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8173678 |
Kappa opioid receptor ligands
Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease...
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8173689 |
6-O-substituted benzoxazole and benzothiazole compounds and methods of inhibiting CSF-1R signaling
Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions of...
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8163749 |
Six-membered heterocycles useful as serine protease inhibitors
The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, R3 and R11 are as defined...
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8158644 |
Pharmaceutical compositions comprising polymorphic forms α, β, and γ of rifaximin
Crystalline polymorphous forms of rifaximin (INN), referred to as rifaximin α and rifaximin β, and a poorly crystalline form referred to as rifaximin γ, useful in the production of medicaments co...
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8153647 |
Aryl- and heteroaryl-ethyl-acylguanidine derivatives, their preparation and their application in therapeutics
Disclosed are compounds according to formula (I): wherein A, Q, X, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. The disclosure also relates to pharmaceutical...
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8153646 |
Phosphodiesterase 4 inhibitors for cognitive and motor rehabilitation
The present invention provides methods of improving cognitive and motor deficits associated with central nervous system (CNS) disorder or condition in an animal. The methods comprise a general...
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8138187 |
Substituted heteroaryl derivatives
The invention relates to substituted heteroaryl derivatives, to methods for the production thereof, to medicaments containing said compounds and to the use of substituted heteroaryl derivatives for...
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8128905 |
Stabilized uncoated particles of reversed liquid crystalline phase materials
Uncoated particles of reversed cubic phase or reversed hexagonal phase material containing an active disposed within are provided. The uncoated particles have an ionic charge that is sufficient to...
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8119653 |
Belactosin derivatives as therapeutic agents/biological probes and their synthesis
Derivatives of belactosin and their synthesis are disclosed. In certain embodiments, compounds of the present invention exhibit anti-cancer, antiviral, antibiotic, and/or auto-immune therapeutic...
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8110582 |
Prophylactic treatment of UV-induced epidermal neoplasia
The present invention provides a method of protecting a subject against UV-induced epidermal neoplasia. Generally, the method includes administering to a subject an IRM compound in an amount...
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8088786 |
Layered pharmaceutical formulations
In one embodiment a layered pharmaceutical formulation includes two or more pharmaceutical layers and an intermediate layer disposed between at least two of the two or more pharmaceutical layers,...
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8076351 |
Camptothecin derivatives with antitumor activity
Novel camptothecin derivatives having antitumor activity, the processes for the preparation thereof, the use thereof as antitumor drugs and pharmaceutical compositions containing them.
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8067429 |
Forms of rifaximin and uses thereof
The present invention relates to Rifaximin polymorphic, salt, hydrate, and amorphous forms, to their use in medicinal preparations and to therapeutic methods using them.
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8058268 |
Neuroprotective agents for the prevention and treatment of neurodegenerative diseases
Disclosed herein are methods of treating neurodegenerative diseases comprising administering to the subject a compound having the structure: wherein α and R1-R8 are described herein, or a compound ...
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8030323 |
Pyrazole carboxamide derivatives, pharmaceutical compositions and its preparation
A compound of formula (I) or pharmaceutically acceptable salts and/or solvates or hydrates thereof. A process for preparing the compound, a pharmaceutical composition comprising the compound and an...
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8030324 |
Pyridine derivatives for the treatment of metabolic disorders related to insulin resistance or hyperglycemia
The present invention provides novel compounds represented by the general formula (I): their stereoisomers, pharmaceutically acceptable salts and their pharmaceutically acceptable solvates thereof,...
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8022080 |
Small molecules with antiprotozoal activity
The present invention provides new chemical compositions with desirable biological activity and toxicity profiles for the enhanced treatment of malaria.
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7964610 |
Buprenorphine derivatives and uses thereof
Ester derivatives of the phenolic hydroxyl group of buprenorphine can be used in the treatment of opiate dependency and/or moderate to severe pain. The esters have an enhanced bioavailability, an...
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7951817 |
Pyridomorphinans, pyridazinomorphinans and use thereof
Compounds represented by the formula: wherein R is C1-6 alkyl; C4-6 cycloalkylalkyl; or C3-6 alkenyl; R′ is H or C1-6 alkyl; X is H or OH; Y is alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl or a...
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7932263 |
Therapeutic treatment
A combination comprising candesartan and rosuvastatin for the prevention or treatment of arteriosclerosis and for the prevention of cardiovascular events is described.
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7928120 |
Cyanoisoquinoline compounds and methods of use thereof
The present invention relates to cyanoisoquinoline compounds suitable for use in treating hypoxia inducible factor-mediated and/or erythropoietin-associated conditions. The cyanoisoquinoline...
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7915275 |
Use of polymorphic forms of rifaximin for medical preparations
The present invention relates to Rifaximin polymorphic forms α, β and γ, to their use in medicinal preparations for the oral or topical route and to therapeutic methods using them.
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7910586 |
Compositions and methods for prevention and treatment of amyloid-β peptide-related disorders
The present invention provides methods and compositions for modulating levels of amyloid-β peptide (Aβ) exhibited by cells or tissues. The invention also provides pharmaceutical compositions and m...
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7902196 |
Synthesis of avrainvillamide, strephacidin B, and analogues thereof
The syntheses of the natural products, avrainvillamide and stephacidin B, are provided. The α,β-unsaturated nitrone functionality of avrainvillamide and its 3-alkylidene-3H-indole 1-oxide core is s...
