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6127373 Method of treating tourette's syndrome and obsessive compulsive disorder  
A method for treating Tourette's syndrome, obsessive compulsive disorder, chronic motor or vocal tic disorder in a mammal, including a human, comprising administering to said mammal an effective...
6124291 Pyrrolo[1,2-a]pyrazine-1,4-dione serine protease inhibitors  
6121264 Imidazole-substituted quinoxalinedione derivatives  
6117871 6-(2-imidazolinylamino)quinoxaline compounds useful as alpha-2 adrenoceptor agonists  
The subject invention relates to methods of treating alpha-2 adenoreceptor modulated disorders, comprising administration, to a mammal in need of such treatment, of a safe and effective amount of a...
6117873 Substituted aminoalkane phosphonic acids  
Compounds of the formula I ##STR1## in which R 1 is hydroxyl or an aliphatic, araliphatic or aromatic radical, X is a divalent aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic,...
6117872 Enhancement of exercise performance by augmenting endogenous nitric oxide production or activity  
NO precursors are administered at elevated levels in addition to the diet of the individual to enhance exercise performance. Particularly, L-arginine and L-lysine by enhancing endothelial NO...
6114331 Substance suppressing allograft rejection  
Use of a substance according to formula (I) including its tautomeric forms, stereoisomeric forms and salts ##STR1## for the production of a drug suppressing the immunoreaction, in particular...
6110935 Benzofurazan compounds for enhancing glutamatergic synaptic responses  
Compounds of the general structural formula ##STR1## are shown to have AMPA receptor enhancing properties. The compounds are useful for such therapeutic purposes as facilitating the learning of...
6110911 Cyclic amine derivatives of substituted quinoxaline 2,3-diones as glutamate receptor antagonists  
A novel series of substituted quinoxaline 2,3-diones useful as neuroprotective agents are taught. Novel intermediates, processes of preparation, and pharmaceutical compositions containing the...
6107274 Piperazines as inhibitors of fructose-1,6-bisphosphatase (FBPase)  
Compounds of formula A are disclosed: ##STR1## wherein R 1 is aralkyl or cycloalkyl; R 2 is cycloalkylmethyl, alkyl, or aralkyl; R 3 is hydrogen, alkyl, substituted phenyl (including...
6103722 Ischemic preconditioning  
Methods and pharmaceutical compositions of matter are disclosed and claimed relating to cardioprotective effect mediated by delta (δ) opioid receptor agonists or more specifically delta-1 (δ 1...
6103723 Inhibitors of farnesyl-protein transferase  
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to...
6103720 Ketobenzamides as calpain inhibitors  
The patent describes ketobenzamides of the formula ##STR1## where R1, R2, R3, R4, X and n have the meanings given in the description, and their preparation. The novel compounds are useful for...
6096744 Sulfonamide derivatives of substituted quinoxaline 2,3-diones as glutamate receptor antagonists  
A novel series of substituted quinoxaline 2,3-diones useful as neuroprotective agents are taught. Novel intermediates, processes of preparation, and pharmaceutical compositions containing the...
6096743 1,2,3,4-tetrahydroquinoxalinedione derivative  
A 1,2,3,4-tetrahydroquinoxalinedione derivative represented by the following formula (I) or salt thereof, an NMDA-glycine receptor and/or AMPA receptor antagonist or kainic acid neurotoxicity...
6093723 4-substituted beta-carbolines and analogs thereof  
This invention relates to 4-substituted β-carbolines and β-carboline analogs that inhibit Ca +2 influx and interleukin-2 (IL-2) production. The 4-substituted β-carbolines and β-carboline...
6093703 Pharmaceutical compositions, containing S-adenosyl-L-methionine salt, 5-methyl-tetrahydrofolic acid and 5-formyltetrahydrofolic acid  
For the therapy of neurological complications in AIDS sufferers, the use of pharmaceutical compositions containing as an active principle at least one compound selected from the group consisting of...
6087361 Aryl-imidazolines and aryl-imidazoles useful as α-2 adrenergic agonists without cardiovascular side effects  
Methods are disclosed for treating a mammal with a condition that responds to α2 agonist treatment without causing cardiovascular side effects using compounds of the formula ##STR1## wherein R 1 ...
6083948 Tetrahydropteridines for treatment of neurological disorders  
Corticotropin releasing factor (CRF) antagonists of formula I: and their use in treating anxiety, depression, and other psychiatric and neurological disorders are disclosed.
6083947 Method for treating sexual dysfunctions  
This invention is a novel treatment for sexual dysfunctions by administering to a subject exhibiting a sexual dysfunction compounds that upmodulate the AMPA receptor. Methods and compositions for...
6080743 2,3-dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives  
2,3-Dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives of formula (I), ##STR1## wherein one of the radicals R 1 , and R 2 is a group R 5 and the other is a group of formula --CH(R 6 )--alk--R 7 ...
6075016 6,5-fused aromatic ring systems having enhanced phosphodiesterase IV inhibitory activity  
Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram, with improved selectivity with regard...
6069151 Quinolines and their therapeutic use  
Compounds of the formula ##STR1## have therapeutic utility, as inhibitors of phosphodiesterase IV and TNF release.
6066635 Avrainvillamide, a cytotoxic marine natural product, and derivatives thereof  
The present invention provides a compound having the structure ##STR1## wherein, R 1 , R 2 , R 3 , R 4 and R 5 are independently selected from H, alkyl, aminoalkyl, perfluoroalkyl, or...
6063784 Heteroaryloxyethylamines, method of preparation, application as medicine and pharmaceutical compositions containing them  
A compound selected from the group consisting of a compound of the formula ##STR1## wherein the substituents are defined as in the application and its non-toxic, pharmaceutically acceptable acid...
