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ZA948285B - 16-Substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors - Google Patents

16-Substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors

Info

Publication number
ZA948285B
ZA948285B ZA948205A ZA948205A ZA948285B ZA 948285 B ZA948285 B ZA 948285B ZA 948205 A ZA948205 A ZA 948205A ZA 948205 A ZA948205 A ZA 948205A ZA 948285 B ZA948285 B ZA 948285B
Authority
ZA
South Africa
Prior art keywords
inhibitors
androstane
aza
reductase
alpha
Prior art date
Application number
ZA948205A
Other languages
English (en)
Inventor
Philippe L Durette
William K Hagmann
Thomas J Lanza Jr
Soumya P Sahoo
Gary H Rasmusson
Richard L Tolman
Derek Von Langen
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 ZA948285B publication Critical patent/ZA948285B/xx

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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)
ZA948205A 1993-10-21 1994-10-21 16-Substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors ZA948285B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US14115393A 1993-10-21 1993-10-21

Publications (1)

Publication Number Publication Date
ZA948285B true ZA948285B (en) 1995-06-19

Family

ID=22494410

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA948205A ZA948285B (en) 1993-10-21 1994-10-21 16-Substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors

Country Status (28)

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

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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
BR9407866A (pt) * 1993-10-21 1996-10-29 Merck & Co Inc Composto processos para inibiçao de 5 -redufase ou isoenzimas da mesma paratratamento de condiçoes de acne vulgar alopécia androgènica hirsutismo feminino hiperplasia prostática benigna prostatite e para o tratamento e/ou prevençao do cancer da próstata para interrupçao e reversao de alopécia androgènica e promoçao do crescimento de cabelo em um mamifero e para inibiçao de conversao biossintética da testosterona para di-hidro- testosterona em um mamifero e composiçao farmacèutica
US5470976A (en) * 1994-09-07 1995-11-28 Merck & Co., Inc. Process for the stereoselective reduction of steroid enelactams
WO1996012487A1 (fr) * 1994-10-21 1996-05-02 Merck & Co., Inc. Procede combine de traitement de l'acne
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
US5886005A (en) * 1995-01-17 1999-03-23 Merck & Co., Inc. 4-Aza-19-norandrostane derivatives
JPH11513684A (ja) * 1995-10-19 1999-11-24 メルク エンド カンパニー インコーポレーテッド １６−置換−６−アザ−ステロイド５α−レダクターゼ阻害剤
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
WO1998041509A1 (fr) * 1997-03-17 1998-09-24 Merck & Co., Inc. Methodes et compositions de traitement de la polykystose ovarienne
US5935968A (en) 1997-03-17 1999-08-10 Merck & Co., Inc. Methods for treating polycystic ovary syndrome
JP2001521000A (ja) * 1997-10-28 2001-11-06 メルク エンド カムパニー インコーポレーテッド 誘発性急性閉尿の予防
US6187925B1 (en) * 1997-12-23 2001-02-13 Merck & Co., Inc. Intermediates and process for the synthesis of azasteroids
AU3977999A (en) * 1998-05-14 1999-11-29 Merck & Co., Inc. 7beta-methyl-16beta-((4-methylsulfonyl)-phenoxy)-4-aza-5alph a-androst-1-en-3-oneas a 5-alpha-reductase isozyme inhibitor
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.
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
JP2002521449A (ja) * 1998-07-29 2002-07-16 メルク エンド カムパニー インコーポレーテッド 三環式化合物
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
MXPA03010458A (es) * 2001-05-15 2004-03-09 Taisho Pharmaceuticals Co Ltd Composicion liquida que contiene minoxidilo.
EP1734963A4 (fr) * 2004-04-02 2008-06-18 Merck & Co Inc Methode destinee a traiter des hommes presentant des troubles metaboliques et anthropometriques
CN101146535A (zh) * 2005-03-25 2008-03-19 默克公司 用睾酮补充剂和5α-还原酶抑制剂治疗男性病人的方法
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
RU2364402C1 (ru) * 2008-04-28 2009-08-20 Государственное образовательное учреждение высшего профессионального образования Московская медицинская академия им. И.М. Сеченова Федерального агентства по здравоохранению и социальному развитию (ГОУВПО ММА им. И.М. Сеченова Росздрава) Способ лечения больных хроническим простатитом
GB201102913D0 (en) 2011-02-18 2011-04-06 Univ Birmingham Novel therapeutic
TWI593411B (zh) 2013-04-30 2017-08-01 徐懷山 組合物於製備抑制雄性素受體有關之功能及治療雄性素 受體相關之疾病的藥物之用途

