PE20020848A1 - 11ß-HALOGENESTEROIDES, SU OBTENCION Y PREPARADOS FARMACEUTICOS QUE LOS CONTIENEN - Google Patents

11ß-HALOGENESTEROIDES, SU OBTENCION Y PREPARADOS FARMACEUTICOS QUE LOS CONTIENEN

Info

Publication number
PE20020848A1
PE20020848A1 PE2002000053A PE2002000053A PE20020848A1 PE 20020848 A1 PE20020848 A1 PE 20020848A1 PE 2002000053 A PE2002000053 A PE 2002000053A PE 2002000053 A PE2002000053 A PE 2002000053A PE 20020848 A1 PE20020848 A1 PE 20020848A1
Authority
PE
Peru
Prior art keywords
estr
ona
alkylene
hydroxy
methyl
Prior art date
Application number
PE2002000053A
Other languages
English (en)
Inventor
Rolf Bohlmann
Dieter Zopf
Reinhard Nubbemeyer
Hermann Kunzer
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 PE20020848A1 publication Critical patent/PE20020848A1/es

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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16Masculine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • 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
    • A61P5/26Androgens
    • 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
    • C07J1/0003Androstane derivatives
    • C07J1/0018Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa
    • C07J1/0022Androstane 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
    • C07J1/0003Androstane derivatives
    • C07J1/0018Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa
    • C07J1/0022Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C07J1/0025Esters
    • 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

Abstract

SE REFIERE A COMPUESTOS 11ß-HALOGENOESTEROIDES DE FORMULA I DONDE: X-Y-Z ES HC=C-C, H2C-C=C; R1 ES H, ESTA EN POSICION O, ß; R, P-Q-R; P Y Q SON ALQUILENO, ALQUENILENO, ALQUINILENO C1-C8; R ES CH3, CF3; Z NO ESTA SUSTITUIDO CON CON R1, CUANDO X-Y-Z ES H2C-C=C; R6 ES H, R7; R7 ES R, P-Q-R; R11 ES HALOGENO, R13 ES METILO, ETILO; R17' ES H, COR18; R18 ES ALQUILO, ALQUENILO, ALQUINILO C1-C18, ARILO, T-U-V OPCIONALMENTE SUSTITUIDO CON NR19R20, SOXR21m; T Y U SON ALQUILENO, ALQUENILENO, ALQUINILENO C1-C18, ALICICLICO C3-C12, ARILO, V ES ALQUILO, ALQUENILO, ALQUINILO C1-C18, ARILO; x ES 0-2; R19, R20, R21 SON H. SON COMPUESTOS PREFERIDOS 11ß-FLUORO-17ß-HIDROXI-7O-METIL-ESTR-4-EN-3-ONA; 11ß-CLORO-17ß-HIDROXI-7O-METIL-ESTR-4-EN-3-ONA, 17ß-HIDROXI-11ß-YODO-7O-METIL-ESTR-4-EN-3-ONA; 7O-ETIL-11ß-FLUORO-17ß-HIDROXI-ESTR-4-EN-3-ONA, ENTRE OTROS; TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS SON DERIVADOS DE TESTOSTERONA NO SENSIBLES A LA REDUCCION DE 5O-REDUCTASA, TIENEN EFECTO ANDROGENO
PE2002000053A 2001-01-24 2002-01-24 11ß-HALOGENESTEROIDES, SU OBTENCION Y PREPARADOS FARMACEUTICOS QUE LOS CONTIENEN PE20020848A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10104327A DE10104327A1 (de) 2001-01-24 2001-01-24 11beta-Halogensteroide, deren Herstellung und Verwendung zur Herstellung von Arzneimitteln sowie 11beta-Halogensteroide enthaltende pharmazeutische Präparate

Publications (1)

Publication Number Publication Date
PE20020848A1 true PE20020848A1 (es) 2002-10-26

Family

ID=7672351

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2002000053A PE20020848A1 (es) 2001-01-24 2002-01-24 11ß-HALOGENESTEROIDES, SU OBTENCION Y PREPARADOS FARMACEUTICOS QUE LOS CONTIENEN

Country Status (35)

