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Class 546/208 - Ring nitrogen in the additional hetero ring


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the additional hetero ring contains ring
No. of patents: 906
Last issue date: 04/10/2012


1                      
NumberTitleIssue Date
8153807Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
The present invention discloses novel compounds of Formula I: (I) having 11-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I,...
04/10/2012
8148534Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
The present invention discloses novel compounds of Formula I: (I) possessing 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Form...
04/03/2012
8115005Pyrazolylphenyl and pyrrolylphenyl inhibitors of LTA4H for treating inflammation
Two chemical genera of pyrazolylphenyl and pyrrolylphenyl derivatives are disclosed. They have the general formula: In these compounds ring (a) is a pyrazole or pyrrole; Q is selected from the group consisting of a direct b...
02/14/2012
8106208Benzamide compounds that act as NK receptor antagonists
The present invention relates to new compounds of formula I, to pharmaceutical compositions comprising said compounds, and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of compounds of formula I. ...
01/31/2012
7897776Sulfonamide containing compounds for treatment of inflammatory disorders
Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of an inflammatory condition, in particular asthma. The compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof:
03/01/2011
7858797Biphenyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, r, R1, R2, R3, R4, R5, R6, R7, and W are as defined in the specificat...
12/28/2010
7851631Biphenyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, r, R1, R2, R3, R4, R5, R6, R7, and W are as defined in the specificat...
12/14/2010
7851632Biphenyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I: wherein a, b, c, m, p, s, t, W, Ar1, X1, R1, R2, R3, R4, R6, and R7 are as defined in t...
12/14/2010
7754885Tubulysins, method for producing the same and tubulysin preparations
The invention relates to a compound of the following general formula (tubulysin) having the following meanings for R, R1, R2, R3, R4, R5, R6, R7, ...
07/13/2010
7700778Acylated piperidine derivatives as melanocortin-4 receptor agonists
Certain novel 4-substituted N-acylated 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 prevent...
04/20/2010
7671206Synthesis and uses of pyroglutamic acid derivatives
Novel pyroglutamic acid derivatives (I), wherein R1 is —OH, —ORa, wherein Ra is alkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, aralkyl or heterocyclyl; R2, R3 and R4 are independently H, a nitrogen protecting group wh...
03/02/2010
7427683c-fms kinase inhibitors
The invention is directed to compounds of Formulae I: wherein A, R1, R2, R3, R4, X, and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceu...
09/23/2008
7425633Pyrrolidine compounds
A compound of the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, T, X, Y, and Z are as defined herein. Also disclosed is a ...
09/16/2008
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
7407974Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thro...
08/05/2008
7407972Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thro...
08/05/2008
7402581Azetidine compounds
The present invention relates to a compound of the general formula (I) wherein Het is an optionally substituted 4-, 5-, 6- or 7-membered heterocyclic ring having at least one nitrogen atom; R1 is hydrogen, hydroxy, C1-C4 alkyl, C3-C
07/22/2008
7399773Process for the synthesis of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1-pyrrole-3-carboxylic acid and phenylamide
An improved process for the preparation of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide by a novel synthesis is described where methyl cyanoacetate is converted in eight ...
07/15/2008
7388007Gamma-lactams as beta-secretase inhibitors
There is provided a series of novel substituted gamma-lactams of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R4, R5 and R6
06/17/2008
7381727Pyrrole derivatives, their preparation and their therapeutic use
The invention concerns compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. The in...
06/03/2008
7368463Substituted 4-amino-1-benzylpiperidine compounds
This invention provides 4-amino-1-benzylpiperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes ...
05/06/2008
7358251N-sulfonylurea apoptosis promoters
Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds. ...
04/15/2008
7351721Amino acid derivatives and pharmaceutical composition comprising, as active ingredients, them
The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification). The compounds of the formula (I) possess inhibitory activity of N-...
04/01/2008
73420271-phenylpiperidin-3-one derivatives and processes for the preparation thereof
Provided are 1-phenylpiperidin-3-one derivatives and pharmaceutically acceptable salts thereof, having cysteine protease inhibitory activity, pharmaceutical compositions containing the same as an active ingredient, and processes for the preparation thereof. ...
03/11/2008
7338947Cyclic derivatives as modulators of chemokine receptor activity
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma, pro...
03/04/2008
7335677Inhibitors of dipeptidyl peptidase IV
Novel compounds that are inhibitors of one or most post-proline cleaving proteases, e.g. dipeptidyl peptidase IV, according to general formula (1). R1 is H or CN, X1 is O, S, CH2, CHF, CF2, CH(CH3), C(CH3
02/26/2008
7332508Substituted homopiperidine, piperidine or pyrrolidine derivatives
A novel class of substituted homopiperidine, piperidine and pyrrolidine derivatives, methods for their preparation, pharmaceutical compositions comprising them and use thereof in the treatment of disorders related to the histamine H3 receptor. More particularly, the...
02/19/2008
7326720Phenyl- and pyridylpiperidines with TNF activity
The present invention relates to compounds of formula (I): in which X represents N or CH; R1 represents a hydrogen or halogen atom or a CF3 group; R2 and R3 independent...
02/05/2008
7326719Cathepsin S inhibitors
This invention relates to peptidyl compounds of the formulas (I) and (II) active as cathepsin S, a cysteine protease, inhibitors. The compounds are selective, reversible inhibitors of the cathepsin S are therefore useful in the treatment of autoimmune and other dise...
02/05/2008
73190981,3-dioxoisoindole derivatives having selective antagonism of T-type calcium channel
The present invention relates to 1,3-dioxoisoindole derivatives of Formula (1) or pharmaceutically acceptable salts thereof, a preparation method thereof and use thereof as a T-type calcium channel antagonist, based on the fact that 1,3-dioxoisoindole derivatives of...
01/15/2008
7317007Benzothiazole derivatives with activity as adenosine receptor ligands
The present invention relates to substituted benzothiazole derivitives and to their pharmaceutically acceptable salts useful for the treatment of diseases related to the adenosine receptor. ...
01/08/2008
7312218Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia-If: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or hetero...
12/25/2007
7309800Biphenylcarboxylic amide derivatives as p38 kinase inhibitors
Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors. ...
12/18/2007
7301028Mitotic kinesin inhibitors
The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which com...
11/27/2007
7294636Chemical compounds
Compounds of formula (I): compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal) ...
11/13/2007
7288559Carboxamide spirohydantoin CGRP receptor antagonists
The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pha...
10/30/2007
7285664Heterocyclic or benzenic derivatives of lipoic acid, their preparation and their use as medicaments
A compound having a formula selected from the group consisting of wherein the substituents are defined as in the specification. The compounds are useful as intermediates in the preparation of compounds of formula...
10/23/2007
7279469Diaminotriazoles useful as inhibitors of protein kinases
The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. ...
10/09/2007
7279491Phenylpiperidines and phenylpyrrolidines
Substituted phenylpiperidines and phenylpyrrolidines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions. ...
10/09/2007
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
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