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6750213 |
Estrogen receptor modulators
The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen...
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6750229 |
Methods for treating skin pigmentation
This invention relates to methods and compositions for bringing about changes in skin pigmentation. More particularly, this invention relates to compounds which affect melanogenesis and can be used...
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6734179 |
Benzothiazoles
The present invention relates to compounds of the formula wherein R1 and R2 are as described within. The compounds of formula I have been found to be adenosine receptor ligands. Specifically,...
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6730677 |
Benzofurazan compounds which enhance AMPA receptor activity
Compounds of general structural formula ( 1 ) are shown to have AMPA receptor enhancing properties. The compounds are useful for such therapeutic purposes as facilitating the learning of behaviors...
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6727263 |
Indole and 2,3-dihydroindole derivatives, their preparation and use
The present invention relates to indole and 2,3-dihydroindole derivatives having formula (I) or any of its any of its enantiometers or any mixture thereof, or an acid addition salt thereof,...
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6720003 |
Serotonin reuptake inhibitor formulations
A process for preparing amorphous paroxetine hydrochloride or sertraline hydrochloride is provided, which comprises preparing a solution in which paroxetine hydrochloride or sertraline...
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6706736 |
Antidepressant azaheterocyclylmethyl derivatives of oxaheterocycle-fused-&lsqb 1,4&rsqb -benzodioxans
Compounds of the formula useful for the treatment of depression such as obsessive compulsive disorder, panic attacks, generalized anxiety disorder, social anxiety disorder, sexual dysfunction,...
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6703408 |
N-formyl derivatives of paroxetine
A compound or composition comprising N-formyl paroxetine of formula (1) is useful as a pharmaceutical and as a synthetic intermediate. The N-formyl paroxetine can be an impurity in paroxetine...
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6699858 |
Halogen substituted tetracyclic tetrahydrofuran derivatives
This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero, 1, 2,...
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6699882 |
Paroxetine compositions
Paroxetine is adsorbed on a carrier to form a free-flowing powder useful for capsule filling or for tablet formulation; and used in therapy to treat depression.
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6689794 |
Aromatic sulfone hydroxamates 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, inhibit matrix metalloproteinase (also known...
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6683078 |
Use of sulfonyl aryl or heteroaryl hydroxamic acids and derivatives thereof as aggrecanase inhibitors
This invention is directed to a process for inhibiting aggrecanase activity. The process comprises administering a therapeutically effective amount of a sulfonyl aromatic or heteroaromatic...
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6673829 |
Aminoazetidine,-pyrrolidine and -piperidine derivatives
Novel aminoazetidine, -pyrrolidine, and -piperidine derivatives, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of...
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6667322 |
Antidepressant chroman and chromene derivatives of 3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H-indole
Compounds of the formula useful for the treatment of depression and other diseases such as obsessive compulsive disorder, panic attacks, generalized anxiety disorder, social anxiety disorder,...
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6660751 |
Sulfonamide derivatives as 5-HT7 receptor antagonists
The invention relates to novel sulfonamide compounds having 5-HT 7 receptor antagonist activity, processes for their preparation, to compositions containing them and to their use in the treatment...
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6656950 |
Antidepressant azaheterocyclylmethyl derivatives of 1,4-dioxino&lsqb 2,3-b&rsqb pyridine
Compounds of the formula useful for the treatment of depression, obsessive compulsive disorder, panic attacks, generalized anxiety disorder, social anxiety disorder, sexual dysfunction, eating...
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6656954 |
Sulfonyl divalent aryl or heteroaryl hydroxamic acid compounds
A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises...
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6653327 |
Cross-regulin composition of tumeric-derived tetrahydrocurcuminoids for skin lightening and protection against UVB rays
The present invention is directed to a mixture of tetrahydrocurcuminoids which can be used for regulating random, intracellular protein cross-linking an optimizing cell electric potential in a...
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6649614 |
Use of a NK-1 receptor antagonist and an antidepressant and/or an anti-anxiety agent for treatment of depression or anxiety
The present invention relates to the treatment of depression and/or anxiety by the administration of a combination of a specific class of NK-1 receptor antagonists and an antidepressant or...
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6642256 |
Piperidine derivatives as subtype selective N-Methyl-D-Aspartate antagonists
Described are piperidines of Formula I and pharmaceutically acceptable salts thereof. The compounds of Formula I are antagonists of NMDA receptor channel complexes useful for treating cerebral...
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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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6638948 |
Amorphous paroxetine composition
A free-flowing, amorphous paroxetine hydrochloride composition suitable as a therapeutic agent for premature ejaculation can be prepared by dissolving paroxetine free base in a hydrochloric...
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6635643 |
Bicyclic benzamides of 3- or 4-substituted 4-(aminomethyl)-piperidine derivatives
The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R 1 and R 2 ...
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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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6620843 |
Anticancer treatment using triptolide prodrugs
Water soluble triptolide prodrugs are used as anticancer agents, and are found to be more effective in vivo, at lower doses, in reducing tumor size than the widely used chemotherapeutic agents...
