CA2421302A1 - 4-halogenated 17-methylene steroids, method for the production thereof and pharmaceutical compositions containing these compounds - Google Patents

4-halogenated 17-methylene steroids, method for the production thereof and pharmaceutical compositions containing these compounds Download PDF

Info

Publication number
CA2421302A1
CA2421302A1 CA002421302A CA2421302A CA2421302A1 CA 2421302 A1 CA2421302 A1 CA 2421302A1 CA 002421302 A CA002421302 A CA 002421302A CA 2421302 A CA2421302 A CA 2421302A CA 2421302 A1 CA2421302 A1 CA 2421302A1
Authority
CA
Canada
Prior art keywords
compounds
production
pharmaceutical compositions
compositions containing
halogenated
Prior art date
Legal status (The legal status 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 status listed.)
Granted
Application number
CA002421302A
Other languages
French (fr)
Other versions
CA2421302C (en
Inventor
Bernd Menzenbach
Walter Elger
Peter Droescher
Alexander Hillisch
Gunter Kaufmann
Hans-Udo Schweikert
Gerd Muller
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer Pharma AG
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2421302A1 publication Critical patent/CA2421302A1/en
Application granted granted Critical
Publication of CA2421302C publication Critical patent/CA2421302C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C07J13/007—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 17 (20)
    • 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
    • A61P15/16—Masculine 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
    • A61P15/18—Feminine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • 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
    • A61P5/28—Antiandrogens
    • 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
    • A61P5/34—Gestagens

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention relates to 17-Methylene steroids. Method for the production thereof and pharmaceutical compositions containing these compounds. The inventive compounds have an active profile with a hybrid character of such that they act as inhibitors of the 5.alpha.-reductase and, at the same time, as gestagens. Said compounds are thus suited for treating medical disorders that, in men and women, are a result of an increased androgen level in certa in organs and tissues. The inventive compounds combined with other hormonal substances such as estrogen, testosterone or a potent androgen are suited as contraceptives for women and men.
CA002421302A 2000-09-04 2001-08-29 4-halogenated 17-methylene steroids, method for the production thereof and pharmaceutical compositions containing these compounds Expired - Fee Related CA2421302C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE10043846.6 2000-09-04
DE10043846A DE10043846A1 (en) 2000-09-04 2000-09-04 17-methylene steroids, process for their preparation and pharmaceutical compositions containing them
PCT/EP2001/009943 WO2002019971A1 (en) 2000-09-04 2001-08-29 4-halogenated 17-methylene steroids, method for the production thereof and pharmaceutical compositions containing these compounds

Publications (2)

Publication Number Publication Date
CA2421302A1 true CA2421302A1 (en) 2003-03-03
CA2421302C CA2421302C (en) 2007-08-14

Family

ID=7655148

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002421302A Expired - Fee Related CA2421302C (en) 2000-09-04 2001-08-29 4-halogenated 17-methylene steroids, method for the production thereof and pharmaceutical compositions containing these compounds

Country Status (29)

Country Link
EP (1) EP1423407B1 (en)
JP (1) JP2004513084A (en)
KR (1) KR100530816B1 (en)
CN (1) CN1262560C (en)
AT (1) ATE319733T1 (en)
AU (2) AU2002210470B2 (en)
BG (1) BG107594A (en)
BR (1) BR0113618A (en)
CA (1) CA2421302C (en)
DE (2) DE10043846A1 (en)
DK (1) DK1423407T3 (en)
EA (1) EA006387B1 (en)
EE (1) EE05186B1 (en)
ES (1) ES2260294T3 (en)
HK (1) HK1060135A1 (en)
HR (1) HRP20030256A2 (en)
HU (1) HUP0300936A3 (en)
IL (2) IL154666A0 (en)
ME (1) MEP14408A (en)
MX (1) MXPA03001912A (en)
NO (1) NO325012B1 (en)
NZ (1) NZ524485A (en)
PL (1) PL360669A1 (en)
PT (1) PT1423407E (en)
RS (1) RS50305B (en)
SK (1) SK286757B6 (en)
UA (1) UA74592C2 (en)
WO (1) WO2002019971A1 (en)
ZA (1) ZA200301715B (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7199115B2 (en) 2004-04-19 2007-04-03 Schering Ag 17α-fluorosteroids, pharmaceutical compositions containing 17α-fluorosteroids and a method of making them

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10141984A1 (en) 2001-08-28 2003-03-20 Jenapharm Gmbh New 17-methylene-4-azasteroids
DE202007019049U1 (en) * 2007-11-05 2010-05-12 Bayer Schering Pharma Aktiengesellschaft Use of a gestagen in combination with an estrogen for the prophylaxis of lactose intolerance in oral contraception

