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Class 514/85 - Hetero ring is six-membered consisting of two nitrogens and four carbons


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter in which the organo-phosphorus compound contains
No. of patents: 201
Last issue date: 11/15/2011


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NumberTitleIssue Date
8058263Substituted 2-phenyl-pyridine derivatives
The present invention relates to compounds of formula I wherein R1, R2, R4, R5, Ra, Rb, n, W and Z are as defined in the application, their preparation and t...
11/15/2011
7410956Caspase inhibitor prodrugs
The present invention relates to compounds of formula I which are prodrugs of caspase inhibitors and pharmaceutically acceptable salts thereof. This invention further relates to the release of caspase inhibitors from these compounds through selective bond cleavage. ...
08/12/2008
7402557Combined treatment with keratinocyte growth factor and epidermal growth factor inhibitor
The present invention relates to compositions and methods for treating the epithelial toxicity caused by administering to a human cancer patient an epidermal growth factor receptor (EGFR) inhibitor. The pharmaceutical composition preferably comprises an EGFR inhibit...
07/22/2008
7371760Medicinal compositions containing aspirin
A combination of 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine or a pharmaceutically acceptable salt thereof, and aspirin, which possess excellent inhibitory activity against platelet aggregation and thrombogenesis, and ...
05/13/2008
7358277Use of a lactate salt for the treatment and prophylaxis of atherosclerosis
The use of a lactate metal salt, in particular an L-lactate, for the treatment of atheroscloerosis and/or for the prophylaxis or treatment of diseases caused by atherosclerosis is disclosed. ...
04/15/2008
7259155Phosphonic diester derivatives
The present invention provides a phosphonic acid diester compound represented by General Formula wherein R1, R2, R3 and R4 are the same or different, and represent hydr...
08/21/2007
7253169Aza compounds, pharmaceutical compositions and methods of use
The present invention relates to N-substituted cyclic aza compounds, pharmaceutical compositions comprising such compounds, and methods of their use for effecting neuronal activities. ...
08/07/2007
7224532Optical uses diamondoid-containing materials
Novel optical devices based on diamondoid-containing materials are disclosed. Materials that may be fabricated from diamondoids included diamondoid nucleated CVD films, diamondoid-containing CVD films, molecular crystals, and polymerized materials. Devices that may ...
05/29/2007
7214701Active substance combinations having insecticidal and acaricdal properties
The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ...
05/08/2007
7205404Phosphorus-containing prodrugs
Novel cyclic phosphoramidate prodrugs of drugs of formula I in their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are described. ...
04/17/2007
7166619Prenylation inhibitors and methods of their synthesis and use
The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising same, and to methods for inhibiting protein prenylatio...
01/23/2007
7144884Phenyl-piperazine derivatives as serotonin reuptake inhibitors
The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disor...
12/05/2006
7122677NK1 antagonists
A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5...
10/17/2006
7115591Prostaglandin endoperoxide H synthase biosynthesis inhibitors
The present invention describes pyridazinone compounds of formula I which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2), COX-2 is the inducible isofo...
10/03/2006
7115664Peptidomimetic ligands for cellular receptors and ion channels
One aspect of the present invention relates to novel peptidomimetic compounds. A second aspect of the present invention relates to the use of the novel peptidomimetic compounds as ligands—agonists or antagonists—for various cellular receptors, e.g., G-protein-co...
10/03/2006
7112596Prenylation inhibitors and methods of their synthesis and use
The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising same, and to methods for inhibiting protein prenylatio...
09/26/2006
RE39264Pharmaceutical combination
The invention relates to pharmaceutical compositions for topical administration comprising a topically acceptable antiviral substance and an antiinflammatory glucocorticoid in a pharmaceutically acceptable carrier. The pharmaceutical composition can be used in the p...
09/05/2006
7078518Forms of 5-Azacytidine
The disclosure includes novel polymorphic and pseudopolymorphic crystalline forms of 5-azacytidine, along with methods for preparing said forms, wherein 5-azacytidine is represented by the formula: The disclosure...
07/18/2006
7067501Aryloxyphenyl and arylsulfanylphenyl derivatives
The invention provides compounds of the formula wherein the substituents are as defined in the application. The compounds are valuable glycine transport inhibitors. ...
06/27/2006
7053055Compounds of unstable DP IV-inhibitors
Novel compounds of unstable inhibitors of the serine peptidase dipeptidyl peptidase IV, are used in the treatment of various disorders, especially of metabolic disorders. The compounds can be used in the treatment of impaired glucose tolerance, glucosuria, hyperlipi...
05/30/2006
7038038Synthesis of 5-azacytidine
The present invention provides a method for the preparation of 5-azacytidine, wherein 5-azacytidine is represented by the structure: The method involves the silylation of 5-azacytosine, followed by the coupling of silylat...
