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8178530 |
Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases
Novel imidazo[1,2-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the...
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8178535 |
Substituted sulfonamide compounds having bradykinin 1 receptor activity and use thereof as medicaments
Substituted sulfonamide compounds corresponding to the formula I′ wherein m, n, p, X, Y, Z, R1, RA and RB have specified meanings, processes for their preparation, pharmaceutical compositions c...
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8178131 |
Pyrrolopyridines as kinase inhibitors
Compounds of Formula (I) are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in...
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8178536 |
Sirtuin modulating compounds
Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing...
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8173656 |
Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases
Novel imidazo[1,2-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the...
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8173618 |
Formulations for reducing neuronal degeneration
Nutriceutical and pharmaceutical formulations for treating neurodegenerative disorders such as Alzheimer's disease are provided. Nutriceutical formulations include two or more of folate, vitamin E,...
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8168637 |
Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment of diabetes
The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in whi...
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8163751 |
Acylated indanyl amines and their use as pharmaceuticals
The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1-R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B is C...
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8163750 |
Fluorene derivatives, compositions containing the same and use thereof as inhibitors of the protein chaperone HSP 90
The present invention relates to compounds of formula (I): wherein R1, R2, R2′, L, Het, p and p′ are as defined herein, compositions containing them, and their use as medicinal products.
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8163725 |
Gel compositions and methods of use
Improved topical gel compositions for the treatment of skin disorders are described. The gel compositions contain carbomer and methylparaben, and are substantially free of methylparaben crystalline...
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8158634 |
Compounds and compositions as inhibitors of cannabinoid receptor 1 activity
The invention provides compounds having Formula Ia, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and Y are as defined in the specification; as well as pharmaceutical...
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8158629 |
Indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, and preparation and uses thereof
The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with...
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8158628 |
Sulfonylated 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine compounds and their use as pharmaceuticals
Sulfonylated tetrahydroazolopyrazine compounds corresponding to the formula I wherein R1, R2a, R2b, R3a, R3b, R4, R8, R9a, R9b, R10, R11, A, B, W1, W2 and W3 have the meanings defined herein,...
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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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8148369 |
Fused pyrazine compounds useful for the treatment of degenerative and inflammatory diseases
Novel fused pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and...
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8148376 |
3, 4-dihydroquinoxalin-2(1H)-ones for use as stearoyl CoA desaturase inhibitors
The present invention discloses 3,4-dihydroquinoxalin-2(1H)-ones for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases,...
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8143254 |
Methods for modulating ion channels
In one embodiment, the invention provides an ion having the formula: (I) In another embodiment, the invention provides a method for modulating potassium, sodium, and cyclic nucleotide-modulated ion...
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8143247 |
Combinations for the treatment of diseases involving cell proliferation
Disclosed are pharmaceutical compositions for the treatment of diseases which involve cell proliferation. Also disclosed are methods for the treatment of said diseases, comprising co-administration...
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8133890 |
Combination of brimonidine and timolol for topical ophthalmic use
Disclosed are pharmaceutical compositions comprising brimondine and timolol for topical ophthalmic delivery and a method of treatment comprising administering said composition when indicated for...
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8129384 |
Imidazo[1,2-a]pyrazines as orexin receptor antagonists
This invention relates to imidazopyrazine substituted piperidine derivatives and their use as pharmaceuticals.
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8129383 |
Aminopterin dosage forms and methods for inflammatory disorders
There is disclosed dosage forms and methods for treating a patient with an inflammatory disorder with a therapeutically effective amount of aminopterin, or a pharmaceutically acceptable salt...
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8129372 |
Compounds having NPY Y5 receptor antagonistic activity
This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or...
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8124653 |
Methods and compositions for the treatment of attention deficit hyperactivity disorder and hyperphenylalanemia
Disclosed is a composition that includes a tetrahydrobiopterin in a controlled-release pharmaceutical preparation. Also disclosed is a method of treating a patient with phenylketonuria that...
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8119637 |
Substituted pyrrolo[2,3-b]pyrazines and methods for kinase modulation, and indications therefor
Compounds active on Fms and/or Kit protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of Fms and/or Kit...
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8119636 |
Pyrrolopyrazine kinase inhibitors
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R are defined as described herein, which inhibit JAK and SYK and are useful...
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8119621 |
Tetrahydro-cyclopentyl pyrazole cannabinoid modulators
This invention is directed to a tetrahydro-cyclopentyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor...
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8114893 |
Compounds and methods of use
In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In...
