BG61978B1 - 16-заместени-4-аза-андростани като инхибитори на изозима 5 алфа-редуктаза 1 - Google Patents

16-заместени-4-аза-андростани като инхибитори на изозима 5 алфа-редуктаза 1 Download PDF

Info

Publication number
BG61978B1
BG61978B1 BG100516A BG10051696A BG61978B1 BG 61978 B1 BG61978 B1 BG 61978B1 BG 100516 A BG100516 A BG 100516A BG 10051696 A BG10051696 A BG 10051696A BG 61978 B1 BG61978 B1 BG 61978B1
Authority
BG
Bulgaria
Prior art keywords
aza
oxo
dimethyl
androstane
methyl
Prior art date
Application number
BG100516A
Other languages
Bulgarian (bg)
English (en)
Other versions
BG100516A (en
Inventor
Philippe L. Durette
William K. Hagmann
Thomas J. Lanza Jun.
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 BG100516A publication Critical patent/BG100516A/xx
Publication of BG61978B1 publication Critical patent/BG61978B1/bg

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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Pyrrole Compounds (AREA)
BG100516A 1993-10-21 1996-04-18 16-заместени-4-аза-андростани като инхибитори на изозима 5 алфа-редуктаза 1 BG61978B1 (bg)

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
BG100516A BG100516A (en) 1996-11-29
BG61978B1 true BG61978B1 (bg) 1998-11-30

Family

ID=22494410

Family Applications (1)

Application Number Title Priority Date Filing Date
BG100516A BG61978B1 (bg) 1993-10-21 1996-04-18 16-заместени-4-аза-андростани като инхибитори на изозима 5 алфа-редуктаза 1

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)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
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
CN1058499C (zh) 1993-10-21 2000-11-15 麦克公司 １６－取代－４－氮杂－雄甾烷－５α－还原酶同工酶１抑制剂
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
WO1996012487A1 (en) * 1994-10-21 1996-05-02 Merck & Co., Inc. 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
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
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.
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
US6902721B1 (en) 1998-07-10 2005-06-07 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
US6838436B1 (en) 1998-07-10 2005-01-04 Osteoscreen Inc. Inhibitors of proteasomal activity for stimulating bone growth
AU754604B2 (en) * 1998-07-29 2002-11-21 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
US20080125403A1 (en) * 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating 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
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU527030B2 (en) * 1978-04-13 1983-02-10 Merck & Co., Inc. 4-aza-17-substituted-5a-androstan-3-ones
US4377584A (en) * 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
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
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
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
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
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
US5138063A (en) * 1984-02-27 1992-08-11 Merck & Co., Inc. 17β-methoxycarbonyl-4-aza-androsten-1-en-3-ones
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
DE3888994T2 (de) * 1987-04-03 1994-11-03 Merck & Co Inc Behandlung von androgener Alopecia mit 17-beta-n-mono-substituierten-carbamoyl-4-aza-5-alpha-androst-1-en-3-onen.
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.
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
WO1993023039A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. Substituted 4-aza-5a-androstan-ones as 5a-reductase inhibitors
WO1993023051A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. New 17-ester, amide, and ketone derivatives of 3-oxo-4-azasteroids as 5a-reductase inhibitors
WO1993023419A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. NEW 7β-SUBSTITUTED-4-AZA-5α-CHOLESTAN-ONES AS 5α-REDUCTASE INHIBITORS
EP0641211A1 (en) * 1992-05-21 1995-03-08 Endorecherche Inc. INHIBITORS OF TESTOSTERONE 5$g(a)-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
CN1058499C (zh) * 1993-10-21 2000-11-15 麦克公司 １６－取代－４－氮杂－雄甾烷－５α－还原酶同工酶１抑制剂
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
AU8086194A (en) 1995-05-08
RU2142956C1 (ru) 1999-12-20
DE69415824D1 (de) 1999-02-18
CN1136318A (zh) 1996-11-20
US5719158A (en) 1998-02-17
DK0724592T3 (da) 1999-08-30
CZ122896A3 (en) 1997-01-15
NO961575L (no) 1996-04-19
UA44257C2 (uk) 2002-02-15
PL179611B1 (pl) 2000-10-31
KR960705839A (ko) 1996-11-08
HK1009047A1 (en) 1999-05-21
CZ292614B6 (cs) 2003-11-12
PL314039A1 (en) 1996-08-05
SK49696A3 (en) 1996-10-02
CA2173863C (en) 2003-05-13
WO1995011254A1 (en) 1995-04-27
ES2125495T3 (es) 1999-03-01
EP0724592A1 (en) 1996-08-07
TW413682B (en) 2000-12-01
JP2862376B2 (ja) 1999-03-03
AU680063B2 (en) 1997-07-17
ZA948285B (en) 1995-06-19
IL111357A0 (en) 1994-12-29
LV12316A (lv) 1999-07-20
KR100363994B1 (ko) 2003-04-10
NO308037B1 (no) 2000-07-10
SK281645B6 (sk) 2001-06-11
HUT74613A (en) 1997-01-28
JPH09511213A (ja) 1997-11-11
HU9601037D0 (en) 1996-06-28
LV12316B (en) 1999-11-20
LV11622A (lv) 1996-12-20
ATE175420T1 (de) 1999-01-15
NO961575D0 (no) 1996-04-19
BR1100217A (pt) 1999-11-09
US6204273B1 (en) 2001-03-20
CN1058499C (zh) 2000-11-15
CA2173863A1 (en) 1995-04-27
LV11622B (en) 1997-06-20
FI961697A (fi) 1996-04-18
CY2136B1 (en) 2002-06-21
US5739137A (en) 1998-04-14
BG100516A (en) 1996-11-29
DE69415824T2 (de) 1999-08-05
EP0724592B1 (en) 1999-01-07
RO116197B1 (ro) 2000-11-30
NZ275293A (en) 1998-02-26
IL111357A (en) 2001-01-28
US5910497A (en) 1999-06-08
FI961697A0 (fi) 1996-04-18
BR9407866A (pt) 1996-10-29

Similar Documents

Publication Publication Date Title
BG61978B1 (bg) 16-заместени-4-аза-андростани като инхибитори на изозима 5 алфа-редуктаза 1
EP0748221B1 (en) 7-substituted-4-aza-steroid derivatives as 5-alpha- reductase inhibitors
EP0756481B1 (en) 17$g(b)-ARYL-4-AZA-STEROID DERIVATIVES
US5741795A (en) 16-substituted-6-aza-androsten-4-ene-3-ones as 5-α-reductase inhibitors
US5763361A (en) 17-alkyl-7-substituted-4-aza steroid derivatives as 5-α-reductase inhibitors
EP0862556B1 (en) 17-alkyl-7-substituted-4-aza steroid derivatives
AU680063C (en) 16-substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors
HRP950100A2 (en) 16-substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors