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RE37729 4-Heteroaryl-1-piperidinealkylamines and derivatives thereof and their therapeutic utility  
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a...
6399631 Carbazole neuropeptide Y5 antagonists  
Carbazoles of the formula which are effective in treating conditions associated with neuropeptide Y-5 neurotransmission.
6395749 Carboxamide compounds, methods, and compositions for inhibiting PARP activity  
The present invention provides carboxamine compounds, methods and compositions for inhibiting PARP activity.
6391878 Guanidinyl heterocycle compounds useful as alpha-2 adrenoceptor agonists  
This invention involves compounds having the following structure: as described in the Claims; and enantiomers, optical isomers, stereoisomers, diastereomers, tautomers, addition salts,...
6387896 Bicyclic oxazolidinones as antibacterial agents  
The present invention provides compounds of formula I useful as antimicrobial agents wherein W, X, Y, R1, R2 and n are as defined in thereof.
6387927 Epothilone derivatives and their use as antitumor agents  
The invention relates to anti-tumour-effective compounds of formula (I), wherein the radicals have the meanings given in the description.
6384065 Spiro compounds or salts thereof and preventives/remedies for autoimmune diseases and AP-1 inhibitors containing the same  
The spiro compounds of the present invention represented by the general formula: wherein A, R2, R3, R4, R5, R6 and n are as defined in the specification, exhibit an AP-1 activity inhibitory action...
6380214 Heterocyclic derivatives useful as anticancer agents  
The present invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein Z, X, X1, R1, R2 and R3 are as defined herein as it...
6380220 Derivatives from piperidine-keto acid, their preparation and use  
Piperidineketocarboxylic acid derivatives of the general formula I and their tautomeric and isomeric forms, and physiologically tolerable salts thereof, where the variables have the meanings given...
6380213 Compounds useful as neuro-protective agents  
This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.
6376514 Substituted six-membered heterocyclic compounds useful for treating multidrug resistance and compositions and methods thereof  
Substituted heterocyclic compounds are disclosed. The compounds are useful for treating multidrug resistance. The compounds can be formulated in compositions with a carrier and, optionally, a...
6369069 Biphenylsulfonyl cyanamides, method for the production thereof and their utilization as a medicament  
The invention relates to compounds of the formula (I), in which the symbols have the following meaning:R(1) is1. alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms;2. alkyl having 1, 2, 3, 4, 5,...
6369076 5-benzyl-octahydroindole and 6-benzyl-decahydroquinoline NMDA/NR2B antagonists  
Novel 5-benzyl-octahydroindoles and 6-benzyl-decahydroquinolines substituted in the 1-position are effective as NMDA NR2B antagonists useful for relieving pain.
6369074 Aminomethylene substituted non-aromatic heterocycles and use as substance P antagonists  
The present invention relates to novel aminomethylene substituted non-aromatic heterocycles and, specifically, to compounds of the formula wherein W, R1, R2, R3, A, X′, Y′ and Z′ are as defined in...
6365584 Arylysulphonamide-substituted benzimidazoles having tryptase-inhibiting activity  
Arylsulphonamide-substituted benzimidazole derivatives of formula (I) having tryptase-inhibiting activity. Exemplary...
6362198 Oxy substituted 4-carboxyamino-2-methyl-1,2,3,4-tetrahydroquinolines  
Cholesteryl ester transfer protein inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to elevate certain plasma lipid levels, including high density...
6358973 Benzazine derivatives as phosphodiesterase 4 inhibitors  
Compounds of formula I: wherein A is a heterocycle containing a nitrogen atom and optionally saturated or unsaturated and optionally further substituted by an oxo group (═O); R is: hydrogen,...
6358978 Substituted benzimidazoles  
Compounds of formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in whose course an increased activity of NFκB is involved.
6358942 Phenyloxazolidinones having a c-c bond 4-8 membered heterocyclic rings  
A compound of Formula (I): or pharmaceutical acceptable salts thereof wherein X is NR1; R1 is H, C1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R1 is —(CH2)h-aryl, —COR1-1,...
6352985 Benzimidazole compounds  
A benzimidazole compound represented by the formula (I): wherein R3 is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl...
6350749 Aminoguanidine hydrazone derivatives, process for producing the same and drugs thereof  
The present invention is to provide a compound of the formula: wherein the ring A is an optionally substituted 5- to 6-membered aromatic heterocyclic ring, the ring B an optionally substituted 5-...
6350759 Dihydro- and tetrahydro-quinoline compounds  
Compound of formula (I): wherein:R1 represents hydrogen or wherein A is as defined in the description,R2 and R3 each independently represents alkyl, cycloalkyl, heterocycloalkyl, optionally...
6339093 Isoquinoline derivatives  
The present invention relates to compounds of the formula whereinR1 is hydrogen, lower alkyl, lower alkoxy, hydroxy, amino, nitro, cyano, lower alkyl-amino, di-lower alkyl-amino or halogen;R2 is...
6323228 3-substituted indole angiogenesis inhibitors  
3-Substituted indole carbohydrazides having the formula ##STR1##are useful for inhibiting angiogenesis. Also disclosed are angiogenesis-inhibiting compositions and methods of inhibiting...
6316466 Pyrazole derivatives P-38 MAP kinase inhibitors  
The present invention relates to certain pyrazole derivatives of Formula (I): ##STR1##that are p-38 MAP kinase inhibitors, pharmaceutical compositions containing them, methods for their use, and...
