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Title:
17-ARYL AND 17-HETEROCYCLYL-14BETA-5ALPHA-ANDROSTANE, ANDROSTENE AND ANDROSTADIENE DERIVATIVE EFFECTIVE FOR CARDIOVASCULAR SYSTEM, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITION CONTAINING THEM
Document Type and Number:
Japanese Patent JPH06192287
Kind Code:
A
Abstract:

PURPOSE: To obtain new safe compounds having low toxicities and useful for treating cardiac and vascular diseases such as heart failure and hypertension.

CONSTITUTION: There compounds of formula I [a wave line means that 17- positioned substituent can take α or β configuration; Y is O or guanidimino when a wave line at 3-position and a solid line are double bonded, or Y is OH, OR2 (R2 is H, a 2-6C alkyl or the like) or the like when the double line is a single bond; R is an aryl ring, or an (un)satd. heterocyclic ring contg. a hetero atom such as O and S; R1 is H, methyl or the like], their stereoisomers, metabolites and metabolite precursors such as 17β-phenyl-5α-androst-15- ene-3β,14β,17α-triol are obtained by reacting an aryl or heterocyclyl organic metal with a compd. of formula II (W is H or a protecting group; Y is Y in formula I other than guanidinoimino, and protected in the case of containing OH or the like) in an inert neutral solvent such as THF at -78°C to the room temperature.


Inventors:
Melloni, Piero
Bernardi, Luigi
Ferrandi, Mara
Frigerio, Marco
Mauro, Marina
Quadri, Luisa
Application Number:
JP1993000243361
Publication Date:
July 12, 1994
Filing Date:
September 29, 1993
Export Citation:
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Assignee:
SIGMA TAU IND FARMACEUT RIUNITE SPA
International Classes:
A61K31/565; A61K31/575; A61K31/58; A61P9/00; A61P9/12; C07J1/00; C07J9/00; C07J17/00; C07J31/00; C07J33/00; C07J41/00; C07J43/00; C07J51/00; (IPC1-7): C07J1/00; A61K31/565; A61K31/58; C07J17/00; C07J33/00; C07J43/00
Attorney, Agent or Firm:
志賀 正武 (外2名)