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1. 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。

2. 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。

3. 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。

4. 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。

5. 发明授权

US07605272B2 IGF-1R inhibitor 有权
标题翻译： IGF-1R抑制剂
公开(公告)号：US07605272B2
公开(公告)日：2009-10-20
申请号：US11814753
申请日：2006-01-27
申请人： Yutaka Kanda , Hiromi Ando , Keiko Kawashima , Takamasa Sugita , Masayo Suzuki , Hisashi Tagaya , Tomoyuki Nakazato , Yoshinori Yamashita , Takeshi Takahashi , Shinji Nara , Hiroaki Nakamura
发明人： Yutaka Kanda , Hiromi Ando , Keiko Kawashima , Takamasa Sugita , Masayo Suzuki , Hisashi Tagaya , Tomoyuki Nakazato , Yoshinori Yamashita , Takeshi Takahashi , Shinji Nara , Hiroaki Nakamura
IPC分类号： C07D231/56 , C07D211/06 , C07D413/10 , C07D403/10 , A61K31/416 , A61K31/4439 , A61K31/496 , A61K31/5355 , A61K31/5377
CPC分类号： C07D231/56 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D491/10 , C07D495/04
摘要： The present invention provides a type I insulin-like growth factor receptor (IGF-1R) inhibitor comprising, as an active ingredient, an indazole derivative represented by Formula (I): {wherein R1 represents —NR4R5 [wherein R4 represents a hydrogen atom or the like, R5 represents substituted or unsubstituted lower alkyl, —C(═O)R6 (wherein R6 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl or the like), or the like], or the like, and R2 and R3 may be the same or different and each represents a hydrogen atom, hydroxy, substituted or unsubstituted lower alkoxy, or the like} or a pharmaceutically acceptable salt thereof, and the like.
摘要翻译：本发明提供一种I型胰岛素样生长因子受体（IGF-1R）抑制剂，其包含作为活性成分的由式（I）表示的吲唑衍生物：其中R 1表示-NR 4 R 5 [其中R 4表示氢原子或 R 5表示取代或未取代的低级烷基，-C（-O）R 6（其中R 6表示取代或未取代的低级烷基，取代或未取代的芳基等），R 2和R 3可以相同或不同的，并且各自表示氢原子，羟基，取代或未取代的低级烷氧基等}或其药学上可接受的盐等。

6. 发明申请

US20090054508A1 IGF-1R INHIBITOR 有权
标题翻译： IGF-1R抑制剂
公开(公告)号：US20090054508A1
公开(公告)日：2009-02-26
申请号：US11814753
申请日：2006-01-27
申请人： Yutaka Kanda , Hiromi Ando , Keiko Kawashima , Takamasa Sugita , Masayo Suzuki , Hisashi Tagaya , Tomoyuki Nakazato , Yoshinori Yamashita , Takeshi Takahashi , Shinji Nara , Hiroaki Nakamura
发明人： Yutaka Kanda , Hiromi Ando , Keiko Kawashima , Takamasa Sugita , Masayo Suzuki , Hisashi Tagaya , Tomoyuki Nakazato , Yoshinori Yamashita , Takeshi Takahashi , Shinji Nara , Hiroaki Nakamura
IPC分类号： A61K31/416 , A61P3/10
CPC分类号： C07D231/56 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D491/10 , C07D495/04
摘要： The present invention provides a type I insulin-like growth factor receptor (IGF-1R) inhibitor comprising, as an active ingredient, an indazole derivative represented by Formula (I): {wherein R1 represents —NR4R5 [wherein R4 represents a hydrogen atom or the like, R5 represents substituted or unsubstituted lower alkyl, —C(═O)R6 (wherein R6 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl or the like), or the like], or the like, and R2 and R3 may be the same or different and each represents a hydrogen atom, hydroxy, substituted or unsubstituted lower alkoxy, or the like} or a pharmaceutically acceptable salt thereof, and the like.
摘要翻译：本发明提供一种I型胰岛素样生长因子受体（IGF-1R）抑制剂，其包含作为活性成分的由式（I）表示的吲唑衍生物：其中R 1表示-NR 4 R 5 [其中R 4表示氢原子或 R 5表示取代或未取代的低级烷基，-C（-O）R 6（其中R 6表示取代或未取代的低级烷基，取代或未取代的芳基等）等，等等，R2和R3 可以相同或不同，各自表示氢原子，羟基，取代或未取代的低级烷氧基等}或其药学上可接受的盐等。

