PROSTAGLANDIN DERIVATIVES
    1.
    发明公开
    PROSTAGLANDIN DERIVATIVES 有权
    前列腺素衍生物

    公开(公告)号:EP1553083A1

    公开(公告)日:2005-07-13

    申请号:EP03741366.3

    申请日:2003-07-11

    CPC分类号: C07C405/0033

    摘要: A prostaglandin derivative represented by Formula (I) :
    wherein X is a halogen atom in the α- or β-substitution, Y is an ethylene group, a vinylene group or an ethynylene group, R 1 is a C 3-10 cycloalkyl group, a C 3-10 cycloalkyl group substituted with a C 1-4 straight or branched chain alkyl group or a C 4-13 cycloalkylalkyl group, R 2 is a hydrogen atom or a CO 2 R 3 group (R 3 is a hydrogen atom, a C 1-4 straight or branched chain alkyl group or a C 2-4 straight or branched chain alkenyl group), n is an integer of 1 to 4 and p is 0, 1 or 2,
    a pharmaceutically acceptable salt thereof or a hydrate thereof.

    摘要翻译: 式(I)所示的前列腺素衍生物:其中X为α-或β-取代基中的卤素原子,Y为亚乙基,亚乙烯基或亚乙炔基,R1为C3-10环烷基,C3 被C 1-4直链或支链烷基或C 4-13环烷基烷基取代的环烷基,R 2是氢原子或CO 2 R 3基团(R 3是氢原子,C 1-4直链或支链烷基 或C2-4直链或支链烯基),n是1至4的整数,并且p是0,1或2,其药学上可接受的盐或其水合物。

    PROCESS FOR PRODUCING INTERMEDIATE FOR 13,14-DIDEHYDROPROSTAGLANDIN E
    4.
    发明公开
    PROCESS FOR PRODUCING INTERMEDIATE FOR 13,14-DIDEHYDROPROSTAGLANDIN E 失效
    生产13,14-二氢前列腺素的中间体的方法E

    公开(公告)号:EP0685462A1

    公开(公告)日:1995-12-06

    申请号:EP94907066.8

    申请日:1994-02-17

    发明人: SATO, Fumie

    摘要: A process for producing an intermediate for a 13,14-didehydroprostaglandin E, represented by general formula (I), (wherein R⁶ represents -COOR⁹, cyano, hydroxy, -OCOR¹⁰ or -CONR¹¹R¹²; A represents vinylene, ethynylene, phenylene -C=C=C-; X represents oxygen or sulfur; m is 0 to 7; n, q and s are each 0 or 1; and p and r are each 0 to 5) by the free-radical reaction of a compound represented by general formula (II), with a compound represented by the following general formula: Y(CR³R⁴) m A n (CH₂) p X q (CHR⁵) r R⁶, (wherein Y represents halogen or (a)) in the presence of a free-radical generator.

    摘要翻译: (I)表示的13,14-二氢脯氨酸E的中间体的制备方法,式中R 7代表-COOR 7,氰基,羟基,-OCOR 10或-CONR 11 R 12; A代表亚乙烯基,亚乙炔基,亚苯基-C = C = C-; X代表氧或硫; m为0-7; n,q和s各自为0或1; p和r各自为0-5)通过一般性代表的化合物的自由基反应 (II)化合物与下式通式Y(CR 3 R 4)mAn(CH 2)pXq(CHR 5)r R 8(其中Y代表卤素或(a))所代表的化合物在自由基生成剂存在下反应。

    PROSTAGLANDIN E1 ANALOGUE
    6.
    发明公开
    PROSTAGLANDIN E1 ANALOGUE 失效
    前列腺素E1类似物

    公开(公告)号:EP0597095A1

    公开(公告)日:1994-05-18

    申请号:EP92908246.9

    申请日:1992-04-21

    IPC分类号: C07C405/00

    CPC分类号: C07C405/00

    摘要: Object: to provide a novel prostaglandin E₁ which is excellent in drug efficacy while reduced in adverse reactions as compared with conventional ones. Constitution: a PGE₁ analogue represented by general formula (I) and its salt, wherein A represents vinylene or ethynylene; R¹ represents hydrogen, C₁ to C₆ alkyl or aryl; and R² represents C₅ to C₁₀ branched aliphatic hydrocarbyl.

