- 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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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.
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Page/Page column 5
(2010/02/14)
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- Novel sPLA2 inhibitors
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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.
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Page/Page column 22
(2010/11/30)
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- Novel sPLA2 inhibitors
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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.
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- Combination therapy for the treatment of inflammatory and respiratory diseases
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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.
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- Process for preparing toluenesulfinates
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A process for preparing novel compounds useful in the preparation of 1H-indole-3-glyoxamides.
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- SPLA2 inhibitor compounds for treatment of disease
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The present invention is directed to compounds for treating inflammatory bowel disease. More specifically, the present invention is directed to 1H-indole-3-glyoxyamide compounds a sPLA2inhibitors for treating inflammatory bowel disease.
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- Method for the treatment of stroke using N-heterocyclic glyoxlyamide compounds
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A method and composition for the treatment and/or prevention of stroke is disclosed using N-heterocyclic glyoxamide compounds having the following general formula: wherein X, E, F, R11, R12, R14, R15, R16and R17are as defined herein.
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- Process for preparing 4-substituted-1h-indole-3-glyoxamides
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A process for preparing 1H-indole-3-glyoxamides useful for inhibiting SPLA2and novel intermediates useful in the preparation of such compounds.
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- Morpholino-n-ethyl ester derivative of an indole sPLA2 inhibitor
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The compound, ((3-(2-amino-1,2-dioxoethyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl)oxy)acetic acid morpholino-N-ethyl ester, is disclosed together with its use as a highly bioavailable indole compound for inhibiting sPLA2 mediated release of fatty acids fo
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- Method for treatment of chronic bronchitis using indole compounds
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A method is disclosed for the treatment of chronic bronchitis by administering to a mammal in need thereof a therapeutically effective amount of a 1H-indole-3-glyoxylamide compound.
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- Process for preparing 4-substituted-1H-indole-3-glyoxamides
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A process for preparing 1H-indole-3-glyoxamides useful for inhibiting SPLA2 and novel intermediates useful in the preparation of such compounds.
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- Process for preparing 4-substituted-1H-indole-3-glyoxamides
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A process for preparing 1H-indole-3-glyoxamides useful for inhibiting SPLA2 and novel intermediates useful in the preparation of such compounds.
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- 1H-INDOLE-3-GLYOXYLAMIDE SPLA2 INHIBITORS
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A class of novel 1H-indole-3-glyoxylamides is disclosed together with the use of such indole compounds for inhibiting sPLA2 mediated release of fatty adds for treatment of conditions such as septic shock
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- Indole inhibitors of human nonpancreatic secretory phospholipase A2. 3. Indole-3-glyoxamides
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The preceding papers of this series detail the development of functionalized indole-3-acetamides as inhibitors of hnps-PLA2. We describe here the extension of the structure-activity relationship to include a series of indole-3-glyoxamide derivatives. Functionalized indole-3-glyoxamides with an acidic substituent appended to the 4- or 5-position of the indole ring were prepared and tested as inhibitors of hnps-PLA2. It was found that the indole-3-glyoxamides with a 4-oxyacetic acid substituent had optimal inhibitory activity. These inhibitors exhibited an improvement in potency over the best of the indole-3-acetamides, and LY315920 (6m) was selected for evaluation clinically as an hnps-PLA2 inhibitor.
- Draheim, Susan E.,Bach, Nicholas J.,Dillard, Robert D.,Berry, Dennis R.,Carlson, Donald G.,Chirgadze, Nickolay Y.,Clawson, David K.,Hartley, Lawrence W.,Johnson, Lea M.,Jones, Noel D.,McKinney, Emma R.,Mihelich, Edward D.,Olkowski, Jennifer L.,Schevitz, Richard W.,Smith, Amy C.,Snyder, David W.,Sommers, Cynthia D.,Wery, Jean-Pierre
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p. 5159 - 5175
(2007/10/03)
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