ZA88549B - Steroid 5-alpha-reductase inhibitors - Google Patents

Steroid 5-alpha-reductase inhibitors

Info

Publication number
ZA88549B
ZA88549B ZA880549A ZA88549A ZA88549B ZA 88549 B ZA88549 B ZA 88549B ZA 880549 A ZA880549 A ZA 880549A ZA 88549 A ZA88549 A ZA 88549A ZA 88549 B ZA88549 B ZA 88549B
Authority
ZA
South Africa
Prior art keywords
alpha
steroid
reductase inhibitors
double bond
reductase
Prior art date
Application number
ZA880549A
Other languages
English (en)
Inventor
Alan Holt Dennis
Alan Levy Mark
Walter Metcalf Brian
Original Assignee
Smithkline Beckman Corporation
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 Smithkline Beckman Corporation filed Critical Smithkline Beckman Corporation
Publication of ZA88549B publication Critical patent/ZA88549B/xx

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/003—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring the S atom directly linked to a ring carbon atom of the cyclopenta(a)hydrophenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J3/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • C07J3/005—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom the carbon atom being part of a carboxylic function
    • 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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
ZA880549A 1987-01-28 1988-01-27 Steroid 5-alpha-reductase inhibitors ZA88549B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US07/007,539 US4888336A (en) 1987-01-28 1987-01-28 Steroid 5-alpha-reductase inhibitors

Publications (1)

Publication Number Publication Date
ZA88549B true ZA88549B (en) 1988-07-27

Family

ID=21726780

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA880549A ZA88549B (en) 1987-01-28 1988-01-27 Steroid 5-alpha-reductase inhibitors

Country Status (13)

Country Link
US (1) US4888336A (OSRAM)
EP (1) EP0277002B1 (OSRAM)
JP (1) JPS63192800A (OSRAM)
AT (1) ATE77388T1 (OSRAM)
AU (1) AU608560B2 (OSRAM)
CA (1) CA1325006C (OSRAM)
DE (1) DE3871965T2 (OSRAM)
DK (4) DK37388A (OSRAM)
ES (1) ES2042725T3 (OSRAM)
GR (1) GR3005284T3 (OSRAM)
IE (1) IE61594B1 (OSRAM)
PT (1) PT86652B (OSRAM)
ZA (1) ZA88549B (OSRAM)

