公开(公告)号：US4032575A

公开(公告)日：1977-06-28

申请号：US618355

申请日：1975-10-01

申请人： Muneyoshi Ikezaki ,  Nobuo Ito ,  Yasushi Okazaki ,  Masao Hoshiyama ,  Taku Nagao ,  Hiromichi Nakajima

发明人： Muneyoshi Ikezaki ,  Nobuo Ito ,  Yasushi Okazaki ,  Masao Hoshiyama ,  Taku Nagao ,  Hiromichi Nakajima

IPC分类号： A61K31/135 ,  A61P9/04 ,  C07B61/00 ,  C07C67/00 ,  C07C213/00 ,  C07C217/60 ,  C07C91/22

CPC分类号： A61K31/135 ,  Y10S514/866

摘要： A compound having the formula: ##STR1## wherein Ring A is monohydroxyphenyl, or a pharmaceutically acceptable acid addition salt thereof is prepared by catalytic hydrogenation of a compound having the formula: ##STR2## wherein A' is monobenzyloxyphenyl, and Y is carbonyl or hydroxymethylene. The compound (I) in which Ring A is 4-hydroxyphenyl or 3-hydroxyphenyl is useful as a cardiotonic agent. On the other hand, the compound (I) in which Ring A is 2-hydroxyphenyl is useful as an anti-diabetic agent.

摘要翻译： 具有下式的化合物：其中环A为单羟基苯基或其药学上可接受的酸加成盐通过具有下式的化合物的催化氢化制备：其中A'为单苄氧基苯基，Y为 羰基或羟基亚甲基。 环A为4-羟基苯基或3-羟基苯基的化合物（I）可用作强心剂。 另一方面，环A为2-羟基苯基的化合物（I）可用作抗糖尿病药。

公开(公告)号：US3952021A

公开(公告)日：1976-04-20

申请号：US462594

申请日：1974-04-22

申请人： Muneyoshi Ikezaki ,  Yasushi Okazaki ,  Nobuo Ito ,  Taku Nagao ,  Masao Hoshiyama ,  Hiromichi Nakajima

发明人： Muneyoshi Ikezaki ,  Yasushi Okazaki ,  Nobuo Ito ,  Taku Nagao ,  Masao Hoshiyama ,  Hiromichi Nakajima

IPC分类号： A61K31/135 ,  A61K31/335 ,  A61K31/357 ,  A61P9/04 ,  C07C45/63 ,  C07C45/64 ,  C07C67/00 ,  C07C213/00 ,  C07C217/56 ,  C07C217/70 ,  C07D317/58 ,  C07C91/16 ,  C07D307/62

CPC分类号： C07C45/63 ,  C07C45/64

摘要： A compound of the formula: ##SPC1##Wherein Ring A' is dibenzyloxyphenyl and Y is carbonyl or hydroxymethylene, is subjected to catalytic hydrogenation. A compound of the formula: ##SPC2##Wherein Ring A is dihydroxyphenyl, is produced. The product is useful as a cardiotonic agent. It is also characterized by the high potency ratio of adrenergic .beta..sub.1 -receptor stimulating activity to adrenergic .beta..sub.2 -receptor stimulating activity.

摘要翻译： 下式的化合物：

公开(公告)号：US4072759A

公开(公告)日：1978-02-07

申请号：US740399

申请日：1976-11-10

申请人： Muneyoshi Ikezaki ,  Nobuo Ito ,  Yasushi Okazaki ,  Masao Hoshiyama ,  Taku Nagao ,  Hiromichi Nakajima

发明人： Muneyoshi Ikezaki ,  Nobuo Ito ,  Yasushi Okazaki ,  Masao Hoshiyama ,  Taku Nagao ,  Hiromichi Nakajima

IPC分类号： A61K31/135 ,  A61P9/04 ,  C07B61/00 ,  C07C67/00 ,  C07C213/00 ,  C07C217/60

CPC分类号： A61K31/135 ,  Y10S514/866

摘要： A compound having the formula: ##STR1## wherein Ring A is monohydroxyphenyl, or a pharmaceutically acceptable acid addition salt thereof is prepared by catalytic hydrogenation of a compound having the formula: ##STR2## wherein A' is monobenzyloxyphenyl, and Y is carbonyl or hydroxymethylene. The compound (I) in which Ring A is 4-hydroxyphenyl or 3-hydroxyphenyl is useful as a cardiotonic agent. On the other hand, the compound (I) in which Ring A is 2-hydroxyphenyl is useful as an anti-diabetic agent.

公开(公告)号：US4131686A

公开(公告)日：1978-12-26

申请号：US747898

申请日：1976-12-06

申请人： Muneyoshi Ikezaki ,  Yashushi Okazaki ,  Nobuo Ito ,  Masao Hoshiyama ,  Taku Nagao ,  Hiromichi Nakajima

发明人： Muneyoshi Ikezaki ,  Yashushi Okazaki ,  Nobuo Ito ,  Masao Hoshiyama ,  Taku Nagao ,  Hiromichi Nakajima

IPC分类号： C07C45/28 ,  C07C45/64 ,  C07D303/22 ,  A61K31/135 ,  C07C91/34

CPC分类号： C07D303/22 ,  C07C45/28 ,  C07C45/64

摘要： A compound of the formula: ##STR1## wherein R is lower alkyl, may be prepared, for example, by reducing a compound of the formula: ##STR2## wherein R is same as above. Other methods for preparing the compound [I] are also disclosed. The compound [I] and a pharmaceutically acceptable acid addition salt thereof are useful as anti-diabetic agents.

摘要翻译： 其中R是低级烷基的下式化合物可以通过例如还原下式的化合物来制备：其中R与上述相同。 还公开了制备化合物[I]的其它方法。 化合物[I]及其药学上可接受的酸加成盐可用作抗糖尿病药。

公开(公告)号：US4665068A

公开(公告)日：1987-05-12

申请号：US793628

申请日：1985-10-31

申请人： Mikio Takeda ,  Tokuro Oh-ishi ,  Hiromichi Nakajima ,  Taku Nagao

发明人： Mikio Takeda ,  Tokuro Oh-ishi ,  Hiromichi Nakajima ,  Taku Nagao

IPC分类号： A61K31/55 ,  A61K31/554 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D281/10

CPC分类号： C07D281/10

摘要： Novel 1,5-benzothiazepine derivative of the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkanoyl and each of R.sup.2 and R.sup.3 is lower alkyl, and a pharmaceutically acceptable acid addition salt thereof are disclosed.Said derivative (I) and a salt thereof are useful as a hypotensive agent and/or a cerebral or coronary vasodilator.

摘要翻译： 新颖的下式的1,5-苯并硫氮杂衍生物：其中R 1是氢或低级烷酰基，R 2和R 3各自是低级烷基，并且其药学上可接受的酸加成盐被公开。 所述衍生物（I）及其盐可用作降压剂和/或脑或冠状血管扩张剂。

公开(公告)号：US4590188A

公开(公告)日：1986-05-20

申请号：US698125

申请日：1985-02-04

申请人： Mikio Takeda ,  Tokuro Oh-ishi ,  Hiromichi Nakajima ,  Taku Nagao

发明人： Mikio Takeda ,  Tokuro Oh-ishi ,  Hiromichi Nakajima ,  Taku Nagao

IPC分类号： C07D281/10 ,  A61K31/55

CPC分类号： C07D281/10

摘要： Novel 1,5-benzothiazepine derivatives of the formula: ##STR1## wherein R.sup.1 is lower alkyl or lower alkoxy, R.sup.2 is hydrogen atom or lower alkanoyl, each one of R.sup.3 and R.sup.4 is lower alkyl, Ring A is a substituted benzene ring of the formula: ##STR2## R.sup.a is lower alkyl, lower alkoxy, lower alkylthio or benzyloxy, each one of R.sup.b and R.sup.c is lower alkyl, lower alkoxy or halogen atom, and either one of R.sup.d and R.sup.e is fluorine atom and the other one is hydrogen atom, or a pharmaceutically acceptable acid addition salt thereof are disclosed. Said derivative (I) and its salt are useful as a hypotensive agent and/or a cerebral or coronary vasodilator.

摘要翻译： 下式的新的1,5-苯并硫氮杂衍生物：其中R 1是低级烷基或低级烷氧基，R 2是氢原子或低级烷酰基，R 3和R 4各自是低级烷基，环A是取代苯 下式的环：R a是低级烷基，低级烷氧基，低级烷硫基或苄氧基，R b和R c中的每一个是低级烷基，低级烷氧基或卤素原子，Rd和Re中的任一个是氟原子，而另一个 一个是氢原子，或其药学上可接受的酸加成盐。 所述衍生物（I）及其盐可用作降压剂和/或脑或冠状血管扩张剂。

公开(公告)号：US4585768A

公开(公告)日：1986-04-29

申请号：US715116

申请日：1985-03-22

申请人： Mikio Takeda ,  Tokuro Oh-ishi ,  Hiromichi Nakajima ,  Taku Nagao

发明人： Mikio Takeda ,  Tokuro Oh-ishi ,  Hiromichi Nakajima ,  Taku Nagao

IPC分类号： A61K31/55 ,  A61K31/554 ,  A61P7/02 ,  C07D281/10

CPC分类号： C07D281/10 ,  C07C323/00 ,  Y02P20/55

摘要： Novel 1,5-benzothiazepine derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl, R.sup.2 is hydrogen, lower alkanoyl or benzyl, R.sup.3 is hydrogen or lower alkyl and either one of R.sup.4 and R.sup.5 is hydrogen and the other is chlorine, or a pharmaceutically acceptable acid addition salt thereof are disclosed. Said derivative (I) and its salt have a potent platelet aggregation-inhibiting activity.

