1079-47-6Relevant academic research and scientific papers
Protective Agent for Retinal Neuronal Cell Comprising Indazole Derivative as Active Ingredient
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Page/Page column 8-9, (2009/01/23)
As a result of intensive studies for the purpose of finding a new medicinal use of an indazole derivative, it was found that an indazole derivative inhibits glutamate-induced retinal neuronal cell death in rat fetal retinal neuronal cells, in other words, the indazole derivative acts directly on the retinal neuronal cells and exhibits an effect of protecting retinal neuronal cells. Accordingly, the indazole derivative is useful for the prevention or treatment of an eye disease associated with retinal neuronal cell damage or retinal damage.
PROTECTIVE AGENT FOR RETINAL NEURONAL CELL COMPRISING INDAZOLE DERIVATIVE AS ACTIVE INGREDIENT
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Page/Page column 12-13, (2010/11/29)
As a result of intensive studies for the purpose of finding a new medicinal use of an indazole derivative, it was found that an indazole derivative inhibits glutamate-induced retinal neuronal cell death in rat fetal retinal neuronal cells, in other words, the indazole derivative acts directly on the retinal neuronal cells and exhibits an effect of protecting retinal neuronal cells. Accordingly, the indazole derivative is useful for the prevention or treatment of an eye disease associated with retinal neuronal cell damage or retinal damage.
N-heterocyclic carbenes of 5-haloindazoles generated by decarboxylation of 5-haloindazolium-3-carboxylates
Schmidt, Andreas,Snovydovych, Bohdan,Habeck, Tobias,Droettboom, Petra,Gjikaj, Mimoza,Adam, Arnold
, p. 4909 - 4916 (2008/03/14)
Syntheses and properties of 5-fluoro-, chloro- bromo-, and iodo-substituted 11,2-dimethylindazohum-3-carboxylates as new representatives of pseudo-cross-conjugated heterocyclic mesomeric betaines are described, and results of an X-ray single crystal analy
NOVEL INDAZOLE DERIVATIVE
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Page/Page column 38-39, (2008/06/13)
An object of the present invention is to create a novel indazole derivative useful as a drug and to find a novel pharmacological action of the derivative. The compound of the present invention is represented by the formula [I] and has an excellent Rho kinase inhibiting action. In the formula, a ring X is a benzene ring or a pyridine ring; R1 and R2 are H or alkyl; R3 and R4 are halogen, H, OH, alkoxy, alkenyloxy, alkynyloxy, cycloalkyloxy, cycloalkenyloxy, aryloxy, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, carboxy, hydrocarbonyl, alkylcarbonyl, etc.; and R5 is halogen atom, H, OH, alkoxy, aryloxy, alkyl or aryl. Each group can be substituted.
Synthesis and SAR of indazole-pyridine based protein kinase B/Akt inhibitors
Woods, Keith W.,Fischer, John P.,Claiborne, Akiyo,Li, Tongmei,Thomas, Sheela A.,Zhu, Gui-Dong,Diebold, Robert B.,Liu, Xuesong,Shi, Yan,Klinghofer, Vered,Han, Edward K.,Guan, Ran,Magnone, Shayna R.,Johnson, Eric F.,Bouska, Jennifer J.,Olson, Amanda M.,Jong, Ron de,Oltersdorf, Tilman,Luo, Yan,Rosenberg, Saul H.,Giranda, Vincent L.,Li, Qun
, p. 6832 - 6846 (2007/10/03)
A series of heteroaryl-pyridine containing inhibitors of Akt are reported. The synthesis and structure-activity relationships are discussed, leading to the discovery of a indazole-pyridine analogue (Ki = 0.16 nM). These compounds bind in the ATP binding site, are potent, ATP competitive, and reversible inhibitors of Akt activity. No selectivity amongst the Akt isoforms is observed for this analogue, but there is good selectivity against an panel of other kinases. It is least selective for other members of the AGC family of kinases but is nonetheless 40-fold selective for Akt over PKA. The compound shows cellular activity and significantly slows tumor growth in vivo.
Kinase inhibitors
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, (2008/06/13)
Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.
