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7384940 Method of treating cancer using kinase inhibitors  
Described herein are methods for treating cancer and other disease conditions in individuals who have either developed a resistance to conventional tyrosine kinase inhibitor (TKI) therapy or who...
7358256 ATP competitive kinase inhibitors  
The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as...
7345049 Phenylalanine derivatives  
Specific phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin.
7329665 Quinazolinone derivative  
An optically active form of the quinazolinone derivatives represented by the general formula (1): [wherein Y represents a phenyl group or C2-C7 alkyl group; E represents —CH═ or nitrogen...
7304059 Substituted quinazolin-4-ylamine analogues  
Substituted quinazolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the...
7285557 Pyrimidinones as melanin concentrating hormone receptor 1  
A compound of formula (Ia) comprising a pharmaceutically acceptable salt or solvate thereof, formulations, processes of preparing, and methods of administering to mammals are provided
7265125 Neuropeptide Y antagonists  
Quinoline and quinazoline derivatives can be used in the form of pharmaceutical preparations as Neuropeptide Y antagonists for the treatment or prevention of arthritis, cardiovascular diseases,...
7230001 Arylalkane, arylalkene and aryl azaalkane, medicaments containing said compounds and method for the production thereof  
The present invention relates to compounds of general formula R—Z 1 —Z 2 —Z 3 —R 1 , (I)
7230000 Methods and compositions utilizing quinazolinones  
Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity
7223756 Quinazoline compounds with therapeutic use  
The invention concerns the use of the quinazoline derivatives of Formula (I) wherein each of m, R 1 , Z, n and R 3 have any of the meanings defined in the description in the manufacture of a...
7214674 Heterocyclymethylpiperidines and -piperazines possessing affinity at 5ht-1 type receptors  
Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein: A is optionally substituted phenyl, naphthyl, indolyl, quinolinyl, quinazolinyl, indazolyl,...
RE39574 Quinazolinone containing pharmaceutical compositions for prevention of neovascularization and for treating malignancies  
The invention provides a composition for attenuating neovascularization and treating malignancies, including a pharmaceutically effective amount of a compound having a formula: wherein: ...
7183274 Piperidine-2,6-diones heterocyclically substituted in the 3-position  
Piperidine-2,6-diones heterocyclically substituted in the 3-position corresponding to formula I Also the production and use of such compounds in pharmaceutical formulations and related methods...
7173038 Quinazoline derivatives as VEGF inhibitors  
The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R 1 represents halogeno or C 1-3 alkyl; X 1 represents —O—; R 2 is selected from one of...
7148230 Quinazoline derivatives  
The invention concerns quinazoline derivatives of Formula I wherein R 1 and R 2 have any of the meanings defined in the description; processes for their preparation, pharmaceutical...
7112590 Thrombin inhibitors  
The invention relates to compounds that are heterocyclic derivatives of dipeptides and dipeptides mimetics and pharmaceutically acceptable salts thereof. The compounds are used as thrombin inhibitors
7094780 3-aminoquinazolin-2,4-dione antibacterial agents  
Antibacterial 3-aminoquinazolin-2,4-diones have formula (I) wherein: R 1 and R 3 include alkyl, alkenyl, cycloalkyl, aryl, hetero-cyclic, and heteroaryl; R 5 , R 6 , and R 8 include H, alkyl,...
7060705 Mitotic kinesin inhibitors  
The present invention relates to quinazolinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for...
RE39096 Treatment of skin disorders  
An effective treatment for skin disorders characterized by abnormal skin cell behavior, including a pharmaceutically effective amount of Halofuginone. Skin disorders which can be treated include...
7019012 Quinazoline derivatives and pharmaceutical compositions containing them  
A compound of general formula I wherein: R a is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; R b is a dimethylamino, N-methyl-N-ethylamino, diethylamino,...
7001904 Guanidine derivatives quinazoline and quinoline for use in the treatment of autoimmune diseases  
The invention concerns quinazoline and quinoline derivatives of Formula (I) wherein Q 1 includes a quinazoline or quinoline ring optionally substituted with a group such as halogeno,...
6982260 Quinazolines and their use for inhibiting cyclin-dependent kinase enzymes  
This invention provides quinazolines that are useful for treating cell proliferative diseases and disorders, such as cardiovascular diseases, infections, cancers, autoimmune diseases, gout, kidney...
6949541 Substituted piperidines, medicaments containing these compounds, and methods for the production thereof  
The present invention relates to substituted piperidines of general formula wherein A 1 , A 2 , R, R 1 and R 2 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers,...
6939866 Quinazoline derivatives  
The invention concerns quinazoline derivatives of Formula (I) wherein each of m, R 1 , n, R 2 and R 3 have any of the meanings defined in the description; process for the preparation,...
6930113 Nitrosated and nitrosylated phosphodiesterase inhibitors, compositions and methods of use  
The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase...
6900222 Pyrrolidinyl, piperdinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives  
The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein...
6844350 Febrifugine, isofebrifugine and method for producing the same  
A febrifugine represented by Formula (A): and an isofebrifugine represented by Formula (B): which exhibit extremely strong activities against tropical malarial protozoan are provided,...
