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    Pseudopolymorphic forms of 2-[2-[4-[bis (4-fluorophenyl) methyl]-1-piperazinyl]ethoxy]acetic acid dihydrochloride
    2.
    发明专利
    Pseudopolymorphic forms of 2-[2-[4-[bis (4-fluorophenyl) methyl]-1-piperazinyl]ethoxy]acetic acid dihydrochloride 审中-公开
    2- [2- [4- [双（4-氟代甲基）甲基] -1-哌嗪基]乙氧基]乙酸二氢氯化物的光学形态

    公开(公告)号：JP2007224042A

    公开(公告)日：2007-09-06

    申请号：JP2007109494

    申请日：2007-04-18

    Applicant: Ucb Sa ,  ユセベ,ソシエテ アノニム

    Inventor： BERWAER MONIQUE ,  BODSON GUY ,  DELEERS MICHEL ,  DOGIMONT CHARLES ,  FANARA DOMENICO ,  TIMMERMANS JACQUES

    IPC: C07D295/08 ,  A61K31/495 ,  A61K47/40 ,  A61P11/02 ,  A61P11/08 ,  A61P17/00 ,  A61P17/04 ,  A61P21/02 ,  A61P25/08 ,  A61P27/16 ,  A61P37/08 ,  A61P43/00 ,  C07D295/084 ,  C07D295/088

    CPC classification number: C07D295/088

    Abstract: PROBLEM TO BE SOLVED: To provide an efletirizine which is a pharmaceutical having excellent antihistaminic properties, namely, a new crystal form of a 2-[2-[4-[bis (4-fluorophenyl) methyl]-1-piperazinyl]ethoxy]acetic acid dihydrochloride, and to provide a method for preparation of the crystal and to a pharmaceutical composition comprising the same.
    SOLUTION: The invention relates to the new pseudopolymorphic forms of 2-[2-[4-[bis(4- fluorophenyl)methyl]-1-piperazinyl]ethoxy]acetic acid dihydrochloride, defined by the X-ray diffraction pattern, namely, anhydrous 2-[2-[4-[bis(4-fluorophenyl)methyl]-l-piperazinyl]ethoxy]acetic acid dihydrochloride and a monohydrate of the crystal, and relates to the method for preparation of the pseudopolymorphic crystal. The invention also relates to the pharmaceutical composition comprising the pseudopolymorphic crystal, slow release excipient and a cyclodextrine.
    COPYRIGHT: (C)2007,JPO&INPIT

    Abstract translation: 待解决的问题：提供作为具有优异的抗组胺性质的药物的efletirizine，即2- [2- [4- [双（4-氟苯基）甲基] -1-哌嗪基 ]乙氧基]乙酸二盐酸盐，并提供制备晶体的方法和包含其的药物组合物。 解决方案：本发明涉及由X-射线衍射图定义的2- [2- [4- [双（4-氟苯基）甲基] -1-哌嗪基]乙氧基]乙酸二盐酸盐的新的假多晶型形式 ，即无水2- [2- [4- [双（4-氟苯基）甲基] -1-哌嗪基]乙氧基]乙酸二盐酸盐和晶体的一水合物，涉及制备假多晶型晶体的方法。 本发明还涉及包含假多晶型晶体，缓释赋形剂和环糊精的药物组合物。 版权所有（C）2007，JPO＆INPIT

    Novel substituted [2-(1-piperazinyl)ethoxy]methyl compounds
    7.
    发明专利
    Novel substituted [2-(1-piperazinyl)ethoxy]methyl compounds 未知

    公开(公告)号：CZ295068B6

    公开(公告)日：2005-05-18

    申请号：CZ315198

    申请日：1997-03-28

    Applicant: UCB SA

    Inventor： DUCHENE GUY ,  DELEERS MICHEL ,  BODSON GUY ,  MOTTE GENEVIEVE ,  LURQUIN FRANCOISE

    IPC: C07D295/14 ,  C07D295/08 ,  C07D295/088 ,  C07D295/16 ,  C07D295/20 ,  C07D295/205

    Abstract: The present invention relates to novel substituted [2-(1-piperazinyl)-ethoxy]methyl compounds of the general formula I, in which Ri1 represents the -CONHi2, -CN, -COOH, -COOM or -COORi3, group, M denotes an alkali metal and Ri3 represents an alkyl radical having from 1 to 4 carbon atoms; and Ri2 represents a hydrogen atom or a group -COR4 or -R5, where Ri4 is selected from the groups --ORi6 or -Ri7, in which Ri5 represents an alkyl or alkylaryl radical, Ri6 represents a linear or branched alkyl radical having from 1 to 4 carbon atoms, a haloalkyl, alkylaryl, alkylnitroaryl or alkylhaloaryl radical, andRi7 represents a haloalkyl radical. The invention further relates to a process for the preparation of the above-indicated compounds, as well as to their use for the preparation of compounds which are themselves valuable intermediates for the preparation of 2-[2-[4[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-acetic acid or 2-[2-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]ethoxy]-acetic acid and/or pharmaceutically acceptable salts thereof.

    NOVEL SUBSTITUTED [2-(1-PIPERAZINYL)ETHOXY] METHYL COMPOUNDS
    8.
    发明专利
    NOVEL SUBSTITUTED [2-(1-PIPERAZINYL)ETHOXY] METHYL COMPOUNDS 未知

    公开(公告)号：PL188819B1

    公开(公告)日：2005-04-29

    申请号：PL32930797

    申请日：1997-03-28

    Applicant: UCB SA

    Inventor： DUCHENE GUY ,  DELEERS MICHEL ,  BODSON GUY ,  MOTTE GENEVIEVE ,  LURQUIN FRANCOISE

    IPC: C07D295/14 ,  C07D295/08 ,  C07D295/088 ,  C07D295/16 ,  C07D295/20 ,  C07D295/205

    Abstract: PCT No. PCT/BE97/00038 Sec. 371 Date Oct. 9, 1998 Sec. 102(e) Date Oct. 9, 1998 PCT Filed Mar. 28, 1997 PCT Pub. No. WO97/37982 PCT Pub. Date Oct. 16, 1997Novel substituted [2-(1-piperazinyl)ethoxy]methyl compounds. The present invention related to novel substituted [2-(1-piperazinyl)-ethoxy]methyl compounds of formula in which R1 represents a -CONH2, -CN, -COOH, -COOM or -COOR3 group, M being an alkali metal and R3 being an alkyl radical having from 1 to 4 carbon atoms; and R2 represents a hydrogen atom or a group -COR4 or -R5, where R4 is chosen from the groups -OR6 or -R7, in which R5 represents an allyl or alkylaryl radical, R6 represents a linear or branched alkyl radical having from 1 to 4 carbon atoms, a haloalkyl, alkylaryl, alkylnitroaryl or alkylhaloaryl radical, and R7 represents a haloalkyl radical, to a process for the preparation of these compounds, and to their use for the preparation of compounds which are themselves valuable intermediates for the preparation of 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-acetic acid or 2-[2-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]ethoxy]-acetic acid and/or pharmaceutically acceptable salts thereof.

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