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6596718 7-Morpholin-4yl-benzothiazole amide derivatives  
A compound of the formula A compound of formula I has a good affinity to the A2A receptor and is useful for the treatment of diseases mediated by this receptor.
6579886 Selective iglur5 receptor antagonists  
The present invention provides compounds of formula (I): wherein W represents hydrogen, C1-C4 alkyl, —CH2CO2H, or CO2H; and X represents hydrogen, C1-C4 alkyl, —CH2CO2H, or CO2H; with the pro...
6562819 Compounds for inhibition of ceramide-mediated signal transduction  
Novel, heterocyclic compounds having at least one ring nitrogen, disclosed side chains and, in some embodiments, an oxygen ortho to the ring nitrogen inhibit inflammatory responses associated with...
6495548 Lactam inhibitors of matrix metalloproteinases, TNF-α and aggrecanase  
The present application describes novel lactams and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 4-8 membered lactam containing from 0-3...
6479515 Heterocyclic benzenesulphonamide compounds as bradykinine antagonists  
The invention concerns compounds selected among the group consisting of (i) compounds of formula (I) wherein: Het1 represents a nitrogenous heterocycle with 5 apices, in particular imidazole,...
6479488 Tetrahydroquinoline derivatives as EAA antagonists  
Compounds of formula (I) or salt, or metabolically labile ester thereof wherein R represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy,...
6472404 HIV protease inhibitors  
The present invention discloses novel isoquinoline carboxamide derivatives which are HIV protease inhibitors or prodrugs thereof, a process for their manufacture, pharmaceutical compositions and...
6413956 Substituted 4-oxo-quinoline-3-carboxamides  
Disclosed are compounds of Formula I: or the pharmaceutically acceptable salts thereof where, R1, R2, and W are defined herein. These compounds are highly selective agonists, antagonists or inverse...
6410529 Phenyl urea and phenyl thiourea derivatives as HFGAN72 antagonists  
Phenyl urea and phenylthiourea derivatives, processes for their production and their uses as pharmaceuticals are disclosed.
6403835 Acylation of an organic group over a zeolite  
The invention relates to the shape selective acylation of an organic compound. In particular, the invention describes a process for such acylation wherein the process comprises reducing the number...
6365587 Substituted aryl hydroxamic acids as metalloproteinase inhibitors  
The present application describes novel substituted aryl hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring A is a 5-8 membered ring containing from 0-1...
6335446 Quinolinium- and pyridinium-based fluorescent dye compounds  
The present invention relates to quinolinium- and pyridinium-based fluorescent dyes. The dyes are useful for staining proteins in solution, in gels and on solid supports. The dyes of the invention...
6300342 Antithrombotic phenylalkyl derivatives  
Antithrombotic phenylalkyl derivatives of the formula ##STR1##Exemplary compounds are: (a) 1-[3-(4-amidino-phenyl)propionyl]-6-(4-fluoro-phenylsulphona mido)-1,2,3,4- tetrahydro-quinoline, (b)...
6297258 Substituted 3-cyanoquinolines  
This invention provides compounds of formula I having the structure ##STR1##wherein G1, G2, R1, R4, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which...
6265402 Use of 2-phenylmorpholin-5-one derivatives  
A 2-phenylmorpholin-5-one derivative having the formula (I): ##STR1##wherein R1 represents a C1 to C8 alkyl group, a C3 to C7 cycloalkyl group or an indanyl group, R2 represents a C1 to C4 alkyl...
6262263 ***WITHDRAWN PATENT AS PER THE LATEST USPTO WITHDRAWN LIST***
Quinolinium- and pyridinium-based fluorescent dye compounds
 
The present invention relates to quinolinium- and pyridinium-based fluorescent dyes. The dyes are useful for staining proteins in solution, in gels and on solid supports. The dyes of the invention...
6248738 Isoquinolines as urokinase inhibitors  
Compounds of formula (I): ##STR1##and pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is H and the other is NC(NH2)2 or NHC(NH)NH2, and the other substituents are as def...
