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1. 发明授权

US4578465A Phenyliperazine derivatives 失效
标题翻译：苯基哌嗪衍生物
公开(公告)号：US4578465A
公开(公告)日：1986-03-25
申请号：US604415
申请日：1984-04-30
申请人： Hiroyuki Nagano , Mitiro Takagi , Noboru Kubodera , Isao Matsunaga , Hiroyuki Nabata , Yasuhiro Ohba , Kazushige Sakai , Shun-ichi Hata , Yasumi Uchida
发明人： Hiroyuki Nagano , Mitiro Takagi , Noboru Kubodera , Isao Matsunaga , Hiroyuki Nabata , Yasuhiro Ohba , Kazushige Sakai , Shun-ichi Hata , Yasumi Uchida
IPC分类号： C07D403/06 , A61K31/505 , A61K31/517 , A61P9/00 , A61P9/12 , C07D239/96
CPC分类号： C07D239/96
摘要： Phenylpiperazine derivatives of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a straight- or branched-chain saturated or unsaturated alkyl group having 1 to 8 carbon atoms which may be substituted at any position by a hydroxyl group, a carboxyl group, a lower alkoxycarbonyl group or an oxo group; and R.sub.2 is a hydrogen atom, a halogen atom, a lower alkyl group or a sulfamoyl group, and a process for producing the same are disclosed. The derivatives of the formula have alpha blocking and serotonin antagonizing activities and are useful as a drug.
摘要翻译：具有下式的苯基哌嗪衍生物：其中R1是氢原子或可以在任何位置被羟基取代的具有1-8个碳原子的直链或支链饱和或不饱和烷基，羧基，低级烷氧基羰基或氧代基; R 2为氢原子，卤素原子，低级烷基或氨磺酰基及其制造方法。该衍生物具有α阻断和5-羟色胺拮抗活性，可用作药物。

2. 发明授权

US4560686A Method for treating circulatory diseases by using (2-lower alkoxyphenyl)piperazine derivatives 失效
标题翻译：通过使用（2-低级烷氧基苯基）哌嗪衍生物治疗循环系统疾病的方法
公开(公告)号：US4560686A
公开(公告)日：1985-12-24
申请号：US532271
申请日：1983-09-14
申请人： Hiroyuki Nagano , Mitiro Takagi , Noboru Kubodera , Isao Matsunaga , Hiroyuki Nabata , Yasuhiro Ohba , Kazushige Sakai , Shun-ichi Hata , Yasumi Uchida
发明人： Hiroyuki Nagano , Mitiro Takagi , Noboru Kubodera , Isao Matsunaga , Hiroyuki Nabata , Yasuhiro Ohba , Kazushige Sakai , Shun-ichi Hata , Yasumi Uchida
IPC分类号： C07D295/12 , A61K31/495 , A61P9/00 , A61P9/06 , A61P9/10 , A61P9/12 , C07D295/13 , C07D317/68 , C07D241/04
CPC分类号： C07D295/13 , C07D317/68
摘要： Compounds of the formula ##STR1## (wherein R.sub.1 is a lower alkyl group, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, represent a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a trifluoromethyl group or a lower alkoxycarbonyl group; two adjacent groups of R.sub.2, R.sub.3 and R.sub.4 may combine to form a methylenedioxy group; n is an integer of 2 to 6) or salts thereof, are disclosed.These compounds are useful as agents for treating circulatory diseases because they have hypotensive action and are capable of increasing the cerebral blood flow, decreasing the heart rate and suppressing ventricular arrhythmia due to myocardial ischemia.
摘要翻译：式（IMAGE）的化合物（其中R 1为低级烷基，R 2，R 3和R 4可相同或不同，表示氢原子，卤素原子，低级烷基，低级烷氧基，羟基，三氟甲基或低级烷氧基羰基; R 2，R 3和R 4的两个相邻基团可以结合形成亚甲二氧基; n是2至6的整数）或其盐。这些化合物可用作治疗循环系统疾病的药剂，因为它们具有降血压作用，并且能够增加脑血流量，降低心率并抑制心肌缺血引起的室性心律失常。

