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Class 540/597 - The additional hetero ring is six-membered and contains nitrogen


Subclass of Class 540 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the additional hetero ring is six-membered
No. of patents: 495
Last issue date: 05/22/2012


1                      
NumberTitleIssue Date
8183366Chemokine receptor antagonists
A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein the variants R, R9, Z, X, Q and Y are defined in the specification. ...
05/22/2012
7456279Coupling process for preparing quinolone intermediates
Process for making 7-cycloamino-1-cyclopropyl-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acids. Borate ester compounds suitable for use in such process. ...
11/25/2008
7419990Piperidine derivatives as melanocortin-4 receptor agonists
Certain novel piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disor...
09/02/2008
7414047Piperazinyl and diazapanyl benzamides and benzthioamides
Substituted piperazinyl and diazepanyl benzamides and benzthioamides of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions. ...
08/19/2008
7405209Protease inhibitors
The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such co...
07/29/2008
7393845Heteroaryl derivates, their preparation and use
A heteroaryl derivative having the formula (I). The compounds of the invention are considered useful for the treatment of affective disorders such as general anxiety disorder, panic disorder, obsessive compulsive disorder, depression, social phobia and eating disord...
07/01/2008
7361682Indole derivatives as H3 inverse agonists
The present invention relates to compounds of formula I: wherein X, R1, R2, R3, R4 and R5 are as defined in the description and claims, and pharmaceutically acceptable ...
04/22/2008
7323456Carboxylic acid derivatives compounds and agents comprising the compounds as active ingredient
A compound of formula (I) (wherein all symbols are as defined in the specification) and a salt thereof, and peroxisome proliferator activated receptor regulator comprising thereof as active ingredient. Because a ...
01/29/2008
7307074Diazepan derivatives or salts thereof
To provide a compound which has an anticoagulation action based upon inhibition of activated blood coagulation factor X and is useful as an anticoagulant or an agent for prevention and treatment of diseases caused by thrombus or embolus. A diazepan derivative such a...
12/11/2007
7304052Substituted homopiperidinyl benzimidazole analogues as fundic relaxants
The present invention relates to compounds of formula (I) their prodrugs, N-oxides, addition salts, quaternary amines and stereochemically isomeric forms, wherein the bivalent radical -{circle around (A)}- repres...
12/04/2007
7291613Inhibitors of p38 kinase
The invention is directed to methods to inhibit p38-α kinase using compounds comprising saturated heterocycles coupled to a fused ring system. ...
11/06/2007
7285547Amidinophenylalanine derivatives as thrombin inhibitors
The compounds of the formula (formula 1) and pharmaceutically acceptable salts thereof and a process for preparing the same and pharmaceutical compositions containing the same are described wherein the substituents have the meaning as specified in the description. T...
10/23/2007
7276524Pyridyl alkane acid amides as cytostatics and immunosuppressives
The invention relates to new pyridyl alkane acid amides according to general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression ...
10/02/2007
7259158Naphthaline derivatives as H3 inverse agonists
The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, to the preparation of such compounds and pharmaceutical compositions containing them. The compounds are usef...
08/21/2007
7241745Pyridyl alkene and pyridyl alkine acid amides as cytostatics and immunosupressives
The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I) as well as methods for their production, medicaments containing these compounds as well as their m...
07/10/2007
7223750Derivatives of 5-(pyridin-3-yl)-1-azabicyclo[3.2.1]octane, the preparation thereof and the application of same in therapeutics
Compounds complying with the general formula (I) in which R either represents a halogen atom or a phenyl group substituted by one or more groups chosen from halogen atoms and (C1–C6)alkyl,...
05/29/2007
7202237Pyridylether derivatives, their preparation and use
The present invention relates to novel pyridylether derivatives which are cholinergic ligands at nicotinic Ach receptors. The compounds of the invention are useful for the treatment of conditions, disorders, or diseases involving the cholinergic system of the centra...
04/10/2007
7183274Piperidine-2,6-diones heterocyclically substituted in the 3-position
Piperidine-2,6-diones heterocyclically substituted in the 3-position corresponding to formula I Also the production and use of such compounds in pharmaceutical formulations and related methods of treatment. ...
