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    Aromatic acid intermediates
    1.
    发明授权
    Aromatic acid intermediates 失效
    芳香酸中间体

    公开(公告)号：US5250725A

    公开(公告)日：1993-10-05

    申请号：US754037

    申请日：1991-09-03

    申请人： Dominique Olliero ,  Bernard Labeeuw ,  Gilles Roche ,  Ali Salhi

    发明人： Dominique Olliero ,  Bernard Labeeuw ,  Gilles Roche ,  Ali Salhi

    IPC分类号： C07C311/32 ,  C07D501/34 ,  C07C311/17

    CPC分类号： C07D501/34 ,  C07C311/32

    摘要： The present invention relates to novel cephalosporin derivatives with improved pharmacokinetics, corresponding to the formula: ##STR1## in which: R.sub.1, R.sub.2 and R.sub.3 represent a hydrogen atom, or R.sub.1 and R.sub.2 represent a hydrogen atom or a methyl group and R.sub.3 represents a carboxyl group, or ##STR2## form a cyclobutyl group and R.sub.3 represents a carboxyl group; and A and B are different and occupy the meta and para positions of the benzene ring, one representing a hydroxyl group and the other being selected from the groups ##STR3## and --NH--SO.sub.2 --Alk--NH.sub.2 in which Alk denotes a C.sub.2 -C.sub.4 lower alkylene group and also to the pharmaceutically acceptable salts and esters of the said derivatives.It further relates to a process for the preparation of such cephalosporins and to pharmaceutical compositions in which they are present.

    摘要翻译： 本发明涉及具有改善的药代动力学的新型头孢菌素衍生物，其对应于下式：其中：R 1，R 2和R 3表示氢原子，或R 1和R 2表示氢原子或甲基 并且R 3表示羧基，或形成环丁基，R 3表示羧基; 并且A和B不同，占据苯环的间位和对位，一个表示羟基，另一个选自下组：其中R 1，R 2，R 2， Alk表示C2-C4低级亚烷基，也表示所述衍生物的药学上可接受的盐和酯。 本发明还涉及一种制备这种头孢菌素的方法及其存在的药物组合物。

    Cephalosporin derivatives and pharmaceutical compositions in which they are present
    2.
    发明授权
    Cephalosporin derivatives and pharmaceutical compositions in which they are present 失效
    CEPHALOSPORIN衍生物及其现有的药物组合物

    公开(公告)号：US5079241A

    公开(公告)日：1992-01-07

    申请号：US420270

    申请日：1989-10-13

    申请人： Dominique Olliero ,  Bernard Labeeuw ,  Gilles Roche ,  Ali Salhi

    发明人： Dominique Olliero ,  Bernard Labeeuw ,  Gilles Roche ,  Ali Salhi

    IPC分类号： C07C311/08 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07C303/38 ,  C07C311/32 ,  C07C311/46 ,  C07D501/04 ,  C07D501/34

    CPC分类号： C07D501/34 ,  C07C311/32

    摘要： The present invention relates to novel cephalosporin derivatives with improved pharmacokinetics, corresponding to the formula: ##STR1## in which: R.sub.1, R.sub.2 and R.sub.3 represent a hydrogen atom, or R.sub.1 and R.sub.2 represent a hydrogen atom or a methyl group and R.sub.3 represents a carboxyl group, or ##STR2## form a cyclobutyl group and R.sub.3 represents a carboxyl group; and A and B are different and occupy the meta and para positions of the benzene ring, one representing a hydroxyl group and the other being selected from the groups ##STR3## and --NH--SO.sub.2 --Alk--NH.sub.2 in which Alk denotes a C.sub.2 -C.sub.4 lower alkylene group and also to the pharmaceutically acceptable salts and esters of the said derivatives.It further relates to a process for the preparation of such cephalosporins and to pharmaceutical compositions in which they are present.

    摘要翻译： 本发明涉及具有改善的药代动力学的新型头孢菌素衍生物，其对应于下式：其中：R 1，R 2和R 3表示氢原子，或R 1和R 2表示氢原子或甲基 并且R 3表示羧基，或形成环丁基，R 3表示羧基; A和B不同，占据苯环的间位和对位，一个表示羟基，另一个选自基团，其中Alk表示 C2-C4低级亚烷基，以及所述衍生物的药学上可接受的盐和酯。 本发明还涉及一种制备这种头孢菌素的方法及其存在的药物组合物。

    Cephalosporin derivatives, and their application as antibiotics
    3.
    发明授权
    Cephalosporin derivatives, and their application as antibiotics 失效
    头孢菌素衍生物及其作为抗生素的应用

    公开(公告)号：US4950661A

    公开(公告)日：1990-08-21

    申请号：US188073

    申请日：1988-04-28

    申请人： Dominique Olliero ,  Ali Salhi

    发明人： Dominique Olliero ,  Ali Salhi

    IPC分类号： C07D501/20 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/34 ,  C07D501/36 ,  C07D501/46 ,  C07D501/56

