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    Metabolically stabilized oxyalkylene esters and uses thereof
    2.
    发明授权
    Metabolically stabilized oxyalkylene esters and uses thereof 失效
    代谢稳定的氧化烯酯及其用途

    公开(公告)号：US06110955A

    公开(公告)日：2000-08-29

    申请号：US814975

    申请日：1997-03-11

    申请人： Abraham Nudelman ,  Ada Rephaeli ,  Edward Neiss ,  Bernard Loev

    发明人： Abraham Nudelman ,  Ada Rephaeli ,  Edward Neiss ,  Bernard Loev

    IPC分类号： C07C69/353 ,  C07C69/612 ,  C07C69/88 ,  C07C69/90 ,  C07C69/94 ,  C07D491/052 ,  A61K31/235 ,  A61K31/407 ,  C07C69/025

    CPC分类号： C07C69/90 ,  C07C69/612 ,  C07C69/88 ,  C07C69/94

    摘要： This invention relates to compositions for and methods of treating, preventing or ameliorating cancer and other proliferative diseases as well as methods of inducing wound healing, treating cutaneous ulcers, treating gastrointestinal disorders, treating blood disorders such as anemias, immunomodulation, enhancing recombinant gene expression, treating insulin-dependent patients, treating cystic fibrosis patients, inhibiting telomerase activity, treating virus-associated tumors, especially EBV-associated tumors, modulating gene expression and particularly augmenting expression of a tumor suppressor gene, inducing tolerance to an antigen and treating, ameliorating or preventing protozoan infection. The methods of the invention use metabolically stabilized oxyalkylene esters.

    摘要翻译： 本发明涉及治疗，预防或改善癌症和其它增殖性疾病的组合物和方法，以及诱导伤口愈合，治疗皮肤溃疡，治疗胃肠道疾病，治疗血液病症如贫血，免疫调节，增强重组基因表达的方法， 治疗胰岛素依赖型患者，治疗囊性纤维化患者，抑制端粒酶活性，治疗病毒相关肿瘤，特别是EBV相关肿瘤，调节基因表达，特别是增加肿瘤抑制基因的表达，诱导对抗原的耐受和治疗，改善或改善 预防原生动物感染。 本发明的方法使用代谢稳定的氧化亚烷基酯。

    N-Substituted-1-aminoalkyl-1,4-dihydropyridines
    5.
    发明授权
    N-Substituted-1-aminoalkyl-1,4-dihydropyridines 失效
    N-取代的-1-氨基烷基-1,4-二氢吡啶

    公开(公告)号：US4472584A

    公开(公告)日：1984-09-18

    申请号：US471959

    申请日：1983-03-03

    申请人： Bernard Loev ,  Howard Jones ,  John T. Suh

    发明人： Bernard Loev ,  Howard Jones ,  John T. Suh

    IPC分类号： C07D211/90 ,  C07D211/82 ,  A61K31/455 ,  C07D401/04 ,  C07D405/04

    CPC分类号： C07D211/90

    摘要： Compounds of the formula: ##STR1## wherein Ar is heteroaryl, cycloalkyl having from 3 to 7 carbon atoms, naphthyl, indanyl, indenyl, tetrahydro naphthyl, or a radical of the formula ##STR2## wherein each of R.sub.5, R.sub.6 and R.sub.7 is independently H, alkyl, aryl, halo, lower alkoxy, nitro, amino, alkylmercapto, cyano, carboxy, carbalkoxy, sulfamyl, trifluoromethyl, hydroxy, acyloxy, methanesulfonyl, alkylamino or acylamino; and R.sub.5 and R.sub.6 when taken together, form a methylenedioxy; Z is alkylene containing 1 to about 5 carbon atoms in the principal chain; each R.sub.1 is independently hydrogen, alkyl or alkoxyalkyl, with the proviso that only one R.sub.1 may be hydrogen; R.sub.2 is lower alkyl; R.sub.3 is hydroxyalkyl containing 2 to 4 carbon atoms and R.sub.4 is H, alkyl, cycloalkyl or hydroxyalkyl containing 2 to 4 carbon atoms; wherein the alkyl, alkoxy, and acyl groups contain up to 10 carbon atoms, and their pharmaceutically-acceptable salts are disclosed. These compounds have anti-hypertensive activity.

    摘要翻译： 下式的化合物：其中Ar是杂芳基，具有3至7个碳原子的环烷基，萘基，茚满基，茚基，四氢萘基或下式的基团其中R 5，R 6和R 7各自独立地是 H，烷基，芳基，卤素，低级烷氧基，硝基，氨基，烷基巯基，氰基，羧基，烷氧基，氨基磺酰基，三氟甲基，羟基，酰氧基，甲磺酰基，烷基氨基或酰基氨基; 并且R 5和R 6一起形成亚甲二氧基; Z是主链中含有1至约5个碳原子的亚烷基; 每个R 1独立地是氢，烷基或烷氧基烷基，条件是只有一个R 1可以是氢; R2是低级烷基; R3是含有2至4个碳原子的羟基烷基，R4是H，含2至4个碳原子的烷基，环烷基或羟基烷基; 其中烷基，烷氧基和酰基含有至多10个碳原子，并且公开了它们的药学上可接受的盐。 这些化合物具有抗高血压活性。

