124420-97-9Relevant academic research and scientific papers
NITROGEN-CONTAINING COMPOUNDS HAVING KINASE INHIBITORY ACTIVITY AND DRUGS CONTAINING THE SAME
-
, (2008/06/13)
An objective of the present invention is to provide compounds having Rho kinase inhibitory activity. The compounds according to the present invention are those represented by formula (I) or pharmaceutically acceptable salts or solvates thereof:Het-X-Z wherein Het represents a monocyclic or bicyclic heterocyclic group containing at least one nitrogen atom, for example, pyridyl or phthalimide; X represents group (i) -NH-C(=O)-NH-Q1-, group (ii) -NH-C(=O)-Q2-, wherein Q1 and Q2 represent a bond, alkylene, or alkenylene, or the like; and Z represents hydrogen, halogen, a monocyclic, bicyclic, or tricyclic carbocyclic group, a heterocyclic group or the like, for example, optionally substituted phenyl.
N-phenyl-N'-pyridinylureas as anticonvulsant agents
Pavia,Lobbestael,Taylor,Hershenson,Miskell
, p. 854 - 861 (2007/10/02)
A series of N-phenyl-N'-pyridinylureas was examined for anticonvulsant activity. Extensive structure/activity investigations revealed optimal activity in the N-(2,6-disubstituted-phenyl)-N'-(4-pyridinyl)urea series, with 37 exhibiting the best overall anticonvulsant profile. Compound 37 was effective against seizures induced by maximal electroshock but did not protect mice from clonic seizures produced by the convulsant pentylenetetrazol. The overall pharmacological profile suggests that 37 would be of therapeutic use in the treatment of generalized tonic-clonic and partial seizures. Compound 37 was selected for Phase 1 clinical trials.
