20481-15-6Relevant articles and documents
Synthesis and characterization of new 1H-pyrazolo[3,4-b]pyridine phosphoramidate derivatives
Pedrosa, Leandro F.,De Macedo, William P.,Furtado, Antonia C.R.,Guedes, Guilherme P.,Borges, Julio C.,Resende, Jackson A.L.C.,Vaz, Maria G.F.,Bernardino, Alice M.R.,De Souza, Marcos C.
, p. 38 - 50 (2014/04/17)
Twelve new 1H-pyrazolo[3,4-b]pyridine phosphoramidate derivatives were synthesized under mild conditions by nucleophilic aromatic substitution reaction of aminoalkylphosphoramidates over 4-Cl substituted pyrazolo[3,4-b]pyridine in good yields. The new com
The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist
Rimland, Joseph,Dunne, Angela,Hunjan, Suchete S.,Sasse, Rosemary,Uings, Iain,Montanari, Dino,Caivano, Matilde,Shah, Poonam,Standing, David,Gray, David,Brown, David,Cairns, William,Trump, Ryan,Smith, Paul W.,Bertheleme, Nicolas,D'Alessandro, Pier,Gul, Sheraz,Vimal, Mythily,Smith, David N.,Watson, Stephen P.
scheme or table, p. 2340 - 2343 (2010/08/22)
The identification of novel, potent, non-steroidal/small molecule functional GR antagonist GSK1564023A selective over PR is described. Associated structure-activity relationships and the process of optimisation of an initial HTS hit are also described.
SUBSTITUTED PYRAZOLO [3,4-B]PYRIDINES AS PHOSPHODIESTERASE INHIBITORS
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Page/Page column 7, (2010/02/17)
The present invention relates to phosphodiesterase (PDE) type IV selective inhibitors. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type IV selective inhibitors are provided. Prepared compounds correspond to structure XIV.
PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS
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Page/Page column 54, (2008/12/07)
The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4 /PDE type 7 inhibitors. Compounds disclosed hereinf having the structure of Formula 1: can be useful in the treatment, prevention, inhibiti
PYRAZOLO (3, 4-B) PYRIDINE DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS
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Page/Page column 77, (2008/12/07)
The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4 /PDE type 7 inhibitors. Compounds disclosed herein having the structure of Formura 1: can be useful in the treatment, prevention, inhibitio
New orally active PDE4 inhibitors with therapeutic potential
Ochiai, Hiroshi,Ishida, Akiharu,Ohtani, Tazumi,Kusumi, Kensuke,Kishikawa, Katuya,Obata, Takaaki,Nakai, Hisao,Toda, Masaaki
, p. 29 - 32 (2007/10/03)
Structural optimization of pyrazolopyridine derivative 2, which is one of the newly discovered chemical leads for PDE4 inhibitors from our in-house library, was carried out successfully. The process of discovery of new orally active PDE4 inhibitors, which
Discovery of new orally active phosphodiesterase (PDE4) inhibitors
Ochiai, Hiroshi,Ishida, Akiharu,Ohtani, Tazumi,Kusumi, Kensuke,Kishikawa, Katuya,Yamamoto, Susumu,Takeda, Hiroshi,Obata, Takaaki,Nakai, Hisao,Toda, Masaaki
, p. 1098 - 1104 (2007/10/03)
A series of 4-anilinopyrazolopyridine derivatives were synthesized and biologically evaluated as inhibitors of phosphodiesterase (PDE4). Chemical modification of 3, a structurally new chemical lead that was found in our in-house library, was focused on 1- and 3-substituents. Full details of the discovery of a new orally active chemical lead 5 are presented. Structure-activity relationship data, pharmacological evaluation, and the subtype selectivity study are also presented.
New orally active PDE4 inhibitors with therapeutic potential
Ochiai, Hiroshi,Ishida, Akiharu,Ohtani, Tazumi,Kusumi, Kensuke,Kishikawa, Katuya,Yamamoto, Susumu,Takeda, Hiroshi,Obata, Takaaki,Nakai, Hisao,Toda, Masaaki
, p. 4089 - 4100 (2007/10/03)
The design, synthesis, and biological evaluation of a series of pyrazolopyridines was carried out. Structural optimization of the aniline moiety of 4-anilinopyrazolopyridine derivative 3a, which is one of the newly discovered chemical leads for PDE4 inhib
Preparation and use of acetylenic ortho-sulfonamido and phosphinic acid amido bicyclic heteroaryl hydroxamic acids as TACE inhibitors
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Page/Page column 22, (2010/01/31)
Compounds of the formula which are useful in disease conditions mediated by TNF-α, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
Synthesis and SAR of bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors
Zask,Gu,Albright,Du,Hogan,Levin,Chen,Killar,Sung,DiJoseph,Sharr,Roth,Skala,Jin,Cowling,Mohler,Barone,Black,March,Skotnicki
, p. 1487 - 1490 (2007/10/03)
Potent and selective bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors were synthesized by a novel convergent route. Selectivity and efficacy versus MMPs and TACE could be controlled by appropriate substitution on the scaffolds and by variation of the P1′ group. Select compounds were found to be effective in in vivo models of arthritis.