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5968954 |
2-aminoindan compounds as 5HT.sub.1B antagonists
New 2-aminoindan compounds of formula: ##STR1## wherein: n, Ar, R, E, X 1 , X 2 , X 3 , and X 4 are as defined in the description, in the form of a racemic mixture and in the form of optical...
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5965575 |
N-aryl piperidine compounds as 5HT.sub.1B antagonists
New N-arylpiperidine compounds of formula: ##STR1## wherein: A, m, R, E, n and Ar are as defined in the description, the isomers thereof and the addition salts thereof with a pharmaceutically...
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5958950 |
Benzimidazole compounds useful for the treatment of inflammatory disease, atherosclerosis, restenosis or inhibiting lipoxygenase
A method for the treatment of inflammatory disease or condition atherosclerosis or restenosis or for inhibiting 15 lipaxygenase in a mammal in need thereof comprising administering to such mammal...
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5955475 |
Process for manufacturing paroxetine solid dispersions
Solid dispersions of poorly soluble drugs are disclosed which are prepared using a solvent or fusion process. Such dispersions are manufactured with the free base of the drug, specifically...
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5955459 |
Fatty acid-antipsychotic compositions and uses thereof
The invention provides compositions that include conjugates of a fatty acid molecule, preferably cis-docosahexaenoic acid, and antipsychotic agents. The conjugates are usefull in treating psychotic...
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5952349 |
Muscarinic antagonists for treating memory loss
1,4 Di-substituted piperidine muscarinic antagonists of formula I ##STR1## or a pharmaceutically acceptable salt, ester, or solvate thereof, wherein X is a bond, --O--, --SO 0 -2 --, --CO--, --C(OR...
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5952351 |
Alpha 1a adrenergic receptor antagonists
This invention relates to novel compounds, their synthesis and use as selective α 1a adrenergic receptor antagonists. One application of the compounds is in the treatment of benign prostatic...
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5952354 |
Tris carbamic acid esters: inhibitors of cholesterol absorption
Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in the inhibition of the esterification of cholesterol and are...
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5942512 |
Method and composition for treating erectile dysfunction
Lipophilic active substance composition and its use in a new method of treating erectile dysfunction by administration thereof, optionally together with a hydrophilic vehicle and optionally an...
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5935973 |
Heterocyclcarboxamide derivatives and their use as therapeutic agents
Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R 1 is an optional substituent; U is an alkylene...
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5919778 |
Cyclic amide derivatives
The cyclic amide derivative is defined by the formula (I) or a salt thereof: R1-(CH2)n-Z in which R1 is a group derived from a cyclic amide compound, substituted or unsubstituted, n is zero or an...
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5919798 |
4-heteroaryl-1-piperidinealkanols 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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5919802 |
Methods of preventing and/or treating temporal lobe epilepsy
A method of preventing and/or treating epileptic seizures in a mammal in need of such treatment, which comprises administration to said mammal of a therapeutic amount of a 5HT1A antagonist.
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5919797 |
Halogenated naphthyl methoxy piperidines for mapping serotonin transporter sites
Halogenated naphthyl methoxy piperidines having a strong affinity for the serotonin transporter are disclosed. Those compounds can be labeled with positron-emitting and/or gamma emitting halogen...
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5916902 |
Processes and intermediates for preparing 5, 7-dihydro-3- 2-(1-benzylpiperidin-4-yl)ethyl-!6H-pyrrolo- 4, 5-F!-1, 2-benzisoxazol-6-one
This invention relates to a process for preparing the compound having the formula ##STR1## which comprises i) heating the compound of formula ##STR2## wherein R 3 is R 4 or benzyl and R 4 is R 5...
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5900423 |
Form of paroxetine hydrochloride anhydrate
"Paroxetine hydrochloride (I) anhydrate ##STR1## free of bound propan-2-ol, and various forms thereof, are useful in the treatment of depression and other disorders for which administration of...
