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    2.
    发明专利
    未知

    公开(公告)号：DK154078C

    公开(公告)日：1989-05-22

    申请号：DK44082

    申请日：1982-02-01

    Applicant: UCB SA

    Inventor： BALTES EUGENE ,  LANNOY JEAN DE ,  RODRIGUEZ LUDOVIC

    IPC: C07D295/08 ,  A61K31/495 ,  A61P37/08 ,  C07D295/088

    Abstract: New 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acids, their amides and their salts, processes for the preparation thereof and therapeutic compositions. These compounds have the formula wherein Y=-OH or -NH2; X and X'=H, halogen, alkoxy or trifluoromethyl; m=1 or 2 and n=1 or 2. The amides of the 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acids are prepared either by reacting a 1-(diphenylmethyl)-piperazine with an omegahaloacetamide, or by reacting an alkali metal salt of an omega-[4-(diphenylmethyl)-1-piperazinyl]-alkanol with a 2-haloacetamide, or yet by reacting ammonia with a halide or alkyl ester of a 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acid, whereas the 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acids are prepared by hydrolyzing the corresponding amide or lower alkyl ester. These compounds have in particular an antiallergic, spasmolytic and antihistaminic activity.

    7.
    发明专利
    未知

    公开(公告)号：IT1145338B

    公开(公告)日：1986-11-05

    申请号：IT4905280

    申请日：1980-06-24

    Applicant: UCB SA

    Inventor： RODRIGUEZ LUDOVIC ,  LECLERQ JACQUES ,  YKMAN PIERRE ,  COSSEMENT ERIC

    IPC: C07D499/46 ,  A61K31/43 ,  A61K31/431 ,  A61P31/04 ,  C07D499/00 ,  C07D499/64 ,  C07D499/68 ,  C07D499/74 ,  C07D499/76 ,  C07D499/80 ,  C07D499/90 ,  A61K

    Abstract: 6-Amino-spiro[penam-2,4'-piperidine]-3-carboxylic acid derivatives having the formula wherein R is a methyl, phenyl or benzyl radical, Z1 is a hydrogen atom and Z2 is a radical selected from those known from penicillin chemistry and is preferably a 2-phenylacetyl, 2-amino-2-phenylacetyl, 5-methyl-3-phenyl-4-isoxazolecarbonyl or 2,6-dimethoxybenzoyl radical, or Z1 and Z2 together represent a bivalent radical Z3 and preferably a (hexahydro-1H-azepin-1-yl)methylene radical, as well as the pharmaceutically acceptable non-toxic salts thereof and process for preparing the same. These compounds have valuable antibacterial properties and are useful as therapeutic agents in the treatment of infectious diseases caused by Gram-positive and Gram-negative bacteria.

    8.
    发明专利
    未知

    公开(公告)号：DK149133B

    公开(公告)日：1986-02-10

    申请号：DK408781

    申请日：1981-09-14

    Applicant: UCB SA

    Inventor： RODRIGUEZ LUDOVIC ,  BALTES EUGENE

    IPC: A61K31/445 ,  A61K31/451 ,  A61K31/452 ,  A61P11/00 ,  A61P11/08 ,  A61P25/20 ,  A61P37/08 ,  A61P43/00 ,  C07D211/70

    Abstract: New 2-[4-(diphenylmethylene)-1-piperidinyl]-acetic acids and their amides, processes for the preparation thereof and therapeutic compositions. These compounds have the formula wherein Y=-OH or -NR1R2, R1 and R2=H, alkyl or phenyl; X=H, halogen or alkoxy; m=0, 1 or 2 and n=1 or 2. The 2-[4-(diphenylmethylene)-1-piperidinyl]-acetic acids are prepared by hydrolyzing the corresponding amide or lower alkyl ester, whereas the amides are prepared either by reacting a 4-(diphenylmethylene)-piperidine with an omega-haloacetamide, or by reacting an alkali metal salt of an omega-[4-diphenylmethylene)-1-piperidinyl]-alkanol (m=1 or 2) with a 2-haloacetamide, or by reacting a nitrogen compound (HNR1R2) with a halide or alkyl ester of a 2-[4-(diphenylmethylene)-1-piperidinyl]-acetic acid. These compounds have in particular an antiallergic, spasmolytic, antihistaminic and broncholytic activity.

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