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.
Abstract:
Compounds, or pharmaceutically acceptable salts and esters thereof, of the formula:wherein A, B, D and E, R1, R2, and Z are specifically defined, having antibacterial activity, pharmaceutical compositions containing said compounds, treatment of bacterial infections with such compositions, and processes for the preparation of the compounds.
Abstract:
Compounds, or pharmaceutically acceptable salts and esters thereof, of formulae (I); (II); (III) or (IV) wherein A, B, D and E, R1, R2 and Z are specifically defined, having antibacterial activity, pharmaceutical compositions containing said compounds, treatment of antibacterial infections with such compositions, and processes for the preparation of the compounds.
Abstract:
2099609 9203136 PCTABS00010 Quinobenzoxazine, quinobenzothiazines, and pyrido-acridine derivatives of formula (I), as well as the pharmaceutically acceptable salts, esters, amides and prodrugs thereof are disclosed, wherein R1 is hydrogen or a carboxy-protecting group, R2 and R3 are substituents, A is oxygen, sulfur, or carbon, Z is a halogen or a nitrogen-containing group, X is hydrogen, halogen or alkyl, and W is hydrogen, alkyl, amino or halogen. The compounds have potent antineoplastic activity.
Abstract:
7-(3-A-amino-1-pyrrolidinyl) substituted naphthyridine and quinoline compounds wherein A is a solubilizing group selected from an amino acid residue or polypeptide chain.
Abstract:
Disclosed herein are fortimicin derivatives represented by the formula: wherein R is hydrogen, loweralkyl, aminoloweralkyl, diaminoloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, hydroxyloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N,N-diloweralkylaminohydroxyloweralkyl, loweracyl, aminoloweracyl, diaminoloweracyl, hydroxyloweracyl, N-loweralkylaminoloweracyl, N,N-diloweralkylaminoloweracyl, or aminohydroxyloweracyl, and the pharmaceutically acceptable salts thereof. Also disclosed are intermediates useful in the preparation of these compounds and compositions of these compounds together with a pharmaceutically acceptable carrier and/or diluent.