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公开(公告)号:US20070105919A1
公开(公告)日:2007-05-10
申请号:US10584633
申请日:2004-12-24
申请人: Takao Nakajima , Masamori Sugawara , Shin-ichi Ushida , Tetsuji Ohno , Yuji Nomoto , Noriaki Uesaka , Yoshisuke Nakasato
发明人: Takao Nakajima , Masamori Sugawara , Shin-ichi Ushida , Tetsuji Ohno , Yuji Nomoto , Noriaki Uesaka , Yoshisuke Nakasato
IPC分类号: A61K31/427
CPC分类号: C07D417/06 , A61K31/427 , A61K31/438 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/5383 , A61K31/541 , A61K31/542 , A61K31/551 , A61K31/553 , A61K31/695 , C07D417/04 , C07D417/14 , C07D491/048 , C07D491/10 , C07D498/04 , C07D513/04
摘要: (Wherein n is an integer of from 0 to 3; R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, or a substituted or unsubstituted aromatic heterocyclic group; R2 is halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, a substituted or unsubstituted aromatic heterocyclic group, —COR8, or the like; R3 and R4 may be the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl, —COR12, or the like) For example, provided are adenosine A2A receptor antagonists comprising, as the active ingredient, a thiazole derivative represented by a general formula (I), or a pharmaceutically acceptable salt thereof, and the like.
摘要翻译: (其中n为0-3的整数; R 1是取代或未取代的环烷基,取代或未取代的芳基,取代或未取代的脂环族杂环基或取代或未取代的芳族杂环基; R 取代或未取代的芳基,取代或未取代的脂环族杂环基,取代或未取代的芳族杂环基,-COR 8或 R 3和R 4可以相同或不同,并且各自表示氢原子,取代或未取代的低级烷基,取代或未取代的芳烷基,-COR 3, 例如,提供了包含作为活性成分的由通式(I)表示的噻唑衍生物或腺苷A 2A受体拮抗剂的腺苷A 2A受体拮抗剂,或 药学上可接受的盐等。
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公开(公告)号:US20110105486A1
公开(公告)日:2011-05-05
申请号:US12960937
申请日:2010-12-06
申请人: Takao Nakajima , Masamori Sugawara , Shin-ichi Uchida , Tetsuji Ohno , Yuji Nomoto , Noriaki Uesaka , Yoshisuke Nakasato
发明人: Takao Nakajima , Masamori Sugawara , Shin-ichi Uchida , Tetsuji Ohno , Yuji Nomoto , Noriaki Uesaka , Yoshisuke Nakasato
IPC分类号: A61K31/541 , C07D277/38 , C07D417/14 , C07D401/14 , C07D213/89 , C07D413/14 , C07D279/12 , A61K31/426 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61P25/28 , A61P25/00 , A61P3/10 , A61P25/12 , A61P25/24
CPC分类号: C07D417/06 , A61K31/427 , A61K31/438 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/5383 , A61K31/541 , A61K31/542 , A61K31/551 , A61K31/553 , A61K31/695 , C07D417/04 , C07D417/14 , C07D491/048 , C07D491/10 , C07D498/04 , C07D513/04
摘要: Wherein n is an integer of from 0 to 3; R1A is a 5-membered aromatic heterocyclic group containing at least one oxygen atom; R2A is —COR8 (wherein R8 is aryl); R3A is hydrogen or lower alkyl; and R12 represents cycloalkyl, aryl, aralkyl, alicyclic heterocyclic group, aromatic heterocyclic group, alicyclic hetocyclic-alkyl, or aromatic heterocyclic-alkyl, and R1A, R2A, R3A and R12 are individually optionally substituted.