    摘要翻译: 目的:提供新型前列腺素E 1,与传统药物相比,药物疗效优异,副反应减少。 构成:由通式(I)表示的PGE 1类似物及其盐,其中A代表亚乙烯基或亚乙炔基; R 1代表氢,C 1至C 6烷基或芳基; R 2代表C 5至C 10支链脂族烃基。

    ANTIPRURITIC AGENT
    7.
    发明公开
    ANTIPRURITIC AGENT 有权
    防腐剂

    公开(公告)号:EP1527781A1

    公开(公告)日:2005-05-04

    申请号:EP03784565.8

    申请日:2003-08-07

    摘要: A pharmaceutical preparation for preventing or treating pruritic symptoms which contains as an effective ingredient a prostaglandin derivative represented by formula [1]
    wherein X 1 and X 2 which are different from each other represent a hydrogen atom, a halogen atom or a hydroxyl group;

    Y is an ethylene group, a vinylene group or an ethynylene group; Z is the formula
    (CH 2 ) k A(CH 2 ) h B(CH 2 ) q ,
    (CH 2 ) k A(CH 2 ) r A'(CH 2 ) t ,
    (CH 2 ) k B(CH 2 ) h B'(CH 2 ) q
    or

    (CH 2 ) k-1 B'(CH 2 ) q-1 A'
    wherein k is an integer of 1 to 4, h is an integer of 0 to 4, q is an integer 1 to 4, r is an integer of 0 to 4, and t is an integer of 0 to 2;

    A and A' which may be the same or different represent an ethylene group, a vinylene group or an ethynylene group;
    B and B' which may be the same or different represent an oxygen atom or a group represented by the formula S(O) u wherein u is an integer of 0 to 2;
    W 1 is a hydroxyl group, a C 1-10 alkyloxy group, a C 3-10 cycloalkyloxy group, an aryloxy group or an arylalkyloxy group;
    W 2 is a C 1-10 alkyl group, a C 2-10 alkenyl group, a C 2-10 alkynyl group, a C 3-10 cycloalkyl group, a C 1-5 alkyl group substituted by C 3-10 cycloalkyl group(s), or a group represented by the formula
    wherein W 4 is a C 1-10 alkyl group, a C 2-10 alkenyl group, a C 2-10 alkynyl group or a C 1-5 alkyl group substituted by C 3-10 cycloalkyl group(s); v is an integer of 0 to 4;
    W 3 is a hydrogen atom or a methyl group, or W 3 when taken together with W 2 and the adjacent carbon atom forms a C 3-10 cycloalkyl group; m is 0 or 1, a pharmaceutically acceptable salt thereof or a hydrate thereof.

    摘要翻译: 一种用于预防或治疗瘙痒症状的药物制剂,其含有式[1]所示的前列腺素衍生物作为有效成分,其中彼此不同的X 1和X 2表示氢原子,卤素原子或羟基; Y是亚乙基,亚乙烯基或亚乙炔基; Z是式(CH 2)k A(CH 2)h B(CH 2)q,(CH 2)k A(CH 2) 1B'(CH 2)q-1A'式中,k为1〜4的整数,h为0〜4的整数,q为1〜4的整数,r为0〜4的整数,t为整数 0到2; A和A'可以相同或不同,表示亚乙基,亚乙烯基或亚乙炔基; B和B'可以相同或不同,表示氧原子或由式S(O)u表示的基团,其中u是0-2的整数; W1是羟基,C1-10烷氧基,C3-10环烷氧基,芳氧基或芳基烷氧基; W2为C1-10烷基,C2-10烯基,C2-10炔基,C3-10环烷基,C3-10环烷基取代的C1-5烷基或基团 由下式表示:其中W4是C1-10烷基,C2-10链烯基,C2-10炔基或被C3-10环烷基取代的C1-5烷基; v是0至4的整数; W3是氢原子或甲基,或者W3与W2一起形成并且相邻的碳原子形成C3-10环烷基; m是0或1,其药学上可接受的盐或其水合物。

    PROSTAGLANDIN E 1? ANALOGUE
    10.
    发明公开
    PROSTAGLANDIN E 1? ANALOGUE 失效
    前列腺素E 1? 类似物

    公开(公告)号:EP0591532A1

    公开(公告)日:1994-04-13

    申请号:EP92908341.8

    申请日:1992-04-21

    IPC分类号: C07C405/00

    CPC分类号: C07C405/00

    摘要: Object: to provide a novel prostaglandin E₁ which is excellent in drug efficacy and prolonged action while reduced in adverse reactions as compared with conventional ones. Constitution: a PGE₁ analogue represented by general formula (I) and its salt, wherein R¹ represents hydrogen, C₁ to C₆ alkyl or aryl; and R² represents C₃ to C₆ alkyl or C₃ to C₆ alkenyl.

    摘要翻译: 目的:提供一种新颖的前列腺素E 1,其与常规药物相比在药物疗效和延长作用方面优异,并且在不良反应中减少。 组成:由通式(Ⅰ)代表的PGE 1类似物及其盐,其中R 1代表氢,C 1至C 6烷基或芳基; R 2代表C 3至C 6烷基或C 3至C 6链烯基。