Oxazinobenzazole compounds
    2.
    发明授权
    Oxazinobenzazole compounds 失效
    恶嗪环唑化合物

    公开(公告)号:US5278158A

    公开(公告)日:1994-01-11

    申请号:US837252

    申请日:1992-02-14

    CPC分类号: C07D513/04

    摘要: Oxazinobenzazole derivatives represented by the formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each independently represents a hydrogen atom or a lower alkyl group; R.sup.5 and R.sup.6 jointly form, in conjunction with the two adjacent carbon atoms, a substituted or unsubstituted 5- or 6-membered heterocyclic ring having at least two nitrogen atoms and optionally having one or more heteroatom(s) selected from the group consisting of an oxygen atom, a sulphur atom and a nitrogen atom; and m is an integer of 0 or 1, and pharmaceutically acceptable salts thereof. The compounds of the present invention are useful as antispasmodic medicaments.

    摘要翻译: 由式(I)表示的恶唑烷基恶唑衍生物:(*化学结构*)(I)其中R 1,R 2,R 3和R 4可以相同或不同,各自独立地表示氢原子或低级烷基; R 5和R 6与两个相邻的碳原子一起形成取代或未取代的具有至少两个氮原子且任选具有一个或多个选自以下的杂原子的取代或未取代的5-或6-元杂环: 氧原子,硫原子和氮原子; 和m为0或1的整数,及其药学上可接受的盐。 本发明的化合物可用作解痉药物。

    Substituted tetrahydroisoquinoline compounds, and process for producing
them, and composition containing them
    3.
    发明授权
    Substituted tetrahydroisoquinoline compounds, and process for producing them, and composition containing them 失效
    取代的四氢异喹啉化合物及其制备方法和含有它们的组合物

    公开(公告)号:US4966904A

    公开(公告)日:1990-10-30

    申请号:US320975

    申请日:1989-03-09

    摘要: A compound of the formula (I) or its salt and a process for producing the compounds; The compounds have the effect to dilate neophrovascular tracts; ##STR1## Wherein ##STR2## represents the formula ##STR3## (wherein R.sup.4 is a hydrogen atom or lower alkylsulfonyl); R.sup.1 is hydrogen, lower alkyl, hydroxyl, halogen, amino, or lower acylamino;R.sup.2 is hydrogen, lower alkyl, hydroxyl, amino, or lower alkylsulfonylamino;R.sup.3 is hydrogen, lower alkyl, or hydroxyl;R is hydrogen or halogen;with the proviso that when R.sup.1 is hydroxyl, there is no case that all of R.sup.2, R.sup.3 and R are hydrogens, and further with the proviso that when R is hydrogen, A excludes ##STR4## or a salt therof.

    摘要翻译: 式(I)化合物或其盐及其制备方法; 该化合物具有扩张新生血管束的作用; (I)其中代表式(IMAGE)(其中R4是氢原子或低级烷基磺酰基); R1是氢,低级烷基,羟基,卤素,氨基或低级酰基氨基; R2是氢,低级烷基,羟基,氨基或低级烷基磺酰基氨基; R3是氢,低级烷基或羟基; R是氢或卤素; 条件是当R 1是羟基时,不存在所有的R 2,R 3和R都是氢的情况,并且进一步条件是当R是氢时,A不包括囟素或盐。

    Substituted tetrahydroisoquinoline compounds, and process for producing
them, and composition containing them
    4.
    发明授权
    Substituted tetrahydroisoquinoline compounds, and process for producing them, and composition containing them 失效
    取代的四氢异喹啉化合物及其制备方法和含有它们的组合物

    公开(公告)号:US5623074A

    公开(公告)日:1997-04-22

    申请号:US269733

    申请日:1994-06-30

    摘要: A compound of the formula (I) or its salt and a process for producing the compounds; The compounds have the effect to dilate neophrovascular tracts; ##STR1## Wherein ##STR2## represents the formula ##STR3## (wherein R.sup.4 is a hydrogen atom or lower alkylsulfonyl); R.sup.1 is hydrogen, lower alkyl, hydroxyl, halogen, amino, or lower acylamino;R.sup.2 is hydrogen, lower alkyl, hydroxyl, amino, or lower alkylsulfonylamino;R.sup.3 is hydrogen, lower alkyl, or hydroxyl;R is hydrogen or halogen;with the proviso that when R.sup.1 is hydroxyl, there is no case that all of R.sup.2, R.sup.3 and R are hydrogens, and further with the proviso that when R is hydrogen, A excludes ##STR4## or a salt thereof.

