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Class 514/264.11 - Nitrogen bonded directly to ring carbon of the 1,3-diazine ring of the bicyclo ring system


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein a ring carbon of the 1,3-diazine
No. of patents: 126
Last issue date: 01/24/2012


1        
NumberTitleIssue Date
8101622Pyridopyrimidinone inhibitors of PI3Kα and mTOR
The invention is directed to Compounds of Formula I: optionally as a single stereoisomer or mixture of stereoisomers thereof, and additionally optionally as a pharmaceutically acceptable salt thereof; as well as methods of ...
01/24/2012
80763452-cyanophenyl-7,8-dihydro-5H-pyrido[4,3-d]pyrimidine compounds, compositions and uses thereof
Fused heterocyclic compounds are provided according to formula 1: where R1, R2, R3, and m are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the...
12/13/2011
80582837H-pyrido[3,4-D]pyrimidin-8-ones, their manufacture and use as protein kinase inhibitors
Objects of the present invention are the compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing the...
11/15/2011
8044062Substituted pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors of phospatidylinositol 3-kinase alpha
The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds. ...
10/25/2011
8030318Fused bicyclic inhibitors of HCV
Substituted fused bicyclic pyrimidine compounds having an amide-substituted pyridylamine group at C-4 of the pyrimidine ring are useful in the treatment of conditions associated with HCV. ...
10/04/2011
8008310Derivatives of pyrido[2,3-d]pyrimidine, the preparation thereof, and the therapeutic application of the same
Derivatives of pyrido[2,3-d]pyrimidine are provided having formula (I) with Ar1, Ar2 and R1 as defined herein, which are useful for treating cell proliferative conditions, and to the prepara...
08/30/2011
7923450Modulators for amyloid beta
The invention relates to compounds of formula wherein R1, R2, R3, R4, X and Y are as defined herein and to pharmaceutically active acid addition salts thereof. The compounds can b...
04/12/2011
7910595Anti-viral compounds
Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or t...
03/22/2011
7879866Inhibition of the activity of the capsaicin receptor in the treatment of obesity or obesity-related diseases and disorders
The present invention provides a method of treating diseases or disorders benefiting from inactivating or down regulating the activity of the capsaicin receptor in a mammal by inhibiting the activity of the capsaicin receptor. The present invention also provi...
02/01/2011
7842698Pyridine methylene azolidinones and use thereof phosphoinositide inhibitors
The present invention relates to pyridine methylene azolidinone compounds of Formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative ...
11/30/2010
7750016Hydroxyalkyl substituted pyrido-7-pyrimidin-7-ones
Compounds of the Formula: where X1, Ar1, R1, and R2 are as defined herein, and compositions comprising the same. Also provided are methods for using compounds of Formula I in trea...
07/06/2010
7745451Tetrahydronaphthyridine and tetrahydropyrido[4,3-d]pyrimidine compounds and compositions thereof useful in the treatment of conditions associated with neurological and inflammatory disorders and dysfunctions
Fused heterocyclic compounds are disclosed that have formula 1: where A, B, L, N, R1, R3, R4′, Y and Z are as defined herein. The compounds and pharmaceutical compositions thereof are usef...
06/29/2010
76962134-methylpyridopyrimidinone compounds
The present invention is directed to novel 4-methylpyridopyrimidinone compounds of Formula (I), and to salts thereof, their synthesis, and their use as inhibitors of phosphoinositide 3-kinase alpha (PI3-Kα). ...
04/13/2010
7662828Substituted 5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine-2-yl compounds and 5,6,7,8-tetrahydroquinazoline-2-yl compounds
Substituted 5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-2-yl and 5,6,7,8-tetrahydro-quinazolin-2-yl compounds, corresponding to formula I processes for the production thereof, pharmaceutical preparations containing these comp...
02/16/2010
7645764Kinase inhibitors and methods for using the same
Compounds of formula I: wherein R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds, pharmaceutical compositions, methods of using the comp...
01/12/2010
7582643Heterocyclic compounds useful in treating diseases and conditions
The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are as defined herein, compositions containing such compounds and the uses of su...
09/01/2009
75315452-amino-3,4-dihydro-pyrido[3,4-d]pyrimidine derivatives useful as inhibitors of β-secretase (BACE)
The present invention is directed to novel 2-amino-3,4-dihydro-pyrido[3,4-d]pyrimidine derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhib...
05/12/2009
7524852Bicyclic pyrimidine derivatives
[wherein m and n may be the same or different and each represents an integer of 1 to 3 wherein m+n is 4 or less; R1 represents —NR4R5 (wherein R4 and R5 may be the same or d...
