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公开(公告)号:US5919806A
公开(公告)日:1999-07-06
申请号:US530252
申请日:1995-09-29
申请人: Kiyotomo Seto , Hiroo Matsumoto , Yoshimasa Kamikawaji , Kazuhiko Ohrai , Toru Yamashita , Yukinori Masuda
发明人: Kiyotomo Seto , Hiroo Matsumoto , Yoshimasa Kamikawaji , Kazuhiko Ohrai , Toru Yamashita , Yukinori Masuda
IPC分类号: A61K31/41 , A61K31/4178 , A61K31/4192 , A61K31/422 , A61K31/4245 , A61K31/433 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5355 , A61K31/5377 , A61P9/04 , C07D491/04 , C07D491/052 , C07D498/04 , C07D513/04 , A61K31/37
CPC分类号: C07D491/04 , A61K31/4178 , A61K31/4192 , A61K31/422 , A61K31/4245 , A61K31/433 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5355 , A61K31/5377 , C07D513/04
摘要: Disclosed are cardiotonic medicines containing, as the active ingredient, at least one of compounds of formula (I) and their pharmacologically acceptable salts when they form salts. ##STR1## wherein X.sup.1 and X.sup.2 do not exist or represents an oxygen atom; A represents OH or a C.sub.1 -C.sub.4 acyloxy group; B represents a hydrogen atom or may form a chemical bond along with A; X is an oxygen atom, nitrogen, sulfur, etc.; R.sup.1 and R.sup.2 each represents a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, etc.; R.sup.3 and R.sup.4 each represents a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, etc., or they may together form a 1,4-butylene or 1,5-pentylene group. The compounds have a strong activity of reinforcing the contraction of cardiac muscles and a strong activity of reducing the rate of heart beats. As they are not toxic, they are useful as cardiotonic medicines.
摘要翻译: PCT No.PCT / JP94 / 00544 Sec。 371 1995年9月29日第 102(e)1995年9月29日PCT PCT 1994年4月1日PCT公布。 第WO94 / 22442号公报 日期1994年10月13日被公开是强心药,当它们形成盐时,含有作为活性成分的至少一种式(I)化合物及其药理学上可接受的盐。 其中X1和X2不存在或表示氧原子; A表示OH或C1-C4酰氧基; B代表氢原子或与A形成化学键; X是氧原子,氮,硫等; R1和R2各自表示氢原子,C1-C4烷基等; R3和R4各自表示氢原子,C1-C4烷基等,或者它们可以一起形成1,4-亚丁基或1,5-亚戊基。 这些化合物具有强化心肌收缩的强烈活性和降低心脏搏动速率的强烈活性。 因为它们没有毒性,它们可用作强心药物。
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公开(公告)号:US20100105636A1
公开(公告)日:2010-04-29
申请号:US12651849
申请日:2010-01-04
IPC分类号: A61K31/675 , A61K31/551 , A61K31/4545
CPC分类号: A61K31/675
摘要: There is provided a T-type calcium channel blocker that is a compound of formula (1), a pharmaceutically acceptable salt thereof or a solvate thereof: wherein Ar1 is phenyl group, pyridyl group, furyl group or 2,1,3-benzoxadiazol-4-yl group; nitrogen-containing hetero ring moiety is 1,4-dihydropyridine ring or pyridine ring; Z is a group of formula (2) or CO2R2; Ra and Rb are independently of each other C1-6alkyl group, ANR8R9, CH2OANR8R9, or the like; in case where the nitrogen-containing hetero ring moiety is 1,4-dihydropyridine ring, R1 is C1-6alkyl group, ANR8R9, AN(CH2CH2)2NR8, AN(CH2CH2)2O, AOR8 or benzyl group; R3 is hydrogen atom, C1-20alkyl group, ANR8R9, a group of formula or the like.
