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公开(公告)号：US08012971B2
公开(公告)日：2011-09-06
申请号：US11919135
申请日：2006-04-28
IPC分类号： A61K31/426 , A61K31/5377 , C07D417/10 , C07D277/38
CPC分类号： A61K31/56 , A61K9/10 , A61K31/5377 , C07D277/42
摘要： Disclosed is a method for the prevention and/or treatment of a chronic obstructive pulmonary disease by administrating a 5-membered cyclic compound represented by the formula below: or a pharmaceutically acceptable salt of the compound or a prodrug of the compound or salt: wherein X represents an oxygen or sulfur atom; R1 represents a hydrogen atom, a substituted or unsubstituted alkyl or the like; R2 represents a hydrogen atom, a substituted or unsubstituted alkyl or the like; Y1 represents single bond, a substituted or unsubstituted alkylene or the like; the wavy line means an (E) or (Z) coordination; R3 represents a hydrogen atom, a substituted or unsubstituted aryl or the like; Y2 represents a substituted or unsubstituted alkylene or an alkenylene; R4 represents a hydrogen atom, a substituted or unsubstituted alkanoyl or the like; and R5 represents a hydrogen atom or a substituted or unsubstituted alkyl.
摘要翻译： 本发明公开了一种预防和/或治疗慢性阻塞性肺疾病的方法，该方法是通过给予由下式表示的5元环状化合物：或化合物的药学上可接受的盐或其化合物或盐的前体药物：其中X 表示氧或硫原子; R1表示氢原子，取代或未取代的烷基等; R 2表示氢原子，取代或未取代的烷基等; Y1表示单键，取代或未取代的亚烷基等; 波浪线表示（E）或（Z）配位; R3表示氢原子，取代或未取代的芳基等; Y2表示取代或未取代的亚烷基或亚烯基; R4表示氢原子，取代或未取代的烷酰基等; 并且R 5表示氢原子或取代或未取代的烷基。
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公开(公告)号：US20090131439A1
公开(公告)日：2009-05-21
申请号：US11919135
申请日：2006-04-28
IPC分类号： A61K31/426 , A61K31/5377 , A61P11/00 , C07D417/10 , C07D277/38
CPC分类号： A61K31/56 , A61K9/10 , A61K31/5377 , C07D277/42
摘要： Disclosed is a method for the prevention and/or treatment of a chronic obstructive pulmonary disease by administrating a 5-membered cyclic compound represented by the formula below: or a pharmaceutically acceptable salt of the compound or a prodrug of the compound or salt: wherein X represents an oxygen or sulfur atom; R1 represents a hydrogen atom, a substituted or unsubstituted alkyl or the like; R2 represents a hydrogen atom, a substituted or unsubstituted alkyl or the like; Y1 represents single bond, a substituted or unsubstituted alkylene or the like; the wavy line means an (E) or (Z) coordination; R3 represents a hydrogen atom, a substituted or unsubstituted aryl or the like; Y2 represents a substituted or unsubstituted alkylene or an alkenylene; R4 represents a hydrogen atom, a substituted or unsubstituted alkanoyl or the like; and R5 represents a hydrogen atom or a substituted or unsubstituted alkyl.
摘要翻译： 本发明公开了一种预防和/或治疗慢性阻塞性肺疾病的方法，该方法是通过给予由下式表示的5元环状化合物：或化合物的药学上可接受的盐或其化合物或盐的前体药物：其中X 表示氧或硫原子; R1表示氢原子，取代或未取代的烷基等; R 2表示氢原子，取代或未取代的烷基等; Y1表示单键，取代或未取代的亚烷基等; 波浪线表示（E）或（Z）配位; R3表示氢原子，取代或未取代的芳基等; Y2表示取代或未取代的亚烷基或亚烯基; R4表示氢原子，取代或未取代的烷酰基等; 并且R 5表示氢原子或取代或未取代的烷基。
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公开(公告)号：US20110263550A1
公开(公告)日：2011-10-27
申请号：US13084503
申请日：2011-04-11
IPC分类号： A61K31/56 , A61P11/00 , A61K31/5377
CPC分类号： A61K31/56 , A61K9/10 , A61K31/5377 , C07D277/42
摘要： Disclosed is a method for the prevention and/or treatment of a chronic obstructive pulmonary disease by administrating a 5-membered cyclic compound represented by the formula below: or a pharmaceutically acceptable salt of the compound or a prodrug of the compound or salt: wherein X represents an oxygen or sulfur atom; R1 represents a hydrogen atom, a substituted or unsubstituted alkyl or the like; R2 represents a hydrogen atom, a substituted or unsubstituted alkyl or the like; Y1 represents single bond, a substituted or unsubstituted alkylene or the like; the wavy line means an (E) or (Z) coordination; R3 represents a hydrogen atom, a substituted or unsubstituted aryl or the like; Y2 represents a substituted or unsubstituted alkylene or an alkenylene; R4 represents a hydrogen atom, a substituted or unsubstituted alkanoyl or the like; and R5 represents a hydrogen atom or a substituted or unsubstituted alkyl.
