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公开(公告)号：US06555574B1
公开(公告)日：2003-04-29
申请号：US10049996
申请日：2002-03-29
申请人： Keizo Tanikawa , Kazuhiko Ohrai , Kazufumi Yanagihara , Yukihiro Shigeta , Toru Tsukagoshi , Toru Yamashita
发明人： Keizo Tanikawa , Kazuhiko Ohrai , Kazufumi Yanagihara , Yukihiro Shigeta , Toru Tsukagoshi , Toru Yamashita
IPC分类号： A61K3135
CPC分类号： C07D405/12 , C07D311/22
摘要： This invention relates to a 4-oxybenzopyran derivative of formula (I) wherein, R1 and R2 represent each independently a hydrogen atom, a C1-6 alkyl group or a phenyl group; R3 represents a hydroxyl group or a C1-6 alkylcarbonyloxy group; R4 represents a hydrogen atom, a C3-6 cycloalkyl group, a C1-6 alkyl group, a C1-6 alkylcarbonyl group, a C1-6 alkylaminocarbonyl group, a di-C1-6 alkylaminocarbonyl group, an aryl group or a heteroaryl group; n represents an integer of 0-4; X represents —C(═O)NR7—, —NR8—, —NHC(═O)NH— or —S(O)2NH—; R5 represents a hydrogen atom or (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), or (l); R6 represents a hydrogen atom, a halogen atom, a nitro group or a cyano group; or a pharmaceutically acceptable salt thereof. And this invention also relates to an antiarrhythmic agent having the prolongation effect of the functional refractory period comprising said compound or a pharmaceutically acceptable salt thereof as an active ingredient.
摘要翻译： 本发明涉及式（I）的4-氧代苯并吡喃衍生物，其中R1和R2各自独立地表示氢原子，C1-6烷基或苯基; R3表示羟基或C1-6烷基羰基氧基; R 4表示氢原子，C 3-6环烷基，C 1-6烷基，C 1-6烷基羰基，C 1-6烷基氨基羰基，二-C 1-6烷基氨基羰基，芳基或杂芳基 ; n表示0-4的整数; X表示-C（= O）NR 7 - ， - NR 8 - ， - NHC（= O）NH-或-S（O）2 NH-; R5代表氢原子或（a），（b），（c），（d），（e），（f），（g），（h），（i），（j），（k） 或（l）; R6表示氢原子，卤素原子，硝基或氰基; 或其药学上可接受的盐。 本发明还涉及具有作为活性成分的所述化合物或其药学上可接受的盐的具有功能性不应期的延长作用的抗心律失常药。
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公开(公告)号：US06677371B1
公开(公告)日：2004-01-13
申请号：US10069002
申请日：2002-03-29
申请人： Keizo Tanikawa , Kazuhiko Ohrai , Kazufumi Yanagihara , Yukihiro Shigeta , Toru Tsukagoshi , Toru Yamashita
发明人： Keizo Tanikawa , Kazuhiko Ohrai , Kazufumi Yanagihara , Yukihiro Shigeta , Toru Tsukagoshi , Toru Yamashita
IPC分类号： A61K3135
CPC分类号： C07D311/22
摘要： This invention relates to a 4-oxybenzopyran derivative of formula (I) wherein, R1 and R2 represent each independently a hydrogen atom, a C1-6 alkyl group or a phenyl group; R3 represents a hydroxyl group or C1-6 alkylcarbonyloxy group; R4 represents a hydrogen atom, a C3-6 cycloalkyl group, a C1-6 alkyl group, a C1-6 alkylcarbonyl group, a C1-6 alkylaminocarbonyl group, a di-C1-6 alkylaminocarbonyl group, an aryl group or a heteroaryl group; R5 represents a hydrogen atom or a C1-6 alkyl group; X is absent or represents C═O or SO2; R6 represents a hydrogen atom, a C1-6 alkyl group or a C3-6 cycloalkyl group; R7 represents a hydrogen atom, a halogen atom, a nitro group or a cyano group; or a pharmaceutically acceptable salt thereof. And this invention also relates to a drug for treating arrhytmia having the prolongation effect on the functional refractory period comprising said compound or a pharmaceutically acceptable salt thereof as an active ingredient.
