Matches 501 - 550 out of 1007 < 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 >
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5698573 Imidazolone and oxazolone derivatives as dopamine antagonists  
A class of imidazolone and oxazolone derivatives of Structure I, ##STR1## wherein X represents oxygen or N--R 1 ; Q represents a substituted five-, six- or seven-membered monocyclic...
5696135 Inhibitors of rotamase enzyme activity effective at stimulating neuronal growth  
This invention relates to the method of using neurotrophic pipecolic acid derivative compounds having an affinity for FKBP-type immunophilins as inhibitors of the enzyme activity associated with...
5679692 Unbridged bis-aryl carbinol derivatives, compositions and methods of use  
Disclosed is a compound of Formula 1.0: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: AR 1 represents ##STR2## AR 2 represents ##STR3## or a five-membered...
5679706 Combination of a potassium channel activator and an antiarrhythmic agent  
A method for the concomitant treatment of ischemia and arrhythmia in mammalian species which includes administering a combination of a potassium channel opener having little or no effect on action...
5677317 Lactam compounds which are useful in the treatment of asthma  
Compounds of formula I ##STR1## wherein J, B, L, X, m and M have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide...
5674883 Derivatives of pyridone, their preparation process, the new intermediates obtained, their use as medicaments and the pharmaceutical compositions containing them  
Products of formula (I): ##STR1## in which: R 1 , R 2 , R 3 and R 4 represent: --a hydrogen atom, a halogen atom, one of the following radicals: hydroxyl, mercapto, cyano, nitro, sulpho,...
5672609 Pyridine compounds, intermediates compositions and methods of use  
The present invention is directed to compounds of Formula I: ##STR1## wherein: n is 2 or 3; R is dimethylamino, diethylamino, 1-piperidinyl, 1-pyrrolidinyl, 4-morpholinyl, or...
5668151 Dihydropyridine NPY antagonists: piperidine derivatives  
A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of piperidine and tetrahydropyridine derivatives of 4-phenyl-1,4-dihydropyridines of Formula I. ##STR1## As...
5668148 Alpha1a adrenergic receptor antagonists  
Compounds that specifically bind to the human alpha1a adrenergic receptor, including compounds effective to reduce symptoms of benign prostatic hypertrophy include compounds of formula: ##STR1##...
5668131 Substituted aminoalkylaminopyridines  
Compounds of formula I ##STR1## wherein R1, R2, R3, R4, R5, R6, X, n and A have the meanings as given in the description, can be used for combatting Helicobacter bacteria.
5665719 Benzoxazinone and benzopyrimidinone piperidinyl tocolytic oxytocin receptor antagonists  
Compounds of the formula ##STR1## X is --O--, --NH-- and --NR 8 --; Y is --CH 2 --, --CHR 8 -- and --C(R 8 ) 2 --; R 1 is camphor-10-yl, C 1 -5 alkoxyl, styryl, hydroxystyryl, furyl,...
5658909 Certain substituted 1-aryl-3-piperazin-1'-yl propanones to treat Alzheimer's Disease  
Disclosed are compounds of formula I: ##STR1## or the pharmaceutically acceptable salts thereof wherein X is a carbonyl, sulfonyl, methylene, or methylene substituted with optionally substituted...
5656632 1-(N'-(arylalkylaminoalkyl)) aminoisoindoles; dopamine receptor subtype specific ligands  
Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently...
5654299 Aryl substituted heterocycles  
The present invention concerns the novel use of aryl substituted heterocycles of formula I, set out below, which antagonize the pharmacological actions of one of ent endogenous neuropeptide...
5654298 Amine derivatives  
This invention concerns novel aminopyridinium compounds of the formula I wherein R 1 , R 2 , R 3 , R 5 and R 6 are selected from the following combinations: ##STR1## (a) one of R 2 and R 6 is a...
5650411 Substituted azolone derivatives  
The use for the manufacture of a medicament for treating Helicobacter-related diseases of a compound of formula ##STR1## a pharmaceutically acceptable acid addition salt or a stereochemically...