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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
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
NZ211145A (en) * 1984-02-27 1988-10-28 Merck & Co Inc 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions
US5138063A (en) * 1984-02-27 1992-08-11 Merck & Co., Inc. 17β-methoxycarbonyl-4-aza-androsten-1-en-3-ones
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
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
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
EP0285382B1 (fr) * 1987-04-03 1994-04-13 Merck & Co. Inc. Traitement d'alopécia androgénique avec 17-bêta-n-monosubstitué-carbamoyl-4-aza-5-alpha-androst-1-en-3-ones
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.
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 (fr) * 1991-12-17 1993-06-18 Glenn J. Gormley Methode de prevention du carcinome prostatique a l'aide de 17beta -acyl -4-a-za-5.-androst-1-ene-3-ones
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
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FI945457L (fi) * 1992-05-21 1995-01-16 Endorecherche Inc Testosteronin 5alfa-reduktaasiaktiviteetin inhibiittorit
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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
BR9407866A (pt) * 1993-10-21 1996-10-29 Merck & Co Inc Composto processos para inibiçao de 5 -redufase ou isoenzimas da mesma paratratamento de condiçoes de acne vulgar alopécia androgènica hirsutismo feminino hiperplasia prostática benigna prostatite e para o tratamento e/ou prevençao do cancer da próstata para interrupçao e reversao de alopécia androgènica e promoçao do crescimento de cabelo em um mamifero e para inibiçao de conversao biossintética da testosterona para di-hidro- testosterona em um mamifero e composiçao farmacèutica
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
DE69415824D1 (de) 1999-02-18
PL179611B1 (pl) 2000-10-31
US5719158A (en) 1998-02-17
FI961697L (fi) 1996-04-18
PL314039A1 (en) 1996-08-05
CA2173863A1 (fr) 1995-04-27
US5910497A (en) 1999-06-08
DK0724592T3 (da) 1999-08-30
NZ275293A (en) 1998-02-26
IL111357A (en) 2001-01-28
TW413682B (en) 2000-12-01
UA44257C2 (uk) 2002-02-15
CN1058499C (zh) 2000-11-15
ES2125495T3 (es) 1999-03-01
CA2173863C (fr) 2003-05-13
AU680063B2 (en) 1997-07-17
CZ292614B6 (cs) 2003-11-12
EP0724592A1 (fr) 1996-08-07
NO961575D0 (no) 1996-04-19
KR960705839A (ko) 1996-11-08
SK49696A3 (en) 1996-10-02
BG61978B1 (bg) 1998-11-30
CY2136B1 (en) 2002-06-21
DE69415824T2 (de) 1999-08-05
JP2862376B2 (ja) 1999-03-03
SK281645B6 (sk) 2001-06-11
KR100363994B1 (ko) 2003-04-10
LV12316B (en) 1999-11-20
EP0724592B1 (fr) 1999-01-07
IL111357A0 (en) 1994-12-29
LV12316A (lv) 1999-07-20
BR9407866A (pt) 1996-10-29
RU2142956C1 (ru) 1999-12-20
US5739137A (en) 1998-04-14
AU8086194A (en) 1995-05-08
FI961697A7 (fi) 1996-04-18
BG100516A (bg) 1996-11-29
US6204273B1 (en) 2001-03-20
BR1100217A (pt) 1999-11-09
HU9601037D0 (en) 1996-06-28
FI961697A0 (fi) 1996-04-18
ATE175420T1 (de) 1999-01-15
LV11622A (lv) 1996-12-20
CN1136318A (zh) 1996-11-20
RO116197B1 (ro) 2000-11-30
LV11622B (en) 1997-06-20
WO1995011254A1 (fr) 1995-04-27
CZ122896A3 (en) 1997-01-15
HK1009047A1 (en) 1999-05-21
NO308037B1 (no) 2000-07-10
NO961575L (no) 1996-04-19
JPH09511213A (ja) 1997-11-11
HUT74613A (en) 1997-01-28

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