Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
Abstract: A method is provided for preparing L-(+)-.beta.-hydroxyisobutyric acid by fermentation employing microorganisms of the species Pseudomonas aeruginosa and of the genus Protaminobacter such as of the species Protaminobacter alboflavus, and isobutyric acid and/or methacrylic acid and/or derivatives thereof as the substrate.
Abstract: Compounds of the formula ##STR1## wherein A is ##STR2## intervene in the conversion of angiotensinogen to angiotensin II by inhibiting renin and thus are useful as anti-hypertensive agents.
Type:
Grant
Filed:
December 14, 1984
Date of Patent:
October 7, 1986
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Denis E. Ryono, Edward W. Petrillo, Jr.
Abstract: Phosphonyl hydroxyacyl amino acids of the formula ##STR1## wherein X is a substituted or unsubstituted imino or amino acid or ester. These compounds possess angiotensin converting enzyme activity and are thus useful as hypotensive agents.
Type:
Grant
Filed:
December 16, 1985
Date of Patent:
October 7, 1986
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Donald S. Karanewsky, Edward W. Petrillo, Jr.
Abstract: 7-Oxabicycloheptane and 7-oxabicycloheptene prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
Type:
Grant
Filed:
July 25, 1985
Date of Patent:
September 30, 1986
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
David L. Snitman, Martin F. Haslanger, Peter W. Sprague
Abstract: 5,6-Epoxy-7-oxabicycloheptane substituted prostaglandin analogs are provided having the structural formula ##STR1## wherein m is 1 to 5, R is H, lower alkyl, alkali metal or polyhydroxylamine, and R.sup.1 is lower alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl or lower alkenyl, including all stereoisomers thereof.The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
Abstract: 7-Oxabicycloheptane substituted prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease and as inhibitors of 5-lipoxygenase enzyme.
Abstract: A controlled release pharmaceutical formulation which undergoes substantially or approaches zero order release of active drug is provided, preferably in the form of a coated tablet, containing a core portion from which medicament, such as procainamide hydrochloride, is slowly released over a controlled length of time. The core also includes one or more hydrocolloid gelling agents having a viscosity of within the range of from about 10,000 to about 200,000 centipoises in 2% solution at 20.degree. C., such as hydroxypropylmethyl cellulose and/or methyl cellulose, one or more non-swellable binders and/or wax binders (where the medicament and/or hydrocolloid gelling agents are non-compressible), one or more inert fillers or excipients, one or more lubricants, and optionally one or more anti-adherents such as silicon dioxide and water. The above-described core is coated with a pharmaceutical coating composition containing a hydrophobic polymer and a hydrophilic polymer.
Type:
Grant
Filed:
October 5, 1984
Date of Patent:
September 9, 1986
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Nemichand B. Jain, Linda P. Gertie, Edward M. Rudnic
Abstract: 5,6-Epoxy-7-oxabicycloheptane substituted ether prostaglandin analogs are provided having the structural formula ##STR1## wherein X is O or ##STR2## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
Abstract: 5-6-Epoxy-7-oxabicycloheptane substituted amino prostaglandin analogs are provided having the structural formula ##STR1## wherein A is CH.dbd.CH or (CH.sub.2).sub.2, m is 1 to 8, n is 0 to 5, R is H, lower alkyl, alkali metal or hydroxylamine salt, and R.sup.1 is lower alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, lower alkenyl, lower alkoxy, aralkoxy or ##STR2## including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
Abstract: 7-Oxabicycloheptane substituted ether prostaglandin analogs are provided having the structural formula ##STR1## wherein X is O or ##STR2## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
Abstract: 7-Oxabicycloheptane substituted thio prostaglandin analogs are provided having the structural formula ##STR1## wherein R is hydrogen, lower alkyl, alkali metal, or a polyhydroxylamine salt, R.sup.1 is hydrogen, lower alkyl, arylalkyl, aryl, cycloalkyl or cycloalkylalkyl, R.sup.2 is hydrogen or lower alkyl, A is --CH.dbd.CH-- or --(CH.sub.2).sub.2, n is 1 to 4, n' is 0, 1 or 2, q is 1 to 10 and m is 0 to 8, and including all stereoisomers thereof.The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease, and as such are useful in inhibiting platelet aggregation.