5646144 1-acylpiperidine compounds  
1-Acylpiperidine compound of the formula I ##STR1## in which R 1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl,...
5643906 Method of using N-arylheteroarylalkyl imidazol-2-one compounds for treatment of a glaucoma disorder  
A class of N-arylheteroarylalkyl imidazol-2-one compounds is described for use in treatment of a glaucoma disorder. Compounds of particular interest are angiotensin II antagonists of the formula...
5637593 Tryptamine analogues as 5-ht1-like agonists  
A compound of structure (I), in which A 1 is O, S(O) n in which n is 0, 1 or 2, NR, CH 2 , or CH(OH); A 2 is a bond or CH 2 ; or A 1 A 2 is CHCH; R is hydrogen or C 1 -4 alkyl; R 1 is an...
5631269 Dopamine receptor subtype ligands  
Compounds of formula (I) ##STR1## wherein one of X and Y represents nitrogen, and the other of X and Y represents oxygen, sulphur or N--R 2 ; Q represents a substituted five- or six- membered...
5629324 Thrombin inhibitors  
Compounds of the invention have the following structure: ##STR1## for example ##STR2## These compounds inhibit thrombin and associated thrombosis.
5622953 1-amino-3-phenoxy propane derivatives as modulator agents and their applications  
This invention relates to 1-amino-3-phenoxy-propane-derivatives of formula 1: ##STR1## (in which A, B, R, R x , X and Z are defined as in the specification described) and methods for their...
5622973 Treatment of osteoporosis with substituted piperidines, pyrrolidines and hexahydro-1H-azepines in combination with bisphosphonates  
The present invention is directed to certain novel compounds identified as di- and tri-substituted piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1##...
5620970 Topical ophthalmic carbonic anhydrase inhibitor formulations  
The present invention is directed to topical ophthalmic formulations of carbonic anhydrase inhibitors and polyethoxylated derivatives of castor oil. Methods for using the formulations for treating...
5618830 Dioxobutanoic acid derivatives as inhibitors of influenza endonuclease  
Dioxobutanoic acids substituted with piperidine or similar N-substituted saturated cycloalkyls are found to inhibit the cap-dependent endonuclease of influenza virus. These compounds are useful in...
5616579 Anti-ulcer pyridyloxy derivatives, their preparation and uses  
Compounds of formula (I): ##STR1## [wherein: R 1 is a cyclic amino group, or a dialkylamino group; R 2 a group of formula --NHCHR 3 R 4 wherein R 3 and R 4 are each alkyl aryl or aralkyl, or...
5616581 Pharmaceutical use of pyridine compounds  
A pyridine compound of the formula ##STR1## wherein R 1 is a hydrogen, a halogen, an alkyl, an alkoxy or the like, R 2 and R 3 are each a hydrogen, a halogen or an alkyl, --PQ-- is...
5616580 Pharmacological composition for preventing neurotoxic side effects of NMDA antagonists  
This invention discloses mixtures of NMDA antagonists and anti-cholinergic agents, which can be used to prevent excitotoxic damage in the central nervous system or for anesthetic purposes in human...
5607950 Muscarinic receptor antagonists  
The invetion is a method of treating irritable bowel syndrome with a compound selected from the formula ##STR1## wherein R, R 1 , m, n p are as defined in the specification, or a pharmaceutically...
5607952 Substituted 4-phenylthiazole derivatives, process for their preparation and pharmaceutical compositions containing them  
The invention concerns compounds of formula ##STR1## in which R, A, R 1 and Y are as defined in claim 1. The instant compounds have an affinity for the fibrinogen receptor: the complex of the...
5604224 Substituted heterocyclylisoquinolinium salts and compositions and methods of use thereof  
Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries...
5604246 2-aminoalkyl-5-aminoalkylamino substituted-isoquinoindazole-6(2H)-ones  
This invention is directed to 2-aminoalkyl-5-aminoalkylamino substituted isoquino[8,7,6-cd]indazole-6-(2H)-ones and to 2-aminoalkyl-5-aminoalkylamino...
