[(2,3,9,9a-tetrahydro-3-oxo-9a-substituted-1h-fluoren-7-yl)...

Details [(2,3,9,9a-tetrahydro-3-oxo-9a-substituted-1h-fluoren-7-yl)... [(2,3,9,9a-tetrahydro-3-oxo-9a-substituted-1h-fluoren-7-yl)...

C - Chemistry, Metallurgy

07

C

167/233, 167/271

C07C 257/14 (2006.01) A61K 31/16 (2006.01) C07D 233/22 (2006.01)

Patent

CA 1284329

TITLE OF THE INVENTION [(2,3,9,9a-TETRAHYDRO-3-OXO-9a-SUBSTITUTED-lH- FLUOREN-7-YL)OXY]ETHANIMIDAMIDES AND [(2,3,9,9a- TETABYDRO-3-OXO-9a-SUBSTITUTED-lH-FLUOREN-7-YL)OXY]- ETHANIMIDIC ACID HYDRAZIDES, THEIR DERIVATIYES AND THEIR SALTS ABSTRACT OF THE DISCLOSURE The invention relates to novel [(2,3,9,9a-tetrahydro-3-oxo-9a-substituted-lH- fluoren-yl)oxy]ethanimidamldes and [(2,3,9,9a-tetra- hydro-3-oxo-9a-substituted-1H-fluoren-7-yl)oxy]- ethanimidic acid hydrazide, their derivatives and their salts. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections, various brain concussions and elevated intracranial pressure. The compounds of the present invention are characterized by the formula: Image wherein: R is lower alkyl, branched or unbranched, containing from 1 to 5 carbon atoms, aryl, halo substituted aryl, aralkyl, cycloalkyl containing from 3 to 6 nuclear carbon atoms, or cycloalkyl-lower alkyl containing from 4 to 7 total carbon atoms; R1 is NH2, NHR3, or NR3R4: R2 is NH2, NHR3; R3, R4 are each independently lower alkyl, branched or unbranched, containing from 1 to 5 carbon atoms, or amino, provided that R3 and R4 are not both amino; where R1 and R2 may be joined together via R3 2 nitrogen atoms and 3 carbon atoms; or wherein R3 and R4 may be joined together to from a 5-membered ring containing one nitrogen atom, and 4 carbon atoms; and x and y are halo or lower alkyl, or the pharmaceutically acceptable salts thereof.

518544

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