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公开(公告)号:US20090270376A1
公开(公告)日:2009-10-29
申请号:US12065234
申请日:2006-12-25
申请人: Takayuki Inoue , Akira Tanaka , Kazuo Nakai , Hiroshi Sasaki , Fumie Takahashi , Shohei Shirakami , Keiko Hatanaka , Yutaka Nakajima , Koichiro Mukoyoshi , Hisao Hamaguchi , Shigeki Kunikawa , Yasuyuki Higashi
发明人: Takayuki Inoue , Akira Tanaka , Kazuo Nakai , Hiroshi Sasaki , Fumie Takahashi , Shohei Shirakami , Keiko Hatanaka , Yutaka Nakajima , Koichiro Mukoyoshi , Hisao Hamaguchi , Shigeki Kunikawa , Yasuyuki Higashi
IPC分类号: A61K31/437 , C07D471/04 , C07D471/14 , A61K31/496 , A61K31/5377 , A61K31/541 , A61P37/00 , A61P25/28 , A61P35/00
CPC分类号: C07D451/04 , C07D471/04 , C07D471/14 , C07D519/00
摘要: The present invention provides a compound of formula (I) having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases inflammatory diseases, and allergic diseases. The compound according to the present invention has an inhibition activity against JAK3 and is thus useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transmission (e.g., rejection during organ/tissue transplantation, autoimmune diseases, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, Alzheimer's disease, and atherosclerotic disease), or diseases caused by abnormal cytokine signal transmission (e.g., cancer and leukemia).
摘要翻译: 本发明提供了具有优异的JAK3抑制活性的式(I)化合物,并且可用作治疗和/或预防各种免疫疾病,包括自身免疫性疾病炎性疾病和过敏性疾病的药剂的活性成分。 根据本发明的化合物对JAK3具有抑制活性,因此可用作治疗或预防由不良细胞因子信号传导引起的疾病(例如器官/组织移植期间的排斥,自身免疫性疾病,多发性硬化症)的活性成分 ,类风湿性关节炎,牛皮癣,哮喘,特应性皮炎,阿尔茨海默病和动脉粥样硬化疾病)或由异常细胞因子信号传导引起的疾病(例如癌症和白血病)。
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公开(公告)号:US20110039822A1
公开(公告)日:2011-02-17
申请号:US12914475
申请日:2010-10-28
申请人: Takayuki INOUE , Akira Tanaka , Kazuo Nakai , Hiroshi Sasaki , Fumie Takahashi , Shohei Shirakami , Keiko Hatanaka , Yutaka Nakajima , Koichiro Mukoyoshi , Hisao Hamaguchi , Shigeki Kunikawa , Yasuyuki Higashi
发明人: Takayuki INOUE , Akira Tanaka , Kazuo Nakai , Hiroshi Sasaki , Fumie Takahashi , Shohei Shirakami , Keiko Hatanaka , Yutaka Nakajima , Koichiro Mukoyoshi , Hisao Hamaguchi , Shigeki Kunikawa , Yasuyuki Higashi
IPC分类号: A61K31/437 , C07D471/04 , C07D471/14 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541 , A61P17/06 , A61P19/02 , A61P37/00 , A61P37/06
CPC分类号: C07D451/04 , C07D471/04 , C07D471/14 , C07D519/00
摘要: The present invention provides a compound having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases, inflammatory diseases, and allergic diseases.As a result of studies on a novel condensed heterocyclic derivative, the inventors have found that a compound having a cross-linked structure has an excellent JAK3 inhibition activity, and have completed the present invention.In other words, it is verified that the compound according to the present invention has an inhibition activity against JAK3 and is thus useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transmission (e.g., rejection during organ/tissue transplantation, autoimmune diseases, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, Alzheimer's disease, and atherosclerotic disease), or diseases caused by abnormal cytokine signal transmission (e.g., cancer and leukemia).
