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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。
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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。
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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。
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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。
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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。
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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。
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公开(公告)号:US5527948A
公开(公告)日:1996-06-18
申请号:US402569
申请日:1995-03-13
申请人: Makoto Okita , Hiroshi Shirota , Masayuki Tanaka , Toshihiko Kaneko , Katsuya Tagami , Shigeki Hibi , Yasushi Okamoto , Seiichiro Nomoto , Takeshi Suzuki , Kenichi Chiba , Masaki Goto , Ryoichi Hashida , Hideki Ono , Hideto Ohhara , Hideki Sakurai , Shigeru Souda , Yoshimasa Machida , Kouichi Katayama , Isao Yamatsu
发明人: Makoto Okita , Hiroshi Shirota , Masayuki Tanaka , Toshihiko Kaneko , Katsuya Tagami , Shigeki Hibi , Yasushi Okamoto , Seiichiro Nomoto , Takeshi Suzuki , Kenichi Chiba , Masaki Goto , Ryoichi Hashida , Hideki Ono , Hideto Ohhara , Hideki Sakurai , Shigeru Souda , Yoshimasa Machida , Kouichi Katayama , Isao Yamatsu
IPC分类号: C07C39/225 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/313 , C07C43/315 , C07C45/00 , C07C45/29 , C07C45/30 , C07C45/51 , C07C45/54 , C07C45/59 , C07C45/63 , C07C45/71 , C07C47/57 , C07C47/575 , C07C49/83 , C07C49/84 , C07C59/68 , C07C69/157 , C07F7/18 , C07C69/76 , C07C49/115
CPC分类号: C07F7/1852 , C07C39/225 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/313 , C07C43/315 , C07C45/00 , C07C45/298 , C07C45/30 , C07C45/305 , C07C45/513 , C07C45/54 , C07C45/59 , C07C45/63 , C07C45/71 , C07C47/57 , C07C47/575 , C07C49/83 , C07C49/84 , C07C59/68
摘要: Naphthalene derivatives of the formula: ##STR1## wherein R.sup.1, represents a hydrogen atom, a lower alkyl group or an acyl group; R.sup.2 independently represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogen atom, a cycloalkyl group, a cycloalkylalkyl group, a hydroxyl group, an aryl group which may be substituted, an arylalkyl group whose aryl group may be substituted, a heteroaryl group, or a heteroaryllakyl group; R.sup.3 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, an aryl group which may have a substituent, an arylalkyl group whose aryl group may be substituted, an arylalkenyl group whose aryl group may be substituted, a cycloalkyl group, an alkoxyalkyl group, a heteroaryl group, a heteroarylalkyl group, a carboxyl group, a carboxyalkyl group, an aminoalkyl group, or a cyano group; R.sup.6 is C.sub.1-6 alkyl; and m is 0 or an integer of from 1 to 2 useful in treating autoimmune diseases are disclosed.
摘要翻译: 下式的萘衍生物:其中R 1,表示氢原子,低级烷基或酰基; R2独立地表示氢原子,低级烷基,低级烷氧基,卤素原子,环烷基,环烷基烷基,羟基,可被取代的芳基,芳基可以被取代的芳基烷基 ,杂芳基或杂芳基烷基; R 3表示氢原子,低级烷基,低级烯基,可以具有取代基的芳基,可以被取代芳基的芳基烷基,可以被芳基取代的芳基烯基,环烷基, 烷氧基烷基,杂芳基,杂芳基烷基,羧基,羧基烷基,氨基烷基或氰基; R6是C1-6烷基; 并且公开了m为0或可用于治疗自身免疫性疾病的1〜2的整数。
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公开(公告)号:US5298649A
公开(公告)日:1994-03-29
申请号:US774237
申请日:1991-10-10
申请人: Makoto Okita , Hiroshi Shirota , Masayuki Tanaka , Toshihiko Kaneko , Katsuya Tagami , Shigeki Hibi , Yasushi Okamoto , Seiichiro Nomoto , Takeshi Suzuki , Kenichi Chiba , Masaki Goto , Ryoichi Hashida , Hideki Ono , Hideto Ohhara , Hideki Sakurai , Shigeru Souda , Yoshimasa Machida , Kouichi Katayama , Isao Yamatsu
发明人: Makoto Okita , Hiroshi Shirota , Masayuki Tanaka , Toshihiko Kaneko , Katsuya Tagami , Shigeki Hibi , Yasushi Okamoto , Seiichiro Nomoto , Takeshi Suzuki , Kenichi Chiba , Masaki Goto , Ryoichi Hashida , Hideki Ono , Hideto Ohhara , Hideki Sakurai , Shigeru Souda , Yoshimasa Machida , Kouichi Katayama , Isao Yamatsu
IPC分类号: C07C39/225 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/313 , C07C43/315 , C07C45/00 , C07C45/29 , C07C45/30 , C07C45/51 , C07C45/54 , C07C45/59 , C07C45/63 , C07C45/71 , C07C47/57 , C07C47/575 , C07C49/83 , C07C49/84 , C07C59/68 , C07C69/157 , C07F7/18 , C07C69/76
CPC分类号: C07F7/1852 , C07C39/225 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/313 , C07C43/315 , C07C45/00 , C07C45/298 , C07C45/30 , C07C45/305 , C07C45/513 , C07C45/54 , C07C45/59 , C07C45/63 , C07C45/71 , C07C47/57 , C07C47/575 , C07C49/83 , C07C49/84 , C07C59/68
摘要: A naphthalene derivative having the formula is new and useful for medicine. ##STR1## wherein R.sup.1 represents a hydrogen atom, a lower alkyl group or an acyl group;R.sup.2 independently represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogen atom, a cycloalkyl group, a cycloalkylalkyl group, a hydroxyl group, an aryl group which may be substituted, an arylalkyl group whose aryl group may be substituted, a heteroaryl group, or a heteroarylalkyl group;R.sup.3 and R.sup.4 are the same or different and represent a hydrogen atom, a lower alkyl group, a lower alkenyl group, an aryl group which may have a substituent, an arylalkyl group whose aryl group may be substituted, an arylalkenyl group whose aryl group may be substituted, a cycloalkyl group, an alkoxyalkyl group, a heteroaryl group, a heteroarylalkyl group, a carboxyl group, a carboxyalkyl group, an aminoalkyl group, or a cyano group;R.sup.5 represents a group of the formula, --OR.sup.7, (wherein R.sup.7 represents a hydrogen atom or a lower alkyl group), or a group of the formula, ##STR2## (wherein R.sup.8 and R.sup.9 are the same or different and represent a hydrogen atom or a lower alkyl group.
摘要翻译: 具有该式的萘衍生物是新的并且可用于药物。 其中R 1表示氢原子,低级烷基或酰基; R2独立地表示氢原子,低级烷基,低级烷氧基,卤素原子,环烷基,环烷基烷基,羟基,可被取代的芳基,芳基可以被取代的芳基烷基 杂芳基或杂芳基烷基; R3和R4相同或不同,表示氢原子,低级烷基,低级烯基,可以具有取代基的芳基,芳基可以被取代的芳基烷基,芳基可以被取代的芳基烯基 烷氧基烷基,杂芳基,杂芳基烷基,羧基,羧基烷基,氨基烷基或氰基; R5表示式-OR7的基团(其中R7表示氢原子或低级烷基)或下式的基团,其中R8和R9相同或不同,表示氢原子 或低级烷基。
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公开(公告)号:US5134111A
公开(公告)日:1992-07-28
申请号:US451468
申请日:1989-12-15
申请人: Makoto Okita , Hiroshi Shirota , Masayuki Tanaka , Toshihiko Kaneko , Katsuya Tagami , Shigeki Hibi , Yasushi Okamoto , Seiichiro Nomoto , Takeshi Suzuki , Kenichi Chiba , Masaki Goto , Ryoichi Hashida , Hideki Ono , Hideto Ohhara , Hideki Sakurai , Shigeru Souda , Yoshimasa Machida , Kouichi Katayama , Isao Yamatsu
发明人: Makoto Okita , Hiroshi Shirota , Masayuki Tanaka , Toshihiko Kaneko , Katsuya Tagami , Shigeki Hibi , Yasushi Okamoto , Seiichiro Nomoto , Takeshi Suzuki , Kenichi Chiba , Masaki Goto , Ryoichi Hashida , Hideki Ono , Hideto Ohhara , Hideki Sakurai , Shigeru Souda , Yoshimasa Machida , Kouichi Katayama , Isao Yamatsu
IPC分类号: C07C39/225 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/313 , C07C43/315 , C07C45/00 , C07C45/29 , C07C45/30 , C07C45/51 , C07C45/54 , C07C45/59 , C07C45/63 , C07C45/71 , C07C47/57 , C07C47/575 , C07C49/83 , C07C49/84 , C07C59/68 , C07C69/157 , C07F7/18
