公开(公告)号：US20140045851A1

公开(公告)日：2014-02-13

申请号：US14058430

申请日：2013-10-21

申请人： University of Kansas

发明人： Emily Scott ,  Anuradha Roy

IPC分类号： C07D295/073

CPC分类号： C07D295/073 ,  A61K31/5375 ,  C07D295/04

摘要： A method of inhibiting formation of cancerous metabolites, of inhibiting cytochrome P450 2A13 from forming carcinogen metabolites, and/or inhibiting formation of cancerous lung cells in a subject can include: providing a morpholine compound that selectively interacts with cytochrome P450 2A13 over cytochrome P450 2A6; administering a therapeutically effective amount of the morpholine compound or derivative to the subject. The morpholine compound or derivative can be substantially more selective for interacting with the cytochrome P450 2A13 over the cytochrome P450 2A6. The morpholine compound or derivative can also be substantially non-interactive with other physiological components. The morpholine compound or derivative can include a structure that selectively interacts with cytochrome P450 2A13 over cytochrome P450 2A6, such as Compounds 1-34 of Formulas A-D.

摘要翻译： 抑制细胞色素P450 2A13形成致癌物代谢物和/或抑制受试者中癌细胞肺癌细胞形成的抑制癌症代谢物形成的方法可以包括：提供选择性地与细胞色素P450 2A13在细胞色素P450 2A6上相互作用的吗啉化合物; 给予受试者治疗有效量的吗啉化合物或衍生物。 吗啉化合物或衍生物可以在细胞色素P450 2A6上与细胞色素P450 2A13相互作用具有更大的选择性。 吗啉化合物或衍生物也可与其他生理组分基本上非交互。 吗啉化合物或衍生物可以包括在细胞色素P450 2A6上选择性地与细胞色素P450 2A13相互作用的结构，例如式A-D的化合物1-34。

公开(公告)号：US11173173B2

公开(公告)日：2021-11-16

申请号：US15745875

申请日：2016-07-28

申请人： UNIVERSITY OF CONNECTICUT ,  STOWERS INSTITUTE FOR MEDICAL RESEARCH ,  UNIVERSITY OF KANSAS

发明人： Rajeswari Kasi ,  Linheng Li ,  Xiuling Lu ,  John M. Perry ,  Gurusingham Sitta Sittampalam ,  Anuradha Roy ,  Xi C. He

IPC分类号： A61K9/51 ,  A61K31/704 ,  A61K31/513 ,  A61K31/136 ,  A61K31/4745 ,  A61K45/06 ,  A61K31/573 ,  A61K9/00 ,  A61K31/18 ,  A61K31/475 ,  A61K31/519 ,  A61K31/7076 ,  A61K31/708 ,  A61K31/337 ,  A61K33/242 ,  A61K33/243 ,  A61P35/02

摘要： The disclosure provides methods of treating cancer by selectively inhibiting p-S552-β-catenin, p-T217-β-catenin, p-T332-β-catenin, and/or p-S675-β-catenin production and/or activity. Such methods also and/or limit cancer-initiating cells.

公开(公告)号：US08962624B2

公开(公告)日：2015-02-24

申请号：US14058430

申请日：2013-10-21

申请人： University of Kansas

发明人： Emily Scott ,  Anuradha Roy

IPC分类号： A61K31/5375 ,  C07D295/04 ,  C07D295/073

CPC分类号： C07D295/073 ,  A61K31/5375 ,  C07D295/04

摘要： A method of inhibiting formation of cancerous metabolites, of inhibiting cytochrome P450 2A13 from forming carcinogen metabolites, and/or inhibiting formation of cancerous lung cells in a subject can include: providing a morpholine compound that selectively interacts with cytochrome P450 2A13 over cytochrome P450 2A6; administering a therapeutically effective amount of the morpholine compound or derivative to the subject. The morpholine compound or derivative can be substantially more selective for interacting with the cytochrome P450 2A13 over the cytochrome P450 2A6. The morpholine compound or derivative can also be substantially non-interactive with other physiological components. The morpholine compound or derivative can include a structure that selectively interacts with cytochrome P450 2A13 over cytochrome P450 2A6, such as Compounds 1-34 of Formulas A-D.

摘要翻译： 抑制细胞色素P450 2A13形成致癌物代谢物和/或抑制受试者中癌细胞肺癌细胞形成的抑制癌症代谢物形成的方法可以包括：提供选择性地与细胞色素P450 2A13在细胞色素P450 2A6上相互作用的吗啉化合物; 给予受试者治疗有效量的吗啉化合物或衍生物。 吗啉化合物或衍生物可以在细胞色素P450 2A6上与细胞色素P450 2A13相互作用具有更大的选择性。 吗啉化合物或衍生物也可与其他生理组分基本上非交互。 吗啉化合物或衍生物可以包括在细胞色素P450 2A6上选择性地与细胞色素P450 2A13相互作用的结构，例如式A-D的化合物1-34。