98019-60-4Relevant articles and documents
SUBSTITUTED XANTHINES AND METHODS OF USE THEREOF
-
Page/Page column 400; 401, (2014/09/29)
Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.
NOVEL ANDROGENS
-
Page/Page column 32, (2010/02/14)
The compounds of the subject invention have a structure according to formula I: wherein X is S or SO2; R1 is (1C-6C)alkyl, (3C-6C)alkenyl, or (3C-6C)alkynyl, each optionally subst ituted with (3C-6C)cycloalkyl, OH, OC(O)(1C-4C)alkyl, (1C- 4C)alkoxy, halogen, cyano, formyl, C(O)(1C-4C)alkyl, CO2H, CO2(1C- 4C)alkyl, C(O)NR5R6, S(O)(1C-4C)alkyl or S(O)2(1C-4C)alkyl; R2 is hydrogen, (1C-4C)alkyl or C(O)(1C-4C)alkyl; R3 is a phenyl group optionally substituted with (1C-4C)alkyl, (1C-4C)fluoroalkyl, (1C-4C)alkoxy, (1C-4C)fluoroalkoxy, halogen, cyano or nitro; or R3 is a 5- or 6-membered aromatic heterocyclic ring structure optionally substituted with (1C-4C)alkyl, (1C-4C)fluoroalkyl, (1C-4C)alkoxy, halogen or cyano; R4 is a phenyl group or an aromatic 6-membered heterocycle, substituted at the ortho position with 1-hydroxy(1C-4C)alkyl, (1C-4C)alkoxy, C(O)(1C- 4C)alkyl, CO2(1C-4C)alkyl, C(O)NH2, cyano, nitro, or CH=NOR7, and optionally further substituted with (1C-2C)alkyl, (1C-2C)fluoroalkyl or halogen; R5 is 2-pyridyl optionally substituted with (1C-2C)alkyl, (1C- 2C)fluoroalkyl or halogen; or R5 and R6 are independently hydrogen or (1C-4C)alkyl; R7 is hydrogen or C(O)(1C-4C)alkyl; R8 , R9 , R10 are independently hydrogen, (1C-2C)alkyl, fluoro or chloro; or a salt or hydrate form thereof.
Regioisomeric 3-, 4- and 5-aminomethyl isoxazoles: Synthesis and muscarinic activity
Dannhardt,Kiefer,Lambrecht,Laufer,Mutschler,Schweiger,Striegel
, p. 839 - 850 (2007/10/03)
A series of 3-, 4- and 5-aminomethyl isoxazoles and isoxazoles with one or two additional methyl groups at the heterocycle were synthesized in order to investigate the structural requirements, ie heterocyclic moiety, regiochemistry and length of an aminoalkyl unit, for muscarinic activity. This was assayed on isolated rabbit vas deferens (M1 receptor subtype) and isolated guinea-pig atrium (M2 receptor subtype) and ileum (M3 receptor subtype). The isoxazoles tested are one to three orders of magnitude less active than furane or oxadiazole derivatives, having similar structural characteristics except for the heterocycle. Thus, the differences in molecular point charges and charge distribution contribute to the muscarinic activity of these compounds more than small differences in molecular shape and conformational energies.