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1. 发明授权

US06525199B1 Arylpiperidinopropanol and arylpiperazinopropanol derivatives and pharmaceuticals containing the same 失效
公开(公告)号：US06525199B1
公开(公告)日：2003-02-25
申请号：US10118045
申请日：2002-04-09
申请人： Hirokazu Annoura , Kyoko Nakanishi , Shigeki Tamura
发明人： Hirokazu Annoura , Kyoko Nakanishi , Shigeki Tamura
IPC分类号： C07D295033
CPC分类号： C07D295/088 , C07C217/84 , C07C271/28 , C07D211/22 , C07D211/52 , C07D295/13 , Y02P20/55
摘要： A compound having the formula (I) or its salt, hydrate, hydrate salt or solvate: wherein R1 to R4 independently represent H, halogen, OH, alkoxy, optionally substituted alkyl, aryl, or aralkyl group, R5 represents H, optionally substituted alkyl, aryl, or aralkyl group, E1 represents O, S, or —NR6, where R6 represents H, an optionally substituted alkyl, aryl, or aralkyl group, E2 represents O, S, or —NR7, where R7 represents H, an optionally substituted alkyl, aryl, or aralkyl group, A represents CH, C(OH), or N, X represents H, halogen, alkoxy, or an optionally substituted alkyl group, and Q represents an optionally substituted phenyl group, phenoxy, phenylmethyl, or cycloalkyloxy group, where when E1 represents O or S, E2 does not represent O or S, which has an action of suppressing the cytotoxic Ca2+ overload and lipid peroxidation and effective for pharmaceutical preparation for the alleviation and treatment of symptoms due to ischemic diseases, etc.

2. 发明授权

US07642262B2 Arylipiperdinopropanol and arylipiperazinopropanol derivatives and pharmaceuticals containing the same 失效
标题翻译：芳基哌啶丙醇和芳基哌嗪丙醇衍生物和含有它们的药物
公开(公告)号：US07642262B2
公开(公告)日：2010-01-05
申请号：US11002793
申请日：2004-12-03
申请人： Hirokazu Annoura , Kyoko Nakanishi , Shigeki Tamura
发明人： Hirokazu Annoura , Kyoko Nakanishi , Shigeki Tamura
IPC分类号： A61K31/495 , C07D295/135
CPC分类号： C07D295/088 , C07C217/84 , C07C271/28 , C07D211/22 , C07D211/52 , C07D295/13 , Y02P20/55
摘要： A compound having the formula (I) or its salt, hydrate, hydrate salt or solvate: wherein R1 to R4 independently represent H, halogen, OH, alkoxy, optionally substituted alkyl, aryl, or aralkyl group, R5 represents H, optionally substituted alkyl, aryl, or aralkyl group, E1 represents O, S, or —NR6, where R6 represents H, an optionally substituted alkyl, aryl, or aralkyl group, E2 represents O, S, or —NR7, where R7 represents H, an optionally substituted alkyl, aryl, or aralkyl group, A represents CH, C(OH), or N, X represents H, halogen, alkoxy, or an optionally substituted alkyl group, and Q represents an optionally substituted phenyl group, phenoxy, phenylmethyl, or cycloalkyloxy group, where when E1 represents O or S, E2 does not represent O or S, which has an action of suppressing the cytotoxic Ca2+ overload and lipid peroxidation and effective for pharmaceutical preparation for the alleviation and treatment of symptoms due to ischemic diseases, etc.
摘要翻译：具有式（I）的化合物或其盐，水合物，水合物盐或溶剂合物：其中R 1至R 4独立地表示H，卤素，OH，烷氧基，任选取代的烷基，芳基或芳烷基，R 5表示H，任选取代的烷基，芳基或芳烷基，E1表示O，S或-NR6，其中R6表示H，任选取代的烷基，芳基或芳烷基，E2表示O，S或-NR7，其中R7表示H，取代的烷基，芳基或芳烷基，A表示CH，C（OH）或N，X表示H，卤素，烷氧基或任选取代的烷基，Q表示任选取代的苯基，苯氧基，苯甲基或环状烷氧基，当E1表示O或S时，E2不表示O或S，其具有抑制细胞毒性Ca 2+过载和脂质过氧化的作用，并且有效用于缓解和治疗由于缺血性疾病引起的症状的药物制剂等。

