公开(公告)号：US20160235743A1

公开(公告)日：2016-08-18

申请号：US15028169

申请日：2014-10-08

Applicant: Qing-Bin LU

Inventor： Qing-Bin Lu

IPC: A61K31/4965 ,  A61K31/44 ,  A61K31/136

Abstract: Disclosed herein are non-platinum-based (NPB) anti-cancer compounds useful for targeted chemotherapy, e.g., to generate anti-cancer effects for the treatment of cancer and other disorders while having no or minimal toxicity. The compounds N have the general formula I: (I) wherein A represents an aromatic core; at least one of Ra and Rb is an electron transfer promoter as defined herein, e.g., NH2; and at least one of Rc is a leaving group as defined herein, e.g., halogen; and the remainder of the molecule is as defined herein. Pharmaceutical compositions, methods, uses, kits and commercial packages comprising the anti-cancer compounds are also disclosed.

Abstract translation: 本文公开了可用于靶向化学疗法的非铂类（NPB）抗癌化合物，例如为了治疗癌症和其它疾病而产生抗癌作用，同时没有或极小的毒性。 化合物N具有通式I：（I）其中A表示芳族核; Ra和Rb中的至少一个是如本文所定义的电子转移促进剂，例如NH 2; 并且R c中的至少一个是如本文所定义的离去基团，例如卤素; 并且分子的其余部分如本文所定义。 还公开了包含抗癌化合物的药物组合物，方法，用途，试剂盒和商业包装。

公开(公告)号：US10463662B2

公开(公告)日：2019-11-05

申请号：US15028169

申请日：2014-10-08

Applicant: Qing-Bin Lu

Inventor： Qing-Bin Lu

IPC: A61K31/44 ,  A61K31/4965 ,  A61K31/136 ,  A61K31/495 ,  C07D213/73 ,  C07C211/52 ,  C07D241/20

Abstract: Disclosed herein are non-platinum-based (NPB) anti-cancer compounds useful for targeted chemotherapy, e.g., to generate anti-cancer effects for the treatment of cancer and other disorders while having no or minimal toxicity. The compounds N have the general formula I: (I) wherein A represents an aromatic core; at least one of Ra and Rb is an electron transfer promoter as defined herein, e.g., NH2; and at least one of Rc is a leaving group as defined herein, e.g., halogen; and the remainder of the molecule is as defined herein. Pharmaceutical compositions, methods, uses, kits and commercial packages comprising the anti-cancer compounds are also disclosed.

公开(公告)号：US11446294B2

公开(公告)日：2022-09-20

申请号：US16574800

申请日：2019-09-18

Applicant: Qing-Bin Lu

Inventor： Qing-Bin Lu

IPC: A61K31/44 ,  A61K31/4965 ,  A61K31/136 ,  A61P19/02 ,  A61P37/06 ,  A61K31/495 ,  C07D213/73 ,  A61P25/00 ,  A61P35/00 ,  A61P17/06 ,  C07D241/20 ,  A61P1/06 ,  C07C211/52

Abstract: Disclosed herein are non-platinum-based (NPB) anti-cancer compounds useful for targeted chemotherapy, e.g., to generate anti-cancer effects for the treatment of cancer and other disorders while having no or minimal toxicity. The compounds have the general formula I: (I) wherein A represents an aromatic core; at least one of Ra and Rb is an electron transfer promoter as defined herein, e.g., NH2; and at least one of Rc is a leaving group as defined herein, e.g., halogen; and the remainder of the molecule is as defined herein. Pharmaceutical compositions, methods, uses, kits and commercial packages comprising the anti-cancer compounds are also disclosed.

公开(公告)号：US20120156311A1

公开(公告)日：2012-06-21

申请号：US13393284

申请日：2010-09-01

Applicant: Qing-Bin Lu

Inventor： Qing-Bin Lu

IPC: A61K33/24 ,  C07C211/51 ,  A61K35/00 ,  C07D403/06

CPC classification number: A61K45/06 ,  A61K31/122 ,  A61K31/136 ,  A61K31/282 ,  A61K31/404 ,  A61K31/555 ,  A61K33/24 ,  A61K2300/00

Abstract: The combination of a biocompatible electron donor and a platinum-based antineoplastic agent exhibits improved efficacy in treating cancer This improved activity appears to be the result of electron transfer from the aforementioned donor compound to the platinum-based antineoplastic agent As the electron donor alone has no chemotherapeutic utility in treating cancer, the resulting combinations appear to be synergistic in nature In select preferred embodiments, the biocompatible electron donor is an amine (such as N,N,N′,N′-tetramethyl-p-phenylene diamine or indocyanine green), a phenolic compound (such as a flavanol or catechin), or a quinone (such as an aromatic quinone), while the antineoplastic is cisplatin.