3. 发明授权

US4438115A Compositions and methods for treating diseases in circulatory organs 失效
标题翻译：用于治疗循环器官疾病的组合物和方法
公开(公告)号：US4438115A
公开(公告)日：1984-03-20
申请号：US272077
申请日：1981-06-10
申请人： Hiroyuki Nagano , Mitiro Takagi , Noboru Kubodera , Isao Matsunaga , Tamotsu Yamazaki , Hiroyuki Nabata , Kazushige Sakai , Shun-ichi Hata
发明人： Hiroyuki Nagano , Mitiro Takagi , Noboru Kubodera , Isao Matsunaga , Tamotsu Yamazaki , Hiroyuki Nabata , Kazushige Sakai , Shun-ichi Hata
IPC分类号： C07D295/02 , A61K31/495 , A61P9/00 , A61P9/10 , A61P9/12 , C07D295/14 , C07D295/15 , A01N43/48
CPC分类号： C07D295/15 , A61K31/495
摘要： An agent for treating diseases in circulatory organs which comprises a piperazine compound of the formula ##STR1## wherein R.sub.1, R.sub.2 and A are as defined hereunder, or a salt thereof and a pharmaceutically acceptable carrier.
摘要翻译：一种用于治疗循环器官疾病的药剂，其包含式IMA IMA的化合物，其中R 1，R 2和A如下文所定义，或其盐和药学上可接受的载体。

4. 发明授权

US4409234A Pyrazoloindazole derivatives and bronchodilating composition 失效
标题翻译：吡唑并唑衍生物和支气管扩张组合物
公开(公告)号：US4409234A
公开(公告)日：1983-10-11
申请号：US384861
申请日：1982-06-03
申请人： Yasuo Fujimura , Sadao Tanaka , Isao Matsunaga , Yasuyuki Shiraki , Yugo Ikeda , Tamotsu Yamazaki , Yasuhiro Ohba , Shun-ichi Hata , Minoru Shindo , Kazushige Sakai
发明人： Yasuo Fujimura , Sadao Tanaka , Isao Matsunaga , Yasuyuki Shiraki , Yugo Ikeda , Tamotsu Yamazaki , Yasuhiro Ohba , Shun-ichi Hata , Minoru Shindo , Kazushige Sakai
IPC分类号： A61K31/415 , A61K31/416 , A61P11/08 , C07D487/04
CPC分类号： C07D487/04
摘要： Novel pyrazoloindazole derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom, halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxyl group or benzyloxyl group; R.sub.2 is a hydrogen atom, a halogen atom, a lower alkyl group or phenyl group (provided R.sub.1 and R.sub.2 are not hydrogen at the same time); and X.sup..crclbar. is a halide ion, a hydroxide ion, a methanesulfonate ion, a p-toluene sulfonate ion, a sulfate ion, a nitrate ion, a carbonate ion, an acetate ion, a benzoate ion or a salicylate ion, a process for preparing the derivatives, and a pharmaceutical composition containing the same are disclosed. The derivatives have good bronchodilating action for human without exhibiting substantially bad effects on the functioning of heart, and therefore, they are useful as a drug.
摘要翻译：新颖的式（Ia）的吡唑并吲唑衍生物，其中R1是氢原子，卤原子，羟基，低级烷基，低级烷氧基或苄氧基; R2是氢原子，卤原子，低级烷基或苯基（R1和R2不同时同时为氢）; 和X（ - ）是卤离子，氢氧根离子，甲磺酸根离子，对甲苯磺酸根离子，硫酸根离子，硝酸根离子，碳酸根离子，乙酸根离子，苯甲酸根离子或水杨酸根离子，公开了制备衍生物的方法和含有该衍生物的药物组合物。该衍生物对人体具有良好的支气管扩张作用，对心脏的功能没有显示不良影响，因此它们可用作药物。

