Abstract: Compounds are provided having the structure ##STR1## whereinR.sup.1 is hydrogen, alkyl of 1-3 carbons, phenyl optionally substituted by R.sup.4 ; R.sup.2 is cyano; ##STR2## (wherein Z is a single bond or ##STR3## X is O or S); ##STR4## (wherein R.sup.9 is hydrogen or alkyl, Q is CH or N); ##STR5## wherein R.sup.6 is amino, alkylamino, dialkylamino, haloalkyl or ##STR6## and R.sup.4 and R.sup.5 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, alkanoyloxy, benzyloxy, substituted benzyloxy, hydroxy, halogen (Cl, Br and F), nitro and trifluoromethyl; and R.sup.7, R.sup.8, m and n are as defined hereinafter.
Abstract: New 7-oxabicycloheptane- and 7-oxabicycloheptene compounds which have the general formula ##STR1## and intermediates therefor which have the general formulas ##STR2## are useful as cardiovascular agents.
Abstract: Carbamoylalkylureido cephalosporins of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion, or the group ##STR2## R.sub.1 is hydrogen or methoxy; A is straight or branched chain alkylene of 1 to 6 carbons; R.sub.2 and R.sub.3 are independently selected from hydrogen and straight chain alkyl of 1 to 4 carbons, or R.sub.2 is hydrogen and R.sub.3 is branched chain alkyl of 3 or 4 carbons, phenyl, benzyl or phenethyl, or R.sub.2 and R.sub.3 taken together with N atom to which they are attached form ##STR3## R.sub.4 is hydrogen or lower alkyl; R.sub.5 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.6 is hydrogen or lower alkyl; R.sub.7 is lower alkyl; and X is hydrogen, lower alkanoyloxy, ##STR4## or certain heterothio groups; are disclosed.
Abstract: A method for alleviating or reducing angiotensin related hypertension in hypertensive mammals comprises administering to such hypertensive mammals an effective amount of an angiotensin converting enzyme inhibitor selected from a group of mercaptoacyl aminoacids.
Abstract: New substituted acyl derivatives of amino acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.
Abstract: A method for alleviating or reducing angiotensin related hypertension in hypertensive mammals comprises administering to such hypertensive mammals an effective amount of an angiotensin converting enzyme inhibitor selected from a group of mercaptoacyl aminoacids.
Abstract: 2,3-Dihydro-1,2,4-triazolo[4,3-b][1,2]benzisothiazol-3-amine, 5,5-dioxides having the formula ##STR1## and salts thereof are new compounds which are useful as anti-inflammatory agents.
Type:
Grant
Filed:
February 3, 1978
Date of Patent:
February 20, 1979
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Peter C. Wade, B. Richard Vogt, Thomas P. Kissick
Abstract: Compounds are provided having the structure ##STR1## wherein n is 1, 2 or 3, m is 0, 1 or 2, R.sub.1 R.sub.2, R.sub.3, R.sub.4 and R.sub.5 may be the same or different and can be hydrogen, lower alkyl, halo-lower alkyl, acyl, lower alkoxy-carbonyl ##STR2## amido ##STR3## or lower alkoxylakylene, X is a straight or branched bivalent aliphatic radical and Y is ##STR4## These compounds are useful in the treatment of hypertension.
Type:
Grant
Filed:
July 29, 1977
Date of Patent:
February 6, 1979
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Frederic P. Hauck, Joseph E. Sundeen, Joyce Reid
Abstract: Benzimidazole derivatives are provided having the structure ##STR1## wherein R.sup.1 is lower alkyl or phenyl-lower alkyl, R.sup.2 and R.sup.3 are the same or different and are hydrogen or lower alkyl, R.sup.4 is lower alkyl or phenyl, and R.sup.5 and R.sup.6 are the same or different and are chlorine, bromine, fluorine or iodine, m is 0 to 3, n is 0 to 3, and m + n is .ltoreq. 5, and physiologically acceptable salts thereof. These compounds are especially useful in treating or preventing tapeworm and whipworm infestation in mammalian species or poultry.
