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53 条记录 (耗时 0.022 秒)

    Cell-specific glycopeptide ligands
    23.
    发明授权
    Cell-specific glycopeptide ligands 失效
    细胞特异性糖肽配体

    公开(公告)号：US4386026A

    公开(公告)日：1983-05-31

    申请号：US255416

    申请日：1981-04-20

    申请人： Mitree M. Ponpipom ,  Robert L. Bugianesi ,  James C. Robbins ,  Tsung-Ying Shen

    发明人： Mitree M. Ponpipom ,  Robert L. Bugianesi ,  James C. Robbins ,  Tsung-Ying Shen

    IPC分类号： C07K9/00 ,  A61K9/18 ,  A61K47/42 ,  C07H15/04 ,  C07H15/14 ,  C07J9/00 ,  C07J31/00 ,  C07J41/00 ,  C07K1/113 ,  C07C103/52 ,  C07H11/00 ,  C08B37/00

    CPC分类号： C07H15/14 ,  A61K47/48092 ,  C07H15/04 ,  C07J31/006 ,  C07J41/005

    摘要： Cell-specific ligands comprising conjugates of saccharides and amino acids or peptides are synthesized from amino acids such as ornithine, lysine, peptides such as dilysine, diornithine or oligolysine and selected saccharides having reactive functional groups protected by appropriate blocking groups. Such glycopeptides are useful as tissue specific substances, which when coupled with bioactive materials through metabolizable or hydrolyzable linkages, deliver such bioactive materials to the selected site. In this manner, antiinflammatory drugs such as dexamethasone are linked through a metabolizable or hydrolyzable linkage and on administration to an animal suffering from inflammatory disease carries the drug to the site of inflammation for intracellular release. Other examples include the macrophage ligand N.sup.2 -N.sup.2, N.sup.6 -Bis-[3-(.alpha.-D-mannopyranosylthio)propionyl]-6-lysyl-N.sup.6 -[3-(.alpha.-D-mannopyranosylthio)propionyl]-L-lysine, 5, which when coupled to .beta.-glucocerebrosidase, can deliver the enzyme selectively to kupffer cells. This is useful in the enzyme replacement therapy of Gaucher's disease.

    摘要翻译： 包括糖和氨基酸或肽的缀合物的细胞特异性配体由氨基酸如鸟氨酸，赖氨酸，肽如二枞氨酸，二氢鸟氨酸或寡聚赖氨酸和选择的具有由适当阻断基团保护的反应性官能团的糖合成。 这种糖肽可用作组织特异性物质，当通过可代谢或可水解的连接与生物活性物质结合时，将这种生物活性物质递送至所选择的位点。 以这种方式，抗炎药物如地塞米松通过可代谢的或可水解的连接物连接，并且在给予患有炎性疾病的动物的情况下将药物运送到炎症部位以进行细胞内释放。 其他实例包括巨噬细胞配体N2-N2，N6-双 - [3-（α-D-吡喃甘露糖基硫代）丙酰] -6-赖氨酰-N6- [3-（α-D-吡喃甘露糖基硫代）丙酰] -L-赖氨酸， 5，当其与β-葡聚糖焦磺酸酶偶联时，可以选择性地将酶递送至枯否细胞。 这在戈谢病的酶替代疗法中是有用的。

    Immunologically active dipeptidyl 4-O-,6-O-acyl-2-amino-2-deoxy-D-glucose derivatives and methods for their preparation
    24.
    发明授权
    Immunologically active dipeptidyl 4-O-,6-O-acyl-2-amino-2-deoxy-D-glucose derivatives and methods for their preparation 失效

    公开(公告)号：US4368190A

    公开(公告)日：1983-01-11

    申请号：US141227

    申请日：1980-04-17

    申请人： Tsung-Ying Shen ,  Philippe L. Durette ,  Conrad P. Dorn, Jr. ,  James B. Doherty ,  Richard T. Dean

    发明人： Tsung-Ying Shen ,  Philippe L. Durette ,  Conrad P. Dorn, Jr. ,  James B. Doherty ,  Richard T. Dean

