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公开(公告)号：US08404681B2
公开(公告)日：2013-03-26
申请号：US10550978
申请日：2004-03-19
申请人： James W. Halbrook , Edward A. Kesicki , Laurence E. Burgess , Stephen T. Schlachter , Charles T. Eary , Justin G. Schiro
发明人： James W. Halbrook , Edward A. Kesicki , Laurence E. Burgess , Stephen T. Schlachter , Charles T. Eary , Justin G. Schiro
IPC分类号： A61K31/535 , C07D413/04
CPC分类号： C07D401/06 , A61K45/06 , C07D219/06 , C07D219/16 , C07D265/30 , C07D311/86 , C07D405/04 , C07D405/12 , C07D413/04 , C07D413/14 , C07D471/04 , C07F9/65586 , C07F9/6561
摘要： Compound that inhibit DNA-dependent protein kinase, compositions comprising the compounds, methods of inhibiting the DNA-PK biological activity, methods of sensitizing cells the agents that cause DNA lesions, and methods of potentiating cancer treatment are disclosed.
摘要翻译： 公开了抑制DNA依赖性蛋白激酶的化合物，包含该化合物的组合物，抑制DNA-PK生物活性的方法，使细胞致敏的方法，导致DNA病变的药剂，以及增强癌症治疗的方法。
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公开(公告)号：US20110021541A1
公开(公告)日：2011-01-27
申请号：US12742904
申请日：2008-11-12
IPC分类号： A61K31/52 , C07D473/34 , C12N5/078 , C12N9/99 , C07D473/38 , A61P19/08 , A61P35/00 , A61P11/06 , A61P19/02 , A61P25/00 , A61P9/12 , A61P35/02
CPC分类号： C07D519/00
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。
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公开(公告)号：US07179912B2
公开(公告)日：2007-02-20
申请号：US09941897
申请日：2001-08-28
申请人： James Halbrook , Edward A. Kesicki , Laurence E. Burgess , Stephen T. Schlachter , Charles T. Eary , Justin G. Schiro , Hongmei Huang , Michael Evans , Yongxin Han
发明人： James Halbrook , Edward A. Kesicki , Laurence E. Burgess , Stephen T. Schlachter , Charles T. Eary , Justin G. Schiro , Hongmei Huang , Michael Evans , Yongxin Han
IPC分类号： C07D265/30 , C07D295/02
CPC分类号： C07D213/40 , A61K45/06 , C07C309/66 , C07D209/36 , C07D211/42 , C07D211/46 , C07D213/50 , C07D213/74 , C07D213/75 , C07D231/12 , C07D233/56 , C07D235/26 , C07D239/48 , C07D249/08 , C07D277/24 , C07D277/54 , C07D279/12 , C07D295/096 , C07D295/112 , C07D295/13 , C07D295/135 , C07D295/155 , C07D295/185 , C07D295/215 , C07D295/30 , C07D307/83 , C07D309/10 , C07D311/30 , C07D333/22 , C07D405/04 , C07D417/12 , C07F9/6533 , C07F9/65785
摘要： Compounds that inhibit DNA-dependent protein kinase, compositions comprising the compounds, methods to inhibit the DNA-PK biological activity, methods to sensitize cells the agents that cause DNA lesions, and methods to potentiate cancer treatment are disclosed.
摘要翻译： 公开了抑制DNA依赖性蛋白激酶的化合物，包含该化合物的组合物，抑制DNA-PK生物活性的方法，使细胞致敏引起DNA病变的药剂，以及加强癌症治疗的方法。
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公开(公告)号：US06949535B2
公开(公告)日：2005-09-27
申请号：US10697912
申请日：2003-10-30
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： 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 , A61K31/33 , C07D239/72
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。
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公开(公告)号：US20100105683A1
公开(公告)日：2010-04-29
申请号：US12551623
申请日：2009-09-01
申请人： Kathleen S. Keegan , Edward A. Kesicki , John Joseph Gaudino , Adam Wade Cook , Scott Douglas Cowen , Laurence Edward Burgess
发明人： Kathleen S. Keegan , Edward A. Kesicki , John Joseph Gaudino , Adam Wade Cook , Scott Douglas Cowen , Laurence Edward Burgess
IPC分类号： A61K31/5377 , A61K31/4965 , A61K31/497 , A61K31/496 , A61P35/00
CPC分类号： A61K45/06 , A61K31/4965 , A61K31/498 , C07D213/30 , C07D213/40 , C07D213/75 , C07D213/77 , C07D215/34 , C07D231/12 , C07D231/40 , C07D233/56 , C07D239/42 , C07D239/47 , C07D241/12 , C07D241/20 , C07D241/44 , C07D249/08 , C07D251/22 , C07D253/07 , C07D257/06 , C07D277/48 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D453/02 , A61K2300/00
摘要： Aryl- and heteroaryl-substituted urea compounds useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division also are disclosed.
