Abstract:
Covers the esters of gamma -glutamyl amide of dopamine selected from the group consisting of
where R is a C1-C20 alkyl radical, and a pharmaceutically acceptable acid addition salt thereof. Also covers the use of said esters of gamma -glutamyl amide of dopamine to increase renal blood flow by administering said amide to warm-blooded mammals by clinically acceptable routes of administration such as oral, parenteral, rectal, etc.
Abstract:
Covers a 4''''-deoxy-4''''-oxoerythromycin compounds and derivatives thereof which are useful as antibiotics having a formula selected from the group consisting of:
WHERE R is -CH2SR3, R2 is hydrogen or loweralkyl, R3 is loweralkyl, and R1 is hydrogen or loweralkanoyl;
WHERE R1 and R2 are as before defined;
WHERE R is hydrogen or CH3CO;
where R1 is hydrogen or RCO, R is loweralkyl, R2 is hydrogen, CH3CO or RCO where R is loweralkyl; and
WHERE R3 is hydrogen or RCO where R is loweralkyl.
Abstract:
An improved process for synthesizing amino acid amides of dopamine comprising reacting an active ester of an appropriate Ncarbobenzyloxy amino acid directly with a dopamine salt. The amino acid amides of dopamine are useful as renal vasodilators and antihypertensive agents.
Abstract:
THE 2''-O-ALKANOYL-4''-ALKANOYLOXY DERIVATIVES OF ERYTHROMYCIN A AND B ARE PREPARED BY REACTING 4''-HYDROXYERYTHROMYCIN A OR B WITH AN APPROPRIATE ACID ANHYDRIDE. THE RESULTING PRODCUTS HAVE ANTIBIOTIC ACTIVITY AGAINST STAPHYLOCOCCUS AUREUS SMITH.
Abstract:
Covers 11-substituted erythromycin B derivatives having a formula selected from the group consisting of:
WHERE R is selected from the group consisting of lower alkyl and -CHR3SR4 where R3 and R4 are loweralkyl, and R1 and R2 are hydrogen or loweralkyl and;
WHERE R1, R2 and R3 are as before defined. Said erythromycin derivatives are useful as antibiotics or as intermediates useful in preparing other useful antibiotic compounds.
Abstract:
THE 9,11-PHENYL; HALO, NITRO, AND LOWER ALKYL SUBSTITUTED PHENYL; LOWER ALKYL; FATTY ALKYL; AND CYCLYOHEXYL CYCLIC BORONATE ESTER OF THE 6,9-HEMIKETAL OF ERYTHROMYCIN A HAVE USEFUL ANTIBIOTIC ACTIVITY.
Abstract:
THE 4''-HYDROXYVERYTHROMYCIN A AND B DERIVATIVES TOGETHER WITH ITS ACID-ADDITION SALTS HAVE BEEN FOUND TO HAVE ANTIBIOTIC ACTIVITY. THE COMPOUND HAS BEEN MADE BY OXIDATION OF ERYTHROMYCIN A OR B TO THE N OXIDE, FOLLOWED BY PYROLYSIS TO 3-(DEDIMETHYLAMINO)-$2''4''-ERYTHROMYCIN. THE UNSATURATE IS THEN EPOXIDIZED AND 3''-(DEDIMETHYLAMINO) - 3''-AZIDO-4''-HYDROXYVERYTHROMYCIN FORMED BY OPENING THE EPOXY RING WITH AN AZIDE. THE AZIDE IS THEN REDUCED TO 3''-(DEDIMETHYLAMINO)-3''-AMINO-4''-HYDROXYVERYTHROMYCIN, WHICH IS FURTHER REDUCED IN THE PRESENCE OF FORMALDEHYDE TO 4''-HYDROXYERYTHROMYCIN.
Abstract:
NOVEL LONG CHAIN ALKYL SULFATE SALTS OF 1-(P-CHLOROBENZHYDRYL)-4-METHYLHOMOPIPERAZINE ARE DISCLOSED. THESE SALT FORMS MASK THE BITTER TASTE ASSOCIATED WITH THE FREE BASE AND SOLUBLE ACID-ADDITION SALT FORMS OF THIS COMPOUND THEREBY ENABLING THE PREPARATION OF AN ORAL DOSAGE FORM OF THIS ANTIHISTAMINIC AND BRONCHODILATING AGENT.