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40 条记录 (耗时 0.041 秒)

    5-substituted-2-arylpyridines
    3.
    发明授权
    5-substituted-2-arylpyridines 失效
    5-取代-2-芳基吡啶

    公开(公告)号：US07223778B2

    公开(公告)日：2007-05-29

    申请号：US10154396

    申请日：2002-05-22

    申请人： Ge Ping ,  Taeyoung Yoon ,  Lu Yan Zhang ,  Raymond F. Horvath

    发明人： Ge Ping ,  Taeyoung Yoon ,  Lu Yan Zhang ,  Raymond F. Horvath

    IPC分类号： C07D213/02 ,  A61K31/44

    CPC分类号： C07D213/68 ,  C07D213/65 ,  C07D213/69 ,  C07D213/74 ,  C07D213/82 ,  C07D413/04

    摘要： Novel 5-substituted-2-arylpyridine compounds are provided. Such compounds can act as selective modulators of CRF receptors. The 5-substituted-2-arylpyridine compounds provided herein are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided.Compounds provided are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.

    摘要翻译： 提供新的5-取代-2-芳基吡啶化合物。 这些化合物可以作为CRF受体的选择性调节剂。 本文提供的5-取代-2-芳基吡啶化合物可用于治疗许多CNS和周围疾病，特别是压力，焦虑，抑郁，心血管疾病和进食障碍。 还提供了治疗这种疾病以及包装的药物组合物的方法。 提供的化合物也可用作CRF受体定位的探针，并且作为用于CRF受体结合的测定中的标准物。 给出了在受体定位研究中使用化合物的方法。

    N-phenyl benzimidazolecarboxamide and N-phenyl indolecarboxamide derivatives
    7.
    发明授权
    N-phenyl benzimidazolecarboxamide and N-phenyl indolecarboxamide derivatives 失效
    N-苯基苯并咪唑酰胺和N-苯基吲哚甲酰胺衍生物

    公开(公告)号：US06583169B2

    公开(公告)日：2003-06-24

    申请号：US09928722

    申请日：2001-08-13

    申请人： Raymond F. Horvath ,  Ping Ge ,  Taeyoung Yoon ,  Alan Hutchison

    发明人： Raymond F. Horvath ,  Ping Ge ,  Taeyoung Yoon ,  Alan Hutchison

    IPC分类号： A61K31404

    CPC分类号： C07D235/14 ,  C07D209/14 ,  G01N2333/726

    摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein; A is N or CH; R1 and R2 represents hydrogen or lower alkyl; G, R3, R4, R5, R6, R7 and R8 are variables defined herein. These compounds are modulators of CRF receptors and are therefore useful for treating affective disorders, anxiety, depression, eating disorders, and stress disorders in humans and other animals. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.

    摘要翻译： 公开了下式的化合物或其药学上可接受的无毒盐，其中A是N或CH; R 1和R 2表示氢或低级烷基; G，R 3，R 4，R 5，R 6，R 7和R 8是本文定义的变量 这些化合物是CRF受体的调节剂，因此可用于治疗人类和其他动物中的情感障碍，焦虑症，抑郁症，进食障碍和应激障碍。 还提供了治疗这种病症以及包装的药物组合物的方法。本发明的化合物还可用作CRF受体定位的探针，并且作为用于CRF受体结合的测定中的标准物。 给出了在受体定位研究中使用化合物的方法。

    Isoquinolinamine and phthalazinamine derivatives which interact with CRF receptors
    8.
    发明授权
    Isoquinolinamine and phthalazinamine derivatives which interact with CRF receptors 失效
    与CRF受体相互作用的异喹啉胺和酞嗪胺衍生物

    公开(公告)号：US06235752B1

    公开(公告)日：2001-05-22

    申请号：US09331380

    申请日：1999-09-20

    申请人： Jun Yuan ,  Taeyoung Yoon

    发明人： Jun Yuan ,  Taeyoung Yoon

    IPC分类号： A61K3147

    CPC分类号： C07D401/12 ,  C07D217/22 ,  C07D237/34

    摘要： Disclosed are compounds that are highly selective partial agonists or antagonists of CRF1 receptors. The disclosed compounds are useful in the diagnosis and treatment of stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache, and anxiety. The compounds are represented by the formula wherein R1, R2, R3, R4, and Ar represent various inorganic and organic substituents. Also disclosed are pharmaceutical compositions and methods of treating post traumatic stress disorder, depression, headache, and anxiety.

