公开(公告)号：US4029780A

公开(公告)日：1977-06-14

申请号：US626042

申请日：1975-10-28

申请人： Haruki Nishimura ,  Masanao Shimizu ,  Naonobu Hatano ,  Katsuyoshi Nakatsuzi ,  Hiroaki Kinugasa ,  Hiroko Kon

发明人： Haruki Nishimura ,  Masanao Shimizu ,  Naonobu Hatano ,  Katsuyoshi Nakatsuzi ,  Hiroaki Kinugasa ,  Hiroko Kon

IPC分类号： C07D417/04 ,  C07D285/24 ,  A61K31/54

CPC分类号： C07D417/04

摘要： A compound of the formula ##STR1## wherein R.sub.1 represents a hydrogen atom or a lower alkyl group, and R.sub.2 represents a hydrogen or halogen atom or a trifluoromethyl group,And its pharmaceutically acceptable salt. The compound is prepared by reacting the corresponding 1,2,4-benzothiadiazine 1,1-dioxide with a piperazine compound or alkylating 1,2,4-benzothiadiazine 1,1-dioxide whose corresponding 3-position is substituted by a piperazinyl group. The above compound has superior antihypertensive activity separated from diuretic, antidiuretic and hyperglycemic activities, and is free from side-effects.

摘要翻译： 式IMA的化合物，其中R 1表示氢原子或低级烷基，R 2表示氢或卤素原子或三氟甲基，以及其药学上可接受的盐。 该化合物通过相应的1,2,4-苯并噻二嗪1,1-二氧化物与相应的3-位被哌嗪基取代的哌嗪化合物或烷基化的1,2,4-苯并噻二嗪1,1-二氧化物反应来制备。 上述化合物具有从利尿，抗利尿和高血糖活性中分离的优异的抗高血压活性，并且没有副作用。

公开(公告)号：US4248883A

公开(公告)日：1981-02-03

申请号：US53206

申请日：1979-06-29

申请人： Tadahiro Sawayama ,  Hiroaki Kinugasa ,  Haruki Nishimura ,  Kunihiko Takeyama ,  Kanoo Hosoki

发明人： Tadahiro Sawayama ,  Hiroaki Kinugasa ,  Haruki Nishimura ,  Kunihiko Takeyama ,  Kanoo Hosoki

IPC分类号： A61K31/40 ,  A61P43/00 ,  C07D207/10 ,  C07D207/16 ,  C07K5/06 ,  C07K5/078 ,  C07K14/81 ,  C07D207/09

CPC分类号： C07K5/06165 ,  C07C327/00 ,  C07D207/16

摘要： 1-(3-Mercapto-2-methylpropanoyl)prolyl amino acid derivatives of the formula ##STR1## wherein R represents a hydrogen atom, a lower alkyl group, a phenyl-lower alkyl group or a substituted phenyl-lower alkyl group, R.sub.1 represents a hydrogen atom, R.sub.4 CO--, R.sub.5 S--, or ##STR2## R.sub.2 represents a hydrogen atom or a lower alkyl group, R.sub.3 represents a hydrogen atom, a phenyl group, a lower alkyl group, or a substituted lower alkyl group, or R.sub.2 and R.sub.3 form a heterocyclic ring together with the nitrogen and carbon atoms to which they are respectively bonded; salts of these compounds; compositions comprising these compounds or salts; and processes for preparing these compounds or salts. These compounds and salts have excellent antihypertensive activity.

摘要翻译： 式（I）的1-（3-巯基-2-甲基丙酰基）脯氨酰氨基酸衍生物，其中R表示氢原子，低级烷基，苯基 - 低级烷基或取代的苯基 - 低级烷基，R 1表示 氢原子，R4CO-，R5S-或R2表示氢原子或低级烷基，R3表示氢原子，苯基，低级烷基或取代的低级烷基，或R2和 R3与它们分别键合的氮和碳原子一起形成杂环; 这些化合物的盐; 包含这些化合物或盐的组合物; 以及制备这些化合物或盐的方法。 这些化合物和盐具有优异的抗高血压活性。

