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1. 发明授权

US07799827B2 Macrocyclic compounds useful as pharmaceuticals 有权
标题翻译：用作药物的大环化合物
公开(公告)号：US07799827B2
公开(公告)日：2010-09-21
申请号：US10507067
申请日：2003-03-07
申请人： Roch Boivin , Kenichi Chiba , Jesse Chow , Hong Du , Yoshihito Eguchi , Masanori Fujita , Masaki Goto , Fabian Gusovsky , Jean-Christophe Harmange , Atsushi Inoue , Yimin Jiang , Megumi Kawada , Takatoshi Kawai , Yoshiyuki Kawakami , Akifumi Kimura , Makoto Kotake , Yoshikazu Kuboi , Charles-André Lemelin , Xiang-Yi Li , Tomohiro Matsushima , Yoshiharu Mizui , Kenzo Muramoto , Hideki Sakurai , Yong-Chun Shen , Hiroshi Shirota , Mark Spyvee , Isao Tanaka , John (Yuan) Wang , Satoshi Yamamoto , Naoki Yoneda
发明人： Roch Boivin , Kenichi Chiba , Jesse Chow , Hong Du , Yoshihito Eguchi , Masanori Fujita , Masaki Goto , Fabian Gusovsky , Jean-Christophe Harmange , Atsushi Inoue , Yimin Jiang , Megumi Kawada , Takatoshi Kawai , Yoshiyuki Kawakami , Akifumi Kimura , Makoto Kotake , Yoshikazu Kuboi , Charles-André Lemelin , Xiang-Yi Li , Tomohiro Matsushima , Yoshiharu Mizui , Kenzo Muramoto , Hideki Sakurai , Yong-Chun Shen , Hiroshi Shirota , Mark Spyvee , Isao Tanaka , John (Yuan) Wang , Satoshi Yamamoto , Naoki Yoneda
IPC分类号： A61K31/335 , C07D313/00
CPC分类号： C07D405/12 , A61K31/335 , A61K31/36 , A61K31/395 , C07D231/12 , C07D233/56 , C07D249/08 , C07D313/00 , C07D401/12 , C07D491/04 , C07D491/044 , C07D493/04 , Y02A50/411
摘要： The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis, wherein R1-R11, X, Y, Z, and n are as defined herein.
摘要翻译：本发明提供了具有式（I）的化合物：另外提供了其合成方法及其用于治疗各种疾病（包括炎性或自身免疫性疾病以及涉及恶性肿瘤或增加血管发生的疾病）的方法，其中R1-R11， X，Y，Z和n如本文所定义。

2. 发明授权

US08329742B2 Macrocyclic compounds useful as pharmaceuticals 有权
标题翻译：用作药物的大环化合物
公开(公告)号：US08329742B2
公开(公告)日：2012-12-11
申请号：US12839873
申请日：2010-07-20
申请人： Roch Boivin , Kenichi Chiba , Jesse Chow , Hong Du , Yoshihito Eguchi , Masanori Fujita , Masaki Goto , Fabian Gusovsky , Jean-Christophe Harmange , Atsushi Inoue , Yimin Jiang , Megumi Kawada , Takatoshi Kawai , Yoshiyuki Kawakami , Akifumi Kimura , Makoto Kotake , Yoshikazu Kuboi , Charles-André Lemelin , Xiang-Yi Li , Tomohiro Matsushima , Yoshiharu Mizui , Kenzo Muramoto , Hideki Sakurai , Yong-Chun Shen , Hiroshi Shirota , Mark Spyvee , Isao Tanaka , John (Yuan) Wang , Satoshi Yamamoto , Naoki Yoneda
发明人： Roch Boivin , Kenichi Chiba , Jesse Chow , Hong Du , Yoshihito Eguchi , Masanori Fujita , Masaki Goto , Fabian Gusovsky , Jean-Christophe Harmange , Atsushi Inoue , Yimin Jiang , Megumi Kawada , Takatoshi Kawai , Yoshiyuki Kawakami , Akifumi Kimura , Makoto Kotake , Yoshikazu Kuboi , Charles-André Lemelin , Xiang-Yi Li , Tomohiro Matsushima , Yoshiharu Mizui , Kenzo Muramoto , Hideki Sakurai , Yong-Chun Shen , Hiroshi Shirota , Mark Spyvee , Isao Tanaka , John (Yuan) Wang , Satoshi Yamamoto , Naoki Yoneda
IPC分类号： A61K31/355 , C07D313/00
CPC分类号： C07D405/12 , A61K31/335 , A61K31/36 , A61K31/395 , C07D231/12 , C07D233/56 , C07D249/08 , C07D313/00 , C07D401/12 , C07D491/04 , C07D491/044 , C07D493/04 , Y02A50/411
摘要： The present invention provides methods for the use of compounds having formula (I) in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis, wherein R1-R11, t, X, Y, Z, and n are as defined herein.
摘要翻译：本发明提供了使用具有式（I）的化合物在治疗各种疾病（包括炎性或自身免疫性疾病）以及涉及恶性肿瘤或增加血管发生的疾病的方法，其中R1-R11，t，X，Y，Z和n 如本文所定义。

