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    Aminoalkyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
    1.
    发明申请
    Aminoalkyl substituted (benzodioxan, benzofuran or benzopyran) derivatives 有权
    氨基烷基取代的（苯并二恶烷，苯并呋喃或苯并吡喃）衍生物

    公开(公告)号：US20050096378A1

    公开(公告)日：2005-05-05

    申请号：US10999187

    申请日：2004-11-29

    申请人： Kristof Van Emelen ,  Marcel De Bruyn

    发明人： Kristof Van Emelen ,  Marcel De Bruyn

    IPC分类号： A61K31/4164 ,  A61K31/4178 ,  A61K31/513 ,  A61P1/14 ,  A61P9/00 ,  A61P9/08 ,  C07D405/12 ,  C07D417/12 ,  C07D327/06 ,  A61K31/382 ,  A61K31/353

    CPC分类号： C07D405/12 ,  C07D417/12

    摘要： The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R6 is hydrogen or phenylmethyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impaired fundic relaxation.

    摘要翻译： 本发明涉及式（I）化合物，其立体化学异构形式，其N-氧化物形式或其药学上可接受的酸加成盐，其中-Z 1 -Z 2， SUP> - 是二价基团; R 1，R 2和R 3各自独立地选自氢，C 1-6烷基，羟基 ，卤素等; 或当R 1和R 2在相邻的碳原子上时，R 1和R 2可以一起形成 式的二价基团; Alk＆lt; 1＆gt;和Alk 2是任选取代的C 1-6烷二基; R 6是氢或苯基甲基; R 5是下式的基团，其中n是1或2; p <0> 1是0，p <2>是1或2; 或p <1> 1是1或2，并且p O是0; X是氧，硫或-NR 9; Y是氧或硫; R 7是氢，C 1-6烷基，C 3-6环烷基，苯基或苯基甲基; R 8是C 1-6烷基，C 3-6环烷基苯基或苯基甲基; R 9是氰基，C 1-6烷基，C 3-6环烷基，C 1-6 烷氧基羰基或氨基羰基; R 10是氢或C 1-6烷基; 而Q是二价基团。 公开了用于制备所述产品的方法，包含所述产品的制剂及其作为药物的用途，特别是用于治疗与减退的放松有关的病症。

    Pyrrolopyrimidine and Pyrrolopyridine Derivatives Substituted with Tetrahydropyridine as Crf Antagonists
    3.
    发明申请
    Pyrrolopyrimidine and Pyrrolopyridine Derivatives Substituted with Tetrahydropyridine as Crf Antagonists 审中-公开
    用四氢吡啶取代的吡咯并嘧啶和吡咯并吡啶衍生物作为Crf拮抗剂

    公开(公告)号：US20070293670A1

    公开(公告)日：2007-12-20

    申请号：US11630041

    申请日：2005-06-24

    申请人： Atsuro Nakazato ,  Taketoshi Okubo ,  Dai Nozawa ,  Ludo Kennis ,  Marcel De Bruyn

    发明人： Atsuro Nakazato ,  Taketoshi Okubo ,  Dai Nozawa ,  Ludo Kennis ,  Marcel De Bruyn

    IPC分类号： C07D487/04

    CPC分类号： C07D487/04 ,  C07D471/04

    摘要： [PROBLEM TO BE SOLVED]An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal diseases, drug dependence, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, pain, etc. [SOLUTION]A pyrrolopyrimidine or pyrrolopyridine derivative substituted with tetrahydropyridine represented by the following formula [I]: has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.

    摘要翻译： [待解决的问题]本发明的目的是提供一种抗CRF受体的拮抗剂，其作为治疗或预防药物是有效的，其涉及CRF被认为涉及的疾病，例如抑郁症，焦虑症，阿尔茨海默病，帕金森病 疾病，亨廷顿氏舞蹈病，饮食失调，高血压，胃肠道疾病，药物依赖，脑梗死，脑缺血，脑水肿，头部外伤，炎症，免疫相关疾病，脱发，肠易激综合征，睡眠障碍，癫痫，皮肤病，精神分裂症 ，疼痛等。[解决方案]由下式[I]表示的用四氢吡啶取代的吡咯并嘧啶或吡咯并吡啶衍生物对CRF受体具有高亲和力，并且对于被认为涉及CRF的疾病是有效的。