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Class 548/195 - The -C(=X)- group is bonded directly to the nitrogen


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the nitrogen is bonded directly to the
No. of patents: 337
Last issue date: 05/15/2012


1                  
NumberTitleIssue Date
8178689Tricyclic compounds
The present invention provides novel compounds of formula I, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the tre...
05/15/2012
8053581Trisubstituted thiazole compounds, preparations methods, pharmaceutical compositions and medicals uses thereof
The present invention relates to 2,4,5-trisubstituted thiazole compounds of formula (I) or all possible isomers, prodrugs, pharmaceutically acceptable salts, solvates or hydrates thereof for the inhibition of plasma PLTP activity and/or plasma CETP activity, wherein...
11/08/2011
7999113Modulators of cystic fibrosis transmembrane conductance regulator
The present invention relates to modulators of cystic fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating CFTR mediated diseases using such modulators. ...
08/16/2011
7973169Modulators of ATP-Binding Cassette transporters
The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including CF Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treati...
07/05/2011
7880013Thiazole derivatives
(Wherein n is an integer of from 0 to 3; R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, or a substituted or unsubstituted aromatic heterocyclic group; R2 ...
02/01/2011
7718808Thiazole derivatives
(Wherein n is an integer of from 0 to 3; R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, or a substituted or unsubstituted aromatic heterocyclic group; R2 ...
05/18/2010
7705158Inhibitors of ion channels
Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted aryl sulfonamides, compositions comp...
04/27/2010
76876375-phenylthiazole derivatives and use as Pi3 kinase inhibitors
Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediate...
03/30/2010
7674912Pro-drugs of -thiazol-2-yl-benzamide derivatives
The invention relates to compounds of the formula I A-B-Z   I wherein the variables are as defined in the claims. The compounds are pro-drugs of A2A-receptor ligands with improved aqueous solubility, and are useful in the treatment...
03/09/2010
75983922-amido-4-phenylthiazole derivatives, the preparation and the therapeutic use thereof
The disclosure relates to 2-amido-4-phenylthiazole derivatives of general formula (I) below: in which R1, R2, R3, Y, m, n, and p are as defined in the disclosure; as well as to their isomers...
10/06/2009
7592461Indane modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
Novel non-steroidal compounds are provided that are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases having the structure of formula (I):...
09/22/2009
7563903Acylaminothiazole derivatives, their preparation and their therapeutic use
Compound corresponding to the general formula (I): in which, X represents an oxygen or sulphur atom; R1 represents a C1-10 alkyl group optionally substituted, a C3-7 cycloalkyl,...
07/21/2009
7553974Crystal of (2R,4R)-monatin potassium salt and sweetener composition containing same
Crystals of (2R,4R)-monatin potassium salt which exhibit an X-ray powder diffraction pattern having characteristic peaks at diffraction angles 2θ of 5.5°, 7.2°, 8.1°, 8.9°, and 16.3°, by powder X-ray diffraction (Cu—Kα radiation), are superior in sweetness,...
06/30/2009
7427635Substituted hydantoins
The present invention relates to compounds of the formula which are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as, ...
09/23/2008
7425555Heteroaryl substituted biphenyl derivatives as p38 kinase inhibitors
Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38. ...
09/16/2008
7414067Ophthalmic compositions for treating ocular hypertension
This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such co...
08/19/2008
74109882-Amido-thiazole-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions, and uses thereof
2-Amido-4-substituted-aryl-thiazole-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, methods of using compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions comprising compounds exhibiting ATP-utilizing enzyme inhibitory ...
08/12/2008
7411071Modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases, and have the structure ...
08/12/2008
7408069Preparation of 2-amino-thiazole-5-carboxylic-acid derivatives
A method for preparing a compound of the structure I, ...
08/05/2008
7390908Compounds effecting glucokinase
The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or preventio...
06/24/2008
7384968Thiazole-amine compounds for the treatment of neurodegenerative disorders
The present invention relates to compounds of the Formula I wherein R1, R3, R4, R5, R6 and R7 are as defined. Compounds of the Formula I have activity inhibi...
