On January 23, 2020, Accetta, Alessandro; Rancati, Fabio; Capelli, Anna Maria; Clark, David Edward; Tisselli, Patrizia; Edwards, Christine; Cheguillaume, Arnaud Jean Francois Auguste; Bhalay, Gurdip published a patent.Name: 4-Benzenesulfonylpiperidine Hydrochloride The title of the patent was Preparation of tyrosine amide derivatives as Rho-kinase inhibitors. And the patent contained the following:
The invention relates to compounds of formula I and pharmaceutically acceptable salts and solvates thereof, wherein X1 and X2 are independently CH and N; p = 1 – 3; each R when present is halo; R0 and R1 are independently H, halo, CN, etc.; R2 and R3 are independently H, C1-6 alkyl, haloalkyl, hydroxyalkyl, aminoalkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl; R4 and R5 are independently H, C1-6 alkyl;R6 is H, alkyl, haloalkyl; were prepared and used as Rho kinase inhibitors. Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH). Example compound II was prepared. The invention compounds were evaluated for their Rho-associated protein kinase ROCK1 and ROCK2 inhibitory activities. From the assay, it was determined that compound II exhibited Ki value of < 3 nM. The experimental process involved the reaction of 4-Benzenesulfonylpiperidine Hydrochloride(cas: 1172500-91-2).Name: 4-Benzenesulfonylpiperidine Hydrochloride
The Article related to human, asthma chronic obstructive pulmonary idiopathic fibrosis hypertension, rho kinase inhibitor tyrosine amide amino acid preparation copd, tyrosine amide rho kinase inhibitor preparation rock1 rock2 pulmonary and other aspects.Name: 4-Benzenesulfonylpiperidine Hydrochloride
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem