-
公开(公告)号:US08242125B2
公开(公告)日:2012-08-14
申请号:US12632396
申请日:2009-12-07
申请人: Gerald David Artman, III , Jason Matthew Elliott , Nan Ji , Donglei Liu , Fupeng Ma , Nello Mainolfi , Erik Meredith , Karl Miranda , James J. Powers , Chang Rao
发明人: Gerald David Artman, III , Jason Matthew Elliott , Nan Ji , Donglei Liu , Fupeng Ma , Nello Mainolfi , Erik Meredith , Karl Miranda , James J. Powers , Chang Rao
IPC分类号: C07D403/12 , C07D403/14 , C07D471/04 , C07D487/04 , C07D487/08 , A61K31/404
CPC分类号: C07D403/12 , A61K31/18 , A61K31/404 , A61K45/06 , C07D403/14 , C07D413/14 , C07D471/04 , C07D487/04 , C07D487/08 , A61K2300/00
摘要: The invention relates to novel organic compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumor diseases and ocular neovascular diseases.
摘要翻译: 本发明涉及式(I)的新型有机化合物及其在治疗动物或人体中的用途,包括式I化合物的药物组合物和式I化合物在制备药物组合物中的用途 用于治疗蛋白激酶依赖性疾病,特别是增殖性疾病,例如治疗肿瘤疾病和眼睛新生血管疾病。
-
公开(公告)号:US20120142685A1
公开(公告)日:2012-06-07
申请号:US12594728
申请日:2008-04-04
申请人: Markus Rolf Dobler , Charles Francis Jewell, JR. , Erik Meredith , Lauren G. Monovich , Sarah Siska , Anette Von Matt , Maurice Van Eis , Taeyoung Yoon , Christoph Gaul , Michael Paul Capparelli
发明人: Markus Rolf Dobler , Charles Francis Jewell, JR. , Erik Meredith , Lauren G. Monovich , Sarah Siska , Anette Von Matt , Maurice Van Eis , Taeyoung Yoon , Christoph Gaul , Michael Paul Capparelli
IPC分类号: A61K31/5377 , C07D471/10 , A61K31/444 , A61P7/10 , A61P9/04 , A61P35/00 , A61P3/04 , A61P3/10 , C07D471/04 , A61K31/496
CPC分类号: C07D471/04
摘要: The present invention provides a compound formula I: (formula I) said compound is inhibitor of selective subset of kinases belonging to the AGC or calmodulin kinase family, such as for example MARK1/2/3, PKD-1/2/3, PKN-1/2, CDK-9, CaMKII, ROCK-I/II, inhibitors of histone deacetylase (HDAC) phosphorylation, or inhibitors of other kinases. Finally, the present invention also provides a pharmaceutical composition.
摘要翻译: 本发明提供式I化合物:(式I)所述化合物是属于AGC或钙调蛋白激酶家族的激酶选择性亚型的抑制剂,例如MARK1 / 2/3,PKD-1/2/3,PKN -1/2,CDK-9,CaMKII,ROCK-I / II,组蛋白脱乙酰酶(HDAC)磷酸化抑制剂或其他激酶抑制剂。 最后,本发明还提供药物组合物。
-
公开(公告)号:US20140171392A1
公开(公告)日:2014-06-19
申请号:US14079018
申请日:2013-11-13
申请人: Qi-Ying Hu , Gary Michael Ksander , Erik Meredith , Lauren G. Monovich , Julien Papillon , Christoph Schumacher
发明人: Qi-Ying Hu , Gary Michael Ksander , Erik Meredith , Lauren G. Monovich , Julien Papillon , Christoph Schumacher
IPC分类号: C07F9/6506 , C07D487/04
CPC分类号: C07F9/6506 , A61K31/4188 , A61K31/55 , A61P5/00 , C07D487/04
摘要: The present invention relates to a method of treating a disease or disorder characterised by increased stress hormone levels and/or decreased androgen hormone levels in a subject, comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I): wherein n is 1 or 3; R is hydrogen or —C(O)N(Ra)(Rb) wherein Ra and Rb are independently —(C1-C4) alkyl, or —(C1-C4) alkyl-(C5-C7) aryl, wherein each of Ra and Rb is optionally substituted by —(C1-C4) alkoxy; R1, R2, and R3, are independently hydrogen, halogen, cyano or —(C6-C10) aryl, wherein said —(C6-C10) aryl is optionally substituted by halogen, with the proviso that no more than one of R1, R2, and R3 is hydrogen; and R4 and R5 are hydrogen; or a pharmaceutically acceptable salt thereof.
