公开(公告)号：US09079899B2

公开(公告)日：2015-07-14

申请号：US13882897

申请日：2011-10-31

Applicant: Ching-Shih Chen ,  Hao-Chieh Chiu ,  Dasheng Wang ,  Samuel K. Kulp

Inventor： Ching-Shih Chen ,  Hao-Chieh Chiu ,  Dasheng Wang ,  Samuel K. Kulp

IPC: A61K31/415 ,  A61K31/5415 ,  C07D471/04 ,  C07D231/12 ,  C07D405/04

CPC classification number: C07D471/04 ,  A61K31/415 ,  A61K31/5415 ,  C07D231/12 ,  C07D405/04

Abstract: A method of treating infection by Staphylococcus in a subject by administering a pharmaceutical composition including a celecoxib derivative of formula I or a pharmaceutically acceptable salt thereof is described. The preparation of numerous celecoxib derivatives for testing as potential anti-staphylococcal agents is also described.

Abstract translation: 描述了通过施用包含式I的塞来昔布衍生物或其药学上可接受的盐的药物组合物来治疗受试者中葡萄球菌感染的方法。 还描述了用于测试作为潜在的抗葡萄球菌剂的众多塞来昔布衍生物的制备。

公开(公告)号：US08580827B2

公开(公告)日：2013-11-12

申请号：US13610967

申请日：2012-09-12

Applicant: Ching-Shih Chen ,  Hao-Chieh Chiu ,  Samuel Kulp ,  John S. Gunn ,  Larry S. Schlesinger

Inventor： Ching-Shih Chen ,  Hao-Chieh Chiu ,  Samuel Kulp ,  John S. Gunn ,  Larry S. Schlesinger

IPC: A61K31/41

CPC classification number: C07D231/12

Abstract: A series of celecoxib derivatives defined by Formula I: were prepared and evaluated for their ability to inhibit the gram-negative bacteria Francisella tularensis. Pharmaceutical compositions including celecoxib derivatives and their use in methods for treating or preventing infection by Francisella tularensis in a subject are described.

Abstract translation: 制备由式I定义的一系列塞来昔布衍生物，并评价其抑制革兰氏阴性细菌弗兰西斯拉氏弧菌的能力。 描述了包括塞来昔布衍生物的药物组合物及其在治疗或预防受试者中的弗朗西斯氏菌感染的方法中的用途。

公开(公告)号：US08445483B1

公开(公告)日：2013-05-21

申请号：US13267943

申请日：2011-10-07

Applicant: Ching-Shih Chen ,  Hao-Chieh Chiu ,  Dasheng Wang ,  John S. Gunn ,  Larry S. Schlesinger

Inventor： Ching-Shih Chen ,  Hao-Chieh Chiu ,  Dasheng Wang ,  John S. Gunn ,  Larry S. Schlesinger

IPC: C07D417/10 ,  C07D417/14 ,  A61K31/5415

CPC classification number: C07D231/12 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C12N2501/06

Abstract: A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of Formula I: wherein X wherein X is —CF3, Ar is selected from and R is selected from where R′ is L-Lys, D-Lys, β-Ala, L-Lue, L-Ile, Phe, SO2CH2CH2NH2, SO2NH2, Asn, Glu or Gyl, and R″ is methyl, ethyl, allyl, CH2CH2OH, CH2CN, CH2CH2CN, CH2CONH2,

Abstract translation: 式I的新一类磷酸肌醇依赖性激酶-1（PDK-1）抑制剂：其中X为X为-CF 3，Ar为选自其中R为选自其中R'为L-Lys，D-Lys，β -Ala，L-Lue，L-Ile，Phe，SO2CH2CH2NH2，SO2NH2，Asn，Glu或Gyl，R“为甲基，乙基，烯丙基，CH2CH2OH，CH2CN，CH2CH2CN，CH2CONH2，

公开(公告)号：US20130109681A1

公开(公告)日：2013-05-02

申请号：US13267943

申请日：2011-10-07

Applicant: Ching-Shih Chen ,  Hao-Chieh Chiu ,  Dasheng Wang ,  John S. Gunn ,  Larry S. Schlesinger

Inventor： Ching-Shih Chen ,  Hao-Chieh Chiu ,  Dasheng Wang ,  John S. Gunn ,  Larry S. Schlesinger

IPC: C07D417/14 ,  C07D417/10

CPC classification number: C07D231/12 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C12N2501/06

Abstract: A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of Formula I: wherein X wherein X is —CF3, Ar is selected from and R is selected from where R′ is L-Lys, D-Lys, β-Ala, L-Lue, L-Ile, Phe, SO2CH2CH2NH2, SO2NH2, Asn, Glu or Gyl, and R″ is methyl, ethyl, allyl, CH2CH2OH, CH2CN, CH2CH2CN, CH2CONH2,

公开(公告)号：US20130005788A1

公开(公告)日：2013-01-03

申请号：US13610967

申请日：2012-09-12

Applicant: Ching-Shih Chen ,  Hao-Chieh Chiu ,  Samuel Kulp ,  John S. Gunn ,  Larry S. Schlesinger

Inventor： Ching-Shih Chen ,  Hao-Chieh Chiu ,  Samuel Kulp ,  John S. Gunn ,  Larry S. Schlesinger

IPC: A61K31/415 ,  A61P31/04

CPC classification number: C07D231/12

Abstract: A series of celecoxib derivatives defined by Formula I: were prepared and evaluated for their ability to inhibit the gram-negative bacteria Francisella tularensis. Pharmaceutical compositions including celecoxib derivatives and their use in methods for treating or preventing infection by Francisella tularensis in a subject are described.

