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30 条记录 (耗时 0.039 秒)

    2-Arylimino-2,3-dihydrothiazoles, and their use thereof as somatostatin receptor ligands
    3.
    发明授权
    2-Arylimino-2,3-dihydrothiazoles, and their use thereof as somatostatin receptor ligands 失效
    2-芳基亚氨基-2,3-二氢噻唑及其作为生长抑素受体配体的用途

    公开(公告)号：US06727269B1

    公开(公告)日：2004-04-27

    申请号：US10031429

    申请日：2002-01-15

    申请人： Christophe Moinet ,  Carole Sackur ,  Christophe Thurieau

    发明人： Christophe Moinet ,  Carole Sackur ,  Christophe Thurieau

    IPC分类号： A61K31426

    CPC分类号： C07D277/42 ,  C07D277/56 ,  C40B40/00

    摘要： The invention concerns novel 2-arylimino-2,3-dihydrothiazole derivatives of general formula (I), their preparation methods and their use as medicines, in particular for treating pathological conditions or diseases wherein one (or several) somatostatin receptors is/are involved. Said pathological conditions include in particular acromegaly, pituitary adenoma or endocrine gastroenteropanceatic tumors including the carcinoid syndrome, and gastrointestinal bleeding. In general formula (I), R1 represents in particular an alkyl, aralkyl, cyclohexyl radical optionally substituted by an amino radical or R1 represents a —C(R11)(R12)—CO—R10 radical wherein R11 represents H, R12 represents in particular H, carbocyclic or heterocyclic alkyl, cycloalkyl or aralkyl and R10 represents in particular an aminoalkylamino radical; R2 represents a carcyclic or heterocyclic aryl radical optionally substituted; R3 represents in particular COR5 or a carbocyclic or heterocyclic alkyl, adamantyl, aryl radical optionally substituted, carbocyclic or heterocyclic aralkyl optionally substituted on the aryl group; and R5 represents a radical fixed by a nitrogen atom to the group CO.

    摘要翻译： 本发明涉及通式（I）的新型2-芳基亚氨基-2,3-二氢噻唑衍生物及其制备方法及其作为药物的用途，特别是用于治疗其中涉及一种（或多种）促生长素抑制素受体的病理状况或疾病 。 所述病理状态特别包括肢端肥大症，垂体腺瘤或包括类癌综合征在内的内分泌胃肠功能肿瘤和胃肠道出血。 在通式（I）中，R 1特别表示任选被氨基取代的烷基，芳烷基，环己基，或R 1表示-C（R 11）（R 12）-CO-R 10基团，其中R 11表示H，R 12特别表示 H，碳环或杂环烷基，环烷基或芳烷基，R 10特别表示氨基烷基氨基; R 2表示任选取代的环状或杂环芳基; R 3特别表示COR 5或碳环或杂环烷基，金刚烷基，任选取代的芳基，芳基上任选取代的碳环或杂环芳烷基; 并且R 5表示由氮原子与基团CO固定的基团。

    Derivatives of 4-aminopiperidine and their use as a medicament
    4.
    发明申请
    Derivatives of 4-aminopiperidine and their use as a medicament 有权
    4-氨基哌啶的衍生物及其作为药物的用途

    公开(公告)号：US20090149652A1

    公开(公告)日：2009-06-11

    申请号：US12151115

    申请日：2008-05-02

    申请人： Christophe Thurieau ,  Jerome Gonzalez ,  Christophe Moinet

    发明人： Christophe Thurieau ,  Jerome Gonzalez ,  Christophe Moinet

    IPC分类号： C07D401/14 ,  C07D401/02

    CPC分类号： C07D401/12 ,  C07D211/58 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

    摘要： A subject of the present application is new derivatives of 4-aminopiperidines of formula in which R1, R2 and R3 represent various radical, and their preparation processes by synthetic methods in parallel in liquid and solid phase. These products having a good affinity with certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) somatostatin receptors are involved.

    摘要翻译： 本申请的主题是式（Ⅰ）的4-氨基哌啶的新衍生物，其中R 1，R 2和R 3表示各种基团，它们通过合成方法在液相和固相中并联制备方法。 这些产品与生长抑素受体的某些亚型具有良好的亲和力，它们特别可用于治疗涉及一种（或更多种）生长抑素受体的病理状态或疾病。

    Derivatives of 4-aminopiperidine and their use as a medicament
    6.
    发明授权
    Derivatives of 4-aminopiperidine and their use as a medicament 有权
    4-氨基哌啶的衍生物及其作为药物的用途

    公开(公告)号：US07393861B2

    公开(公告)日：2008-07-01

    申请号：US11122293

    申请日：2005-05-04

    申请人： Christophe Thurieau ,  Jérôme Gonzalez ,  Christophe Moinet

    发明人： Christophe Thurieau ,  Jérôme Gonzalez ,  Christophe Moinet

    IPC分类号： A61K31/435 ,  C07D211/00

    CPC分类号： C07D401/12 ,  C07D211/58 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

    摘要： A subject of the present application is new derivatives of 4-aminopiperidines of formula in which R1, R2 and R3 represent various radical, and their preparation processes by synthetic methods in parallel in liquid and solid phase. These products having a good affinity with certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) somatostatin receptors are involved.

    摘要翻译： 本申请的主题是下式的4-氨基哌啶的新衍生物，其中R 1，R 2和R 3代表各种基团， 并通过合成方法在液相和固相中并行制备其制备方法。 这些产品与生长抑素受体的某些亚型具有良好的亲和力，它们特别可用于治疗涉及一种（或更多种）生长抑素受体的病理状态或疾病。

    4-aminopiperidine and their use as a medicine
    7.
    发明授权
    4-aminopiperidine and their use as a medicine 有权
    4-氨基哌啶及其作为药物的用途

    公开(公告)号：US07115634B2

    公开(公告)日：2006-10-03

    申请号：US10130924

    申请日：2000-12-13

    申请人： Christophe Thurieau ,  Jérôme Gonzalez ,  Christophe Moinet

    发明人： Christophe Thurieau ,  Jérôme Gonzalez ,  Christophe Moinet

    IPC分类号： A61K31/47 ,  C07D211/58

    CPC分类号： C07D401/12 ,  C07D211/58 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

    摘要： A subject of the present application is new derivatives of 4-aminopiperidines of formula in which R1, R2 and R3 represent various radical, and their preparation processes by synthetic methods in parallel in liquid and solid phase. These products having a good affinity with certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) somatostatin receptors are involved.

    摘要翻译： 本申请的主题是下式的4-氨基哌啶的新衍生物，其中R 1，R 2和R 3代表各种基团， 并通过合成方法在液相和固相中并行制备其制备方法。 这些产品与生长抑素受体的某些亚型具有良好的亲和力，它们特别可用于治疗涉及一种（或更多种）生长抑素受体的病理状态或疾病。