摘要翻译: 提供了式(1)化合物,其药学上可接受的盐或其溶剂化物的T型钙通道阻断剂:其中Ar1是苯基,吡啶基,呋喃基或2,1,3-苯并恶二唑-2-基, 4-基; 含氮杂环部分为1,4-二氢吡啶环或吡啶环; Z是式(2)或CO 2 R 2的基团; R a和R b彼此独立地为C 1-6烷基,ANR 8 R 9,CH 2 OANR 8 R 9等; 在含氮杂环部分为1,4-二氢吡啶环的情况下,R 1为C 1-6烷基,ANR 8 R 9,AN(CH 2 CH 2)2 NR 8,AN(CH 2 CH 2)2 O,AOR 8或苄基; R3是氢原子,C1-20烷基,ANR8R9,式等基团。
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公开(公告)号:US20070129335A1
公开(公告)日:2007-06-07
申请号:US10580532
申请日:2004-11-25
IPC分类号: A61K31/675 , A61K31/551 , A61K31/496 , A61K31/455 , A61K31/4439 , C07D403/02
CPC分类号: A61K31/675
摘要: There is provided a T-type calcium channel blocker that is a compound of formula (1), a pharmaceutically acceptable salt thereof or a solvate thereof. wherein Ar1 is phenyl group, pyridyl group, furyl group or 2,1,3-benzoxadiazol-4-yl group; nitrogen-containing hetero ring moiety is 1,4-dihydropyridine ring or pyridine ring; Z is a group of formula (2) or CO2R2; Ra and Rb are independently of each other C1-6alkyl group, ANR8R9, CH2OANR8R9, or the like; in case where the nitrogen-containing hetero ring moiety is 1,4-dihydropyridine ring, R1 is C1-6alkyl group, ANR8R9, AN(CH2CH2)2NR8, AN(CH2CH2)2O, AOR8 or benzyl group; R3 is hydrogen atom, C1-20alkyl group, ANR8R9, a group of formula or the like.
摘要翻译: 提供了一种T型钙通道阻断剂,其是式(1)的化合物,其药学上可接受的盐或其溶剂化物。 其中Ar 1是苯基,吡啶基,呋喃基或2,1,3-苯并二唑-4-基; 含氮杂环部分为1,4-二氢吡啶环或吡啶环; Z是式(2)或CO 2 R 2的基团; R a a和R b彼此独立地是C 1-6烷基,ANR 8 R 12 > 9 SUP>,CH 2,OANR 8,9,9等等; 在含氮杂环部分为1,4-二氢吡啶环的情况下,R 1为C 1-6烷基,ANR 8 O AN(CH 2 CH 2 CH 2)2 NR 8,其中R 1,R 2, AN(CH 2 CH 2)2 O,AOR 8或苄基; R 3是氢原子,C 1-20烷基,ANR 8 R 9,式 或类似物。
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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:US06486178B1
公开(公告)日:2002-11-26
申请号:US09701281
申请日:2000-11-28
申请人: Keizo Tanikawa , Kazuhiko Ohrai , Masayuki Sato , Kazufumi Yanagihara , Yukihiro Shigeta , Toru Yamashita
发明人: Keizo Tanikawa , Kazuhiko Ohrai , Masayuki Sato , Kazufumi Yanagihara , Yukihiro Shigeta , Toru Yamashita
IPC分类号: A61K314418
CPC分类号: C07D207/335 , C07C233/44 , C07C233/55 , C07C235/34 , C07C235/38 , C07C235/78 , C07C237/20 , C07C237/22 , C07C255/57 , C07C255/60 , C07C261/04 , C07C275/40 , C07C275/42 , C07C2601/02 , C07C2602/08 , C07D207/337 , C07D209/14 , C07D209/18 , C07D213/38 , C07D213/40 , C07D213/56 , C07D239/26 , C07D295/135 , C07D303/36 , C07D303/38 , C07D303/40 , C07D303/46 , C07D307/52 , C07D307/54 , C07D333/20 , C07D333/24
摘要: The present invention provides medicines for treating cardiac insufficiency which contain as an active ingredient indane derivatives of formula (I) wherein R1 represents hydrogen atom, nitro group, cyano group, C1-6 alkylcarbonylamino, R2 and R3 each independently represent C1-6 alkyl group, R4 represents hydroxyl group or C1-6 alkylcarbonyloxy group or represents a bond or oxygen atom together with R5, R5 represents hydrogen atom or represents a bond or oxygen atom together with R4, R6 represents hydrogen atom, hydroxyl group or NR7R8, n means 0 or an integer of 1 to 4, X represents C═O, CH2, SO2 or NR16, Y represents NR17 when X is C═O, CH2 or SO2 and represents C═O when X is NR16, Z is absent when Y represents NR17 or represents NR18 when Y is C═O, W represents aromatic groups or lactam rings, or pharmaceutically acceptable salt thereof.