    CPC分类号： C07D501/36 ,  C07D501/34 ,  Y02P20/55

    摘要： The present invention relates to derivatives of the cephalosporin family, of formula: ##STR1## in which: X is an oxygen atom or a sulfur atomn is zero, 1 or 2.R.sub.1, R.sub.2 and R.sub.3 each designate, a hydrogen atom or else R.sub.1 and R.sub.2 designate a hydrogen atom or a methyl group, and R.sub.3 designates a carboxyl or cyclopropyl group, or elseR.sub.1 and R.sub.2 taken together with the carbon atom to which they are linked form a cyclobutyl or cyclopentyl group and R.sub.3 is a carboxyl group.B is the residue of a primary or secondary amine;their preparation process and application in therapeutics.

    摘要翻译： 本发明涉及头孢菌素家族的衍生物，其结构如下：其中：X是氧原子或硫原子，n是0,1或2.R 1，R 2和R 3各自表示氢 或者R 1和R 2表示氢原子或甲基，R 3表示羧基或环丙基，或者R 1和R 2与它们所连接的碳原子一起形成环丁基或环戊基，R 3为 羧基。 B是伯胺或仲胺的残基; 其制备方法和在治疗中的应用。

    Antibiotic compounds derived from cephalosporins, process for their production and pharmaceutical compositions
    4.
    发明授权
    Antibiotic compounds derived from cephalosporins, process for their production and pharmaceutical compositions 失效
    来自头孢菌素的抗生素化合物，其制备方法和药物组合物

    公开(公告)号：US4656166A

    公开(公告)日：1987-04-07

    申请号：US612896

    申请日：1984-05-22

    申请人： Ali Salhi ,  Dominique Olliero

    发明人： Ali Salhi ,  Dominique Olliero

    IPC分类号： A61K20060101 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/24 ,  C07D501/26 ,  C07D501/34 ,  C07D501/36 ,  C07D501/46 ,  C07D501/54 ,  C07D501/56 ,  C07D501/60

    CPC分类号： C07D501/36 ,  C07D501/34

    摘要： The compounds according to the invention correspond to the formula: ##STR1## in which: The COOA group at the 4 position is an acid radical, or an alkaline or alkaline-earth salt, or an amino acid or amine salt, for example triethylamine or ethanolamines, or an easily hydrolyzable or metabolically labile and pharmaceutically acceptable ester radical.X denotes an oxygen atom or a sulfur atomn is zero or 1R.sub.1 and R.sub.2 each denote independently hydrogen or a lower alkyl group, preferably a methyl group, orR.sub.1 and R.sub.2 taken together with the carbon atom to which they are linked form a cyclobutyl or cyclopentyl nucleus.B is the residue of a primary or secondary amine.

    摘要翻译： 根据本发明的化合物对应于下式：其中：4位的COOA基团是酸基或碱金属或碱土金属盐或氨基酸或胺盐，用于 例如三乙胺或乙醇胺，或易水解或代谢不稳定和药学上可接受的酯基。 X表示氧原子或硫原子，n为0或1，R 1和R 2各自独立地表示氢或低级烷基，优选甲基，或者R 1和R 2与它们所连接的碳原子一起形成环丁基 或环戊基核。 B是伯胺或仲胺的残基。

    Derivatives of 1,3,4-thiadiazole, a method of obtaining them and pharmaceutical compositions containing them
    6.
    发明授权
    Derivatives of 1,3,4-thiadiazole, a method of obtaining them and pharmaceutical compositions containing them 失效
    1,3,4-噻二唑的衍生物，获得它们的方法和含有它们的药物组合物

    公开(公告)号：US5086053A

    公开(公告)日：1992-02-04

    申请号：US394321

    申请日：1989-08-16

    申请人： Roger Brodin ,  Dominique Olliero ,  Paul Worms

    发明人： Roger Brodin ,  Dominique Olliero ,  Paul Worms

    IPC分类号： C07D285/12 ,  A61K31/41 ,  A61K31/433 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61P25/00 ,  C07D285/135 ,  C07D417/04 ,  C07D417/12

    CPC分类号： C07D285/135 ,  C07D417/04 ,  C07D417/12

    摘要： The present invention relates to thiadiazole derivatives having the formula: ##STR1## in which: R.sub.1 represents a phenyl group, non-substituted or substitued 1 to 3 times by a halogen atom, preferably chlorine or fluorine, or by a C.sub.1 -C.sub.4 alkyl group, preferably the methyl group, or by a C.sub.1 -C.sub.4 alkoxy group, preferably the methoxy group, or by a hydroxy group or by a trifluoromethyl group or a phenyl group substituted simultaneously by 1 to 3 halogen atoms and by 1 or 2 methyl groupings;R.sub.2 represents hydrogen or a C.sub.1 -C.sub.4 alkyl group,R.sub.3 represents an alkylamino group or a heterocyclic group,Application: Drugs for treatment of notably senile dementia.

