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44 条记录 (耗时 0.027 秒)

    Benzimidazole derivatives useful as antiproliferative agents
    21.
    发明授权
    Benzimidazole derivatives useful as antiproliferative agents 有权
    可用作抗增殖剂的苯并咪唑衍生物

    公开(公告)号：US07019147B1

    公开(公告)日：2006-03-28

    申请号：US10148335

    申请日：2000-11-10

    申请人： Wayne E. Barth ,  Michael J. Luzzio ,  Joseph P. Lyssikatos

    发明人： Wayne E. Barth ,  Michael J. Luzzio ,  Joseph P. Lyssikatos

    IPC分类号： C07D27/02 ,  C07D401/00 ,  C07D215/20 ,  A61K31/47 ,  A01N43/50

    CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D413/14 ,  C07D417/14 ,  C07D491/04 ,  C07D491/10

    摘要： The invention relates to compounds of formula (1) and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R7, R8, R9, R10, and R11 are as defined herein. The invention also relates to methods of treating abnormal cell growth, such as cancer, in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula (1). The invention also relates to methods of preparing the compounds of formula (1).

    摘要翻译： 本发明涉及式（1）的化合物及其药学上可接受的盐，前药和溶剂化物，其中R 1，R 7，R 8， >，R 9，R 10和R 11如本文所定义。 本发明还涉及通过施用式1化合物和用于治疗含有式（1）化合物的这种病症的药物组合物来治疗哺乳动物中异常细胞生长如癌症的方法。 本发明还涉及制备式（1）化合物的方法。

    6-Aminoalkylpenicillanic acid 1,1-dioxides as beta-lactamase inhibitors
    22.
    发明授权
    6-Aminoalkylpenicillanic acid 1,1-dioxides as beta-lactamase inhibitors 失效
    6-氨基烷基青霉烷酸1,1-二氧化物作为β-内酰胺酶抑制剂

    公开(公告)号：US4452796A

    公开(公告)日：1984-06-05

    申请号：US434371

    申请日：1982-10-21

    申请人： Wayne E. Barth

    发明人： Wayne E. Barth

    IPC分类号： A61K31/43 ,  A61K31/545 ,  C07D499/00 ,  C07D499/32 ,  C07D519/00 ,  C07D499/46

    CPC分类号： A61K31/43 ,  A61K31/545 ,  C07D499/00

    摘要： Beta-lactamase inhibitors which are 6-alpha- and 6-beta-(aminomethyl) and (1-aminoethyl)pencillanic acid 1,1-dioxides; pharmaceutically-acceptable salts thereof; conventional esters thereof which are hydrolyzable in vivo; bis-methanediol esters thereof; or mixed methanediol esters with said beta-lactamase inhibitors and sulbactam. Pharmaceutical compositions comprising said beta-lactamase inhibitors and a conventional beta-lactam antibiotic, used in the treatment of bacterial infections. Compounds useful as intermediates in the synthesis of said beta-lactamase inhibitors. Antibacterial mixed bis-methanediol esters of said aminoalkyl penicillanic acid 1,1-dioxides and ampicillin or amoxicillin, also used in the treatment of bacterial infections; and intermediates therefor.

    摘要翻译： β-内酰胺酶抑制剂，其为6-α-和6-β-（氨基甲基）和（1-氨基乙基）pencillanic acid 1,1-二氧化物; 其药学上可接受的盐; 其在体内可水解的其常规酯; 双甲烷二醇酯; 或与所述β-内酰胺酶抑制剂和舒巴坦混合的甲二醇酯。 包含所述β-内酰胺酶抑制剂和用于治疗细菌感染的常规β-内酰胺抗生素的药物组合物。 可用作合成所述β-内酰胺酶抑制剂的中间体的化合物。 所述氨基烷基青霉烷酸1,1-二氧化物和氨苄青霉素或阿莫西林的抗菌混合双甲磺酸酯也用于治疗细菌感染; 及其中间体。

    6-Aminomethylpenicillanic acid 1,1-dioxide derivatives as beta-lactamase inhibitors
    23.
    发明授权
    6-Aminomethylpenicillanic acid 1,1-dioxide derivatives as beta-lactamase inhibitors 失效
    6-氨基甲基青霉烷酸1,1-二氧化物衍生物作为β-内酰胺酶抑制剂

    公开(公告)号：US4427678A

    公开(公告)日：1984-01-24

    申请号：US388323

    申请日：1982-06-14

    申请人： Wayne E. Barth

    发明人： Wayne E. Barth

    IPC分类号： A61K20060101 ,  A61K31/43 ,  A61K31/545 ,  C07C20060101 ,  C07D499/00 ,  C07D519/00

    CPC分类号： A61K31/43 ,  A61K31/545 ,  C07D499/00

    摘要： beta-Lactamase inhibitors which are 6-alpha- and 6-beta(aminomethyl)pencillanic acid 1,1-dioxides which are substituted on amino nitrogen with benzyl, hydroxybenzyl, picolyl or phenethyl; pharmaceutically-acceptable salts thereof; conventional esters thereof hydrolyzable in vivo; pharmaceutical compositions thereof with conventional beta-lactam antibiotics; and a method of treating bacterial infections with said pharmaceutical compositions.

