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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...
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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...
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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.
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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...
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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...
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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
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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,...
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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)
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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
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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...
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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,...
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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:
...
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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...
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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...
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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...
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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
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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,...
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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...
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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...
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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,...
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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,...
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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...
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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,...
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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,...
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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...
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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...
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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,...
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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...
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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...
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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...
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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...
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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...
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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...
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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.
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6583155 |
Method for treating allergies using substituted pyrazoles
A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.
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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.
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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...
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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...
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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...
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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...
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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...
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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....
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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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