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1. 发明授权

US5310902A Alkylenediamine derivatives 失效
标题翻译：烷二胺衍生物
公开(公告)号：US5310902A
公开(公告)日：1994-05-10
申请号：US741590
申请日：1991-08-07
申请人： Mitsuo Masaki , Masaru Satoh , Naoya Moritoh , Koichi Hashimoto , Toshiro Kamishiro , Haruhiko Shinozaki
发明人： Mitsuo Masaki , Masaru Satoh , Naoya Moritoh , Koichi Hashimoto , Toshiro Kamishiro , Haruhiko Shinozaki
IPC分类号： C07D295/13 , C07D223/00 , C07D211/26
CPC分类号： C07D295/13
摘要： Novel alkylenediamine derivatives effectively employable glutamate blockers have the formula (I) or (II): ##STR1## wherein each of R.sup.1 and R.sup.6 is an aliphatic hydrocarbon group, an alicyclic hydrocarbon group, an aryl group, or an aralkyl group; each of R.sup.2 and R.sup.7 is an aliphatic hydrocarbon group, an alkoxy group, an aliphatic hydrocarbon group containing an ester bonding, an aliphatic hydrocarbon group containing an ether bonding, or an aryloxy group; each of R.sup.3, R.sup.4, R.sup.5 R.sup.8, R.sup.9 and R.sup.10 is hydrogen, an alkyl group, an alkoxy group, an acyloxy group, an aryl group, an aralkyl group, hydroxyl, a hydroxylalkyl group, halogen, nitrile, nitro, amino, carbamoyl or alkoxycarbonyl; and each of m and n is an integer of 0-3 (m+n does not exceed 3); k is an integer of 1-4; each of p and i is an integer of 2-13; and each of q and j is an integer of 4-7.
摘要翻译：新型亚烷基二胺衍生物有效地可用的谷氨酸盐阻滞剂具有式（I）或（II）：其中R 1和R 6各自为脂族烃基，脂环族烃基，芳基，或芳烷基; R 2和R 7各自为脂族烃基，烷氧基，含酯键的脂族烃基，含有醚键的脂族烃基或芳氧基; R 3，R 4，R 5，R 9和R 10各自为氢，烷基，烷氧基，酰氧基，芳基，芳烷基，羟基，羟基烷基，卤素，腈，硝基，氨基，氨基甲酰基或烷氧基羰基; 并且m和n分别为0-3的整数（m + n不超过3）; k是1-4的整数; p和i中的每一个是2-13的整数; 并且q和j中的每一个是4-7的整数。

2. 发明授权

US5070196A Alkylenediamine derivatives 失效
标题翻译：烷二胺衍生物
公开(公告)号：US5070196A
公开(公告)日：1991-12-03
申请号：US562422
申请日：1990-08-01
申请人： Mitsuo Masaki , Masaru Satoh , Naoya Moritoh , Koichi Hashimoto , Toshiro Kamishiro , Haruhiko Shinozaki
发明人： Mitsuo Masaki , Masaru Satoh , Naoya Moritoh , Koichi Hashimoto , Toshiro Kamishiro , Haruhiko Shinozaki
IPC分类号： C07D295/13
CPC分类号： C07D295/13
摘要： Novel alkylenediamine derivatives effectively employable as glutamate blockers have the formula (I) or (II): ##STR1## wherein each of R.sup.1 and R.sup.6 is an aliphatic hydrocarbon group, an alicyclic hydrocarbon group, an aryl group, or an aralkyl group; each of R.sup.2 and R.sup.7 is an aliphatic hydrocarbon group, an alkoxy group, an aliphatic hydrocarbon group containing an ester bonding, an aliphatic hydrocarbon group containing an ether bonding, or an aryloxy group; each of R.sup.3, R.sup.4, R.sup.5, R.sup.8, R.sup.9 and R.sup.10 is hydrogen, an alkyl group, an alkoxy group, an acyloxy group, an aryl group, an aralkyl group, hydroxyl, a hydroxylalkyl group, halogen, nitrile, nitro, amino, carbamoyl or alkoxycarbonyl; and each of m and n is an integer of 0-3 (m+n does not exceed 3); k is an integer of 1-4; each of p and i is an integer of 2-13; and each of q and j is an integer of 4-7.
摘要翻译：作为谷氨酸盐阻滞剂有效利用的新型亚烷基二胺衍生物具有式（I）或（II）：其中R 1和R 6各自为脂族烃基，脂环族烃基，芳基基团或芳烷基; R 2和R 7各自为脂族烃基，烷氧基，含酯键的脂族烃基，含有醚键的脂族烃基或芳氧基; R 3，R 4，R 5，R 8，R 9和R 10各自为氢，烷基，烷氧基，酰氧基，芳基，芳烷基，羟基，羟烷基，卤素，腈，硝基，氨基，氨基甲酰基或烷氧基羰基; 并且m和n分别为0-3的整数（m + n不超过3）; k是1-4的整数; p和i中的每一个是2-13的整数; 并且q和j中的每一个是4-7的整数。

