17764-92-0Relevant articles and documents
The synthesis of a selective PDE4/TNFα inhibitor
Caron, Stephane,Vazquez, Enrique
, p. 587 - 592 (2001)
Two syntheses of cis-4-cyano-4-(1-cyclohexyl-3-ethyl-1H-indazol-6-yl)cyclohexanecarboxylic acid (1), a selective PDE4/TNFα inhibitor are described. The first synthesis relied on a solvolysis of a tertiary benzylic alcohol to the nitrile using T
Discovery, Structure-Activity Relationship, and Biological Characterization of a Novel Series of 6-((1 H-Pyrazolo[4,3- b]pyridin-3-yl)amino)-benzo[ d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mG
Bollinger, Sean R.,Engers, Darren W.,Panarese, Joseph D.,West, Mary,Engers, Julie L.,Loch, Matthew T.,Rodriguez, Alice L.,Blobaum, Anna L.,Jones, Carrie K.,Thompson Gray, Analisa,Conn, P. Jeffrey,Lindsley, Craig W.,Niswender, Colleen M.,Hopkins, Corey R.
supporting information, p. 342 - 358 (2018/10/20)
This work describes the discovery and characterization of novel 6-(1H-pyrazolo[4,3-b]pyridin-3-yl)amino-benzo[d]isothiazole-3-carboxamides as mGlu4 PAMs. This scaffold provides improved metabolic clearance and CYP1A2 profiles compared to previo
HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
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Paragraph 0175, (2014/05/24)
Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
Synthesis of the unique angular tricyclic chromone structure proposed for aspergillitine, and its relationship with alkaloid TMC-120B
Simonetti, Sebastian O.,Larghi, Enrique L.,Bracca, Andrea B. J.,Kaufman, Teodoro S.
scheme or table, p. 4124 - 4134 (2012/06/15)
The synthesis of the tricyclic angular chromone structure originally assigned to aspergillitine is reported. The synthesis was achieved in 11 steps and 15% overall yield from 2,4-dihydroxypropiophenone, through the intermediacy of 2,3-dimethyl-7-hydroxych
ARYLSULFONAMIDE-BASED MATRIX METALLOPROTEASE INHIBITORS
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Page/Page column 109, (2009/10/22)
The present invention provides a compound of formula (I):said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP- 13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP- 13. Finally, the present invention also provides a pharmaceutical composition.
A versatile and efficient synthesis of substituted 1H-indazoles
Caron, Stéphane,Vazquez, Enrique
, p. 588 - 592 (2007/10/03)
A facile synthesis of substituted 1H-indazole 4 from aryl mesylate 3 is described. The reaction, which proceeds through the intermediate hydrazone, was general with regard to the substituents on the arene and was applicable to several hydrazines. It was a