HYBRID PROTEINS
    4.
    发明申请
    HYBRID PROTEINS 审中-公开
    杂交蛋白

    公开(公告)号:WO1983003971A1

    公开(公告)日:1983-11-24

    申请号:PCT/US1983000723

    申请日:1983-05-12

    Abstract: A hybrid protein including protein fragments joined together by peptide bonds, the hybrid protein including, in sequential order, beginning at the amino terminal end of the hybrid protein, (a) the enzymatically active Fragment A of diphtheria toxin, (b) a fragment including the cleavage domain 11 adajacent Fragment A, (c) a fragment including at least the portion of Fragment B of diphtheria toxin encoded by the portion of the Fragment B encoding gene fragment of the tox operon between 11 and the position about 90 base pairs upstream from the position on the tox operon of the NRU I site of the tox allele, and (d) a fragment including a portion of a cell-specific polypeptide ligand, such portion including at least a portion of the binding domain of the polypeptide ligand, such portion of the binding domain being effective to cause the hybrid protein to bind selectively to a predetermined class of cells to be attacked by enzymatically active Fragment A.

    Abstract translation: 一种杂合蛋白,包括通过肽键连接在一起的蛋白质片段,杂合蛋白包括从杂交蛋白的氨基末端开始的顺序,(a)白喉毒素的酶活性片段A,(b)包括 切割结构域11相邻片段A,(c)包含由11个毒素操纵子的片段B编码基因片段的部分编码的至少部分白喉毒素片段B的片段和在上游约90个碱基对之间的位置 tox等位基因的NRU I位点的tox操纵子上的位置,和(d)包含一部分细胞特异性多肽配体的片段,该部分包括多肽的结合结构域的至少一部分 配体,这样的部分结合结构域有效地使杂交蛋白选择性地结合预定类别的细胞被酶活性片段A攻击。

    PHARMACEUTICAL COMPOSITIONS OF MELANOCORTIN RECEPTOR LIGANDS
    5.
    发明申请
    PHARMACEUTICAL COMPOSITIONS OF MELANOCORTIN RECEPTOR LIGANDS 审中-公开
    梅毒素受体配体的药物组合物

    公开(公告)号:WO2011060352A1

    公开(公告)日:2011-05-19

    申请号:PCT/US2010/056690

    申请日:2010-11-15

    Abstract: The present invention relates to improvements in compositions containing peptides that are ligands of one or more of the melanocortin receptors (MC-R), or pharmaceutically acceptable salts thereof, methods for preparing such compositions, and method of using such compositions to treat mammals. In particular, the present invention relates to a pharmaceutical composition comprising a pamoate salt of Ac-Arg-cyclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2 which is a ligand of the melanocortin receptor subtype 4 (MC4-R), and in which, after subcutaneous or intramuscular administration to a subject, the peptide forms a depot at physiological pH that is slowly dissolved and released into the body fluid and bloodstream. The present invention may further comprise an organic component such as dimethylacetamide (DMA) or polyethylene glycol (PEG) with an average molecular weight of lower than 1000.

    Abstract translation: 本发明涉及包含作为一种或多种黑皮质素受体(MC-R)的配体的肽或其药学上可接受的盐的组合物的组合物的改进,以及使用这些组合物治疗哺乳动物的方法。 特别地,本发明涉及包含作为黑皮质素受体的配体的Ac-Arg-环(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH 2的双羟萘酸盐的药物组合物 亚型4(MC4-R),并且其中在对受试者皮下或肌肉内施用后,肽在生理pH下形成缓慢溶解并释放到体液和血流中的贮库。 本发明还可以包含平均分子量低于1000的有机组分如二甲基乙酰胺(DMA)或聚乙二醇(PEG)。