摘要翻译: 其中n为0至3的整数; R1A是含有至少一个氧原子的5元芳族杂环基; R2A是-COR8(其中R8是芳基); R3A是氢或低级烷基; R 12表示环烷基,芳基,芳烷基,脂环族杂环基,芳香族杂环基,脂环族环状烷基或芳香族杂环烷基,R1A,R2A,R3A,R12分别任意取代。
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公开(公告)号:US20100256361A1
公开(公告)日:2010-10-07
申请号:US12766986
申请日:2010-04-26
申请人: Takao Nakajima , Masamori Sugawara , Shin-ichi Uchida , Tetsuji Ohno , Yuji Nomoto , Noriaki Uesaka , Yoshisuke Nakasato
发明人: Takao Nakajima , Masamori Sugawara , Shin-ichi Uchida , Tetsuji Ohno , Yuji Nomoto , Noriaki Uesaka , Yoshisuke Nakasato
IPC分类号: C07D417/14 , C07D413/14 , C07D498/04
CPC分类号: C07D417/06 , A61K31/427 , A61K31/438 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/5383 , A61K31/541 , A61K31/542 , A61K31/551 , A61K31/553 , A61K31/695 , C07D417/04 , C07D417/14 , C07D491/048 , C07D491/10 , C07D498/04 , C07D513/04
摘要: (Wherein n is an integer of from 0 to 3; R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, or a substituted or unsubstituted aromatic heterocyclic group; R2 is halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, a substituted or unsubstituted aromatic heterocyclic group, —COR8, or the like; R3 and R4 may be the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl, —COR12, or the like)For example, provided are adenosine A2A receptor antagonists comprising, as the active ingredient, a thiazole derivative represented by a general formula (I), or a pharmaceutically acceptable salt thereof, and the like.
摘要翻译: (其中n为0〜3的整数; R 1为取代或未取代的环烷基,取代或未取代的芳基,取代或未取代的脂环族杂环基或取代或未取代的芳香族杂环基; R2为卤素,取代或未取代的低级烷基 取代或未取代的芳基,取代或未取代的脂环族杂环基,取代或未取代的芳族杂环基,-COR 8等; R 3和R 4可以相同或不同,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,-COR 12等)例如,提供的是腺苷A 2A受体拮抗剂,其包含作为活性成分的由通式(I)表示的噻唑衍生物或其药学上可接受的盐,以及 类似。
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公开(公告)号:US07718808B2
公开(公告)日:2010-05-18
申请号:US10584633
申请日:2004-12-24
申请人: Takao Nakajima , Masamori Sugawara , Shin-ichi Uchida , Tetsuji Ohno , Yuji Nomoto , Noriaki Uesaka , Yoshisuke Nakasato
发明人: Takao Nakajima , Masamori Sugawara , Shin-ichi Uchida , Tetsuji Ohno , Yuji Nomoto , Noriaki Uesaka , Yoshisuke Nakasato
IPC分类号: A61K31/427 , C07D417/14
CPC分类号: C07D417/06 , A61K31/427 , A61K31/438 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/5383 , A61K31/541 , A61K31/542 , A61K31/551 , A61K31/553 , A61K31/695 , C07D417/04 , C07D417/14 , C07D491/048 , C07D491/10 , C07D498/04 , C07D513/04
摘要: (Wherein n is an integer of from 0 to 3; R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, or a substituted or unsubstituted aromatic heterocyclic group; R2 is halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, a substituted or unsubstituted aromatic heterocyclic group, —COR8, or the like; R3 and R4 may be the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl, —COR12, or the like)For example, provided are adenosine A2A receptor antagonists comprising, as the active ingredient, a thiazole derivative represented by a general formula (I), or a pharmaceutically acceptable salt thereof, and the like.
摘要翻译: 本发明提供的腺苷A 2A受体拮抗剂包含作为活性成分的由通式(I)表示的噻唑衍生物或其药学上可接受的盐:......(其中n为0-3的整数; R 1为取代或 取代或未取代的芳基,取代或未取代的脂环族杂环基或取代或未取代的芳族杂环基; R2为卤素,取代或未取代的低级烷基,取代或未取代的芳基,取代或未取代的脂环族杂环基, 或未取代的芳族杂环基,-COR 8等; R 3和R 4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,-COR 12等)。
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公开(公告)号:US08420827B2
公开(公告)日:2013-04-16
申请号:US12960937
申请日:2010-12-06
申请人: Takao Nakajima , Masamori Sugawara , Shin-ichi Uchida , Tetsuji Ohno , Yuji Nomoto , Noriaki Uesaka , Yoshisuke Nakasato
发明人: Takao Nakajima , Masamori Sugawara , Shin-ichi Uchida , Tetsuji Ohno , Yuji Nomoto , Noriaki Uesaka , Yoshisuke Nakasato
IPC分类号: A61K31/427 , C07D417/14
CPC分类号: C07D417/06 , A61K31/427 , A61K31/438 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/5383 , A61K31/541 , A61K31/542 , A61K31/551 , A61K31/553 , A61K31/695 , C07D417/04 , C07D417/14 , C07D491/048 , C07D491/10 , C07D498/04 , C07D513/04
摘要: Wherein n is an integer of from 0 to 3; R1A is a 5-membered aromatic heterocyclic group containing at least one oxygen atom; R2A is —COR8 (wherein R8 is aryl); R3A is hydrogen or lower alkyl; and R12 represents cycloalkyl, aryl, aralkyl, alicyclic heterocyclic group, aromatic heterocyclic group, alicyclic hetocyclic-alkyl, or aromatic heterocyclic-alkyl, and R1A, R2A, R3A and R12 are individually optionally substituted.
