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E. R. Squibb & Sons, Inc. Patents
Assignee:
E. R. Squibb & Sons, Inc.
Address:
Princeton, NJ
No. of patents:
1537
Patents:












Patent Number Title Of Patent Date Issued
5237095 Process for the preparation of an antiviral agent August 17, 1993
Racemic Feist's acid is treated with (R)-(+)-.alpha.-methylbenzylamine to yield (1R-trans)-3-methylenecyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzylamine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl es
5236932 Method for treating Parkinson's disease employing quinine August 17, 1993
A method is provided for treatment of Parkinson's disease or controlling movement of a Parkinsonian patient by administering an ATP-sensitive potassium channel blocker, such as a sulfonyl urea, (for example, tolbutamide), or quinine.
5236916 Oxadiazinone substituted indole and benzimidazole derivatives August 17, 1993
Novel compounds having the formula ##STR1## wherein X, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
5234923 Substitute indole and benzimidazole derivatives August 10, 1993
Novel compounds are disclosed having the formula ##STR1## or its isomer ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and X are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as
5233086 Intermediates for the preparation of an antiviral agent August 3, 1993
Racemic Feist's acid is treated with (R)-(+)-.alpha.-methylbenzylamine to yield (1R-trans)-3-methylene-cyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzylamine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl e
5233076 Process for preparing an optically active cyclobutanone, an intermediate in the synthesis of an August 3, 1993
A novel process and intermediates are disclosed for the preparation of the optically active compound ##STR1## wherein R.sup.3 is a protecting group. This cyclobutanone compound is used to prepare a compound of the formula ##STR2## having anti-viral activity.
5232453 Catheter holder August 3, 1993
A catheter holder has a pad of medical grade adhesive material having one surface for attachment to the skin of a wearer, and a pair of tapes secured to and extending from the other surface of the pad. A multiple use adhesive is placed on a surface of at least one tape which surface face
5226564 Manufacture of bags July 13, 1993
A synthetic plastic bag for containing liquids, e.g., urine, has a plastic outlet tube. It is manufactured by a first step of seam welding the tube between two superposed bag walls. In a subsequent step, an encircling sleeve is slide over the tube to a position where it contains within i
5225408 Biphenyl oxadiazinone angiotensin II inhibitors July 6, 1993
Angiotension II inhibition is exhibited by ##STR1## wherein: R.sup.1 and R.sup.2 are each independently hydrogen, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, thiophenalkyl, pyridylalkyl, or --R.sup.8 CO.sub.2 R.sup.9 ;R.sup.3 is a single bond, --S--, or --O--;R.sup.4 is hydrog
5225401 Treatment of congestive heart failure July 6, 1993
Congestive heart failure is treated by administration of a selective inhibitor of neutral endopeptidase and an angiotensin converting enzyme inhibitor. Captopril, fosinopril sodium, enalapril maleate and lisinopril are the preferred angiotensin converting enzyme inhibitors and the me
5225202 Enteric coated pharmaceutical compositions July 6, 1993
An enteric coated pharmaceutical composition is provided which includes a medicament which is sensitive to a low pH environment of less than 3, such as pravastatin, which composition is preferably in the form of pellets which includes an enteric coating formed of neutralized hydroxyp
5224935 Catheter retainer July 6, 1993
A catheter retainer is disclosed that includes an adhesive pad with projections. The catheter is secured to the pad by being tied to the projections.
5223516 3,3,3-trifluoro-2-mercaptomethyl-N-tetrazolyl substituted propanamides and method of using same June 29, 1993
Compounds of the formula ##STR1## wherein Y can be tetrazolyl are disclosed. These compounds are useful as cardiovascular agents.
5218142 Process for the preparation of an antiviral agent June 8, 1993
Racemic Feist's acid is treated with (R)-(+)-.alpha.-methylbenzylamine to yield (1R-trans)-3-methylenecyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzylamine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl es
5217958 1,2-hydroxy phosphonates and derivatives thereof June 8, 1993
Compounds of the formula ##STR1## are disclosed. These compounds are inhibitors of renin and therefore useful as cardiovascular agents.
5215985 Method for treating ischemic insult to neurons employing an ATP-sensitive potassium channel bloc June 1, 1993
A method is provided for treatment of neuronal insult, such as caused by lack of oxygen, by administering an ATP-sensitive potassium channel blocker, such as a sulfonyl urea, for example, tolbutamide.
5212177 Indole and benzimidazole-substituted dihydropyrimidine derivatives May 18, 1993
Novel compounds having the formula ##STR1## and its isomer ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and X are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, an antihypertens
5212165 Method for rehabilitating the vasorelaxant action of the coronary arteries impaired through athe May 18, 1993
A method is provided for rehabilitating or restoring the vasorelaxant action of the endothelium impaired by atherosclerosis and/or hypercholesterolemia, thereby preventing arteriospasm in the coronary arteries using an angiotensin converting enzyme inhibitor such as captopril, fosino
5212164 Phosphorus-containing squalene synthetase inhibitors May 18, 1993
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 m is 0, 1, 2 or 3; n is 0, 1, 2, 3 or
5210262 Method for preparing a phosphonic acid ester May 11, 1993
A method is provided for preparing a phosphonic acid ester having the structure ##STR1## wherein R.sup.1 is farnesyl or a derivative or analog thereof, and R.sup.2 is lower alkyl, by treating a farnesyl halide R.sup.1 Hal(Hal=Cl,Br,I) with an alkoxide of the structure ##STR2#
5208235 Indole- and benzimidazole-substituted imidazole derivatives May 4, 1993
Novel compounds having the formula ##STR1## where X R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore for example, as antihypertensive agents.
5208234 Substituted imidazole phosphonic and phosphinic acid derivatives May 4, 1993
Novel compounds having the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
5206244 Hydroxymethyl (methylenecyclopentyl) purines and pyrimidines April 27, 1993
Antiviral activity is exhibited by compounds having the formula ##STR1## and its pharmaceutically acceptable salts.
5202486 Tetrahydroethanonaphthaleneamine derivatives April 13, 1993
Tetrahydronaphthaleneamine derivatives having the formula ##STR1## wherein R, R', R.sub.1 and R.sub.2 are as defined herein, are novel calcium channel blockers.
5202330 2-thio or oxo-4-aryl or heterocyclo-1,5(2H)-pyrimidinedicarboxylic acid diesters and 3-acyl-5-py April 13, 1993
Pyrimidine compounds of the formula ##STR1## wherein X is sulfur or oxygen, Y is R.sub.11 or --O--R.sub.1, and R.sub.4 is aryl or heterocyclo are disclosed. These compounds are useful as cardiovascular agents, particularly anti-hypertensive agents, due to their calcium entry bloc
5202327 Phosphorus-containing HMG-CoA reductase inhibitors April 13, 1993
Novel phosphorus-containing compounds which inhibit the activity of HMG-CoA reductase, including a 5-pyrimidinyl-containing moiety. Pharmaceutical compositions and methods of use for the treatment or prevention of hypercholesterolemia, atheroschlerosis, hyperlipoproteinaemia and hype
5200324 Method of diagnosing senile dementia of the Alzheimer type April 6, 1993
A method is provided for the screening of senile dementia of the Alzheimer type (Alzheimer's disease) by testing for an anomalous molecular form of acetylcholinesterase in cerebrospinal fluid of a patient.
5198583 Optically active cyclobutane nucleoside and intermediates, therefor March 30, 1993
The optically active antiviral compound [1R-(1.alpha., 2.beta., 3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)-cyclobutyl]-1,9-dihydro-6H-pu rin-6-one and novel intermediates useful in its preparation are described.
5194634 Dihydroxyheptanoic acids containing an oxabicycloheptane nucleus useful as antihypercholesterole March 16, 1993
Dihydroxyheptanoic acids containing an oxabicyloheptane nucleus are provided which have the structure ##STR1## including all stereoisomers thereof, wherein Z is ##STR2## and X, R.sub.1, R.sub.2 and R.sub.3 are as defined herein.
5194604 Process and intermediates for beta-lactams having aminothiazole(iminooxyacetic acid)acetic acid March 16, 1993
Disclosed herein are processes for preparing a compound of the formula ##STR1## in which a novel compound of the formula ##STR2## is reacted with a beta lactam of the formula ##STR3## by treatment with a base, wherein the symbols are as defined in the specification.
5191086 Imidazole and benzimidazole derivatives March 2, 1993
Novel angiotensin-II receptor antagonists are disclosed having the general formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, W and X are as defined herein.
5190970 Method for preventing onset of or treating Type II diabetes employing a cholesterol lowering dru March 2, 1993
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 combintion with an ACE inhibitor, such as captopril, zofenopril, ceranapril, fosinopril, enalapril or lisinopril.