摘要翻译： 本发明公开了一种预防和/或治疗慢性阻塞性肺疾病的方法，该方法是通过给予由下式表示的5元环状化合物：或化合物的药学上可接受的盐或其化合物或盐的前体药物：其中X 表示氧或硫原子; R1表示氢原子，取代或未取代的烷基等; R 2表示氢原子，取代或未取代的烷基等; Y1表示单键，取代或未取代的亚烷基等; 波浪线表示（E）或（Z）配位; R3表示氢原子，取代或未取代的芳基等; Y2表示取代或未取代的亚烷基或亚烯基; R4表示氢原子，取代或未取代的烷酰基等; 并且R 5表示氢原子或取代或未取代的烷基。
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公开(公告)号：US07396842B2
公开(公告)日：2008-07-08
申请号：US11111845
申请日：2005-04-22
IPC分类号： A61K31/44 , C07D417/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/42 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14
摘要： A 5-membered cyclic compound of the formula: wherein X is oxygen or sulfur, R1 is hydrogen, substituted or unsubstituted alkyl, etc., R2 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, etc., Y1 is a direct bond, substituted or unsubstituted alkylene, —CO(CH2)n—, etc., the wavy line means (E)-configuration or (Z)-configuration, R3 is substituted or unsubstituted aryl, etc., Y2 is substituted or unsubstituted alkylene, etc., R4 is hydrogen, substituted or unsubstituted alkanoyl, substituted or unsubstituted alkyl, etc., R5 is hydrogen, etc., or a salt thereof, these compound being able to inhibit infiltration of leukocytes such as eosinophils and lymphocytes, by which being useful for the treatment of various kinds of inflammation.
摘要翻译： 下式的5元环状化合物：其中X是氧或硫，R 1是氢，取代或未取代的烷基等，R 2是氢，被取代的 或未取代的烷基，取代或未取代的芳基等，Y 1是直接键，取代或未取代的亚烷基，-CO（CH 2）n， （E）构型或（Z）构型，R 3是取代或未取代的芳基等。Y 2 - 是取代或未取代的亚烷基等，R 4是氢，取代或未取代的烷酰基，取代或未取代的烷基等，R 5是氢等，或 其盐，这些化合物能够抑制白细胞如嗜酸性粒细胞和淋巴细胞的浸润，由此可用于治疗各种炎症。
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公开(公告)号：US20050222226A1
公开(公告)日：2005-10-06
申请号：US11111845
申请日：2005-04-22
IPC分类号： A61P29/00 , A61P37/06 , A61P37/08 , C07D277/42 , C07D277/56 , C07D417/04 , C07D417/12 , C07D417/14 , C07D521/00 , A61K31/426 , C07D277/38
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/42 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14
摘要： A 5-membered cyclic compound of the formula: wherein X is oxygen or sulfur, R1 is hydrogen, substituted or unsubstituted alkyl, etc., R2 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, etc., Y1 is a direct bond, substituted or unsubstituted alkylene, —CO(CH2)n—, etc., the wavy line means (E)-configuration or (Z)-configuration, R3 is substituted or unsubstituted aryl, etc., Y2 is substituted or unsubstituted alkylene, etc., R4 is hydrogen, substituted or unsubstituted alkanoyl, substituted or unsubstituted alkyl, etc., R5 is hydrogen, etc., or a salt thereof, these compound being able to inhibit infiltration of leukocytes such as eosinophils and lymphocytes, by which being useful for the treatment of various kinds of inflammation.
