DK165371C - 17beta-n-monosubstituerede carbamoyl-4-aza-5alfa-androst-1-en-3-on-forbindelser og praeparater indeholdende disse forbindelser - Google Patents

17beta-n-monosubstituerede carbamoyl-4-aza-5alfa-androst-1-en-3-on-forbindelser og praeparater indeholdende disse forbindelser

Info

Publication number
DK165371C
DK165371C DK607287A DK607287A DK165371C DK 165371 C DK165371 C DK 165371C DK 607287 A DK607287 A DK 607287A DK 607287 A DK607287 A DK 607287A DK 165371 C DK165371 C DK 165371C
Authority
DK
Denmark
Prior art keywords
compounds
5alfa
17beta
androst
aza
Prior art date
Application number
DK607287A
Other languages
English (en)
Other versions
DK165371B (da
DK607287A (da
DK607287D0 (da
Inventor
Josephine R Carlin
Gary H Rasmusson
W J A Vandenheuvel
Original Assignee
Merck & Co Inc
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 Merck & Co Inc filed Critical Merck & Co Inc
Publication of DK607287D0 publication Critical patent/DK607287D0/da
Publication of DK607287A publication Critical patent/DK607287A/da
Publication of DK165371B publication Critical patent/DK165371B/da
Application granted granted Critical
Publication of DK165371C publication Critical patent/DK165371C/da

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
    • C07J73/005—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by nitrogen as hetero atom
    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
DK607287A 1986-11-20 1987-11-19 17beta-n-monosubstituerede carbamoyl-4-aza-5alfa-androst-1-en-3-on-forbindelser og praeparater indeholdende disse forbindelser DK165371C (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US06/932,550 US4845104A (en) 1986-11-20 1986-11-20 Oxidized analogs of 17β-N-monosubstituted-carbamoyl-4-aza-5-α-androstan-3-ones
US93255086 1986-11-20

Publications (4)

Publication Number Publication Date
DK607287D0 DK607287D0 (da) 1987-11-19
DK607287A DK607287A (da) 1988-05-21
DK165371B DK165371B (da) 1992-11-16
DK165371C true DK165371C (da) 1993-04-05

Family

ID=25462484

Family Applications (1)

Application Number Title Priority Date Filing Date
DK607287A DK165371C (da) 1986-11-20 1987-11-19 17beta-n-monosubstituerede carbamoyl-4-aza-5alfa-androst-1-en-3-on-forbindelser og praeparater indeholdende disse forbindelser

Country Status (11)

Country Link
US (1) US4845104A (da)
EP (1) EP0271220B1 (da)
JP (1) JP2592870B2 (da)
AT (1) ATE72249T1 (da)
CA (1) CA1284636C (da)
CY (1) CY1700A (da)
DE (1) DE3776520D1 (da)
DK (1) DK165371C (da)
ES (1) ES2032452T3 (da)
HK (1) HK57493A (da)
IE (1) IE61020B1 (da)

Families Citing this family (48)

