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1. 发明申请

US20050069999A1 Sh3 domain binding inhibitors 审中-公开
标题翻译： Sh3结构域结合抑制剂
公开(公告)号：US20050069999A1
公开(公告)日：2005-03-31
申请号：US10483439
申请日：2002-04-19
申请人： Sreenath Sharma , Noriko Matsushita , Katsuhiko Ando , Chitose Yoshida , Hirofumi Nakano , Tsutomu Agatsuma , Yutaka Kanda
发明人： Sreenath Sharma , Noriko Matsushita , Katsuhiko Ando , Chitose Yoshida , Hirofumi Nakano , Tsutomu Agatsuma , Yutaka Kanda
IPC分类号： C12N9/99
CPC分类号： C07D309/10 , C07D491/06 , C07D491/20
摘要： The present invention provides SH3 domain binding inhibitors comprising, as an active ingredient, a non-peptide compound exhibiting SH3 domain binding inhibitory activity, a low molecular weight compound with molecular weight less than 750 which exhibit SH3 domain binding inhibitory activity, in particular, a compound represented by the general formula (I) or (II) described above, a cytochalsin, etc., or pharmaceutically acceptable salts thereof. The present invention also provides compounds represented by the general formula (Va), (Vb) or (VI) described above or pharmaceutically acceptable salts thereof.
摘要翻译：本发明提供SH3结构域结合抑制剂，其包含作为活性成分的表现SH3结构域结合抑制活性的非肽化合物，分子量小于750的低分子量化合物，其表现出SH3结构域结合抑制活性，特别是由上述通式（I）或（II）表示的化合物，细胞松弛素等，或其药学上可接受的盐。本发明还提供由上述通式（Va），（Vb）或（VI）表示的化合物或其药学上可接受的盐。

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

US5925641A Farnesyltransferase inhibitor 失效
标题翻译：法呢基转移酶抑制剂
公开(公告)号：US5925641A
公开(公告)日：1999-07-20
申请号：US912870
申请日：1997-08-19
申请人： Yutaka Kanda , Yutaka Saitoh , Kazuhito Akasaka , Tamio Mizukami , Hirofumi Nakano
发明人： Yutaka Kanda , Yutaka Saitoh , Kazuhito Akasaka , Tamio Mizukami , Hirofumi Nakano
IPC分类号： A61K31/495 , A61K31/54 , C07D241/08 , C07D513/08
CPC分类号： C07D513/08 , A61K31/495 , A61K31/54 , C07D241/08
摘要： The present invention relates to a farnesyltransferase inhibitor and an antitumor agent comprising, as an active ingredient, a piperazinedione derivative represented by formula (I): ##STR1## wherein R.sup.1 and R.sup.2 independently represent lower alkyl, lower alkoxyalkyl, substituted or unsubstituted aryl, or aralkyl; R.sup.3 and R.sup.4 independently represent mercapto, lower alkanoylthio, aroylthio, lower alkoxycarbonylthio, or aryloxycarbonylthio, or alternatively R.sup.3 and R.sup.4 are combined together to form disulfide; and R.sup.5 and R.sup.6 independently represent hydrogen, lower alkyl, lower alkoxyalkyl, hydroxyalkyl, lower alkanoyloxyalkyl, aroyloxyalkyl, aralkyloxyalkyl, or aralkyl.
摘要翻译：本发明涉及法呢基转移酶抑制剂和抗肿瘤剂，其包含作为活性成分的由式（I）表示的哌嗪二酮衍生物：其中R1和R2独立地表示低级烷基，低级烷氧基烷基，取代或未取代的芳基或芳烷基; R3和R4独立地表示巯基，低级烷酰硫基，芳酰硫基，低级烷氧基羰基硫基或芳氧基羰基硫基，或者R3和R4组合在一起形成二硫化物; R 5和R 6独立地表示氢，低级烷基，低级烷氧基烷基，羟烷基，低级烷酰氧基烷基，芳氧基烷基，芳烷氧基烷基或芳烷基。

4. 发明授权

US5728830A Farnesyltransferase inhibitor 失效
标题翻译：法呢基转移酶抑制剂
公开(公告)号：US5728830A
公开(公告)日：1998-03-17
申请号：US436458
申请日：1995-05-22
申请人： Yutaka Kanda , Yutaka Saitoh , Kazuhito Akasaka , Tamio Mizukami , Hirofumi Nakano
发明人： Yutaka Kanda , Yutaka Saitoh , Kazuhito Akasaka , Tamio Mizukami , Hirofumi Nakano
IPC分类号： A61K31/495 , A61K31/54 , C07D241/08 , C07D513/08 , C07D285/15
CPC分类号： C07D513/08 , A61K31/495 , A61K31/54 , C07D241/08
摘要： The present invention relates to a farnesyltransferase inhibitor and an antitumor agent comprising, as an active ingredient, a piperazinedione derivative represented by formula (I): ##STR1## wherein R.sup.1 and R.sup.2 independently represent lower alkyl, lower alkoxyalkyl, substituted or unsubstituted aryl, or aralkyl; R.sup.3 and R.sup.4 independently represent mercapto, lower alkanoylthio, aroylthio, lower alkoxycarbonylthio, or aryloxycarbonylthio, or alternatively R.sup.3 and R.sup.4 are combined together to form disulfide; and R.sup.5 and R.sup.6 independently represent hydrogen, lower alkyl, lower alkoxyalkyl, hydroxyalkyl, lower alkanoyloxyalkyl, aroyloxyalkyl, aralkyloxyalkyl, or aralkyl.
摘要翻译： PCT No.PCT / JP94 / 01543 Sec。 371日期：1995年5月22日 102（e）日期1995年5月22日PCT 1994年9月20日PCT公布。出版物WO95 / 08542 日期：1995年3月30日本发明涉及法呢基转移酶抑制剂和抗肿瘤剂，其包含作为活性成分的式（I）表示的哌嗪二酮衍生物：其中R 1和R 2独立地表示低级烷基，低级烷氧基烷基，取代或未取代的芳基或芳烷基; R3和R4独立地表示巯基，低级烷酰硫基，芳酰硫基，低级烷氧基羰基硫基或芳氧基羰基硫基，或者R3和R4组合在一起形成二硫化物; R 5和R 6独立地表示氢，低级烷基，低级烷氧基烷基，羟烷基，低级烷酰氧基烷基，芳氧基烷基，芳烷氧基烷基或芳烷基。

