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8178553 |
Compounds for the treatment of inflammatory disorders
This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by...
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8178552 |
7-Azaindole derivatives and their use in the inhibition of c-Jun N-terminal kinase
The present invention provides a compound of formula (I); or a pharmaceutically acceptable salt thereof, the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof in the...
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8168651 |
Protein kinase modulators
The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and...
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8168652 |
Inhibitors of AKT activity
The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The...
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8163751 |
Acylated indanyl amines and their use as pharmaceuticals
The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1-R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B is C...
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8163760 |
Use of pyridopyrimidine compounds in the treatment of gliomas
The present invention relates generally to therapeutic agents, formulations comprising them and their use in the treatment, amelioration and/or prophylaxis of glioma brain tumors and related...
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8163769 |
Antibacterial compounds
Antibacterials having formula (I) and salts, prodrugs, and salts of prodrugs thereof, processes for making the compounds and intermediates used in the processes, compositions containing the...
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8163750 |
Fluorene derivatives, compositions containing the same and use thereof as inhibitors of the protein chaperone HSP 90
The present invention relates to compounds of formula (I): wherein R1, R2, R2′, L, Het, p and p′ are as defined herein, compositions containing them, and their use as medicinal products.
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8158647 |
Substituted pyrrolopyridines and pyrazolopyridines as kinase modulators
Provided herein are substituted pyrrolopyridine heterocycles and substituted pyrazolopyridine heterocycles, pharmaceutical compositions comprising said heterocycles and methods of using said...
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8158622 |
Pyrrolopyridine-2-carboxylic acid amide inhibitors of glycogen phosphorylase
Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes,...
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8153652 |
Fab I inhibitors
Compounds are disclosed which are Fab I inhibitors and are useful in the treatment bacterial infections.
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8148361 |
Kinase inhibitors
The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts thereof. The Formula (I) compounds inhibit the tyrosine kinase activity of growth factor receptors...
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8148395 |
Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases
The present invention relates to azolopyridin-3-one derivatives of the general formula I with the meanings indicated in the description, their pharmaceutically usable salts and their use as...
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8148393 |
Zolpidem tablets
A zolpidem tablet having modified release is designed as a tablet-in-tablet dosage form.
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8148370 |
Polysubstituted derivatives of 2-aryl-6-phenyl-imidazo[1,2-a]pyridines, and preparation and therapeutic use thereof
Compounds of formula (I): wherein R1, R2, R3, R4 and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.
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8148394 |
Azaindoles having serotonin receptor affinity
Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula I: wherein A, B, D, E, R1 to R3 and n are described herein. Also described is the use of these...
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8143271 |
Compounds and methods for kinase modulation, and indications therefor
Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
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8143248 |
Tricyclic N-heteroaryl-carboxamide derivatives containing a benzimidazole unit, method for preparing same and their therapeutic use
The invention concerns tricyclic N-heteroarylcarboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also...
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8138202 |
Stable SNS-595 compositions and methods of preparation
Methods of preparing substantially pure SNS-595 substance are disclosed. Also provided are compositions comprising SNS-595 substance that are substantially pure and essentially free of visible...
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8138201 |
Treatment of progressive neurodegenerative disease with ibudilast
Compositions and methods for treating progressive neurodegenerative diseases, and their associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine).
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8138181 |
Imidazo[1,2-a]pyridine compounds as receptor tyrosine kinase inhibitors
Compounds of Formula I: in which A, B, R1, R1a, R2, R3, R4, R5 R6, R7 and R8 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases...
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8129404 |
Compounds and uses thereof
N-[3-(4-Cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difl
uoro-phenyl]-4-trifluoromethyl-benzenesulfonamide,...
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8129403 |
Chemical compounds
This invention relates to novel compounds having the formula (I); and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.
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8129372 |
Compounds having NPY Y5 receptor antagonistic activity
This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or...
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8124615 |
Diketo substituted pyrrolo[2,3-C]pyridines
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, diketo fused azolopiperidine and azolopiperazine derivatives...
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8119635 |
Diazabicyclic central nervous system active agents
Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.
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8119657 |
Enantiomeric compositions of 2-amino-1-(2-isopropylpyrazolo[1,5-α]pyridin-3-yl)propan-1-one and related methods
Enantiomerically pure (S)-2-amino-1-(2-isopropylpyrazolo[1,5-a]pyridin-3-yl)propan
-1-one, (S)-AV1013, is a candidate therapeutic for treating neuropathic pain, addiction behavior and drug...
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8114890 |
Anti-constipation composition
An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in ratio of bi-cyclic/mono-cyclic structure of...
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8114889 |
Nicotinic acetylcholine receptor sub-type selective amides of diazabicycloalkanes
Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain...
