On March 15, 2018, Jiang, Lan; Morgans, David John; Bergne, Gustave; Chen, Chun; Li, Hui; Andre, Patrick; Halcomb, Randall Lynn; Cha, Jacob; Hom, Timothy published a patent.Category: naphthyridine The title of the patent was Preparation of N-acyl amino acid compounds as αvβ1 integrin inhibitors for treating tissue specific fibrosis. And the patent contained the following:
The invention is related to the preparation of compounds R1CONHCH(CO2H)CH2ALR2 [R1 = (un)substituted C6-14 aryl or C5-10-membered heteroaryl; R2 = (un)substituted 5- to 10-membered heteroaryl containing at least 2 ring N’s, 3- to 12-membered heterocyclyl containing at least 2 ring N’s, NHR3, etc.; R3 =(un)substituted 5- to 10-membered heteroaryl containing at least 1 ring N, or 3- to 12-membered heterocyclyl containing at least 1 ring N, wherein the 5- to 10- membered heteroaryl and 3- to 12-membered heterocyclyl; -A-L- = -A1-L1-,-A2-L2-, A3; A1 = (un)substituted C3-8 cycloalkyiene, C3-8 cycloalkenylene, C6-14 arylene, 5- to 10-membered heteroarylene or 3- to 12-membered heterocyclylene; A2 = = (un)substituted C3-8 cycloalkyiene, C3-8 cycloalkenylene; A3 = = (un)substituted C5-10 cycloalkyiene, C5-10 cycloalkenylene; L1 = OZ, (un)substituted saturated 3- to 4-membered heterocyclylene, OZX1, etc.; Z = CR5aR5b; R5a, R5b = independently H, C1-6 alkyl; X1 = (un)substituted C1-6 alkylene or C2-6 alkenylene; with the exception of specified compounds], e.g., I, that are αvβ1 integrin inhibitors, pharmaceutical compositions containing them and for treating tissue specific fibrosis. Thus, I was prepared by a multi-step synthesis starting from 2-aminonicotinaldehyde and Et 4-oxopentanoate using Me (2S)-2-[(benzyloxycarbonyl)amino]-3-(4-hydroxyphenyl)propanoate and benzoic acid. The compounds of the invention were tested for αvβ1 integrin inhibition in a cell adhesion assay and in a solid phase integrin αvβ1 binding assay. The experimental process involved the reaction of tert-Butyl 7-(2-hydroxyethyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxylate(cas: 445490-78-8).Category: naphthyridine
The Article related to acyl amino acid alpha v beta 1 integrin inhibitor, preparation acyl amino acid tissue specific fibrosis, Amino Acids, Peptides, and Proteins: Amino Acids and other aspects.Category: naphthyridine
Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem