Class 546/123 - Chalcogen and -C(=X)-, wherein X is chalcogen, bonded directly to ring carbons of the bicyclo ring system (e.g., 4-oxo-naphthyridine -3-carboxylic acid, etc.)

Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which both chalocogen (i.e., oxygen, sulfur,
No. of patents: 309
Last issue date: 05/29/2012

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Number	Title	Issue Date
8188283	Modulators of cystic fibrosis transmembrane conductance regulator The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to metho...	05/29/2012
8148530	Process for the preparation of 3.7-diazabicyclo[3.3.1] nonane compounds The present invention relates to a process for the preparation of 3,7-diazabicyclo[3.3.1]nonane compounds. According to the invention, in a first step, a dicarboxylic acid ester is reacted with a pyridine aldehyde and a primary amine. The piperidone which forms is r...	04/03/2012
8124773	1,8-naphthyridine compounds for the treatment of cancer Compounds and compositions for treating, preventing or managing cancer are disclosed. The compositions provided herein comprise SNS-595 and N-desmethyl-SNS-595. Also provided are pharmaceutical compositions comprising the compounds and methods of treatment using the...	02/28/2012
7919623	Naphthyridine derivatives having inhibitory activity against HIV integrase A compound having HIV Integrase Inhibitory activity of the formula: (wherein: R1 is optionally substituted aralkyl; R2 and R3 are each independently hydrogen, optio...	04/05/2011
7875722	Method for producing quinolone carboxylic acid derivative The present invention relates to a method for producing a quinolone compound having high antibacterial activity and high safety, at high yield and in a simple manner. A quinolonecarboxylic acid derivative (1) of interest is produced through a one-pot manner b...	01/25/2011
7728141	Substituted naphthyridinone derivatives Novel compounds of the 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...	06/01/2010
7700774	Heterocyclic compounds and their pharmaceutical compositions The present invention provides, among other things, new bicyclic heterocyclic compounds, compositions comprising these heterocyclic compounds, methods of making the heterocyclic compounds, and methods of using these heterocyclic compounds for treating or preventing ...	04/20/2010
7687629	Process for preparing 4-aminomethyl-3-alkoxyiminopyrrolidine methanesulfonate The present invention relates to a process for the preparation of 4-aminomethyl-3-alkoxyiminopyrrolidine methanesulfonate, a key intermediate of quinolone antibiotics. According to the process of the present invention, the total number of steps has been shortened to...	03/30/2010
7576214	Process for preparing 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1, 4-dihydro-1,8-naphthyridine-3-carboxylic acid Starting from ethyl 3-(2,6-dichloro-5-fluoropyridin-3-yl)-3-oxo-propanoate (1), the present invention provides highly pure 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid (5) in one-pot four steps using a single solvent. ...	08/18/2009
7449581	6-Substituted pyrido-pyrimidines The present invention provides compounds of the Formula I and II: wherein R1, R3, W, Z, X1, X2, Ar1, R8 and R9 are as defined herein, and methods ...	11/11/2008
7442710	Substituted phenyl methanones The present invention relates to compounds of general formula IA or IB wherein X1 and X2 are each independently N or C—R″ and R1, R2,R3, R...	10/28/2008
7439254	Compounds, compositions, and methods Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed. ...	10/21/2008
7402674	7-Phenylamino-4-quinolone-3-carboxylic acid derivatives, process for their preparation and their use as medicaments 7-Phenylamino-4-quinolone-3-carboxylic acid derivatives, process for their preparation and their use as medicaments The invention relates to 7-phenylamino-4-quinolone-3-carboxylic acid derivatives and to the physiologically tolerated salts and physiologically...	07/22/2008
7361762	Process for preparing acid salts of Gemifloxacin The present invention relates to a process for preparing acid salts of Gemifloxacin, a quinolone type antibiotic agent having potent antimicrobial activity. The process according to the present invention can provide advantages such as simplicity of process, improvem...	04/22/2008
7342024	4-Oxo-1-3-substituted phenyl-1,4-dihydro-1,8-naphthyridine-3-carboxamide phosphodiesterase-4 inhibitors Compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, are phosphodiesterase 4 inhibitors useful in the treatment of asthma and inflammation and useful for the enhancement of cognition ...	03/11/2008
7323460	N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides useful as HIV integrase inhibitors N-(Substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides are inhibitors of HIV integrase and inhibitors of HIV replication. The naphthyridine carboxamides are of Formula (I): wherein R1′, R	01/29/2008
7312334	Method of preparing inhibitors phosphodiesterase-4 In one aspect, the present invention is directed to a one pot method of preparing intermediates of Formula (V), which are useful in making inhibitors of phosphodiesterase-4: The present invention is also directed to a method of preparing phosphodiesterase inhibitors...	12/25/2007
7279487	Hydroxynaphthyridinone carboxamides useful as HIV integrase inhibitors Hydroxynaphthyridinone carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein L, R1a, R1b, R1c, R2a, R2b	10/09/2007
