PEPTIDES
    6.
    发明申请
    PEPTIDES 审中-公开

    公开(公告)号:US20080318838A1

    公开(公告)日:2008-12-25

    申请号:US12169134

    申请日:2008-07-08

    摘要: PTH compounds having PTH-like activity and comprising at least one modification, said modification being either 1. at least one radical selected from a L- or D-α-amino acid, C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to the terminal amino group of the PTH compound, and/or at least one radical selected from C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to one or more side chain amino groups of the PTH compound, or 2. at least one α-amino acid unit in the positions 1 to 38 of a naturally occurring PTH sequence being replaced by a natural or unnatural amino acid unit optionally in protected form, whereby the α-amino acid units present in positions 1 and 2 at the amino terminus of the PTH sequence may be replaced by a pseudo-peptide, or a combination of such modifications, in free form or in salt form, have pharmacological activity, e.g. for preventing or treating all bone conditions which are associated with increased calcium depletion or resorption or in which calcium fixation in the bone is desirable.

    摘要翻译: 具有PTH样活性并且包含至少一个修饰的PTH化合物,所述修饰是1.至少一个选自L-或D-α-氨基酸,C2-6羰基和任选取代的C 1-8烷基的基团,C 2-8烯基 ,C 2-8炔基,芳烷基,芳烯基或C 3-6环烷基-C 1-4烷基,并且连接到PTH化合物的末端氨基,和/或至少一个选自C 2-6烷氧基羰基和任选取代的C 1-8烷基基团,C 2-8烯基 ,C 2-8炔基,芳烷基,芳烯基或C 3-6环烷基-C 1-4烷基,并且连接到PTH化合物的一个或多个侧链氨基,或2个至少一个α-氨基酸单元的位置1至38 天然存在的PTH序列被任选以保护形式的天然或非天然氨基酸单元替代,由此存在于PTH序列的氨基末端的位置1和2中的α-氨基酸单元可被假肽替代,或 这些修改的组合,免费的 m或盐形式,具有药理活性,例如。 用于预防或治疗与增加的钙耗竭或吸收相关的所有骨骼状况或其中期望骨中的钙固定。

    Polypeptide derivatives
    8.
    发明授权
    Polypeptide derivatives 失效
    多肽衍生物

    公开(公告)号:US5686410A

    公开(公告)日:1997-11-11

    申请号:US276280

    申请日:1994-07-18

    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。

    Somatostatine derivatives
    9.
    发明授权
    Somatostatine derivatives 失效
    生长激素衍生物

    公开(公告)号:US4728638A

    公开(公告)日:1988-03-01

    申请号:US816663

    申请日:1986-01-07

    摘要: Somatostatine derivatives of the general formula ##STR1## wherein either (a)A is ##STR2## W is -CO-N(A.sub.4) or -N(A.sub.5)-CO- and Y.sub.1 and Y.sub.2 are H or together a bondor (b)A is H, alkyl, phenylalkyl or RCO andY.sub.1 and Y.sub.2 are acyl groups as defined in claim 1,A', B, C, D, E, F, A.sub.1, A.sub.2, A.sub.3, A.sub.4, A.sub.5, R and Z having the meanings recited in claim 1, have pharmacological, in particular GH-, gastric- and pancreatic secretion inhibiting activity.

    摘要翻译: 其中(a)A是-CO-N(A4)或-N(A5)-CO-,Y1和Y2是H或一起键或(b)的通式的生长激素衍生物 )A是H,烷基,苯基烷基或RCO,Y 1和Y 2是如权利要求1中定义的酰基,A',B,C,D,E,F,A1,A2,A3,A4,A5,R和Z具有 权利要求1所述的含义具有药理学,特别是GH-,胃和胰腺分泌抑制活性。