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41. 发明授权

US5519016A Aryl group- or aromatic heterocyclic group-substituted aminoquinolone derivatives and anti-HIV agent 失效
标题翻译：芳基或芳族杂环基取代的氨基喹诺酮衍生物和抗HIV剂
公开(公告)号：US5519016A
公开(公告)日：1996-05-21
申请号：US341295
申请日：1994-11-15
申请人： Tomio Kimura , Tetsushi Katsube
发明人： Tomio Kimura , Tetsushi Katsube
IPC分类号： C07D487/04 , A61K31/4375 , A61K31/47 , A61K31/535 , A61P31/18 , C07D215/56 , C07D401/04 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/06 , C07D487/14 , C07D498/06 , C07D513/04 , C07D513/06 , A61K31/495 , C07D215/227 , C07D215/233
CPC分类号： C07D215/56 , C07D401/04 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D471/06 , C07D513/04 , C07D513/06 , Y10S514/934
摘要： Disclosed are an aryl group- or heterocyclic group-substituted aminoquinolone compound represented by the formula (Ia), (Ib) or (Ic): ##STR1## wherein each of the substitutents are defined in the specification, or a salt of the compound, and an AIDS curing agent containing the same as an effective ingredient.
摘要翻译：公开了由式（Ia），（Ib）或（Ic）表示的芳基或杂环基取代的氨基喹诺酮化合物：（Ia）取代基在说明书中定义，或化合物的盐，和含有该有效成分的AIDS固化剂。

42. 发明授权

US5436367A Intermediates for certain 4-oxoquinoline-3-carboxylic acid derivatives 失效
标题翻译：某些4-氧代喹啉-3-羧酸衍生物的中间体
公开(公告)号：US5436367A
公开(公告)日：1995-07-25
申请号：US227678
申请日：1994-04-14
申请人： Masayuki Iwata , Tomio Kimura , Teruhiko Inoue , Yoshimi Fujihara , Tetsushi Katsube
发明人： Masayuki Iwata , Tomio Kimura , Teruhiko Inoue , Yoshimi Fujihara , Tetsushi Katsube
IPC分类号： C07D215/56 , C07D401/04 , C07D521/00 , C07C65/21
CPC分类号： C07D231/12 , C07D215/56 , C07D233/56 , C07D249/08 , C07D401/04 , Y02P20/55
摘要： Compounds of formula (I): ##STR1## (in which: R.sup.1 represents fluorinated methoxy; R.sup.2 represents a nitrogen-containing heterocyclic group and R.sup.3 represents hydrogen or amino) and pharmaceutically acceptable salts, esters and amides thereof are valuable antibacterial agents, which may be prepared by reacting a compound similar to that of formula (I) but in which R.sup.2 is replaced by a halogen atom with a compound providing the required group R.sup.2.
摘要翻译：式（I）的化合物：其中：R1表示氟化甲氧基; R2表示含氮杂环基，R3表示氢或氨基），其药学上可接受的盐，酯和酰胺是有价值的抗菌剂其可以通过使类似于式（I）的化合物与其中R 2被卤素原子替换的化合物与提供所需基团R2的化合物反应来制备。

43. 发明授权

US5436242A Tetrahydrothienopyridine derivatives, furo and pyrrolo analogs thereof for inhibiting blood platelet aggregation 失效
标题翻译：四氢噻吩并吡啶衍生物，呋喃和吡咯类似物用于抑制血小板聚集
公开(公告)号：US5436242A
公开(公告)日：1995-07-25
申请号：US161046
申请日：1993-12-01
申请人： Hiroyuki Koike , Fumitoshi Asai , Atsuhiro Sugidachi , Tomio Kimura , Teruhiko Inoue , Shigeyoshi Nishino , Yasunori Tsuzaki
发明人： Hiroyuki Koike , Fumitoshi Asai , Atsuhiro Sugidachi , Tomio Kimura , Teruhiko Inoue , Shigeyoshi Nishino , Yasunori Tsuzaki
IPC分类号： A61K31/435 , A61K31/135 , A61K31/365 , A61K31/4365 , A61P7/02 , C07D221/00 , C07D333/00 , C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04 , A61K31/535 , C07D273/01
CPC分类号： C07D471/04 , C07D491/04 , C07D495/04
摘要： Compounds of formula (I): ##STR1## wherein R.sup.1 is hydrogen, alkyl, halogen, haloalkyl, hydroxy, alkoxy, haloalkoxy, alkylthio, haloalkylthio, amino, alkanoyl, haloalkanoyl, carboxy, alkoxycarbonyl, carbamoyl, cyano, nitro, alkanesulfonyl, haloalkanesulfonyl or sulfamoyl; R.sup.2 is 5,6-dihydro-1,4,2-dioxazin-3-yl; R.sup.3 is hydrogen, hydroxy, optionally substituted alkoxy, aralkyloxy, alkanoyloxy, alkenoyloxy, cycloalkylcarbonyloxy, arylcarbonyloxy, alkoxycarbonyloxy, aralkyloxycarbonylxy, phthalidyloxy, (5-methyl-2-oxo-1,3-dioxolen-4-yl)methoxy, (5-phenyl-2-oxo-1,3-dioxolen-4-yl)methoxy, optionally substituted amino or nitro; Y is --NH-- or oxygen or sulfur; n is 1 to 5; and tautomers and salts of said compounds of formula (I), have the ability to inhibit blood platelet aggregation, and can thus be used for treatment and prophylaxis of thrombosis and embolisms.
摘要翻译：式（I）化合物：其中R1是氢，烷基，卤素，卤代烷基，羟基，烷氧基，卤代烷氧基，烷硫基，卤代烷硫基，氨基，烷酰基，卤代烷酰基，羧基，烷氧基羰基，氨基甲酰基，氰基，硝基，烷磺酰基，卤代烷磺酰基或氨磺酰基; R 2是5,6-二氢-1,4,2-二恶嗪-3-基; R3是氢，羟基，任选取代的烷氧基，芳烷氧基，烷酰氧基，烯酰基氧基，环烷基羰基氧基，芳基羰基氧基，烷氧基羰基氧基，芳烷氧基羰基氧基，邻苯二甲酰氧基，（5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基）甲氧基，（5- 苯基-2-氧代-1,3-二氧杂环戊烯-4-基）甲氧基，任选取代的氨基或硝基; Y是-NH-或氧或硫; n为1至5; 和所述式（I）化合物的互变异构体和盐具有抑制血小板聚集的能力，因此可用于治疗和预防血栓形成和栓塞。

