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Attorney: Daignault; Ronald a.


Number of patents: 161
Last date: January 10, 1984

1          
NumberTitleIssue Date
53128212-heterocyclic-5-hydroxy-1,3-pyrimidines useful as antiinflammatory agents
The present invention is novel compounds which are 2-heterocyclic-4,6-ditertiarybutyl-5-hydroxy-1,3-pyrimidines, where heterocyclic is selected from imidazole, thiazole, and oxazole, and pharmaceutically acceptable additional salts, bases, and base salts ...
05/17/1994
5306822Arylmethylenyl derivatives of oxazolidinone
The present invention is for selected novel compounds, as well as, pharmaceutical compositions and methods of use for known and the selected novel compounds both of the formula ##STR1## having activity useful for treating allergies and inflammation....
04/26/1994
5278317Optically pure R-enantiomer of alpha,alpha-dilower alkyl-pyrrolidine-3-methane amines
Optically pure isomers of 7-[3-(1,1-dialkylmethyl-1-amino)-1-pyrrolidinyl]quinolones and naphthyridones as therapeutically active and safe antibacterial agents are described, as well as pharmaceutical compositions thereof, and a method of treating ba...
01/11/1994
5273995[R-(R*R*)]-2-(4-fluorophenyl)-ଲ,δ-dihydroxy-5-( 1-methylethyl-3-phenyl-4-[(phenylamino) carbonyl]- 1H-pyrrole-1-heptanoic acid, its lactone form and salts thereof
[R-(R*,R*)]-2-(4-fluorophenyl)-ଲ,δ-dihydroxy-5-((1-methylethyl)- 3-phenyl-4-[(phenylamino)-carbonyl]-1H-pyrrole-1-heptanoic acid or (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl-N,4-diphenyl-1-[2-(tetrahyd ro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-...
12/28/1993
5274002Trisubstituted phenyl analogs having activity for congestive heart failure
Novel trisubstituted phenyl analogs are now found to have activity as for the treatment of congestive heart failure....
12/28/1993
52703195-hydroxy-2-pyrimidinylmethylene derivatives useful as antiinflammatory agents
The present invention is novel compounds which are 5-hydroxy-2-pyrimidinylmethylene derivatives and pharmaceutically acceptable addition salts, bases, and base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds...
12/14/1993
5258528Individual stereoisomers of pyrrolidine methanamines substituted on the ring nitrogen by a 1-phenylethyl group
Individual stereoisomers of 7-[3-(1-aminoalkyl)-1-pyrrolidinyl]-quinolones and naphthyridones are described, their therapeutic advantages as antibacterial agents, as well as a novel method for the preparation and isolation of such stereoisomers....
11/02/1993
5256662Quinolinecarboxylic acid antibacterial agents
Novel 8-alkenyl, alkynyl, allenyl and cycloalkyl-quinolinecarboxylic acids are described as antibacterial agents as well as methods of manufacture including novel intermediates used in said manufacture....
10/26/1993
5250704Process for the manufacture of (S)-3-amino-1-substituted-pyrrolidines
A novel process for preparing a stereospecific (S)-3-amino-1-substituted pyrrolidine used as a key intermediate in preparing quinolone and naphthyridone antibacterial agents where the 7-position is occupied with a sterospecific 3-aminopyrrolidine side cha...
10/05/1993
52486822-substituted-4,6-di-tertiary-butyl-5-hydroxy-1,3-pyrimidines useful as antiinflammatory agents
The present invention is novel compounds which are 2-substituted-4,6-di-tertiarybutyl-5-hydroxy-1,3-pyrimidines and pharmaceutically acceptable acid addition or base salts thereof, pharmaceutical compositions and methods of use therefor. The invention ...
09/28/1993
52409292-heterocyclic-5-hydroxy-1,3-pyrimidines useful as antiinflammatory agents
The present invention is novel compounds which are 2-heterocyclic-4,6-ditertiarybutyl-5-hydroxy-1,3-pyrimidines, where heterocyclic is selected from imidazole, thiazole, and oxazole, and pharmaceutically acceptable additional salts, bases, and base salts ...
08/31/1993
5239082Sulfonamide tetrazole ACAT inhibitors
Pharmaceutically useful compounds having ACAT inhibitory activity of the formula ##STR1## wherein R1 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, a heteroaromatic group or a hydrocarbon group having from 1 to 18 carb...
