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8618102 Bridged diazepan orexin receptor antagonists  
The present invention is directed to bridged diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric...
8618127 Methods and compositions for alleviating stuttering  
Methods of treating stuttering include treating people with gamma-aminobutyric acid (GABA) receptor modulators, including cyclopyrrolones. A second active agent may be used with GABA receptor...
8614226 Hetaryl-[1,8]naphthyridine derivatives  
Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed,...
8609686 Substituted azabicyclic compounds and the use thereof  
The present application relates to novel substituted pyrrolopyridine, pyrazolopyridine and isoxazolopyridine derivatives, to processes for their preparation, to their use for the treatment and/or...
8609653 Azaindole compounds and methods for treating HIV  
Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a...
8604050 Bicyclic derivatives of azabicyclic carboxamides, preparation thereof and therapeutic use thereof  
The disclosure relates to compounds of formula (I): wherein X1, X2, X3, X4, Y, n, A, and W are as defined in the disclosure, or a salt thereof, or a hydrate or solvate thereof, and to processes for...
8604049 4-dimethylamino-phenyl-substituted naphthyridines, and use thereof as medicaments  
The invention relates to novel substituted naphthyridines of formula 1 as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates, or solvates thereof. In...
8598166 Polysubstituted derivatives of 6-heteroarylimidazo[1,2-a]pyridines, and preparation and therapeutic use thereof  
Compounds of formula (I): wherein R1, R2, R3, R4, Het and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.
8592448 Substituted pyrrolo[2,3-b]-pyridines and -pyrazines  
Compounds of Formula I, as shown below and defined herein: (I) pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including...
8586602 Derivatives of 7 alkynyl-1,8 naphthyridones, preparation method thereof and use of same in therapeutics  
The disclosure relates to method of treating a disease in which VEGFR-3 is involved, comprising administering a therapeutically effective amount of a compound of the formula wherein R1, R2, R3, and...
8586603 Aminotetraline derivatives  
The present application relates to compounds of formula (I): and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are as defined herein, compositions containing such...
8586601 Stable SNS-595 compositions and methods of preparation  
Methods of preparing substantially pure SNS-595 substance are disclosed. Also provided are compositions comprising SNS-595 substance that are substantially pure and essentially free of visible...
8586581 Ethynyl compounds useful for treatment of CNS disorders  
The present invention relates to ethynyl compounds of formula wherein X, Y, Z, and R4 are as defined herein or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or...
8580815 Derivatives of azaindoles as inhibitors of protein kinases ABL and SRC  
The present invention relates to compounds of general formula I and use thereof as inhibitors of protein kinases AbI and Src and the method of production thereof. The present invention also relates...
8580814 Methods of using (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4- oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid for treatment of cancer  
Methods of treating, preventing or managing cancer, including certain leukemias are disclosed. The methods encompass the administration of enantiomerically pure...
8569283 Compounds and compositions as c-Kit kinase inhibitors  
The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent...
8569334 P2X7R antagonists and their use  
The present application is directed to novel P2X7R antagonists that are indol-3-carboxamide or azaindole-3-carboxamide compounds, pharmaceutical compositions comprising the same and their use for...
8563573 Azaindole derivatives as CFTR modulators  
The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), composi...
8563027 Drug delivery through hydrogel plugs  
An embodiment is a medical prosthesis for blocking or reducing tear flow through a punctum or canaliculus of a human eye and delivering a drug to the eye that comprises a dehydrated covalently...
8563574 Parenteral formulation of clopidogrel  
Described herein are ways to solubilize clopidogrel for parenteral administration containing clopidogrel and a diluent NNDMA (N,N-dimethylacetamide); useful in the prevention of platelet...
8557840 Herbicidal compounds  
The present invention relates to a method of controlling plants or inhibiting plant growth which comprises applying to the plants or to the locus thereof a herbicidally effective amount of a...
8557816 Aurora kinase modulators and method of use  
The present invention relates to chemical compounds having a general formula I wherein A1-8, D′, L1, L2, R1, R6-8 and n are defined herein, and synthetic intermediates, which are capable of m...
8551992 Aminooxazole inhibitors of cyclin dependent kinases  
Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon...
8552026 Isatin derivatives, medicaments containing the isatin derivatives and method for its preparation  
The present invention relates to an isatin derivative having the formula (I), a medicament for treatment of tuberculoses containing that isatin derivative as well as a method for preparing isatin...
8552027 Luminescent compounds  
Dyes and photoluminescent compounds based on polymethine dyes that contain at least one alkyl-phosphonate or substituted alkyl-phosphonate group, including the synthetic precursors, methods of...
8551986 Treatment of sequelae of psychiatric disorders  
In general, the invention provides methods and compositions for treating sequela of weight gain or pain insensitivity, e.g., in a subject suffering from a psychiatric disorder, such as...
8546403 Compounds that modulate intracellular calcium  
Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of...
8546424 Acetylene derivatives of 5-phenyl-pyrazolopyridine, preparation thereof, and therapeutic use thereof  
Compounds of formula (I): in which: R1 and R2 represent, independently of one another, a hydrogen atom or a (C1-C6)alkyl group,R3 represents one or more hydrogen or halogen atoms,X represents from...
8546405 Anti-viral compounds  
Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such com...
8546385 Benzoic pyrrolopyridine derivatives  
The present invention relates to compounds of formula: in which A, Cy, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the description. The compounds of the invention are modulators of the...
8546407 Ortho-condensed pyridine and pyrimidine derivatives (e.g., purines) as protein kinases inhibitors  
The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (Ic) or salts, tautomers or N-oxides thereof.
8545897 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 situ,...
8541402 Viral polymerase inhibitors  
Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
8536164 Fused pyridine compounds as casein kinase inhibitors  
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y,...
8530469 Therapeutic combinations of hydroxybenzamide derivatives as inhibitors of HSP90  
The invention provides a combination comprising an Hsp90 inhibitor compound of the formula (VII): or tautomer or salt thereof and one or more therapeutic agents selected from topoisomerase I...
8518911 Pyrazolo[1,5-a]pyridines as MARK inhibitors  
The invention encompasses pyrazolo[1,5-a]pyridine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of...
8518943 2-oxo-1-pyrrolidine derivatives, processes for preparing them and their uses  
The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
8518872 Methods of using (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-OXO-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid in combination therapy  
Methods of treating, preventing or managing cancers are disclosed. The methods encompass the administration of SNS-595 in combination with a second active agent. In certain embodiments, the method...
8513231 Use of oxazolidinone-quinoline hybrid antibiotics for the treatment of anthrax and other infections  
The present invention relates to the use of compounds, in which the pharmacophores of quinolone and oxazolidinone are chemically linked together through a linker that is stable under physiological...
8513276 Imidazo[1,2-a]pyridine compounds for use in treating cancer  
The invention relates to new bicyclic heterocyclic derivative compounds of Formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of...
8513277 Pyrrolo[3,2-C] pyridine derivatives and processes for the preparation thereof  
The present invention provides novel pyrrolo[3,2-c]pyridine derivatives or pharmaceutically acceptable salts thereof, processes for the preparation thereof, and compositions comprising the same....
8507521 Heterocyclic derivatives  
The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The...
8507520 Polysubstituted 2-aryl-6-phenylimidazo[1,2-A]pyridine derivatives, and preparation and therapeutic use thereof  
Compounds of formula (I): wherein R, R1, R2, R3, R4, and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.
8507472 Bicyclic pyridinylpyrazoles  
Bicyclic pyridinylpyrazoles of the formula (I) in which the symbols have the meanings given in the description and agrochemically active salts thereof and their use for controlling unwanted...
8501767 Imidazopyridines and imidazopyrimidines as HIV-1 reverse transcriptase inhibitors  
The invention provides compounds of formula A or B which are useful in the treatment of a subject infected with HIV.
8501750 Heterocyclic compound and use thereof  
Heterocyclic compounds, pharmaceutical agent and methods thereof, having superior pharmacological action and/or physicochemical properties, which are useful for the prophylaxis or treatment of...
8501768 Hexahydrocyclopentapyrrolone, hexahydropyrrolopyrrolone, octahydropyrrolopyridinone and octahydropyridinone compounds  
The invention provides novel compounds having the general formula (I) wherein R1, R2, A, E, G and n are as described herein, compositions including the compounds and methods of using the compounds....
8501732 Aminomethyl quinolone compounds  
The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors,...
8501478 Trehalose click polymers for delivery of biologically active molecules  
Novel trehalose click polymers have in vitro and in vivo application in the cellular delivery of biologically active molecules, including nucleic acids and polypeptides. The trehalose click...
8497282 Method of preparing (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid  
Methods of preparing (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrro lidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxyli c acid are disclosed. Also provided are pharmaceutical...