Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1999-04-09
2000-12-26
Ramsuer, Robert W.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
544238, 544295, 544328, 544333, 544405, A61K 31506, A61P 900
Patent
active
061660272
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to new heterocyclylmethyl-substituted pyrazole derivatives, processes for their preparation and their use as medicaments, in particular as medicaments for treatment of cardiovascular diseases.
It is already known that 1-benzyl-3-(substituted heteroaryl)-fused pyrazole derivatives inhibit stimulated platelet aggregation in vitro (cf. EP 667 345 A1).
The present invention relates to new heterocyclylmethyl-substituted pyrazole derivatives, in the embodiment designated I (roman one), of the general formula (I-I) ##STR1## in which R.sup.1 represents a 5-membered aromatic heterocyclic ring having one heteroatom from the series consisting of S, N and/or O, or represents phenyl, which are optionally substituted up to 3 times in an identical or different manner by formyl, carboxyl, mercaptyl, hydroxyl, straight-chain or branched acyl, alkylthio, alkoxy or alkoxycarbonyl having in each case up to 6 carbon atoms, nitro, cyano, halogen, phenyl or straight-chain or branched alkyl having up to 6 carbon atoms, which in its turn can be substituted by hydroxyl, amino, carboxyl, straight-chain or branched acyl, alkoxy, alkoxycarbonyl or acylamino having in each case up to 5 carbon atoms or by a radical of the formula --OR.sup.4, wherein or a group of the formula --SiR.sup.5 R.sup.6 R.sup.7, wherein having 6 to 10 carbon atoms or alkyl having up to 6 carbon atoms, ##STR2## wherein b1 and b1' are identical or different and denote the number 0, 1, 2 or 3, carbon atoms, straight-chain or branched alkyl having up to 10 carbon atoms, which is optionally substituted by cycloalkyl having 3 to 8 carbon atoms or by aryl having 6 to 10 carbon atoms, which in its turn can be substituted by halogen, or halogen, or 7-membered saturated heterocyclic ring, which can optionally contain a further oxygen atom or a radical --NR.sup.11, wherein carbon atoms or a radical of the formula ##STR3## or denotes benzyl or phenyl, wherein the ring systems are optionally substituted by halogen, heterocyclic ring having one heteroatom from the series consisting of S, N and/or O, or a phenyl ring, which are optionally substituted up to 3 times in an identical or different manner by formyl, carboxyl, hydroxyl, amino, straight-chain or branched acyl, alkoxy or alkoxycarbonyl having in each case up to 6 carbon atoms, nitro, cyano, azido, halogen, phenyl or straight-chain or branched alkyl having up to 6 carbon atoms, wherein the alkyl in its turn can be substituted by hydroxyl, amino, carboxyl, straight-chain or branched acyl, alkoxy or alkoxycarbonyl having in each case up to 5 carbon atoms, --S(O).sub.cl' NR.sup.9' R.sup.10', wherein c.sub.1',R.sup.9' and R.sup.10' have the abovementioned meaning of c.sub.1, R.sup.9 and R.sup.10 and are identical to or different from these, ring having up to 3 heteroatoms from the series consisting of S, N and/or O, which is optionally substituted up to 3 times in an identical or different manner by mercaptyl, hydroxyl, formyl, carboxyl, straight-chain or branched acyl, alkylthio, alkyloxyacyl, alkoxy or alkoxycarbonyl having in each case up to 6 carbon atoms, nitro, cyano, trifluoromethyl, azido, halogen, phenyl or straight-chain or branched alkyl having up to 6 carbon atoms, which in its turn can be substituted by hydroxyl, carboxyl, straight-chain or branched acyl, alkoxy or alkoxycarbonyl having in each case up to 5 carbon atoms, R.sup.13, wherein phenyl, benzyl or straight-chain or branched alkyl or acyl having in each case up to 5 carbon atoms,
The compounds of the general formula (I-I) according to the invention can also be present in the form of their salts. Salts with organic or inorganic bases or acids may be mentioned in general here.
In the context of embodiment I of the present invention, physiologically acceptable salts are preferred. Physiologically acceptable salts of the heterocyclylmethyl-substituted pyrazole derivatives can be salts of the substances according to the invention with mineral acids, carboxylic acids or sulphonic acids. Particularly preferred salts are, for examp
REFERENCES:
Chemical Abstracts, vol. 125, No. 3, Jul. 15, 1996, Abstract No. 3363m, S. Guo, et al., "Preparation . . . inhibitors" & CN 1 112 926 (Yongxin Pharmaceutical Industry Co., Ltd. Peop. Rep. China) Dec. 6, 1995.
S.-M. Yu et al., "Inhibition of Platelet . . . Vivo", vol. 87, No. 9, May 1, 1996, pp. 3758-3767.
C.-C. Wu, et al. "YC-1 inhibited . . . cyclase", British Journal of Pharmacology, vol. 116, No.13, 1995, pp. 1973-1978.
C.R. Self, et al., "Romazarit: A Potential Disease . . . Drug" Journal of Medicinal Chemistry, vol. 34, No. 2, 1991, Washington, U.S. pp. 772-777.
G. Capozzi, et al., "Neighbouring Group . . . 3-benzamidopropyne", Tetrahedron Letters, vol. 22, No. 34, 1981 pp. 3325-3328.
Arlt Dieter
Dembowsky Klaus
Feurer Achim
Furstner Chantal
Hutter Joachim
Bayer Aktiengesellschaft
Ramsuer Robert W.
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