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7608618 |
Urea or thiourea substituted 1,4-pyrazine compounds useful as anti-cancer agents and for inhibiting Chk1
Compounds of the formula
wherein: Y′ is O or S, W′ is
optionally substituted,
Z′ is selected from the group consisting of
wherein Q′ is OR 7 and R 7 is C 1-3 alkyleneC 3-8...
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7585861 |
HIV inhibiting 1,2,4-triazines
The present invention relates to HIV replication inhibitors of formula (I) as defined in the specification their use as a medicine, their processes for preparation and pharmaceutical compositions...
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7560450 |
Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to substituted xanthines of general formula
the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable...
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7550463 |
Carbamoylpyridone derivatives having inhibitory activity against HIV integrase
An object of the present invention provides a novel compound having the anti-viral activity, particularly, the HIV integrase inhibitory activity, and a drug containing the same, particularly, an...
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7517881 |
Triazine derivatives, their preparation and therapeutic application thereof
The invention relates to triazine derivatives of general formula (I):
Wherein R 1 , R 2 and R 3 are as defined herein. The invention also relates to a method for preparing these triazine...
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7510726 |
Methods and compositions for deterring abuse of opioid containing dosage forms
This invention relates to an abuse deterrent dosage form of opioid analgesics, wherein an analgesically effective amount of opioid analgesic is combined with a polymer to form a matrix.
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7504501 |
Antiprotozoal imidazopyridine compounds
Compounds described by the Formula (I): (I) or pharmaceutically acceptable salts, or N-oxides thereof. The compounds are useful for the treatment and prevention of protozoal diseases in mammals and...
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7501415 |
Selective inhibitors of ERK protein kinase and uses thereof
Described herein are compounds that are useful as ERK2 inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a...
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7494997 |
Amide derivative
The present invention provides an amide derivative represented by the following general formula (1):
wherein R 1 represents a saturated cyclic amino group, R 2 represents alkyl, halogen or...
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7494996 |
Substituted 4,5-dihydro-1,2,4-triazin-6-ones, 1,2,4-triazin-6-ones and their use as fungicides and insecticides
This invention relates to dihydrotriazinones, triazinones and related compounds, compositions comprising such compounds and an agronomically acceptable carrier, and the use thereof as broad...
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7485639 |
4-(benzylidene-amino)-3-(methylsulfanyl)-4h-(1,2,4)triazin-5-one derivatives having a PDE-IV inhibiting and TNF-antagonistic effect for the treatment of cardiac diseases and allergies
Triazine derivatives of the formula (I) and physiologically acceptable salts and solvates thereof, in which R 1 , R 2 , A and R 5 are as defined in Claim 1 , exhibit phosphodiesterase IV...
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7452906 |
Pyridine derivatives as Raf kinase inhibitors
Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac...
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7452882 |
Thyroid hormone analogs
Provided herein are compounds of the formula (I):
as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds,...
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7439268 |
Compositions containing prodrugs of florfenicol and methods of use
The present invention provides compositions and methods for administering florfenicol to mammals. The compositions contain a prodrug of florfenicol in a pharmaceutically acceptable carrier. In one...
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7432254 |
Method for treating glaucoma IC
Provided is a method of treating or ameliorating or preventing glaucoma, decreasing intraocular pressure or improving or amemliorting ocular accommodation in an animal, including a human comprising...
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7429590 |
Antiprotozoal imidazopyridine compounds
Compounds described by the Formula (I) or (II): or pharmaceutically acceptable salts, or N-oxides thereof. The compounds are useful for the treatment and prevention of protozoal diseases in mammals...
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7410968 |
Capped pyrazinoylguanidine sodium channel blockers
The present invention relates to compounds represented by formula (I):
where the structural variables are as defined herein. The compounds are useful for promoting hydration of mucosal surfaces.
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7390807 |
Crystal forms of lamotrigine and processes for their preparations
The present invention relates to lamotrigine, a useful agent for anti-epilepsia. New crystal forms of lamotrigine containing molecules of the solvent in stoichiometric ratios are disclosed. The...
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7390806 |
Antibiotics containing borinic acid complexes and methods of use
The structure and preparation of antibiotics incorporating borinic acid complexes are disclosed, especially hydroxyquinoline, imidazole and picolinic acid derivatives, along with compositions of...
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7371750 |
Compounds and compositions as protein kinase inhibitors
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated...
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7348335 |
Compositions useful as inhibitors of JAK and other protein kinases
The present invention provides a compound of formula I:
or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising the...
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7326706 |
Pyrazine modulators of cannabinoid receptors
The present application describes compounds according to Formula I, wherein A, G 1 , G 2 and R 1 are described herein. Additionally, the present application describes pharmaceutical compositions...
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7312227 |
Compositions useful as inhibitors of JAK and other protein kinases
The present invention provides a compound of formula I:
or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising the...
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7262200 |
Indazolinone compositions useful as kinase inhibitors
The present invention provides compounds of formula I:
These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as...
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7214677 |
Benzamide, heteroarylamide and reverse amides
The present invention relates to novel to P2X 7 inhibitors of formula I
and to processes for their preparation, intermediates useful in their preparation, pharmaceutical compositions...