5. 发明授权

US4447453A Anti-peptic ulcer agent 失效
标题翻译：抗消化性溃疡剂
公开(公告)号：US4447453A
公开(公告)日：1984-05-08
申请号：US322182
申请日：1981-11-17
申请人： Mitsura Tanemura , Tamotsu Yamazaki , Koji Mizuno , Shin-ichi Kaiho , Morio Kakimoto , Eiichi Hoshino , Isao Matsunaga , Shun-ichi Hata
发明人： Mitsura Tanemura , Tamotsu Yamazaki , Koji Mizuno , Shin-ichi Kaiho , Morio Kakimoto , Eiichi Hoshino , Isao Matsunaga , Shun-ichi Hata
IPC分类号： A61K31/195 , A61K20060101 , A61K31/245 , A61P1/04 , C07C20060101
CPC分类号： C07C229/58 , Y10S514/927
摘要： An anti-peptic ulcer agent which contains as an active ingredient aminobenzoic acid compounds of the formula ##STR1## (wherein R.sub.1, R.sub.2, and R.sub.3 which may be the same or different represent a hydrogen atom, halogen atom, lower alkyl group or lower alkoxy group but they do not represent a hydrogen atom at the same time) or pharmaceutically acceptable salts thereof and a method of preventing or treating a human in need of said prevention or treatment an effective amount of said active ingredient are disclosed.
摘要翻译：作为活性成分的抗消化性溃疡剂，其含有下式的氨基苯甲酸化合物（其中R1，R2和R3可以相同或不同，表示氢原子，卤素原子，低级烷基或低级烷氧基但是它们不同时表示氢原子）或其药学上可接受的盐，并且公开了预防或治疗需要所述预防或治疗的人的有效量的所述活性成分的方法。

6. 发明授权

US4891364A Vitamin D derivatives, process for producing the same and their use in the differentiation of tumor cells 失效
标题翻译：维生素D衍生物，其制备方法及其在肿瘤细胞分化中的应用
公开(公告)号：US4891364A
公开(公告)日：1990-01-02
申请号：US211096
申请日：1988-06-13
申请人： Noboru Kubodera , Katsuhito Miyamoto , Kiyoshige Ochi , Isao Matsunaga , Eigoro Murayama
发明人： Noboru Kubodera , Katsuhito Miyamoto , Kiyoshige Ochi , Isao Matsunaga , Eigoro Murayama
IPC分类号： C07C401/00 , C07J7/00 , C07J41/00 , C07J51/00 , C07J71/00
CPC分类号： C07J7/002 , C07C401/00 , C07J41/005 , C07J51/00 , C07J7/007 , C07J71/0042
摘要： Vitamin D derivatives of the formula ##STR1## where R.sub.1, R.sub.2 and R.sub.3 which may be the same or different each represents a hydrogen atom or a hydroxyl group; X is an oxygen atom, the group of the formula OR.sub.4 (where R.sub.4 is either a hydrogen atom or a lower alkyl having 4 to 6 carbon atoms that may or may not be substituted by a hydroxyl group), or the group of the formula=N-OR.sub.5 (where R.sub.5 is either a hydrogen atom or a lower alkyl group having 1 to 5 carbon atoms that may or may not be substituted by a hydroxyl group, an amino group or a lower alkylamino group having 1 to 3 carbon atoms), provided that the carbon atom at 20-position is linked to X by a single bond when X is the group of the formula OR.sub.4, and by a double bond in other cases, and a process for preparing the derivatives are disclosed.The derivatives have both the immunoregulating action and the ability to induce differentiation in tumor cells and hence are useful as medicines such as antiallergic agents, antirheumatic agents and antitumor agents.
摘要翻译：其中R1，R2和R3可以相同或不同的维生素D衍生物表示氢原子或羟基; X是氧原子，式OR4（其中R4是氢原子或具有4-6个碳原子的低级烷基，可以被羟基取代或不被羟基取代）的基团，或式= N-OR5（其中R5为氢原子或碳原子数1〜5的低级烷基，可以被羟基，氨基或碳原子数1〜3的低级烷基氨基取代）条件是当X是式OR4的基团时，20位上的碳原子通过单键与X连接，并且在其它情况下通过双键，并且公开了制备衍生物的方法。所述衍生物具有免疫调节作用和在肿瘤细胞中诱导分化的能力，因此可用作药物如抗过敏剂，抗风湿剂和抗肿瘤剂。

