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5 条记录 (耗时 0.016 秒)

    Antagonists of specific excitatory amino acid neurotransmitter receptors
    1.
    发明授权
    Antagonists of specific excitatory amino acid neurotransmitter receptors 失效
    特异性兴奋性氨基酸神经递质受体的拮抗剂

    公开(公告)号：US4657899A

    公开(公告)日：1987-04-14

    申请号：US849696

    申请日：1986-04-09

    申请人： Waclaw J. Rzeszotarski ,  Robert L. Hudkins ,  Maria E. Guzewska

    发明人： Waclaw J. Rzeszotarski ,  Robert L. Hudkins ,  Maria E. Guzewska

    IPC分类号： A61K31/66 ,  A61P25/04 ,  A61P25/08 ,  C07F9/38 ,  A61K31/04 ,  A61K31/135 ,  A61K31/195

    CPC分类号： C07F9/3882 ,  C07F9/3834

    摘要： The invention pertains to novel, potent anticonvulsants, analgesics and cognition enhancers achieving their action through the antagonism of specific excitatory amino acid neurotransmitter receptors. In particular, the invention is directed to .omega.-[2-phosphonoalkyleneyl)phenyl]-2-aminoalkanoic acids having general formula: ##STR1## Wherein R.sub.1 and R.sub.2 are the same or different and are selected from the group consisting of hydrogen, lower alkyl, halogen, --CH.dbd.CH--CH.dbd.CH.dbd., amino, nitro, trifluoromethyl or cyano; n and m=0, 1, 2, or 3; and the pharmaceutically acceptable salts and derivatives thereof.Examples of specific preferred compounds of general formula are selected from the group consisting of: 4-[2-phosphonomethylphenyl]-2-aminobutanoic acid, ethyl 3-[2-(2-diethylphosphonoethyl)phenyl]-2-acetamido-2-carboethoxypropanoate, 3-[2-(2-phosphonomethyl)phenyl]-2-aminopropanoic acid, ethyl 3-[2-(3-bromopropyl)phenyl]-2-acetamido-3-carboethoxypropanoate, ethyl 3-[2-(3-diethylphosphonopropyl)phenyl]-2-acetamido-2-carboethoxypropanoate, ethyl 3-[2-(3-phosphonopropyl)-phenyl]-2-aminopropanoic acid, ethyl 5-[2-(diethylphosphonomethyl)-phenyl]-2-acetamido-2-carboethoxypentanoate, and 5-[2-phosphonomethylphenyl]-2-aminopentanoic acid.

    摘要翻译： 本发明涉及通过特异性兴奋性氨基酸神经递质受体的拮抗作用实现其作用的新型有效的抗惊厥药，止痛剂和认知增强剂。 特别地，本发明涉及具有以下通式的ω-[2-膦酰基亚烷基）苯基] -2-氨基链烷酸：其中R 1和R 2相同或不同，并且选自氢，低级烷基 ，卤素，-CH = CH-CH = CH =，氨基，硝基，三氟甲基或氰基; n和m = 0,1,2或3; 及其药学上可接受的盐和衍生物。 具体优选的通式化合物的实例选自：4- [2-膦酰基甲基苯基] -2-氨基丁酸，3- [2-（2-二乙基膦酰基乙基）苯基] -2-乙酰氨基-2-羰基乙氧基丙酸乙酯 3- [2-（2-膦酰基甲基）苯基] -2-氨基丙酸，3- [2-（3-溴丙基）苯基] -2-乙酰氨基-3-甲氧基丙酸乙酯，3- [2-（3 - 二乙基膦酰基丙基）苯基] -2-乙酰氨基-2-甲氧基丙酸乙酯，3- [2-（3-膦酰基丙基） - 苯基] -2-氨基丙酸乙酯，5- [2-（二乙基膦酰基甲基） - 苯基] -2- 乙酰氨基-2-甲氧基戊酸，和5- [2-膦酰基甲基苯基] -2-氨基戊酸。

    2-aminomethylalkynylalkyl-1,3-dithiane derivatives
    2.
    发明授权
    2-aminomethylalkynylalkyl-1,3-dithiane derivatives 失效
    2-氨基甲基炔基烷基-1,3-二噻烷衍生物

    公开(公告)号：US4877779A

    公开(公告)日：1989-10-31

    申请号：US194903

    申请日：1988-05-17

    申请人： Waclaw J. Rzeszotarski ,  Maria E. Guzewska ,  John P. Carter ,  Theodore C. Adams ,  Andrea C. Dupont ,  Carl Kaiser

    发明人： Waclaw J. Rzeszotarski ,  Maria E. Guzewska ,  John P. Carter ,  Theodore C. Adams ,  Andrea C. Dupont ,  Carl Kaiser