5604245 Use of 4-amino-1-(2-pyridyl)piperidines for the preparation of a medicament for the treatment of conditions deriving from disorders of the serotoninergic systems mediated by 5-HT.sub.3 receptors  
The present invention concerns the use of 4-amino-1-(2-pyridyl)piperidines of general formula (I') ##STR1## wherein R' represents hydrogen, a halogen atom, a methyl, methylthio, trifluoromethyl,...
5585390 Alpha-amino acid compounds  
Compounds of the general formula: ##STR1## wherein m, X, Y, A, R 2 and R 3 are defined in the description, and medicaments containing the same.
5580889 Insecticidal nitromethyl or niteoimino-heteromethyl-heterocyclics  
Novel insecticides of the formula ##STR1## in which n is 0 or 1, X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R 9 variously...
5580883 Aminobenzene compounds to prevent nerve cell degradation  
A compound useful for central antioxidant having inhibitory activity of degeneration and necrocytosis of cerebral cells of the formula (I): ##STR1## wherein A and B are independently (1) a group of...
5578611 Use of α-1C specific compounds to treat benign prostatic hyperplasia  
The subject invention provides a method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound which...
5576313 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...
5576333 Carboxamide derivatives  
The present invention concerns novel carboxamide derivatives of formula I, ##STR1## wherein R 1 , R 2 , J, m, and M have any of the values defined in the specification, which antagonize the...
5576334 Acylurea derivatives  
The invention concerns chemical compounds of formula I R 1 --CON(R 2 )--CON(R 3 )--X 1 --Q--X 2 --GI and pharmaceutically acceptable metabolically labile esters or amides thereof, and...
5574049 2,2-dialkyl- and 2,2-dialkyl-3,4-dihydro-3-hydroxy-2H-1-benzopyrans  
2,2-di(C 1 -5 alkyl)- and trans-2,2-di(C 1 -5 alkyl)-3,4-dihydro-3-hydroxy-6-(pyridin-4-yl)-2H-1-benzopyra ns, e.g. of formula ##STR1## in which R 1 and R 2 =H, alkyl, hydroxyalkyl or...
5569655 Substituted heterocyclylisoquinolinium salts and compositions and method of use thereof  
Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries...
5565456 Anxiolytic aroyl piperidinyl and piperazinylacyl pyrroles  
Aroyl(piperidinyl and piperazinyl)acyl pyrroles of the following formula have anxiolytic activity: ##STR1## wherein, Y is selected from the group consisting of N, CH or COH; A 1 is selected...
5563142 Diaromatic substituted compounds as anti-HIV-1 agents  
The present invention includes diaromatic substituted heterocyclic compounds (III) ##STR1## which are useful in treating individuals infected with the HIV virus.
5561142 Substituted sulfonamides as selective β.sub.3 agonists for the treatment of diabetes and obesity  
Substituted sulfonamides are selective β 3 adrenergic receptor agonists with very little β 1 and β 2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis...
5561128 N-[(4-(hete roaryl)-1-piperidinyl)alkyl]-10,11-dihydro-5H-dibenz[B,F]azepines and related compounds 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...
5561146 Modified guanidino and amidino thrombin inhibitors  
Thrombin inhibitors are provided which have the formula ##STR1## wherein Z is a thrombin inhibitor substructure containing distal and proximal binding site residues; and R 1 is cyano, hydroxyl,...
5559128 3-substituted piperidines promote release of growth hormone  
The present invention is directed to certain novel compounds identified as 3-substituted piperidines of the general structural formula: ##STR1## wherein R 1 , R 1a , R 2a , R 4 , R 5 , A, X, and Y...
5556858 Cis-2-[(4-heteroaryl-1-piperazinyl)alkyl] hexahydro-1H-isoindole-1,3 (2H)-diones and related compounds 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...
5554611 Use of coumarin derivatives  
The present invention consequently relates to the use of coumarins of the general formula I ##STR1## in which R 1 and R 6 are defined as indicated in the claims, for controlling and preventing...
Matches 501 - 550 out of 1007 < 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 >