摘要翻译： 下式的5元环状化合物：其中X是氧或硫，R 1是氢，取代或未取代的烷基等，R 2是氢，被取代的 或未取代的烷基，取代或未取代的芳基等，Y 1是直接键，取代或未取代的亚烷基，-CO（CH 2）n， （E）构型或（Z）构型，R 3是取代或未取代的芳基等。Y 2 - 是取代或未取代的亚烷基等，R 4是氢，取代或未取代的烷酰基，取代或未取代的烷基等，R 5是氢等，或 其盐，这些化合物能够抑制白细胞如嗜酸性粒细胞和淋巴细胞的浸润，由此可用于治疗各种炎症。
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公开(公告)号：US06919361B2
公开(公告)日：2005-07-19
申请号：US10312692
申请日：2001-06-28
IPC分类号： A61P29/00 , A61P37/06 , A61P37/08 , C07D277/42 , C07D277/56 , C07D417/04 , C07D417/12 , C07D417/14 , C07D521/00 , A61K31/425 , C07P277/08
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/42 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14
摘要： A 5-membered cyclic compound of the formula: wherein X is oxygen or sulfur, R1 is hydrogen, substituted or unsubstituted alkyl, etc., R2 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, etc., Y1 is a direct bond, substituted or unsubstituted alkylene, —CO(CH2)n—, etc., the wavy line means (E)-configuration or (Z)-configuration, R3 is substituted or unsubstituted aryl, etc., Y2 is substituted or unsubstituted alkylene, etc., R4 is hydrogen, substituted or unsubstituted alkanoyl, substituted or unsubstituted alkyl, etc., R5 is hydrogen, etc., or a salt thereof, these compound being able to inhibit infiltration of leukocytes such as eosinophils and lymphocytes, by which being useful for the treatment of various kinds of inflammation.
摘要翻译： 下式的5元环状化合物：其中X是氧或硫，R 1是氢，取代或未取代的烷基等，R 2是氢，被取代的 或未取代的烷基，取代或未取代的芳基等，Y 1是直接键，取代或未取代的亚烷基，-CO（CH 2）n， （E）构型或（Z）构型，R 3是取代或未取代的芳基等。Y 2 - 是取代或未取代的亚烷基等，R 4是氢，取代或未取代的烷酰基，取代或未取代的烷基等，R 5是氢等，或 其盐，这些化合物能够抑制白细胞如嗜酸性粒细胞和淋巴细胞的浸润，由此可用于治疗各种炎症。
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公开(公告)号：US20110034466A1
公开(公告)日：2011-02-10
申请号：US12989516
申请日：2009-04-23
申请人： Hitoshi Fujita , Toshio Kanai , Satoki Imai
发明人： Hitoshi Fujita , Toshio Kanai , Satoki Imai
IPC分类号： A61K31/5377 , C07D413/10 , A61P29/00
CPC分类号： C07D277/20 , C07D277/42 , C07D417/10
摘要： Disclosed is a five-membered ring compound represented by formula (1) or a pharmaceutically acceptable salt thereof. The compound inhibits infiltration of leukocytes including eosinophils and lymphocytes, and is effective as a drug for treating various inflammations. The compound is highly safe and can be administered for a long period. A pharmaceutical product containing the five-membered ring compound or a pharmaceutically acceptable salt thereof is also disclosed. (In the formula, R1 represents a halogen atom or a phenyl group which may be substituted by a C1-C3 alkyl group or a C1-C3 alkoxy group; R2 represents a C1-C3 alkylene group which may be substituted by a C1-C3 alkyl group or a carbonyl group; R3 represents a C1-C3 alkyl group; R4 and R5 independently represent a hydrogen atom or a C1-C3 alkyl group, or —N(R4)R5 may represent a morpholino group which may be substituted by a C1-C3 alkyl group; Y2 represents a C2-C4 alkylene group; and R6 represents a hydrogen atom, a halogen atom, a C1-C3 alkyl group or a C1-C3 alkoxy group.)
