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47 条记录 (耗时 0.233 秒)

    5-(3-Phenyl-3-oxo-propyl)-1H-tetrazole derivatives
    1.
    发明授权
    5-(3-Phenyl-3-oxo-propyl)-1H-tetrazole derivatives 失效
    5-（3-苯基-3-氧代 - 丙基）-1H-四唑衍生物

    公开(公告)号：US6133302A

    公开(公告)日：2000-10-17

    申请号：US446895

    申请日：1999-12-30

    申请人： Paolo Pevarello ,  Antonio Giordani ,  Manuela Villa ,  Carmela Speciale ,  Mario Varasi

    发明人： Paolo Pevarello ,  Antonio Giordani ,  Manuela Villa ,  Carmela Speciale ,  Mario Varasi

    IPC分类号： A61K31/41 ,  A61P25/00 ,  A61P43/00 ,  C07D257/04

    CPC分类号： C07D257/04

    摘要： 5-(3-phenyl-3-oxo-propyl)-1H-tetrazole derivatives of formula (I) wherein each of R and R.sub.1, being the same or different, is hydrogen, halogen, hydroxy, trifluoromethyl, cyano, nitro, phenyl, benzyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, SOR.sub.4 or SO.sub.2 R.sub.4 wherein R.sub.4 is C.sub.1 -C.sub.6 alkyl, --N(R.sub.5 R.sub.6) in which each of R.sub.5 and R.sub.6 is, independently, hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 acyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, benzyl, phenyl; R.sub.3 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, benzyl, phenyl or a group --N(R.sub.7 R.sub.8) in which each of R.sub.7 and R.sub.8 is, independently, hydrogen, C.sub.1 -C.sub.4 alkyl, benzyl, phenyl, or one of R.sub.7 and R.sub.8 is hydrogen and the other is COR.sub.9 wherein R.sub.9 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, phenyl or a group --N(R.sub.10 R.sub.11) in which R.sub.10 and R.sub.11 are, each independently, hydrogen or C.sub.1 -C.sub.4 alkyl or, taken together, R.sub.2 and R.sub.3 form a carbocyclic C.sub.3 -C.sub.6 ring; and pharmaceutically acceptable salts thereof have kynurenine-3-hydroxylase enzyme inhibitory activity. ##STR1##

    摘要翻译： PCT No.PCT / EP98 / 04032 Sec。 371 1999年12月30日第 102（e）1999年12月30日PCT PCT。1998年6月25日PCT公布。 公开号WO99 /​​ 02506 日本1月21日，19995-（3-苯基-3-氧代 - 丙基）-1H-四唑衍生物，其中R和R 1相同或不同，为氢，卤素，羟基，三氟甲基， 氰基，硝基，苯基，苄基，C1-C6烷基，C1-C6烷氧基，C1-C6烷硫基，SOR4或SO2R4，其中R4是C1-C6烷基，-N（R5R6），其中R5和R6各自独立地为 氢，C 1 -C 6烷基，甲酰基或C 2 -C 6酰基; R2是氢，C1-C6烷基，C1-C6烷氧基，苄基，苯基; R3是氢，羟基，C1-C6烷基，C1-C6烷氧基，苄基，苯基或基团-N（R7R8），其中R7和R8各自独立地是氢，C1-C4烷基，苄基，苯基或 R 7和R 8中的一个是氢，另一个是COR 9，其中R 9是氢，C 1 -C 4烷基，C 1 -C 4烷氧基，苯基或基团-N（R 10 R 11），其中R 10和R 11各自独立地是氢或C1- C4烷基或一起为R2和R3形成碳环C 3 -C 6环; 及其药学上可接受的盐具有犬尿氨酸-3-羟化酶抑制活性。

    4-phenyl-4-oxo-butanoic acid derivatives with kynurenine-3-hydroxylase inhibiting activity
    2.
    发明授权
    4-phenyl-4-oxo-butanoic acid derivatives with kynurenine-3-hydroxylase inhibiting activity 失效
    具有犬尿氨酸-3-羟化酶抑制活性的4-苯基-4-氧代 - 丁酸衍生物

    公开(公告)号：US06323240B1

    公开(公告)日：2001-11-27

    申请号：US09068016

    申请日：1998-05-01

    申请人： Antonio Giordani ,  Paolo Pevarello ,  Carmela Speciale ,  Mario Varasi

    发明人： Antonio Giordani ,  Paolo Pevarello ,  Carmela Speciale ,  Mario Varasi

    IPC分类号： A61K31195

    CPC分类号： C07C59/90 ,  C07C69/738 ,  C07C205/56

    摘要： 4-phenyl-4-oxo-butanoic acid derivatives for use in the treatment of the human or animal body by therepy; particularly as kynurenine-3-hydroxylase inhibitors, in the prevention and/or treatment of a neurodegenerative disease wherein the inhibition of such an enyzme is needed. The present invention further comprises a selected class of the above mentioned 4-phenyl-4-oxo-butanoic acid derivatives, their pharmaceutically acceptable salts, a process for their preparation and pharmaceutical compositions containing them.

    摘要翻译： 4-苯基-4-氧代 - 丁酸衍生物，用于通过该药物治疗人体或动物体; 特别是作为犬尿氨酸-3-羟化酶抑制剂，在预防和/或治疗需要抑制这种乙烯的神经变性疾病中。 本发明还包括所选类别的上述4-苯基-4-氧代 - 丁酸衍生物，其药学上可接受的盐，其制备方法和含有它们的药物组合物。

    Novel piperidine derivatives
    9.
    发明授权
    Novel piperidine derivatives 失效
    新型哌啶衍生物

    公开(公告)号：US4879300A

    公开(公告)日：1989-11-07

    申请号：US135839

    申请日：1987-12-21

    申请人： Antonio Giordani ,  Vittorio Vecchietti

    发明人： Antonio Giordani ,  Vittorio Vecchietti

    IPC分类号： C07D211/16 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/451 ,  A61P25/04 ,  C07D211/26 ,  C07D401/04

    CPC分类号： C07D401/04 ,  C07D211/26

    摘要： A compound, or a solvate or salt thereof, of formula I: ##STR1## in which: R.CO-- is an acyl group containing a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic group;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkenyl, C.sub.1-6 cycloalkyl or C.sub.1-12 cycloalkylalkyl or together form a C.sub.2-6 polymethylene or C.sub.2-6 alkenylene group, optionally substituted with a hetero-atom, provided that R.sub.1 and R.sub.2 are not simultaneously hydrogen;Rx is C.sub.1-6 alkyl or phenyl, or Rx together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group, is useful for the treatment of pain.