On January 27, 2022, Wu, Hao; Wu, Wenmao; Li, Ling; Zhang, Zhan; Wang, Feng; Yuan, Ding; Wu, Yunfei; Chen, Qiang; Han, Han; Guo, Jing; Lan, Hong; Ding, Lieming; Wang, Jiabing published a patent.Category: amides-buliding-blocks The title of the patent was Piperidine-spiro-fused heterocyclic compounds as SHP2 inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:
The invention relates to piperidine-spiro-fused heterocyclic compounds of formula I, which are serving as an Src homol. region 2-containing protein tyrosine phosphatase 2 (SHP2) inhibitors, as well as to their pharmaceutical compositions thereof, the preparation method therefor, and the use in treating an SHP2 mediation disease. The compounds of formula I exert effects by means of participating in the regulation of multiple processes such as cell proliferation, apoptosis, migration, and angiogenesis. Compounds of formula I wherein the dotted double bond is either a single bond, or a double bond; ring A is (un)saturated 5- to 10-membered (hetero)cyclic ring; ring C is (un)saturated 5- to 10-membered heterocyclic ring, C6-10 aryl, 5- to 10-membered heteroaryl; each Rc is independently H, halo, CN, NO2, SF5, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, etc.; two of the Rc may be taken together with the atom attached to form C3-8 cycloalkyl, 3- to 10-membered heterocyclic ring, C6-10 aryl, 5- to 10-membered heteroaryl, etc.; T is (CRc1Rc2)0-3; Rc1 and Rc2 are independently H, halo, C1-4 alkly, -OR5; Rc1Rc2 may be taken together with the atom attached to form C3-6 cycloalkyl, 3- to 6-membered heterocyclic ring; each R1 is independently H, halo, CN, NO2, C1-6 alkyl, C2-4 alkenyl, C2-4 alkynyl, C3-6 cycloalkyl, etc.; X is O, NH and derivatives, SO0-2, CO, -CO-O-, -CO-NH- and derivatives, etc.; M is O, NH and derivatives, (un)substituted CH; Y1 and Y2 are independently NH and derivatives, (un)substituted CH; each R4 is independently H, halo, CN, NO2, C1-8 alkyl, C2-8 alkenyl, etc.; R5 is H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkenyl, etc.; and their pharmaceutically acceptable salts, deuterium,stereoisomers, chelates, prodrugs as SHP2 inhibitors in the treatment of diseases thereof, are claimed. Example compound II was prepared by using spirocyclization, imination, reduction, cross-coupling as the key steps. All the invention compounds were evaluated for their SHP2 inhibitory activity. The experimental process involved the reaction of 2-Fluoro-4-hydroxybenzamide(cas: 1133122-96-9).Category: amides-buliding-blocks
The Article related to piperidine spiro fused heterocyclic preparation shp2 inhibitor treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Category: amides-buliding-blocks
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics