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8143246 |
1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivatives
The invention relates to 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, (C1-3)alkyloxy,...
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8063036 |
Benzamides and related inhibitors of factor Xa
Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described....
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RE42376 |
Substituted 3-cyanoquinolines
This invention provides compounds of formula I having the structure wherein G1, G2, R1, R4, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which are...
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7928133 |
Compounds and compositions as hedgehog signaling pathway modulators
The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from...
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7888351 |
Organic compounds
The present invention relates to compounds of the formula; and their use in therapy.
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7829567 |
Imino-indeno[1,2-c] quinoline derivatives, their preparation processes, and pharmaceutical compositions comprising the same
Disclosed herein are novel imino-indeno[1,2-c]quinoline derivatives of formula (I): or a pharmaceutically acceptable salt or solvate thereof,wherein each of the substituents is given the definition...
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7709466 |
Pyridazinone derivatives, methods for their production and their use as pharmaceuticals
The present invention relates to pyridazinone compounds and their derivatives according to the general formula (I), with the substituents X, R1 and R2 defined herein, as well as their...
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7704995 |
Protein kinase modulators and methods of use
This invention relates to compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and...
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7511036 |
Dihydrothiazine prodrugs of thiazolium agents
Provided are compounds of the formula (and pharmaceutically acceptable salts thereof): wherein: R is hydrogen, methyl, hydroxymethyl or α-hydroxyethyl; R1 and R2 are independently selected from ...
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7491732 |
Compositions and methods for inhibition of the JAK pathway
The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of...
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7442710 |
Substituted phenyl methanones
The present invention relates to compounds of general formula IA or IB wherein X1 and X2 are each independently N or C—R″ andR1, R2,R3, R4,R5, and R6 are as defined in the specification and to pha...
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7312212 |
Aminopiperidine derivatives
Piperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.
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7294629 |
Quinazoline derivatives
A compound of the formula (I) or a pharmaceutically acceptable salt thereof, a hydrate thereof, a solvate thereof, an optically active compound thereof, a racemate thereof or a diastereomer mixture...
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7196080 |
Phenylpyridinecarbonylpiperazinederivative
The present invention relates to a compound which is represented by the following general formula and has type 4 phosphodiesterase inhibitory action, and uses and an intermediate compound thereof....
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7101874 |
Antimicrobial dihydrothiazine and dihydrothiopyran oxazolidinones
The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof wherein Y is —S(═O)n—, —S(═NR8)—, or —S(═NR8)(═O)—; Z is —NHC(═O)R1, —NHC(═S)R1, —NH-het1, —...
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6992092 |
Anti-diabetic agents
The present invention provides compounds of formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs; wherein R1,...
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6921759 |
Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors
Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV...
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6894046 |
IL-5 inhibiting 6-azauracil derivatives
The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to 4; X...
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6849732 |
Metalloproteinase inhibitors, pharmaceutical compositions containing them and their pharmaceutical uses, and methods and intermediates useful for their preparation
The invention relates to compounds of the formula 1: wherein: Z is O or S; V is a divalent radical which together with C* and N forms a ring having six ring atoms, where each of said ring atoms...
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6844347 |
Substituted 4-amino-2aryl-pyrimidines, their production and use and pharmaceutical preparations containing same
The invention relates to compounds of formula I, in which R1, R2, R3 and R4 have the meanings given in the claims. Said compounds are valuable active ingredients for the treatment and prophylaxis...
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6770596 |
Fused tricyclic compounds, process for their preparation, and herbicidal compositions containing them
Novel fused tricyclic compounds represented by formula (I) are described. Q, Y, —L—X—, A, A′, B, E, D, n and m are as defined in the disclosure. Also described are the processes for the manufac...
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6743798 |
Substituted pyrazole derivatives condensed with six-membered heterocyclic rings
The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which R1, R2, R3 and A are each as defined, and to processes for their preparation and to their...
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6683081 |
Triazolotriazinones and the use thereof
The invention relates to novel triazolotriazinones of the general formula (I), to a method for their production and to the pharmaceutical use thereof.
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6660732 |
Compounds useful as anti-inflammatory agents
Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are...
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6656933 |
Compounds useful as anti-inflammatory agents
Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are...
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6620810 |
4-thioxo-4,7-dihydro-thieno&lsqb 2,3-b&rsqb pyridine-5-carboxamides as antiviral agents
The invention provides a compound of formula I: wherein R1, R2, R3, and R4 have any of the values defined in the specification, or a pharmaceutically acceptable salt thereof, as well as processes...
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6613772 |
Substituted 2-aryl-4-amino-chinazolines, method for the production and use thereof as medicaments
Compounds of the formula I in which R1, R2, R3 and Ar have the meanings indicated in the claims, are suitable for the production of pharmaceuticals, for example for the prophylaxis and therapy of...
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6608052 |
Compounds useful as anti-inflammatory agents
Disclosed are novel aromatic compounds of the formula(I) wherein G, E, W, Ar, X, Y and Z. The compounds are useful for treating diseases or pathological conditions involving inflammation such as...