摘要翻译: 本发明涉及治疗受试者特征为增加的应激激素水平和/或降低雄激素激素水平的疾病或病症的方法,包括向受试者施用治疗有效量的由式(I)表示的化合物:其中 n为1或3; 其中R a和R b独立地为 - (C 1 -C 4)烷基或 - (C 1 -C 4)烷基 - (C 5 -C 7)芳基),其中R a为 并且R b任选被 - (C 1 -C 4)烷氧基取代; R 1,R 2和R 3独立地是氢,卤素,氰基或 - (C 6 -C 10)芳基,其中所述 - (C 6 -C 10)芳基任选被卤素取代,条件是不大于1个, ,R3为氢; R4和R5是氢; 或其药学上可接受的盐。
-
公开(公告)号:US08609862B2
公开(公告)日:2013-12-17
申请号:US13521548
申请日:2011-01-13
申请人: Qi-Ying Hu , Gary Michael Ksander , Erik Meredith , Lauren G. Monovich , Julien Papillon , Christoph Schumacher
发明人: Qi-Ying Hu , Gary Michael Ksander , Erik Meredith , Lauren G. Monovich , Julien Papillon , Christoph Schumacher
IPC分类号: A61K31/4188 , C07D235/02
CPC分类号: C07F9/6506 , A61K31/4188 , A61K31/55 , A61P5/00 , C07D487/04
摘要: The present invention relates to a method of treating a disease or disorder characterised by increased stress hormone levels and/or decreased androgen hormone levels in a subject, comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I): wherein n is 1 or 3; R is hydrogen or —C(O)N(Ra)(Rb) wherein Ra and Rb are independently —(C1-C4)alkyl, or —(C1-C4)alkyl-(C5-C7)aryl, wherein each of Ra and Rb is optionally substituted by —(C1-C4)alkoxy; R1, R2, and R3, are independently hydrogen, halogen, cyano or —(C6-C10) aryl, wherein said —(C6-C10)aryl is optionally substituted by halogen, with the proviso that no more than one of R1, R2, and R3 is hydrogen; and R4 and R5 are hydrogen; or a pharmaceutically acceptable salt thereof.
摘要翻译: 本发明涉及治疗受试者特征为增加的应激激素水平和/或降低雄激素激素水平的疾病或病症的方法,包括向受试者施用治疗有效量的由式(I)表示的化合物:其中 n为1或3; 其中R a和R b独立地为 - (C 1 -C 4)烷基或 - (C 1 -C 4)烷基 - (C 5 -C 7)芳基),其中R a为 并且R b任选被 - (C 1 -C 4)烷氧基取代; R 1,R 2和R 3独立地是氢,卤素,氰基或 - (C 6 -C 10)芳基,其中所述 - (C 6 -C 10)芳基任选被卤素取代,条件是不大于1个, ,R3为氢; R4和R5是氢; 或其药学上可接受的盐。
-
公开(公告)号:US08431584B2
公开(公告)日:2013-04-30
申请号:US13488760
申请日:2012-06-05
申请人: Gerald David Artman, III , Jason Matthew Elliott , Nan Ji , Donglei Liu , Fupeng Ma , Nello Mainolfi , Erik Meredith , Karl Miranda , James J. Powers , Chang Rao
发明人: Gerald David Artman, III , Jason Matthew Elliott , Nan Ji , Donglei Liu , Fupeng Ma , Nello Mainolfi , Erik Meredith , Karl Miranda , James J. Powers , Chang Rao
IPC分类号: C07D487/04 , C07D487/08 , A61K31/404
CPC分类号: C07D403/12 , A61K31/18 , A61K31/404 , A61K45/06 , C07D403/14 , C07D413/14 , C07D471/04 , C07D487/04 , C07D487/08 , A61K2300/00
摘要: The invention relates to novel organic compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumor diseases and ocular neovascular diseases.
-
公开(公告)号:US20120295888A1
公开(公告)日:2012-11-22
申请号:US13521548
申请日:2011-01-13
申请人: Qi-Ying Hu , Gary Michael Ksander , Erik Meredith , Lauren G. Monovich , Julien Papillon , Christoph Schumacher
发明人: Qi-Ying Hu , Gary Michael Ksander , Erik Meredith , Lauren G. Monovich , Julien Papillon , Christoph Schumacher
IPC分类号: A61K31/4188 , A61K31/55 , A61P9/04 , A61P5/00 , A61P9/00 , A61P43/00 , A61P5/06 , A61P3/00 , C07D487/04 , A61P21/00
CPC分类号: C07F9/6506 , A61K31/4188 , A61K31/55 , A61P5/00 , C07D487/04
摘要: The present invention relates to a method of treating a disease or disorder characterised by increased stress hormone levels and/or decreased androgen hormone levels in a subject, comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I): wherein n is 1 or 3; R is hydrogen or —C(O)N(Ra)(Rb) wherein Ra and Rb are independently —(C1-C4)alkyl, or —(C1-C4)alkyl-(C5-C7)aryl, wherein each of Ra and Rb is optionally substituted by —(C1-C4)alkoxy; R1, R2, and R3, are independently hydrogen, halogen, cyano or —(C6-C10) aryl, wherein said —(C6-C10)aryl is optionally substituted by halogen, with the proviso that no more than one of R1, R2, and R3 is hydrogen; and R4 and R5 are hydrogen; or a pharmaceutically acceptable salt thereof.
