- PYRAZOLE PYRAZINE AMINE COMPOUNDS AS KINASE INHIBITORS, COMPOSITIONS THEREOF AND METHODS OF TREATMENT THEREWITH
-
Provided herein are Pyrazole Pyrazine Amine Compounds having the following structure:Formula (I). Wherein Q and R1-R3 are as defined herein, compositions comprising an effective amount of a Pyrazole Pyrazine Amine Compound and methods for treating or preventing inflammatory conditions, immunological conditions, cancer, neurodegenerative diseases, age-related diseases, cardiovascular diseases and metabolic conditions, or conditions treatable or preventable by inhibition of an IKK, or an IKK pathway, comprising administering an effective amount of a Pyrazole Pyrazine Amine Compound to a patient in need thereof.
- -
-
Page/Page column 128
(2009/09/04)
-
- New low-density lipoprotein receptor upregulators acting via a novel mechanism
-
The synthesis and biological activity of a new series of benzamides and related compounds that upregulate the expression of the low-density lipoprotein (LDL) receptor in human hepatocytes (HepG2 cells) by a novel mechanism are described. The lead compound, N-[5-[(3- cyclohexylpropionyl)amino]-2-methylphenyl]-4-hydroxybenzamide (1, RPR102359), increased the expression of the LDL receptors in HepG2 cells by 80% when tested at a concentration of 3 μM. Mevinolin (lovastatin) was found to increase the LDL receptor expression by 70% at the same concentration. In contrast to mevinolin, 1 was found to have no effect on cholesterol biosynthesis in liver homogenates or in HepG2 cells at doses where substantial upregulation of the LDL receptor was observed and thus stimulated LDL receptor expression by a novel mechanism.
- Ashton, Michael J.,Brown, Thomas J.,Fenton, Garry,Halley, Frank,Harper, Mark F.,Lockey, Peter M.,Porter, Barry,Roach, Alan G.,Stuttle, Keith A. J.,Vicker, Nigel,Walsh, Roger J. A.
-
p. 3343 - 3356
(2007/10/03)
-
- One pot preparation of pyrido[2,3,4-de] quinazolines and benzo[de][1,6] naphthyridines by a consecutive process involving an aza-Wittig/ electrocyclic ring-closure/heterocumulene-mediated annelation or intramolecular Diels-Alder cycloaddition sequence
-
Aza Wittig-type reaction of bis(iminophosphorane)1 with one mole of isocyanate leads to the iminophosphoranes 5 which by treatment with a second mole of isocyanate afforded pyrido[2,3,4-de]quinazolines 6. Similarly, reaction with ketenes leads to the formation of benzo[de][1,6] naphthyridines 9. Direct conversion 1→6 and 1→9 were achieved using two moles of isocyanate or ketene respectively.
- Molina, Pedro,Alajarin, Mateo,Vidal, Angel
-
p. 5379 - 5382
(2007/10/02)
-
- Molecular Armatures. Synthesis and Structure of Troegers Base Analogues Derived from 4-, 2,4-, 3,4-, and 2,4,5-Substituted Aniline Derivatives
-
The preparation of biomimetic systems designed to mimic natural receptor sites and enzymic active sites requires the development of new synthetic strategies for preparing large molecules with predictable and well-defined shapes.In this paper a number of derivatives of 6H,12H-5,11-methanodibenzodiazocines are prepared.The scope and limitations of the reaction of formaldehyde with aniline derivatives are examined.The molecules prepared have potential value as conformationally restricted armatures for the construction of biomimetic molecular systems.A crystallographic study reveals that the molecules are folded and that the angle formed by the two aryl rings ranges from 88 deg to 104 deg.Sulfonamides, bromides, alcohols, and amines can be introduced as side-chain substituents in these systems.
- Sucholeiki, Irving,Lynch, Vincent,Phan, Ly,Wilcox, Craig S.
-
-