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151 条记录 (耗时 0.029 秒)

    Process for the synthesis of 3-cyano-6-alkoxy-7-nitro-4-quinolones
    45.
    发明授权
    Process for the synthesis of 3-cyano-6-alkoxy-7-nitro-4-quinolones 失效
    合成3-氰基-6-烷氧基-7-硝基-4-喹诺酮的方法

    公开(公告)号：US06933388B2

    公开(公告)日：2005-08-23

    申请号：US10820115

    申请日：2004-04-07

    申请人： Scott Mason Duncan ,  Miguel Angel Pagan ,  Middleton Brawner Floyd, Jr.

    发明人： Scott Mason Duncan ,  Miguel Angel Pagan ,  Middleton Brawner Floyd, Jr.

    IPC分类号： C07D215/56 ,  C07D215/36

    CPC分类号： C07D215/56

    摘要： There is provided a process for the preparation of 3-cyano-6-alkoxy-7-nitro-4-quinolone intermediates useful for the preparation of protein tyrosine kinase (PTK) inhibitors which are useful in the treatment of cancer of the formula: wherein R is alkyl(C1-C3) prepared by reacting a substituted anthranilate with N,N-dimethylformamide dimethyacetal to obtain a N,N-dimethylamidine which is condensed with t-butylcyanoacetate to obtain a N-(2-cyano-2-t-butoxycarbonylvinyl)anthranilate, which is hydrolyzed to yield a N-(2-cyano-2-carboxyvinyl)anthranilate followed by decarboxylating to obtain a N-(2-cyano-2-carboxyvinyl)anthranilate followed by cyclizing to obtain a 3-cyano-6-alkoxy-7-nitro-4-quinolone.

    摘要翻译： 提供了用于制备可用于治疗下列癌症的蛋白酪氨酸激酶（PTK）抑制剂的3-氰基-6-烷氧基-7-硝基-4-喹诺酮中间体的方法：其中 R是通过使取代的邻氨基苯甲酸酯与N，N-二甲基甲酰胺二甲基缩醛反应制得的烷基（C 1 -C 3 -C 3），得到与t缩合的N，N-二甲基脒 （2-氰基-2-叔丁氧基羰基乙烯基）邻氨基苯甲酸酯，将其水解，得到N-（2-氰基-2-羧基乙烯基）邻氨基苯甲酸酯，然后脱羧，得到N-（2-氰基-2- -2-羧基乙烯基）邻氨基苯甲酸甲酯，然后环化，得到3-氰基-6-烷氧基-7-硝基-4-喹诺酮。

    6-[(Substituted)phenyl]triazolopyrimidines as anticancer agents
    46.
    发明申请
    6-[(Substituted)phenyl]triazolopyrimidines as anticancer agents 失效
    6 - [（取代的）苯基]三唑并嘧啶作为抗癌剂

    公开(公告)号：US20050090508A1

    公开(公告)日：2005-04-28

    申请号：US10950543

    申请日：2004-09-24

    申请人： Nan Zhang ,  Semiramis Ayral-Kaloustian ,  Thai Nguyen ,  Yanzhong Wu ,  Wei Tong

    发明人： Nan Zhang ,  Semiramis Ayral-Kaloustian ,  Thai Nguyen ,  Yanzhong Wu ,  Wei Tong

    IPC分类号： A61P35/00 ,  A61P35/04 ,  C07D487/04 ,  A61K31/519

    CPC分类号： C07D487/04

    摘要： This invention relates to certain 6-[(substituted)phenyl]triazolopyrimidine compounds or pharmaceutically acceptable salts thereof, and compositions containing said compounds or pharmaceutically acceptable salts thereof, wherein said compounds are anti-cancer agents useful for the treatment of cancer in mammals. This invention further relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal and further provides a method for the treatment or prevention of cancerous tumors that express multiple drug resistance (MDR) or are resistant because of MDR, in a mammal in need thereof which method comprises administering to said mammal an effective amount of said compounds or pharmaceutically acceptable salts thereof. The present invention relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal in need thereof by promotion of microtubule polymerization which comprises administering to said mammal an effective amount of said compounds and pharmaceutically acceptable salts thereof.

