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7345038 |
Pyridyloxymethyl and benzisoxazole azabicyclic derivatives
An aminomethylpyridyloxymethyl/benzisoxazole substituted azabicyclic compound of formula I, pharmaceutical composition comprising same, and a method of treating one or more CNS or other disorders,...
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7345040 |
Reverse-turn mimetics and compositions and methods relating thereto
Reverse-turn mimetics and methods relating to the same having the following structure are disclosed:
including pharmaceutically acceptable salts and stereoisomers thereof, wherein R 1 , R 2 , R...
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7342012 |
Inhibitors of αLβ2 mediated cell adhesion
The present invention relates to a compound of the following formula:
or a pharmaceutically acceptable salt thereof. Also disclosed are compositions containing the compound and methods of...
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7335657 |
Cytokine inhibitors
Disclosed are compounds of formula (I)
Where Ar 1 , X, Y, Q, W, R 3 , R 4 , R 5 , R 6 and R y are defined herein. The compounds of the invention inhibit production of cytokines involved in...
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7335384 |
Nutrient compositions for the treatment and prevention of inflammation and disorders associated therewith
The present disclosure describes a novel composition for the treatment and/or prevention of neurogenic inflammation. Such composition is also useful in the treatment and/or prevention of disease...
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7332498 |
Modulation of KSP kinesin activity with heterocyclic-fused pyrimidinone derivatives
A method of modulating KSP kinesin activity in vitro comprising contacting KSP kinesin with at least one chemical entity chosen from compounds represented by Formula I:
and pharmaceutically...
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7326708 |
Phosphoric acid salt of a dipeptidyl peptidase-IV inhibitor
The dihydrogenphosphate salt of 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluoroph
enyl)butan-2-amine is a potent inhibitor of dipeptidyl...
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7326707 |
Bicyclic melanocortin-specific compounds
Melanocortin receptor-specific bicyclic compounds having the structure:
and stereoisomer and pharmaceutically acceptable salts thereof, where R 1 , R 2 , R 3 X and z are as described in the...
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7323468 |
Pyridopyrazines and the use thereof as kinase inhibitors
The invention relates to novel pyrido[2,3-b]pyrazine derivatives of the general Formula I, their preparation and use as medicaments, in particular for the treatment of malignant and other disorders...
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7320984 |
Remedies or preventives for urinary frequency or urinary incontinence and morphinan derivatives having nitrogen-containing heterocyclic group
The invention provides a morphinan derivative of the Formula (I):
wherein R 1 is methyl, cyclopropylmethyl or the like; R 2 and R 3 are hydroxy, methoxy, acetoxy or the like; both Y and Z...
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7319105 |
Cytotoxic agents
The invention provides compounds of the invention pharmaceutical compositions comprising a compound of the invention, processes for preparing compounds of the invention, intermediates useful for...
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7319097 |
Compounds
The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the...
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7312218 |
Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia-If:
or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic...
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7312217 |
Aminopterin dosage forms and methods for inflammatory disorders
Embodiments of the present invention provide dosage forms and methods for treating a patient with an inflammatory disorder with a therapeutically effective amount of aminopterin, or a...
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7304044 |
Lowering blood glucose, urea, cholesterol, triglycerides and normalizing homocysteine levels by dietary addition of selected essential amino acids and three vitamins
Administration of a dietary supplement consisting of L-Tryptophan (80 mgs), L-Methionine (90 mgs), L-Valine (103 mgs), L-Lysine Monohydrochloride (128 mgs), Vitamin B-12 (0.5 mg), Vitamin B-6 (10...
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7304064 |
1-[(indol-3-yl)carbonyl]piperazine derivatives
The present invention relates to 1-[(indol-3-yl)carbonyl]piperazine derivative according to the general formula I
or a pharmaceutically acceptable salt thereof. The invention also relates to...
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7300933 |
Diazabicyclic biaryl derivatives
This invention relates to novel diazabicyclic biaryl derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and...
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7300934 |
Benzamide nitriles
Compounds of the formula (I)
wherein m, n, A, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as described herein, together with methods for making the compounds and using the compounds for treatment...
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7297696 |
Antagonists of MCP-1 function and methods of use thereof
Compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant...
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7288545 |
Piperazinedione compounds
This invention relates to a method for treating an angiogenesis-related disease. The method includes administering to a subject in need thereof an effective amount of a piperazinedione compound...
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7276522 |
4-(substituted cycloalkylmethyl) imidazole-2-thiones, 4-(substituted cycloalkenylmethyl) imidazole-2-thiones, 4-(substituted cycloalkylmethyl) imidazol-2-ones, 4-(substituted cycloalkenylmethyl) imidazol-2-ones and related compounds
The compound of the formula
wherein the * indicates an asymmetric carbon, is specific to alpha 2B adrenergic receptors in preference over alpha 2A and alpha 2C adrenergic receptors, and as...
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7273868 |
Pyrazine derivatives
1. A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof,
wherein X is ═CH— or ═N—, Y is —NH—, —NR 4 —, —S—, —O—, —CH═N—,...
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7273863 |
Benzophenones as inhibitors of reverse transcriptase
The present invention includes benzophenone compounds (I)
which are useful in the treatment of HIV infections.
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7268127 |
Azaindoles having serotonin receptor affinity
Described herein are compounds with affinity for the 5-HT 6 receptor, which have the general formula I:
Wherein A, B, D, E, R 1 to R 3 and n are described herein. Also described is the use...
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7268137 |
Ocular therapy
A method for treating a subject suffering from epiretinal membrane formation or retinal detachment due to epiretinal membrane formation is disclosed. The method comprises administering a compound...
