Abstract: The S-acylation of a mercaptoacyl amino acid having ACE inhibitory action with a diuretic containing a carboxyl group yields a product having both ACE inhibitory action and diuretic activity in vivo.
Abstract: A novel powdered wax is provided which is especially adapted for use as a polishing agent for tablets and as a substrate for print carried by such tablets. A method for forming such powdered wax is also provided which includes the steps of milling pieces of wax with dry ice and then allowing the dry ice to evaporate while maintaining the milled wax at cool temperatures to prevent clumping.
Abstract: Antiinflammatory activity is exhibited by steroids having the formula ##STR1## and the 1,2-dehydro derivatives thereof, wherein R is hydrogen, alkyl, or aryl;R.sub.1 is hydrogen, alkyl, ##STR2## alkylthio, alkoxy, fluoro, hydroxyalkyl, cyanoalkyl, alkoxycarbonyl-(CH.sub.2).sub.p -, mono-, di- or trifluoromethyl, or ##STR3## wherein p is 0, 1, 2, 3 or 4, Y.sub.1 is alkyl or aryl, and Y.sub.2 and Y.sub.3 are the same or different and each is hydrogen or alkyl;R.sub.2 is alkyl, alkenyl or alkynyl;R.sub.3 is carbonyl or .beta.-hydroxymethylene;R.sub.4 is hydrogen or halogen;R.sub.5 is hydrogen, methyl or fluorine; andn is 0, 1 or 2.
Abstract: Myocardial perfusion can be measured and ischemia and infarction can be diagnosed using compounds having the formula[.sup.99m Tc(L).sub.n ].sup..sym. A.sup..crclbar.whereinA is an anion;n is 1, 2, 3 or 6;if n is 1, L is a hexadentate ligand, if n is 2, L is a tridentate ligand, if n is 3, L is a monodentate ligand.
Abstract: Antibacterial activity is exhibited by .beta.-lactams having a phosphinic or phosphonic substituent in the 1-position and an acylamino substituent in the 3-position.
Type:
Grant
Filed:
March 15, 1982
Date of Patent:
October 23, 1984
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
William H. Koster, Christopher M. Cimarusti
Abstract: 7-Oxabicycloheptane substituted thio prostaglandin analogs are provided having the structural formula ##STR1## wherein R is hydrogen, lower alkyl or alkali metal, R.sup.1 is lower alkyl, arylalkyl, aryl, cycloalkyl or cycloalkylalkyl. A is --CH.dbd.CH or --(CH.sub.2).sub.2, n is 1 to 4, n' is 0 to 2 and m is 1 to 8, and including all stereoisomers thereof.The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
Abstract: The degradation of enkephalins in a mammalian host is inhibited by administration of an enkephalinase enzyme inhibitor of the formula ##STR1##
Type:
Grant
Filed:
May 27, 1983
Date of Patent:
October 2, 1984
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Roland Greenberg, David W. Cushman, B. Richard Vogt, Frank L. Weisenborn, Michael J. Antonaccio
Abstract: Optically active 7-oxabicycloheptane prostaglandin intermediates are provided having the general structure ##STR1## wherein one of R.sup.1 and R.sup.2 is --COOH, ##STR2## or --CH.sub.2 OH and the other is ##STR3## A method for preparing the above intermediates is also provided.
Abstract: Antiinflammatory activity is exhibited by pregnenes having the structural formula ##STR1## wherein R.sub.1 is hydrogen, hydroxy, halogen, or acyloxy;R.sub.2 and R.sub.3 are each hydrogen, R.sub.2 and R.sub.3 are each methyl, R.sub.2 and R.sub.3 are each alkylthio, R.sub.2 is hydrogen and R.sub.3 is alkyl, R.sub.2 is hydroxyl and R.sub.3 is alkyl, or R.sub.2 and R.sub.3 taken together are --(CH.sub.2).sub.2 --, methylene, or oxo; andR.sub.4 is hydrogen, fluorine, chlorine or bromine.