摘要翻译: - 根据式(1A)的化合物,其中n为0至3的整数; R1A是含有至少一个氧原子的5元芳族杂环基; R2A是-COR8(其中R8是芳基); R3A是氢或低级烷基; R 12表示环烷基,芳基,芳烷基,脂环族杂环基,芳香族杂环基,脂环族环状烷基或芳香族杂环烷基,R1A,R2A,R3A,R12分别任选被取代,及其药学上可接受的盐。
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公开(公告)号:US07880013B2
公开(公告)日:2011-02-01
申请号:US12766986
申请日:2010-04-26
IPC分类号: A61K31/427 , C07D417/14
CPC分类号: C07D417/06 , A61K31/427 , A61K31/438 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/5383 , A61K31/541 , A61K31/542 , A61K31/551 , A61K31/553 , A61K31/695 , C07D417/04 , C07D417/14 , C07D491/048 , C07D491/10 , C07D498/04 , C07D513/04
摘要: (Wherein n is an integer of from 0 to 3; R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, or a substituted or unsubstituted aromatic heterocyclic group; R2 is halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, a substituted or unsubstituted aromatic heterocyclic group, —COR8, or the like; R3 and R4 may be the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl, —COR12, or the like)For example, provided are adenosine A2A receptor antagonists comprising, as the active ingredient, a thiazole derivative represented by a general formula (I), or a pharmaceutically acceptable salt thereof, and the like.
摘要翻译: 本发明提供的腺苷A 2A受体拮抗剂包含作为活性成分的通式(I)所示的噻唑衍生物或其药学上可接受的盐等(其中,n为0〜3的整数,R1为 取代或未取代的环烷基,取代或未取代的芳基,取代或未取代的脂环族杂环基或取代或未取代的芳族杂环基; R2为卤素,取代或未取代的低级烷基,取代或未取代的芳基,取代或未取代的脂环族杂环基, 取代或未取代的芳族杂环基,-COR 8等; R 3和R 4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,-COR 12等) 。
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公开(公告)号:US20100280023A1
公开(公告)日:2010-11-04
申请号:US11917972
申请日:2006-06-23
IPC分类号: A61K31/537 , A61K31/427 , C07D417/14 , A61K31/5377 , A61K31/4439 , A61P25/00 , A61P25/16 , A61P25/28 , A61P25/24 , A61P9/10
CPC分类号: C07D491/08 , C07D417/04 , C07D417/14 , C07D493/08 , C07D493/10
摘要: It is intended to provide an adenosine A2A receptor antagonist containing as an active ingredient a thiazole derivative represented by the general formula (I) [in the formula, R1 represents a substituted or unsubstituted five-membered aromatic heterocyclic group containing at least one oxygen atom, R2 represents a substituted or unsubstituted heterocyclic group, —COR6 (in the formula, R6 represents a substituted or unsubstituted heterocyclic group, a substituted or unsubstituted aromatic heterocyclic group or the like) or the like, R3 represents the general formula (II), —NHCOR (in the formula, R7 represents —NR8R9 or the like) or the like], or a pharmacologically acceptable salt thereof, etc. (I) (II)
摘要翻译: 本发明提供一种含有作为活性成分的通式(I)表示的噻唑衍生物的腺苷A 2A受体拮抗剂[式中,R 1表示取代或未取代的含有至少一个氧原子的5元芳族杂环基, R2表示取代或未取代的杂环基,-COR6(式中,R6表示取代或未取代的杂环基,取代或未取代的芳香族杂环基等)等,R3表示通式(II), - NHCOR(式中,R7表示-NR8R9等)或其药理学上可接受的盐等。(I)(II)
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公开(公告)号:US07928098B2
公开(公告)日:2011-04-19
申请号:US11997585
申请日:2006-08-02
申请人: Noriaki Uesaka , Shunji Ichikawa , Takao Nakajima
发明人: Noriaki Uesaka , Shunji Ichikawa , Takao Nakajima
IPC分类号: A61K31/555 , A61K31/54 , A61K31/535 , A61K31/4965 , A61K31/44 , A61K31/425
CPC分类号: C07D417/14 , A61K31/4439 , A61K31/444 , A61K31/506 , A61K31/5377
摘要: The present invention provides a therapeutic and/or preventive agent for a sleep disorder comprising, as an active ingredient, a thiazole derivative represented by the general formula (I), [wherein R1 represents a five-membered aromatic heterocyclic group including at least one oxygen atom, or the like, R2 represents halogen or the like, and R3 represents —NR10R11 (wherein R10 and R11 may be the same or different, and each represents a hydrogen atom or the like), or the like] or a pharmaceutically acceptable salt thereof.
