公开(公告)号：US4543354A

公开(公告)日：1985-09-24

申请号：US550423

申请日：1983-11-10

申请人： Toru Nakao ,  Tsuguo Ikebe ,  Tetsuya Tahara ,  Yutaka Maruyama ,  Osamu Yaoka

发明人： Toru Nakao ,  Tsuguo Ikebe ,  Tetsuya Tahara ,  Yutaka Maruyama ,  Osamu Yaoka

IPC分类号： A61K31/47 ,  A61K31/473 ,  A61K31/535 ,  A61P7/04 ,  A61P9/04 ,  A61P9/12 ,  C07D221/10 ,  C07D401/06

CPC分类号： C07D401/06 ,  A61K31/47 ,  C07D221/10

摘要： Benzo[f]quinoline derivatives which are useful as antihypertensive agents and are represented by the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl, R.sup.2 is hydrogen, lower alkyl, hydroxy-lower-alkyl or lower-alkoxy-lower-alkyl, R.sup.3 and R.sup.4 are the same or different and each is hydrogen, lower alkyl, halogen, lower alkoxy, benzyloxy or hydroxy, R.sup.5 and R.sup.6 are the same or different and each is hydrogen, straight or branched alkyl, aralkyl or cycloalkyl, or R.sup.5 and R.sup.6 together with the adjacent nitrogen atom form a heterocycle, and the dotted line in the ring is an optional bond between 1- and 2-positions, and pharmaceutically acceptable acid addition salts thereof.

摘要翻译： 苯并[f]喹啉衍生物，其可用作抗高血压剂并由下式表示：其中R 1为氢或低级烷基，R 2为氢，低级烷基，羟基 - 低级烷基或低级烷氧基 - 低级烷基 R 3和R 4相同或不同，各自为氢，低级烷基，卤素，低级烷氧基，苄氧基或羟基，R 5和R 6相同或不同，各自为氢，直链或支链烷基，芳烷基或环烷基或R5 和R6与相邻的氮原子一起形成杂环，并且环中的虚线是1-位和2-位之间的任选键及其药学上可接受的酸加成盐。

公开(公告)号：US4555510A

公开(公告)日：1985-11-26

申请号：US626837

申请日：1984-06-27

申请人： Kazuhiro Goto ,  Osamu Yaoka ,  Takanori Oe

发明人： Kazuhiro Goto ,  Osamu Yaoka ,  Takanori Oe

IPC分类号： A61K31/44 ,  C07D491/04 ,  A61K31/435

CPC分类号： C07D491/04 ,  A61K31/44

摘要： An agent for the therapy of hypertension, which comprises as an effective component at least one compound selected from the group consisting of 9-chloro-5-oxo-7-(1H-tetrazol-5-yl)-5H-[1]benzopyrano[2,3-b]pyridine, a salt thereof and hydrates thereof.

摘要翻译： PCT No.PCT / JP82 / 00425 Sec。 371日期1984年6月27日第 102（e）日期1984年6月27日PCT提交1982年10月30日PCT公布。 出版物WO84 / 01711 日期：1984年5月10日。用于治疗高血压的药剂，其包含作为有效成分的至少一种选自9-氯-5-氧代-7-（1H-四唑-5-基） - 5H- [1]苯并吡喃并[2,3-b]吡啶，其盐及其水合物。

公开(公告)号：US5021432A

公开(公告)日：1991-06-04

申请号：US340271

申请日：1989-04-19

申请人： Tsutomu Yamanaka ,  Toshio Seki ,  Tohru Nakajima ,  Osamu Yaoka

发明人： Tsutomu Yamanaka ,  Toshio Seki ,  Tohru Nakajima ,  Osamu Yaoka

IPC分类号： C07D311/68 ,  A61K31/35 ,  A61K31/352 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/455 ,  A61K31/50 ,  A61K31/535 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P25/02 ,  C07D311/70 ,  C07D311/96 ,  C07D405/04 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12