6306911 Substituted amino acids as neutral sphingomyelinase inhibitors  
This invention relates to a series of substituted amino acids of Formula I ##STR1##pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the...
6303628 Bicycliccarbonyl indole compounds as anti-inflammatory/analgesic agents  
This invention provides a compound of the following formula: ##STR1##or the pharmaceutically acceptable salts thereof wherein A is C 1-6 alkylene or --NR1 --; Z is C(L)R2, or SO2 R3 ; U is CH or...
6303639 Propanolamine derivatives substituted by heterocyclic radicals, processes for their preparation, pharmaceuticals comprising these compounds and their use  
Substituted propanolamine derivatives and pharmaceutically tolerated salts and physiologically functional derivatives thereof are described.Also described are compounds of formula (I), ##STR1##in...
6303627 Inhibitors of serotonin reuptake  
This invention provides compounds and a method for the inhibition of serotonin reuptake in mammals.
6302837 Benzothiophene, benzofuran and indole compounds  
A compound selected from those of formula (I): ##STR1##wherein: X represents oxygen, sulphur, or NR3 wherein R3 is as defined in the description, Y represents oxygen, sulphur, NR3, or may...
6299906 Process for making submicron particles  
The present invention relates to a process for manufacturing a pulverous preparation of a submicron-sized biologically active compound comprising the steps of dissolving a biologically active...
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)...
6297256 Aryl and heteroaryl substituted pyridino derivatives GABA brain receptor ligands  
Disclosed are aryl and heteroaryl substitated pyridino compounds. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists,...
6294553 Method for treating ocular pain  
The invention relates to the use of brimonidine for treating ocular pain.
6294551 N-linked sulfonamides of heterocyclic thioesters  
This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as...
6291477 Tetrahydroquinolines, processes for their preparation, pharmaceutical compositions containing them, and their use to prevent or treat hyperlipoproteinaemia  
The tetrahydroquinolines can be prepared by condensing appropriately substituted tetrahydroquinoline aldehydes with suitable substances and subsequently varying the substituents present by...
6291514 Heteroaryl amidines, methylamidines and guanidines, preparation thereof, and use thereof as protease inhibitors  
The present invention is directed to compounds of Formula I: ##STR1##wherein X is O, S or NR7 and R1 -R7, Y and Z are set forth in the specification, as well as hydrates, solvates or...
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,...
6284784 Substituted 2-pyrrolidinone activators of PKC  
Compounds of formula I: ##STR1##wherein R1 and R2 have any of the values defined in the specification, and their pharmaceutically acceptable salts, are PKC activators and are useful for treating...
6277862 Quinoline derivatives  
A compound, or a solvate or a salt thereof, of formula (I), wherein, Ar is an optionally substituted aryl or a C5-7 cycloalkdienyl group, or an optionally substituted single or fused ring aromatic...
6277863 Methods and compositions for producing novel conjugates of thrombin inhibitors and endogenous carriers resulting in anti-thrombins with extended lifetimes  
Novel compounds comprising chemically reactive intermediates which can react with available reactive functionalities on blood components to form covalent linkages, where the resulting...
6277865 Piperididinyl and N-amidinopiperidinyl derivatives  
This invention is directed to a compound of formula I which is useful for inhibiting the activity of Factor Xa, by combining said compound with a composition containing Factor Xa. The present...
6277829 Process for preparing of aqueous formulation for opthalmic use  
The present invention describes a process for the preparation of aqueous formulations containing azithromycin for ophthalmic use, as well any formulations obtained by this process and their...
6274596 Benzoquinoline derivatives useful as antibacterial agents  
Disclosed are pharmaceutical compositions and formulations comprising benzoquinoline derivatives having the formula (I) to (V), wherein formula (I) is: ##STR1## X is selected from the group...
6271236 Diaminopyridine-containing thiourea inhibitors of herpes virus  
Compounds of the formula ##STR1##wherein R1 -R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl...
6262074 4-Hetaroylpyrazol derivatives and the use thereof as herbicides  
Hetaroyl derivatives of the formula I ##STR1##where: R1 and R2 are each hydrogen, nitro, halogen, cyano, thiocyanato, hydroxyl, mercapto, C1 -C6 -alkyl, C1 -C6 -alkoxy, C1 -C6 -alkylthio, C1 -C6...
6255324 Amino-and mercurio-substituted 4',5'-dihydropsoralens and therapeutical uses thereof  
5'-substituted, 4',5'-dihydropsoralen compounds (5) bearing tertiary amines (and salts thereof), quaternary ammonium moieties or organomercurial moieties are described. ##STR1##Also described are...
6248736 4-oxo-1,4-dihydro-3-quinolinecarboxamides as antiviral agents  
The present invention provides a compound of formula I ##STR1##Wherein R1 is C1-7 alkyl, optionally substituted by hydroxy or NR4 R5 ; R2 is C1-7 alkyl substituted by hydroxy or NR4 R5 ; R3 is H,...
6242446 Method for treating attention deficit disorder  
Tachykinin receptor antagonists that are useful for treating or preventing attention deficit disorder, optionally associated with hyperactivity in a patient, are desclosed.
6242450 5-HT1F antagonists  
This invention provides 5-HT1f antagonists of Formula I: ##STR1##where AR1, AR2, R, and R' are as defined in the specification.