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29 条记录 (耗时 0.029 秒)

    Dihomo-seco-cholestanes
    1.
    发明授权
    Dihomo-seco-cholestanes 失效

    公开(公告)号：US5994569A

    公开(公告)日：1999-11-30

    申请号：US115188

    申请日：1998-07-14

    申请人： Pierre Barbier ,  Peter Mohr ,  Marc Muller ,  Christopher Self

    发明人： Pierre Barbier ,  Peter Mohr ,  Marc Muller ,  Christopher Self

    IPC分类号： A61K31/59 ,  A61P3/02 ,  A61P3/10 ,  A61P19/10 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  C07C401/00

    CPC分类号： C07C401/00

    摘要： Polyunsaturated 24a,24b-dihomo-9,10-secocholestane derivatives of formula ##STR1## wherein A is a single or double bond,B.sup.1 and B.sup.2 are each independently CH.dbd.CH or C.tbd.C,T is CH.sub.2 or CH.sub.2 CH.sub.2,X is --CH.sub.2 -- or >C.dbd.CH.sub.2,R.sup.1 is H, F or OH,R.sup.2 and R.sup.3 are each independently lower alkyl or CF.sub.3, orC(R.sup.2,R.sup.3) is C.sub.3-6 -cycloalkyl,are useful in the treatment or prevention of vitamin D dependent disorders and of IL-12-dependent autoimmune diseases, particularly psoriasis, basal cell carcinomas, disorders of keratinization and keratosis, leukemia, osteoporosis, hyperparathyroidism accompanying renal failure, multiple sclerosis, transplant rejection, graft vs. host disease, rheumatoid arthritis, insulin-dependent diabetes mellitus, inflammatory bowel disease, septic shock and allergic encephalomyelitis.

    摘要翻译： 多不饱和的24a，24b-二氢-9,10-断氧胆甾烷衍生物，其中A为单键或双键，B1和B2各自独立地为CH = CH或C，3BOND C，T为CH2或CH2CH2，X为-CH2-或 > C = CH 2，R 1为H，F或OH，R 2和R 3各自独立地为低级烷基或CF 3，或C（R 2，R 3）为C 3-6环烷基，可用于治疗或预防维生素D依赖性疾病 和IL-12依赖性自身免疫性疾病，特别是牛皮癣，基底细胞癌，角质化和角化病，白血病，骨质疏松症，伴随肾衰竭的甲状旁腺功能亢进，多发性硬化，移植排斥，移植物抗宿主病，类风湿性关节炎，胰岛素依赖性 糖尿病，炎性肠病，败血性休克和过敏性脑脊髓炎。

    Modulators of ß-amyloid peptide aggregation
    8.
    发明申请
    Modulators of ß-amyloid peptide aggregation 失效
    β-淀粉样肽聚集的调节剂

    公开(公告)号：US20050137128A1

    公开(公告)日：2005-06-23

    申请号：US10989763

    申请日：2004-11-15

    申请人： Mark Findeis ,  Kathryn Phillips ,  Gary Olsen ,  Christopher Self

    发明人： Mark Findeis ,  Kathryn Phillips ,  Gary Olsen ,  Christopher Self

    IPC分类号： G01N33/68 ,  A61K38/00 ,  A61K38/17 ,  A61P25/28 ,  A61P43/00 ,  C07K5/083 ,  C07K7/06 ,  C07K14/47 ,  A61K38/12 ,  C07K5/12

    CPC分类号： C07K14/4711 ,  A61K38/00

    摘要： Compounds that modulate natural β amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a β amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3-5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a β amyloid peptide, preferably a retro-inverso isomer of Aβ17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an acetate group, an alkyl amide group, an aryl amide group or a hydroxy group. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.

    摘要翻译： 提供调节天然β淀粉样肽聚集的化合物。 本发明的调节剂包含优选基于β-淀粉样肽的肽，其完全由D-氨基酸组成。 优选地，肽包含3-5个D-氨基酸残基，并且包括独立地选自D-亮氨酸，D-苯丙氨酸和D-缬氨酸的至少两个D-氨基酸残基。 在特别优选的实施方案中，肽是β淀粉样肽的逆反异构体，优选Abeta 17-21的逆反异构体。 在某些实施方案中，肽在氨基末端，羧基末端或两者都被修饰。 优选的氨基末端修饰基团是烷基。 优选的羧基末端修饰基团包括酰胺基，乙酸基，烷基酰胺基，芳基酰胺基或羟基。 还公开了包含本发明化合物的药物组合物，以及使用本发明化合物的淀粉样变性疾病的诊断和治疗方法。

    Modulators of β-amyloid peptide aggregation
    9.
    发明授权
    Modulators of β-amyloid peptide aggregation 失效
    β-淀粉样肽聚集的调节剂

    公开(公告)号：US07803774B2

    公开(公告)日：2010-09-28

    申请号：US10989763

    申请日：2004-11-15

    申请人： Mark A. Findeis ,  Kathryn Phillips ,  Gary L. Olsen ,  Christopher Self

    发明人： Mark A. Findeis ,  Kathryn Phillips ,  Gary L. Olsen ,  Christopher Self

    IPC分类号： A61K38/00 ,  A61K49/00

    CPC分类号： C07K14/4711 ,  A61K38/00

    摘要： Compounds that modulate natural β amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a β amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3-5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a β amyloid peptide, preferably a retro-inverso isomer of Aβ17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an acetate group, an alkyl amide group, an aryl amide group or a hydroxy group. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.

    摘要翻译： 调节天然化合物的化合物 提供淀粉样肽聚集。 本发明的调节剂包含肽，优选基于 淀粉样肽，其完全由D-氨基酸组成。 优选地，肽包含3-5个D-氨基酸残基，并且包括独立地选自D-亮氨酸，D-苯丙氨酸和D-缬氨酸的至少两个D-氨基酸残基。 在一个特别优选的实施方案中，该肽是一种反式异构体， 淀粉样蛋白肽，优选A-Bgr; 17-21的逆反异构体。 在某些实施方案中，肽在氨基末端，羧基末端或两者都被修饰。 优选的氨基末端修饰基团是烷基。 优选的羧基末端修饰基团包括酰胺基，乙酸基，烷基酰胺基，芳基酰胺基或羟基。 还公开了包含本发明化合物的药物组合物，以及使用本发明化合物的淀粉样变性疾病的诊断和治疗方法。