06/10/2008
7381734Serine protease inhibitors
Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents. ...
06/03/2008
7371869Substituted hydantoins
The present invention relates to compounds of the formula which are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as, cancer, ...
05/13/2008
7371770Acylaminothiazole derivatives and use thereof as β-amyloid inhibitors
Compounds of formula (I) as defined herein: inhibit the formation of the β-amyloid peptide (β-A4) and are, therefore, useful in the treatment of pathologies in which a β-amyloid peptide (β-A4) formation inhibitor provid...
05/13/2008
73356732,3-Diphenylpropionic acid derivatives or their salts, medicines or cell adhesion inhibitors containing the same, and their usage
A 2,3-diphenylpropionic acid derivatives or the salts represented by general formula (1) below; and pharmaceutical compositions and cell adhesion inhibitors comprising the derivatives or the salts as the active ingredient. In the formula, A, B and C independently re...
02/26/2008
7329670Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas
The compounds are aryl and heteroaryl substituted heterocyclic ureas of the formula A—NH—C(O)—NH—B where A is the aryl or hetaryl substituted heterocyclic group and B is an aryl or heteroaryl moiety. The compounds inhibit raf kinase and are useful in the tre...
02/12/2008
7329680Heterocycle substituted carboxylic acids
The present invention relates to compounds and pharmaceutically acceptable salts of formula (I): which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or hyper...
02/12/2008
7326728Modulators of glucocorticoid receptor, AP-1, and/or NF-κβ activity and use thereof
Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula ...
02/05/2008
7323482Thiazolyl-based compounds useful as kinase inhibitors
The present invention provides thiazolyl-based compounds of formula (I), useful for treating p38 kinase-associated conditions, wherein ring A is phenyl or pyridyl, and X, Y, B, R2, R3, Z
01/29/2008
7291636Acylaminothiazole derivatives, preparation and therapeutic use thereof
This invention discloses and claims a compound conforming to the general formula (I): Wherein R1, R2, R′2, R3, R4 and R5 are as described herein...
11/06/2007
7288659Acylaminothiazole derivatives, their preparation and therapeutic use
The invention concerns a compound of general formula (I), wherein: X represents an oxygen or sulphur atom; R1 represents, independently of each other when n=2 or 3, a halogen atom, a hydroxy, a C1-C3 alkyl, a C1-C3
10/30/2007
7285567Halogenated benzamide derivatives
A halogenated benzamide derivative characterized by greater specificity for viral pathogens and less disruptive to beneficial gut microflora, according to formula (III): in which ...
10/23/2007
7273881Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases, and have the structure ...
09/25/2007
7259166Substituted-cycloalkyl and oxygenated-cycloalkyl glucokinase activators
2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a polar ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of...
08/21/2007
7229988Dialkylhydroxybenzoic acid derivatives containing metal chelating groups and their therapeutic uses
The present invention provides novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups and the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen spe...
06/12/2007
7220765Derivatives of 2-arylimino-2,3-dihydrothiazoles, their preparation processes and their therapeutic use
The present invention is drawn to compounds of the formula in racemic and enantiomeric form or all combinations of these forms wherein the various substituents are as defined in the application which compounds ha...
05/22/2007
7169931Cyclic compounds exhibiting thrombopoietin receptor agonism
Pharmaceutical compositions containing as an active ingredient compounds of the general formula (I), prodrugs of the same, pharmaceutically acceptable salts of both, or solvates of them and exhibiting thrombopoietin receptor agonism: X1—Y...
01/30/2007
7160902Amide derivatives and methods of their use
Amide derivatives of the general formulae Ia and Ib: are disclosed. Pharmaceutical compositions containing these compounds, and methods for their use, inter alia, for treating and/or preventing gastrointestinal d...
01/09/2007
7125901Thiazole derivatives
A compound of the formula (I): R1—NH—X—Y-Z (I) wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor, a pharmaceutical composition, a method fo...
10/24/2006
7105671Substituted-cycloalkyl and oxygenated-cycloalkyl glucokinase activators
2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a polar ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of...
09/12/2006
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