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    2-[4-(Diphenylmethylene)-1-piperidinyl]-acetic acids and their amides
    4.
    发明授权
    2-[4-(Diphenylmethylene)-1-piperidinyl]-acetic acids and their amides 失效
    2- [4-（二苯基亚甲基）-1-哌啶基] - 乙酸及其酰胺

    公开(公告)号：US4443460A

    公开(公告)日：1984-04-17

    申请号：US303522

    申请日：1981-09-17

    Applicant: Ludovic Rodriguez ,  Eugene Baltes

    Inventor： Ludovic Rodriguez ,  Eugene Baltes

    IPC: A61K31/445 ,  A61K31/451 ,  A61K31/452 ,  A61P11/00 ,  A61P11/08 ,  A61P25/20 ,  A61P37/08 ,  A61P43/00 ,  C07D211/70 ,  C07D211/22

    CPC classification number: C07D211/70 ,  Y10S514/816 ,  Y10S514/826

    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 ##STR1## wherein Y=--OH or --NR.sub.1 R.sub.2, R.sub.1 and R.sub.2 =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 (HNR.sub.1 R.sub.2) 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.

    Abstract translation: 新的2- [4-（二苯基亚甲基）-1-哌啶基] - 乙酸及其酰胺，其制备方法和治疗组合物。 这些化合物具有其中Y = -OH或-NR1R2，R1和R2 = H，烷基或苯基的式“IMAGE” X = H，卤素或烷氧基; m = 0,1或2，n = 1或2.通过水解相应的酰胺或低级烷基酯制备2- [4-（二苯基亚甲基）-1-哌啶基] - 乙酸，而酰胺由 使4-（二苯基亚甲基） - 哌啶与ω-卤代乙酰胺反应，或通过使ω-[4-二苯基亚甲基] -1-哌啶基] - 烷醇（m = 1或2）的碱金属盐与2-卤代乙酰胺 或通过使氮化合物（HNR1R2）与2- [4-（二苯基亚甲基）-1-哌啶基] - 乙酸的卤化物或烷基酯反应。 这些化合物特别具有抗过敏，解痉，抗组胺和支气管分解活性。

    6-Amino-spiro[penam-2,4'-piperidine]-3-carboxylic acid, antibacterial compositions thereof and method of use thereof
    6.
    发明授权
    6-Amino-spiro[penam-2,4'-piperidine]-3-carboxylic acid, antibacterial compositions thereof and method of use thereof 失效
    6-氨基螺[penam-2,4'-哌啶] -3-羧酸，其抗菌组合物及其使用方法

    公开(公告)号：US4271173A

    公开(公告)日：1981-06-02

    申请号：US162615

    申请日：1980-06-24

    Applicant: Ludovic Rodriguez ,  Jacques Leclercq ,  Pierre Ykman ,  Eric Cossement

    Inventor： Ludovic Rodriguez ,  Jacques Leclercq ,  Pierre Ykman ,  Eric Cossement

    IPC: C07D499/46 ,  A61K31/43 ,  A61K31/431 ,  A61P31/04 ,  C07D499/00 ,  C07D499/64 ,  C07D499/68 ,  C07D499/74 ,  C07D499/76 ,  C07D499/80 ,  C07D499/90 ,  C07D499/32 ,  A61K31/425

    CPC classification number: C07D499/00

    Abstract: 6-Amino-spiro[penam-2,4'-piperidine]-3-carboxylic acid derivatives having the formula ##STR1## wherein R is a methyl, phenyl or benzyl radical, Z.sub.1 is a hydrogen atom and Z.sub.2 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 Z.sub.1 and Z.sub.2 together represent a bivalent radical Z.sub.3 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.

    Abstract translation: 6-氨基螺[penam-2,4'-哌啶] -3-羧酸衍生物，其结构式为：其中R为甲基，苯基或苄基，Z1为氢原子，Z2为选自 由青霉素化学已知的那些，优选2-苯基乙酰基，2-氨基-2-苯基乙酰基，5-甲基-3-苯基-4-异恶唑羰基或2,6-二甲氧基苯甲酰基，或Z 1和Z 2一起代表二价基团Z 3 并且优选为（六氢-1H-吖庚因-1-基）亚甲基，以及其药学上可接受的无毒盐及其制备方法。 这些化合物具有有价值的抗菌性质，可用作治疗由革兰氏阳性菌和革兰氏阴性菌引起的传染病的治疗剂。

    2-[4-(Diphenylmethyl)-1-piperazinyl]-acetic acids and their amides
    7.
    发明授权
    2-[4-(Diphenylmethyl)-1-piperazinyl]-acetic acids and their amides 失效
    2- [4-（二苯基甲基）-1-哌嗪基] - 乙酸及其酰胺

    公开(公告)号：US4525358A

    公开(公告)日：1985-06-25

    申请号：US496489

    申请日：1983-05-17

    Applicant: Eugene Baltes ,  Jean de Lannoy ,  Ludovic Rodriguez

    Inventor： Eugene Baltes ,  Jean de Lannoy ,  Ludovic Rodriguez

    IPC: C07D295/08 ,  A61K31/495 ,  A61P37/08 ,  C07D295/088 ,  A61K31/50 ,  C07D295/14

    CPC classification number: 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 ##STR1## wherein Y=--OH or --NH.sub.2 ; 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.

