On March 15, 2005, Mavunkel, Babu J.; Chakravarty, Sarvajit; Perumattam, John J.; Dugar, Sundeep; Lu, Qing; Liang, Xi published a patent.Recommanded Product: 256935-86-1 The title of the patent was Preparation of indolylcarboxamide derivatives as inhibitors of p38 kinase. And the patent contained the following:
Title compounds I [X independently = CA, CR4A, CR5, CR52, NR6, or N; L1 = CO, SO2, or alkylene; L2 = (un)substituted-alkylene or -alkenylene; Ar = (un)substituted aryl group with substituents consisting of alkyl, alkenyl, halo, CN, etc.; Z = N or CR7 wherein R7 = H or non-interfering substituent; R1 = H, alkyl, alkenyl, alkynyl, aryl, arylalkyl, etc.; R2 independently = halo, alkyl, OH, alkoxy, etc.; R3 independently = CN, CF3, NO2, alkyl, aryl, acyl, etc.; R4 = H, halo, alkyl or alkenyl; R5 independently = H, halo, alkyl, OH, etc.; R6 = H, alkyl, alkenyl, aryl, acyl, aroyl, etc.; A = -WiCOXjY wherein Y is COR8 wherein R8 = H, (un)substituted-alkyl, -alkenyl, -alkynyl, etc.; W and X = (un)substituted-alkylene, -alkenylene, -alkynylene; Y = tetrazole, 1,2,3-triazole, 1,2,4-triazole, or imidazole and each of i and j independently = 0 or 1; m = 0-4; n = 0-3], and their pharmaceutically acceptable salts are prepared and disclosed as useful for treatment of rheumatoid arthritis. Thus, e.g., II, was prepared by carbonylation of 6-methoxy-(4-benzylpiperidinyl)-indole-5-carboxamide with oxalyl chloride and subsequent amination using 4-methylpiperazine. ELISA assays for evaluation of inhibition of p38 kinase by I revealed that all compounds of the invention possessed IC50 values in the range of 0.1-1.5 μM. I as inhibitors of p38 kinase should prove useful in the treatment of rheumatoid arthritis. The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).Recommanded Product: 256935-86-1
The Article related to indolylcarboxamide derivative preparation p38 kinase inhibitor antirheumatic agent, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Recommanded Product: 256935-86-1
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