- NOVEL PHARMACEUTICALS
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The present invention relates to immune response modifiers of formula (I), which act selectively through agonism, of Toll-Like Receptors (TLRs), uses thereof, processes for the preparation thereof, intermediates used in the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including the treatment of infectious disease such as Hepatitis (e.g. HCV, HBV), genetically related viral infection and cancer.
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Page/Page column 67
(2010/11/28)
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- Synthesis of the CD-ring of the anticancer agent streptonigrin: studies of aryl-aryl coupling methodologies
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A series of functionalized 4-bromopyridines, representing the C-ring of the anticancer agent streptonigrin have been prepared and their abilities to undergo Pd-catalyzed cross-coupling with streptonigrin D-ring siloxanes were evaluated. The coupling reaction was generally tolerant to the preparation of hindered CD biaryls; however, the electronic effects of both partners play a pivotal role in the success of the coupling process. Analogs of the CD biaryl were prepared by coupling of aryl siloxane derivatives (D-ring component) with highly functionalized 4-bromopyridines (C-ring); however, the CD biaryl of the natural product could not be prepared in high yield by siloxane coupling due to the facile formation of reduced pyridine under the coupling conditions. Alternatively, the fully functionalized CD biaryl of streptonigrin was prepared using a Suzuki coupling of appropriately functionalized C-ring bromide and D-ring aryl boronic acid. The described approach is highly convergent and readily amenable to the synthesis of analogs.
- McElroy, William T.,DeShong, Philip
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p. 6945 - 6954
(2007/10/03)
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- Process for imidazo[4,5-c]pyridin-4-amines
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A process and intermediates for preparing 1H-imidazo[4,5-c]pyridin-4-amines are disclosed. The process includes providing a 4-phenoxy-1H-imidazo[4,5-c]pyridine and aminating the 4-phenoxy-1H-imidazo[4,5-c]pyridine to provide a 1H-imidazo[4,5-c]pyridin-4-a
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- Siloxane-Based Cross-Coupling of Bromopyridine Derivatives: Studies for the Synthesis of Streptonigrin and Lavendamycin
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(Equation Presented) Highly functionalized 4-bromopyridines were prepared and found to undergo fluoride-promoted, Pd-catalyzed cross-coupling with aryltrialkoxy-silanes to give sterically demanding biaryls. The 3-nitro-4-bromopyridine derivative coupled i
- McElroy, William T.,DeShong, Philip
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p. 4779 - 4782
(2007/10/03)
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- Benzopyrans
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A compound of the formula: STR1 or a pharmaceutically acceptable salt thereof, wherein X is O, S or NH; R and R1 are each independently selected from H and C1 -C4 alkyl or taken together represent C2 -C6 alkylene; R2 is H or C1 -C4 alkyl; R3 is a 6-membered heterocyclic ring containing 2N hetero-atoms, said ring being linked to X by a ring carbon atom, optionally benzo-fused and optionally substituted, including in the benzo-fused portion, by C1 -C6 alkyl, hydroxy, --OR5, halo, --S(O)m R5, oxo, amino, --NHR5, --N(R5)2, cyano, --CO2 R5, --CONH2, --CONHR5 or --CON(R5)2, with the proviso that R3 is not an N--(C1 -C6 alkyl)pyridonyl group; R4 is phenyl substituted by a hydroxy group and optionally further substituted by 1 or 2 substitutents each independently selected from hydroxy, C1 -C6 alkyl, --OR5, halo, cyano and nitro; R5 is C1 -C6 alkyl; R6 is --OR5, --NHR5, --N(R5)2, --SR5 or --NHR9 ; R7 is cyano; R8 is --OR5, --NHR5, --N(R5)2, or --NHR9 ; R9 is phenyl optionally substituted by C1 -C6 alkyl, hydroxy, --OR5, halo, cyano or nitro; and m is 0, 1 or 2.
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