    Abstract translation: 新的2- [4-（二苯基甲基）-1-哌嗪基] - 乙酸，它们的酰胺及其盐，其制备方法和治疗组合物。 这些化合物具有其中Y = -OH或-NH 2的式“IMAGE”; X和X'= H，卤素，烷氧基或三氟甲基; m = 1或2，n = 1或2. 2- [4-（二苯基甲基）-1-哌嗪基] - 乙酸的酰胺通过1-（二苯基甲基） - 哌嗪与ω加酰胺乙酰胺或 通过使ω-[4-（二苯基甲基）-1-哌嗪基] - 烷醇的碱金属盐与2-卤代乙酰胺反应，或者通过使氨与2- [4-（二苯基甲基） -1-哌嗪基] - 乙酸，而2- [4-（二苯基甲基）-1-哌嗪基] - 乙酸通过水解相应的酰胺或低级烷基酯来制备。 这些化合物特别具有抗过敏，解痉和抗组胺活性。

    Amino-spiro[oxa(or thia)cycloalkane-penam]-carboxylic acid derivatives
    9.
    发明授权
    Amino-spiro[oxa(or thia)cycloalkane-penam]-carboxylic acid derivatives 失效
    氨基螺（8）氧杂（或硫杂）环烷烃 - penam {9-羧酸衍生物

    公开(公告)号：US4139628A

    公开(公告)日：1979-02-13

    申请号：US869860

    申请日：1978-01-16

    Applicant: Ludovic Rodriguez ,  Jacques Leclercq ,  Pierre Ykman ,  Eric Cossement

    Inventor： Ludovic Rodriguez ,  Jacques Leclercq ,  Pierre Ykman ,  Eric Cossement

    IPC: C07D513/20 ,  A61K31/43 ,  A61K31/431 ,  A61P31/04 ,  C07D499/00 ,  C07D499/21 ,  C07D499/44 ,  C07D499/90

    CPC classification number: C07D499/00

    Abstract: Amino-spiro[oxa(or thia)cycloalkane-penam]-carboxylic acid derivatives having the formula ##STR1## WHEREIN X is a sulfur or oxygen atom or the sulfinyl group, n is 1 or 2, m is 1 or 2, R.sub.1 is hydrogen, R.sub.2 is one of the radicals known in the chemistry of the penicillins, preferably 2-phenylacetyl, 2-amino-2-phenylacetyl, 5-methyl-3-phenyl-4-isoxazolecarbonyl or 2,6-dimethoxybenzoyl, or R.sub.1 and R.sub.2 together represent a bivalent radical R.sub.3, preferably (hexahydro-1H-azepin-1-yl)methylene and their therapeutically acceptable non-toxic salts 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.

    Abstract translation: 具有式“IMAGE”的X'（或硫杂）环烷烃 - penam] - 羧酸衍生物，X为硫或氧原子或亚磺酰基，n为1或2，m为1或2，R 1为 氢，R2是青霉素化学中已知的基团之一，优选2-苯乙酰基，2-氨基-2-苯乙酰基，5-甲基-3-苯基-4-异恶唑羰基或2,6-二甲氧基苯甲酰基，或R1和 R2一起代表二价基团R 3，优选（六氢-1H-吖庚因-1-基）亚甲基及其治疗上可接受的无毒盐及其制备方法。

    6'-Amino-spiro(cycloalkane-1,2'-penam)-3'-carboxylic acids
    10.
    发明授权
    6'-Amino-spiro(cycloalkane-1,2'-penam)-3'-carboxylic acids 失效
    6 {40-氨基螺（环烷-1,1 {40-对氨基）-3 {40-羧酸

    公开(公告)号：US4091027A

    公开(公告)日：1978-05-23

    申请号：US800082

    申请日：1977-05-24

    Applicant: Ludovic Rodriguez ,  Jacques Leclercq

    Inventor： Ludovic Rodriguez ,  Jacques Leclercq

    IPC: C07D277/60 ,  C07D499/00 ,  C07D499/42

    CPC classification number: C07D277/60 ,  C07D499/00 ,  Y02P20/55

    Abstract: 6'-Amino-spiro[cycloalkane-1,2'-penam]-3'-carboxylic acids of the formula ##STR1## WHEREIN Z is a hydrogen or an alkali metal atom, or a protective group, and n a whole number of from 3 to 6, and process of preparing the same.These compounds are useful as intermediates in the synthesis of a new group of antibiotics having properties similar to the penicillins.

    Abstract translation: 式“IMAGE”的6'-氨基螺[环烷-1,2'-半胱氨酸] -3'-羧酸，其中Z是氢或碱金属原子，或保护基，并且na整数 3〜6及其制备方法。

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