Type:
Grant
Filed:
January 20, 1984
Date of Patent:
October 2, 1984
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Donald S. Karanewsky, Christopher M. Cimarusti
Abstract: The degradation of enkephalins in a mammalian host is inhibited by administration of an enkephalinase enzyme inhibitor of the formula ##STR1##
Type:
Grant
Filed:
May 27, 1983
Date of Patent:
October 2, 1984
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Roland Greenberg, David W. Cushman, B. Richard Vogt, Frank L. Weisenborn, Michael J. Antonaccio
Abstract: 7-Oxabicyclo substituted prostaglandin phenyl carboxylic acid derivatives 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.
Abstract: N.sup.2 -[N-(N-acetylmuramoyl)-L-alanyl]-N-(5,6-diamino-1-carboxy-6-oxohexyl)-D-.a lpha.-glutamine, N.sup.2 -[N-(N-acetylmuramoyl)-L-alanyl]-N-[5,6-diamino-1-[[1-[(1-carboxyethyl)car bamoyl]ethyl]carbamoyl]-6-oxohexyl]-D-.alpha.-glutamine and EM5556C are obtained as a mixture by cultivating a strain of the microorganism Nocardia orientalis A.T.C.C. No. 39444.
Type:
Grant
Filed:
October 31, 1983
Date of Patent:
October 2, 1984
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Pushpa Singh, Karen Bush, Dorothy S. Slusarchyk
Abstract: Substituted peptide 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: Nitrobenzofurazan derivatives having the formula ##STR1## are provided wherein R.sub.1 and R.sub.2 each is hydrogen, lower alkyl or phenyl-lower alkyl; R.sub.3 is hydrogen, hydroxy or lower alkyl; R.sub.4 is hydrogen or lower alkyl; m is 2 or 3; and n is 0, 1 or 2; these compounds are useful analytical tools.
Type:
Grant
Filed:
April 28, 1983
Date of Patent:
September 4, 1984
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Callixtus E. Ita, Anthony F. Heald, Peter Egli
Abstract: Hypotensive activity is exhibited by compounds having the formula ##STR1## and salts thereof wherein R.sub.1 is alkyl, aryl, arylalkyl, cycloalkyl, or cycloalkylalkyl;R.sub.2 is cycloalkyl, 3-cyclohexenyl or 2-alkyl-3-cyclohexenyl;R.sub.3 is alkyl, cycloalkyl, phenyl or alkoxy;R.sub.4 is hydrogen or alkyl;one of R.sub.5 and R.sub.6 is hydrogen and the other is alkyl-X-, phenyl-X-, alkoxy, phenyloxy, phenyl, cycloalkyl, alkyl, or phenylalkyl; or together R.sub.5 and R.sub.6 are --XCH.sub.2 CH.sub.2 X--;R.sub.7 is hydrogen or ##STR2## and n is 0 or 1.
Abstract: 7-Oxabicycloheptane substituted carbamate 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.
Abstract: An open ended ostomy pouch having a folding bar attached to the bottom of the pouch. The folding bar extends on both sides beyond the width of the pouch at the bottom opening and includes interlocking closure components on opposite ends.
Abstract: Carboxyalkyl dipeptides of the formula ##STR1## wherein R.sub.4 is a 3-, 4-, 5-, or 4,4-substituted proline are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity.
Type:
Grant
Filed:
September 28, 1981
Date of Patent:
July 31, 1984
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Edward W. Petrillo, Jr., Eric M. Gordon, John Krapcho, Peter W. Sprague
Abstract: A method is provided for preparing compounds of the formulae ##STR1## wherein A may be --C.dbd.C-- or --C.tbd.C--, by reducing an epoxy lactone of the structure ##STR2## to form the corresponding epoxy hemiacetal, reacting the epoxy hemiacetal with a silyl compound to form an epoxy silyl acetal, reacting the epoxy silyl acetal with an acetylenic derivative to form a silyl acetal, removing the silyl protecting group to form a hemiacetal, reacting the hemiacetal compound with an appropriate Wittig reagent to form a protected difluoro PGF.sub.2.alpha. type compound, removing the protecting group, reacting the difluoro PGF.sub.2.alpha. with an iodine compound to form an iodoether and reacting the iodoether with a base to form the desired compounds.Novel intermediates produced in the above method are also provided.