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Class 544/256 - Four ring nitrogens in the bicyclo ring system


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the bicyclo ring system contains four
No. of patents: 194
Last issue date: 01/10/2012


1          
NumberTitleIssue Date
8093383P70 S6 kinase inhibitors
The present invention provides p70 S6 kinase inhibitors of the formula: pharmaceutical formulations comprising them, and methods for their use. ...
01/10/2012
7923555Fused bicyclic mTor inhibitors
Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer. ...
04/12/2011
7897762Kinase inhibitors useful for the treatment of proliferative diseases
The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of sy...
03/01/2011
7632947Pyrimidopyrimidine derivatives, organic thin film transistors using pyrimidopyrimidine derivatives and method for fabricating the same
Pyrimidopyrimidine derivatives, organic thin film transistors using pyrimidopyrimidine derivatives and method for fabricating the same are provided. Pyrimidopyrimidine derivative structures, along with example syntheses, are provided. The pyrimidopyrimidine derivati...
12/15/2009
7432281Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
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 conditions in mammals ...
10/07/2008
7432273Phosphonate analogs of antimetabolites
The invention is related to phosphorus substituted antimetabolites, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds. ...
10/07/2008
7419981Synergistic combinations of an alpha-2-delta ligand and a cGMP phosphodieterse 5 inhibitor
The instant invention relates to a combination of an alpha-2-delta ligand and a PDEV inhibitor for use in therapy, particularly in the treatment of pain, particularly neuropathic pain. Particularly preferred alpha-2-delta ligands are gabapentin and pregabalin. A par...
09/02/2008
7414053Dihydropteridione derivatives, process for their manufacture and their use as medicament
Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes f...
08/19/2008
7378409Substituted cycloalkylamine derivatives as modulators of chemokine receptor activity
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.
05/27/2008
7378423Pyrimidine compound and medical use thereof
The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I] wherein each symbol is as defined in the specification and a method of therapeuti...
05/27/2008
7371766Curcumin analogs with anti-tumor and anti-angiogenic properties
The present invention is directed to curcumin analogs exhibiting anti-tumor and anti-angiogenic properties, pharmaceutical formulations including such compounds and methods of using such compounds. ...
05/13/2008
7371750Compounds and compositions as protein kinase inhibitors
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or d...
05/13/2008
7365074Pyridazine, pyrimidine and pyrazine ethyne compounds
In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted, unsaturated five, six or seven membered heterocyclic ring that includes at least one nitrogen atom and at least one...
04/29/2008
7351827Substituted oxetanes, method of making, and method of use thereof
Oxetane-containing nucleosides, particularly non-reducing psiconucleoside oxetanes are described herein. Therapeutic application of these oxetane compounds toward the treatment of nucleoside analog related disorders such as disorders involving cellular proliferation...
04/01/2008
7351826Aryl acid pyrimidinyl methyl amides, pyridazinyl methyl amides and related compounds
The invention provides compounds of Formula (I) that bind to GABAA receptors. In the above formula, variables are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly...
04/01/2008
7345048Heterocyclic compounds and uses thereof as D-alanyl-D-alanine ligase inhibitors
The invention relates to D-Ala-D-Ala ligase inhibitors having the formula: wherein R1 is NH2; R2 is NH2; R3 is selected from hydrogen, alkyl, amino, hydroxy, alkoxy, an...
03/18/2008
7345174Cytodifferentiating agents and histone deacetylase inhibitors, and methods of use thereof
The present invention provides the compound having the formula: wherein each of R1 and R2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-buty...
03/18/2008
7332504Heterocyclic substituted aminoazacycles useful as central nervous system agents
Heterocyclic substituted aminoazacyclic compounds of formula I Z-R3I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions ...
02/19/2008
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
73149344-amino substituted-6-aryl/heteroaryl substituted-2-methylsulfanyl-pyrimidine-5-carbaldehyde intermediates
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
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
7265129Anti-infective biaryl compounds
Compounds represented by the formula (I), where R1, R2, R3, R4, R5, and Q are as defined herein, exhibit activity against infectious pathogens ...
09/04/2007
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
7223760Substituted triazole compounds
Novel substituted triazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. ...
05/29/2007
7223759Antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compounds
The invention relates to antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compounds and pharmaceutical compositions thereof. This invention also relates to a method of using such compounds in the treatment of bacterial infections in mammal...
05/29/2007
7208493Vasculostatic agents and methods of use thereof
Compositions and methods and are provided for treating disorders associated with compromised vasculostasis. Invention methods and compositions are useful for treating a variety of disorders including for example, stroke, myocardial infarction, cancer, ischemia/reper...
04/24/2007
7196090Kinase inhibitors
This invention provides phenyl-substituted pyrimidopyrimidines, dihydropyrimido-pyrimidines, pyridopyrimidines, naphthyridines, and pyridopyrazines of the general formula: that inhibit cyclin-dependent kinase and...
03/27/2007
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
7193080Dye-forming coupler, silver halide photographic light-sensitive material and azomethine dye compound
A dye-forming coupler and compound of formula (I): wherein Q represents a residue that forms, together with —N—C═N—, a nitrogen-containing 6-membered ring; RA represents an aryl, heterocyclic, ...
03/20/2007
7183273Chemokine receptor binding heterocyclic compounds
Heterocyclic compounds that bind chemokine receptors and inhibit the binding of their natural ligands are disclosed. The invention compounds are protective against infection by HIV and exert effects characteristic of antagonists to the CXCR4 receptor. ...
02/27/2007
7148349Cyclic phosphate diesters of 1,3-propane-1-aryl diols and their use in preparing prodrugs
Compounds of Formula I, their preparation and synthetic intermediates, and their use in the synthesis of prodrugs: wherein: V and L are trans relative to one another; ...
12/12/2006
7141669Cannabiniod receptor ligands and uses thereof
Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein ...
11/28/2006
7132418Peptidyl heterocyclic ketones useful as tryptase inhibitors
The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment of a variety of immunomediated inflammatory disorders. More particul...
11/07/2006
7129351Pyrimido compounds having antiproliferative activity
Disclosed are novel pyrimido compounds that are inhibitors of Src family of tyrosine kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, h...
10/31/2006
7115739Triazole compounds useful as protein kinase inhibitors
This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2
10/03/2006
7115740Pyrimido compounds having antiproliferative activity
Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR and FGFR kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, col...
10/03/2006
7112676Pyrimido compounds having antiproliferative activity
Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR and FGFR kinases and are selective against LCK. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tum...
09/26/2006
7091345Amino-substituted dihydropyrimido[4,5-D]pyrimidinone derivatives
Compounds of formula I are described. These compounds are protein kinase inhibitors, in particular they inhibit the src family tyrosine kinases. Thus, these compounds are useful for the treatment of diseases medi...
08/15/2006
7084270Pyrimido compounds having antiproliferative activity
Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR an FGFR kinases and are selective against LCK. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumo...
08/01/2006
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