- ANTI-CANCER DRUGS AND USES RELATING THERETO FOR METASTATIC MALIGNANT MELANOMA AND OTHER CANCERS
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The present invention discloses triazene analogs of the general formula (I) and formula (II), their tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, and pharmaceutically acceptable salts thereof for the metastatic malignant melanoma and other cancers including but not limited to lymphomas, sarcomas, carcinomas, and gliomas. The invention further discloses a process for the preparation of the above said triazene analogs of formula (I) and formula (II), and their pharmaceutically acceptable compositions.
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Page/Page column 46
(2010/04/06)
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- ANTI-CANCER DRUGS AND USES RELATING THERETO FOR METASTATIC MALIGNANT MELANOMA AND OTHER CANCERS
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The present invention discloses triazene analogs of the general formula (I) and formula (II), their tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, and pharmaceutically acceptable salts thereof for the metastatic malignant melanoma and other cancers including but not limited to lymphomas, sarcomas, carcinomas, and gliomas. The invention further discloses a process for the preparation of the above said triazene analogs of formula (I) and formula (II), and their pharmaceutically acceptable compositions.
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Page/Page column 19
(2010/04/23)
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- Evolution of the thienopyridine class of inhibitors of IκB kinase-β: Part I: Hit-to-lead strategies
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High-throughput screening is routinely employed as a method for the identification of novel hit structures. Large numbers of active compounds are typically procured in this way and must undergo a rigorous validation process. This process is described in detail for a collection of screening hits identified as inhibitors of IκB kinase-β (IKKβ), a key regulatory enzyme in the nuclear factor-κB (NF-κB) pathway. From these studies, a promising hit series was selected. Subsequent lead generation activities included the development of a pharmacophore hypothesis and structure-activity relationship (SAR) for the hit series. This led to the exploration of related scaffolds offering additional opportunities, and the various structural classes were comparatively evaluated for enzyme inhibition, selectivity, and drug-like properties. A novel lead series of thienopyridines was thereby established, and this series advanced into lead optimization for further development.
- Morwick, Tina,Berry, Angela,Brickwood, Janice,Cardozo, Mario,Catron, Katrina,DeTuri, Molly,Emeigh, Jonathan,Homon, Carol,Hrapchak, Matt,Jacober, Stephen,Jakes, Scott,Kaplita, Paul,Kelly, Terence A.,Ksiazek, John,Liuzzi, Michel,Magolda, Ronald,Mao, Can,Marshall, Daniel,McNeil, Daniel,Prokopowicz II, Anthony,Sarko, Christopher,Scouten, Erika,Sledziona, Cynthia,Sun, Sanxing,Watrous, Jane,Wu, Jiang Ping,Cywin, Charles L.
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p. 2898 - 2908
(2007/10/03)
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- Hit-to-lead studies: The discovery of potent, orally active, thiophenecarboxamide IKK-2 inhibitors
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A hit-to-lead optimisation programme was carried out on the thiophenecarboxamide high throughput screening hits 1 and 2 resulting in the discovery of the potent and orally bioavailable IKK-2 inhibitor 22.
- Baxter, Andrew,Brough, Steve,Cooper, Anne,Floettmann, Eike,Foster, Steve,Harding, Christine,Kettle, Jason,McInally, Tom,Martin, Craig,Mobbs, Michelle,Needham, Maurice,Newham, Pete,Paine, Stuart,St-Gallay, Steve,Salter, Sylvia,Unitt, John,Xue, Yafeng
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p. 2817 - 2822
(2007/10/03)
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