02/27/2007
7135466Quinoline and quinazoline derivatives and drugs containing the same
There are provided compounds which can be used in the treatment of diseases mediated by the autophosphorylation of a PDGF receptor, specifically, compounds which can inhibit neointima formation hypertrophy. The compounds are those represented by formula (I) or pharm...
11/14/2006
7115596Thiazole compounds as integrin receptor antagonists derivatives
The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of ...
10/03/2006
7115635Benzylpiperidine compound
The object of the present invention is to provide a compound having a treatment effect based on a chemokine inhibitory activity, which is satisfactory as a pharmaceutical product for oral administration. The present inventors have found that the following ben...
10/03/2006
7105556Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method
Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2
09/12/2006
7087628N-heterocyclyl hydrazides as neurotrophic agents
This invention relates to a series of N-heterocyclyl hydrazides of Formula I, and pharmaceutical compositions containing them. The compounds of the invention have neurotrophic activity and are useful in the treat...
08/08/2006
7071184Protease inhibitors
The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel int...
07/04/2006
7067532Substituted quinolines as antitumor agents
The invention provides a compound of Formula (Ia), or a pharmaceutically acceptable salt pro-drug or solvate thereof. The invention also provides a process for the preparation of a compound of Formula (Ia), pharmaceutical compositions of a compound of Formula (Ia) a...
06/27/2006
7041675Heterocyclic compounds and their use as PARP inhibitors
The invention relates to compounds of the formula I and the tautomeric forms, possible enantiomeric and diasteromeric forms thereof, and prodrugs thereof, and use thereof as PARP inhibitors. ...
05/09/2006
7026310Heteroaryl derivatives and their use as medicaments
The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors. ...
04/11/2006
7022695Thioether-substituted benzamides as inhibitors of Factor Xa
Thioether-substituted benzamide compounds having the formula: are provided that exhibit exceptionally strong inhibition of Factor Xa in combination with weak hERG binding. ...
04/04/2006
7012073Quinoline derivatives
Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3, A1 and A2 have the significance given in claim 1,...
03/14/2006
6992092Anti-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, R2
01/31/2006
6984637Cyclic amine derivatives-CCR-3 receptor antagonists
This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compound...
01/10/2006
6974870Substituted 3-amino-thieno [2,3-b]pyridine-2-carboxylic acid amide compounds and processes for preparing and their uses
Disclosed are compounds of formula (I): wherein R1 and R2 are defined herein, which are useful as inhibitors of the kinase activity of the IκB kinase (IKK) complex. The compounds are therefore us...
12/13/2005
6964956Substituted 3-amino-thieno [2,3-b]pyridine-2-carboxylic acid amide compounds and processes for preparing and their uses
Disclosed are compounds of formula (I): wherein R1 and R2 are defined herein, which are useful as inhibitors of the kinase activity of the IκB kinase (IKK) complex. The compounds are therefore us...
11/15/2005
6962926Antagonist of MCP-1 function, and compositions and methods of use thereof
Compounds of formula A and formula B: and their pharmaceutically acceptable salts, compositions comprising them, methods for their use, and their use in the preparation of medicaments. The compounds are antagonists of ...
11/08/2005
6953792Cyclohexyl derivatives and their use as therapeutic agents
The present invention relates compounds of the formula (I): wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of: (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l) and R1, R2, R3
10/11/2005
6939867β3 agonists and uses thereof
Sulfamide compounds having formula (I) are described as well as their use in the treatment of diseases dependent on the signaling pathways associated with β-adrenergic receptors, such as obesity, diabetes, hypertension, gastrointestinal hypo- or hyper-motility and ...
09/06/2005
6919368N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases. ...
07/19/2005
6919456Catalytic compositions and methods for asymmetric aldol reactions
Methods and compositions are provided for the direct catalytic asymmetric aldol reaction of aldehydes with donor molecules selected from ketones and nitroalkyl compounds. The reactions employ as catalyst a Group 2A or Group 2B metal complex of a ligand of formula I,...
07/19/2005
6908929Phenyl-substituted imidazopyridines
The invention features pharmaceutically-active imidazopyridines and derivatives that are substituted with phenyl, methods of making them, and methods of using them. ...
06/21/2005
6887864Azepane derivatives
This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their ...
05/03/2005
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