51440-81-4Relevant academic research and scientific papers
The kinetic resolution of oxazinones by alcoholysis: access to orthogonally protected β-amino acids
Connon, Stephen J.,Cronin, Sarah A.
supporting information, p. 7348 - 7352 (2021/09/07)
The catalytic, alcoholytic kinetic resolution of oxazinones is reported. A novel, stereochemically dense cinchona alkaloid-based catalyst can facilitate the highly enantiodiscriminatory (Sup to 101) ring-opening of oxazinones equipped with electrophilic aryl units to generate orthogonally protected β-amino acids for the first time.
Trimethyl-substituted carbamate as a versatile self-immolative linker for fluorescence detection of enzyme reactions
Inoue, Kazuya,Nakamura, Noriaki,Ojida, Akio,Uchinomiya, Shohei
supporting information, (2020/05/25)
Self-immolative linker is a useful building block of molecular probes, with broad applications in the fields of enzyme activity analysis, stimuli-responsive material science, and drug delivery. This manuscript presents N-methyl dimethyl methyl (i.e., trimethyl) carbamate as a new class of self-immolative linker for the fluorescence detection of enzyme reactions. The trimethyl carbamate was shown to spontaneously undergo intramolecular cyclization upon formation of a carboxylate group, to liberate a fluorophore with the second time rapid reaction kinetics. Interestingly, the auto-cleavage reaction of trimethyl carbamate was also induced by the formation of hydroxyl and amino groups. Fluorescent probes with a trimethyl carbamate could be applicable for fluorescence monitoring of the enzyme reactions catalyzed by esterase, ketoreductase, and aminotransferase, and for fluorescence imaging of intracellular esterase activity in living cells, hence demonstrating the utility of this new class of self-immolative linker.
ARYL SULTAM DERIVATIVES AS RORc MODULATORS
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Page/Page column 40, (2017/01/26)
Compounds of the formula I: or a pharmaceutical salt thereof, wherein p, s, A, R3 and Re are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
ARYL SULTAM DERIVATIVES AS RORc MODULATORS
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Page/Page column 69-70, (2017/01/26)
Compounds of the formula I, or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, X1, X2, X3, X4, Y, Z, A, Het, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined herein.. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis, muscular sclerosis and psoriasis.
HETEROARYL AMIDE SULTAM DERIVATIVES AS RORc MODULATORS
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Page/Page column 45; 46, (2017/07/06)
Compounds of the formula I: (I) or a pharmaceutical salt thereof, wherein m, n, p, q, Het, A, W, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
ARYL SULTAM DERIVATIVES AS RORc MODULATORS
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Paragraph 1210; 1211, (2016/07/05)
Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, W, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
HETEROARYLALKYLENE ARYL SULTAM DERIVATIVES AS RORc MODULATORS
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Page/Page column 42, (2016/07/05)
Compounds of the formula (I): or a pharmaceutical salt thereof, wherein m, n, p, q, Het, A, W, R1, R2, R3, R4, R5, R6, R7, R8, R and R10are as defined herein are modulators of retinoid-receptor related orphan receptor RORc (RORy). Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
Synthesis of Substituted Quinolizidines via a Gold-Catalyzed Double Cyclization Cascade
Nonaka, Shiori,Sugimoto, Kenji,Ueda, Hirofumi,Tokuyama, Hidetoshi
supporting information, p. 380 - 385 (2016/02/12)
A novel synthesis of quinolizidines by a cationic gold-catalyzed double cyclization cascade has been developed. The reaction was initiated by the gold-catalyzed 6-exo-dig cyclization of ynamides, which was followed by a second cyclization of an enamide intermediate to provide the corresponding quinolizidine derivatives. The utility of this reaction was demonstrated by application to the synthesis of multi-substituted quinolizidines and by the total synthesis of a quinolizidine alkaloid, (±)-lupinine.
ARYL SULTAM DERIVATIVES AS RORc MODULATORS
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Paragraph 1201; 1202, (2015/07/22)
Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, W, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
IOP-lowering effect of isoquinoline-5-sulfonamide compounds in ocular normotensive monkeys
Sumi, Kengo,Inoue, Yoshihiro,Nishio, Masahiro,Naito, Yasuhito,Hosoya, Takamitsu,Suzuki, Masaaki,Hidaka, Hiroyoshi
, p. 831 - 834 (2014/02/14)
Rho-associated coiled coil-formed protein kinase (ROCK) inhibitors are under development as a new class of antiglaucoma agents. Based on the potent ROCK inhibitor H-1152, previously developed by us, we explored the possibility of related compounds as anti
