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6878700 |
Cell adhesion-inhibiting antiinflammatory and immune-suppressive compounds
The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immunune diseases, to pharmaceutical compositions containing these compounds, and to methods...
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6878737 |
Reversal of multidrug resistance in human colon carcinoma cells
The present invention describes the use of fumitremorgin A, B and C and a series of diketopiperazines of Formula (I) to resensitize multidrug resistant (MDR) cancer cells to the cytotoxic effects...
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6875439 |
Formulation containing amphipathic weak base and/or amphipathic cation and multiple drug resistance inhibitor
Methods are provided relating to the enhanced cytoplasmic accumulation of amphipathic weakly basic or amphipathic cationic molecules in prokaryotes and eukaryotes under conditions of high...
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6875770 |
Indole derivative having heterocycle and mono- or diazaindole derivative
There is provided a compound represented by the general formula (1):
wherein Het represents an optional substituted heterocylic group A 1 and A 2 each independently represent —CH═, etc.;...
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6867203 |
Cell adhesion-inhibiting antiinflammatory and immune-suppressive compounds
The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immune diseases and cerebral vasospasm, to pharmaceutical compositions containing these...
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6867200 |
(Hetero)aryl-bicyclic heteroaryl derivatives, their preparation and their use as protease inhibitors
The present invention provides novel compounds of the Formula (I): A-B, its prodrug forms, or pharmaceutically acceptable salts thereof, wherein A represents a saturated, unsaturated, or a...
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6867184 |
Methods of treating diabetic cardiomyopathy using glycogen phosphorylase inhibitors
The present invention provides methods of treating diabetic cardiomyopathy, the methods comprising administering to a patient having or at risk of having diabetic cardiomyopathy a therapeutically...
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6861443 |
Positive modulators of nicotinic receptors
The present invention relates to pharmaceutical compositions comprising a positive modulator of a nicotinic receptor agonist, said positive modulator having the capability to increase the efficacy...
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6861418 |
4-aryl substituted indolinones
The present invention relates to 4-arylindolinones, as well as pharmaceutical compositions thereof, capable of modulating protein kinase signal transduction in order to regulate, modulate and/or...
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6861444 |
Bicyclic compounds
Compounds of the general formula (I):
or a salt thereof, wherein R 1 is hydrogen, hydroxyl or halogen; R 2 is NHSO 2 CH 3 , SO 2 NHCH 3 or the like; R 5 and R 6 each independently is...
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6858641 |
Substituted indolinones
The present invention relates to indolinones substituted in the 6-position of general formula
wherein
R 1 to R 5 and X are defined as in claim 1, the isomers and the salts thereof,...
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6855729 |
Treatment of fibromyalgia and related fatigue syndromes using antagonists or partial agonists of 5HT1a receptors
The present invention provides a method for treating fibromyalgia and/or chronic fatigue syndrome by administering an antagonist or partial agonist of 5HT1 a receptors.
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6849654 |
5-methoxy-carbonylamino-N-acetyltryptamine compounds and derivates thereof
Compositions comprising 5-methoxy-carbonylamino-N-acetyltryptamine compounds and derivatives thereof for the treatment of depression are disclosed.
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6846492 |
Use of phenylethylamine derivatives for the antimicrobial treatment of surfaces
The use of compounds of formula (1) is described, in which compounds R 1 , R 2 and R 3 are each independently of the others hydrogen; C 1 -C 20 alkyl; C 3 -C 7 cycloalkyl; C 2 -C 20 alkenyl; C 4...
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6841563 |
Aryloxy propanolamines for improving livestock production
Disclosed is a compound represented by structural formula (I): R1 is a substituted or unsubstituted aryl group. R2 and R3 are independently —H, a C1-C4 straight chained or branched alkyl group....
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6838484 |
Formulations comprising selective androgen receptor modulators
The present invention relates to pharmaceutical compositions and formulations comprising a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic...
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6835729 |
2-phenyl-1-&lsqb 4(2-aminoethoxy)-benzyl&rsqb -indoles as estrogenic agents
The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: which are useful in lowering cholesterol levels.
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6833383 |
Methods for treating patients suffering from drug dependencies which lead to plasma melatonin deficiencies
A method of treating a patient suffering from a dependence on, tolerance of, or addiction to at least one benzodiazepine comprises administering melatonin to said patient on a daily basis in an...
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6833384 |
Deacetylase inhibitors
The present invention provides hydroxamate compounds which are deacetylase inhibitors. The compounds are suitable for pharmaceutical compositions having anti-proliferative properties.
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6818665 |
Treatment of obstructive sleep apnea
The method is for a hormonal treatment to compensate for the weakening of farynx components, tongue, tonsils, uvula, soft palate that occur during deep sleep and blocks the airways to cause...
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6815440 |
Cyclic and heterocyclic N-substituted α-iminohydroxamic and -carboxylic acids
Cyclic and heterocyclic N-substituted α-iminohydroxamic and -carboxylic acids Compounds of the formula I are suitable for preparing pharmaceuticals for the treatment of disorders in the course...
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6809098 |
Compounds
The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity. The invention also relates to pharmaceutical formulations, the use...
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6794407 |
Methods for treating circadian rhythm phase disturbances
A method for treating circadian rhythm phase disorders is described. The invention provides methods to specifically advance or delay the phase of certain circadian rhythms in humans. The disclosed...
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6794406 |
Indole derivatives
The invention relates to new indole derivatives, processes for their preparation, and their use in medicaments.
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6787535 |
Indole derivatives with 5HT6 receptor affinity
This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula I: wherein one of R 5 , R 6 or R 7 is a group of general Formula B,...
