- BICYCLIC HETEROARYL SUBSTITUTED COMPOUNDS
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Disclosed are compounds of Formula (I) to (VIII): (I) (II) (III) (IV) (V) (VI) (VII) (VIII); or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein R3 is a bicyclic heteroaryl group substituted with zero to 3 R3a; and R1, R2, R3a, R4, and n are defined herein. Also disclosed are methods of using such compounds as PAR4 inhibitors, and pharmaceutical compositions comprising such compounds. These compounds are useful in inhibiting or preventing platelet aggregation, and are useful for the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder.
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Page/Page column 717; 718
(2018/03/25)
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- Photoswitchable anticancer activity via trans-cis isomerization of a combretastatin A-4 analog
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Combretastatin A-4 (CA4) is highly potent anticancer drug that acts as an inhibitor of tubulin polymerization. The core of the CA4 structure contains a cis-stilbene, and it is known that the trans isomer is significantly less potent. We prepared an azoben
- Sheldon, Jonathon E.,Dcona, M. Michael,Lyons, Charles E.,Hackett, John C.,Hartman, Matthew C. T.
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- Isoindole-imide compounds and compositions comprising and methods of using the same
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This invention relates to isoindole-imide compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
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Page/Page column 76-77
(2010/11/26)
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- New prodrugs derived from 6-aminodopamine and 4-aminophenol as candidates for melanocyte-directed enzyme prodrug therapy (MDEPT)
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Two novel tyrosinase mediated drug delivery pathways have been investigated for the selective delivery of cytotoxic units to melanocytes from urea and thiourea prodrugs. The synthesis of these prodrugs is reported, as well as oximetry data that illustrate that the targets are substrates for tyrosinase. The stability of each of the prodrugs in (i) phosphate buffer and (ii) bovine serum is discussed, and the urea prodrugs are identified as lead candidates for further studies. Finally, HPLC studies and preliminary cytotoxicity studies in a melanotic and an amelanotic cell line, that illustrate the feasibility of the approach, are presented. The Royal Society of Chemistry 2005.
- Knaggs, Sarah,Malkin, Hugh,Osborn, Helen M.I.,Williams, Nana Aba O.,Yaqoob, Parveen
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p. 4002 - 4010
(2007/10/03)
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- Structure-activity relationship and rational design of 3,4-dephostatin derivatives as protein tyrosine phosphatase inhibitors
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Several alkyl- and O-methylated-3,4-dephostatin were synthesized and evaluated for their inhibitory activity toward protein tyrosine phosphatase. Alkyl chains with a length up to that of the pentyl group gave tolerable inhibition, whereas methylation of h
- Watanabe, Takumi,Suzuki, Takayuki,Umezawa, Yoji,Takeuchi, Tomio,Otsuka, Masami,Umezawa, Kazuo
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p. 741 - 752
(2007/10/03)
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