ES2066003T3 - Esteroides aromaticos sustituidos con acido sulfonico como inhibidores del esteroide 5-alfa-reductasa. - Google Patents

Esteroides aromaticos sustituidos con acido sulfonico como inhibidores del esteroide 5-alfa-reductasa.

Info

Publication number
ES2066003T3
ES2066003T3 ES89313260T ES89313260T ES2066003T3 ES 2066003 T3 ES2066003 T3 ES 2066003T3 ES 89313260 T ES89313260 T ES 89313260T ES 89313260 T ES89313260 T ES 89313260T ES 2066003 T3 ES2066003 T3 ES 2066003T3
Authority
ES
Spain
Prior art keywords
reductase
inhibitors
steroid
alpha
sulphonic acid
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.)
Expired - Lifetime
Application number
ES89313260T
Other languages
English (en)
Inventor
Dennis Alan Holt
Brian Walter Metcalf
Mark Alan Levy
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
Application granted granted Critical
Publication of ES2066003T3 publication Critical patent/ES2066003T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime 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
    • 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
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0072—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the A ring of the steroid being aromatic

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)

Abstract

COMPONENTES DE ESTRUCTURA (I) EN LA QUE LAS LINEAS DOTADAS INDICAN LA PRESENCIA OPCIONAL DE UN DOBLE ENLACE, X1, X2 Y X3 SON H, HALOGENO, CF3, ALQUIL C1-6, ALCOXI C1-6, CN, NO2, N(R1)2, CHO O CO2R1; R1 ES H O ALQUIL C1-8 Y R ES HIDROGENO, HIDROXI O ACETOXI; PROCESOS PARA SU PREPARACION, COMPOSICIONES QUE LOS CONTIENEN Y SU USO EN MEDICINA COMO INHIBIDORES DE REDUCTASA-A-5.
ES89313260T 1988-12-23 1989-12-19 Esteroides aromaticos sustituidos con acido sulfonico como inhibidores del esteroide 5-alfa-reductasa. Expired - Lifetime ES2066003T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US07/290,020 US4970205A (en) 1988-12-23 1988-12-23 Sulfonic acid substituted aromatic steroids as inhibitors of steroid 5-α-reductase

Publications (1)

Publication Number Publication Date
ES2066003T3 true ES2066003T3 (es) 1995-03-01

Family

ID=23114202

Family Applications (1)

Application Number Title Priority Date Filing Date
ES89313260T Expired - Lifetime ES2066003T3 (es) 1988-12-23 1989-12-19 Esteroides aromaticos sustituidos con acido sulfonico como inhibidores del esteroide 5-alfa-reductasa.

Country Status (14)

Country Link
US (1) US4970205A (es)
EP (1) EP0375347B1 (es)
JP (1) JPH02225494A (es)
CN (1) CN1051181A (es)
AT (1) ATE115960T1 (es)
AU (2) AU627528B2 (es)
CA (1) CA2005215A1 (es)
DE (1) DE68920128T2 (es)
DK (1) DK645189A (es)
ES (1) ES2066003T3 (es)
GR (1) GR3015476T3 (es)
IE (1) IE894108L (es)
PT (1) PT92719A (es)
ZA (1) ZA899669B (es)

