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Class 546/121 - Ring nitrogen is shared by the two cyclos


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the ring nitrogen is a member of both
No. of applications: 359
Last issue date: 05/24/2012


1                  
Application No.Application TitleIssue Date
20120129872FUSED HETEROARYL INHIBITORS OF PRO-MATRIX METALLOPROTEINASE ACTIVATION
This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables A, Q, J, R1, R3, and R5 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.

05/24/2012

20120108595PLATELET-ACTIVATING FACTOR RECEPTOR ANTAGONISTS
Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorder...
05/03/2012
20120071460PYRAZOLE OXADIAZOLE DERIVATIVES AS S1P1 AGONISTS
The present invention relates to pyrazole oxadiazoles derivatives of Formula (I), and their use for treating multiple sclerosis and other diseases, wherein R1, R2 and R3 are as defined in the description....
03/22/2012
20120071474INHIBITORS OF PI3 KINASE
The present invention relates to compounds of Formula I, II or III or a pharmaceutically acceptable salt thereof;

03/22/2012
20120053132COMPOSITIONS AND METHODS FOR INHIBITING CYTOCHROME P450
Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the...
03/01/2012
20120053350PREPARATION OF ALKYL ESTERS OF N-PROTECTED OXO-AZACYCLOALKYLCARBOXYLIC ACIDS
A process for the preparation of alkyl esters of N-protected oxo-azacycloalkylcarboxylic acids of Formula III: comprises contacting a ketosulfoxonium ylide of Formula II: with an iridium catalyst to obtain Compound III, wherein PG1 is an amine protective grou...
03/01/2012
20120053171Nitrogen-Containing Fused Heterocyclic Compounds and Their use as Beta Amyloid Production Inhibitors
A compound represented by the formula [I]: or a pharmacologically acceptable salt or ester thereof, wherein Ring A represents a five-membered aromatic heterocyclic group or the like fused with a non-aromatic ring group, which may be substituted, Ring B represents a phen...
03/01/2012
20120053202POLYSUBSTITUTED 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 ...

03/01/2012
20120045412CYCLOALKYLIDENE AND HETEROCYCLOALKYLIDENE INHIBITOR COMPOUNDS
The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.

...

02/23/2012
20120041002SUBSTITUTED PYRAZOLO [1,5-A] PYRIMIDINES AS METABOTROPIC GLUTAMATE ANTAGONISTS
The present invention relates to compounds of formula (I)

wherein A, E G, J, L, M, R1, R2, and R3 are as defined in the specification and claims. The invention also relates to...

02/16/2012
20120041000IMIDAZO [1,2-A]PYRIDINE DERIVATIVES AS FGFR KINASE INHIBITORS FOR USE IN THERAPY
The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer....
02/16/2012
20120035153BICYCLIC 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...
02/09/2012
20120035167INDOLE AND BENZOXAZINE DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
The present invention relates to novel indole and benzoxazine derivatives which are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”) and which are useful for the treatment or prevention of neurological and psychiatric disord...
02/09/2012
20120035168N-((6-AMINO-PYRIDIN-3-YL)METHYL)-HETEROARYL-CARBOXAMIDES
The invention relates to compound of the formula I

in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments ...

02/09/2012
20120035171BICYCLIC HETEROCYCLYL DERIVATIVES AS FGFR KINASE INHIBITORS FOR THERAPEUTIC USE
The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer....
02/09/2012
20120015941Antibacterial Amide and Sulfonamide Substituted Heterocyclic Urea Compounds
The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided....
01/19/2012
20120015974IMIDAZOPYRIDINE INHIBITORS OF IAP
The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I:

wherein Q, X1, X2, Y, Z R

01/19/2012
20120015930SUBSTITUTED IMIDAZOHETEROCYCLE DERIVATIVES
The present invention provides substituted imidazoheterocycles having the general structure of formula I:

wherein Y is chosen from —O—, —OCRgRh—, —CRgRhO...

01/19/2012
20120014906ORGANIC COMPOUNDS
The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also enco...
01/19/2012
20120009141FUNCTIONALIZED PYRROLIDINES AND USE THEREOF AS IAP INHIBITORS
A compound of Formula 1: or a salt thereof, and methods for the use thereof, especially as an IAP inhibitor, as well as related compounds, compositions, and methods.

...

