CY1553A - 17 beta-substituted-4-aza-5-alpha-androstenones and their use as 5-alpha-reductase inhibitors - Google Patents

17 beta-substituted-4-aza-5-alpha-androstenones and their use as 5-alpha-reductase inhibitors

Info

Publication number
CY1553A
CY1553A CY1553A CY155391A CY1553A CY 1553 A CY1553 A CY 1553A CY 1553 A CY1553 A CY 1553A CY 155391 A CY155391 A CY 155391A CY 1553 A CY1553 A CY 1553A
Authority
CY
Cyprus
Prior art keywords
alpha
androstenones
aza
beta
substituted
Prior art date
Application number
CY1553A
Other languages
English (en)
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27078980&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CY1553(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of CY1553A publication Critical patent/CY1553A/xx

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C62/00—Compounds having carboxyl groups bound to carbon atoms of rings other than six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C62/30—Unsaturated compounds
    • C07C62/38—Unsaturated compounds containing keto groups
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/18—Ring systems of four or more rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/16—Benz[e]indenes; Hydrogenated benz[e]indenes

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CY1553A 1984-02-27 1991-03-22 17 beta-substituted-4-aza-5-alpha-androstenones and their use as 5-alpha-reductase inhibitors CY1553A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US58406284A 1984-02-27 1984-02-27
US58406184A 1984-02-27 1984-02-27

Publications (1)

Publication Number Publication Date
CY1553A true CY1553A (en) 1991-03-22

Family

ID=27078980

Family Applications (1)

Application Number Title Priority Date Filing Date
CY1553A CY1553A (en) 1984-02-27 1991-03-22 17 beta-substituted-4-aza-5-alpha-androstenones and their use as 5-alpha-reductase inhibitors

Country Status (16)

Country Link
EP (1) EP0155096B1 (forum.php)
JP (1) JPH0193600A (forum.php)
KR (1) KR900001206B1 (forum.php)
AU (4) AU584321B2 (forum.php)
CA (1) CA1314541C (forum.php)
CY (1) CY1553A (forum.php)
DE (2) DE3573429D1 (forum.php)
DK (1) DK166704B1 (forum.php)
ES (1) ES8702430A1 (forum.php)
GR (1) GR850483B (forum.php)
HK (1) HK63090A (forum.php)
IE (2) IE922862L (forum.php)
IL (1) IL74365A (forum.php)
NL (1) NL930005I2 (forum.php)
NZ (1) NZ211145A (forum.php)
PT (1) PT80010B (forum.php)

