摘要:
Novel 4-(2'-pyridylamino)phenylacetic acid derivatives of the formula: ##STR1## wherein R.sub.1 is hydrogen, a halogen, a lower alkyl having 1 to 3 carbon atoms, or nitro, R.sub.2 is hydrogen, a halogen, or a lower alkyl having 1 to 3 carbon atoms, R.sub.3 is hydrogen, a halogen, or a lower alkyl having 1 to 3 carbon atoms, R.sub.4 is hydrogen or a lower alkyl having 1 to 3 carbon atoms, R.sub.5 is hydrogen or --CH.sub.2 CH.sub.2 OR.sub.6 wherein R.sub.6 is a lower alkyl having 2 or 3 carbon atoms and being substituted with 1 or 2 hydroxy groups, provided that R.sub.1 or R.sub.2 is not 4-halogen, or pharmaceutically acceptable salts thereof, and a process for the preparation thereof, pharmaceutical composition of said compounds, and a method of using said compounds as anti-inflammatory and analgesic agents. They have excellent anti-inflammatory and analgesic activities with an extremely weak ulcerogenicity in the gastrointestinal tract. Some of the compounds have superior inhibitory activity against chronic inflammation mediated by cellular immunity.
摘要:
Novel dibenz[b,f]oxepin and dibenzo[b,f]thiepin derivatives of the formula ##STR1## wherein X is an oxygen or sulfur atom, each of R.sub.1 and R.sub.2 is a hydrogen atom or a methyl group, and R.sub.3 is a hydrogen atom or a 2-(2-hydroxyethoxy)ethyl group; provided that when R.sub.1 is a hydrogen atom, the group ##STR2## is a group other than a 1-carboxyethyl group; and when X is a sulfur atom, both R.sub.1 and R.sub.2 are methyl groups;and pharmaceutically acceptable salts of said compounds in which R.sub.3 is a hydrogen atom. Compositions of said compounds, processes for the preparation of said compounds, and a method of using said compounds are also provided. These novel compounds have excellent anti-inflammatory, analgesic and antipyretic activities.
摘要:
Compounds of the formula: ##STR1## wherein R.sub.1 represents fluorine atom at the para position, chlorine atom at the para position, methyl group at the para position or trifluoromethyl group at the para or meta position; and R.sub.2 represents hydrogen atom, methyl group, ethyl group, 2-hydroxyethyl group or 3-hydroxypropyl group, provided that R.sub.2 represents ethyl group, 2-hydroxyethyl group or 3-hydroxypropyl group when R.sub.1 represents fluorine atom at the para position, methyl group at the para position or trifluoromethyl group at the para position, and a pharmaceutically acceptable salt therof, process for the preparation thereof, and pharmaceutical composition containing the same. The compounds and pharmaceutically acceptable salts thereof show excellent cytoprotective effect and useful for prophylaxis and treatment of peptic ulcer and inflammatory gastrointestinal diseases.
摘要:
Use of a compound of the formula: ##STR1## wherein R is hydrogen atom or ethyl group, or a pharmaceutically acceptable salt thereof for prophylaxis and/or treatment of peptic ulcer, and a method for prophylaxis and/or treatment of peptic ulcer disease which comprises administering an effective amount of the above-mentioned compound to warm blooded aninal, especially human. Said active compounds have excellent pharmacological activities such as inhibition of ulceration and inhibition of gastric secretion, and hence, are useful as an anti-peptic ulcer agent.
摘要:
2-(4-Ethyl-1-piperazinyl)-4-phenylquinoline and its pharmaceutically acceptable acid addition salts, which are useful as antidepressant agents in the treatment of depression or depressive state in mammals including humans, and processes for the preparation thereof.
摘要:
Hexahydro-.gamma.-carboline derivatives of the formula: ##SPC1##Wherein R.sub.1 is methyl or ethyl, and R.sub.2 is hydrogen, methyl or ethyl, with proviso that when R.sub.1 is ethyl, R.sub.2 is hydrogen, and their pharmaceutically acceptable acid addition salts, which exhibit excellent psychotropic effect, and a process for the preparation thereof.