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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]
US4814324A (en) * 1987-03-06 1989-03-21 Merck & Co., Inc. Sterol inhibitors of testosterone 5α-reductase
US5372996A (en) * 1989-03-10 1994-12-13 Endorecherche, Inc. Method of treatment of androgen-related diseases
US5595985A (en) * 1989-03-10 1997-01-21 Endorecherche Inc. Combination therapy for prophylaxis and/or treatment of benign prostatic hyperplasia
US5405978A (en) * 1989-05-30 1995-04-11 The Upjohn Company Oxidative preparation of 3,5-secoandrost-5-one-3,17 β-dioic acid
KR0181264B1 (ko) * 1989-07-07 1999-03-20 라브리 페르낭 성스테로이드 활성 억제용 안드로겐 유도체
EP0595796B1 (en) * 1989-07-07 2003-01-15 Endorecherche Inc. Method of treatment of androgen-related diseases
DE69034148T2 (de) * 1989-07-07 2005-06-30 Endorecherche Inc., Ste-Foy Kombinationstherapie zur Prophylaxe und/oder Behandlung von gutartiger prostatischer Hyperplasie
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
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
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
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
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
US5250539A (en) * 1991-08-21 1993-10-05 Eli Lilly And Company Hexahydrobenzo[f]quinolinones
US5304562A (en) * 1991-10-09 1994-04-19 Ciba-Geigy Corporation 17β-substituted Aza-androstane derivatives
CA2084799C (en) 1991-12-17 2003-01-28 Glenn J. Gormley Method of prevention of prostatic carcinoma with 17 beta-n-monosubstituted-carbamoyl-4-aza-5 alpha-androst-1 -en-3-ones
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
EP0641356B1 (en) * 1991-12-20 1998-04-22 Glaxo Wellcome Inc. Inhibitors of 5-alpha-testosterone reductase
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
AU668180B2 (en) * 1992-05-20 1996-04-26 Merck & Co., Inc. 17-ethers and thioethers of 4-aza-steroids
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
US5510351A (en) * 1992-05-20 1996-04-23 Merck & Co., Inc. Delta-17 and delta-20 olefinic and saturated 17 beta-substituted 4-aza-5 alpha-androstan-ones as 5 alpha reductase inhibitors useful in the prevention and treatment of hyperandrogenic disorders
ES2149208T3 (es) * 1992-05-20 2000-11-01 Merck & Co Inc Inhibidores 4-azaesteroides de 5-alfa-reductasa.
WO1993023039A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. Substituted 4-aza-5a-androstan-ones as 5a-reductase inhibitors
US5710275A (en) * 1992-05-20 1998-01-20 Merck & Co., Inc. 7β-substituted-4-aza-5α-androstan-3-ones as 5α-reductase inhibitors
AU674145B2 (en) * 1992-05-20 1996-12-12 Merck & Co., Inc. New 17-ester, amide, and ketone derivatives of 3-oxo-4-azasteroids as 5a-reductase inhibitors
ATE198601T1 (de) * 1992-05-20 2001-01-15 Merck & Co Inc Ester derivate von 4-aza-steroiden
DE69326008T2 (de) * 1992-05-20 2000-03-02 Merck & Co., Inc. 17-amino-substituierte 4-azasteroide als 5-alpha-reductase inhibitoren
AU680818B2 (en) * 1992-05-21 1997-08-14 Endorecherche Inc. Improved antiandrogens
GB9210880D0 (en) * 1992-05-21 1992-07-08 Smithkline Beecham Corp Compounds
TW239145B (OSRAM) * 1992-05-21 1995-01-21 Endorech Inc
GB9213901D0 (en) * 1992-06-30 1992-08-12 Smithkline Beecham Corp Compounds
US5302589A (en) * 1992-08-07 1994-04-12 Glaxo, Inc. Heterocyclic inhibitors of 5-α-testosterone reductase
US5324734A (en) * 1992-09-15 1994-06-28 Merck & Co., Inc. Oxidization metabolites of 5-α-23-methyl-4-aza-21-nor-chol-1-ene-3, 20-dione
HU212459B (en) * 1992-10-02 1996-06-28 Richter Gedeon Vegyeszet Process for producing new 17-beta-substituted 4-aza-androstane-derivatives and pharmaceutical compositions containing them
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
US5359071A (en) * 1993-03-12 1994-10-25 Merck & Co., Inc. 15-substituted 4-azasteroids
WO1994021614A1 (en) * 1993-03-24 1994-09-29 Merck & Co., Inc. SUBSTITUTED 3-PHENANTHRIDINONE DERIVATIVES AS 5α-REDUCTASE INHIBITORS
EP0711164B1 (en) * 1993-06-28 1997-09-17 Merck & Co. Inc. 4-aza-pregnane 5-alpha-reductase isozyme 1 inhibitors
TW408127B (en) * 1993-09-17 2000-10-11 Glaxo Inc Androstenones
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
US5817818A (en) * 1994-09-16 1998-10-06 Glaxo Wellcome Inc. Androstenones
US5541322A (en) * 1994-10-14 1996-07-30 Glaxo Wellcome Inc. Synthesis of 6-azaandrostenones
US5595996A (en) * 1994-10-25 1997-01-21 Merck & Co., Inc. 7-substituted 4-aza cholanic acid derivatives and their use
US6365597B1 (en) * 1996-02-14 2002-04-02 Aventis Pharmaceuticals Inc. 4-aza steroids
US5998427A (en) * 1998-05-14 1999-12-07 Glaxo Wellcome Inc. Androstenones
DE69942578D1 (de) 1998-05-22 2010-08-26 Univ R Bifunktionelle moleküle sowie darauf basierende therapien.
JP2008539047A (ja) 2005-04-28 2008-11-13 プロテウス バイオメディカル インコーポレイテッド ファーマインフォーマティックスシステム
EP1945240B1 (en) 2005-09-16 2016-12-28 Raptor Pharmaceutical Inc Compositions comprising receptor-associated protein (rap) variants specific for cr-containing proteins and uses thereof
EP3395372B1 (en) 2009-02-20 2022-04-06 EnhanX Biopharm Inc. Glutathione-based drug delivery system
SG10201402069PA (en) 2009-05-06 2014-07-30 Lab Skin Care Inc Dermal delivery compositions comprising active agent-calcium phosphate particle complexes and methods of using the same

Family Cites Families (10)

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US2897202A (en) * 1956-03-19 1959-07-28 Monsanto Chemicals 3-keto-4-aza-delta5-steroids and method of preparing same
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
US4191759A (en) * 1978-04-13 1980-03-04 Merck & Co., Inc. N-substituted-17β-carbamoylandrost-4-en-3-one 5α reductase inhibitors
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
US4317817A (en) * 1979-08-27 1982-03-02 Richardson-Merrell Inc. Novel steroid 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
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
GB8505862D0 (en) * 1985-03-07 1985-04-11 Erba Farmitalia Steroidic 5alpha-reductase inhibitors

Also Published As

Publication number Publication date
AU608560B2 (en) 1991-04-11
GR3005284T3 (OSRAM) 1993-05-24
EP0277002A2 (en) 1988-08-03
DK37388D0 (da) 1988-01-26
DK196691A (da) 1991-12-05
DK37388A (da) 1988-07-29
JPS63192800A (ja) 1988-08-10
DK168525B1 (da) 1994-04-11
AU1077888A (en) 1988-08-04
PT86652B (pt) 1992-02-28
DK73594A (da) 1994-06-21
ES2042725T3 (es) 1993-12-16
DE3871965T2 (de) 1993-01-14
DK196691D0 (da) 1991-12-05
PT86652A (pt) 1988-02-01
IE880189L (en) 1988-07-28
CA1325006C (en) 1993-12-07
DK169840B1 (da) 1995-03-13
DK169438B1 (da) 1994-10-31
DE3871965D1 (de) 1992-07-23
IE61594B1 (en) 1994-11-16
EP0277002A3 (en) 1988-10-26
EP0277002B1 (en) 1992-06-17
ATE77388T1 (de) 1992-07-15
US4888336A (en) 1989-12-19

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