44. 发明授权

US5288726A Tetrahydrothienopyridine derivatives, furo and pyrrolo analogs thereof and their preparation and uses for inhibiting blood platelet aggregation 失效
标题翻译：四氢噻吩并吡啶衍生物，呋喃和吡咯类似物及其制备和用途，用于抑制血小板聚集
公开(公告)号：US5288726A
公开(公告)日：1994-02-22
申请号：US941676
申请日：1992-09-08
申请人： Hiroyuki Koike , Fumitoshi Asai , Atsuhiro Sugidachi , Tomio Kimura , Teruhiko Inoue , Shigeyoshi Nishino , Yasunori Tsuzaki
发明人： Hiroyuki Koike , Fumitoshi Asai , Atsuhiro Sugidachi , Tomio Kimura , Teruhiko Inoue , Shigeyoshi Nishino , Yasunori Tsuzaki
IPC分类号： A61K31/435 , A61K31/135 , A61K31/365 , A61K31/4365 , A61P7/02 , C07D221/00 , C07D333/00 , C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04 , A01K3/14 , C07D513/04
CPC分类号： C07D471/04 , C07D491/04 , C07D495/04
摘要： Compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen, alkyl, halogen, haloalkyl, hydroxy, alkoxy, haloalkoxy, alkylthio, haloalkylthio, amino, alkanoyl, haloalkanoyl, carboxy, alkoxycarbonyl, carbamoyl, cyano, nitro, alkanesulfonyl, haloalkanesulfonyl or sulfamoyl; R.sup.2 is optionally substituted alkanoyl, optionally substituted alkenoyl, optionally substituted cycloalkylcarbonyl, substituted benzoyl, or 5,6-dihydro-1,4,2-dioxazin-3-yl; R.sup.3 is hydrogen, hydroxy, optionally substituted alkoxy, aralkyloxy, alkanoyloxy, alkenoyloxy, cycloalkylcarbonyloxy, arylcarbonyloxy, alkoxycarbonyloxy, aralkyloxycarbonylxy, phthalidyloxy, (5-methyl-2-oxo-1,3-dioxolen-4-yl)methoxy, (5-phenyl-2-oxo-1,3-dioxolen-4-yl)methoxy, optionally substituted amino or nitro; Y is --NH-- or oxygen or sulfur; n is 1 to 5; and tautomers and salts of said compounds of formula (I), have the ability to inhibit blood platelet aggregation, and can thus be used for treatment and prophylaxis of thrombosis and embolisms.
摘要翻译：式（I）化合物：（*化学结构*）（I）其中：R1是氢，烷基，卤素，卤代烷基，羟基，烷氧基，卤代烷氧基，烷硫基，卤代烷硫基，氨基，烷酰基，卤代烷酰基，羧基，烷氧基羰基，氨基甲酰基，氰基，硝基，烷磺酰基，卤代烷磺酰基或氨磺酰基; R 2是任选取代的烷酰基，任选取代的烯酰基，任选取代的环烷基羰基，取代的苯甲酰基或5,6-二氢-1,4,2-二恶嗪-3-基; R3是氢，羟基，任选取代的烷氧基，芳烷氧基，烷酰氧基，烯酰氧基，环烷基羰基氧基，芳基羰基氧基，烷氧基羰基氧基，芳烷氧基羰基氧基，邻苯二甲酰氧基，（5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基）甲氧基，（5- 苯基-2-氧代-1,3-二氧杂环戊烯-4-基）甲氧基，任选取代的氨基或硝基; Y是-NH-或氧或硫; n为1至5; 和所述式（I）化合物的互变异构体和盐具有抑制血小板聚集的能力，因此可用于治疗和预防血栓形成和栓塞。

45. 发明授权

US4443548A Process for preparing L-.alpha.-methylphenyl alanines 失效
标题翻译：制备L-α-甲基苯基丙氨酸的方法
公开(公告)号：US4443548A
公开(公告)日：1984-04-17
申请号：US376236
申请日：1982-05-07
申请人： Tokio Oshima , Tomio Kimura , Tetsuo Omata , Noritada Iwamoto
发明人： Tokio Oshima , Tomio Kimura , Tetsuo Omata , Noritada Iwamoto
IPC分类号： C12P13/02 , C12N9/80 , C12P13/04 , C12P41/00 , C12R1/01 , C12R1/06 , C12R1/07 , C12R1/32 , C12R1/365 , C12R1/38 , C12R1/465 , C12R1/645 , C12R1/72 , C12R1/78 , C12R1/845 , C12R1/88 , C12R1/885 , C07B19/02 , C12P13/22
CPC分类号： C12P13/04 , C12N9/80
摘要： Biochemical optical resolution of DL-.alpha.-methylphenyl alanines in which DL-.alpha.-methylphenyl alanine amides are interacted with the culture products, or their treated products, of a microorganism capable of producing amidase is described. L-.alpha.-methylphenyl alanines having the general formula (I): ##STR1## wherein R.sub.1 and R.sub.2 may be independently a hydrogen atom or lower alkyl groups, or R.sub.1 and R.sub.2 may be alkylene groups combined together to form 5 through 8-membered rings is produced by the steps of:(a) making a DL-.alpha.-methylphenyl alanine amide having the general formula (II): ##STR2## wherein R.sub.1 and R.sub.2 are the same as defined above, interact with the culture product of a microorganism capable of producing enzyme catalyzing the hydrolysis of L-isomer of DL-.alpha.-methylphenyl alanine amides or the treated product thereof, whereby asymmetric hydrolysis of an L-.alpha.-methylphenyl alanine amide is effected; and(b) separating the resultant L-.alpha.-methylphenyl alanines from the hydrolysis mixture.
摘要翻译：描述了DL-α-甲基苯丙氨酰胺与能够产生酰胺酶的微生物或其处理产物相互作用的DL-α-甲基苯基丙氨酸的生物化学光学拆分。具有通式（I）的L-α-甲基苯基丙氨酸：其中R 1和R 2可以独立地为氢原子或低级烷基，或者R 1和R 2可以是亚烷基结合在一起形成5至8个通过以下步骤制备环状环：（a）制备具有通式（II）的DL-α-甲基苯基丙氨酸酰胺：其中R 1和R 2与上述定义相同，与能够产生催化DL-α-甲基苯丙氨酸酰胺的L-异构体或其处理产物的水解的酶的微生物的培养产物，从而实现了L-α-甲基苯丙氨酸酰胺的不对称水解; 和（b）从水解混合物中分离所得的L-α-甲基苯基丙氨酸。

