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1. 发明授权

US08779142B2 Azabicyclo compound and salt thereof 有权
标题翻译：氮杂双环化合物及其盐
公开(公告)号：US08779142B2
公开(公告)日：2014-07-15
申请号：US13378527
申请日：2010-07-09
申请人： Makoto Kitade , Shuichi Ohkubo , Chihoko Yoshimura , Satoshi Yamashita , Hiromi Oshiumi , Takao Uno , Yuichi Kawai
发明人： Makoto Kitade , Shuichi Ohkubo , Chihoko Yoshimura , Satoshi Yamashita , Hiromi Oshiumi , Takao Uno , Yuichi Kawai
IPC分类号： A61K31/4365 , C07D471/04
CPC分类号： C07D471/04 , C07D209/08 , C07D519/00
摘要： It is intended to provide a novel azabicyclo compound which exhibits both HSP90 inhibitory activity and cell proliferation inhibitory effect. Specifically disclosed is a compound represented by the following general formula (I) or a salt thereof: wherein X1 represents CH or N; any one of X2, X3 and X4 represents N, and the others represent CH; any one or two of Y1, Y2, Y3 and Y4 represent C—R4, and the others are the same or different and represent CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S and O; R2 represents an alkyl group having 1 to 6 carbon atoms, or the like; and R3 and R4 represent —CO—R5 or the like.
摘要翻译：旨在提供表现出HSP90抑制活性和细胞增殖抑制作用的新型氮杂双环化合物。具体公开的是由下列通式（I）表示的化合物或其盐：其中X1表示CH或N; X2，X3和X4中的任一个表示N，其余的表示CH; Y 1，Y 2，Y 3和Y 4中的任何一个或两个表示C-R 4，其余的相同或不同，表示CH或N; R1表示具有1至4个选自N，S和O的杂原子的任选取代的单环或双环不饱和杂环基; R2表示碳原子数1〜6的烷基等。 R3和R4表示-CO-R5等。

2. 发明申请

US20120108589A1 AZABICYCLO COMPOUND AND SALT THEREOF 有权
标题翻译：雅各布酯化合物及其盐
公开(公告)号：US20120108589A1
公开(公告)日：2012-05-03
申请号：US13378527
申请日：2010-07-09
申请人： Makoto Kitade , Shuichi Ohkubo , Chihoko Yoshimura , Satoshi Yamashita , Hiromi Oshiumi , Takao Uno , Yuichi Kawai
发明人： Makoto Kitade , Shuichi Ohkubo , Chihoko Yoshimura , Satoshi Yamashita , Hiromi Oshiumi , Takao Uno , Yuichi Kawai
IPC分类号： A61K31/437 , A61K31/5377 , A61P35/00 , C07D471/04
CPC分类号： C07D471/04 , C07D209/08 , C07D519/00
摘要： It is intended to provide a novel azabicyclo compound which exhibits both HSP90 inhibitory activity and cell proliferation inhibitory effect. Specifically disclosed is a compound represented by the following general formula (I) or a salt thereof: wherein X1 represents CH or N; any one of X2, X3 and X4 represents N, and the others represent CH; any one or two of Y1, Y2, Y3 and Y4 represent C—R4, and the others are the same or different and represent CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S and O; R2 represents an alkyl group having 1 to 6 carbon atoms, or the like; and R3 and R4 represent —CO—R5 or the like.
摘要翻译：旨在提供表现出HSP90抑制活性和细胞增殖抑制作用的新型氮杂双环化合物。具体公开的是由下列通式（I）表示的化合物或其盐：其中X1表示CH或N; X2，X3和X4中的任一个表示N，其余的表示CH; Y 1，Y 2，Y 3和Y 4中的任何一个或两个表示C-R 4，其余的相同或不同，表示CH或N; R1表示具有1至4个选自N，S和O的杂原子的任选取代的单环或双环不饱和杂环基; R2表示碳原子数1〜6的烷基等。 R3和R4表示-CO-R5等。

