Dendrimers as molecular translocators
    1.
    发明授权
    Dendrimers as molecular translocators 有权
    树枝状聚合物作为分子转运体

    公开(公告)号:US07862807B2

    公开(公告)日:2011-01-04

    申请号:US10522128

    申请日:2003-07-18

    IPC分类号: A61K31/74

    摘要: Transport molecules include a dendrimer and a biologically active molecule. The dendrimer of such transport molecules includes at least one guanidine group, at least one protonated guanidine group, at least one protected guanidine group, at least one amidine group, at least one protonated amidine group, at least one protected amidine group, at least one ureido group, at least one protonated ureido group, at least one protected ureido group, at least one thioureido group, at least one protonated thioureido group, or at least one protected thioureido group. The biologically active molecule is bonded to the dendrimer. A method of increasing the bioavailability of a drug includes bonding the drug to a dendrimer of the invention.

    摘要翻译: 运输分子包括树枝状大分子和生物活性分子。 该转运分子的树枝状大分子包括至少一个胍基,至少一个质子化胍基,至少一个被保护的胍基,至少一个脒基,至少一个质子化的脒基,至少一个保护的脒基,至少一个 脲基,至少一个质子化脲基,至少一个保护的脲基,至少一个硫脲基,至少一个质子化硫脲基或至少一个被保护的硫脲基。 生物活性分子与树枝状大分子结合。 提高药物的生物利用度的方法包括将药物结合到本发明的树枝状大分子。

    Dendrimers as Molecular Translocators
    2.
    发明申请
    Dendrimers as Molecular Translocators 审中-公开
    树枝状大分子作为分子转运子

    公开(公告)号:US20080221020A1

    公开(公告)日:2008-09-11

    申请号:US10522130

    申请日:2003-07-18

    摘要: Transport molecules include a dendrimer and a biologically active molecule. The dendrimer of such transport molecules includes at least one guanidine group, at least one protonated guanidine group, at least one protected guanidine group, at least one amidine group, at least one protonated amidine group, at least one protected amidine group, at least one ureido group, at least one protonated ureido group, at least one protected ureido group, at least one thioureido group, at least one protonated thioureido group, or at least one protected thioureido group. The biologically active molecule is bonded to the dendrimer. A method of increasing the bioavailability of a drug includes bonding the drug to a dendrimer of the invention.

    摘要翻译: 运输分子包括树枝状大分子和生物活性分子。 该转运分子的树枝状大分子包括至少一个胍基,至少一个质子化胍基,至少一个被保护的胍基,至少一个脒基,至少一个质子化的脒基,至少一个保护的脒基,至少一个 脲基,至少一个质子化脲基,至少一个保护的脲基,至少一个硫脲基,至少一个质子化硫脲基或至少一个被保护的硫脲基。 生物活性分子与树枝状大分子结合。 提高药物的生物利用度的方法包括将药物结合到本发明的树枝状大分子。

    Metabolically acceptable polyisocyanate adhesives
    5.
    发明授权
    Metabolically acceptable polyisocyanate adhesives 失效
    代谢可接受的多异氰酸酯粘合剂

    公开(公告)号:US4829099A

    公开(公告)日:1989-05-09

    申请号:US74597

    申请日:1987-07-17

    摘要: Metabolically-acceptable, surgical adhesives are prepared from polyisocyanates having the structral formula: ##STR1## wherein R is a polyvalent aliphatic radical of about 1 to 10 carbon atoms or a polyvalent aromatic radical of 6 to about 24 carbon atoms;A is C, S or P;Z is O or S;Y is 1 when A is C or P, and 2 when A is S;n is 1 or 2;p is at least 1;q is 0 or 1, with the proviso that when A is carbon or sulfur, q is 0;r is 0 or 1, with the proviso that when A is carbon or sulfur, r is 0;X is a residue of an organic compound having active hydrogen-containing groups; andX' is a residue of an organic compound having at least 1 active hydrogen-containing group.

    摘要翻译: 代谢可接受的手术粘合剂由具有以下结构式的多异氰酸酯制备:其中R是约1-10个碳原子的多价脂肪族基团或6至约24个碳原子的多价芳族基团; A是C,S或P; Z是O或S; 当A为C或P时,Y为1,A为S时为2; n为1或2; p至少为1; q为0或1,条件是当A为碳或硫时,q为0; r为0或1,条件是当A为碳或硫时,r为0; X是具有含活性氢基团的有机化合物的残基; X'是具有至少1个含活性氢基团的有机化合物的残基。

    Biologically active catecholamine derivatives
    6.
    发明授权
    Biologically active catecholamine derivatives 失效
    生物活性儿茶酚胺衍生物