Abstract: 7-Oxabicycloheptane substituted aryl amino prostaglandin analogs are provided having the structural formula ##STR1## wherein A is --CH.dbd.CH-- or --(CH.sub.2).sub.2 --; m is 1 to 8; n is 1 to 5; R is H, lower alkyl, alkali metal or a polyhydroxyamino salt; R.sup.1 is H, lower alkyl, hydroxyalkyl or aryl; R.sup.2 is H, lower alkyl, aryl or cycloalkyl, R.sup.3 is substituted aryl wherein the aryl group (which may be phenyl or naphthyl) is substituted with one or two of the following groups: hydroxy, ##STR2## SR.sup.4, --CN, --NO.sub.2, ##STR3## wherein R.sup.4 and R.sup.5 may be the same or different and are H or lower alkyl, and including all stereoisomers thereof.The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
Abstract: Arylhydroxamates are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, aryl, lower alkenyl, cycloalkenyl, aralkyl, or ##STR2## wherein n is 1 to 4 and X is hydroxy, alkoxy, amino, C.sub.1 -C.sub.4 -alkylamino or C.sub.1 -C.sub.4 -dialkylamino.R.sup.2 is hydrogen or lower alkyl; andR.sup.3 is C.sub.1 -C.sub.20 alkyl or C.sub.3 -C.sub.20 alkenyl, aryl, aryl-alkyl, cycloalkyl, aryl-alkenyl, lower alkoxy, lower alkenyloxy, aryl-alkoxy or cycloalkyloxy.These compound are useful as inhibitors of .DELTA..sup.5 -lipoxygenase and as such are useful as antiallergy agents.
Type:
Grant
Filed:
April 4, 1985
Date of Patent:
August 19, 1986
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Donald S. Karanewsky, Martin F. Haslanger
Abstract: Hydroxamates are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, aryl, lower alkenyl, cycloalkenyl, aralkyl, or ##STR2## wherein n is 1 to 4 and X is hydroxy, alkoxy, amino, C.sub.1 -C.sub.4 -alkylamino or C.sub.1 -C.sub.4 -dialkylamino.R.sup.2 is hydrogen or lower alkyl; andR.sup.3 is C.sub.1 -C.sub.20 alkyl or C.sub.3 -C.sub.20 alkenyl, aryl, aryl-alkyl, cycloalkyl, aryl-alkenyl, lower alkoxy, lower alkenyloxy, aryl-alkoxy or cycloalkyloxy, and m is 0 to 5. These compounds are useful as inhibitors of .DELTA..sup.5 -lipoxygenase and as such are useful as antiallergy agents.
Type:
Grant
Filed:
April 4, 1985
Date of Patent:
August 5, 1986
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Martin F. Haslanger, Donald S. Karanewsky
Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
Type:
Grant
Filed:
March 30, 1984
Date of Patent:
August 5, 1986
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Jollie D. Godfrey, Jr., Eric M. Gordon, Sesha I. Natarajan
Abstract: A method is provided for preparing phosphinic acid prodrug intermediates which are useful in preparing phosphinic acid angiotensin-converting enzyme inhibitors which method includes the step of coupling a phosphonous acid or its ester of the structure ##STR1## wherein R is H or lower alkyl and R.sup.1 is lower alkyl, aryl, arylalkyl, cycloalkyl or cycloalkylalkyl, with an alkylating agent of the structure ##STR2## wherein Hal is Cl, Br or I, n is 0 or 1, R.sup.2 is H or lower alkyl, and Z is H, lower alkyl, --CO.sub.2 R.sup.3 (wherein R.sup.3 is H or lower alkyl), ##STR3## (wherein R.sup.4 is H, lower alkyl, aryl or arylalkyl), --CN, or ##STR4## (wherein R.sup.5 and R.sup.6 may be the same or different and are selected from the group consisting of H, lower alkyl, aryl, aryl-lower alkyl, cycloalkyl or cycloalkylalkyl and at least one of R.sup.5 and R.sup.6 is other than H, or R.sup.5 and R.sup.