FI961697A0 - 16-substituoidut-4-atsa-androstaani 5alfa-reduktaasi-isotsyymi-1-inhibiittorit - Google Patents

16-substituoidut-4-atsa-androstaani 5alfa-reduktaasi-isotsyymi-1-inhibiittorit

Info

Publication number
FI961697A0
FI961697A0 FI961697A FI961697A FI961697A0 FI 961697 A0 FI961697 A0 FI 961697A0 FI 961697 A FI961697 A FI 961697A FI 961697 A FI961697 A FI 961697A FI 961697 A0 FI961697 A0 FI 961697A0
Authority
FI
Finland
Prior art keywords
5alpha
inhibitors
androstane
aza
substituted
Prior art date
Application number
FI961697A
Other languages
English (en)
Swedish (sv)
Other versions
FI961697A (fi
Inventor
Philippe L Durette
William K Hagmann
Jr Thomas J Lanza
Soumya P Sahoo
Gary H Rasmusson
Richard L Tolman
Langen Derek Von
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 FI961697A publication Critical patent/FI961697A/fi
Publication of FI961697A0 publication Critical patent/FI961697A0/fi

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
    • 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
    • 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
FI961697A 1993-10-21 1996-04-18 16-substituoidut-4-atsa-androstaani 5alfa-reduktaasi-isotsyymi-1-inhibiittorit FI961697A0 (fi)

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
FI961697A FI961697A (fi) 1996-04-18
FI961697A0 true FI961697A0 (fi) 1996-04-18

Family

ID=22494410

Family Applications (1)

Application Number Title Priority Date Filing Date
FI961697A FI961697A0 (fi) 1993-10-21 1996-04-18 16-substituoidut-4-atsa-androstaani 5alfa-reduktaasi-isotsyymi-1-inhibiittorit

Country Status (29)

Country Link
US (4) US5739137A (fi)
EP (1) EP0724592B1 (fi)
JP (1) JP2862376B2 (fi)
KR (1) KR100363994B1 (fi)
CN (1) CN1058499C (fi)
AT (1) ATE175420T1 (fi)
BG (1) BG61978B1 (fi)
BR (2) BR9407866A (fi)
CA (1) CA2173863C (fi)
CY (1) CY2136B1 (fi)
CZ (1) CZ292614B6 (fi)
DE (1) DE69415824T2 (fi)
DK (1) DK0724592T3 (fi)
ES (1) ES2125495T3 (fi)
FI (1) FI961697A0 (fi)
HK (1) HK1009047A1 (fi)
HU (1) HUT74613A (fi)
IL (1) IL111357A (fi)
LV (2) LV11622B (fi)
NO (1) NO308037B1 (fi)
NZ (1) NZ275293A (fi)
PL (1) PL179611B1 (fi)
RO (1) RO116197B1 (fi)
RU (1) RU2142956C1 (fi)
SK (1) SK281645B6 (fi)
TW (1) TW413682B (fi)
UA (1) UA44257C2 (fi)
WO (1) WO1995011254A1 (fi)
ZA (1) ZA948285B (fi)

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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
ATE175420T1 (de) 1993-10-21 1999-01-15 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
CA2199979A1 (en) * 1994-10-21 1996-05-02 Joanne Waldstreicher Combination method for acne treatment
US5886005A (en) * 1995-01-17 1999-03-23 Merck & Co., Inc. 4-Aza-19-norandrostane derivatives
AU704933B2 (en) * 1995-10-19 1999-05-06 Merck & Co., Inc. 16-substituted-6-aza-steroid 5-alpha-reductase inhibitors
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
US5935968A (en) 1997-03-17 1999-08-10 Merck & Co., Inc. Methods for treating polycystic ovary syndrome
CA2283098A1 (en) * 1997-03-17 1998-09-24 Merck & Co., Inc. Methods and compositions for treating polycystic ovary syndrome
US5942519A (en) * 1997-10-28 1999-08-24 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
US6048869A (en) * 1998-07-29 2000-04-11 Merck & Co., Inc. Tricyclic compounds
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
EP2305352A1 (en) 2004-04-02 2011-04-06 Merck Sharp & Dohme Corp. 5-alpha-reductase inhibitors for use in the treatment of men with metabolic and anthropometric disorders
EP1865955A4 (en) * 2005-03-25 2009-04-15 Merck & Co Inc TREATMENT OF MALE-HUMAN HUMANS BY TESTOSTERONE SUPPLEMENTATION ASSOCIATED WITH 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