公开(公告)号：US3948928A

公开(公告)日：1976-04-06

申请号：US340195

申请日：1973-03-12

申请人： Haruki Nishimura ,  Masanao Shimizu ,  Hitoshi Uno ,  Tetsuo Hirooka ,  Yoshinobu Masuda ,  Mikio Kurokawa

发明人： Haruki Nishimura ,  Masanao Shimizu ,  Hitoshi Uno ,  Tetsuo Hirooka ,  Yoshinobu Masuda ,  Mikio Kurokawa

IPC分类号： A61K31/42 ,  C07D261/20

CPC分类号： A61K31/42 ,  C07D261/20

摘要： 3-Substituted-1,2-benzisoxazole derivative of the following formula: ##SPC1##Wherein R.sub.1 is hydrogen, hydroxy, nitro, alkyl, alkoxy, halogen or amino; R.sub.2 is hydroxyamino, amino, hydrazino, mono- or di- alkyl substituted amino, aralkylamino, acyloxyamino, morpholino, piperazine which is unsubstituted or substituted with alkyl, aralkyl or aryl at 4 position, or pyrrolidino, or R.sub.2 may combine with imino group and form together with the adjacent carbon atom a heterocyclic ring such as imidazoline or tetrahydropyrimidine; and n is an integer of 0 to 3, and its pharmaceutically acceptable acid addition salt, and preparation thereof. The present compounds show valuable pharmacological properties, such as anti-reserpine activity, central nervous depressing activity, anti-hypertensive activity and l-dopa potentiating activity.

摘要翻译： 3-取代的1,2-苯并异恶唑衍生物：

公开(公告)号：US4080453A

公开(公告)日：1978-03-21

申请号：US663158

申请日：1976-03-02

申请人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

发明人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

IPC分类号： C07D295/02 ,  C07D295/03 ,  C07D295/096 ,  C07D295/14 ,  A61K31/495

CPC分类号： C07D295/03 ,  C07D295/096

摘要： 1-Substituted-4-(1,2-diphenylethyl)piperazine derivatives of the formula: ##STR1## wherein X is 2- or 3-hydroxy, 2-methoxy, 3-methyl, 3-alkoxy having 1 to 4 carbon atoms, or 2- or 3-alkanoyloxy having 2 to 5 carbon atoms; R is allyl, 3-hydroxyisoamyl, 3-methyl-2-butenyl, 3-methyl-3-butenyl, propyl, an unsubstituted monocycloalkyl having 5 to 8 carbon atoms, 2-chlorophenyl, or a phenyl substituted by hydroxy or methoxy; with proviso that when X is a substituent at position 2, R is cyclohexyl and when X is 3-methyl, R is 2-methoxyphenyl or an unsubstituted monocycloalkyl having 6 to 8 carbon atoms, and their pharmaceutically acceptable salts, and the preparation thereof, and analgesic or antitussive compositions containing the same as the essentially active ingredient.

摘要翻译： 1-取代的4-（1,2-二苯基乙基）哌嗪衍生物，其结构式如下：其中X是2-或3-羟基，2-甲氧基，3-甲基，具有1至4个碳原子的3-烷氧基， 或具有2至5个碳原子的2-或3-烷酰氧基; R是烯丙基，3-羟基异戊基，3-甲基-2-丁烯基，3-甲基-3-丁烯基，丙基，未取代的具有5-8个碳原子的单环烷基，2-氯苯基或被羟基或甲氧基取代的苯基; 条件是当X是位置2的取代基时，R是环己基，当X是3-甲基时，R是2-甲氧基苯基或未取代的具有6-8个碳原子的单环烷基及其药学上可接受的盐及其制备方法， 以及含有与基本上活性成分相同的镇痛或镇咳药物。

