Patents Assigned to E. R. Squibb & Sons
  • Method for preventing onset of restenosis after angioplasty employing pravastatin
    Patent number: 5140012
    Abstract: A method is provided for preventing or reducing the risk of restenosis following angioplasty by administering pravastatin alone or in combination with an ACE inhibitor such as captopril or ceranapril, prior to, during and/or after angioplasty.
    Type: Grant
    Filed: May 31, 1990
    Date of Patent: August 18, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Mark E. McGovern, Miguel A. Ondetti, Henry Y. Pan
  • Pyranyl cyanoguanidine derivatives
    Patent number: 5140031
    Abstract: Novel compounds having the formula ##STR1## wherein ##STR2## are disclosed. These compounds have potassium channel activating activity and are useful, for example, as cardiovascular agents, especially as antiischemic agents.
    Type: Grant
    Filed: February 27, 1991
    Date of Patent: August 18, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Karnail Atwal, Gary J. Grover, Kyoung S. Kim
  • Tablet composition and method for problem pharmaceutical materials using citric acid
    Patent number: 5137730
    Abstract: In accordance with the present invention an improved tablet composition for drugs or active ingredients prone to poor tabletting properties is disclosed. The improved composition comprises a premixture, consisting essentially of between about 85 and 99.9 percent by weight of the active ingredient and between about 0.1 and 15 percent by weight of citric acid, and one or more other formulation ingredients added to premixture. The present invention also involves the process for making such compositions and products therefrom.
    Type: Grant
    Filed: May 28, 1991
    Date of Patent: August 11, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Andrew B. Dennis, Peter Timmins, Himadri Sen
  • Heterocyclic ketone prostaglandin analogs
    Patent number: 5135939
    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.sup.1 is hydrogen, alkyl, alkenyl, alkynyl, aralkyl, aryl cycloalkyl, cycloalkylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl, heteroaryl or heteroarylalkyl, each of R.sup.1 being unsubstituted or optionally substituted with alkyl, aryl, cycloalkyl, or cycloalkylalkyl;R.sup.2 is CO.sub.2 R CONHSO.sub.2 R.sup.3, CONHR.sup.4 ;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 O;Z is --CH.dbd.CH--, --(CH.sub.2).sub.2 --, or ##STR2## and the remaining symbols are as defined in the specification.
    Type: Grant
    Filed: January 28, 1991
    Date of Patent: August 4, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Raj N. Misra
  • Cyclobutane derivatives
    Patent number: 5130462
    Abstract: Cyclobutane derivatives of the formulas ##STR1## wherein P is a hydroxy protecting group and X is a leaving group are useful intermediates in the preparation of antiviral compounds.
    Type: Grant
    Filed: February 19, 1991
    Date of Patent: July 14, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: William A. Slusarchyk, Robert Zahler
  • Method for treating type II diabetes employing a cholesterol lowering drug
    Patent number: 5130333
    Abstract: A method is provided for preventing or reducing the risk of or treating Type II diabetes by administering a cholesterol lowering drug, such as pravastatin, alone or in combination with an ACE inhibitor, such as captopril, zofenopril, ceranapril, fosinopril, enalapril or lisinopril.
    Type: Grant
    Filed: October 19, 1990
    Date of Patent: July 14, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Henry Y. Pan, Michael Bergman
  • Enzymatic resolution process hydrolyzing thio-ester
    Patent number: 5128263
    Abstract: A novel enzymatic resolution process for preparing resolved compounds of the formula ##STR1## with improved yields and high optical purity is disclosed. The thioester bond of the compound is hydrolyzed and the hydrolyzed compound is separated from the unhydrolyzed. Compounds of formula I' are useful, for example, as intermediates for the preparation of physiologically active compounds, e.g. captopril and zofenopril.
    Type: Grant
    Filed: October 25, 1989
    Date of Patent: July 7, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jeffrey M. Howell, Ramesh N. Patel, Laszlo J. Szarka
  • Anti-thrombotic heterocyclic amido prostaglandin analogs
    Patent number: 5126370
    Abstract: Prostaglandin analogs useful in treating thrombotic and vasospastic disease having the structural formula ##STR1## wherein: m is 1, 2 or 3:n is 1, 2 or 3, except that n is O when Y is vinylene;p is 1, 2 or 3;R is CO.sub.2 R', CH.sub.2 OH, CONHSO.sub.2 R.sup.3, CONHR.sup.4, or --CH.sub.2 -5-tetrazolyl;R' is hydrogen, alkyl, or alkali metal;Y is --O--, a single bond or vinylene, except that Y cannot be --O-- when n is 0;and the remaining symbols are as defined in the specification.