    摘要翻译： β-内酰胺酶抑制剂，其是在氨基氮上被苄基，羟基苄基，吡啶甲基或苯乙基取代的6-α和6-β（氨基甲基）青霉酸1,1-二氧化物; 其药学上可接受的盐; 其在体内可水解的常规酯; 其药物组合物与常规的β-内酰胺抗生素; 以及用所述药物组合物治疗细菌感染的方法。

    Antibacterial 3-phosphono penams
    27.
    发明授权
    Antibacterial 3-phosphono penams 失效
    抗菌3-膦酰基阴茎

    公开(公告)号：US4031077A

    公开(公告)日：1977-06-21

    申请号：US680423

    申请日：1976-04-26

    申请人： Wayne E. Barth

    发明人： Wayne E. Barth

    IPC分类号： A23K1/16 ,  A23K1/17 ,  A61K31/426 ,  A61K31/43 ,  A61K31/675 ,  A61P31/04 ,  C07D277/10 ,  C07D499/00 ,  C07F9/6561 ,  C07D499/32

    CPC分类号： C07D499/00 ,  A23K20/116 ,  A23K20/137 ,  C07D277/10 ,  C07F9/65611

    摘要： The present invention discloses novel 6-acylamino-2,2-dimethyl-3-phosphonopenams and certain lower alkyl esters thereof possessing antibacterial activity, methods for their production, and intermediates therefor; the production comprises the steps of reacting 6-triphenylmethylamino-2,2-dimethylpenam-3-carboxylic acid with lead tetraacetate to form the corresponding 3-acetoxy compound, the latter is converted to .alpha.-triphenylmethylamino-5,5-dimethyl-3-thiazoline-2-acetic acid which is condensed with dimethyl phosphite to produce .alpha.-triphenylmethylamino-5,5-dimethyl-4(0,0-dimethylphosphono)-thiazolidine-2-acetic acid which is cyclized to 6-triphenylmethylamino-2,2-dimethyl-3-(0,0-dimethylphosphono)penam and the latter is subsequently deblocked and acylated.

    摘要翻译： 本发明公开了具有抗菌活性的新颖的6-酰基氨基-2,2-二甲基-3-膦草丁酸及其某些低级烷基酯，其生产方法及其中间体; 该制备包括使6-三苯基甲基氨基-2,2-二甲基联苯-3-羧酸与四乙酸铅反应形成相应的3-乙酰氧基化合物的步骤，将其转化成α-三苯甲基氨基-5,5-二甲基-3- 与亚磷酸二甲酯缩合以产生α-三苯基甲基氨基-5,5-二甲基-4（0,0-二甲基膦酰基） - 噻唑烷-2-炔酸的4-噻唑啉-2-乙酸，将其环化为6-三苯基甲基氨基-2， 2-二甲基-3-（0,0-二甲基膦酰基）半缩醛，后者随后被去封闭并酰化。

    Process for preparing 6-chloro-2-chloromethyl-4-phenylquinazoline-3-oxide and intermediates therefor
    29.
    发明授权
    Process for preparing 6-chloro-2-chloromethyl-4-phenylquinazoline-3-oxide and intermediates therefor 失效
    制备6-氯-2-氯代乙酰基-4-苯基环丙烷-3-氧化物的方法及其中间体

    公开(公告)号：US3998883A

    公开(公告)日：1976-12-21

    申请号：US626319

    申请日：1975-10-28

    申请人： Susumu Nakanishi ,  Wayne E. Barth

    发明人： Susumu Nakanishi ,  Wayne E. Barth

    IPC分类号： C07D239/76 ,  C07C119/00

    CPC分类号： C07D239/76

    摘要： A novel process is described for the preparation of 6-chloro-2-chloromethyl-4-phenylquinazoline-3-oxide, a key intermediate in the synthesis of the known useful psychotherapeutic agents: chlorodiazepoxide and diazepam. This intermediate is prepared by the cyclization of 2-(1'-chloroimino-2'-chloromethyl)-5-chlorobenzophenone, itself a new compound. This compound in turn is prepared by the chloroacetylation of 2-amino-5-chlorobenzophenone to 2-chloroacetamido-5-chlorobenzophenone, another novel compound, and subsequent iminochloride formation.

    Method of preventing asthmatic symptoms
    30.
    发明授权
    Method of preventing asthmatic symptoms 失效
    预防哮喘症状的方法

    公开(公告)号：US3968213A

    公开(公告)日：1976-07-06

    申请号：US541017

    申请日：1975-01-14

    申请人： Wayne E. Barth

    发明人： Wayne E. Barth

    IPC分类号： A61K31/505 ,  C07D239/36

    CPC分类号： C07D239/36 ,  A61K31/505

    摘要： 5-Carboxypyrimidine derivatives and their pharmaceutically acceptable basic salts, and their use as antiallergy agents.

    摘要翻译： 5-羧甲嘧啶衍生物及其药学上可接受的碱性盐，以及它们作为抗过敏剂的用途。