摘要翻译: 本发明提供了治疗心功能不全的药物,其含有作为活性成分的式(I)的二氢化茚衍生物,其中R 1表示氢原子,硝基,氰基,C 1-6烷基羰基氨基,R 2和R 3各自独立地表示C 1-6烷基 R 4表示羟基或C 1-6烷基羰基氧基,或表示键或氧原子连同R 5,R 5表示氢原子,或表示键或氧原子与R 4,R 6表示氢原子,羟基或NR 7 R 8,n表示0 或1〜4的整数,X表示C = O,CH2,SO2或NR16,当X为C = O,CH2或SO2时,Y表示NR17,当X为NR16时,表示C = O,当Y表示NR17时Z不存在 或当Y为C = O时表示NR18,W表示芳族基团或内酰胺环,或其药学上可接受的盐。
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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: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: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:US6066631A
公开(公告)日:2000-05-23
申请号:US232645
申请日:1999-01-19
IPC分类号: C07D311/68 , C07D311/70 , C07D405/04 , C07D405/12 , C07D407/12 , C07D409/12 , C07F7/18 , A61K31/352 , C07D251/00 , C07D405/00 , C07D401/00
CPC分类号: C07D405/04 , C07D311/70 , C07D405/12 , C07D407/12 , C07D409/12 , C07F7/1856
摘要: The present invention relates to chroman derivatives of the formula (I): ##STR1## [wherin R.sup.1 represents a hydrogen atom, a halogen atom, a C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a C.sub.3-6 alkoxymethyl group, etc., R.sup.3 and R.sup.4 each independently represent a hydrogen atom, a C.sub.1-6 alkyl group, etc., R.sup.5 represents a hydroxyl group or a C.sub.1-6 alkylcarbonyloxyl group or forms a bond together with R.sup.5, R.sup.6 represents a hydrogen atom or forms a bond together with R.sup.5, R.sup.7 and R.sup.8 each independently represent a hydrogen atom, a C.sub.1-6 alkyl group, a C.sub.3-6 cycloalkyl group, a phenyl group, etc. n is 0 or an integer of 1, 2, 3 or 4, W represents a phenyl group, etc., X represents C.dbd.O, CH.sub.2, SO.sub.2, etc., Y represents NR.sup.17 (in which R.sup.17 represents a hydrogen atom, a C.sub.1-4 alkyl group, a phenyl group, etc.), etc., Z does not exist or represents CH.sub.2 or NR.sup.18 (R.sup.18 represents a hydrogen atom, a C.sub.1-4 alkyl group, or a phenyl group, etc.)] or their salts.
摘要翻译: 本发明涉及式(I)的苯并二氢吡喃衍生物:其中R1表示氢原子,卤素原子,C1-6烷基,C1-6烷氧基,C3-6烷氧基甲基等, R 3和R 4各自独立地表示氢原子,C 1-6烷基等,R 5表示羟基或C 1-6烷基羰氧基,或与R 5一起形成键,R 6表示氢原子或者一起形成键 R5,R7和R8各自独立地表示氢原子,C1-6烷基,C3-6环烷基,苯基等,n为0或1,2,3或4的整数,W表示 苯基等,X表示C = O,CH 2,SO 2等,Y表示NR 17(其中R 17表示氢原子,C 1-4烷基,苯基等)等, Z不存在或表示CH2或NR18(R18表示氢原子,C1-4烷基或苯基等)]或其盐。
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