Abstract:
A NEW SERIES OF PIPERDINE DERIVATIVES HAS BEEN DISCOVERED; THEY ARE COMPOUNDS CARRYING, IN THE 4-POSITION OF THE PIPERIDINE RING, A SUBSTITUTED ANILINO GROUP AND IN THE 1-POSITION, A P-FLUOROPHENYL RING SEPARATED FROM THE PIPERIDINE RING BY A CARBON CHAIN OF 4. THESE NEW COMPOUNDS AND THEIR NON-TOXIC ACID ADDITION SALTS ARE HIGHLY EFFECTIVE ANALGEICES OF LOW TOXICITY.
Abstract:
A new series of piperidine derivatives has been discovered; they are the N-(3-(p-fluorophenoxy)propyl)piperidines carrying in the 4-position of the piperidine ring a substituted anilino group. These new compounds and their non-toxic acid addition salts are highly effective analgesics of low toxicity.
Abstract:
Covers sulfonyl derivatives of erythromycin A, B and C falling within the following structural formula:
WHERE R is selected from the group consisting of amino, monoalkyl amino, dialkyl amino, alkoxy, morpholino, substituted morpholino, piperazino, substituted piperazino, piperidino, substituted piperidino, alkylthio, alkylsulfonyl, arylthio, substituted arylthio, arylsulfonyl, substituted arylsulfonyl, thiamorpholino, aziridino, substituted aziridino, benzylthio, substituted benzylthio, thiamorpholinosulfone, substituted thiamorpholinosulfone, benzylsulfinyl, substituted benzylsulfinyl, arylsulfinyl, substituted arylsulfinyl, benzylsulfonyl, substituted benzylsulfonyl, cyanoalkyl, halocyanoalkyl, haloalkanoate, dialkanoate, ketaolkyl, ketoalkanoate, benzylamino, substituted benzylamino, benzoxy, substituted benzoxy, phenoxy, substituted phenoxy, benzycyano, and substituted benzylcyano; R1 is hydrogen or mmethyl, R2 is hydrogen or loweralkanoyl, R3 is hydrogen or hydroxy, and R4 is selected from the group consisting of loweralkyl, cycloalkyl, subtituted cycloalkyl, aryl, substituted aryl, benzyl, and substituted benzyl. The present sulfonyl derivatives of erythromycin A, B and C are useful as antibiotics.