LV12316A - 16-aizvietoti 4-azoandrostani ka 5-alfa-reduktazes izozima 1 inhibitori - Google Patents

16-aizvietoti 4-azoandrostani ka 5-alfa-reduktazes izozima 1 inhibitori

Info

Publication number
LV12316A
LV12316A LV990070A LV990070A LV12316A LV 12316 A LV12316 A LV 12316A LV 990070 A LV990070 A LV 990070A LV 990070 A LV990070 A LV 990070A LV 12316 A LV12316 A LV 12316A
Authority
LV
Latvia
Prior art keywords
inhibitors
azoandrostanes
substituted
alpha reductase
isozyme
Prior art date
Application number
LV990070A
Other languages
English (en)
Other versions
LV12316B (lv
Inventor
Philippe L Durette
William K Hagmann
Thomas J Lanza
Soumya P Sahoo
Gery 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 LV12316A publication Critical patent/LV12316A/lv
Publication of LV12316B publication Critical patent/LV12316B/lv

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)
  • Pyrrole Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
LVP-99-70A 1993-10-21 1999-04-26 16-aizvietoti 4-azoandrostāni kā 5-alfa-reduktāzes izozīma 1 inhibitori LV12316B (lv)

Applications Claiming Priority (1)

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

Publications (2)

Publication Number Publication Date
LV12316A true LV12316A (lv) 1999-07-20
LV12316B LV12316B (lv) 1999-11-20

Family

ID=22494410

Family Applications (2)

Application Number Title Priority Date Filing Date
LVP-96-125A LV11622B (en) 1993-10-21 1996-04-24 16-substituted-4-aza-androstane 5-alpha-reductase 16-substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors isozyme 1 inhibitors
LVP-99-70A LV12316B (lv) 1993-10-21 1999-04-26 16-aizvietoti 4-azoandrostāni kā 5-alfa-reduktāzes izozīma 1 inhibitori

Family Applications Before (1)

Application Number Title Priority Date Filing Date
LVP-96-125A LV11622B (en) 1993-10-21 1996-04-24 16-substituted-4-aza-androstane 5-alpha-reductase 16-substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors isozyme 1 inhibitors

Country Status (29)

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

Families Citing this family (27)

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Publication number Priority date Publication date Assignee Title
US5547957A (en) 1993-10-15 1996-08-20 Merck & Co., Inc. Method of treating androgenic alopecia with 5-α reductase inhibitors
US5739137A (en) * 1993-10-21 1998-04-14 Merck & Co., Inc. 16-substituted-4-aza-3-oxo-androstane as 5-alpha-reductase isozyme 1 inhibitors
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
JPH10508586A (ja) * 1994-10-21 1998-08-25 メルク エンド カンパニー インコーポレーテッド 組み合わせ式アクネ治療方法
US5886005A (en) * 1995-01-17 1999-03-23 Merck & Co., Inc. 4-Aza-19-norandrostane derivatives
WO1997014418A1 (en) * 1995-10-19 1997-04-24 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
EP1009740A1 (en) * 1997-03-17 2000-06-21 Merck & Co., Inc. Methods and compositions for treating polycystic ovary syndrome
US5935968A (en) 1997-03-17 1999-08-10 Merck & Co., Inc. Methods 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
US6462019B1 (en) 1998-07-10 2002-10-08 Osteoscreen, Inc. Inhibitors of proteasomal activity and production for stimulating bone growth
US6838436B1 (en) 1998-07-10 2005-01-04 Osteoscreen Inc. Inhibitors of proteasomal activity for stimulating bone growth
US6902721B1 (en) 1998-07-10 2005-06-07 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone growth
CA2338298A1 (en) * 1998-07-29 2000-02-10 Merck & Co., Inc. Tricyclic compounds
US6268377B1 (en) 1998-09-28 2001-07-31 Merck & Co., Inc. Method for treating androgen-related conditions
WO2002054996A2 (en) * 2000-10-23 2002-07-18 Euro Celtique Sa 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
EP2371367A1 (en) 2005-03-25 2011-10-05 Merck Sharp & Dohme (I.A.) Corp. 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
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

