Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-02-25
1996-05-21
Geist, Gary
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514680, 546285, 568326, C07J 6300, A61K 31565, A61K 3158
Patent
active
055190278
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/EP91/02495 filed Dec. 21, 1991, published as WO/92/11279.
This invention relates to compounds of general formula I ##STR2## in which
X stands for an oxygen atom, the hydroxyimino grouping >N.about.OH or two hydrogen atoms,
R.sup.1 stands for a hydrogen atom or a methyl group,
R.sup.2 stands for an hydroxy group, a C.sub.1 -C.sub.10 alkoxy or C.sub.1 -C.sub.10 acyloxy group,
R.sup.3 stands for a hydrogen atom, the grouping --(CH.sub.2).sub.n CH.sub.2 Z, in which n is 0, 1, 2, 3, 4 or 5, Z means a hydrogen atom, the cyano group or the radical --OR.sup.5 with R.sup.5 =H, C.sub.1 -C.sub.10 alkyl or C.sub.1 -C.sub.10 acyl, the grouping --(CH.sub.2).sub.m C.tbd.C--Y, in which m means 0, 1 or 2 and Y means a hydrogen, fluorine, chlorine, bromine or iodine atom, a methyl, C.sub.1 -C.sub.10 hydroxy alkyl, methyl, C.sub.1 -C.sub.10 alkoxyalkyl, methyl, C.sub.1 -C.sub.10 acyloxyalkyl radical, the grouping --(CH.sub.2).sub.p --CH.dbd.CH--(CH.sub.2).sub.k CH.sub.2 R.sup.6, in which p means 0 or 1 and k means 0, 1 or 2 and R.sup.6 means a hydrogen atom, a hydroxy group, a C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 acyloxy radical,
or else R.sup.2 and R.sup.3 together stand for a radical of the formula ##STR3## in which x=1 or 2
R.sup.4 stands for a hydrogen atom, a cyano group, a chlorine, fluorine, bromine, iodine atom, for a trialkylsilyl group, trialkylstannyl group, for a straight-chain or branched, saturated or unsaturated C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 acyl or alkoxyalkyl radical, for an amino group ##STR4## in which R.sup.7 and R.sup.8, independently of one another, mean a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, or for a corresponding amine oxide ##STR5## or stands for the groupings --OR.sup.9 or --S(O).sub.i R.sup.9 with i=0, 1 or 2, in which R.sup.9 means a hydrogen atom, a methyl, ethyl, propyl, isopropyl, methoxyphenyl, allyl or a 2-dimethylaminoethyl group, or for a heteroaryl radical of the formula I.alpha. ##STR6## in which A symbolizes a nitrogen, oxygen or sulfur atom, --B--D--E-- the element sequence --C--C--C--, --N--C--C-- or --C--N--C-- and R.sup.10 a hydrogen atom, a cyano group, a chlorine, fluorine, bromine or iodine atom, a trialkylsilyl, trialkylstannyl group, a straight-chain or branched, saturated or unsaturated C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -acyl or alkoxyalkyl radical, for an amino group ##STR7## in which R.sup.7 and R.sup.8 independently of one another, mean a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, or a corresponding amine oxide ##STR8## or the grouping --OR.sup.9 or --S (O).sub.i R.sup.9 with i=0, 1 or 2, in which R.sup.9 means a hydrogen atom, a methyl, ethyl, propyl, isopropyl, methoxyphenyl, allyl or a 2-dimethylaminoethyl group,
or for a heteroaryl radical of formula I.beta. ##STR9## in which A means a nitrogen atom and --B--D--E-- means the element sequence --C--C--C--, --N--C--C--, --C--N--C-- or --C--C--N-- and R.sup. has the meaning already indicated,
or for a phenyl radical of formula I.gamma. ##STR10##
in which R.sup.10 has the meaning already indicated,
R.sup.11 stands for a fluorine, chlorine or bromine atom, and then R.sup.12 and R.sup.13 together mean an additional bond or
R.sup.11 stands for a straight-chain or branched-chain C.sub.1 -C.sub.4 -alkyl radical or a hydrogen atom, and then R.sup.12 and R.sup.13 each mean a hydrogen atom or together mean an additional bond,
as well as their pharmacologically compatible addition salts with acids, process for their production, pharmaceutical preparations containing these compounds, their use for the production of pharmaceutical agents as well as the new intermediate products necessary for this purpose.
The invention relates especially to compounds, in which X stands for an oxygen atom.
The alkoxy, acyloxy, alkyl, acyl as well as hydroxyalkyl groups contained in R.sup.2, R.sup.3, R.sup.5 and Y of general formula I each are to contain 1 to 10 carbon atoms and the alkoxylalkyl or acyloxyalkyl groups in Y, 2 to 10 carbon atoms. In this case, the methoxy, etho
REFERENCES:
patent: 4536401 (1985-08-01), Neef et al.
patent: 4609651 (1986-09-01), Rohde et al.
CA 120: 323998 (Abstract of Chinese patent CN 92-101450 Jan. 31, 1992) Faming.
CA 115: 114882 (Abstract of East German patent DD 289542 May 2 1991) Kasch, et al.
Chwalisz Krzysztof
Cleve Arwed
Elger Walter
Ottow Eckhard
Schneider Martin
Geist Gary
Scalzo Catherine
Schering Aktiengesellschaft
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