    摘要翻译： 本发明涉及某些6 - [（取代的）苯基]三唑并嘧啶化合物或其药学上可接受的盐，以及含有所述化合物或其药学上可接受的盐的组合物，其中所述化合物是可用于治疗哺乳动物癌症的抗癌剂。 本发明还涉及治疗或抑制哺乳动物中癌性肿瘤细胞和相关疾病的生长的方法，并进一步提供了治疗或预防表达多重耐药性（MDR）或耐多药耐药性的癌性肿瘤的方法 在有需要的哺乳动物中，所述方法包括向所述哺乳动物施用有效量的所述化合物或其药学上可接受的盐。 本发明涉及通过促进微管聚合来治疗或抑制有需要的哺乳动物中癌性肿瘤细胞和相关疾病的生长的方法，其包括对所述哺乳动物施用有效量的所述化合物及其药学上可接受的盐。

    Method of enhancing immune responses to herpes
    48.
    发明授权
    Method of enhancing immune responses to herpes 失效
    增强单纯疱疹病毒疫苗免疫应答的方法

    公开(公告)号：US06867000B2

    公开(公告)日：2005-03-15

    申请号：US10169057

    申请日：2000-12-07

    申请人： Eric M. Mishkin ,  Robert J. Natuk ,  Michael W. Pride ,  Maninder K. Sidhu

    发明人： Eric M. Mishkin ,  Robert J. Natuk ,  Michael W. Pride ,  Maninder K. Sidhu

    IPC分类号： A61K39/12 ,  A61K39/245 ,  A61K39/39 ,  C12Q1/68

    CPC分类号： A61K39/39 ,  A61K39/12 ,  A61K39/245 ,  A61K2039/53 ,  A61K2039/545 ,  A61K2039/55505 ,  A61K2039/55522 ,  A61K2039/55538 ,  A61K2039/57 ,  C12N2710/16634

    摘要： A method for inducing and enhancing protective and/or therapeutic immunity in a mammal to HSV includes the steps of at least one immunization with an effective amount of a DNA vaccine composition which comprises a first nucleic acid molecule comprising a DNA sequence encoding the HSV type 1 or type 2 gD protein, and a second nucleic acid molecule comprising a DNA sequence encoding each Interleukin-12 heterodimer subunit. The method also comprises at least one subsequent immunization with an effective amount of a protein vaccine composition which comprises the HSV type 1 or type 2 gD protein; and the IL-12 heterodimer. A local anesthetic may be included in the DNA vaccine composition in an amount that forms one or more complexes with the nucleic acid molecules. When provided to the mammal in suitable effective dosages according to this protocol, the vaccine compositions used in this method produce an unexpectedly good protective and/or therapeutic immune response against HSV in an immunized mammal.

    摘要翻译： 用于诱导和增强哺乳动物对HSV的保护和/或治疗免疫的方法包括以下步骤：用有效量的DNA疫苗组合物进行至少一次免疫，所述DNA疫苗组合物包含第一核酸分子，其包含编码HSV 1型的DNA序列 或2型GD蛋白，以及包含编码每个白细胞介素-12异二聚体亚基的DNA序列的第二核酸分子。 该方法还包括至少一次随后的免疫与有效量的包含HSV 1型或2型GD蛋白的蛋白质疫苗组合物; 和IL-12异源二聚体。 局部麻醉剂可以以与核酸分子形成一种或多种复合物的量包含在DNA疫苗组合物中。 当根据本方案以合适的有效剂量提供给哺乳动物时，在该方法中使用的疫苗组合物在免疫的哺乳动物中产生意想不到的良好的针对HSV的保护性和/或治疗性免疫应答。

    Process for preparation of 4-amino-3-quinolinecarbonitriles
    49.
    发明申请
    Process for preparation of 4-amino-3-quinolinecarbonitriles 失效
    制备4-氨基-3-喹啉碳腈的方法

    公开(公告)号：US20050043537A1

    公开(公告)日：2005-02-24

    申请号：US10918947

    申请日：2004-08-16

    申请人： Karen Sutherland ,  Gregg Feigelson ,  Diane Boschelli ,  David Blum ,  Henry Strong

    发明人： Karen Sutherland ,  Gregg Feigelson ,  Diane Boschelli ,  David Blum ,  Henry Strong