公开(公告)号：US4162316A

公开(公告)日：1979-07-24

申请号：US821918

申请日：1977-08-04

申请人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

发明人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

IPC分类号： C07D295/02 ,  C07D295/03 ,  C07D295/096 ,  C07D241/04 ,  A61K31/495

CPC分类号： C07D295/03 ,  C07D295/096

摘要： 1-Substituted-4-(1,2-diphenylethyl)piperazine derivatives of the formula: ##STR1## wherein X is 2- or 3-hydroxy, 2-methoxy, 3-methyl, 3-alkoxy having 1 to 4 carbon atoms, or 2- or 3-alkanoyloxy having 2 to 5 carbon atoms; R is allyl, 3-hydroxyisoamyl, 3-methyl-2-butenyl, 3-methyl-3-butenyl, propyl, an unsubstituted monocycloalkyl having 5 to 8 carbon atoms, 2-chlorophenyl, or a phenyl substituted by hydroxy or methoxy; with proviso that when X is a substituent at position 2, R is cyclohexyl and when X is 3-methyl, R is 2-methoxyphenyl or an unsubstituted monocycloalkyl having 6 to 8 carbon atoms, and their pharmaceutically acceptable salts, and the preparation thereof, and analgesic or antitussive compositions containing the same as the essentially active ingredient.

公开(公告)号：US3988456A

公开(公告)日：1976-10-26

申请号：US561336

申请日：1975-03-24

申请人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

发明人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

IPC分类号： C07D295/08 ,  A61K31/495 ,  A61P9/12 ,  A61P11/14 ,  A61P25/00 ,  A61P25/04 ,  C07D213/74 ,  C07D295/084 ,  C07D295/10

CPC分类号： C07D295/092 ,  Y10S514/849

摘要： 1,2-Diphenylethanolamine derivatives of the formula: ##SPC1##Wherein R.sub.1 and R.sub.2 are each hydrogen, a halogen, nitro, hydroxy, an alkyl or methoxy; R.sub.3 is a group of the formula: ##SPC2##Wherein R.sub.4, R.sub.5 and R.sub.6 are each hydrogen, a halogen or methoxy and n is an integer of 0 to 3, or a pyridyl; and Z is hydroxy or an acyloxy; with proviso that when R.sub.1 and/or R.sub.2 are hydroxy, Z is hydroxy, and their pharmaceutically acceptable salts, which have excellent analgesic and anti-tussive activities, and a process for the preparation thereof.

摘要翻译： 下式的1,2-二苯乙醇胺衍生物：

公开(公告)号：US3957788A

公开(公告)日：1976-05-18

申请号：US541351

申请日：1975-01-15

申请人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

发明人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

IPC分类号： C07D295/02 ,  C07D295/03 ,  C07D295/096 ,  C07D295/145 ,  C07D295/08

CPC分类号： C07D295/03 ,  C07D295/096 ,  C07D295/145 ,  Y10S514/849

摘要： 1-Substituted-4-(1,2-diphenylethyl)piperazine derivatives of the formula: ##SPC1##Wherein X is hydroxy, methoxy, methyl or trifluoromethyl; and R is an unsubstituted monocycloalkyl group having 6 to 8 carbon atoms or 2-methoxyphenyl; provided that when X is hydroxy, R is cyclohexyl, and when X is trifluoromethyl, R is 2-methoxyphenyl,And their pharmaceutically acceptable salts, which have excellent analgesic, anti-tussive and anti-inflammatory activities, without undesirable side effect such as narcotic activity, and a process for the preparation thereof.

公开(公告)号：US4447439A

公开(公告)日：1984-05-08

申请号：US411515

申请日：1982-08-25

申请人： Haruki Nishimura ,  Shunsuke Naruto ,  Hiroyuki Mizuta ,  Toshiaki Kadokawa ,  Katsuyoshi Kawashima

发明人： Haruki Nishimura ,  Shunsuke Naruto ,  Hiroyuki Mizuta ,  Toshiaki Kadokawa ,  Katsuyoshi Kawashima

IPC分类号： B60G11/26 ,  C07D261/20 ,  A61K31/42 ,  A61K31/423 ,  B60G11/56 ,  B60G17/015 ,  B62D53/06 ,  B62D53/08 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14

CPC分类号： C07D413/12 ,  C07D413/14

摘要： Novel 2-cyclic amino-2-(1,2-benzisoxazol-3-yl)acetic acid derivatives of the formula: ##STR1## wherein R.sub.1 is hydrogen or a halogen atom, R.sub.2 is a lower alkyl group, Am is a 5- to 9-membered saturated cyclic amino group which may be substituted by a lower alkyl group, and the group: ##STR2## binds to the piperidine moiety at 3- or 4-position of the latter, and their pharmaceutically acceptable acid addition salts and quaternary ammonium salts, process for their preparation, and pharmaceutical compositions containing these compounds. They have potent anticholinergic antispasmodic activity, while they are weak in side effects such as mydriasis, inhibition of salivary secretion and tachycardia.