3. 发明授权

US06706734B2 Arylpiperidinol and arylpiperidine derivatives and pharmaceuticals containing the same 失效
标题翻译：芳基哌啶醇和芳基哌啶衍生物和含有它们的药物
公开(公告)号：US06706734B2
公开(公告)日：2004-03-16
申请号：US10196362
申请日：2002-07-17
申请人： Hirokazu Annoura , Kyoko Nakanishi , Shigeki Tamura
发明人： Hirokazu Annoura , Kyoko Nakanishi , Shigeki Tamura
IPC分类号： A61K314465
CPC分类号： C07D211/44 , C07D211/12 , C07D211/14 , C07D211/18 , C07D211/52 , C07D211/70
摘要： A pharmaceutical composition, especially a pharmaceutical composition for the alleviation or treatment of symptoms due to ischemic diseases and symptoms derived from seizures, epilepsy, and migraine, and a Ca2+ overload suppressant, containing an arylpiperidinol or arylpiperidine derivative having the formula (I): wherein, R is H, an optionally substituted phenyl, an optionally substituted phenoxy, or an optionally substituted benzoyl, A is a connecting bond, a cycloalkylene, or an alkenylene optionally substituted with a lower alkyl, B is an alkylene optionally substituted with OH or an alkoxy or —NHCO(CH2)n— where n is an integer of 1 to 5, E is a connecting bond, O, or a methylene, X is OH or H provided that when E is O or a methylene, X is not H, and Y and Z are independently H, a halogen, an alkoxy, or an alkyl optionally substituted with a halogen.
摘要翻译：一种药物组合物，特别是用于缓解或治疗由缺血性疾病引起的症状和由癫痫发作，癫痫和偏头痛引起的症状的药物组合物，以及包含具有下式的芳基哌啶醇或芳基哌啶衍生物的Ca 2+过量抑制剂 I）：其中R为H，任选取代的苯基，任选取代的苯氧基或任选取代的苯甲酰基，A为任选被低级烷基取代的连接键，亚环烷基或亚烯基，B为任选取代的亚烷基与OH或烷氧基或-NHCO（CH 2）n - ，其中n为1至5的整数，E为连接键，O或亚甲基，X为OH或H，条件是当E为O或亚甲基时， X不为H，Y和Z独立地为H，卤素，烷氧基或任选被卤素取代的烷基。

