Process Safety Considerations for the Supply of a High-Energy Oxadiazole IDO1-Selective Inhibitor
The development of a stereospecific synthesis of a IDO1-selective inhibitor is described. The synthetic strategy toward enabling early discovery efforts along with additional findings pertaining to process safety that limited scalability are outlined. A convergent approach that supported the synthesis of material suitable for early preclinical and/or good laboratory practice toxicology studies and avoided the formation of key high-energy intermediates is summarized.
Martinot, Theodore A.,Ardolino, Michael,Chen, Lu,Lam, Yu-Hong,Li, Chaomin,Maddess, Matthew L.,Muzzio, Daniel,Qi, Ji,Saurí, Josep,Song, Zhiguo J.,Tan, Lushi,Vickery, Thomas,Yin, Jingjun,Zhao, Ralph
NOVEL SUBSTITUTED N'-HYDROXYCARBAMIMIDOYL-1,2,5-OXADIAZOLE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS
Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Formula (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
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Page/Page column 33
(2018/03/25)
NOVEL SUBSTITUTED SULFOXIMINE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS
Compounds of Formula I, or a pharmaceutically acceptable salt, solvate or hydrate thereof: (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
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Page/Page column 30
(2018/09/26)
NOVEL SUBSTITUTED N'-HYDROXYCARBAMIMIDOYL-1,2,5-OXADIAZOLE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS
Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof. Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
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Page/Page column 35
(2018/10/25)
BICYCLO (4.2.0) 1,3,5-OCTATRIENE COMPOUNDS AND USE AS ALPHA-ADRENERGICS
Compounds of the formula: STR1 in which: R 1 and R 2 each represent, independently of one another, hydrogen, halogen, alkyl or alkoxy having from 1 to 4 carbon atoms, sulphonamide possibly substituted by an alkyl radical having from 1 to 4 carbon atoms; o
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(2008/06/13)
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