08/24/1993
52369269-substituted-8-halo or -8-hydroxy-9-deazaguanines as inhibitors or PNP for pharmaceutical compositions
The present invention is novel 9-substituted-8-hydroxy or -8-halo-9 deazaguanines and pharmaceutical compositions and methods of use therefor. The derivatives are inhibitors of purine nucleoside phosphorylase selectively cytotoxic to T-cells but not to B-...
08/17/1993
5232950Method for using ketamine for prevention or reduction of the effects of stroke in a subject having increased risk for stroke
The present invention is a method of use for the prevention or reduction of the effects of stroke in a subject susceptible to or at risk of stroke with ketamine. The method also includes combination of ketamine and a benzodiazepine in the use....
08/03/1993
52216767-substituted quinolones and naphthyridones as antibacterial agents
7-Substituted quinolones and naphthyridones are described as antibacterial agents as well as a process for their manufacture, compositions therefor, wherein the 7-substituent is a pyrrolidine ring substituted at the 3-position by a substituted aromatic hy...
06/22/1993
52200252-substituted amino-4, 6-di-tertiary-butyl-5-hydroxy-1, 3-pyrimidines as antiinflammatory agents
The present invention is novel compounds which are 2-substituted amino-4,6-di-tertiarybutyl-5-hydroxy-1,3-pyrimidines and pharmaceutically acceptable acid addition or base salts thereof, pharmaceutical compositions and methods of use therefor. The inventi...
06/15/1993
5218090EGF receptor truncates
The present invention is for EGF receptor truncates which retain the activity of ligand binding for the EGF receptor. The specific truncates include LD1 D2 D3.Apa L encompassing amino acids Met-24 to Val505...
06/08/1993
52159865-hydroxy-2-pyrimidinylmethylene oxaza heterocycles
Novel 5, 6, or 7 membered oxaza heterocycles substituted at the 4-carbon by a 5-hydroxypyrimidinylmethylene group inhibitors of 5-lipoxygenase and/or cyclooxygenase and are thus useful in treating inflammatory diseases are described as well as pharmaceuti...
06/01/1993
5212189Thiadiazole or oxadiazole analogs of fenamic acids containing substituted hydroxamate side chains as antiinflammatory agents
The present invention is a novel compound which is a thiadiazole or oxadiazole analog of a fenamic acid having a substituted hydroxamate side chain and pharmaceutically acceptable acid addition or base salts thereof, pharmaceutical compositions and method...
05/18/1993
5210204Biphenyl oxadiazoles and thiadiazoles as angiothesin II antagonists
Heterocyclic methyl derivatives of biphenyl oxadiazoles and thiadiazoles are described, as well as methods for the preparation of said derivatives and pharmaceutical compositions of the same, which are useful as antagonists of the angiotensin II enzyme an...
05/11/1993
52082533-alkyloxy-, aryloxy-, or arylalkyloxy-benzo(b) thiophene-2-carboxamides as inhibitors of cell adhesion
3-Alkyloxy-, aryloxy-, or arylalkyloxy-benzo[b]thiophene-2-carboxamides are described as agents which block leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases. Certain of these com...
05/04/1993
5208225Compositions containing fixed combinations
Continuous administration of compositions containing a fixed quantity of synthetic estrogen in combination with a synthetic progestogenic agent are useful to relieve menopausal symptoms, to prevent osteoporosis and for other hormone-replacement treatments...
05/04/1993
5198466Oxysulfonyl urea ACAT inhibitors
Novel compounds of the formula ##STR1## wherein R is hydrogen, a straight or branched alkyl group having from 1 to 8 carbon atoms or benzyl; wherein each of R1 and R2 is hydrogen, an aralkyl group, a straight or branched hydroca...
03/30/1993
51964312-substituted amino-4, 6-di-tertiary-buthyl-5-hydroxy-1, 3-pyrimidines as antiinflammatory agents
The present invention is novel compounds which are 2-substituted amino-4,6-di-tertiarybutyl-5-hydroxy-1,3-pyrimidines and pharmaceutically acceptable acid addition or base salts thereof, pharmaceutical compositions and methods of use therefor. The inventi...
03/23/1993
5192792Isatine derivatives, and their method of use
A method of treatment of central nervous system disorders with compounds having the formula ##STR1## and isomers thereof wherein R1, R2, R4, R5, R6, and R7 and as defined in the specif...
03/09/1993
5189058Iminodicarbonic, iminodicarbonodithioic, and thiocarbonylcarbamic acid esters useful as ACAT inhibitors
The compounds of the present invention have the formula ##STR1## wherein each of X and Y is oxygen or sulfur, R is hydrogen or lower alkyl, and each of R1 and R2 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, ara...