3. 发明授权

US09120780B2 Indole or indazole derivative or salt thereof 有权
标题翻译：吲哚或吲唑衍生物或其盐
公开(公告)号：US09120780B2
公开(公告)日：2015-09-01
申请号：US13978632
申请日：2012-01-06
申请人： Makoto Kitade , Shuichi Ohkubo , Chihoko Yoshimura
发明人： Makoto Kitade , Shuichi Ohkubo , Chihoko Yoshimura
IPC分类号： C07D209/04 , C07D213/02 , A61K31/404 , A61K31/4439 , A61K31/4178 , C07D401/14 , C07D403/14
CPC分类号： C07D401/14 , A61K31/4178 , A61K31/4439 , C07D403/14
摘要： The invention provides an indazole compound of formula (I) which is capable of inhibiting HSP90 and shows a cytostatic effect on cancer cells:
摘要翻译：本发明提供能够抑制HSP90并对癌细胞具有细胞抑制作用的式（I）吲唑化合物：

4. 发明申请

US20130289072A1 NOVEL INDOLE OR INDAZOLE DERIVATIVE OR SALT THEREOF 有权
标题翻译：新颖的吲哚或吲哚衍生物或其盐
公开(公告)号：US20130289072A1
公开(公告)日：2013-10-31
申请号：US13978632
申请日：2012-01-06
申请人： Makoto Kitade , Shuichi Ohkubo , Chihoko Yoshimura
发明人： Makoto Kitade , Shuichi Ohkubo , Chihoko Yoshimura
IPC分类号： C07D401/14 , C07D403/14
CPC分类号： C07D401/14 , A61K31/4178 , A61K31/4439 , C07D403/14
摘要： The present invention relates to provision of a novel indazole compound which is capable of inhibiting HSP90 and shows a cytostatic effect on cancer cells. The present invention also relates to provision of a drug useful for preventing and/or treating, on the basis of an HSP90 inhibitory effect, a disease in which HSP90 participates, in particular, cancer. A compound represented by the general formula (I) or a salt thereof: wherein X represents CH or N; any one or two of Y1, Y2, Y3, and Y4 represent C—R3 or N, and the others represent CH; A and B are the same or different and represent an optionally substituted monocyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S, and O; R1 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.; R2 represents a hydrogen atom, a halogen atom etc.; R3 represents a hydrogen atom, a halogen atom etc.; R4 and R5 are the same or different and represent a hydroxyl group etc.; R6 and R7 are the same or different and represent a hydrogen atom, an alkyl group having 1 to 6 carbon atoms etc.; and R8 represents an optionally substituted cycloalkyl group having 3 to 7 carbon atoms etc.
摘要翻译：本发明涉及提供能够抑制HSP90并对癌细胞具有细胞抑制作用的新型吲唑化合物。本发明还涉及提供可用于预防和/或治疗HSP90抑制作用的药物，其特征在于HSP90参与的疾病，特别是癌症。由通式（I）表示的化合物或其盐：其中X表示CH或N; Y1，Y2，Y3和Y4中的一个或两个表示C-R3或N，其余的表示CH; A和B相同或不同，表示具有1至4个选自N，S和O的杂原子的任选取代的单环不饱和杂环基; R1表示氢原子，可以具有取代基的碳原子数1〜6的烷基等。 R2表示氢原子，卤素原子等; R3表示氢原子，卤素原子等; R4和R5相同或不同，表示羟基等。 R6和R7相同或不同，表示氢原子，碳原子数1〜6的烷基等。 R8表示可以具有取代基的碳原子数为3〜7的环烷基等。

