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5807865 |
3,3-disubstituted piperidine derivatives and their use as therapeutic agents
The present invention relates to compounds of the formula (I) ##STR1## wherein X, Z, R, R 1 , R 2 , Ar, n and m are as defined herein which are of use in the treatment or prevention of neuropathy,...
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5807870 |
Substituted pipecolinic acid derivatives as HIV protease inhibitors
Disclosed herein are compounds of formula 1 ##STR1## wherein X is a terminal group, for example, an aryloxycarbonyl, an alkanoyl or an optionally mono- or disubstituted carbamoyl; B is absent or an...
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5807872 |
Imidazoylalkyl substituted with a six membered nitrogen containing heterocyclic ring
Disclosed is a compound of Formula 1.0: ##STR1## or a pharmaceutically acceptable salt or solvate thereof. Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable...
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5804578 |
Piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone
The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R 1 , R 1a , R...
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5801170 |
Heterocyclic biphenylylamides useful as 5HT1D antagonists
A compound of formula (I) or a salt thereof: ##STR1## wherein P is a 5 to 7 membered heterocyclic ring selected from the group consisting of thienyl, furyl, pyrrolyl, triazolyl, diazolyl,...
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5795901 |
Insecticidal N-(substituted arylmethyl)-4- bis(substituted aryl)hydroxymethyl!piperidinium salts
Compounds of the following structure are disclosed as effective insecticides: ##STR1## in which Q is hydroxy; U is --(CH 2 ) n --, where n is 1; R is ##STR2## in which V, W, Y, and Z are each...
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5795893 |
Fibrinogen receptor antagonists
This invention relates to novel compounds which inhibit platelet aggregation, pharmaceutical compositions containing the compounds, and methods of using the compounds.
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5792778 |
2-substituted aryl pyrroles, compositions containing such compounds and methods of use
The present invention addresses 2-substituted aryl pyrroles, as well as compositions containing such compounds and methods of treatment. Cytokine mediated diseases refers to diseases or conditions...
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5789405 |
Oxaspiro(2,5)octane derivative
An oxaspiro 2,5!octane derivative of the formula: ##STR1## useful in inhibiting angiogenesis in solid tumors.
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5783576 |
Benzoyl guanidine derivatives, the preparation thereof and their use in pharmaceutical compositions
New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions.
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5783563 |
Method for treatment or prophylaxis of venous thrombosis
A method is disclosed for treatment or prophylaxis of venous thrombosis employing the peptide HOOC--CH 2 --(R)Cgl--aze--Pab or a stereoisomer thereof or a physiologically acceptable salt thereof.
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5773459 |
Urea- and thiourea-type compounds
The present invention relates to molecules capable of modulating tyrosine signal transduction to prevent and treat cell proliferative disorders or cell differentiation disorders associated with...
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5767118 |
4-Heterocyclic peperidines promote release of growth hormone
The present invention is directed to certain novel compounds identified as 4-heterocycle substituted piperidines of the general structural formula: ##STR1## wherein R 1 , R 4 , R 5 , A, R 3 and...
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5763460 |
N-(piperidinyl-1-alkyl)-substituted cyclohexane carboxylic acid amides as 5-htia receptor antagonists
Compounds of formula (I) and the pharmaceutically acceptable acid addition salts thereof are 5-HT 1A binding agents and may be used, for example, as anxiolytics. In the formula a and b each...
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5763436 |
Guanidine derivatives
Compounds of the formula ##STR1## wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and...
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5760029 |
Spirocycle integrin inhibitors
This invention relates to novel heterocycles, including (S)-2-phenylsulfonylamino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspi ro- 4,5!-dec-2-en-3-yl!carbonylamino! propionic acid, which are...
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5760035 |
Therapeutic agents
Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which R 1 , R 2 and R 3 independently represent hydrogen, hydroxy, halo, alkyl or alkoxy; ALK 1 represents a C...
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5760018 |
Gem-disubstituted azacyclic tachykinin antagonists
The present invention is directed to certain compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 ,...
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5756529 |
Substituted pyrazolyl benzenesulfonamides for use in veterinary therapies
A method of using pyrazolyl benzenesulfonamide compounds in treating inflammation and inflammation-related disorders in companion animals is disclosed.
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5753691 |
Agents for inhibiting the production of IL-1β and the release of TNFα
The pharmaceutical use of 1-cinnamoyl-2-pyrrolidinone derivatives having the activities to inhibit the production of IL-1β and the release of TNFα. Those derivatives are useful in the treatment...
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5750540 |
1,4-di-substituted piperidine derivatives
This invention provides novel 1,4-di-substituted piperidine derivatives of the general formula I! ##STR1## and the pharmaceutically acceptable salts thereof, wherein: Ar represents a phenyl group...
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5744487 |
Prolineamide derivatives
A prolineamide derivative represented by the formula (I): ##STR1## or a salt or hydrate thereof or a pharmaceutically acceptable salt thereof, which has a protease inhibition activity and is useful...
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5741800 |
Azolyl-cyclic amine derivates with immunomodulatory activity
A compound of the formula (I), ##STR1## as defined in the specification, having immunomodulatory activity, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the...
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5741799 |
Heterocyclic thrombin inhibitors
Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R 1 , R 2 , R 3 , G, G x , R 6 ', Ra, Xa, R 6 , Rb, R 3 , p, Q, A and R 4 are as defined herein.
