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Class 546/281.1 - Polycyclo ring system having the additional hetero ring as one of the cyclos


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the additional hetero ring is one of
No. of patents: 242
Last issue date: 11/15/2011


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NumberTitleIssue Date
8058446Certain substituted amides, method of making, and method of use thereof
At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein. Pharmaceutical c...
11/15/2011
7419986Antidepressant azaheterocyclylmethyl derivatives of heterocycle-fused benzodioxans
Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, pre...
09/02/2008
7410982Propanamine derivatives as serotonin and norepinephrine reuptake inhibitors
There is provided a heretoaryloxy/thio 3-substituted propanamine compound of formula (I) wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C1-C...
08/12/2008
7393846Heterocyclic compounds useful for the treatment of inflammatory and allergic disorders
The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, the...
07/01/2008
7393865Sleep inducing compounds and methods relating thereto
Compounds having the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts, esters and solvates thereof, wherein R1, R2, R3a, R3b, L
07/01/2008
7390907Vanilloid receptor ligands and their use in treatments
Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascu...
06/24/2008
7335666Antidepressant azaheterocyclylmethyl derivatives of heterocycle-fused benzodioxans
Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, pre...
02/26/2008
7288567Inhibitors of histone deacetylase
The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and cond...
10/30/2007
7238725Tricyclic compounds useful for the treatment of inflammatory and allergic disorders: process for their preparation and pharmaceutical compositions containing them
The present invention relates to novel tricyclic compounds useful for the treatment of inflammatory conditions, diseases of the central nervous and insulin resistant diabetes. ...
07/03/2007
7223789Heterocyclic compounds useful for the treatment of inflammatory and allergic disorders: process for their preparation and pharmaceutical compositions containing them
The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, the...
05/29/2007
7217723Heterocyclic compound having oxime group
The present invention provides a compound that has an excellent inhibitory activity on STAT6 activation and is effective against allergic diseases, and a medicinal composition thereof. According to the present invention, disclosed is the compound represented by the ...
05/15/2007
7208491N-monoacylated o-phenylenediamines
Mono-acylated o-phenylendiamines derivatives of formula I wherein X and R are as described herein, have been found useful for the treatment of diseases mediated by the inhibition of histone deacetylase, such as c...
04/24/2007
7205305Inhibitors of p38
The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceut...
04/17/2007
7183293Ether derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds of the formula wherein j is 1; k is 0 or 1; m is 1, 2 or 3; n is 1 or 2; W1 and W2 are independently —O— or —S(═O)t—, where t i...
02/27/2007
7135479Antidepressant azaheterocyclylmethyl derivatives of heterocycle-fused benzodioxans
Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress di...
11/14/2006
7129234Phenyl heterocyclyl ethers
The invention relates to compounds of formula I ...
10/31/2006
7105513Acylated, heteroaryl-condensed cycloalkenylamines and their use as pharmaceuticals
The present invention relates to acylated, heteroaryl-condensed cycloalkenylamines, to pharmaceutical compositions comprising such compounds, to methods for the stimulation of the expression of endothelial NO synthase, and methods of treatment comprising administeri...
09/12/2006
7034044Conjugated aromatic compounds with a pyridine substituent
The present invention relates to compounds of formulae The compounds of the present invention are NMDA (N-methyl-D-aspartate)-receptor subtype blockers and are used in the treatment of diseases related to this receptor.
04/25/2006
6921827Process for preparing 3-aryl-benzo{b} thiophenes
The present invention relates to a process for preparing a compound of formula (I): which includes cyclodehydrating a compound of formula (II): in the presence of an acid activated clay or acid activated zeolite catalyst and in the presence of a suitable solvent
07/26/2005
6897226NK-1 receptor active amine oxide prodrugs
Compounds of the invention are amine oxide prodrugs showing activity on the NK1 receptor. ...
05/24/2005
6872730Substituted benzofurans and benzothiophenes, methods of making and methods of use as integrin antagonists
The present invention relates to novel substituted benzofurans and benzothiophenes compounds that are antagonists of alpha V (αv) integrins, for example αvβ3 and αvβ5 integrins, their pharmaceutically acceptable salts...