CPC分类号: C07F7/1852 , C07C39/225 , C07C43/215 , C07C43/23 , C07C43/30 , C07C43/313 , C07C43/315 , C07C45/00 , C07C45/298 , C07C45/30 , C07C45/305 , C07C45/513 , C07C45/54 , C07C45/59 , C07C45/63 , C07C45/71 , C07C47/57 , C07C47/575 , C07C49/83 , C07C49/84 , C07C59/68
摘要: A naphthalene derivative having the formula is new and useful for medicine. ##STR1## [wherein R.sup.1 represents a hydrogen atom, a lower alkyl group or an acyl group;R.sup.2 independently represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogen atom, a cycloalkyl group, a cycloalkylalkyl group, a hydroxyl group, an aryl group which may be substituted, an arylalkyl group whose aryl group may be substituted, a heteroaryl group, or a heteroarylalkyl group;R.sup.3 and R.sup.4 are the same or different and represent a hydrogen atom, a lower alkyl group, a lower alkenyl group, an aryl group which may have a substituent, an arylalkyl group whose aryl group may be substituted, an arylalkenyl group whose aryl group may be substituted, a cycloalkyl group, an alkoxyalkyl group, a heteroaryl group, a heteroarylalkyl group, a carboxy group, a carboxyalkyl group, an aminoalkyl group, or a cyano group;R.sup.5 represents a group of the formula, --OR.sup.7, (wherein R.sup.7 represents a hydrogen atom or a lower alkyl group), or a group of the formula ##STR2## (wherein R.sup.8 and R.sup.9 are the same or different and represent a hydrogen atom or a lower alkyl group, or R.sup.8 and R.sup.9 can form, along with the nitrogen atom bonded with R.sup.8 and R.sup.9, a ring which may contain an oxygen atom);R.sup.6 independently represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, an amino group, an arylalkyl group, or an aryl group; andm is 0 or an integer of from 1 to 2, and n is 0 or an integer of from 1 to 4.]
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10.
公开(公告)号:US06949585B2
公开(公告)日:2005-09-27
申请号:US10473568
申请日:2002-04-01
IPC分类号: A61K31/12 , A61K31/235 , A61K31/24 , A61K31/4402 , A61P1/04 , A61P1/16 , A61P3/10 , A61P13/12 , A61P17/00 , A61P19/02 , A61P27/02 , A61P29/00 , A61P43/00 , C07C49/657 , C07C49/747 , C07C49/753 , C07C205/57 , C07D207/12 , C07D401/04 , C07D453/02 , C07C69/76 , C07C205/00
CPC分类号: C07D401/04 , A61K31/12 , A61K31/235 , A61K31/24 , A61K31/4402 , C07C49/657 , C07C49/747 , C07C49/753 , C07C205/57 , C07D207/12 , C07D453/02
摘要: The present invention provides a compound which has cytokine production inhibitory activity and is useful for the treatment of diseases which is associated with cytokine. The compound is represented by the following general formula (I) [wherein A represents a cyclic group which may be substituted; the partial structure -DE- represents a group represented by —CH2CH2— or —CH═CH—; W represents a group represented by —CH2—, —CH2CH2—, —CH═CH— or —CH═; the partial structure >XY— represents a group represented by >CH—(CH2)n—, >C═CH—, >CH—CH2—CH(OH)—, >CH—CH2—C(═O)—, >CH—O— or >CH—O—CO—, provided that when W is —CH═, then XY— represents C—(CH2)p—; Z represents a divalent aliphatic hydrocarbon group; R1 and R2, which may be the same or different, each represents a hydrogen atom, or a hydroxyl, alkoxy or alkoxyalkoxy group; m is an integer of 0 or 1].
摘要翻译: 本发明提供具有细胞因子产生抑制活性的化合物,可用于治疗与细胞因子相关的疾病。 该化合物由以下通式(I)表示[其中A表示可以被取代的环状基团; 部分结构-D E-表示由-CH 2 CH 2 - 或-CH-CH-表示的基团。 W表示由-CH 2 - , - CH 2 CH 2 - , - CH-CH-或-CH-表示的基团。 部分结构> X Y-表示由CH-(CH 2)n - ,> C-CH-,CH -CH 2 OH(OH) - ,> CH-CH 2 -C(-O) - ,> CH-O-或> CH-O-CO- 条件是当W是-CH-时,则X Y-表示C-(CH 2) Z表示二价脂族烃基; R 1和R 2可以相同或不同,各自表示氢原子,或羟基,烷氧基或烷氧基烷氧基; m为0或1的整数]。
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