ES2110109T3 - Derivados de 4-aza-5-alfa-androstan-3-ona 17-beta-sustituidos. - Google Patents

Derivados de 4-aza-5-alfa-androstan-3-ona 17-beta-sustituidos.

Info

Publication number
ES2110109T3
ES2110109T3 ES93917706T ES93917706T ES2110109T3 ES 2110109 T3 ES2110109 T3 ES 2110109T3 ES 93917706 T ES93917706 T ES 93917706T ES 93917706 T ES93917706 T ES 93917706T ES 2110109 T3 ES2110109 T3 ES 2110109T3
Authority
ES
Spain
Prior art keywords
group
alkilo
prostatic
alkyl
hydrogen
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
ES93917706T
Other languages
English (en)
Inventor
Achille Panzeri
Marcella Nesi
Salle Enrico Di
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.)
Pfizer Italia SRL
Original Assignee
Pharmacia and Upjohn SpA
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 Pharmacia and Upjohn SpA filed Critical Pharmacia and Upjohn SpA
Application granted granted Critical
Publication of ES2110109T3 publication Critical patent/ES2110109T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • 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

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)
  • Indole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Crystals, And After-Treatments Of Crystals (AREA)

Abstract

UN COMPUESTO DE LA FORMULA (I) EN LA QUE R ES UN ATOMO DE HIDROGENO O UN GRUPO ALKILO C1-C4; A ES UN ENLACE SENCILLO O UNA CADENA DE ALKILENO C1-C6 RECTA O RAMIFICADA; R1 ES UN ATOMO DE HIDROGENO O UN GRUPO ALKILO C1-C6; R2 ES UN GRUPO ALKILO C1-C6, UN CICLOALKILO C5-C7 O UN GRUPO CICLOALKILO C6-C10, ARILO O UN GRUPO ARILALKILO C7-C10 O UN GRUPO HETEROCICLOALKILO C6-C10; R3 ES HIDROGENO, UN GRUPO ALKILO C1-C4 O UN ARILO O UN GRUPO ARILALKILO C7-C10; Z ES UN GRUPO ALKILO C1-C6, UN GRUPO -OR5 EN EL QUE R5 ES UN GRUPO ALKILO C1-C6, UN GRUPO (A) EN EL QUE CADA R6 Y R7 ES HIDROGENO, ALKILO C1-C6, CICLOALKILO C5-C7, FENILO O R6 Y R7 JUNTO CON EL NITROGENO AL QUE SE ENCUENTRAN ENLAZADOS FORMAN UN ANILLO HETEROMONOCICLICO SATURADO PENTATOMICO O HEXATOMICO; Y EL SIMBOLO DE LA RAYA CONTINUA CON LOS GUIONES ENCIMA REPRESENTA UN ENLACE DOBLE O UNO SENCILLO, ES UN INHIBIDOR DE LA 5(ALFA)REDUCTASA Y ES TERAPEUTICAMENTE UTIL PARA LA HIPERPLASIA PROSTATICA BENIGNA, EL CANCER PROSTATICO Y EL DE MAMA, LA SEBORREA, EL HIRSUTISMO FEMENINO Y LA CALVICIE MASCULINA.
ES93917706T 1992-07-31 1993-07-29 Derivados de 4-aza-5-alfa-androstan-3-ona 17-beta-sustituidos. Expired - Lifetime ES2110109T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB929216329A GB9216329D0 (en) 1992-07-31 1992-07-31 17beta-substituted 4-aza-5alpha-androstan-3-one derivatives

Publications (1)

Publication Number Publication Date
ES2110109T3 true ES2110109T3 (es) 1998-02-01

Family

ID=10719633

Family Applications (1)

Application Number Title Priority Date Filing Date
ES93917706T Expired - Lifetime ES2110109T3 (es) 1992-07-31 1993-07-29 Derivados de 4-aza-5-alfa-androstan-3-ona 17-beta-sustituidos.

Country Status (21)