摘要翻译： 本发明涉及式（I）的4-氧代苯并吡喃衍生物，其中R 1和R 2各自独立地表示氢原子，C 1-6烷基或苯基; R 3表示羟基或C 1-6烷基羰基氧基; R 4表示氢原子，C 3-6环烷基，C 1-6烷基，C 1-6烷基羰基，C 1-6烷基氨基羰基，二-C 1-6烷基氨基羰基，芳基或 杂芳基; R 5表示氢原子或C 1-6烷基; X不存在或表示C = O或SO 2; R 6表示氢原子，C 1-6烷基或C 3-6环烷基; R 7表示氢原子，卤素原子，硝基或氰基; 或其药学上可接受的盐。 本发明还涉及一种用于治疗对包含所述化合物或其药学上可接受的盐作为活性成分的具有对功能不应期的延长作用的心律的药物。
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公开(公告)号：US06589983B1
公开(公告)日：2003-07-08
申请号：US10048026
申请日：2002-03-29
申请人： Keizo Tanikawa , Kazuhiko Ohrai , Kazufumi Yanagihara , Yukihiro Shigeta , Toru Tsukagoshi , Toru Yamashita
发明人： Keizo Tanikawa , Kazuhiko Ohrai , Kazufumi Yanagihara , Yukihiro Shigeta , Toru Tsukagoshi , Toru Yamashita
IPC分类号： A61K335
CPC分类号： C07D405/12 , C07D311/68 , C07D311/70
摘要： This invention relates a benzopyran denvative of formula (I) wherein, R1 and R2 represent each independently a hydrogen atom, a (substituted)C1-6 alkyl group or a (substituted)phenyl group,R3 represents a hydroxyl group or C1-6 alkylcarbonyloxy group, R4 represents a hydrogen atom, or R3 and R4 together form a bond, m represents an integer of 0-4, n represents an integer of 0-4, Y is absent, or represents CR11R12 in which R11 and R12 represent each independently a hydrogen atom or a C1-6 alkyl group, R5 represents an aryl group or a (substituted)heteroaryl group,R6 represents a hydrogen atom or a C1-6 alkyl group,R7 represents a hydrogen atom or a C1-6 alkyl group,X is absent, or represents C=O or SO2, R8 represents a hydrogen atom, a (substituted)C1-6 alkyl group or C3-6 cycloalkyl group, and R9 represents a nitro group, etc., or a pharmaceutically acceptable salt thereof. And this invention also relates an antiarrhythmic agent having the prolongation effect on the functional refractory period comprising said compound or a pharmaceutically acceptable salt thereof as an active ingredient.
摘要翻译： 本发明涉及式（I）的苯并吡喃类抗坏血酸，其中R1和R2各自独立地表示氢原子，（取代的）C1-6烷基或（取代的）苯基，R3表示羟基或C1-6烷基羰氧基 基团，R4表示氢原子，或R3和R4一起形成键，m表示0-4的整数，n表示0-4的整数，Y不存在，或表示其中R 11和R 12各自独立地表示的CR 11 R 12 氢原子或C1-6烷基，R5表示芳基或（取代）杂芳基，R6表示氢原子或C1-6烷基，R7表示氢原子或C1-6烷基， X不存在，或表示C = O或SO 2，R 8表示氢原子，（取代的）C 1-6烷基或C 3-6环烷基，R 9表示硝基等，或其药学上可接受的盐 。 本发明还涉及具有作为活性成分的所述化合物或其药学上可接受的盐具有对功能不应期的延长作用的抗心律失常药。
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公开(公告)号：US07041700B2
公开(公告)日：2006-05-09
申请号：US10479118
申请日：2002-06-17
申请人： Yoshio Ohara , Kazuhiko Ohrai , Kazufumi Yanagihara , Yukihiro Shigeta , Toru Tsukagoshi , Toru Yamashita
发明人： Yoshio Ohara , Kazuhiko Ohrai , Kazufumi Yanagihara , Yukihiro Shigeta , Toru Tsukagoshi , Toru Yamashita
IPC分类号： A61K31/35
CPC分类号： C07D311/68
摘要： This invention relates to benzopyran derivatives of the formula (1) or the formula (2) wherein R1 and R2 represent independently of each other hydrogen atom or C1-6alkyl group, R3 represents hydroxyl group or C1-6 alkylcarbonyloxy group, R4 represents hydrogen atom or C1-6 alkyl group, R5 represents C1-6 alkyl group substituted with C6-14 aryl group or heteroaryl group, R6 represents C1-6 alkyl group, C1-6 alkoxy group, halogen atom, nitro group, C(O)NH2, C(O)NHR8 or C(O)NR8R9, or pharmaceutically acceptable salts thereof. These compounds are useful as an antiarrhythmic agent
摘要翻译： 本发明涉及式（1）或式（2）的苯并吡喃衍生物，其中R 1和R 2各自独立地表示氢原子或C 1-6个烷基，R 3表示羟基或C 1-6烷基羰基氧基，R 4表示氢原子或 C 1-6烷基，R 5表示被C 6-14烷基取代的C 1-6烷基。 芳基或杂芳基，R 6表示C 1-6烷基，C 1-6烷氧基，卤素原子，硝基， C（O）NH 2，C（O）NHR 8或C（O）NR 8 R 9， ，或其药学上可接受的盐。 这些化合物可用作抗心律失常药
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公开(公告)号：US06809114B2
公开(公告)日：2004-10-26
申请号：US10466175
申请日：2003-07-14
申请人： Yoshio Ohara , Kazuhiko Ohrai , Kazufumi Yanagihara , Yukihiro Shigeta , Toru Tsukagoshi , Toru Yamashita
发明人： Yoshio Ohara , Kazuhiko Ohrai , Kazufumi Yanagihara , Yukihiro Shigeta , Toru Tsukagoshi , Toru Yamashita
IPC分类号： A61K31335
CPC分类号： C07D311/72 , C07D311/70
摘要： This invention relates to benzopyran derivatives of the formula (I) wherein, R1 and R2 represent each independently a C1-6alkyl group, etc, R3 represents a hydroxyl group, etc, R4 represents a hydrogen atom, etc, R6 represents a hydrogen atom, R7 represents a hydrogen atom, etc, X is absent, or represents C═O, etc, R8 represents a hydrogen atom, a C1-6alkyl group, etc, R9 represents a hydrogen atom or a nitro group, when R9 represents a nitro group, Y represents a C4-8alkylene group, —(CH2)m—CR11R12—(CH2)n— or —(CH2)o—O—(CH2)p—, R5 represents a hydrogen atom, an amino group, a C1-6alkoxy group, a C1-6alkylthio group, a C1-6alkylamino group, a C1-6 alkoxycarbonylamino group, etc, or pharmaceutically acceptable salts thereof. These compounds are useful as an antiarrhythmic agent.
