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6239146 |
Neurotrophic difluoroamide agents
The present invention relates to the design, synthesis, and the peptidyl-prolyl isomerase (PPIase or rotamase) inhibitory activity of novel α,α-difluoroacetamido compounds that are neurotrophic...
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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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6232326 |
Treatment for schizophrenia and other dopamine system dysfunctions
Methods and compositions for the treatment of positive and negative symptoms of schizophrenia and tardive dyskinesia are provided. Compositions include 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine...
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6225324 |
Antidepressant heterocyclic compounds
Compounds of formula I are useful antidepressant agents ##STR1## demonstrating potent inhibition of 5-HT reuptake. Z is selected from among various phenyl and hetaryl moieties while Y is benzyl or...
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6221871 |
Certain aminomethyl biphenyl, aminomethyl phenyl pyridine and aminomethyl phenyl pyrimidine derivatives; novel dopamine receptor subtype selective ligands
Disclosed are compounds of the formula: ##STR1## where S and V are various organic or inorganic substituents; G and K are the same or different and represent N or CR' where R' is an organic...
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6214827 |
Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
Novel compounds of Formula ##STR1## are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a...
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6214845 |
Insecticidal N-(substituted arylmethyl)-4[bis(substituted phenyl or pyridyl)methyl] piperidines
Compounds of the following structure, the corresponding N-oxides and agriculturally acceptable salts, are disclosed as effective insecticides: ##STR1## in which U is --(CH 2 ) n --; Q is...
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6211199 |
Substituted 4-(1H-benzimidazol-2-yl-amino)piperidines useful for the treatment of allergic diseases
The present invention relates to novel substituted piperidine derivatives of formula (1), stereoisomers ##STR1## thereof, and pharmaceutically acceptable salts thereof which are useful as histamine...
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6197791 |
N-hdroxy-2-(alkyl, aryl, or heteroaryl, sulfanyl, sulfinyl or sulfonyl)-3-substituted alkyl, aryl or heteroarylamides as matrix metalloproteinase inhibitors
Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases...
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6191145 |
Orally-active nipecotamide glycolamide esters for the treatment of thrombosis disorders
Orally-active nipecotamide glycolamide ester derivatives of formula (I): ##STR1## are disclosed as useful in treating platelet-mediated thrombotic disorders.
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6187752 |
Method for treating schizophrenia employing an ace inhibitor
A method is provided for treating schizophrenia in a mammalian species by administering an ACE inhibitor, such as captopril, alone or with a neuroleptic such as cholecystokinin, fluphenazine or...
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6184221 |
Sulfonamide-substituted compounds, processes for their preparation, their use as a medicament or diagnostic, and medicament comprising them
Compounds of the formula I ##STR1## having the meanings of the substituents indicated in the claims are outstandingly active substances for the production of medicaments for the prophylaxis and for...
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6174900 |
Substituted piperidine derivative for treating urinary disturbance
Disclosed herein is a substituted piperidine derivative represented by the following general formula (1): ##STR1## wherein R 1 means an aryl or heteroaryl group which may have at least one...
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6172085 |
Cyclic ether compounds as sodium channel modulators
A compound of the formula: ##STR1## wherein R 1 and R 2 each represents hydrogen, lower alkyl which may be substituted or acyl; R 3 , R 4 and R 5 each represents lower alkyl which may be...
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6166034 |
Spiro piperidine derivatives as 5HT1D receptor antagonists
Novel spiro piperdine derivatives of formula (I), in which P 1 , P 2 , R 1 , R 2 , R 2 ', R 3 , m, A, E, G, X, Y, R 7 , R 8 , R 9 and R 10 have the meanings defined in claim 1 are described, as...
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6166035 |
1,4-dihydropyridine derivatives and their use in therapy
Novel 1,4-DHP of the following structures are described having better therapeutic activities in coronary diseases: ##STR1## wherein n and R1 are as defined in the specification.