Family Cites Families (34)

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Publication number Priority date Publication date Assignee Title
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
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
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
US5138063A (en) * 1984-02-27 1992-08-11 Merck & Co., Inc. 17β-methoxycarbonyl-4-aza-androsten-1-en-3-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
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]
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
NZ211145A (en) * 1984-02-27 1988-10-28 Merck & Co Inc 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions
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 (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
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
EP0641209A4 (en) * 1992-05-20 1995-08-23 Merck & Co Inc NEW 17-ESTER, AMID AND KETONE DERIVATIVES OF 3-OXO-4-AZASTEROIDS AS 5-ALPHA REDUCTINE INHIBITORS.
WO1993023039A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. Substituted 4-aza-5a-androstan-ones as 5a-reductase inhibitors
HUT71484A (en) * 1992-05-20 1995-11-28 Merck & Co Inc Process for producing of 7beta-substituted-4-aza-5alpha-cholestan-ones as 5-alpha-reductase inhibitors and pharmaceuticals compositions containing them
RU2141967C1 (ru) * 1992-05-21 1999-11-27 Андорешерш Инк. ИНГИБИТОРЫ ТЕСТОСТЕРОН 5α-РЕДУКТАЗЫ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ИНГИБИРОВАНИЯ АКТИВНОСТИ ТЕСТОСТЕРОН 5α-РЕДУКТАЗЫ
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
US5739137A (en) * 1993-10-21 1998-04-14 Merck & Co., Inc. 16-substituted-4-aza-3-oxo-androstane as 5-alpha-reductase isozyme 1 inhibitors
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
ATE175420T1 (de) 1999-01-15
US5719158A (en) 1998-02-17
WO1995011254A1 (en) 1995-04-27
CA2173863A1 (en) 1995-04-27
US5910497A (en) 1999-06-08
NZ275293A (en) 1998-02-26
CN1136318A (zh) 1996-11-20
BR1100217A (pt) 1999-11-09
BG61978B1 (bg) 1998-11-30
FI961697A0 (fi) 1996-04-18
PL314039A1 (en) 1996-08-05
LV11622B (en) 1997-06-20
US6204273B1 (en) 2001-03-20
PL179611B1 (pl) 2000-10-31
NO961575D0 (no) 1996-04-19
CN1058499C (zh) 2000-11-15
HUT74613A (en) 1997-01-28
EP0724592A1 (en) 1996-08-07
FI961697A (fi) 1996-04-18
NO961575L (no) 1996-04-19
CZ292614B6 (cs) 2003-11-12
ES2125495T3 (es) 1999-03-01
KR960705839A (ko) 1996-11-08
SK49696A3 (en) 1996-10-02
AU8086194A (en) 1995-05-08
LV11622A (lv) 1996-12-20
BR9407866A (pt) 1996-10-29
BG100516A (en) 1996-11-29
KR100363994B1 (ko) 2003-04-10
ZA948285B (en) 1995-06-19
UA44257C2 (uk) 2002-02-15
CA2173863C (en) 2003-05-13
EP0724592B1 (en) 1999-01-07
CY2136B1 (en) 2002-06-21
LV12316B (lv) 1999-11-20
SK281645B6 (sk) 2001-06-11
DK0724592T3 (da) 1999-08-30
CZ122896A3 (en) 1997-01-15
HK1009047A1 (en) 1999-05-21
US5739137A (en) 1998-04-14
IL111357A (en) 2001-01-28
HU9601037D0 (en) 1996-06-28
TW413682B (en) 2000-12-01
DE69415824T2 (de) 1999-08-05
NO308037B1 (no) 2000-07-10
RU2142956C1 (ru) 1999-12-20
DE69415824D1 (de) 1999-02-18
JP2862376B2 (ja) 1999-03-03
RO116197B1 (ro) 2000-11-30
AU680063B2 (en) 1997-07-17
JPH09511213A (ja) 1997-11-11
IL111357A0 (en) 1994-12-29

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