公开(公告)号：US08304411B2

公开(公告)日：2012-11-06

申请号：US12863964

申请日：2008-05-20

Applicant: Peng Cho Tang ,  Zhigang Lin ,  Hejun Lu ,  Fuqiang Zhao ,  Li Li ,  Fanglong Yang ,  Jianghong Fu ,  Lin Wang ,  Guangyuan Shen ,  Dongliang Guan

Inventor： Peng Cho Tang ,  Zhigang Lin ,  Hejun Lu ,  Fuqiang Zhao ,  Li Li ,  Fanglong Yang ,  Jianghong Fu ,  Lin Wang ,  Guangyuan Shen ,  Dongliang Guan

IPC: A61K31/5377 ,  A61K31/403 ,  A61K31/454 ,  C07D403/12 ,  C07D401/14 ,  C07D413/14 ,  A61P3/10

CPC classification number: C07D209/52 ,  C07D403/12

Abstract: Disclosed are new dicycloazaalkane derivates represented by general formula (I), preparation processes and pharmaceutical compositions containing them, and the uses for treatment especially for dipeptidyl peptidase inhibitor (DPP-IV), in which each substitute group of general formula (I) is as defined in specification.

Abstract translation: 公开了由通式（I）表示的新的二环扎烷烃衍生物，其制备方法和含有它们的药物组合物，以及特别用于二肽基肽酶抑制剂（DPP-IV）的用途，其中通式（I）的每个取代基为 在规范中定义。

公开(公告)号：US20100311747A1

公开(公告)日：2010-12-09

申请号：US12863964

申请日：2008-05-20

Applicant: Peng Cho Tang ,  Zhigang Lin ,  Hejun Lu ,  Fuqiang Zhao ,  Li Li ,  Fanglong Yang ,  Jianghong Fu ,  Lin Wang ,  Guangyuan Shen ,  Dongliang Guan

Inventor： Peng Cho Tang ,  Zhigang Lin ,  Hejun Lu ,  Fuqiang Zhao ,  Li Li ,  Fanglong Yang ,  Jianghong Fu ,  Lin Wang ,  Guangyuan Shen ,  Dongliang Guan

IPC: A61K31/5377 ,  C07D403/12 ,  A61K31/403 ,  C07D401/14 ,  A61K31/454 ,  C07D413/14 ,  A61P3/10

CPC classification number: C07D209/52 ,  C07D403/12

Abstract: Disclosed are new dicycloazaalkane derivates represented by general formula (I), preparation processes and pharmaceutical compositions containing them, and the uses for treatment especially for dipeptidyl peptidase inhibitor (DPP-IV), in which each substitute group of general formula (I) is as defined in specification.

Abstract translation: 公开了由通式（I）表示的新的二环唑烷衍生物，其制备方法和含有它们的药物组合物，以及特别用于二肽基肽酶抑制剂（DPP-IV）的用途，其中通式（I）的每个取代基为 在规范中定义。

公开(公告)号：US08686041B2

公开(公告)日：2014-04-01

申请号：US13484392

申请日：2012-05-31

Applicant: Yaron Ilan ,  Ehud Zigmond ,  Richard B. Silverman ,  Hejun Lu

Inventor： Yaron Ilan ,  Ehud Zigmond ,  Richard B. Silverman ,  Hejun Lu

IPC: A01N37/08 ,  A01N53/00 ,  A61K31/19 ,  A61K31/557

CPC classification number: A61K31/196 ,  A61K31/198

Abstract: The invention relates to inhibition of ornithine aminotransferase (OAT) for suppression of tumor cells proliferation. More particularly, the invention relates to methods of treatment of proliferative disorders by the selective inhibition of OAT, and further provides the use of OAT inhibitors, specifically, 5-amino-1,3-hexadienyl-carboxylic acid (Gabaculine), and Gabaculine analogue 8, for compositions and methods for the treatment of proliferative disorders such as hepatocellular carcinoma. The invention further provides methods and kits for the diagnosis of a pathologic proliferative disorder in a mammalian subject, based on determining the level of OAT expressed in a biological sample obtained from a subject.