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6620815 |
Oxazolidinones and uses thereof
This invention is directed to oxazolidinone compounds which are selective antagonists for human α 1A receptors. This invention is also related to uses of these compounds for lowering intraocular...
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6617334 |
Antidepressant azaheterocyclylmethyl derivatives of 7,8-dihydro-1,6,9-trioxa-3-aza-cyclopenta&lsqb a&rsqb naphthalene
Compounds of the formula: useful for the treatment of depression and other diseases such as obsessive compulsive disorder, panic attacks, generalized anxiety disorder, social anxiety disorder,...
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6613776 |
Pyrazole compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula V: wherein Z 1 is N, CR a , or CH, and Z 2 is N or CH, provided...
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6613780 |
Heat shock factor activity inhibitor
A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor. The novel compound benzo-1,3-dioxole provides an inhibitor of HSF activity or an...
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6602881 |
Anti-inflammatory uses of manzamines
The subject invention pertains to compounds which are useful as anti-inflammatory agents and to compositions containing such compounds as active ingredients. The novel uses of the compounds relate...
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6589956 |
Benzenesulphonamide compounds
A compound of formula (I): wherein: R a represents a hydroxy, alkoxy, aryloxy or arylalkyloxy group, A represents a CH group or a nitrogen atom, in which case R 1 is as defined in the...
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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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6576630 |
Compounds and compositions as protease inhibitors
The present invention relates to novel alkanoyl-substituted heterocyclic derivatives which are cysteine protease inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses...
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6559169 |
Antidepressant azaheterocyclymethyl derivatives of 2,3-dihydro-1,4-benzodioxan
Compounds of the formula useful for the treatment of depression and other conditions such as obsessive compulsive disorder, panic attacks, generalized anxiety disorder, sexual dysfunction,...
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6552049 |
Antidepressant azaheterocyclylmethyl derivatives of oxaheterocycle-fused-&lsqb 1,4&rsqb -benzodioxans
Compounds of the formula useful for the treatment of depression such as obsessive compulsive disorder, panic attacks, generalized anxiety disorder, social anxiety disorder, sexual dysfunction,...
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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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6548516 |
1-(3-heteroarylpropyl- or -prop-2-enyl)-4-benzylpiperidines used as NMDA receptor antagonists
Piperidine derivatives of the formula I and their physiologically acceptable salts in which X, Y, Z, R 1 , R 2 , R 3 and R 4 are as defined in claim 1 can be as excitatory amino acid...
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6548084 |
Controlled release compositions
A controlled release or delayed release formulation contains a selective serotonin reuptake inhibitor (SSRI) such as paroxetine.
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6541478 |
Smoking cessation treatments using naltrexone and related compounds
Nicotine dependency is treated by administration of an opioid antagonist. In some embodiments, rapid or ultra rapid detoxification techniques include using a combination of an effective amount of...
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6528514 |
IgE antibody production inhibitors and autoimmune diseases inhibitors
The present invention relates to an IgE antibody production inhibitor and an autoimmune disease suppressant containing a heterocyclic amide compound represented by the following general formula (1)...
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6514967 |
Compound for preparing medicines for treating pathologies involving extracellular glutamate, and methods for obtaining same
The invention relates to compounds of the following general formula (I): in which: R 1 and R 2 represent a hydrogen atom, or form a ring, especially a benzene ring, R 3 represents a hydrogen...
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6509368 |
Use of catechol derivatives as proteinase inhibitors
Use of catechol derivatives of the general formula I wherein R 1 to R 5 are as defined according to claim 1 , as protease inhibitors.
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6500846 |
CDK inhibitors having flavone structure
The present invention relates to a novel flavone derivative, pharmaceutically acceptable salt, hydrate, solvate and isomer thereof which is useful as an inhibitor against Cyclin Dependent Kinase...
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6500818 |
Naphthalenecarboxamides as tachykinin receptor antagonists
Compounds having the following formula wherein L, M, R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , X 1 and X 2 are as defined in the specification, pharmaceutically-acceptable salt thereof, useful for...
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6500845 |
Lactam derivatives as immunomodulating agents
The invention relates to the use of certain lactam derivatives corresponding to the formula I as pharmaceutical compounds with immunomodulatory activity, to new lactam derivatives, and to...
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6498161 |
Pyrrolidine modulators of chemokine receptor activity
The present invention is directed to pyrrolidine compounds of the formula I: (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and n are defined herein) which are useful as modulators of chemokine...
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6498170 |
Cyclamine sulfonamides as β-3 adrenergic receptor agonists
This invention provides compounds of Formula I having the structure wherein R 1 , R 2 , R 3 , W, X, and Z are as defined hereinbefore or a pharmaceutically acceptable salt thereof, which are...
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6495568 |
Hydroxamic acid derivatives as matrix metalloprotease (MMP) inhibitors
Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line...
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6489340 |
Macrolide compounds for inducing chondrogenic differentiation
Chondrogenic differentiations is induced by administering a macrocyclic lactone to mammals to prevent or treat damage to cartilage.
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6479517 |
Phosphorous-containing benzothiophenes
This invention relates to the fields of pharmaceutical and organic chemistry and provides novel phosphorous-containing benzothiophene compounds which are useful for the treatment of the various...
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