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6166032 |
Method for controlling tobacco use and alleviating withdrawal symptoms due to cessation of tobacco use
A method for controlling tobacco use and alleviating withdrawal symptoms due to the cessation of tobacco use comprising administering to a human desiring to control tobacco use and/or suffering...
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6159968 |
Activation of chloride channels for correction of defective chloride transport
This invention provides a method for increasing the permeability of epithelial cells to a chloride ion in a subject comprising administering a permeability enhancing amount of a composition...
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6156752 |
Optically active 1,4-dihydropyridine compounds as bradykinin antagonists
This invention provides a compound of the formula (I): ##STR1## and its pharmaceutically acceptable salts, wherein A 1 and A 2 are each halo; R 1 and R 2 are independently C 1 -4 alkyl; R 3 is...
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6153611 |
Piperazinyl-cyclohexanes and cyclohexenes
Novel non-dopaminergic antiischemic compounds have Formula I: ##STR1## wherein R=R 1 and is independently H, C 1 -4 alky C 1 -4 alkoxy, C 1 -4 trihaloalkyl or halogen, or R and R 1 may be taken...
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6140333 |
N-acyl cyclic amine derivatives
The invention relates to compounds represented by the general formula [I] ##STR1## [wherein Ar means an aryl group or a heteroaryl group which may have a substitutive group selected from a group...
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6140330 |
Thiazole derivative
A thiazole compound of the formula: ##STR1## wherein T is lower alkylene; u is 0 or 1; R 1 and R 2 are the same or different and are each H, or lower alkyl, etc.; R 3 is ##STR2## R 4 is H or...
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6140344 |
4-aroylpiperidine derivatives-CCR-3 receptor antagonists
This invention relates to certain piperidine quaternary salts of Formula (I) ##STR1## that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and...
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6140338 |
Chemokine receptor antagonists
The present invention relates to a compound of the general formula: ##STR1## wherein each of R 1 and R 2 which may be the same or different, is e.g. a hydrogen atom, a halogen atom or a lower...
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6140345 |
1-(aryloxyalkyl)-4-(heteroaryl)piperidines 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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6136827 |
Cyclic amine modulations of chemokine receptor activity
The present invention is directed to cyclic amines of the formula I: ##STR1## (wherein R 1 , R 2 , R 3 , m and n are defined herein) which are useful as modulators of chemokine receptor activity....
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6133287 |
Piperidine-indole compounds having 5-HT.sub.6 affinity
Described herein are compounds with affinity for the 5-HT 6 receptor, which have the general formula: wherein: R 1 is selected from the group consisting of H and C 1 -4 alkyl; R 2 is...
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6130217 |
Compounds enhancing antitumor activity of other cytotoxic agents
This invention relates to certain heterocyclic compounds and their pharmaceutically acceptable salts, which are useful for sensitizing multidrug-resistant tumor cells to anticancer agents and...
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6130232 |
Substituted piperidine derivatives as muscarinic M.sub.3 receptor antagonists
This invention provides substituted heteroaromatic ring derivatives which are represented by a general formula [I] below: ##STR1## [in the formula, R 1 and R 2 may be same or different and each...
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6124318 |
Diphenylalkyl-tetrahydropyridines, process for their preparation, and pharmaceutical compositions containing them
The invention relates to compounds of the formula ##STR1## in which: Y is --CH-- or --N--; R 1 is a halogen or a CF 3 , (C 1 -C 4 )alkyl or (C 1 -C 4 )alkoxy group; R 2 and R 3 are each...
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6124319 |
3,3-disubstituted piperidines as modulators of chemokine receptor activity
The present invention is directed to 3,3-disubstituted piperidines of the formula I: ##STR1## (wherein X, Y, Z, Ar, R, m and n are defined herein) which are useful as modulators of chemokine...
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6107310 |
Heteroarylcarboxamide derivatives for treating CNS disorders
Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or --O--; B is methylene or --O--; G 1 --G 2 --G 3 are absent or form a heteroaromatic...
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6107312 |
Thiopyridines for use in the control of helicobacter bacteria
Thiopyridines of formula (I) ##STR1## in which the substituents and symbols are as defined in the specification are suitable for use in controlling Helicobacter bacteria. They are compounded into...