3. 发明申请

US20110144101A1 MACROCYCLIC COMPOUNDS USEFUL AS PHARMACEUTICALS 有权
标题翻译：大环化合物作为药物有用
公开(公告)号：US20110144101A1
公开(公告)日：2011-06-16
申请号：US12839873
申请日：2010-07-20
申请人： Roch Boivin , Kenichi Chiba , Jesse Chow , Hong Du , Yoshihito Eguchi , Masanori Fujita , Masaki Goto , Fabian Gusovsky , Jean-Christophe Harmange , Atsushi Inoue , Yimin Jiang , Megumi Kawada , Takatoshi Kawai , Yoshiyuki Kawakami , Akifumi Kimura , Makoto Kotake , Yoshikazu Kuboi , Charles-André Lemelin , Xiang-Yi Li , Tomohiro Matsushima , Yoshiharu Mizui , Kenzo Muramoto , Hideki Sakurai , Yong-Chun Shen , Hiroshi Shirota , Mark Spyvee , Isao Tanaka , John (Yuan) Wang , Satoshi Yamamoto , Naoki Yoneda
发明人： Roch Boivin , Kenichi Chiba , Jesse Chow , Hong Du , Yoshihito Eguchi , Masanori Fujita , Masaki Goto , Fabian Gusovsky , Jean-Christophe Harmange , Atsushi Inoue , Yimin Jiang , Megumi Kawada , Takatoshi Kawai , Yoshiyuki Kawakami , Akifumi Kimura , Makoto Kotake , Yoshikazu Kuboi , Charles-André Lemelin , Xiang-Yi Li , Tomohiro Matsushima , Yoshiharu Mizui , Kenzo Muramoto , Hideki Sakurai , Yong-Chun Shen , Hiroshi Shirota , Mark Spyvee , Isao Tanaka , John (Yuan) Wang , Satoshi Yamamoto , Naoki Yoneda
IPC分类号： A61K31/5377 , A61K31/335 , A61K31/4184 , A61P29/00 , A61P37/00 , A61P17/06 , A61P11/06 , A61P35/00 , A61P1/00
CPC分类号： C07D405/12 , A61K31/335 , A61K31/36 , A61K31/395 , C07D231/12 , C07D233/56 , C07D249/08 , C07D313/00 , C07D401/12 , C07D491/04 , C07D491/044 , C07D493/04 , Y02A50/411
摘要： The present invention provides methods for the use of compounds having formula (I) in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis, wherein R1-R11, t, X, Y, Z, and n are as defined herein.
摘要翻译：本发明提供了使用具有式（I）的化合物在治疗各种疾病（包括炎性或自身免疫性疾病）以及涉及恶性肿瘤或增加血管发生的疾病的方法，其中R1-R11，t，X，Y，Z和n 如本文所定义。

4. 发明申请

US20130196987A1 MACROCYCLIC COMPOUNDS USEFUL AS PHARMACEUTICALS 审中-公开
标题翻译：大环化合物作为药物有用
公开(公告)号：US20130196987A1
公开(公告)日：2013-08-01
申请号：US13663857
申请日：2012-10-30
申请人： Roch Boivin , Kenichi Chiba , Jesse Chow , Hong Du , Yoshihito Eguchi , Masanori Fujita , Masaki Goto , Fabian Gusovsky , Jean-Christophe Harmange , Atsushi Inoue , Yimin Jiang , Megumi Kawada , Takatoshi Kawai , Yoshiyuki Kawakami , Akifumi Kimura , Makoto Kotake , Yoshikazu Kuboi , Charles-Andre Lemelin , Xiang-Yi Li , Tomohiro Matsushima , Yoshiharu Mizui , Kenzo Muramoto , Hideki Sakurai , Yong-Chun Shen , Hiroshi Shirota , Mark Spyvee , Isao Tanaka , John (Yuan) Wang , Satoshi Yamamoto , Naoki Yoneda
发明人： Roch Boivin , Kenichi Chiba , Jesse Chow , Hong Du , Yoshihito Eguchi , Masanori Fujita , Masaki Goto , Fabian Gusovsky , Jean-Christophe Harmange , Atsushi Inoue , Yimin Jiang , Megumi Kawada , Takatoshi Kawai , Yoshiyuki Kawakami , Akifumi Kimura , Makoto Kotake , Yoshikazu Kuboi , Charles-Andre Lemelin , Xiang-Yi Li , Tomohiro Matsushima , Yoshiharu Mizui , Kenzo Muramoto , Hideki Sakurai , Yong-Chun Shen , Hiroshi Shirota , Mark Spyvee , Isao Tanaka , John (Yuan) Wang , Satoshi Yamamoto , Naoki Yoneda
IPC分类号： C07D405/12 , C07D491/044 , C07D313/00
CPC分类号： C07D405/12 , A61K31/335 , A61K31/36 , A61K31/395 , C07D231/12 , C07D233/56 , C07D249/08 , C07D313/00 , C07D401/12 , C07D491/04 , C07D491/044 , C07D493/04 , Y02A50/411
摘要： The present invention provides compounds, methods for the synthesis thereof and methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis.
摘要翻译：本发明提供了化合物，其合成方法及其用于治疗各种疾病（包括炎性或自身免疫性疾病）以及涉及恶性肿瘤或增加血管生成的疾病的方法。

5. 发明申请

US20060247448A1 Macrocyclic compounds useful as pharmaceuticals 有权
标题翻译：用作药物的大环化合物
公开(公告)号：US20060247448A1
公开(公告)日：2006-11-02
申请号：US10507067
申请日：2003-03-07
申请人： Roch Boivin , Kenichi Chiba , Jesse Chow , Hong Du , Yoshihito Eguchi , Masanori Fujita , Masaki Goto , Fabian Gusovsky , Jean-Christophe Harmanage , Atsushi Inoue , Yimin Jiang , Megumi Kawada , Takatoshi Kawai , Yoshiyuki Kawakami , Akifumi Kimura , Makoto Kotake , Yoshikazu Kuboi , Charles-Andre Lemelin , Xiang-Yi Li , Tomohiro Matsushima , Yoshiharu Mizui , Kenzo Muramoto , Hideki Sakurai , Yong-Chun Shen , Hiroshi Shirota , Mark Spyvee , Isao Tanaka , John Wang , Satoshi Yamamoto , Naoki Yoneda
发明人： Roch Boivin , Kenichi Chiba , Jesse Chow , Hong Du , Yoshihito Eguchi , Masanori Fujita , Masaki Goto , Fabian Gusovsky , Jean-Christophe Harmanage , Atsushi Inoue , Yimin Jiang , Megumi Kawada , Takatoshi Kawai , Yoshiyuki Kawakami , Akifumi Kimura , Makoto Kotake , Yoshikazu Kuboi , Charles-Andre Lemelin , Xiang-Yi Li , Tomohiro Matsushima , Yoshiharu Mizui , Kenzo Muramoto , Hideki Sakurai , Yong-Chun Shen , Hiroshi Shirota , Mark Spyvee , Isao Tanaka , John Wang , Satoshi Yamamoto , Naoki Yoneda
IPC分类号： C07D313/08
CPC分类号： C07D405/12 , A61K31/335 , A61K31/36 , A61K31/395 , C07D231/12 , C07D233/56 , C07D249/08 , C07D313/00 , C07D401/12 , C07D491/04 , C07D491/044 , C07D493/04 , Y02A50/411
摘要： The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis, wherein R1-R11, X, Y, Z, and n are as defined herein.
摘要翻译：本发明提供具有式（I）的化合物：另外提供其合成方法及其用于治疗各种疾病（包括炎性或自身免疫性疾病）以及涉及恶性肿瘤或增加血管发生的疾病的方法，其中R 1，R 11，X，Y，Z和n如本文所定义。

6. 发明授权

US07915306B2 Macrocyclic compounds useful as pharmaceuticals 有权
标题翻译：用作药物的大环化合物
公开(公告)号：US07915306B2
公开(公告)日：2011-03-29
申请号：US10657910
申请日：2003-09-09
申请人： Kenichi Chiba , Hong Du , Yoshihito Eguchi , Masanori Fujita , Masaki Goto , Fabian Gusovsky , Jean-Christophe Harmange , Atsushi Inoue , Megumi Kawada , Takatoshi Kawai , Yoshiyuki Kawakami , Akifumi Kimura , Makoto Kotake , Yoshikazu Kuboi , Tomohiro Matsushima , Yoshiharu Mizui , Kenzo Muramoto , Hideki Sakurai , Yong-Chun Shen , Hiroshi Shirota , Mark Spyvee , Isao Tanaka , John (Yuan) Wang , Ray Wood , Satoshi Yamamoto , Naoki Yoneda
发明人： Kenichi Chiba , Hong Du , Yoshihito Eguchi , Masanori Fujita , Masaki Goto , Fabian Gusovsky , Jean-Christophe Harmange , Atsushi Inoue , Megumi Kawada , Takatoshi Kawai , Yoshiyuki Kawakami , Akifumi Kimura , Makoto Kotake , Yoshikazu Kuboi , Tomohiro Matsushima , Yoshiharu Mizui , Kenzo Muramoto , Hideki Sakurai , Yong-Chun Shen , Hiroshi Shirota , Mark Spyvee , Isao Tanaka , John (Yuan) Wang , Ray Wood , Satoshi Yamamoto , Naoki Yoneda
IPC分类号： A61K31/335
CPC分类号： C07D493/04 , C07D313/00
摘要： The present invention provides compositions comprising compounds having formula (I): and additionally provides methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis, wherein R1-R11, X, Y, Z, and n are as defined herein. In certain embodiments, the compositions are for systemic (e.g., oral) administration. In certain embodiments, methods for the treatment of various disorders including inflammatory or autoimmune disorders comprise systemically (e.g., orally) administering to a subject in need thereof a therapeutically effective amount of a compound of formula (I).
摘要翻译：本发明提供了包含具有式（I）的化合物的组合物：另外提供了其用于治疗各种疾病（包括炎性或自身免疫性疾病）以及涉及恶性肿瘤或增加血管发生的疾病的方法，其中R1-R11，X，Y， Z和n如本文所定义。在某些实施方案中，组合物用于全身（例如口服）给药。在某些实施方案中，用于治疗各种疾病（包括炎性或自身免疫性疾病）的方法包括全身（例如，口服）向有需要的受试者施用治疗有效量的式（I）化合物。

