1199782-88-1Relevant academic research and scientific papers
Identification of N-acyl-N-indanyl-α-phenylglycinamides as selective TRPM8 antagonists designed to mitigate the risk of adverse effects
Kobayashi, Jun-ichi,Hirasawa, Hideaki,Fujimori, Yoshikazu,Nakanishi, Osamu,Kamada, Noboru,Ikeda, Tetsuya,Yamamoto, Akitoshi,Kanbe, Hiroki
, (2020/12/21)
Transient receptor potential melastatin 8 (TRPM8), a temperature-sensitive ion channel responsible for detecting cold, is an attractive molecular target for the treatment of pain and other disorders. We have previously discovered a selective TRPM8 antagon
alpha-SUBSTITUTED GLYCINAMIDE DERIVATIVE
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Paragraph 0341-0342; 0346, (2016/05/24)
The present invention is to provide a novel α-substituted glycinamide derivative, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and a pharmaceutical use thereof. The present invention provides a compound represented by the general formula (I), which has TRPM8 inhibitory effects: [wherein A1 represents a C6-10 aryl and the like, A2 represents a C6-10 aryl and the like, X represents CH and the like, Y represents —CR1R2— and the like, R1 and R2 independently represent a hydrogen atom and the like, R3 and R4 independently represent a halogen atom and the like, n is 1 or 2], or a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing diseases or symptoms caused by hyperexcitability or disorder of afferent neurons.
[alpha]-substituted glycineamide derivative
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Page/Page column 34, (2016/10/07)
The present invention provides: a novel [alpha]-substituted glycineamide derivative or a pharmacologically acceptable salt thereof; a pharmaceutical composition containing the [alpha]-substituted glycineamide derivative or a pharmacologically acceptable salt thereof; and a use of the [alpha]-substituted glycineamide derivative or a pharmacologically acceptable salt thereof for medical purposes. The present invention provides a compound which has an inhibitory activity on TRPM8 and is represented by general formula (I) [wherein A1 represents a C6-10 aryl group or the like; A2 represents a C6-10 aryl group or the like; X represents CH or the like; Y represents -CR1R2- or the like; R1 and R2 independently represent a hydrogen atom or the like; R3 and R4 independently represent a halogen atom or the like; and n represents 1 or 2] or a pharmacologically acceptable salt thereof. The compound (I) according to the present invention can be used as a therapeutic or prophylactic agent for diseases or conditions associated with afferent nerve hyperexcitability or injury.
NOVEL TRPM8 INHIBITOR
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Paragraph 0100; 0102; 0107, (2016/10/09)
PROBLEM TO BE SOLVED: To provide a novel α-substituted glycine amide derivative, or a pharmaceutical composition containing pharmacologically acceptable salt thereof, and a medicinal use thereof. SOLUTION: The present invention provides a compound expressed by a general formula (I) having TRPM8 inhibitory action (in the formula, A1 denotes C6-10 aryl or the like, A2 denotes C6-10 aryl or the like, X denotes CH or the like, Y denotes -CR1R2- or the like, R1 and R2 denote hydrogen atom or the like independently, R3 and R4 denote halogen atom or the like independently, and n denotes 1 or 2), or a pharmaceutical composition containing pharmacologically acceptable salt thereof. Furthermore, a pharmaceutical composition of the present invention is usable as treatment or a prophylactic drug of disease or symptom caused by hyperexcitement or disorder of afferent nerves. SELECTED DRAWING: None COPYRIGHT: (C)2016,JPOandINPIT