Country Link
US (1) US7361645B2 (es)
EP (1) EP1353938B1 (es)
JP (1) JP4339591B2 (es)
KR (1) KR100728088B1 (es)
CN (1) CN1234721C (es)
AR (1) AR053299A1 (es)
AT (1) ATE386045T1 (es)
AU (1) AU2002238516B2 (es)
BG (1) BG66133B1 (es)
BR (1) BR0206653A (es)
CA (1) CA2434187C (es)
CY (1) CY1110377T1 (es)
CZ (1) CZ303553B6 (es)
DE (2) DE10104327A1 (es)
DK (1) DK1353938T3 (es)
EA (1) EA006674B1 (es)
EE (1) EE05274B1 (es)
ES (1) ES2300431T3 (es)
HK (1) HK1064678A1 (es)
HR (1) HRP20030661B1 (es)
HU (1) HUP0303020A3 (es)
IL (2) IL156807A0 (es)
MX (1) MXPA03006578A (es)
NO (1) NO325754B1 (es)
NZ (1) NZ527041A (es)
PE (1) PE20020848A1 (es)
PL (1) PL207582B1 (es)
PT (1) PT1353938E (es)
RS (1) RS50740B (es)
SK (1) SK287444B6 (es)
TW (1) TWI333494B (es)
UA (1) UA75907C2 (es)
UY (1) UY27133A1 (es)
WO (1) WO2002059139A1 (es)
ZA (1) ZA200306537B (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10234525A1 (de) * 2002-07-25 2004-02-05 Schering Ag Zusammensetzung, enthaltend ein androgenes 11ß-Halogensteroid und ein Gestagen sowie männliches Kontrazeptivum auf Basis dieser Zusammensetzung
KR101041328B1 (ko) 2002-07-24 2011-06-14 바이엘 쉐링 파마 악티엔게젤샤프트 7 알파-치환 11 알파-히드록시 스테로이드의 생산을위한 미생물학적 방법
DE10233723A1 (de) 2002-07-24 2004-02-12 Schering Ag Mikrobiologische Verfahren zur Herstellung von 7α-substituierten 11α-Hydroxysteroiden, daraus herstellbare 7α,17α-substituierte 11β-Halogensteroide, deren Herstellungsverfahren und Verwendung sowie pharmazeutische Präparate, die diese Verbindungen enthalten, sowie daraus herstellbare 7α-substituierte Estra-1,3,5(10)-triene
EP1524983B1 (de) * 2002-07-25 2008-01-02 Bayer Schering Pharma Aktiengesellschaft Zusammensetzung, enthaltend ein androgenes 11-b-halogensteroid und ein gestagen sowie m nnliches kontrazeptivum auf basis dieser zusammensetzung
JO2492B1 (en) * 2003-04-28 2009-10-05 شيرينج ايه جي A pharmaceutical formula in the form of aqueous gel for the skin use of its active ingredients
US7879357B2 (en) * 2003-04-28 2011-02-01 Bayer Schering Pharma Ag Pharmaceutical composition in the form of a hydrogel for transdermal administration of active ingredients
CN106188201B (zh) * 2014-10-08 2017-10-24 常州大学 工艺简单、适于降低还原剂浓度的合成睾酮方法
TWI530504B (zh) * 2014-12-01 2016-04-21 臺灣永光化學工業股份有限公司 烷基酸睾酮化合物之合成方法
US20220411460A1 (en) * 2021-06-29 2022-12-29 Board Of Regents, The University Of Texas System Modified glucocorticoids

