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7199265 |
Thyroid receptor ligands, pharmaceutical compositions comprising them and their use in the treatment of disorders influenced by thyroid hormones
This invention relates to compounds of the formula (I) which are thyroid receptor ligands, and are preferably selective for the thyroid hormone receptor β, to methods of preparing such compounds...
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7186276 |
Dye composition comprising at least one direct dye, dyeing processes, uses and multi-compartment devices
Disclosed herein is a dye composition for dyeing human keratin fibers, such as the hair, comprising a direct polycationic dye of formula (I) below:
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7179918 |
HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
Compounds of the formula:
where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as...
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7179826 |
Compositions useful as inhibitors of protein kinases
The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of...
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7169194 |
Dye composition comprising at least one particular tricationic direct dye, dyeing process, use and multi-compartment devices
A dye composition for dyeing human keratin fibers, such as hair, comprising at least one direct tricationic dye of formula (I) below:
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7166614 |
Tetrahydropyranyl cyclopentyl tetrahydroisoquinoline modulators of chemokine receptor activity
The present invention is directed to compounds of the formula I: I(wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n and the dashed line are defined herein) which are useful as modulators of...
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7160877 |
Aliphatic nitrogen-containing 5-membered ring compound
The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]:
wherein A represents —CH 2 — or —S—, R 1 represents...
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7157463 |
Substituted piperidines/piperazines as melanocortin receptor agonists
The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction
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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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7144895 |
Benzene acetamide compounds useful as serine protease inhibitors
Compounds having the formula (I),
and pharmaceutically-acceptable salts, hydrates, or prodrugs thereof, are useful as serine protease inhibitors, wherein X is —OH, —O(alkyl), —O(aryl),...
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7129261 |
Cytotoxic agents
The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming...
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7125871 |
Excitatory amino acid receptor modulators
Compounds of the formula (I) in which R 1 , R 2 and X 1 have the meanings given in the specification, modulate metabotropic glutamate receptor function and are useful in treating disorders of the...
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7125863 |
Inhibitors of dipeptidyl peptidase IV
Compounds according to formula (1), wherein R 1 is H or CN, X 1 is S, O, SO 2 or CH 2 , X 2 is CO, CH 2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The...
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7126001 |
Class of cytodifferentiating agents and histone deacetylase inhibitors, and methods of use thereof
The present invention provides the compound having the formula:
wherein each of R 1 and R 2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino,...
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7122673 |
Preparation of fused polycyclic alkaloids by ring closure of azomethine ylides, novel compounds thereof and their use as chemotherapeutic agents
A method for the preparation of a compound of general Formula:
or pharmaceutically acceptable derivatives and salts, racemates, isomers and/or tautomers thereof comprising cyclizing an...
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7122547 |
Anthranilic acid amides and the use thereof as medicaments
The invention relates to anthranilic acid amides and the use thereof as medicaments for the treatment of diseases that are triggered by persistent angiogenesis, in addition to intermediate products...
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7122559 |
Phenylglycine derivatives useful as serine protease inhibitors
Compounds having the formula (I),
or a stereoisomer or pharmaceutically-acceptable salt, or hydrate thereof, are useful as factor VIIa inhibitors, wherein X is —NR 6 S(O) p R 16 ; W is...
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7105507 |
Cyclohexane derivatives and their use as therapeutic agents
The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and...
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RE39265 |
Heteroarylpiperidines, and their use as antipsychotics and analgetics
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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7094262 |
Dye composition comprising at least one particular dissymetrical polycationic direct dye, dyeing process, use and multi-compartment devices
A dye composition for dyeing human keratin fibres, such as hair, comprising at least one dissymmetrical polycationic direct dye of formula (I) below:
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7078565 |
Benzamide derivatives as antagonists of orexin receptors
Disclosed are phenyl-alkylene benzamides useful as orexin antagonists
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7074796 |
4-phenyl-1-piperazinyl, -piperidinyl and -tetrahydropyridyl derivatives
The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I
wherein W is C, CH or N, and the dotted line emanating from W indicates a bond when W is C...
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7067533 |
Aminophenoxyacetamide derivatives and pharmaceutical composition containing thereof
The present invention relates to an aminophenoxyacetamide derivative of the formula (I):
wherein R 1 to R 4 are, independent from each other, a hydrogen atom or an optionally substituted...
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7041829 |
Antagonists of the magnesium binding defect as therapeutic agents and methods for treatment of abnormal physiological states
This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential...
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7041667 |
CCR5 modulators
Compounds of Formula 1
[R egion α]—[R egion β]—[R egion γ]—[R egion δ] (1)
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7037924 |
Glutamine fructose-y-phosphate amidotransferase (GFAT) inhibitors
Compounds of formula (I) are provided,
wherein R 1 and R 2 are as designated in the specification. The compounds have utility for the treatment of type 2 diabetes mellitus.
