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Class 514/263.21 - The additional hetero ring is a 1,3-diazine ring (including hydrogenated)


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein a 1,3-diazine ring is the additional
No. of patents: 81
Last issue date: 05/15/2012


1      
NumberTitleIssue Date
81785418-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts ther...
05/15/2012
81196488-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts ther...
02/21/2012
7879865Treatment of cancer of the brain using histone deacetylase inhibitors
The present application is directed to a method of treating diseases of the central nervous system (CNS) comprising administering to a individual in need of treatment a therapeutically effective amount of an inhibitor of histone deacetylase. In particular embodiment...
02/01/2011
76457638-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical composition
The present invention relates to substituted xanthines of general formula wherein R1 and R2 are defined as in the claims, the tautomers, the stereoisomers, the mixtures thereof, and the salts thereof, ...
01/12/2010
75014268-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions
Disclosed are substituted xanthines of the formula wherein R is defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, par...
03/10/2009
7495004Purine derivatives as liver X receptor agonists
The invention relates to methods for the treatment or prevention of an LXR mediated disease or condition, including cardiovascular disease and atherosclerosis, novel compounds of formula (I) for use in such methods and pharmaceutical compositions comprising compound...
02/24/2009
7423041A1 adenosine receptor antagonists
Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described. ...
09/09/2008
74079558-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to substituted xanthines of general formula wherein R1 to R3 are defined as in claims 1 to 16, the tautomers, the stereoisomers, the mixtures, the prodrugs t...
08/05/2008
7358235Analogs of nitrobenzylthioinosine
Analogs or derivatives of nitrobenzylthioinosine compounds. The use of these new analogs of nitrobenzylthioinosine and methods for the treatment of pain and various other indications using these analogs of nitrobenzylthioinosine as well as pharmaceutical composition...
04/15/2008
7342006Substituted 8-heteroaryl xanthines
Selective antagonists of A2B adenosine receptors like those of formula I are provide. The compounds and compositions are useful as pharmaceutical agents. ...
03/11/2008
7335654Phosphodiesterase 4 inhibitors
PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein. ...
02/26/2008
73356558-heteroaryl xanthine adenosine Areceptor antagonists
The present invention relates generally to compounds of formula (I): wherein X is a five or six-membered heteroaromatic ring, containing one to four heteroatoms, selected from nitrogen, ox...
02/26/2008
7291623Compounds that interact with kinases
A method of inhibiting or effecting the activity of protein kinase activity which comprises contacting a protein kinase with a compound of formula (I) being a derivative of a furanose or pyranose form of a monosaccharide, or a pharmaceutically acceptable salt thereo...
11/06/2007
7268141Xanthine phosphodiesterase V inhibitors
A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders:
09/11/2007
7259159Guanidino derivatives as inhibitors of cell adhesion
The present invention relates to acylguanidino derivatives of formula (I), in which R1, R2, R3, A, B, X, Y and n have the meanings indicated in claim 1, their physiologically tolerable salts and their prodrugs. The compounds o...
08/21/2007
7241890Purine analogs having HSP90-inhibiting activity
Novel purine compounds of Formula I. and tautomers, pharmaceutically acceptable salts, and prodrugs thereof, wherein X is S, S(O), or S(O)2; and O is selected from alkyl, cycloalkyl, arylalkyl, aryl, h...
07/10/2007
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
7217702Selective antagonists of A2A adenosine receptors
Selective antagonists of A2A adenosine receptors like those of formula I are provided, wherein Y forms a ring. The novel A2A blockers are useful for the treatment of Parkinsons disease and o...
05/15/2007
7202252Aadenosine receptor antagonists
Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described. ...
04/10/2007
7157465Adenine derivatives
This invention relates to an adenine derivative, a tautomer thereof, or a pharmaceutically acceptable salt thereof represented by general formula (I): wherein X represents NR3 (wherein R3 re...
01/02/2007
7148229Sulfonamide substituted xanthine derivatives
The present invention is a sulfonamide substituted xanthine derivative of formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is lower alkyl, lower alkyl substituted by phenyl, or lower alkyl sub...