4. 发明授权

US06838470B2 Arylpiperidinopropanol and arylpiprazinopropanol derivatives and pharmaceuticals containing the same 失效
标题翻译：芳基哌啶丙醇和芳基哌嗪丙醇衍生物和含有它们的药物
公开(公告)号：US06838470B2
公开(公告)日：2005-01-04
申请号：US10331508
申请日：2002-12-31
申请人： Hirokazu Annoura , Kyoko Nakanishi , Shigeki Tamura
发明人： Hirokazu Annoura , Kyoko Nakanishi , Shigeki Tamura
IPC分类号： A61P25/04 , A61K31/451 , A61K31/495 , A61P3/10 , A61P9/10 , A61P25/28 , C07C217/84 , C07C271/28 , C07D211/18 , C07D211/22 , C07D211/52 , C07D295/08 , C07D295/092 , C07D295/13 , C07D295/135
CPC分类号： C07D295/088 , C07C217/84 , C07C271/28 , C07D211/22 , C07D211/52 , C07D295/13 , Y02P20/55
摘要： A compound having the formula (I) or its salt, hydrate, hydrate salt or solvate: wherein R1 to R4 independently represent H, halogen, OH, alkoxy, optionally substituted alkyl, aryl, or aralkyl group, R5 represents H, optionally substituted alkyl, aryl, or aralkyl group, E1 represents O, S, or —NR6, where R6 represents H, an optionally substituted alkyl, aryl, or aralkyl group, E2 represents O, S, or —NR7, where R7 represents H, an optionally substituted alkyl, aryl, or aralkyl group, A represents CH, C(OH), or N, X represents H, halogen, alkoxy, or an optionally substituted alkyl group, and Q represents an optionally substituted phenyl group, phenoxy, phenylmethyl, or cycloalkyloxy group, where when E1 represents O or S, E2 does not represent O or S, which has an action of suppressing the cytotoxic Ca2+ overload and lipid peroxidation and effective for pharmaceutical preparation for the alleviation and treatment of symptoms due to ischemic diseases, etc.
摘要翻译：具有式（I）的化合物或其盐，水合物，水合物盐或溶剂化物：其中R 1至R 4独立地表示H，卤素，OH，烷氧基，任选取代的烷基，芳基或芳烷基，R 代表H，任选取代的烷基，芳基或芳烷基，E 1表示O，S或-NR 6，其中R 6表示H，任选取代的烷基，芳基或芳烷基，E 2表示O，S或-NR 7，其中R 7表示H，任选取代的烷基，芳基或芳烷基，A表示CH，C（OH）或N，X表示 H，卤素，烷氧基或任选取代的烷基，Q表示任选取代的苯基，苯氧基，苯甲基或环烷氧基，其中当E 1表示O或S时，E 2不表示O或 S具有抑制细胞毒性Ca 2+过载和脂质过氧化的作用，并且对于由于缺血性疾病等引起的症状缓解和治疗药物制剂有效。

5. 发明授权

US06455549B1 Arylpiperidinol and arylpiperidine derivatives and drugs containing the same 失效
标题翻译：芳基哌啶醇和芳基哌啶衍生物和含有相同的药物
公开(公告)号：US06455549B1
公开(公告)日：2002-09-24
申请号：US09043563
申请日：1998-03-20
申请人： Hirokazu Annoura , Kyoko Nakanishi , Shigeki Tamura
发明人： Hirokazu Annoura , Kyoko Nakanishi , Shigeki Tamura
IPC分类号： A61K31445
CPC分类号： C07D211/44 , C07D211/12 , C07D211/14 , C07D211/18 , C07D211/52 , C07D211/70
摘要： A pharmaceutical composition, especially a pharmaceutical composition for the alleviation or treatment of symptoms due to ischemic diseases and symptoms derived from seizures, epilepsy, and migraine, and a Ca2+ overload suppressant, containing an arylpiperidinol or arylpiperidine derivative having the formula (I): wherein, R is H, an optionally substituted phenyl, an optionally substituted phenoxy, or an optionally substituted benzoyl, A is a connecting bond, a cycloalkylene, or an alkenylene optionally substituted with a lower alkyl, B is an alkylene optionally substituted with OH or an alkoxy or —NHCO(CH2)n— where n is an integer of 1 to 5, E is a connecting bond, O, or a methylene, X is OH or H provided that when E is O or a methylene, X is not H, and Y and Z are independently H, a halogen, an alkoxy, or an alkyl optionally substituted with a halogen.
摘要翻译：一种药物组合物，特别是用于缓解或治疗由于缺血性疾病引起的症状和由癫痫发作，癫痫和偏头痛引起的症状的药物组合物和含有具有式（I）的芳基哌啶醇或芳基哌啶衍生物的Ca2 +过量抑制剂：其中 R是H，任意取代的苯基，任意取代的苯氧基或任选取代的苯甲酰基，A是任选被低级烷基取代的连接键，亚环烷基或亚烯基，B是任选被OH取代的亚烷基或烷氧基或-NHCO（CH 2）n - ，其中n为1至5的整数，E为连接键，O或亚甲基，X为OH或H，条件是当E为O或亚甲基时，X不为H ，Y和Z独立地为H，卤素，烷氧基或任选被卤素取代的烷基。