CPC分类号： C07D405/12 ,  C07D311/68 ,  C07D407/12

摘要： A benzopyran compound of the general formula (I) ##STR1## wherein A represents --OR.sup.1 or --NH--COR.sup.2 (wherein R.sup.1 represents hydrogen, a lower alkyl, formyl, an alkanoyl, an aroyl or an aralkyl and R.sup.2 represents hydrogen, a lower alkyl, a lower alkoxy, amino, mono- or di-lower alkylamino, an amino-lower alkyl, a hydroxy-lower alkyl, a halo-lower alkyl, a lower alkoxy-lower alkyl, an acyloxy-lower alkyl, a lower alkoxy-carbonyl-lower alkyl, an aryl or a heteroaryl); R.sup.3 represents hydrogen, a lower alkyl, a lower alkoxy, amino, a mono- or di-lower alkylamino, an amino-lower alkyl, a hydroxy-lower alkyl, a halo-lower alkyl, a lower alkoxy-lower alkyl, an acyloxy-lower alkyl, a lower alkoxycarbonyl-lower alkyl, an aryl or a heteroaryl, or R.sup.2 and R.sup.3 combinedly together form an alkylene having 1 to 2 carbon atoms; R.sup.4 and R.sup.5 are the same or different, and respectively represent hydrogen or a lower alkyl, or combinedly together form an alkylene having 2 to 5 carbon atoms; R.sup.6 represents hydroxyl group, formyloxy, an alkanoyloxy, a haloalkanoyloxy, a lower alkoxycarbonyloxy, an aroyloxy, a heteroaroyloxy, carbamoyloxy, a mono- or di-lower alkylcarbamoyloxy and R.sup.7 represents hydrogen, or R.sup.6 and R.sup.7 combinedly together form a bond and X and Y are the same or different, and respectively represent hydrogen, halogen, nitro, cyano, a lower alkyl, a lower alkoxy, a halo-lower alkyl, carboxyl, formyl, and alkanoyl, an aroyl, a halo-alkanoyl, carbamoyl, a lower alkylsulfinyl, an arylsulfinyl, a lower alkylsulfonyl, and arylsulfonyl, sulfonamido or a mono- or di-lower alkylsulfonamido, or their pharmaceutically acceptable salts and its pharmaceutical use.The compounds of the present invention exhibit remarkable and long lasting antihypertensive actions and peripheral vascular relaxant actions and therefore are useful as therapeutic medicines for hypertensive. Since they also display selective coronary vasodilating actions and the duration of actions are very long, they are of use as therapeutic medicines for cardiovascular disturbances such as angina pectoris and cardiac insufficiency.

公开(公告)号：US4258185A

公开(公告)日：1981-03-24

申请号：US139625

申请日：1980-04-14

申请人： Toru Nakao ,  Shinro Setoguchi ,  Osamu Yaoka

发明人： Toru Nakao ,  Shinro Setoguchi ,  Osamu Yaoka

IPC分类号： C07D401/04 ,  A61K31/50

CPC分类号： C07D401/04 ,  Y10S514/822

摘要： Pyridazinone compounds of the formula: ##STR1## wherein A, B, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined hereinafter, and pharmaceutically acceptable acid addition salts thereof are disclosed. They are useful as antithrombotic and antihypertensive drugs.

摘要翻译： 其中A，B，R 1，R 2，R 3，R 4和R 5如下文所定义的下式的哒嗪酮化合物及其药学上可接受的酸加成盐被公开。 它们可用作抗血栓和抗高血压药物。

公开(公告)号：US5318969A

公开(公告)日：1994-06-07

申请号：US897253

申请日：1992-06-11

申请人： Tsutomu Yamanaka ,  Toshio Seki ,  Tohru Nakajima ,  Osamu Yaoka

发明人： Tsutomu Yamanaka ,  Toshio Seki ,  Tohru Nakajima ,  Osamu Yaoka

IPC分类号： C07D311/68 ,  A61K31/35 ,  A61K31/352 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/455 ,  A61K31/50 ,  A61K31/535 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P25/02 ,  C07D311/70 ,  C07D311/96 ,  C07D405/04 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12

