260254-80-6Relevant articles and documents
3-AMINO-PYRROLO[3,4-C] PYRAZOLE- 5 (1H, 4H, 6H) CARBALDEHYDE DERIVATIVES AS PKC INHIBITORS
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Page/Page column 41, (2008/12/08)
The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: (A) and (B) wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disase pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.
3-AMIDO-PYRROLO[3,4-C]PYRAZOLE-5(1H, 4H,6H) CARBALDEHYDE DERIVATIVES AS INHIBITORS OF PROTEIN KINASE C
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Page/Page column 20; 22, (2008/12/08)
The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ
Indole-type derivatives as inhibitors of p38 kinase
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Page/Page column 44-45, (2008/06/13)
The invention is directed to methods to inhibit p38-α kinase using compounds comprising a phenyl or thienyl coupled through a piperidine or piperazine nucleus to an indole residue wherein the indole residue mandatorily has a substituent on the ring nitrogen which is an amino or substituted amino group.
Indole-based heterocyclic inhibitors of p38α MAP kinase: Designing a conformationally restricted analogue
Mavunkel, Babu J.,Chakravarty, Sarvajit,Perumattam, John J.,Luedtke, Gregory R.,Liang, Xi,Lim, Don,Xu, Yong-Jin,Laney, Maureen,Liu, David Y.,Schreiner, George F.,Lewicki, John A.,Dugar, Sundeep
, p. 3087 - 3090 (2007/10/03)
p38α Mitogen Activated Protein Kinase (MAP kinase) is an intracellular soluble serine threonine kinase. p38α kinase is activated in response to cellular stresses, growth factors and cytokines such as interleukin-1 (IL-1) and tumor necrosis factor alpha (TNF-α). The central role of p38α activation in settings of both chronic and acute inflammation has led efforts to find inhibitors of this enzyme as possible therapies for diseases such as rheumatoid arthritis, where p38α activation is thought to play a causal role. Herein, we report structure-activity relationship studies on a series of indole-based heterocyclic inhibitors that led to the design and identification of a new class of p38α inhibitors.
BENZOFURYLPIPERAZINES AND BENZOFURYLHOMOPIPERAZINES: SEROTONIN AGONISTS
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, (2013/12/12)
The present invention provides serotonergic benzofurylpiperazines of Formula I: where: A is a piperazine of formula: and R, R1, R2, R3, R4, R5, R5', R6, R6', R7, R7', R8, and R8' are as described in the specification.