7. 发明授权

US6080771A DC107 derivatives 失效
标题翻译： DC107衍生品
公开(公告)号：US6080771A
公开(公告)日：2000-06-27
申请号：US133363
申请日：1998-08-13
申请人： Yutaka Kanda , Hitoshi Arai , Hiroyuki Yamaguchi , Tadashi Ashizawa , Shun-ichi Ikeda , Chikara Murakata , Tatsuya Tamaoki
发明人： Yutaka Kanda , Hitoshi Arai , Hiroyuki Yamaguchi , Tadashi Ashizawa , Shun-ichi Ikeda , Chikara Murakata , Tatsuya Tamaoki
IPC分类号： C07D513/08 , C07D513/18 , C07D513/20 , C07H15/26 , C07H17/02 , A61K31/425 , A61K31/70 , C07D519/00
CPC分类号： C07D513/08 , C07H15/26 , C07H17/02
摘要： DC107 derivatives represented by formula (I) or pharmaceutically acceptable salts thereof which have antimicrobial activity and antitumor activity are provided: ##STR1## wherein R.sup.1 represents CO(CR.sup.4A R.sup.4B).sub.n1 (O(CH.sub.2).sub.p1).sub.n2 OR.sup.5 {wherein n1 represents an integer of 1 or 2; R.sup.4A and R.sup.4B are the same or different, and each represents hydrogen or lower alkyl; p1 and n2 each represents an integer of 1 to 10; and R.sup.5 represents hydrogen, lower alkyl, or the like), or ##STR2##
摘要翻译：提供了具有抗微生物活性和抗肿瘤活性的由式（I）表示的DC107衍生物或其药学上可接受的盐，其中R1表示CO（CR4AR4B）n1（O（CH2）p1）n2OR5 {其中n1表示1或2的整数; R4A和R4B相同或不同，各自表示氢或低级烷基; p1和n2各自表示1〜10的整数，和R 5表示氢，低级烷基等）

8. 发明授权

US5981558A DC107 derivatives 失效
标题翻译： DC107衍生品
公开(公告)号：US5981558A
公开(公告)日：1999-11-09
申请号：US133614
申请日：1998-08-13
申请人： Hitoshi Arai , Yutaka Kanda , Hiroyuki Yamaguchi , Tadashi Ashizawa , Chikara Murakata , Shun-ichi Ikeda , Tatsuya Tamaoki
发明人： Hitoshi Arai , Yutaka Kanda , Hiroyuki Yamaguchi , Tadashi Ashizawa , Chikara Murakata , Shun-ichi Ikeda , Tatsuya Tamaoki
IPC分类号： C07D513/18 , C07H15/26 , C07D513/08 , A61K31/425
CPC分类号： C07D513/18 , C07H15/26
摘要： DC107 derivatives represented by formula (I) or pharmaceutically acceptable salts thereof which have antimicrobial activity and antitumor activity are provided: ##STR1## wherein R.sup.1 represents hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR.sup.4, or the like; R.sup.2 represents hydrogen or COR.sup.6 ; R.sup.3 represents --CH.sub.2 OCOR.sup.7, phthalimidomethyl, or the like; and W represents oxygen or NR.sup.8 (wherein R.sup.8 represents hydroxy, lower alkoxy, lower alkenyloxy, aralkyloxy, substituted or unsubstituted arylsulfonylamino, or lower alkoxycarbonylamino).
摘要翻译：提供了具有抗微生物活性和抗肿瘤活性的由式（I）表示的DC107衍生物或其药学上可接受的盐，其中R1表示氢，低级烷氧基烷基，芳烷氧基烷基，低级烷氧基烷氧基烷基，低级烷氧基烷氧基烷氧基烷基，芳烷基，四氢吡喃基，COR4等; R2表示氢或COR6; R3表示-CH2OCOR7，苯二甲酰亚氨基甲基等; W表示氧或NR8（其中R8表示羟基，低级烷氧基，低级烯氧基，芳烷氧基，取代或未取代的芳基磺酰基氨基或低级烷氧基羰基氨基）。