摘要:
Novel acetic acid derivatives of the formula: ##STR1## wherein X is oxygen or sulfur; R.sub.1 is hydrogen or a lower alkyl; R.sub.2 is hydroxy, an alkoxy, an alkenyloxy, a cycloalkyloxy, an aryloxy, a substituted aryloxy, an aryl-lower alkoxy, a substituted aryl-lower alkoxy, an aryl-lower alkenyloxy, a substituted aryl-lower alkenyloxy, an .omega.-disubstituted amino-lower alkoxy, a lower alkoxycrbonyl-lower alkoxy, a lower alkoxy-lower alkoxy, a hydroxy-lower alkoxy-lower alkoxy, an acyl-lower alkoxy, or a group ##STR2## wherein R.sub.3 is hydrogen, hydroxy, a lower alkyl, an aryl-lower alkyl, a hydroxy-lower alkyl, or a carboxy-lower alkyl, R.sub.4 is hydrogen, a lower alkyl or a hydroxy-lower alkyl, or the R.sub.3 and R.sub.4 may combine together with the nitrogen atom to which they are joined to form a heterocyclic group; and the group --CH(R.sub.1)COR.sub.2 is joined to the carbon atom at 2- or 3-position, and pharmaceutically acceptable salts thereof, processes for their preparation, and pharmaceutical compositions containing these compounds. They have excellent anti-inflammatory, analgesic and antipyretic activities with weak ulcerogenicity in the gastrointestinal tract and toxicity.
摘要:
1-Substituted-4-(1,2-diphenylethyl)piperazine derivatives of the formula: ##STR1## wherein X is 2- or 3-hydroxy, 2-methoxy, 3-methyl, 3-alkoxy having 1 to 4 carbon atoms, or 2- or 3-alkanoyloxy having 2 to 5 carbon atoms; R is allyl, 3-hydroxyisoamyl, 3-methyl-2-butenyl, 3-methyl-3-butenyl, propyl, an unsubstituted monocycloalkyl having 5 to 8 carbon atoms, 2-chlorophenyl, or a phenyl substituted by hydroxy or methoxy; with proviso that when X is a substituent at position 2, R is cyclohexyl and when X is 3-methyl, R is 2-methoxyphenyl or an unsubstituted monocycloalkyl having 6 to 8 carbon atoms, and their pharmaceutically acceptable salts, and the preparation thereof, and analgesic or antitussive compositions containing the same as the essentially active ingredient.
摘要:
1,2-Diphenylethanolamine derivatives of the formula: ##SPC1##Wherein R.sub.1 and R.sub.2 are each hydrogen, a halogen, nitro, hydroxy, an alkyl or methoxy; R.sub.3 is a group of the formula: ##SPC2##Wherein R.sub.4, R.sub.5 and R.sub.6 are each hydrogen, a halogen or methoxy and n is an integer of 0 to 3, or a pyridyl; and Z is hydroxy or an acyloxy; with proviso that when R.sub.1 and/or R.sub.2 are hydroxy, Z is hydroxy, and their pharmaceutically acceptable salts, which have excellent analgesic and anti-tussive activities, and a process for the preparation thereof.
摘要:
1-Substituted-4-(1,2-diphenylethyl)piperazine derivatives of the formula: ##SPC1##Wherein X is hydroxy, methoxy, methyl or trifluoromethyl; and R is an unsubstituted monocycloalkyl group having 6 to 8 carbon atoms or 2-methoxyphenyl; provided that when X is hydroxy, R is cyclohexyl, and when X is trifluoromethyl, R is 2-methoxyphenyl,And their pharmaceutically acceptable salts, which have excellent analgesic, anti-tussive and anti-inflammatory activities, without undesirable side effect such as narcotic activity, and a process for the preparation thereof.