6. 发明授权

US07498344B2 Arylpiperidinol and arylpiperidine derivatives and pharmaceuticals containing the same 失效
标题翻译：芳基哌啶醇和芳基哌啶衍生物和含有它们的药物
公开(公告)号：US07498344B2
公开(公告)日：2009-03-03
申请号：US10799681
申请日：2004-03-15
申请人： Hirokazu Annoura , Kyoko Nakanishi , Shigeki Tamura
发明人： Hirokazu Annoura , Kyoko Nakanishi , Shigeki Tamura
IPC分类号： A61K31/4465 , C07D211/22 , C07D211/40
CPC分类号： C07D211/44 , C07D211/12 , C07D211/14 , C07D211/18 , C07D211/52 , C07D211/70
摘要： A pharmaceutical composition, especially a pharmaceutical composition for the alleviation or treatment of symptoms due to ischemic diseases and symptoms derived from seizures, epilepsy, and migraine, and a Ca2+ overload suppressant, containing an arylpiperidinol or arylpiperidine derivative having the formula (I): wherein, R is H, an optionally substituted phenyl, an optionally substituted phenoxy, or an optionally substituted benzoyl, A is a connecting bond, a cycloalkylene, or an alkenylene optionally substituted with a lower alkyl, B is an alkylene optionally substituted with OH or an alkoxy or —NHCO(CH2)n— where n is an integer of 1 to 5, E is a connecting bond, O, or a methylene, X is OH or H provided that when E is O or a methylene, X is not H, and Y and Z are independently H, a halogen, an alkoxy, or an alkyl optionally substituted with a halogen.
摘要翻译：一种药物组合物，特别是用于缓解或治疗由于缺血性疾病引起的症状和由癫痫发作，癫痫和偏头痛引起的症状的药物组合物和含有具有式（I）的芳基哌啶醇或芳基哌啶衍生物的Ca2 +过量抑制剂：其中 R是H，任意取代的苯基，任意取代的苯氧基或任选取代的苯甲酰基，A是任选被低级烷基取代的连接键，亚环烷基或亚烯基，B是任选被OH取代的亚烷基或烷氧基或-NHCO（CH 2）n - ，其中n为1至5的整数，E为连接键，O或亚甲基，X为OH或H，条件是当E为O或亚甲基时，X不为H ，Y和Z独立地为H，卤素，烷氧基或任选被卤素取代的烷基。

7. 发明申请

US20050101610A1 Arylipiperdinopropanol and arylipiperazinopropanol derivatives and pharmaceuticals containing the same 失效
标题翻译：芳基哌啶丙醇和芳基哌嗪丙醇衍生物和含有它们的药物
公开(公告)号：US20050101610A1
公开(公告)日：2005-05-12
申请号：US11002793
申请日：2004-12-03
申请人： Hirokazu Annoura , Kyoko Nakanishi , Shigeki Tamura
发明人： Hirokazu Annoura , Kyoko Nakanishi , Shigeki Tamura
IPC分类号： A61P25/04 , A61K31/451 , A61K31/495 , A61P3/10 , A61P9/10 , A61P25/28 , C07C217/84 , C07C271/28 , C07D211/18 , C07D211/22 , C07D211/52 , C07D295/08 , C07D295/092 , C07D295/13 , A61K31/445 , C07D211/20 , C07D241/04
CPC分类号： C07D295/088 , C07C217/84 , C07C271/28 , C07D211/22 , C07D211/52 , C07D295/13 , Y02P20/55
摘要： A compound having the formula (I) or its salt, hydrate, hydrate salt or solvate: wherein R1 to R4 independently represent H, halogen, OH, alkoxy, optionally substituted alkyl, aryl, or aralkyl group, R5 represents H, optionally substituted alkyl, aryl, or aralkyl group, E1 represents O, S, or —NR6, where R6 represents H, an optionally substituted alkyl, aryl, or aralkyl group, E2 represents O, S, or —NR7, where R7 represents H, an optionally substituted alkyl, aryl, or aralkyl group, A represents CH, C(OH), or N, X represents H, halogen, alkoxy, or an optionally substituted alkyl group, and Q represents an optionally substituted phenyl group, phenoxy, phenylmethyl, or cycloalkyloxy group, where when E1 represents O or S, E2 does not represent O or S, which has an action of suppressing the cytotoxic Ca2+ overload and lipid peroxidation and effective for pharmaceutical preparation for the alleviation and treatment of symptoms due to ischemic diseases, etc.
摘要翻译：具有式（I）的化合物或其盐，水合物，水合物盐或溶剂合物：其中R 1至R 4独立地表示H，卤素，OH，烷氧基，任选地取代的烷基，芳基或芳烷基，R 5表示H，任选取代的烷基，芳基或芳烷基，E 1表示O，S或-NR > 6，其中R 6表示H，任选取代的烷基，芳基或芳烷基，E 2表示O，S或-NR