    摘要翻译: 式(I)化合物或其盐及其制备方法; 该化合物具有扩张新生血管束的作用; 式(IMA)(其中R4是氢原子或低级烷基磺酰基); R1是氢,低级烷基,羟基,卤素,氨基或低级酰基氨基; R2是氢,低级烷基,羟基,氨基或低级烷基磺酰基氨基; R3是氢,低级烷基或羟基; R是氢或卤素; 条件是当R 1是羟基时,不存在所有的R 2,R 3和R都是氢的情况,并且进一步条件是当R是氢时,A不包括它们或其盐。

    Arylethenesulfonamide derivatives and drug composition containing the
same
    9.
    发明授权
    Arylethenesulfonamide derivatives and drug composition containing the same 失效
    芳香磺酰胺衍生物和含有相同的药物组合物

    公开(公告)号:US6083955A

    公开(公告)日:2000-07-04

    申请号:US91524

    申请日:1998-06-19

    摘要: Novel arylethenesulfonamide derivative having a high affinity for drugs, especially endoserine receptors, and represented by general formula (I); pharmaceutically acceptable salts thereof; and drugs comprising the same as the active ingredient, especially endoserine receptor antagonist, whereinAr: optionally substituted aryl group or optionally substituted five- to six-membered heteroaryl group;X: oxygen atom, sulfur atom or a group represented by a formula --NH--;Y: oxygen atom or sulfur atom;R.sub.1 : hydrogen atom, optionally halogen-substituted lower alkyl group, cycloalkyl group, optionally substituted aryl group or optionally substituted five- to six-membered heteroaryl group.R.sub.2 : lower alkyl group, lower alkenyl group or lower alkynyl group where each of which may be substituted with one to three substituent(s) selected from a group consisting of hydroxyl group, lower alkoxy group, cycloalkyl group, halogen atom, carboxyl group and lower alkoxycarbonyl group;R.sub.3 : phenyl group which may be substituted with one to four substituent(s) selected from a group consisting of optionally halogen-substituted lower alkyl group, lower alkoxy group, halogen atom, lower alkylthio group, lower alkylsulfinyl group, lower alkanesulfonyl group, carboxyl group, lower alkoxycarbonyl group and carbamoyl group; andR.sub.4 and R.sub.5 : they may be same or different and each is hydrogen atom or lower alkyl.

    摘要翻译: PCT No.PCT / JP96 / 03701 Sec。 371日期:1998年6月19日 102(e)1998年6月19日PCT 1996年12月19日PCT PCT。 公开号WO97 / 22595 日期:1996年6月26日由通式(I)表示的对药物特别是内丝胞受体具有高亲和力的新型芳酰基磺酰胺衍生物; 其药学上可接受的盐; 和包含与活性成分相同的药物,特别是内丝氨酸受体拮抗剂,其中Ar:任选取代的芳基或任选取代的五至六元杂芳基; X:氧原子,硫原子或式-NH-表示的基团; Y:氧原子或硫原子; R1:氢原子,任选卤素取代的低级烷基,环烷基,任选取代的芳基或任选取代的五至六元杂芳基。 R2:低级烷基,低级烯基或低级炔基,其中每个可被一至三个选自羟基,低级烷氧基,环烷基,卤素原子,羧基和 低级烷氧基羰基; R3:可被一至四个选自任选卤素取代的低级烷基,低级烷氧基,卤素原子,低级烷硫基,低级烷基亚磺酰基,低级链烷磺酰基,羧基的取代基取代的苯基 低级烷氧基羰基和氨基甲酰基; 和R 4和R 5:它们可以相同或不同,各自为氢原子或低级烷基。