US 2003/0158117 A1 · Coniosulfides and their derivatives, processes for preparing them, and their use as pharmaceuticals

Abstract

The present invention relates to compounds of the formula 1 which are formed during fermentation by the microorganism Coniochaeta ellipsoidea Udagawa, DSM 13856, or by one of its mutations and/or variants, and chemically derivatized if appropriate. The invention furthermore relates to a process for preparing compounds of the formula (I), and to their use as pharmaceuticals. In addition, the invention relates to the use of a compound of the formula (VI) 2 for producing a pharmaceutical for the treatment and prophylaxis of degenerative neuropathics or of Alzheimer's disease.

Claims38

Dependent claims

A compound of formula (I)

12
where
R1 is
(a) H, or
(b) a radical selected from —C1-C6-alkyl, —C2-C6-alkenyl, —C2-C6-alkynyl or —C6-C10-aryl, which can be substituted once or twice by
(b1) —OH,
(b2) ═O,
(b3) —O—(C1-C6-alkyl),
(b4) —O—(C2-C6-alkenyl),
(b5) —C6-C10-aryl,
(b6) —NH—C1-C6-alkyl,
(b7) —NH—C2-C6-alkenyl,
(b8) —NH2 or
(b9) fluorine, chlorine, bromine or iodine,
in which the substituents (b3) to (b8) can also be still further substituted by —CN, -amide or -oxime functions, or
(c) —(C1-C4-alkyl)-(C6-C10-aryl), or
(d) —NH2, —NH—(C1-C6-alkyl), or —NH—(C2-C6-alkenyl),
R2 is H, methyl, ethyl, n-propyl, isopropyl, n-butyl or iso-butyl,
R3 is a radical which is composed of from 1 to 10 amino acids and which can be N-terminally protected,
R4 is H, —C1-C6-alkyl, or —CO—(C1-C6-alkyl), and
p is an integer 0, 1 or 2,
with the exception of the compounds of the formula (I) in which, at the same time,
R1 is H,
R2 is H,
R3 is —CO—CH3,
R4 is H, and
p is 0 or 1,
and/or a stereoisomeric form of the compound of the formula (I) and/or mixtures of this form in any ratio,
and/or a physiologically tolerated salt of the compound of the formula (I).

26 more elements

Dependencies are inferred from the claim text.

Coniosulfides and their derivatives, processes for preparing them, and their use as pharmaceuticals

Life of this patent

Coniosulfides and their derivatives, processes for preparing them, and their use as pharmaceuticals

Life of this patent

Abstract

Claims38