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7030239 |
Compounds to treat Alzheimer's disease
The present invention is directed toward substituted hydroxyethylene compounds of formula (XII)
useful in treating Alzheimer's disease and other similar diseases.
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7019003 |
Peptide deformylase inhibitors
Novel PDF inhibitors and novel methods for their use are provided.
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6992092 |
Anti-diabetic agents
The present invention provides compounds of formula (I)
the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs; wherein...
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6987118 |
Tetrahydroisoquinoline derivatives as PPAR-alpha activators
PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and...
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6984735 |
Process for making an aldehyde
A process for making an aromatic aldehyde in which a sulfoxide is reacted with a dihalogenated aromatic compound in the absence of an effective amount of an activating reagent. The aldehyde may...
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6956033 |
3,4-dihydroisoquinoline derivative compound and a pharmaceutical agent comprising it as active ingredient
A 3,4-dihydroisoquinoline derivative compound of formula (I) or a non-toxic salt thereof and a pharmaceutical agent comprising it as active ingredient (wherein all symbols have the same meaning as...
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6949565 |
Protein kinase inhibitors
Novel isoquinoline derivatives which are useful as inhibitors of protein kinases for experimental, medical, and drug design purposes are disclosed. Preferred compounds which are specific inhibitors...
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6943183 |
5-substituted tetralones as inhibitors of ras farnesyl transferase
The present invention provides novel 5-substituted tetralones of Formulas I, II, III, and IV and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof, which are useful for...
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6939986 |
Process for preparing 1,2-diamino compounds
The invention provides a multistep process for preparing 1,2-diamino compounds and pharmaceutically acceptable addition salts thereof from 1,2-epoxides.
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6936602 |
Benzazepine derivatives, process for the preparation of the same and uses thereof
Compounds of the general formula (I):
or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R 1 is a 5- to 6-membered...
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6930208 |
3-Keto- or 3- oxime-ether-substituted benzoylcyclohexanediones
What is described are derivatives of benzoylcyclohexanediones of the formula (I) and their use as herbicides.
In this formula (I), R 1a , R 1b , R 1c , R 2 , R 3 , R 4 and R 5 denote various...
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6916905 |
Dmt-Tic di-and tri-peptidic derivatives and related compositions and methods of use
A compound of formula:
wherein X is a spacer comprising one or more amino acid residues and Y comprises an aromatic group and related compositions and methods of use.
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6908931 |
Tetrahydroisoquinoline derivatives as melatonin MT2 antagonists
The invention encompasses a series of tetrahydroisoquinolines of formula I which are antagonists of the human melatonin MT 2 receptor and are useful as chronobiotic and sleep agents.
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6900319 |
Thrombin inhibitors
The invention relates to a compound of the formula I:
or a salt thereof with a physiologically tolerated acid, or stereoisomers thereof, wherein R 1 , R 2 , A, B, C and D have the meanings...
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6897319 |
Useful aroyl pyrrole heteroaryl methanones and methanols
This invention is directed to aroyl pyrrole heteroaryl methanone and methanol compounds pharmaceutically useful as agents for treating or modulating a central nervous system disorder and methods...
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6894041 |
Oxazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic...
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6878706 |
Cyanamides useful as reversible inhibitors of cysteine proteases
Compounds according to the following formula (I):
wherein the variables Q and R 1 to R 6 are as described herein, which reversibly inhibit the cysteine proteases, such as cathepsins K, S, F,...
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6855717 |
Tetrahydroisoquinoline derivatives as modulators of dopamine D3 receptors
Compounds of formula (I):
wherein:
R 2 represents a hydrogen atom or a C 1-4 alkyl group; q is 1 or 2;
A represents a group of formula (a) or (b)
wherein
T, U,...
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6849644 |
Isoquinoline derivatives useful in the treatment of CNS disorders
The invention relates to novel tetrahydroquinoline compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of...
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6849622 |
Aliphatic nitrogenous five-membered ring compounds
The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]:
wherein
A represents —CH 2 — or —S—, R 1 ...
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6838465 |
N-acyltetrahydroisoquinoline derivatives
This invention relates to novel compounds represented by the general formula [I]:
(wherein, R 1 and R 4 are the same or different, and represent hydrogen atoms, lower alkyl groups or the...
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6838479 |
Amidine inhibitors of serine proteases
Inhibitors of serine proteases are provided having formula (I)
wherein X, R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein. In particular, the compounds bind to factor VIIa, tissue...
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6825213 |
β3-adrenoreceptor agonists, agonist compositions and methods of using
The invention provides β 3 -adrenoreceptor agonists, pharmaceutical compositions comprising β 3 -adrenoreceptor agonist compounds, and methods of using such compounds for stimulating, regulating...
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6803466 |
HIV/FIV protease inhibitors having a small P3 residue
With the help of X-ray structural analyses of drug-resistant HIV proteases and molecular modeling, a new type of inhibitor with a small P3 residue has been developed. These inhibitors are effective...
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