Country Link
US (1) US5418238A (es)
EP (1) EP0611374B1 (es)
JP (1) JPH06511498A (es)
CN (1) CN1085223A (es)
AT (1) ATE159531T1 (es)
AU (1) AU660374B2 (es)
CA (1) CA2120339A1 (es)
CZ (1) CZ153693A3 (es)
DE (1) DE69314769T2 (es)
DK (1) DK0611374T3 (es)
ES (1) ES2110109T3 (es)
FI (1) FI941423A7 (es)
GB (1) GB9216329D0 (es)
HU (1) HUT67900A (es)
IL (1) IL106519A0 (es)
MX (1) MX9304587A (es)
NO (1) NO941081L (es)
NZ (1) NZ254788A (es)
PH (1) PH30459A (es)
WO (1) WO1994003476A1 (es)
ZA (1) ZA935480B (es)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
EP0705272B1 (en) * 1993-06-24 2002-03-27 Richter Gedeon Vegyeszeti Gyar R.T. Novel process for preparing 17 beta-substituted 4-azaandrostane derivatives
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
HUT74613A (en) * 1993-10-21 1997-01-28 Merck & Co Inc 16-substituted-4-aza-androstane derivatives as 5-alpha-reductase isozyme 1 inhibitors and pharmaceutical compositions containing the same
GB9415178D0 (en) * 1994-07-28 1994-09-21 Erba Carlo Spa 4-azasteroids with side-chain fluoroketones
US5541322A (en) * 1994-10-14 1996-07-30 Glaxo Wellcome Inc. Synthesis of 6-azaandrostenones
US5543417A (en) * 1994-10-21 1996-08-06 Merck & Co., Inc. Combination method of treating acne using 4-AZA-5α-cholestan-ones and 4-AZA-5α-androstan-ones as selective 5α-reductase inhibitors with anti-bacterial, keratolytic, or anti-inflammatory agents
US5595996A (en) * 1994-10-25 1997-01-21 Merck & Co., Inc. 7-substituted 4-aza cholanic acid derivatives and their use
IT1271325B (it) * 1994-12-23 1997-05-27 Poli Ind Chimica Spa Composti diastereomericamente puri derivati da 3-oxo e 3-tioxo-4-azaandrostani e loro uso come antiandrogeni
GB9518858D0 (en) * 1995-09-14 1995-11-15 Pharmacia Spa Phenylsubstituted 4-azasteroid fluoroderivatives
US6274602B1 (en) 1998-06-03 2001-08-14 Gpi Nil Holdings, Inc. Heterocyclic thioester and ketone hair growth compositions and uses
US6187796B1 (en) 1998-06-03 2001-02-13 Gpi Nil Holdings, Inc. Sulfone hair growth compositions and uses
US6271244B1 (en) 1998-06-03 2001-08-07 Gpi Nil Holdings, Inc. N-linked urea or carbamate of heterocyclic thioester hair growth compositions and uses
US20010049381A1 (en) 1997-06-04 2001-12-06 Gpl Nil Holdings, Inc., Pyrrolidine derivative hair growth compositions and uses
US6187784B1 (en) 1998-06-03 2001-02-13 Gpi Nil Holdings, Inc. Pipecolic acid derivative hair growth compositions and uses
US5945441A (en) * 1997-06-04 1999-08-31 Gpi Nil Holdings, Inc. Pyrrolidine carboxylate hair revitalizing agents
GB9727522D0 (en) 1997-12-31 1998-02-25 Pharmacia & Upjohn Spa Process for preparing carboxamido-4-azasteroids
EP1085853A1 (en) * 1998-06-03 2001-03-28 GPI NIL Holdings, Inc. Heterocyclic ester and amide hair growth compositions and uses
CN1295561A (zh) 1998-06-03 2001-05-16 Gpinil控股公司 N－杂环羧酸或羧酸等排物的n－结合氨磺酰
US6172087B1 (en) 1998-06-03 2001-01-09 Gpi Nil Holding, Inc. N-oxide of heterocyclic ester, amide, thioester, or ketone hair growth compositions and uses
US6331537B1 (en) 1998-06-03 2001-12-18 Gpi Nil Holdings, Inc. Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds
ES2237408T3 (es) * 1999-01-25 2005-08-01 Smithkline Beecham Corporation Antiandrogenos y procedimientos para tratar una enfermedad.
AU2004255749B2 (en) 2003-06-30 2008-12-18 Merck Sharp & Dohme Corp. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
JP2007521297A (ja) * 2003-06-30 2007-08-02 メルク　エンド　カムパニー　インコーポレーテッド アンドロゲン受容体モジュレータとしての１７−アセトアミド−４−アザステロイド誘導体
CA2530025A1 (en) * 2003-06-30 2005-01-20 William P. Dankulich 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
US7329750B2 (en) * 2003-06-30 2008-02-12 Merck & Co., Inc. 17-Acetamido-4-azasteroid derivatives as androgen receptor modulators
AU2004272007B2 (en) * 2003-09-10 2009-05-28 Merck Sharp & Dohme Corp. 17-heterocyclic-4-azasteroid derivatives as androgen receptor modulators
CA2537663A1 (en) 2003-09-10 2005-03-24 Merck & Co., Inc. 17-heterocyclic-4-azasteroid derivatives as androgen receptor modulators
CA2562132A1 (en) * 2004-04-08 2005-10-27 Merck & Co., Inc. 17 beta-acetamide-4-azasteroids as androgen receptor modulators
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
JP5260114B2 (ja) * 2008-03-31 2013-08-14 株式会社カネカ Ｎ−アルコキシカルボニル−ｔｅｒｔ−ロイシンの製造法
CN104147139A (zh) * 2013-05-08 2014-11-19 浙江大学 桂花多酚提取物的用途

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
GB8505862D0 (en) * 1985-03-07 1985-04-11 Erba Farmitalia Steroidic 5alpha-reductase inhibitors
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
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
IE76452B1 (en) * 1990-10-29 1997-10-22 Sankyo Co Azasteroid compounds for the treatment of prostatic hypertrophy their preparation and use

Also Published As

Publication number Publication date
GB9216329D0 (en) 1992-09-16
IL106519A0 (en) 1993-11-15
PH30459A (en) 1997-05-28
NO941081L (es) 1994-05-31
JPH06511498A (ja) 1994-12-22
HU9400913D0 (en) 1994-06-28
CZ153693A3 (en) 1994-02-16
EP0611374B1 (en) 1997-10-22
AU660374B2 (en) 1995-06-22
CA2120339A1 (en) 1994-02-17
CN1085223A (zh) 1994-04-13
AU4704993A (en) 1994-03-03
NO941081D0 (es) 1994-03-24
NZ254788A (en) 1995-11-27
WO1994003476A1 (en) 1994-02-17
FI941423A0 (fi) 1994-03-28
DE69314769T2 (de) 1998-02-26
US5418238A (en) 1995-05-23
FI941423A7 (fi) 1994-05-27
MX9304587A (es) 1994-02-28
HUT67900A (en) 1995-05-29
DK0611374T3 (da) 1997-12-15
ZA935480B (en) 1994-02-23
ATE159531T1 (de) 1997-11-15
DE69314769D1 (de) 1997-11-27
EP0611374A1 (en) 1994-08-24

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