PROSTAGLANDIN DERIVATIVES
    5.
    发明公开
    PROSTAGLANDIN DERIVATIVES 审中-公开
    PROSTAGLANDINDERIVATE

    公开(公告)号:EP1598335A4

    公开(公告)日:2006-04-12

    申请号:EP04712705

    申请日:2004-02-19

    CPC分类号: C07C405/0016

    摘要: A prostaglandin derivative represented by the following general formula [I], its pharmaceutically acceptable salt or a hydrate thereof which has an excellent antagonism to prostaglandin DP receptor and, therefore, is useful against diseases such as allergic rhinitis, nasal obstruction, asthma, allergic conjunctivitis, systemic mastocytosis and systemic mast cell disease; [I] wherein X represents halogeno; Y represents ethylene, vinylene or ethynylene; Z represents -(CH2)m-, -O(CH2)n- or -S(O)p-(CH2)n- (wherein m is an integer of from 0 to 3; n is an integer of from 0 to 2; and p is an integer of from 0 to 2); R represents hydrogen or optionally substituted C1-5 alkyl; R represents C3-10 cycloalkyl optionally substituted by C1-4 alkyl or C4-15 cycloalkyl; and R represents hydrogen, halogeno or optionally substituted C1-5 alkyl.

    摘要翻译: 由以下通式[I]表示的前列腺素衍生物,其药学上可接受的盐或其水合物对前列腺素DP受体具有优良的拮抗作用,因此可用于治疗变应性鼻炎,鼻塞,哮喘,过敏性结膜炎 ,系统性肥大细胞增多症和系统性肥大细胞病; [I]其中X代表卤代; Y代表亚乙基,亚乙烯基或亚乙炔基; Z代表 - (CH2)m-,-O(CH2)n-或-S(O)p-(CH2)n-(其中m是0-3的整数; n是0-2的整数 ;并且p是0-2的整数); R 1代表氢或任选取代的C 1-5烷基; R 2表示任选被C 1-4烷基或C 4-15环烷基取代的C 3-10环烷基; 且R 3代表氢,卤代或任选取代的C 1-5烷基。

    PROSTAGLANDIN DERIVATIVES
    6.
    发明公开
    PROSTAGLANDIN DERIVATIVES 有权
    前列腺素

    公开(公告)号:EP1553083A4

    公开(公告)日:2006-04-12

    申请号:EP03741366

    申请日:2003-07-11

    CPC分类号: C07C405/0033

    摘要: Prostaglandin derivatives represented by the general formula (I), pharmaceutically acceptable salts thereof, or hydrates of the salts: (I) wherein X is halogeno of alpha or beta configuration; Y is ethylene, vinylene, or ethynylene; R is C3-10 cycloalkyl which may be substituted with a linear or branched C1-4 alkyl group, or C4-13 cycloalkylalkyl; R is hydrogen or CO2R ; R is hydrogen, linear or branched C1-4 alkyl, or linear or branched C2-4 alkenyl; n is an integer of 1 to 4; and p is 0, 1, or 2.

    PROSTAGLANDIN DERIVATIVES
    8.
    发明公开
    PROSTAGLANDIN DERIVATIVES 审中-公开
    PROSTAGLANDIN DERIVATE

    公开(公告)号:EP1219601A4

    公开(公告)日:2004-10-27

    申请号:EP00957063

    申请日:2000-09-08

    CPC分类号: C07C405/00

    摘要: Novel prostaglandin derivatives represented by general formula (I), pharmaceutically acceptable salts thereof, or hydrates of both, wherein X is CH2, O, S, or the like; Y is ethylene, vinylene, ethynylene, or the like; Z is ethylene, vinylene, or ethynylene; R is hydrogen, alkyl, or cycloalkyl; R is alkyl, alkenyl, alkynyl, cycloalkyl, or the like; and R is hydrogen, alkyl, or the like. The prostaglandin derivatives exhibit an excellent inhibitory activity against the proliferation of vascular smooth muscle and are useful as preventive or therapeutic drugs for post-PTCA restenosis and so on.

    PROCESS FOR PRODUCING INTERMEDIATE FOR 13,14-DIDEHYDROPROSTAGLANDIN E.
    9.
    发明公开
    PROCESS FOR PRODUCING INTERMEDIATE FOR 13,14-DIDEHYDROPROSTAGLANDIN E. 失效
    VERFAHREN ZUR HERSTELLUNG EINES INTERMEDIATESFÜR13,14-Didehydroprostaglandin。

    公开(公告)号:EP0685462A4

    公开(公告)日:1998-08-05

    申请号:EP94907066

    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 R represents -COOR , cyano, hydroxy, -OCOR or -CONR R ; 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(CR R )mAn(CH2)pXq(CHR )rR , (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,其中R 6表示-COOR 9,氰基,羟基,-OCOR 10或-CONR 11 > R 12; A表示亚乙烯基,亚乙炔基,亚苯基-C = C = C-; X表示氧或硫; m为0至7; n,q和s各自为0或1; p和r各自为 (CR 3 R 4)mA n(CH 2)p X q(CHR 5)n表示的化合物与通式(II)所示的化合物进行自由基反应, (其中Y代表卤素或(a))在自由基生成剂存在下反应。

    PROSTAGLANDIN DERIVATIVES
    10.
    发明公开
    PROSTAGLANDIN DERIVATIVES 有权
    前列腺素衍生物

    公开(公告)号:EP1211242A4

    公开(公告)日:2004-11-03

    申请号:EP00957064

    申请日:2000-09-08

    CPC分类号: C07C405/00 C07C405/0016

    摘要: Prostaglandin derivatives of general formula (I), pharmaceutically acceptable salts thereof, or hydrates of both: [wherein X is alpha a- or beta -substituent halogeno; Y is ethylene, vinylene, or ethynylene; A is 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); R is C3-10 cycloalkyl, C1-4 alkyl C3-10 cycloalkyl, C3-10 cycloalkyl C1-4 alkyl, C5-10 alkyl, C5-10 alkenyl, C5-10 alkynyl, or a bridged cyclic hydrocarbon group; R is H, C1-10 alkyl, or C3-10 cycloalkyl; and m is 0, 1 or 2]. These compounds are novel and exhibit excellent prostaglandin D2-like agonism and a sleep-inducing effect.

    摘要翻译: 通式(I)的前列腺素衍生物,其药学上可接受的盐或两者的水合物:[其中X是α-或β-取代基卤代; Y是亚乙基,亚乙烯基或亚乙炔基; (O)p(CH 2)n,O(CH 2)q O(CH 2)r,O(CH 2)q S(O)p qS(O)p(CH 2)r或S(O)p(CH 2)q O(CH 2)r(其中n是1至5的整数; p是0,1或2; q是1至 3;并且r是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,C 5-10炔基或桥环烃基; R 2是H,C 1-10烷基或C 3-10环烷基; 并且m是0,1或2]。 这些化合物是新颖的并且表现出优异的前列腺素D 2样激动作用和睡眠诱导作用。