MXPA02010066A - Estratrienos sustituidos en 8beta-hidrocarbilo para uso como estrogenos selectivos. - Google Patents

Estratrienos sustituidos en 8beta-hidrocarbilo para uso como estrogenos selectivos.

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Publication number
MXPA02010066A
MXPA02010066A MXPA02010066A MXPA02010066A MXPA02010066A MX PA02010066 A MXPA02010066 A MX PA02010066A MX PA02010066 A MXPA02010066 A MX PA02010066A MX PA02010066 A MXPA02010066 A MX PA02010066A MX PA02010066 A MXPA02010066 A MX PA02010066A
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MX
Mexico
Prior art keywords
8szlig
compounds
uterus
estrogen
estratrienes
Prior art date
Application number
MXPA02010066A
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English (en)
Inventor
Karl-Heinrich Fritzemeier
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
Priority claimed from DE10019167A external-priority patent/DE10019167A1/de
Application filed by Schering Ag filed Critical Schering Ag
Publication of MXPA02010066A publication Critical patent/MXPA02010066A/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
    • C07J1/0066Estrane 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
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    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • AHUMAN NECESSITIES
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    • 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
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    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
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    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16Masculine contraceptives
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    • 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
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    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • 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
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • AHUMAN NECESSITIES
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    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30Oestrogens
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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
    • 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
    • C07J1/0074Esters
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    • 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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  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La invencion se relaciona con estratrienos sustituidos en 8° novedosos de la formula general (I), en donde R2, R3, R6, R6', R7, R7', R9, R11, R11',R12, R14, R15, R15', R16, R16', R17 y R17' son como se definen en la descripcion, y R8 representa un grupo alquilo o alquenilo lineal o de cadena ramificada, opcional, parcial o completamente halogenado con hasta 5 átomos de carbono, un grupo etinilo o prop-1-inilo. Los estratrienos de la invencion se utilizan como sustancias farmacéuticamente activas que tienen una mayor afinidad in vitro por las preparaciones de receptor de estrogeno de prostata de rata en comparacion con las preparaciones de receptor de estrogeno de °tero de rata y las cuales preferiblemente tienen un efecto preferencial in vivo sobre material oseo, en comparacion con el °tero, o un efecto pronunciado con respecto a la estimulacion de la expresion del receptor y transportador 5HT2a. La invencion se relaciona además con la produccion de estos compuestos novedosos, con su uso en terapia y con formas farmacéuticas de administracion que contienen compuestos novedosos. La invencion describe además el uso de tales compuestos para tratar a enfermedades y condiciones relacionadas con deficiencia de estrogeno, y con el uso de una parte estructural de estratrieno sustituido en 8°, en las estructuras totales de compuestos que están caracterizadas por una disociacion a favor de su efecto estrogénico en el hueso, en comparacion con el °tero.
MXPA02010066A 2000-04-12 2001-04-12 Estratrienos sustituidos en 8beta-hidrocarbilo para uso como estrogenos selectivos. MXPA02010066A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE10019167A DE10019167A1 (de) 2000-04-12 2000-04-12 Substituierte Estratriene als selektiv wirksame Estrogene
US20737000P 2000-05-26 2000-05-26
PCT/EP2001/004290 WO2001077139A1 (de) 2000-04-12 2001-04-12 8.beta.-hydrocarbyl-substituierte estratriene als selektiv wirksame estrogene

Publications (1)

Publication Number Publication Date
MXPA02010066A true MXPA02010066A (es) 2003-06-04

Family

ID=26005365

Family Applications (1)

Application Number Title Priority Date Filing Date
MXPA02010066A MXPA02010066A (es) 2000-04-12 2001-04-12 Estratrienos sustituidos en 8beta-hidrocarbilo para uso como estrogenos selectivos.

Country Status (26)

Country Link
US (3) US7378404B2 (es)
EP (2) EP1272505B1 (es)
JP (2) JP3828423B2 (es)
CN (1) CN100453549C (es)
AT (2) ATE302790T1 (es)
AU (3) AU2001258341B2 (es)
BG (1) BG107173A (es)
BR (1) BR0109983A (es)
CA (1) CA2406177C (es)
CZ (1) CZ20023382A3 (es)
DE (1) DE50112561D1 (es)
DK (2) DK1272504T3 (es)
EA (1) EA006299B1 (es)
EE (1) EE200200589A (es)
ES (2) ES2287127T3 (es)
HK (1) HK1057219A1 (es)
HR (1) HRP20020892B1 (es)
HU (1) HUP0300335A2 (es)
IL (2) IL152248A0 (es)
MX (1) MXPA02010066A (es)
NO (2) NO325337B1 (es)
NZ (1) NZ543724A (es)
PL (1) PL207488B1 (es)
PT (1) PT1272504E (es)
SK (1) SK14632002A3 (es)
WO (2) WO2001077139A1 (es)

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GB0020498D0 (en) * 2000-08-18 2000-10-11 Sterix Ltd Compound
DE10151363A1 (de) * 2001-10-17 2003-05-08 Schering Ag Somatotrope Therapie
DE10226326A1 (de) * 2002-06-11 2004-01-15 Schering Ag 9-alpha-substiuierte Estratriene als selektiv wirksame Estrogene
EP1468690B1 (en) * 2003-03-27 2008-10-08 Pantarhei Bioscience B.V. Use of estrogens for the treatment of infertility in male mammals
DE10318896A1 (de) 2003-04-22 2004-11-25 Schering Ag 8beta-Vinyl-11beta-(omega-substituierte)alkyl-estra-1,3,5(10)-triene
PT1689410E (pt) * 2003-11-26 2008-08-18 Bayer Schering Pharma Ag Prevenção e tratamento de doenças cardíacas hipertensivas pelos estrogénios selectivos 8beta-vinil-estra-1,3,5(10)-trieno-3,17beta-diol e 17beta-fluoro-9alfa-vinil-estra-1,3,5(10)-trieno-3,16alfa-diol
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EP2014672A1 (en) * 2007-07-12 2009-01-14 Bayer Schering Pharma Aktiengesellschaft 8-beta-substituted estratrienes as selectively active estrogens
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