摘要翻译: 本发明提供具有优异的JAK3抑制活性的化合物,可用作治疗和/或预防各种免疫疾病,包括自身免疫性疾病,炎症性疾病和过敏性疾病的药剂的活性成分。 作为研究新型稠合杂环衍生物的结果,本发明人发现具有交联结构的化合物具有优异的JAK3抑制活性,并且完成了本发明。 换句话说,证实了本发明的化合物对JAK3具有抑制活性,因此可用作治疗或预防由不期望的细胞因子信号传导引起的疾病的药剂的活性成分(例如器官/ 组织移植,自身免疫性疾病,多发性硬化,类风湿性关节炎,牛皮癣,哮喘,特应性皮炎,阿尔茨海默病和动脉粥样硬化疾病)或由异常细胞因子信号传导引起的疾病(例如癌症和白血病)。
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公开(公告)号:US07879844B2
公开(公告)日:2011-02-01
申请号:US12065234
申请日:2006-12-25
申请人: Takayuki Inoue , Akira Tanaka , Kazuo Nakai , Hiroshi Sasaki , Fumie Takahashi , Shohei Shirakami , Keiko Hatanaka , Yutaka Nakajima , Koichiro Mukoyoshi , Hisao Hamaguchi , Shigeki Kunikawa , Yasuyuki Higashi
发明人: Takayuki Inoue , Akira Tanaka , Kazuo Nakai , Hiroshi Sasaki , Fumie Takahashi , Shohei Shirakami , Keiko Hatanaka , Yutaka Nakajima , Koichiro Mukoyoshi , Hisao Hamaguchi , Shigeki Kunikawa , Yasuyuki Higashi
IPC分类号: A61K31/437 , A61K31/496 , A61K31/5377 , A61K31/541 , C07D471/04 , C07D471/14 , A61P37/00 , A61P25/28 , A61P35/00
CPC分类号: C07D451/04 , C07D471/04 , C07D471/14 , C07D519/00
摘要: The present invention provides a compound of formula (I) having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases inflammatory diseases, and allergic diseases. The compound according to the present invention has an inhibition activity against JAK3 and is thus useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transmission (e.g., rejection during organ/tissue transplantation, autoimmune diseases, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, Alzheimer's disease, and atherosclerotic disease), or diseases caused by abnormal cytokine signal transmission (e.g., cancer and leukemia).
摘要翻译: 本发明提供了具有优异的JAK3抑制活性的式(I)化合物,并且可用作治疗和/或预防各种免疫疾病,包括自身免疫性疾病炎性疾病和过敏性疾病的药剂的活性成分。 根据本发明的化合物对JAK3具有抑制活性,因此可用作治疗或预防由不良细胞因子信号传导引起的疾病(例如器官/组织移植期间的排斥,自身免疫性疾病,多发性硬化症)的活性成分 ,类风湿性关节炎,牛皮癣,哮喘,特应性皮炎,阿尔茨海默病和动脉粥样硬化疾病)或由异常细胞因子信号传导引起的疾病(例如癌症和白血病)。
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公开(公告)号:US08163767B2
公开(公告)日:2012-04-24
申请号:US11995445
申请日:2006-07-13
申请人: Takayuki Inoue , Takashi Tojo , Masataka Morita , Yutaka Nakajima , Keiko Hatanaka , Shohei Shirakami , Hiroshi Sasaki , Akira Tanaka , Fumie Takahashi , Koichiro Mukoyoshi , Yasuyuki Higashi , Akira Okimoto , Takeshi Hondo , Hitoshi Sawada
发明人: Takayuki Inoue , Takashi Tojo , Masataka Morita , Yutaka Nakajima , Keiko Hatanaka , Shohei Shirakami , Hiroshi Sasaki , Akira Tanaka , Fumie Takahashi , Koichiro Mukoyoshi , Yasuyuki Higashi , Akira Okimoto , Takeshi Hondo , Hitoshi Sawada
IPC分类号: A61K31/44 , C07D471/14
CPC分类号: C07D471/14 , C07D519/00
摘要: The invention relates to compound of the formula (I) or its salt, wherein —R1, —R2, —R3, —R4, —R5, -M-, —X— and —Y═ are as defined in the description, their use of as, medicament, the process for their preparation and use for the treatment of JAK3 mediated diseases.
