164082-80-8Relevant articles and documents
Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2
Oslund, Rob C.,Cermak, Nathan,Gelb, Michael H.
supporting information; experimental part, p. 4708 - 4714 (2009/06/06)
We report a series of inhibitors of secreted phospholipases A2 (sPLA2s) based on substituted indoles, 6,7-benzoindoles, and indolizines derived from LY315920, a well-known indole-based sPLA2 inhibitor. Using the human group X sPLA2 crystal structure, we prepared a highly potent and selective indole-based inhibitor of this enzyme. Also, we report human and mouse group IIA and IIE specific inhibitors and a substituted 6,7-benzoindole that inhibits nearly all human and mouse sPLA 2s in the low nanomolar range.
Regioselective synthesis of 4- and 7-alkoxyindoles from 2,3-dihalophenols: Application to the preparation of indole inhibitors of phospholipase A 2
Sanz, Roberto,Castroviejo, M. Pilar,Guilarte, Veronica,Perez, Antonio,Fananas, Francisco J.
, p. 5113 - 5118 (2008/02/05)
(Chemical Equation Presented) An efficient and regioselective synthesis of 4- and 7-alkoxyindoles has been developed from commercially available starting materials such as 3-halophenols and 3-chloroanisole. Directed ortho-metalation followed by two pallad
PHARMACEUTICAL COMPOSITIONS CONTAINING THE PHOSPHOLIPASE INHIBITOR SODIUM 3-(2-AMINO-1,2-DIOXOETHYL)-2-ETHYL-1-PHENYLMETHYL)-1H-INDOL-4-YL]OXY]ACETATE
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Page/Page column 5, (2010/02/14)
A lyophilized pharmaceutical composition is described which contains Sodium [[3-(2-amino-1,2-dioxoethyl)-2-ethyl-1-phenylmethyl)-1H-indol-4-yl]oxy]acetate, a Solubilizer, and a Stabilizer. Such compositions are storage stable and readily dissolve in aqueous medium to give injectable solution for treatment of sepsis, etc.
Novel sPLA2 inhibitors
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Page/Page column 21-22, (2010/11/30)
A class of novel indole is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.
Novel sPLA2 inhibitors
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, (2008/06/13)
A class of novel indole is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.
Method for the treatment of renal dysfunction with spla2 inhibitors
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, (2008/06/13)
A method is disclosed for the treatment of of the symptoms associated with renal dysfunction by administering to an animal in need thereof a therapeutically effective amount of a sPLA2 inhibitor, such as a 1H-indole-3-glyoxylamide.
METHOD FOR TRATMENT OF NON-RHEUMATOID ARTHRITIS
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, (2008/06/13)
A method is disclosed for the treatment of non-rheumatoid arthritis by administering to a mammal in need thereof a therapeutically effective amount of an sPLA 2 inhibitor.
Indole sPLA2 inhibitors
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, (2008/06/13)
A class of novel acylsulfonamide substituted indole compounds is disclosed together with the use of such compounds for inhibiting sPLA2mediated release of fatty acids for treatment of inflammatory diseases.
Method for the treatment of cystic fibrosis
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, (2008/06/13)
A method is disclosed for the treatment of cystic fibrosis by administering to a human in need thereof a therapeutically effective amount of an sPLA2inhibitor, such as a 1H-indole-3-glyoxylamide.
Combination therapy for the treatment of inflammatory and respiratory diseases
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, (2008/06/13)
A pharmaceutical composition for the treatment of Inflammatory Disease or Respiratory Disease in mammals, which comprises, as active ingredients, a neutrophil elastase inhibitor and an sPLA2 inhibitor.