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB863661A (en) * 1958-06-06 1961-03-22 Upjohn Co Improvements in or relating to steroids and the manufacture thereof
CH380118A (de) * 1959-06-17 1964-07-31 Ciba Geigy Neue Halogenandrostenverbindungen und Verfahren zu deren Herstellung
GB1159434A (en) * 1965-08-16 1969-07-23 Glaxo Lab Ltd 11beta&;-Fluoro-19-nor-Steroids
FR1489519A (fr) * 1965-08-16 1967-07-21 Glaxo Lab Ltd Procédé de préparation de nouveaux 19-nor-stéroïdes et produits obtenus
US3665021A (en) * 1966-07-29 1972-05-23 Glaxo Lab Ltd 9alpha-unsubstituted-11beta-chloro-l9 nos-steroids
GB1260463A (en) * 1968-01-29 1972-01-19 Glaxo Lab Ltd 11beta-BROMO-19-NOR-STEROIDS
DE2410443A1 (de) * 1974-03-01 1975-09-11 Schering Ag 11beta-fluor-androstene
DE2410442A1 (de) * 1974-03-01 1975-09-11 Schering Ag Verfahren zur herstellung von 11-fluorandrostenen
DE3214690A1 (de) * 1982-04-16 1983-10-27 Schering AG, 1000 Berlin und 4709 Bergkamen 11ss-chlor-(delta)(pfeil hoch)1(pfeil hoch)(pfeil hoch)5(pfeil hoch)-steroide, verfahren zu ihrer herstellung und diese enthaltende pharmazeutische praeparate
GB8721384D0 (en) * 1987-09-11 1987-10-21 Erba Farmitalia 17-substituted andro-sta-1 4-dien-3-one derivatives
US5342834A (en) * 1989-04-07 1994-08-30 The Population Council, Inc. Method for androgen supplementation
US20020012694A1 (en) * 1997-09-17 2002-01-31 Alfred J. Moo-Young Transdermal administration of ment
US6767902B2 (en) * 1997-09-17 2004-07-27 The Population Council, Inc. Androgen as a male contraceptive and non-contraceptive androgen replacement
US5952319A (en) * 1997-11-26 1999-09-14 Research Triangle Institute Androgenic steroid compounds and a method of making and using the same
CA2359218A1 (en) * 1999-03-08 2000-09-14 Akzo Nobel N.V. 14.beta., 17-alpha-hydroxymethylandrostane derivatives as androgens
ATE246703T1 (de) 1999-04-06 2003-08-15 Akzo Nobel Nv Oral wirksame 7-alpha-alkyl androgene
DE19959696A1 (de) * 1999-12-08 2001-06-21 Jenapharm Gmbh Ungesättigte 14,15-Cyclopropano-Androstane, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen

Also Published As

Publication number Publication date
NO325754B1 (no) 2008-07-14
BR0206653A (pt) 2004-02-03
KR100728088B1 (ko) 2007-06-14
PL207582B1 (pl) 2011-01-31
EA006674B1 (ru) 2006-02-24
IL156807A (en) 2008-08-07
YU59403A (sh) 2006-08-17
DE60224982T2 (de) 2009-04-09
DE60224982D1 (de) 2008-03-27
ATE386045T1 (de) 2008-03-15
HUP0303020A3 (en) 2012-03-28
UY27133A1 (es) 2002-07-31
EA200300756A1 (ru) 2004-02-26
SK9542003A3 (en) 2003-12-02
EP1353938B1 (en) 2008-02-13
BG108023A (bg) 2004-02-27
AU2002238516B2 (en) 2007-08-23
HUP0303020A2 (hu) 2003-12-29
CY1110377T1 (el) 2015-04-29
PT1353938E (pt) 2008-04-29
EE200300346A (et) 2003-12-15
NZ527041A (en) 2005-02-25
WO2002059139A1 (en) 2002-08-01
TWI333494B (en) 2010-11-21
CZ303553B6 (cs) 2012-12-05
ZA200306537B (en) 2004-09-08
PL361730A1 (en) 2004-10-04
BG66133B1 (bg) 2011-06-30
CA2434187A1 (en) 2002-08-01
JP4339591B2 (ja) 2009-10-07
HRP20030661A2 (en) 2005-06-30
HRP20030661B1 (en) 2011-10-31
CN1234721C (zh) 2006-01-04
HK1064678A1 (en) 2005-02-04
UA75907C2 (en) 2006-06-15
MXPA03006578A (es) 2003-09-22
DK1353938T3 (da) 2008-05-26
IL156807A0 (en) 2004-02-08
NO20033321D0 (no) 2003-07-23
US7361645B2 (en) 2008-04-22
EP1353938A1 (en) 2003-10-22
KR20030081391A (ko) 2003-10-17
EE05274B1 (et) 2010-02-15
CN1487950A (zh) 2004-04-07
JP2004517153A (ja) 2004-06-10
RS50740B (sr) 2010-08-31
CZ20032006A3 (cs) 2004-01-14
US20050075322A1 (en) 2005-04-07
DE10104327A1 (de) 2002-07-25
CA2434187C (en) 2009-06-16
ES2300431T3 (es) 2008-06-16
AR053299A1 (es) 2007-05-02
NO20033321L (no) 2003-09-24
SK287444B6 (sk) 2010-09-07

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FG Grant, registration
FD Application declared void or lapsed