Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-12-09
2000-04-25
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514218, 5142358, 5142375, 514252, 514253, 514256, 514318, 514323, 514327, 514329, 514330, 514352, 514356, 514357, 514365, 514374, 514381, 514417, 514423, 514427, 514447, 514518, 514532, 514534, 514535, 514538, 514539, 514540, 514543, 514544, 514595, 514602, 514603, 514604, 514616, 514617, 514618, 514619, 514620, 514622, 540575, 544121, 544165, 544335, 544357, 544360, 544373, 544379, 544382, 544388, 544391, 544400, 546194, 546200, 546221, 546223, 546226, 546298, 546309, 546322, 546336, 548204, 548238, 548253
Patent
active
060544570
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This invention relates to new benzamide derivatives and pharmaceutically acceptable salts thereof which are useful as a medicament.
BACKGROUND ART
Some benzamide derivatives have been known as vasopressin antagonist, for example, in PCT International Publication Nos. WO 91/05549 and WO 95/29152, and EP Application Publication No. 0620216.
DISCLOSURE OF INVENTION
This invention relates to new benzamide derivatives and pharmaceutically acceptable salts thereof.
More particularly, it relates to new benzamide derivatives and pharmaceutically acceptable salts thereof which possess activities as vasopressin antagonistic activity, vasodilating activity, hypotensive activity, activity for inhibiting saccharide release in liver, activity for inhibiting growth of mesangium cells, water diuretic activity, platelet agglutination inhibitory activity, oxytocin antagonistic activity and the like, to a pharmaceutical composition comprising the same and to a method for the treatment and/or prevention of hypertension, heart failure, renal insufficiency, edema, ascites, vasopressin parasecretion syndrome, hepatocirrhosis, hyponatremia, hypokalemia, diabetic, circulation disorder, cerebrovascular disease (e.g. cerebral edema, cerebral infarction, etc.), Meniere's syndrome (e.g. Meniere's disease, etc.), motion sickness and the like in human beings or animals.
One object of this invention is to provide new and useful benzamide derivative which possess aforesaid activities.
Another object of this invention is to provide processes for the preparation of said benzamide derivatives and salts thereof.
A further object of this invention is to provide a pharmaceutical composition comprising, as an active ingredient, said benzamide derivatives and pharmaceutically acceptable salts thereof.
Still further object of this invention is to provide a therapeutical method for the treatment and/or prevention of aforesaid diseases in human beings or animals, using said benzamide derivatives and pharmaceutically acceptable salts thereof.
The object benzamide derivatives of this invention are new and can be represented by the following general formula (I): ##STR3## wherein: R.sup.1 is aryl, cyclo(lower)alkyl or a heterocyclic group, each of which may be substituted with substituent(s) selected from the group consisting of halogen; hydroxy; nitro; amino; acyl; substituted acyl; acyl(lower)alkylsulfinyl; acyl(lower)alkylsulfonyl; acyloxy; lower alkylamino(lower) alkylcarbamoyloxy; aryl; cyano; a heterocyclic group; lower alkenyl optionally substituted with acyl, substituted acyl, aryl or acyl-substituted aryl; lower alkynyl optionally substituted with amino, acylamino or substituted acylamino; lower alkyl optionally substituted with halogen, amino, lower alkylamino, acylamino, substituted acylamino, hydroxy, acyloxy, acyl(lower)alkanoyloxy, acyl, substituted acyl, acyl(lower)alkoxyimino, aryl or acyl-substituted aryl; lower alkylthio optionally substituted with acyl or substituted acyl; alkoxy optionally substituted with aryl, substituted aryl, hydroxy, acyloxy, amino, lower alkylamino, protected amino, a heterocyclic group, acyl-substituted pyridyl, substituted acyl-substituted pyridyl, halogen, acyl(lower)alkylamino, N-protected-acyl(lower)alkylamino, N-acyl(lower)alkyl-N-lower alkylamino, acyl, substituted acyl, acylamino, substituted acylamino, lower alkylhydrazinocarbonylamino, hydroxyimino, acyl(lower)alkoxyimino, substituted acyl(lower)alkoxyimino, acyl(lower)alkoxy, guanidino or N-protected guanidino; and lower alkenyloxy optionally substituted with acyl or substituted acyl; or acyl; or cyclo(lower)alkyl; alkyl optionally substituted with hydroxy or lower alkoxy; lower alkoxy optionally substituted with aryl, amino, protected amino, acyl, hydroxy, cyano or lower alkylthio; nitro; amino; acyl; substituted acyl; or cyclo(lower)alkyloxy; alkylamino; acyloxy; amino(lower)alkylamino; N-protected amino(lower)alkylamino; lower alkoxy optionally substituted with hydroxy, aryl, substituted aryl, acyl, substituted acyl, amino,
REFERENCES:
patent: 5521170 (1996-05-01), Setoi et al.
Plescia et al., A New Pyrazolo[4,3-c][1,5]benzodiazocine Derivative, Bollettino Chimico Farmaceutico, vol. 122, No. 4, pp. 190-195, Apr. 1983.
CAS Online Printout for WO 95/29152, Nov. 1995.
Imagawa et al., Studies on Cyclic-Oligo-Amides (III) Syntheses of 1,9,17-Triaza[2.2.2]orthocyclophane-2,10,18-trione and N-Methyl Derivative, Memoirs of Osaka Kyoiku University, Series III, vol. 36, No. 2, pp. 123-128, Dec. 1987.
CAS Online Printout for DE 35 23 705, Jan. 1987.
Hoorfar et al., Conformational Behaviour of Medium-sized Rings. Part 11. Dianthranilides and Trianthranilides, Journal of the Chemical Society, Perkin Transactions I, vol. 8, pp. 1649-1699, Aug. 1982.
Elhadi et al., Conformational Behaviour of Medium-sized Rings. Part 15. 1,9,17-Triaza[2.2.2]metacyclophane-2,10,18-trione Derivatives, Journal of the Chemical Society, Perkin Transactions I, vol. 8, pp. 1727-1732, Aug. 1982.
Hoorfar et al., Conformational Behaviour of Medium-sized Rings. Part 14. Tetraanthranilides, Journal of the Chemical Society, Perkin Transactions I, vol. 8, pp. 1721-1726, Aug. 1982.
Edge et al., Conformational Behaviour of Medium-sized Rings. Part 12. Tri-3-methyltrianthranilide, Journal of the Chemical Society, Perkin Transactions I, vol. 8, pp. 1701-1714, Aug. 1982.
Ollis et al., Synthese und Konformationsverhalten von N,N',N"-Trimethyltrianthranilid, Angewandte Chemie, vol. 87, No. 5, pp. 169-170, Mar. 1975.
Ohkawa Takehiko
Sato Kentaro
Sawada Hitoshi
Setoi Hiroyuki
Tanaka Hirokazu
Coleman Brenda
Fujisawa Pharmaceutical Co. Ltd.
Shah Mukund J.
LandOfFree
Benzamide derivatives and their use as vasopressin antagonists does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Benzamide derivatives and their use as vasopressin antagonists, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Benzamide derivatives and their use as vasopressin antagonists will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-993574