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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,...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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,...
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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.
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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...
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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...
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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.
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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.
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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...
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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...
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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.
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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...
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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
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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...
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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...
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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...
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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 ,...
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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...
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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...
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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,...
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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...
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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...
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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...
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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...
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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.
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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...
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7482458 |
Quinoline derivatives
NK 3 receptor antagonists of formula (I):
are useful in treating inter alia pulmonary disorders, CNS disorders and neurodegenerative disorders.
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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