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6495566 |
Tetrahydroquinoline derivatives as glycine antagonists
The present invention provides compounds of formula (I) or a salt or a non-toxic metabolically labile ester thereof, processes for their preparation, pharmaceutical compositions containing the...
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6492368 |
Benzamidine derivatives as factor XA inhibitors
Novel compounds of the formula I in which X, Y, R 1 , R 2 and R 3 are as defined in Patent Claim 1 are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or...
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6492373 |
6-fluoro-1,4-dihydro-7-&lsqb 4-(2-hydroxyiminoethyl)-1-piperazinyl&rsqb -4-oxoquinoline-3-carboxylic acid derivatives, their preparation and pharmaceutical compositions
The present invention discloses a novel 6-fluoro-1,4-dihydro-7-[4-(2-hydroxyiminoethyl)-1-piperaziny
l]-4-oxoquinoline-3-carboxylic acid derivatives (formula I), with a process for their...
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6492421 |
Substituted phenylalanine type compounds which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4. Certain of these compounds aslo inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the...
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6486153 |
Phenylindole derivatives as 5-HT2A receptor ligands
A class of tryptamine analogues bearing an optionally substituted phenyl nucleus at the 2-position are selective antagonists of the human 5-HT 2A receptor and are therefore useful as...
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6479495 |
Aminoalkylphenol derivatives and related compounds
Novel aminoalkylphenols, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction utilizing the aminoalkylphenols or compositions thereof are disclosed.
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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,...
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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...
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6472392 |
Triazole compounds and the use thereof as dopamine-D3 -ligands
Triazole compounds of the following formula: where Ar 1 , A, B and Ar 2 have the meanings given in the description, possess a high affinity for the dopamine D 3 receptor and can therefore be...
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6469006 |
Antiviral indoleoxoacetyl piperazine derivatives
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with indoleoxoacetyl...
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6455520 |
Benzamide derivatives and their use as cytokine inhibitors
The invention concerns amide derivatives of formula (I) wherein R 3 is (1-6C)alkyl or halogeno; m is 0-3, p is 0-2 and q is 0-4; each of R 1 and R 2 is a group such as hydroxy, halogeno,...
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6448244 |
Water soluble azoles as broad-spectrum antifungals
The present invention concerns novel water-soluble azole compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof;...
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6429312 |
N-aminoalkyldibenzothiopencarboxamide receptor subtype specific ligands
Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof, wherein: R 1 , R 2 , R 3 , R 4 are the same or different and represent hydrogen, C 1 -C 6...
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6417362 |
Nitrogenous heterocyclic compounds and hyperlipemia remedy containing the same
Disclosed are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof. The compounds can inhibit the biosynthesis of triglycerides in the liver and can...
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6413969 |
Gatifloxacin pentahydrate
There are provided in accordance with the present invention crystalline gatifloxacin pentahydrate represented by the formula in a highly homogeneous form with respect to other crystalline forms...
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6413956 |
Substituted 4-oxo-quinoline-3-carboxamides
Disclosed are compounds of Formula I: or the pharmaceutically acceptable salts thereof where, R 1 , R 2 , and W are defined herein. These compounds are highly selective agonists, antagonists or...
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6410563 |
Substituted 8-arylquinoline phosphodiesterase-4 inhibitors
Novel substituted 8-arylquinolines, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, are PDE4 inhibitors.
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6399614 |
1-(N-phenylaminoalkyl)piperazine derivatives substituted at position 2 of the phenyl ring
The present invention is directed to novel 1-(N-phenylaminoalkyl)piperazine derivatives substituted at the position 2 of the phenyl ring. Pharmaceutical compositions comprising the compounds of the...
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6395749 |
Carboxamide compounds, methods, and compositions for inhibiting PARP activity
The present invention provides carboxamine compounds, methods and compositions for inhibiting PARP activity.
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6391874 |
Fused heterocyclic compounds as protein tyrosine kinase inhibitors
Substituted heteroaromatic compounds of formula (I) and in particular substituted quinolines and quinazolines, are protein tyrosine kinase inhibitors. The compounds are described as are methods for...
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6391872 |
Indazole bioisostere replacement of catechol in therapeutically active compounds
Therapeutically active compositions of matter and member species thereof are described which comprise indazole-containing compounds, said compounds and their therapeutic activity resulting directly...
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6387389 |
Sustained-release derivatives of hydroxylated analogs of substituted 1-&lsqb 2&lsqb bis(aryl)methoxy&rsqb ethyl&rsqb -piperazines and -homopiperazines and their use
The present invention provides sustained-release derivatives of hydroxylated analogs of substituted 1-[2[bis(aryl)methoxy]ethyl]-piperazines and -homopiperazines, pharmaceutical compositions...
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6369063 |
Selective factor Xa inhibitors
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating...
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6355643 |
Inhibitors of prenyl-protein transferase
The present invention comprises unsubstituted and substituted piperazine-containing compounds having alkanoyl, alkylsulfonyl, alkylamido or alkoxycarbonyl substituents, and having the formula A, ...
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6344456 |
Piperazinone derivatives and their uses
The invention concerns compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein. Said compounds are useful in therapy as antithrombotic agents.
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6340682 |
Diamide compound and drugs containing the same
The present invention provides diamide derivatives represented by the following general formula (1): wherein A is a phenyl group or the like, which may be substituted, B is —CH═CH—,...