3. 发明授权

US5250546A Amino-alcohol derivatives and processes for their preparation 失效
标题翻译：氨基醇衍生物及其制备方法
公开(公告)号：US5250546A
公开(公告)日：1993-10-05
申请号：US551037
申请日：1990-07-11
申请人： Mitsuo Masaki , Haruhiko Shinozaki , Masaru Satoh , Naoya Moritoh , Koichi Hashimoto , Toshiro Kamishiro
发明人： Mitsuo Masaki , Haruhiko Shinozaki , Masaru Satoh , Naoya Moritoh , Koichi Hashimoto , Toshiro Kamishiro
IPC分类号： C07D295/13 , A61K31/445
CPC分类号： C07D295/13
摘要： Amino-alcohol derivatives of the formula, ##STR1## where R.sub.1 is a straight or branched alkyl group having 3 to 8 carbon atoms, R.sub.2 and R.sub.3 are each a lower alkyl group, or R.sub.2 and R.sub.3 form a 5- to 7-membered ring together with the adjacent nitrogen atom which may have an oxygen atom attached thereto, R.sub.4 is a hydrogen atom or a lower alkyl group, R.sub.5 is a hydrogen atom or a lower alkyl group, X is a hydrogen or halogen atom or a lower alkyl or lower alkoxy group, and n is an integer of 2 or 3, and acid addition salts thereof, are effectively useful as medicines and agricultural chemicals. Processes are also disclosed for preparing such compounds.
摘要翻译：其中R1是具有3至8个碳原子的直链或支链烷基，R2和R3各自为低级烷基，或R2和R3形成5-至7-元环的下式的氨基醇衍生物，与可能具有氧原子的相邻氮原子一起，R4是氢原子或低级烷基，R5是氢原子或低级烷基，X是氢或卤素原子或低级烷基或低级烷基烷氧基，n为2或3的整数，其酸加成盐可有效用作药物和农药。还公开了制备这些化合物的方法。

4. 发明授权

US4764617A Quinaldinamide derivatives 失效
标题翻译：喹哪啶衍生物
公开(公告)号：US4764617A
公开(公告)日：1988-08-16
申请号：US895938
申请日：1986-08-13
申请人： Mitsuo Masaki , Haruhiko Shinozaki , Masaru Satoh , Naoya Moritoh , Koichi Hashimoto , Toshiro Kamishiro
发明人： Mitsuo Masaki , Haruhiko Shinozaki , Masaru Satoh , Naoya Moritoh , Koichi Hashimoto , Toshiro Kamishiro
IPC分类号： C07D295/12 , A01N43/42 , A61K31/47 , A61K31/55 , A61P25/00 , C07C67/00 , C07C209/00 , C07C209/40 , C07C209/60 , C07C211/27 , C07C213/00 , C07C225/16 , C07C239/00 , C07C251/48 , C07D20060101 , C07D215/48 , C07D215/52 , C07D217/00 , C07D295/10 , C07D401/06 , C07D401/12
CPC分类号： C07D215/48 , Y10S514/906
摘要： A novel quinaldinamide derivative having the formula: ##STR1## wherein each of R.sup.1 and R.sup.2 independently represents a lower alkyl group or R.sup.1 and R.sup.2 are combined together with the adjacent nitrogen atom to form a 5-7 membered ring; and X represents the hydrogen atom, a lower alkyl group or a lower alkoxy group, and its acid-addition salt, which show prominent central muscle relaxant effect, namely rigidity relieving effect on anemic decerebrated rigidity.