摘要翻译: 本发明涉及式(I)化合物或其盐,其中-R1,-R2,-R3,-R4,-R5,-M-,-X-和-Y =如说明书中所定义,它们 使用as,药物,其制备方法和用于治疗JAK3介导的疾病。
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公开(公告)号:US20090264399A1
公开(公告)日:2009-10-22
申请号:US11995445
申请日:2006-07-13
申请人: Takayuki Inoue , Takashi Tojo , Masataka Morita , Yutaka Nakajima , Keiko Hatanaka , Shohei Shirakami , Hiroshi Sasaki , Akira Tanaka , Fumie Takahashi , Koichiro Mukoyoshi , Yasuyuki Higashi , Akira Okimoto , Takeshi Hondo , Hitoshi Sawada
发明人: Takayuki Inoue , Takashi Tojo , Masataka Morita , Yutaka Nakajima , Keiko Hatanaka , Shohei Shirakami , Hiroshi Sasaki , Akira Tanaka , Fumie Takahashi , Koichiro Mukoyoshi , Yasuyuki Higashi , Akira Okimoto , Takeshi Hondo , Hitoshi Sawada
IPC分类号: A61K31/437 , C07D471/04 , C07D413/14 , C07D471/14 , A61K31/5377 , A61K31/397 , A61P25/00 , A61P37/06 , A61P35/00 , A61P35/02 , A61P11/06
CPC分类号: C07D471/14 , C07D519/00
摘要: The invention relates to compound of the formula (I) or its salt, wherein —R1, —R2, —R3, —R4, —R5, -M-, —X— and —Y═ are as defined in the description, their use of as, medicament, the process for their preparation and use for the treatment of JAK3 mediated diseases.
摘要翻译: 本发明涉及式(I)或其盐的化合物,其中-R1,-R2,-R3,-R4,-R5,-M-,-X-和-Y-如说明书中所定义,它们 使用as,药物,其制备方法和用于治疗JAK3介导的疾病。
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公开(公告)号:US20100105661A1
公开(公告)日:2010-04-29
申请号:US12522987
申请日:2008-01-11
申请人: Shohei Shirakami , Takayuki Inoue , Koichiro Mukoyoshi , Yutaka Nakajima , Hiroyuki Usuda , Hisao Hamaguchi , Yasuyuki Higashi , Keiko Hatanaka
发明人: Shohei Shirakami , Takayuki Inoue , Koichiro Mukoyoshi , Yutaka Nakajima , Hiroyuki Usuda , Hisao Hamaguchi , Yasuyuki Higashi , Keiko Hatanaka
IPC分类号: A61K31/55 , A61K31/501 , A61K31/4965 , A61K31/506 , A61K31/437 , C07D471/04
CPC分类号: C07D471/04 , C07D471/14
摘要: The present invention provides a compound having excellent JAK3 inhibitory activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases, inflammatory diseases, and allergic diseases.As a result of investigations with respect to novel condensed heterocyclic derivatives, the inventors have verified that a condensed pyridine compound has excellent JAK3 inhibitory activity, thereby completing the present invention.More specifically, it has been verified that since the compound according to the present invention has inhibitory activity against JAK3, the compound is useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transduction (e.g., rejection during live organ/tissue transplantation, autoimmune diseases, asthma, atopic dermatitis, rheumatism, psoriasis and atherosclerotic disease), or diseases caused by abnormal cytokine signal transduction (e.g., cancer and leukemia).
摘要翻译: 本发明提供了具有优异的JAK3抑制活性的化合物,可用作治疗和/或预防各种免疫疾病,包括自身免疫性疾病,炎症性疾病和过敏性疾病的药剂的活性成分。 作为关于新的稠合杂环衍生物的研究结果,本发明人证实了缩合的吡啶化合物具有优异的JAK3抑制活性,从而完成了本发明。 更具体地说,由于本发明的化合物对JAK3具有抑制活性,所以该化合物可用作治疗或预防由不良细胞因子信号转导引起的疾病(例如活体排斥)的药剂的有效成分 器官/组织移植,自身免疫疾病,哮喘,特应性皮炎,风湿病,牛皮癣和动脉粥样硬化疾病)或由细胞因子信号转导异常引起的疾病(例如癌症和白血病)。
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公开(公告)号:US20110230467A1
公开(公告)日:2011-09-22
申请号:US13130527
申请日:2009-11-20
申请人: Shohei Shirakami , Fumie Takahashi , Yutaka Nakajima , Hirofumi Omura , Naohiro Aoyama , Hiroshi Sasaki , Takeshi Hondo , Hiroaki Tominaga
发明人: Shohei Shirakami , Fumie Takahashi , Yutaka Nakajima , Hirofumi Omura , Naohiro Aoyama , Hiroshi Sasaki , Takeshi Hondo , Hiroaki Tominaga
IPC分类号: A61K31/55 , A61K31/5513 , A61K31/5377 , A61P43/00 , A61K31/497 , A61K31/506 , A61K31/444 , A61K31/4439 , C07D401/14 , C07D413/14 , C07D401/12 , C07D417/14 , C07D409/14 , C07D401/00
CPC分类号: C07D401/12 , C07D213/82 , C07D401/14 , C07D405/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/10
摘要: [Problem] The present invention provides a 4,6-diaminonicotinamide compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for treating diseases caused by undesirable and/or abnormal cytokine signal transduction.[Means for Solution] The present inventors have extensively studied compounds having a JAK3 inhibitory action, and as a result, they have found that a 4,6-diaminonicotinamide compound which is the compound of the present invention has an excellent JAK3 inhibitory action and is useful as an agent for preventing or treating diseases caused by undesirable and/or abnormal cytokine signal transduction, thereby completing the present invention.