46. 发明申请

US20120220593A1 Substituted Acrylamide Derivative and Pharmaceutical Composition Comprising the Same 失效
标题翻译：取代的丙烯酰胺衍生物和药物组合物
公开(公告)号：US20120220593A1
公开(公告)日：2012-08-30
申请号：US13404647
申请日：2012-02-24
申请人： Kazumasa Aoki , Koji Suda , Toshio Kaneko , Tomio Kimura
发明人： Kazumasa Aoki , Koji Suda , Toshio Kaneko , Tomio Kimura
IPC分类号： A61K31/166 , C07D207/327 , A61K31/402 , A61P19/10 , A61K31/5375 , A61P19/00 , A61P3/00 , C07C233/87 , C07D295/15
CPC分类号： A61K31/166 , C07C237/22 , C07C2601/02 , C07C2601/04 , C07C2601/10 , C07C2602/08 , C07D207/327 , C07D277/30 , C07D295/13 , C07D307/54 , C07D317/54 , C07D333/16 , C07D407/04 , C07D409/04 , Y02P20/55
摘要： A pharmaceutical composition comprising a compound having Formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein, R1 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group α; R2 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group α; and X is, for example, a hydroxyl group or a C1-C6 alkoxy group].
摘要翻译：一种药物组合物，其包含具有式（I）的化合物或其药理学上可接受的盐作为活性成分：[其中，R 1为例如可以被一个或多于一个基团取代的C 6 -C 10芳基来自取代基组α; R2是例如可以被一个或多个选自取代基组α的一个基团取代的C 6 -C 10芳基; X是例如羟基或C1-C6烷氧基]。

47. 发明授权

US08143446B2 Substituted acrylamide derivative and pharmaceutical composition comprising the same 有权
标题翻译：取代的丙烯酰胺衍生物和包含它们的药物组合物
公开(公告)号：US08143446B2
公开(公告)日：2012-03-27
申请号：US11914209
申请日：2006-05-11
申请人： Kazumasa Aoki , Koji Suda , Toshio Kaneko , Tomio Kimura
发明人： Kazumasa Aoki , Koji Suda , Toshio Kaneko , Tomio Kimura
IPC分类号： C07C235/30 , C07C235/42 , A61K31/16
CPC分类号： A61K31/166 , C07C237/22 , C07C2601/02 , C07C2601/04 , C07C2601/10 , C07C2602/08 , C07D207/327 , C07D277/30 , C07D295/13 , C07D307/54 , C07D317/54 , C07D333/16 , C07D407/04 , C07D409/04 , Y02P20/55
摘要： A pharmaceutical composition comprising a compound having Formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein, R1 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group α; R2 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group α; and X is, for example, a hydroxyl group or a C1-C6 alkoxy group].
摘要翻译：一种药物组合物，其包含具有式（I）的化合物或其药理学上可接受的盐作为活性成分：[其中，R 1为例如可以被一个或多于一个基团取代的C 6 -C 10芳基来自取代基组α; R2是例如可以被一个或多个选自取代基组α的一个基团取代的C 6 -C 10芳基; X是例如羟基或C1-C6烷氧基]。

