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6677354 Piperdines for use as orexin receptor antagonists  
Disclosed are compounds of formula (I): wherein:Y represents a group (CH2)n, wherein n represents 0, 1 or 2;R1 is phenyl, naphthyl, a mono or bicyclic heteroaryl group containing up to 3...
6670377 Quinoline derivatives, having in particular antiviral properties, preparation and biological applications thereof  
The invention concerns quinoline derivatives of formula (I) in which: Ra, Rb and Rc, identical or different represent one or several substituents, themselves identical or different, in any...
6667302 Heterocyclic topoisomerase poisons  
The invention provides compounds of formula I: wherein R1 to R5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds, pharmaceutical...
6653312 Amidine derivatives, their preparation and application as medicines and pharmaceutical compositions containing same  
Amidine compounds of the formula wherein the substituents are defined as in the application useful as NO-synthase enzyme inhibitors.
6653302 Quinoline and quinazoline compounds useful in therapy  
Compounds of formula I, whereinR1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms;R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms;R3...
6645957 Cyclic amide compound  
The invention relates to compounds represented by the following general formula (1): wherein A is an aromatic compound which may be substituted, or the like, B is a nitrogen atom or CH, X is a...
6646009 N-(aryl)-2-arylethenesulfonamides and therapeutic uses thereof  
N-(Aryl)-2-arylethenesulfonamides and pharmaceutically acceptable salts and compositions thereof are useful as antiproliferative agents, including, for example, anticancer agents. They are also...
6642228 α1b-adrenergic receptor antagonists  
There are provided compounds represented by the general formula (I): [wherein Ar is indole etc., R1 is hydrogen etc., B is bond, or B—N—R1 forms a ring structure and is piperidine etc., n is 0, 1,...
6641800 Pressurized aerosol compositions comprising powdered medicament dispersed in hydrofluoroalkane  
Pressurized aerosol composition for administration by inhalation comprising a liquefied hydrofluoroalkane, a powdered medicament dispersed therein, and a suspending agent comprising a polymer...
6635656 Cytotoxic alkaloids halitulin  
Compounds of general formula (I), wherein the nature of the group R is not particularly critical and typically takes various forms, include the natural compound halitulin of formula (I) and have...
6630489 Quinoline derivatives as tyrosine kinase inhibitors  
The invention concerns quinoline derivatives of formula (I) wherein n is 0-3 and each R4, which may be the same or different, is a substituent such as halogeno, hydroxy, amino, nitro,...
6627643 Methods for preparing sodium-hydrogen exchanger type-1 inhibitors  
This invention relates to methods of preparing sodium-hydrogen exchanger type 1 (NHE-1) inhibitors of formula I′ and methods of preparing pharmaceutical compositions comprising such NHE-1 inhibitors.
6624175 4-Substituted quinoline derivatives  
Disclosed are compounds of the Formula where R1, R2, R3, R4, X, Y1, and Y2 are defined herein. These compounds bind with high affinity to NK-3 receptors and/or GABAA receptors. Also provided are...
6620823 Lactam metalloprotease inhibitors  
The present application describes novel lactams and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 4-8 membered cyclic amide comprising...
6617333 Antineoplastic combinations comprising  
This invention provides the use of a combination of CCI-779 and EKB-569 in the treatment of neoplasms.
6617336 2-arylquinoline derivatives, preparation and therapeutic use thereof  
Compounds of general formula (I) in which:A represents a hydrogen atom, a hydroxyl, a C1-3 alkoxy group, a hydroxy(C1-6 alkyl) group, a (C1-3 alkoxy)(C1-3 alkyl) group, a thiol, (C1-6...
6613781 Heterocyclylaklylindole or -azaindole compounds as 5-hydroxytryptamine-6 ligands  
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor
6613776 Pyrazole compounds useful as protein kinase inhibitors  
This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula V: wherein Z1 is N, CRa, or CH, and Z2 is N or CH, provided one of...
6608083 Quinoline derivatives(2)  
NK3 receptor antagonists of formula (I): in which:Ar is an optionally substituted phenyl group, or a naphthyl or C5-7 cycloalkdienyl group, or an optionally substituted single or fused ring...
6608084 Aza-bicycles which modulate the inhibition of cell adhesion  
The invention is directed to physiologically active compounds of formula (I) wherein R1 represents R3—Z3—, R3—L2—R4—Z3—, R3—L3—Ar1—L4—Z3— or R3—L3—Ar1—L2—R4—Z3—; R2 represents hydrogen, halogen,...
6608085 4-quinolinemethanol derivatives as purine receptor antagonists (II)  
Use of a compound of formula (I) as defined herein, or a pharmaceutically acceptable salt or prodrug thereof, in the manufacture of a medicament for the treatment or prevention of a disorder in...
6605615 Hydrazones and analogs as cholesterol lowering agents  
Hydrazones and hydrazone analogs are provided which are useful as upregulators of LDL receptors and can be used in the treatment of hypercholesterolemia and related disorders and conditions.
6605628 Method of using 5-(arysulfonyl)-, 5-(arylsulfanyl)-and 5-(arylsulfanyl)thiazolidine-2,4-diones for inhibition of farnesyl-protein transferase  
This invention relates to a method of using novel 5-(arylsulfonyl)-5-(arylsulfinyl)- and 5-(arylsulfanyl)thiazolidine-2,4-diones of Formula (I), wherein Ar, Ar′, R6, m and n are as defined in the...
6602884 Quinolylpropylpiperidine derivatives, their preparation, and compositions containing them  
Quinolylpropylpiperidine derivatives of general formula (I) are described, and are useful as antimicrobial agents. Their preparation is also described.
6599918 Substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benzopyrans  
This invention is directed to substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benzopyrans that inhibit Factor Xa, pharmaceutical compositions comprising these compounds and...
