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11. 发明申请

US20050119304A1 Urea derivatives 审中-公开
标题翻译：尿素衍生物
公开(公告)号：US20050119304A1
公开(公告)日：2005-06-02
申请号：US10499788
申请日：2002-12-13
申请人： Takeshi Yura , Muneto Mogi , Yuka Ikegami , Tsutomu Masuda , Toshio Kokubo , Klaus Urbahns , Nagahiro Yoshida , Makiko Marumo , Masahiro Shiroo , Masaomi Tajimi , Keisuke Takeshita , Toshiya Moriwaki , Yasuhiro Tsukimi
发明人： Takeshi Yura , Muneto Mogi , Yuka Ikegami , Tsutomu Masuda , Toshio Kokubo , Klaus Urbahns , Nagahiro Yoshida , Makiko Marumo , Masahiro Shiroo , Masaomi Tajimi , Keisuke Takeshita , Toshiya Moriwaki , Yasuhiro Tsukimi
IPC分类号： A61K31/343 , A61K31/365 , A61K31/381 , A61K31/404 , A61K31/416 , A61K31/4184 , A61K31/4192 , A61K31/428 , A61P9/00 , A61P9/10 , A61P13/02 , A61P13/10 , A61P19/02 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/18 , A61P25/28 , A61P29/00 , A61P43/00 , C07D209/08 , C07D231/56 , C07D235/06 , C07D235/08 , C07D235/10 , C07D249/18 , C07D277/62 , C07D277/64 , C07D277/70 , C07D277/72 , C07D277/74 , C07D307/83 , C07D307/88 , C07D333/54 , A61K31/4709 , A61K31/405
CPC分类号： C07D333/54 , A61K31/365 , A61K31/404 , A61K31/416 , A61K31/4184 , A61K31/4192 , A61K31/428 , C07D209/08 , C07D231/56 , C07D235/06 , C07D235/08 , C07D235/10 , C07D249/18 , C07D277/62 , C07D277/64 , C07D277/72 , C07D277/74 , C07D307/83
摘要： A medicament which contains a urea derivative or a salt thereof as an active ingredient is disclosed. The medicament has an excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, incontinence and/or inflammatory disorders.
摘要翻译：公开了含有脲衍生物或其盐作为活性成分的药物。该药物作为VR1拮抗剂具有优异的活性，可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗急性尿失禁，膀胱过度活动症，慢性疼痛，神经性疼痛，术后疼痛，类风湿性关节炎疼痛，神经痛，神经病，酸痛，神经损伤，局部缺血，神经变性，中风，失禁和/或炎症性疾病。

12. 发明申请

US20050154230A1 Urea derivatives 审中-公开
标题翻译：尿素衍生物
公开(公告)号：US20050154230A1
公开(公告)日：2005-07-14
申请号：US10499785
申请日：2002-12-13
申请人： Takeshi Yura , Muneto Mogi , Yuka Ikegami , Tsutomu Masuda , Toshio Kokubo , Klaus Urbahns , Nagahiro Yoshida , Makiko Marumo , Masahiro Shiroo , Masaomi Tajimi , Keisuke Takeshita , Toshiya Moriwaki , Yasuhiro Tsukimi
发明人： Takeshi Yura , Muneto Mogi , Yuka Ikegami , Tsutomu Masuda , Toshio Kokubo , Klaus Urbahns , Nagahiro Yoshida , Makiko Marumo , Masahiro Shiroo , Masaomi Tajimi , Keisuke Takeshita , Toshiya Moriwaki , Yasuhiro Tsukimi
IPC分类号： C07D295/12 , A61K31/167 , A61K31/17 , A61K31/216 , A61K31/277 , A61K31/341 , A61K31/36 , A61K31/381 , A61K31/403 , A61K31/416 , A61K31/44 , A61K31/4406 , A61K31/4453 , A61K31/47 , A61K31/472 , A61K31/496 , A61P9/10 , A61P13/10 , A61P25/00 , A61P25/04 , A61P25/28 , A61P29/00 , A61P29/02 , A61P43/00 , C07C275/10 , C07C275/24 , C07C275/28 , C07C275/30 , C07C275/32 , C07C275/34 , C07C275/36 , C07C275/38 , C07C275/40 , C07C275/42 , C07C323/33 , C07C323/43 , C07D209/88 , C07D213/40 , C07D213/75 , C07D215/38 , C07D217/06 , C07D231/56 , C07D295/135 , C07D307/52 , C07D317/06 , C07D317/58 , C07D317/66 , C07D333/20 , C07D333/36
CPC分类号： C07D333/36 , C07C275/24 , C07C275/28 , C07C275/30 , C07C275/32 , C07C275/40 , C07C275/42 , C07C323/43 , C07C2602/10 , C07C2603/18 , C07D209/88 , C07D213/40 , C07D213/75 , C07D217/06 , C07D231/56 , C07D295/135 , C07D307/52 , C07D317/06 , C07D317/58 , C07D333/20
摘要： This invention relates to urea derivatives and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The urea derivatives of the present invention has an excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, incontinence and/or inflammatory disorders.
摘要翻译：本发明涉及尿素衍生物及其盐，其可用作药物制剂的活性成分。本发明的脲衍生物作为VR1拮抗剂具有优异的活性，可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗急性尿失禁，膀胱过度活动症，慢性疼痛，神经性疼痛，术后疼痛，类风湿性关节炎疼痛，神经痛，神经病，酸痛，神经损伤，局部缺血，神经变性，中风，失禁和/或炎症性疾病。

