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)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Endocrinology (AREA)
  • Bioinformatics & Cheminformatics (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)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5138063A (en) * 1984-02-27 1992-08-11 Merck & Co., Inc. 17β-methoxycarbonyl-4-aza-androsten-1-en-3-ones
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]
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
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
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
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
ATE195129T1 (de) * 1992-05-20 2000-08-15 Merck & Co Inc 4-azasteroide als 5-alpha-reduktase
CZ283894A3 (en) * 1992-05-20 1995-09-13 Merck & Co Inc 7beta-substituted 4-aza-5alpha-cholestanones, their use for the preparation of pharmaceutical preparations and pharmaceutical compositions containing thereof
CA2135173A1 (en) * 1992-05-20 1993-11-25 Bruce E. Witzel Ester derivatives of 4-aza-steroids
US5237064A (en) * 1992-05-20 1993-08-17 Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
EP0641204B1 (en) * 1992-05-20 2000-08-16 Merck & Co. Inc. 17-ethers and thioethers of 4-aza-steroids
DE69326008T2 (de) * 1992-05-20 2000-03-02 Merck & Co., Inc. 17-amino-substituierte 4-azasteroide als 5-alpha-reductase inhibitoren
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
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
US5621104A (en) * 1993-03-24 1997-04-15 Merck & Co., Inc. Substituted 3-phenanthridinone derivatives as 5-alpha-reductase inhibitors
FR2706454B1 (fr) * 1993-06-17 1995-09-15 Roussel Uclaf Nouveaux 19-Nor stéroïdes, procédé et intermédiaires de préparation, application comme médicaments et compositions pharmaceutiques les contenant.
DE69405760T2 (de) * 1993-06-28 1998-04-09 Merck & Co Inc 4-aza-pregnan-5-alpha-reductase isozym 1 inhibitoren
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
ES2347027T3 (es) 1998-05-22 2010-10-22 The Board Of Trustees Of The Leland Stanford Junior University Moleculas bifuncionales y terapias basadas en las mismas.
EP2671507A3 (en) 2005-04-28 2014-02-19 Proteus Digital Health, Inc. Pharma-informatics system
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
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
CA2752373C (en) 2009-02-20 2017-10-10 To-Bbb Holding B.V. Glutathione-based drug delivery system
IL255113B (en) 2009-05-06 2022-09-01 Laboratory Skin Care Inc Dermal delivery compositions comprising active agent-calcium phosphate particle complexes and methods of using the same

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
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
US4191759A (en) * 1978-04-13 1980-03-04 Merck & Co., Inc. N-substituted-17β-carbamoylandrost-4-en-3-one 5α 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
DK645189D0 (da) 1989-12-19
CN1051181A (zh) 1991-05-08
AU627528B2 (en) 1992-08-27
DE68920128D1 (de) 1995-02-02
EP0375347B1 (en) 1994-12-21
CA2005215A1 (en) 1990-06-23
JPH02225494A (ja) 1990-09-07
IE894108L (en) 1990-06-23
EP0375347A1 (en) 1990-06-27
AU2960292A (en) 1993-01-21
ATE115960T1 (de) 1995-01-15
GR3015476T3 (en) 1995-06-30
AU655691B2 (en) 1995-01-05
PT92719A (pt) 1990-06-29
ZA899669B (en) 1990-11-28
US4970205A (en) 1990-11-13
AU4700589A (en) 1990-06-28
DE68920128T2 (de) 1995-05-11
DK645189A (da) 1990-06-24

Similar Documents

Publication Publication Date Title
ES2066003T3 (es) Esteroides aromaticos sustituidos con acido sulfonico como inhibidores del esteroide 5-alfa-reductasa.
ES2059789T3 (es) Esteroides sustituidos con acido fosfinico como inhibidores de la esteroide-5 alfa-reductasa.
ES2067557T3 (es) Esteroides aromaticos sustituidos con acido fosfinico como inhibidores de la esteroide 5-d-reductasa.
ZA899672B (en) Phosphonic acid substituted aromatic steroids as inhibitors of steroid 5-1-reductase
MX9200374A (es) Nuevos esteres esteroides, procedimiento para su preparacion y preparacion farmaceutica que los contiene.
IT1215165B (it) Derivati del naftalene aventi azione retinoide procedimento per la loro preparazione e composizioni medicinali o cosmetiche che li con tengono
IT1130455B (it) Derivati dell acido & amminopropan solfonico ad attivita membranaria rinforzata e procedimento per la loro preparazione
IT1107833B (it) Derivati dell acido 5 2 pirroil 1.2 diidro 3h pirrolo 1.2a pirroil i carbossilico e procedimento per la loro preparazione
ES2052603T3 (es) Derivados de bencimidazol, procedimiento para su produccion y composicion farmaceutica que los contienen.
ES2056105T3 (es) Di-t-butilfenoles sustituidos.
ES2090217T3 (es) Laca fotosensible.
ES2059740T3 (es) Un metodo de fabricacion de un medicamento para inducir la contraccion uterina.
ES2052761T3 (es) Nuevos esteres del acido androstano 17-carboxilico, procedimiento para su preparacion y medicamento que los contiene.
IT946142B (it) Derivati dell acido 2 fosfonobutan 1 2 dicarbossilico procedimento per la loro preparazione e loro impiego come complessanti
ES2054738T3 (es) Derivados de acido 3-desmetil-4-fluoromevalonico, procedimiento para su preparacion, preparados farmaceuticos a base de estos compuestos, su empleo y productos intermedios.
MX9203642A (es) Compuestos substituidos del acido 1,3,4,9-tetrahidropirano (3,4-b)-indol-1-acetico y composiciones farmaceuticas que los contienen.
ES2046345T3 (es) Procedimiento para la obtencion de esteres substituidos del acido acrilico.
ES2070202T3 (es) Nuevos derivados de serina, procedimiento para su preparacion y su uso en terapia humana.
YU46838B (sh) Postupak za dobijanje preparata za lečenje kožne bolesti psoriazisa
ES2069990T3 (es) Acido acilaminoalquilidenhidroxibisfosfonico util en la terapia de enfermedades osteoarticulares.
IT1143801B (it) Procedimento per la preparazione di derivati dell'acido sulfamil benzoico
ES2179206T3 (es) Derivados de 12h-dibenzo(d,g)(1,3)dioxocina.
IT8522358A0 (it) Derivati dell'acido 19,20-bis,nor-prostanoico adattivita' antiulcera e anoressica, procedimento epr la loro preparazione e composizioni farmaceutiche.
ES2051386T3 (es) Rejilla mezcladora intermedia.
ES387494A1 (es) Procedimiento para la preparacion de nuevos esteres de la 6alfa, 9 alfa-difluoro - 11 beta, 21-dihidroxi-16 alfa, 17 alfa-isopropiliden-dioxi-pregna-1,4-dien - 3,20-diona.

Legal Events

Date Code Title Description
FG2A Definitive protection

Ref document number: 375347

Country of ref document: ES