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5889035 |
1-(Arylthioalkyl, arylaminoalkyl or arylmethylenealkyl)-3-(heteroaryl) pyrrolidines 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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5886011 |
Piperidine derivatives as substance P antagonists
Piperidine derivatives represented by general formula (I) ##STR1## or pharmaceutically acceptable acid addition salts thereof: wherein n represents an integer of 0 or 1; X represents CH 2 , O or...
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5883109 |
Method for lowering serum lipid levels employing an MTP inhibitor in combination with another cholesterol lowering drug
A method is provided for lowering serum lipids, cholesterol and/or triglycerides and thereby inhibiting atherosclerosis by administering to a patient an MTP inhibitor, in combination with a...
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5880121 |
4,5-dihydronaphth (1,2-c) isoxazoles and derivatives thereof
4,5-Dihydronaphth 1,2-c!isoxazole derivatives of the general formula: ##STR1## where A, X and n are defined herein are disclosed. Such compounds are useful as serotonin 5-HT 3 antagonists. These...
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5877171 |
Method of treating pre-menstrual syndrome using chromium
The method of this invention is directed to a treatment of depression in men and women and to a treatment of pre-menstrual syndrome (PMS) in women by administering to a patient a therapeutically...
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5874432 |
Saccharin derivatives useful as proteolytic enzyme inhibitors and compositions and method of use thereof
Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula ##STR1## wherein: L is --O--,...
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5874447 |
4-Phenylpiperidine compounds for treating depression
The invention relates to a compound, and pharmaceutically acceptable salts, having the formula I: ##STR1## wherein: R represents an alkyl or alkynyl group having 1-4 carbon atoms, or a phenyl group...
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5874431 |
Benzazole compounds
There are disclosed herein benzazole compounds, exemplified by 2-(4-aminophenyl)benzothiazole and analogues or salts thereof, which exhibit very significant selective cytotoxic activity in respect...
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5866589 |
Alkyl substituted piperadinyl and piperazinyl anti-AIDS compounds
Anti-AIDS compounds of formula (I) ##STR1## wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 are as defined in the specification and R 8 is alkyl of substituted alkyl.
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5861429 |
13-substituted milbemycin 5-oxime derivatives, their preparation and their use against insects and other pests
Compounds of formula (I): ##STR1## wherein: R 1 is methyl, ethyl, isopropyl or sec-butyl; X is carbonyl or methylene; Z is C(R 2 ) 2 or C(CH 2 ) m , in which R 2 is alkyl, and m is...
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5861415 |
Bioprotectant composition, method of use and extraction process of curcuminoids
Curcuminoids have been found to have anti-oxidant, anti-inflammatory, antibacterial, antifungal, antiparasitic, anti-mutagen, anticancer and detox properties. The present invention is directed to...
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5856349 |
2-Saccharinylmethyl heterocyclic carboxylates useful as proteolytic enzyme inhibitors and compositions and method of use thereof
4-R 4 -R 5 -2-Saccharinylmethyl heterocyclic carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R 4 -R 5 -2-halomethylsaccharin with either a...
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5854263 |
1- (1,4-benzodioxanyl)alkyl!-3-(heteroaryl) pyrrolidines 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...
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5854243 |
3-heteroaryl-1-pyrrolidinealkylthiols 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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5834499 |
5-HT.sub.3 receptor agonist, novel thiazole derivative and intermediate thereof
A 5-HT 3 receptor against containing a thiazole derivative as the effective ingredient is provided and is represented by the Formula (I): ##STR1## wherein the A ring is substituted or...
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5817665 |
Composition and method of treating depression using naloxone or naltrexone in combination with a serotonin reuptake inhibitor
This invention relates to a composition and method for treating depression by administering to a patient a pharmacologically effective dose of an opioid antagonist having a pentacyclic nucleus...
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5811435 |
2- (4-heteroaryl-1-piperidinyl)alkyl!-1,3-dioxanes 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...
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5811436 |
Oral liquid compositions containing paroxetine resinate
An oral liquid pharmaceutical composition comprising a paroxetine-Amberlite IRP88 complex.
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5789449 |
Treatment of symptoms associated with premenstrual disorders
There is disclosed a method for treating certain psychiatric symptoms including anger, rejection sensitivity and a lack of mental or physical energy with administration of a nontoxic dose of a...
