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Class 546/233 - Acyclic nitrogen bonded directly to a -C(=X)- group, wherein X is chalcogen


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds containing an acyclic nitrogen which is bonded
No. of applications: 52
Last issue date: 01/26/2012


1    
Application No.Application TitleIssue Date
20120022069ACRYLAMIDE COMPOUNDS AND THE USE THEREOF
The invention relates to acrylamide compounds of Formula I mentioned below.

The invention is also directed to the use compounds of Formula I to treat or prevent a disorder responsive to the blockade of calcium channels, and particularly N-t...

01/26/2012
20110306603LARGE SUBSTITUENT, NON-PHENOLIC OPIOIDS AND METHODS OF USE THEREOF
8-Substituted-2,6-methano-3-benzazocines of general structure

are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications....

12/15/2011
20110275670New Compounds VII
The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight g...
11/10/2011
20110263651NOVEL PIPERIDINE-BUTYRAMIDE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS
The present invention relates to novel piperidine-4-butyramide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprisi...
10/27/2011
20110218217PIPERIDYLPROPIONAMIDE DERIVATIVES USEFUL FOR THE TREATMENT OF CNS DISORDERS INCLUDING DEPRESSION AND PANIC DISORDER
This invention relates to novel piperidine-4-propionamide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising th...
09/08/2011
20110172174Antibacterial agents
Antibacterial compounds of formula I are provided:

As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of ...

07/14/2011
20110144108SUBSTITUTED PIPERIDINE COMPOUNDS AND METHODS OF THEIR USE
Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as an...
06/16/2011
20110105485Alpha-(N-Sulfonamido)Acetamide Derivatives as Beta-Amyloid Inhibitors
There is provided a series of novel α-(N-sulfonamido)acetamide compounds of the Formula (I)

wherein R, R1, R2 and R3 are defined herein, which are inhibitors of β-amyloid pe...

05/05/2011
20110046106ARYL SULFONAMIDES AS EFFECTIVE ANALGESICS
The present invention relates to compounds of general formula I

wherein A, B, R1, R2 and R3 are defined as in claim 1, the enantiomers, the diastereomers, the mixtures ...

02/24/2011
20110003856N-ADAMANTYL BENZAMIDES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE
Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. ...
01/06/2011
20100324025Antibacterial Agents
Antibacterial compounds of formula I are provided:

As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of ...

12/23/2010
20100093801PIPERIDINE COMPOUNDS, PHARMACEUTICAL COMPOSITION COMPRISING THE SAME AND ITS USE
Piperidine compounds and pharmaceutically useful salts thereof, a pharmaceutical composition including an effective amount of the racemic or enantiomerically enriched piperidine compounds to treat gastrointestinal diseases, and a method of treating gastrointestinal dise...
04/15/2010
20100063292PROCESS FOR THE PREPARATION OF TRIFLUOROETHOXYTOLUENES.
The present invention relates to an process for the preparation 2,5-bis(2,2,2-trifluoroethoxy)toluene [II]. The compound 2,5-bis(2,2,2-trifluoroethoxy)toluene is useful as intermediate for pharmaceutical industry, especially useful as an intermediate for the preparation...
03/11/2010
20100056794PROCESS FOR THE PREPARATION OF 2,5-BIS-(2,2,2-TRIFLUOROETHOXY)-N-(2-PIPERIDYL-METHYL)-BENZAMIDE AND SALTS THEREOF
Process for the preparation of 2,5-bis(2,2,2-trifluoroethoxy)-N-(2-piperidylmethyl)benzamide, its pharmaceutically acceptable salts and important intermediates thereof that involves 1,4-dihalotoluenes as starting material. The method involves a technique for preparing t...
03/04/2010
20090306141Novel Compounds
The invention provides compounds of general formula (I) wherein m, n, Q, Z1, Z2, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the specification, processe...
12/10/2009
20090286765Therapeutic Agents
A compound of the formula (I): wherein R1, R2, R3, R4, Ar, A, n and m are defined herein, is disclosed as a GlyT1 inhibitor; pharmaceutical compositions containing the compound of the formula (I) are also disclosed as are thei...
11/19/2009
20090270451Piperdine Glycine Transporter Inhibitors
The present invention is directed to piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases i...
10/29/2009
20090253701ORGANIC COMPOUNDS
Disclosed are δ-amino-γ-hydroxy-ω-aryl-alkanoic acid amide compounds of formula (I)

and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising thes...

10/08/2009
200902037402-phenylpropionic acid derivatives and pharmaceutical compositions containing them
4-(trifluoromethanesulfonyloxyphenyl)propionic acid derivatives and pharmaceutical composition containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and...
08/13/2009
20090181943Inhibitors of Histone Deacetylase
This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula compounds of the Formula (I)

and N-oxides, hydrates, solvates,...

