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Attorney: Almaula; Prabodh I.


Number of patents: 437
Last date: July 13, 1999

1                      
NumberTitleIssue Date
5922907Precursors of ଲ-lactam antibacterials having soluble side chain esters
Disclosed is a process for the synthesis of ଲ-lactam antibacterials using soluble side chain esters in the presence of enzyme acylase. Also disclosed are novel esters useful as reactants in said process....
07/13/1999
5869734Preparation of optically active (S)-(-) and (R)-(+)-deoxyspergualin and novel intermediates thereof
A process for preparing optically active (S)-(-) and (R)-(+)-deoxyspergualin and salts thereof of the formula I ##STR1## by reacting a compound of formula II ##STR2## with a compound of formula III ##STR3## in the presence of a condens...
02/09/1999
5837828Pradimicin derivatives
The present invention concerns neutral sugar derivatives of pradimicins, their use as antifungal agents, methods for their preparation, and intermediates for their synthesis....
11/17/1998
58377024-arylamino-benzopyran and related compounds
Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is alkyl, Y is a single bond, --CH2 --, --C(O)--, --O--, --S-- or --N(R8)-- where R8 is hydrogen, alkyl, haloalkyl, aryl, a...
11/17/1998
5705645Hereroaryl derivatives of monocyclic beta-lactam antibiotics
Antibacterial activity is exhibited by novel compounds having the formula ##STR1## where R1, R2, and M are as defined herein and X is --(CH2)n -- wherein n is 0, 1, 2, 3 or 4 or CR3 R4 ...
01/06/1998
5627192Antihyperlipidemic/antioxidant dihydroquinolines
The present invention relates to novel dihydroquinolines which are useful for cholesterol lowering and as antioxidant agents. Also provided is a process for preparing the dihydroquinolines of the present invention, pharmaceutical compositions, and a metho...
05/06/1997
5411969Antihyperlipidemic/antioxidant dihydroquinolines
The present invention relates to novel dihydroquinolines which are useful for cholesterol lowering and as antioxidant agents. Also provided is a process for preparing the dihydroquinolines of the present invention, pharmaceutical compositions, and a metho...
05/02/1995
5410029Pradimicin derivatives
The present invention concerns neutral sugar derivatives of pradimicins, their use as antifungal agents, methods for their preparation, and intermediates for their synthesis....
04/25/1995
5391765Cholesterol lowering/antioxidant nitroxides
The present invention relates to novel nitroxides which are useful for cholesterol lowering and as antioxidant agents. Also provided is a process for preparing the nitroxides of the present invention, pharmaceutical compositions, and a method of treating ...
02/21/1995
5380854Diphenyl-heterocyclic-oxazole as platelet aggregation inhibitors
A novel series of oxazole derivatives having enhanced water solubility bioavailability and metabolic stability is disclosed in the Formula I ##STR1## or pharmaceutically acceptable salt thereof....
01/10/1995
5380713Peptide aldehydes as antithrombotic agents
This invention relates to novel arginine aldehydes, their salts and hydrates, which compounds selectively exhibit serine proteases inhibitory activity, are highly stable in aqueous solutions, and are useful for anti-trypsin and anti-thrombin activity....
01/10/1995
53628794-5-diphenyloxazole derivatives as inhibitors of blood platelet aggregation
A novel series of oxazole derivatives having the Formulae I and II ##STR1## wherein R is H or C1 -C5 lower alkyl, X is N or CH, Y is H or CO2 R1, or CO.R2, provided that when X is CH, Y is not H, R1
11/08/1994
5348960Imidazo[4,5-b]quinolinyl oxy alkyl tetrazolyl piperidine derivatives
A series of 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones having enhanced water solubility bioavailability and metabolic stability is disclosed in the Formula I ##STR1## wherein R1 is H, or C1 -C4 lower alkyl; R2
09/20/1994
5348969Diphenyloxazolyl-oxazoles as platelet aggregation inhibitors
A novel series of oxazole derivatives having enhanced water solubility bioavailability and metabolic stability is disclosed in the Formula I ##STR1## Y is CH3, Ph, or OH, provided that when Y is OH, the compound exists in the keto-enol tau...
