公开(公告)号：US06518277B1

公开(公告)日：2003-02-11

申请号：US09841341

申请日：2001-04-24

申请人： Chanchal Sadhu ,  Ken Dick ,  Jennifer Treiberg ,  C. Gregory Sowell ,  Edward A. Kesicki ,  Amy Oliver

发明人： Chanchal Sadhu ,  Ken Dick ,  Jennifer Treiberg ,  C. Gregory Sowell ,  Edward A. Kesicki ,  Amy Oliver

IPC分类号： A61K3152

CPC分类号： C07D473/00 ,  C07D403/12 ,  C07D473/16 ,  C07D473/24 ,  C07D473/30 ,  C07D473/34 ,  C07D473/38 ,  C07D473/40 ,  C07D487/04

摘要： Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K&dgr;) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K&dgr; plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K&dgr;, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K&dgr; activity, including compounds that selectively inhibit PI3K&dgr; activity. Methods of using PI3K&dgr; inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K&dgr; inhibitory compounds to inhibit PI3K&dgr;-mediated processes in vitro and in vivo.

公开(公告)号：US08653077B2

公开(公告)日：2014-02-18

申请号：US13247962

申请日：2011-09-28

申请人： Chanchal Sadhu ,  Kennith O. Dick ,  Jennifer Treiberg ,  C. Gregory Sowell ,  Edward A. Kesicki ,  Amy Oliver

发明人： Chanchal Sadhu ,  Kennith O. Dick ,  Jennifer Treiberg ,  C. Gregory Sowell ,  Edward A. Kesicki ,  Amy Oliver

IPC分类号： C07D413/12 ,  C07D413/14 ,  A01N43/54 ,  C07D403/12 ,  A61K31/517 ,  A61P3/14

CPC分类号： A61K31/506 ,  C07D403/12 ,  C07D473/00 ,  C07D473/16 ,  C07D473/24 ,  C07D473/30 ,  C07D473/32 ,  C07D473/34 ,  C07D473/38 ,  C07D473/40 ,  C07D487/04 ,  C12N9/1205 ,  C12N9/99 ,  C12Y207/01137

摘要： Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.

摘要翻译： 公开了抑制磷脂酰肌醇3-激酶δ同种型（PI3Kdelta）活性的方法，以及治疗PI3Kdelta在白细胞功能中起作用的疾病如免疫和炎症疾病的方法。 优选地，所述方法使用选择性抑制PI3Kdelta的活性剂，而不显着抑制其它PI3K同种型的活性。 提供抑制PI3Kdelta活性的化合物，包括选择性抑制PI3Kdelta活性的化合物。 还提供了使用PI3Kdelta抑制化合物抑制癌细胞生长或增殖的方法。 因此，本发明提供了使用PI3Kdelta抑制化合物在体外和体内抑制PI3Kdelta介导的过程的方法。

公开(公告)号：US08138195B2

公开(公告)日：2012-03-20

申请号：US11110204

申请日：2005-04-20

申请人： Chanchal Sadhu ,  Kenneth O. Dick ,  Jennifer Treiberg ,  C. Gregory Sowell ,  Edward A. Kesicki ,  Amy Oliver

发明人： Chanchal Sadhu ,  Kenneth O. Dick ,  Jennifer Treiberg ,  C. Gregory Sowell ,  Edward A. Kesicki ,  Amy Oliver

IPC分类号： A61K31/52 ,  A01N43/90 ,  C07D487/04

CPC分类号： A61K31/506 ,  C07D403/12 ,  C07D473/00 ,  C07D473/16 ,  C07D473/24 ,  C07D473/30 ,  C07D473/32 ,  C07D473/34 ,  C07D473/38 ,  C07D473/40 ,  C07D487/04 ,  C12N9/1205 ,  C12N9/99 ,  C12Y207/01137

摘要： Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.

摘要翻译： 公开了抑制磷脂酰肌醇3-激酶δ同种型（PI3Kδ）活性的方法，以及治疗PI3Kδ在白细胞功能中起作用的疾病如免疫和炎症疾病的方法。 优选地，所述方法使用选择性抑制PI3Kδ的活性剂，而不显着抑制其它PI3K同种型的活性。 提供抑制PI3Kδ活性的化合物，包括选择性抑制PI3Kδ活性的化合物。 还提供了使用PI3Kδ抑制化合物抑制癌细胞生长或增殖的方法。 因此，本发明提供了在体外和体内使用PI3Kδ抑制化合物抑制PI3Kδ介导的过程的方法。

公开(公告)号：US20050261317A1

公开(公告)日：2005-11-24

申请号：US11110204

申请日：2005-04-20

申请人： Chanchal Sadhu ,  Ken Dick ,  Jennifer Treiberg ,  C. Sowell ,  Edward Kesicki ,  Amy Oliver

发明人： Chanchal Sadhu ,  Ken Dick ,  Jennifer Treiberg ,  C. Sowell ,  Edward Kesicki ,  Amy Oliver

