Abstract: Novel intermediates useful in the preparation of the optically active antiviral compound [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobut yl]-1,9-dihydro-6H-purin-6-one are described.
Abstract: Novel intermediates useful in the preparation of the optically active antiviral compound [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobut yl]-1,9-dihydro-6H-purin-6-one are described.
Abstract: A bandage including a superabsorbent pad covered by a porous cover pad placed on a thin, flexible hydrocolloid adhesive layer leaving a portion of the adhesive layer around the pads as an adhesive border is disclosed. One side of the adhesive layer is laminated to a polymeric backing or non-woven fabric layer and a protective cover layer is applied over the pads and border portion. The protective cover layer may be silicone coated release paper and the bandage may be subjected to a vacuum thus forming the adhesive layer to the pads resulting in the border portion being substantially coplanar with the exposed surface of the cover pad overlaying the superabsorbent pad.
Abstract: A compound of the formula: ##STR1## wherein A is a purin-9-yl group, a heterocyclic isostere of a purin-9-yl group, a pyrimidin-1-yl group or a heterocyclic isostere of a pyrimidin-1-yl group; E is hydrogen, --CH.sub.2 OH or --OH; and G and D are independently selected from hydrogen, C.sub.1 to C.sub.10 alkyl, --OH, --CH.sub.2 OH, --CH.sub.2 OR.sub.20 wherein R.sub.20 is C.sub.1 to C.sub.6 alkyl, --CH.sub.2 OC(O)R.sub.21 wherein R.sub.21 is C.sub.1 to C.sub.10 alkyl, --CH.sub.2 OC(O)CH(R.sub.22)(NHR.sub.23) wherein R.sub.22 is the side chain of any of the naturally occurring amino acids and R.sub.23 is hydrogen or --C(O)CH(R.sub.24)(NH.sub.2) wherein a R.sub.24 is the side chain of any of the naturally occurring amino acids, --CH.sub.2 SH, --CH.sub.2 Cl, --CH.sub.2 F, --CH.sub.2 Br, --CH.sub.2 I, --C(O)H, --CH.sub.2 CN, --CH.sub.2 N.sub.3, --CH.sub.2 NR.sub.1 R.sub.2, --CO.sub.2 R.sub.1, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 OR.sub.20 wherein R.sub.20 is as defined above, --CH.sub.2 CH.sub.2 OC(O)R.sub.
Type:
Grant
Filed:
May 1, 1991
Date of Patent:
September 21, 1993
Assignee:
Bristol-Myers Squibb Company
Inventors:
Daniel W. Norbeck, Jacob J. Plattner, Terry J. Rosen, David L. Garmaise, Richard J. Pariza, Steven M. Hannick, Thomas J. Sowin
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: The present invention relates to a process for the preparation of substantially pure enantiomer of the purines substituted with cyclobutanes.
Type:
Grant
Filed:
March 11, 1991
Date of Patent:
August 10, 1993
Assignee:
Bristol-Myers Squibb Company
Inventors:
Richard J. Pariza, Steven M. Hannick, Thomas J. Sowin, Elizabeth M. Doherty
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: 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: Pyrimidine compounds of the formula ##STR1## wherein X is sulfur or oxygen, Y is R.sub.11 or --O--R.sub.1, and R.sub.4 is aryl or heterocyclo are disclosed. These compounds are useful as cardiovascular agents, particularly anti-hypertensive agents, due to their calcium entry blocking vasodilator activity.
Type:
Grant
Filed:
January 5, 1987
Date of Patent:
April 13, 1993
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Karnail Atwal, George C. Rovnyak, Spencer D. Kimball
Abstract: The optically active antiviral compound [1R-(1.alpha., 2.beta., 3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)-cyclobutyl]-1,9-dihydro-6H-pu rin-6-one and novel intermediates useful in its preparation are described.
Abstract: Compounds of the formula ##STR1## wherein Z is oxygen or sulfur are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inbitition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
Abstract: Cyclobutanols of the formula ##STR1## wherein P is a hydroxy protecting group are useful intermediates in the preparation of antiviral compounds.
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)cyclobutyl]-1,9-dihydro-6H-pur in-6-one. The improved process also enables the recovery of racemic Feist's acid from the resolution.
Type:
Grant
Filed:
October 2, 1991
Date of Patent:
February 9, 1993
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Jollie D. Godfrey, Jr., Richard H. Mueller, Thomas P. Kissick, Janak Singh
Abstract: A catheter attachment device comprises a first pad of medical grade adhesive having one surface covered by a removable protective layer, a second surface covered by a plastics film, and, attached to the film, a second pad of medical grade adhesive. A surface of this second pad which faces away from the first pad is covered by a removable protective layer and has a plastics film on its other surface. The two plastics films are attached to each other over a central region substantially smaller in area than the areas of both the first and second pads.