TRIAZOLE DERIVATIVE
    11.
    发明申请
    TRIAZOLE DERIVATIVE 失效
    三唑衍生物

    公开(公告)号:US20100041655A1

    公开(公告)日:2010-02-18

    申请号:US12278054

    申请日:2007-02-05

    CPC分类号: C07D249/08

    摘要: An object of the present invention is to provide a compound having an action of inhibiting binding between S1P and its receptor, Edg-1 (S1P1), and is useful as a pharmaceutical compound. A compound or a pharmaceutically acceptable salt thereof, which compound is represented by the formula below (where A represents an oxygen atom, a sulfur atom, a group represented by Formula —SO—, a group represented by Formula —SO2— or the like, R1 represents a hydrogen atom, an alkyl group having 1-6 carbon atoms, or the like, R1A represents a hydrogen atom or the like, R2 represents an alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-6 carbon atoms, or the like, represents an aryl group, R4 represents a hydrogen atom or an alkyl group having 1-6 carbon atoms and optionally substituted with a carboxyl group, and R5 represents an alkyl group having 1-carbon atoms, a cycloalkyl group having 3-8 carbon atoms, an aryl group which is optionally substituted, or the like).

    摘要翻译: 本发明的目的是提供具有抑制S1P与其受体Edg-1(S1P1)结合的作用的化合物,可用作药物化合物。 一种化合物或其药学上可接受的盐,该化合物由下式表示(其中A表示氧原子,硫原子,由式-SO-表示的基团,由式-SO2-等表示的基团, R1表示氢原子,具有1-6个碳原子的烷基等,R1A表示氢原子等,R2表示具有1-6个碳原子的烷基,具有3-6个碳原子的环烷基 等表示芳基,R 4表示氢原子或具有1-6个碳原子并且任选被羧基取代的烷基,R 5表示具有1个碳原子的烷基,环烷基具有3个 -8个碳原子,任选取代的芳基等)。

    Prostaglandin derivatives
    13.
    发明授权
    Prostaglandin derivatives 失效
    前列腺素衍生物

    公开(公告)号:US06822112B1

    公开(公告)日:2004-11-23

    申请号:US10048926

    申请日:2002-02-05

    IPC分类号: C07C6976

    CPC分类号: C07C405/00

    摘要: A prostaglandin derivative represented by the formula: wherein X is a halogen atom, R1 is a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl group, m is an integer of 0 to 5, and Y is a group represented by the formula: wherein R2 is a C3-10 cycloalkyl group, a C3-10 cycloalkyl group substituted with C1-4 alkyl group(s), a C1-4 alkyl group substituted with C3-10 cycloalkyl group(s), a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group or a bridged cyclic hydrocarbon group, or a group represented by the formula: wherein n is an integer of 1 to 8; a pharmaceutically acceptable salt thereof or a hydrate thereof.

    摘要翻译: 由下式表示的前列腺素衍生物:其中X是卤素原子,R 1是氢原子,C 1-10烷基或C 3-10环烷基,m是0-5的整数,Y是 由下式表示的基团:其中R 2为C 3-10环烷基,被C 1-4烷基取代的C 3-10环烷基,被C 3-10环烷基取代的C 1-4烷基 C 1-10烷基,C 2-10烯基,C 2-10炔基或桥连环烃基,或由下式表示的基团:其中n为1至8的整数; 其药学上可接受的盐或其水合物。

    Prostaglandin derivatives
    14.
    发明授权
    Prostaglandin derivatives 失效
    前列腺素衍生物

    公开(公告)号:US06740772B1

    公开(公告)日:2004-05-25

    申请号:US10070643

    申请日:2002-03-11

    IPC分类号: C07C17700

    CPC分类号: C07C405/00 C07C405/0016

    摘要: A prostaglandin derivative represented by the formula: wherein X is a halogen atom in the &agr;- or &bgr;-position, Y is an ethylene group, a vinylene group or an ethynylene group, A is a group represented by the formula: O(CH2)n, S(O)p(CH2)n, O(CH2)qO(CH2)r, O(CH2)qS(O)p(CH2)r, S(O)p(CH2)qS(O)p(CH2)r or S(O)p(CH2)qO(CH2)r (wherein n is an integer of 1 to 5, p is 0, 1 or 2, q is an integer of 1 to 3, and r is 0 or 1), R1 is a C3-10 cycloalkyl group, a C1-4 alkyl-C3-10 cycloalkyl group, a C3-10 cycloalkyl-C1-4 alkyl group, a C5-10 alkyl group, a C5-10 alkenyl group, a C5-10 alkynyl group or a bridged cyclic hydrocarbon group, R2 is a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl group, and m is 0, 1 or 2], a pharmaceutically acceptable salt thereof or a hydrate thereof. The present invention is to provide novel PG derivatives having an excellent PGD2-like agonistic activity and a sleep-inducing action.