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US5120742A (en) * 1984-02-27 1992-06-09 Merck & Co., Inc. 17 β-acyl-4-aza-5 α-androst-1-ene-3-ones as 5 α-reductase inhibitors
US5151429A (en) * 1984-02-27 1992-09-29 Merck & Co., Inc. 17β-acyl-4-aza-5α-androst-1-ene-3-ones as 5α reductase inhibitors
US5571817A (en) * 1984-02-27 1996-11-05 Merck & Co., Inc. Methods of treating androgenic alopecia with finasteride [17β-N-mono-substituted-carbamoyl-4-aza-5-α-androst-1-en-ones]
US5138063A (en) * 1984-02-27 1992-08-11 Merck & Co., Inc. 17β-methoxycarbonyl-4-aza-androsten-1-en-3-ones
US5049562A (en) * 1984-02-27 1991-09-17 Merck & Co., Inc. 17β-acyl-4-aza-5α-androst-1-ene-3-ones as 5α-reductase inhibitors
US5084574A (en) * 1988-04-18 1992-01-28 Merck & Co., Inc. Dehydrogenation process
US5237061A (en) * 1988-10-31 1993-08-17 Merck & Co., Inc. Methods of synthesizing benign prostatic hypertropic agents and their intermediates
GB9002922D0 (en) * 1990-02-09 1990-04-04 Erba Carlo Spa 17 beta-substituted-4-aza-5 alpha-androstan-3-one derivatives and process for their preparation
US5162332A (en) * 1990-06-20 1992-11-10 Merck & Co., Inc. Selected 17 β-polyaroyl-4-aza-5 α-androst-1-en-3-ones as steroidal reductase inhibitors
US5098908A (en) * 1990-06-20 1992-03-24 Merck & Co., Inc. 17β-hydroxybenzoyl-4-aza-5α-androst-1-en-3-ones as testosterone reductase inhibitors
US5151430A (en) * 1990-06-20 1992-09-29 Merck & Co., Inc. Specific 17β-thiobenzoyl-4-aza-5α-androst-1-en-3-ones as antiandrogen agents
US5061802A (en) * 1990-06-20 1991-10-29 Merck & Co. Inc. 17β-aminobenzoyl-4-aza-5α-androst-1-en-3-ones as benign prostatic hypertrophy agents
US5075450A (en) * 1990-06-28 1991-12-24 Merck & Co., Inc. Intermediates in the synthesis of 17β-acyl-3-carboxy-androsta-3,5-dienes
US5091380A (en) * 1990-06-28 1992-02-25 Merck & Co., Inc. N-monosubstituted adamantyl/norbornanyl 17β-carbamides of 3-carboxy-androst-3,5-dienes as testosterone 5α-reductase inhibitors
NZ241979A (en) * 1991-03-20 1996-01-26 Merck & Co Inc Treatment of benign prostatic hyperplasia using 5alpha-reductase inhibitor and an alpha1-adrenergic recepter blocker
US5196411A (en) * 1991-08-16 1993-03-23 Merck & Co., Inc. 17β-acyl-3-carboxy-androsta-3,5-dienes as testosterone 5α-reductase inhibitors
US5304562A (en) * 1991-10-09 1994-04-19 Ciba-Geigy Corporation 17β-substituted Aza-androstane derivatives
CA2084799C (en) 1991-12-17 2003-01-28 Glenn J. Gormley Method of prevention of prostatic carcinoma with 17 beta-n-monosubstituted-carbamoyl-4-aza-5 alpha-androst-1 -en-3-ones
US5543406A (en) * 1991-12-20 1996-08-06 Glaxo Wellcome, Inc. Inhibitors of 5-α-testosterone reductase
ATE195530T1 (de) * 1992-05-20 2000-09-15 Merck & Co Inc 17-ether und thioether von 4-aza-steroiden
CA2135173A1 (en) * 1992-05-20 1993-11-25 Bruce E. Witzel Ester derivatives of 4-aza-steroids
US5639741A (en) * 1992-05-20 1997-06-17 Merck & Co., Inc. 17-amino substituted 4-azasteroid 5α-reductase inhibitors
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
CZ283894A3 (en) * 1992-05-20 1995-09-13 Merck & Co Inc 7beta-substituted 4-aza-5alpha-cholestanones, their use for the preparation of pharmaceutical preparations and pharmaceutical compositions containing thereof
US5620986A (en) * 1992-05-20 1997-04-15 Merck & Co., Inc. 17 urea, thiourea, thiocarbamyl and carbamyl4-azasteroid 5-reductase inhibitors useful in the prevention and treatment of hyperandrogenic disorders
SK140494A3 (en) * 1992-05-21 1995-07-11 Endorecherche Inc Inhibitors of testosterone 5-alpha-reductase activity
GB9216329D0 (en) * 1992-07-31 1992-09-16 Erba Carlo Spa 17beta-substituted 4-aza-5alpha-androstan-3-one derivatives
US5302589A (en) * 1992-08-07 1994-04-12 Glaxo, Inc. Heterocyclic inhibitors of 5-α-testosterone reductase
US5324734A (en) * 1992-09-15 1994-06-28 Merck & Co., Inc. Oxidization metabolites of 5-α-23-methyl-4-aza-21-nor-chol-1-ene-3, 20-dione
HU212459B (en) * 1992-10-02 1996-06-28 Richter Gedeon Vegyeszet Process for producing new 17-beta-substituted 4-aza-androstane-derivatives and pharmaceutical compositions containing them
US5278159A (en) * 1992-10-06 1994-01-11 Merck & Co., Inc. Aryl ester derivatives of 3-oxo-4-aza-androstane 17-β-carboxylates as 5-α-reductase inhibitors
ATE203162T1 (de) * 1992-12-18 2001-08-15 Merck & Co Inc Verfahren zur behandlung von chronischer prostatitis mit 17-beta-n-tertbutylcarbamoyl-4- aza-5 alpha-androst-1-en-3-one
US5380728A (en) * 1993-02-10 1995-01-10 Merck & Co., Inc. Aldehyde metabolite of 17β-N-monosubstituted-carbamoyl-4-aza-5α-a
US5359071A (en) * 1993-03-12 1994-10-25 Merck & Co., Inc. 15-substituted 4-azasteroids
AU6413594A (en) * 1993-03-24 1994-10-11 Merck & Co., Inc. Substituted 3-phenanthridinone derivatives as 5alpha-reductase inhibitors
EP0711164B1 (en) * 1993-06-28 1997-09-17 Merck & Co. Inc. 4-aza-pregnane 5-alpha-reductase isozyme 1 inhibitors
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
TW408127B (en) * 1993-09-17 2000-10-11 Glaxo Inc Androstenones
US5470976A (en) * 1994-09-07 1995-11-28 Merck & Co., Inc. Process for the stereoselective reduction of steroid enelactams
US5817818A (en) * 1994-09-16 1998-10-06 Glaxo Wellcome Inc. Androstenones
US5541322A (en) * 1994-10-14 1996-07-30 Glaxo Wellcome Inc. Synthesis of 6-azaandrostenones
US5543417A (en) * 1994-10-21 1996-08-06 Merck & Co., Inc. Combination method of treating acne using 4-AZA-5α-cholestan-ones and 4-AZA-5α-androstan-ones as selective 5α-reductase inhibitors with anti-bacterial, keratolytic, or anti-inflammatory agents
IT1271325B (it) * 1994-12-23 1997-05-27 Poli Ind Chimica Spa Composti diastereomericamente puri derivati da 3-oxo e 3-tioxo-4-azaandrostani e loro uso come antiandrogeni
US5656613A (en) * 1995-01-04 1997-08-12 Merck & Co., Inc. Treatment of hyperandrogenic conditions
US5670643A (en) * 1995-03-16 1997-09-23 Glaxo Wellcome Inc. Method for preparing finasteride
US5998427A (en) * 1998-05-14 1999-12-07 Glaxo Wellcome Inc. Androstenones
TWI233932B (en) * 2001-08-24 2005-06-11 Theravance Inc Process for purifying glycopeptide phosphonate derivatives
US7531658B2 (en) 2006-01-20 2009-05-12 Apotex Pharmachem Inc. Process for the preparation of 17-N-substituted-carbamoyl-4-aza-androst-1-en-3-ones