6248739 Quinolinecarboxamides as antiviral agents  
The present invention provides a compound of formula I ##STR1##which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.
6221864 Prophylactic or therapeutic agent for diseases attributable to infection with helicobacters  
The present invention relates to an agent for the prophylaxis and treatment of diseases caused by Helicobacter infections, which comprises...
6218537 Process for making pyridyl and pyrimidine substituted imidazole compounds  
1,4,5,-substituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.
6211376 8-hydroxy-7-substituted quinolines as anti-viral agents  
The present invention provides for 8-hydroxy-7-substituted quinoline compounds such as formula III ##STR1##These compounds are useful as anti-viral agents. Specifically, these compounds have...
6143764 Quinoline and quinazoline derivatives inhibiting platelet-derived growth factor receptor autophosphorylation and pharmaceutical compositions containing the same  
The present invention relates to novel quinoline derivatives and quinazoline derivatives represented by the following formula (I): ##STR1## [wherein R1 and R2 are each independently H or C1 -C4...
6133264 Carbostyril derivatives for inhibiting skin erythema and/or skin pigmentation  
The present invention provides an agent for inhibiting skin erythema and/or skin pigmentation, containing at least one selected from the group consisting of the carbostyril derivative and salt...
6133285 Quinoline derivatives  
The invention is related to compounds of general formula (I) wherein R is methyl, ethyl, n-propyl, iso-propyl, n-butyl or allyl; R' is methyl, methoxy, fluoro, chloro, bromo, trifluoromethyl, or...
6093731 Isoquinolines  
Isoquinolinylguanidine compounds of formula (I): ##STR1## wherein the substituents are as defined herein, and salts thereof, are disclosed as urokinase inhibitors.
6087359 Thioaryl sulfonamide hydroxamic acid compounds  
A thioaryl sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated thioaryl...
6083944 Quinoline-containing α-ketoamide cysteine and serine protease inhibitors  
The present invention is directed to quinoline-containing α-ketoamide inhibitors of cysteine and serine proteases are disclosed. Methods for making these compounds, and methods for using the same ...
6083959 Quinoline derivatives, processes for their preparation and their use as medicaments  
A compound of the formula: ##STR1## wherein R1 is lower alkyl, R2 is hydrogen, lower alkyl or a heterocyclic group, R3 is hydrogen, lower alkyl or halogen, R4 is lower alkyl or halogen, R5 is nitro...
6080758 Benzenesulfonamide derivatives as bradykinin antagonists  
The present invention relates to compounds selected from the group consisting of the compounds of formula (I): ##STR1## X is a halogen atom, A is --CH2 --, --CH(OH)--, --CH(NH--COCH3)-- or S, R is...
6015902 Intercalators having affinity for DNA and methods of use  
Intercalator compounds of formula I-Tm as defined herein are provided which are comprised of intercalator moieties, or substituted intercalator moieties, having one or more functionalized chains,...
5977136 Tetrahydroquinolines as NMDA antagonists  
Compounds of formula (I) or a salt, or metabolically labile ester thereof, processes for the preparation thereof and their use as antagonists of excitatory amino acids. ##STR1##
5965730 Pyridine derivatives  
A pyridine derivative of the formula (I): ##STR1## wherein A is group of the following formulae: ##STR2## (R1 and R2 are each H, or protected or unprotected OH, R31, R41 and R42 are protected or...
5948791 Quinoline derivatives for treating malaria  
The invention relates to novel quinoline derivatives and their therapeutic use against malaria.
5905149 Substituted quinolymethylen-oxindole analogues as tyrosine kinase inhibitors  
Quinolylmethylen-oxindole derivatives having general formula (I), wherein R is H or --(CH2)n --COR7 group in which n is an integer of 1 to 4 and R7 is hydroxy, amino, C1 -C6 alkoxy or --NR5 R6 in...