    IPC分类号： C07D339/08 ,  C07D409/04

    CPC分类号： C07D409/04 ,  C07D339/08

    摘要： Novel compounds and their salts are disclosed having the Formulas: ##STR1## wherein: R.sub.1 is hydrogen, phenyl, 9H-fluoren-9-yl, 10,11-dihydro-5H-dibenzo [a,d]cyclohepten-5-yl, 5H-dibenzo[a,d]cyclohepten-5-yl, 1,2,3,4-tetrahydro-1-naphthyl, 9H-xanthen-9-yl, 9H-thioxanthen-9-yl, 2-chloro-9H-thioxanthen-9-yl, 4H-chromanyl, diphenylmethyl, phenylcycloalkylmethyl wherein the bridgehead methylene may optionally be substituted with a hydroxy group and any of the phenyl or benzo-fused rings may be substituted with one or more R.sub.5 groups wherein R.sub.5 is selected from halogen, trifluoromethyl, lower alkyl, hydroxy or lower alkoxy groups; andR.sub.2 and R.sub.3, which may be the same or different, are hydrogen, lower alkyl, phenylalkyl (C.sub.1 -C.sub.5), wherein the phenyl ring may be substituted with one or more R.sub.5 groups or NR.sub.2 R.sub.3 taken together are pyrrolidinyl, piperidinyl, morpholinyl, thiomorpholinyl, or 1-piperazinyl (where the 4-position may optionally be substituted with hydrogen, lower alkyl, hydroxy-substituted lower alkyl, amino-substituted lower alkyl, or acetoxy-substituted lower alkyl;R.sub.4 is hydrogen, hydroxyl or trimethylsilyloxy;Ph is an unsubstituted phenyl group or a phenyl group substituted by one or more R.sub.5 groups; andn is 2-4.Pharmaceutical compositions effective as calcium channel blockers and therapeutic methods utilizing such compounds, particularly in the treatment of irritable bowel syndrome, are also disclosed.

    摘要翻译： 公开了新的化合物及其盐，其具有下式：其中：R1是氢，苯基，9H-芴-9-基，10,11-二氢-5H-二苯并[a，d]环庚烯-1-酮， 噻吩-5-基，5H-二苯并[a，d]环庚烯-5-基，1,2,3,4-四氢-1-萘基，9H-呫吨-9-基，9H-噻吨-9-基， 氯代-9H-噻吨-9-基，4H-苯并二氢吡喃基，二苯基甲基，苯基环烷基甲基，其中桥头甲基可以任选被羟基取代，任何苯基或苯并稠合环可以被一个或多个R 5基团取代，其中R 5 选自卤素，三氟甲基，低级烷基，羟基或低级烷氧基; 和可以相同或不同的R 2和R 3是氢，低级烷基，苯基烷基（C 1 -C 5），其中苯环可以被一个或多个R 5基团取代，或者NR 2 R 3一起是吡咯烷基，哌啶基，吗啉基， 硫代吗啉基或1-哌嗪基（其中4位可以任选被氢取代，低级烷基，羟基取代的低级烷基，氨基取代的低级烷基或乙酰氧基取代的低级烷基; R 4是氢，羟基或三甲基甲硅烷氧基; Ph 是未被取代的苯基或被一个或多个R 5基取代的苯基; n是2-4。还公开了有效作为钙通道阻断剂的药物组合物和利用这些化合物，特别是治疗肠易激综合征的治疗方法 。

    1,7-substituted heptyn-2-ones and use
    5.
    发明授权
    1,7-substituted heptyn-2-ones and use 失效
    使用1,7-取代庚炔-2-酮

    公开(公告)号：US5036107A

    公开(公告)日：1991-07-30

    申请号：US437165

    申请日：1989-11-16

    申请人： Waclaw J. Rzeszotarski ,  Maria E. Guzewska ,  Daniel W. McPherson ,  Ciro J. Spagnuolo ,  Kenneth J. Natalie, Jr.

    发明人： Waclaw J. Rzeszotarski ,  Maria E. Guzewska ,  Daniel W. McPherson ,  Ciro J. Spagnuolo ,  Kenneth J. Natalie, Jr.

    IPC分类号： C07D295/104

    CPC分类号： C07D295/104 ,  Y10S514/906 ,  Y10S514/929 ,  Y10S514/93 ,  Y10S514/935

    摘要： 1-Phenyl-7-substituted-hept-5-yn-2-ones substituted with a C.sub.1 to C.sub.7 alkyl, C.sub.3 to C.sub.6 cycloalkyl, aryl, heteroaryl or heterocycloalkyl group at the 1-position and an amino, a dialkylamino, a piperidyl, a pyrrolidyl or a hexahydroazepinyl group at the 7-position are disclosed which may have one or two substituents in addition to the phenyl group at the 1-position and also may have a p-fluoro substituent on the phenyl group. The preferred compounds are, 1-cyclohexyl-1-phenyl-1-hydroxy-7-dimethylaminohept-5-yn-2-one, 1-cyclobutyl-1-phenyl-1-hydroxy-7-dimethylaminohept-5-yn-2-one and 1-cyclo-1-phenyl-1-hydroxy-7-ethylaminohept-5-yn-2-one.The compounds are highly specific M.sub.1 -AChR antagonists with relatively prolonged duration of activity. They are particularly useful in the treatment of neurogenic bladder disorders and may be administered orally or parenterally in conventional formulations containing optional conventional additives such as binders, surfactants, emulsifiers, flavorants, preservatives and the like.

    摘要翻译： 被1-取代的C1-C7烷基，C3至C6环烷基，芳基，杂芳基或杂环烷基取代的1-苯基-7-取代的庚-5-炔-2-酮和一个氨基，二烷基氨基，哌啶基 ，公开了7-位上的吡咯烷基或六氢氮杂基，除了在1-位上的苯基之外，还可以具有一个或两个取代基，并且在苯基上也可以具有对氟取代基。 优选的化合物是1-环己基-1-苯基-1-羟基-7-二甲基氨基庚基-5-炔-2-酮，1-环丁基-1-苯基-1-羟基-7-二甲基氨基庚基-5-炔-2 - 酮和1-环-1-苯基-1-羟基-7-乙基氨基庚-5-酮-2-酮。 这些化合物是具有较长活性持续时间的高度特异性的M1-AChR拮抗剂。 它们在治疗神经性膀胱疾病中特别有用，并且可以在含有任选的常规添加剂如粘合剂，表面活性剂，乳化剂，调味剂，防腐剂等的常规制剂中口服或肠胃外给药。