On December 6, 2018, Fan, Pingchen; Lange, Christopher W.; Lui, Rebecca M.; Malathong, Viengkham; Mali, Venkat Reddy; Punna, Sreenivas; Singh, Rajinder; Tanaka, Hiroko; Zeng, Yibin; Zhang, Penglie published a patent.Category: pyrimidines The title of the patent was 6-5 Fused ring as C5a inhibitors and their preparation. And the patent contained the following:
The disclosure provides, inter alia, compounds of formula I or pharmaceutically acceptable salts thereof that are modulators of the C5a receptor. Also provided are pharmaceutical compositions and methods of use including the treatment of diseases or disorders involving pathol. activation from C5a and non-pharmaceutical applications. Compounds of formula I wherein A0 is Nh and CO; A1 and A3 are independently N, NH, CH, CO and CR4; A2, A5 and A6 are independently N, CH and CR4; A4 is N, NC1-4 alkyl, CH and CR4; provided that no more than two of A3, A4, A5 and A6 are N; dashed bonds are single and double bonds; n is 0, 1, 2 and 3; R1 is heteroaryl, C6-10 aryl, C1-8 alkylene-heteroaryl, etc.; each R2a is independently C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, etc.; each R2b is independently H, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, CN, etc.; each R3 is independently C1-4 alkyl, C1-4 haloalkyl, and OH; two R3 groups can be taken together to form oxo; each R4 is independently C1-6 alkyl, C1-6 alkoxy, C1-6 hydroxyalkyl, halo, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their C5a inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of < 5 nM. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Category: pyrimidines
The Article related to indazole preparation c5a inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Category: pyrimidines
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia