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1. 发明授权

US5962448A Pyrroloazepine derivatives 失效
标题翻译：吡咯并氮衍生物
公开(公告)号：US5962448A
公开(公告)日：1999-10-05
申请号：US875495
申请日：1997-08-21
申请人： Akira Mizuno , Makoto Shibata , Tomoe Iwamori , Tetsuo Shimamoto , Kyoko Nakanishi , Norio Inomata
发明人： Akira Mizuno , Makoto Shibata , Tomoe Iwamori , Tetsuo Shimamoto , Kyoko Nakanishi , Norio Inomata
IPC分类号： A61P7/00 , A61P9/00 , C07D207/34 , C07D487/04 , C07D495/20 , A61K31/55
CPC分类号： C07D487/04 , C07D207/34
摘要： A pyrroloazepine compound having the following formula (I): whereinthe ring P represented by ##STR1## is a pyrrole ring having the following structure: ##STR2## wherein R.sub.1 represents C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.4 -C.sub.8 cycloalkyl-alkyl, C.sub.6 -C.sub.14 aryl or C.sub.7 -C.sub.22 aralkyl, which are optionally substituted; and R.sub.2 represents H or C.sub.1 -C.sub.8 alkyl, which is optionally substituted; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z.sub.2 is not present and Z.sub.1 represents H, but, when the bond is absent, Z.sub.1 and Z.sub.2 are both H; Z.sub.1 represents H and Z.sub.2 represents a group OR.sub.3, in which R.sub.3 represents H, C.sub.1 -C.sub.8 alkyl, or C.sub.7 -C.sub.22 aralkyl, which are optionally substituted; Z.sub.1 and Z.sub.2 both represent groups SR.sub.4, in which R.sub.4 represents C.sub.1 -C.sub.8 alkyl or C.sub.7 -C.sub.22 aralkyl, which are optionally substituted; or Z.sub.1 and Z.sub.2 are combined together to represent O, a group NOR.sub.5, in which R.sub.5 represents H, or C.sub.1 -C.sub.8 alkyl or C.sub.2 -C.sub.3 alkylenedithio, which are optionally substituted; A represents alkylene, alkenylene or alkynylene; and Y represents a group in which W is CH, C.dbd. or N, m is for 0 or 1, n is for 1, 2 or 3, G is O, S, C.dbd.O, sulfinyl, sulfonyl, alkylene, alkenylene or acetal; E.sub.1 and E.sub.2 is H or C.sub.1 -C.sub.8 alkyl; and D represents an aromatic hydrocarbon or an aromatic heterocyclic ring. The compound (I) has strong serotonin-2 receptor antagonistic action and low toxicity and less side effects, and is therapeutically useful in the treatment of circulatory diseases and/or conditions related thereto.
摘要翻译： PCT No.PCT / JP96 / 03522 Sec。 371日期1997年8月21日 102（e）日期1997年8月21日PCT提交1996年12月2日PCT公布。出版物WO97 / 20845 日期：1997年6月12日具有下式（I）的吡咯并氮吡啶化合物：其中由代表的环P是具有以下结构的吡咯环：其中R1表示C1-C8烷基，C3-C8环烷基，C4-C8环烷基 - 烷基，任选被取代的C 6 -C 14芳基或C 7 -C 22芳烷基; 并且R 2表示H或被任选取代的C 1 -C 8烷基; 虚线表示存在或不存在键; 当存在键时，Z 2不存在，Z1表示H，但不存在键时，Z 1和Z 2均为H; Z1表示H，Z2表示OR3，其中R3表示H，任选取代的C 1 -C 8烷基或C 7 -C 22芳烷基; Z 1和Z 2均表示SR 4，其中R 4表示任选取代的C 1 -C 8烷基或C 7 -C 22芳烷基; 或Z 1和Z 2组合在一起表示O，其中R 5表示H的基团NOR 5或任选被取代的C 1 -C 8烷基或C 2 -C 3亚烷基二硫基; A表示亚烷基，亚烯基或亚炔基; 并且Y表示W为CH，C =或N的基团，m为0或1，n为1,2或3，G为O，S，C = O，亚磺酰基，磺酰基，亚烷基，亚烯基或亚磺酰基乙缩醛 E1和E2是H或C1-C8烷基; D表示芳族烃或芳香族杂环。化合物（I）具有强的5-羟色胺-2受体拮抗作用和低毒性和较少的副作用，并且在治疗循环系统疾病和/或与之有关的病症中是治疗上有用的。

2. 发明授权

US06713634B2 Pyrroloazepine derivatives 失效
标题翻译：吡咯并氮衍生物
公开(公告)号：US06713634B2
公开(公告)日：2004-03-30
申请号：US10188234
申请日：2002-07-03
申请人： Akira Mizuno , Makoto Shibata , Tomoe Iwamori , Tetsuo Shimamoto , Kyoko Nakanishi , Norio Inomata
发明人： Akira Mizuno , Makoto Shibata , Tomoe Iwamori , Tetsuo Shimamoto , Kyoko Nakanishi , Norio Inomata
IPC分类号： C07D20700
CPC分类号： C07D487/04 , C07D207/34
摘要： A method of effecting serotonin-2-receptor antagonism in a mammal in need thereof, which includes administering to the mammal an effective amount of the compound of the formula (I), or a pharmaceutically acceptable salt thereof: wherein ring P, the dashed line, A, Y, Z1 and Z2 are defined herein.
摘要翻译：一种在有需要的哺乳动物中实现5-羟色胺-2-受体拮抗作用的方法，其包括向哺乳动物施用有效量的式（I）化合物或其药学上可接受的盐：其中环P为虚线 A，Y，Z 1和Z 2在本文中定义。

3. 发明授权

US06258805B1 Pyrroloazepine derivatives 失效
标题翻译：吡咯并氮衍生物
公开(公告)号：US06258805B1
公开(公告)日：2001-07-10
申请号：US09312713
申请日：1999-05-17
申请人： Akira Mizuno , Makoto Shibata , Tomoe Iwamori , Tetsuo Shimamoto , Kyoko Nakanishi , Norio Inomata
发明人： Akira Mizuno , Makoto Shibata , Tomoe Iwamori , Tetsuo Shimamoto , Kyoko Nakanishi , Norio Inomata
IPC分类号： A61K3155
CPC分类号： C07D487/04 , C07D207/34
摘要： A method for treating a circulatory disease or condition in a mammal, which entails administering to the mammal an effective amount of a compound of the formula (I) or a pharmaceutically acceptable salt thereof: wherein the ring P represented by is a pyrrole ring having the following structure: wherein R1 represents C1-C8 alkyl, C3-C8 cycloalkyl, C4-C8 cycloalkyl-alkyl, C6-C14 aryl or C7-C22 aralkyl, which are optionally substituted; and R2 represents H or C1-C8 alkyl, which is optionally substituted; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present and Z1 represents H, but, when the bond is absent, Z1 and Z2 are both H; Z1 represents H and Z2 represents a group OR3, in which R3 represents H, C1-C8 alkyl, or C7-C22 aralkyl, which are optionally substituted; Z1 and Z2 both represent groups SR4, in which R4 represents C1-C8 alkyl or C7-C22 aralkyl, which are optionally substituted; or Z1 and Z2 are combined together to represent O, a group NOR5, in which R5 represents H, or C1-C8 alkyl or C2-C3 alkylenedithio, which are optionally substituted; A represents alkylene, alkenylene or alkynylene; and Y represents a group in which W is CH, C═ or N, m is for 0 or 1, n is for 1, 2 or 3, G is O, S, C═O, sulfinyl, sulfonyl, alkylene, alkenylene or acetal; E1 and E2 is H or C1-C8 alkyl; and D represents an aromatic hydrocarbon or an aromatic heterocyclic ring. The compound (I) has strong serotonin-2 receptor antagonistic action and low toxicity and less side effects, and is therapeutically useful in the treatment of circulatory diseases and/or conditions related thereto.
摘要翻译：一种用于治疗哺乳动物的循环系统疾病或病症的方法，其需要向哺乳动物施用有效量的式（I）化合物或其药学上可接受的盐：其中由表示的环P是具有以下基团的吡咯环结构：其中R 1表示任选取代的C 1 -C 8烷基，C 3 -C 8环烷基，C 4 -C 8环烷基 - 烷基，C 6 -C 14芳基或C 7 -C 22芳烷基; 并且R 2表示H或被任选取代的C 1 -C 8烷基; 虚线表示存在或不存在键; 当存在键时，Z 2不存在，Z1表示H，但不存在键时，Z 1和Z 2均为H; Z1表示H，Z2表示OR3，其中R3表示H，任选取代的C 1 -C 8烷基或C 7 -C 22芳烷基; Z 1和Z 2均表示SR 4，其中R 4表示任选取代的C 1 -C 8烷基或C 7 -C 22芳烷基; 或Z 1和Z 2组合在一起表示O，其中R 5表示H的基团NOR 5或任选被取代的C 1 -C 8烷基或C 2 -C 3亚烷基二硫基; A表示亚烷基，亚烯基或亚炔基; 并且Y表示W为CH，C =或N的基团，m为0或1，n为1,2或3，G为O，S，C = O，亚磺酰基，磺酰基，亚烷基，亚烯基或亚磺酰基乙缩醛 E1和E2是H或C1-C8烷基; D表示芳族烃或芳香族杂环。化合物（I）具有强的5-羟色胺-2受体拮抗作用和低毒性和较少的副作用，并且在治疗循环系统疾病和/或与之有关的病症中是治疗上有用的。

4. 发明授权

US06489473B2 Pyrroloazepine derivatives 失效
标题翻译：吡咯并氮衍生物
公开(公告)号：US06489473B2
公开(公告)日：2002-12-03
申请号：US09801816
申请日：2001-03-09
申请人： Akira Mizuno , Makoto Shibata , Tomoe Iwamori , Tetsuo Shimamoto , Kyoko Nakanishi , Norio Inomata
发明人： Akira Mizuno , Makoto Shibata , Tomoe Iwamori , Tetsuo Shimamoto , Kyoko Nakanishi , Norio Inomata
IPC分类号： C07D48704
CPC分类号： C07D487/04 , C07D207/34
摘要： A method of effecting serotonin-2-receptor antagonism in a mammal in need thereof, which entails administering to the mammal an effective amount of a compound of the formula (I), or a pharmaceutically acceptable salt thereof: wherein ring P, the dashed line, Z1, Z2, A and Y are as defined herein.
摘要翻译：在有需要的哺乳动物中实现5-羟色胺-2-受体拮抗作用的方法，其需要向哺乳动物施用有效量的式（I）化合物或其药学上可接受的盐：其中环P，虚线，Z1，Z2，A和Y如本文所定义。

5. 发明授权

US5874429A Benzothiazine derivative 失效
标题翻译：苯并噻嗪衍生物
公开(公告)号：US5874429A
公开(公告)日：1999-02-23
申请号：US669615
申请日：1996-06-24
申请人： Akira Mizuno , Makoto Shibata , Tomoe Iwamori , Norio Inomata
发明人： Akira Mizuno , Makoto Shibata , Tomoe Iwamori , Norio Inomata
IPC分类号： C07D275/06 , C07D279/02 , C07D417/06 , C07D513/10 , A61K31/54 , C07D279/16
CPC分类号： C07D275/06 , C07D279/02 , C07D417/06 , C07D513/10
摘要： Disclosed are benzothiazine derivatives represented by the following formula (I): ##STR1## The benzothiazine derivatives (I) and their salts according to the present invention have strong serotonin-2 blocking action, have excellent selectivity to this action against .alpha..sub.1 blocking action and have high safety. Accordingly, the present invention has made it possible to provide pharmaceuticals making use of antagonistic action against serotonin-2 receptors, for example, therapeutics for various circulatory diseases such as ischemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.
摘要翻译：公开了由下式（I）表示的苯并噻嗪衍生物：其中根据本发明的苯并噻嗪衍生物（I）及其盐具有强的5-羟色胺-2阻断作用，对α1的这种作用具有优异的选择性阻塞作用，安全性高。因此，本发明使得可以提供利用针对5-羟色胺-2受体的拮抗作用的药物，例如用于各种循环系统疾病如缺血性心脏病，脑血管障碍和周围循环障碍的治疗剂。

6. 发明授权

US6100265A Thiopyran derivatives 失效
标题翻译：噻喃衍生物
公开(公告)号：US6100265A
公开(公告)日：2000-08-08
申请号：US353773
申请日：1999-07-15
申请人： Akira Mizuno , Makoto Shibata , Tomoe Iwamori , Norio Inomata
发明人： Akira Mizuno , Makoto Shibata , Tomoe Iwamori , Norio Inomata
IPC分类号： A61K31/4436 , A61K31/506 , C07D335/06 , C07D409/06 , C07D409/14 , C07D495/04 , C07D495/10 , C07D495/20
CPC分类号： C07D335/06 , C07D495/04 , C07D495/10
摘要： A thiopyran derivative represented by the following formula (I) or (I'), or the salt thereof. ##STR1## wherein A is S or --CH.dbd.CH--; the dotted line indicates that the bond may be either present or absent; Z and Z' are typically ##STR2## L is an ethylene or trimethylene group; Y is CH or N; n is 2; B is a carbonyl group; m is 0 or 1; D is a phenyl group; and E.sub.1 and E.sub.2 are hydrogen atoms. These compounds exhibit a strong serotonin-2 blocking action and highly safe. Some compounds also exhibit an .alpha..sub.1 -blocking action and therefore are useful as an antihypertensive agent with less side effects. Thus, the thiopyran derivatives are useful as drugs for the treatment of circulatory diseases in general such as hypertension, ischemic heart disease, cerebrovascular disturbance, and peripheral circulatory disturbance.
摘要翻译：由下式（I）或（I'）表示的噻喃衍生物或其盐。其中A为S或-CH = CH-; 虚线表示债券可能存在或不存在; Z和Z'通常为L是乙烯或三亚甲基; Y是CH或N; n为2; B是羰基; m为0或1; D是苯基; E1和E2是氢原子。这些化合物表现出强烈的5-羟色胺-2阻断作用和高度安全性。一些化合物还表现出α1-阻断作用，因此可用作具有较少副作用的抗高血压药。因此，噻喃衍生物可用作治疗循环系统疾病的药物，例如高血压，缺血性心脏病，脑血管障碍和外周循环障碍。