IPC分类号： A61K31/517 ,  A61K31/52 ,  A61P3/10 ,  A61P7/08 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P17/04 ,  A61P17/06 ,  A61P19/02 ,  A61P25/02 ,  A61P27/02 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P35/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D403/12 ,  C07D473/00 ,  C07D473/16 ,  C07D473/24 ,  C07D473/30 ,  C07D473/34 ,  C07D473/38 ,  C07D473/40 ,  C07D487/04

CPC分类号： A61K31/506 ,  C07D403/12 ,  C07D473/00 ,  C07D473/16 ,  C07D473/24 ,  C07D473/30 ,  C07D473/32 ,  C07D473/34 ,  C07D473/38 ,  C07D473/40 ,  C07D487/04 ,  C12N9/1205 ,  C12N9/99 ,  C12Y207/01137

摘要： Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K5, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.

摘要翻译： 公开了抑制磷脂酰肌醇3-激酶δ同种型（PI3Kdelta）活性的方法，以及治疗PI3Kdelta在白细胞功能中起作用的疾病如免疫和炎症疾病的方法。 优选地，所述方法使用选择性抑制PI3K5的活性剂，而不显着抑制其它PI3K同种型的活性。 提供抑制PI3Kdelta活性的化合物，包括选择性抑制PI3Kdelta活性的化合物。 还提供了使用PI3Kdelta抑制化合物抑制癌细胞生长或增殖的方法。 因此，本发明提供了使用PI3Kdelta抑制化合物在体外和体内抑制PI3Kdelta介导的过程的方法。

公开(公告)号：US20100256168A1

公开(公告)日：2010-10-07

申请号：US12732128

申请日：2010-03-25

申请人： Kerry W. Fowler ,  Danwen Huang ,  Edward A. Kesicki ,  Hua Chee Ooi ,  Amy Oliver ,  Fuqiang Ruan ,  Jennifer Treiberg

发明人： Kerry W. Fowler ,  Danwen Huang ,  Edward A. Kesicki ,  Hua Chee Ooi ,  Amy Oliver ,  Fuqiang Ruan ,  Jennifer Treiberg

IPC分类号： A61K31/52 ,  A61P35/02 ,  A61P35/00

CPC分类号： C07D473/34 ,  A61K31/52 ,  C07D239/91 ,  C07D473/16 ,  C07D487/04

摘要： Compounds that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3Kδ plays a role in leukocyte function, using the compounds also are disclosed.

摘要翻译： 公开了抑制PI3Kδ活性的化合物，包括选择性抑制PI3Kδ活性的化合物。 公开了抑制磷脂酰肌醇3-激酶δ同种型（PI3Kδ）活性的方法，以及使用该化合物治疗PI3Kδ在白细胞功能中起作用的免疫力和炎症疾病等疾病的方法。

公开(公告)号：USRE44638E1

公开(公告)日：2013-12-10

申请号：US13730256

申请日：2012-12-28

申请人： Kerry W. Fowler ,  Danwen Huang ,  Edward A. Kesicki ,  Hua Chee Ooi ,  Amy Oliver ,  Fuqiang Ruan ,  Jennifer Treiberg ,  Kamal Deep Puri

发明人： Kerry W. Fowler ,  Danwen Huang ,  Edward A. Kesicki ,  Hua Chee Ooi ,  Amy Oliver ,  Fuqiang Ruan ,  Jennifer Treiberg ,  Kamal Deep Puri

IPC分类号： A61K31/517

CPC分类号： C07D473/34 ,  A61K31/52 ,  C07D239/91 ,  C07D473/16 ,  C07D487/04

摘要： The invention provides a class of substituted quinazolinone compounds and methods of treating diseases mediated by PI3Kδ activity. The disclosed compounds are useful in treating diseases such as bone-resorption disorders; and cancer, especially hematopoietic cancers, lymphomas, multiple myelomas and leukemia. The compounds are also useful in disrupting or inhibiting cellular processes such as leukocyte function or accumulation, neutrophils function, lymphocyte proliferation, and endogenous immune responses.

摘要翻译： 本发明提供了一类取代喹唑啉酮化合物和治疗由PI3Kdelta活性介导的疾病的方法。 所公开的化合物可用于治疗疾病如骨吸收障碍; 和癌症，特别是造血癌，淋巴瘤，多发性骨髓瘤和白血病。 所述化合物还可用于破坏或抑制细胞过程，例如白细胞功能或积累，嗜中性粒细胞功能，淋巴细胞增殖和内源性免疫应答。

公开(公告)号：US20120015964A1

公开(公告)日：2012-01-19

申请号：US13163597

申请日：2011-06-17

申请人： Kerry W. Fowler ,  Danwen Huang ,  Edward A. Kesicki ,  Hua Chee Ooi ,  Amy Oliver ,  Fuqiang Ruan ,  Jennifer Treiberg

发明人： Kerry W. Fowler ,  Danwen Huang ,  Edward A. Kesicki ,  Hua Chee Ooi ,  Amy Oliver ,  Fuqiang Ruan ,  Jennifer Treiberg

IPC分类号： A61K31/52 ,  C12N5/09 ,  A61P35/02 ,  C07D473/34 ,  A61P35/00

CPC分类号： C07D473/34 ,  A61K31/52 ,  C07D239/91 ,  C07D473/16 ,  C07D487/04

摘要： Compounds that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3Kδ plays a role in leukocyte function, using the compounds also are disclosed.

