UY26665A1 - Estratrienos sustituidos como estrógenos selectivamente activos - Google Patents

Estratrienos sustituidos como estrógenos selectivamente activos

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Publication number
UY26665A1
UY26665A1 UY26665A UY26665A UY26665A1 UY 26665 A1 UY26665 A1 UY 26665A1 UY 26665 A UY26665 A UY 26665A UY 26665 A UY26665 A UY 26665A UY 26665 A1 UY26665 A1 UY 26665A1
Authority
UY
Uruguay
Prior art keywords
uterus
compounds
effect
substituted
8beta
Prior art date
Application number
UY26665A
Other languages
English (en)
Inventor
Walter Elger
Christa Hegele-Hartung
Uwe Kollenkirchen
Olaf Peters
Alexander Hillisch
Ina Thieme
Karl-Heinrich Fritzemeier
Vladimir Patchev
Original Assignee
Schering Ag
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Publication date
Application filed by Schering Ag filed Critical Schering Ag
Publication of UY26665A1 publication Critical patent/UY26665A1/es

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    • 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
    • C07J1/0059Estrane derivatives substituted in position 17 by a keto group
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • 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
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • 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
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16Masculine 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
    • A61P15/18Feminine contraceptives
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    • A61P19/00Drugs for skeletal disorders
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    • 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
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
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    • A61P5/00Drugs for disorders of the endocrine system
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • 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
    • C07J1/0062Estrane derivatives substituted in position 17 alfa not substituted in position 17 beta
    • 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
    • C07J1/007Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • 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
    • C07J1/007Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C07J1/0074Esters
    • 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

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

Abstract

Estratrienos 8beta - sustituidos de la fórmula general I donde R2, R3, R6, R6´, R7, R7´, R9, R11, R11´, R12, R14, R15, R15´, R16, R16´, R17 y R17´ tienen los significados indicados en la descripción y R8 significa un radical alquilo o alquenilo de cadena lineal o ramificada, opcionalmente parcial o completamente halogenado con hasta 5 átomos de carbono, un radical etinilo o prop -1- inilo, como principios activos farmacéuticos que presentan in vitro una mayor afinidad con preparaciones de receptores estrogénicos de próstata de rata que con preparaciones de receptores estrogénicos de útero de rata, y que presentan in vivo preferentemente un efecto preferencial en el hueso en comparación con el útero y/o un marcado efecto respecto de la estimulación de la expresión del receptor y transportador 5HT2a, a su preparación, su aplicación terapéutica y a formas de administración farmacéutica que contienen los nuevos compuestos. La invención describe, además, la utilización de estos compuestos para el tratamiento de enfermedades y estados originados por la deficiencia estrogénica y a la utilización de una parte estructural de estratrienos 8beta- sustituidos en estructuras generales de compuestos que presentan una disociación a favor de su efecto estrógeno en el hueso en comparación con el útero.
UY26665A 2000-04-12 2001-04-11 Estratrienos sustituidos como estrógenos selectivamente activos UY26665A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10019167A DE10019167A1 (de) 2000-04-12 2000-04-12 Substituierte Estratriene als selektiv wirksame Estrogene

Publications (1)

Publication Number Publication Date
UY26665A1 true UY26665A1 (es) 2001-11-30

Family

ID=7639163

Family Applications (1)

Application Number Title Priority Date Filing Date
UY26665A UY26665A1 (es) 2000-04-12 2001-04-11 Estratrienos sustituidos como estrógenos selectivamente activos

Country Status (11)

Country Link
JP (1) JP4860880B2 (es)
KR (1) KR100825534B1 (es)
AR (1) AR028329A1 (es)
DE (2) DE10019167A1 (es)
PE (1) PE20011215A1 (es)
SI (1) SI1272504T1 (es)
TW (1) TWI288138B (es)
UA (1) UA79073C2 (es)
UY (1) UY26665A1 (es)
YU (1) YU77302A (es)
ZA (1) ZA200209149B (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ543724A (en) * 2000-04-12 2007-07-27 Schering Ag 8beta-hydrocarbyl-substituted estratrienes as selectively active estrogens
DE10151114A1 (de) * 2001-10-15 2003-04-17 Schering Ag 8ß-Substituierte-11ß-aryl-estra-2,3,5(10)-trienderivate
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
EP2094651A1 (en) * 2006-11-17 2009-09-02 Trustees Of Dartmouth College Synthesis and biological activities of new tricyclic-bis-enones (tbes)
EP2014672A1 (en) * 2007-07-12 2009-01-14 Bayer Schering Pharma Aktiengesellschaft 8-beta-substituted estratrienes as selectively active estrogens
EP2358351A1 (en) * 2008-11-21 2011-08-24 Bayer Pharma Aktiengesellschaft Drug delivery system

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3681407A (en) 1969-06-18 1972-08-01 American Cyanamid Co 3-methoxy 8{62 -methylestra 1,3,5(10),9(11)-tetraene-17{62 -carboxylic acid lower alkyl ester and intermediates in the preparation thereof
US3806546A (en) 1969-06-18 1974-04-23 American Cyanamid Co Steroid-like compounds and method of synthesis
US3736345A (en) 1971-05-18 1973-05-29 American Cyanamid Co Steroid-like compounds and method of synthesis

Also Published As

Publication number Publication date
ZA200209149B (en) 2007-10-31
SI1272504T1 (sl) 2007-10-31
JP2003534248A (ja) 2003-11-18
DE10019167A1 (de) 2001-10-18
PE20011215A1 (es) 2001-11-29
UA79073C2 (en) 2007-05-25
DE50107204D1 (de) 2005-09-29
JP4860880B2 (ja) 2012-01-25
KR100825534B1 (ko) 2008-04-25
KR20030028734A (ko) 2003-04-10
AR028329A1 (es) 2003-05-07
YU77302A (sh) 2005-11-28
TWI288138B (en) 2007-10-11

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