13. 发明申请

US20070027187A1 Hydroxy-tetrahydro-naphthalenylurea derivatives 失效
标题翻译：羟基 - 四氢 - 萘基脲衍生物
公开(公告)号：US20070027187A1
公开(公告)日：2007-02-01
申请号：US10545556
申请日：2004-02-05
申请人： Takeshi Yura , Muneto Mogi , Hiroshi Fujishima , Klaus Urbahns , Tsutomu Masuda , Yasuhiro Tsukimi , Masaomi Tajimi , Noriyuki Yamamoto , Nagahiro Yoshida , Toshiya Moriwaki
发明人： Takeshi Yura , Muneto Mogi , Hiroshi Fujishima , Klaus Urbahns , Tsutomu Masuda , Yasuhiro Tsukimi , Masaomi Tajimi , Noriyuki Yamamoto , Nagahiro Yoshida , Toshiya Moriwaki
IPC分类号： A61K31/445 , A61K31/277 , A61K31/195 , A61K31/17
CPC分类号： C07D295/096 , C07C275/32 , C07C2602/10
摘要： This invention relates to hydroxy-tetrahydro-naphthalenylurea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The hydroxy-tetrahydro-naphthalenylurea derivatives of the present invention have an excellent activity as VR1 antagonist and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.
摘要翻译：本发明涉及可用作药物制剂活性成分的羟基 - 四氢 - 萘基脲衍生物及其盐。本发明的羟基 - 四氢 - 萘基脲衍生物作为VR1拮抗剂具有优异的活性，并且可用于预防和治疗与VR1活性有关的疾病，特别是用于治疗尿失禁，敦促性尿失禁，膀胱过度活动症，慢性疼痛，神经性疼痛，术后疼痛，类风湿关节炎疼痛，神经痛，神经病，痛觉，神经损伤，局部缺血，神经变性，中风，炎性疾病，哮喘和COPD。

