USE OF THE COMPOUND 9-(P-(N-METHYLACETAMIDO)ANILINO)-7-METHYL-1H-IMIDAZO(4,5-F)QUINOLINE HYDROCHLORIDE (I) AS ANTITUMOR AGENT

Abstract: The use of 9-[p-(N-methylacetamido)anilino]-7-methyl-1H-imidazo[4,5-f]quinoline hydrochloride for preparing parenterally injectable solutions for treating malignant tumors in a host afflicted therewith is described.

Description: Description Use of the compound 9-[p-(N-methylacetamido)-anilino]- 7-methyl-1H-imidazo[4,5-f]quinoline hydrochloride (I) as antitumor agent. This invention is concerned with the use of the compound 9- EP- (N-methylacetamido ) -anilino -7-methyl-IH-imidazo [4,5-f]quinoline hydrochloride (I) for preparing parenterally injectable solutions for treating malignant tumors in a host afflicted therewith. That compound is described in U.S. patent No. 3,878,206 wherein its utility as an anti-bacterial agent is disclosed. It has now been found that (I) possesses noteworthy antitumor activity. Such activity is evinced in those systems currently regarded and acknowledged by those skilled in the art to unearth candidates for successful use as antitumor agents and to be reasonable predictors of such use in a variety of species. Such systems comprise murine tumors such as P-388 lymphocytic leukemia, B-16 melanocarcinoma and L-1210 lymphoid leukemia (Cancer Clinical Trials, 1979; 2:195-216; Recent Results in Cancer Research, Vol. 70.) It has been discovered that when (I) is administered parenterally as a solution in isotonic saline to a host harboring one of the aforecited tumors, a salutary effect is elicited. The results are depicted in the following table: Antitumor Activitya L-1210 P-388 B-16 Limphoid Leukemiab Lymphocytic Leukemiab Melanocarcinomab Dosec ILSd T/Ce T-Cf Dosec ILSd T/Ce T-Cf Dosec ILSd T/Ce T-Cf 50 43 143 -2.3 50 46 146 -3.0 50 49 149 -0.7 12.5 25 125 1.9 25 43 143 -1.0 25 98 198 -0.4 12.5 34 134 -0.8 50 84 184 -2.3 6.25 26 126 -0.8 a. Protocols and tumor systems described in Geran, et al. Cancer Chemother. Rep. Part 3. 3 (No. 2) 1 (1972). b. Intraperitoneal tumor implantation, intraperitoneal QD-1 treatment schedule. c. In mg/kg/injection ih isotonic saline. d. Increased life span = T/C - 100 in percent. e. T/C = ratio (expressed as %) of the mean survival time of the treated group divided by the mean survival time of the control group. f. T-C = average weight change of test group minus average weight change of control animals in grams. The values such as ILS and T/C depicted in the foregoing table demonstrate the efficacy of (I)in the various antitunior systems.

Claims: Patent claim The use of the compound 9-[p-(N-methylacetamido)anilino]- 7-methyl-1H-imidazo[4,5-f]quinoline hydrochloride for preparing parenterally injectable solutions for treating malignant tumors in a host afflicted therewith.

Inventors: EBETINO, FRANK F.
Applicants: NORWICH EATON PHARMACEUTICALS, INC.
Application year: 1982
Main classification: A61K31
IPC codes: A61K31