5. 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。

6. 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。

7. 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。

8. 发明申请

US20070265268A1 Hsp90 Family protein Inhibitors 有权
标题翻译： Hsp90家族蛋白抑制剂
公开(公告)号：US20070265268A1
公开(公告)日：2007-11-15
申请号：US11718079
申请日：2005-11-09
申请人： Yushi Kitamura , Yutaka Kanda , Takayuki Nakashima
发明人： Yushi Kitamura , Yutaka Kanda , Takayuki Nakashima
IPC分类号： A61K31/166 , A61K31/235 , A61K31/24 , A61K31/40 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/5375 , C07C229/34 , C07C235/44 , C07C69/84 , C07D207/08 , C07D213/04 , C07D265/30 , C07D295/14
CPC分类号： C07C235/64 , C07C69/88 , C07C235/60 , C07D213/40 , C07D295/192
摘要： The present invention provides Hsp90 family protein inhibitors comprising, as an active ingredient, a benzoic acid derivative represented by General Formula (I): [wherein n represents an integer of 0 to 10; R1 represents substituted or unsubstituted lower alkoxycarbonyl, substituted or unsubstituted aroyl, or the like; R2 represents —NR14R15 (wherein R14 and R15 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl or the like); R3 and R5 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl or the like; and R4 and R6 may be the same or different and each represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl or the like] or a prodrug thereof, or a pharmaceutically acceptable salt of said benzoic acid derivative or said prodrug.
摘要翻译：本发明提供Hsp90家族蛋白抑制剂，其包含通式（I）表示的苯甲酸衍生物作为活性成分：[其中，n表示0〜10的整数， R 1表示取代或未取代的低级烷氧基羰基，取代或未取代的芳酰基等; R 2表示-NR 14 R 15（其中R 14和R 15）可以相同或不同，各自表示氢原子，取代或未取代的低级烷基，取代或未取代的芳烷基等）; R 3和R 5可以相同或不同，各自表示氢原子，取代或未取代的低级烷基等; R 4和R 6可以相同或不同，各自表示氢原子，卤素，取代或未取代的低级烷基等]或其前药，或所述苯甲酸衍生物或所述前药的药学上可接受的盐。

9. 发明申请

US20070166305A1 Method of Modulating the Activity of Functional Immune Molecules 有权
公开(公告)号：US20070166305A1
公开(公告)日：2007-07-19
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： A61K39/395
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.

10. 发明申请

US20070117856A1 Indazole derivatives 失效
标题翻译：吲唑衍生物
公开(公告)号：US20070117856A1
公开(公告)日：2007-05-24
申请号：US10548475
申请日：2004-07-30
申请人： Yoshihisa Ohta , Fumihiko Kanai , Shinji Nara , Yutaka Kanda , Hiroshi Umehara , Yukimasa Shiotsu , Tomoki Naoe , Hitoshi Kiyoi , Keiko Kawashima , Hiromi Ando , Motoki Miyama
发明人： Yoshihisa Ohta , Fumihiko Kanai , Shinji Nara , Yutaka Kanda , Hiroshi Umehara , Yukimasa Shiotsu , Tomoki Naoe , Hitoshi Kiyoi , Keiko Kawashima , Hiromi Ando , Motoki Miyama
IPC分类号： A61K31/416 , C07D231/56
CPC分类号： C07D231/56
摘要： The present invention provides a compound represented by Formula (I): [wherein R1 represents CONR1aR1b (wherein R1a and R1b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R1a and R1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group) or the like, R2 represents a hydrogen atom, CONR2aR2b (wherein R2a and R2b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R2a and R2b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group), NR2cR2d (wherein R2c and R2d may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkanoyl, substituted or unsubstituted aroyl, substituted or unsubstituted heteroaroyl, substituted or unsubstituted ararkyl, substituted or unsubstituted lower alkylsulfonyl or substituted or unsubstituted lower arylsulfonyl) or the like].
摘要翻译：本发明提供由式（I）表示的化合物：[其中R 1表示CONR 1a 1b 1b（其中R 1a） R 1b和R 1b可以相同或不同，各自表示氢原子，取代或未取代的低级烷基，取代或未取代的芳基，取代或未取代的芳烷基或取代或未取代的杂环基，或R 1a和R 1b与相邻的氮原子一起形成取代或未取代的杂环基）等，R 2 O， >表示氢原子，其中R 2a，R 2b和R 2b可以相同或不同，各自表示氢原子，取代或未取代的低级烷基，取代或未取代的芳基，取代或未取代的芳烷基或取代或未取代的杂环基，或R 2b和R 2b >与t结合在一起它与氮原子相邻以形成取代或未取代的杂环基），NR 2c R 2d（其中R 2c和R 2d）取代或未取代的低级烷酰基，取代或未取代的芳酰基，取代或未取代的杂芳酰基，取代或未取代的芳烷基，取代或未取代的低级烷基磺酰基或取代或未取代的低级芳基磺酰基等）。

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