5. 发明授权

US4962096A Heterocyclic glycerol derivatives and their use as anti-hypertensive agents 失效
标题翻译：杂环甘油衍生物及其作为抗高血压剂的用途
公开(公告)号：US4962096A
公开(公告)日：1990-10-09
申请号：US172581
申请日：1988-03-24
申请人： Mitsuo Masaki , Hiromitsu Takeda , Toshiro Kamishiro , Masao Yamamoto
发明人： Mitsuo Masaki , Hiromitsu Takeda , Toshiro Kamishiro , Masao Yamamoto
IPC分类号： C07F9/10 , C07F9/572 , C07F9/576 , C07F9/58 , C07F9/59 , C07F9/60 , C07F9/62 , C07F9/6539
CPC分类号： C07F9/60 , C07F9/10 , C07F9/5722 , C07F9/5725 , C07F9/5765 , C07F9/582 , C07F9/592 , C07F9/595 , C07F9/62 , C07F9/6539
摘要： A novel glycerol derivative which is effective to reduce blood pressure has the formula: ##STR1## wherein R.sup.1 is an alkyl group having 10-22 carbon atoms, R.sup.2 is lower acyl, benzoyl, aryl, mono-, di- or triarylalkyl, alkyl, cycloalkyl, or cycloalkylalkyl; Q is substituted or unsubstituted alkylene containing 1-4 carbon atoms, l is 0 or 1; Y is a nitrogen-containing heterocyclic group or a nitrogen-containing bridged heterocyclic group (--(Q).sub.l -- is attached to a carbon atom contained in a hetero-ring of the heterocyclic group) in which Y is the bridged heterocyclic group where l is 0; and each of R.sup.5, R.sup.6 and R.sup.7 is hydrogen, lower alkyl, aryl or aralkyl.

6. 发明授权

US4891433A Process for the preparation of dibenzothiepin derivative 失效
标题翻译：二苯并噻吩衍生物的制备方法
公开(公告)号：US4891433A
公开(公告)日：1990-01-02
申请号：US102981
申请日：1987-09-30
申请人： Mitsuo Masaki , Hiromitsu Takeda , Naoya Moritoh , Toshihiro Takahashi
发明人： Mitsuo Masaki , Hiromitsu Takeda , Naoya Moritoh , Toshihiro Takahashi
IPC分类号： C07C323/62 , C07D337/14
CPC分类号： C07C323/62 , C07D337/14
摘要： A novel process for the preparation of 2-(10,11-dihydro-10-oxodibenzo[b, f]thiepin-2-yl)propionic acid which shows high anti-inflammatory and analgetic action is disclosed. The process starts from a propiophenone derivative having the formula (II): ##STR1## wherein R.sup.1 is hydrogen or a lower alkyl group, which is once converted into a haloacetal compound via a halo-ketone compound, and then converted into the desired dibenzothiepin derivative through a combination of rearrangement, hydrolysis and ring closure in variable sequences.
摘要翻译：公开了一种制备显示出高抗炎和止痛作用的2-（10,11-二氢-10-氧代二苯并[b，f]硫杂-2-基）丙酸的新方法。该方法从具有式（II）的苯丙酮衍生物开始：其中R1是氢或低级烷基，其通过卤代酮化合物一度转化为卤代缩醛化合物，然后转化为通过可变序列的重排，水解和闭环的组合，所需的二苯并噻吩衍生物。