    IPC分类号： C07D215/54 ,  C07D405/04 ,  C07D495/04 ,  C07D215/38

    CPC分类号： C07D405/04 ,  C07D215/54 ,  C07D495/04

    摘要： This invention discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile comprising combining an amine compound with a cyanoacetic acid and an acid catalyst to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline in an alcoholic solvent and a trialkylorthoformate to yield a 3-amino-2-cyanoacrylamide; combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride in acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 4-amino-3-quinolinecarbonitrile and also discloses a process for the preparation of a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile comprising combining a disubstituted 3-amino thiophene with a cyanoacetamide and trialkylorthoformate in an alcoholic solvent to obtain a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride and acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile and also discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile by combining an amine compound with a cyanoacetic acid and a peptide coupling reagent to obtain a suspension; filtering the suspension to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline, an alcoholic solvent, and triethylorthoformate to yield a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride to yield a 4-amino-3-quinolinecarbonitrile.

    摘要翻译： 本发明公开了一种制备4-氨基-3-喹啉甲腈的方法，包括将胺化合物与氰基乙酸和酸催化剂混合以产生氰基乙酰胺; 将氰基乙酰胺与任选至多四取代的苯胺在醇溶剂和三烷基原甲酸酯中缩合，得到3-氨基-2-氰基丙烯酰胺; 任选在催化剂存在下，将3-氨基-2-氰基丙烯酰胺与三氯氧化磷在乙腈，丁腈，甲苯或二甲苯中的混合，得到4-氨基-3-喹啉腈，并公开了制备7-氨基-2-氰基丙烯酰胺的方法， 氨基 - 噻吩并[3,2-b]吡啶-6-甲腈，其包括在醇溶剂中组合二取代的3-氨基噻吩与氰基乙酰胺和三烷基酯，得到3-氨基-2-氰基丙烯酰胺; 并将3-氨基-2-氰基丙烯酰胺与磷酰氯和乙腈，丁腈，甲苯或二甲苯组合，任选在催化剂存在下，得到7-氨基 - 噻吩并[3,2-b]吡啶-6-甲腈和 还公开了通过将胺化合物与氰基乙酸和肽偶联剂组合以制备悬浮液来制备4-氨基-3-喹啉腈的方法; 过滤悬浮液，得到氰基乙酰胺; 将氰基乙酰胺与任选的高达四取代的苯胺，醇溶剂和原甲酸三乙酯缩合，得到3-氨基-2-氰基丙烯酰胺; 并将3-氨基-2-氰基丙烯酰胺与磷酰氯组合，得到4-氨基-3-喹啉腈。

    4-Substituted or unsubstituted-7-hydro-1,4-thiazepine-7-[bicyclic or tricyclic heteroaryl] substituted-3,6-dicarboxylic acid derivatives as beta-lactamase inhibitors
    50.
    发明申请
    4-Substituted or unsubstituted-7-hydro-1,4-thiazepine-7-[bicyclic or tricyclic heteroaryl] substituted-3,6-dicarboxylic acid derivatives as beta-lactamase inhibitors 失效
    4-取代或未取代的7-氢-1,4-硫杂氮杂-7- [双环或三环杂芳基]取代-3,6-二羧酸衍生物作为β-内酰胺酶抑制剂

    公开(公告)号：US20040214812A1

    公开(公告)日：2004-10-28

    申请号：US10834301

    申请日：2004-04-28

    申请人： Wyeth Holdings Corporation

    发明人： Tarek Suhayl Mansour ,  Aranapakam Mudumbai Venkatesan

    IPC分类号： A61K031/554 ,  C07D417/02

    CPC分类号： C07D487/04

    摘要： The present invention relates to novel, low molecular weight broad spectrum compounds in particular to a class of 4-substituted or unsubstituted-7-hydro-1,4-thiazepine-7-nullbicyclic or tricyclic heteroarylnull substituted-3,6-dicarboxylic acid or their derivatives which have null-lactamase inhibitory and antibacterial properties. The compounds are therefore useful in the treatment of antibacterial infections in humans or animals, either alone or in combination with other antibiotics.

    摘要翻译： 本发明涉及新的低分子量宽谱化合物，特别涉及一类4-取代或未取代的7-氢-1,4-硫杂氮杂-7- [二环或三环杂芳基]取代-3,6-二羧酸 酸或其衍生物具有β-内酰胺酶的抑制和抗菌性能。 因此，该化合物可用于单独或与其它抗生素联合治疗人或动物中的抗菌感染。