CPC分类号： C07D405/12 ,  C07D311/68 ,  C07D407/12

摘要： A benzopyran compound of the general formula (I) ##STR1## wherein A represents --OR.sup.1 or --NH--COR.sup.2 ; R.sup.3 represents hydrogen, a lower alkyl, a lower alkoxy, amino, a mono- or di-lower alkylamino, an amino-lower alkyl, a hydroxy-lower alkyl, a halo-lower alkyl, a lower alkoxy-lower alkyl, an acyloxy-lower alkyl, a lower alkoxycarbonyl-lower alkyl, an aryl or a heteroaryl, or R.sup.2 and R.sup.3 combinedly together form an alkylene having 1 to 2 carbon atoms; R.sup.4 and R.sup.5 are the same or different, and respectively represent hydrogen or a lower alkyl, or combinedly together form an alkylene having 2 to 5 carbon atoms; R.sup.6 represents hydroxyl group, formyloxy, an alkanoyloxy, a haloalkanoyloxy, a lower alkoxycarbonyloxy, an aroyloxy, a heteroaroyloxy, carbamoyloxy, a mono- or di-lower alkylcarbamoyloxy and R.sup.7 represents hydrogen, or R.sup.6 and R.sup.7 combinedly together form a bond and X and Y are the same or different, and respectively represent hydrogen, halogen, nitro, cyano, a lower alkyl, a lower alkoxy, a halo-lower alkyl, carboxyl, formyl, an alkanoyl, an aroyl, a halo-alkanoyl, carbamoyl, a lower alkylsulfinyl, an arylsulfinyl, a lower alkylsulfonyl, an arylsulfonyl, sulfonamido or a mono- or di-lower alkylsulfonamido, or their pharmaceutically acceptable salts and its pharmaceutical use.

摘要翻译： 通式（I）的苯并吡喃化合物其中A表示-OR1或-NH-COR2; R 3表示氢，低级烷基，低级烷氧基，氨基，一或二低级烷基氨基，氨基 - 低级烷基，羟基 - 低级烷基，卤代低级烷基，低级烷氧基 - 低级烷基，酰氧基 低级烷基，低级烷氧基羰基 - 低级烷基，芳基或杂芳基，或R2和R3组合在一起形成具有1至2个碳原子的亚烷基; R4和R5相同或不同，分别表示氢或低级烷基，或者组合在一起形成具有2-5个碳原子的亚烷基; R6表示羟基，甲酰氧基，烷酰氧基，卤代烷酰氧基，低级烷氧基羰氧基，芳酰氧基，杂芳氧基，氨基甲酰氧基，一或二低级烷基氨基甲酰氧基，R7表示氢，或R6和R7组合在一起形成键，X和 Y分别相同或不同，分别表示氢，卤素，硝基，氰基，低级烷基，低级烷氧基，卤代低级烷基，羧基，甲酰基，烷酰基，芳酰基，卤代烷酰基，氨基甲酰基， 低级烷基亚磺酰基，芳基亚磺酰基，低级烷基磺酰基，芳基磺酰基，亚磺酰氨基或单 - 或二 - 低级烷基亚磺酰氨基，或其药学上可接受的盐及其药物用途。

公开(公告)号：US5143936A

公开(公告)日：1992-09-01

申请号：US672657

申请日：1991-03-21

申请人： Tsutomu Yamanaka ,  Toshio Seki ,  Tohru Nakajima ,  Osamu Yaoka

发明人： Tsutomu Yamanaka ,  Toshio Seki ,  Tohru Nakajima ,  Osamu Yaoka

IPC分类号： C07D311/68 ,  A61K31/35 ,  A61K31/352 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/455 ,  A61K31/50 ,  A61K31/535 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P25/02 ,  C07D311/70 ,  C07D311/96 ,  C07D405/04 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12