5. 发明申请

US20130296320A1 NOVEL BICYCLIC COMPOUND OR SALT THEREOF 有权
标题翻译：新型双环化合物或其盐
公开(公告)号：US20130296320A1
公开(公告)日：2013-11-07
申请号：US13978613
申请日：2012-01-06
申请人： Makoto Kitade , Satoshi Yamashita , Shuichi Ohkubo
发明人： Makoto Kitade , Satoshi Yamashita , Shuichi Ohkubo
IPC分类号： C07D401/14 , C07D403/14 , C07D403/04 , C07D417/04 , C07D413/04 , C07D401/04 , C07D471/04
CPC分类号： C07D403/04 , A61K31/4375 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/517 , A61K31/5377 , C07D401/04 , C07D401/14 , C07D403/14 , C07D413/04 , C07D417/04 , C07D471/04
摘要： Provided is a novel bicyclic compound which has an HSP90 inhibitory effect and a carcinostatic effect. Also provided is a pharmaceutical agent which is based on the HSP90 inhibitory effect and is useful in the prevention and/or treatment of a disease involving HSP90, particularly, cancer. The present invention provides a compound represented by the following general formula (I) or a salt thereof wherein at least one of X1, X2, X3, and X4 represents N or N-oxide and the rest thereof are the same or different and each represent C—R2; any one or two of Y1, Y2, Y3, and Y4 represent C—R4 and the rest thereof are the same or different and each represent CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S, and O; R2 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.; R3 represents a hydrogen atom, —CO—R5 etc.; R4 represents a hydrogen atom, —CO—R6, —N(R7)(R8) etc.; R5 represents a hydroxyl group, an amino group etc.; R6 represents a hydroxyl group etc.; R7 and R8 are the same or different and each represent a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.; and R9 represents an optionally substituted cycloalkyl group having 3 to 7 carbon atoms etc.
摘要翻译：提供具有HSP90抑制作用和制癌作用的新型双环化合物。还提供了基于HSP90抑制作用的药剂，并且可用于预防和/或治疗涉及HSP90，特别是癌症的疾病。本发明提供由以下通式（I）表示的化合物或其盐，其中X 1，X 2，X 3和X 4中的至少一个表示N或N-氧化物，其余的相同或不同，表示 C-R2; Y1，Y2，Y3和Y4中的任何一个或两个表示C-R 4，其余的相同或不同，各自表示CH或N; R1表示具有1至4个选自N，S和O的杂原子的任选取代的单环或双环不饱和杂环基; R2表示氢原子，可以具有取代基的碳原子数1〜6的烷基等。 R3表示氢原子，-CO-R5等; R4代表氢原子，-CO-R6，-N（R7）（R8）等; R5代表羟基，氨基等; R6表示羟基等。 R 7和R 8相同或不同，各自表示氢原子，可以具有取代基的碳原子数1〜6的烷基等。 R9表示碳原子数3〜7的任意取代环烷基等。

6. 发明授权

US08912181B2 Bicyclic compound or salt thereof 有权
标题翻译：双环化合物或其盐
公开(公告)号：US08912181B2
公开(公告)日：2014-12-16
申请号：US13978613
申请日：2012-01-06
申请人： Makoto Kitade , Satoshi Yamashita , Shuichi Ohkubo
发明人： Makoto Kitade , Satoshi Yamashita , Shuichi Ohkubo
IPC分类号： C07D401/04 , C07D401/14 , A61K31/47 , C07D403/04 , A61K31/4375 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/517 , A61K31/5377 , C07D403/14 , C07D413/04 , C07D417/04 , C07D471/04
CPC分类号： C07D403/04 , A61K31/4375 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/517 , A61K31/5377 , C07D401/04 , C07D401/14 , C07D403/14 , C07D413/04 , C07D417/04 , C07D471/04
摘要： A novel bicyclic compound having an HSP90 inhibitory effect and a carcinostatic effect. A pharmaceutical agent based on the HSP90 inhibitory effect and useful in the prevention and/or treatment of a disease involving HSP90, particularly cancer. The compound has a general formula (I) or is a salt thereof wherein at least one of X1, X2, X3, and X4 represents N or N-oxide and the rest thereof are each independently C—R2; any one or two of Y1, Y2, Y3, and Y4 represent C—R4 and the rest thereof are each independently CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S, and O; R2 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.; R3 represents a hydrogen atom, —CO—R5 etc.
摘要翻译：具有HSP90抑制作用和制癌作用的新型双环化合物。基于HSP90抑制作用的药剂，可用于预防和/或治疗涉及HSP90的疾病，特别是癌症。该化合物具有通式（I）或其盐，其中X 1，X 2，X 3和X 4中的至少一个表示N或N-氧化物，其余各自独立地为C-R 2; Y1，Y2，Y3和Y4中的一个或两个表示C-R4，其余的各自独立地为CH或N; R1表示具有1至4个选自N，S和O的杂原子的任选取代的单环或双环不饱和杂环基; R2表示氢原子，可以具有取代基的碳原子数1〜6的烷基等。 R3表示氢原子，-CO-R5等