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2611773A (en) * 1951-08-21 1952-09-23 Upjohn Co Estradiol 17-cyclopenetanepropionate
US3146239A (en) * 1957-09-23 1964-08-25 Syntex Corp 4-halo-19-nor-progesterone
US3232960A (en) * 1959-10-08 1966-02-01 Upjohn Co 3-keto-4-fluoro- and 3-keto-4,4-difluorosteroids and process
US3661940A (en) * 1970-04-13 1972-05-09 Sandoz Ag Derivatives of 21-methyl-19-norpregnanes
US4389345A (en) * 1981-10-09 1983-06-21 G.D. Searle & Co. 3-Oxoestra-17-acetonitrile and unsaturated analogs
US5994334A (en) * 1997-02-05 1999-11-30 University Of Maryland Androgen synthesis inhibitors
AU2001268661A1 (en) * 2000-06-27 2002-01-08 Aventis Pharma S.A. 20-fluoro-17(20)-vinyl steroids as inhibitors of c17-20-lyase and 5-alpha reductase

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7199115B2 (en) 2004-04-19 2007-04-03 Schering Ag 17α-fluorosteroids, pharmaceutical compositions containing 17α-fluorosteroids and a method of making them

Also Published As

Publication number Publication date
CN1452628A (en) 2003-10-29
RS50305B (en) 2009-09-08
KR100530816B1 (en) 2005-11-25
AU2002210470B2 (en) 2006-07-20
MEP14408A (en) 2010-06-10
YU16403A (en) 2006-05-25
IL154666A0 (en) 2003-09-17
EP1423407A1 (en) 2004-06-02
HUP0300936A2 (en) 2003-11-28
KR20030028836A (en) 2003-04-10
CA2421302C (en) 2007-08-14
EA200300322A1 (en) 2003-10-30
IL154666A (en) 2008-12-29
NZ524485A (en) 2005-11-25
HUP0300936A3 (en) 2010-01-28
DK1423407T3 (en) 2006-07-03
MXPA03001912A (en) 2004-07-08
EE200300087A (en) 2005-02-15
HRP20030256A2 (en) 2005-10-31
DE10043846A1 (en) 2002-04-04
WO2002019971A9 (en) 2002-08-08
SK2442003A3 (en) 2003-08-05
HK1060135A1 (en) 2004-07-30
NO20030989D0 (en) 2003-03-03
CN1262560C (en) 2006-07-05
NO20030989L (en) 2003-05-02
BG107594A (en) 2003-09-30
NO325012B1 (en) 2008-01-14
ZA200301715B (en) 2004-08-13
UA74592C2 (en) 2006-01-16
EP1423407B1 (en) 2006-03-08
AU1047002A (en) 2002-03-22
PT1423407E (en) 2006-07-31
EE05186B1 (en) 2009-06-15
WO2002019971A1 (en) 2002-03-14
ATE319733T1 (en) 2006-03-15
JP2004513084A (en) 2004-04-30
ES2260294T3 (en) 2006-11-01
PL360669A1 (en) 2004-09-20
BR0113618A (en) 2003-07-15
EA006387B1 (en) 2005-12-29
DE50109175D1 (en) 2006-05-04
SK286757B6 (en) 2009-05-07

Similar Documents

Publication Publication Date Title
HUP0102483A2 (en) Pharmaceutical compositions containing androst-5-ene-3betha,17betha-diol
HK1054332A1 (en) Novel topical oestroprogestational compositions with systemic effect
MEP38008A (en) Drospirenone for hormone replacement therapy
UA66861C2 (en) 2-phenyl-1-[4-(2-aminoeihoxy)benzyl]-indole in combination with estrogens, method for treatment and pharmaceutical product
WO2006023496A3 (en) Vaginal cream compositions, kits thereof and methods of using thereof
WO2002058706A3 (en) Combination of an estrogen and an androgen for treating hormonal deficiencies in women undergoing estrogen replacement therapy
AU2003263663A1 (en) Pharmaceutical application of 15- or 16- substituted testosterone analogues
SG153645A1 (en) Hormone replacement therapy
WO2002019982A3 (en) Cosmetic composition and method for reducing or preventing wrinkling
SG154323A1 (en) Estrogen replacement therapy
AU2690297A (en) Combination of dehydroepiandrosterone and aromatase inhibitors and use of this combination for the production of a pharmaceutical agent for treating a relative and absolute androgen deficiency in men
CA2421302A1 (en) 4-halogenated 17-methylene steroids, method for the production thereof and pharmaceutical compositions containing these compounds
HUP0101005A2 (en) Medicament for preventing and/or treating a mammary carcinoma, containing a steroidal aromatase inhibitor
Whitehead Hormone replacement therapy with estradiol and drospirenone: an overview of the clinical data
WO2000067708A3 (en) Oral steroidal hormone compositions and methods of use
JO2334B1 (en) Drospirenone for hormone replacement therapy

Legal Events

Date Code Title Description
EEER Examination request
MKLA Lapsed