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4104285A (en) * 1977-04-22 1978-08-01 Hoffmann-La Roche Inc. Taurine and glycine derivatives
US4191759A (en) * 1978-04-13 1980-03-04 Merck & Co., Inc. N-substituted-17β-carbamoylandrost-4-en-3-one 5α reductase inhibitors
AU527030B2 (en) * 1978-04-13 1983-02-10 Merck & Co., Inc. 4-aza-17-substituted-5a-androstan-3-ones
US4220775A (en) * 1979-03-15 1980-09-02 Merck & Co., Inc. Preparation of 4-aza-17-substituted-5α-androstan-3-ones useful as 5α-reductase inhibitors
NZ211145A (en) * 1984-02-27 1988-10-28 Merck & Co Inc 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions
US4760071A (en) * 1984-02-27 1988-07-26 Merck & Co., Inc. 17β-N-monosubstituted carbamoyl-4-aza-5α-androst-1-en-3-ones which are active as testosterone 5α-reductase inhibitors
GB8505862D0 (en) * 1985-03-07 1985-04-11 Erba Farmitalia Steroidic 5alpha-reductase inhibitors

Also Published As

Publication number Publication date
CY1700A (en) 1994-01-14
DK165371B (da) 1992-11-16
JP2592870B2 (ja) 1997-03-19
ATE72249T1 (de) 1992-02-15
US4845104A (en) 1989-07-04
DK607287A (da) 1988-05-21
HK57493A (en) 1993-06-18
JPS63139195A (ja) 1988-06-10
ES2032452T3 (es) 1993-02-16
EP0271220B1 (en) 1992-01-29
EP0271220A1 (en) 1988-06-15
IE873122L (en) 1988-05-20
DE3776520D1 (de) 1992-03-12
IE61020B1 (en) 1994-09-07
DK607287D0 (da) 1987-11-19
CA1284636C (en) 1991-06-04

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