摘要翻译： 公开了可用于治疗与DNA复制中的DNA损伤或病变相关的疾病和病症的芳基和杂芳基取代的脲化合物。 还公开了制备化合物的方法及其作为治疗剂的用途，例如用于治疗癌症和其它以DNA复制，染色体分离或细胞分裂缺陷为特征的疾病。
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公开(公告)号：US07176229B2
公开(公告)日：2007-02-13
申请号：US11268374
申请日：2005-11-07
申请人： Timothy J. Martins , Kerry W. Fowler , Joshua Odingo , Edward A. Kesicki , Amy Oliver , Laurence Edward Burgess , John Joseph Gaudino , Zachary S. Jones , Bradley J. Newhouse , Stephen T. Schlachter
发明人： Timothy J. Martins , Kerry W. Fowler , Joshua Odingo , Edward A. Kesicki , Amy Oliver , Laurence Edward Burgess , John Joseph Gaudino , Zachary S. Jones , Bradley J. Newhouse , Stephen T. Schlachter
IPC分类号： A61K31/40 , A61K31/403 , C07D207/04
CPC分类号： C07D207/08 , A61K31/40 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/06 , C07D417/12 , Y02A50/411
摘要： Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
摘要翻译： 公开了作为PDE4的有效和选择性抑制剂的新型吡咯烷化合物及其制备方法。 还公开了化合物在治疗炎性疾病和涉及细胞因子水平升高的其它疾病以及中枢神经系统（CNS）病症中的用途。
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公开(公告)号：US06998416B2
公开(公告)日：2006-02-14
申请号：US10758675
申请日：2004-01-15
申请人： Timothy J. Martins , Kerry W. Fowler , Joshua Odingo , Edward A. Kesicki , Amy Oliver , Laurence E. Burgess , John J. Gaudino , Zachary S. Jones , Bradley J. Newhouse , Stephen T. Schlachter
发明人： Timothy J. Martins , Kerry W. Fowler , Joshua Odingo , Edward A. Kesicki , Amy Oliver , Laurence E. Burgess , John J. Gaudino , Zachary S. Jones , Bradley J. Newhouse , Stephen T. Schlachter
IPC分类号： A61K31/40
CPC分类号： C07D207/08 , A61K31/40 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/06 , C07D417/12 , Y02A50/411
摘要： Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
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公开(公告)号：US06716871B2
公开(公告)日：2004-04-06
申请号：US10151202
申请日：2002-05-17
申请人： Timothy J. Martins , Kerry W. Fowler , Joshua Odingo , Edward A. Kesicki , Amy Oliver , Laurence E Burgess , John J. Gaudino , Zachary S Jones , Bradley J Newhouse , Stephen T. Schlachter
发明人： Timothy J. Martins , Kerry W. Fowler , Joshua Odingo , Edward A. Kesicki , Amy Oliver , Laurence E Burgess , John J. Gaudino , Zachary S Jones , Bradley J Newhouse , Stephen T. Schlachter
IPC分类号： A61K3140
CPC分类号： C07D207/08 , A61K31/40 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/06 , C07D417/12 , Y02A50/411
摘要： Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
摘要翻译： 公开了作为PDE4的有效和选择性抑制剂的新型吡咯烷化合物及其制备方法。 还公开了化合物在治疗炎性疾病和涉及细胞因子水平升高的其它疾病以及中枢神经系统（CNS）病症中的用途。
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9.发明授权
公开(公告)号：US4861726A
公开(公告)日：1989-08-29
申请号：US166420
申请日：1988-03-10
CPC分类号： G01N33/6842 , C07K1/12 , C07K1/122 , C07K1/128 , G01N33/6824 , Y10T436/141111
摘要： A protein micro sequencing method for use in conjunction with the thiocylation degradation of polypeptides and proteins is disclosed. The process involves reaction of the N-terminal amino acid of a polypeptide with an excess of a thioacylating reagent. After sufficient time to insure quantitative coupling and removal of excess reagent, the derivatized polypeptide is subjected to cleavage by acid which affords a 2-substituted-5(4H)-thiazolinone. After removal of excess acid, the thiazolinone is reacted with a small excess of a fluorescent or enhanced ultraviolet absorbance reagent having a reactive carboxylic acid chloride, sulfonic acid chloride, chloroformate, isocyanate or anhydride functionality, in the presence of a tertiary amine catalyst, to yield the corresponding 5-O-acyl-2-(substituted)thiazole derivative, detectible by enhanced ultravoilet absorobance or fluorescence emission at extremely low concentration thereby providing a method of sequencing very small amounts of protein.
摘要翻译： 公开了与多肽和蛋白质的硫代酰化降解结合使用的蛋白质微测序方法。 该方法涉及多肽的N-末端氨基酸与过量的硫代酰化试剂的反应。 在足够的时间确保定量偶联和除去过量试剂后，将衍生的多肽经酸提供2-取代的-5（4H） - 噻唑啉酮。 除去过量的酸后，噻唑啉酮与少量过量的在叔胺催化剂存在下具有反应性羧酸氯化物，磺酰氯，氯甲酸酯，异氰酸酯或酸酐官能团的荧光或增强的紫外线吸收剂反应，与 产生相应的5-O-酰基-2-（取代的）噻唑衍生物，通过增强的超疏水吸收或极低浓度的荧光发射可检测，从而提供了非常少量蛋白质的测序方法。
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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。
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