48. 发明授权

US07935835B2 Substituted cycloalkene derivative 有权
标题翻译：取代的环烯烃衍生物
公开(公告)号：US07935835B2
公开(公告)日：2011-05-03
申请号：US12066813
申请日：2006-09-13
申请人： Tomio Kimura , Nobuyuki Ohkawa , Takayoshi Nagasaki , Atsuhiro Sugidachi , Osamu Ando
发明人： Tomio Kimura , Nobuyuki Ohkawa , Takayoshi Nagasaki , Atsuhiro Sugidachi , Osamu Ando
IPC分类号： C07D319/00 , C07D315/00 , C07D327/00
CPC分类号： C07C311/14 , C07C2601/16 , C07C2602/50 , C07D303/38 , C07D307/94 , C07D317/72 , C07D319/08 , C07D321/10 , C07D327/04 , C07D339/06 , C07D339/08 , C07D493/04 , C07D493/10
摘要： A compound of formula (I) Wherein X, Y, ring A, ring B, l, m, R1, R2, R4 and R5 are as defined herein, to supress intracellular signal transduction or cell activation induced by endotoxin and to suppress cell responses due to the intracellular signal transduction and cell activation such as an excess generation of inflammatory mediators such as TNF-α, pharmacologically acceptable salts therefor, a preparation method therefor, and a medicament containing the aforementioned substituted cycloalkene derivative as an active ingredient which is superior in prophylaxis and/or treatment of diseases such as sepsis (septic shock, disseminated intravascular coagulation, multiple organ failure and the like), that are associated with intracellular signal transduction or cell activation induced by endotoxin and to cell responses to the intracellular signal transduction and cell activation.
摘要翻译：式（I）化合物其中X，Y，环A，环B，l，m，R 1，R 2，R 4和R 5如本文所定义，以抑制由内毒素诱导的细胞内信号转导或细胞活化并抑制细胞反应由于细胞内信号转导和细胞活化，例如过量产生炎症介质如TNF-α，其药理学上可接受的盐，其制备方法，以及含有上述取代的环烯烃衍生物作为活性成分的药物，其优于与细胞内信号转导或由内毒素诱导的细胞活化以及对细胞内信号转导和细胞的细胞反应相关的诸如败血症（败血症休克，弥散性血管内凝血，多器官功能衰竭等）的疾病的预防和/或治疗激活。

49. 发明申请

US20100211267A1 PARKING ASSISTANCE APPARATUS, VEHICLE-SIDE APPARATUS OF PARKING ASSISTANCE APPARATUS, PARKING ASSIST METHOD, AND PARKING ASSIST PROGRAM 失效
标题翻译：停车辅助装置，停车辅助装置的车辆装置，停车辅助方法和停车辅助程序
公开(公告)号：US20100211267A1
公开(公告)日：2010-08-19
申请号：US12670713
申请日：2008-07-04
申请人： Kazunori Shimazaki , Tomio Kimura , Yutaka Nakashima , Masami Tomioka , Hideo Yanagisawa
发明人： Kazunori Shimazaki , Tomio Kimura , Yutaka Nakashima , Masami Tomioka , Hideo Yanagisawa
IPC分类号： B62D6/00 , B62D15/02 , B60Q1/48
CPC分类号： G08G1/168 , B60R1/00 , B60R2300/108 , B60R2300/302 , B60R2300/50 , B60R2300/70 , B60R2300/8026 , B60R2300/806 , B60W30/095 , B60W40/02 , B60W2420/403 , B62D15/028
摘要： A parking assistance apparatus makes it easy for a driver to grasp a relative positional relation between a vehicle and a target parking position and makes it possible to park the vehicle at the target parking position in a parking space with accuracy.An image of a mark M in a parking space S is taken by a vehicle-side camera 7. A relative position calculation portion 8 calculates a relative positional relation between the vehicle and a target parking position T based on the taken image of the mark M. A backward locus calculation portion 9 calculates an expected locus when the vehicle moves based on the relative positional relation and based on a steering angle detected by a steering angle sensor 15. An image of the parking space S is taken by a parking-space-side camera 3 and transmitted to a vehicle-side apparatus 1. An image composition portion 12 composes the image of the parking space S from the parking-space-side camera 3 and the expected locus calculated by the backward locus calculation portion 9. The composed image is displayed on the monitor 14 located in the vicinity of a drivers seat of the vehicle.
摘要翻译：停车辅助装置使驾驶员容易掌握车辆与目标停车位置之间的相对位置关系，并且能够准确地将车辆停放在停车位置的目标停车位置。停车空间S中的标记M的图像由车辆侧照相机7拍摄。相对位置计算部8基于拍摄到的标记M的图像计算车辆与目标停车位置T之间的相对位置关系反向轨迹计算部9基于相对位置关系，基于由转向角传感器15检测到的转向角来计算车辆移动时的预期轨迹。停车位S的图像由停车位 - 图像合成部12从停车位侧摄像机3构成停车空间S的图像，由向后轨迹计算部9计算出的预期轨迹构成。图像显示在位于车辆驾驶员座位附近的监视器14上。

