1489-58-3Relevant academic research and scientific papers
IMIDAZOLIDINONE DERIVATIVES AS INHIBITORS OF PERK
-
Page/Page column 92, (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.
An efficient and improved process for the scale-up preparation of cis-cyclopropanediamine dihydrochloride
Wang, Fan,Xu, Xiao-Ying,Wang, Fei-Ying,Peng, Lin,Zhang, Yong,Wang, Liang-Liang,Wang, Li-Xin
, p. 741 - 744 (2016/03/25)
An effective and improved process for the preparation of cis-cyclopro panediamine dihydrochloride was developed in a 100 g scale. The key step in the process is the preparation of ciscyclopropane-1, 2-dicarboxylic acid from a mixture of cis- and transisomers by the formation of cyclic acidic anhydride. The whole process and all of the procedures are economical, industrially reliable and easily scaled up.
Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors
Simpkins, Ligaya M.,Bolton, Scott,Pi, Zulan,Sutton, James C.,Kwon, Chet,Zhao, Guohua,Magnin, David R.,Augeri, David J.,Gungor, Timur,Rotella, David P.,Sun, Zhong,Liu, Yajun,Slusarchyk, William S.,Marcinkeviciene, Jovita,Robertson, James G.,Wang, Aiying,Robl, Jeffrey A.,Atwal, Karnail S.,Zahler, Robert L.,Parker, Rex A.,Kirby, Mark S.,Hamann, Lawrence G.
, p. 6476 - 6480 (2008/09/16)
The synthesis and structure-activity relationships of novel dipeptidyl peptidase IV inhibitors replacing the classical cyanopyrrolidine P1 group with other small nitrogen heterocycles are described. A unique potency enhancement was achieved with β-branched natural and unnatural amino acids, particularly adamantylglycines, linked to a (2S,3R)-2,3-methanopyrrolidine based scaffold.
Novel bisbenzamidines as potential drug candidates for the treatment of Pneumocystis carinii pneumonia
Vanden Eynde, Jean Jacques,Mayence, Annie,Huang, Tien L.,Collins, Margaret S.,Rebholz, Sandra,Walzer, Peter D.,Cushion, Melanie T.
, p. 4545 - 4548 (2007/10/03)
A series of pentamidine congeners has been synthesized and screened for their in vitro activity against Pneumocystis carinii. Among the tested compounds, bisbenzamidines linked by a flexible pentanediamide or hexanediamide chain (7 and 9) emerged as excep
SUBSTITUTED CYCLOALKANECARBOXYLIC ACID DERIVATIVES AS MATRIX METALLOPROTEASE INHIBITORS
-
, (2008/06/13)
Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula STR1 wherein each T is a substituent g roup; x is 0, 1, or 2; the group D represents STR2 the subscript "e" is 2 or 3; the group R 14 represents a variety of possible substituent groups of the cycloalkyl ring between D and G; the subscript "k" is 0-2; and the group G represents M, STR3 in which M represents--CO 2 H,--CON(R 11) 2, or--CO 2 R 12 ; and R 13 represents any of the side chains of the 19 noncyclic occurring amino acids. "
Herbicidal tricyclic heterocycles
-
, (2008/06/13)
Compounds of Formula I having herbicidal utility are disclosed: STR1 wherein Q, R1, R2, V, m and p are defined in the text, including compositions containing such compounds, and a method for controlling weeds employing such compounds.
The Synthesis and Cycloaddition Reactions of 3-Azabicyclohex-2-ene 3-oxide and 3-Azabicyclohept-2-ene 3-oxide. Highly Strained Bicyclic Nitrones
Tufariello, Joseph J.,Milowsky, Arnold S.,Al-Nuri, Mohammed,Goldstein, Steven
, p. 267 - 270 (2007/10/02)
The synthesis of two strained bicyclic nitrones is described.Subsequent cycloadditions demonstrated a high degree of regiochemical and stereochemical control.
1,1-Alkanediol dicarboxylate linked antibacterial agents
-
, (2008/06/13)
Useful antibacterial agents in which a penicillin and/or a beta-lactamase inhibitor are linked via 1,1-alkanediol dicarboxylates are of the formula STR1 where A is the residue of certain dicarboxyic acids, R3 is H or (C1 -C3), n is zero or 1 such that when n is zero R is P or B and R1 is the residue of certain esters, H or a salt thereof; and when n is 1, one of R and R1 is P and the other is B, and P is STR2 where R2 is H or certain acyl groups, and B is the residue of a beta-lactamase inhibiting carboxylic acid; a method for their use, pharmaceutical compositions thereof and intermediates useful in their production.
