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7550469 |
Heterocyclic amide derivatives and their use as dopamine D3 receptor ligands
The invention relates to heterocyclic substituted amide derivatives that display selective binding to dopamine D 3 receptors. In another aspect, the invention relates to a method for treating...
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7524841 |
4,4-disubstituted piperidine derivatives having CCR3 antagonism
The invention provides low molecular compounds having activity which inhibits binding of CCR3 ligands to CCR3 on target cells, i.e. CCR3 antagonists. The invention also provides...
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7517875 |
Piperidine derivatives having CCR3 antagonism
The invention provides low molecular compounds having activity which inhibits binding of CCR3 ligands to CCR3 on target cells, i.e. CCR3 antagonists. The invention also provides compounds...
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7511064 |
Derivatives of 4-(thio- or selenoxanthene-9-ylidene)-piperidine or acridine and its use as a selective 5-HT2B receptor antagonist
The present invention relates to derivatives of 4-(Thio- or Selenoxanthene-9-ylidene)-piperidine or acridine and pharmaceutically acceptable salts thereof, use of these compounds as a medicament...
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7479500 |
Antidepressant piperidine derivatives of heterocyclefused benzodioxans
Compounds of the Formula:
are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder,...
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7470710 |
N-aroyl cyclic amine derivatives as orexin receptor antagonists
This invention relates to N-aroyl cyclic amine derivatives of formula (I), wherein X represents a bond, oxygen, NR 3 or a group (CH 2 ), wherein n represents 1, 2 or 3; Y represents CH 2 , CO,...
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7468443 |
Alkyl ether derivatives or salts thereof
An alkyl ether derivative represented by the general formula:
wherein each of R 1 and R 2 represents one or more groups selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl...
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7462630 |
Diarylalkene derivatives and novel diarylalkane derivatives
The invention relates to a compound represented by the following general formula (1) or its analogue, which selectively inhibit N-type calcium channels or its analogue, and to a method for treating...
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7449481 |
Thio-substituted biaryl-methanesulfinyl derivatives
The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that...
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7449483 |
Heteroaromate OSC inhibitors
The present invention relates to heteroaromate OSC inhibitors. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol...
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7326716 |
Treatment of inflammatory bowel disease
The present invention provides a method of treating inflammatory bowel disease which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of...
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7282497 |
Pyrrolidin-2-one derivatives as inhibitors of factor xa
The invention relates to compounds of formula (Ic)
processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the...
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7271264 |
Pentacyclic oxepines and derivatives thereof, compositions and methods
The present invention provides a compound of the formula (I) wherein R 1 is —H, —OH, —O(C 1 -C 4 alkyl), —OCOC 6 H 5 , —OCO(C 1 -C 6 alkyl), or —OSO 2 (C 2 -C 6 alkyl); R 0 , R 2 ...
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7238713 |
Muscarinic agonists
Compounds and methods are provided for the treatment of disease conditions in which modification of cholinergic, especially muscarinic m1, m4, or both m1 and m4, receptor activity has a beneficial...
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7226934 |
Optically active isomers of ketotifen and therapeutically active metabolites thereof
Racemic norketotifen, racemic 10-hydroxy-ketotifen, racemic 10-hydroxy-nor-ketotifen and optically active isomers of ketotifen, norketotifen, 10-hydroxy-ketotifen and 10-hydroxy-norketotifen were...
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7208491 |
N-monoacylated o-phenylenediamines
Mono-acylated o-phenylendiamines derivatives of formula I
wherein X and R are as described herein, have been found useful for the treatment of diseases mediated by the inhibition of histone...
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7157454 |
Derivatives of n-(arylsulfonyl)beta-aminoacids comprising a substituted aminomethyl group, the preparation method thereof and the pharmaceutical compositions containing same
The invention relates to compounds of formula:
These compounds show affinity for the bradykinin receptors with selectivity towards the B 1 receptors; they may be used for the preparation of...
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7148240 |
Aminoalkoxybenzoyl-benzofuran or benzothiophene derivatives, method for preparing same and compositions containing same
The invention relates to benzofuran or benzothiophene derivatives of general formula:
These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes...
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7144883 |
Bicyclic sulfonamide compounds
The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful...
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7144898 |
Indole derivatives for the treatment of depression and anxiety
The present invention provides compounds of formula (I): which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of...
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7112594 |
Fused bicyclic amide compounds and medicinal use thereof
Compounds represented by the following general formula (I) wherein ring A is benzene, cyclohexane, pyridine, piperidine, a derivative thereof, imidazole, a derivative thereof, etc.; the ring B...
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7071201 |
Quinoline derivatives
A novel compound of the formula:
wherein A, B, C, D, T, Y, and Z represent each methine or nitrogen; R 1, R 2 , R 3 , R 4 , and R 5 represent each a substituent; n represents 0 or an integer...
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6984637 |
Cyclic amine derivatives-CCR-3 receptor antagonists
This invention relates to certain cyclic amine derivatives of Formula (I)
that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods...
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6977263 |
Chemical compounds
Provided herein are novel and useful compounds having a tryptase inhibition activity, pharmaceutical compositions comprising such compounds, and methods treating subjects suffering from a...
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6977265 |
Piperidine CCR-3 receptor antagonists
The invention provides compounds of Formula (I):
wherein: R 1 -R 5 , A, L, and X have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical...
