66361-80-6Relevant articles and documents
Conformationally constrained analogues of N′-(4-tert-butylbenzyl)-N-(4-methylsulfonylaminobenzyl)thiourea as TRPV1 antagonists
Lim, Ju-Ok,Jin, Mi-Kyoung,Ryu, HyungChul,Kang, Dong Wook,Lee, Jeewoo,Pearce, Larry V.,Tran, Richard,Toth, Attila,Blumberg, Peter M.
experimental part, p. 322 - 331 (2009/04/07)
A series of bicyclic analogues having indan and tetrahydronaphthalene templates in the A-region were designed as conformationally constrained analogues of our previously reported potent TRPV1 antagonists (1, 3). The activities for rat TRPV1 of the conformationally restricted analogues were moderately or markedly diminished, particularly in the case of the tetrahydronaphthalene analogues. The analysis indicated that steric constraints at the benzylic position in the bicyclic analogues may be an important factor for their unfavorable interaction with the receptor.
1-aminomethyl-1,2,3,4-tetrahydronaphthalenes
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, (2008/06/13)
The present invention provides compounds of the formula STR1 or a pharmaceutically acceptable salt thereof wherein R1 is selected from hydrogen, halo, lower alkyl, lower alkoxy, or thioalkoxy; and R2 is lower alkoxy; or R1 and R2 together form a methylenedioxy or ethylenedioxy ring; R3 and R4 are independently selected from hydrogen, hydroxy, lower alkyl, lower alkoxy, lower alkylthio, (lower alkyl)amino, (lower alkylsulfonyl)amino, and halo; and R7 is selected from the group consisting of 2- or 3-thienyl, 2- or 3-furyl, and STR2 where R13 and R14 are independently selected from the group consisting of hydrogen, hydroxy, halogen, amino, lower alkyl, lower alkoxy, lower alkylthio, methylenedioxy, or ethylenedioxy. The compounds of the present invention selectively inhibit α2 -adrenergic receptors as well as inhibit the uptake of biogenic amines and are thus useful in the treatment of certain cardiovascular and psychiatric disorders.