5869484 Phenylcarbamate derivatives suitable to the use as anticholinesterase substances  
Phenylcarbamate derivatives suitable to the use as anticholinesterase substances having the general formula (I) ##STR1## wherein the meaning of R1 -R7 and X substituentes together with n will be...
5869661 Method of producing a quinolonecarboxylic acid derivative  
The present invention is a method of producing a 6-fluoro-7-substituted quinolonecarboxylic acid derivative represented by the general formula (4): ##STR1## wherein the variables are defined in the...
5861412 Dihydro-isoquinoline compounds and their use as pharmaceuticals  
Compound of general formula I ##STR1## wherein A is a benzo or thieno group; R1 is (C4-6)cycloalkyl, (C4-6)cycloalkyl-(C1-5)alkyl or ##STR2## R2, m, R3, R4, R and u are defined as in the...
5840745 Hydrosoluble 3-arylidene-2-oxindole derivatives as tyrosine kinase inhibitors  
Novel hydrosoluble 3-arylidene-2-oxindole derivatives, having tyrosine kinase inhibitor activity, encompassed by general formula (I), wherein m is zero, 1 or 2; A is a bicyclic ring chosen from...
5824677 Substituted amino alcohol compounds  
Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty....
5817674 Quinoline compounds  
Compounds of the formula ##STR1## in all possible racemic, enantiomeric and diastereoisomeric forms and their non-toxic, pharmaceutically acceptable salts with acids and bases having antagonistic...
5770734 N-substituted-2-aminoquinolines useful for treating hypofunction of the cholinergic system  
I wherein R1 is H, alkyl or cycloalkyl of 1 to 6 carbon atoms; R2 is H, alkyl of 1 to 6 carbon atoms, cyano, halo, nitro, amino or mono or dialkylamino in which the alkyl groups have 1 to 6 carbon...
5756422 Substituted quinoline compounds and their use as safeners  
Substituted quinoline compounds, processes for their preparation, composition containing them, and their use as safenersCompounds of the formula I and salts thereof ##STR1## in which R1 lacuna! CN,...
5753673 Quinolinecarboxylic acid derivatives  
Quinolinecarboxylic acid derivatives represented by the following formula: ##STR1## wherein C is hydroxymethyl, methoxy, ethoxy or morpholinyl, or pharmaceutically acceptable salts thereof exhibit...
5744607 Basic derivatives of glutamic acid and aspartic acid as gastrin or cholecystokinin antagonists  
The invention is directed to glutamic acid and aspartic acid derivatives represented by formula (I): ##STR1## wherein R1 is selected from the group consisting of unsubstituted, mono- or...
5714497 Compounds bearing sulphamoyl and amidino radicals, their preparation process and pharmaceutical compositions containing them  
The subject of the invention is the compounds of formula I ##STR1## in which Ar1 represents naphtyl, phenyl, quinolyl or isoquinolyl optionally substituted; Ar2 represents a phenyl or thienyl...
5708173 Heterocyclic compounds  
A compound of the formula: ##STR1## or its salt is prepared by reacting a compound of the formula: ##STR2## with a compound of the formula: ##STR3## Wherein the variables are all defined in claim 1.
5691356 Disubstituted heterocyclic thrombin inhibitors  
Disubstituted heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein G is ##STR2## wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; p is 0, 1 or 2, Q...
5672600 Antimicrobial dithiocarbamoyl quinolones  
Antimicrobial dithiocarbamoyl quinolone compounds of the general formula: ##STR1## wherein (1) A1, A2, A3, R1, R3, R4, and R6 form any of a variety of quinolone and related heterocyclic structures...
5658926 Carbostyril derivative and platelets aggregation inhibitory agent  
The present invention provides a carbostyril derivative represented by the following general formula ##STR1## (wherein A, R and W have the same definitions as given above; and the carbon-to-carbon...
5654298 Amine derivatives  
This invention concerns novel aminopyridinium compounds of the formula I wherein R1, R2, R3, R5 and R6 are selected from the following combinations: ##STR1## (a) one of R2 and R6 is a basic group...