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5739149 |
Substituted piperidinobutyl nitrogen-containing heterocyclic compounds and analogues thereof as neurokinin antagonists
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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5739150 |
Piperidinyl thiacyclic derivatives
Piperidinyl thiacyclic derivatives useful in the treatment of allergic diseases and diseases responding to antagonism of 5HT 2 receptors, pharmaceutical compositions and a methods of treatment...
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5728716 |
Aralkylamino substituted azacyclic therapeutic agents
Aralkylamino substituted azacyclic compounds of formula (I) and their salts and prodrugs. The variables are defined herein. The compounds are useful as tachykinin antagonists and are of particular...
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5726188 |
Optically active imidazolidinone derivatives and processes for preparing them
An optically active imidazolidinone derivative represented by general formula (1), having a cholinergic activity (a muscarine M 1 activity) and being useful for treating senile dementia, a...
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5714500 |
2-phenyl- and 2-thienyl-(2)-piperidine derivatives having neuroprotective properties
Compounds of formula (I) ##STR1## in which R 1 is hydrogen, R 2 is hydrogen or C 1 -6 alkyl, R 3 and R 4 independently represent one or more radicals selected from hydrogen, NH 2 , NO 2 ,...
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5714502 |
Piperidinylmethyloxazolidinones
The invention relates to novel piperidinylmethyloxazolidin-2-one derivatives of the formula I ##STR1## in which R 1 and R 2 in each case independently of one another are unsubstituted or mono- to...
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5710169 |
Therapeutic heterocycles
Compounds of formula I ##STR1## wherein Q 1 , Q 2 , Q 3 , Q 4 , and Q 5 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are...
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5710153 |
Tetrazole compound
A tetrazole derivatives of formula (I) ##STR1## a non-toxic salt thereof, an acid addition salt thereof or a hydrate thereof which has an inhibitory effect on interleukin-1β converting enzyme (ICE).
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5710168 |
2-piperidino-1-alkanol derivatives as neuroprotective agents
A method of blocking N-methyl-D-aspartic acid (NMDA) receptor sites in a mammal in need thereof with an effective NMDA blocking (neuroprotective and antiischemic) amount of 2-piperidino-1-alkanol...
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5703104 |
Cyclic amides and derivatives thereof
Compounds, topical compositions and methods useful for preventing the penetration of toxic chemicals through the skin of a mammal are disclosed. The compounds of the invention provide an enhanced...
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5703065 |
Heteroarylamino and heteroarylsulfonamido substituted 3-benyzlaminomethyl piperidines and related compounds
The invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof, wherein A, W, P, R 3 , Q and R 1 are as defined herein. The compounds of formula I, and...
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5698581 |
Substituted N-heteroaroylguanidines, a process for their preparation, their use as a medicament or diagnostic agent, and a medicament containing them
The invention relates to heteroaroylguanidines of the formula I ##STR1## in which the substituents HA and R(1) to R(5) have the meanings given in the specification. These compounds exhibit very...
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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...
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5696134 |
Irreversible HIV protease inhibitors, intermediates, compositions and processes for the preparation thereof
Novel cis-epoxide compounds of formula (I) are useful for treating or preventing diseases caused by HIV infection: ##STR1## wherein A, B, R 1 to R 4 and n have the same meanings as defined in the...
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5696142 |
Aminoalkyloximes
Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.
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5693674 |
Method of using triaryl-ethylene derivatives in the treatment and prevention of osteoporosis
The present invention relates to a method of using triaryl-ethylene derivatives in the treatment or prevention bone tissue loss or osteoporosis.
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5691329 |
Compounds containing basic and acidic termini useful as fibrinogen receptor antagonists
This invention relates to novel compounds containing basic and acidic termini, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using...
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5691356 |
Disubstituted heterocyclic thrombin inhibitors
Disubstituted heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein G is ##STR2## wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; p is 0, 1 or 2, Q...
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5691368 |
Substituted oxazolidine calpain and/or cathepsin B inhibitors
This invention relates to oxazolidine inhibitors of calpain and/or cathepsin B and to compositions containing them. As inhibitors of calpain and/or cathepsin B, the compounds are useful in the...
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5688804 |
3-Benzylamino-2-phenyl-piperidine derivatives as substance P receptor antagonists
The present invention relates to the derivatives of the compound of formula (I), which are useful in the treatment of inflammatory and central nervous system disorders, as well as other diorders...
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5686463 |
Oxadiazoles useful in the treatment of senile dementia
A class of novel oxadiazoles, substituted on one of the ring carbon atoms with a non-aromatic azacyclic or azabicyclic ring, and substituted on the other ring carbon atom with a substituent of low...
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5684004 |
Triaryl-ethylene derivatives
The present invention relates to novel triaryl-ethylene derivatives that are useful as anti-neoplastic agents, antiatherosclerotic agents, and hypocholesterolemic agents.
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5670511 |
Indolepiperidine derivatives
Indolepiperidine derivatives of the formula I ##STR1## and their physiologically acceptable salts exhibit action on the central nervous system, in particular dopamine-agonistic or...
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5668159 |
1,3,4-thiadiazoles and 1,3,4-oxadiazoles as IIb/IIIa antagonists
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5668161 |
Substituted thiazoles for the treatment of inflammation
A class of substituted thiazolyl compounds is described for use in treating inflammation disorders. Compounds are defined by Formula II ##STR1## wherein R 1 is selected from hydrido, alkyl,...
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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##...
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