09/20/1994
5328932Bisamidine derivatives as thrombin inhibitors
The present invention provides new thrombin inhibiting bisamidines derivatives, their pharmaceutically acceptable salts and hydrates, methods for their preparation, pharmaceutical composition, a process for their preparation, and use of the compounds in t...
07/12/1994
5321046Hypocholesterolemic unsymmetrical dithiol ketals
Disclosed herein are novel unsymmetrical dithiol ketals which are useful in the treatment or prevention of hypercholesterolemia, hyperlipoproteinemia, and atherosclerosis....
06/14/1994
5318989Cytotoxic bicyclo [7.3.1.]tridec-4-ene-2,6-diyne compounds and process for the preparation thereof
The present invention relates to a novel and efficient process for the preparation of 8-hydroxybicyclo[7.3.1]tridec-4-ene-2,6-diyne ring system which is part of the aglycone of esperemicin and to novel cytotoxic antitumor agents having said bicyclic ring ...
06/07/1994
5318993Antihyperlipidemic benzoquinones
The present invention relates to novel benzoquinones which are useful as antihyperlipidemic agents. The present invention also provides a process for their preparation, pharmaceutical compositions, and a method for treating birds and mammals in need there...
06/07/1994
5296508Farnesylated tetrahydro-naphthalenols as hypolipidemic agents
The invention relates to novel farnesylated tetrahydro-naphthalenols, that inhibit HMGR activity which results in a decrease in serum total cholesterol, a decrease in LDL cholesterol levels, and inhibition of LDL oxidation. The farnesylated tetrahydro-nap...
03/22/1994
4447360Intermediates for thia-aza compounds with a ଲ-lactam ring
2-Penem-3-carboxylic acid compounds of the formula ##STR1## in which R1 represents hydrogen, an organic radical bonded by a carbon atom to the ring carbon atom or an etherified mercapto group and R2 represents hydroxy or a radical R
05/08/1984
4386097Benzimidazoles, processes for their preparation and pharmaceutical preparations containing such compounds
The invention relates to 2-carboethoxyamino-5(6)-(2-amino-5-thiazoloyl)-benzimidazole compounds with anthelmintic properties and to processes for their preparation and pharmaceutical preparations containing such compounds....
05/31/1983
4376166Nocardia strain
New antibiotically active compounds having the basic structure of rifamycin S, namely 3-hydroxyrifamycin S (formula A: X=
03/08/1983
4374129Antibiotically active aminopapulacandin derivatives
N-acylated 11-amino derivatives of papulacandin A or B of the formula I ##STR1## in which Pap is the remainder of papulacandin A or B, R represents methyl or hydrogen and Ac represents the acyl radical of an organic acid, including salts of compounds...
02/15/1983
4369179Acylpeptides
Acylpeptides derived from somatostatin or from a derivative thereof having analogous action, in which the amino acids sequence is modified by omitting individual amino acids and/or by exchanging them for other amino acids, and in which the &3xb5;-amino gr...
01/18/1983
4364865Bicyclic unsaturated thia-aza compounds and 4-acylthio azetidinone intermediates
The invention relates to 6-amino-2-penem-3-carboxylic acid compounds of the formula ##STR1## in which R1a denotes hydrogen or an amino protective group R1A and R1b represents hydrogen ...
12/21/1982
4361558Halogenated steroids
Novel halogenated steroids of the formula ##STR1## in which X represents a halogen atom having a maximum atomic number of 17, Y represents a hydrogen atom or hydroxyl, and R represents an alkyl radical having a maximum of 6 carbon atoms, and their 1,2-dehydro ...
11/30/1982
4359555Salts formed from formamidines with polymers containing sulfonic acid groups
Salts of formamidines with polymers containing sulfonic acid groups; processes for producing these salts; and the use thereof in combating pests....
11/16/1982
4358439Cyclooctapeptides
Cyclic peptides of the formula ##STR1## in which trp represents L-Trp, D-Trp, or an analogous radical which carries a halogen atom in the indole nucleus, AcA represents hydrogen, or an acyl radical Ac of a carboxylic acid present at the ...
