DE69415824D1 - 16-substituierte-4-aza-androstan-5-alpha-reduktase-isozym-i-inhibitoren - Google Patents

16-substituierte-4-aza-androstan-5-alpha-reduktase-isozym-i-inhibitoren

Info

Publication number
DE69415824D1
DE69415824D1 DE69415824T DE69415824T DE69415824D1 DE 69415824 D1 DE69415824 D1 DE 69415824D1 DE 69415824 T DE69415824 T DE 69415824T DE 69415824 T DE69415824 T DE 69415824T DE 69415824 D1 DE69415824 D1 DE 69415824D1
Authority
DE
Germany
Prior art keywords
reductase
inhibitors
isozym
androstan
aza
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.)
Expired - Fee Related
Application number
DE69415824T
Other languages
English (en)
Other versions
DE69415824T2 (de
Inventor
Philippe Durette
William Hagmann
Thomas Lanza
Soumya Sahoo
Gary Rasmusson
Richard Tolman
Langen Derek Von
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.)
Merck and Co Inc
Original Assignee
Merck and 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 and Co Inc filed Critical Merck and Co Inc
Publication of DE69415824D1 publication Critical patent/DE69415824D1/de
Application granted granted Critical
Publication of DE69415824T2 publication Critical patent/DE69415824T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J73/00Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J73/00Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C07J73/001Steroids 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
    • C07J73/005Steroids 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • A61P5/28Antiandrogens
DE69415824T 1993-10-21 1994-10-21 16-substituierte-4-aza-androstan-5-alpha-reduktase-isozym-i-inhibitoren Expired - Fee Related DE69415824T2 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US14115393A 1993-10-21 1993-10-21
PCT/US1994/012071 WO1995011254A1 (en) 1993-10-21 1994-10-21 16-substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors

Publications (2)

Publication Number Publication Date
DE69415824D1 true DE69415824D1 (de) 1999-02-18
DE69415824T2 DE69415824T2 (de) 1999-08-05

Family

ID=22494410

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69415824T Expired - Fee Related DE69415824T2 (de) 1993-10-21 1994-10-21 16-substituierte-4-aza-androstan-5-alpha-reduktase-isozym-i-inhibitoren

Country Status (29)

Country Link
US (4) US5739137A (de)
EP (1) EP0724592B1 (de)
JP (1) JP2862376B2 (de)
KR (1) KR100363994B1 (de)
CN (1) CN1058499C (de)
AT (1) ATE175420T1 (de)
BG (1) BG61978B1 (de)
BR (2) BR9407866A (de)
CA (1) CA2173863C (de)
CY (1) CY2136B1 (de)
CZ (1) CZ292614B6 (de)
DE (1) DE69415824T2 (de)
DK (1) DK0724592T3 (de)
ES (1) ES2125495T3 (de)
FI (1) FI961697A (de)
HK (1) HK1009047A1 (de)
HU (1) HUT74613A (de)
IL (1) IL111357A (de)
LV (2) LV11622B (de)
NO (1) NO308037B1 (de)
NZ (1) NZ275293A (de)
PL (1) PL179611B1 (de)
RO (1) RO116197B1 (de)
RU (1) RU2142956C1 (de)
SK (1) SK281645B6 (de)
TW (1) TW413682B (de)
UA (1) UA44257C2 (de)
WO (1) WO1995011254A1 (de)
ZA (1) ZA948285B (de)