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7265117 |
Topical brimonidine tartrate formulations that lack chlorine dioxide
Topical solution compositions of brimonidine tartrate are disclosed. The solution compositions lack an oxidative preservative.
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7265116 |
Aryl and heteroaryl substituted tetrahydroisoquinolines and use thereof
Provided herein are compounds of the formula (I):
wherein R 1 -R 8 are as described herein, R 4 being phthalazinyl, pyrazinyl, pyridazinyl, or quinoxalinyl. Such compounds are particularly...
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7265118 |
Regulation of substrate activity
A method for regulating substrate activity in vivo is useful for the treatment of medical disorders such as inflammation, arteriolosclerosis and angiogenesis. The method involves the administration...
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7262186 |
Substituted pyrazolo[3,4-d] pyrimidinones as a mitotic kinesin inhibitor
The present invention relates to azolopyriniidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for...
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7262187 |
Substituted oxazolo- and thizaolopyrimidinones as a mitotic kinesin inhibitor
The present invention relates to azolopyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for...
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7259164 |
Certain substituted imidazo[1,2-a]pyrazines, as modulators of kinase activity
Certain substituted imidazo[1,2-a]pyrazines and the pharmaceutically acceptable salts thereof, are provided herein. Pharmaceutical compositions containing one or more compound of Formula I, or a...
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7259163 |
4-(6-membered)-heteroaryl acyl pyrrolidine derivatives as HCV inhibitors
Novel anti-viral agents of Formula
wherein:
A represents OR 1 , NR 1 R 2 , or R 1 wherein R 1 and R 2 are hydrogen, C 1-6 alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; or R 1 and...
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7255882 |
Enkephalinase inhibitor and GABA precursor loading as anti-anxiety compositions
Benzodiazepine withdrawal induced anxiety is treated by administration of an enkephalinase inhibitor, and a gamma-aminobutyric acid (“GABA”) precursor, or an endorphin or enkephalin releaser....
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7253169 |
Aza compounds, pharmaceutical compositions and methods of use
The present invention relates to N-substituted cyclic aza compounds, pharmaceutical compositions comprising such compounds, and methods of their use for effecting neuronal activities.
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7253168 |
Substituted 1-benzyl-4-substituted piperazine analogues
Compounds of Formula I are provided, in which variables are as described herein:
Such compounds may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly...
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7250417 |
Arylmethyl triazolo- and imidazopyrazines as c-Met inhibitors
The present invention relates to compounds of the Formulae (I)-(IV), wherein R 1 -R 6 , R 11 -R 13 , X and Y are defined herein, and their pharmaceutically acceptable salts. These compounds...
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7244734 |
Hexa- and octahydro-pyrido[1,2-a]pyrazine derivatives with NK1 antagonistic activity
The invention relates to hexahydro-pyrido[1,2-a]pyrazine derivatives having interesting neurokinin-NK 1 receptor antagonistic activity. The invention also relates to methods for the preparation of...
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7244722 |
Amino-substituted 1H-pyrazin-2-ones and 1H-quinoxalin-2-ones
Compounds of the general formula (I):
wherein m, n, R 1 , R 2 , R 3 and R 4 are as described in the specification.
Further included are pharmaceutical compositions comprising the...
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7241745 |
Pyridyl alkene and pyridyl alkine acid amides as cytostatics and immunosupressives
The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I)
as well as methods for their production, medicaments containing these compounds...
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7238683 |
Fused phenylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
The present invention is directed to fused phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-RV inhibitors”) and which are useful in the treatment or...
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7232817 |
α- and β-amino acid hydroxyethlamino sulfonyl urea derivatives useful as retroviral protease inhibitors
α- and β-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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7232824 |
Quinazoline derivatives as medicaments
Quinazoline derivatives have the formula:
or the pharmaceutically acceptable salts thereof; wherein each of Z 5 , Z 6 , Z 7 and Z 8 is N or CH and wherein one or two Z 5 , Z 6 , Z 7 and...
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7226924 |
Substituted 3,4-dihydro-pyrimido[1,2a]pyrimidines and 3,4-dihydro-pyrazino[1,2a]pyrimidines, and methods for their preparation and use
Substituted 3,4-dihydro-pyrimido[1,2a]pyrimidines and 3,4-dihydro-pyrazino[1,2a]pyrimidines of general formula I, the invention also relates to a method for the production thereof, substance...
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7220741 |
1,4-diazabicycloalkane derivatives, their preparation and use
This invention relates to novel 1,4-diazabicycloalkane derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic...
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7220736 |
Pyrimidine compounds
A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof,
wherein X is ═CH— or ═N—, Y is —NH—, —NR 4 —, —S—, —O—, —CH═N—,...
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7220757 |
Compositions and methods for topical administration of 2-NH-heteroarylimidazoles
Compounds of formula (I):
are inhibitors of bacterial methionyl tRNA synthetase and are of use in treating bacterial infections.
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7214674 |
Heterocyclymethylpiperidines and -piperazines possessing affinity at 5ht-1 type receptors
Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed:
wherein: A is optionally substituted phenyl, naphthyl, indolyl, quinolinyl, quinazolinyl, indazolyl,...
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7211572 |
Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
The present invention relates to a nitrogen-containing fused ring compound represented by the following formula [I]
wherein each symbol is as defined in the specification, or a pharmaceutically...
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7211599 |
Use of etodolac to treat hyperplasia
The present invention provides a therapeutic method to treat non-malignant diseases characterized by the excessive tissue growth, e.g., hyperplastic diseases, comprising administering to a mammal...
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7208493 |
Vasculostatic agents and methods of use thereof
Compositions and methods and are provided for treating disorders associated with compromised vasculostasis. Invention methods and compositions are useful for treating a variety of disorders...
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