摘要翻译: 本发明涉及治疗受试者特征为增加的应激激素水平和/或降低雄激素激素水平的疾病或病症的方法,包括向受试者施用治疗有效量的由式(I)表示的化合物:其中 n为1或3; 其中R a和R b独立地为 - (C 1 -C 4)烷基或 - (C 1 -C 4)烷基 - (C 5 -C 7)芳基),其中R a为 并且R b任选被 - (C 1 -C 4)烷氧基取代; R 1,R 2和R 3独立地是氢,卤素,氰基或 - (C 6 -C 10)芳基,其中所述 - (C 6 -C 10)芳基任选被卤素取代,条件是不大于1个, ,R3为氢; R4和R5是氢; 或其药学上可接受的盐。
-
公开(公告)号:US20110092505A1
公开(公告)日:2011-04-21
申请号:US12996901
申请日:2009-06-12
申请人: Robin Burgis , Michael Paul Capparelli , Lucian Dipietro , Gabriel G. Gamber , Charles Francis Jewell, JR. , Erik Meredith , Karl Miranda , Lauren G. Monovich , Chang Rao , Nicolas Soldermann , Taeyoung Yoon , Qingming Zhu
发明人: Robin Burgis , Michael Paul Capparelli , Lucian Dipietro , Gabriel G. Gamber , Charles Francis Jewell, JR. , Erik Meredith , Karl Miranda , Lauren G. Monovich , Chang Rao , Nicolas Soldermann , Taeyoung Yoon , Qingming Zhu
IPC分类号: A61K31/535 , A61K31/4985 , A61K31/501 , A61K31/497 , A61K31/437 , A61K31/4545 , C07D417/14 , C07D487/04 , C07D413/14 , C07D471/04 , C07D401/14 , A61P17/00 , A61P9/00 , A61P35/00 , A61P37/00
CPC分类号: C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D519/00
摘要: The present invention provides novel organic compounds of Formula I: methods of use, and pharmaceutical compositions thereof.
-
公开(公告)号:US09957254B2
公开(公告)日:2018-05-01
申请号:US15320815
申请日:2015-07-02
申请人: Christopher M. Adams , David B. Belanger , Doug Bevan , Philippe Bolduc , Takeru Ehara , Luciana Ferrara , Nan Ji , Mitsunori Kato , Erik Meredith , Muneto Mogi , James J. Powers , Ganesh Prasanna
发明人: Christopher M. Adams , David B. Belanger , Doug Bevan , Philippe Bolduc , Takeru Ehara , Luciana Ferrara , Nan Ji , Mitsunori Kato , Erik Meredith , Muneto Mogi , James J. Powers , Ganesh Prasanna
IPC分类号: C07D401/14 , C07D401/04
CPC分类号: C07D401/14 , A61K31/4545 , A61K31/4985 , A61K31/519 , A61K31/53 , A61K45/06 , C07D401/04 , C07D401/12 , A61K2300/00
摘要: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
-
公开(公告)号:US09765067B2
公开(公告)日:2017-09-19
申请号:US15320813
申请日:2015-07-02
申请人: Christopher M. Adams , David B. Belanger , Doug Bevan , Takeru Ehara , Luciana Ferrara , Nan Ji , Donglei Liu , Erik Meredith , Muneto Mogi , James Powers , Ganesh Prasanna , Mitsunori Kato
发明人: Christopher M. Adams , David B. Belanger , Doug Bevan , Takeru Ehara , Luciana Ferrara , Nan Ji , Donglei Liu , Erik Meredith , Muneto Mogi , James Powers , Ganesh Prasanna , Mitsunori Kato
IPC分类号: A61K31/4545 , A61K31/4725 , A61K31/4439 , C07D409/14 , A61K9/00
CPC分类号: C07D409/14 , A61K9/0048 , A61K31/4439 , A61K31/4545 , A61K31/4725
摘要: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
-
公开(公告)号:US20170197950A1
公开(公告)日:2017-07-13
申请号:US15320813
申请日:2015-07-02
申请人: Christopher M. ADAMS , David B. BELANGER , Doug BEVAN , Takeru EHARA , Luciana FERRARA , Nan JI , Donglei LIU , Erik MEREDITH , Muneto MOGI , James POWERS , Ganesh PRASANNA , Mitsunori KATO
发明人: Christopher M. ADAMS , David B. BELANGER , Doug BEVAN , Takeru EHARA , Luciana FERRARA , Nan JI , Donglei LIU , Erik MEREDITH , Muneto MOGI , James POWERS , Ganesh PRASANNA , Mitsunori KATO
IPC分类号: C07D409/14 , A61K31/4439 , A61K31/4725 , A61K9/00 , A61K31/4545
CPC分类号: C07D409/14 , A61K9/0048 , A61K31/4439 , A61K31/4545 , A61K31/4725
摘要: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
-
-
-
-
-
-
-
-
-