86852-11-1Relevant articles and documents
GPR40 AGONISTS IN ANTI-DIABETIC DRUG COMBINATIONS
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Paragraph 0656, (2017/10/27)
Disclosed are compositions comprising (a) a GPR40 agonist and (b) an SGLT2 inhibitor, and methods for treating of disorders that are affected by the modulation of the GPR40 receptor and SGLT2 transporter. Such GPR40 compounds are represented by Formula (I) as follows: wherein ring W, R1, R2, R3, R5, R6, A, and Z, are defined herein.
Synthesis and anticonvulsant activities of N-benzyl (2R)-2-acetamido-3-oxysubstituted propionamide derivatives
Morieux, Pierre,Stables, James P.,Kohn, Harold
experimental part, p. 8968 - 8975 (2009/04/06)
Lacosamide has been submitted for regulatory approval in the United States and Europe for the treatment of epilepsy. Previous synthetic methods did not permit the elaboration of the structure-activity relationship (SAR) for the 3-oxy site in lacosamide. We report an expedient five-step stereospecific synthesis for N-benzyl (2R)-2-acetamido-3-oxysubstituted propionamide analogs beginning with d-serine methyl ester. The procedure incorporated alkyl (e.g. methyl, primary, secondary, and tertiary) and aryl groups at this position. The SAR for the 3-oxy site showed maximal activity in animal seizure models for small 3-alkoxy substituents.
An expeditious in situ preparation of benzyl (S)-2-aziridinecarboxylate
Kuyl-Yeheskiely, E.,Dreef-Tromp, C. M.,Marel, G. A. van der,Boom, J. H. van
, p. 314 - 316 (2007/10/02)
The use of diethoxytriphenylphosphorane in the preparation of benzyl (S)-2-aziridinecarboxylate is illustrated.The latter compound has been coupled with Z-Ala-OH and the aziridine dipeptide thus obtained ring-opened via C-3-N-1 cleavage with benzyl alcoho
