- Chiral Hexahalogenated 4,4′-Bipyridines
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The preparation of 27 isomers of chiral hexahalogeno-4,4′-bipyridines by means of two complementary methods is described. The first one is convergent and based on the LDA-induced 4,4′-dimerization of trihalopyridines, whereas the second method is divergent and achieved through regioselective halogenation reactions of 4,4′-bipyridine-2,2′-diones. Iodine in 2,2′-positions of the 4,4′-bipyridines was introduced by a copper-catalyzed Finkelstein reaction (Buchwald procedure) performed on 2,2′-dibromo derivatives. Selected compounds of this new family of atropisomeric 4,4′-bipyridines were enantioseparated by high performance liquid chromatography on chiral stationary phases, and the absolute configurations of the separated enantiomers were assigned by using X-ray diffraction analysis. The latter revealed that various halogen bond types are responsible for crystal cohesion.
- Mamane,Peluso,Aubert,Cossu,Pale
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p. 4576 - 4587
(2016/07/06)
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- AMINONITRILES AS KYNURENINE PATHWAY INHIBITORS
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The present application provides novel kynurenine pathway inhibitors and pharmaceutically acceptable salts and prodrugs thereof. Also provided are methods for preparing these compounds. These compounds are useful in regulating the kynurenine pathway and the activity of indoleamine 2,3-dioxygenase and/or tryptophan 2,3-dioxygenase by administering a therapeutically effective amount of one or more of the compounds of formula (I) to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the kynurenine pathway. A variety of conditions can be treated using these compounds and include diseases which are characterized by immunosuppression, abnormal cellular proliferation and/or inflammation. In one embodiment, the disease is cancer. In another embodiment, the disease is a viral infection. In a further embodiment, the disease is depression.
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Page/Page column 83; 84
(2014/09/29)
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- SPIROINDOLINONE PYRIDINE DERIVATIVES
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There are provided compounds of the formula or a pharmaceutically acceptable salt, ester or enantiomer thereof wherein W, X, Y, V, R1 and R2 are as described herein. The compounds have utility as antiproliferative agents, especially,
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Page/Page column 6
(2010/08/18)
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- 2,3'-BIPYRIDINES DERIVATIVES AS SELECTIVE COX-2 INHIBITORS
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The present invention relates to 2,3'-bipyridines of formula (I). Processes for their preparation, pharmaceutical compositions containing them, and their medical uses.
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- PHENYL COMPOUNDS
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Compounds of formula (I) or derivatives thereof: wherein A, B, Z, R, R, R, R, R, and R are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
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- 4-pyridinyl-n-acyl-l-phenylalanines
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Compounds of Formula I have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4 and are useful for treating disease whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4.
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- Combination therapy for reducing the risks associated with cardio-and-cerebrovascular disease
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The instant invention provides a drug combination comprised of an HMG-CoA reductase inhibitor in combination with a COX-2 inhibitor, which is useful for treating, preventing, and/or reducing the risk of developing atherosclerosis and atherosclerotic disease events.
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- Substituted pyridines as selective cyclooxygenase-2 inhibitors
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The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. STR1 The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.
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- 2-pyridinyl-3(4-methylsulfonyl)phenylpyridines: Selective and orally active cyclooxygenase-2 inhibitors
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A series of novel 2-pyridinyl-3-(4-methylsulfonyl)phenylpyridines has been synthesized and evaluated with respect to their ability to inhibit the isozymes of cyclooxygenase, COX-1, and COX-2. Optimum COX-2 activity is observed by introduction of a substituent at C5 of the central pyridine. 5- Chloro-3-(4-methylsulfonyl)phenyl-2(2-methyl-5-pyridinyl)pyridine 33 was identified as the optimum compound in this series.
- Friesen, Richard W.,Brideau, Christine,Chan, Chi Chung,Charleson, Stella,Deschenes, Denis,Dube, Daniel,Ethier, Diane,Fortin, Rejean,Gauthier, Jacques Yves,Girard, Yves,Gordon, Robert,Greig, Gillian M.,Riendeau, Denis,Savoie, Chantai,Wang, Zhaoyin,Wong, Elizabeth,Visco, Denise,Xu, Li Jing,Young, Robert N.
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p. 2777 - 2782
(2007/10/03)
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- 6-CHLORO-3,4-DIHYDRO-PYRANO [2,3-B]PYRIDINES HAVING THE R CONFIGURATION
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The present invention relates to processes and intermediates for the preparation of spiro-heteroazolones. The latter compounds are useful as aldose reductase inhibitors
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