摘要:
It has been found that nonimmunosuppressive, cyclophilin-binding cyclosporins are useful in the treatment and prevention of AIDS and AIDS-related disorders. Such cyclosporins include novel Ciclosporin derivatives modified at the 4- and/or 5-positions.
摘要:
An aldehyde (R.sup.1 CHO) and optically active 3-hydroxybutyric acid (CH.sub.3 CH(OH)CH.sub.2 COOH) are reacted to form an optically active dioxanone. This dioxanone is reacted with a compound R.sup.2 --X to form an intermediate (R.sup.1 R.sup.2 CHOCH(CH.sub.3) CH.sub.2 COOH) which is then subjected to elimination to form an optically active secondary alcohol (R.sup.1 R.sup.2 CHOH) in good yield and purity.
摘要:
The present invention relates to chemical compounds and in particular to substituted dioxanones obtained from (R)-3-hydroxybutyric acid. This invention also relates to a method for the production of such dioxanones and to processes using such dioxanones as starting-materials.
摘要:
Chiral compounds of the formula I ##STR1## where: R.sup.1,R.sup.2,R.sup.3,R.sup.4 are hydrogen or aromatic, aliphatic or araliphatic radicals having 1 to 40 carbon atoms,R.sup.5,R.sup.6,R.sup.7,R.sup.8 are aromatic or aliphatic radicals having 1 to 20 carbon atoms,with the proviso that at least one of the radicals R.sup.1 to R.sup.8 contains a polymerizable group,are used as dopes in liquid crystals, in compositions for coating substrates and in the preparation of interference pigments which can be used in printing inks and surface coatings.
摘要:
Nonimmunosuppressant cyclosporin derivatives having cyclophilin-binding activity, for example, the compound, �MeIle!.sup.4 -ciclosporin, are useful in inhibiting HIV-1 replication in treating AIDS and AIDS related disorders.
摘要:
Novel substituted dioxanones obtained from (R)-3-hydroxybutyric acid, for example 2,2-dimethoxy-6-methyl-1,3-dioxan-4-one, a method for their preparation and processes using the dioxanones as starting material. The dioxanones can be used in particular as intermediates in the preparation of (S)-4-methyl-.beta.-butyrolactone.
摘要:
Cylosporins e.g. of formula II ##STR1## in which X is -MeBmt- or -dihydro-MeBmt- andY is -.alpha.Abu-, -Thr-, -Val- or -Nva-,wherein the residue at the 3-position, i.e. the residue Z in formula II, is an optically active, .alpha.-N-methylated .alpha.-amino acid residue of the (D)-configuration, possess pharmaceutical, in particular immunosuppressive, anti-inflammatory and anti-parasitic activity, Intermediate cyclosporin poly-anions having a de-protonated sarcosyl residue at the 3-position, e.g. polyanions of cyclosporins of formula II above wherein X and Y have the meanings given above and Z is -Sar-, in which the said residue Z is de-protonated, are also novel and part of the invention.
摘要:
.alpha.-Vinyl-.alpha.-aminocarboxylic acids of the general formula: ##STR1## where * indicates a center of asymmetry and R is hydrogen, deuterium, lower alkyl, allyl, benzyl, or benzyl substituted 1 to 3 times by alkyl, alkoxy, fluorine or chlorine and produced enantioselectively from L-methionine by a multistep process.
摘要:
TADDOL dendrimers are described. Their use as crosslinkers in polymerisation reactions and the use of Ti salts of polymer-bound TADDOL dendrimers as catalysts in enantioselective addition reactions is disclosed.
摘要:
2.2. 1,3-imidazolidine-4-ones having the General Formula: ##STR1## are obtained in a pure form especially by means of precipitation, in which production an optically active acid can be used at 0.5-0.8 eq. for the separation of racemates. The non-desired enantiomer can be racemized in an inert solvent and the cyclization to imidazolidinone can take place by means of the optically active acid, whereupon the separation of racemates takes place directly thereafter. 1,3-imidazolidine-4-ones are valuable educts for the preparation of branched or unbranched, proteinogenic or non-proteinogenic .alpha.-amino acids by means of diastereoselective alkylation and subsequent ring splitting.