14. 发明授权

US07423175B2 Hydroxy-tetrahydro-naphthalenylurea derivatives 失效
标题翻译：羟基 - 四氢 - 萘基脲衍生物
公开(公告)号：US07423175B2
公开(公告)日：2008-09-09
申请号：US10545556
申请日：2004-02-05
申请人： Takeshi Yura , Muneto Mogi , Hiroshi Fujishima , Klaus Urbahns , Tsutomu Masuda , Yasuhiro Tsukimi , Masaomi Tajimi , Noriyuki Yamamoto , Nagahiro Yoshida , Toshiya Moriwaki
发明人： Takeshi Yura , Muneto Mogi , Hiroshi Fujishima , Klaus Urbahns , Tsutomu Masuda , Yasuhiro Tsukimi , Masaomi Tajimi , Noriyuki Yamamoto , Nagahiro Yoshida , Toshiya Moriwaki
IPC分类号： C07C275/32 , A61K31/17
CPC分类号： C07D295/096 , C07C275/32 , C07C2602/10
摘要： This invention relates to hydroxy-tetrahydro-naphthalenylurea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The hydroxy-tetrahydro-naphthalenylurea derivatives of the present invention have an excellent activity as VR1 antagonist and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.
摘要翻译：本发明涉及可用作药物制剂活性成分的羟基 - 四氢 - 萘基脲衍生物及其盐。本发明的羟基 - 四氢 - 萘基脲衍生物作为VR1拮抗剂具有优异的活性，并且可用于预防和治疗与VR1活性有关的疾病，特别是用于治疗尿失禁，敦促性尿失禁，膀胱过度活动症，慢性疼痛，神经性疼痛，术后疼痛，类风湿关节炎疼痛，神经痛，神经病，痛觉，神经损伤，局部缺血，神经变性，中风，炎性疾病，哮喘和COPD。

15. 发明申请

US20060258742A1 Hydroxy tetrahydro-naphthalenylurea derivatives 有权
公开(公告)号：US20060258742A1
公开(公告)日：2006-11-16
申请号：US10513848
申请日：2003-04-28
申请人： Takeshi Yura , Muneto Mogi , Klaus Urbahns , Hiroshi Fujishima , Tsutomu Masuda , Toshiya Moriwaki , Nagahiro Yoshida
发明人： Takeshi Yura , Muneto Mogi , Klaus Urbahns , Hiroshi Fujishima , Tsutomu Masuda , Toshiya Moriwaki , Nagahiro Yoshida
IPC分类号： A61K31/277 , A61K31/195 , A61K31/17 , C07C275/28
CPC分类号： C07C275/42 , C07C275/32 , C07C275/40
摘要： This invention relates to tetrahydro-naphthalene derivatives and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, incontinence, inflammatory disorders such as asthma and COPD.

16. 发明授权

US06911443B2 Imidazopyrimidine derivatives and triazolopyrimidine derivatives 失效
标题翻译：咪唑并嘧啶衍生物和三唑并嘧啶衍生物
公开(公告)号：US06911443B2
公开(公告)日：2005-06-28
申请号：US10258628
申请日：2001-04-17
申请人： Takeshi Yura , Arnel B. Concepcion , Gyoonhee Han , Makiko Marumo , Hiroko Yoshino , Norihiro Kawamura , Toshio Kokubo , Hiroshi Komura , Yingfu Li , Timothy B. Lowinger , Muneto Mogi , Noriyuki Yamamoto , Nagahiro Yoshida , Scott Miller , Margaret A. Popp , Aniko M. Redmann , Martha E. Rodriguez , William J. Scott , Ming Wang
发明人： Takeshi Yura , Arnel B. Concepcion , Gyoonhee Han , Makiko Marumo , Hiroko Yoshino , Norihiro Kawamura , Toshio Kokubo , Hiroshi Komura , Yingfu Li , Timothy B. Lowinger , Muneto Mogi , Noriyuki Yamamoto , Nagahiro Yoshida , Scott Miller , Margaret A. Popp , Aniko M. Redmann , Martha E. Rodriguez , William J. Scott , Ming Wang
IPC分类号： A61K31/505 , A61K31/519 , A61K31/5377 , A61K31/541 , A61P1/04 , A61P3/04 , A61P7/02 , A61P7/06 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P21/04 , A61P25/28 , A61P27/02 , A61P27/14 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D487/04 , C07D519/00 , C07D417/10
CPC分类号： C07D487/04
摘要： A compound of the formula (I) in which R1 is —OR11, —SR11, —SOR11, —SO2R11, —NHR11, or —NR12R13 , and R11, R12, and R13 are as defined broadly in the text. R2 is H, C1-C6alkyl, carbamoyl, or an ester group. R3 is thienyl, pyridyl optionally substituted by halogen or C1-C6alkoxy; naphthyl optionally substituted by C1-C6alkoxy; dioxane fused phenyl; dioxacyclopentane fused phenyl; or optionally substituted phenyl. Y is CH or N. A process for preparing such compounds, pharmaceutical compositions containing such compounds, and a method of treating asthma using them are also disclosed and claimed.
摘要翻译：其中R 1为-OR 11，-SR 11，-SOR 11的式（I）化合物， SO 2，-SO 2，R 11，-NHR 11或-NR 12 R 13 ＆lt; / SUP＆gt;和R 11，R 12和R 13如在文中广义地定义的。 R 2是H，C 1 -C 6烷基，氨基甲酰基或酯基。 R 3是噻吩基，任选被卤素或C 1 -C 6烷氧基取代的吡啶基; 任选被C 1 -C 6烷氧基取代的萘基; 二恶烷稠合苯基; 二氧杂环戊烷稠合苯基; 或任选取代的苯基。 Y是CH或N.一种制备这种化合物的方法，含有这些化合物的药物组合物和使用它们治疗哮喘的方法也被公开和要求保护。