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US5547957A (en) * 1993-10-15 1996-08-20 Merck & Co., Inc. Method of treating androgenic alopecia with 5-α reductase inhibitors
EP0724592B1 (de) * 1993-10-21 1999-01-07 Merck & Co. Inc. 16-substituierte-4-aza-androstan-5-alpha-reduktase-isozym-i-inhibitoren
US5470976A (en) * 1994-09-07 1995-11-28 Merck & Co., Inc. Process for the stereoselective reduction of steroid enelactams
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
AU694576B2 (en) * 1994-10-21 1998-07-23 Merck & Co., Inc. Combination method for acne treatment
US5886005A (en) * 1995-01-17 1999-03-23 Merck & Co., Inc. 4-Aza-19-norandrostane derivatives
EP0862436A1 (de) * 1995-10-19 1998-09-09 Merck & Co., Inc. 16-substituierte-6-aza-steroid 5-alpha reduktaseinhibitoren
US5872126A (en) * 1996-09-06 1999-02-16 Merck & Co., Inc. Methods and compositions for treating preterm labor
US5945412A (en) * 1996-12-09 1999-08-31 Merck & Co., Inc. Methods and compositions for preventing and treating bone loss
EP1009740A1 (de) * 1997-03-17 2000-06-21 Merck & Co., Inc. Verfahren und zubereitungen zur behandlung von eierstockzysten
US5935968A (en) 1997-03-17 1999-08-10 Merck & Co., Inc. Methods for treating polycystic ovary syndrome
WO1999021563A1 (en) * 1997-10-28 1999-05-06 Merck & Co., Inc. Prevention of precipitated acute urinary retention
US6187925B1 (en) * 1997-12-23 2001-02-13 Merck & Co., Inc. Intermediates and process for the synthesis of azasteroids
AR016257A1 (es) * 1998-05-14 2001-06-20 Merck & Co Inc Proceso para la sintesis estereoselectiva de ariloxi-4-aza-5alfa-androstan-3-onas, 16 alfa y 16 beta-sustituidas e insustituidas, e intermediariosobtenidos en dicho proceso.
WO1999058550A1 (en) * 1998-05-14 1999-11-18 Merck & Co., Inc. 7beta-methyl-16beta-((4-methylsulfonyl)-phenoxy)-4-aza-5alpha-androst-1-en-3-one as a 5-alpha-reductase isozyme 1 inhibitor
US6838436B1 (en) 1998-07-10 2005-01-04 Osteoscreen Inc. Inhibitors of proteasomal activity for stimulating bone growth
US6462019B1 (en) 1998-07-10 2002-10-08 Osteoscreen, Inc. Inhibitors of proteasomal activity and production for stimulating bone growth
US6902721B1 (en) * 1998-07-10 2005-06-07 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone growth
EP1105133A4 (de) * 1998-07-29 2002-03-27 Merck & Co Inc Tricyclische verbindungen
US6268377B1 (en) 1998-09-28 2001-07-31 Merck & Co., Inc. Method for treating androgen-related conditions
US20020198215A1 (en) * 2000-10-23 2002-12-26 Lino Tavares Terazosin transdermal device and methods
EP1734963A4 (de) * 2004-04-02 2008-06-18 Merck & Co Inc Verfahren zur behandlung von menschen mit metabolischen und anthropometrischen störungen
WO2006104762A2 (en) * 2005-03-25 2006-10-05 Merck & Co., Inc. Method of treating men with testosterone supplement and 5alpha-reductase inhibitor
US20060241696A1 (en) * 2005-04-26 2006-10-26 Stjepan Krco Method of limiting hair loss and promoting hair growth
FR2910002B1 (fr) * 2006-12-13 2009-01-30 Sanofi Aventis Sa Nouveau procede pour l'obtention diastereoselective d'une amine primaire chirale sur un steroide
GB201102913D0 (en) 2011-02-18 2011-04-06 Univ Birmingham Novel therapeutic
TWI522102B (zh) 2013-04-30 2016-02-21 長庚醫療財團法人 組合物於製備治療或預防性治療痤瘡的藥物之用途

Family Cites Families (34)