6057304 Quinoxaline-phosphonic acid derivatives  
The disclosure relates to quinoxaline derivatives of Formula I ##STR1## wherein R 1 , R 4 , R 5 , R 6 , R 7 and R 8 are as defined in the disclosure, as well as their production and use in...
6057321 1,4-diazabicyclo [2.2.2] oct-2-ylmethyl derivatives, their preparation and therapeutic application  
The invention concerns compounds of general formula (I) ##STR1## in which R 1 represents a methyl group, X 1 represents a hydrogen atom, or OR 1 and X 1 together form a group of formula --O(CH...
6057314 Low molecular weight bicyclic thrombin inhibitors  
This invention relates to the discovery of heterocyclic competitive inhibitors of the enzyme thrombin, their preparation, and pharmaceutical compositions thereof. As well, this invention relates to...
6057319 3,4-Diaryl-2-hydroxy-2,5-dihydrofurans as prodrugs to cox-2 inhibitors  
The invention encompasses the novel compound of formula (I) useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions for...
6048869 Tricyclic compounds  
The novel compounds of the present invention are those of structural formula I: ##STR1## or a pharmaceutically acceptable salt, ester, or stereoisomer thereof, which are inhibitors of...
6046190 Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors  
The invention relates to sulfonamide-containing hydroxyethylamine protease inhibitor compounds, their process of making, composition and method of use for inhibiting retroviral proteases such as...
6042849 Unit dosage forms for treatment of vasoconstriction and related conditions  
Magnesium is formulated in combination with vitamin E, vitamin C, folate, selenium, and optionally melatonin a unit dosage form for oral administration, for the treatment of vasoconstriction and...
6043240 3-heteroaryl-1-pyrrolidinealkylamines 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...
6028071 Purified compositions of 10-propargyl-10-deazaaminopterin and methods of using same in the treatment of tumors  
Highly purified 10-propargyl-10-deazaaminopterin (10-propargyl-10dAM) compositions tested in xenograft models for their efficacy against human tumors are shown to be far superior to methotrexate...
6015557 Tumor necrosis factor antagonists for the treatment of neurological disorders  
A method for inhibiting the action of TNF for treating neurological conditions in a human by administering a TNF antagonist for reducing damage to neuronal tissue or for modulating the immune...
6015800 Substituted quinoxaline-2-ones as glutamate receptor antagonists  
A novel series of substituted quinoxaline 2-ones useful as neuroprotective agents are taught. Novel intermediates, processes of preparation, and pharmaceutical compositions containing the compounds...
6011037 Thiazole derivatives with phosphodiesterase-inhibiting action  
6004933 Cysteine protease inhibitors  
The present invention relates to cysteine protease inhibitors of the general formula (I): ##STR1## wherein Z is a cysteine protease binding moiety; X and Y are S, O or optionally substituted N; and...
6001831 Process for producing quinazoline derivatives  
A process for producing 1,2,3,4-tetrahydro-2,4-dioxo-quinazoline-1-yl acetic acid derivatives of the formula (I) in which R 1 , R 2 , R 3 and R 4 are mutually independently hydrogen, halogen, OH,...
5994359 Imino oxyphenyl acetic acid derivatives, methods and intermediates for their preparation and use thereof  
2-Iminooxyphenylacetic acid derivatives ##STR1## where the substituents and the index have the following meanings: R 1 is C(CO 2 CH 3 )NOCH 3 (Ia), C(CONHCH 3 )NOCH 3 (Ib), C(CONH 2...
5994379 Bisaryl COX-2 inhibiting compounds, compositions and methods of use  
The present invention relates to inhibitors of COX-2, compositions which contain such compounds and methods of use. The compounds are represented by formula I: ##STR1## and include pharmaceutically...
5990111 Aldose reductase inhibition in preventing or reversing diabetic cardiomyopathy  
This invention relates to the use of aldose reductase inhibitors in the treatment, prevention or reversal of diabetic cardiomyopathy in a human subject.
5985926 Method for inhibiting intracellular viral replication  
There is disclosed a method of preventing or delaying the occurrence of acquired immunodeficiency syndrome (AIDS) in human immunodeficiency virus (HIV) seropositive humans by administering an...
5985877 Combination of tyrosine kinase inhibitor and chemical castration to treat prostate cancer  
A method of treating prostate cancer by co-administering a tyrosine kinase inhibitor such as an indolocarbazole and a chemical castration agent is disclosed. A composition containing a tyrosine...
5985869 Benzoheterocyclic compounds  
Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R 1 is H, halogen, alkyl, optionally substituted amino, alkoxy; R 2 is H, halogen, alkoxy, phenylalkoxy, OH, alkyl, optionally...
5985860 System for transdermal delivery of pain relieving substances  
Compositions for pain relieving non-steroidal anti-inflammatory drugs and/or medicaments such as ibuprofen, methotrexate, capsaicin, diphenhydramine, aspirin, methyl-nicotinate and other...
5981537 Pyrimidine-thioalkyl and alkylether compounds  
The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula (I) and pyrimidine-thioalkyl and alkylethers of Formula (IA), namely the compounds of Formula (I) where R 4...
5977113 4-heteroaryl-1-piperazine alkylamines 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...
5972975 Substituted 2-aminopyridines as inhibitors of nitric oxide synthase  
Substituted 2-aminopyridine compounds of Formula (I) and pharmaceutically acceptable salts which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders....
5962455 Certain substituted benzylamine derivatives a new class of neuropeptide Y1 specific ligands  
This invention encompasses compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein X 1 , X 2 , X 3 represent organic or inorganic substituents, n is 1, 2, or 3,...