9. 发明授权

US07776849B2 Benzenoid ansamycin derivative 失效
标题翻译：苯并安沙霉素衍生物
公开(公告)号：US07776849B2
公开(公告)日：2010-08-17
申请号：US11917239
申请日：2006-06-29
申请人： Shinpei Yamaguchi , Takayuki Nakashima , Yutaka Kanda
发明人： Shinpei Yamaguchi , Takayuki Nakashima , Yutaka Kanda
IPC分类号： A61K31/395 , C07D225/06 , A61P35/00
CPC分类号： C07D225/06 , C07F7/1804
摘要： The present invention provides a benzenoid ansamycin derivative represented by Formula (I) (wherein R1 and R2 each represent a hydrogen atom or are combined together to form a bond, R8 represents a bond or an oxygen atom, R11 represents hydroxy, substituted or unsubstituted lower alkoxy or substituted or unsubstituted lower alkanoyloxy, R15 represents a hydrogen atom or methoxy, R22 represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkanoyl or substituted or unsubstituted aroyl, R4 and R5 each represent a hydrogen atom or are combined together to form a bond, R18 represents a hydrogen atom, or the like, R21 represents hydroxy or the like, and R17 and R19 may be the same or different and each represents a hydrogen atom, or the like) or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供由式（I）表示的苯并安莎霉素衍生物（其中R1和R2各自表示氢原子或组合在一起形成键，R8表示键或氧原子，R11表示羟基，取代或未取代的低级烷氧基或取代或未取代的低级烷酰氧基，R 15表示氢原子或甲氧基，R 22表示氢原子，取代或未取代的低级烷基，取代或未取代的低级烷酰基或取代或未取代的芳酰基，R4和R5各自表示氢原子或被结合一起形成键，R 18表示氢原子等，R 21表示羟基等，R 17和R 19可以相同或不同，各自表示氢原子等）或其药学上可接受的盐。

10. 发明授权

US07687061B2 Method of modulating the activity of functional immune molecules to Her-2 有权
标题翻译：将功能性免疫分子活性调节为Her-2的方法
公开(公告)号：US07687061B2
公开(公告)日：2010-03-30
申请号：US11686920
申请日：2007-03-15
申请人： Nobuo Hanai , Kazuyasu Nakamura , Emi Hosaka , Motoo Yamasaki , Kazuhisa Uchida , Toyohide Shinkawa , Susumu Imabeppu , Yutaka Kanda , Naoko Yamane , Hideharu Anazawa
发明人： Nobuo Hanai , Kazuyasu Nakamura , Emi Hosaka , Motoo Yamasaki , Kazuhisa Uchida , Toyohide Shinkawa , Susumu Imabeppu , Yutaka Kanda , Naoko Yamane , Hideharu Anazawa
IPC分类号： A61K39/00 , A61K39/395
CPC分类号： C07K16/3084 , A61K2039/505 , C07K16/2866 , C07K16/30 , C07K2317/21 , C07K2317/24 , C07K2317/41 , C07K2317/52 , C07K2317/565 , C07K2317/73 , C07K2317/732 , C07K2319/00 , C12P21/005 , G01N33/53
摘要： The invention relates to a method for controlling the activity of an immunologically functional molecule, such as an antibody, a protein, a peptide or the like, an agent of promoting the activity of an immunologically functional molecule, and an immunologically functional molecule having the promoted activity.
摘要翻译：本发明涉及一种控制免疫功能性分子如抗体，蛋白质，肽等的活性的方法，促进免疫功能性分子活性的试剂和具有促进作用的免疫功能分子活动。

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