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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...
6399627 Inhibitors of factor Xa  
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...
6395749 Carboxamide compounds, methods, and compositions for inhibiting PARP activity  
The present invention provides carboxamine compounds, methods and compositions for inhibiting PARP activity.
6384028 N-acylpiperidinylcarbonylaminocarboxylic acids and their use as glycoprotein IIb/IIIa antagonists and fibrinogen-blood platelets binding inhibitors  
β-alanine compounds or a pharmaceutically acceptable salt thereof, which is useful as a glycoprotein IIB/IIIa antagonist, inhibitor of blood platelet aggregation and inhibitor of the binding of...
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, R 1 , R 2 , R 3 , A, X′, Y′ and Z′ are...
6365584 Arylysulphonamide-substituted benzimidazoles having tryptase-inhibiting activity  
Arylsulphonamide-substituted benzimidazole derivatives of formula (I) having tryptase-inhibiting activity. Exemplary are:...
6362196 Method to treat pain utilizing benzimidazole NMDA/NR2B antagonists  
Substituted benzimidazole derivatives that are NMDA NR2B antagonists are utilized to treat pain.
6362195 Branched alkoxy-substituted 2-aminopyridines as NOS inhibitors  
The present invention relates to 6-phenyl-pyridin-2-ylamine derivatives of the formula wherein R 1 , R 2 , R 3 and R 4 are defined as in the specification, that exhibit activity as nitric...
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 NR 1 ; R 1 is H, C 1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R 1 is —(CH 2 ) h...
6358974 Isoquinoline derivatives  
Compounds of formula (I) wherein: R 1 represents a substituent selected from: a hydrogen or halogen atom; a hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy, trifluoromethanesulfonyloxy,...
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,...
6353014 15-ketal postaglandins for the treatment of glaucoma or ocular hypertension  
A method of treating glaucoma or ocular hypertension in a patient, which comprises administering to the patient a pharmaceutically effective amount of a compound of formula I:
6352985 Benzimidazole compounds  
A benzimidazole compound represented by the formula (I): wherein R 3 is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl...
6350760 Substituted piperidines as melanocortin-4 receptor agonists  
Certain novel substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are...
6348476 Pharmaceutical combination preparation of an inhibitor of the sodium/hydrogen exchanger and a medicament for the treatment of cardiovascular diseases  
Pharmaceutical combination preparation of an inhibitor of the sodium/hydrogen exchanger and a medicament for the treatment of cardiovascular diseases. These combinations of an NHE inhibitor can...
6344466 Benzamide and sulfonamide substitued aminoguanidines and alkoxyguanidines as protease inhibitors  
The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I: wherein X is O or NH, L is —O— or —SO 2 —, and R 1 -R 4 , R 9 -R 19 ,...
6339093 Isoquinoline derivatives  
The present invention relates to compounds of the formula wherein R 1 is hydrogen, lower alkyl, lower alkoxy, hydroxy, amino, nitro, cyano, lower alkyl-amino, di-lower alkyl-amino or halogen; R...
6331545 Heterocycyclic piperidines as modulators of chemokine receptor activity  
The present application describes modulators of CCR3 of formula (I): ##STR1## or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
RE37478 1-(arylthioalkyl, arylaminoalkyl, or arylmethylenealkyl)-4-(heteroaryl)piperazines and related compounds useful as antipsychotics and analgesics  
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...
6329389 Amine compounds, their production and use  
The present invention provides a compound of the formula: ##STR1## wherein Ar represents an aromatic group which may be substituted; X represents methylene, S, SO, SO 2 or CO; Y...
6329377 Ketomethylene group-containing cysteine and serine protease inhibitors  
The present invention is directed to novel ketomethylene group-containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.
6326372 Lactam and cyclic urea derivatives useful as alpha 1a adrenoceptor antagonists  
Lactam and cyclic urea derivatives and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also...
6323215 Neurotrophic tetrahydroisoquinolines and tetrahydrothienopyridines, and related compositions and methods  
This invention provides compounds having the following general structure: ##STR1## This invention also provides pharmaceutical compositions comprising same and methods of using these compositions...
6323217 Piperidine-4 sulphonamide compounds  
A compound of formula (I): ##STR1## wherein: R 1 represents hydrogen or alkyl, R 2a and R 2b represent a group selected from hydrogen, halogen, alkyl, hydroxy, alkoxy, trihaloalkyl, cyano,...
6319931 Use of a compound with affinity for the mitochondrial benzodiazepine receptor in cancer therapy  
The present invention relates in particular to a combination product comprising at least one compound with affinity for the mitochondrial benzodiazepine receptor, and to at least one...
6310073 Methods and compositions to treat glycosaminoglycan-associated molecular interactions  
Therapeutic compounds and methods for inhibiting a glycosaminoglycan (GAG)-associated molecular interaction in a subject, whatever its clinical setting, are described.