CPC分类号： C07D405/12 ,  C07D311/68 ,  C07D407/12

摘要： A benzopyran compound of the general formula (I) ##STR1## wherein A represents --OR.sup.1 or --NH--COR.sup.2 (wherein R.sup.1 represents hydrogen, a lower alkyl, formyl, an alkanoyl, an aroyl or an aralkyl and R.sup.2 represents hydrogen, a lower alkyl, a lower alkoxy, amino, mono- or di-lower alkylamino, an amino-lower alkyl, a hydroxy-lower alkyl, a halo-lower alkyl, a lower alkoxy-lower alkyl, an acyloxy-lower alkyl, a lower alkoxycarbonyl-lower alkyl, an aryl or a heteroaryl); R.sup.3 represents hydrogen, a lower alkyl, a lower alkoxy, amino, a mono- or di-lower alkylamino, an amino-lower alkyl, a hydroxy-lower alkyl, a halo-lower alkyl, a lower alkoxy-lower alkyl, an acyloxy-lower alkyl, a lower alkoxycarbonyl-lower alkyl, an aryl or a heteroaryl, or R.sup.2 and R.sup.3 combinedly together form an alkylene having 1 to 2 carbon atoms; R.sup.4 and R.sup.5 are the same or different, and respectively represent hydrogen or a lower alkyl, or combinedly together form an alkylene having 2 to 5 carbon atoms; R.sup.6 represents hydroxyl group, formyloxy, an alkanoyloxy, a haloalkanoyloxy, a lower alkoxycarbonyloxy, an aroyloxy, a heteroaroyloxy, carbamoyloxy, a mono- or di-lower alkycarbamoyloxy and R.sup.7 represents hydrogen, or R.sup.6 and R.sup.7 combinedly together form a bond and X and Y are the same or different, and respectively represent hydrogen, halogen, nitro, cyano, a lower alkyl, a lower alkoxy, a halo-lower alkyl, carboxyl, formyl, an alkanoyl, an aroyl, a halo-alkanoyl, carbamoyl, a lower alkylsulfinyl, an arylsulfinyl, a lower alkylsulfonyl, an arylsulfonyl, sulfonamido or a mono- or di-lower alkylsulfonamido, or their pharmaceutically acceptable salts and its pharmaceutical use.The compounds of the present invention exhibit remarkable and long lasting antihypertensive actions and peripheral vascular relaxant actions and therefore are useful as therapeutic medicines for hypertensive. Since they also display selective coronary vasodilating actions and the duration of actions are very long, they are of use as therapeutic medicines for cardiovascular disturbances such as angina pectoris and cardiac insufficiency.

公开(公告)号：US4882326A

公开(公告)日：1989-11-21

申请号：US197877

申请日：1988-05-24

申请人： Shu Murakami ,  Tsuguo Ikebe ,  Ichiro Hakamada ,  Osamu Yaoka

发明人： Shu Murakami ,  Tsuguo Ikebe ,  Ichiro Hakamada ,  Osamu Yaoka

IPC分类号： A61K31/55 ,  A61K38/00 ,  A61P9/00 ,  A61P9/12 ,  A61P43/00 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07K5/02 ,  C12N9/99

CPC分类号： C07K5/0222 ,  A61K38/00 ,  Y02P20/55

摘要： Piperidine compounds of the formula: ##STR1## or isomers thereof as well as pharmaceutically acceptable salts and/or hydrate forms thereof, and piperidine compounds of the formula: ##STR2## or isomers thereof as well as salt and/or hydrate forms thereof. In the above formulae, A represents a methylene group, an oxygen atom or a sulfur atom; B represents an oxygen atom or a sulfur atom; R.sup.1 and R.sup.2 independently represent a hydrogen atom, a lower alkyl group or an aralkyl group; R.sup.3 represents a hydrogen atom or an amino protecting group; Z represents an amino group or a protected amino group, a hydroxy group, or a reactive atom or group; m represents 1 or 2; and n represents the integer of 0 to 3.Piperidine compounds (I) possess an inhibitory activity against angiotensin-converting enzyme, and exhibit a long lasting hypotensive activity and are useful as antihypertensive agents. Piperidine compounds (II) are useful as intermediates for said piperidine compounds (I).

公开(公告)号：US4874759A

公开(公告)日：1989-10-17

申请号：US261836

申请日：1988-09-23

申请人： Tetsuya Tahara ,  Tsuguo Ikebe ,  Ichiro Hakamada ,  Osamu Yaoka

发明人： Tetsuya Tahara ,  Tsuguo Ikebe ,  Ichiro Hakamada ,  Osamu Yaoka

IPC分类号： C07D209/42 ,  C07D401/12

CPC分类号： C07D401/12 ,  C07D209/42

摘要： Hydroxyindole-3-carboxylic acid amide compounds of the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are, the same or different, respectively a hydrogen atom, an alkyl group, an aryl group, an aralkyl group or a heteroaryl group, or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4 are respectively groups which are combined to each other taken together with the adjacent nitrogen atom to form a heterocyclic group, R.sup.5 is an alkyl group, R.sup.6 is a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group or an aralkyl group and X is a hydrogen atom, a halogen atom or a lower alkanoyl group, or their acid addition salts.These compounds are of use as diuretics or a therapeutic medicine for circulation system diseases.

