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公开(公告)号：US06812246B2
公开(公告)日：2004-11-02
申请号：US10240883
申请日：2003-06-12
IPC分类号： A61K3135
CPC分类号： C07D311/30
摘要： The invention provides an aminoflavone having formula (I), wherein each of R1 and R2 is H, COCH2—R7, wherein R7 is amino alkylamino, dialkylamino, or alkyl- or dialkylaminoalkyl, or an &agr;-amino acid residue, provided that at least one of R1 or R2 is other than H, and R3 is H, branched or straight-chain alkyl, hydroxyalkyl, alkanoyloxyalkyl, alkanoyloxy, alkoxy, or alkoxyalkyl, or pharmaceutically acceptable salts thereof. The present invention also provides a pharmaceutical composition comprising an aminoflavone as described above, and a method of inhibiting the growth of a tumor in a host by administering a tumor growth-inhibiting amount of an aminoflavone compound having the formula as described above.
摘要翻译： 本发明提供具有式（I）的氨基黄酮，其中R 1和R 2各自为H，COCH 2 -R 7，其中R 7为氨基烷基氨基，二烷基氨基或烷基 - 或二烷基氨基烷基， 或α-氨基酸残基，条件是R 1或R 2中的至少一个不是H，R 3是H，支链或直链烷基，羟烷基，烷酰氧基烷基，烷酰氧基，烷氧基 ，或烷氧基烷基，或其药学上可接受的盐。 本发明还提供了包含如上所述的氨基黄酮的药物组合物，以及通过施用具有抑制肿瘤生长抑制量的具有上述通式的氨基黄酮化合物来抑制宿主中肿瘤生长的方法。
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公开(公告)号：US08895534B2
公开(公告)日：2014-11-25
申请号：US12848051
申请日：2010-07-30
申请人： Stephen J. Baker , Vincent S. Hernandez , Rashmi Sharma , James A. Nieman , Tsutomu Akama , Yong-Kang Zhang , Jacob J. Plattner , Michael Richard Kevin Alley , Rajeshwar Singh , Fernando Rock
发明人： Stephen J. Baker , Vincent S. Hernandez , Rashmi Sharma , James A. Nieman , Tsutomu Akama , Yong-Kang Zhang , Jacob J. Plattner , Michael Richard Kevin Alley , Rajeshwar Singh , Fernando Rock
IPC分类号： C07F5/02
CPC分类号： C07F5/025 , A61K31/69 , Y02A50/387
摘要： Novel monosubstituted and disubstutituted oxaboroles and pharmaceutical compositions containing such oxaboroles are provided, which are useful for treating bacterial infections, as well as combinations of these oxaboroles with at least one additional therapeutically effective agent.
摘要翻译： 提供了新的单取代和二取代的奥沙伏醇和含有这种恶唑烷的药物组合物，其可用于治疗细菌感染，以及这些恶唑烷与至少一种另外的治疗有效药剂的组合。
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公开(公告)号：US20100267981A1
公开(公告)日：2010-10-21
申请号：US12629753
申请日：2009-12-02
申请人： Stephen J. Baker , Tsutomu Akama , Michael Richard Kevin Alley , Steven J. Benkovic , Michael DiPierro , Vincent S. Hernandez , Karin M. Hold , Isaac Kennedy , Igor Likhotvorik , Weimin Mao , Kirk R. Maples , Jacob J. Plattner , Fernando Rock , Virginia Sanders , Aaron M. Stemphoski , George Petros Yiannikouros , Siead Zegar , Yong-Kang Zhang , Huchen Zhou
发明人： Stephen J. Baker , Tsutomu Akama , Michael Richard Kevin Alley , Steven J. Benkovic , Michael DiPierro , Vincent S. Hernandez , Karin M. Hold , Isaac Kennedy , Igor Likhotvorik , Weimin Mao , Kirk R. Maples , Jacob J. Plattner , Fernando Rock , Virginia Sanders , Aaron M. Stemphoski , George Petros Yiannikouros , Siead Zegar , Yong-Kang Zhang , Huchen Zhou
IPC分类号： C07F5/02
CPC分类号： C07F5/025 , A61K9/0012 , A61K9/08 , A61K31/69 , A61K31/70 , A61K31/7076 , A61K47/10 , C07F5/04 , C07H19/06 , C07H19/16 , C07H21/00 , C07H23/00 , Y02A50/473
摘要： This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.
