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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...
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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...
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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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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...
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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...
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6365584 |
Arylysulphonamide-substituted benzimidazoles having tryptase-inhibiting activity
Arylsulphonamide-substituted benzimidazole derivatives of formula (I) having tryptase-inhibiting activity. Exemplary are:...
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6362196 |
Method to treat pain utilizing benzimidazole NMDA/NR2B antagonists
Substituted benzimidazole derivatives that are NMDA NR2B antagonists are utilized to treat pain.
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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...
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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...
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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,...
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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,...
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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:
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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...
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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...
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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...
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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 ,...
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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...
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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.
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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...
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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...
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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.
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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...
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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...
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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,...
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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...
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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.
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6303627 |
Inhibitors of serotonin reuptake
This invention provides compounds and a method for the inhibition of serotonin reuptake in mammals.
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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 ;...
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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, ...
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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...
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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...
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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...
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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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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 ...
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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.
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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,...
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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...
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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 ...
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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 ...
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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...
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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...
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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 ,...
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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.
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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.
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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...
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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...
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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 ...
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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...
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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 ...
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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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