138113-73-2Relevant academic research and scientific papers
MONAMINE AND MONOAMINE DERIVATIVES AS INHIBITORS OF LEUKOTRIENE A4 HYDROLASE
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Paragraph 0248; 0250; 0259; 0261; 0285; 0287, (2018/06/29)
This present disclosure is directed to compounds of formula (I): where r, q, R1a, R1b, R1c, R1d, R1e, R2, R3, R4a, R5a, R5b, R6a, Rsu
LTA4 Hydrolase inhibitors
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Page 202, (2010/01/31)
The present invention provides compounds of the formula Ar1-Q-Ar2-Y-R-Z and pharmaceutically acceptable salts thereof wherein Ar1 and Ar2 are optionally substituted aryl moieties, Z is an optionally substituted nitrogen-containing moiety which may be an acyclic, cyclic or bicyclic amine or an optionally substituted monocyclic or bicyclic nitrogen-containing heteroaromatic moiety; Q is a linking group capable of linking two aryl groups; R is an alkylene moiety; Y is a linking moiety capable of linking an aryl group to an alkylene moiety and wherein Z is bonded to R through a nitrogen atom. The compounds and pharmaceutical compositions of the present invention are useful in the treatment of inflammatory diseases which are mediated by LTB4 production, such as proriasis, ulcerative colitis, IBD and asthma.
Structure-activity relationship studies on 1-[2-(4- phenylphenoxy)ethyl]pyrrolidine (SC-22716), a potent inhibitor of leukotriene A4 (LTA4) hydrolase
Penning, Thomas D.,Chandrakumar, Nizal S.,Chen, Barbara B.,Chen, Helen Y.,Desai, Bipin N.,Djuric, Stevan W.,Docter, Stephen H.,Gasiecki, Alan F.,Haack, Richard A.,Miyashiro, Julie M.,Russell, Mark A.,Yu, Stella S.,Corley, David G.,Durley, Richard C.,Kilpatrick, Brian F.,Parnas, Barry L.,Askonas, Leslie J.,Gierse, James K.,Harding, Elizabeth I.,Highkin, Maureen K.,Kachur, James F.,Kim, Suzanne H.,Krivi, Gwen G.,Villani-Price, Doreen,Pyla, E. Yvonne,Smith, Walter G.,Ghoreishi-Haack, Nayereh S.
, p. 721 - 735 (2007/10/03)
Leukotriene B4 (LTB4) is a pro-inflammatory mediator that has been implicated in the pathogenesis of a number of diseases including inflammatory bowel disease (IBD) and psoriasis. Since the action of LTA4 hydrolase is the rate-limiting step for LTB4 production, this enzyme represents an attractive pharmacological target for the suppression of LTB4 production. From an in- house screening program, SC-22716 (1, 1-[2-(4- phenylphenoxy)ethyl]pyrrolidine) was identified as a potent inhibitor of LTA4 hydrolase. Structure-activity relationship (SAR) studies around this structural class resulted in the identification of a number of novel, potent inhibitors of LTA4 hydrolase, several of which demonstrated good oral activity in a mouse ex vivo whole blood assay.
Pyrimidine derivatives and fungicides and/or acaricides containing them as active ingredient
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, (2008/06/13)
A compound which is effective as an active ingredient of fungicides and/or acaricides, and is represented by the formula and a method for preparing the same are provided: STR1 wherein R1 and R2 are bonded together at their termini and represent trimethylene or teramethylene, R3 represents a hydrogen atom, a lower alkyl group or a halogen atom, R4 represents a hydrogen atom or a lower alkyl group, R5 represents a hydrogen atom, a lower alkyl group or a methylthio group and n represents 2 or 3.