    摘要翻译： 本发明涉及具有下式的噻二唑衍生物：其中：R 1表示苯基，被卤素原子，优选氯或氟或未被取代或取代1至3倍的苯基，或由C1- C4烷基，优选甲基，或通过C1-C4烷氧基，优选甲氧基，或羟基或被同时被1至3个卤素原子取代的三氟甲基或苯基取代，以及1或2个 甲基组; R2表示氢或C1-C4烷基，R3表示烷基氨基或杂环基。应用：用于治疗特别是老年性痴呆的药物。

    Carboxamidothiazole derivatives, preparation, pharmaceutical compositions containing them
    7.
    发明授权
    Carboxamidothiazole derivatives, preparation, pharmaceutical compositions containing them 失效
    载体酰胺噻唑衍生物，制剂，含有它们的药物组合物

    公开(公告)号：US06380230B1

    公开(公告)日：2002-04-30

    申请号：US09508830

    申请日：2000-06-02

    申请人： Roger Brodin ,  Robert Boigegrain ,  Eric Bignon ,  Jean Charles Molimard ,  Dominique Olliero

    发明人： Roger Brodin ,  Robert Boigegrain ,  Eric Bignon ,  Jean Charles Molimard ,  Dominique Olliero

    IPC分类号： C07D41712

    CPC分类号： C07D471/04 ,  C07D417/12 ,  C07D417/14

    摘要： The present invention relates to cholecystokinin (CCK)-agonist substituted thiazoles of formula: in which R1 is a substituted phenyl group, R2 is a group chosen from CH2—R7, (CH2)2—R7, S—CH2—R7, CH2—S—R7 and (C5-C8)alkyl with R7 being a (C5-C7)cycloalkyl group, and R3 is a group with R8 being a group (CH2)nR15 or and R15 being COOH or COO(C1-C4)alkyl. The invention also relates to a process for the preparation of the pharmaceutical compositions containing them and to their uses for the preparation of medicines.

    摘要翻译： 本发明涉及下列通式的缩胆囊素（CCK） - 拮抗剂取代的噻唑：其中R1是取代的苯基，R2是选自CH2-R7，（CH2）2-R7，S-CH2-R7，CH2- S-R7和（C5-C8）烷基，其中R7是（C5-C7）环烷基，R3是具有R8（CH 2）nR15的基团，R15是COOH或COO（C1-C4）烷基）。 本发明还涉及制备含有它们的药物组合物及其用于制备药物的用途的方法。

    Thiazole derivatives active on the cholinergic system, process for obtention and pharmaceutical compositions
    9.
    发明授权
    Thiazole derivatives active on the cholinergic system, process for obtention and pharmaceutical compositions 失效
    在胆碱能系统上活性的噻唑衍生物，获得的过程和药物组合物

    公开(公告)号：US5232921A

    公开(公告)日：1993-08-03

    申请号：US632609

    申请日：1990-12-27

    申请人： Kathleen Biziere ,  Dominique Olliero ,  Paul Worms

    发明人： Kathleen Biziere ,  Dominique Olliero ,  Paul Worms

    IPC分类号： C07D277/42 ,  C07D277/60 ,  C07D277/84

    CPC分类号： C07D277/60 ,  C07D277/42 ,  C07D277/84

    摘要： The invention relates to thiazole derivatives corresponding to the general formula: ##STR1## in which: R.sub.1 and R.sub.2 each independently represent hydrogen; a C.sub.1 -C.sub.4 alkyl group; a phenyl group or a phenyl group monosubstituted or polysubstituted by a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy, nitro or hydroxyl group; or one of the groups R.sub.1 and R.sub.2 denotes hydrogen and the other represents a naphthyl group; a benzyl group; an .alpha.,.alpha.-dimethyl-benzyl group; a cyclohexyl group; a biphenyl group; a thienyl group of an adamantyl group; or alternatively R.sub.1 and R.sub.2, taken together, represent a group; ##STR2## in which the phenyl group is bonded to the 4-position of the thiazole and the group (CH.sub.2).sub.m to the 5-position, m represents an integer equal to 2 or 3 and R.sub.5 denotes hydrogen or a nitro group, R.sub.3 is H or an alkyl group and R.sub.4 is notably an alkyl substituted by an amino group, a pyrrolidino, or a pyridino group.

    摘要翻译： 本发明涉及对应于以下通式的噻唑衍生物：其中：R 1和R 2各自独立地表示氢; C1-C4烷基; 苯基或被卤素原子，C1-C4烷基，C1-C4烷氧基，硝基或羟基单取代或多取代的苯基; 或者R1和R2中的一个表示氢，另一个表示萘基; 苄基; α，α-二甲基 - 苄基; 环己基; 联苯基 金刚烷基的噻吩基; 或者R1和R2一起表示一个基团; 其中苯基与噻唑的4-位键合（CH2）m至5-位，m表示等于2或3的整数，R 5表示氢或硝基，R 3 是H或烷基，R4特别是被氨基，吡咯烷子基或吡啶基取代的烷基。