Abstract: A compound having the structure ##STR1## is reacted with Ph.sub.3 P.dbd.CH(CH.sub.2).sub.3 Y wherein Y is --CO.sub.2 .sup..crclbar. M.sup..sym. or --C.tbd.N to form ##STR2## which is aminated and esterified to form ##STR3## which may be used to form [1S-[1.alpha.,2.alpha.(Z),3.alpha., 4.alpha.[[-7-[3-[[[[1-oxoheptyl) -amino]acetyl]amino]methyl]-7-oxabicyclo-[2.2.1]-hept-2-yl]-5-heptenoic acid.
Abstract: Prostaglandin analogs useful in treating thrombotic and vasospastic disease having the structural formula ##STR1## wherein: m is 1, 2, or 3;n is 0, 1, 2 or 3;R is CO.sub.2 R', CH.sub.2 OH, CONHSO.sub.2 R.sub.hu 3, CONHR.sup.4, or --CH.sub.2 -5-tetrazolyl;R' is hydrogen, alkyl, or alkali metal;X is O or NH;Y is --O--, a single bond or vinylene, except that Y cannot be --O-- when n is 0 and if Y is vinylene, then n=0; ##STR2## and the remaining symbols are as defined in the specification.
Abstract: Novel compounds having the formula ##STR1## wherein X, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
Abstract: Racemic Feist's acid is treated with (R)-(+)-.alpha.-methylbenzylamine to yield (1R-trans)-3-methylenecyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzylamine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl ester which is an intermediate in the preparation of the antiviral agent [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobut yl]-1,9-dihydro-6H-purin-6-one. The improved process also enables the recovery of racemic Feist's acid from the resolution.
Type:
Grant
Filed:
October 16, 1992
Date of Patent:
August 17, 1993
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Jollie D. Godfrey, Jr., Richard H. Mueller, Thomas P. Kissick, Janak Singh
Abstract: Racemic Feist's acid is treated with (R)-(+)-.alpha.-methylbenzylamine to yield (1R-trans)-3-methylenecyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzylamine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl ester which is an intermediate in the preparation of the antiviral agent [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobut yl]-1,9-dihydro-6H-purin-6-one. The improved process also enables the recovery of racemic Feist's acid from the resolution.
Type:
Grant
Filed:
October 16, 1992
Date of Patent:
August 17, 1993
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Jollie D. Godfrey, Jr., Richard H. Mueller, Thomas P. Kissick, Janak Singh
Abstract: A method is provided for treatment of Parkinson's disease or controlling movement of a Parkinsonian patient by administering an ATP-sensitive potassium channel blocker, such as a sulfonyl urea, (for example, tolbutamide), or quinine.
Abstract: Novel compounds are disclosed having the formula ##STR1## or its isomer ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and X are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
Abstract: A catheter holder has a pad of medical grade adhesive material having one surface for attachment to the skin of a wearer, and a pair of tapes secured to and extending from the other surface of the pad. A multiple use adhesive is placed on a surface of at least one tape which surface faces generally towards the other tape. With such an arrangement, the two tapes can be stuck together to enclose the catheter and at the same time the tape carrying the adhesive sticks to the adjacent wall of the catheter so preventing logitudinal movement of the catheter relative to the pad.
Abstract: A novel process and intermediates are disclosed for the preparation of the optically active compound ##STR1## wherein R.sup.3 is a protecting group. This cyclobutanone compound is used to prepare a compound of the formula ##STR2## having anti-viral activity.
Abstract: Racemic Feist's acid is treated with (R)-(+)-.alpha.-methylbenzylamine to yield (1R-trans)-3-methylene-cyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzylamine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl ester which is an intermediate in the preparation of the antiviral agent [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobut yl]-1,9-dihydro-6H-purin-6-one. The improved process also enables the recovery of racemic Feist's acid from the resolution.
Type:
Grant
Filed:
October 16, 1992
Date of Patent:
August 3, 1993
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Jollie D. Godfrey, Jr., Richard H. Mueller, Thomas P. Kissick, Janak Singh
Abstract: A synthetic plastic bag for containing liquids, e.g., urine, has a plastic outlet tube. It is manufactured by a first step of seam welding the tube between two superposed bag walls. In a subsequent step, an encircling sleeve is slide over the tube to a position where it contains within it the portions of the bag walls on either side of the tube. Thirdly, this sleeve is compressed onto the tube by a crimping operation conducted with the crimping force applied in a direction radially of the tube but at substantially right angles to the plane in which the bag walls lie. Alternatively, after the tube is seam welded between the bag walls, the bag and tube combination is then placed between the blocks of a mold, each block having confronting recesses of a particular shape and molten plastics material is injected to fill these recesses. The injected material forms a collar which completely surrounds the tube.
Abstract: An enteric coated pharmaceutical composition is provided which includes a medicament which is sensitive to a low pH environment of less than 3, such as pravastatin, which composition is preferably in the form of pellets which includes an enteric coating formed of neutralized hydroxypropylmethyl cellulose phthalate, plasticizer and anti-adherent. The so-coated pellets have good resistance to deterioration at pH less than 3 but have good drug release properties at greater than 3.
Abstract: A catheter retainer is disclosed that includes an adhesive pad with projections. The catheter is secured to the pad by being tied to the projections.
Abstract: Angiotension II inhibition is exhibited by ##STR1## wherein: R.sup.1 and R.sup.2 are each independently hydrogen, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, thiophenalkyl, pyridylalkyl, or --R.sup.8 CO.sub.2 R.sup.9 ;R.sup.3 is a single bond, --S--, or --O--;R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, aryl, cycloalkyl, aralkyl, cycloalkylalkyl, or thiophenalkyl;R.sup.7 --(CH.sub.2).sub.n --CO.sub.2 R.sup.9, ##STR2## --NHSO.sub.2 CF.sub.3, --SO.sub.3 H, --C(CF.sub.3).sub.2 OH, ##STR3## --PO.sub.3 H, ##STR4## --CONHOR.sup.12, --CONHNHSO.sub.2 CF.sub.3, --(CH.sub.2).sub.n --5--tetrazolyl (optionally substituted with R.sup.9), and the remaining symbols are as defined in the specification.
Abstract: Congestive heart failure is treated by administration of a selective inhibitor of neutral endopeptidase and an angiotensin converting enzyme inhibitor. Captopril, fosinopril sodium, enalapril maleate and lisinopril are the preferred angiotensin converting enzyme inhibitors and the mercapto compounds of the formula ##STR1## are the preferred selective inhibitors of neutral endopeptidase.
Abstract: Racemic Feist's acid is treated with (R)-(+)-.alpha.-methylbenzylamine to yield (1R-trans)-3-methylenecyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzylamine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl ester which is an intermediate in the preparation of the antiviral agent [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobut yl]-1,9-dihydro-6H-purin-6-one. The improved process also enables the recovery of racemic Feist's acid from the resolution.
Type:
Grant
Filed:
October 16, 1992
Date of Patent:
June 8, 1993
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Jollie D. Godfrey, Jr., Richard H. Mueller, Thomas P. Kissick, Janak Singh
Abstract: A method is provided for treatment of neuronal insult, such as caused by lack of oxygen, by administering an ATP-sensitive potassium channel blocker, such as a sulfonyl urea, for example, tolbutamide.
Type:
Grant
Filed:
January 27, 1992
Date of Patent:
June 1, 1993
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Kerry P. S. J. Murphy, Susan A. Greenfield