    摘要翻译: 由下式表示的前列腺素衍生物:其中X是α-位或β-位的卤素原子,Y是亚乙基,亚乙烯基或亚乙炔基,A是由下式表示的基团:O(CH 2) (O)p(CH2)q(O)p(CH2)q(O)p(CH2)q(O)p(CH2) CH 2)r或S(O)p(CH 2)q O(CH 2)r(其中n为1〜5的整数,p为0,1或2,q为1〜3的整数,r为0或1 ),R 1为C 3-10环烷基,C 1-4烷基-C 3-10环烷基,C 3-10环烷基-C 1-4烷基,C 5-10烷基,C 5-10烯基 基团,C5-10炔基或桥连环烃基,R 2是氢原子,C 1-10烷基或C 3-10环烷基,m是0,1或2],药学上可接受的 其盐或其水合物。本发明提供具有优异的PGD 2样激动活性和睡眠诱导作用的新型PG衍生物。

    Prostaglandin E.sub.1 analogues
    15.
    发明授权
    Prostaglandin E.sub.1 analogues 失效
    前列腺素E1类似物

    公开(公告)号:US5639899A

    公开(公告)日:1997-06-17

    申请号:US133171

    申请日:1993-10-19

    IPC分类号: C07C405/00 C07C59/00

    CPC分类号: C07C405/00

    摘要: Object: To provide novel prostaglandin E.sub.1 analogues which have more excellent pharmaceutical effects, longer duration of the effects and less side-effects than the prior art prostaglandin E.sub.1 's.Constitution: A PGE.sub.1 analogue represented by the formula: ##STR1## (wherein A is a vinylene group or an ethynylene group, R.sup.1 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or an allyl group, R.sup.2 is a branched aliphatic hydrocarbon group having 5 to 10 carbon atoms), or a salt thereof.

    摘要翻译: PCT No.PCT / JP92 / 00513 Sec。 371日期:1993年10月19日 102(e)日期1993年10月19日PCT 1992年4月21日PCT PCT。 第WO92 / 18472号公报 日期1990年10月29日二氧化物目标:提供与现有技术的前列腺素E1相比,具有更优异的药物作用,更长的作用时间和更少的副作用的新型前列腺素E1类似物。 结构:由下式表示的PGE1类似物:其中A是亚乙烯基或亚乙炔基,R 1是氢原子,具有1至6个碳原子的烷基或烯丙基,R 2是支链脂族 具有5〜10个碳原子的烃基)或其盐。

    Triazole derivative
    19.
    发明授权
    Triazole derivative 失效
    三唑衍生物

    公开(公告)号:US08022225B2

    公开(公告)日:2011-09-20

    申请号:US11659103

    申请日:2005-08-04

    IPC分类号: C07D249/12 C07D249/08

    摘要: A compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof has an effect of inhibiting binding between S1P and its receptor Edg-1(S1P1), and is useful as a pharmaceutical product. [where A represents a sulfur atom, an oxygen atom, a formula —SO— or a formula —SO2—; R1 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like; R2 represents an alkyl group having 1 to 6 carbon atoms, a cycloalkyl group having 3 to 8 carbon atoms or the like; R3 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; R4 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a phenyl group or the like; R5 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; and R6 represents an alkyl group having 1 to 6 carbon atoms, a phenyl group or a substituted phenyl group].

    摘要翻译: 由下式(I)表示的化合物或其药学上可接受的盐具有抑制S1P与其受体Edg-1(S1P1)结合的作用,可用作药物。 [其中A表示硫原子,氧原子,式-SO-或式-SO 2 - ; R1表示氢原子,碳原子数1〜6的烷基等; R2表示碳原子数1〜6的烷基,碳原子数3〜8的环烷基等; R3表示氢原子或碳原子数1〜6的烷基。 R4表示氢原子,碳原子数1〜6的烷基,苯基等; R5表示氢原子或碳原子数1〜6的烷基。 R6表示碳原子数1〜6的烷基,苯基或取代苯基]。

    Triazole derivative
    20.
    发明申请
    Triazole derivative 失效
    三唑衍生物

    公开(公告)号:US20090131438A1

    公开(公告)日:2009-05-21

    申请号:US11659103

    申请日:2005-08-04

    摘要: A compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof has an effect of inhibiting binding between S1P and its receptor Edg-1(S1P1), and is useful as a pharmaceutical product. [where A represents a sulfur atom, an oxygen atom, a formula —SO— or a formula —SO2—; R1 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like; R2 represents an alkyl group having 1 to 6 carbon atoms, a cycloalkyl group having 3 to 8 carbon atoms or the like; R3 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; R4 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a phenyl group or the like; R5 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; and R6 represents an alkyl group having 1 to 6 carbon atoms, a phenyl group or a substituted phenyl group].

    摘要翻译: 由下式(I)表示的化合物或其药学上可接受的盐具有抑制S1P与其受体Edg-1(S1P1)结合的作用,可用作药物。 [其中A表示硫原子,氧原子,式-SO-或式-SO 2 - ; R1表示氢原子,碳原子数1〜6的烷基等; R2表示碳原子数1〜6的烷基,碳原子数3〜8的环烷基等; R3表示氢原子或碳原子数1〜6的烷基。 R4表示氢原子,碳原子数1〜6的烷基,苯基等; R5表示氢原子或碳原子数1〜6的烷基。 R6表示碳原子数1〜6的烷基,苯基或取代苯基]。