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
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 UY26665A1 publication Critical patent/UY26665A1/es

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    • 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
    • C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • 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
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    • A61P15/16—Masculine contraceptives
    • A—HUMAN NECESSITIES
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    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • 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
    • C07J1/0062—Estrane derivatives substituted in position 17 alfa not substituted in position 17 beta
    • 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
    • C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • 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
    • C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C07J1/0074—Esters
    • 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

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
AU2001258341B2 (en) * 2000-04-12 2007-03-15 Schering Aktiengesellschaft 8beta-hydrocarbyl-substituted estratrienes for use as selective estrogens
DE10151114A1 (de) * 2001-10-15 2003-04-17 Schering Ag 8ß-Substituierte-11ß-aryl-estra-2,3,5(10)-trienderivate
PL1689410T3 (pl) * 2003-11-26 2008-10-31 Bayer Schering Pharma Ag Sposób zapobiegania i leczenia nadciśnieniowych chorób serca za pomocą selektywnych estrogenów: 8ß-winylo-estra-1,3,5(10)-trien-3,17ß-diolu i 17ß-fluoro-9a-winylo-estra-1,3,5(10)-trien-3,16a-diolu
US7714012B2 (en) * 2006-11-17 2010-05-11 Trustees Of Dartmouth University 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
US20120282340A1 (en) * 2008-11-21 2012-11-08 Bayer Schering 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
JP2003534248A (ja) 2003-11-18
KR20030028734A (ko) 2003-04-10
KR100825534B1 (ko) 2008-04-25
JP4860880B2 (ja) 2012-01-25
PE20011215A1 (es) 2001-11-29
DE10019167A1 (de) 2001-10-18
DE50107204D1 (de) 2005-09-29
ZA200209149B (en) 2007-10-31
YU77302A (sh) 2005-11-28
AR028329A1 (es) 2003-05-07
TWI288138B (en) 2007-10-11
UA79073C2 (en) 2007-05-25
SI1272504T1 (sl) 2007-10-31

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Effective date: 20130717