Patents Assigned to E. R. Squibb & Sons
  • Patent number: 4714714
    Abstract: Analogs of arachidonic acid are provided having the structure ##STR1## wherein R is CH.sub.2 OH or CO.sub.2 H and m is 1 or 2. These compounds are useful as inhibitors of leukotriene and prostaglandin biosynthesis and as such are useful an antiallergy and antiinflammatory agents.
    Type: Grant
    Filed: March 7, 1986
    Date of Patent: December 22, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Raj N. Misra
  • Patent number: 4714605
    Abstract: Technetium-99m labeled dioxime complexes are useful for imaging the myocardium, brain and hepatobiliary system, in humans and other mammalian species.
    Type: Grant
    Filed: October 14, 1986
    Date of Patent: December 22, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Thomas A. Feld, Pedro N. Juri, Elizabeth N. Treher
  • Patent number: 4714757
    Abstract: Aminopeptidase inhibitory activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, alkyl, carboxyalkyl, halo-substituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl or heteroaryl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl, (heteroaryl)alkyl, ##STR2## R.sub.4 and R.sub.5 are each independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl, or (heteroaryl)alkyl;A is glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, valyl, aspartyl, prolyl, norleucyl, or norvalyl; andn is an integer of 1 to 6.
    Type: Grant
    Filed: September 18, 1985
    Date of Patent: December 22, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Eric M. Gordon, Jollie D. Godfrey, Jr., Norma G. Delaney
  • Patent number: 4711900
    Abstract: Arylhydroxamates are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, aryl, lower alkenyl, cycloalkyl, or aralkyl;R.sup.2 is hydrogen, lower alkyl, aryl, cycloalkyl, alkanoyl or aroyl;m is 2 to 8; and ##STR2## wherein R.sup.3 is OH, COOH ##STR3## These compounds are useful as inhibitors of .DELTA..sup.5 -lipoxygenase and as such are useful as antiallergy agents.
    Type: Grant
    Filed: July 23, 1986
    Date of Patent: December 8, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Ravi K. Varma, Eric M. Gordon
  • Patent number: 4711884
    Abstract: This invention is directed to compounds of the formula ##STR1## wherein X is a thiazine or thiazepine of the formula ##STR2## These compounds possess angiotensin converting enzyme inhibition activity and are thus useful as hypotensive agents.
    Type: Grant
    Filed: December 27, 1983
    Date of Patent: December 8, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Donald S. Karanewsky
  • Patent number: 4709046
    Abstract: Spiro compounds of the formula ##STR1## wherein X is oxygen or sulfur. These compounds possess antgiotensin converting enzyme inhibition activity and are thus useful as anti-hypertension agents.
    Type: Grant
    Filed: May 9, 1983
    Date of Patent: November 24, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: John Krapcho
  • Patent number: 4707494
    Abstract: 7-Oxabicyclo(2.2.1)heptane analogs are disclosed having the general formula ##STR1## wherein R.sub.1 is lower alkyl, alkenyl, substituted alkenyl or alkynyl; R.sub.2 is lower alkyl, alkenyl or alkynyl; A is --CH.sub.2 --CH.dbd.CH-- or a single bond; X is --CH.sub.2, --CH(CH.sub.3) or --C(CH.sub.3).sub.2 ; n is an integer from 0 to 9, with the proviso that when A is a single bond, n is an integer from 1 to 9; including all stereoisomers.These new compounds have been found to be inhibitors of arachidonic acid cyclooxygenase and are therefore useful as antiinflammatory antipyretic and analgesic agents.
    Type: Grant
    Filed: August 26, 1986
    Date of Patent: November 17, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Ravi K. Varma, Carl P. Ciosek, Eric M. Gordon
  • Patent number: 4705849
    Abstract: Boronic acid adducts of technetium-99m dioxime complexes are useful for imaging the myocardium, hepatobiliary system, brain and blood pool in humans and other mammalian species.
