108274-33-5Relevant academic research and scientific papers
Discovery of Orally Bioavailable and Liver-Targeted Hypoxia-Inducible Factor Prolyl Hydroxylase (HIF-PHD) Inhibitors for the Treatment of Anemia
Liu, Ping,Wang, Liping,Dubois, Byron G.,Colandrea, Vincent J.,Liu, Rongqiang,Cai, Jiaqiang,Du, Xiaoxing,Quan, Weiguo,Morris, William,Bai, Jianwu,Bishwokarma, Bimjhana,Cheng, Mangeng,Piesvaux, Jennifer,Ray, Kallol,Alpert, Carla,Chiu, Chi-Sung,Zielstorff, Mark,Metzger, Joseph M.,Yang, Liming,Leung, Dennis,Alleyne, Candice,Vincent, Stella H.,Pucci, Vincenzo,Li, Xiaofang,Crespo, Alejandro,Stickens, Dominique,Hale, Jeffrey J.,Ujjainwalla, Feroze,Sinz, Christopher J.
, p. 1193 - 1198 (2018/12/11)
We report herein the design and synthesis of a series of orally active, liver-targeted hypoxia-inducible factor prolyl hydroxylase (HIF-PHD) inhibitors for the treatment of anemia. In order to mitigate the concerns for potential systemic side effects, we
IMIDAZOLIDINONE DERIVATIVES AS INHIBITORS OF PERK
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Page/Page column 63, (2017/04/11)
The invention is directed to substituted imidazolidinone derivatives. Specifically, the invention is directed to compounds according to Formula I (I) wherein R1, R2, R3, R4, R5, R6, R7, X, Y1, Y2 and Z are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, pre-cancerous syndromes, as Alzheimer's disease, neuropathic pain, spinal cord injury, traumatic brain injury, ischemic stroke, stroke, Parkinson disease, diabetes, metabolic syndrome, metabolic disorders, Huntington's disease, Creutzfeldt-Jakob Disease, fatal familial insomnia, Gerstmann-Str?ussler-Scheinker syndrome, and related prion diseases, amyotrophic lateral sclerosis, progressive supranuclear palsy, myocardial infarction, cardiovascular disease, inflammation, organ fibrosis, chronic and acute diseases of the liver, fatty liver disease, liver steatosis, liver fibrosis, chronic and acute diseases of the lung, lung fibrosis, chronic and acute diseases of the kidney, kidney fibrosis, chronic traumatic encephalopathy (CTE), neurodegeneration, dementias, frontotemporal dementias, tauopathies, Pick's disease, Neimann-Pick's disease, amyloidosis, cognitive impairment, atherosclerosis, ocular diseases, arrhythmias, in organ transplantation and in the transportation of organs for transplantation. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Nitromethylene derivatives and their use as insecticides
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, (2008/06/13)
The present invention provides novel nitromethylene derivatives of the formula (I) STR1 wherein R represents a hydrogen atom or an alkyl group, X represents a haloalkyl, haloalkoxy, haloalkylthio, haloalkylsulfinyl, haloalkylsulfonyl, nitro, cyano, thiocyanato, haloalkenyl, haloalkynyl, hydroxyl, alkoxycarbonyl, amino, acyl, dialkylamino, acylamino or alkoxy group, l represents 1, 2 or 3 provided that when l is 1, X does not represent an alkoxy group and when l is 2 or 3, not all substituents X represent an alkoxy group, m represents 2, 3 or 4, and n represents 0 or 1, and the use of the new compounds as insecticides.