7. 发明授权

US5053402A Certain glyceryl phosphate-cyclic ammonium compounds useful for treating hypertension 失效
标题翻译：某些用于治疗高血糖症的糖果 - 磷酸循环氨基甲酸酯化合物
公开(公告)号：US5053402A
公开(公告)日：1991-10-01
申请号：US438996
申请日：1989-11-22
申请人： Mitsuo Masaki , Hiromitsu Takeda , Toshiro Kamishiro , Masao Yamamoto
发明人： Mitsuo Masaki , Hiromitsu Takeda , Toshiro Kamishiro , Masao Yamamoto
IPC分类号： A61K31/685 , A61P7/02 , A61P9/12 , C07F9/10 , C07F9/553 , C07F9/572 , C07F9/59
CPC分类号： C07F9/5532 , C07F9/10 , C07F9/5725 , C07F9/595
摘要： A glycerol derivative which is effective to reduce blood pressure and has the formula: ##STR1## wherein R.sup.1 is an alkyl group having 10-22 carbon atoms, R.sup.2 is a lower acyl group or benzoyl, each of R.sup.3 and R.sup.4 independently is hydrogen or a straight or branched chain alkyl group having 1-6 carbon atoms; each of R.sup.5, R.sup.6 and R.sup.7 independently is hydrogen, a straight or branched chain alkyl group having 1-6 carbon atoms, an aryl group or an aralkyl group; and each of m and n independently is 0 or a positive integer under the condition of m+n=2-8.
摘要翻译：一种有效降低血压的甘油衍生物，具有下式：其中R1是具有10-22个碳原子的烷基，R2是低级酰基或苯甲酰基，R3和R4各自独立地是氢或一个具有1-6个碳原子的直链或支链烷基; R5，R6和R7各自独立地为氢，具有1-6个碳原子的直链或支链烷基，芳基或芳烷基; 在m + n = 2-8的条件下，m和n各自独立地为0或正整数。

8. 发明授权

US5183811A Glycerol derivative and anti-hypertensive agent 失效
标题翻译：甘油衍生物和抗高血压药
公开(公告)号：US5183811A
公开(公告)日：1993-02-02
申请号：US554343
申请日：1990-07-19
申请人： Mitsuo Masaki , Hiromitsu Takeda , Toshiro Kamishiro , Masao Yamamoto
发明人： Mitsuo Masaki , Hiromitsu Takeda , Toshiro Kamishiro , Masao Yamamoto
IPC分类号： C07F9/10 , C07F9/572 , C07F9/576 , C07F9/58 , C07F9/59 , C07F9/60 , C07F9/62 , C07F9/6539
CPC分类号： C07F9/582 , C07F9/10 , C07F9/5722 , C07F9/5725 , C07F9/5765 , C07F9/592 , C07F9/595 , C07F9/60 , C07F9/62 , C07F9/6539
摘要： A novel glycerol derivative which is effective to reduce blood pressure has the formula: ##STR1## wherein R.sup.1 is an alkyl group having 10-22 carbon atoms, R.sup.2 is lower acyl, benzoyl, aryl, mono-, di- or triarylalkyl, alkyl, cycloalkyl, or cycloalkylalkyl; Q is substituted or unsubstituted alkylene containing 1-4 carbon atoms, l is 0 or 1; Y is a nitrogen-containing heterocyclic group or a nitrogen-containing bridged heterocyclic group (--(Q).sub.l -- is attached to a carbon atom contained in a hetero-ring of the heterocyclic group) in which Y is the bridged heterocyclic group where l is 0; and each of R.sup.5, R.sup.6 and R.sup.7 is hydrogen, lower alkyl, aryl or aralkyl.
摘要翻译：有效降低血压的新型甘油衍生物具有下式：其中R1是具有10-22个碳原子的烷基，R2是低级酰基，苯甲酰基，芳基，单 - ，三 - 芳基烷基，烷基，环烷基或环烷基烷基; Q是取代或未取代的含有1-4个碳原子的亚烷基，l是0或1; Y是含氮杂环基或含氮桥接杂环基（ - （Q）1-连接到杂环基杂环中含有的杂原子上的碳原子），其中Y是桥连杂环基，其中l 是0; R 5，R 6和R 7各自为氢，低级烷基，芳基或芳烷基。