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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]
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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
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US4845104A (en) * 1986-11-20 1989-07-04 Merck & Co., Inc. Oxidized analogs of 17β-N-monosubstituted-carbamoyl-4-aza-5-α-androstan-3-ones
US4888336A (en) * 1987-01-28 1989-12-19 Smithkline Beckman Corporation Steroid 5-alpha-reductase inhibitors
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
NZ225100A (en) * 1987-06-29 1991-09-25 Merck & Co Inc Reaction of steroids (including 4-azasteroids) with a silylating agent in the presence of a quinone to introduce a delta' double bond and silylated intermediates
US5116983A (en) * 1988-04-18 1992-05-26 Merck & Co., Inc. Dehydrogenation process intermediates
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US5021575A (en) * 1989-11-13 1991-06-04 Merck & Co., Inc. Method for introducing a 1,2 double bond into azasteroids
GB9002922D0 (en) * 1990-02-09 1990-04-04 Erba Carlo Spa 17 beta-substituted-4-aza-5 alpha-androstan-3-one derivatives and process for their preparation
US5162332A (en) * 1990-06-20 1992-11-10 Merck & Co., Inc. Selected 17 β-polyaroyl-4-aza-5 α-androst-1-en-3-ones as steroidal reductase inhibitors
US5151430A (en) * 1990-06-20 1992-09-29 Merck & Co., Inc. Specific 17β-thiobenzoyl-4-aza-5α-androst-1-en-3-ones as antiandrogen agents
EP0462664A3 (en) * 1990-06-20 1992-11-25 Merck & Co. Inc. Specific 17beta-thiobenzoyl-4-aza-5alpha-androst-1-en-3-ones as antiandrogenic agents
EP0462662A3 (en) * 1990-06-20 1992-08-19 Merck & Co. Inc. 17beta-n-monosubstituted adamantyl/norbornanyl carbamoyl-4-aza-5alpha-androst-1-en-3-ones and androstan-3-ones
US5061802A (en) * 1990-06-20 1991-10-29 Merck & Co. Inc. 17β-aminobenzoyl-4-aza-5α-androst-1-en-3-ones as benign prostatic hypertrophy agents
EP0462665A3 (en) * 1990-06-20 1993-06-30 Merck & Co. Inc. Selected 17beta-polyaroyl-4-aza-5alpha-androst-1-en-3-ones as steroidal reductase inhibitors
US5098908A (en) * 1990-06-20 1992-03-24 Merck & Co., Inc. 17β-hydroxybenzoyl-4-aza-5α-androst-1-en-3-ones as testosterone reductase inhibitors
US5091380A (en) * 1990-06-28 1992-02-25 Merck & Co., Inc. N-monosubstituted adamantyl/norbornanyl 17β-carbamides of 3-carboxy-androst-3,5-dienes as testosterone 5α-reductase inhibitors
US5091534A (en) * 1990-08-27 1992-02-25 Merck & Co., Inc. Trialkylsilyl trifluoromethanesulfonate mediated α-methylenic carbon functionalization of 4-AZA-5α-androstan-3-one steroids
US5120847A (en) * 1990-08-27 1992-06-09 Merck & Co., Inc. Process for iodinating or brominating the α-methylenic carbon of a secondary amide
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US5061801A (en) * 1990-09-24 1991-10-29 Merck & Co., Inc. Intermediate for making 3-oxo-4-aza-androst-1-ene 17β-ketones
CA2050824A1 (en) * 1990-09-24 1992-03-25 John M. Williams Process for making 3-oxo-4-aza-androst-1-ene 17-.beta.-ketones
IE76452B1 (en) * 1990-10-29 1997-10-22 Sankyo Co Azasteroid compounds for the treatment of prostatic hypertrophy their preparation and use
NZ241979A (en) * 1991-03-20 1996-01-26 Merck & Co Inc Treatment of benign prostatic hyperplasia using 5alpha-reductase inhibitor and an alpha1-adrenergic recepter blocker
GB9115676D0 (en) * 1991-07-19 1991-09-04 Erba Carlo Spa Process for the preparation of 17 beta substituted-4-aza-5 alpha-androstan-3-one derivatives
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EP0547687A1 (en) * 1991-12-18 1993-06-23 Merck & Co. Inc. 17B-N-Substituted adamantyl/norbonanyl carbamoyl-4-aza-5a-and-rost-1-en-3-ones and androstan-3 ones
JPH07502511A (ja) * 1991-12-20 1995-03-16 グラクソ、インコーポレーテッド ５‐α‐テストステロンレダクターゼ阻害剤
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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
WO1993023048A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. 4-azasteroid 5-alpha-reductase inhibitors
ATE195530T1 (de) * 1992-05-20 2000-09-15 Merck & Co Inc 17-ether und thioether von 4-aza-steroiden
CA2135173A1 (en) * 1992-05-20 1993-11-25 Bruce E. Witzel Ester derivatives of 4-aza-steroids
AU4251993A (en) * 1992-05-20 1993-12-13 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
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US5710275A (en) * 1992-05-20 1998-01-20 Merck & Co., Inc. 7β-substituted-4-aza-5α-androstan-3-ones as 5α-reductase inhibitors
JPH07506575A (ja) * 1992-05-21 1995-07-20 アンドルシェルシュ・インコーポレイテッド テストステロン５α−レダクターゼ活性の阻害剤
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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
US5468860A (en) 1992-11-19 1995-11-21 Merck & Co., Inc. New finasteride processes
US5359071A (en) * 1993-03-12 1994-10-25 Merck & Co., Inc. 15-substituted 4-azasteroids
US5621104A (en) * 1993-03-24 1997-04-15 Merck & Co., Inc. Substituted 3-phenanthridinone derivatives as 5-alpha-reductase inhibitors
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CN1314241C (zh) * 2002-09-27 2007-05-02 华为技术有限公司 在城域网相同虚容器映射通道内传送不同用户数据的方法
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US3285918A (en) * 1962-04-18 1966-11-15 Norman J Doorenbos 1', 4', 5', 6'-tetrahydropyrimidino[a-4, 3]-4-aza-5-cholestene
US4377584A (en) * 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
ZA791752B (en) * 1978-04-13 1980-11-26 Merck & Co Inc 4-aza-17 beta -substituted-5 alpha -androstan-3-ones useful as 5 alpha -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
GB8505862D0 (en) * 1985-03-07 1985-04-11 Erba Farmitalia Steroidic 5alpha-reductase inhibitors

Also Published As

Publication number Publication date
IE850476L (en) 1985-08-27
DK85985A (da) 1985-10-22
AU7083591A (en) 1991-07-11
AU3916785A (en) 1985-09-05
PT80010A (en) 1985-03-01
DE3584172D1 (de) 1991-10-24
DK166704B1 (da) 1993-06-28
AU3313589A (en) 1989-08-10
JPH0193600A (ja) 1989-04-12
IL74365A0 (en) 1985-05-31
ES540705A0 (es) 1987-01-01
IE58058B1 (en) 1993-06-16
GR850483B (forum.php) 1985-06-26
JPH0541638B2 (forum.php) 1993-06-24
AU651741B2 (en) 1994-07-28
IL74365A (en) 1990-07-26
EP0155096A2 (en) 1985-09-18
ES8702430A1 (es) 1987-01-01
AU626293B2 (en) 1992-07-30
DK85985D0 (da) 1985-02-26
NL930005I1 (nl) 1993-04-01
NZ211145A (en) 1988-10-28
HK63090A (en) 1990-08-17
NL930005I2 (nl) 1993-09-16
AU584321B2 (en) 1989-05-25
EP0155096A3 (en) 1986-07-02
CA1314541C (en) 1993-03-16
EP0155096B1 (en) 1989-10-04
AU2748192A (en) 1993-03-18
DE3573429D1 (en) 1989-11-09
IE922862L (en) 1985-08-27
PT80010B (pt) 1987-09-18
KR850006185A (ko) 1985-10-02
KR900001206B1 (ko) 1990-02-28

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