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8114867 |
Oxazolidinone antibiotic derivatives
The invention relates to antibacterial compounds of formula I wherein R1 is hydrogen, halogen, hydroxy, alkoxy or cyano; Y1 and Y2 each represent CH, one or two of U, V, W and X represent(s) N and...
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8110585 |
Bicyclic compound and pharmaceutical use thereof
The present invention provides a compound represented by the formula wherein R1 is a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally...
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8106069 |
Pyrrolo[2,3-b]pyridine derivatives active as kinase inhibitors and pharmaceutical compositions comprising them
Compounds which are pyrrolo[2,3-b]pyridine derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these...
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8106072 |
7- (4-substituted-3-cyclopropylaminomethyl-1-pyrrolidinyl) quinolonecarboxylic acid derivative
Object To provide novel quinolinecarboxylic acid compounds serving as safe, strong antibacterial agents that are effective against drug-resistant bacteria that are less susceptible to conventional...
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8106068 |
Compositions and methods for modulating c-kit and PDGFR receptors
The invention provides compounds of Formula (2), and pharmaceutical compositions thereof, wherein R1, R2, R3, R4 and L are as described herein; as well as methods for using such compounds to treat,...
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8097617 |
Organic compounds
New compounds of the Formula (I): for the treatment of non-insulin-dependent diabetes mellitus.
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8088765 |
Polysubstituted derivatives of 6-heteroarylimidazo[1,2-a]pyridines, and preparation and therapeutic use thereof
Compounds of formula (I): wherein R1, R2, R3, R4, Het and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.
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8088762 |
Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use
The invention describes novel nitrosated nonsteroidal anti-inflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated...
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8080561 |
Pyridopyrazines and derivatives thereof as ALK and c-Met inhibitors
The present invention provides a compound of Formula I or a pharmaceutically acceptable salt form thereof, wherein A, L1, R1, R2, R3, R4, R5, R6, and X are as defined herein. The compounds of...
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8080547 |
Triazolopyridine carboxamide derivatives and triazolopyrimidine carboxamide derivatives, preparation thereof and therapeutic use thereof
The invention relates to the triazolopyridine carboxamide derivative and trizolopyrimidine carboxamide derivative of general Formula (I): Wherein X, R1 and R2 are as defined herein. The invention...
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8076354 |
Bicyclic heterocyclic compounds as protein tyrosine kinase inhibitors
The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R1, A, X1, X2, X3, X4, X5 and R2 are as defined herein, to pharmaceutical compositions comprising...
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8071614 |
Bicyclic heterocyclic compounds as protein tyrosine kinase inhibitors
The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R1, q, A, B, X1, X2, X3, X4, X5 and R2 are as defined herein, to pharmaceutical compositions...
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8071651 |
5-amino-4-hydroxy-7-(imidazo [1,2-A] pyridin-6-ylmethyl)-8-methyl-nonamide derivatives and related compounds as renin inhibitors for the treatment of hypertension
Compounds of the general formula (I) or its salt or a compound in which one or more atoms are replaced by their stable, nonradio-active isotopes, in particular its pharmaceutically acceptable salt;...
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8071595 |
1,2-disubstituted heterocyclic compounds
1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and...
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8071613 |
Anti-constipation composition
An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in a ratio of bi-cyclic/mono-cyclic structure...
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8067433 |
Methods, compositions, and kits for the treatment of ophthalmic disorders
The invention features methods, kits, and compositions for the treatment of ophthalmic disorders. The compositions include a corticosteroid in combination with a non-steroidal...
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8067435 |
Nitrogen-containing heterocyclic compounds, their preparation and their use as antibacterial drugs
The invention relates to nitrogen-containing heterocyclic compounds of general formula (I) wherein: R1 represents a (CH2)n—NH2 radical, n being equal to 1 or 2; R2 represents a hydrogen atom; R3 a...
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8067415 |
Compounds useful as antagonists of CCR2
The present invention provides compounds of general formula (I) or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the...
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8067434 |
Compounds and methods for development of Ret modulators
Compounds active on Ret are described, as well as methods of using such compounds. Also described are crystal structures of Ret surrogates that were determined using X-ray crystallography. The use...
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8063048 |
Acetylenyl-pyrazolo-pyrimidine derivatives
The present invention relates to compounds of formula (I): wherein R1 to R3, A, M, L, E, G, and J are as defined in the description and claims. The invention also relates to a process for the...
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8053433 |
Pyrrolo[2,3-b]pyridin-4-yl-amines and pyrrolo[2,3-b]pyrimidin-5-yl-amines as janus kinase inhibitors
The present invention provides pyrrolo[2,3-b]pyridine-4-yl amines pyrrolo[2,3-b]pyrimidin-4-yl amines that modulate the activity of Janus kinases and are useful in the treatment of diseases related...
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