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6780884 |
Derivating of tryptamine and analogous compounds and pharmaceutical formulations containing them
This invention relates to novel substituted tryptamines and related derivatives, as well as pharmaceutical compositions formulated therefrom. These compounds, compositions and their salts can be...
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6765014 |
1-Acyl-7-nitroindoline derivatives, their preparation and their use as photocleavable precursors
Photoreleasable compounds comprising a caging moiety linked to an effector moiety represented by structural formula (I) wherein R 1 is hydrogen; C 1-10 alkyl or substituted alkyl; O(CH 2 ) n...
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6762182 |
Converting cox inhibition compounds that are not COX-2 selective inhibitors to derivatives that are COX-2 selective inhibitors
A method of altering specificity of cyclooxygenase-inhibiting compounds that have a COOH moiety by changing the various COOH containing compounds, such as indomethacin, into ester derivatives or...
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6762193 |
Method of treating hair loss
A method of treating inflammatory skin diseases and/or hair loss, comprising administering to a patient in need of such treatment a therapeutically effective amount of a leukotriene receptor...
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6759427 |
Synthesis and methods of use of tetrahydroindolone analogues and derivatives
A tetrahydroindolone derivative or analogue comprises a 9-atom bicyclic moiety, moiety A, linked through a linker L to a moiety B, where B is a carboxylic acid, a carboxylic acid ester, or a moiety...
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6756396 |
Ethylene glycol esters as photoactive agents
New compounds useful in photodynamic therapy are of the formula and their 1,4-diene isomers and the metallated and/or labeled and/or conjugated forms thereof wherein each R 1 is independently...
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6743793 |
Indole derivatives, process for preparation of the same and use thereof
Indole derivatives represented by formula (I): (wherein all symbols are described in the description), a process for the preparation of the same and a DP receptor antagonist comprising it as an...
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6740654 |
Squaric acid derivatives
Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L 2 is a covalent bond or an atom or group —O—,...
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6737435 |
Indole derivatives and their use as MCP-1 antagonist
A compound of formula (1) wherein R1 is hydrogen, halo or methoxy, R2 is hydrogen, halo, methyl, ethyl or methoxy; R3 is carboxy, tetrazolyl, or —CONHSO 2 R 4 where R 4 is methyl, ethyl,...
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6730700 |
3,4,5,-trisubstituted aryl nitrone compounds and pharmaceutical compositions containing the same
Disclosed are 3,4,5-trisubstituted aryl nitrone compounds and pharmaceutical compositions containing such compounds. The 3,4,5-trisubstituted aryl nitrone compounds have formula (I); where R 1 -R 4...
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6727237 |
Inhibitors of bacterial NAD synthetase
The present invention provides methods of synthesizing and screening inhibitors of bacterial NAD synthetase enzyme, compounds thereof, and methods of treating bacterial and microbial infections...
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6727270 |
Pyrrolylalkylidene-hydrazinecarboximidamide derivatives as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
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6716837 |
Heterocyclic compounds for the treatment of migraine
Described herein are compounds useful in the treatment of migraine, which have the general formula: wherein: W is a CH group or a N atom; Z is N or C—R4; B and D are selected independently...
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6716831 |
2,4-diamino-pyrimidine deprivatives having anti-cell proliferative activity
A pyrimidine derivative of formula (I) or (I′): wherein: R x is a substituent as defined within; Q 1 is optionally substituted phenyl, and Q 1 bears a substituent of formula (Ia) wherein: X, Y...
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6706751 |
Dihydroindole and tetrahydroquinoline derivatives
The present invention relates to novel dihydroindole and tetrahydroquinoline derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are...
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6699862 |
Indolyl-2-phenyl bisamidines useful as antiproliferative agents
Novel indolyl- 2 -phenyl bisamidines are described which are DNA methyltransferase inhibiting agents, and pharmaceutical compositions containing them are used as antiproliferative agents for...
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6696479 |
Crystalline forms
Novel crystalline forms of Fluvastatin sodium hydrates were found, referred to hereinafter as polymorphic Forms C, D, E and F. Furthermore, the present invention is directed to processes for the...
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6689784 |
Carbamate caspase inhibitors and uses thereof
This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R 1 is hydrogen, —CHN 2 , R, CH 2 OR, CH 2 SR, or —CH 2 Y; Y is an electronegative leaving group; R 2...
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6689806 |
Indolinone compounds as kinase inhibitors
The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds of the invention. The invention also relates to...
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6686388 |
Regulators of the hedgehog pathway, compositions and uses related thereto
The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function...
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6677353 |
Substituted N-phenyl-N-heteroaralkyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer...
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6673787 |
Sulfonamide-containing indole compounds
The present invention creates a novel antiangiogenic agent and provides an antitumor agent which shows high safety as compared with conventional antitumor agents, has a sure effect and is able to...
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6673827 |
Methods of treating fungal infections with inhibitors of NAD synthetase enzyme
The present invention provides methods of treating or preventing fungal infections in a host comprising administering a treatment effective or treatment effective amount of a yeast NAD synthetase...
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6673797 |
Heterocyclic indole derivatives and mono- or diazaindole derivatives
There is provided a compound represented by the general formula (1): wherein Het represents an optionally substituted heterocyclic group; A 1 and A 2 each independently represent —CH═,...
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6664266 |
Axon regeneration with PKC inhibitiors
Regenerative growth of an adult mammalian central nervous system neuron axon subject to growth inhibition by endogenous, myelin growth repulsion factors is promoted by delivering to the axon a...
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