摘要翻译: 本发明提供了一种睡眠障碍的治疗和/或预防剂,其包含作为活性成分的由通式(I)表示的噻唑衍生物,其中R 1表示包含至少一个氧的五元芳族杂环基 原子等,R 2表示卤素等,R 3表示-NR 10 R 11(其中R 10和R 11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 其中。
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公开(公告)号:US20100152162A1
公开(公告)日:2010-06-17
申请号:US11997585
申请日:2006-08-02
申请人: Noriaki Uesaka , Shunji Ichikawa , Takao Nakajima
发明人: Noriaki Uesaka , Shunji Ichikawa , Takao Nakajima
IPC分类号: A61K31/444 , A61K31/497 , A61K31/5377 , A61K31/541 , A61K31/427 , A61K31/553 , A61P25/00
CPC分类号: C07D417/14 , A61K31/4439 , A61K31/444 , A61K31/506 , A61K31/5377
摘要: It is intended to provide an agent for treating and/or preventing sleep disorder containing as an active ingredient a thiazole derivative represented by the general formula (I) (in the formula, R1 represents a five-membered aromatic heterocyclic group containing at least one oxygen atom or the like, R2 represents halogen or the like, and R3 represents —NR10R11 (in the formula, R10 and R11 are the same or different and represent a hydrogen atom or the like) or the like) or a pharmacologically acceptable salt thereof.
摘要翻译: 旨在提供一种治疗和/或预防睡眠障碍的药剂,其含有作为活性成分的由通式(I)表示的噻唑衍生物(式中,R1表示含有至少一个氧的五元芳族杂环基) 原子等,R2表示卤素等,R3表示-NR10R11(式中,R10和R11相同或不同,表示氢原子等)或其药理学上可接受的盐。
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公开(公告)号:US20060252780A1
公开(公告)日:2006-11-09
申请号:US10554254
申请日:2004-04-23
申请人: Takao Nakajima , Kimihisa Ueno , Yuji Nomoto , Yuichi Matsumoto , Hiroshi Yano , Satoshi Nakanishi , Kotaro Takasaki , Hideaki Kusaka
发明人: Takao Nakajima , Kimihisa Ueno , Yuji Nomoto , Yuichi Matsumoto , Hiroshi Yano , Satoshi Nakanishi , Kotaro Takasaki , Hideaki Kusaka
IPC分类号: A61K31/519 , C07D487/14
CPC分类号: C07D487/14
摘要: A fused pyrimidine derivative is presented. The derivatie has an insulin secretion stimulating activity represented by Formula (I): {wherein R1 represents a hydrogen atom, lower alkyl, or the like; n represents an integer of 0 to 3; and X1 and X2 may be the same or different and each represents a hydrogen atom, lower alkyl, or the like; and formula (II): represents formula (III): [wherein X—Y—Z represents R2C═CR3—NR4 (wherein R2, R3 and R4 may be the same or different and each represents a hydrogen atom, lower alkyl, or the like)]}, or a pharmaceutically acceptable salt thereof.
摘要翻译: 提出了一种稠合的嘧啶衍生物。 衍生物具有由式(I)表示的胰岛素分泌刺激活性:其中R 1表示氢原子,低级烷基等; n表示0〜3的整数, X 1和X 2可以相同或不同,各自表示氢原子,低级烷基等; 和式(II):表示式(III):[其中XYZ表示R 2 C-CR 3 -NR 4(其中R' O 2,R 3和R 4可以相同或不同,各自表示氢原子,低级烷基等)]}, 或其药学上可接受的盐。
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