Abstract translation: 制备由式I定义的一系列塞来昔布衍生物，并评价其抑制革兰氏阴性细菌弗兰西斯拉氏弧菌的能力。 描述了包括塞来昔布衍生物的药物组合物及其在治疗或预防受试者中的弗朗西斯氏菌感染的方法中的用途。

公开(公告)号：US20130289004A1

公开(公告)日：2013-10-31

申请号：US13882897

申请日：2011-10-31

Applicant: Ching-Shih Chen ,  Hao-Chieh Chiu ,  Dasheng Wang ,  Samuel K. Kulp

Inventor： Ching-Shih Chen ,  Hao-Chieh Chiu ,  Dasheng Wang ,  Samuel K. Kulp

IPC: C07D231/12 ,  C07D405/04 ,  C07D471/04

CPC classification number: C07D471/04 ,  A61K31/415 ,  A61K31/5415 ,  C07D231/12 ,  C07D405/04

Abstract: A method of treating infection by Staphylococcus in a subject by administering a pharmaceutical composition including a celecoxib derivative of formula I or a pharmaceutically acceptable salt thereof is described. The preparation of numerous celecoxib derivatives for testing as potential anti-staphylococcal agents is also described.

Abstract translation: 描述了通过施用包含式I的塞来昔布衍生物或其药学上可接受的盐的药物组合物来治疗受试者中葡萄球菌感染的方法。 还描述了用于测试作为潜在的抗葡萄球菌剂的众多塞来昔布衍生物的制备。

公开(公告)号：US08039502B2

公开(公告)日：2011-10-18

申请号：US12179134

申请日：2008-07-24

Applicant: Ching-Shih Chen ,  Hao-Chieh Chiu ,  Dasheng Wang ,  John S. Gunn ,  Larry S. Schlesinger

Inventor： Ching-Shih Chen ,  Hao-Chieh Chiu ,  Dasheng Wang ,  John S. Gunn ,  Larry S. Schlesinger

IPC: C07D231/12 ,  A61K31/415

CPC classification number: C07D231/12 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C12N2501/06

Abstract: A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of Formula I: wherein X wherein X is —CF3, Ar is selected from and R is selected from where R′ is L-Lys, D-Lys, β-Ala, L-Lue, L-Ile, Phe, SO2CH2CH2NH2, SO2NH2, Asn, Glu or Gyl, and R″ is methyl, ethyl, allyl, CH2CH2OH, CH2CN, CH2CH2CN, CH2CONH2,

Abstract translation: 一类新的式I的磷酸肌醇依赖性激酶-1（PDK-1）抑制剂：其中X为X为-CF 3，Ar为选自R为选自其中R'为L-Lys，D-Lys，bgr ; -Ala，L-Lue，L-Ile，Phe，SO2CH2CH2NH2，SO2NH2，Asn，Glu或Gyl，R“为甲基，乙基，烯丙基，CH2CH2OH，CH2CN，CH2CH2CN，CH2CONH2，

公开(公告)号：US20090111799A1

公开(公告)日：2009-04-30

申请号：US12179134

申请日：2008-07-24

Applicant: Ching-Shih Chen ,  Hao-Chieh Chiu ,  Dasheng Wang

Inventor： Ching-Shih Chen ,  Hao-Chieh Chiu ,  Dasheng Wang

IPC: A61K31/5415 ,  C07D231/10 ,  C12N5/00 ,  A61K31/415 ,  C07D257/04 ,  A61P35/00 ,  A61P31/00 ,  A61K31/41 ,  C07D403/02 ,  A61K31/496 ,  C07D279/18

CPC classification number: C07D231/12 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C12N2501/06

Abstract: A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of Formula I: wherein X wherein X is —CF3, Ar is selected from and R is selected from where R′ is L-Lys, D-Lys, β-Ala, L-Lue, L-Ile, Phe, SO2CH2CH2NH2, SO2NH2, Asn, Glu or Gyl, and R″ is methyl, ethyl, allyl, CH2CH2OH, CH2CN, CH2CH2CN, CH2CONH2,

Abstract translation: 式I的新一类磷酸肌醇依赖性激酶-1（PDK-1）抑制剂：其中X为X为-CF 3，Ar为选自其中R为选自其中R'为L-Lys，D-Lys，β -Ala，L-Lue，L-Ile，Phe，SO2CH2CH2NH2，SO2NH2，Asn，Glu或Gyl，R“为甲基，乙基，烯丙基，CH2CH2OH，CH2CN，CH2CH2CN，CH2CONH2，