6303627 Inhibitors of serotonin reuptake  
This invention provides compounds and a method for the inhibition of serotonin reuptake in mammals.
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 --NR 1 --; Z is C(L)R 2 , or SO 2 R 3 ;...
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, ...
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...
6291453 4-amino-phenylalanine type compounds which inhibit leukocyte adhesion mediated by VLA-4  
Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the...
6288071 1-ethylene-2-alkylene-1,4-cyclohexadiene pesticides  
Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in...
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,...
6277849 N-sulphonyl and N-sulphinyl amino acid amides as microbiocides  
The invention relates to novel pesticidally active compounds of the general formula I ##STR1## as well as possible isomers and isomeric mixtures thereof, wherein n is a number zero or one; and ...
6274593 Substituted tetrahydro isoquinolines as modulators of dopamine D3 receptors  
The present invention provides compounds of formula (I): ##STR1## which are useful as antipsychotic agents.
6271236 Diaminopyridine-containing thiourea inhibitors of herpes virus  
Compounds of the formula ##STR1## wherein R 1 -R 5 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,...
6268379 Substituted aryl hydroxamic acids as metalloproteinase inhibitors  
The present application describes novel substituted aryl hydroxamic acids of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein ring A is a 5-8 membered ring containing...
6262049 Method of reducing nicotine and tobacco craving in mammals  
A method of reducing cravings in a mammal to nicotine or tobacco is disclosed. The method comprises administering to the mammal an effective amount of a D 1 /D 5 antagonist or a D 1 /D 5 ...
6262074 4-Hetaroylpyrazol derivatives and the use thereof as herbicides  
Hetaroyl derivatives of the formula I ##STR1## where: R 1 and R 2 are each hydrogen, nitro, halogen, cyano, thiocyanato, hydroxyl, mercapto, C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy, C 1 -C 6 ...
6262123 Ortho-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them  
Ortho-substituted benzoylguanidines of the formula I ##STR1## in which R(1) to R(4) have the meanings given in the claims, are suitable, as antiarrhythmic pharmaceuticals having a cardioprotective...
6251913 Hydroxamic acids substituted by heterocycles useful for inhibition of tumor necrosis factor  
Compounds of formula (I), ##STR1## wherein: n is 1 to 6; Het is a nitrogen containing ring fused to the benzene ring on two adjacent carbon atoms to form a bicyclic ring system which ring system...
6245780 Tetrahydroisoquinolinyl-indole derivatives for the treatment of depression  
Compounds are provided which have the formula: ##STR1## wherein: R 1 , R 2 , R 3 , and R 4 are, independently, hydrogen, halogen, alkoxy, or carboxamide; R 5 is hydrogen, halogen, CF 3 ,...
6242450 5-HT1F antagonists  
This invention provides 5-HT 1f antagonists of Formula I: ##STR1## where AR 1 , AR 2 , R, and R' are as defined in the specification.
6242462 Pharmacological agents  
Antagonists selective for the GluR5 receptor are useful for the treatment of pain. Also disclosed are novel decahydroisoquinoline derivatives which are selective GluR5 receptor antagonists.
6239126 Arylpiperidine and aryl-1,2,5,6-tetra-hydropyridine urea derivatives  
Compounds of the formula ##STR1## are useful for the treatment of disorder of the central nervous system including anxiety, depression, panic, alcohol and drug addiction, sexual dysfunction, sleep...
6235750 6-phenylpyridyl-2-amine derivatives useful as NOS inhibitors  
The present invention relates to 6-phenyl-pyridin-2-ylamine derivatives of the formula ##STR1## wherein G, R 1 and R 2 are defined as in the specification, that exhibit activity as nitric...
6228869 Ortho-sulfonamido bicyclic hydroxamic acids as matrix metalloproteinase and TACE inhibitors  
This invention provides, low molecular weight, non-peptide inhibitors of matrix metalloproteinases and TNF-α converting enzyme (TACE, tumor necrosis factor-α converting enzyme) of formula: B ...
6221377 Administration media for analgesic, anti-inflammatory and anti-pyretic drugs containing nitrous oxide and pharmaceutical compositions containing such media and drugs  
Administration mediums comprising solutions of nitrous oxide in water, alcohols, ethers or oils, and optionally including essential fatty acids or C 1 -C 6 alkyl esters thereof enhance the action...
6218393 Anthranilic acid derivatives as multi drug resistance modulators  
Anthranilic acids of formula (I): ##STR1## wherein each of R to R 9 is an organic substituent, n is 0 or 1, m is 0 or an integer of 1 to 6, q is 0 or 1, X is a direct bond, O, S, --S--(CH 2 ) p ...
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...