Patents Assigned to E. R. Squibb & Sons, Inc.
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • Enzymatic process for enantiomer-specific perparation of mercapto alkanoic acid compounds
    Patent number: 5106736
    Abstract: An enzymatic process for the enantiomer-specific preparation of mercapto alkanoic acids by stereoselective hydrolysis of mercapto or thioester alkanoic acid esters.
    Type: Grant
    Filed: April 23, 1991
    Date of Patent: April 21, 1992
    Assignee: E.R. Squibb & Sons, Inc.
    Inventors: Ramesh N. Patel, Laszlo J. Szarka
  • 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
  • Dihydropyrimidine lactone derivatives
    Patent number: 5103006
    Abstract: Novel compounds of the formula ##STR1## wherein X is sulfur or oxygen, R.sub.2 is aryl or heterocyclo and R.sub.1 is as defined herein, are disclosed. Compounds of formula I possess calcium channel activating activity.
    Type: Grant
    Filed: August 21, 1990
    Date of Patent: April 7, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: George C. Rovnyak, Spencer D. Kimball
  • Process for preparing 3-alkenylidene-1,1-bisphosphonates
    Patent number: 5103036
    Abstract: A process is provided for preparing a 3-alkenylidene-1,1-bisphosphonate which is an intermediate for preparing an inhibitor of the enzyme squalene synthetase which is useful as an inhibitor of cholesterol biosynthesis, or which bisphosphonate itself is useful as an inhibitor of cholesterol biosynthesis. The process involves the palladium catalyzed coupling of an allylic ester with a tetraester of a methylenebisphosphonate to form a 3-alkenylidene-1,1-bisphosphonate containing an alkene moiety located .gamma., .delta. to the phosphonates.
    Type: Grant
    Filed: May 13, 1991
    Date of Patent: April 7, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: David R. Magnin, Richard B. Sulsky
  • Phosphonate substituted amino acids useful as antihypertensives
    Patent number: 5102875
    Abstract: Hypotensive activity is exhibited by new phosphonate substituted amino or imino acids of the formula ##STR1## isomeric mixtures thereof and pharmaceutically acceptable salts thereof, wherein:X is an imino or amino acid of the formula ##STR2##
    Type: Grant
    Filed: June 25, 1990
    Date of Patent: April 7, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Donald S. Karanewsky
  • 7-oxabicycloheptyl substituted heterocyclic amide or ester prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease
    Patent number: 5100889
    Abstract: 7-Oxabicycloheptane substituted prostaglandin analogs useful in treating thrombotic and vasopastic disease have the structural formula ##STR1## wherein m is 1, 2 or 3; n is 1, 2, 3 or 4; Z is --(CH.sub.2).sub.2 --, --CH.dbd.CH-- or ##STR2## wherein Y is O, a single bond or vinyl, with the proviso that when n is 0, if Z is ##STR3## then Y cannot be O, and Z is --CH.dbd.CH--, n is 1, 2, 3 or 4; and when Y=vinyl, n=0; R is CO.sub.2 H, CO.sub.2 lower alkyl, CH.sub.2 OH, CO.sub.2 alkali metal, CONHSOR.sup.3, CONHR.sup.3a or --CH.sub.2 --5-tetrazolyl, X is O, S or NH; and where R.sup.1, R.sup.2, R.sup.3 and R.sup.3a are as defined herein.
    Type: Grant
    Filed: June 18, 1990
    Date of Patent: March 31, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Raj N. Misra, Philip M. Sher, Philip D. Stein, Steven E. Hall, David Floyd, Joel C. Barrish
  • Mevinic acid derivatives useful as antihypercholesterolemic agents and method for preparing same
    Patent number: 5099035
    Abstract: Mevinic acid derivatives are provided which are 6-hydroxy-8-(2,2-dimethyl-1-oxybutoxy-2-methyl)-substituted-decahydronapht halene esters and have the structure ##STR1## wherein Z is ##STR2## wherein R is alkali metal such as Na, or H or lower alkyl, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis, and also as antifungal agents.In addition, a method for preparing the above-mevinic acid derivatives is also provided.
    Type: Grant
    Filed: March 1, 1991
    Date of Patent: March 24, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jeffrey O. Saunders, Eric M. Gordon
  • Diol sulfonamide and sulfinyl renin inhibitors
    Patent number: 5098924
    Abstract: Compounds of the formula ##STR1## wherein Z is SO or SO.sub.2 possess renin inhibition activity and are useful in treating hypertension and other diseases where the reduction of the levels of circulating angiotensin II are beneficial.
    Type: Grant
    Filed: September 15, 1989
    Date of Patent: March 24, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Michael A. Poss
  • Method for preventing or inhibiting loss of cognitive function employing a combination of an ace inhibitor and a drug that acts at serotonin receptors
    Patent number: 5098889
    Abstract: A method is provided for imhibiting loss of cognitive functon, including memory, which may or may not be associated with Alzheimer's disease, by administering an ACE inhibitor, such as captopril, fosinopril, zofenopril or ceranapril in combination with a drug that acts as serotonin receptors such as zacopride, over a prolonged period of treatment.
    Type: Grant
    Filed: September 17, 1990
    Date of Patent: March 24, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Brenda Costall, Zola P. Horovitz