7. 发明授权

US5965600A 3-(bis-substituted phenylmethylene) oxindole derivatives 失效
标题翻译： 3-（双取代的苯基亚甲基）羟基吲哚衍生物
公开(公告)号：US5965600A
公开(公告)日：1999-10-12
申请号：US913239
申请日：1997-09-10
申请人： Atsushi Sato , Tetsuji Asao , Yuichi Hagiwara , Makoto Kitade , Yasundo Yamazaki
发明人： Atsushi Sato , Tetsuji Asao , Yuichi Hagiwara , Makoto Kitade , Yasundo Yamazaki
IPC分类号： C07D209/34 , C07D401/06 , C07D401/14 , C07D471/04 , A01N43/38
CPC分类号： C07D401/06 , C07D209/34 , C07D401/14 , C07D471/04
摘要： The present invention is directed to an oxindole derivative represented by formula (1): ##STR1## (wherein R represents a methyl group or a methoxy group), and pharmaceuticals containing the compound. The compound exhibits excellent granulation inhibiting activity while providing minimal liver toxicity and is useful as a pharmaceutical in the prevention and treatment of articular rheumatism, arteriosclerosis, hepatocirrhosis, etc., and also in the prevention and treatment of arthrosis deformans, psoriasis, gout, nephritis, angiitis, inflammatory intestinal diseases (ulcerative colitis, Crohn's disease), bronchitis, and chronic granulomatosis, etc.
摘要翻译： PCT No.PCT / JP97 / 00066 Sec。 371日期：1997年9月10日 102（e）1997年9月10日PCT 1997年1月16日PCT PCT。出版物WO97 / 26242 日期1997年7月24日本发明涉及由式（1）表示的羟吲哚衍生物：其中R表示甲基或甲氧基，以及含有该化合物的药物。该化合物表现出优异的造粒抑制活性，同时提供最小的肝毒性，并且可用作预防和治疗关节风湿病，动脉硬化，肝硬化等的药物，并且还用于预防和治疗畸形关节炎，牛皮癣，痛风，肾炎，血管炎，炎症性肠病（溃疡性结肠炎，克罗恩病），支气管炎和慢性肉芽肿病等。

8. 发明申请

US20110319413A1 PIPERAZINE COMPOUND CAPABLE OF INHIBITING PROSTAGLANDIN D SYNTHASE 有权
标题翻译： PIPERAZINE化合物可抑制PROSTAGLANDIN D合成酶
公开(公告)号：US20110319413A1
公开(公告)日：2011-12-29
申请号：US13255134
申请日：2010-03-08
申请人： Yoshihiro Urade , Makoto Kitade , Kazuhiko Shigeno , Keiko Yamane , Katsunao Tanaka
发明人： Yoshihiro Urade , Makoto Kitade , Kazuhiko Shigeno , Keiko Yamane , Katsunao Tanaka
IPC分类号： A61K31/496 , C07D413/14 , A61P21/00 , A61K31/5377 , A61P37/08 , A61P29/00 , C07D401/14 , C07D403/14
CPC分类号： C07D401/14 , A61K31/496 , A61K31/5377 , C07D207/34 , C07D213/81 , C07D277/82 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14
摘要： This invention relates to a piperazine compound represented by Formula (I), wherein R1 is C1-6 alkyl; R2 is hydroxy, C1-6 alkyl that may have one or more substituents, —(C═O)—N(R3)(R4), or —(C═O)—OR5; R3 and R4 are the same or different, and each represents hydrogen or C1-6 alkyl that may have one or more substituents, or R3 and R4, taken together with a nitrogen atom to which R3 and R4 are attached, may form a saturated heterocyclic group; R5 is hydrogen or C1-6 alkyl that may have one or more substituents; and n is 1 or 2; or a salt thereof.
摘要翻译：本发明涉及由式（I）表示的哌嗪化合物，其中R 1是C 1-6烷基; R 2是羟基，可具有一个或多个取代基的C 1-6烷基， - （C = O）-N（R 3）（R 4）或 - （C = O） R 3和R 4相同或不同，各自表示氢或可具有一个或多个取代基的C 1-6烷基，或者R 3和R 4与R 3和R 4连接的氮原子一起可以形成饱和杂环组; R5是氢或可具有一个或多个取代基的C 1-6烷基; n为1或2; 或其盐。