5190942 Benzoxazole and related heterocyclic substituted imidazole and benzimidazole derivatives March 2, 1993
Novel compounds are disclosed having the formula ##STR1## wherein X, Y, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
5189180 Seco-mevinic acid derivatives useful as antihypercholesterolemic agents and new intermediates February 23, 1993
Seco-mevinic acid derivatives are provided which have the structure ##STR1## including all stereoisomers thereof, wherein Z is ##STR2## R is H, alkali metal or lower alkyl, R.sup.1 is H, lower alkyl, aryl, lower alkoxy, cycloalkyl, heteroaryl, aralkyl, heteroaralkyl or hetero
5187290 Acylaminoalkanoyl urethanes or thiourethanes February 16, 1993
Compounds of the formula ##STR1## wherein Z is oxygen or sulfur are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inbitition activity and depending upon the definition of X may also be useful as analgesics due to their enke
5185463 Process for the preparation of an antiviral agent February 9, 1993
Racemic Feist's acid is treated with (R)-(+)-.alpha.-methylbenzylamine to yield (1R-trans)-3-methylenecyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzylamine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl es
5185459 Bis protected (hydroxymethyl)cyclobutanols February 9, 1993
Cyclobutanols of the formula ##STR1## wherein P is a hydroxy protecting group are useful intermediates in the preparation of antiviral compounds.
5185248 Farnesyl-protein transferase assay for identifying compounds that block neoplastic transformatio February 9, 1993
Assays for farnesyl-protein transferase (FT) which can be used to identify substances that block the farnesylation of ras oncogene products are described. Because farnesylation is required for ras oncogene activity, inhibitory compounds identified in the assays of the invention can block
5183653 Boronic acid adducts of metal dioxime complexes useful in labelling proteins and other amine-con February 2, 1993
Boronic acid adducts of metal dioxime complexes are useful as reagents for labeling proteins and other amine-containing compounds.
5180589 Pravastatin pharmaceuatical compositions having good stability January 19, 1993
A pharmaceutical composition is provided which has excellent stability, when dispersed in water has a pH of at least about 9, and includes a medicament which is sensitive to a low pH environment such as pravastatin, one or more fillers such as lactose and/or microcrystalline cellulose, o
5178615 Ostomy bag coupling January 12, 1993
An ostomy bag coupling appliance has body side and bag side couplings each including a seal means. The bag side coupling includes one ring like member carrying the seal means associated with a locking ring which can be rotated relative to the member. The locking ring and the body side
5177239 Method for preparing a phosphonic acid ester January 5, 1993
A method is provided for preparing a phosphonic acid ester having the structure ##STR1## wherein R.sup.1 is farnesyl or a derivative or analog thereof, and R.sup.2 is lower alkyl, by treating a farnesyl halide R.sup.1 Hal(Hal.dbd.Cl,Br,I) with an alkoxide of the structure ##S
5177104 6-.alpha.-hydroxy derivatives of mevinic acids January 5, 1993
Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof have been found to possess activity as cell-selective HMG-CoA reductase inhibitors, thus making them useful as antihypercholesterolemic agents. In the above formula, ##STR2## R.sup.1 is hydrogen,
5177097 Acyl amidine and acyl, guanidine substituted biphenyl derivatives January 5, 1993
Novel compounds are disclosed having the formula ##STR1## and wherein R.sub.1, R.sub.2 and R.sub.3 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
5177006 Enzymatic resolution process January 5, 1993
A novel enzymatic resolution process for preparing resolved compounds of the formula ##STR1## with improved yields and high optical purity is disclosed. Compounds of formula I' are useful, for example, as intermediates for the preparation of physiologically active compounds, e.g.
5173487 Mevinic acid derivatives December 22, 1992
Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, is exhibited by a compound of the formula ##STR1## m is 0 to 3; R is selected from:(1) alkyl;(2) substituted alkyl;(3) alkoxy;(4) alkenyl;(5) cycloalkyl;(6) phenyl; and(7) substituted aryl; andR.sup.1
5169638 Buoyant controlled release powder formulation December 8, 1992
A buoyant controlled release pharmaceutical powder formulation is provided which may be filled into capsules and releases a pharmaceutical of a basic character at a controlled rate regardless of the pH of the environment, which formulation includes a basic pharmaceutical, up to about 45%
5167639 Catheter attachment device December 1, 1992
A catheter attachment device comprises a first pad of medical grade adhesive having one surface covered by a removable protective layer, a second surface covered by a plastics film, and, attached to the film, a second pad of medical grade adhesive. A surface of this second pad which
5166386 Process of making isoprenoid phosphinylformic acid squalene synthetase inhibitors November 24, 1992
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 o
5166364 Mevinic acid derivatives useful as antihypercholesterolemic agents and method for preparing same November 24, 1992
Mevinic acid derivatives are provided which are 6-hydroxy-8-(2,2-dimethyl-1-oxybutoxy- 2-methyl)-substituted-decahydronaphthalene 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 reduct

 
 
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