85386-84-1Relevant articles and documents
Benzimidazoles that are useful in treating sexual dysfunction
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, (2008/06/13)
The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction, wherein L is C1-4 alkyl;RA, RB, RC, RD, and RE, are as described in the specification;Z is selected from the group consisting of N, C and CH; andA is aryl and heteroaryl as described in the specification.
Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction
Cowart, Marlon,Latshaw, Steven P.,Bhatia, Pramila,Daanen, Jerome F.,Rohde, Jeffrey,Nelson, Sherry L.,Patel, Meena,Kolasa, Teodozyi,Nakane, Masaki,Uchic, Marie E.,Miller, Loan N.,Terranova, Marc A.,Chang, Renjie,Donnelly-Roberts, Diana L.,Namovic, Marian T.,Hollingsworth, Peter R.,Martino, Brenda R.,Lynch III, James J.,Sullivan, James P.,Hsieh, Gin C.,Moreland, Robert B.,Brioni, Jorge D.,Stewart, Andrew O.
, p. 3853 - 3864 (2007/10/03)
A new class of agents with potential utility for the treatment of erectile dysfunction has been discovered, guided by the hypothesis that selective D 4 agonists are erectogenic but devoid of the side effects typically associated with dopaminergic agents. The lead agent 2-(4-pyridin-2-ylpiperazin- 1-ylmethyl)-1H-benzimidazole (1, ABT-724) was discovered by optimization of a series of benzimidazole arylpiperazines. This highly selective D4 agonist was found to be very potent and efficacious in vivo, eliciting penile erections in rats at a dose of 0.03 μmol/kg, with a positive response rate of 77% erectile incidence. Even at high doses, it was devoid of side effects in animal models of central nervous system behaviors, emesis, or nausea. The structure-activity relationship of the parent benzimidazole series leading to 1 is described, with the detailed in vitro and in vivo profiles described. Distinctive structural features were discovered that are associated with D 4 selective agonism in this series of analogues.
Benzimidazoles that are useful in treating sexual dysfunction
-
, (2008/06/13)
The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
Benzimidazoles that are useful in treating sexual dysfunction
-
, (2008/06/13)
The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
Benzimidazoles that are useful in treating sexual dysfunction
-
, (2008/06/13)
The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
Benzimidazoles that are useful in treating sexual dysfunction
-
, (2008/06/13)
The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
Pyridinylpiperazines, a new class of selective α2-adrenoceptor antagonists
Saari, Walfred S.,Halczenko, Wasyl,King, Stella W.,Huff, Joel R.,Guare, James P.,et al.
, p. 1696 - 1701 (2007/10/02)
A series of 1-(2-pyridinyl)piperazine derivatives was synthesized and evaluated for adrenergic activity. In vitro activity was assessed through the antagonism of clonidine's effect in the rat, isolated, field-stimulated vas deferens and by the displacemen
