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Class 514/303 - Exactly three ring nitrogens in the bicyclo ring system


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the bicyclo ring system contains
No. of patents: 767
Last issue date: 05/15/2012


1                      
NumberTitleIssue Date
8178556Pyridopyrazinones derivatives insulin secretion stimulators, methods for obtaining them and use thereof for the treatment of diabetes
Described are pyridopyrazinone derivatives of formula (I), wherein X, Y, Z, W, A and R1 are as defined in claim 1, as insulin secretion stimulators. Also described is the preparation and use of these pyridopyrazinone deriva...
05/15/2012
8168653Mediators of hedgehog signaling pathways, compositions and uses related thereto
The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist of formula (I) in...
05/01/2012
8158648Heteroaryl 11-beta hydroxysteroid dehydrogenase type I inhibitors
Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrog...
04/17/2012
8148396Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrog...
04/03/2012
8124617Imidazopyridine compounds
Compounds, pharmaceutical compositions, kits and methods are provided for use with glucokinase that comprise a compound selected from the group consisting of formula (I) wherein the variables are as defined herein. ...
02/28/2012
8119658Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrog...
02/21/2012
8106070Substituted imidazoles as bombesin receptor subtype-3 modulators
Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders ...
01/31/2012
8101633Preparation and utility of substituted imidazopyridine compounds with hypnotic effects
The present disclosure is directed to modulators of GABAA receptors and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the medical use of such compounds for the treatment and/or management of sleep disorders an...
01/24/2012
8088792Triazolopyridinone derivatives for use as stearoyl CoA desaturase inhibitors
The present invention discloses triazolopyridinone derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: The compounds are useful in treating and/or preventing various human disease...
01/03/2012
8076356Triazolopyridinylsulfanyl derivatives as P38 map kinase inhibitors
A compound of formula (I), or a pharmaceutical acceptable salt and/or solvate (including hydrate) thereof; and the use of a compound of formula (I) in the treatment of a TNF-mediated disease, disorder, or condition, or a p3...
12/13/2011
8063065Azaindazole compounds as CCR1 receptor antagonists
Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis.
11/22/2011
8063063Immunopotentiating compounds
The invention provides novel compositions comprising Imidazopyridine compounds. Also provided are methods of administering the compositions in an effective amount to enhance the immune response of a subject. Further provided are novel compositions and methods of adm...
11/22/2011
8063064Non-nucleoside reverse transcriptase inhibitors
The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A2 and R1, R2, R3, R4a
11/22/2011
80582907-substituted aza-indazoles, compositions containing same, production method and use thereof
The disclosure relates to compounds of formula (I): which modulate the activity of proteins, particularly kinases, and to compositions containing the same, and to the use thereof as medicaments, in particular as anticancer ...
11/15/2011
8030328Imidazolone phenylalanine derivatives
Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein the variables A, n, R5, R21-R24 and Q are defined herein. These compounds bind VLA-4. Certai...
10/04/2011
8022085Pyrazolo-pyridinone and pyrazolo-pyrazinone compounds as P38 modulators and methods of use thereof
The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wh...
09/20/2011
8008322Substituted pyrazolopyridines, compositions containing them, method for the production thereof, and their use
The disclosure relates to substituted pyrazolo-pyridines, compositions containing them, methods for the production thereof, and to their use as medicaments, in particular, as anticancer agents. ...
08/30/2011
8003663Pyrazolo[3,4-b]pyridine compounds, and their use as PDE4 inhibitors
The invention provides N-{[1,6-diethyl-4-(tetrahydro-2H-pyran-4-ylamino)-1H-pyrazolo [3,4-b]pyridin-5-yl]methyl}-4-({8-[(2-hydroxyethyl) (methyl)amino]octanoyl}amino)benzamide, whose formula is or a salt thereof, such as th...
08/23/2011
7998975Nitrogenous fused-ring derivatives, medicinal compositions containing the derivatives, and use thereof as drugs
The present invention provides nitrogen-containing fused-ring derivatives represented by the following general formula, or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as ...