04/28/2009
7504406Derivatives of pyrido[2,3-d]pyrimidine, the preparation thereof, and the therapeutic application of the same
The invention relates to derivatives of pyrido[2,3-d]pyrimidine, to the preparation thereof, and to the therapeutic application of the same. ...
03/17/2009
7442710Substituted 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
7423042Compounds
This invention relates to a novel group of 8-Alkyl/Aryl-4-aryl-2-N-(alkylamino)-N″-substituted-N′-cyanoguanidino-8H-pyrido[2,3-d]pyrimidin-7-one compounds, processes for the preparation thereof, the use thereof in treating CSBP/p38 kinase mediated diseases and p...
09/09/2008
7361662Pyridopyrimidinone compounds, method for production thereof and medicaments comprising the same
A compound of formula (I): wherein: R1, R2, R3, R4 are defined in the description, its enantiomers, diastereoisomers, tautomers and also addition salts thereof with a phar...
04/22/2008
7348331Hydroxyalkyl substituted pyrido-7-pyrimidin-7-ones
Compounds of the Formula: where X1, Ar1, R1, and R2 are as defined herein, and compositions comprising the same. Also provided are methods for using compounds of Formula I in trea...
03/25/2008
7334538Topical medicants for aquatic animals
A topical medicant for fishes, amphibians, reptiles, and aquatic macroinvertebrates applied in a site-specific manner for the localized treatment of skin wounds, lesions and diseases. The medicant comprises a hydrophilic carrier with an antimicrobial therapeutant fo...
02/26/2008
7329664Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues
Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with ...
02/12/2008
73234722,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds
The present invention is directed to the novel use of a CSBP/p38 inhibitor for the treatment, including prophylaxis of inflammation enhanced cough in a mammal in need thereof. ...
01/29/2008
73209876-Alkoxy-pyrido-pyrimidines
The present invention provides compounds of the Formula I: wherein R1 is alkyl, cycloalkyl, cycloalkylalkyl, or —CH2-alkenyl, X1 is O, NH, N(alkyl), S or —C(═O), Z is N or C...
01/22/2008
73148812,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds
Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. ...
01/01/2008
7312330Bicycloheteroarylamine compounds as ion channel ligands and uses thereof
Amine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of condi...
12/25/2007
7279484Heterocyclic compounds
The inventive subject matter relates to compounds, pharmaceutical compositions, and kits containing a heterocyclic compound represented by the formula (I) wherein R is an alkyl group optionally having substituent...
10/09/2007
7253284Chemical compounds
Compounds of the formula I, Wherein X is N, n is 1 and R2and R3 together form a ring, R, R1 and R4 are as defined in the specifications. ...
08/07/2007
72355511,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
Novel substituted pyrimidol[4,5-d]pyrimidin-2-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. ...
06/26/2007
72084892-(pyridin-2-ylamino)-pyrido [2,3-d]pyrimidin-7-ones
The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders. The novel compounds of the present invention are potent inhibitors of cyclin-dependent kinases 4 (cdk4) ...
04/24/2007
7202249Antagonists of chemokine receptors
Compounds are provided which are antagonists of chemokine receptor activity. The compounds thereof have the structure including enantiomers, diastereomers, tautomers, pharmaceutically acceptable salts and ...
04/10/2007
71960976-alkoxy-pyrido-pyrimidines
The present invention provides compounds of the Formula I: wherein R1 is alkyl, cycloalkyl, cycloallkylalkyl, or —CH2-alkenyl, X1 is O, NH, N(alkyl), S or —C(═O), Z is N or ...
03/27/2007
7189732Pyrido[2,3-d]pyrimidine dichloro-phenyl derivatives
The invention describes compounds of the general formula I a process for their manufacture, compositions containing them and their manufacture as well as the use of these compounds as pharmaceutically active agen...
03/13/2007
7189731Substituted 7-azaquinazoline compounds useful as p38 kinase inhibitors
Compounds having the formula (I) or (II), are useful as p38 kinase inhibitors, wherein R is an optionally substituted alkyl, cycloalkyl, or aryl; R6 is hydrogen or lower alkyl; R7 is hydroge...
03/13/2007
71731363-Cyano-quinoline derivatives
The invention concerns quinoline derivatives of Formula (I) wherein each of Z1, m, R1, n, R3, Z2 and R14 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmac...
02/06/2007
7163941Pyrido[2,3-d]pyrimidin-7-carboxylic acid derivatives, their manufacture and use as pharmaceutical agents
The invention describes compounds of the general formula I a process for their manufacture, medicaments containing them and their manufacture as well as the use of these compounds as pharmaceutically active agent...
01/16/2007
7157466Quinazoline ditosylate salt compounds
Ditosylate salts of 4-quinazolineamines are described as well as methods of using the same in the treatment of disorde4rs characterized by aberrant erbB family PTK activity. ...
01/02/2007
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