850697-57-3Relevant academic research and scientific papers
Novel N-substituted benzimidazolones as potent, selective, CNS-penetrant, and orally active M1 mAChR agonists
Budzik, Brian,Garzya, Vincenzo,Shi, Dongchuan,Walker, Graham,Woolley-Roberts, Marie,Pardoe, Joanne,Lucas, Adam,Tehan, Ben,Rivero, Ralph A.,Langmead, Christopher J.,Watson, Jeannette,Wu, Zining,Forbes, Ian T.,Jin, Jian
, p. 244 - 248 (2010)
Virtual screening of the corporate compound collection yielded compound 1 as a subtype selective muscarinic M1 receptor agonist hit. Initial optimization of the N-capping group of the central piperidine ring resulted in compounds 2 and 3 with s
1-(1-CYCLOBUTYL-4-PIPERIDINYL)-1,3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE DERIVATIVES WHICH HAVE ACTIVITY ON THE ML RECEPTOR AND THEIR USE IN MEDICINE
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Page/Page column 57-58, (2008/12/04)
Compounds of formula I or a salt thereof are provided wherein R4, R5, R6, Q, L and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders and cognitive impairments are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
BENZIMIDAZOLONES WHICH HAVE ACTIVITY AT Ml RECEPTOR
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Page/Page column 46, (2008/06/13)
Compounds of formula (I) and salts and solvates are provided: wherein R6 is selected from hydrogen, halogen, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C3-6cycloalkyl, C3-6cycloalkyl substituted with one or more fluorine atoms, C1-6 alkoxy, C1-6 alkoxy substituted with one or more fluorine atoms, and cyano, and Q is hydrogen or C1-6alkyl. The compounds are M1 agonists and are useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.
Discovery and SAR studies of a novel series of noncovalent cathepsin S inhibitors
Gustin, Darin J.,Sehon, Clark A.,Wei, Jianmei,Cai, Hui,Meduna, Steven P.,Khatuya, Haripada,Sun, Siquan,Gu, Yin,Jiang, Wen,Thurmond, Robin L.,Karlsson, Lars,Edwards, James P.
, p. 1687 - 1691 (2007/10/03)
A novel series of competitive, reversible cathepsin S (CatS) inhibitors was discovered and optimized. The 4-(2-keto-1-benzimidazolinyl)-piperidin-1-yl moiety was found to be an effective replacement for the 4-arylpiperazin-1-yl group found in our earlier series of CatS inhibitors. This replacement imparted improved PK properties as well as decreased off-target activity. Optimization of the ketobenzimidazole moiety led to the discovery of the lead compound JNJ 10329670, which represents a novel class of selective, noncovalent, reversible, and orally bioavailable inhibitors of cathepsin S.
