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    • 3. 发明授权
    • Serotonin 5-HT3 receptor partial activator
    • 5-羟色胺5-HT3受体部分激活剂
    • US06333328B1
    • 2001-12-25
    • US09686759
    • 2000-10-12
    • Yasuo SatoMegumi YamadaKazuko KobayashiKatsuyoshi IwamatsuFukio KonnoKoichi Shudo
    • Yasuo SatoMegumi YamadaKazuko KobayashiKatsuyoshi IwamatsuFukio KonnoKoichi Shudo
    • A61K31495
    • C07D263/58A61K31/496C07D263/30C07D413/04
    • This invention provides a serotonin 5-HT3 receptor partial activator which has a serotonin 5-HT3 receptor activating action, in addition to its serotonin 5-HT3 receptor antagonism, and does not cause constipation as a side effect. Particularly, based on the finding that newly synthesized benzoxazole derivatives typified by the compounds of the following formula (2) have strong serotonin 5-HT3 receptor antagonism and serotonin 5-HT3 receptor activating action, this invention provides these benzoxazole derivatives as serotonin 5-HT3 receptor partial activators. In the above formula, R1 to R4 may be the same or different from one another and each represents a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkenyl group or a substituted or unsubstituted amino group, or two groups of R1 and R2 may be linked together to form a ring structure, namely benzene ring; R5 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or a substituted or unsubstituted lower alkenyl group; and m is an integer of 1 to 4.
    • 本发明提供除5-羟色胺5-HT 3受体拮抗作用之外还具有5-羟色胺5-HT 3受体激活作用的5-羟色胺5-HT 3受体部分活化剂,并且不引起便秘作为副作用。特别地,基于以下发现: 以下式(2)化合物为代表的新合成苯并恶唑衍生物具有强烈的5-羟色胺5-HT 3受体拮抗作用和5-羟色胺5-HT 3受体激活作用,本发明提供了这些苯并恶唑衍生物作为5-羟色胺5-HT 3受体部分激活因子。 式中,R 1〜R 4可以相同或不同,表示氢原子,卤素原子,取代或未取代的低级烷基,取代或未取代的低级烯基或取代或未取代的氨基,或二 R1和R2的基团可以连接在一起形成环结构,即苯环; R5表示氢原子,取代或未取代的低级烷基或取代或未取代的低级烯基; m为1〜4的整数。
    • 5. 发明授权
    • Serotonin 5-HT3 receptor partial activator
    • 5-羟色胺5-HT3受体部分激活剂
    • US06552057B2
    • 2003-04-22
    • US09796805
    • 2001-03-02
    • Yasuo SatoMegumi YamadaKazuko KobayashiKatsuyoshi IwamatsuFukio KonnoKoichi Shudo
    • Yasuo SatoMegumi YamadaKazuko KobayashiKatsuyoshi IwamatsuFukio KonnoKoichi Shudo
    • A61K3142
    • C07D263/58A61K31/496C07D263/30C07D413/04
    • This invention provides a serotonin 5-HT3 receptor partial activator which has a serotonin 5-HT3 receptor activating action, in addition to its serotonin 5-HT3 receptor antagonism, and does not cause constipation as a side effect. Particularly, based on the finding that newly synthesized benzoxazole derivatives typified by the compounds of the following formula (2) have strong serotonin 5-HT3 receptor antagonism and serotonin 5-HT3 receptor activating action, this invention provides these benzoxazole derivatives as serotonin 5-HT3 receptor partial activators. In the above formula, R1 to R4 may be the same or different from one another and each represents a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkenyl group or a substituted or unsubstituted amino group, or two groups of R1 and R2 may be linked together to form a ring structure, namely benzene ring; R5 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or a substituted or unsubstituted lower alkenyl group; and m is an integer of 1 to 4.
