T-TYPE CALCIUM CHANNEL BLOCKER
    2.
    发明申请
    T-TYPE CALCIUM CHANNEL BLOCKER 审中-公开
    T型钙通道阻塞器

    公开(公告)号:US20100105636A1

    公开(公告)日:2010-04-29

    申请号:US12651849

    申请日:2010-01-04

    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。

    T-type calcium channel blocker
    3.
    发明申请
    T-type calcium channel blocker 审中-公开
    T型钙通道阻滞剂

    公开(公告)号:US20070129335A1

    公开(公告)日:2007-06-07

    申请号:US10580532

    申请日:2004-11-25

    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 ,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。

    Substituted benzopyran derivatives against arrhythmia
    4.
    发明授权
    Substituted benzopyran derivatives against arrhythmia 失效
    取代苯并吡喃衍生物抗心律失常

    公开(公告)号:US07041700B2

    公开(公告)日:2006-05-09

    申请号:US10479118

    申请日:2002-06-17

    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

    4-oxybenzopyran derivative
    6.
    发明授权
    4-oxybenzopyran derivative 失效
    4-羟基苯并吡喃衍生物

    公开(公告)号:US06677371B1

    公开(公告)日:2004-01-13

    申请号:US10069002

    申请日:2002-03-29

    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。

    Benzopyran derivative
    7.
    发明授权
    Benzopyran derivative 失效
    苯并吡喃衍生物

    公开(公告)号:US06589983B1

    公开(公告)日:2003-07-08

    申请号:US10048026

    申请日:2002-03-29

    IPC分类号: A61K335

    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。

    4-aminobenzopyran derivatives
    8.
    发明授权
    4-aminobenzopyran derivatives 失效
    4-氨基苯并吡喃衍生物

    公开(公告)号:US06809114B2

    公开(公告)日:2004-10-26

    申请号:US10466175

    申请日:2003-07-14

    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。

    4-oxybenzopyran derivative
    9.
    发明授权
    4-oxybenzopyran derivative 失效
    4-羟基苯并吡喃衍生物

    公开(公告)号:US06555574B1

    公开(公告)日:2003-04-29

    申请号:US10049996

    申请日:2002-03-29

    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。

    Chroman derivatives
    10.
    发明授权
    Chroman derivatives 失效
    色原衍生物

    公开(公告)号:US6066631A

    公开(公告)日:2000-05-23

    申请号:US232645

    申请日:1999-01-19

    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。