7. 发明授权

US4666634A vitamin D.sub.3 derivatives having a substituent at 2-position 失效
标题翻译：在2-位具有取代基的维生素D3衍生物
公开(公告)号：US4666634A
公开(公告)日：1987-05-19
申请号：US800320
申请日：1985-11-20
申请人： Katsuhito Miyamoto , Noboru Kubodera , Kiyoshige Ochi , Isao Matsunaga , Eigoro Murayama
发明人： Katsuhito Miyamoto , Noboru Kubodera , Kiyoshige Ochi , Isao Matsunaga , Eigoro Murayama
IPC分类号： A61K31/59 , A61P3/00 , A61P3/02 , A61P3/14 , C07C67/00 , C07C401/00 , C07J9/00 , C07J41/00 , C07J71/00
CPC分类号： C07J71/0042 , C07C401/00 , C07J41/0011 , C07J41/0027 , C07J71/001 , C07J9/00
摘要： A 1.alpha.-hydroxy vitamin D.sub.3 derivative of the formula: ##STR1## where R.sub.1 is a hydroxyl group, an amino group or the group: OR' (where R' is a lower alkyl group having 1 to 7 carbon atoms that may or may not be substituted by a hydroxyl group, a halogen atom, a cyano group, a lower alkoxy group having 1 to 3 carbon atoms, an amino group, or an acylamino group); R.sub.2 is a hydrogen atom or a hydroxyl group), and a process for preparing the same are disclosed.The compound represented by the formula above has the calcium control action and the ability to induce differentiation in tumor cells and, therefore, are useful as an antitumor agents and a medicine for treating calcium dysbolism-caused diseases.
摘要翻译： 1α-羟基维生素D3衍生物，其结构式如下：其中R1是羟基，氨基或基团：OR'（其中R'是具有1至7个碳原子的低级烷基，可以或可以不被羟基，卤素原子，氰基，具有1至3个碳原子的低级烷氧基，氨基或酰氨基取代）; R2是氢原子或羟基），以及其制备方法。由上式表示的化合物具有钙控制作用和诱导肿瘤细胞分化的能力，因此可用作抗肿瘤剂和用于治疗钙异常引起的疾病的药物。

8. 发明授权

US4200640A Nitric ester of N-(2-hydroxyethyl)nicotinamide and pharmaceutical use 失效
标题翻译： N-（2-羟乙基）烟酰胺的硝酸酯和药物用途
公开(公告)号：US4200640A
公开(公告)日：1980-04-29
申请号：US940194
申请日：1978-09-07
申请人： Hiroyuki Nagano , Takashi Mori , Sakae Takaku , Isao Matsunaga , Tatsuo Kujirai , Toshichika Ogasawara , Shigeru Sugano , Minoru Shindo
发明人： Hiroyuki Nagano , Takashi Mori , Sakae Takaku , Isao Matsunaga , Tatsuo Kujirai , Toshichika Ogasawara , Shigeru Sugano , Minoru Shindo
IPC分类号： C07D213/81 , A61K31/455 , C07D213/82
CPC分类号： C07D213/81
摘要： A compound of the formula ##STR1## is useful for treating circulatory diseases.
摘要翻译：式的化合物可用于治疗循环系统疾病。