Abstract translation: 生物相容性电子给体和铂类抗肿瘤剂的组合在治疗癌症中表现出改进的功效。这种改善的活性似乎是从上述供体化合物向铂基抗肿瘤药物的电子转移的结果。由于电子给体单独没有 生物相容性电子给体是一种胺（如N，N，N'，N'-四甲基 - 对苯二胺或吲哚菁绿），其特征在于， ，酚类化合物（例如黄烷醇或儿茶素）或醌（如芳香醌），而抗肿瘤药是顺铂。

公开(公告)号：US20200009133A1

公开(公告)日：2020-01-09

申请号：US16574800

申请日：2019-09-18

Applicant: Qing-Bin Lu

Inventor： Qing-Bin Lu

IPC: A61K31/4965 ,  A61K31/136 ,  A61K31/44

Abstract: Disclosed herein are non-platinum-based (NPB) anti-cancer compounds useful for targeted chemotherapy, e.g., to generate anti-cancer effects for the treatment of cancer and other disorders while having no or minimal toxicity. The compounds have the general formula I: (I) wherein A represents an aromatic core; at least one of Ra and Rb is an electron transfer promoter as defined herein, e.g., NH2; and at least one of Rc is a leaving group as defined herein, e.g., halogen; and the remainder of the molecule is as defined herein. Pharmaceutical compositions, methods, uses, kits and commercial packages comprising the anti-cancer compounds are also disclosed.

公开(公告)号：US09655965B2

公开(公告)日：2017-05-23

申请号：US14654165

申请日：2013-12-20

Applicant: Qing-Bin Lu

Inventor： Qing-Bin Lu

IPC: A61K31/136 ,  A61K31/44 ,  A61K31/4965 ,  A61K41/00 ,  C07D213/73 ,  C07C211/52 ,  C07D241/20 ,  A61N5/10

CPC classification number: A61K41/0038 ,  A61K31/136 ,  A61K31/44 ,  A61K31/4965 ,  A61N2005/1098 ,  C07C211/52 ,  C07D213/73 ,  C07D241/20

Abstract: Disclosed herein are radiosensitizer compounds useful in combination with radiation therapy, e.g., a synergistic combination therapy for the treatment of cancer and other disorders. The radiosensitizer compounds have the general formula I: wherein A represents an aromatic core; at least one of Ra and Rb is an electron transfer promoter as defined herein, e.g., NH2; and at least one of Rc is a leaving group as defined herein, e.g., halogen; and the remainder of the molecule is as defined herein. Pharmaceutical compositions, methods, uses, kits and commercial packages comprising the radiosensitizer compounds are also disclosed.

公开(公告)号：US20150343059A1

公开(公告)日：2015-12-03

申请号：US14654165

申请日：2013-12-20

Applicant: Qing-Bin LU

Inventor： Qing-Bin Lu

IPC: A61K41/00 ,  A61K31/44 ,  A61K31/4965 ,  A61K31/136

CPC classification number: A61K41/0038 ,  A61K31/136 ,  A61K31/44 ,  A61K31/4965 ,  A61N2005/1098 ,  C07C211/52 ,  C07D213/73 ,  C07D241/20

Abstract: Disclosed herein are radiosensitizer compounds useful in combination with radiation therapy, e.g., a synergistic combination therapy for the treatment of cancer and other disorders. The radiosensitizer compounds have the general formula I: wherein A represents an aromatic core; at least one of Ra and Rb is an electron transfer promoter as defined herein, e.g., NH2; and at least one of Rc is a leaving group as defined herein, e.g., halogen; and the remainder of the molecule is as defined herein. Pharmaceutical compositions, methods, uses, kits and commercial packages comprising the radiosensitizer compounds are also disclosed.

Abstract translation: 本文公开了与放射治疗组合使用的放射增敏剂化合物，例如用于治疗癌症和其它疾病的协同组合疗法。 放射增敏剂化合物具有通式I：其中A表示芳族核; Ra和Rb中的至少一个是如本文所定义的电子转移促进剂，例如NH 2; 并且R c中的至少一个是如本文所定义的离去基团，例如卤素; 并且分子的其余部分如本文所定义。 还公开了包含放射增敏剂化合物的药物组合物，方法，用途，试剂盒和商业包装。