7. 发明授权

US06664251B2 Benzothiazine derivative 失效
标题翻译：苯并噻嗪衍生物
公开(公告)号：US06664251B2
公开(公告)日：2003-12-16
申请号：US09955416
申请日：2001-09-19
申请人： Akira Mizuno , Makoto Shibata , Tomoe Iwamori , Norio Inomata
发明人： Akira Mizuno , Makoto Shibata , Tomoe Iwamori , Norio Inomata
IPC分类号： C07D27916
CPC分类号： C07D275/06 , C07D279/02 , C07D417/06 , C07D513/10
摘要： Disclosed are benzothiazine derivatives represented by the following formula (I): wherein the dashed line indicates the presence or absence of a bond; Z represents one of the following groups: in which R1 and R2 individually represent alkyl, aralkyl or the like, R3 represents H, alkyl or the like, R4 represents H, aralkyl or the like, X1, X2 and X3 individually represent O or S, and G represents substituted or unsubstituted ethylene, trimethylene or the like; Q1 and Q2 individually represent H, OH, halogen, alkoxy or the like; A represents alkylene, alkenylene or the like; Y represents CH, C═ or N; when Y is CH, m stands for 0 or 1, n stands for 1 or 2, B represents O, S, carbonyl or the like, when Y is C═, m stands for 1, n stands for 1 or 2, B represents: in which the double bond is linked to Y, R6 represents substituted or unsubstituted aryl or the like; when Y is N, m stands for 0 or 1, n stands for 2 or 3 and B represents carbonyl, sulfonyl or the like, E1 and E2 individually represent H or lower alkyl; and D represents an aromatic hydrocarbon group or an aromatic heterocyclic group; and salts thereof. The benzothiazine derivatives (I) and their salts according to the present invention have strong serotonin-2 blocking action, have excellent selectivity to this action against &agr;1 blocking action and have high safety. Accordingly, the present invention has made it possible to provide pharmaceuticals making use of antagonistic action against serotonin-2 receptors, for example, therapeutics for various circulatory diseases such as ishemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.
摘要翻译：公开了由下式（I）表示的苯并噻嗪衍生物：其中虚线表示存在或不存在键; Z表示以下基团之一：其中R1和R2分别表示烷基，芳烷基等，R3表示H，烷基等，R4表示H，芳烷基等，X1，X2和X3各自表示O或S ，G表示取代或未取代的乙烯，三亚甲基等; Q1和Q2各自表示H，OH，卤素，烷氧基等; A表示亚烷基，亚烯基等; Y表示CH，C =或N; 当Y是CH时，m代表0或1，n代表1或2，B代表O，S，羰基等，当Y是C =，m代表1，n代表1或2，B代表：其中双键与Y连接，R6表示取代或未取代的芳基等; 当Y为N时，m代表0或1，n代表2或3，B代表羰基，磺酰基等，E1和E2分别代表H或低级烷基; D表示芳香族烃基或芳香族杂环基; 其盐。根据本发明的苯并噻嗪衍生物（I）及其盐具有强的5-羟色胺-2阻断作用，对该作用对α1阻断作用具有优异的选择性并具有高安全性。因此，本发明使得可以提供利用针对5-羟色胺-2受体的拮抗作用的药物，例如用于各种循环系统疾病如血液性心脏病，脑血管障碍和外周循环障碍的治疗剂。