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7138414 |
Heterocyclically substituted benzoylureas, process for their preparation and their use as pharmaceuticals
The invention relates to heterocyclically substituted benzoylureas and also to their physiologically tolerated salts and physiologically functional derivatives. Compounds are described of the...
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7078403 |
Antiviral agents
Disclosed herein are compounds of formula II:
wherein Alk, Z, X 1 , X 2 , R 1 , —R 10 and R 11 are defined herein, and their salts and pharmaceutically acceptable derivatives thereof, as...
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7056919 |
Synergistic combination of fungicides to protect wood and wood-based products and wood treated by such combination as well as methods of making the same
A wood treatment composition having a synergistic combination of fungicides which may include two or more compounds. These combinations are shown to be especially effective in providing resistance...
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7041670 |
Florfenicol-type antibiotics
The present invention relates to novel florfenicol compounds having the chemical structure:
wherein the compounds are useful for the treatment and/or prevention of bacterial infections in a...
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7026316 |
Dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in...
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7015223 |
Substituted polycyclic aryl and heteroaryl 1,2,4-triazinones useful for selective inhibition of the coagulation cascade
The invention relates to substituted polycyclic aryl and heteroaryl pyrimidinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and...
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6995157 |
Substituted 4,5-dihydro-1,2,4-triazin-3-ones, 1,2,4-triazin-3-ones, and their use as fungicides and insecticides
This invention relates to dihydrotriazinones, triazinones and related compounds, compositions comprising such compounds and an agronomically acceptable carrier, and the use thereof as broad...
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6974812 |
Benzamide inhibitors of the P2X7 Ereceptor
The present invention provides benzamide inhibitors of the P2X 7 receptor of the formula:
wherein R 1 -R 3 are as defined herein. The compounds of the invention are useful in the treatment...
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6969716 |
5-phenyl[1,2,4]triazines as ligands for GABA-A α2/α3 receptors for treating anxiety or depression
The present invention provides a compound of formula I, or an N-oxide thereof or a pharmaceutically acceptable salt thereof:
wherein
X 1 represents hydrogen, halogen, C 1-6 alkyl,...
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6969715 |
6-membered heterocyclic compounds useful for selective inhibition of the coagulation cascade
The present invention relates to compounds, and prodrugs thereof, compositions and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present...
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6951858 |
Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure:...
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6951857 |
6-Azauracil derivatives as IL-5 inhibitors
The present invention is concerned with the use of compounds of formula
the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p...
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6930107 |
6-azauracil derivatives as thyroid receptor ligands
The present invention provides novel compounds of the Formula I
and prodrugs thereof, geometric and optical isomers thereof, and pharmaceutically acceptable salts of such compounds, prodrugs...
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6927219 |
N-alkyl-adamantyl triazinyl benzamide derivatives
The present invention relates to novel to N-alkyl adamantyl triazinyl benzylamide derivatives of formmula I:
and to processs for their preparation, intermediates useful in their preparation,...
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6911444 |
Non-steroidal IL-5 inhibitors, processes and intermediates for their preparation and pharmaceutical compositions comprising said inhibitors
The present invention relates to IL-5 inhibiting 6-azauracil derivatives useful for treating eosinophil-dependent inflammatory diseases, to processes and intermediates for their preparation as well...
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6906068 |
Substituted polycyclic aryl and heteroaryl 1,2,4 - triazinones useful as anticoagulants
The invention relates to substituted polycyclic aryl and heteroaryl pyrimidinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and...
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6903094 |
Amide derivatives and nociceptin antagonists
The present invention relates to a compound of the formula [1′]
wherein R 2 is lower alkyl optionally substituted by hydroxy, amino and the like, ring B is phenyl, thienyl and the...
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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...
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6867207 |
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, p and q are 0, 1,...
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6838458 |
5-(alkylidene-cycloalkyl)-and 5-(alkylidene-heterocyclyl)-pyrazoles
The present invention relates to 5-(alkylidene-cycloalkyl)-pyrazoles and 5-(alkylidene-heterocyclyl)-pyrazoles of the formula I:
wherein the ring of the formula (R 5 )-A-(SO m R 4 ), m, B,...
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6831075 |
Heterocyclic substituted pyrazolones
The present invention is directed to novel heterocyclic substituted pyrazolones, including pharmaceutical compositions, diagnostic kits, assay standards or reagents containing the same, and methods...
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6828338 |
Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade
The present invention relates to compounds, and prodrugs thereof, composition and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present...
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6825192 |
Heterodiazinone derivatives
The present invention provides a hetrodiazinon compound having 2-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor antagonistic action, which is represented by the following...
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6818641 |
Arthropodicidal carboxanilides
Compounds of Formula (I), and their N-oxides and agriculturally suitable salts, are disclosed which are useful as arthropodicides wherein A is H; E is H or C 1 -C 3 alkyl; or A and E can be taken...
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6794398 |
Preventive/remedies for liver diseases
The invention provides an agent for the prophylaxis and treatment of liver disease and an activation inhibitor of hepatic stellate cells, which contains a compound having a Rho kinase inhibitory...
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