05/02/2006
7030124Method of treating depression with delta receptor agonist compounds
Methods for treatment of depression or other affective mood disorders, such as bipolar manic depression or seasonal affective disorder, are disclosed by administration to a subject suffering or susceptible to same, of therapeutically effective diarylpiperazine compo...
04/18/2006
7001895Prostaglandin endoperoxide H synthase biosynthesis inhibitors
The present invention describes pyridazinone compounds of formula I which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2). COX-2 is the inducible isoform ass...
02/21/2006
6998391Method for treating diseases associated with abnormal kinase activity
Methods are provided for treating diseases associated with abnormal activity of kinases. The method comprises: administering a DNA methylation inhibitor to the patient in therapeutically effective amount; and administering a kinase inhibitor to the patient in therap...
02/14/2006
69952614-pyridazinecarboxamides and esters as interleukin-1β converting enzyme inhibitors
Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein R1 is a halogen, or an oxygen linked leaving group including an aromatic et...
02/07/2006
6977302Triazole derivatives useful in therapy
The invention provides compounds of formula I, R1—OP(O)(OH)2  I wherein R1 represents the non-hydroxy portion of a triazole antifungal compound of the type comprising a tertiary hydroxy group; or a pharmaceu...
12/20/2005
6960603Prenylation inhibitors and methods of their synthesis and use
The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising same, and to methods for inhibiting protein prenylatio...
11/01/2005
6949528Compositions containing lysophosphatidic acids which inhibit apoptosis and uses thereof
The invention provides anti-apoptotic compositions lysophosphatidic acids and methods for making and using the compositions. Such compositions can also contain LPA potentiating agents, including proteins, lipid membrane structures and polymers such as polyethylene g...
09/27/2005
6949529Compositions containing lysophosphotidic acids which inhibit apoptosis and uses thereof
The present invention provides therapeutic compositions containing lysophosphatidic acids, methods for making the compositions, and methods of use thereof. ...
09/27/2005
6943159Compounds and their use as positive AMPA receptor modulators
The invention provides novel compounds represented by general formula (I) wherein the bond represented by the broken line may be a single, double bond or absent; and if the bond is absent, then the nitrogen is substitu...
09/13/2005
6930097Matrix metalloproteinase and tumor necrosis factor inhibitors
A compound of formula 1-[3,4-dihydroxy-5-(2-hydroxyethyl)tetrahydrofuran-2-yl]pryimidine-2,4(1H,3H)-dione has inhibitory effects of matrix metalloproteinase-2 (gelatinase A) enzyme and binding of TNFα to TNFα-RI. ...
08/16/2005
6919323Pyridazinone inhibitors of fatty acid binding protein and method
aP2 inhibiting compounds are provided having the formula wherein A, X, R and Z are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employi...
07/19/2005
6919347Bradykinin B1 receptor antagonists
Bradykinin B1-receptor antagonists of formula are disclosed. The compounds are useful for treating diseases associated with inappropriate bradykinin receptor activity, such as diabetic vasculopathy, inflamma...
07/19/2005
6919322Phenyl Phosphonate Fructose-1,6-Bisphosphatase Inhibitors
Novel FBPase inhibitors of the formula I are useful in the treatment of diabetes and other conditions associated with elevated blood glucose. ...
07/19/2005
6916797α-arylethylpiperazine derivatives as neurokinin antagonists
The invention relates to new α-arylethylpiperazine of the formula wherein Z represents 0 or S; n′ represents 1 or 2; R2 represents a hy...
07/12/2005
6916816Phenanthryl piperazinyl dicarboxylic acids as selective NMDA receptor modulating agents
Disclosed are compounds of formula (I) wherein: L is (a) optionally substituted by replacement of one or more of the hydrogen atoms on the phenanthrene ring system by one or more groups other than hydrogen; A is CH2, SO2 or C═O; X is CO2...
07/12/2005
6914052Selective anti-viral nucleoside chain terminators
The present invention relates to dideoxynucleoside analog compounds containing a dideoxy ribofuranosyl moiety that exhibit selective anti-viral activity coupled with substantially low toxicity toward the host cells. In particular, the compounds according to the pres...
07/05/2005
6864276Active substance combinations having insecticidal and acaricidal properties
The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I)  in which W, X, Y, Z, A, B, D and G ...
03/08/2005
6833364Substituted pyrazole derivatives
The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which the substituents R1, R2, R3, A, X and Y are each as defined, and to processes...
12/21/2004
6756391Antiviral compounds
The present invention is drawn to novel antiviral compounds, pharmaceutical compositions and their use. More specifically this invention is drawn to derivatives of monocyclic polyamines which have activity in standard tests against HIV-infected cells as well as othe...
06/29/2004
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