摘要翻译： 下式的新的1,5-苯并硫氮杂衍生物：其中R 1是氢或低级烷基，R 2是氢，低级烷酰基或苄基，R 3是氢或低级烷基，R 4和R 5中的任一个是氢和 另一种是氯，或其药学上可接受的酸加成盐。 所述衍生物（I）及其盐具有有效的血小板聚集抑制活性。

公开(公告)号：US4594342A

公开(公告)日：1986-06-10

申请号：US715115

申请日：1985-03-22

申请人： Mikio Takeda ,  Tokuro Oh-ishi ,  Hiromichi Nakajima ,  Taku Nagao

发明人： Mikio Takeda ,  Tokuro Oh-ishi ,  Hiromichi Nakajima ,  Taku Nagao

IPC分类号： C07D281/10 ,  A61K31/55

CPC分类号： C07D281/10

摘要： Novel 1,5-benzothiazepine derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.4 are:(a) R.sup.1 is lower alkyl or lower alkoxy, and R.sup.4 is lower alkyl, lower alkoxy, fluorine, benzyloxy, hydroxy or lower alkylthio, or(b) R.sup.1 is lower alkyl, and R.sup.4 is hydrogen, or(c) R.sup.1 is hydroxy, and R.sup.4 is lower alkyl, fluorine, hydroxy or lower alkylthio;R.sup.2 is hydrogen, lower alkanoyl or benzoyl; and R.sup.3 is lower alkyl; and a pharmaceutically acceptable acid addition salt thereof are disclosed. Said derivative (I) and its salt have a potent platelet aggregation-inhibiting activity.

摘要翻译： 下式的新的1,5-苯并硫氮杂衍生物：其中R 1和R 4是：（a）R 1是低级烷基或低级烷氧基，R 4是低级烷基，低级烷氧基，氟，苄氧基，羟基或低级 或（b）R1为低级烷基，R4为氢，或（c）R1为羟基，R4为低级烷基，氟，羟基或低级烷硫基; R2是氢，低级烷酰基或苯甲酰基; 并且R 3是低级烷基; 及其药学上可接受的酸加成盐。 所述衍生物（I）及其盐具有有效的血小板聚集抑制活性。

公开(公告)号：US4567175A

公开(公告)日：1986-01-28

申请号：US610856

申请日：1984-05-16

申请人： Mikio Takeda ,  Tokuro Oh-ishi ,  Hiromichi Nakajima ,  Taku Nagao

发明人： Mikio Takeda ,  Tokuro Oh-ishi ,  Hiromichi Nakajima ,  Taku Nagao

IPC分类号： C07D271/10 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/554 ,  A61P9/12 ,  C07D281/00 ,  C07D281/02 ,  C07D281/10

CPC分类号： C07D281/10 ,  C07C323/00

摘要： Novel 8-chloro-1,5-benzothiazepine derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl or a group of the formula: R.sup.4 CO--, each of R.sup.2 and R.sup.3 is lower alkyl and R.sup.4 is hydrogen or lower alkyl, and a pharmaceutically acceptable acid addition salt thereof are disclosed. Said derivative (I) and a pharmaceutically acceptable acid addition salt thereof are useful as hypotensive agents and/or coronary or cerebral vasodilators.

摘要翻译： 下式的新型8-氯-1,5-苯并硫氮杂衍生物：其中R 1是氢，低级烷基或下式的基团：R 4 CO-，R 2和R 3各自是低级烷基，R 4是氢 或低级烷基，及其药学上可接受的酸加成盐。 所述衍生物（I）及其药学上可接受的酸加成盐可用作降压剂和/或冠状动脉或脑血管扩张剂。

公开(公告)号：US4521430A

公开(公告)日：1985-06-04

申请号：US614743

申请日：1984-05-25

申请人： Tokuro Oh-ishi ,  Mikio Takeda ,  Hiromichi Nakajima ,  Taku Nagao

发明人： Tokuro Oh-ishi ,  Mikio Takeda ,  Hiromichi Nakajima ,  Taku Nagao

IPC分类号： A61K31/55 ,  A61K31/554 ,  A61P3/06 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P25/28 ,  C07D281/10 ,  A61K31/555 ,  C07D281/02

CPC分类号： C07D281/10 ,  Y10S514/929

摘要： A compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl, R.sup.3 is hydrogen, lower alkyl or hydroxy-lower alkyl, R.sup.4 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkylthio or nitro, and A is lower alkylene, is disclosed. Said compound (I) and a pharmaceutically acceptable acid addition salt thereof are useful as cerebral or coronary vasodilators.

摘要翻译： 下式的化合物：其中R 1和R 2各自为低级烷基，R 3为氢，低级烷基或羟基 - 低级烷基，R 4为氢，卤素，低级烷基，低级烷氧基，低级烷硫基或硝基， 并且A是低级亚烷基。 所述化合物（I）及其药学上可接受的酸加成盐可用作脑或冠状血管扩张剂。