6596745 Method for treating fibrotic diseases with azolium chroman compounds  
Provided is a method of treating or ameliorating hypertension in an animal comprising administering an effective amount of a compound of formula I:
6596735 Quinoline derivatives useful for inhibiting farnesyl protein transferase  
The invention relates to compounds of the formula: and to pharmaceutically acceptable salts and solvates thereof wherein Y, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 have the meanings defined in...
6593324 Dervatives of quinoline as alpha-2 antagonists  
A compound of formula I, wherein A, Ra, Rb, R1 to R5, m and t are as defined as disclosed, or a pharmaceutically acceptable salt or ester thereof, useful as an alpha-2 antagonist. The compounds I...
6586447 3,3-disubstituted-oxindole derivatives useful as anticancer agents  
The present invention relates to compounds of formula 1 and to pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein n is 0 or 1 and R1, R2, R3, R4, and R5 are as defined...
6583179 Substituted aminoalkylamide derivatives as antagonists of follicle stimulating hormone  
The present invention is directed to a series of novel substituted aminoalkylamide derivatives, pharmaceutical compositions containing them and their use in the treatment of reproductive disorders...
6579873 3 (5)-heteroaryl substituted pyrazoles as p38 kinase inhibitors  
A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula I wherein R1, R2, Ar1 and HetAr2 are as...
6579871 Methods of using novel compounds as neuro-protective agents  
This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.
6576656 Oxindole derivative  
An oxindole of Formula 1 or a prodrug thereof, or a pharmaceutically acceptable salt thereof is useful for growth hormone releaser: whereinR1, R2, R3 and R4 are independently hydrogen, optionally...
6576642 Diamide compounds and compositions containing the same  
Compounds having the formula (1): wherein A is a phenyl, naphthyl, dihydronaphthyindeny, pyridyl, indolyl,isoindolyl, quinolyl or isoquinolyl group which are optionally substituted; X is...
6573278 Aryl sulfonamides and analogues thereof and their use in the treatment of neurodegenerative diseases  
The present invention relates to new aryl ether sulphonamides and analogues, processes for their preparation and their use for the treatment of neurodegenerative disorders, in particular for the...
6573260 Cycloalkyl-substituted aminomethylpyrrolidine derivatives  
This invention provides a quinolone derivative which exerts strong antibacterial action upon various bacteria and has high safety, and it relates to a compound having a structure of formula (I),...
6569870 Fluorinated quinolones as antimitotic and antitumor agents  
The present invention provides fluorinated quinolones which are fluorinated on the phenyl group thereof, along with pharmaceutical formulations containing the same, methods of treating tumors or...
6566373 Protease inhibitors  
The invention relates to 3-hydroxy-and 3-keto-cyclohetero-substituted leucine compounds that are inhibitors of cysteine proteases, particularly cathepsin K, and are useful in the treatment of...
6559163 2,4-substituted quinoline derivatives  
Disclosed are compounds of the formula or pharmaceutically acceptable salts thereof wherein: represents: and A, B, G, D, E, Ra, Rb, W, and Z are defined herein. These compounds are agonists,...
6559146 Aminophenoxyacetic acid derivatives as neuroprotectants  
There is provided an aminophenoxyacetic acid derivative of the following formula (I): wherein, R1, R2, R3 and R4 are, independent from each other, alkoxy group, alkyl group or aryl group, etc.; E1...
6555569 Use of heteroaryl substituted N-(indole-2-carbonyl-) amides for treatment of infection  
A pharmaceutical composition containing a glycogen phosphorylase inhibitor of Formula I or IA as defined herein is administered to a mammal to treat infection.
6548520 Substituted imidazoles having anti-cancer and cytokine inhibitory activity  
The present invention is related to novel 2-alkyl substituted imidazoles of formula (I) useful for the treatment of CSBP kinase mediated diseases.
6545020 Farnesyl Protein transferase inhibitors with in vivo radiosensitizing properties  
The present invention is concerned with the finding that farnesyl protein transferase inhibitors have radiosensitizing properties which makes them useful for preparing a pharmaceutical composition...
6531478 Amino pyrazole derivatives useful for the treatment of obesity and other disorders  
Amino pyrazole derivatives of the formula: which are ligands for the neuropeptide Y, subtype 5 receptor and pharmaceutical compositions containing an amino pyrazole derivative as the active...
6531448 Insoluble compositions for controlling blood glucose  
The present invention relates to insoluble compositions comprising a protein selected from the group consisting of insulin, insulin analogs, and proinsulins; a derivatized protein selected from...
6521638 2,3-dihydro-1H-isoindole derivatives useful as modulators of dopamine D3 receptors (antipsychotic agents)  
Compounds of formula (I) wherein R1, R2, A, q are as defined herein, and salts thereof, have affinity for dopamine receptors, in particular the D3 receptor, and thus have potential in the...
6512000 Aminocarbonyl-substituted benzimidazoles having tryptase-inhibitory activity  
A method for treating diseases in which tryptase inhibitors may be of thereapeutic value, which comprises the administration of a thereapeutic amount of a compound of the formula  The invention...
6509351 Phenyl- and pyridyl-tetrahydro-pyridines having TNF inhibiting activity  
The present invention relates to compounds of formula (I): as well as the salts or solvates thereof, to pharmaceutical compositions containing them, to a process for preparing them and to...
6506751 Thiazolidinone compounds useful as chemokine inhibitors  
Disclosed are compounds of the Formula I wherein:Z is C or nothing, provided that when Z is nothing, R3 and R4 are nothing;A is S, S═O or O═S═O;R1 and R2 are independently hydrogen, lower alkyl,...
6506763 3-(substituted)-2-indolinones compounds and use thereof as inhibitors of protein kinase activity  
The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and...