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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...
8492334 Sustained intraocular delivery of drugs from biodegradable polymeric microparticles  
Biodegradable polymeric microparticle compositions containing one or more active agents, especially those useful for treating or preventing one or more diseases or disorders of the eye, and methods...
8492374 Azaazulene compounds  
An azaazulene compound is provided. The azaazulene compound has formula (I) shown below. Each variable in formula (I) is defined in the specification. The compound can be used to treat cancer. The...
8486964 Fused pyrrolidino-cyclopropane derivatives as selective 11-beta-hydroxysteroid dehydrogenase type 1 inhibitors  
The present invention relates to fused pyrrolidino-cyclopropane derivatives according to formulae (I) to (IV) as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1...
8486965 Pyrrolo[2,3-b]pyridine derivative and use thereof for treatment of cancer  
The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. Specially, the present invention relates to a compound represented by the...
8486936 Antagonist of smoothened  
Described herein are compounds, pharmaceutical compositions and methods for the inhibition of Hedgehog signaling. Said compounds, pharmaceutical compositions and methods have utility in the...
8486963 Azaindolizines and methods of use  
The invention relates to azaindolizines of formula I-a or I-b with anti-cancer and/or anti-inflammatory activity and more specifically to azaindolizines which inhibit MEK kinase activity. The...
8481532 PDE-10 inhibitors  
Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical...
8481534 5- and 6-membered heterocyclic compounds  
5- and 6-membered heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use...
8481531 Bicyclic heterocyclyl derivatives as FGFR kinase inhibitors for therapeutic use  
The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of...
8476257 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.
8470847 Derivatives of 7-alkynyl-1,8-naphthyridones, preparation method thereof and use of same in therapeutics  
The disclosure relates to 7-alkynyl-1,8-naphthyridones of formula (I): wherein R1, R2, R3, and R4 are as defined in the disclosure, to compositions containing them, to processes for preparing them,...
8470848 Organic compounds  
There are provided according to the invention compounds of formula (I), in free or salt form, wherein R1, R2, R3, R4, R5, R6, Q, W, X, m, n and p are as described in the specification, process for...
8470351 Embedding antibiotic compounds in solid polymers  
The present invention is directed to providing antimicrobial compositions consisting of a polymeric material and, embedded therein, an antimicrobial compound. The antimicrobial compound contains at...
8470850 Inhibitors of VEGF receptor and HGF receptor signalling  
The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor...
8470818 Compounds and methods for kinase modulation, and indications therefor  
Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
8470849 7-azaindole derivatives as selective 11-β-hydroxysteroid dehydrogenase type 1 inhibitors  
The present invention relates to 7-azaindole derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) and the use of such compounds ...