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    4-(2-furoyl) aminopiperidines, intermediates in synthesizing the same, process for producing the same and medicinal use of the same
    2.
    发明授权
    4-(2-furoyl) aminopiperidines, intermediates in synthesizing the same, process for producing the same and medicinal use of the same 失效
    4-（2-糠酰基）氨基哌啶，其合成中间体，其制备方法及其药学用途

    公开(公告)号：US07375115B2

    公开(公告)日：2008-05-20

    申请号：US10492065

    申请日：2002-10-08

    申请人： Ryuuta Fukutomi ,  Hitoshi Inoue ,  Koji Kawamura ,  Takuya Kishimoto ,  Masashi Suzuki ,  Rie Shibayama ,  Kazuko Kojima ,  Kouichirou Hagihara

    发明人： Ryuuta Fukutomi ,  Hitoshi Inoue ,  Koji Kawamura ,  Takuya Kishimoto ,  Masashi Suzuki ,  Rie Shibayama ,  Kazuko Kojima ,  Kouichirou Hagihara

    IPC分类号： A01N43/40 ,  C07D401/00

    CPC分类号： C07D401/12 ,  C07D211/58 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14

    摘要： There are provided novel 4(2-furoyl)aminopiperidines represented by the general formula (I), their synthetic intermediates, processes for their preparation and medicaments containing them. In the above formula, X is OH or N, and Y is a group of the following general formula (II), formula (II-a) or formula (III): wherein a, b and c are each an integer of 0-6; Z is CH2 or NH; W is O or S; T is O or N—R15 wherein R15 is H, a C1-C6 alkyl group, a benzyl group or a phenethyl group; and R1 is H, a C1-C6 alkoxycarbonyl group, a benzyloxy-carbonyl group, or the like. The 4-(2-furoyl)aminopiperidine derivatives according to this invention possess opioid μ antagonistic activity and are useful for the treatment or prevention of side effects which are caused by μ receptors agonist and which are selected from constipation, nausea/emesis or itch, or for the treatment or prevention of idiopathic constipation, postoperative ileus, paralytic ileus, irritable bowel syndrome or chronic pruritus.

    摘要翻译： 提供由通式（I）表示的新型4（2-糠酰基）氨基哌啶，其合成中间体，其制备方法和含有它们的药物。 在上式中，X为OH或N，Y为下列通式（II），式（II-a）或式（III）的基团：其中a，b和c各自为0〜 6; Z是CH 2或NH; W为O或S; T是O或N-R 15，其中R 15是H，C 1 -C 6烷基，苄基或苯乙基; R 1是H，C 1 -C 6烷氧基羰基，苄氧基羰基等。 根据本发明的4-（2-糠酰基）氨基哌啶衍生物具有阿片样物质μ拮抗活性，可用于治疗或预防由mu受体激动剂引起的副作用，其选自便秘，恶心/呕吐或瘙痒， 或用于治疗或预防特发性便秘，术后肠梗阻，麻痹性肠梗阻，肠易激综合征或慢性瘙痒。