- Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering
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The propensity for cancer cells to accumulate additional centrosomes relative to normal cells could be exploited for therapeutic benefit in oncology. Following literature reports that suggested TNKS1 (tankyrase 1) and PARP16 may be involved with spindle s
- Johannes, Jeffrey W.,Almeida, Lynsie,Daly, Kevin,Ferguson, Andrew D.,Grosskurth, Shaun E.,Guan, Huiping,Howard, Tina,Ioannidis, Stephanos,Kazmirski, Steven,Lamb, Michelle L.,Larsen, Nicholas A.,Lyne, Paul D.,Mikule, Keith,Ogoe, Claude,Peng, Bo,Petteruti, Philip,Read, Jon A.,Su, Nancy,Sylvester, Mark,Throner, Scott,Wang, Wenxian,Wang, Xin,Wu, Jiaquan,Ye, Qing,Yu, Yan,Zheng, Xiaolan,Scott, David A.
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Read Online
- PYRIDAZINONES AND METHODS OF USE THEREOF
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Disclosed are therapeutic methods, e.g., of treating kidney diseases, using compounds of Formula (A) in combination with a second therapeutic agent.
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Page/Page column 140; 141
(2020/10/09)
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- PYRIDAZINONES AND METHODS OF USE THEREOF
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Disclosed are compounds according to Formula (A), and related tautomers and pharmaceutical compositions. Also disclosed are therapeutic methods, e.g., of treating kidney diseases, using the compounds of Formula (A).
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Page/Page column 373; 374
(2019/04/11)
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- Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists
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Abstract The optimization efforts that led to a novel series of methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones that are potent rat and human P2X7 antagonists are described. These efforts resulted in the discovery of co
- Rudolph, Dale A.,Alcazar, Jesus,Ameriks, Michael K.,Anton, Ana Belen,Ao, Hong,Bonaventure, Pascal,Carruthers, Nicholas I.,Chrovian, Christa C.,De Angelis, Meri,Lord, Brian,Rech, Jason C.,Wang, Qi,Bhattacharya, Anindya,Andres, Jose Ignacio,Letavic, Michael A.
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p. 3157 - 3163
(2015/07/08)
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- COMPOUNDS FOR TREATING DISORDERS MEDIATED BY METABOTROPIC GLUTAMATE RECEPTOR 5, AND METHODS OF USE THEREOF
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Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
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Page/Page column 194
(2011/07/07)
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