3-Arylquinazoline derivatives as selective estrogen receptor beta modulators
    51.
    发明申请
    3-Arylquinazoline derivatives as selective estrogen receptor beta modulators 有权
    3-芳基喹唑啉衍生物作为选择性雌激素受体β调节剂

    公开(公告)号:US20030220227A1

    公开(公告)日:2003-11-27

    申请号:US10387666

    申请日:2003-03-13

    摘要: Novel quinazoline derivatives possessing activity as estrogen receptor beta (ERnull) modulators are provided which have the general formula I 1 wherein X is O or S; A and B are each independently CRnullnull or N; R, Rnull and Rnull are each independently hydrogen, alkyl, benzyl, p-methoxybenzyl, allyl, or Si(R4)3, wherein at least one of R, Rnull and Rnull is hydrogen; Rnullnull is hydrogen, halogen, CF3, OR5, S(O)nR6, NR7R8, cycloalkyl or alkyl; R1, R2 and R3 are each independently hydrogen, halogen, CF3, OR5, S(O)nR6, NR7R8, cycloalkyl or alkyl; R4 is a alkyl; R5, R6, R7 and R8 in each functional group are each independently hydrogen, cycloalkyl or alkyl; and n is an integer from 0 to 2. In addition, a method is provided for preventing, inhibiting or treating the progression or onset of pathological conditions associated with the estrogen receptor and to pharmaceutical compositions containing such compounds.

    摘要翻译: 提供具有雌激素受体β(ERbeta)调节剂活性的新型喹唑啉衍生物,其具有通式I,其中X为O或S; A和B各自独立地为CR“或N; R,R'和R“各自独立地为氢,烷基,苄基,对甲氧基苄基,烯丙基或Si(R4)3,其中R,R'和R”中的至少一个为氢; R“'是氢,卤素,CF 3,OR 5,S(O)n R 6,NR 7 R 8,环烷基或烷基; R 1,R 2和R 3各自独立地为氢,卤素,CF 3,OR 5,S(O)n R 6,NR 7 R 8,环烷基或烷基; R4是烷基; 各官能团中的R 5,R 6,R 7和R 8各自独立地为氢,环烷基或烷基; n为0-2的整数。此外,提供了用于预防,抑制或治疗与雌激素受体相关的病理状况的进展或发作的方法以及含有这些化合物的药物组合物。

    Polypeptide derivatives
    52.
    发明申请
    Polypeptide derivatives 审中-公开
    多肽衍生物

    公开(公告)号:US20030198598A1

    公开(公告)日:2003-10-23

    申请号:US10373371

    申请日:2003-02-24

    摘要: A biologically active peptide selected from growth factors, peptide hormones, interferons and cytokines and analogues and derivatives thereof, and bearing at least one chelating group linked to an amino group of said peptide, the chelating group being capable of complexing a detectable element and such amino group having no significant binding affinity to target receptors, are complexed with a detectable element and are useful as a pharmaceutical, e.g. a radiopharmaceutical for in vivo imaging of target tissues or for therapy.

    摘要翻译: 选自生长因子,肽激素,干扰素和细胞因子及其类似物和衍生物的生物活性肽,并且具有与所述肽的氨基连接的至少一个螯合基团,所述螯合基团能够络合可检测元件,并且所述氨基 与靶受体没有显着结合亲和力的基团与可检测元件复合并且可用作药物,例如, 用于靶组织的体内成像或用于治疗的放射性药物。

    Novel neuropilin/growth factor complexes and uses thereof
    58.
    发明申请
    Novel neuropilin/growth factor complexes and uses thereof 失效
    新型神经蛋白/生长因子复合物及其用途

    公开(公告)号:US20030125523A1

    公开(公告)日:2003-07-03

    申请号:US10303786

    申请日:2002-11-26

    摘要: Complexes of a protein selected from the group consisting of VEGF-B167, VEGF-C, VEGF-D and processed VEGF-B186 and analogs thereof and the neuropilin-1 (NP-1) receptor, the extracellular domain or a ligand-binding fragment or analogue thereof; the use of such complexes in assays for growth factor proteins having substantially the same binding affinity for a cell surface receptor as VEGF-B167, VEGF-C, VEGF-D or processed VEGF-B186 and/or in promoting or antagonizing a cellular response mediated by VEGF-B167, VEGF-C, VEGF-D and/or processed VEGF-B186; and specific binding partners, e.g. antibodies, for such complexes.

    摘要翻译: 选自VEGF-B167,VEGF-C,VEGF-D和加工的VEGF-B186及其类似物的蛋白质与神经蛋白-1(NP-1)受体,细胞外结构域或配体结合片段的复合物 或其类似物; 对于对VEGF-B167,VEGF-C,VEGF-D或加工的VEGF-B186具有基本上与细胞表面受体具有相同结合亲和力的生长因子蛋白和/或促进或拮抗细胞应答介导的生长因子蛋白 通过VEGF-B167,VEGF-C,VEGF-D和/或加工的VEGF-B186; 和特异性结合配偶体,例如 抗体。

    Method of long-term reversible contraception for animals
    59.
    发明申请
    Method of long-term reversible contraception for animals 审中-公开
    长期可逆避孕方法

    公开(公告)号:US20030108586A1

    公开(公告)日:2003-06-12

    申请号:US10014694

    申请日:2001-12-11

    发明人: Jacques Ramey

    IPC分类号: A61K038/24

    摘要: A method of preventing fertility in a non-human animal includes administering a GnRH antagonist to the animal in an amount sufficient to prevent fertility.

    摘要翻译: 在非人类动物中预防生育力的方法包括以足以防止生育能力的量向动物施用GnRH拮抗剂。