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Attorney: Levy; David J.


Number of patents: 83
Last date: October 12, 1993

1      
NumberTitleIssue Date
5252560Cyclic imide derivatives, compositions and use
Compounds are described of the formula ##STR1## wherein: R1 is C3-6 alkyl or C1-3 alkylthioC1-3 alkyl; R2 is an optionally substituted C1-6 alkyl or C1-6 alkoxy group, aryl, hete...
10/12/1993
5233041Synthesis of a 3,4-dihydroxy-1-cyclopentanylpurinone from a 2,3-unsaturated-1-cyclopentanylpurinone
Synthesis of the triol of formula (I) or its amine-protected derivative from a cyclopentene of the formula (II) or its amine-protected derivative: ##STR1## via steps including oxidation to the aldehyde, migration of the double bond, reduction of the ...
08/03/1993
5174475Sequential dosing of antifungal and antiinflammatory compositions
A sequential dosing medicament for topical treatment of fungal infections comprising a first pharmaceutical composition having an antifungal agent and an antiinflammatory agent, e.g. a steroid, a second separate pharmaceutical composition having only an a...
12/29/1992
5136085Synthesis of 2-aminobenzophenones
Process for synthesizing 2-aminobenzophenones such as the following formula (I): ##STR1## wherein X1 and X2 are substituents and r and s are 1 or 2, by reacting an anthranilic acid amide e.g. an N-alkoxy-N-alkyl anthranilic ...
08/04/1992
5053543Synthesis of 2-aminobenzophenones
Process for synthesizing 2-aminobenzophenones such as the following formula (I): ##STR1## wherein X1 and X2 are substituents and r and s are 1 or 2, by reacting an anthranilic acid amide e.g. an N-alkoxy-N-alkyl anthranilic ...
10/01/1991
5053338Kinetic resolution of pyridazinones using lipase
A kinetic resolution of pyridazinones of the following formula (A): ##STR1## where R1 is alkyl by enzymatic hydrolysis results in good optical purity of the phenolic product. This is significant considering the distance in the molecule (A)...
10/01/1991
5051431Pyridone nitriles useful in treating cardiovascular disease
Pyridones of formula (I) for treating congestive heart failure: ##STR1## wherein: R1 and R2 are a variety of phenyl substituents, L is a divalent alkylene or amide containing alkylene linking group. Pharmaceutical composition, m...
09/24/1991
4851094Process for producing amidine sulfonic acid intermediates for guanidines
An efficient synthesis of quanidines, e.g. of the formula (III), by oxidizing a thiourea, e.g. of the following formula (II): ##STR1## with H2 O2 and a molybdenum catalyst to yield an aminoiminomethane sulfonic acid which can th...
07/25/1989
4837328Stereoselective reaction for hexahydro-6-arylpyrrolo(2,1-A) isoquinolines
A diastereoselective process for known antidepressive compounds (I) via reduction of the corresponding alcohol (VII): ##STR1## whereby the product mixture of diastereomers is surprisingly and unexpectedly rich in the content of the trans configuratio...
06/06/1989
4826848Antidepressive substituted N-[(4-piperidinyl)alkyl] bicyclic condensed oxazol- and thiazolamines
Novel substituted N-[(4-piperidinyl)alkyl] bicyclic condensed oxazol- and thiazolamines useful as anti-depressives, in the treatment of Parkinson's disease and in the treatment of diseases related with disturbed enterokinesia....
05/02/1989
4820822Novel N-(bicyclic heterocyclyl)-4-piperidinamines
Novel N-(bicyclic heterocyclyl)-4-piperidinamines having anti-histaminic and serotonin-antagonistic properties which are useful in the treatment of allergic diseases....
04/11/1989
48032183-aminoalkyl-1H-indole-5-urea and amide derivatives
Compounds useful as antihypertensive agents which are 3-aminoalkyl-1H-indole-5-urea or amide derivatives having the following formula: ##STR1## or a pharmaceutically acceptable acid addition salts thereof, wherein: R is C1-4 loweralky...
02/07/1989
4800207Hexahydropyrrolizine compounds useful as analgesics
Hexahydropyrrolizines of the formula (I): ##STR1## wherein A is a 3-7 carbon or hetero-containing ring, R1 is a substituent, and x is 0-3. Also, pharmaceutical compositions for treating pain and methods for synthesis and use as well as novel in...
01/24/1989
4798893Process for producing 1-(5-substituted-2-ethynylphenyl)-2-propanones
A method for the synthesis of the 2-propanone (I) is described starting from alkoxide (II) through the lactone (IV). ##STR1## Excellent control of the location of the substitution on the phenyl ring is achieved and the reaction proceeds in high yield...
01/17/1989
4792569Anticonvulsant phenethyl sulfamates
Sulfamates of the following formula (I) are anticonvulsants and are useful in the treatment of epilepsy: ##STR1## wherein R is one or more substituents such as alkyl, halo, alkoxy, CH3 or nitro; and x is 0-3....
12/20/1988
4783483Epoxides useful as antiallergic agents
Alkenes of the formula (I) and epoxides (II) used to make them are useful as anti-inflammatory and antiallergic pharmaceuticals: ##STR1## wherein R1 =H or CH3 ; R2 =phenyl, substituted phenyl, benzyl or a cysteinyl mo...
11/08/1988
4781866Process for producing amidine sulfonic acid intermediates for guanidines
An efficient synthesis of quanidines, e.g. of the formula (III), by oxidizing a thiourea, e.g. of the following formula (II): ##STR1## with H2 O2 and a molybdenum catalyst to yield an aminoiminomethane sulfonic acid which can th...
11/01/1988
47727551,2-1,4 addition reaction sequence leading to disubstituted acelylenes
A method for synthesizing a tri-substituted phenyl compound (I) by using a 1,2-addition followed by a 1,4-addition to 1,4-benzoquinone (II): ##STR1## wherein X is hydroxy, alkoxy or alkanoyloxy, Ar1 is an organic group and R is an unsubsti...
09/20/1988
47585633-alkoxy-2-aminopropyamines, cardiovascular compositions and use
Propylamines of the formula (I): ##STR1## and isomers thereof, particularly those enantiomers and racemates relative to the chiral carbon indicated by an asterisk (*). The propylamines can be used for the treatment of hypertension or angina in humans...
07/19/1988
4749702Antidepressive substituted N-[(4-piperidinyl)alkyl] bicyclic condensed oxazol- and thiazolamines
Novel substituted N-[(4-piperidinyl)alkyl] bicyclic condensed oxazol- and thiazolamines useful as anti-depressives, in the treatment of Parkinson's disease and in the treatment of diseases related with disturbed enterokinesia....
06/07/1988
4745185D-arabinose-1,5-diphosphate salts and methods for the treatment of diabetes
Novel D-arabinose-1,5-diphosphate salts of the formula (I): ##STR1## wherein n is from about 3 to 4 and M+ is a cation as well as racemic and isomeric mixtures of the so-defined and forms of formula (I) are useful as hypoglycemic agents fo...
05/17/1988
4742156Peptide antagonists of neurokinin B and opthalmic solutions containing them
Four decapeptides found to be analgesics and have antagonist activity to Neurokinin B which is also known as Neuromedin K. The decapeptide are of the following formula (I): wherein A1 and D4 are Asp or D-Asp amino acids. Also described is...
05/03/1988
4742084Aralykyl (arylethynyl)aralkyl amines and their use as vasodilators and antihypertensives
Acetylenes of the formula (I): ##STR1## wherein Y, m, R1, R2, q, Alk, R3 n and R4 are as defined herein and Ar1 and Ar2 are aromatic, including the salts and ammonium derivatives of fo...
05/03/1988
4742068Dihydropyridine compounds having 1,4,4-trisubstitution useful as antihypertensive agents
Dihydropyridine compounds having 1,4,4-trisubstitution of the following formula (I): ##STR1## wherein R is one of --COR3, R3 being a group such as phenyl or benzyl; R4 where R4 is a heterocycle; --(CH2...
05/03/1988
4729994Benzothiazepine vasodilators having aralkyl substitution
N-Aminoalkyl 1,5-benzothiazepines of the following formula (I): ##STR1## for the treatment of angina or hypertension or the prevention of heart attacks in mammals, in particular their use as coronary vasodilators....
03/08/1988
4727866Intrauterine device detection and removal system
A system for the detection, location and extraction of an intrauterine device ("IUD") including a magnetic IUD, a locator probe to be used intravaginally and an extractor probe to be used intrauterinally, both containing at least one Hall effect generator...
03/01/1988
4728666Heteroaromatic acetylenes useful as antihypertensive agents
Heterocyclic acetylenes of the formula (I): ##STR1## wherein Y and R1 are substituents such as hydrogen, alkyl, alkoxy, chloro or fluoro, m is 0-2, R2 is branched alkyl and Het is an aromatic heterocycle. The acetylenes are usef...
03/01/1988
47270723-alkoxy-2-aminopropylamines compositions and use as cardiovascular agents
Propylamines of the formula (I): ##STR1## and isomers thereof, particularly those enantiomers and racemates relative to the chiral carbon indicated by an asterisk (*). The propylamines can be used for the treatment of hypertension or angina in humans...
02/23/1988
4725602Acetylene amines and their use as vasodilators and antihypertensives
Acetylenes of the following formula (I): ##STR1## wherein Y, m, R1, R2, R3, n and R4 are defined herein and R5 is hydrogen, alkyl, cycloalkyl or substituted alkyl are useful vasodilators and anti...
02/16/1988
4725604Methods for the treatment of ventricular dysrhythmia and prevention of ventricular fibrillation
Various indole and benzothiophene compounds having a pendant pyrrolidinylidene amino or piperidinylideneamino group are useful in the prevention of ventricular fibrillation, e.g., in humans. The invention comprises methods for the treatment of ventricular...
02/16/1988
4719216Hexahydropyrrolo(2,1-A)isoquinoline derivatives as antidepressants
Novel compounds are disclosed, which are derivatives of 1,2,3,5,6,10b-hexahydropyrrolo[2,1-a]-isoquinolines, represented by general formula (I): ##STR1## as well as pharmaceutical compositions and methods for the treatment of depression in warm-...
01/12/1988
4716163Hypoglycemic method using 5-substituted pyrrolidinylidene compounds
Pyrrolidinylidene compounds substituted at the 5-position of the following formula (I): ##STR1## wherein R=H, alkyl or alkanoyl, and their use as hypoglycemic agents, e.g. in the treatment of diabetes, in a manner similar to linogliride....
12/29/1987
47161724-substituted octahydroquinolizine analgesic compounds and octahydroquinolizinium intermediates
Octahydroquinolizine and corresponding octahydroquinolizinium compounds of formulae (I) and (Va): ##STR1## where A is a 3 to 7 membered carbocyclic ring, R1 is a substituent, n is 0-2, x is 0-3, and Y is an anion. Also, pharmaceutical comp...
12/29/1987
4713386Tetrahydroazeto [2,1-a]isoquinolines and methods for treating depression
Tetrahydroazeto[2,1-a]isoquinoline of the formula (I): ##STR1## wherein R, R1, R2 and R3 are substituents and x and y are 0-2. Also pharmaceutical compositions for relieving depression in mammals, e.g. in humans, and ...
12/15/1987
4693850Methane sulfonic acid derivatives
Novel synthetic steps and intermediates leading to guanidines such as the anti-diabetic compound linogliride. Included is a hydrogen peroxide oxidation of a thiourea (II) to a sulfonic acid (I) which may then be reacted with morpholine to form the carboxi...
09/15/1987
4692460Cyclopenta[b]thiophenes having anti-inflammatory activity similar to steroids
Cyclopenta[b]thiophenes of the following formulae (I) and (II): ##STR1## wherein R1 and R4 are H or alkyl and R2, R3, R5 and R6 are alkyl, as well their salts, are anti-inflammatory agents ...
09/08/1987
46893295-substituted octahydroindolizine analgesics compounds and 7-keto intermediates
Octahydroindolizidines and corresponding ketones of the formulae (I) and (II): ##STR1## where A is a 3-7 carbon or hetero-containing ring, R1 is a substituent, n is 0-6 and x is 0-3. Also, pharmaceutical compositions for treating pain...
08/25/1987
46832393-diphenyl substituted octahydroindolizine analgesic compounds
Octahydroindolizine compounds of formula (I): ##STR1## wherein Q is --NR--, --(CH2)z --, --CH.dbd.CH--, --C.tbd.C--, --OCH2 --, --SCH2 --, --SO2 --, --SO--, --CO--, or an oxygen or a sulfur atom ...
07/28/1987
4670436Hypoglycemic 5-substituted pyrrolidinylidene compounds, compositions and use
Pyrrolidinylidene compounds substituted at the 5-position of the following formula (I): ##STR1## wherein R=H, alkyl or alkanoyl, and their use as hypoglycemic agents, e.g. in the treatment of diabetes, in a manner similar to linogliride....
06/02/1987
4665098Pharmaceutical composition of N-(4-hydroxyphenyl) retinamide having increased bioavailability
A dosage of N-(4-hydroxyphenyl)retinamide, also known as fenretimide, of the following formula: ##STR1## with increased bioavailability comprising corn oil and a non-ionic surfactant. The formulation if useful in the treatment of breast or bladd...
05/12/1987
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