4-oxybenzopyran derivative
    1.
    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
    2.
    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。

    Benzimidazole compound
    6.
    发明授权
    Benzimidazole compound 失效
    苯并咪唑化合物

    公开(公告)号:US6114369A

    公开(公告)日:2000-09-05

    申请号:US403763

    申请日:1999-11-01

    CPC分类号: C07D235/14 C07D235/30

    摘要: A benzimidazole derivative of the formula (I) or its salt: wherein A is a single bond or a C.sub.1-2 alkylene group (this alkylene group may optionally be substituted by a C.sub.1-4 alkyl group), R.sup.6 is a C.sub.1-4 alkyl group (this alkyl group may optionally be substituted by a phenyl group), B is a C.sub.2-3 alkylene group (this alkylene group may optionally be substituted by a C.sub.1-4 alkyl group), X is an oxygen atom, a sulfur atom or NR.sup.7 (wherein R.sup.7 is a nitro group, a cyano group or a C.sub.1-4 alkoxy group), each of R.sup.1 and R.sup.2 which are independent of each other, is a hydrogen atom, a halogen atom, a C.sub.1-4 alkyl group or a C.sub.1-4 alkoxy group, E is a C.sub.1-2 alkylene group (this alkylene group may optionally be substituted by a C.sub.1-4 alkyl group), R.sup.3 is a phenyl group (this phenyl group may optionally be substituted by a halogen atom, a C.sub.1-4 alkyl group or a C.sub.1-4 alkoxy group), a C.sub.1-4 alkoxy group or a benzyloxy group, each of R.sup.4 and R.sup.5 which are independent of each other, is a C.sub.1-4 alkyl group (this alkyl group may optionally be substituted by a phenyl group), D is a C.sub.1-2 alkylene group (this alkylene group may optionally be substituted by a C.sub.1-4 alkyl group), and Ar is a phenyl group.

    摘要翻译: PCT No.PCT / JP98 / 01986 Sec。 371日期:1999年11月1日 102(e)1999年11月1日PCT 1998年4月30日PCT PCT。 WO98 / 50368 PCT出版物 日期:1998年11月12日一种式(I)的苯并咪唑衍生物或其盐:其中A为单键或C1-2亚烷基(该亚烷基可任选被C 1-4烷基取代),R 6为 C 1-4烷基(该烷基可以任选被苯基取代),B是C2-3亚烷基(该亚烷基可以任选被C 1-4烷基取代),X是氧原子 ,硫原子或NR 7(其中R 7为硝基,氰基或C 1-4烷氧基),R 1和R 2各自独立地为氢原子,卤素原子,C1- 4烷基或C 1-4烷氧基,E是C1-2亚烷基(该亚烷基可以任选被C 1-4烷基取代),R 3是苯基(该苯基可以任选地被 卤素原子,C 1-4烷基或C 1-4烷氧基),C 1-4烷氧基或苄氧基,R 4和R 5各自独立地为C 1-4烷基( t 其烷基可任选被苯基取代),D为C1-2亚烷基(该亚烷基可任选被C 1-4烷基取代),Ar为苯基。

    Organic bismuth derivatives for X-ray imaging
    7.
    发明授权
    Organic bismuth derivatives for X-ray imaging 失效
    有机铋衍生物用于X射线成像

    公开(公告)号:US5939045A

    公开(公告)日:1999-08-17

    申请号:US860320

    申请日:1997-07-18

    IPC分类号: A61K49/04 C07F9/94

    CPC分类号: C07F9/94 A61K49/04 Y10S424/90

    摘要: An organic bismuth derivative represented by formula (I) or its salt: �wherein X.sup.1 is YNR.sup.1 R.sup.2 (wherein Y is --SO.sub.2 -- or --C(O)--, R.sup.1 is a C.sub.3-6 alkyl group which have from 2 to 5 hydroxyl groups which may be protected, and R.sup.2 is a hydrogen atom, a C.sub.1-6 alkyl group or a C.sub.1-5 acyl group which may have from 1 to 5 hydroxyl groups which may be protected, or R.sup.1 and R.sup.2, together with each other, represent a C.sub.2-6 cyclic alkylene which may have from 1 to 4 hydroxyl groups which may be protected), and each of X.sup.2 and X.sup.3 is, independently of each other, a hydrogen atom, a C.sub.1-4 alkyl group, a C.sub.1-4 alkoxy group, a C.sub.1-4 alkylsulfonyl group, a C.sub.1-4 alkylcarbonyl group, a nitro group, a cyano group or the same as defined for X.sup.1 !.

    摘要翻译: PCT No.PCT / JP95 / 02551 Sec。 371日期1997年7月18日 102(e)1997年7月18日PCT 1995年12月13日PCT PCT。 WO96 / 19487 PCT出版物 日期:1996年6月27日由式(I)表示的有机铋衍生物或其盐:[其中X1为YNR1R2(其中Y为-SO2-或-C(O) - ,R1为C3-6烷基, 2〜5个可被保护的羟基,R2是氢原子,可以具有1〜5个可被保护的羟基的C1-6烷基或C1-5酰基,或者R1和R2一起 彼此表示可以具有1〜4个可被保护的羟基的C 2-6环状亚烷基,X2和X3各自独立地为氢原子,C1-4烷基, C 1-4烷氧基,C 1-4烷基磺酰基,C 1-4烷基羰基,硝基,氰基或与X 1所定义的相同]。

    Agent for prophylaxis and treatment of thromboxane A.sub.2 -mediated
diseases
    9.
    发明授权
    Agent for prophylaxis and treatment of thromboxane A.sub.2 -mediated diseases 失效
    用于预防和治疗血栓素A2介导的疾病的药剂

    公开(公告)号:US5798357A

    公开(公告)日:1998-08-25

    申请号:US687604

    申请日:1996-08-08

    CPC分类号: A61K31/501 A61K31/50

    摘要: An agent for the prophylaxis or treatment of TXA.sub.2 -mediated diseases, particularly, a TXA.sub.2 synthetase inhibitor, which comprises a pyridazinone compound of the formula (I) ##STR1## wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof as an active ingredient. The pyridazinone compound (I) and pharmacologically acceptable salts thereof used in the present invention have prophylactic and therapeutic activities against TXA.sub.2 -mediated diseases, particularly a TXA.sub.2 synthetase inhibitory action and are useful as an agent for the prophylaxis or treatment of TXA.sub.2 -mediated diseases, particularly as TXA.sub.2 synthetase inhibitors.

    摘要翻译: PCT No.PCT / JP95 / 00244 Sec。 371日期:1996年8月8日 102(e)日期1996年8月8日PCT提交1995年2月20日PCT公布。 第WO95 / 22329号公报 日期1995年8月24日用于预防或治疗TXA2介导的疾病的药剂,特别是TXA2合成酶抑制剂,其包含式(I)的哒嗪酮化合物(I)其中每个符号如 说明书或其药理学上可接受的盐作为活性成分。 用于本发明的哒嗪酮化合物(I)及其药理学上可接受的盐具有抗TXA2介导的疾病,特别是TXA2合成酶抑制作用的预防和治疗活性,可用作预防或治疗TXA2介导的疾病, 特别是作为TXA2合成酶抑制剂。