Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-04-06
2000-06-06
Jordan, Kimberly
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514381, 514394, 514397, A61K 3144, A61K 3141, A61K 31415
Patent
active
060719311
DESCRIPTION:
BRIEF SUMMARY
The enzyme cascade of the renin-angiotensin system (RAS) comprises a series of bio chemical sequences and, as is known, there are different approaches for opening up possibilities for the treatment of, for example, hypertension by regulatory intervention.
Angiotensinogen, .alpha.2-macroglycoprotein, is split by the renin enzyme into the deca peptide angiotensin I, which itself is biologically only very weakly active. The next step in the cascade is the removal of a further two amino acids by the action of the angiotensin-converting enzyme (ACE), bonded mainly in the endothelium, with formation of angiotensin II. This latter is held to be one of the strongest natural vasoconstrictors.
The vasoconstrictive effects of angiotensin II are produced by its action on the non-striated muscle cells, the stimulation of the formation of the adrenergenic hormones epinephrine and norepinephrine as well as by the increase of the activity of the sympathetic nervous system as a result of the formation of norepinephrine. Angi otensin II also has an influence on the electrolytic balance, produces e.g. antinatriuretic and anitdiurectic effects in the kidney and accordingly promotes the release of, on the one hand, the vasopressin peptide from the pituitary gland and, on the other hand, of aldosterone from the adrenal glomerulosa. These influences all play an important part in the regulation of blood pressure.
Angiotensin II interacts with specific receptors on the surface of the target cell. It has been possible to identify receptor subtypes which are termed e.g. AT.sub.1 - and AT.sub.2 -receptors. Great efforts have been made lately to identify substances that bind to AT.sub.1 -receptors. Such active ingredients are often termed angiotensin II antagonists. Because of the inhibition of the AT.sub.1 -receptor such antagonists can be used e.g. as antihypertensives or for the treatment of congestive heart failure.
Angiotensin II antagonists are understood to mean those active ingredients which bind to the AT.sub.1 -receptor subtype. These include compounds having different structural features. Compounds to be mentioned are, for example, those cited in the compound claims of EP-443983, the subject matter of which is herewith incorporated by reference in this application.
A compound to be highlighted is (S)-N-(1-carboxy-2-methyl-prop-1-yl)-N-pentanoyl-N-[2'(1H-tetrazol-5-yl)bi phenyl-4-yl-methy]amine (hereinafter termed valsartan) of formula ##STR2## cited in European patent application having the publication no. EP-443983, Example 16, or a salt thereof, preferably a pharmaceutically acceptable salt thereof.
Furthermore, the compounds cited in the compound claims of European patent application having the publication no. EP-253310 are incorporated by reference in this application.
A compound to be highlighted is that of the following formula ##STR3## and the pharmaceutically acceptable salts thereof.
Furthermore, the compounds cited in the compound claims of European patent application having the publication no. EP-403159 are incorporated by reference in this application.
A compound to be highlighted is that of the following formula ##STR4## and the pharmaceutically acceptable salts thereof.
Furthermore, the compounds cited in the compound claims of PCT patent application WO 91/14679 are, with reference to this literature, herewith also included in this application.
A compound to be highlighted is that of the following formula ##STR5## and the pharmaceutically acceptable salts thereof.
Furthermore, the compounds cited in the compound claims of European patent application having the publication no. EP-420 237 are incorporated by reference in this application.
A compound to be highlighted is that of the following formula ##STR6## and the pharmaceutically acceptable salts thereof.
Furthermore, the compounds cited in the compound claims of European patent application having the publication no. EP-502314 are incorporated by reference in this application.
A compound to be highlighted is that of the following formula ##STR7## and the phar
REFERENCES:
Takishita et al., Hypertension, vol. 24, No. 4, 1994, pp. 445-450.
Huland et al., Urol Int, vol. 36, No. 1, 1981, pp. 15-22.
Huland et al., Transplantation, vol. 36, No. 2, 1983, pp. 139-142.
Dalaney et al., Anesthesiology, vol. 51, No. 3, 1979, p. s73.
Ferraro Gregory D.
Jordan Kimberly
Novartis AG
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