摘要翻译： 本发明涉及可用于治疗真菌感染的化合物，更具体地涉及甲真菌病和/或皮肤真菌感染的局部治疗。 本发明涉及对真菌具有活性的化合物，并具有允许化合物与患者接触时达到感染真菌的皮肤，指甲，毛发，爪或蹄特定部位的性质。 特别地，本发明化合物具有促进钉板穿透的物理化学性质。
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公开(公告)号：US20100256092A1
公开(公告)日：2010-10-07
申请号：US12464829
申请日：2009-05-12
申请人： Yi Xia , Michael Richard Kevin Alley , Yasheen Zhou , Vincent S. Hernandez , Jacob J. Plattner , Charles Z. Ding , Kathy Cao , Yong-Kang Zhang , Andrew Benowitz , Tsutomu Akama , Jessica Sligar , Guofeng Jia , Ligong Ou , Neerja Saraswat , Sreekanth Ramachandran , Chris Diaper , Yanchen Zhang , Goverdhan Reddy Banda , James A. Nieman , Mehdi Keramane , Rahim Mohammed , Rajendra Subedi , Hong Liang , Rajeshwar Singh
发明人： Yi Xia , Michael Richard Kevin Alley , Yasheen Zhou , Vincent S. Hernandez , Jacob J. Plattner , Charles Z. Ding , Kathy Cao , Yong-Kang Zhang , Andrew Benowitz , Tsutomu Akama , Jessica Sligar , Guofeng Jia , Ligong Ou , Neerja Saraswat , Sreekanth Ramachandran , Chris Diaper , Yanchen Zhang , Goverdhan Reddy Banda , James A. Nieman , Mehdi Keramane , Rahim Mohammed , Rajendra Subedi , Hong Liang , Rajeshwar Singh
CPC分类号： A61K31/33 , A61K31/43 , A61K45/06 , C07F5/025 , Y02A50/401 , Y02A50/411 , A61K2300/00
摘要： This invention relates to, among other items, 6-substituted benzoxaborole compounds and their use for treating bacterial infections.
摘要翻译： 本发明涉及6-取代的苯并恶唑化合物及其用于治疗细菌感染的用途。
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公开(公告)号：US07582621B2
公开(公告)日：2009-09-01
申请号：US11357687
申请日：2006-02-16
申请人： Stephen J. Baker , Tsutomu Akama , Carolyn Bellinger-Kawahara , Vincent S. Hernandez , Karin M. Hold , James J. Leyden , Kirk R. Maples , Jacob J. Plattner , Virginia Sanders , Yong-Kang Zhang
发明人： Stephen J. Baker , Tsutomu Akama , Carolyn Bellinger-Kawahara , Vincent S. Hernandez , Karin M. Hold , James J. Leyden , Kirk R. Maples , Jacob J. Plattner , Virginia Sanders , Yong-Kang Zhang
CPC分类号： C07F5/025 , A61K9/0012 , A61K31/69 , C07F5/02 , C07F5/027
摘要： This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.
摘要翻译： 本发明涉及可用于治疗真菌感染的化合物，更具体地涉及甲真菌病和/或皮肤真菌感染的局部治疗。 本发明涉及对真菌具有活性的化合物，并具有允许化合物与患者接触时达到感染真菌的皮肤，指甲，毛发，爪或蹄特定部位的性质。 特别地，本发明化合物具有促进钉板穿透的物理化学性质。
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公开(公告)号：US07465836B2
公开(公告)日：2008-12-16
申请号：US10868268
申请日：2004-06-15
申请人： Ving Lee , Jacob J. Plattner , Stephen J. Benkovic , Stephen J. Baker , Kirk R. Maples , Carolyn Bellinger-Kawahara , Tsutomu Akama , Yong-Kang Zhang , Rajeshwar Singh , Vittorio A. Sauro
发明人： Ving Lee , Jacob J. Plattner , Stephen J. Benkovic , Stephen J. Baker , Kirk R. Maples , Carolyn Bellinger-Kawahara , Tsutomu Akama , Yong-Kang Zhang , Rajeshwar Singh , Vittorio A. Sauro
IPC分类号： C07F9/02
CPC分类号： C07F5/025
摘要： Compositions and methods of use of borole derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.
摘要翻译： 公开了用于治疗由细菌或病毒引起的疾病的治疗剂的硼烷衍生物，包括苯并恶唑，苯并唑并苯并噻唑的组合物和方法，以及合成所述试剂及其组合物的方法。
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公开(公告)号：US06869971B1
公开(公告)日：2005-03-22
申请号：US10110964
申请日：2000-10-19
申请人： Tsutomu Akama , Akira Asai , Tsutomu Agatsuma , Shinji Nara , Yoshinori Yamashita , Tamio Mizukami , Shun-ichi Ikeda , Yutaka Saitoh , Yutaka Kanda
发明人： Tsutomu Akama , Akira Asai , Tsutomu Agatsuma , Shinji Nara , Yoshinori Yamashita , Tamio Mizukami , Shun-ichi Ikeda , Yutaka Saitoh , Yutaka Kanda
IPC分类号： A61P31/04 , A61P35/00 , C07D487/04 , C07D487/14 , C07D487/16 , C07D491/14 , C07D491/147 , C07D491/16 , C07D498/08 , A61K31/403 , A61K31/4453 , C07D209/52 , C07D401/06
CPC分类号： C07D487/04 , C07D487/14 , C07D491/14
摘要： UCS 1025 derivatives having antitumor activity or antibacterial activity which are represented by formula (I): wherein R1 represents hydrogen, lower alkyl, etc.; R2 represents hydrogen, or is combined with R3 to represent a bond, etc., or is combined with R4 to represent —O(C═O)—, etc.; R3 represents hydrogen, etc., or is combined with R2 to represent a bond, etc.; R4 represents hydrogen, etc., or is combined with R2 to represent —(C═O)O—, etc.; R5 represents hydrogen or is combined with R6 to represent a bond; R6 represents hydrogen, etc., or is combined with R5 to represent a bond; R7 represents hydrogen or is combined with R8 to represent ═O; R8 represents hydroxy or is combined with R7 to represent ═O; ---- represents a single bond or a double bond, and a represents a single bond (two carbon atoms to which a is bound are combined to form a single bond) or an oxygen atom, or pharmaceutically acceptable salts thereof.
摘要翻译： 由式（I）表示的具有抗肿瘤活性或抗菌活性的UCS 1025衍生物：其中R 1表示氢，低级烷基等; R 2表示氢，或与R 3结合以表示键等，或与R 4结合以表示-O（C = O） - 等; R 3表示氢等，或与R 2结合以表示键等; R 4表示氢等，或与R 2结合代表 - （C = O）O-等; R 5表示氢或与R 6结合以表示键; R 6表示氢等，或与R 5结合以表示键; R 7表示氢或与R 8结合以代表= O; R 8表示羟基或与R 7结合代表= O; ----表示单键或双键，a表示单键（被结合形成单键的两个碳原子）或氧原子，或其药学上可接受的盐。
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公开(公告)号：US20050054644A1
公开(公告)日：2005-03-10
申请号：US10868268
申请日：2004-06-15
申请人： Ving Lee , Jacob Plattner , Stephen Benkovic , Stephen Baker , Kirk Maples , Carolyn Bellinger-Kawahara , Tsutomu Akama , Yong-Kang Zhang , Rajeshwar Singh , Vittorio Sauro
发明人： Ving Lee , Jacob Plattner , Stephen Benkovic , Stephen Baker , Kirk Maples , Carolyn Bellinger-Kawahara , Tsutomu Akama , Yong-Kang Zhang , Rajeshwar Singh , Vittorio Sauro
IPC分类号： A61K20060101 , A61K31/498 , A61K31/53 , A61K31/69 , C07D471/02 , C07D487/02 , C07F5/02
CPC分类号： C07F5/025
摘要： Compositions and methods of use of borole derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.
摘要翻译： 公开了用于治疗由细菌或病毒引起的疾病的治疗剂的硼烷衍生物，包括苯并恶唑，苯并唑并苯并噻唑的组合物和方法，以及合成所述试剂及其组合物的方法。
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公开(公告)号：US06815449B2
公开(公告)日：2004-11-09
申请号：US10289317
申请日：2002-11-07
申请人： Tsutomu Akama , Hiroyuki Nagata , Atsuhiro Hasegawa , Harumi Ue , Isami Takahashi , Yutaka Saitoh , Kenichi Mochida , Shun-ichi Ikeda , Yutaka Kanda
发明人： Tsutomu Akama , Hiroyuki Nagata , Atsuhiro Hasegawa , Harumi Ue , Isami Takahashi , Yutaka Saitoh , Kenichi Mochida , Shun-ichi Ikeda , Yutaka Kanda
IPC分类号： A61K314745
CPC分类号： C07D471/06
摘要： Compounds having immunosuppressive activity, cell growth inhibitory activity, anti-tumor activity, etc. are represented by formula I: and pharmaceutically acceptable salts thereof.
摘要翻译： 具有免疫抑制活性，细胞生长抑制活性，抗肿瘤活性等的化合物由式I表示：及其药学上可接受的盐。
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公开(公告)号：US09248088B2
公开(公告)日：2016-02-02
申请号：US10562410
申请日：2004-06-24
发明人： Calvin B. Harley , Allison C. Chin , Tsutomu Akama , Nancy Yuk-yu Ip , Yung-hou Wong , David M. Miller-Martini
摘要： Methods and cosmetic compositions for conditioning the skin, utilizing as active ingredients selected compounds structurally related to astragenols, cycloastragenols, and/or protopanaxatriols, are provided. Such compounds include those of formulas (I), (II) and (III) described herein.
摘要翻译： 提供用于调理皮肤的方法和化妆品组合物，其利用选择的与阿斯特灵醇，环状天冬氨酸和/或原人参三醇结构相关的化合物作为活性成分。 这些化合物包括本文所述的式（I），（II）和（III）的化合物。
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