8. 发明授权

US5977111A Thiopyran derivatives 失效
公开(公告)号：US5977111A
公开(公告)日：1999-11-02
申请号：US667713
申请日：1996-06-21
申请人： Akira Mizuno , Makoto Shibata , Tomoe Iwamori , Norio Inomata
发明人： Akira Mizuno , Makoto Shibata , Tomoe Iwamori , Norio Inomata
IPC分类号： A61K31/4436 , A61K31/506 , C07D335/06 , C07D409/06 , C07D409/14 , C07D495/04 , C07D495/10 , C07D495/20 , A61K31/495
CPC分类号： C07D335/06 , C07D495/04 , C07D495/10
摘要： A thiopyran derivative represented by the following formula (I) or (I'), or the salt thereof. ##STR1## wherein A is S or --CH.dbd.CH--; the dotted line indicates that the bond may be either present or absent; Z and Z' are typically ##STR2## L is an ethylene or trimethylene group; Y is CH or N; n is 2; B is a carbonyl group; m is 0 or 1; D is a phenyl group; and E.sub.1 and E.sub.2 are hydrogen atoms. These compounds exhibit a strong serotonin-2 blocking action and highly safe. Some compounds also exhibit an .alpha..sub.1 -blocking action and therefore are useful as an antihypertensive agent with less side effects. Thus, the thiopyran derivatives are useful as drugs for the treatment of circulatory diseases in general such as hypertension, ischemic heart disease, cerebrovascular disturbance, and peripheral circulatory disturbance.

9. 发明授权

US06316442B1 Benzothiazine derivative 失效
标题翻译：苯并噻嗪衍生物
公开(公告)号：US06316442B1
公开(公告)日：2001-11-13
申请号：US09379853
申请日：1999-08-24
申请人： Akira Mizuno , Makoto Shibata , Tomoe Iwamori , Norio Inomata
发明人： Akira Mizuno , Makoto Shibata , Tomoe Iwamori , Norio Inomata
IPC分类号： A61K3154
CPC分类号： C07D275/06 , C07D279/02 , C07D417/06 , C07D513/10
摘要： Disclosed are benzothiazine derivatives represented by the following formula (I): wherein the dashed line indicates the presence or absence of a bond; Z represents one of the following groups: in which R1 and R2 individually represent alkyl, aralkyl or the like, R3 represents H, alkyl or the like, R4 represents H, aralkyl or the like, X1, X2 and X3 individually represent O or S, and G represents substituted or unsubstituted ethylene, trimethylene or the like.
摘要翻译：公开了由下式（I）表示的苯并噻嗪衍生物：其中虚线表示存在或不存在键; Z表示以下基团之一：其中R1和R2分别表示烷基，芳烷基等，R3表示H，烷基等，R4表示H，芳烷基等，X1，X2和X3各自表示O或S ，G表示取代或未取代的亚乙基，三亚甲基等。

10. 发明授权

US06294677B1 Thiopyran derivatives 失效
标题翻译：噻喃衍生物
公开(公告)号：US06294677B1
公开(公告)日：2001-09-25
申请号：US09531141
申请日：2000-03-17
申请人： Akira Mizuno , Makoto Shibata , Tomoe Iwamori , Norio Inomata
发明人： Akira Mizuno , Makoto Shibata , Tomoe Iwamori , Norio Inomata
IPC分类号： C07D33506
CPC分类号： C07D335/06 , C07D495/04 , C07D495/10
摘要： An intermediate represented by the following formula (XVIII), wherein A is a sulfur atom or the group —CH═CH—; L is an alkylene group which may be substituted, an alkenylene group which may be substituted, or an alkynylene group which may be substituted; W represents a leaving group selected from the group consisting of a halogen atom, an alkyl sulfonyloxy group, and an aryl sulfonyloxy group, and Z represents the group; (wherein R1 is an alkyl group which may be substituted, an aromatic carbocyclic group which may be substituted, or an aralkyl group which may be substituted, X1, X2, and X3 individually represent an oxygen atom or a sulfur atom, and G represents an ethylene group or a trimethylene group, of which one or more hydrogen atoms of the ethylene group or trimethylene group may be replaced by a halogen atom, alkyl group, aromatic carbocyclic group, aralkyl group, or alkylidene group).
摘要翻译：由下式（XVIII）表示的中间体，其中A为硫原子或基团-CH = CH-; L可以被取代的亚烷基，可被取代的亚烯基或可被取代的亚炔基; W表示选自卤原子，烷基磺酰氧基和芳基磺酰氧基的离去基团，Z表示基团;（其中，R 1为可被取代的烷基，可以具有芳香族碳环基或可被取代的芳烷基，X 1，X 2和X 3分别表示氧原子或硫原子，G表示亚乙基的一个或多个氢原子的亚乙基或三亚甲基或三亚甲基可以被卤素原子，烷基，芳族碳环基，芳烷基或亚烷基取代）。

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