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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]
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
US5300294A (en) * 1990-06-27 1994-04-05 Smithkline Beecham Corporation Method of treating prostatic adenocarcinoma
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
IL101243A (en) * 1991-03-20 1999-12-22 Merck & Co Inc Pharmaceutical preparations for the treatment of benign prostatic hyperplasia containing steroid history
IL104303A0 (en) * 1992-01-06 1993-05-13 Smithkline Beecham Corp Process
RU94046044A (ru) * 1992-05-20 1996-10-10 Мерк Энд Ко. Новые 7 бета -замещенные 4-аза- 5 альфа -холестан-оны в качестве ингибиторов 5 альфа -редуктазы, фармацевтическая композиция на их основе, способ ее получения
EP0641204B1 (en) * 1992-05-20 2000-08-16 Merck & Co. Inc. 17-ethers and thioethers of 4-aza-steroids
DE69329856D1 (de) * 1992-05-20 2001-02-15 Merck & Co Inc Ester derivate von 4-aza-steroiden
ATE195129T1 (de) * 1992-05-20 2000-08-15 Merck & Co Inc 4-azasteroide als 5-alpha-reduktase
AU675225B2 (en) * 1992-05-20 1997-01-30 Merck & Co., Inc. 17-amino substituted 4-azasteroid 5alpha-reductase inhibitors
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
WO1993023053A1 (en) * 1992-05-21 1993-11-25 Endorecherche Inc. INHIBITORS OF TESTOSTERONE 5α-REDUCTASE ACTIVITY
JPH0641038A (ja) 1992-07-17 1994-02-15 Mitsubishi Kasei Corp カルボン酸誘導体
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
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
AU6413594A (en) * 1993-03-24 1994-10-11 Merck & Co., Inc. Substituted 3-phenanthridinone derivatives as 5alpha-reductase inhibitors
JP3325026B2 (ja) * 1993-06-28 2002-09-17 メルク エンド カンパニー インコーポレーテッド ４−アザ−プレグナン５α−レダクターゼアイソザイム１阻害剤
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
US5637310A (en) * 1993-12-20 1997-06-10 Smithkline Beecham Corporation Method of treating prostatic adenocarcinoma
DE4447714C2 (de) * 1994-08-09 1998-02-05 Jenapharm Gmbh Verwendung von Estra-1,3,5(10)-trien-Derivaten zur Hormonsubstitutions-Therapie
US5541322A (en) * 1994-10-14 1996-07-30 Glaxo Wellcome Inc. Synthesis of 6-azaandrostenones
ATE473759T1 (de) 1998-05-22 2010-07-15 Univ Leland Stanford Junior Bifunktionelle moleküle sowie darauf basierende therapien.
CN103259027A (zh) 2005-04-28 2013-08-21 普罗透斯数字保健公司 药物信息系统
JP2009508494A (ja) 2005-09-16 2009-03-05 ラプトール ファーマシューティカル インコーポレイテッド Ｃｒを含むタンパク質に対して特異的な受容体−結合タンパク質（ｒａｐ）変異体を含む組成物およびその使用
CN100355772C (zh) * 2005-12-28 2007-12-19 天津大学 具有5α－还原酶抑制活性的甾体化合物及其制备方法
PT2398500T (pt) 2009-02-20 2019-06-14 2 Bbb Medicines B V Sistema de entrega de medicamentos à base de glutationas
TWI556839B (zh) 2009-05-06 2016-11-11 研究室護膚股份有限公司 包含活性劑－磷酸鈣粒子複合物之皮膚遞送組成物及其使用方法

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2555579A (en) * 1950-05-24 1951-06-05 Ayerst Mckenna & Harrison P-aminobenzoyl-diethyl aminoethanol salts of steroids 3-monosulphates
DE1107664B (de) * 1959-11-05 1961-05-31 Schering Ag Verfahren zur Herstellung neuer in 3-Stellung substituierter OEstratriene
FR1521896A (fr) * 1966-05-04 1968-04-19 Ohio State University Represen Procédé de transformation de thioncarbamates en thiolcarbamates
FR2022104A1 (es) * 1968-07-24 1970-07-31 Farmaceutici Italia
US4191759A (en) * 1978-04-13 1980-03-04 Merck & Co., Inc. N-substituted-17β-carbamoylandrost-4-en-3-one 5α reductase inhibitors
US4179453A (en) * 1978-04-13 1979-12-18 Merck & Co., Inc. Process for preparing 17β-carboxy-5-androsten-3-ones
US4377584A (en) * 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
US4317817A (en) * 1979-08-27 1982-03-02 Richardson-Merrell Inc. Novel steroid 5α-reductase inhibitors
DK465481A (da) * 1980-11-21 1982-05-22 Hoffmann La Roche Fremgangsmaade til fremstilling af d-homostemoider
JPS5953417A (ja) * 1982-09-21 1984-03-28 Shiseido Co Ltd 皮膚外用剤
JPS60116657A (ja) * 1983-11-30 1985-06-24 Ono Pharmaceut Co Ltd アニリン誘導体
JPS60142941A (ja) * 1983-12-28 1985-07-29 Ono Pharmaceut Co Ltd ケトン化合物
JPS60146855A (ja) * 1984-01-11 1985-08-02 Ono Pharmaceut Co Ltd アニリン誘導体
CA1261835A (en) * 1984-08-20 1989-09-26 Masaaki Toda (fused) benz(thio)amides
US4910226A (en) * 1987-04-29 1990-03-20 Smithkline Beckman Corporation Steroid 5-alpha-reductase inhibitors

Also Published As

Publication number Publication date
US4970205A (en) 1990-11-13
DK645189D0 (da) 1989-12-19
CN1051181A (zh) 1991-05-08
AU655691B2 (en) 1995-01-05
DE68920128T2 (de) 1995-05-11
AU627528B2 (en) 1992-08-27
IE894108L (en) 1990-06-23
EP0375347B1 (en) 1994-12-21
ZA899669B (en) 1990-11-28
CA2005215A1 (en) 1990-06-23
GR3015476T3 (en) 1995-06-30
DK645189A (da) 1990-06-24
DE68920128D1 (de) 1995-02-02
AU2960292A (en) 1993-01-21
PT92719A (pt) 1990-06-29
EP0375347A1 (en) 1990-06-27
AU4700589A (en) 1990-06-28
ATE115960T1 (de) 1995-01-15
JPH02225494A (ja) 1990-09-07

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