公开(公告)号：US4709095A

公开(公告)日：1987-11-24

申请号：US853809

申请日：1986-03-25

申请人： Tsutomu Yamanaka ,  Osamu Yaoka

发明人： Tsutomu Yamanaka ,  Osamu Yaoka

IPC分类号： A61K31/15 ,  A61K31/35 ,  A61K31/352 ,  A61K31/47 ,  A61P7/10 ,  A61P9/12 ,  A61P25/04 ,  A61P29/00 ,  C07C67/00 ,  C07C239/00 ,  C07C251/48 ,  C07D215/42 ,  C07D311/68 ,  C07C131/00

CPC分类号： C07D311/68

摘要： Ortho-aminomethylphenol compounds of the formula: ##STR1## wherein X is hydrogen or halogen, R is hydrogen or alkyl having 1 to 4 carbon atoms and A is alkyl having 1 to 4 carbon atoms, phenyl, benzyl or a bivalent radical selected from --(CH.sub.2).sub.3 -- and --O(CH.sub.2).sub.2 -- and joined together with the 3 or 5 position of the benzene nucleus to form a bicycle, or pharmaceutically acceptable salts thereof, a method of preparing said compounds and a pharmaceutical composition containing said compounds, are disclosed.Such compounds exhibit antiinflammatory, analgesic, diuretic and antihypertensive activities, so they are useful in the treatment for diseases caused by inflammation, edema or hypertension.

摘要翻译： PCT No.PCT / JP85 / 00440 Sec。 371日期：1986年3月25日 102（e）日期1986年3月25日PCT提交1985年8月2日PCT公布。 出版物WO86 / 01201 日本：1986年2月27日。下式的邻氨基甲基苯酚化合物：其中X是氢或卤素，R是氢或具有1至4个碳原子的烷基，A是具有1至4个碳原子的烷基，苯基，苄基 或选自 - （CH 2）3 - 和-O（CH 2）2 - 的二价基团并且与苯核的3或5位相连接以形成自行车或其药学上可接受的盐，制备所述化合物的方法 和含有所述化合物的药物组合物。 这些化合物表现出抗炎，止痛，利尿和抗高血压活性，因此它们可用于治疗由炎症，水肿或高血压引起的疾病。

公开(公告)号：US4581355A

公开(公告)日：1986-04-08

申请号：US680727

申请日：1984-12-12

申请人： Tetsuya Tahara ,  Tsuguo Ikebe ,  Yutaka Maruyama ,  Osamu Yaoka ,  Yohji Miura

发明人： Tetsuya Tahara ,  Tsuguo Ikebe ,  Yutaka Maruyama ,  Osamu Yaoka ,  Yohji Miura

IPC分类号： A61K31/40 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/55 ,  A61P9/00 ,  A61P9/04 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P25/28 ,  A61P43/00 ,  C07D401/12 ,  C07D403/12

CPC分类号： C07D401/12 ,  C07D403/12

摘要： 3-Indolecarboxamide compounds of the formula: ##STR1## inclusive of pharmaceutically acceptable acid addition salt and/or hydrate forms thereof, wherein R.sup.1 is hydrogen or C.sub.1-4 alkyl; each of R.sup.2 and R.sup.3 is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, benzyloxy, C.sub.2-6 alkanoyloxy or hydroxy; R.sup.4 is hydrogen or C.sub.1-4 alkyl; R.sup.5 is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or hydroxy; R.sup.6 is hydrogen or C.sub.1-4 alkyl; X is oxygen, sulfur or direct bond; each of k and m is an integer of 1 to 3; and n is 1 or 2, are useful as drug for the prevention and treatment of various circulatory diseases.

摘要翻译： 具有下式的3-吲哚甲酰胺化合物：包括其药学上可接受的酸加成盐和/或其水合物形式，其中R 1是氢或C 1-4烷基; R 2和R 3各自为氢，卤素，C 1-4烷基，C 1-4烷氧基，苄氧基，C 2-6烷酰氧基或羟基; R4是氢或C1-4烷基; R5是氢，卤素，C1-4烷基，C1-4烷氧基或羟基; R6是氢或C1-4烷基; X是氧，硫或直接键; k和m各自为1〜3的整数， 和n为1或2，可用作预防和治疗各种循环系统疾病的药物。