6844338 Piperidyindoles as serotonin receptor ligands  
A pharmaceutical compound of the formula (I) in which R 1 and R 2 are each hydrogen or C 1-6 alkyl, R 3 is —SR 10 , —SOR 10 , —SO 2 R 10 , —COR 10 , —CH 2 OH or —CONHR 11 , where R...
6800628 N-substituted 4-((-4′-aminobenzoyl)-oxymethyl)-piperidines having gastric prokinetic properties  
This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R 1 is C 1-6...
6699861 Anti-quinazoline compounds  
Dihydroquinazoline derivatives of the formula where R 3 is —(CH 2 ) p —A where p is from 1 to 4 and A is a 5- or 6-membered N-containing heterocyclic ring attached via the N atom or A is...
6680329 N-(heterocyclyl)benzene or pyridinesulphonamides as antithrombotic agents and anticoagulants  
Compounds of formula [I] in which: W may represent a —(CH 2 ) 2 —, —(CH 2 ) 3 —, —CH 2 —C≡C— or —CH 2 —CH═CH— group, R 2 may in particular represent a piperidyl group, an...
6645971 Quinazolinone derivatives  
A compound given by general formula (1): [wherein T represents oxygen or sulfur atom, Y represents alkyl, cycloalkyl group, etc., ring W represents benzene ring, etc., R 1 and R 2 represent...
6617325 Biphenyl derivatives, production thereof and uses as medicines  
The present invention relates to biphenyl derivatives of general formula wherein R a to R g and n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically...
6602882 Quinoline derivatives and their use as antibacterial agents  
Piperidine derivatives and pharmaceutical derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.
6583155 Method for treating allergies using substituted pyrazoles  
A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.
6562829 Treatment of hepatic cirrhosis  
A composition for treating hepatic fibrosis and a method of using and manufacturing the composition are provided. The composition includes a quinazolinone derivative, preferably Halofuginone.
6559153 Quinazoline derivatives as alpha-1 adrenergic antagonists  
This invention relates to compounds which are generally alpha-1B adrenergic receptor antagonists and which are represented by Formula (I): wherein R′, R″, R 1 , R 2 , m, n, and A are as...
6559136 Fungicidal active substance combinations  
Novel active compound combinations of compounds of the formula (I) in which Z, X and A are each as defined in the description with known active compounds and their use for controlling...
6479499 2-phenyl-4-quinazolinone compounds, 2-phenyl-4-alkoxy-quinazoline compounds and their pharmaceutical compositions  
Two series of 6,7,2′,3′,4′,5′-substituted 2-phenyl-4-quinazolinones and 6,2′,3′,4′,5′-substituted 2,3-dihydro-2-phenyl-4-quinazolinones are synthesized and evaluated for...
6472394 MCH antagonists and their use in the treatment of obesity  
Disclosed are compounds represented by structural formula I: or a pharmaceutically acceptable salt, ester or solvate thereof, wherein W is R 1 —CR 3 R 12 NR 4 C(O)— or R 11 C(O)NR 4 —; the...
6448270 4-substituted piperidine analogs and their use as subtype selective NMDA receptor antagonists  
Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using the 4-substituted piperidine analogs as selectively active antagonists of...
RE37828 Treatment and prevention of adhesions  
An inhibitor of adhesion formation which can be used to prevent adhesions within the abdominal cavity, particularly following surgical intervention, trauma or inflammation in the area is disclosed....
6417194 Quinolines and quinazolines useful in therapy  
Compounds of formula I, wherein R 1 represents C 1-4 alkoxy optionally substituted by one or more fluorine atoms; R 2 and R 3 independently represent H or C 1-6 alkoxy (which is optionally...
6417178 Amyloid binding nitrogen-linked compounds for the antemortem diagnosis of alzheimer's disease, in vivo imaging and prevention of amyloid deposits  
Amyloid binding compounds which are derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other...
6407116 Nitrogenous fused-ring compounds, process for the preparation of the same, and drugs  
A compound represented by the formula: [wherein ring A represents a homocycle optionally having substituents or a nitrogen-containing heterocycle optionally having substituents; D and E are O or...
6391874 Fused heterocyclic compounds as protein tyrosine kinase inhibitors  
Substituted heteroaromatic compounds of formula (I) and in particular substituted quinolines and quinazolines, are protein tyrosine kinase inhibitors. The compounds are described as are methods for...
6376503 Alpha 1a adrenergic receptor antagonists  
This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the...
6358959 Polyazanaphthalenone derivatives useful as alpha 1a adrenoceptor antagonists  
Dihydro-polyazanaphthalen-2-one compounds (e.g., dihydroquinazolin-2-one and dihydropteridin-2-one derivatives) and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these...
6339089 Pyrimidine nucleus-containing compound and a medicament containing the same for a blood oxygen partial pressure amelioration, and a method for preparing the same  
A pyrimidine nucleus-containing compound represented by the formula (I): wherein ring A represents the ring of the formula (a): in which R 1 is a nitro group, an amino group, a substituted...
6337332 Neuropeptide Y receptor antagonists  
Compounds of the structures are useful for treating conditions related to an excess of neuropeptide Y including obesity and circulatory disorders.
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