    Antihypertensive 1,4-thiazepine-ones, 1,4-thiazonine-ones, and method of use thereof
    7.
    发明授权
    Antihypertensive 1,4-thiazepine-ones, 1,4-thiazonine-ones, and method of use thereof 失效
    抗高血压药物1,4-硫氮杂菌素，1,4-噻嗪酮类药物及其应用方法

    公开(公告)号：US4287203A

    公开(公告)日：1981-09-01

    申请号：US142945

    申请日：1980-04-23

    申请人： John T. Suh ,  Bruce E. Williams ,  Jerry W. Skiles ,  Bernard Loev

    发明人： John T. Suh ,  Bruce E. Williams ,  Jerry W. Skiles ,  Bernard Loev

    IPC分类号： A61K31/55 ,  A61K31/554 ,  A61P9/12 ,  A61P43/00 ,  C07D277/06 ,  C07D279/12 ,  C07D281/06 ,  C07D513/04 ,  C07D281/04 ,  C07D281/18

    CPC分类号： C07D513/04 ,  C07D277/06 ,  C07D279/12 ,  C07D281/06

    摘要： Antihypertensive compounds of the structure ##STR1## wherein: n is an integer from 0 to 2 inclusive,R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 are independently hydrogen, alkyl having from 1 to 6 carbon atoms, alkenyl having from 2 to 6 carbon atoms, alkynyl having from 2 to 6 carbon atoms, cycloalkyl having from 3 to 16 carbon atoms, phenyl, benzyl, tolyl, naphthyl, phenethyl, indanyl, tetrahydronaphthyl, decanydronaphthyl, pyridyl, quinolyl, pyrrolidyl, pyrrolyl, morpholinyl, thiomorpholinyl, furyl, furfuryl, tetrahydrofurfuryl, benzimidazole, thienyl, imidolyl, or tetrahydroindolyl, and where the R.sub.1 to R.sub.7 groups are alkyl, said groups carrying a substituent selected from hydroxy, alkoxy, amino, carboxy, or carbalkoxy, the alkyl group in alkoxy and carbalkoxy having from 1 to 6 carbon atoms, or R.sub.2 taken together with R.sub.3 and the carbons to which they are attached is tetrahydronaphthyl or phenyl, and when phenyl R.sub.1 and R.sub.4 are absent, or R.sub.6 and R.sub.7 taken together with the carbon to which R.sub.6 is attached and the nitrogen to which R.sub.7 is attached form a heterocycle selected from pyrrolidyl, thiazolidine, tetrahydro-isoquinoline, thiomorpholine, or 2,2,5,5-tetramethylthiazolidinie, andY is .dbd.O, .dbd.S, .dbd.NR.sub.1, .dbd.NOR.sub.1 or .dbd.N--NH.sub.2, R.sub.1 being the same as defined above.

    摘要翻译： 结构的抗高血压化合物其中：n为0〜2的整数，R1，R2，R3，R4，R5，R6和R7独立地为氢，具有1-6个碳原子的烷基， 2至6个碳原子，具有2至6个碳原子的炔基，具有3至16个碳原子的环烷基，苯基，苄基，甲苯基，萘基，苯乙基，茚满基，四氢萘基，癸烷基萘基，吡啶基，喹啉基，吡咯烷基，吡咯基，吗啉基， 硫代吗啉基，呋喃基，糠基，四氢糠基，苯并咪唑，噻吩基，亚氨基或四氢吲哚基，其中R 1至R 7基团是烷基，所述基团含有选自羟基，烷氧基，氨基，羧基或烷氧基的取代基，烷氧基 和具有1至6个碳原子的烷氧基，或者R 2与R 3和它们所连接的碳一起为四氢萘基或苯基，当不存在R 1和R 4时，或者R 6和R 7与R 6一起 是attac 和R7连接的氮形成选自吡咯烷基，噻唑烷，四氢 - 异喹啉，硫代吗啉或2,2,5,5-四甲基噻唑烷的杂环，Y = O，= S，= NR1，= NOR1或 = N-NH 2，R 1与上述定义相同。

    1,3,5-Tricarbo-1,4-dihydropyridines
    9.
    发明授权
    1,3,5-Tricarbo-1,4-dihydropyridines 失效
    1,3,5-三甲基-1,4-二氢吡啶

    公开(公告)号：US3956341A

    公开(公告)日：1976-05-11

    申请号：US444455

    申请日：1974-02-21

    申请人： Bernard Loev

    发明人： Bernard Loev

    IPC分类号： C07D211/82 ,  C07D211/90 ,  C07D401/04 ,  C07D211/80

    CPC分类号： C07D211/82 ,  C07D211/90

    摘要： N-Substituted 1,4-dihydropyridines are prepared by reaction of the corresponding N-unsubstituted 1,4-dihydropyridines with an alkyl haloformate, an acid halide or a carbamyl halide in the presence of base. These compounds have hypotensive activity.

    摘要翻译： N-取代的1,4-二氢吡啶通过相应的N-未取代的1,4-二氢吡啶与卤代甲酸烷基酯，酰卤或氨基甲酰基卤在碱存在下反应来制备。 这些化合物具有降血压活性。