AU608560B2 - Steroid 5-alpha-reductase inhibitors - Google Patents

Steroid 5-alpha-reductase inhibitors Download PDF

Info

Publication number
AU608560B2
AU608560B2 AU10778/88A AU1077888A AU608560B2 AU 608560 B2 AU608560 B2 AU 608560B2 AU 10778/88 A AU10778/88 A AU 10778/88A AU 1077888 A AU1077888 A AU 1077888A AU 608560 B2 AU608560 B2 AU 608560B2
Authority
AU
Australia
Prior art keywords
hydrogen
alpha
alk
alkyl
methyl
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
AU10778/88A
Other languages
English (en)
Other versions
AU1077888A (en
Inventor
Dennis Alan Holt
Mark Alan Levy
Brian Walter Metcalf
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
SmithKline Beecham Corp
Original Assignee
SmithKline Beecham Corp
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 Beecham Corp filed Critical SmithKline Beecham Corp
Publication of AU1077888A publication Critical patent/AU1077888A/en
Application granted granted Critical
Publication of AU608560B2 publication Critical patent/AU608560B2/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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)
AU10778/88A 1987-01-28 1988-01-27 Steroid 5-alpha-reductase inhibitors Ceased AU608560B2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US007539 1987-01-28
US07/007,539 US4888336A (en) 1987-01-28 1987-01-28 Steroid 5-alpha-reductase inhibitors

Publications (2)

Publication Number Publication Date
AU1077888A AU1077888A (en) 1988-08-04
AU608560B2 true AU608560B2 (en) 1991-04-11

Family

ID=21726780

Family Applications (1)

Application Number Title Priority Date Filing Date
AU10778/88A Ceased AU608560B2 (en) 1987-01-28 1988-01-27 Steroid 5-alpha-reductase inhibitors

Country Status (13)

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

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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
EP0485392B1 (en) * 1989-07-07 1998-09-09 Endorecherche Inc. Androgen derivatives for use in the inhibition of sex steroid activity
WO1991000731A1 (en) * 1989-07-07 1991-01-24 Endorecherche Inc. Combination therapy for prophylaxis and/or treatment of benign prostatic hyperplasia
AU5851690A (en) * 1989-07-07 1991-02-06 Endorecherche Inc. Method of treatment of androgen-related diseases
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
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
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
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
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
DE69225244T2 (de) * 1991-12-20 1998-09-24 Glaxo Wellcome Inc Inhibitoren von testosteron-5-alpha reductase.
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
WO1993023040A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. 17-ethers and thioethers of 4-aza-steroids
FI945442A7 (fi) * 1992-05-20 1994-11-18 Merck & Co Inc Uudet 7beta-substituoidut 4-atsa-5alfa-kolestanonit 5alfa-reduktaasi-i nhibiittoreina
JPH07508034A (ja) * 1992-05-20 1995-09-07 メルク　エンド　カンパニー　インコーポレーテッド １７−アミノ置換４−アザステロイド５α−レダクターゼ阻害剤
WO1993023039A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. Substituted 4-aza-5a-androstan-ones as 5a-reductase inhibitors
DE69329149T2 (de) * 1992-05-20 2001-03-29 Merck & Co., Inc. 4-azasteroide als 5-alpha-reduktase
JPH07508032A (ja) * 1992-05-20 1995-09-07 メルク　エンド　カンパニー　インコーポレーテッド ５α−レダクターゼ阻害剤としての新規Δ−１７−及びΔ−２０オレフィン性並びに飽和１７β−置換４−アザ−５α−アンドロスタン−オン
WO1993023420A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. NEW 7β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS
JPH07508033A (ja) * 1992-05-20 1995-09-07 メルク　エンド　カンパニー　インコーポレーテッド ５α−レダクターゼ阻害剤としての３−オキソ−４−アザステロイドの新規１７−エステル，アミド及びケトン誘導体
EP0649306B1 (en) * 1992-05-20 2001-01-10 Merck & Co. Inc. Ester derivatives of 4-aza-steroids
EP0641211A1 (en) * 1992-05-21 1995-03-08 Endorecherche Inc. INHIBITORS OF TESTOSTERONE 5$g(a)-REDUCTASE ACTIVITY
GB9210880D0 (en) * 1992-05-21 1992-07-08 Smithkline Beecham Corp Compounds
AU680818B2 (en) * 1992-05-21 1997-08-14 Endorecherche Inc. Improved antiandrogens
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
US5658922A (en) * 1993-06-28 1997-08-19 Merck & Co., Inc. 4-aza-pregnane 5α-reductase isozyme 1 inhibitors
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
TW408127B (en) * 1993-09-17 2000-10-11 Glaxo Inc Androstenones
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
CA2330611A1 (en) 1998-05-22 1999-12-02 The Board Of Trustees Of The Leland Stanford Junior University Bifunctional molecules and therapies based thereon
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
US9062126B2 (en) 2005-09-16 2015-06-23 Raptor Pharmaceuticals Inc. Compositions comprising receptor-associated protein (RAP) variants specific for CR-containing proteins and uses thereof
PT2398500T (pt) 2009-02-20 2019-06-14 2 Bbb Medicines B V Sistema de entrega de medicamentos à base de glutationas
CN102458374A (zh) 2009-05-06 2012-05-16 实验室护肤股份有限公司 包含活性剂-磷酸钙颗粒复合物的皮肤递送组合物及其使用方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0155096A2 (en) * 1984-02-27 1985-09-18 Merck & Co. Inc. 17 Beta-Substituted-4-aza-5-alpha-androstenones and their use as 5-alpha-reductase inhibitors

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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
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
US4191759A (en) * 1978-04-13 1980-03-04 Merck & Co., Inc. N-substituted-17β-carbamoylandrost-4-en-3-one 5α 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
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
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

Patent Citations (3)

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EP0155096A2 (en) * 1984-02-27 1985-09-18 Merck & Co. Inc. 17 Beta-Substituted-4-aza-5-alpha-androstenones and their use as 5-alpha-reductase inhibitors
AU584321B2 (en) * 1984-02-27 1989-05-25 Merck & Co., Inc. 17 ```(N-t-butylcarbamoyl)-4-aza-5```-androst-1-en-3-one
AU3313589A (en) * 1984-02-27 1989-08-10 Merck & Co., Inc. 17beta-n-monosubstituted carbamoyl or 17beta-acyl-4-aza- 5alpha-androst-1-en-3-ones as 5alpha reductase inhibitors

Also Published As

Publication number Publication date
ZA88549B (en) 1988-07-27
PT86652B (pt) 1992-02-28
DK196691A (da) 1991-12-05
DK169840B1 (da) 1995-03-13
DK37388D0 (da) 1988-01-26
GR3005284T3 (esLanguage) 1993-05-24
DE3871965T2 (de) 1993-01-14
DE3871965D1 (de) 1992-07-23
JPS63192800A (ja) 1988-08-10
AU1077888A (en) 1988-08-04
EP0277002B1 (en) 1992-06-17
DK169438B1 (da) 1994-10-31
IE880189L (en) 1988-07-28
DK37388A (da) 1988-07-29
ATE77388T1 (de) 1992-07-15
CA1325006C (en) 1993-12-07
IE61594B1 (en) 1994-11-16
PT86652A (pt) 1988-02-01
EP0277002A2 (en) 1988-08-03
DK168525B1 (da) 1994-04-11
EP0277002A3 (en) 1988-10-26
US4888336A (en) 1989-12-19
DK196691D0 (da) 1991-12-05
ES2042725T3 (es) 1993-12-16
DK73594A (da) 1994-06-21

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