167758-88-5Relevant articles and documents
Pyridazone derivative and its uses
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Paragraph 0109, (2022/01/12)
The present invention belongs to the pharmaceutical field, specifically relates to a pyridazone derivative and its uses, compounds thereof and pharmaceutically acceptable salts, solvates including hydrates, polycrystallines, prodrugs, co-crystallines, tau
Influenza virus replication inhibitor and uses thereof
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Paragraph 0500; 0502-0504, (2020/05/05)
The invention belongs to the field of medicines, and particularly relates to a new compound serving as an influenza virus replication inhibitor, a preparation method thereof, a pharmaceutical composition containing the compound, and application of the compound and the pharmaceutical composition in the treatment of influenza. The compound is a compound shown in a formula (I) or a stereoisomer, a tautomer, oxynitride, a solvate, a metabolite, a pharmaceutically acceptable salt or prodrugs of the compound shown in the formula (I). The compound can well inhibit influenza viruses, and/or has lowercytotoxicity, more excellent in-vivo metabolic dynamics properties and in-vivo pharmacodynamic properties.
INFLUENZA VIRUS REPLICATION INHIBITOR AND USES THEREOF
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Paragraph 00190; 00283-00284, (2020/05/21)
The invention belongs to the field of medicine, and particularly relates to a novel compound as a replication inhibitor of influenza virus and a preparation method thereof, a pharmaceutical composition comprising the compound and use of the compound and pharmaceutical composition thereof in treating influenza. The present invention provides a compound having Formula (I) or a stereoisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, The compound of the present invention can inhibit influenza virus well, and/or has lower cytotoxicity, better in vivo pharmacokinetic properties and in vivo pharmacodynamic properties.
Design, synthesis, and pharmacological evaluation of 4-azolyl-benzamide derivatives as novel GPR52 agonists
Tokumaru, Kazuyuki,Ito, Yoshiteru,Nomura, Izumi,Nakahata, Takashi,Shimizu, Yuji,Kurimoto, Emi,Aoyama, Kazunobu,Aso, Kazuyoshi
, p. 3098 - 3115 (2017/05/24)
G protein-coupled receptor 52 (GPR52) agonists are expected to improve the symptoms of psychiatric disorders. During exploration for a novel class of GPR52 agonists with good pharmacokinetic profiles, we synthesized 4-(3-(3-fluoro-5-(trifluoromethyl)benzyl)-5-methyl-1H-1,2,4-triazol-1-yl)-2-methylbenzamide (4u; half maximal effective concentration (EC50)?=?75?nM, maximal response (Emax)?=?122%) starting from a high-throughput screening hit 3 (EC50?=?470?nM, Emax?=?56%). The structural features of a reported GPR52 agonist were applied to 3, led to design 4-azolylbenzamides as novel GPR52 agonists. A structure–activity relationship study of 4-azolylbenzamide resulted in the design of the 1,2,4-triazole derivative 4u, which demonstrated excellent bioavailability in rats (F?=?53.8%). Oral administration of 4u (10?mg/kg) significantly suppressed methamphetamine-induced hyperlocomotion in mice. Thus, 4u is a promising lead compound for drug discovery research of GPR52 agonists.
Novel cyclic amide derivatives
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, (2008/06/13)
Novel compounds represented by the following formula (I) that act as a ligand to sigma receptor/binding cite and a medicament comprising the same as an active ingredient: wherein X represents an alkyl group, an aryl group, a heterocyclic group or the like; Q represents a group represented by —CH2—, —CO—, —O—, —CH(OR7)— or the like wherein R7 represents a hydrogen atom, an alkyl group or the like; n represents an integer of from 0 to 5; R1 and R2 each represent a hydrogen atom, an alkyl group or the like; B represents either of the following groups: wherein R3, R4, R5, and R6 each represent a hydrogen atom, a halogen atom, an alkoxyl group or the like; m represents 1 or 2; and the ring of: represents an aromatic heterocyclic ring.