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7612208 Crystalline form of the salt of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide or the solvate of the salt and a process for preparing the same  
A crystal of a 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-meth oxy-6-quinolinecarboxamide hydrochloride, hydrobromide, p-toluenesulfonate, sulfate, methanesulfonate or ethanesulfonate,...
7612115 Aqueous pharmaceutical compositions  
The present invention has an object to provide an antibacterial aqueous pharmaceutical composition and an aqueous pharmaceutical composition which have a sufficiently low gelation temperature even...
7612092 Nitrogen-containing aromatic derivatives  
Compounds represented by the following general formula: [wherein A g is an optionally substituted 5- to 14-membered heterocyclic group, etc.; X g is —O—, —S—, etc.; Y g is an...
7601841 Quinolinyl and benzothiazolyl modulators  
Compounds, compositions and methods are provided that are useful in the treatment or prevention of a condition or disorder mediated by PPARγ. In particular, the compounds of the invention modulate...
7598268 Quinolinone derivatives  
Organic compounds having the formula I are provided where the variables have the values described herein. Pharmaceutical formulations include the organic compounds or pharmaceutically...
7598258 Quinoline derivatives and quinazoline derivatives inhibiting autophosphorylation of macrophage colony stimulating factor receptor  
An objective of the present invention is to provide compounds which have inhibitory activity against autophosphorylation of macrophage colony-stimulating factor receptors. The compounds of the...
7595328 Methods of use of quinolone compounds against pneumococcal and Haemophilus bacteria  
This invention relates, in part, to newly identified methods of using quinolone antibiotics, particularly a gemifloxacin compound against certain pathogenic bacteria, particularly quinolone...
7585845 Hepatitis C inhibitor compounds  
Compounds of formula (I): wherein B, X, R 3 , L 0 , L 1 , L 2 , R 2 , R 1 and R C are defined herein. The compounds are useful as inhibitors of HCV NS3 protease for the treatment of hepatitis...
7582765 Aryl aniline β2 adrenergic receptor agonists  
The invention provides novel β 2 adrenergic receptor agonist compounds of formula (I): wherein R 1 -R 13 and w have any of the values described in the specification. The invention also...
7579473 c-Met modulators and methods of use  
The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration...
7579363 Bicyclic compounds and compositions as PDF inhibitors  
This invention is directed to novel bicyclic compounds, to the uses of these compounds in various medicinal applications, including treating disorders amenable to treatment by peptidyl deformylase...
7576100 Muscarinic agonists  
The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with...
7572914 Kinase inhibitors  
The invention relates to compounds of the following formula that may be used to inhibits kinases, as well as compositions of matter and kits comprising these compounds. The present invention also...
7572913 4-substituted piperidine derivatives  
Substituted piperidine compounds represented by the structure I are provided, wherein each of R 1a , R 1b , R 1c , R 1d , R 1e , R 1f , R 1g , R 1h , R 2 , R 2A , R 3 , R 4 , A, X, a, x and n...
7563806 Substituted cycloalkyl derivatives, process for the manufacture thereof and use thereof as medicament  
The present invention relates to compounds of formula 1 wherein the groups R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , n, m and X may have the meanings given in the claims and in the...
7563805 Tri-, tetra-substituted-3-aminopyrrolidine derivative  
A quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria,...
7563804 FMF treatment  
The method of improving FMF control, in humans, which includes administering, on an average daily basis, between 5 and 15 milligrams of LTRA to a patient suffering from FMF.
7563460 Enteric coated oral pharmaceutical to erode kidney stones  
A treatment protocol by which a renal stone patient is administered a chelating agent, generally once a day and preferably by mouth, during a treatment phase and is later administered the same...
7560483 Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof  
The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require...
7557213 Substituted quinolones and methods of use  
Substituted quinolone compounds and compositions are provided along with methods for the use of those compounds in the treatment of diseases and disorders such as cancer.
7553855 Compositions of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide  
Pharmaceutical compositions including N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4 -oxoquinoline-3-carboxamide (Compound 1) and methods of using such compositions are described herein.
7553854 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...
7550598 Kinase inhibitors  
Compounds, pharmaceutical compositions, kits and methods are provided for use with kinases that comprise a compound of the formula: wherein R 1 , R 2 , R 3 , Q, U, V, W, X, and Y are as defined...
7550453 2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof  
The invention relates particularly to 2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof as a medicament, particularly as anti-cancer agents.
7534802 Compounds having 4-pyridylalkylthio group as substituent  
A subject of the present invention is to provide a novel aromatic five- or six-memberd heterocyclic derivative having 4-pyridylalkylthio as a substituent or a salt thereof which is useful as a...
7534793 Aminopiperidine quinolines and their azaisosteric analogues with antibacterial activity  
Aminopiperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man
7531553 Heterocyclic compounds and methods of use  
Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically...
7514557 Process for preparing acyclic HCV protease inhibitors  
Disclosed are highly convergent processes for preparing compounds of formula (I), which compounds are potent active agents for the treatment of hepatitis C virus (HCV) infection: The disclosed...
7514451 7-(4-Substituted-3-cyclopropylaminomethyl-1 pyrrolidinyl) quinolonecarboxylic acid derivative  
To provide novel quinolonecarboxylic acid compounds serving as safe, strong antibacterial agents that are effective against drug-resistant bacteria that are less susceptible to conventional...
7511062 Substituted 2-quinolyl-oxazoles useful as PDE4 inhibitors  
The invention claims compounds of the formula wherein is a 5-membered heteroaryl; X is S or O; R 1 is H, alkyl, cycloalkyl, cylcoalkylalkyl-, —CH 2 F, —CHF 2 , —CF 3 ,...
7507749 Antitumor agents  
The invention provides compounds of formula I: wherein Y is F, Cl, Br, methyl or methoxy; and pharmaceutically acceptable salts thereof. The compounds are effective antitumor agent. The...
7504416 4-substituted quinolines as antitumor agents  
The invention concerns compounds of formula (I), wherein each of R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 8 , R 9 , R 10 m, n, p, X, Y and Z have any meanings defined in the description, processes...
7504378 Macrocyclic peptides active against the hepatitis C virus  
Compounds of formula (I): wherein R 1 is (C 1-8 )alkyl, (C 3-7 )cycloalkyl, {(C 1-6 )alkyl-(C 3-7 )cycloalkyl} or Het, which are all optionally substituted from 1 to 3 times with halo, cyano,...
7498343 Mycobacterial inhibitors  
The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or the general Formula (Ib) the pharmaceutically acceptable acid or base addition...
7495104 Quinoline or quinazoline derivatives inhibiting auto-phosphorylation of fibroblast growth factor receptors  
An objective of the present invention is to provide novel compounds which have inhibitory activity against autophosphorylation of an FGF receptor family and, when orally or intraveneously...
7495103 Modulators of ATP-binding cassette transporters  
The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions...
7488739 Quinolone derivative or salt thereof  
A platelet aggregation inhibitor comprising a quinolone derivative or a pharmaceutically acceptable salt thereof as an active ingredient, and a novel quinolone derivative or a pharmaceutically...
7488725 Pyrrolidinyl beta-amino amide-based inhibitors of dipeptidyl peptidase IV and methods  
Compounds are provided having the formula: wherein R 1 , R 2 , R 2′ , R 3 , R 3′ , R 4 , R 4′ , R 5 , X, Y and Z are as defined herein.
7488494 Compositions and therapeutic methods involving isoflavones and analogues thereof  
Isoflavone compounds are described and recommended as therapeutic agents. Exemplified and preferred compounds are (a). Indications show compounds have good competitive binding to estrogen...
7482458 Quinoline derivatives  
NK 3 receptor antagonists of formula (I): are useful in treating inter alia pulmonary disorders, CNS disorders and neurodegenerative disorders.
7482341 Pyridines  
Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R 1 to R 6 have the significance given in claim 1 can be used in the form of pharmaceutical...
7476675 Quinolinone derivatives and uses thereof  
The invention provides compounds of the formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein m, p, q, r, A, E, X, Y, R 1 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and are as...
7476673 Disubstituted chalcone oximes as selective agonists of RARγ retinoid receptors  
Compounds of the formula where the variables are as defined in the specification, are useful for preventing or treating emphysema and related pulmonary conditions of mammals and other diseases...
7470709 Benzimidazole quinolinones and uses thereof  
Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt...
7470708 Acidic quinoline derivatives and their use for the prevention and/or treatment of hyperglycaemia-related pathologies  
The invention relates to compounds of the general formula (I): in which R1, R2, X, and A are as defined in claim 1. These compounds can be used in the treatment of hyperglycaemia-related...
7468378 Substituted quinoline compounds  
This invention relates to MTP/Apo-B secretion inhibitors of Formula (I) wherein R 1 —R 7 , X 1 , m and n are as defined in the specification, as well as pharmaceutical compositions comprising...
7456196 Bicyclic-substituted amines as histamine-3 receptor ligands  
Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising...
7455840 Compositions and methods to reduce mutagenesis  
The present invention provides methods and compositions for said inhibition of drug resistance. In one embodiment, said invention provides methods and compositions for said inhibition of antibiotic...
7452874 Thrombopoietin mimetics  
Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating...
7449479 Hepatitis C virus inhibitors  
Hepatitis C virus inhibitors are disclosed having the general formula: wherein R 1 , R 2 , R 3 , R′, B, Y and X are described in the description. Compositions comprising the compounds and...