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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
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
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
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
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
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]
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
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
US5138063A (en) * 1984-02-27 1992-08-11 Merck & Co., Inc. 17β-methoxycarbonyl-4-aza-androsten-1-en-3-ones
EP0285383B1 (en) * 1987-04-03 1994-03-16 Merck & Co. Inc. Treatment of prostatic carcinoma with 17beta-n-monosubstituted-carbamoyl-4-aza-5alpha-androst-1-en-3-ones
EP0285382B1 (en) * 1987-04-03 1994-04-13 Merck & Co. Inc. Treatment of androgenic alopecia with 17beta-n-monosubstituted-carbamoyl-4-aza-5alpha-androst-1-en-3-ones
US5084574A (en) * 1988-04-18 1992-01-28 Merck & Co., Inc. Dehydrogenation process
US5116983A (en) * 1988-04-18 1992-05-26 Merck & Co., Inc. Dehydrogenation process intermediates
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
WO1993023039A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. Substituted 4-aza-5a-androstan-ones as 5a-reductase inhibitors
RU94046044A (ru) * 1992-05-20 1996-10-10 Мерк Энд Ко. Новые 7 бета -замещенные 4-аза- 5 альфа -холестан-оны в качестве ингибиторов 5 альфа -редуктазы, фармацевтическая композиция на их основе, способ ее получения
CA2135167A1 (en) * 1992-05-20 1993-11-25 Donald W. Graham New 17-ester, amide, and ketone derivatives of 3-oxo-4- azasteroids as 5a-reductase inhibitors
KR950701527A (ko) * 1992-05-21 1995-04-28 라브리 페르낭 테스토스테론 5α 환원효소 활성 저해제(INHIBITORS OF TESTOSTERONE 5α-REDUCTASE ACTIVITY)
GB9216329D0 (en) * 1992-07-31 1992-09-16 Erba Carlo Spa 17beta-substituted 4-aza-5alpha-androstan-3-one derivatives
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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
ATE175420T1 (de) * 1993-10-21 1999-01-15 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
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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
CY2136B1 (en) 2002-06-21
JP2862376B2 (ja) 1999-03-03
HUT74613A (en) 1997-01-28
FI961697A (fi) 1996-04-18
CN1136318A (zh) 1996-11-20
BG100516A (en) 1996-11-29
LV12316A (lv) 1999-07-20
SK281645B6 (sk) 2001-06-11
CN1058499C (zh) 2000-11-15
IL111357A0 (en) 1994-12-29
KR960705839A (ko) 1996-11-08
PL179611B1 (pl) 2000-10-31
CA2173863A1 (en) 1995-04-27
NO308037B1 (no) 2000-07-10
LV12316B (en) 1999-11-20
ZA948285B (en) 1995-06-19
US5739137A (en) 1998-04-14
LV11622B (en) 1997-06-20
RO116197B1 (ro) 2000-11-30
LV11622A (lv) 1996-12-20
US5910497A (en) 1999-06-08
ATE175420T1 (de) 1999-01-15
NZ275293A (en) 1998-02-26
US6204273B1 (en) 2001-03-20
HK1009047A1 (en) 1999-05-21
SK49696A3 (en) 1996-10-02
EP0724592A1 (en) 1996-08-07
ES2125495T3 (es) 1999-03-01
BG61978B1 (bg) 1998-11-30
CA2173863C (en) 2003-05-13
DE69415824T2 (de) 1999-08-05
PL314039A1 (en) 1996-08-05
UA44257C2 (uk) 2002-02-15
NO961575D0 (no) 1996-04-19
JPH09511213A (ja) 1997-11-11
IL111357A (en) 2001-01-28
EP0724592B1 (en) 1999-01-07
DK0724592T3 (da) 1999-08-30
AU680063B2 (en) 1997-07-17
US5719158A (en) 1998-02-17
BR1100217A (pt) 1999-11-09
BR9407866A (pt) 1996-10-29
CZ292614B6 (cs) 2003-11-12
HU9601037D0 (en) 1996-06-28
CZ122896A3 (en) 1997-01-15
RU2142956C1 (ru) 1999-12-20
WO1995011254A1 (en) 1995-04-27
NO961575L (no) 1996-04-19
AU8086194A (en) 1995-05-08
TW413682B (en) 2000-12-01
DE69415824D1 (de) 1999-02-18
KR100363994B1 (ko) 2003-04-10

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