摘要翻译： 新的2-环氨基-2-（1,2-苯并异恶唑-3-基）乙酸衍生物，其分子式如下：其中R1是氢或卤素原子，R2是低级烷基，Am是 可以被低级烷基取代的5-至9-元饱和环状氨基，并且下列基团与后者的3-或4-位上的哌啶部分结合，并且其药学上可接受的酸加成 盐和季铵盐，其制备方法和含有这些化合物的药物组合物。 它们具有有效的抗胆碱能抗痉挛活性，而副作用较弱，如散瞳，抑制唾液分泌和心动过速。

公开(公告)号：US20100025140A1

公开(公告)日：2010-02-04

申请号：US12507070

申请日：2009-07-22

申请人： Hiroshi TAKENAKA ,  Akira Kato ,  Haruki Nishimura

发明人： Hiroshi TAKENAKA ,  Akira Kato ,  Haruki Nishimura

IPC分类号： B62K11/14 ,  B62K21/16

CPC分类号： B62K11/14 ,  B62K21/04 ,  Y10T74/2078 ,  Y10T74/20804

摘要： A steering system for a motorcycle includes a head pipe, a steering stem, a top bridge, a bottom bridge, a front fork, and a steering handlebar. The steering stem is supported by the head pipe. The top bridge has a center portion, a side portion extending from the center portion, and a holding portion provided at the side portion. The top bridge is supported by the steering stem at the center portion to steerably move around the head pipe. The bottom bridge is supported by the steering stem to steerably move around the head pipe. The front fork is held by the top bridge through the holding porting and is held by the bottom bridge. The top bridge has a protruding portion provided on an upper face of the top bridge and extending from the holding portion toward the center portion of the top bridge.

摘要翻译： 用于摩托车的转向系统包括头管，转向杆，顶桥，底桥，前叉和转向车把。 转向杆由头管支撑。 顶桥具有中心部分，从中心部分延伸的侧部分和设置在侧部的保持部分。 顶桥由中心部分的转向杆支撑，以可操纵地围绕头管移动。 底部桥梁由转向杆​​支撑以可控地围绕头部管道移动。 前叉由顶桥通过保持口固定，并由底桥保持。 顶桥具有设置在顶桥的上表面上并从保持部向顶桥的中心部延伸的突出部。

公开(公告)号：US07798511B2

公开(公告)日：2010-09-21

申请号：US12507070

申请日：2009-07-22

申请人： Hiroshi Takenaka ,  Akira Kato ,  Haruki Nishimura

发明人： Hiroshi Takenaka ,  Akira Kato ,  Haruki Nishimura

IPC分类号： B62K21/04

CPC分类号： B62K11/14 ,  B62K21/04 ,  Y10T74/2078 ,  Y10T74/20804

摘要： A steering system for a motorcycle includes a head pipe, a steering stem, a top bridge, a bottom bridge, a front fork, and a steering handlebar. The steering stem is supported by the head pipe. The top bridge has a center portion, a side portion extending from the center portion, and a holding portion provided at the side portion. The top bridge is supported by the steering stem at the center portion to steerably move around the head pipe. The bottom bridge is supported by the steering stem to steerably move around the head pipe. The front fork is held by the top bridge through the holding porting and is held by the bottom bridge. The top bridge has a protruding portion provided on an upper face of the top bridge and extending from the holding portion toward the center portion of the top bridge.

摘要翻译： 用于摩托车的转向系统包括头管，转向杆，顶桥，底桥，前叉和转向车把。 转向杆由头管支撑。 顶桥具有中心部分，从中心部分延伸的侧部分和设置在侧部的保持部分。 顶桥由中心部分的转向杆支撑，以可操纵地围绕头管移动。 底部桥梁由转向杆​​支撑以可控地围绕头部管道移动。 前叉由顶桥通过保持口固定，并由底桥保持。 顶桥具有设置在顶桥的上表面上并从保持部向顶桥的中心部延伸的突出部。