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US4377584A (en) * 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-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
US5138063A (en) * 1984-02-27 1992-08-11 Merck & Co., Inc. 17β-methoxycarbonyl-4-aza-androsten-1-en-3-ones
IL74365A (en) * 1984-02-27 1990-07-26 Merck & Co Inc 17beta-(n-t.-butylcarbamoyl)-4-aza-5alpha-androst-1-en-3-one and pharmaceutical compositions containing it
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
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
US4859681A (en) * 1984-02-27 1989-08-22 Merck & Co., Inc. 17 α-Acyl-4-aza-5a-androst-1-en-3-ones as 5 alpha-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]
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
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
DE3888378T2 (de) * 1987-04-03 1994-09-29 Merck & Co Inc Behandlung von Prostatacarcinoma mit 17-beta-n-monosubstituierten-Carbamoyl-4-aza-5-alpha-Androst-1-en-3-onen.
EP0285382B1 (de) * 1987-04-03 1994-04-13 Merck & Co. Inc. Behandlung von androgener Alopecia mit 17-bêta-n-mono-substituierten-carbamoyl-4-aza-5-alpha-androst-1-en-3-onen
US5116983A (en) * 1988-04-18 1992-05-26 Merck & Co., Inc. Dehydrogenation process intermediates
US5084574A (en) * 1988-04-18 1992-01-28 Merck & Co., Inc. Dehydrogenation process
CA2084798A1 (en) * 1991-12-17 1993-06-18 Glenn J. Gormley Method of preventing prostatic carcinoma with 17beta -acyl-4-aza-5.- androst-1-ene-3-ones
GB2264494A (en) * 1992-02-25 1993-09-01 Merck & Co Inc 17b-n-monosubstituted carbamoyl-11-oxo-4-aza-5-a-androst-1-en-3-one testosterone-5-alpha reductase inhibitors
US5215894A (en) * 1992-02-25 1993-06-01 Merck & Co., Inc. Biological process for producing 17β-N-monosubstituted carbamoyl-11-oxo-4-aza-5-α-androst-3-one testosterone-5-α reductase inhibitors
JPH07508033A (ja) * 1992-05-20 1995-09-07 メルク エンド カンパニー インコーポレーテッド 5α−レダクターゼ阻害剤としての3−オキソ−4−アザステロイドの新規17−エステル,アミド及びケトン誘導体
SK137994A3 (en) * 1992-05-20 1995-04-12 Merck & Co Inc 7-beta-substituted-4-aza-5-alpha-cholestan-ons their using for production of pharmaceutical agent and pharmaceutical agent containing them
WO1993023039A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. Substituted 4-aza-5a-androstan-ones as 5a-reductase inhibitors
CA2136304A1 (en) * 1992-05-21 1993-11-25 Fernand Labrie Inhibitors of testosterone 5.alpha.-reductase activity
GB9216284D0 (en) * 1992-07-31 1992-09-16 Erba Carlo Spa Fluorinated 17beta-substituted 4-aza-5alpha-androstane-3-one derivatives
GB9216329D0 (en) * 1992-07-31 1992-09-16 Erba Carlo Spa 17beta-substituted 4-aza-5alpha-androstan-3-one derivatives
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
US5380728A (en) * 1993-02-10 1995-01-10 Merck & Co., Inc. Aldehyde metabolite of 17β-N-monosubstituted-carbamoyl-4-aza-5α-a
US5407944A (en) * 1993-02-19 1995-04-18 Goldman; Boris E. Compositions and methods for promoting hair growth
US5359071A (en) * 1993-03-12 1994-10-25 Merck & Co., Inc. 15-substituted 4-azasteroids
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
US5547957A (en) * 1993-10-15 1996-08-20 Merck & Co., Inc. Method of treating androgenic alopecia with 5-α reductase inhibitors
EP0724592B1 (de) * 1993-10-21 1999-01-07 Merck & Co. Inc. 16-substituierte-4-aza-androstan-5-alpha-reduktase-isozym-i-inhibitoren
US5525608A (en) * 1994-04-20 1996-06-11 Merck & Co., Inc. 17b-aryl-4-aza-steroid derivatives useful as 5-alpha-reductase inhibitors
US5512555A (en) * 1994-07-21 1996-04-30 Merck & Co., Inc. Method of treating sweat-related conditions using finasteride, epristeride and a cholestan-3-one
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

Also Published As

Publication number Publication date
LV11622A (lv) 1996-12-20
ATE175420T1 (de) 1999-01-15
EP0724592A1 (de) 1996-08-07
RO116197B1 (ro) 2000-11-30
CZ292614B6 (cs) 2003-11-12
US5719158A (en) 1998-02-17
HUT74613A (en) 1997-01-28
US5739137A (en) 1998-04-14
CY2136B1 (en) 2002-06-21
HU9601037D0 (en) 1996-06-28
CA2173863A1 (en) 1995-04-27
SK281645B6 (sk) 2001-06-11
KR960705839A (ko) 1996-11-08
BR9407866A (pt) 1996-10-29
BR1100217A (pt) 1999-11-09
LV11622B (en) 1997-06-20
EP0724592B1 (de) 1999-01-07
LV12316B (en) 1999-11-20
BG61978B1 (bg) 1998-11-30
AU680063B2 (en) 1997-07-17
HK1009047A1 (en) 1999-05-21
ZA948285B (en) 1995-06-19
NZ275293A (en) 1998-02-26
FI961697A0 (fi) 1996-04-18
AU8086194A (en) 1995-05-08
FI961697A (fi) 1996-04-18
PL179611B1 (pl) 2000-10-31
CN1136318A (zh) 1996-11-20
US6204273B1 (en) 2001-03-20
UA44257C2 (uk) 2002-02-15
LV12316A (lv) 1999-07-20
US5910497A (en) 1999-06-08
PL314039A1 (en) 1996-08-05
ES2125495T3 (es) 1999-03-01
CA2173863C (en) 2003-05-13
NO308037B1 (no) 2000-07-10
JPH09511213A (ja) 1997-11-11
SK49696A3 (en) 1996-10-02
NO961575D0 (no) 1996-04-19
NO961575L (no) 1996-04-19
JP2862376B2 (ja) 1999-03-03
CZ122896A3 (en) 1997-01-15
BG100516A (en) 1996-11-29
CN1058499C (zh) 2000-11-15
TW413682B (en) 2000-12-01
WO1995011254A1 (en) 1995-04-27
IL111357A0 (en) 1994-12-29
IL111357A (en) 2001-01-28
DE69415824T2 (de) 1999-08-05
DK0724592T3 (da) 1999-08-30
RU2142956C1 (ru) 1999-12-20
KR100363994B1 (ko) 2003-04-10

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Legal Events

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8364 No opposition during term of opposition
8339 Ceased/non-payment of the annual fee