Abstract translation: 本发明涉及抑制鸟氨酸氨基转移酶（OAT）抑制肿瘤细胞增殖。 更具体地说，本发明涉及通过选择性抑制OAT来治疗增殖性疾病的方法，并进一步提供使用OAT抑制剂，特别是5-氨基-1,3-己二烯基羧酸（Gabaculine）和加珠菌素类似物 8，用于治疗增殖性疾病如肝细胞癌的组合物和方法。 本发明还基于确定从受试者获得的生物样品中表达的OAT水平，提供用于诊断哺乳动物受试者中病理性增殖性病症的方法和试剂盒。

公开(公告)号：US20120245380A1

公开(公告)日：2012-09-27

申请号：US13484392

申请日：2012-05-31

Applicant: Yaron ILAN ,  Ehud ZIGMOND ,  Richard B. SILVERMAN ,  Hejun LU

Inventor： Yaron ILAN ,  Ehud ZIGMOND ,  Richard B. SILVERMAN ,  Hejun LU

IPC: C07C229/48

CPC classification number: A61K31/196 ,  A61K31/198

Abstract: The invention relates to inhibition of ornithine aminotransferase (OAT) for suppression of tumor cells proliferation. More particularly, the invention relates to methods of treatment of proliferative disorders by the selective inhibition of OAT, and further provides the use of OAT inhibitors, specifically, 5-amino-1,3-hexadienyl-carboxylic acid (Gabaculine), and Gabaculine analogue 8, for compositions and methods for the treatment of proliferative disorders such as hepatocellular carcinoma. The invention further provides methods and kits for the diagnosis of a pathologic proliferative disorder in a mammalian subject, based on determining the level of OAT expressed in a biological sample obtained from a subject.

Abstract translation: 本发明涉及抑制鸟氨酸氨基转移酶（OAT）抑制肿瘤细胞增殖。 更具体地说，本发明涉及通过选择性抑制OAT来治疗增殖性疾病的方法，并进一步提供使用OAT抑制剂，特别是5-氨基-1,3-己二烯基羧酸（Gabaculine）和加珠菌素类似物 8，用于治疗增殖性疾病如肝细胞癌的组合物和方法。 本发明还基于确定从受试者获得的生物样品中表达的OAT水平，提供用于诊断哺乳动物受试者中病理性增殖性病症的方法和试剂盒。

公开(公告)号：US08211865B2

公开(公告)日：2012-07-03

申请号：US12377889

申请日：2007-08-20

Applicant: Yaron Ilan ,  Ehud Zigmond ,  Richard B. Silverman ,  Hejun Lu

Inventor： Yaron Ilan ,  Ehud Zigmond ,  Richard B. Silverman ,  Hejun Lu

IPC: A61K48/00

CPC classification number: A61K31/196 ,  A61K31/198

Abstract: The invention relates to inhibition of ornithine aminotransferase (OAT) for suppression of tumor cells proliferation. More particularly, the invention relates to methods of treatment of proliferative disorders by the selective inhibition of OAT, and further provides the use of OAT inhibitors, specifically, 5-amino-1,3-hexadienyl-carboxylic acid (Gabaculine), and Gabaculine analogue 8, for compositions and methods for the treatment of proliferative disorders such as hepatocellular carcinoma. The invention further provides methods and kits for the diagnosis of a pathologic proliferative disorder in a mammalian subject, based on determining the level of OAT expressed in a biological sample obtained from a subject.

Abstract translation: 本发明涉及抑制鸟氨酸氨基转移酶（OAT）抑制肿瘤细胞增殖。 更具体地说，本发明涉及通过选择性抑制OAT来治疗增殖性疾病的方法，并进一步提供使用OAT抑制剂，特别是5-氨基-1,3-己二烯基羧酸（Gabaculine）和加珠菌素类似物 8，用于治疗增殖性疾病如肝细胞癌的组合物和方法。 本发明还基于确定从受试者获得的生物样品中表达的OAT水平，提供用于诊断哺乳动物受试者中病理性增殖性病症的方法和试剂盒。