9. 发明授权

US5977130A Intimal hypertrophy inhibitors 失效
公开(公告)号：US5977130A
公开(公告)日：1999-11-02
申请号：US913237
申请日：1997-09-10
申请人： Atsushi Sato , Tetsuji Asao , Yuichi Hagiwara , Makoto Kitade , Yasundo Yamazaki
发明人： Atsushi Sato , Tetsuji Asao , Yuichi Hagiwara , Makoto Kitade , Yasundo Yamazaki
IPC分类号： A61K31/404 , A61K31/407 , A61P9/10 , C07D209/34 , C07D401/06 , C07D401/14 , C07D471/04 , A61K31/40 , A61K31/44
CPC分类号： C07D401/06 , C07D209/34 , C07D401/14 , C07D471/04
摘要： The present invention is directed to an intimal hypertrophy inhibitor containing as the active ingredient an oxyindole derivative represented by the following formula (I) or a salt thereof: ##STR1## (wherein R.sup.1 represents a hydrogen atom; a phenyl group which may be substituted by a lower alkyl group, a lower alkoxy group, a lower alkylaminoalkoxy group, a hydroxy group, an amino group, a lower alkylamino group, or a halogen atom; or a pyridyl group which may be substituted by a lower alkyl group, a lower alkoxy group, a lower alkylaminoalkoxy group, a hydroxy group, an amino group, a lower alkylamino group, a halogen atom, a lower alkoxycarbonyl group, or a carboxyl group; R.sup.2 represents a phenyl group which may be substituted; or a pyridyl group which may be substituted by a lower alkyl group, a lower alkoxy group, a lower alkylaminoalkoxy group, a hydroxy group, an amino group, a lower alkylamino group, a halogen atom, a lower alkoxycarbonyl group, or a carboxyl group; R.sup.3 represents a hydrogen atom; a lower alkyl, benzyl, or a benzenesulfonyl group which may be substituted; or an acyl group; R.sup.4 represents a hydrogen atom; a lower alkoxy group, a halogen atom, an amino group, a lower alkylamino group, a carboxyl group, a lower alkoxycarbonyl group; a phenylcarbomoyl group which may be substituted; or a trifluoromethyl group; X represents CH or N; n represents a number between 0 and 4 inclusive that indicates the number of substituents; and the broken/solid double line denotes a single bond or a double bond). The intimal hypertrophy inhibitor of the present invention exhibits excellent inhibitory action against intimal hypertrophy, and thus is useful as a preventive/therapeutic/ameliorating agent for proliferative vascular diseases such as restenosis after PTCA, arteriosclerosis, peripheral embolism, and angiitis.

10. 发明授权

US08765750B2 Piperazine compound having a PGDS inhibitory effect 有权
标题翻译：具有PGDS抑制作用的哌嗪化合物
公开(公告)号：US08765750B2
公开(公告)日：2014-07-01
申请号：US13522605
申请日：2011-01-19
申请人： Yoshihiro Urade , Makoto Kitade , Kazuhiko Shigeno , Keiko Yamane , Katsunao Tanaka
发明人： Yoshihiro Urade , Makoto Kitade , Kazuhiko Shigeno , Keiko Yamane , Katsunao Tanaka
IPC分类号： A61K31/496 , A61K31/5377 , C07D401/14 , C07D413/14 , C07D403/14
CPC分类号： C07D403/14 , A61K31/496 , A61K31/5377 , C07D211/58 , C07D213/81 , C07D277/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention provides a piperazine compound represented by Formula (I) or a salt thereof, wherein X represents CH or an N atom; R1 represents C1-6 alkyl; R2 represents C1-6 alkyl that may have one or more substituents, C2-6 alkenyl that may have one or more substituents, —(C═O)—N(R3)(R4), or —(C═O)—OR5, R3 and R4 are the same or different, and each represents hydrogen or C1-6 alkyl that may have one or more substituents; or R3 and R4, taken together with a nitrogen atom to which R3 and R4 are attached, may form a saturated heterocyclic group; and R5 represents hydrogen or C1-6 alkyl that may have one or more substituents or aralkyl.
摘要翻译：本发明提供由式（I）表示的哌嗪化合物或其盐，其中X表示CH或N原子; R1表示C1-6烷基; R 2表示可具有一个或多个取代基的C 1-6烷基，可具有一个或多个取代基的C 2-6烯基， - （C = O）-N（R 3）（R 4）或 - （C = O） R 3和R 4相同或不同，各自表示氢或可具有一个或多个取代基的C 1-6烷基; 或者R3和R4与R3和R4连接的氮原子一起形成饱和杂环基; 并且R 5表示氢或可以具有一个或多个取代基或芳烷基的C 1-6烷基。

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