160388-53-4Relevant articles and documents
Pyrrolidin-3-yl-N-methylbenzamides as potent histamine 3 receptor antagonists
Zhou, Dahui,Gross, Jonathan L.,Sze, Jean Y.,Adedoyin, Adedayo B.,Bowlby, Mark,Di, Li,Platt, Brian J.,Zhang, Guoming,Brandon, Nicholas,Comery, Thomas A.,Robichaud, Albert J.
scheme or table, p. 5957 - 5960 (2011/10/18)
On the basis of the previously reported benzimidazole 1,3′- bipyrrolidine benzamides (1), a series of related pyrrolidin-3-yl-N- methylbenzamides were synthesized and evaluated as H3 receptor antagonists. In particular, compound 32 exhibits pot
AZACYCLYLBENZAMIDE DERIVATIVES AS HISTAMINE-3 ANTAGONISTS
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Page/Page column 40, (2009/01/20)
The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor
FIBROSIS INHIBITOR
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, (2008/06/13)
Medicament being useful as a fibrosis inhibitor for organs or tissues, which comprises a compound of the formula (I): wherein Ring Z is optionally substituted pyrrole ring, etc.; W2 is -CO-, -SO2-, optionally substituted C1-C4 alkylene, etc.; Ar2 is optionally substituted aryl, etc.; W1 and Ar1 mean the following (1) and (2):(1) W1 is optionally substituted C1-C4 alkylene, etc.; Ar1 is optionally substituted bicyclic heteroaryl having 1 to 4 nitrogen atoms as ring-forming atoms:(2) W1 is optionally substituted C2-C5 alkylene, optionally substituted C2-C5 alkenylene, etc.; and Ar1 is aryl or monocyclic heteroaryl, which is substituted by carboxyl, alkoxycarbonyl, etc. at the ortho- or meta-position thereof with respect to the binding position of W1, or a pharmaceutically acceptable salt thereof.
Pyrrole derivatives
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, (2008/06/13)
Pyrrole derivatives represented by the following formula: wherein Ring Z is an optionally substituted pyrrole ring, etc.; W2 is —CO—, —SO2—, an optionally substituted C1-C4 alkylene, etc.; Ar2 is an optionally substituted aryl, etc.; W2 and Ar1 mean the following (1) and (2): (1) W1 is an optionally substituted C1-C4 alkylene, etc.; Ar1 is an optionally substituted bicyclic heteroaryl having 1 to 4 nitrogen atoms as ring-forming atoms: (2) W1 is an optionally substituted C2-C5 alkylene, an optionally substituted C2-C5 alkenylene, etc.; and Ar1 is an aryl or monocyclic heteroaryl, which are substituted by carboxyl, an alkoxycarbonyl, etc. at the ortho- or meta-position thereof with respect to the binding position of W1, or a pharmaceutically acceptable salt thereof These compounds are useful as medicaments such as a fibrosis inhibitor for organs or tissues.
A structure-Permeability study of small drug-like molecules
Fichert, Thomas,Yazdanian, Mehran,Proudfoot, John R.
, p. 719 - 722 (2007/10/03)
A systematic structure-permeability relationship study on a set of small drug-like molecules with log D values in the range -2.5 to 3 and carrying a diverse array of functionality reveals that the compounds with log D>0 and 3 are highly permeable. Surprisingly, several tetrazole derivatives were found to be substrates for efflux pump(s).
Non-steroidal antiinflammatory agents. Synthesis and enzyme inhibition of 2-[4-(heteroarylmethyl)phenyl]propanoic acids and analogues
Silvestri,Pagnozzi,Valoti,Fusi
, p. 625 - 632 (2007/10/02)
Some 2-[4-(heteroarylmethyl)phenyl]propanoic acids and phenylacetic and benzoic analogues have been synthesized. All above acids were tested for their inhibitory activity on lipoxygenase and cyclooxygenase, in comparison with NDGA and tolmetin. 2-[4-(Thie
