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Class 514/252.19 - Five-membered nitrogen hetero ring attached directly or indirectly to the 1,3-diazine ring by nonionic bonding


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the 1,3-diazine ring is attached
No. of patents: 262
Last issue date: 09/27/2011


1              
NumberTitleIssue Date
8026241Vanilloid receptor ligands and their use in treatments
Therapeutic benzimidazoles and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, ...
09/27/2011
7968550Substituted N-aryl heterocycles, process for their preparation and their use as medicaments
The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have the stated...
06/28/2011
7935704Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof
Compounds represented by the following structure (I) are disclosed: as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate ...
05/03/2011
7888361Tyrosine kinase inhibitors containing a zinc binding moiety
The present invention relates to tyrosine kinase inhibitors that contain a zinc-binding moiety and their use in the treatment of tyrosine related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors. ...
02/15/2011
7622473'N-(2-chloro-6-methylphenyl)-2-[[(6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamides metabolites
The present invention is directed to metabolites of ′N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide, the compound of formula (I), pharmaceutical compositions thereof, and to methods of using...
11/24/2009
7576087Heterocyclyl-3-sulfonylazaindole or -azaindazole derivatives as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor. ...
08/18/2009
7557106Substituted pyrimidines useful as protein kinase inhibitors
The present invention provides a facile process for the preparation of tri- and tetra-substituted pyrimidines. The process is useful for preparing inhibitors of protein kinases, especially Aurora kinase. These inhibitors are useful for treating or lessening the seve...
07/07/2009
7491725Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors
The invention relates to processes for preparing compounds having the formula, and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R2, R...
02/17/2009
7473691Pyrazole compounds useful as protein kinase inhibitors
This invention describes novel protein kinase inhibitors of formula VII: wherein G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said...
01/06/2009
7465732(2S,4S)-4-(piperazin-1-yl)pyrrolidine-2-methanone derivatives
The invention provides compounds of formula (I), or a pharmaceutically acceptable salt of said compound, or a solvate of said compound or salt, wherein R1, R2, R3, HET, n, Q, X, Y, and Z are...
12/16/2008
7414046Gyrase inhibitors and uses thereof
The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also re...
08/19/2008
7390815Pyrazole compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compounds of formula II: wherein Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, and R2, R2′, R...
06/24/2008
7384944Piperazine derivatives useful as CCR5 antagonists
The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R
06/10/2008
7358253Indolylmaleimide derivatives
Provided are compounds of formula (I) which are useful in the treatment and/or prevention of diseases or disorders mediated by T lymphocytes and/or PKC, e.g. acute or chronic rejection of organ or tissue allo- or xenografts...
04/15/2008
RE40245Gyrase inhibitors and uses thereof
The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates ...
04/15/2008
7351828Benzimidazoles that are useful in treating sexual dysfunction
The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction. ...
04/01/2008
7342015Indole derivatives
A heteroaryl derivative having the formula (I). The compounds of the invention are considered useful for the treatment of affective disorders such as general anxiety disorder, panic disorder, obsessive compulsive disorder, depression, social phobia and eating disord...
03/11/2008
7300937Derivatives of cyano-aryl (or cyanoheteroaryl)-carbonyl-piperazinyl-pyrimidines, their preparation and application as medication
New derivatives of cyanoaryl (or cyanoheteroaryl)-carbonyl-piperazinyl-pyrimidines (I), where R1 represents an OR3 radical, where R3 represents a radical derived from a saturated hydrocarbon, with a linear or branched chain of 1 to 4...
11/27/2007
7291618Therapeutic compounds
The invention provides compounds of formula (I), prodrugs and stereoisomers thereof, and the pharmaceutically acceptable salts of the compounds, prodrugs, and stereoisomers, wherein R1, R2, ...
11/06/2007
7276502Thiazoles useful as inhibitors of protein kinases
The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, ...
10/02/2007
7230000Methods and compositions utilizing quinazolinones
Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity ...
