On March 23, 2017, Axten, Jeffrey Michael; Faucher, Nicolas Eric; Daugan, Alain Claude-Marie published a patent.Product Details of 386704-04-7 The title of the patent was Preparation of imidazolidinone derivatives as inhibitors of PERK. And the patent contained the following:
The title imidazolidinones I [R1 = (un)substituted bicycloheteroaryl, heteroaryl; R2 = alkyl, (un)substituted aryl, heteroaryl, etc.; R3 = H, NH2, NH(alkyl), etc.; R4 and R5 = (independently) H and alkyl; R4 and R5 taken together with the carbon atoms to which they are attached form 3-4 membered cycloalkyl, optionally substituted with 1-3 alkyl; R6 = H, alkyl, CF3, etc.; R7 = H, alkyl, CF3, etc.; X = N or (un)substituted CH; Y1 and Y2 = (independently) H, CF3, alkyl; or Y1 and Y2 are taken together with the carbon to which they are attached to form C3-6 cycloalkyl; z = 0-1] or salts thereof including a pharmaceutically acceptable salts thereof, which are inhibitors of PERK and can be useful in the treatment of cancer, pre-cancerous syndromes, Alzheimer’s disease, neuropathic pain, etc., were prepared and formulated. E.g., a multi-step synthesis of II, starting from 4-bromo-3-fluoroaniline and 1-chloro-2-isocyanatoethane, was described. Exemplified compounds I were tested for activity against PERK (data given). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound I. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound I or a pharmaceutical composition comprising I. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Product Details of 386704-04-7
The Article related to imidazolidinone preparation perk inhibitor antitumor analgesic alzheimer’s disease, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Product Details of 386704-04-7
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