Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1982-07-12
1985-10-29
Rotman, Alan L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546196, 546126, 546133, 514304, 514305, C07D31130, A61K 31445
Patent
active
045501157
ABSTRACT:
Novel 3-methylflavone-8-carboxylates having the structural formula (I): ##STR1## wherein Z is N-methylpiperidinyl, tropinyl or quinuclidinyl, or a group having the structural formula (II): ##STR2## in which n is 0 or 1, R is hydrogen or alkyl having from 1 to 4 carbon atoms, or phenyl, R.sub.1 is hydrogen or alkyl having from 1 to 4 carbon atoms, R.sub.2 is hydrogen or hydroxy, and further wherein R, R.sub.1 and R.sub.2 may together form, with the carbon atoms from which they depend, a cycloalkyl ring having from 4 to 6 carbon atoms, and R.sub.3 is hydrogen or alkyl having from 1 to 4 carbon atoms, with the proviso that R, R.sub.1, R.sub.2 and R.sub.3 cannot at the same time all be hydrogen, and the pharmaceutically acceptable salts thereof, are effective smooth muscle relaxants, calcium blockers, anaesthetics and anti-inflammatories.
REFERENCES:
patent: 2921070 (1960-01-01), daRe
The Merck Index, Ninth Edition, p. 533, (1976).
Nomura et al., Chem. Abstracts, vol. 88, No. 19, Abst. No. 130, 978c, May 8, 1978.
A. Cova, et al., "Flavoxate and 3-Methylflavone-8-carboxylic Acid", Arzneim.-Forsch., (Drug Res.), vol. 25, No. 11, pp. 1707-1709, (1975).
T. Argia, et al., "Gaschromatographic Determination of Flavoxate and Its Metabolites in Plasma and Urine After Oral Administration to Healthy Volunteers," Ann. Sankyo Res. Lab, vol. 26, pp. 94-105, (1974).
M. Windholz, et al., "#4012 Flavoxate," The Merck Index, p. 533, Merck & Co., Inc., Rahway, N.J., (1976).
A. Nomura et al., "General Pharmocological Studies on Flavoxate Hydrochloride (2-piperidinoethyl-3-methylflavone-8-carboxylate hydrochloride)", Oyo Yakuri, vol. 10, #3, pp. 365-381, (1975); see Chem. Abst., vol. 88, 103978c, (1978).
C. S. Weil, "Table for Convenient Calculation of Median Effective Dose (LD.sub.50 or ED.sub.50) and Instructions in Their Use," Biometrics, vol. 8, p. 249ff, (1952).
M. Ferrari and F. Carpenedo, "On the Mechanism of Action of Some Myolytic Agents on Depolarized Guinea Pig Taenia Coli," Arch. Int. Pharmocodyn. (France), vol. 174, pp. 223-232, (1968).
Casadio Silvano
Cazzulani Pietro
Graziani Gabriele
Nardi Dante
Pennini Renzo
Recordati S.A., Chemical & Pharmaceutical Company
Rotman Alan L.
LandOfFree
Certain piperidino-lower-alkylene esters of 3-methylflavone-8-ca does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Certain piperidino-lower-alkylene esters of 3-methylflavone-8-ca, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Certain piperidino-lower-alkylene esters of 3-methylflavone-8-ca will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-728748