- CRYSTALLINE FORMS OF QUINOLINE ANALOGS AND SALTS THEREOF, COMPOSITIONS, AND THEIR METHODS FOR USE
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The present invention includes crystalline forms of 2-(4-Methyl-[1,4]diazepan-1-yl)-5-oxo-5H-7-thia-1,11b-diaza-benzo[c]fluorene-6-carboxylic acid (5-methyl-pyrazin-2-ylmethyl)-amide (Compound I). Furthermore, the present invention provides compositions comprising the crystalline forms and therapeutic use of the crystalline forms and the compositions thereof.
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Paragraph 0244-0254
(2021/02/19)
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- Discovery of CX-5461, the first direct and selective inhibitor of RNA polymerase I, for cancer therapeutics
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Accelerated proliferation of solid tumor and hematologic cancer cells is linked to accelerated transcription of rDNA by the RNA polymerase I (Pol I) enzyme to produce elevated levels of rRNA (rRNA). Indeed, upregulation of Pol I, frequently caused by mutational alterations among tumor suppressors and oncogenes, is required for maintenance of the cancer phenotype and forms the basis for seeking selective inhibitors of Pol I as anticancer therapeutics. 2-(4-Methyl-[1,4]diazepan-1-yl)-5-oxo-5H-7-thia-1,11b-diaza-benzo[c] fluorene-6-carboxylic acid (5-methyl-pyrazin-2-ylmethyl)-amide (CX-5461, 7c) has been identified as the first potent, selective, and orally bioavailable inhibitor of RNA Pol I transcription with in vivo activity in tumor growth efficacy models. The preclinical data support the development of CX-5461 as an anticancer drug with potential for activity in several types of cancer.
- Haddach, Mustapha,Schwaebe, Michael K.,Michaux, Jerome,Nagasawa, Johnny,O'Brien, Sean E.,Whitten, Jeffrey P.,Pierre, Fabrice,Kerdoncuff, Pauline,Darjania, Levan,Stansfield, Ryan,Drygin, Denis,Anderes, Kenna,Proffitt, Chris,Bliesath, Josh,Siddiqui-Jain, Adam,Omori, May,Huser, Nanni,Rice, William G.,Ryckman, David M.
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p. 602 - 606
(2012/10/08)
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- Facile and efficient generation of quinolone amides from esters using aluminum chloride
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Quinolone esters are readily converted into the corresponding amides using aluminum chloride at room temperature in excellent yields and purities. The method is both general and scalable to multi-kilogram quantities.
- Schwaebe, Michael K.,Ryckman, David M.,Nagasawa, Johnny Y.,Pierre, Fabrice,Vialettes, Anne,Haddach, Mustapha
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scheme or table
p. 1096 - 1100
(2011/03/22)
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- QUINOLONE ANALOGS AND METHODS RELATED THERETO
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The present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.
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Page/Page column 135; 136
(2009/04/24)
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