Type:
Grant
Filed:
March 13, 1978
Date of Patent:
February 6, 1979
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Rudiger D. Haugwitz, Larry R. Cruthers, Barbara V. Maurer
Abstract: Benzimidazolecarbamate derivatives are provided having the structure ##STR1## wherein R is lower alkyl, R.sub.1, R.sub.2 and R.sub.3 may be the same or different and may be lower alkyl or lower alkoxy, m is 0, 1 or 2 and n is 1 to 5. These compounds are useful as anthelmintic agents.
Abstract: Steroids having the formula ##STR1## wherein X is --S--, ##STR2## R.sub.1 is alkyl or aryl; R.sub.2 is hydrogen or halogen; and R.sub.3 is hydrogen, fluorine or methyl; can be used as antiinflammatory agents.
Abstract: Compounds of the following formula ##STR1## are useful as central nervous system depressants, tranquilizers, sedatives, growth promotors, anti-convulsants and muscle relaxants in mammalian species.
Abstract: Compounds of the formula ##STR1## wherein R is hydrogen, ##STR2## R.sub.1 and R.sub.2 are independently selected from hydrogen, lower alkyl, and cycloalkyl or R.sub.1 and R.sub.2 taken together with the nitrogen atom to which they are attached form a ring of the formula ##STR3## N IS 0 OR AN INTEGER FROM 1 TO 3; M IS AN INTEGER FROM 1 TO 3; R.sub.3 and R.sub.4 are independently selected from hydrogen and lower alkyl; X is hydrogen, halogen, lower alkyl, lower alkoxy, or nitro; and their salts; are disclosed. These compounds possess useful antiinflammatory properties.
Abstract: Compounds having the structure ##STR1## and pharmaceutically acceptible salts thereof, wherein R.sub.1 is hydrogen, halogen, hydroxy, alkanoyloxy, alkoxy, alkylthio, alkyl, trifluoromethyl or methylenedioxy; R.sub.2 is hydrogen, halogen, alkyl, alkoxy, alkylthio, or trifluoromethyl; R.sub.3 is formyl or alkanoyl; m is 1 or 2; and n is 0, 1 or 2, have useful sedative and muscle relaxant activity, and can be used as tranquilizers.
Abstract: New 5-phenylpyrazolo[1,5-a]pyrimidin-7(1H)-ones which have the general formula ##STR1## wherein R.sup.1 is lower alkyl, phenyl, phenyl-lower alkyl or cyclo-lower alkyl;R.sup.2 is hydrogen, lower alkyl or phenyl; andR.sup.4 is hydrogen, halogen, hydroxy, lower alkoxy or amino, are useful for the production of 6-phenyl-2H-pyrazolo[3,4-b]pyridine anti-inflammatory agents.
Abstract: New substituted acyl derivatives of amino acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.
Abstract: This invention relates to the preparation of 3-heterothiomethyl cephalosporanic acid esters of the formula ##STR1## by treating a 3-methylene cephalosporin of the formula ##STR2## with a compound of the formulaHETERO-S-S-hetero or X-S-heteroin the presence of a base wherein R is a readily removable ester group, R.sub.1 is in the .alpha.-configuration and is hydrogen or methoxy, and X is a leaving group. The resulting 3-heterothio cephalosporin esters are treated according to known methods to remove the ester protecting group and yield the corresponding free acids which have antibacterial activity.
Type:
Grant
Filed:
December 8, 1976
Date of Patent:
December 12, 1978
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
William A. Slusarchyk, Eric M. Gordon, William H. Koster
Abstract: Cyanoalkylureido cephalosporins of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion, or the group ##STR2## R.sub.1 is hydrogen or methoxy; A is straight or branched chain alkylene or ##STR3## R.sub.2 is phenyl, 2-thienyl, or 3-thienyl; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.5 is hydrogen or lower alkyl; R.sub.6 is lower alkyl; and X is hydrogen, lower alkanoyloxy, ##STR4## or certain heterothio groups; are disclosed. These compounds are useful as antibacterial agents.