    IPC分类号： A61K39/39 ,  A61P31/04 ,  C07K9/00 ,  A61K37/02 ,  A61K39/00 ,  C07C103/52

    CPC分类号： C07K9/005

    摘要： Immunologically active compounds of the formula: ##STR1## wherein: R.sub.1 is C.sub.1-7 alkyl; substituted C.sub.1-7 alkyl; phenyl; or substituted phenyl;R.sub.2 is hydrogen; C.sub.1-7 alkyl; substituted C.sub.1-7 alkyl; phenyl; substituted phenyl; phenyl C.sub.1-4 alkyl; or substituted phenyl C.sub.1-4 alkyl;R.sub.3 and R.sub.4 may be the same or different and are each independently hydrogen, provided that R.sub.3 and R.sub.4 may not both be hydrogen; or ##STR2## where X is --O--; --S--; or ##STR3## R.sub.10 is hydrogen; C.sub.1-30 alkyl; C.sub.2-30 alkenyl; C.sub.1-30 alkoxy; phenyl; C.sub.1-20 alkylsulfonyl; or cholesteryl;R.sub.11, R.sub.12, R.sub.13, R.sub.14, and R.sub.15 may be the same or different and are each independently hydrogen; C.sub.1-20 alkyl; C.sub.1-20 alkylcarbonyloxy; amino; benzyl; C.sub.1-20 alkoxymethyl; C.sub.1-20 alkylamido; or ##STR4## r is 0 or 1; s is 0 or 1; and t is 0 to 20; provided that s may only be 0 when both r and t are greater than 0 or when r is 0 and R.sub.10 is amino; phenyl; substituted phenyl; 1-adamantyl; or heterocycle selected from the group consisting of 2- or 3-furyl, 2- or 3- thienyl, 2- or 3- pyrrolidinyl, 2-, 3- or 4- pyridyl, and 1-tetrazolyl, said heterocycle optionally substituted with C.sub.1-20 alkylcarbonyl; and where R.sub.3 or R.sub.4 is other than hydrogen, the other of R.sub.3 and R.sub.4 may additionally be C.sub.1-4 alkylcarbonyl;R.sub.5 is hydrogen or C.sub.1-10 alkyl;R.sub.6 is hydrogen or R.sub.6 and R.sub.7 taken together are --(CH.sub.2).sub.3 --;R.sub.7 is hydrogen; C.sub.1-7 alkyl; hydroxymethyl; mercaptomethyl; benzyl; or substituted benzyl;R.sub.8 and R.sub.9 may be the same or different and are each independently COOR, or CONR'R", where R is hydrogen or C.sub.1-7 alkyl, and R' and R" are hydrogen or C.sub.1-3 alkyl;when R.sub.5 is C.sub.1-10 alkyl, the stereochemistry at asymmetric center I is D or L;when R.sub.7 is other than hydrogen, the stereochemistry at asymmetric center II is L; and the stereochemistry at asymmetric center III is D; and acid addition and quaternary salts thereof.

    Anti-inflammatory, analgesic and antipyretic phenylacetic acids
    30.
    发明授权
    Anti-inflammatory, analgesic and antipyretic phenylacetic acids 失效
    抗炎，镇痛和解热的苯乙酸

    公开(公告)号：US4046905A

    公开(公告)日：1977-09-06

    申请号：US604524

    申请日：1975-08-14

    申请人： Tsung-Ying Shen ,  Jorge P. Li ,  Conrad P. Dorn, Jr.

    发明人： Tsung-Ying Shen ,  Jorge P. Li ,  Conrad P. Dorn, Jr.

    IPC分类号： A61K31/42

    摘要： The invention relates to a novel class of 4-(benzoxazol-2-yl)phenylacetic acids, alcohols, esters, amides and the non-toxic pharmaceutically acceptable salts thereof and processes for their preparation. The invention further pertains to a class of (benzoxazol-2-yl)phenylacetic acids useful as antiinflammatory agents.

    摘要翻译： 本发明涉及新型的4-（苯并恶唑-2-基）苯乙酸，醇，酯，酰胺及其无毒的药学上可接受的盐及其制备方法。 本发明还涉及可用作抗炎剂的一类（苯并恶唑-2-基）苯乙酸。