Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-10-05
2000-12-19
Powers, Fiona T.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514406, 5483681, 5483657, A61K 314155, A61K 31416, C07D40504
Patent
active
061628190
ABSTRACT:
The present invention relates to pyrazole derivatives of the formula I, their preparation and their use in pharmaceuticals: ##STR1## in which X, R.sup.1, R.sup.1a, R.sup.2, R.sup.3, R.sup.4 and n are as defined in the claims, which are useful pharmaceutically active compounds for the therapy and prophylaxis of illnesses, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate "cGMP" and are generally suitable for the therapy and prophylaxis of illnesses which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula 1, to their use for the therapy and prophylaxis of the abovementioned illnesses and for preparing pharmaceuticals for this purpose, and also to pharmaceutical preparations which comprise the compounds of the formula I.
REFERENCES:
patent: 4072498 (1978-02-01), Moon et al.
patent: 4325962 (1982-04-01), Rainer
patent: 5434178 (1995-07-01), Talley et al.
patent: 5574168 (1996-11-01), Kuo et al.
Gnichtel et al., Chemical Abstracts, 111;57617, 1989.
Yoshina et al., Chemical Abstracts, 88:105211, 1978.
Shimanskaya et al., Chemical Abstracts, 69:112873, 1968.
Huang et al., Chemical Abstracts, 98:107203, 1993.
S. Guo, et al., "Preparation of condensed 1-benzyl-3-arylpyrazole derivatives as blood platelet aggregation inhibitors," Chemical Abstracts, Columbus, Ohio, US, (1996) vol. 125, No. 3, 125: 33633m, p. 903.
S. Yoshina et al., "Pyrazole derivatives," Chemical Abstracts, Columbus, Ohio, US, (1976) vol. 84, 84:180207p, p. 575.
S. M. Yu, et al., "Inhibition of Platelet Function by A02131-1, a Novel Inhibitor of cGMP-Specific Phosphodiesterase, In Vitro and In Vivo," Blood, (1996) vol. 87, No. 9, pp 3758-3767.
D. L. Vesely, "B complex vitamins activate rat guanylate cyclase and increase cyclic GMP levels," European Journal of Clinical Investigation, (1985) vol. 15, pp. 258-262.
D. L. Vesely, "Phencyclidine Stimulates Guanylate Cyclase Activity," Biochemical and Biophysical Research Communications, (1979) vol. 88, No. 4, pp. 1244-1248.
L. J. Ignarro, "Regulation of Cytosolic Guanylyl Cyclase by Porphyrins and Metalloporphyrins," Advances in Pharmacology, (1994) vol. 26, pp. 35-65.
D. J. Pettibone, et al., "A Structurally Novel Stimulator of Guanylate Cyclase With Long-Lasting Hypotensive Activity In The Dog," European Journal of Pharmacology, (1985) vol. 116, pp. 307-312.
S. M. Yu, et al., "Vasorelaxant effect of isoliquiritigenin, a novel soluble guanylate cyclase activator, in rat aorta," British Journal of Pharmacology, (1995) vol. 114, pp. 1587-1594.
F. N. Ko, et al., "YC-1, a Novel Activator of Platelet Guanylate Cyclase," Blood, (1994) vol. 84, No. 12, pp. 4226-4233.
S. M. Yu, et al., "Mechanism of anti-proliferation caused by YC-1, an indazole derviative, in cultured rat A10 vascular smooth-muscle cells," Biochem. J., (1995) vol. 306, pp. 787-792.
C. C. Wu, et al., "YC-1 inhibited human platelet aggregation through NO-independent activation of soluble guanylate cyclase," British Journal of Pharmacology, (1995) vol. 116, pp. 1973-1978.
Schindler Ursula
Schonafinger Karl
Strobel Hartmut
Aventis Pharma Deutschland GmbH
Powers Fiona T.
LandOfFree
Pyrazole derivatives, their preparation and their use in pharmac does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Pyrazole derivatives, their preparation and their use in pharmac, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Pyrazole derivatives, their preparation and their use in pharmac will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-271629