7. 发明授权

US6051705A Substituted thiazolo[3,2-a]azepine derivatives 失效
标题翻译：取代的噻唑并[3,2-a]吖庚因衍生物
公开(公告)号：US6051705A
公开(公告)日：2000-04-18
申请号：US85729
申请日：1998-05-27
申请人： Hitoshi Oinuma , Shinji Suda , Naoki Yoneda , Makoto Kotake , Masanori Mizuno , Tomohiro Matsushima , Yoshio Fukuda , Mamoru Saito , Toshiyuki Matsuoka , Hideyuki Adachi , Masayuki Namiki , Takeshi Sudo , Kazutoshi Miyake , Makoto Okita
发明人： Hitoshi Oinuma , Shinji Suda , Naoki Yoneda , Makoto Kotake , Masanori Mizuno , Tomohiro Matsushima , Yoshio Fukuda , Mamoru Saito , Toshiyuki Matsuoka , Hideyuki Adachi , Masayuki Namiki , Takeshi Sudo , Kazutoshi Miyake , Makoto Okita
IPC分类号： A61K38/00 , C07D513/04 , C07K5/078 , C07D211/60 , C07D277/06
CPC分类号： C07D513/04 , C07K5/06139 , A61K38/00 , Y02P20/55
摘要： The present invention relates to a substituted thiazolo[3,2-a] azepine derivative having inhibitory activity against angiotensin I converting enzyme and neutral endpeptidase and is represented by the following general formula (I): ##STR1##
摘要翻译：本发明涉及对血管紧张素I转换酶和中性内肽酶具有抑制活性的取代噻唑并[3,2-a]吖庚因衍生物，由以下通式（I）表示：

8. 发明授权

US5789403A Substituted thiazolo �3,2-a!azepine derivatives 失效
标题翻译：取代的噻唑并[3,2-a]吖庚因衍生物
公开(公告)号：US5789403A
公开(公告)日：1998-08-04
申请号：US612864
申请日：1996-03-11
申请人： Hitoshi Oinuma , Shinji Suda , Naoki Yoneda , Makoto Kotake , Masanori Mizuno , Tomohiro Matsushima , Yoshio Fukuda , Mamoru Saito , Toshiyuki Matsuoka , Hideyuki Adachi , Masayuki Namiki , Takeshi Sudo , Kazutoshi Miyake , Makoto Okita
发明人： Hitoshi Oinuma , Shinji Suda , Naoki Yoneda , Makoto Kotake , Masanori Mizuno , Tomohiro Matsushima , Yoshio Fukuda , Mamoru Saito , Toshiyuki Matsuoka , Hideyuki Adachi , Masayuki Namiki , Takeshi Sudo , Kazutoshi Miyake , Makoto Okita
IPC分类号： A61K38/00 , C07D513/04 , C07K5/078 , A61K31/425 , C07D211/60 , C07D277/06
CPC分类号： C07D513/04 , C07K5/06139 , A61K38/00 , Y02P20/55
摘要： The present invention relates to a substituted thiazolo�3,2-a!azepine derivative having inhibitory activity against angiotensin I converting enzyme and neutral endpeptidase. The above substituted thiazolo�3,2-a!azepine derivative is represented by the following general formula (I): ##STR1## (wherein R1 represents a hydrogen atom or a protecting group of a thiol group; R2 represents a hydrogen atom, a lower alkyl group, an aryl group which may have a substituent, a hetroaryl group which may have a substituent, a lower alkoxyl group or a lower alkylthio group; R3, R4 and R5 may be the same or different from one another and represent each a hydrogen atom, a lower alkyl group, a lower alkoxyl group, a lower alkylthio group or the like, with the proviso that the case wherein all of R3, R4 and R5 are hydrogen atoms are excepted; R6 and R7 may be the same or different from each other and represent each a hydrogen atom or a lower alkyl group; R8 represents a hydrogen atom or a protecting group of a carboxyl group; and m and m are each independently 0 or, 1 or 2).
摘要翻译： PCT No.PCT / JP95 / 01139 Sec。 371日期：1996年3月11日 102（e）1996年3月11日PCT提交1995年6月7日PCT公布。出版物WO96 / 02549 日期1996年2月1日本发明涉及对血管紧张素I转换酶和中性内肽酶具有抑制活性的取代噻唑并[3,2-a]吖庚因衍生物。上述取代的噻唑并[3,2-a]吖庚因衍生物由以下通式（I）表示：其中R 1表示氢原子或硫醇基的保护基; R 2表示氢原子，低级烷基，可以具有取代基的芳基，可以具有取代基的杂芳基，低级烷氧基或低级烷硫基; R3，R4和R5可以相同或不同，代表氢原子，低级烷基，低级烷氧基，低级烷硫基等，条件是其中R3，R4和R5全部为氢原子的情况除外; R6和R7可以是相同或不同，表示氢原子或低级烷基; R8表示氢原子或羧基的保护基; m和m各自独立地为0或1或2）。