07/16/2009
20090124664(R)-Arylalkylamino Derivatives and Pharmaceutical Compositions Containing Them
The present invention relates to selected (R)-arylalkylamino derivatives of formula (I), in which R, R1 and Ar are as defined in the claims. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention ab...
05/14/2009
20090062296Prostaglandin derivatives
Nitroderivatives of prostaglandin amides having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension....
03/05/2009
20090053721VOLTAGE-GATED ION CHANNEL MUTANTS FOR USE IN IDENTIFYING ION CHANNEL MODULATING COMPOUNDS
The present invention provides novel methods and compositions for identifying ion channel modulating compounds, including atrial-selective antiarrhythmic agents and ion channel modulating compounds that preferentially modulate K+ channels. The ion channel mod...
02/26/2009
20080312446IMAGING AGENTS FOR DIAGNOSIS OF PARKINSON'S DISEASE
Generally, the present invention is directed to central nervous system dopamine transporter-imaging agents and methods of use thereof. In certain embodiments, the present invention relates to radiolabeled piperidine derivatives for use as imaging agents in the diagnosis...
12/18/2008
20080275028Modulators or Alpha7 Nicotinic Acetylcholine Receptors and Therapeutic Uses Thereof
The present invention relates to compounds with α7 nAChR agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological, psychiatric, cognitive, immunological and inflammatory d...
11/06/2008
20080207694Hydroxamates as Histone Deacetylase Inhibitors and Pharmaceutical Formulations Containing Them
Compounds of structure (I) having histone deacetylase (HDAC) inhibitor activity are described. The compounds are chemically characterised by the presence of hydroxamic acid, with zinc as chelator, and an aromatic nucleus connected by a linker in which either a bicyclic ...
08/28/2008
20080200467SOLUBLE EPOXIDE HYDROLASE INHIBITORS
Disclosed are alpha keto amide and alpha hydroxy amide compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, c...
08/21/2008
20080194520Sulfonyl Amino Cyclic Derivatives and Use Thereof
The present invention is related to derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibros...
08/14/2008
20080166332Methods of Treatment of Amyloidosis Using Subsituted Ethanolcyclicamine Aspartyl Protease Inhibitors
The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein...
07/10/2008
20080108663Cyclopropyl Piperidine Glycine Transporter Inhibitors
The present invention is directed to cyclopropyl piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neuro-transmission dysfunction a...
05/08/2008
20080090785Compounds For Enzyme Inhibition
Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by th...
04/17/2008
20080076769Norvaline Derivative and Method for Preparation Thereof
Norvaline derivative of the formula [I] or pharmaceutically acceptable salt thereof, method for preparing the same, pharmaceutical composition containing the same, and use of said compound for inhibiting transporting activity of glycine transporter type 2 (GlyT2). <...
03/27/2008
20070232661Hedgehog Pathway Antagonists
Aromatic compounds for treating various diseases and pathologies are disclosed. The methods use of such compounds are also provided. Accordingly, the present invention makes available methods and compositions for inhibiting aberrant growth states resulting from hedgehog...
10/04/2007
20060229336Ccr5 antagonists as therapeutic agents
The present invention relates to compounds of formula (I) or a pharmaceutically acceptable derivatives thereof, useful in the treatment of prophylazis of CCR5-related diseases and disorders, for example, in the inhibition of HIV replication, the prevention or treatment ...
10/12/2006
20060089383Substituted piperidine compounds and methods of their use
Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as an...
04/27/2006
20060079555Diarylmethylidene piperidine derivatives, preparations thereof and uses thereof
Compounds of general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, m and n are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in th...
04/13/2006
20050250758Nitrosated and nitrosylated H2 receptor antagonist compounds, compositions and methods of use
The invention describes novel nitrosated and/or nitrosylated H2 receptor antagonist compounds, and novel compositions comprising at least one H2 receptor antagonist compound that is optionally substituted with at least one NO and/or NO2 ...
11/10/2005
20050245743Secondary amino anilinic piperidines as mch1 antagonists and uses thereof
This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmac...
11/03/2005
20050239828Spirocyclic amides as cannabinoid receptor modulators
Novel compounds of structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful ...
10/27/2005
20050234050Ph sensitive prodrugs of 2,6-diisopropylphenol
The present invention is directed to water-soluble derivatives of 2,6-diisopropylphenol (Propofol). The compounds act as prodrugs of 2,6-diisopropylphenol and metabolize rapidly to Propofol thereby providing an alternative to the water-insoluble 2,6-diisopropylphenol. P...
10/20/2005
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