    Type: Grant
    Filed: April 15, 1985
    Date of Patent: November 10, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Adrian D. Nunn, Thomas A. Feld, Elizabeth N. Treher
  • Patent number: 4704457
    Abstract: A compund having the formula ##STR1## can be prepared by coupling a compound having the formula ##STR2## or a salt thereof, with a compound having the formula ##STR3## to yield a compound having the formula ##STR4## and oxidizing that compound to yield the desired compound; wherein R is hydrogen or an amino protecting group;R.sub.1 is hydrogen, methly or ethyl;M.sup..sym. is an inorganic cation or a substituted ammonium ion; andM.sub.1.sup..sym. is hydrogen, an organic cation, or a substituted ammonium ion.
    Type: Grant
    Filed: June 21, 1982
    Date of Patent: November 3, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jerome L. Moniot, Christopher M. Cimarusti, Rita T. Fox
  • Patent number: 4703043
    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 27, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Donald S. Karanewsky, Edward W. Petrillo, Jr.
  • Patent number: 4695585
    Abstract: A compound of the formula ##STR1## wherein R.sub.1 is hydrogen, hydroxy, alkoxy or aryloxy; R.sub.2 is hydrogen, hydroxy, alkoxy or aryloxy; or wherein R.sub.1 and R.sub.2 taken together is an aromatic ring; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is lower alkyl, substituted alkyl, alkenyl or alkynyl; X is amino, alkylamino, alkanoylamino, oxygen or a single bond; A is CH.sub.2 --CH.dbd.CH or a single bond; and n is an integer from 0 to 9, with the proviso that when A is a single bond, n is an integer from 1 to 9 including all stereoisomers thereof.These new compounds have been found to simultaneously inhibit the arachidonic acid enzymes 5-lipoxygenase and cyclooxygenase and as such are useful, for example, as antiinflammatory agents.
    Type: Grant
    Filed: September 23, 1986
    Date of Patent: September 22, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Ravi K. Varma, Eric M. Gordon
  • Patent number: 4695586
    Abstract: 7-Oxabicyclo(2.2.1)heptane-based N-hydroxy-N-alkyl (or aryl) ureas, carbamic acids and carbamothioic acids are disclosed having the general formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, alkenyl, aryl or aralkyl; R.sub.2 is hydrogen, lower alkyl, aralkyl, alkanoyl or aroyl; R.sub.3 is lower alkyl, alkenyl or alkynyl; A is --CH.sub.2 --CH.dbd.CH-- or a single bond; X is oxygen, sulfur or NH; n is an integer from 1 to 8; and all stereoisomers thereof.These new compounds have been found to simultaneously inhibit the enzymes arachidonic acid cyclooxygenase and arachidonic acid 5-lipoxygenase and are therefore useful as antiinflammatory, antiasthma and antipsoriatic agents.
    Type: Grant
    Filed: September 23, 1986
    Date of Patent: September 22, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Ravi K. Varma, Sam T. Chao, Eric M. Gordon
  • Patent number: 4694002
    Abstract: Calcium channel blocking activity is exhibited by compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein the stereochemistry at the chiral centers in the 3 and 4-positions of the benzothiazepine nucleus is cis, and whereinR.sub.1 is alkyl, aryl, arylalkyl, alkenyl or alkynyl;R.sub.2 and R.sub.5 are each independently hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen or trifluoromethyl; andR.sub.3 and R.sub.4 are each independently alkyl or cycloalkyl or R.sub.3 and R.sub.4 together with the nitrogen atom to which they are attached are pyrrolidinyl, piperidinyl or morpholinyl.
    Type: Grant
    Filed: August 21, 1986
    Date of Patent: September 15, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: David Floyd, Karnail Atwal
  • Patent number: 4694083
    Abstract: Disclosed herein is a process for preparing a compound having the formula ##STR1## which comprises sulfonating a compound having the formula ##STR2## with a complex having the formula ##STR3## and cyclizing the resulting compound having the formula ##STR4## by treatment with a base.