摘要翻译： 公开了抑制PI3Kδ活性的化合物，包括选择性抑制PI3Kδ活性的化合物。 公开了抑制磷脂酰肌醇3-激酶δ同种型（PI3Kδ）活性的方法，以及使用该化合物治疗PI3Kδ在白细胞功能中起作用的免疫力和炎症疾病等疾病的方法。

公开(公告)号：US08207153B2

公开(公告)日：2012-06-26

申请号：US12732128

申请日：2010-03-25

申请人： Kerry W. Fowler ,  Danwen Huang ,  Edward A. Kesicki ,  Hua Chee Ooi ,  Amy Oliver ,  Fuqiang Ruan ,  Jennifer Treiberg

发明人： Kerry W. Fowler ,  Danwen Huang ,  Edward A. Kesicki ,  Hua Chee Ooi ,  Amy Oliver ,  Fuqiang Ruan ,  Jennifer Treiberg

IPC分类号： A01N43/54 ,  A01N43/00 ,  C07D473/00 ,  C07D239/72

CPC分类号： C07D473/34 ,  A61K31/52 ,  C07D239/91 ,  C07D473/16 ,  C07D487/04

摘要： Compounds that inhibit P13Kδ activity, including compounds that selectively inhibit P13Kδ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (P13Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which P13Kδ plays a role in leukocyte function, using the compounds also are disclosed.

摘要翻译： 公开了抑制P13Kδ活性的化合物，包括选择性抑制P13Kδ活性的化合物。 公开了抑制磷脂酰肌醇3-激酶δ同种型（P13Kδ）活性的方法，以及使用该化合物治疗P13Kδ在白细胞功能中起作用的免疫力和炎症疾病等疾病的方法。

公开(公告)号：US07932260B2

公开(公告)日：2011-04-26

申请号：US11596092

申请日：2005-05-12

申请人： Kerry W. Fowler ,  Danwen Huang ,  Edward A. Kesicki ,  Hua Chee Ooi ,  Amy Oliver ,  Fuqiang Ruan ,  Jennifer Treiberg

发明人： Kerry W. Fowler ,  Danwen Huang ,  Edward A. Kesicki ,  Hua Chee Ooi ,  Amy Oliver ,  Fuqiang Ruan ,  Jennifer Treiberg

IPC分类号： A61K31/517

CPC分类号： C07D473/34 ,  A61K31/52 ,  C07D239/91 ,  C07D473/16 ,  C07D487/04

摘要： The invention provides a class of substituted quinazolinone compounds and methods of treating diseases mediated by PI3Kδ activity. The disclosed compounds are useful in treating diseases such as bone-resorption disorders; and cancer, especially hematopoietic cancers, lymphomas, multiple myelomas and leukemia. The compounds are also useful in disrupting or inhibiting cellular processes such as leukocyte function or accumulation, neutrophils function, lymphocyte proliferation, and endogenous immune responses.

摘要翻译： 本发明提供一类取代喹唑啉酮化合物和治疗由PI3Kδ活性介导的疾病的方法。 所公开的化合物可用于治疗疾病如骨吸收障碍; 和癌症，特别是造血癌，淋巴瘤，多发性骨髓瘤和白血病。 所述化合物还可用于破坏或抑制细胞过程，例如白细胞功能或积累，嗜中性粒细胞功能，淋巴细胞增殖和内源性免疫应答。

公开(公告)号：US20100256167A1

公开(公告)日：2010-10-07

申请号：US12732124

申请日：2010-03-25

申请人： Kerry W. Fowler ,  Danwen Huang ,  Edward A. Kesicki ,  Hua Chee Ooi ,  Amy Oliver ,  Fuqiang Ruan ,  Jennifer Treiberg

发明人： Kerry W. Fowler ,  Danwen Huang ,  Edward A. Kesicki ,  Hua Chee Ooi ,  Amy Oliver ,  Fuqiang Ruan ,  Jennifer Treiberg

IPC分类号： A61K31/52 ,  C07D473/32 ,  A61P35/00 ,  A61P35/02

CPC分类号： C07D473/34 ,  A61K31/52 ,  C07D239/91 ,  C07D473/16 ,  C07D487/04

摘要： Compounds that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3Kδ plays a role in leukocyte function, using the compounds also are disclosed.