公开(公告)号：US11780833B2

公开(公告)日：2023-10-10

申请号：US16045254

申请日：2018-07-25

Applicant: HOWARD UNIVERSITY

Inventor： Oladapo Bakare ,  Samuel Ray Denmeade ,  Emmanuel S. Akinboye

IPC: C07K7/06 ,  C07D455/08 ,  C07D401/06

CPC classification number: C07D455/08 ,  C07D401/06 ,  C07K7/06

Abstract: Compounds are provided herein which are emetine derivatives that can be used as prodrugs which selectively undergo activation to release emetine in specific cellular conditions. In one aspect, a blocking group is incorporated onto the emetine molecule by the derivization of the N2′-position with moieties that can be selectively removed by hydrolysis in the cancer/tumor microenvironment. Such compounds are less cytotoxic than emetine and are substantially inactive in non-cancerous cells. In one aspect, the compounds described herein can be used for the treatment of metastatic and non-metastatic cancers, including, for example, breast cancer, prostate cancer, lung cancer, and leukemia.

公开(公告)号：US20140336187A1

公开(公告)日：2014-11-13

申请号：US14359035

申请日：2012-11-16

Applicant: HOWARD UNIVERSITY

Inventor： Oladapo Bakare ,  Clarence M. Lee ,  Yakini Brandy ,  Cheu Manka

IPC: C07C225/30 ,  C07D207/408 ,  C07D265/33 ,  C07D209/48 ,  C07C233/33 ,  C07C233/92 ,  C07C235/88

CPC classification number: C07C225/30 ,  A61K31/122 ,  A61K31/167 ,  A61K31/4035 ,  C07C233/33 ,  C07C233/92 ,  C07C235/88 ,  C07D207/408 ,  C07D209/48 ,  C07D265/33 ,  Y02A50/409

Abstract: Methods are provided to inhibit proliferation of Leishmania parasites, and in particular Leshmania donovani with imido-substituted 1,4-naphthoquinones, including novel compounds. Administering an imido-substituted 1,4-naphthoquinone can used to provide prophylaxis or treatment to a patient in need of treatment against leishmaniasis disease.

Abstract translation: 提供了抑制利什曼原虫寄生虫增殖的方法，特别是具有亚氨基取代的1,4-萘醌（包括新化合物）的灭丹参。 施用亚氨基取代的1,4-萘醌可用于对需要治疗利什曼病的患者提供预防或治疗。