12/12/2006
7135191Urogenital or anorectal transmucosal vaccine delivery system
The invention is directed to a suppository based vaccine delivery system for immunizing against urogenital and anorectally transmitted infectious disease in humans and animals and a method for treating the same. More particularly, this invention is directed to a sup...
11/14/2006
7135475Amide substituted xanthine derivatives
The present invention is a 1,3,8 substituted xanthine derivative of formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined in the specificat...
11/14/2006
7053096Compounds having selective hydrolytic potentials
Disclosed are compounds having selective hydrolytic potential. The disclosed compounds are useful as compounds having selective stability and are capable of undergoing programmed hydrolysis in biologic systems. ...
05/30/2006
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
6969720Biaryl substituted purine derivatives as potent antiproliferative agents
The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of the present ...
11/29/2005
6949559Nitrogen substituted biaryl purine derivatives as potent antiproliferative agents
The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of the present ...
09/27/2005
6890926Heteroaryl derivatives and their use as medicaments
The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors. ...
05/10/2005
6812232Heterocycle substituted purine derivatives as potent antiproliferative agents
The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of the present ...
11/02/2004
6780865Compounds having selective hydrolytic potentials
Disclosed are compounds having selective hydrolytic potential. The disclosed compounds are useful as compounds having selective stability and are capable of undergoing programmed hydrolysis in biologic systems. The disclosed compounds have a structure of formula I: ...
08/24/2004
67679062-amino-6-anilino-purines and their use as medicaments
This application discloses 2-amino-6-anilino-purine derivatives of the formula I in which q is 1-5, and R1 is α) —S(═O)k—NR6R7, in which  k...
07/27/2004
6747016Substituted purine derivatives as inhibitors of cell adhesion
The present invention relates to compounds of formula (I), in which B, D, E, G, X, Y, Z, R1, R2 and s have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (I) are valuable...
06/08/2004
6723727Substituted purine derivatives, processes for their preparation, their use, and compositions comprising them
The present invention relates to compounds of the formulae I and Ia in which X, Y, W, Wa, G and Ga have the meanings given in the patent claims, and their physiologically tolerable salts and their p...
04/20/2004
6667311Nitrogen substituted biaryl purine derivatives as potent antiproliferative agents
The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of t...
12/23/2003
6645969Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase
This invention relates to the modulation and/or inhibition of cell signaling, cell proliferation, cell inflammatory response, the control of abnormal cell growth and cell reproduction. More specifically, this invention relates to the use of mono- and/or b...
11/11/2003
66422316,9-disubstituted 2-[trans-(4-aminocyclohexyl)amino] purines
The present invention comprises 6-9-Disubstituted 2-[trans-(4-aminocyclohexyl]aminopurines that are useful in inhibiting cyclin dependent kinases, particularly cdk-2. The present invention also provides a method of preventing apoptosis in neuronal cells a...
11/04/2003
66276336-substituted biaryl purine derivatives as potent cyclin/CDK inhibitors and antiproliferative agents
The compounds of the present invention are 2,6,9-trisubstituted purine inhibitors of cyclin/cdk complexes. The compounds also are potent inhibitors of human cellular proliferation. As such, the compounds constitute pharmaceutical compositions with a pharm...
09/30/2003
6613773Fungicides
The invention provides fungicidal compounds of formula (I) or stereoisomers thereof: ##STR1## wherein X is CH2 O; A is hydrogen; E is hydrogen; q is 1; any two of K, L and M are nitrogen and the other is CH; T is oxygen or sulfur; and Z is an o...
09/02/2003
6613772Substituted 2-aryl-4-amino-chinazolines, method for the production and use thereof as medicaments
Compounds of the formula I ##STR1## in which R1, R2, R3 and Ar have the meanings indicated in the claims, are suitable for the production of pharmaceuticals, for example for the prophylaxis and therapy of cardiovascular di...
09/02/2003
6506762Certain alkylene diamine-substituted heterocycles
The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor. The present invention provides novel, potent, non-peptidic antagonists of N...
01/14/2003
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