摘要翻译： 本发明涉及式（I）的苯并吡喃衍生物，其中R 1和R 2各自独立地为C 1-6烷基等，R 3表示羟基等，R 4表示 氢原子等，R 6表示氢原子，R 7表示氢原子等，X不存在，或表示C = O等，R 8表示氢原子，C1- 6烷基等，当R 9表示硝基时，R 9表示氢原子或硝基，Y表示C4-8亚烷基， - （CH2）m-CR11R12 - （CH 2）n - 或 - （CH 2）o O-（CH 2）p - ，R 5表示氢原子，氨基，C 1-6烷氧基，C 1-6烷硫基，C 1-6烷基氨基， C 1-6烷氧基羰基氨基等，或其药学上可接受的盐。 这些化合物可用作抗心律失常药。
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公开(公告)号：US20070299130A1
公开(公告)日：2007-12-27
申请号：US10590207
申请日：2005-02-25
IPC分类号： A61K31/352 , A61P9/00 , C07D311/00
CPC分类号： C07D311/68 , C07D311/72
摘要： This invention relates to benzopyran compounds of formula (I) wherein X is NR6, Y is a bond, SO or SO2, Z is C1-4alkyl group or phenyl group, W is hydrogen atom, hydroxy group, C1-6 alkoxy group, a halogen atom, C1-4alkyl group or C1-6alkylsulfonylamino group, R1 and R2 are independently of each other C1-3alkyl group, R3 is hydrogen atom, hydroxy group or methoxy group, m is an integer of 0 to 4, n is an integer of 0 to 4, V is a single bond, CR7R8, NR9, O, S, SO or SO2, R4 is hydrogen atom or C1-6alkyl group, R5 is hydrogen atom, C1-6alkyl group, C3-8cycloalkyl group, C3-8cycloalkenyl group, C6-14aryl group or C2-9heteroaryl group. These compounds are useful as an anti-arrhythmic agent.
摘要翻译： 本发明涉及式（I）的苯并吡喃化合物，其中X为NR 6，Y为键，SO或SO 2，Z为C 1-4 烷基或苯基，W是氢原子，羟基，C 1-6烷氧基，卤素原子，C 1-4烷基或 C 1-6烷基磺酰基氨基，R 1和R 2彼此独立地为C 1-3烷基 基团R 3为氢原子，羟基或甲氧基，m为0〜4的整数，n为0〜4的整数，V为单键，CR 7 R 9，R 9，O，S，SO或SO 2，R 4是 氢原子或C 1-6烷基，R 5是氢原子，C 1-6烷基，C 3〜C 6烷基， 8个环烷基，C 3〜8个环烯基，C 6-14芳基或C 2-9杂芳基。 这些化合物可用作抗心律不齐剂。
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公开(公告)号：US07781483B2
公开(公告)日：2010-08-24
申请号：US10590207
申请日：2005-02-25
IPC分类号： A61K31/353 , C07D311/68 , C07D311/70
CPC分类号： C07D311/68 , C07D311/72
摘要： This invention relates to benzopyran compounds of formula (I) wherein X is NR6, Y is a bond, SO or SO2, Z is C1-4alkyl group or phenyl group, W is hydrogen atom, hydroxy group, C1-6 alkoxy group, a halogen atom, C1-4alkyl group or C1-6alkylsulfonylamino group, R1 and R2 are independently of each other C1-3alkyl group, R3 is hydrogen atom, hydroxy group or methoxy group, m is an integer of 0 to 4, n is an integer of 0 to 4, V is a single bond, CR7R8, NR9, O, S, SO or SO2, R4 is hydrogen atom or C1-6alkyl group, R5 is hydrogen atom, C1-6alkyl group, C3-8cycloalkyl group, C3-8cycloalkenyl group, C6-14aryl group or C2-9heteroaryl group. These compounds are useful as an anti-arrhythmic agent.
摘要翻译： 本发明涉及式（I）的苯并吡喃化合物，其中X为NR6，Y为键，SO或SO2，Z为C1-4烷基或苯基，W为氢原子，羟基，C1-6烷氧基， 卤素原子，C 1-4烷基或C 1-6烷基磺酰基氨基，R 1和R 2彼此独立地为C 1-3烷基，R 3为氢原子，羟基或甲氧基，m为0〜4的整数，n为整数 0〜4，V为单键，CR7R8，NR9，O，S，SO或SO2，R4为氢原子或C1-6烷基，R5为氢原子，C1-6烷基，C3-8环烷基，C3- 8环烯基，C6-14芳基或C2-9杂芳基。 这些化合物可用作抗心律不齐剂。
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