9. 发明授权

US4022768A Process for preparation of 1.alpha.,25-dihydroxycholecalciferol 失效
标题翻译：制备1 {60,25-二羟基胆钙化甾醇的方法
公开(公告)号：US4022768A
公开(公告)日：1977-05-10
申请号：US657375
申请日：1976-02-12
申请人： Isao Matsunaga , Kiyoshige Ochi , Hiroyuki Nagano , Minoru Shindo , Masayuki Ishikawa , Chikara Kaneko , Hector F. DeLuca
发明人： Isao Matsunaga , Kiyoshige Ochi , Hiroyuki Nagano , Minoru Shindo , Masayuki Ishikawa , Chikara Kaneko , Hector F. DeLuca
IPC分类号： C07J9/00 , C07J71/00
CPC分类号： C07J71/0042 , C07J9/00
摘要： 1.alpha.,25-dihydroxycholecalciferol is prepared by reacting 1,5,7-trien-3.beta.,25-diol with a 1,2,4-triazoline-dione derivative represented by the formula: ##STR1## wherein R represents an alkyl group or an aryl or substituted-aryl group; reacting the resulting 1,4-cyclic adduct represented by the general formula ##STR2## wherein R is as defined above, with a peroxide to form a 1.alpha.,2.alpha.-epoxide compound represented by the general formula ##STR3## wherein R is as defined above, reducing the so formed compound with a metal hydride to form cholesta-5,7-diene-1.alpha.,3.beta.,25-triol, irradiating the so formed compound with ultraviolet rays to form 1.alpha.,25-dihydroxyprevitamin D.sub.3, isomerizing the so formed previtamin D.sub.3, and recovering 1.alpha.,25-dihydroxycholecalciferol.
摘要翻译： 1α，25-二羟基胆钙化醇通过使1,5,7-三烯-3β，25-二醇与下式表示的1,2,4-三唑啉二酮衍生物反应制备：其中R表示烷基或芳基或取代的芳基; 使得到的由通式“IMAGE”表示的所得1,4-环加成物与上述定义相同，与过氧化物反应，形成由通式“IMAGE”表示的1α，2α-环氧化合物，其中R为用金属氢化物还原形成的化合物以形成胆甾烯-5,7-二烯-1α，3β，25-三醇，用紫外线照射所形成的化合物以形成1α，25-二羟维生素D3，异构化所形成的维生素D3，并回收1α，25-二羟基胆钙化甾醇。

10. 发明授权

US4698364A Benzoic acid derivatives 失效
标题翻译：苯甲酸衍生物
公开(公告)号：US4698364A
公开(公告)日：1987-10-06
申请号：US788972
申请日：1985-10-18
申请人： Mitsuru Tanemura , Isao Matsunaga , Masami Saitou
发明人： Mitsuru Tanemura , Isao Matsunaga , Masami Saitou
IPC分类号： A61K31/165 , A61K31/19 , C07C317/00 , C07C317/44 , A61K31/10 , C07C149/40 , C07C149/41
CPC分类号： C07C323/00 , A61K31/19 , C07C317/00
摘要： Benzoic acid derivatives of the formula: ##STR1## wherein n is an integer of 0 to 2; R.sub.1 to R.sub.3 which may be the same or different each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or nitro group; R.sub.4 is a hydroxyl group or the group --NHZ (Z is hydrogen atom or a lower alkyl group), or an alkali metal salts thereof are useful as an infection control agent.These derivatives excepting compounds of the formula above wherein n is 0 or 1; any one of R.sub.1 to R.sub.3 is 5-chloro, 5-methoxy or 5-nitro and the remainder is a hydrogen atom; and R.sub.4 is a hydroxyl group; and compounds of the formula wherein n is 0 or 1; two of R.sub.1 to R.sub.3 are 3,5-dichloro or 3,5-dinitro and the remainder is a hydrogen atom; and R.sub.4 is a hydroxy group) are novel, and they were first prepared in this invention.
摘要翻译：下式的苯甲酸衍生物：其中n是0-2的整数; 可以相同或不同的R 1〜R 3表示氢原子，卤素原子，低级烷基，低级烷氧基或硝基; R4是羟基或基团-NHZ（Z是氢原子或低级烷基）或其碱金属盐可用作感染控制剂。这些衍生物除了上式的化合物，其中n为0或1; R 1至R 3中的任一个为5-氯，5-甲氧基或5-硝基，其余为氢原子; R4为羟基; 和下式的化合物其中n为0或1; R 1至R 3中的两个为3,5-二氯或3,5-二硝基，其余为氢原子; 和R4是羟基）是新的，并且它们首先在本发明中制备。

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