    • 本发明提供除5-羟色胺5-HT 3受体拮抗作用之外还具有5-羟色胺5-HT 3受体激活作用的5-羟色胺5-HT 3受体部分活化剂,并且不引起便秘作为副作用。特别地,基于以下发现: 以下式(2)化合物为代表的新合成苯并恶唑衍生物具有强烈的5-羟色胺5-HT 3受体拮抗作用和5-羟色胺5-HT 3受体激活作用,本发明提供了这些苯并恶唑衍生物作为5-羟色胺5-HT 3受体部分激活因子。 式中,R 1〜R 4可以相同或不同,表示氢原子,卤素原子,取代或未取代的低级烷基,取代或未取代的低级烯基或取代或未取代的氨基,或二 R1和R2的基团可以连接在一起形成环结构,即苯环; R5表示氢原子,取代或未取代的低级烷基或取代或未取代的低级烯基; m为1〜4的整数。
    • 6. 发明授权
    • Serotonin 5-HT3, receptor partial activator
    • 5-羟色胺5-HT3,受体部分活化剂
    • US06297246B1
    • 2001-10-02
    • US09298952
    • 1999-04-26
    • Yasuo SatoMegumi YamadaKazuko KobayashiKatsuyoshi IwamatsuFukio KonnoKoichi Shudo
    • Yasuo SatoMegumi YamadaKazuko KobayashiKatsuyoshi IwamatsuFukio KonnoKoichi Shudo
    • A61K31496
    • C07D263/58A61K31/496C07D263/30C07D413/04
    • This invention provides a serotonin 5-HT3 receptor partial activator which has a serotonin 5-HT3 receptor activating action, in addition to its serotonin 5-HT3 receptor antagonism, and does not cause constipation as a side effect. Particularly, based on the finding that newly synthesized benzoxazole derivatives typified by the compounds of the following formula (2) have strong serotonin 5-HT3 receptor antagonism and serotonin 5-HT3 receptor activating action, this invention provides these benzoxazole derivatives as serotonin 5-HT3 receptor partial activators. In the above formula, R1 to R4 may be the same or different from one another and each represents a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkenyl group or a substituted or unsubstituted amino group, or two groups of R1 and R2 may be linked together to form a ring structure, namely benzene ring; R5 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or a substituted or unsubstituted lower alkenyl group; and m is an integer of 1 to 4.
    • 本发明提供除5-羟色胺5-HT 3受体拮抗作用之外还具有5-羟色胺5-HT 3受体激活作用的5-羟色胺5-HT 3受体部分活化剂,并且不引起便秘作为副作用。 特别地,基于以下结构式(2)所示的新合成的苯并恶唑衍生物具有强的5-羟色胺5-HT 3受体拮抗作用和5-羟色胺5-HT 3受体活化作用,本发明提供了这些苯并恶唑衍生物作为血清素5-HT3 在上式中,R 1〜R 4可以相同或不同,表示氢原子,卤素原子,取代或未取代的低级烷基,取代或未取代的低级烯基或取代的 或未取代的氨基,或两个R 1和R 2可以连接在一起形成环结构,即苯环; R5表示氢原子,取代或未取代的低级烷基或取代或未取代的低级烯基; m为1〜4的整数。
    • 9. 发明授权
    • Compound having heterocyclic ring
    • 具有杂环的化合物
    • US08148362B2
    • 2012-04-03
    • US12225819
    • 2007-03-30
    • Hideyuki SuzukiShoji HizatateIwao UtsunomiyaKoichi Shudo
    • Hideyuki SuzukiShoji HizatateIwao UtsunomiyaKoichi Shudo
    • A61K31/00C07D255/00
    • C07D273/06C07D255/02C07D413/10C07D413/14C07D417/14C07D471/14Y02P20/55
    • The invention provides a novel oxazolidinone derivative represented by the formula (I): wherein Ring A is optionally substituted or fused and represents (A-1) at least 7-membered monocyclic hetero ring containing at least three N atoms; (A-2) at least 6-membered monocyclic hetero ring containing at least two N atoms and at least one O atom; or (A-3) at least 7-membered monocyclic hetero ring containing at least two N atoms and at least one S atom; X1 is a single bond, —O—, —S—, —NR2—, —CO—, —CS—, —CONR3—, —NR4CO—, —SO2NR5—, and —NR6SO2— (wherein R2-R6 are independently hydrogen or lower alkyl), or lower alkylene or lower alkenylene in which one of the preceding groups may intervene; Ring B is optionally substituted carbocycle or optionally substituted heterocycle; R1 is hydrogen, or an organic residue which is able to bind to the 5-position of oxazolidinone ring in oxazolidinone antimicrobial agent, and an antibacterial agent containing the same.
    • 本发明提供由式(I)表示的新型恶唑烷酮衍生物:其中环A任选被取代或稠合并且代表(A-1)含有至少三个N原子的至少七元单环杂环; (A-2)至少含有至少两个N原子和至少一个O原子的6元单环杂环; 或(A-3)至少含有至少两个N原子和至少一个S原子的7元单环杂环; X 1是单键,-O - , - S - , - NR 2 - , - CO - , - C - , - CONR 3 - , - NR 4 CO-,-SO 2 NR 5 - 和-NR 6 SO 2 - 或低级烷基)或其中一个前述基团可以介入的低级亚烷基或低级亚烯基; 环B是任选取代的碳环或任选取代的杂环; R1是氢,或能够与恶唑烷酮抗微生物剂中的恶唑烷酮环的5位结合的有机残基,以及含有该残基的抗菌剂。