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Class 514/252.18 - Additional six-membered hetero ring consisting of five ring carbons and one ring nitrogen attached directly or indirectly to the 1,3-diazine 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: 263
Last issue date: 03/16/2010


1              
NumberTitleIssue Date
7678798Piperazinylpiperidine derivatives as chemokine receptor antagonists
The present invention relates to compounds of Formula I: wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds of the...
03/16/2010
7557105N-oxides of N-phenyl-2-pyrimidine-amine derivatives
The invention relates to N-phenyl-2-pyrimidine-amine derivatives in which at least one nitrogen atom carries an oxygen atom to form the corresponding N-oxides, to processes for the preparation thereof, to pharmaceutical compositions comprising those compounds, and t...
07/07/2009
7521452Preparation of pharmaceutical salts of piperazine compounds
The present invention is generally directed to a process to directly prepare pharmaceutically acceptable salts enriched with respect to selected rotameric salts of a basic compound, by creative choice of an acid and a solvent medium. The process is particularly usef...
04/21/2009
7470691Fused 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, wherein A, L, D a...
12/30/2008
7365069Pyrimidone derivatives
The present invention relates to novel pyrimidones of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutical...
04/29/2008
7361691Method of treating cancers using β-lapachone or analogs or derivatives thereof
Cancers and/or malignancies can be treated by administration of a cell cycle checkpoint activator, which is preferably β-lapachone, or a derivative or analog thereof, combined with an oncogenic kinase modulator, preferably imatinib. This combination of the cell cyc...
04/22/2008
7354924Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
This invention provides Compounds I having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral acti...
04/08/2008
7345046Heteroaryl-fused pyrimidinyl compounds as anticancer agents
Heteroaryl-fused pyrimidinyl compounds, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the heteroaryl-fused pyrimidinyl compounds, either alone or in combination with at lea...
03/18/2008
7335663Heteroaryl compounds which inhibit leukocyte adhesion mediated by αintegrins
Disclosed are compounds which bind α4 integrins, where the α4 integrin is preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by α4 integrins, where the α
02/26/2008
73296712,4-pyrimidinediamine compounds and their uses
The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a...
02/12/2008
7329661N-phenyl-3-pyrimidine-amine derivatives
The invention relates to N-phenyl-2-pyrimidine-amine derivatives of formula I wherein the substituents are defined as indicated in the description, to processes for the preparation thereof, to medicaments compris...
02/12/2008
73296722,4-pyrimidinediamine compounds and their uses
The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a...
02/12/2008
73266994-Amino-5-phenyl-7-cyclobutyl-pyrrolo(2,3-d)pyrimidine derivatives
The invention relates to new 4-amino-5-phenyl-7-cyclobutyl-pyrrolo[2,3-d]pyrimidine derivatives, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof-alone or in combination with o...
02/05/2008
7312216N-phenyl-2-pyrimidine-amine derivatives
The invention relates to N-phenyl-2-pyrimidine-amine derivatives of formula I wherein the substituents are defined as indicated in the description, to processes for the preparation thereof, to medicaments compris...
12/25/2007
7307081Piperidine derivatives useful as CCR5 antagonists
The present invention provides a compound of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein the various moieties are as defined in the specification. The present invention also provides pharma...
12/11/2007
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
7300938Polymorphs of imatinib mesylate
The present invention relates to novel polymorphs of imatinib mesylate, to processes for their preparation and to pharmaceutical compositions containing them. ...
11/27/2007
7297694Pyridylfurans and pyrroles as Raf kinase inhibitors
Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. ...
11/20/2007
7285545Cytokine inhibitors
Disclosed are compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as...
10/23/2007
7244748Pyridines for treating injured mammalian nerve tissue
The invention provides novel pyridines, pharmaceutical compositions comprising such pyridines, and the use of such compositions in treating injured mammalian nerve tissue, including but not limited to an injured spinal cord. In one embodiment, the compounds, composi...
07/17/2007
7238525Strategy for leukemia therapy
The chimeric Bcr-Abl oncoprotein is the molecular hallmark of chronic myelogenous leukemia (CML). In the cytoplasm, the protein transduces a growth signal that is responsible for overexpansion of cells. In the nucleus, the protein induces apoptosis. The invention is...
07/03/2007
7235538Heterocyclic compounds, which are inhibitors of the enzyme DPP-IV
The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV, which are of formula I wherein each n is one or two independently and R1, R2, R3
06/26/2007
7232825Phenylaminopyrimidine derivatives and methods of use
The present invention relates to phenylaminopyrimidine derivatives, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states such as cancers associated with tyrosine kinases, espec...
06/19/2007
7196080Phenylpyridinecarbonylpiperazinederivative
The present invention relates to a compound which is represented by the following general formula and has type 4 phosphodiesterase inhibitory action, and uses and an intermediate compound thereof. (wherein ...
03/27/2007
7186723Tyrosine 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...
03/06/2007
7173025Aminoheterocyclic derivatives as antithrombotic or anticoagulant agents
Compounds of formula (I), wherein G1 is CH or N; G2 is CH or N; R1 is a variety of optional substituents; L1 is (1-4C)alkylene; T1 is CH or N; R2 and R3 are independently hydrogen or (1-4C)...
02/06/2007
7166597Fused pyrazole derivatives being protein kinase inhibitors
Compounds of Formula (I): salts or solvates or physiologically functional derivatives thereof, wherein Z is CH or N, and R1, R2, and R4 are various substituent groups, are protein kinase inhibitors
01/23/2007
7163940Pyrazolopyridinyl pyrimidine therapeutic compounds
The present invention provides compounds of formula (I): wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceuti...
01/16/2007
71574554-Aminopyrimidine-5-one derivatives
Novel 4-aminopyrimidine-5-one derivatives are disclosed. These compounds inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are ...
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
7153855Pyrazolopyridinyl pyrimidine therapeutic compounds
The present invention provides compounds of formula (I): pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents. ...
12/26/2006
71449143,7-diazabicyclo[3.3.0]octanes and their use in the treatment of cardiac arrhythmias
There is provided compounds of formula (I) wherein R1 to R4, Ra to Rf, A and B have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventr...
12/05/2006
7141569Antiviral pyrazolopyridine compounds
The present invention provides compounds of formula (I): pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents. ...
11/28/2006
7135477Heterocyclic compounds which inhibit leukocyte adhesion mediated by αintegrins
Disclosed are compounds which bind α4 integrins, preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by α4 integrins, preferably VLA-4. Such compounds are useful in the ...
11/14/2006
7122544Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto
Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 and R6
10/17/2006
7119203Piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors
This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metallop...
10/10/2006
7109197N-phenyl-4-(4-pyridyl)-2-pyrimidineamine derivatives
The present invention relates to a method of protecting plants against attack or infestation by phytopathogenic organisms, such as nematodes or especially microorganisms, preferably fungi, bacteria and viruses, or combinations of two or more of these organisms, by a...
09/19/2006
7098213CCR5 antagonists useful for treating AIDS
Compounds of the formula or a pharmaceutically acceptable salt or isomer thereof, wherein: Q, X and Z are CH or N; R, R4–R7 and R13...
08/29/2006
7094784High affinity ligands for nociceptin receptor ORL-1
Novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1
08/22/2006
7094785Method of treating polycythemia vera
The invention is directed to the use of imatinib mesylate for treating polycythemia vera. Imatinib mesylate is surprisingly effective at controlling the symptoms of polycythemia vera and reducing the need for phlebotomy. ...
08/22/2006
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