    Type: Grant
    Filed: December 24, 1990
    Date of Patent: June 30, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Raj N. Misra
  • Bis (hydroxymethyl) cyclobutyl triazolopyrimidines
    Patent number: 5126345
    Abstract: Antiviral activity is exhibited by compounds having the formula ##STR1## and its pharmaceutically acceptable salts wherein R.sub.1 is ##STR2## R.sub.6 is hydrogen, alkyl, substituted alkyl, or aryl; and R.sub.7 and R.sub.
    Type: Grant
    Filed: February 8, 1991
    Date of Patent: June 30, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: William A. Slusarchyk, Robert Zahler
  • Process for preparing certain 5,6,7,8-tetrahydroindolizinyl (ethyl or ethynyl)-hydroxy or methoxy-phosphinyl-3-hydroxy-butanoates and derivatives thereof
    Patent number: 5124453
    Abstract: Compounds which are useful as inhibitors of cholesterol biosynthesis and thus as hypocholesterolemic agents are provided which have the structure ##STR1## including salts thereof, wherein R is OH, or lower alkoxy; R.sup.x is H or alkyl;X is --(CH.sub.2).sub.a -- (where a is 1, 2, or 3), --CH.dbd.CH--, or --C.tbd.C--.New intermediates used in preparing the above compounds, pharmaceutical compositions containing such compounds and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.
    Type: Grant
    Filed: January 28, 1991
    Date of Patent: June 23, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Donald S. Karanewsky
  • Selective inhibition of DNA polymerase
    Patent number: 5120639
    Abstract: Two peptides, P6 and P7, having the amino acid sequence APGDEPAPPY and AGATAEETRY have been used to obtain antibodies made against them, which antibodies specifically neutralize HSV-1 and HSV-2 DNA polymerase. The present invention also contemplates a method of screening for inhibitors of HSV-1 and HSV-2 polymerase utilizing the antibodies.
    Type: Grant
    Filed: April 3, 1989
    Date of Patent: June 9, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Mary L. Haffey, James T. Matthews
  • Rhenium tris dioxime complexes
    Patent number: 5118797
    Abstract: Rhenium tris dioxime complexes are useful in the synthesis of boronic acid adducts of rhenium dioxime complexes which are useful as radiotherapeutic agents.
    Type: Grant
    Filed: August 28, 1989
    Date of Patent: June 2, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Silvia Jurisson, Karen E. Linder, Lynn C. Francesconi
  • Pharmaceutical composition and method for treating cardiovascular diseases using substituted anilides and sulfonamides
    Patent number: 5116851
    Abstract: A novel pharmaceutical composition and method is disclosed for the treatment of cardiovascular diseases, e.g. myocardial ischemia and/or arrhythmia. The method and composition include an effective amount of a compound of the formula ##STR1## wherein X, Y, R, R.sub.1, A, A', m, n, p, p' and B are as defined herein.
    Type: Grant
    Filed: January 26, 1990
    Date of Patent: May 26, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: John Krapcho, James L. Bergey, Gary J. Grover
  • Monobactam hydrazide derivatives
    Patent number: 5112968
    Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof which possess antibacterial activity.R.sub.s is a substituted hydroxy pyridone of the formulae: ##STR2## wherein Y.sub.1 is CH.sub.2 X; COOR.sub.6 ; CONR.sub.7 R.sub.8 ; OH; OCH.sub.2 R.sub.9 ; CHF.sub.2 ; CHO; CH.dbd.N--OR.sub.10 ; CH.dbd.CH--R.sub.11 ; CN; CH.dbd.N--NHR.sub.12, and Y.sub.2 is hydrogen; COOH; CONH.sub.2 ; CN; CSNH.sub.2 ; COO lower alkyl; CONR.sub.7 /R.sub.8.