50. 发明申请

US20100066515A1 PARKING ASSISTANCE APPARATUS, PARKING ASSISTANCE APPARATUS PART, PARKING ASSIST METHOD, PARKING ASSIST PROGRAM, VEHICLE TRAVEL PARAMETER CALCULATION METHOD, VEHICLE TRAVEL PARAMETER CALCULATION PROGRAM, VEHICLE TRAVEL PARAMETER CALCULATION APPARATUS AND VEHICLE TRAVEL PARAMETER CALCULATION APPARATUS PART 审中-公开
标题翻译：停车辅助装置，停车辅助装置部件，停车辅助方法，停车辅助程序，车辆行驶参数计算方法，车辆行驶参数计算程序，车辆行驶参数计算装置和车辆行驶参数计算装置
公开(公告)号：US20100066515A1
公开(公告)日：2010-03-18
申请号：US12521101
申请日：2007-11-19
申请人： Kazunori Shimazaki , Tomio Kimura , Masami Tomioka , Yutaka Nakashima , Hideo Yanagisawa
发明人： Kazunori Shimazaki , Tomio Kimura , Masami Tomioka , Yutaka Nakashima , Hideo Yanagisawa
IPC分类号： B60Q1/00 , B62D6/00
CPC分类号： B62D15/028 , B60W50/14 , G06T7/73 , G06T2207/30204 , G06T2207/30244 , G06T2207/30248 , H04N7/18
摘要： An image of a mark M is taken by a camera (1) with positioning a vehicle at a location in the vicinity of a parking space, an image processing unit (2) extracts a characteristic point from the image of the mark M and recognizes two-dimensional coordinates on the image, a positional parameter calculation unit (3) calculates positional parameters including six parameters of the camera (1) with reference to the mark M, and a relative position identification unit (4) identifies a relative positional relation between the vehicle and the parking space. A parking locus calculation unit (5) calculates a parking locus for leading the vehicle to the parking space based on the relative positional relation between the vehicle and the parking space identified by the relative position identification unit (4), and a guide apparatus (6) outputs drive operation guide information for causing the vehicle to travel along the calculated parking locus to a driver of the vehicle.
摘要翻译：图像处理单元（2）从标记M的图像中提取特征点，并识别两个图像上的三维坐标，位置参数计算单元（3）参照标记M计算包括照相机（1）的六个参数的位置参数，相对位置识别单元（4）识别相机车辆和停车位。停车轨迹计算单元（5）基于由相对位置识别单元（4）识别的车辆与停车空间之间的相对位置关系，计算用于将车辆引导到停车位的停车轨迹，以及引导装置（6））输出用于使车辆沿着计算出的停车轨迹行进到车辆驾驶员的驾驶操作指导信息。

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