- PYRROLO[2,3-B]PYRIDINE CDK9 KINASE INHIBITORS
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Disclosed are compounds of Formula (IIa), wherein R1, R2, R3A, R3B, R3C, R3D, R3E, and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (IIa)
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Page/Page column 626; 627
(2014/09/29)
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- Exploration of the molecular origin of the azinomycin epoxide: Timing of the biosynthesis revealed
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(Equation Presented) Streptomyces sahachiroi whole cell feeding experiments, utilizing putative precursors labeled with stable isotopes, established that the epoxide unit of the DNA cross-linked agents, azinomycin A and B, proceeds via a valine-dependent pathway and that hydroxylation and dehydration precedes formation of the terminal epoxide. Sodium 3-methyl-2-oxobutenoate, formed through a transimination reaction, was shown to be the penultimate precursor incorporated into the azinomycin epoxide.
- Sharma, Vasudha,Kelly, Gilbert T.,Watanabe, Coran M. H.
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supporting information; experimental part
p. 4815 - 4818
(2009/05/31)
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- NITROGEN-CONTAINING HETEROCYCLIC COMPOUND AND PHARMACEUTICAL APPLICATION THEREOF
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It is intended to provide a compound represented by the general formula (I): (I) (wherein all the symbols are as defined in the description) which has a p38 MAP kinase inhibitory activity, a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. The compound of the invention is useful for preventing or treating a disease in which the abnormal production of a cytokine such as an inflammatory cytokine or a chemokine or overreaction to them is considered to be involved in the cause and aggravation of pathological conditions, in other words, an inflammatory disease, a respiratory disease, a cardiovascular disease, a central nervous system disease or the like, which is a cytokine-mediated disease.
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Page/Page column 180
(2010/11/26)
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- Asymmetric synthesis of the left hand portion of the azinomycins
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A nine step synthesis of the left hand portion of the azinomycins is described starting from 3,3-dimethyl-acrylic acid. The approach relies on a Sharpless asymmetric dihydroxylation (AD) reaction to install the requisite (2S,3S)-stereochemistry of epoxy alcohol 4. This epoxide is converted to crystalline amide derivative 12 whose structure and absolute stereochemistry have been unambiguously established using X-ray crystallography. Coupling of epoxy alcohol (2S,3S)-4 with naphthoyl chloride 16 and subsequent manipulations furnish epoxy amide (2S,3S)-1 identical in all respects with the natural material.
- Bryant, Helen J.,Dardonville, Christophe Y.,Hodgkinson, Timothy J.,Hursthouse, Michael B.,Malik, K. M. Abdul,Shipman, Michael
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p. 1249 - 1255
(2007/10/03)
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