02/23/1993
51871752-carbonyl substituted-5-hydroxy-1, 3-pyrimidines as antiinflammatory agents
The present invention is novel compounds which are 2-carbonyl substituted-5-hydroxy-1,3-pyrimidines and pharmaceutically acceptable acid addition or base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are n...
02/16/1993
51853583-heteroatom containing urea and thiourea ACAT inhibitors
Compounds useful in treating hypercholesterolemia and atherosclerosis having the formula ##STR1## wherein X is oxygen or sulfur, Het is a monocyclic heterocyclic group having three hetero atoms selected from nitrogen, oxygen and sulfur, and R
02/09/1993
5185349Substituted amide ACAT inhibitors lactone derivatives
Novel lactone and lactam compounds which are useful to lower blood cholesterol levels in a patient, said compounds containing an arylcarboxamide or arylthiocarboxamide moiety....
02/09/1993
5177217Process for the manufacture of (S)-3-amino-1-substituted-pyrrolidines
A novel process for preparing a stereospecific (S)-3-amino-1-substituted pyrrolidine used as a key intermediate in preparing quinolone and naphthyridone antibacterial agents where the 7-position is occupied with a sterospecific 3-amino-pyrrolidine side ch...
01/05/1993
5175153Substituted alpha-amino acids having pharmaceutical activity
The present invention is novel substituted ଱-amino acids, pharmaceutical compositions, method of use, and preparations therefore having utility for treating disorders which benefit from blockade of aspartate and glutamate receptors....
12/29/1992
5175356Quinolinecarboxylic acid antibacterial agents
Novel 8-alkenyl, alkynyl, allenyl and cycloalkyl-quinolinecarboxylic acids are described as antibacterial agents as well as methods of manufacture including novel intermediates used in said manufacture....
12/29/1992
5157128Certain optically active substituted ଱,଱-dialkyl-pyrrolidine-3-methamines useful as intermediates
Optically pure isomers of 7-[3-(1,1-dialkylmethyl-1-amino)-1 -pyrrolidinyl[quinolones and naphthyridones as therapeutically active and safe antibacterial agents are described, as well as pharmaceutical compositions thereof, and a method of treating bacter...
10/20/1992
5151355Process for the production of high purity thrombin
A liquid thrombin preparation is prepared by reacting a unit of prothrombin with less than 5 units of thromboplastin in the presence of calcium, contacting the resultant thrombin with a phosphate buffer, and diluting and filtering the suspension. The filt...
09/29/1992
5116834Quinolinecarboxylic acid antibacterial agents
Novel 8-alkenyl, alkynyl, allenyl and cycloalkyl-quinolinecarboxylic acids are described as antibacterial agents as well as methods of manufacture including novel intermediates used in said manufacture....
05/26/1992
51149581,2,4-oxadiazole and 1,2,4-thiadiazole derivatives of fenamates as antiinflammatory agents
1,2,4-Oxadiazole and 1,2,4-thiadiazole derivatives of the fenamic acids, in which the fenamate residue is present at the 3-position of the 1,2,4-oxadiazole or 1,2,4-thiadiazole, pharmaceutically acceptable acid addition or base salts and methods of prepar...
05/19/1992
5112868Hydroxamate derivatives of selected nonsteroidal antiinflammatory acyl residues having cyclooxygenase and 5-lipoxygenase inhibition
The present invention is novel selected hydroxamic acid derivatives of acyl residues of selected NSAIDS, i.e. having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by th...
05/12/1992
5112846N-hydroxyamide, N-hydroxythioamide, hydroxyurea, and N-hydroxythiourea derivatives of selected nsaids as antiinflammatory agents
The present invention includes N-hydroxyamide, N-hydroxyurea, N-hydroxythioamide, and N-hydroxythiourea derivatives of fenamates, indomethacin, cicloprofen, oxepinac, and indoprofen as dual inhibitors or selective inhibitors of cyclooxygenase and 5-lipoxy...
05/12/1992
5074426Dividable capsule
A capsule which is dividable into accurate individual dosage units by the user is comprised of first and second capsule units, each being cylindrical about a longitudinal axis along the major part of its length. The capsule units are detachably joined in ...
12/24/1991
5072001Certain optically active substituted 3-pyrraidine acetic acid derivatives useful as intermediates
Optically pure isomers of 7-[3-(1,1-dialkylmethyl-1-amino)-1-pyrrolidinyl]quinolones and naphthyridones as therapeutically active and safe antibacterial agents are described, as well as pharmaceutical compositions thereof, and a method of treating ba...
12/10/1991
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