1802977-61-2Relevant academic research and scientific papers
Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice
Purkey, Hans E.,Robarge, Kirk,Chen, Jinhua,Chen, Zhongguo,Corson, Laura B.,Ding, Charles Z.,Dipasquale, Antonio G.,Dragovich, Peter S.,Eigenbrot, Charles,Evangelista, Marie,Fauber, Benjamin P.,Gao, Zhenting,Ge, Hongxiu,Hitz, Anna,Ho, Qunh,Labadie, Sharada S.,Lai, Kwong Wah,Liu, Wenfeng,Liu, Yajing,Li, Chiho,Ma, Shuguang,Malek, Shiva,O'Brien, Thomas,Pang, Jodie,Peterson, David,Salphati, Laurent,Sideris, Steve,Ultsch, Mark,Wei, Binqing,Yen, Ivana,Yue, Qin,Zhang, Huihui,Zhou, Aihe
, p. 896 - 901 (2016)
A series of trisubstituted hydroxylactams was identified as potent enzymatic and cellular inhibitors of human lactate dehydrogenase A. Utilizing structure-based design and physical property optimization, multiple inhibitors were discovered with 50 in a MiaPaca2 cell line. Optimization of the series led to 29, a potent cell active molecule (MiaPaca2 IC50 = 0.67 μM) that also possessed good exposure when dosed orally to mice.
LDHA ACTIVITY INHIBITORS
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, (2018/12/13)
The invention provides compounds of formula (I), stereoisomers and pharmaceutically acceptable salts thereof: (I) wherein A1 to A4, R1 and RP are as defined herein. Such compounds are suitable for use in the treatment or prevention of diseases or conditions which are mediated by the activation of lactate dehydrogenase A (LDHA), for example cancer.
LDHA ACTIVITY INHIBITORS
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, (2018/12/13)
The invention provides compounds of formula (I), stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof: (I) wherein A1 to A6 and R1 to R4 are as defined herein. Such compounds are suit
PIPERIDINE-DIONE DERIVATIVES FOR USE AS CONTRACEPTIVES
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, (2018/12/13)
The invention relates to a method of reducing sperm motility or of contraception in a subject, said method comprising the step of administering to said subject an effective amount of a compound of formula (I), a stereoisomer, tautomer, pharmaceutically ac
METHOD OF CONTROLLING LACTATE PRODUCTION WITH PIPERDINE-DIONE DERIVATIVES
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Page/Page column 79-80; 241, (2015/11/10)
The invention provides novel compounds having the general formula: and tautomers and pharmaceutically acceptable salts thereof, wherein A1, A2, A3, A4, R1, R4, R5, R6, R7 and R8 are as defined herein, compositions including the compounds and methods of using the compounds.
PIPERIDINE-DIONE DERIVATIVES
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Page/Page column 150, (2015/11/10)
The invention provides novel compounds having the general formula (I) and tautomers and pharmaceutically acceptable salts thereof, wherein A1, A2, A3, A4, R1, R4, R5, R6, R7 and R8 are as defined herein, compositions including the compounds and methods of using the compounds.
