Patent ES-8601206-A1 (ES)
Title: Aromatic substituted cyclic amidines.
IPC: C07C231/00
Filed: 1983-10-11
Abstract: The treatment comprises admin. of a cpd. of formula (I) or its salts, opt. in hydrated form. (R1-R3 are H, 1-6C alkyl or halogen, but they are not both H; one of R4 and R5 is H, alkyl or halogen and the other is NR6R7; R6 and R6 are H, 1-6C alkyl, 2-7C alkoxycarbonyl, 7-12C aryloxycarbonyl, 2-7C alkylcarbonyl, 7-12C arylcarbonyl or 3-7C hydroxyalkoxy carbonyl; or R6 and R7 form (CH2)p or (CH2)mCO; n is 1-3; p is 4 or 5; and m is 3 or 4). - Cpds. (I) are new when R4 is NR6R7 and the other terms are as defined above, except that R6 and R7 may also be 2-7C haloalkylcarbonyl. Cpds. (I) cause a decrease in aq. secretions in the intestines and so they are antidiarrhoeals without causing the complications caused with known agents such as opiates. Known cpds. (I) are described as parasiticides and hypotensives in U.S. 3769274. Dose is 0.01-100 mg/kg orally.  (0/0) EPAB- EP-111095 B Use of compounds of the formula (I) wherein R1, R2, and R3 each being the same or different are: (a) hydrogen; (b) alkyl of 1 to 6 carbon atoms, inclusive; or (c) halogen; with the proviso that R1 and R2 are not hydrogen at the same time; wherein one of R4 and R5 is hydrogen, alkyl of 1 to 6 carbon atoms, inclusive, or halogen and the other is of the formula -NR6R7 wherein R6 and R7, each being the same or different, are: (a) hydrogen; (b) alkyl of 1 to 6 carbon atoms, inclusive; (c) alkoxycarbonyl or 2 to 7 carbon atoms, inclusive; (d) aryloxycarbonyl of 6 to 12 carbon atoms inclusive wherein aryl includes pyridyl and may be substituted by halogen or nitro groups; (e) alkylcarbonyl of 2 to 7 carbon atoms, inclusive; (f) arylcarbonyl of 6 to 12 carbon atoms inclusive wherein aryl includes pyridyl and may be substituted by halogen or nitro groups; (g) hydroxyalkoxycarbonyl of 3 to 7 carbon atoms, inclusive; (h) wherein R6 and R7 are taken together to form (1) -(CH2)p-; wherein p is 4 or 5; (2) -(CH2)mCO-, wherein m is 3 or 4; wherein n is an integer of from 1 to 3, inclusive; or the pharmacologically acceptable salts; the compounds being either hydrated or unhydrated, for the manufacture of a medicament against diarrhea. - EP-111095 B Use of compounds of the formula (I) wherein R1, R2, and R3 each being the same or different are: (a) hydrogen; (b) alkyl of 1 to 6 carbon atoms, inclusive; or (c) halogen; with the proviso that R1 and R2 are not hydrogen at the same time; wherein one of R4 and R5 is hydrogen, alkyl of 1 to 6 carbon atoms, inclusive, or halogen and the other is of the formula -NR6R7 wherein R6 and R7, each being the same or different, are: (a) hydrogen; (b) alkyl of 1 to 6 carbon atoms, inclusive; (c) alkoxycarbonyl or 2 to 7 carbon atoms, inclusive; (d) aryloxycarbonyl of 6 to 12 carbon atoms inclusive wherein aryl includes pyridyl and may be substituted by halogen or nitro groups; (e) alkylcarbonyl of 2 to 7 carbon atoms, inclusive; (f) arylcarbonyl of 6 to 12 carbon atoms inclusive wherein aryl includes pyridyl and may be substituted by halogen or nitro groups; (g) hydroxyalkoxycarbonyl of 3 to 7 carbon atoms, inclusive; (h) wherein R6 and R7 are taken together to form (1) -(CH2)p-; wherein p is 4 or 5; (2) -(CH2)mCO-, wherein m is 3 or 4; wherein n is an integer of from 1 to 3, inclusive; or the pharmacologically acceptable salts; the compounds being either hydrated or unhydrated, for the manufacture of a medicament against diarrhea. (26pp) USAB- US4533739 A 2-(Aminophenyl) -1-azacycloalkanes of formula (I), opt. hydrated, and their pharmaceutically acceptable salts are new. R1-R5, the same or different, are H, 1-6C alkyl or halogen, R1 and R2 not being H at the same time. R6 and R7, the same or different, are H, 1-6C alkyl, 2-7C alkoxycarbonyl, 6-12C aryloxycarbonyl, 3-7C hydroxyalkoxycarbonyl or 2-7C haloalkylcarbonyl. - A typical cpd. is 2-((2-methyl 3-aminophenyl) amino) 1-pyrroline dihydrochloride.