459448-04-5

Upstream product

• 68-12-2 N,N-dimethyl-formamide 
• 459448-06-7 6-bromo-3-isopropyl-[1,2,4]triazolo[4,3-a]pyridine 
• 1068-55-9 isopropylmagnesium chloride 

Downstream Products

• 459448-03-4 6-[5-(4-Fluoro-phenyl)-3H-imidazol-4-yl]-3-isopropyl-[1,2,4]triazolo[4,3-a]pyridine 
• 876372-14-4 6-[(Z)-2-(2,4-difluorophenyl)vinyl]-3-isopropyl[1,2,4]triazolo[4,3-a]pyridine 
• 745828-06-2 (4-fluoro-phenyl)-(3-isopropyl-[1,2,4]triazolo[4,3-a]pyridin-6yl)-methanol 
• 908837-16-1 3-(2,5-difluoro-phenyl)-2-(3-isopropyl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)-3-oxo-propionaldehyde 
• 908837-12-7 1-(2,5-difluoro-phenyl)-2-(3-isopropyl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)-ethanone 

Relevant academic research and scientific papers

NOVEL TRIAZOLOPYRIDINE COMPOUNDS

This invention is directed generally to triazolopyridine compounds that generally inhibit p38 kinase, TNF, and/or cyclooxygenase activity. Such triazolopyridine include compounds generally corresponding in structure to the following formula (I): wherein R

NOVEL TRIAZOLOPYRIDINE COMPOUNDS FOR THE TREATMENT OF INFLAMMATION

This invention is directed generally to triazolopyridine compounds that generally inhibit p38 kinase, TNF, and/or cyclooxygenase activity. Such triazolopyridine include compounds generally corresponding in structure to the following formula (I): Wherein R1, R2, R3, R4, and R5are as defined in this specification. This invention also is directed to compositions of such triazolopyridines (particularly pharmaceutical compositions), intermediates for the syntheses of such triazolopyridines, methods for making such triazolopyridines, and methods for treating (including preventing) conditions (typically pathological conditions) associated with p38 kinase activity, TNF activity, and/or cyclooxygenase-2 activity.

Theoretical and experimental design of atypical kinase inhibitors: Application to p38 MAP kinase

Mimics of the benzimidazolone nucleus found in inhibitors of p38 kinase are proposed, and their theoretical potential as bioisosteres is described. A set of calculated descriptors relevant to the anticipated binding interaction for the fragments 1-methyl-

Novel crystalline forms of 3-isopropyl-6-[4-(2,5-difluoro-phenyl)-oxazol-5-yl]-[1,2,4]triazolo-[4,3-A]pyridine

The present invention relates to novel crystalline forms of 3-isopropyl-6-[4-(2,5-difluoro-phenyl)-oxazol-5-yl]-[1,2,4]triazolo-[4,3-a]pyridine to pharmaceutical compositions containing such crystal forms and to methods of treatment. 3-Isopropyl-6-[4-(2,5-difluoro-phenyl)-oxazol-5-yl]-[1,2,4]triazolo-[4,3-a]pyridine is a potent inhibitor of MAP kinases, preferably p38 kinase (MAPK14/CSBP/RK kinase). 3-Isopropyl-6-[4-(2,5-difluoro-phenyl)-oxazol-5-yl]-[1,2,4]triazolo-[4,3-a]pyridine is useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

DI AND TRIFLUORO-TRIAZOLO-PYRIDINES ANTI-INFLAMMATORY COMPOUNDS

The present invention relates to novel triazolo-pyridines of the formula (I) wherein R1 is fluoro; s is an integer from two to three; R2 is (C3-C6)cycloalkyl optionally substituted by one or two moieties independently selected from the group consisting of halo, (Cl-C4)alkyl, hydroxy, (Cl-C6)alkoxy and (C1-C6)alkyl-(C=O)-0-; or R2 is (Cl-C6)alkyl optionally substituted by one or two moieties independently selected from the group consisting of halo, (C1-C6)alkyl, hydroxy, (C1-C6)alkoxy and (C1-C6)alkyl-(C=O)-0-; with the proviso that said compound of formula (I) cannot be 6-[4-(2,4-Difluoro-phenyl)-oxazol-5-yl]-3-isopropyl-[1,2,4]triazolo[4,3-a]pyridine; or 6-[4-(3,4-Difluoro-phenyl)-oxazol-5-yl]-3-isopropyl-[1,2,4]triazolo[4,3-a]pyridine; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

NOVEL PROCESSES AND INTERMEDIATES FOR PREPARING TRIAZOLO-PYRIDINES

The present invention relates and intermediates to a novel process for preparing triazolo-pyridines of the formula I wherein R1 is selected from the group consisting of hydrogen, (C,-C6)alkyl or other suitable substituents; R3 is selected from the group consisting óf hydrogen, (Cl-C6)alkyl or other suitable substituents; s is an integer from 0-5; R4is hydrogen or a suitable substituent and to intermediates for their preparation. The compounds prepared by the methods of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

Alkyl-[4-(trifluorophenyl)-oxazol-5-yl]-triazolo-pyridines

The present invention relates to novel alkyl-[4-(trifluorophenyl)-oxazol-5-yl]-triazolo-pyridines, to intermediates and methods for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

Cycloalkyl-[4-(difluorophenyl)-oxazol-5-yl]-triazolo-pyridines

The present invention relates to novel cycloalkyl-[4-(difluorophenyl)-oxazol-5-yl]triazolo-pyridines, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

Alkyl-[4-(difluorophenyl)-oxazol-5-yl]-triazolo-pyridines

The present invention relates to novel alkyl-[4-(difluorophenyl)-oxazol-5-yl]-triazolo-pyridines, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

Cycloalkyl-[4-(trifluorophenyl)-oxazol-5yl]-triazolo-pyridines

The present invention relates to novel cycloalkyl-[4-(trifluorophenyl)-oxazol-5-yl]-triazolo-pyridines, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.