    Type: Grant
    Filed: July 28, 1989
    Date of Patent: May 12, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Uwe D. Treuner
  • Method for diagnosing senile dementia of the Alzheimer's type
    Patent number: 5109868
    Abstract: A method is provided for detecting senile dementia of the Alzheimer's type (SDAT) wherein atrophy of the medial temporal lobe of the brain (for example as determined by CT scan) as indicated by a thickness thereof, at its narrowest point, of 11.5 mm or less represents a positive finding of SDAT. In an extension of such method, atrophy of the medial temporal lobe as described above combined with reduced blood flow in the posterior parietal/superior temporal cortex (for example as determined by SPET), represents a positive finding of SDAT.
    Type: Grant
    Filed: March 18, 1991
    Date of Patent: May 5, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Anthony D. Smith, Kim A. Jobst
  • Geminally substituted thiaheterocyclic carboxylic acids and derivatives thereof
    Patent number: 5106991
    Abstract: Novel thromboxane receptor antagonists are disclosed, having the formula ##STR1## wherein: A is aryl, optionally substituted withhalogen,lower alkoxy,carboalkoxy,lower alkyl,alkylamino, orphenyl;R.sub.1 is COOH, COO--alkali metal (such as Na, K, or Li), COO--lower alkyl, CONHSO.sub.2 R.sub.2, or 5-tetrazolyl;R.sub.2 is lower alkyl or aryl;m is 0, 1, or 2; andp is 2, 3, 4, or 5.Also disclosed are novel intermediates of formula I compounds.
    Type: Grant
    Filed: July 27, 1990
    Date of Patent: April 21, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Philip M. Sher, Steven E. Hall
  • Isoprenoid phosphinylformic acid squalene synthetase inhibitors and method
    Patent number: 5107011
    Abstract: Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthesis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents, are provided which have the structure ##STR1## wherein R.sup.2 is a metal ion, lower alkyl or H; R.sup.3 is a metal ion or lower alkyl;R is R.sup.1 --(CH.sub.2).sub.n --, R.sup.1 --(CH.sub.2).sub.m --O-- or R.sup.1 --(CH.sub.2).sub.m --OCH.sub.2 --, wherein n is 1 to 4 and m is 0 to 3, andR.sup.1 is R.sup.5 --Q.sup.1 --Q.sup.2 --Q.sup.3 -- wherein R.sup.5, Q.sup.1, Q.sup.2 and Q.sup.3 are as defined herein.New intermediates, new methods of preparation and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.
    Type: Grant
    Filed: February 5, 1991
    Date of Patent: April 21, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Scott A. Biller
  • Intermediates for a process for making 2-oxo-1-[[(substituted sulfonyl)-amino]carbonyl]azetidines
    Patent number: 5106977
    Abstract: Novel intermediates for preparing 2-oxo-1-[[(substituted sulfonyl)-amino]carbonyl]azetidines are disclosed. These intermediates have the formula ##STR1## wherein Prot is as defined herein.
    Type: Grant
    Filed: September 27, 1990
    Date of Patent: April 21, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jollie D. Godfrey, Jr., Richard H. Mueller
  • Piperidinyl carbonyl derivatives
    Patent number: 5106982
    Abstract: Novel compounds having the general formula ##STR1## wherein A and A' are amino acid residues linked by a peptidal bond to the nucleus, are disclosed. These compounds are CNS agents with anxiogenic activity.
    Type: Grant
    Filed: December 10, 1990
    Date of Patent: April 21, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Callixtus E. Ita, Peter Egli
  • 3,5-dihydroxypentanoic acid derivatives useful as antihypercholesterolemic agents and method for preparing same
    Patent number: 5106992
    Abstract: 3,5-Dihydroxypentanoic acid derivatives are provided which are 6-hydroxy-8-(2,2-dimethyl-1-oxybutoxy-2-methyl)-substituted-thiazolidine derivatives and have the structure ##STR1## wherein Z is ##STR2## R.sup.6 is an alkali metal, lower alkyl or H; R.sup.1 and R.sup.2 are the same or different and are H, lower alkyl or aryl; X is S, O, ##STR3## or a single bond; R.sup.7 is lower alkyl; R.sup.3 is lower alkyl or aryl; R.sup.4 and R.sup.5 are the same or different and are H or lower alkyl; and --- represents a single bond or a double bond, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis, and also as antifungal agents.In addition, novel intermediates for use in preparing the above mevinic acid derivatives are also provided.
    Type: Grant
    Filed: April 30, 1990
    Date of Patent: April 21, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: David R. Magnin, Eric M. Gordon