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6096771 |
Isoxazole derivatives
An isoxazole compound having the following formula: ##STR1## wherein R 1 represents hydrogen, halogen, alkyl, alkoxy, hydroxyl, alkylthio, amino, alkanoyl, alkanoylamino, alkanoyloxy,...
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6096761 |
Esters of 3-hydroxy-piperidinemethanol derivatives
The present invention of compounds of formula (I), ##STR1## a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R 1 is C...
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6090824 |
Therapeutic neurokinin receptor antagonist compounds
Compounds of formula I ##STR1## wherein Q 1 , Q 2 , Q 3 , and Q 4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide...
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6083943 |
Substituted azaheterocyclecarboxylic acid
A compound of the chemical formula (I) and its pharmaceutically acceptable salt: ##STR1## wherein Y is C 2 -C 4 alkylene; Z is a valence bond or C 1 -C 6 alkylene; R 1 is substituted or...
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6083960 |
Constrained somatostatin agonists and antagonists
The present invention relates to a compound of general formula I ##STR1## for treating medical disorders related to binding to human somatostatin receptor subtypes.
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6083950 |
1-(4-arylpiperazin-1-yl)-ω-[n-(α,ω-dicarboximido)]-alka nes useful as uro-selective α1-adrenoceptor blockers
Novel piperzine derivatives substituted on one nitrogen by an aromatic system and on the other nitrogen by (2,5-dioxopyrrolidin)-1-yl) alkanes or (2,6-dioxopiperidin-1-yl) alkanes have been found...
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6069143 |
Fibrinogen receptor antagonists
This invention relates to compounds of the formula: ##STR1## which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for...
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6066650 |
Inhibitors of microsomal triglyceride transfer protein and method
Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the...
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6060485 |
Arylacetic amide derivative or salt thereof, and pharmaceutical comprising it
Described is an arylacetic amide derivative represented by the following formula (1): ##STR1## wherein R 1 represents an aryl group or the like, R 2 and R 3 each independently represents an...
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6051570 |
Benzimidazole derivatives as antiulcer agents, process for their preparation and pharmaceutical compositions containing them
This invention particularly relates to novel pyridylmethylsulfinyl benzimidazole represented by the general formula (I), its tautomers, its derivatives, its analogs, its stereoisomers, its...
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6046205 |
Indole and indazole compounds
Compound of formula (I): ##STR1## wherein: n is 0 or 1, A represents a σ bond or alkylene or alkenylene, X represents nitrogen or C--R 2 , R 1 represents hydrogen or alkyl, G 1 ...
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6040317 |
Sulfonamide fibrinogen receptor antagonists
A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases...
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6028082 |
Human NK.sub.3 receptor-selective antagonist compounds, method for obtaining them and pharmaceutical compositions containing them
Compounds of formula (I), a method for obtaining them and pharmaceutical compositions containing them are described. The compounds are useful as human NK 3 receptor antagonists.
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6022880 |
Substituted pyridylamino indoles
There are disclosed various compounds of the formula below, ##STR1## where R, R 1 , W, X, Y and Z are as defined in the specification; which are useful for alleviating various memory dysfunctions...
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6020345 |
Pyridin-2-yl-methylamine derivatives, method of preparing and application as medicine
The invention concerns novel pyridin-2-yl-methylamine derivatives of formula (I): ##STR1## in which: u represents hydrogen or methyl; v represents hydrogen, chlorine, or methyl; w represents...
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6020327 |
Control of hair growth
A method for treating hair loss is disclosed by topically adminstering an aromatase inhibitor to a mammal, including humans, on the area to be treated.
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6017931 |
Insecticidal compositions containing n-(substituted phenylmethyl)-4-[bis(substituted phenyl)methyl]piperidines
Compositions containing compounds of the following structure, some of which are novel, and the corresponding N-oxides and agriculturally acceptable salts, are disclosed as effective insecticides:...
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