08/16/2011
7998976Certain chemical entities, compositions and methods
Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the...
08/16/2011
7989469Certain chemical entities, compositions, and methods
Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the...
08/02/2011
7977353Heterocyclic aromatic compounds useful as growth hormone secretagogues
Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I wherein R1, R1
07/12/2011
7960407Crystal forms of an imidazole derivative
The invention relates to the essentially pure Λ/-[({2-[4-(2-Ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenyl]ethyl}amino)carbonyl]-4-methylbenzenesulfonamide Polymorph Forms A and B and to processes for the preparation of, compositions containing and to the ...
06/14/2011
7951818Imidazolopyridine compounds useful for the treatment of degenerative and inflammatory diseases
Novel imidazolopyridine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of ...
05/31/2011
7951819Imidazo[4, 5-B]pyridin-2-one and oxazolo[4, 5-B] pyridin-2-one compounds and analogs thereof as cancer therapeutic compounds
The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5 b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B RAF) activity, inhibit cell proliferation, treat cancer, etc. The present invention also pert...
05/31/2011
7947709Non-nucleoside reverse transcriptase inhibitors
Compounds of formula I, wherein R1, R2, R3, X and Ar, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and th...
05/24/2011
7928119Use of EP4 receptor ligands in the treatment of IL-6 involved diseases
Methods of treating IL-6 involved diseases with EP4 receptor ligands, including EP4 receptor antagonists. Assays to determine the effect of test compounds on PGE2-induced whole blood cells activation. ...
04/19/2011
79234565-anilinoimidazo[1,5-a]-pyridines inhibitors of MEK kinase
The invention relates to imidazopyridines of formula I with anti-cancer and/or anti-inflammatory activity and more specifically to imidazopyridines which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell...
04/12/2011
7915286Substituted pyrazolo [3,4-b] pyridines as phosphodiesterase inhibitors
The present invention relates to phosphodiesterase (PDE) type IV selective inhibitors. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type IV selective inhibitors are provided...
03/29/2011
7915285Method for treating drug and behavioral addictions
The present invention is directed to the use of ibudilast for treating addictions, including drug and behavioral addictions. In particular, ibudilast is used to diminish the dopamine-mediated reward associated with addictions and to treat withdrawal syndromes after ...
03/29/2011
7910602Pyrazolopyridine derivatives as inhibitors of β-Adrenergic receptor kinase 1
The invention relates to 6-amido substituted pyrazolopyridine derivatives of the formula (I) useful as inhibitors of beta-adrenergic receptor kinase 1 (βARK-1), compositions containing such compounds and their use for the ...
03/22/2011
7897616Imidazopyridin-2-one derivatives as inhibitors of lipases and phospholipases
The present invention relates to imidazopyridin-2-one derivatives of the formula I with the definitions specified in the description, to their pharmaceutically usable salts and to their use as medicaments. ...
03/01/2011
7879873Azaindazole compounds as CCR1 receptor antagonists
Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis.
02/01/2011
7858639Bicyclic heterocycles as cannabinoid-1 receptor modulators
The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to...
12/28/2010
7851484Certain chemical entities, compositions, and methods
Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the...
12/14/2010
7846944Pyrazolo-pyridinone compounds and methods of use thereof
The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wh...
12/07/2010
7834028Pyrazolo-tetrahydro pyridine derivatives as orexin receptor antagonists
The invention relates to novel pyrazolo-tetrahydropyridines compounds and their use as orexin receptor antagonists. ...
11/16/2010
7816369Mediators of hedgehog signaling pathways, compositions and uses related thereto
The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small ...
10/19/2010
7807691Substituted N-arylpyrrolidines as selective androgen receptor modulators
The present invention provides a compound of the Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and met...
10/05/2010
7799801Heterocyclic aromatic compounds useful as growth hormone secretagogues
Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I wherein R1, R1
09/21/2010
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