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8114867 |
Oxazolidinone antibiotic derivatives
The invention relates to antibacterial compounds of formula I wherein R1 is hydrogen, halogen, hydroxy, alkoxy or cyano; Y1 and Y2 each represent CH, one or two of U, V, W and X represent(s) N and...
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8114422 |
Methods and compositions for reducing skin damage
The Notch signal transduction pathway has been identified as a target for screening and treatment methods for the prevention and/or reduction of short- and long-term UVB-induced skin damage, e.g.,...
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8114871 |
3-amido-pyrrolo[3,4-C]pyrazole-5(1H,4H,6H) carbaldehyde derivatives
The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to...
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8110576 |
Substituted pyrrolo[2,3b]pyrazines and methods for treatment of raf protein kinase-mediated indications
Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described, wherein the compounds have the formula: In certain aspects...
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8106052 |
Luminescence-based methods and probes for measuring cytochrome P450 activity
The present invention provides methods, compositions, substrates, and kits useful for analyzing the metabolic activity in cells, tissue, and animals and for screening test compounds for their...
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8106051 |
Utilities of amide compounds
Compounds having an activity to enhance the expression of apoAI are provided, which are used as medicaments. Compounds of formula (I): in which ring A and Ar1 are independently a monocyclic or...
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8106050 |
Derivatives of pyrrolo-pyrazines having a kinase inhibitory activity and their biological applications
The invention relates to pyrrolo[2,3b]-pyrazine derivatives having the general Formula (I) wherein R2 and R3 are identical or different and represent H, C1-C6 alkyl, said alkyl being a straight or...
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8101613 |
6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors
Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment...
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8101614 |
Substituted pyrrolo [1,2-a] pyrazines as calcium channel blockers
The present application relates to calcium channel inhibitors comprising compounds of formula (I), formula (II), formula (III), or formula (IV), wherein L1, R1, R2, R3, R4, R5, R6, R7 and Rc are as...
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8101626 |
GPR119 receptor agonists in methods of increasing bone mass and of treating osteoporosis and other conditions characterized by low bone mass, and combination therapy relating thereto
The present invention relates to the use of GPR119 receptor agonists for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an...
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8097611 |
Sulfonyl-derivatives as novel or histone deacetylase
This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their...
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8092840 |
Dietary supplement and a method to enhance sleep and lucid dreaming
A nutritional supplement for enhancing sleep and lucid dreaming in humans. It contains a combination of ingredients in proportions calculated to enhance lucid dreaming. The primary ingredients are...
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8088753 |
Heparin conjugates and methods
Heparin conjugates and methods of making and use thereof are disclosed. An illustrative heparin conjugate includes a composition wherein a bile acid is bonded to heparin through the 3-carbon of the...
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8088770 |
Modulators of pharmacokinetic properties of therapeutics
The present application provides for a compound of Formula IV: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that...
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8080550 |
Anesthetic compositions and methods of use
The invention generally relates to anesthetic compositions comprising low doses of a selective a-2 adrenergic receptor agonists in combination with anesthetic agents. The invention also relates to...
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8071597 |
Pyrazine compounds and uses as PI3K inhibitors
The present invention is related to pyrazine derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular...
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8071599 |
Methods of treatment of chronic pain using eszopiclone
The invention relates to the use of eszopiclone for the treatment of low-level, chronic pain and fatigue associated with pain.
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8071598 |
3,9-diazabicyclo[3.3.1]nonane derivatives and their use as monoamine neurotransmitter re-uptake inhibitors
3,9-diazabicyclo[3.3.1]nonane derivatives, useful as monoamine neurotransmitter re-uptake inhibitors. Also, use of these compounds in a method for therapy and in pharmaceutical compositions...
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8071595 |
1,2-disubstituted heterocyclic compounds
1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and...
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8071557 |
Treatment of pulmonary hypertension with carbonic anhydrase inhibitors
This disclosure relates generally to methods and pharmaceutical compositions useful in treating pulmonary hypertension. In one embodiment, for example, the disclosure provides a method for treating...
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8067415 |
Compounds useful as antagonists of CCR2
The present invention provides compounds of general formula (I) or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the...
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8067416 |
Methods and compositions for the treatment of metabolic disorders
The present invention is directed to a novel methods and compositions for the therapeutic intervention in hyperphenylalaninemia. More specifically, the specification describes methods and...
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8058269 |
Oxindole derivatives
There is provided compounds of the formula wherein R6, V, W, X, Y, Q and n are as described. The compounds exhibit activity as anticancer agents.
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