摘要翻译: 本发明提供了可用作药物组合物的活性成分的特征的4,6-二氨基烟酰胺化合物,特别是用于治疗由不希望的和/或异常的细胞因子信号转导引起的疾病的药物组合物。 [解决方案]本发明人广泛研究了具有JAK3抑制作用的化合物,结果发现作为本发明化合物的4,6-二氨基烟酰胺化合物具有优异的JAK3抑制作用, 可用作预防或治疗由不良和/或异常细胞因子信号转导引起的疾病的药剂,从而完成本发明。
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公开(公告)号:US20120034250A1
公开(公告)日:2012-02-09
申请号:US13264008
申请日:2010-04-13
申请人: Shohei Shirakami , Yutaka Nakajima , Jun Maeda , Hiroaki Tominaga , Hiroaki Yamagishi , Takeshi Hondo , Masamichi Inami , Hiroki Morio , Takayuki Inoue , Tsuyoshi Mizutani , Hiroki Ishioka
发明人: Shohei Shirakami , Yutaka Nakajima , Jun Maeda , Hiroaki Tominaga , Hiroaki Yamagishi , Takeshi Hondo , Masamichi Inami , Hiroki Morio , Takayuki Inoue , Tsuyoshi Mizutani , Hiroki Ishioka
IPC分类号: A61K31/437 , A61K31/55 , A61P37/06 , A61K31/541 , A61K31/5377 , A61K31/496 , C07D471/14 , A61K31/497
CPC分类号: C07D471/14 , C07D519/00
摘要: [Problem]The present invention provides a condensed pyrrolopyridine derivative which is useful as an active ingredient for a pharmaceutical composition, in particular, a pharmaceutical composition for preventing or treating diseases caused by undesirable cytokine signal transduction or diseases caused by abnormal cytokine signal transduction.[Means for Solution]The present inventors have extensively studied a compound having a JAK inhibitory action, and as a result, they have found that a condensed pyrrolopyridine derivative which is the compound of the present invention has an excellent JAK inhibitory action, and is therefore useful as an agent for preventing or treating diseases caused by undesirable cytokine signal transduction or diseases caused by abnormal cytokine signal transduction, thereby completing the present invention.
摘要翻译: 本发明提供可用作药物组合物的活性成分的特别是用于预防或治疗由不良细胞因子信号转导引起的疾病或由异常细胞因子信号转导引起的疾病的药物组合物的缩合吡咯并吡啶衍生物。 [解决方案]本发明人广泛研究了具有JAK抑制作用的化合物,结果发现,作为本发明化合物的缩合吡咯并吡啶衍生物具有优异的JAK抑制作用,因此 可用作预防或治疗由不良细胞因子信号转导引起的疾病或由异常细胞因子信号转导引起的疾病的药剂,从而完成本发明。
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公开(公告)号:US07035788B1
公开(公告)日:2006-04-25
申请号:US09557741
申请日:2000-04-25
申请人: Yutaka Nakajima , Yutaka Suzue , Kevin B. Gjerstad , Dong-Hui Zhang , Hiroaki Kanokogi , Benjamin M. Westbrook
发明人: Yutaka Nakajima , Yutaka Suzue , Kevin B. Gjerstad , Dong-Hui Zhang , Hiroaki Kanokogi , Benjamin M. Westbrook
IPC分类号: G06F17/27
CPC分类号: G06F17/273 , G06F17/2715 , G06F17/2725 , G06F17/2765
摘要: The sharing of language models is disclosed. In one embodiment, a language model service is provided that is shareable among handlers for input devices. The service includes a pre-processing mode of operation, and a correction mode of operation. In the former mode, the language model service is designed to receive a range within a document from a handler for an input device, and in response provide advice regarding text under consideration by the handler to insert within the document at the range, based on the context of the document within the range. In the latter mode, the language model service is designed to supervise correction over a range of text within a document, in which a number of different handlers for a number of different input devices were initially responsible for insertion of the text, such that the service solicits suggestions from the handlers, and based thereon determines text corrections. The corrections can then be made by the handlers, or by the service.