9. 发明授权

US09012458B2 Antitumor agent using compounds having kinase inhibitory effect in combination 有权
标题翻译：使用具有激酶抑制作用的化合物的抗肿瘤剂组合
公开(公告)号：US09012458B2
公开(公告)日：2015-04-21
申请号：US13805826
申请日：2011-06-23
申请人： Takayuki Nakagawa , Tomohiro Matsushima , Yasuhiro Funahashi
发明人： Takayuki Nakagawa , Tomohiro Matsushima , Yasuhiro Funahashi
IPC分类号： A61K31/497 , A61K31/496 , A61K31/4427 , A61K31/4545 , A61K31/47
CPC分类号： A61K31/496 , A61K31/4427 , A61K31/4545 , A61K31/47 , A61K2300/00
摘要： An antitumor agent for combined use of a compound or pharmaceutically acceptable salt thereof represented by Formula (I) and a compound or pharmaceutically acceptable salt thereof represented by Formula (II) exhibits an excellent antitumor effect compared to cases where these are individually used, and exhibits antitumor effects against various cancer types: wherein R1 is azetidinyl and the like, R2 to R5 is a hydrogen atom or a halogen atom, R6 is C3-8 cycloalkyl and the like, R7 is a hydrogen atom and the like, and R8 is a halogen atom and the like.
摘要翻译：由式（I）表示的化合物或其药学上可接受的盐及其由式（II）表示的化合物或其药学上可接受的盐组合使用的抗肿瘤剂与单独使用它们的情况相比显示出优异的抗肿瘤效果，针对各种癌症类型的抗肿瘤效果：其中R1为氮杂环丁烷基等，R2至R5为氢原子或卤素原子，R6为C3-8环烷基等，R7为氢原子等，R8为卤素原子等。

10. 发明授权

US08497675B2 Angle detector 有权
标题翻译：角度检测器
公开(公告)号：US08497675B2
公开(公告)日：2013-07-30
申请号：US12814774
申请日：2010-06-14
申请人： Tomohiro Matsushima , Yasuhiro Sugimori
发明人： Tomohiro Matsushima , Yasuhiro Sugimori
IPC分类号： G01B7/30
CPC分类号： G01B7/30
摘要： An angle detector includes a rotating member, a housing, a detector and an urging member. The rotating member is rotatable with a shaft inserted therethrough. The housing rotatably supports the rotating member. The detector detects a rotating angle of the rotating member with respect to the housing. The urging member urges the rotating member in a rotating direction of the rotating member. An engagement portion is provided on the housing. An engaged portion is provided on the rotating member. The engaged portion is adapted to be brought into engagement with the engagement portion by urged by the urging member.
摘要翻译：角度检测器包括旋转构件，壳体，检测器和推动构件。旋转构件可以随着插入其中的轴而旋转。壳体可旋转地支撑旋转构件。检测器检测旋转构件相对于壳体的旋转角度。推动构件沿旋转构件的旋转方向推压旋转构件。在壳体上设置有接合部。在旋转构件上设置有被接合部。被卡合部分通过推动构件的推动而与接合部分接合。

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