SUBSTITUTED 5-HYDROXYINDOLE COMPOUNDS AS MODULATORS OF ALPHA-1 ANTITRYPSIN
Novel compounds, compositions, and methods of using and preparing the same, which may be useful for treating alpha-1 antitrypsin deficiency (AATD).
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Paragraph 00141; 00187
(2021/10/11)
New MKLP-2 inhibitors in the paprotrain series: Design, synthesis and biological evaluations
Members of the kinesin superfamily are involved in key functions during intracellular transport and cell division. Their involvement in cell division makes certain kinesins potential targets for drug development in cancer chemotherapy. The two most advanc
Use of derivatives of indoles for the treatment of cancer
The present invention relates to the use of derivatives of indoles having a general formula (I) as follow: for the manufacture of a pharmaceutical composition intended for the treatment of cancer.
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Page/Page column 64; 65
(2016/01/09)
Indole inhibitors of human nonpancreatic secretory phospholipase A2. 1. Indole-3-acetamides
Phospholipases (PLAs) produce rate-limiting precursors in the biosynthesis of various types of biologically active lipids involved in inflammatory processes. Increased levels of human nonpancreatic secretory phospholipase A2 (hnps-PLA2) have been detected in several pathological conditions. An inhibitor of this enzyme could have therapeutic utility. A broad screening program was carried out to identify chemical structures which could inhibit hnps-PLA2. One of the lead compounds generated by the screening program was 5-methoxy-2-methyl-1-(phenylmethyl)-1H-indole-3-acetic acid (13a). We describe the syntheses, structure-activity relationships, and pharmacological activities of a series of indole-3-acetamides and related compounds derived from this lead. This SAR was undertaken with the aid of X- ray crystal structures of complexes between the inhibitors and hnps-PLA2 which were of great value in directing the SAR.
Dillard, Robert D.,Bach, Nicholas J.,Draheim, Susan E.,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
p. 5119 - 5136
(2007/10/03)
Syntheses of 2(5)-substituted 1-acetyl-3-oxo-2,3-dihydroindoles, 3-acetoxy-1-acetylindoles, and of 2-methyl-5-methoxyindole-3-acetic acid
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Merour,Coadou,Tatibouet
p. 1053 - 1056
(2007/10/02)
New amidine derivatives of indole
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Piotrowska,Serafin,Wejroch Matacz
p. 297 - 303
(2007/10/04)
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