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5786372 |
Heteroaryl compounds used as pharmaceuticals
Compounds of formula (I), or pharmaceutically acceptable salts thereof are provided: ##STR1## in which X 1 --(CH 2 ) x --X 2 forms a 5-7 membered ring wherein: X 1 is O or S; X 2 is O, S...
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5783589 |
2-saccharinylmethyl aryl and arloxy acetates useful as proteolytic enzyme inhibitors and compositions and method of use thereof
4-R 4 -R 5 -2-Saccharinylmethyl aryl and aryloxy acetates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R 4 -R 5 -2-halomethylsaccharin with an aryl or...
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5780474 |
3-(piperid-4-yl)-1,2-benzisoxazole and 3-(piperazin-4-yl)-1,2-benzisoxazole compounds
Compounds of formula: ##STR1## wherein: A, m, n, E and Y are as defined in the description, the optical isomers thereof and the physiologically-tolerable salts thereof. These compounds, their...
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5776963 |
3-(heteroaryl)-1- (2,3-dihydro-1h-isoindol-2-yl)alkyl!pyrrolidines and 3-(heteroaryl)-1- (2,3-dihydro-1h-indol-1-yl)alkyl!pyrrolidines and related compounds and their therapeutic untility
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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5773456 |
Saccharin derivative proteolytic enzyme inhibitors
Compounds having the structural formula ##STR1## wherein L is N, O or SO n wherein n is 0, 1 or 2; L--R 1 is a leaving group, H--L--R 1 is the conjugate acid thereof and, when L is N, H--L--R...
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5773434 |
Facilitation of AMPA receptor-mediated synaptic transmission in brain as a treatment for schizophrenia
Psychotic symptoms are treated by the administration of drugs which amplify the ability of natural stimulators of AMPA receptors to enhance the mediation of excitatory synaptic response. What is...
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5770598 |
Heterocyclic compounds
The present invention relates to heterocyclic compounds which have been found to have anti-tumour activity. More specifically, the invention concerns Pyrrolo 3,2-b! carbazoles, 1H-Benzofuro ...
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5767116 |
Bicyclic aromatic compounds as therapeutic agents
Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or --O--; B is methylene or --O--; and g is 0, 1, 2, 3 or 4; R 1 , R 2 , R 3 , R 4 , U, Q...
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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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5760054 |
Alpha IC adrenergic receptor antagonists
This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1C adrenergic receptor antagonists. One application of these compounds...
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5753661 |
Fused benzo compounds containing a nitrogen heterocycle for the treatment of central nervous system disorders
Fused benzo compounds of formula I are provided, wherein A is a 2 to 6 membered hydrocarbon spacer group, B is a polar divalent group selected from a group (a); U is C, N or CH; X is a divalent 3-4...
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5750542 |
Benzisoxazole and benzisothizole derivatives as cholinesterase inhibitors
Described herein are compounds of the formula ##STR1## wherein R 1 R 2 , R 7 , R 8 , X, Y, M and L are defined as below. The compounds of formula I are cholinesterase inhibitors and are useful in...
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5744484 |
Lubeluzole intravenous solutions
A solution is disclosed for intravenous administration containing lubeluzole or a pharmaceutically acceptable addition salt thereof, an isotonizing agent, water and acid and base substances to...
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5744501 |
Method for treating late luteal phase dysphoric disorder
There is disclosed a method for treating Late Luteal Phase Dysphoric Disorder with administration of a nontoxic dose of a serotonin re-uptake blocker. Preferably, the serotonin re-uptake blocker is...
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5736558 |
4-(6-fluoro-1,2-benzisoxazolyl)-1 piperidinyl-propoxy-chromen-4-one-one-derivatives, their preparation and their use in the treatment of psychosis, schizophrenia and anxiety
The present invention relates to 4-(6-fluoro-1,2-benzisoxazolyl)-1-piperidinyl-propoxy-chrome
n-4-one derivatives having the formula (I): ##STR1## wherein R is hydrogen or alkyl having 1 to 4...
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