (1) HRP20050009B1 (pt)
IL (1) IL165321A (pt)
MX (1) MXPA04012491A (pt)
NO (1) NO329563B1 (pt)
PE (1) PE20040613A1 (pt)
PL (1) PL209910B1 (pt)
RS (1) RS50878B (pt)
TW (1) TWI286140B (pt)
UA (1) UA78062C2 (pt)
UY (1) UY27844A1 (pt)
WO (1) WO2003104253A2 (pt)
ZA (1) ZA200500217B (pt)

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
ES2307064T3 (es) * 2003-11-26 2008-11-16 Bayer Schering Pharma Aktiengesellschaft Prevencion y tratamiento de enfermedades cardiacas hipertensivas por los estrogenos selectivos 8beta-vinil-estra-1,3,5(10)-trien-3,17beta-diol y 17beta-fluor-9alfa-vinil-estra-1,3,5(10)-trien-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
MX2010008945A (es) * 2008-02-13 2010-09-07 Bayer Schering Pharma Ag Sistema de administracion de drogas con efecto estabilizante.
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
CA2744127A1 (en) * 2008-11-21 2010-05-27 Bayer Schering Pharma Aktiengesellschaft Drug delivery system
AU2015308987B2 (en) 2014-08-26 2021-02-18 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
DK1226155T3 (da) * 1999-11-02 2007-09-10 Bayer Schering Pharma Ag 18-nor-steroider som selektivt virksomme östrogener
CZ20023382A3 (cs) * 2000-04-12 2003-02-12 Schering Aktiengesellschaft Substituované estratrieny jako selektivně účinné estrogeny

Also Published As

Publication number Publication date
HRP20050009B1 (hr) 2013-07-31
CN1293090C (zh) 2007-01-03
DE10226326A1 (de) 2004-01-15
TWI286140B (en) 2007-09-01
HK1081203A1 (en) 2006-05-12
NO20050127L (no) 2005-03-11
EA200401544A1 (ru) 2005-06-30
RS107004A (en) 2006-10-27
ATE303397T1 (de) 2005-09-15
JP2005533053A (ja) 2005-11-04
WO2003104253A3 (de) 2004-09-16
ECSP055530A (es) 2005-03-10
AR040188A1 (es) 2005-03-16
AU2003242683A1 (en) 2003-12-22
JP4615998B2 (ja) 2011-01-19
UY27844A1 (es) 2003-12-31
CN1659181A (zh) 2005-08-24
CA2486495A1 (en) 2003-12-18
KR101006612B1 (ko) 2011-01-10
AU2003242683B2 (en) 2009-07-02
PL373090A1 (en) 2005-08-08
TW200407331A (en) 2004-05-16
EP1517914A2 (de) 2005-03-30
ES2248770T3 (es) 2006-03-16
KR20050009745A (ko) 2005-01-25
EA008442B1 (ru) 2007-06-29
PE20040613A1 (es) 2004-12-01
MXPA04012491A (es) 2005-06-08
EP1517914B1 (de) 2005-08-31
IL165321A (en) 2009-08-03
PL209910B1 (pl) 2011-11-30
NO329563B1 (no) 2010-11-15
DE50301116D1 (de) 2005-10-06
RS50878B (sr) 2010-08-31
CU23414B7 (es) 2009-09-08
AU2003242683B9 (en) 2009-08-27
CA2486495C (en) 2011-04-19
WO2003104253A2 (de) 2003-12-18
ZA200500217B (en) 2006-03-29
CR10289A (es) 2008-11-26
UA78062C2 (en) 2007-02-15
DK1517914T3 (da) 2006-01-16
HRP20050009A2 (en) 2005-04-30
NO20050127D0 (no) 2005-01-10

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Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B25D Requested change of name of applicant approved

Owner name: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT (DE)

B25D Requested change of name of applicant approved

Owner name: BAYER PHARMA AKTIENGESELLSCHAFT (DE)

B25A Requested transfer of rights approved

Owner name: BAYER INTELLECTUAL PROPERTY GMBH. (DE)

B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 13A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2385 DE 20-09-2016 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.