Abstract:
1-(Disubstituted-amino)pyrazole compounds are provided herein of the formula: WHEREIN EACH OF R1 and R2 stands for lower alkyl or R1 and R2, taken together with the adjacent N-atom form morpholino, piperidino, pyrrolidino, N-methylpiperazino, N-benzylpiperazino and N-phenylpiperazino, R''s, which are the same or different from each other, stand for hydrogen, alkyl having one to ten carbon atoms, phenyl, naphthyl, phenyl or naphthyl substituted by halogen or lower alkyl, respectively, and R3 stands for hydrogen, lower alkyl, N,N-di-loweralkylaminoethyl, N-morpholinomethyl, Npiperidinomethyl, N-pyrrolidinomethyl, N-methylpiperazinomethyl, N-benzylpiperazinomethyl and N-phenylpiperazinomethyl. The above compounds as well as the pharmaceutically acceptable salts thereof are useful as analgesics, antipyretics and mild muscle relaxants.
Abstract:
5-AMINO-4-AROLYPYRAZOLE COMPOUNDS, ALSO SUBSTITUTED IN THE 1-AND 3-POSITION BY LOWER ALKYL GROUPS, ACID-ADDITION SALTS THEREOF, AND THEIR PRODUCTION BY (1) REACTING A 4AROYL-5-HALOPYRAZOLE WITH AMMONIA OR METHYLAMINE; (2) HYDROLYZING A 4-AROYL-5-ARYLAMIDOPYRAZOLE; OR (3) REACTING A 5-AMINO-4-CYANOPYRAZOLE WITH AN ARYL ORGANOMETALLIC COMPOUND. THE COMPOUNDS OF THE INVENTION ARE USEFUL AS PHARMACOLOGICAL AGENTS THAT EXERT A DEPRESSANT EFFECT UPON THE CENTRAL NERVOUS SYSTEM AND AS CHEMICAL INTERMEDIATES.
Abstract:
Acrylamides of N-containing heterocyclic moieties that optionally carry a further hetero atom adjacent to the said N and/or methyl substituent(s) on said hetero ring and at least one chlorine atom adjacent to the double bond of the acrylic moiety have been found to have anti-inflammatory properties at reasonably low dosage levels.
Abstract:
New amino derivatives of pyrazolo(3,4-b)pyridine-5-ketones as well as their salts are useful as central nervous system depressants. These compounds also increase the intracellular concentration of adenosine-3'',5''-cyclic monophosphate.
Abstract:
A NOVEL SERIES OF N''-(4-FORMYL)-5-AMIDO-PYRAZOLES WHICH ARE USEFUL AS INTERMEDIATS IN PREPARING N''-(4(HYDROXYMETHYL)-5-PYRAZOLYL)AMIDINES, THE AMIDINES ARE EFFECTIVE ANTI-FLAMMATORY AGENTS.
Abstract:
5-Amino-4-cyano-3-(5-nitro-2-furyl)-pyrazoles, substituted in 1position of the pyrazole moiety by alkyl, hydroxyalkyl or carbalkoxy, and pharmaceutically acceptable acid addition salts thereof, have antimicrobial properties; compositions containing these compounds and methods for the treatment of microbial infections and protecting organic material against microbial attack; a typical embodiment is 5-amino-4-cyano-1-methyl-3-(5nitro-2-furyl)-pyrazole.