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6583146 |
Thiazolopyrimidine compounds, its production and use
Compounds represented by general formula (I): and salts thereof, exhibiting excellent adenosine A3 receptor antagonism: wherein A is an optionally substituted benzene ring; B may be further...
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6579982 |
Pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, Ar1, Z, R1, R2 and R3 are as defined in the specification, and to pharmaceutical...
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6559155 |
Pyrimidinone derivatives for the treatment of atherosclerosis
Pyrimidones of formula (I) are inhibitors of the enzyme LpPLA2 and thereof use in treating inter alia atherosclerosis, in which:R1 is COOH or a salt thereof, COOR10, CONR11R12, CN or CH2OH;R2 is a...
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6518423 |
Benzopiperidine derivatives
Benzopiperidine derivatives represented by formula (I), salts thereof or hydrates thereof, processes for producing the same and drugs comprising the same: wherein the variables are as described in...
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6509338 |
Pyrazolo&lsqb 1,5-A&rsqb triazine corticotropin releasing factor antagonists
The present invention describes novel pyrazolo[1,5-a]triazines of formula: wherein R3 is an alkyl, alkenyl, alkynyl, or cycloalkyl group, or pharmaceutically acceptable salt forms thereof, which...
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6500948 |
Metalloproteinase inhibitors-compositions, uses preparation and intermediates thereof
The invention relates to compounds of the formula 1: wherein: Z is O or S; V is a divalent radical which together with C* and N forms a ring having six ring atoms, where each of said ring atoms...
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6479483 |
4-phenyl-pyridine derivatives
Compounds of the present invention are 4-phenyl-pyridine derivatives with activity as NK-1 receptor antagonists.
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6458950 |
Compounds and pharmaceutical compositions containing the same
A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the...
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6407103 |
Indeno &lsqb 1,2-c&rsqb pyrazol-4-ones and their uses
The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases,...
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6380387 |
4-Pyrimidinyl-n-acyl-l phenylalanines
Compounds of Formula I are disclosed, having activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4, and accordingly useful for treating diseases whose symptoms and or damage...
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6358946 |
C-6 ring-substituted pyrido&lsqb 1,2-a&rsqb benzimidazole derivatives useful in treating central nervous system disorders
A C-6 ring-substituted pyrido[1,2-a]benzimidazole derivative of the formula: methods of preparation and pharmaceutical compositions containing a substituted pyrido[1,2-a]benzimidzole derivative as...
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6297258 |
Substituted 3-cyanoquinolines
This invention provides compounds of formula I having the structure ##STR1##wherein G1, G2, R1, R4, Z, n, and X are defined in the specification or a pharmaceutically acceptable salt thereof which...
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6218391 |
Triazinones and derivatives thereof
Corticotropin releasing factor (CRF) antagonists of Formula (I) ##STR1##and their use in treating psychiatric disorders and neurological diseases including major depression, anxiety-related...
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6200378 |
Thiazine indigo pigments, solid solutions thereof and their preparation
A compound according to the formula (I) ##STR1##wherein R1 and R2 are independently the atoms necessary to complete the formation of a substituted or unsubstituted aromatic or aliphatic carbocyclic...
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6159980 |
Pyrazinones and triazinones and their derivatives thereof
Corticotropin releasing factor (CRF) antagonists of Formula (I) ##STR1## and their use in treating psychiatric disorders and neurological diseases including major depression, anxiety-related...
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6147078 |
Pyrazinone thrombin inhibitors
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: ##STR1## wherein ##STR2##
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6133264 |
Carbostyril derivatives for inhibiting skin erythema and/or skin pigmentation
The present invention provides an agent for inhibiting skin erythema and/or skin pigmentation, containing at least one selected from the group consisting of the carbostyril derivative and salt...
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6124306 |
Thioalkyl alpha substituted pyrimidine compounds
The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula I ##STR1## and pyrimidine-thioalkyl and alkylethers of Formula I, where R4 is selected from the group...
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6093717 |
Imidazopyridine thrombin inhibitors
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: ##STR1## wherein Y1 and Y2 are independently selected from the...
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6080738 |
Heterocyclic amide compounds and medicinal uses thereof
A heterocyclic amide compound of the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof...
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6069141 |
Substituted aminophenyl isoxazoline derivatives useful as antimicrobials
The present invention provides novel substituted amionphenyl isoxazoline derivatives of formula I ##STR1## wherein R1 is H, alkyl, cycloalkyl, alkoxy, amino, or alkylamino; X and Y are the same and...
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6001832 |
[1,2,4]triazolo[4,3-a]quinoxalinone derivatives, their preparation and use
The present invention relates to [1,2,4]triazolo[4,3-a]quinoxalinone compounds of the formula ##STR1## wherein R1 is POX'X" or alkyl substituted with COX' or POX'X", and X' and X" independently are...
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