公开(公告)号：US09701646B2

公开(公告)日：2017-07-11

申请号：US14777630

申请日：2014-03-18

Applicant: Tufts University ,  Council of Scientific and Industrial Research

Inventor： Alexei Degterev ,  Chepuri V. Ramana ,  Jinbo Lee ,  Yadagiri Kommagalla

IPC: C07D249/06

CPC classification number: C07D249/06

Abstract: Provided are certain 1,2,3-triazole and 1,2,3-triazole dimer analogs of DM-PIT-1 which are second-generation selective non-phosphoinositide small molecule inhibitors of phosphatidylinositol-3,4,5-trisphosphate (PIP3), including 1,2,3-triazoles represented by formula (I) where: Ar represents aryl or heteroaryl; X represents O or S; each of Ra, Rb, Rc, and Rd independently represents hydrogen, halogen, C1-C10alkyl, —OH, —CF3, aryl, amino, or nitro; and Ar is optionally substituted with one or more substituents independently selected from the group consisting of halogen, C1-C10alkyl, —OH, —CF3, amino, and nitro. Also provided are pharmaceutical compositions comprising compounds of the invention and a pharmaceutical carrier. Also provided are methods of inhibiting PIP3-mediated signaling in a cell and treating cancer using compounds of the invention.

公开(公告)号：US09890132B2

公开(公告)日：2018-02-13

申请号：US14914378

申请日：2014-08-25

Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH

Inventor： Chepuri Venkata Ramana ,  Yadagiri Kommagalla ,  Kolluru Srinivas

IPC: C07D307/80

CPC classification number: C07D307/80

Abstract: Disclosed herein an efficient process for synthesis of benzofuran analogs having anti-inflammatory activity which comprises, Ru-catalyzed branched and linear selective alkylation of aroylbenzofurans formula-I with alpha, beta unsaturated esters of formula-II via C—H activation in presence of base, additives and organic solvent at suitable temperature to give high yield of desired linear alkylated benzofuran compounds of formula-III or branched alkylated benzofuran compounds of formula-IV or mixture thereof.

公开(公告)号：US20160297777A1

公开(公告)日：2016-10-13

申请号：US14777630

申请日：2014-03-18

Applicant: TUFTS UNIVERSITY ,  COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH

Inventor： Alexei Degterev ,  Chepuri V. Ramana ,  Jinbo Lee ,  Yadagiri Kommagalla

IPC: C07D249/06

CPC classification number: C07D249/06

Abstract: Provided are certain 1,2,3-triazole and 1,2,3-triazole dimer analogs of DM-PIT-1 which are second-generation selective non-phosphoinositide small molecule inhibitors of phosphatidylinositol-3,4,5-trisphosphate (PIP3), including 1,2,3-triazoles represented by formula (I) where: Ar represents aryl or heteroaryl; X represents O or S; each of Ra, Rb, Rc, and Rd independently represents hydrogen, halogen, C1-C10alkyl, —OH, —CF3, aryl, amino, or nitro; and Ar is optionally substituted with one or more substituents independently selected from the group consisting of halogen, C1-C10alkyl, —OH, —CF3, amino, and nitro. Also provided are pharmaceutical compositions comprising compounds of the invention and a pharmaceutical carrier. Also provided are methods of inhibiting PIP3-mediated signaling in a cell and treating cancer using compounds of the invention.