    Type: Grant
    Filed: April 28, 1986
    Date of Patent: September 15, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: William A. Slusarchyk, Tamara Dejneka
  • Patent number: 4692455
    Abstract: Compounds of the formula ##STR1## wherein Y is oxygen or sulfur are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of R.sub.1 may also be useful as analgesics due to their enkepahlinase inhibition activity.
    Type: Grant
    Filed: January 25, 1985
    Date of Patent: September 8, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Eric M. Gordon
  • Patent number: 4689414
    Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3 or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;R.sub.5 is hydrogen, alkyl, aryl, arylalkyl, cyano, nitro, ##STR2## Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl-(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl-(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR3## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR4## amino, or substituted amino; m is 0 or an integer of 1 to 6;n is an integer of 1 to 6; andp is an integer of 2 to 6.
    Type: Grant
    Filed: February 24, 1986
    Date of Patent: August 25, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4687865
    Abstract: A process is provided for preparing a 7-oxabicycloheptane amino alcohol intermediate of the general structure ##STR1## (wherein the above structures represents (D) or (L) isomers) which is useful in preparing thromboxane A.sub.2 receptor antagonists. This intermediate is prepared by reacting mesoanhydride with an aryl amine ##STR2## wherein R is alkyl, CH.sub.2 OH, CO.sub.2 H or CO.sub.2 alkyl, to form the acid ##STR3## which is reduced by treatment with lithium aluminum hydride or diisobutylaluminum hydride or Red-Al to form the alcohol ##STR4## wherein R.sup.1 is CH.sub.2 OH when R is CO.sub.2 H, CO.sub.2 alkyl or CH.sub.2 OH, and R.sup.1 is alkyl when R is alkyl; where in the above alcohol R.sup.1 is CH.sub.2 OH, such alcohol compound is treated with an alkyl chloroformate in the presence of base such as an alkali metal alkoxide to form the alcohol ##STR5## which undergoes cleavage by treatment with alkali metal, ammonia and acid to form the amino alcohol intermediate.Where in the above alcohol R.sup.
    Type: Grant
    Filed: June 4, 1986
    Date of Patent: August 18, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: John K. Thottathil
  • Patent number: 4685990
    Abstract: An ostomy device comprises an ostomy bag with a first coupling member attached thereto. A second coupling member for mating engagement with the first is attached to an adhesive backed label for adhering to the skin of the wearer around a stoma by a flexible mounting member comprising first and second sections coupled together at an inner peripheral region defining a stoma aperture therein. The second coupling member is attached to the first section at an outer peripheral region spaced apart from the inner peripheral region by hot melt adhesive while the second section is attached to the label at an outer peripheral region spaced apart from the inner peripheral region. The second section is attached by hot melt adhesive.
    Type: Grant
    Filed: September 29, 1986
    Date of Patent: August 11, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Keith T. Ferguson
  • Patent number: 4686299
    Abstract: Aerocavin, a novel antibiotic substance having the structure ##STR1## and aerocyanidin, a novel antibiotic substance having the structure ##STR2## can be prepared by cultivation of the microorganism Aerocavin caviae SC 14,030 A.T.C.C. No. 53434.
    Type: Grant
    Filed: July 14, 1986
    Date of Patent: August 11, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Wen-Chih Liu, William L. Parker, Pushpa Singh, Richard B. Sykes
  • Patent number: 4686298
    Abstract: Compounds of the formula ##STR1## are useful in the preparation of .alpha.-acyloxy phosphonate compounds. The final products are useful as anti-hypertensive agents due to their angiotensin converting enzyme inhibition activity.
    Type: Grant
    Filed: February 4, 1987
    Date of Patent: August 11, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Donald S. Karanewsky, Tamara Dejneka