01/12/2012
20120010209IMIDAZO[1,2-A]PYRIDINES AND IMIDAZO[1,2-b]PYRIDAZINES AS MARK INHIBITORS
The invention encompasses imidazo[1,2-a]pyridine and imidazo[1,2-b]pyridazine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions...
01/12/2012
20120010188Imidazopyridine Compounds
The invention relates to compounds of formula (I): and their pharmaceutically acceptable salts and solvates, which are inhibitors of SSAO activity. The invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds ...
01/12/2012
20120010414GLYCINE TRANSPORTER INHIBITING SUBSTANCES
The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's dise...
01/12/2012
20120010206IMIDAZOLOPYRIDINE 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...

01/12/2012
20120004243AMIDE DERIVATIVES BEARING A CYCLOPROPYLAMINOACARBONYL SUBSTITUENT USEFUL AS CYTOKINE INHIBITORS
The invention concerns a compound of the Formula (I), wherein Qa is heteroaryl and is substituted with halogeno; R1 and R2 are hydrogen; and Qb is phenyl or heteroaryl, and Qb may optionally bear 1 or 2 substituents selected from hydroxy, halogeno and (1-6C)alkyl, or a ...
01/05/2012
20120004222CB2 RECEPTOR LIGANDS FOR THE TREATMENT OF PAIN
The present invention relates to compounds represented by Formula (I) and Formula (II):

or pharmaceutically acceptable salts thereof. The present invention also provides pharmaceutical compositions comprising...

01/05/2012
201103114851,2,4-OXADIAZOLE DERIVATIVES AND THEIR THERAPEUTIC USE
The present disclosure relates to 1, 2, 4 oxadiazole derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the S1P1 receptors....
12/22/2011
201103129351H-Benz Imidazole-5-Carboxamides As Anti-Inflammatory Agents
There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds ...
12/22/2011
20110312957IMIDAZOPYRIDINES AND IMIDAZOPYRIMIDINES AS HIV-I REVERSE TRANSCRIPTASE INHIBITORS
The invention provides compounds of formula A or B which are useful in the treatment of a subject infected with HIV.

...

12/22/2011
20110312940TETRA-AZA-HETEROCYCLES AS PHOSPHATIDYLINOSITOL-3-KINASES (P13-KINASES) INHIBITOR
The present invention encompasses compounds of general formula (1) wherein R1 to R4, A, X, m and k are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use th...
12/22/2011
20110309348ORGANIC LIGHT-EMITTING DEVICE
A heterocyclic compound represented by Formula 1 below and an organic light-emitting device including the heterocyclic compound:

    • ...
12/22/2011
201103131535-HT4 INHIBITORS FOR TREATING AIRWAY DISEASES, IN PARTICULAR ASTHMA
The invention relates generally to the treatment of diseases of the respiratory system such as asthma and chronic obstructive pulmonary disease. More particularly, the present invention relates to methods of treating and preventing asthmatic airway inflammation. The tre...
12/22/2011
20110305618METHOD FOR SYNTHESIS OF A RADIONUCLIDE-LABELED COMPOUND USING AN EXCHANGE RESIN
The invention pertains to a method for eluting a radionuclide-label or a radionuclide-labeled compound using a solid phase extraction resin, to a device for performing such a method, and to a computer program for controlling such a device....
12/15/2011
20110306542NOVEL GLP-1 RECEPTOR STABILIZERS AND MODULATORS
Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the ...
12/15/2011
20110306597Nicotinamide Derivatives
The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are defined herein, to compositions containing such compounds and to the uses of such compounds for the treatment of allerg...
12/15/2011
20110297919ORGANIC LIGHT-EMITTING DEVICE
A heterocyclic compound represented by Formula 1 or Formula 2 below and an organic light-emitting device including the heterocyclic compound:

    12/08/2011
    20110294819Hepatitis C Virus Inhibitors
    The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the...
    12/01/2011
    20110294777BETA-LACTAMASE INHIBITORS
    Substituted bicyclic beta-lactams of Formula I: (I), are β-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combina...
    12/01/2011
    20110294779NOVEL IMIDAZOPYRIDINES
    The invention is concerned with novel imidazopyridine derivatives of formula (I)

    wherein R1, R2, R3, R4, R5 and A are as defined in the description and i...

    12/01/2011
    20110288085IMIDAZOPYRIDINE AND IMIDAZOPYRAZINE COMPOUNDS USEFUL AS KINASE INHIBITORS
    A compound of Formula (I) or Formula (II) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula (I) or Formula (II), and methods of treating conditions associated with...
    11/24/2011
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