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6916831 |
Flavone acetic acid analogs and methods of use thereof
Compounds are described having a structure according to Formula I or Formula II:
wherein: X is selected from the group consisting of O, NH, and S; Y is selected from the group consisting of O...
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6908922 |
Linear cyclic ureas
Compound of formula (I):
wherein:
V represents a single bond or an alkylene chain, M represents a single bond or an alkylene chain, A and E each represents nitrogen or CH, but at least...
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6897211 |
Thienodibenzoazulene compounds as tumor necrosis factor inhibitors
The present invention relates to the dibenzoazulene compounds represented by formula I as well as to their pharmaceutical preparations for the inhibition of tumor necrosis factor alpha (TNF-α) and...
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6894064 |
Benzothiophenes, formulations containing same, and methods
This invention provides compounds of formula I
and pharmaceutically acceptable salts and solvates thereof, characterized that the compound is in particulate form and having a specific size...
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6861530 |
Piperidine derivatives
This invention relates to substituted piperidine derivatives having at least one six-membered ring substituent. The piperidine derivatives exhibit antitumor activity and are useful as...
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6849658 |
Biaromatic compounds and pharmaceutical and cosmetic compositions comprising them
The invention concerns bi-aromatic compounds of formula (I) in which Ar represents (a), Z being O or S, R 1 is CH 3 , —CH 2 —O—R 6 , —OR 6 or —COR 7 ; R 2 is —OR 8 , —SR 8 or a...
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6844344 |
Benzofuran derivatives
The present invention provides compounds of formula (I) which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of...
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6787650 |
Urea compounds, process for producing the same and use thereof
A compound of the formula: [wherein R 1 is a hydrocarbon group which may be substituted; R 2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be...
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6784180 |
Piperidines derivatives and their use as serotonin receptor antagonists
The present invention provides compounds of formula (I): which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of...
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6767915 |
Substituted piperidines as melanocortin receptor agonists
Certain novel 4-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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6768007 |
Substituted 3′,4′-di-O-camphanoyl-(&plus )-cis-khellactone analogs, compositions thereof, and methods for using thereof
3′,4′-di-O-camphanoyl-(+)-cis-khellactone analogs according to the present invention have been found to have anti-HIV activity. The compounds of the present invention have the following...
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6756388 |
Benzothiophenes and related compounds as estrogen agonists
The invention is a compound of Formula (I): wherein R is —OH, R 1 is —OH, R 2 is —H, n is 2 or 3 and X is sulfur, or a pharmaceutically acceptable salt of a compound having Formula (1),...
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6743808 |
4-aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl) tetrahydropyridines or piperazines
4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl)piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I), wherein one of X and Y is CH 2 and...
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6740649 |
Cyclic hydroxamic acids as inhibitors of matrix metalloproteinases and/or TNF- α converting enzyme (TACE)
The present application describes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from...
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6730670 |
7-phenyl-benzo&lsqb b&rsqb thiophen amide derivatives
A compound of the formula Compounds of formula I have a good affinity to the A2A receptor and are useful for the treatment of diseases mediated by this receptor.
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6683093 |
Aromatic sulfone hydroxamic acids and their use as protease inhibitors
This invention is directed to aromatic sulfone hydroxamates (also known as aromatic sulfone hydroxamic acids) and salts thereof that, inter alia, tend to inhibit matrix metalloproteinase (also...
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6653479 |
Crystalline form of 6-hydroxy-3-(4-&lsqb 2-(piperidin-1-yl)ethoxy&rsqb phenoxy)-2-(4-methoxyphenyl)benzo&lsqb b&rsqb thiophene hydrochloride
The present invention is directed to a novel crystalline hydrate of 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-metho
xyphenyl)benzo[b]thiophene hydrochloride and uses for same,...
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6653328 |
3-benzyl-benzothiophenes
This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 3-benzyl-benzothiophenes which are α-substituted with ether, thioether amino, cyano or halo that are...
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6642228 |
α1b-adrenergic receptor antagonists
There are provided compounds represented by the general formula (I): [wherein Ar is indole etc., R 1 is hydrogen etc., B is bond, or B—N—R 1 forms a ring structure and is piperidine etc.,...
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6627645 |
Muscarinic agonists
Compounds and methods are provided for the treatment of disease conditions in which modification of cholinergic, especially muscarinic m1, m4, or both m1 and m4, receptor activity has a beneficial...
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RE38257 |
Piperdine derivatives and hypotensives containing the same
A piperidine compound of the formula (I): wherein A is a fused aromatic ring; R is hydrogen, chloro or methoxy; X is (CH 2 ) n , which may be substituted, in which n is 0 or an integer of 1 to...
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6617325 |
Biphenyl derivatives, production thereof and uses as medicines
The present invention relates to biphenyl derivatives of general formula wherein R a to R g and n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically...
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6608090 |
Benzothiophenes with novel basic side chains
The instant invention provides novel benzothiophene compounds for use in treating skeletal diseases.
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6579881 |
Indoles
A 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: wherein A, B, C, D, T, Y, and Z each represent a methine or a...
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6552043 |
Benzimidazolinyl piperidines as CGRP ligands
The present invention relates to benzimidazolinylpiperidine derivatives useful as ligands for CGRP (Calcitonin Gene-Related Peptide) receptors, their use in therapy, pharmaceutical compositions...
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