Abstract: A purine salt of the formula ##STR1## wherein Y.sub.1 is chloro, bromo, or iodo, and R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are independently selected from alkyl and substituted alkyl is reacted with the compound of the formulaZ.sub.1 --Xto yield the purine of the formula ##STR2## wherein x is a leaving group, and Z.sub.1 is a protected form of the carbohydrate surrogate Z.
Type:
Grant
Filed:
January 25, 1993
Date of Patent:
February 23, 1999
Assignee:
Bristol-Myers Squibb
Inventors:
Janak Singh, Gregory S. Bisacchi, Jollie D. Godfrey, Jr., Toomas Mitt, Richard H. Mueller, Robert Zahler, Thomas P. Kissick
Abstract: Compounds of the formula ##STR1## wherein X.sub.1 is ##STR2## are disclosed. These compounds possess inhibitory activity against angiotensin converting enzyme and neutral endopeptidase and thus useful as cardiovascular agents.
Abstract: Inhibition of UL42 stimulation of herpesvirus DNA polymerase activity is exhibited by novel compounds of the formulasW'--A.sub.1 --A.sub.2 --A.sub.3 --A.sub.4 --A.sub.5 --A.sub.6 --A.sub.7 --A.sub.8 --A.sub.9 --A.sub.10 --A.sub.11 --X ?SEQ. ID NO: 1!andY'--A.sub.12 --A.sub.13 --A.sub.14 --A.sub.15 --A.sub.16 --A.sub.17 --Z ?SEQ. ID NO: 2!that are useful as antiviral agents.
Type:
Grant
Filed:
January 29, 1992
Date of Patent:
January 12, 1999
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
James T. Matthews, Katerina Leftheris, Robert K. Hamatake, John T. Stevens, Mary L. Haffey
Abstract: The azepine intermediates of the formula ##STR1## wherein R.sub.6 and R.sub.7 are other than hydrogen are disclosed. These intermediates can be reacted with acylmercaptocarboxylic acids of the formula ##STR2## to give the pharmaceutically active products.
Abstract: Processes are disclosed for preparing the azepine intermediates of the formula ##STR1## These intermediates can be reacted with acylmercaptocarboxylic acids of the formula ##STR2## to give the pharmaceutically active products.
Abstract: (1R,trans) Diprotected 3-methylene-1,2-cyclopropanedimethanol is oxidized to an optically active diol ##STR1## which is then cyclized to an orthoester ##STR2## This orthoester is then treated with a Lewis acid catalyst to give the cyclobutanone ##STR3## which is useful as 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.
Type:
Grant
Filed:
September 13, 1996
Date of Patent:
June 30, 1998
Assignee:
Bristol-Myers Squibb Co.
Inventors:
Jollie D. Godfrey, Jr., Richard H. Mueller
Abstract: Amino acid esters of the formula ##STR1## wherein m is zero or one and R.sub.3 is an acid protecting group are prepared. These amino acid esters are useful as intermediates in the preparation of fused bicyclic ring compounds.
Abstract: Compounds of the formula ##STR1## wherein X.sub.1 is ##STR2## are disclosed. These compounds possess inhibitory activity against angiotensin converting enzyme and neutral endopeptidase and thus are useful as cardiovascular agents.
Abstract: Compounds of the formula ##STR1## wherein X.sub.1 is ##STR2## are disclosed. These compounds possess inhibitory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and are thus useful as cardiovascular agents.
Abstract: Antiviral activity is exhibited by compounds having the formula ##STR1## and its pharmaceutically acceptable salts wherein R.sub.1 is ##STR2## wherein R.sub.2 is hydrogen, methyl, fluoro, chloro, bromo, iodo, hydroxy or amino; or trifluoromethyl; R.sub.5 is alkyl; R.sub.6 is hydrogen, alkyl, substituted alkyl, or aryl; and R.sub.7 and R.sub.
Abstract: Compounds of the formula ##STR1## wherein X is O or S--(O).sub.t ; n is one; m is zero or one; Y is CH.sub.2, O, or S--(O).sub.t provided that Y is O or S--(O).sub.t only when m is one; and A is ##STR2## are dual inhibitors of NEP and ACE. Compounds wherein A is ##STR3## are selective ACE inhibitors. Also disclosed are methods of preparation and intermediates.
Abstract: Amino acid esters of the formulas ##STR1## wherein m is zero or one and R.sub.3 is an acid protecting group are prepared. These amino acid esters are useful as intermediates in the preparation of fused bicyclic ring compounds.
Abstract: Compounds of the formula ##STR1## are disclosed as possessing inhibotory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular agents. Processes for preparing these compounds are also disclosed.
Abstract: Compounds of the formula ##STR1## wherein X.sub.1 is ##STR2## are disclosed as possessing inhibotory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular agents.
Abstract: Compounds of the formula ##STR1## wherein: ##STR2## A is are dual inhibitors of NEP and ACE. Compounds wherein A is ##STR3## are selective ACE inhibitors.
Abstract: A process for preparing compounds of the formula ##STR1## wherein X is O or S; n is one or two; m is zero or one; Y is CH.sub.2, O, or S provided that Y is O or S only when m is one; and A is ##STR2## is disclosed. Also disclosed are processes for preparing the corresponding amino intermediates.
Abstract: Homocysteine analogs of the formula ##STR1## wherein P.sub.1 is a nitrogen protecting group and R.sub.6 is alkyl, substituted alkyl or benzyl are prepared by esterifying N-protected L-methionine, oxidizing, treating the resulting sulfoxide with an acid anhydride, treating the resulting product with an alkali metal hydroxide followed by removal of formaldehyde and the treatment with an acid anhydride or acid halide. The L-homocysteine analogs are useful as intermediates in the preparation of compounds containing a fused bicyclic ring.
Type:
Grant
Filed:
February 5, 1996
Date of Patent:
April 1, 1997
Assignee:
Bristol-Myers Squibb Co.
Inventors:
David R. Kronenthal, Jollie D. Godfrey, Jr.
Abstract: A purine salt of the formula ##STR1## wherein Y.sub.1 is chloro, bromo, or iodo, and R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are independently selected from alkyl and substituted alkyl.
Type:
Grant
Filed:
June 1, 1995
Date of Patent:
March 4, 1997
Assignee:
Bristol-Myers Squibb Co.
Inventors:
Janak Singh, Gregory S. Bisacchi, Jollie D. Godfrey, Jr., Toomas Mitt, Richard H. Mueller, Robert Zahler, Thomas P. Kissick
Abstract: Compounds of the formula ##STR1## are disclosed as possessing inhibitory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular agents. Processes for preparing these compounds are also disclosed.