- 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
-
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).
- 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)
-
- HETEROCYCLIC COMPOUNDS AS PESTICIDES
-
The present application relates to thiadiazole compounds, compositions containing such compounds, their use for controlling animal pests including arthropods, insects and nematodes, and to processes and intermediates for the preparation of the thiadiazole compounds.
- -
-
Page/Page column 71
(2017/01/26)
-
- AROMATIC 5-MEMBERED HETEROCYCLIC DERIVATIVE HAVING TRPV4-INHIBITING ACTIVITY
-
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.
- -
-
Paragraph 0633-0635
(2015/02/19)
-
- AZOLE COMPOUNDS AS PIM INHIBITORS
-
The invention relates to bicyclic compounds of formulas I and Ia, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further em
- -
-
Page/Page column 186
(2012/10/08)
-
- Facile synthesis of substituted 5-amino- And 3-amino-1,2,4-thiadiazoles from a common precursor
-
[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
- Wehn, Paul M.,Harrington, Paul E.,Eksterowicz, John E.
-
supporting information; experimental part
p. 5666 - 5669
(2010/03/01)
-
- DERIVATlVES OF UREA AND RELATED DIAMINES, METHODS FOR THEIR MANUFACTURE AND USES THEREFOR
-
The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes
- -
-
Page/Page column 36
(2009/03/07)
-