11/09/1982
4353918Dextrorotatory bicyclic thiadiaza compounds and pharmaceutical preparations containing them
The invention relates to the dextrorotatory enantiomer of trans-5,6-di-p-methoxyphenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole and its pharmaceutically acceptable salts and to pharmaceutical preparations containing them. The new compounds have valuable p...
10/12/1982
4353887Divisible tablet having controlled and delayed release of the active substance
Divisible tablet having controlled and delayed release of the active substance and consisting of a compact that is optionally provided with a coating and is formed by at least one active substance in an adjunct composition that effects a delayed and contr...
10/12/1982
4353826Substituted rifamycins
Antibiotically active compounds derived from rifamycin S or from the corresponding hydroquinone, rifamycin SV, or from derivatives at least partially hydrogenated in positions 16, 17; 18, 19; 28, 29, such as the 16, 17; 18, 19--tetrahydro- or the 16, 17; ...
10/12/1982
4344957Benz-acyl-benzimidazole derivatives and antiallergic compositions
New heterocyclylcarboxylic acid derivatives which are acylated in the nucleus, especially benz-acyl-benzimidazole-2-carboxylic acid derivatives of the formula ##STR1## in which R is a free, esterified or amidated carboxyl group or a free, etheri...
08/17/1982
4331676Thia-aza compounds with a ଲ-lactam ring
2-Penem-3-carboxylic acid compounds of the formula ##STR1## in which R1 represents hydrogen, an organic radical bonded by a carbon atom to the ring carbon atom or an etherified mercapto group and R2 represents hydroxy or a radical R
05/25/1982
4329348N-Oxacyclic-alkylpiperidines as psychostimulants
N-Oxacyclic-alkylpiperidyl-diazacompounds, e.g., those of the formula ##STR1## and salts thereof are antidepressants and psychostimulants....
05/11/1982
4328214Cyclopeptides and pharmaceutical preparations thereof and also processes for their manufacture
The somatostatin-analogous cyclic octapeptides according to the invention of the general formula ##STR1## in which trp represents L-Trp or D-Trp, in which the benzene ring may be substituted by a halogen atom, and Gaba(Ar) represents the residue of a...
05/04/1982
4327091N,N-Di and N,N,N-tri(hydroxy-lower alkyl) ammonium salts of substituted 3,4-dihydro-2H-1,2-benzothiazine 1,1 dioxide and pharmaceutical compositions thereof
3,4-Dihydro-2H-1,2-benzothiazine 1,1-dioxides of the formula ##STR1## wherein Ph represents a substituted or unsubstituted 1,2-phenylene radical, R represents a substituted or unsubstituted benzopyrone radical, and R1 represents hydrogen o...
04/27/1982
4323688Benzimidazole-2-carboxylic acid and derivatives thereof
Novel substituted heterocyclyl compounds of the formula ##STR1## in which R is a free, esterified or amidated carboxyl group or a free, etherified or esterified hydroxymethyl group, R1 is an aliphatic, cycloaliphatic, aromatic, araliphatic...
04/06/1982
4323560Novel phosphorylmuramyl peptides and processes for the manufacture thereof
Phosphorylmuramyl peptides of the formula ##STR1## are immuno-potentiating. In the formula, R1 represents optionally substituted alkyl or aryl, R2, R4, R6 and R7 represent, for example, hydrogen,...
04/06/1982
4322431Pharmaceutical preparations containing benzimidazole 2-derivatives
Benzimidazole 2-derivatives that are acylated in the nucleus and have the formula ##STR1## in which R1 represents an aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic or heterocyclic-aliphatic radical, R2 represents...
03/30/1982
4322419Bicyclomycin derivatives, compositions thereof and process of use thereof
Derivatives of 5-norbicyclomycin of the formula ##STR1## wherein R represents an unsubstituted or substituted monovalent hydrocarbon radical in which one, two or more carbon atoms can be replaced by heteroatoms, and X represents a bivalent group of t...
03/30/1982
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