190198-15-3Relevant academic research and scientific papers
Discovery, Structure-Activity Relationships, and in Vivo Evaluation of Novel Aryl Amides as Brain Penetrant Adaptor Protein 2-Associated Kinase 1 (AAK1) Inhibitors for the Treatment of Neuropathic Pain
Hartz, Richard A,Ahuja, Vijay T.,Nara, Susheel J.,Kumar, C.M. Vijaya,Brown, Jeffrey M.,Bristow, Linda J.,Rajamani, Ramkumar,Muckelbauer, Jodi K.,Camac, Daniel,Kiefer, Susan E.,Hunihan, Lisa,Gulianello, Michael,Lewis, Martin,Easton, Amy,Lippy, Jonathan S.,Surti, Neha,Pattipati, Sreenivasulu N.,Dokania, Manoj,Elavazhagan, Saravanan,Dandapani, Kumaran,Hamman, Brian D.,Allen, Jason,Kostich, Walter,Bronson, Joanne J.,Macor, John E.,Dzierba, Carolyn D.
, p. 11090 - 11128 (2021/08/03)
Effective treatment of chronic pain, in particular neuropathic pain, without the side effects that often accompany currently available treatment options is an area of significant unmet medical need. A phenotypic screen of mouse gene knockouts led to the d
Microwave-promoted N-arylation of imidazole and amino acids in the presence of Cu2O and CuO in poly(ethylene glycol)
Yakushev,Averin,Colacino,Lamaty,Beletskaya
, p. 1243 - 1248 (2017/02/05)
Copper(I)-catalyzed N-arylation of imidazole with iodobenzene, its derivatives, and bromobenzene in poly(ethylene glycol) under microwave irradiation was studied. The influence of the following factors on the yield of arylation product was investigated: the nature of the source of copper and ligand, type of poly(ethylene glycol) (PEG) used, and substituents in iodoarene. An optimal catalytic system was selected: CuO/l-Hys/Cs2CO3/PEG-400, a possibility of recycling of copper-containing catalyst was demonstrated. N-Arylation of eight natural amino acids using catalysis with Cu2O/Cs2CO3/PEG-400 and microwave irradiation was studied, the dependence of the reaction results on temperature, duration of the process, and the ratio of the starting reagents was found. The highest yields of the target products were reached in the case of leucine, valine, and phenylalanine.
ARYL AMIDE KINASE INHIBITORS
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Page/Page column 96, (2015/02/02)
The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
IMIDAZOPYRAZINE SYK INHIBITORS
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Paragraph 0219; 0315, (2014/01/08)
Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suf-fering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of an imidazopyrazine compound effective to reduce signs or symptoms of the disease or dis-order are provided.
MODULATORS OF AMYLOID BETA
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Page/Page column 14, (2011/07/06)
The invention relates to compounds of formula wherein hetaryl I, hetaryl II, and R1 are as described herein. Compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease.
Compounds derived from an amine nucleus that are inhibitors of IMPDH enzyme
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, (2008/06/13)
The present invention discloses the identification of the novel inhibitors of IMPDH (inosine-5′-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH mediated diseases, such as transplant rejection and autoimmune diseases.