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7902206 |
Polymorphic forms α, β and γ of rifaximin
Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin α and rifaximin β, and a poorly crystalline form named rifaximin γ, useful in the production of medicinal pr...
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7893080 |
Method of restoring the incretin effect
The present invention relates to methods of treating metabolic syndrome, Type 2 diabetes mellitus, atherogenic dyslipidemia and/or obesity. The present invention also relates to methods of...
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7888368 |
Treatment of drug-resistant tumors
A subclass of camptothecin derivatives is disclosed to be useful for the preparation of a medicament for the treatment of drug-resistant tumors and/or for the administration to patients who show...
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7879869 |
Drugs for ameliorating postcibal hyperglycemia
It is mentioned to provide drugs for ameliorating postcibal hyperglycemia, drugs for inhibiting an increase in blood glucose level and pharmaceutical compositions for preventing or treating...
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7872023 |
Kappa opioid receptor ligands
Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease...
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7872016 |
Method for treating skeletal disorders resulting from FGFR malfunction
The invention provides materials, reagents, systems, and methods for identifying agents useful for treating diseases resulting from abnormal (e.g., excessive) FGF receptor signaling. The invention...
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7868015 |
Phosphodiesesterase 4 inhibitors for the treatment of a cognitive deficit
The present invention provides methods of treating cognitive deficits associated with mental retardation. The methods comprise combining cognitive training protocols and a general administration of...
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7858637 |
Administration of TLR7 ligands and prodrugs thereof for treatment of infection by hepatitis C virus
This invention relates to methods for treating or preventing hepatitis C virus infections in mammals using Toll-Like Receptor (TLR)7 ligands and prodrugs thereof. More particularly, this invention...
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7858636 |
Hexarylene and pentarylene tetracarboxylic acid diimides
Rylenetetracarboximides of the general formula I in which the variables are defined as follows: R are identical or different radicals: hydrogen; alkyl, cycloalkyl, aryl or hetaryl, each substituted...
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7851439 |
EFTU inhibitors or aminothiazoles and their uses
Organic compounds that are useful for the treatment, prevention and/or amelioration of diseases are described.
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7838532 |
Aerosolized fluoroquinolones and uses thereof
Disclosed herein are formulations of fluoroquinolones suitable for aerosolization and use of such formulations for aerosol administration of fluoroquinolone antimicrobials for the treatment of...
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7820143 |
Water soluble tetrapyrollic photosensitizers for photodynamic therapy
A tetrapyrollic photosensitizer compound having at least one pendant —CH2CH2CON(CH2CON(CH2COOH)2)2 or —N(CH2COOH)2 group or esters thereof said tetrapyrollic compound being a chlorin, bac...
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7799778 |
5-substituted 2-aminopyridine analogs for treating allergic and inflammatory diseases
Methods for treating an allergic or inflammatory disease or other Syk-mediated disease or Syk-mediated condition characterized by administering a composition which contains a therapeutically...
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7781449 |
Trospium chloride treatment method
A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum...
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7781450 |
Substituted pyrroline kinase inhibitors
The present invention is directed to novel substituted pyrroline compounds useful as kinase inhibitors and methods for treating or ameliorating a kinase mediated disorder.
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7781448 |
Once daily dosage forms of trospium
A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum...
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7781445 |
Synthesis of indenoisoquinoliniums and methods of use
Substituted indenoisoquinolinium compounds, and pharmaceutical formulations of substituted indenoisoquinolinium compounds are described. Also described are processes for preparing substituted...
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7763635 |
Once daily dosage forms of trospium
A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum...
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7759359 |
Method of treating bladder dysfunction with once-a-day trospium salt formulation
A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum...
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7736624 |
Methods and compositions for diagnostic and therapeutic targeting of COX-2
The presently disclosed subject matter provides compositions that selectively bind cyclooxygenase-2 and comprise a therapeutic and/or diagnostic moiety. Also provided are methods for using the...
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7737158 |
Processes for regulating blood glucose in a mammal
The present invention relates to processes for regulating the blood glucose concentration of a mammal.
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7705015 |
Substituted pyrroline kinase inhibitors
The present invention is directed to novel substituted pyrroline compounds useful as kinase inhibitors and methods for treating or ameliorating a kinase mediated disorder.
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7678807 |
Isoquinoline and benzo[H] isoquinoline derivatives, preparation and therapeutic use thereof as antagonists of the histamine H3 receptor
The invention concerns a compound of formula (I): Wherein A, l, m, n, R1 and R2 are as defined herein. The compounds of this invention are useful as medicaments, particularly, in the treatment of...
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7674797 |
2-phenoxy- and 2-phenylsulfonamide derivatives with CCR3 antagonistic activity for the treatment of asthma and other inflammatory or immunological disorders
The present invention relates to a benzenesulfonamide derivative of formula (I), which is useful as an active ingredient of pharmaceutical preparations. The benzenesulfonamide derivatives of the...
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7671068 |
N-(alkoxyalkyl) carbamoyl-substituted 6-phenyl-benzonaphthyridine derivatives and their use as PDE ¾ inhibitors
Compounds of the formula I in which the substitutents have the definitions provided in the specification, are novel, effective PDE 3/4 inhibitors.
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7659281 |
HMG-CoA reductase inhibitors
Compounds are provided of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example, lowering...
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