8. 发明授权

US06407099B1 Arylpiperidinopropanol and arylpiperazinopropanol derivatives and pharmaceuticals containing the same 失效
标题翻译：芳基哌啶丙醇和芳基哌嗪丙醇衍生物和含有它们的药物
公开(公告)号：US06407099B1
公开(公告)日：2002-06-18
申请号：US09331712
申请日：1999-06-25
申请人： Hirokazu Annoura , Kyoko Nakanishi , Shigeki Tamura
发明人： Hirokazu Annoura , Kyoko Nakanishi , Shigeki Tamura
IPC分类号： A61K31495
CPC分类号： C07D295/088 , C07C217/84 , C07C271/28 , C07D211/22 , C07D211/52 , C07D295/13 , Y02P20/55
摘要： A compound having the formula (I) or its salt, hydrate, hydrate salt or solvate: wherein R1 to R4 independently represent H, halogen, OH, alkoxy, optionally substituted alkyl, aryl, or aralkyl group, R5 represents H, optionally substituted alkyl, aryl, or aralkyl group, E1 represents O, S, or —NR6, where R6 represents H, an optionally substituted alkyl, aryl, or aralkyl group, E2 represents O, S, or —NR7, where R7 represents H, an optionally substituted alkyl, aryl, or aralkyl group, A represents CH, C(OH), or N, X represents H, halogen, alkoxy, or an optionally substituted alkyl group, and Q represents an optionally substituted phenyl group, phenoxy, phenylmethyl, or cycloalkyloxy group, where when E1 represents O or S, E2 does not represent O or S, which has an action of suppressing the cytotoxic Ca2+ overload and lipid peroxidation and effective for pharmaceutical preparation for the alleviation and treatment of symptoms due to ischemic diseases, etc.
摘要翻译：具有式（I）的化合物或其盐，水合物，水合物盐或溶剂合物：其中R 1至R 4独立地表示H，卤素，OH，烷氧基，任选取代的烷基，芳基或芳烷基，R 5表示H，任选取代的烷基，芳基或芳烷基，E1表示O，S或-NR6，其中R6表示H，任选取代的烷基，芳基或芳烷基，E2表示O，S或-NR7，其中R7表示H，取代的烷基，芳基或芳烷基，A表示CH，C（OH）或N，X表示H，卤素，烷氧基或任选取代的烷基，Q表示任选取代的苯基，苯氧基，苯甲基或环状烷氧基，当E1表示O或S时，E2不表示O或S，其具有抑制细胞毒性Ca 2+过载和脂质过氧化的作用，并且有效用于缓解和治疗由于缺血性疾病引起的症状的药物制剂等。

9. 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。

10. 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。

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