06/12/2007
7210814Dental curing light with specially arranged LEDs
A dental curing light including an elongate wand having a proximal end and a distal end, a plurality of LEDs disposed at or near a distal end of the elongate wand and a printed circuit board for mounting the plurality of LEDs. The LEDs include a main through mount L...
05/01/2007
7179806Δ1-pyrrolines used as pesticides
The invention relates to novel Δ1-pyrrolines of the formula (I) in which R1, R2, R3, m, and Q have the meanings given in the disclosure, to a plurality of processes fo...
02/20/2007
7173034Respiratory syncytial virus replication inhibitors
This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of for CH═CH—, —N═CH—CH═CH—, —CH═N—CH═CH—, —CH═CH—N═CH—, —CH═CH—CH═N— wherein each ...
02/06/2007
7166723Process for the synthesis of derivatives of 2,3-dihydro-1,4-dioxino-[2,3-f] quinoline
Methods of preparing compounds of Formula I are provided. ...
01/23/2007
7157464Substituted piperazines
Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful ...
01/02/2007
7157462Therapeutic agents useful for treating pain
A compound of formula: wherein Ar, Ar1, Ar2, R3–R6, R13, m, and t are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Hydroxyiminopip...
01/02/2007
7151103Method of treating female hypoactive sexual desire disorder with flibanserin
The invention relates to the use of flibanserin, or a pharmaceutically acceptable acid addition salt thereof, for the treatment of disorders of sexual desire. ...
12/19/2006
7125875Cyclic protein tyrosine kinase inhibitors
Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders. ...
10/24/2006
7119086Phenylsulfonyl-1,3-dihydro-2h-indole-2-one derivatives, their preparation and their therapeutic use
The invention relates to compounds of formula: and also to the salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, with affinity for and selectivity towards the arginine-vasopress...
10/10/2006
7115597Tyrosine kinase inhibitors
The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogen...
10/03/2006
7098214Dopamine Dreceptor ligands or antagonists for use in the treatment of renal function disorders
Dopamine D3 receptor ligands or antagonists are disclosed for use in the treatment of renal function disorders, such as diabetic nephropathy. ...
08/29/2006
7094783Bicyclic pyrimidinones as coagulation cascade inhibitors
The present invention relates generally to compounds that inhibit serine proteases. In particular it is directed to novel amino-bicyclic pyrimidinone compounds of Formula (I): or a stereoisomer or pharmaceuticall...
08/22/2006
7057042Fused bicyclic aromatic compounds that are useful in treating sexual dysfunction
The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction, wherei...
06/06/2006
7045519Inhibitors of glycogen synthase kinase 3
New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may...
05/16/2006
7041305Stable water in oil aminophylline emulsions
A water in oil emulsion system and a process for preparing such a emulsion has been provided for topically applying aminophylline for reducing cellulite conditions. ...
05/09/2006
7038052Process for the synthesis of derivatives of 2, 3-dihydro-1, 4-dioxino- [2, 3-f] quinoline
Methods of preparing compounds of Formula I are provided. ...
05/02/2006
7022639Catalytic activity accelerant used in petroleum hydrogenation
The present invention provides a catalytic activity accelerant. The accelerant is added to stock oil for increasing the catalyst activity, the depth of catalytic hydrogenation and the yield of catalytic hydrogenation product, degrading the reaction conditions of cat...
04/04/2006
7019025Derivatives of amidines, their preparation and their use as medicaments
Compounds of the formula wherein R1 is alkyl and R2 is alkenyl, alkynyl, allenyl or cyanoalkyl, n is 0 or 1, k is an integer from 1 to 3, X is —(CH2)m— ...
03/28/2006
69951595-HT receptor ligands and uses thereof
Compounds of Formula (IC) that act as 5-HT receptor ligands and their uses in the treatment of diseases linked to the activation of 5-HT2 receptors in animals are described herein . ...
02/07/2006
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