    LIGANDS OF MELANOCORTIN RECEPTORS
    6.
    发明申请
    LIGANDS OF MELANOCORTIN RECEPTORS 审中-公开
    MELANOCORTIN受体配体

    公开(公告)号:WO2007008684A3

    公开(公告)日:2009-05-07

    申请号:PCT/US2006026554

    申请日:2006-07-10

    CPC classification number: C07K14/685 A61K38/00 C07K14/69 C07K14/695

    Abstract: The present invention is directed to a compound according to formula, (R2R3)-B1-A1-c(A2-A3-A4-A5-A6-A7-A8-A9)-A10-A11-A12-A13-B2-B3-R1, that act as ligands for one or more of the melanocortin receptors, the pharmaceutically- acceptable salts thereof, to methods of using such peptides to treat mammals and to pharmaceutical compositions useful therefore comprising said peptides.

    Abstract translation: 本发明涉及下式化合物:(R2R3)-B1-A1-c(A2-A3-A4-A5-A6-A7-A8-A9)-A10-A11-A12-A13-B2-B3 -R1,其用作一种或多种黑皮质素受体的配体,其药学上可接受的盐,用于使用这些肽来治疗哺乳动物的方法和用于因此包含所述肽的药物组合物。

    LIGANDS OF MELANOCORTIN RECEPTORS
    9.
    发明申请
    LIGANDS OF MELANOCORTIN RECEPTORS 审中-公开
    MELANOCORTIN受体配体

    公开(公告)号:WO2007008684A2

    公开(公告)日:2007-01-18

    申请号:PCT/US2006/026554

    申请日:2006-07-10

    CPC classification number: C07K14/685 A61K38/00 C07K14/69 C07K14/695

    Abstract: The present invention is directed to a compound according to formula, (R 2 R 3 )-B 1 -A 1 -c(A 2 -A 3 -A 4 -A 5 -A 6 -A 7 -A 8 -A 9 )-A 10 -A 11 -A 12 -A 13 -B 2 -B 3 -R 1 , that act as ligands for one or more of the melanocortin receptors, the pharmaceutically- acceptable salts thereof, to methods of using such peptides to treat mammals and to pharmaceutical compositions useful therefore comprising said peptides.

    Abstract translation: 本发明涉及下式的化合物,其中R 1,R 2,R 3,R 3, SUP> -c(A 2 -A 3 -A 4 -A 5 -A 6 -A 7 -A 8 -A 9 ) - A 10 -A 11 -A 12 -A 13 -B 2 -B 3 -R 1,其用作一种或多种黑皮质素受体的配体,其药学上可接受的盐,用于使用这些肽治疗哺乳动物的方法和用于因此包含所述肽的药物组合物。

    COMPOUNDS FOR USE IN THE TREATMENT OF INFLAMMATION
    10.
    发明申请
    COMPOUNDS FOR USE IN THE TREATMENT OF INFLAMMATION 审中-公开
    用于治疗感染的化合物

    公开(公告)号:WO00005263A3

    公开(公告)日:2000-05-04

    申请号:PCT/GB1999/002392

    申请日:1999-07-22

    CPC classification number: C07K5/1024 A61K38/00 C07K14/69 C07K14/695

    Abstract: Use of a compound comprising an amino acid sequence HFRW in the manufacture of a medicament for inhibition of neutrophil chemoattractant production, inhibition of polymorphonuclear cell (PMN) accumulation, or reduction/treatment of inflammatory response/disease, and/or in the manufacture of an agonist of melanocortin receptor type 3 (MC3-R); wherein the compound is not adrenocorticotrophic hormone (ACTH)>1-39

    Abstract translation: 包含氨基酸序列HFRW的化合物在制备用于抑制中性粒细胞化学引诱物产生,抑制多形核细胞(PMN)积累或减少/治疗炎症反应/疾病的药物中的用途,和/或制造 黑色素皮质素受体3型(MC3-R)的激动剂; 其中所述化合物不是激活糖皮质激素产生的促肾上腺皮质激素(ACTH)> 1-39或其片段。

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