    公开(公告)号:US4337207A

    公开(公告)日:1982-06-29

    申请号:US184000

    申请日:1980-09-04

    IPC分类号: C07C233/00 C07C103/29

    CPC分类号: C07C233/00

    摘要: Biologically active derivatives of norepinephrine are disclosed. Such derivatives are catecholamines wherein isoproterenol is modified by extending the isopropyl functional grouping to an alkyl, aryl, or alkyl-aryl chain of variable length where said chain terminates in a carboxylic acid functional group, or in a substituted amide functional group. Such derivatives are .beta.-adrenergic and a number of such derivatives e.g., 6-(.beta.-3,4-dihydroxyphenyl-.beta.-hydroxy)-ethylamino heptanoic acid p-toluide, 6-(.beta.-3,4-dihydroxyphenyl-.beta.-hydroxy)-ethylamino heptanoic acid para-n-butyl anilide; 6-(.beta.,3,4-dihydroxyphenyl-.beta.-hydroxy)-ethylamino heptanoic acid para-methoxy anilide; 6-(.beta.-3,4-dihydroxyphenyl-.beta.-hydroxy)-ethylamino heptanoic acid paratrifluoromethyl anilide; and 6-(.beta.-3,4-dihydroxyphenyl-.beta.-hydroxy)-ethylamino heptanoic acid N-methyl para-toluide display a .beta.-adrenergic activity at least several orders of magnitude greater than isoproterenol itself. Several methods of producing such active derivatives are also disclosed.

    摘要翻译: 公开了去甲肾上腺素的生物活性衍生物。 这样的衍生物是儿茶酚胺,其中异丙肾上腺素通过将异丙基官能团延伸到可变长度的烷基,芳基或烷基 - 芳基链来修饰,其中所述链终止于羧酸官能团,或在取代的酰胺官能团中。 这样的衍生物是β-肾上腺素能的,并且许多这样的衍生物例如6-(β-3,4-二羟基苯基-β-羟基) - 乙基氨基庚酸对甲苯胺,6-(β-3,4-二羟基苯基-β- 羟基) - 乙基氨基庚酸对 - 丁基苯胺; 6-(β,3,4-二羟基苯基-β-羟基) - 乙基氨基庚酸对甲氧基苯胺; 6-(β-3,4-二羟基苯基-β-羟基) - 乙基氨基庚酸对三氟甲基苯胺; 和6-(β-3,4-二羟基苯基-β-羟基) - 乙基氨基庚酸N-甲基对甲苯甲酸显示比异丙肾上腺素本身至少几个数量级的β-肾上腺素能活性。 还公开了生产这种活性衍生物的几种方法。

    Template-assisted triple helical collagen-like structures
    9.
    发明授权
    Template-assisted triple helical collagen-like structures 失效
    模板辅助三螺旋胶原样结构

    公开(公告)号:US06329506B1

    公开(公告)日:2001-12-11

    申请号:US09388916

    申请日:1999-09-01

    IPC分类号: C07K1400

    摘要: Synthetic collagen in triple helical conformation and comprising amino acid chains of repeating trimers of highly populated collagen sequences as well as those sequences wherein the proline or hydroxyproline residue is replaced with a peptoid residue. The invention includes methods of preparing synthetic collagen structures having the triple helix conformation present in collagen from collagen-type polypeptides and poly(peptide-peptoid residue) chains by means of a helix-inducing template.

    摘要翻译: 三重螺旋构象中的合成胶原,并且包含高度人口稠密的胶原序列的重复三聚体的氨基酸链以及其中脯氨酸或羟脯氨酸残基被拟肽残基替代的那些序列。 本发明包括通过螺旋诱导模板从胶原型多肽和聚(肽 - 拟肽残基)链制备具有存在于胶原中的三螺旋构象的合成胶原结构的方法。

    Histamine derivatives useful as immunomodulators
    10.
    发明授权
    Histamine derivatives useful as immunomodulators 失效
    组胺衍生物可用作免疫调节剂

    公开(公告)号:US5556872A

    公开(公告)日:1996-09-17

    申请号:US483947

    申请日:1995-06-07

    CPC分类号: C07D233/64 A61K31/415

    摘要: The present invention provides histamine derivatives and methods for using histamine derivatives as immunomodulators and in immunotherapeutics. More specifically the present invention provides methods for inhibiting at least a portion of an an antigen specific antibody response and/or a portion of a T-cell proliferative response by the immune system of a mammal comprising administering to said mammal an effective amount of a composition comprising at least one histamine derivative having binding specificity for at least one histamine receptor.

    摘要翻译: 本发明提供组胺衍生物和使用组胺衍生物作为免疫调节剂和免疫治疗剂的方法。 更具体地,本发明提供了用于通过哺乳动物的免疫系统抑制至少一部分抗原特异性抗体应答和/或一部分T细胞增殖应答的方法,所述方法包括向所述哺乳动物施用有效量的组合物 包含至少一种对至少一种组胺受体具有结合特异性的组胺衍生物。