03/29/2005
6846819Fab I inhibitors
Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections. ...
01/25/2005
6828333Ether derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds of the formula wherein j is 1; k is 0 or 1; m is 1, 2 or 3; n is 1 or 2; W1 and W2 are independently —O— or —S(═O)t—, where t is 0, 1...
12/07/2004
6822093Synthesis of heteroarylamine intermediate compounds
Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines. ...
11/23/2004
6720423Dihydrobenzofuran and dihydrobenzothiophene 2,4-pentadienoic acid derivatives having selective activity for retinoid X (RXR) receptors
Compounds of the formula where the variables have the meaning defined in the specification, are specific or selective agonists of RXR retinoid receptors. ...
04/13/2004
6696470Pyridylthiophene compounds
A compound of the formula: ##STR1## and its pharmaceutically effective salts, wherein R1 and R2 are independently selected from the following: (a) hydrogen, halo, R5 --, C2-6 alkenyl, C2-6 alkynyl, ...
02/24/2004
6689797Tetrahydropyridines, preparation method and pharmaceutical compositions containing same
The present invention relates to compounds of formula (I): ##STR1## in which R1 represents a hydrogen or halogen atom, or a group CF3 ; R2 and R3 represent, independently, a hydrogen atom or a methyl group; n and n' ...
02/10/2004
6683192Small organic molecule regulators of cell proliferation
A compound represented in general formula (X) and (XI): ##STR1##...
01/27/2004
6664274Piperidine derivatives as serotonine reuptake inhibitors
The present invention provides compounds of formula I ##STR1## and a method of inhibiting the reuptake of serotonin, antagonizing the 5-HT1A receptor and antagonizing the 5-HT2A receptor which comprises administering to a subject in ...
12/16/2003
6608060Inhibitors of p38
The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides...
08/19/2003
6608090Benzothiophenes with novel basic side chains
The instant invention provides novel benzothiophene compounds for use in treating skeletal diseases....
08/19/2003
6593471Synthesis of heteroarylamine intermediate compounds
Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines....
07/15/2003
6590099Synthesis of heteroarylamine intermediate compounds
Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines....
07/08/2003
6559167Prodrugs of proton pump inhibitors
Prodrugs of the pyridyl methyl sulfinyl benzimidazole type proton pump inhibitor drugs have a hydrolyzable arylsulfonyl or heteroarylsulfonyl group attached to the benzimidazole nitrogen. The prodrugs of the invention hydrolyze under physiological conditi...
05/06/2003
6555028Polymeric matrix compatibilized naphthopyrans
Described are polymeric matrix compatibilized naphthopyran compounds, examples of which are certain 2H-naphtho[1,2-b]pyrans, 3H-naphtho[2,1-b]pyrans and indeno[2,1-f]naphtho[1,2-b]pyrans each having at least one substituent containing terminal and/or pend...
04/29/2003
6544986Pyridones and their use as modulators of serine hydrolase enzymes
This invention relates to a compound of formula I: ##STR1## or a pharmaceutically acceptable salt thereof; in which preferably R3, R4 and R6 are each hydrogen; X is C.dbd.O or CH2 ; and R7 and R8 are...
04/08/2003
6458787Cyclic AMP-specific phosphodiesterase inhibitors
Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, a...
10/01/2002
6429312N-aminoalkyldibenzothiopencarboxamide receptor subtype specific ligands
Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R1, R2, R3, R4 are the same or different and represent hydrogen, C1 -C6 ...
08/06/2002
6423717Sulphonamide derivatives, process for their preparation, and their use as medicaments
Novel sulphonamide derivatives having CNS activity, processes for their preparation and their use as medicaments are disclosed. The present compounds are of formula (I) or a salt thereof: ##STR1## wherein: P isbenzothiophene, benzothiadiazole, quinoline, ...
07/23/2002
6388105Benzofuran, indole or benzothiophene 2,4-pentadienoic acid derivatives having selective activity for retinoid X (RXR) receptors
Compounds of the formula ##STR1## Where the variables are defined as in the specification, are selective agonists of RXR retinoid receptors....
05/14/2002
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