摘要翻译: 披露了语言模型的共享。 在一个实施例中,提供可在输入设备的处理程序之间共享的语言模型服务。 该服务包括预处理操作模式和操作的校正模式。 在前一模式中,语言模型服务被设计为从输入设备的处理程序接收文档中的范围,并且作为响应,提供关于由处理程序考虑的文本的建议,以便在该范围内的文档内插入,基于 范围内文件的上下文。 在后一种模式中,语言模型服务被设计为对文档内的一系列文本进行校正,其中许多不同的输入设备的不同处理程序最初负责插入文本,使得服务 征求处理人员的意见,并据此确定文本更正。 然后可以由处理程序或服务进行更正。
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公开(公告)号:US06826033B2
公开(公告)日:2004-11-30
申请号:US10380627
申请日:2003-03-21
申请人: Minoru Sakurai , Kenichi Washizuka , Hitoshi Hamashima , Yasuyo Tomishima , Masashi Imanishi , Yutaka Nakajima , Hiroaki Ohtake , Satoru Kuroda , Masayoshi Murata , Hiroshi Kayakiri , Naoaki Fujii , Kiyoshi Taniguchi
发明人: Minoru Sakurai , Kenichi Washizuka , Hitoshi Hamashima , Yasuyo Tomishima , Masashi Imanishi , Yutaka Nakajima , Hiroaki Ohtake , Satoru Kuroda , Masayoshi Murata , Hiroshi Kayakiri , Naoaki Fujii , Kiyoshi Taniguchi
IPC分类号: H01G902
CPC分类号: C07D207/416 , C07C233/43 , C07C233/62 , C07C233/80 , C07C235/56 , C07C275/40 , C07C275/42 , C07C275/54 , C07C311/08 , C07C2601/10 , C07C2601/14 , C07C2602/10 , C07D207/34 , C07D209/08 , C07D209/18 , C07D209/40 , C07D209/42 , C07D209/88 , C07D213/40 , C07D213/56 , C07D213/75 , C07D213/81 , C07D213/82 , C07D215/38 , C07D215/40 , C07D215/48 , C07D215/50 , C07D217/22 , C07D217/26 , C07D231/14 , C07D231/56 , C07D233/90 , C07D235/06 , C07D235/08 , C07D235/16 , C07D237/28 , C07D241/20 , C07D241/42 , C07D241/44 , C07D249/08 , C07D261/14 , C07D261/18 , C07D261/20 , C07D263/34 , C07D277/28 , C07D277/56 , C07D295/215 , C07D307/54 , C07D307/66 , C07D307/68 , C07D307/82 , C07D333/36 , C07D333/38 , C07D333/66 , C07D333/70 , C07D487/04 , Y02P20/55
摘要: The present invention relates to a compound formula (I) wherein X1 is bond or —O—CH2—, (II) or (III) R1 is hydrogen or an amino protective group, a is phenyl, indolyl or carbazolyl, each of which may be substituted with one or two substituent(s), and B is hydrogen; halogen; lower alkyl; lower alkoxycarbonyl; cyclo(lower)alkyl; or a heterocyclic group, naphthyl, 1,2,3,4-tetrahydronaphthyl, benzyl or phenyl, each of which may be substituted with one or two substituent(s), or a salt thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiures or urinary incontinence.
摘要翻译: 本发明涉及其中X 1为键或-O-CH 2 - ,(II)或(III)R 1为氢或氨基保护基的化合物式(I),a为苯基,吲哚基或咔唑基,各自为 可以被一个或两个取代基取代,B是氢; 卤素; 低级烷基 低级烷氧基羰基; 环(低级)烷基; 或杂环基,萘基,1,2,3,4-四氢萘基,苄基或苯基,其各自可以被一个或两个取代基取代,或其盐。 本发明的化合物(I)及其药学上可接受的盐可用于预防和/或治疗感染或尿失禁。
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