On May 17, 2012, Cheng, Clifford; Shipps, Gerald W., Jr.; Huang, Xiaohua; Huang, Ying; Shao, Ning; Rao, Ashwin; Palani, Anandan; Orth, Peter; Voigt, Johannes H.; Herr, Robert J.; Rossiter, Lana Michele; Zeng, Qi; Sun, Xianfeng published a patent.Application of 52537-00-5 The title of the patent was Preparation of heterocyclic inhibitors of fatty acid binding protein for use in therapy. And the patent contained the following:
The present invention relates to novel heterocyclic compounds of general formula I (wherein each of X, Y, and Z is C or N; R1 is H, halo, CN, etc.; R2 is OH, halo, C1-6alkyl, etc.; one of R3 and R4 is H or C1-6alkyl, and the other is, e.g., heteroaryl(Ra)3; Ra is H, halo, OH, etc.; or R3 and R4 together are part of a 4-7-membered ring) as Fatty Acid Binding Protein (“”FABP””) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity, or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. Synthetic procedures for preparing I are exemplified. Example compound II, prepared from 6,7-difluoro-3-hydroxyquinoxaline-2-carboxylic acid and racemic-2-(3-chlorobenzyl)pyrrolidine, had a TdF Kd value of 0.08 μM in an assay to demonstrate FABP inhibitory activity. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Application of 52537-00-5
The Article related to heterocyclic inhibitor fatty acid binding protein preparation therapy, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application of 52537-00-5
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles