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1. 发明授权

US06815449B2 LK6-A derivatives 失效
标题翻译： LK6-A衍生物
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。

2. 发明授权

US06613774B1 Pyrrolo [4,3,2-de] quinoline derivatives 失效
标题翻译：吡咯并[4,3,2-de]喹啉衍生物
公开(公告)号：US06613774B1
公开(公告)日：2003-09-02
申请号：US09720900
申请日：2001-01-02
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： LK6-A derivatives which have immmunosuppressive activity, cell growth inhibitory activity, anti-tumor activity, etc. and which are represented by general formula (I): as defined herein, and pharmaceutically acceptable salts thereof.
摘要翻译： LK6-A衍生物，其具有免疫抑制活性，细胞生长抑制活性，抗肿瘤活性等，并且由通式（I）表示：如本文所定义，及其药学上可接受的盐。

3. 发明授权

US06869971B1 UCS1025 derivatives 失效
标题翻译： UCS1025衍生品
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。

4. 发明授权

US5539112A 5-aminoflavone derivatives 失效
标题翻译： 5-氨基黄酮衍生物
公开(公告)号：US5539112A
公开(公告)日：1996-07-23
申请号：US464093
申请日：1995-06-05
申请人： Tsutomu Akama , Shun-ichi Ikeda , Yasushi Shida , Masaji Kasai , Hiroyuki Ishida , Uichiro Kimura , Katsushige Gomi , Hiromitsu Saito , Kimihisa Ueno
发明人： Tsutomu Akama , Shun-ichi Ikeda , Yasushi Shida , Masaji Kasai , Hiroyuki Ishida , Uichiro Kimura , Katsushige Gomi , Hiromitsu Saito , Kimihisa Ueno
IPC分类号： C07D311/30 , C07D413/12
CPC分类号： C07D311/30
摘要： 5-Aminoflavone derivatives represented by the formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and represent hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, halogen-substituted or unsubstituted lower alkanoyl or lower alkoxycarbonyl, X.sup.1, X.sup.2, Y.sup.1 and Y.sup.2 are the same or different and represent hydrogen, halogen or lower alkyl, at least one of X.sup.1 and X.sup.2 represents halogen or lower alkyl, X.sup.3 represents hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, lower alkynyl, halogen, hydroxy, substituted or unsubstituted lower alkoxy, NR.sup.5 R.sup.6 (wherein R.sup.5 and R.sup.6 are the same or different and represent hydrogen, or substituted or unsubstituted lower alkyl, or R.sup.5 and R.sup.6 are taken together to form a heterocyclic group containing the nitrogen atom in the ring), lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, carboxy, lower alkoxycarbonyl, lower alkanoyl, adizo, cyano, substituted or unsubstituted carbamoyl or lower alkylthiothiocarbonyl: or pharmaceutically acceptable salts thereof.
摘要翻译：由式（I）表示的5-氨基黄酮衍生物：其中R 1，R 2，R 3和R 4相同或不同，表示氢，取代或未取代的低级烷基，低级烯基，卤素取代或未取代的低级烷酰基或低级烷氧基羰基，X 1，X 2，Y 1和Y 2相同或不同，表示氢，卤素或低级烷基，X 1和X 2中的至少一个表示卤素或低级烷基，X 3表示氢，取代或未取代的低级烷基，低级烯基，低级炔基，卤素，羟基，取代或未取代的低级烷氧基，NR5R6（其中R5和R6相同或不同，代表氢，或取代或未取代的低级烷基，或R5和R6一起形成含有环中的氮原子），低级烷硫基，低级烷基亚磺酰基，低级烷基磺酰基，羧基，低级烷氧基羰基，低级烷酰基，二唑基，氰基，取代或未取代的氨基甲酰基或低级烷硫基硫代辛基或其药学上可接受的盐。

5. 发明授权

US06518268B1 Telomerase inhibitors and methods of their use 失效
标题翻译：端粒酶抑制剂及其使用方法
公开(公告)号：US06518268B1
公开(公告)日：2003-02-11
申请号：US09608636
申请日：2000-06-30
申请人： Allison C. Chin , Ryan Holcomb , Mieczyslaw A. Piatyszek , Upinder Singh , Richard L. Tolman , Tsutomu Akama , Yutaka Kanda , Akira Asai , Yoshinori Yamashita , Kaori Endo , Hiroyuki Yamaguchi
发明人： Allison C. Chin , Ryan Holcomb , Mieczyslaw A. Piatyszek , Upinder Singh , Richard L. Tolman , Tsutomu Akama , Yutaka Kanda , Akira Asai , Yoshinori Yamashita , Kaori Endo , Hiroyuki Yamaguchi
IPC分类号： A61K31535
CPC分类号： A61K31/426 , A61K31/4439 , A61K31/506 , C07D277/34 , C07D277/36 , C07D417/06 , C07D417/10 , C07D513/04
摘要： Thiazolidinedione compounds, compositions, and methods of inhibiting telomerase activity in vitro and treatment of telomerase mediated conditions or diseases ex vivo and in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of conditions or diseases mediated by telomerase activity, such as in the treatment of cancer. Also disclosed are novel methods for assaying or screening for inhibitors of telomerase activity.
摘要翻译：提供噻唑烷二酮化合物，组合物和在体外抑制端粒酶活性的方法以及离体和体内治疗端粒酶介导的病症或疾病。本发明的方法，化合物和组合物可以单独使用或与其它药理学活性剂组合用于治疗由端粒酶活性介导的病症或疾病，例如治疗癌症。还公开了用于测定或筛选端粒酶活性抑制剂的新方法。

6. 发明授权

US08895534B2 Boron containing small molecules 有权
标题翻译：硼含有小分子
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。

7. 发明申请

US20100267981A1 BORON-CONTAINING SMALL MOLECULES 有权
标题翻译：含硼的小分子
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。

8. 发明申请

US20100256092A1 BORON-CONTAINING SMALL MOLECULES 审中-公开
标题翻译：含硼的小分子
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
IPC分类号： A61K31/69 , C07F5/02 , A61P31/04 , A01N55/08 , A01P1/00 , C12N9/99
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。

9. 发明授权

US07582621B2 Boron-containing small molecules 有权
标题翻译：含硼的小分子
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
IPC分类号： A61K31/69 , C07F5/04
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。

10. 发明授权

US07465836B2 Hydrolytically-resistant boron-containing therapeutics and methods of use 有权
标题翻译：耐水解硼含量治疗剂及使用方法
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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