7273868	Pyrazine derivatives 1. A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, wherein X is ═CH— or ═N—, Y is —NH—, —NR4—, —S—, �...	09/25/2007
7238706	4-oxo-1-(3-substituted phenyl-1,4-dihydro-1,8-naphthyridine-3-carboxamide phosphodiesterase-4 inhibitors Compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, are phosphodiesterrase 4 inhibitors useful in the treatment of asthma and inflammation and useful for the enhancement of cognit...	07/03/2007
7232907	Process for production of naphthyridine-3-carboxylic acid derivatives A process for the production of naphthyridine-3-carboxylic acid derivatives of formula (I) having antibacterial activity. ...	06/19/2007
7220736	Pyrimidine compounds A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, wherein X is ═CH— or ═N—, Y is —NH—, —NR4—, —S—, —O—, —CH═N—,...	05/22/2007
7199242	Processes for the production of amino-protected derivatives of 4-aminomethylene-pyrrolidin-3-one and/or 4-aminomethylene-pyrrolidin-3-alkoxyimino derivatives and/or gemifloxacin or a salt thereof The invention provides a process for the production of a compound of formula (I): wherein P1 and P2, which may be the same or different, are amino protecting groups, which comprises protection of a compound of formula (II) in solution phase con...	04/03/2007
7179805	7-amino alkylidenyl-heterocyclic quinolones and naphthyridones The present invention relates to compounds having a structure according to Formula I wherein n, m, z, R, R2, R3, R4, R5, R6, A, E, X, Y, a and b are as defin...	02/20/2007
7169794	6-substituted pyrido-pyrimidines The present invention provides compounds of the Formula I and II: wherein R1, R3, W, Z, X1, X2, Ar1, R8 and R9 are as defined herein, a...	01/30/2007
7163948	Heterocyclic substituted 1,4-dihydri-4ox9-1,8-naphthyridine analogs The present invention relates to 1,4-dihydro-4-oxo-1,8-napthpyridine analogs of the formula and pharmaceutically acceptable salts, esters, and prodrugs thereof, wherein A, X, W and Y are ...	01/16/2007
7138409	Heterocyclic compounds Organic compounds having the structural formula I are provided where the variables have the values described herein and R1 and R2 join together to form a 6 membered substituted or unsubstituted ring including at least one O, N, or S atom, and Z...	11/21/2006
7129237	[1,4]Diazepino[6,7,1-ij]quinoline derivatives as antipsychotic and antiobesity agents Compounds of Formula I or a pharmaceutically acceptable salt thereof are provided: where R1 through R7 are defined herein. The compounds of Formula I are 5HT2c agonists or partial agonists, ...	10/31/2006
7115744	Method for producing 8-methoxy-quinolinecarboxylic acids The present invention relates to a novel process for preparing 8-methoxy-3-quinolonecarboxylic acids which are antibiotics having potent antibacterial action. ...	10/03/2006
7078522	Pyridopyrimidine or naphthyridine derivative A pyridopyrimidine or a naphthyridine derivative of the formula (I): wherein R1 is an optionally substituted nitrogen-containing heterocyclic group, etc.; R2 is H or a lower alkyl group; R	07/18/2006
7071187	Naphthyridine derivatives The present invention provides a novel naphthyridine derivative that is effective for relieving pain, less toxic, and also is effective for treating diabetic neuropathy, the derivative being represented by the general formula (1):	07/04/2006
7071185	1,2,3,4,7,8-hexahydro-6H-[1,4]diazepino[6,7,1-ij]quinoline derivatives as antipsychotic and antiobesity agents Compounds of Formula I or a pharmaceutically acceptable salt thereof are provided: where R1 through R7 are defined herein. The compounds of Formula I are 5HT2c agonists or partial ago...	07/04/2006
7037922	Aryl fused 2,4-disubstituted pyridines: NK3 receptor ligands Disclosed are compounds of formula (I) or pharmaceutically acceptable non-toxic salts or pharmaceutically acceptable solvates thereof wherein: (II) represents (a), (b), (c) or (d) and W, X, Y, A, B, C, D, E are variables as described herein. These compounds are high...	05/02/2006
7019142	Process for preparing naphthyridones and intermediates A process for preparing a naphthyridone carboxylic acid and its derivatives makes use of side chain intermediates of formulae I and IV herein. ...	03/28/2006
7012144	Quinolone carboxylic acid derivatives Quinolone carboxylic acid derivatives of formula (I) and pharmaceutically acceptable salts thereof have potent antibacterial activity: wherein, R1 is a C1-4 alkyl...	03/14/2006
6989447	Compounds Aminopiperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man. ...	01/24/2006
6974822	3-isoquinolinone derivatives as matrix metalloproteinase inhibitors This invention provides compounds defined by Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, Q, R2, R3, R4, and n are as defined in the specif...	12/13/2005
6921759	Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the prevention...	07/26/2005
6919351	Aza-and polyaza-naphthalenyl-carboxamides useful as HIV integrase inhibitors Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or tr...	07/19/2005
6909002	Method of preparing inhibitors of phosphodiesterase-4 In one aspect, the present invention is directed to a one pot method of preparing intermediates of Formula V, which are useful in making inhibitors of phosphodiesterase-4: The present invention is also directed to a me...	06/21/2005

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Class 546/123 - Chalcogen and -C(=X)-, wherein X is chalcogen, bonded directly to ring carbons of the bicyclo ring system (e.g., 4-oxo-naphthyridine -3-carboxylic acid, etc.)