1101173-93-6Relevant articles and documents
Pharmacological evaluation of novel (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives as TRPV4 antagonists for the treatment of pain
Tsuno, Naoki,Yukimasa, Akira,Yoshida, Osamu,Suzuki, Shinji,Nakai, Hiromi,Ogawa, Tomoyuki,Fujiu, Motohiro,Takaya, Kenji,Nozu, Azusa,Yamaguchi, Hiroki,Matsuda, Hidetoshi,Funaki, Satoko,Yamanada, Natsue,Tanimura, Miki,Nagamatsu, Daiki,Asaki, Toshiyuki,Horita, Narumi,Yamamoto, Miyuki,Hinata, Mikie,Soga, Masahiko,Imai, Masayuki,Morioka, Yasuhide,Kanemasa, Toshiyuki,Sakaguchi, Gaku,Iso, Yasuyoshi
, p. 2177 - 2190 (2017/03/23)
A novel series of (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives were identified as selective transient receptor potential vanilloid 4 (TRPV4) channel antagonist and showed analgesic effect in Freund's Complete Adjuvant (FCA) induced mechanical hyperalgesia model in guinea pig and rat. Modification of right part based on the compound 16d which was disclosed in our previous communication led to the identification of compound 26i as a flagship compound. In this paper, we described the details about design, synthesis and structure-activity relationship (SAR) analysis at right and left part of these derivatives (Fig. 1).
AROMATIC 5-MEMBERED HETEROCYCLIC DERIVATIVE HAVING TRPV4-INHIBITING ACTIVITY
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Paragraph 0633-0635, (2015/02/19)
The present invention is related to a compound represented by formula (I) wherein R1 is a hydrogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted aromatic carbocyclyl, or the like; X is —N(R3)—, —O—, or —S—; Y is ═C(R4)—, or ═N—; Z is —N(R7)—, —O—, or —S—; R2 is substituted or unsubstituted alkyloxy, or the like, or a group represented by the following formula: —(CR2aR2b)n—R2c, wherein R2a is each independently a hydrogen atom, halogen, or the like; R2b is each independently a hydrogen atom, halogen, or the like; R2a and R2b which are attached to the same carbon atom may be taken together to form oxo, a substituted or unsubstituted non-aromatic carbocycle, or the like; two of R2a which are attached to the adjacent carbon atoms and/or two of R2b which are attached to the adjacent carbon atoms may be taken together to form a bond; R2c is substituted or unsubstituted aromatic carbocyclyl, or the like; n is an integer from 1 to 3; R3 and R7 are each independently a hydrogen atom, substituted or unsubstituted alkyl, or the like; R4 and R5 are each independently a hydrogen atom, halogen, substituted or unsubstituted alkyl, or the like; R6 is a hydrogen atom, halogen, substituted or unsubstituted alkyl, or the like, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising thereof.
Facile synthesis of substituted 5-amino- And 3-amino-1,2,4-thiadiazoles from a common precursor
Wehn, Paul M.,Harrington, Paul E.,Eksterowicz, John E.
supporting information; experimental part, p. 5666 - 5669 (2010/03/01)
[Chemical Equation Presented] A novel approach to the synthesis of substituted 5-amino- and 3-amino-1,2,4-thiadiazoles beginning from a common precursor has been achieved. Derivatization by palladium-catalyzed Suzuki-Miyaura coupling enables the rapid pre