摘要翻译： 公开了由式（1）表示的五元环化合物或其药学上可接受的盐。 该化合物抑制嗜酸性粒细胞和淋巴细胞等白细胞的浸润，作为治疗各种炎症的药物是有效的。 该化合物是高度安全的，可以长期施用。 还公开了含有五元环化合物或其药学上可接受的盐的药物。 （式中，R1表示卤原子或可被C1-C3烷基或C1-C3烷氧基取代的苯基; R2表示可被C1-C3取代的C1-C3亚烷基 烷基或羰基; R3表示C1-C3烷基; R4和R5独立地表示氢原子或C1-C3烷基，或-N（R4）R5可以表示可以被 C1-C3烷基; Y2表示C2-C4亚烷基; R6表示氢原子，卤素原子，C1-C3烷基或C1-C3烷氧基）。
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公开(公告)号：US06907095B1
公开(公告)日：2005-06-14
申请号：US09709203
申请日：2000-11-09
申请人： Fumio Nakano , Hitoshi Fujita
发明人： Fumio Nakano , Hitoshi Fujita
CPC分类号： H04L7/0012
摘要： A clock ride-over circuit in which clock ride-over may be achieved even if jitter is contained in clocks prior to and subsequent to ride-over and no control input signal for write and readout is applied from outside. A clock prior to rideover CLK—1 is detected by a clock subsequent to ride-over CLK—2 which is of a higher speed than the clock prior to ride-over. A timing signal TIM of a constant period, generated by a counter adapted for self-running with the clock prior to ride-over, is compared to the phase comparison signal COMP which is the result of the clock detection. Stable clock ride-over is possible by the phase comparison signal COMP having a pulse width larger than the jitter period of the clock subsequent to ride-over.
摘要翻译： 即使在骑乘之前和之后的时钟中包含抖动也可以实现时钟转换的时钟转换电路，并且不从外部施加用于写入和读出的控制输入信号。 Rideover之前的一个时钟CLK乘以一个比乘法之前的时钟更快的乘法器CLK-2之后的时钟来检测。 由适应于在乘坐之前的时钟自行运行的计数器产生的恒定周期的定时信号TIM与作为时钟检测结果的相位比较信号COMP进行比较。 可以通过相位比较信号COMP具有比乘坐后的时钟的抖动周期大的脉冲宽度的稳定的时钟跳变。
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公开(公告)号：US06458798B1
公开(公告)日：2002-10-01
申请号：US09763728
申请日：2001-02-27
申请人： Hitoshi Fujita , Fujio Antoku , Norio Fujiwara , Kiyotaka Iwai , Hiroshi Tanaka , Hajime Kawakami
发明人： Hitoshi Fujita , Fujio Antoku , Norio Fujiwara , Kiyotaka Iwai , Hiroshi Tanaka , Hajime Kawakami
IPC分类号： C07D23995
CPC分类号： C07D405/04 , C07D405/12 , C07D405/14
摘要： A pyrimidine derivative of the formula (1) or a salt thereof; has an inhibitory activity of production of Th2 type cytokines such as IL-4, IL-5, etc., and is useful as an therapeutic agent for allergic diseases, autoimmune diseases such as systemic lupus erythemathosus, etc., and acquired immunodeficiecy syndrome (AIDS) and so on.
摘要翻译： 式（1）的嘧啶衍生物或其盐具有产生Th2型细胞因子如IL-4，IL-5等的抑制活性，可用作过敏性疾病，自身免疫性疾病的治疗剂 如系统性红斑狼疮等，以及获得性免疫缺陷综合征（AIDS）等。
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公开(公告)号：US4975772A
公开(公告)日：1990-12-04
申请号：US346669
申请日：1989-05-03
申请人： Hitoshi Fujita
发明人： Hitoshi Fujita
CPC分类号： H04N5/217
摘要： The present invention relates to an image processing system for afterimage reduction for suitable use in a stereoscopic television apparatus. This system has been devised in consideration of the fact that the afterimage in a TV camera image to be displayed is most influenced by a frame image previous to the image to be displayed. The afterimage can be reduced by performing a novel algorism operation on each pixel value. Pixel values of a right image stored in a second input frame memory, which has been output from the TV camera prior to a left image to be displayed which is supplied from an input selector, is multiplied by a predetermined coefficient. The multiplied value is subtracted from pixel values of the left image to be displayed. Thus, a left image to be displayed, which has been subjected to afterimage reduction processing, is produced, and stored in a first output frame memory. Similarly, a right image to be displayed, which has been subjected to afterimage reduction processing, is produced.
摘要翻译： 本发明涉及一种用于立体电视设备中适用的余像减少的图像处理系统。 考虑到要显示的电视摄像机图像中的残像受到要显示的图像之前的帧图像的影响最大的事实，已经设计了该系统。 可以通过对每个像素值执行新颖的算法操作来减少残像。 将从输入选择器提供的要显示的左图像之前从TV摄像机输出的第二输入帧存储器中存储的右图像的像素值乘以预定系数。 从要显示的左图像的像素值中减去相乘值。 因此，产生已经进行了余像减少处理的待显示的左图像，并将其存储在第一输出帧存储器中。 类似地，产生已经进行了余像减少处理的要显示的右图像。
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