9. 发明授权

US5523317A Method of reducing blood pressure 失效
标题翻译：降低血压的方法
公开(公告)号：US5523317A
公开(公告)日：1996-06-04
申请号：US188446
申请日：1994-01-26
申请人： Mitsuo Masaki , Fumiyo Hara , Toshiro Kamishiro
发明人： Mitsuo Masaki , Fumiyo Hara , Toshiro Kamishiro
IPC分类号： A61K31/415 , A61K31/47 , A01N43/50
CPC分类号： A61K31/47 , A61K31/415
摘要： Disclosed is a method of reducing blood pressure which comprises administering to a patient an imidazole derivative of the formula: ##STR1## wherein: each of R.sup.1 and R.sup.2 is hydrogen, substituted or unsubstituted alkyl, alkoxyalkyl, cycloalkyl, aryl, aralkyl, or R.sup.1 and R.sup.2 are combined to form hetero ring; each of R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is hydrogen, halogen, substituted or unsubstituted alkoxy, substituted or unsubstituted alkyl, aryl, aryloxy, alkoxycarbonyl, nitro, amino, acyl, or R.sup.3 is combined with R.sup.2 to form heteroring; R.sup.7 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylcarbonyl, or S-containing heteroring; each of R.sup.8 and R.sup.9 is hydrogen, halogen, substituted or unsubstituted alkoxy, unsubstituted or substituted alkyl, alkoxycarbonyl, aralkyl, nitro, amino, acyl, substituted or unsubstituted aryl, or R.sup.8 and R.sup.9 are combined to from alkylene; and n is 0 or 1.
摘要翻译：公开了降低血压的方法，其包括向患者施用下式的咪唑衍生物：其中：R 1和R 2各自为氢，取代或未取代的烷基，烷氧基烷基，环烷基，芳基，芳烷基，或R 1和R 2结合形成杂环; R 3，R 4，R 5和R 6中的每一个为氢，卤素，取代或未取代的烷氧基，取代或未取代的烷基，芳基，芳氧基，烷氧基羰基，硝基，氨基，酰基或R3与R 2结合形成杂环; R 7是氢，取代或未取代的烷基，取代或未取代的芳基，取代或未取代的芳基羰基或含S的杂环; R8和R9各自为氢，卤素，取代或未取代的烷氧基，未取代或取代的烷基，烷氧基羰基，芳烷基，硝基，氨基，酰基，取代或未取代的芳基，或R8和R9与亚烷基结合; n为0或1。

10. 发明授权

US4596803A Piperazine derivatives and a medicine containing the same 失效
标题翻译：哌嗪衍生物和含有其的药物
公开(公告)号：US4596803A
公开(公告)日：1986-06-24
申请号：US587545
申请日：1984-03-08
申请人： Tomoh Masaki , Toshiro Kamishiro , Takashi Okazoe , Koichi Kumakura , Mitsuo Masaki
发明人： Tomoh Masaki , Toshiro Kamishiro , Takashi Okazoe , Koichi Kumakura , Mitsuo Masaki
IPC分类号： C07D295/10 , A61K31/495 , A61K31/496 , A61K31/505 , A61P9/00 , A61P9/08 , A61P9/10 , C07D213/74 , C07D213/75 , C07D239/42 , C07D295/18 , C07D295/185 , C07D303/48 , C07D405/12 , C07D405/14
CPC分类号： C07D303/48 , Y02P20/55
摘要： A compound is disclosed which has the formula, ##STR1## where R.sup.1 is a hydrogen atom, or a straight or branched chain alkyl group having 1 to 4 carbon atoms, and R.sup.2 is a straight or branched chain alkyl group having 1 to 4 carbon atoms, ##STR2## in which n is an integer of 0 to 3, or a pharmaceutically acceptable salt thereof. A process for producing the compound and a medicine containing the compound are also disclosed. Such medicine is effectively useful for inhibiting myocardial infarction.
摘要翻译：公开了具有下式的化合物，其中R 1是氢原子，或具有1至4个碳原子的直链或支链烷基，R 2是具有1至4个碳原子的直链或支链烷基，其中n为0〜3的整数， + TR ，或其药学上可接受的盐。还公开了制备该化合物的方法和含有该化合物的药物。这种药物有效地用于抑制心肌梗死。

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