    摘要翻译： 公开了作为CRF1受体的高选择性部分激动剂或拮抗剂的化合物。 所公开的化合物可用于诊断和治疗应激相关疾病如创伤后应激障碍（PTSD）以及抑郁，头痛和焦虑。 这些化合物由化学式R 1表示，R 2，R 3，R 4和Ar表示各种无机和有机取代基。还公开了治疗创伤后应激障碍，抑郁症，头痛和焦虑的药物组合物和方法。

    Enediyne quinone imines and methods of preparation and use thereof
    9.
    发明授权
    Enediyne quinone imines and methods of preparation and use thereof 失效
    烯二炔醌及其制备方法及用途

    公开(公告)号：US5622958A

    公开(公告)日：1997-04-22

    申请号：US347952

    申请日：1994-12-01

    申请人： Samuel J. Danishefsky ,  Matthew D. Shair ,  Taeyoung Yoon ,  T.-C. Chou

    发明人： Samuel J. Danishefsky ,  Matthew D. Shair ,  Taeyoung Yoon ,  T.-C. Chou

    IPC分类号： A61K47/48 ,  C07D491/044 ,  C07D491/08 ,  A61K31/47

    CPC分类号： C07D491/08 ,  A61K47/48384 ,  A61K47/48407

    摘要： A quinone imine enediyne possessing cytotoxic activity towards cancer cells having the general structure: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are independently the same or different and are H, Br, Cl, F, NH.sub.2, CO.sub.2 H, or OH or a linear or branched alkyl, etc.; wherein R.sub.4 is H, OH or a linear or branched alkoxy, linear or branched alkoxycarbonyl, etc.; wherein R.sub.5 is H, Br, Cl, F, O.dbd., OH or S--SR, or a linear or branched alkyl, etc.; wherein R.sub.6 is H, Br, Cl, F, CO.sub.2 H, OH or S--SR', or a linear or branched alkyl, etc; wherein R.sub.7 is H, OH or S--SR", or a linear or branched alkyl, linear or branched alkoxycarbonyl, linear or branched alkoxy or linear or branched hydroxyalkyl group; and wherein R, R' and R" are independently the same or different and are a linear or branched alkyl, linear or branched acyl or linear or branched alkoxyalkyl group. Also provided are conjugates of the compound with cleavable peptides and carbohydrates, monoclonal antibodies immunoreactive with cancer cells, compositions comprising the analogues and conjugates, methods of treating tumors and a method of preparing the analogues.

    摘要翻译： 对具有一般结构的癌细胞具有细胞毒性活性的醌亚胺烯二酮：其中R 1，R 2和R 3独立地相同或不同，为H，Br，Cl，F，NH 2，CO 2 H或OH或线性或 支链烷基等; 其中R4是H，OH或直链或支链烷氧基，直链或支链烷氧基羰基等; 其中R 5是H，Br，Cl，F，O =，OH或S-SR，或直链或支链烷基等; 其中R6是H，Br，Cl，F，CO2H，OH或S-SR'，或直链或支链烷基等; 其中R 7为H，OH或S-SR“，或直链或支链烷基，直链或支链烷氧基羰基，直链或支链烷氧基或直链或支链羟烷基; 并且其中R，R'和R“独立地相同或不同，并且是直链或支链烷基，直链或支链的酰基或直链或支链烷氧基烷基。 还提供了化合物与可切割肽和碳水化合物的缀合物，与癌细胞免疫反应的单克隆抗体，包含类似物和缀合物的组合物，治疗肿瘤的方法和制备类似物的方法。