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6335337 |
Substituted piperazinones and their therapeutic uses
Novel compounds which are inhibitors of the binding of fibrinogen to the Gp iib/iiia platelet receptors, and which can be used therapeutically as antithrombotic agents.
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6335343 |
Inhibitors of prenyl-protein transferase
The present invention comprises piperazine/piperazinone-containing compounds having multicyclic ring system substituents on one of the piperazine/piperazinone nitrogens, which inhibit...
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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...
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H002007 |
Insecticidal N-heterocyclylalkyl-or N-[(polycyclyl)alkyl]-N'substituted piperazines
Compounds of the following structure are disclosed as effective insecticides: ##STR1## in which: A and B are independently lower alkyl; U is lower alkylidene, lower alkenylidene, or CH--Z, where Z...
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6316618 |
Process for preparing (-)pyridobenzoxazine carboxylic acid derivatives
Disclosed is a process for preparing optically active (-)pyridobenzoxazine carboxylic acid derivative and pharmaceutically acceptable salt thereof by employing a starting material of (+)ethyl...
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6316450 |
Compounds
The invention relates to novel compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders.
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6306859 |
N-substituted imide derivatives with serotonergic activity
Compounds of the Formula (I) ##STR1## wherein R 2 , Y, X and n are as defined in the specification which compounds are useful in the treatment of disorders associated with serotonergic...
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6297258 |
Substituted 3-cyanoquinolines
This invention provides compounds of formula I having the structure ##STR1## wherein G 1 , G 2 , R 1 , R 4 , Z, n, and X are defined in the specification or a pharmaceutically acceptable salt...
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6284775 |
3-[4-(1-substituted-4-piperazinyl)butyl]-4-thiazolidinone and related compounds
There are disclosed compounds of the formula, ##STR1## where n is 0, 1 or 2; A is ##STR2## where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy,...
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6281215 |
4-(1-piperazinyl) benzoic acid derivatives, process for preparing them and their therapeutic applications
New 4-(1-piperazinyl)benzoic acid derivatives of the formula (I) are described. Also described is methods for making these compounds and their use as therapeutic agents. In particular, the...
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6281216 |
2-aminoquinoline derivatives having d4-agonistic activity
The present invention relates to a group of novel 2-aminoquinoline derivatives which are potent and selective agonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R...
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6265228 |
Process for preparing combinatorial amide alcohol libraries
Combinatorial chemical libraries of the Formula [S]--C(O)--L'--Z containing dihyroxy amides and hydroxyphosphonate amides are disclosed, in which [S] represents a solid support and --L'--Z is a...
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6248738 |
Isoquinolines as urokinase inhibitors
Compounds of formula (I): ##STR1## and pharmaceutically acceptable salts thereof, wherein one of R 1 and R 2 is H and the other is NC(NH 2 ) 2 or NHC(NH)NH 2 , and the other substituents...
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6232314 |
Arylalkylpiperazine compounds as antioxidants
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6214996 |
Naphthalene derivates, process for the preparation thereof, and intermediates therefor
Naphthalene derivatives of the formula [I]: ##STR1## wherein R 1 and R 2 are the same or different and are each H, protected or unprotected OH, one of R 3 and R 4 is protected or unprotected...
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6214829 |
Piperazine compounds, their preparation, and methods of using them
Novel piperazine and piperidine derivative compounds having interesting and advantageous pharmacological properties. The disdosed compounds have the general formula (a) ##STR1## and salts thereof....
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6211183 |
Selective factor Xa inhibitors
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating...
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6211196 |
Benzyloxy-substituted, fused N-heterocycles, processes for their preparation, and their use as bradykinin receptor antagonists
Benzyloxy-substituted, fused N-heterocycles, because of their ability to act as bradykinin receptor antagonists, have been found to be useful as therapeutics for the treatment and prevention of...
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6211181 |
1-Benzenesulfonyl pyrrolidine derivatives as bradykinin receptor antagonists
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6200986 |
Hemoregulatory compounds
The present invention relates to novel compounds which have hemoregulatory activities and can be used to stimulate hematopoiesis and for the treatment of viral, fungal and bacterial infectious...
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6175012 |
Processes and intermediates for the preparation of piperazine derivatives
Compounds having the formula R 5 O--A--NR 4 --R 2 (V) where R 2 is a heteroaryl group linked to the remainder of the molecule via a carbon atom adjacent a nitrogen atom and R 4 and R 5 are...
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6166205 |
2-Aryl-4-(1-[4-heteroaryl]piperazin-1-yl)methylimidazoles: dopamine . D.sub4 receptor subtype ligands
Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof wherein: R a represents ##STR2## where X, Y and Z are the same or different and...
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6166020 |
Aryl and heteroaryl alkoxynaphthalene derivatives
Compounds of the formula ##STR1## wherein R 1 , R 2 , R 4 , R 23 , R 24 , R 25 and R 26 are defined as in the specification. These compounds are useful psychotherapeutics and are potent serotonin...
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6153611 |
Piperazinyl-cyclohexanes and cyclohexenes
Novel non-dopaminergic antiischemic compounds have Formula I: ##STR1## wherein R=R 1 and is independently H, C 1 -4 alky C 1 -4 alkoxy, C 1 -4 trihaloalkyl or halogen, or R and R 1 may be taken...
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