17. 发明授权

US07674797B2 2-phenoxy- and 2-phenylsulfonamide derivatives with CCR3 antagonistic activity for the treatment of asthma and other inflammatory or immunological disorders 有权
标题翻译：具有CCR3拮抗活性的2-苯氧基和2-苯基磺酰胺衍生物，用于治疗哮喘和其他炎症或免疫疾病
公开(公告)号：US07674797B2
公开(公告)日：2010-03-09
申请号：US10550482
申请日：2004-03-11
申请人： Yingfu Li , Kevin Bacon , Hiromi Sugimoto , Keiko Fukushima , Kentaro Hashimoto , Makiko Marumo , Toshiya Moriwaki , Noriko Nunami , Naoki Tsuno , Klaus Urbahns , Nagahiro Yoshida
发明人： Yingfu Li , Kevin Bacon , Hiromi Sugimoto , Keiko Fukushima , Kentaro Hashimoto , Makiko Marumo , Toshiya Moriwaki , Noriko Nunami , Naoki Tsuno , Klaus Urbahns , Nagahiro Yoshida
IPC分类号： A01N43/42 , A61K31/496 , C07D221/18 , C07D221/22
CPC分类号： C07D487/04 , A61K31/439 , C07C311/29 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/40 , C07D207/404 , C07D207/48 , C07D211/54 , C07D223/12 , C07D241/04 , C07D243/08 , C07D257/04 , C07D295/13 , C07D295/22 , C07D295/26 , C07D303/06 , C07D303/36 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/12 , C07D453/02 , C07D487/02 , C07D487/08
摘要： The present invention relates to a benzenesulfonamide derivative of formula (I), which is useful as an active ingredient of pharmaceutical preparations. The benzenesulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders. In said formula, X represents O or S; R4 represents formulae (a), (b), (c), (d), (e), (f), (g), (h), (i) or (j), the other substituents are as defined in claim 1.
摘要翻译：本发明涉及式（I）的苯磺酰胺衍生物，其可用作药物制剂的活性成分。本发明的苯磺酰胺衍生物具有CCR3（CC型趋化因子受体）拮抗活性，可用于预防和治疗与CCR3活性有关的疾病，特别是用于治疗哮喘，特应性皮炎，过敏性鼻炎等炎症 /免疫学障碍。在所述式中，X表示O或S; R4代表式（a），（b），（c），（d），（e），（f），（g），（h），（i）或（j）权利要求1。

18. 发明申请

US20090286771A1 2-Phenoxy- and 2-Phenylsulfonamide Derivatives with CCR3 Antagonistic Activity for the Treatment of Inflammatory or Immunological Disorders 审中-公开
标题翻译：具有CCR3拮抗活性的2-苯氧基 - 和2-苯基磺酰胺衍生物用于治疗炎症或免疫疾病
公开(公告)号：US20090286771A1
公开(公告)日：2009-11-19
申请号：US12504606
申请日：2009-07-16
申请人： Yingfu Li , Kevin Bacon , Hiromi Sugimoto , Keiko Fukushima , Kentaro Hashimoto , Makiko Marumo , Toshiya Moriwaki , Noriko Nunami , Naoki Tsuno , Klaus Urbahns , Nagahiro Yoshida
发明人： Yingfu Li , Kevin Bacon , Hiromi Sugimoto , Keiko Fukushima , Kentaro Hashimoto , Makiko Marumo , Toshiya Moriwaki , Noriko Nunami , Naoki Tsuno , Klaus Urbahns , Nagahiro Yoshida
IPC分类号： A61K31/496 , A61K31/439 , A61K31/551 , A61K31/55 , A61P9/10 , A61P25/28 , A61P31/18
CPC分类号： C07D487/04 , A61K31/439 , C07C311/29 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/40 , C07D207/404 , C07D207/48 , C07D211/54 , C07D223/12 , C07D241/04 , C07D243/08 , C07D257/04 , C07D295/13 , C07D295/22 , C07D295/26 , C07D303/06 , C07D303/36 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/12 , C07D453/02 , C07D487/02 , C07D487/08
摘要： Provided herein are 2-phenoxy- and 2-phenylsulfonamide derivatives with CCR3 antagonistic activity. These compounds are useful for the treatment of diseases associated with CCR3 activity, including but not limited to, atopic dermatitis, allergic rhinitis, rheumatoid arthritis, Grave's disease, HIV infection, Alzheimer's disease, atherosclerosis and other inflammatory and/or immunological disorders.
摘要翻译：本文提供具有CCR3拮抗活性的2-苯氧基 - 和2-苯基磺酰胺衍生物。这些化合物可用于治疗与CCR3活性相关的疾病，包括但不限于特应性皮炎，过敏性鼻炎，类风湿性关节炎，格雷夫氏病，艾滋病毒感染，阿尔茨海默病，动脉粥样硬化和其他炎症和/或免疫学疾病。

19. 发明申请

US20070155725A1 2-Phenoxy- and 2-phenylsulfomamide derivatives with ccr3 antagonistic activity for the treatment of asthma and other inflammatory or immunological disorders 有权
标题翻译：具有ccr3拮抗活性的2-苯氧基-2-苯磺酰胺衍生物，用于治疗哮喘和其他炎性或免疫性疾病
公开(公告)号：US20070155725A1
公开(公告)日：2007-07-05
申请号：US10550482
申请日：2004-03-11
申请人： Yingfu Li , Kevin Bacon , Hiromi Sugimoto , Keiko Fukushima , Kentaro Hashimoto , Makiko Marumo , Toshiya Moriwaki , Noriko Nunami , Naoki Tsuno , Klaus Urbahns , Nagahiro Yoshida
发明人： Yingfu Li , Kevin Bacon , Hiromi Sugimoto , Keiko Fukushima , Kentaro Hashimoto , Makiko Marumo , Toshiya Moriwaki , Noriko Nunami , Naoki Tsuno , Klaus Urbahns , Nagahiro Yoshida
IPC分类号： A61K31/551 , A61K31/495 , A61K31/4745 , A61K31/445 , A61K31/4025 , A61K31/18 , C07D211/54 , C07D403/02 , C07D453/02
CPC分类号： C07D487/04 , A61K31/439 , C07C311/29 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/40 , C07D207/404 , C07D207/48 , C07D211/54 , C07D223/12 , C07D241/04 , C07D243/08 , C07D257/04 , C07D295/13 , C07D295/22 , C07D295/26 , C07D303/06 , C07D303/36 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/12 , C07D453/02 , C07D487/02 , C07D487/08
摘要： The present invention relates to a benzenesulfonamide derivative of formula (I), which is useful as an active ingredient of pharmaceutical preparations. The benzenesulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders. In said formula, X represents O or S; R4 represents formulae (a), (b), (c), (d), (e), (f), (g), (h), (i) or (j), the other substituents are as defined in claim 1.
摘要翻译：本发明涉及式（I）的苯磺酰胺衍生物，其可用作药物制剂的活性成分。本发明的苯磺酰胺衍生物具有CCR3（CC型趋化因子受体）拮抗活性，可用于预防和治疗与CCR3活性有关的疾病，特别是用于治疗哮喘，特应性皮炎，过敏性鼻炎等炎症 /免疫学障碍。在所述式中，X表示O或S; R 4表示式（a），（b），（c），（d），（e），（f），（g），（h），（i）或（j），其它取代基如权利要求1中所定义。

20. 发明授权

US06589949B1 3-oxo-2,1-benzisoxazol-1(3H)-carboxamides for treatment of CNS diseases 失效
标题翻译： 3-氧代-2,1-苯并异恶唑-1（3H） - 甲酰胺，用于治疗CNS疾病
公开(公告)号：US06589949B1
公开(公告)日：2003-07-08
申请号：US10149658
申请日：2002-10-22
申请人： Toshiya Moriwaki , Chantal Fürstner , Bernd Riedl , Jens-Kerim Ergüden , Frank Böss , Bernard Schmidt , Franz-Josef van der Staay , Werner Schröder , Karl-Heinz Schlemmer , Nagahiro Yoshida
发明人： Toshiya Moriwaki , Chantal Fürstner , Bernd Riedl , Jens-Kerim Ergüden , Frank Böss , Bernard Schmidt , Franz-Josef van der Staay , Werner Schröder , Karl-Heinz Schlemmer , Nagahiro Yoshida
IPC分类号： A61K315377
CPC分类号： C07D261/20
摘要： The invention relates to novel 3-oxo-2,1-benzisomazol-1(3H)-carboxamides (I), where R1, R2 are the same or different and independently=H, halogen, C1 C6 alkyl C1 C6 alkoxy, C1 C3 perfluoroalkyl, or a group NR5R6; R3, R4 are the same or different and independently=C1 C8 alkyl, whose carbon chain is optionally interrupted by an O, S or NR7 and is optionally singly or severally substituted by C3 C6 cycloalkyl, C1 C4 alkoxy, OH, halogen or NR8R9; C3 C8 cycloalkyl whose carbon chain is optionally interrupted by an O, S or NR10 and is optionally singly or severally substituted by C1 C4 alkoxy, OH, halogen or NR11R12, or R3 and R4 together with a nitrogen atom form a saturated or partially unsaturated 3- to 10-membered mono- or bi-cyclic heteocycle, which, optionally, contains up to two further heteroatoms, from N, O or S and is, optionally, substituted by C1 C4 alkyl, C1 C4 alkoxy, OH, halogen, COOR13 or NR14R15 and X=O or S. The invention further relates to methods for production thereof and use thereof in the production of medicaments for the prophylaxis and/or treatment of diseases of the central nervous system, in particular, cognitive disorders, such as Alzheimer's disease and other forms of dementia, cerebral infarct, skull and brain trauma and pain.
摘要翻译：本发明涉及新的3-氧代-2,1-苯并异恶唑-1（3H） - 甲酰胺（I），其中R 1，R 2相同或不同且独立地为H，卤素，C 1 -C 6烷基C 1 -C 6烷氧基，C 1 C 3 全氟烷基或NR5R6基团; R 3，R 4相同或不同且独立地为C 1 -C 8烷基，其碳链任选地被O，S或NR 7中断，并且任选地被C 3 -C 6环烷基，C 1 -C 4烷氧基，OH，卤素或NR 8 R 9单独或多个取代; C 8 -C 8环烷基，其碳链任选地被O，S或NR 10中断，并且任选地被C 1 -C 4烷氧基，OH，卤素或NR 11 R 12单独或多个取代，或者R 3和R 4与氮原子一起形成饱和或部分不饱和的3 至10元单环或双环杂环，其任选地含有至多两个另外的N，O或S的杂原子，并且任选地被C 1 -C 4烷基，C 1 -C 4烷氧基，OH，卤素，COOR 13 或NR14R15和X = O或S.本发明还涉及其生产方法及其在生产用于预防和/或治疗中枢神经系统疾病的药物中的用途，特别是认知障碍，例如阿尔茨海默病疾病和其他形式的痴呆，脑梗塞，头骨和脑外伤和疼痛。

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