Sulfated .alpha.-glycolipid derivatives as cell adhesion inhibitors
    1.
    发明授权
    Sulfated .alpha.-glycolipid derivatives as cell adhesion inhibitors 失效
    硫酸化α-糖脂衍生物作为细胞粘附抑制剂

    公开(公告)号:US5663151A

    公开(公告)日:1997-09-02

    申请号:US379381

    申请日:1995-01-27

    CPC分类号: C07H15/10 C07H15/04

    摘要: There is provided novel sulfated .alpha.-glycolipid compounds of the formula ##STR1## wherein R is an acyl residue of a fatty acid;R.sup.1 is --(CH.dbd.CH).sub.m --(CH.sub.2).sub.n --CH.sub.3 ;R.sup.2, R.sup.3, R.sup.4and R.sup.6 are independently at least two --SO.sub.3 H;R.sup.2, R.sup.3, R.sup.4R.sup.5 and R.sup.6 each are independently hydrogen, unsubstituted or substituted alkanoyl, arylalkyl or arylcarbonyl wherein said substituent is selected from halogen, C.sub.1-4 alkyl, trifluoromethyl, hydroxy and C.sub.1-4 alkoxy;m is an integer of 0 or 1;n is an integer of from 5 to 14, inclusive;or a non-toxic pharmaceutically acceptable salt, solvate or hydrate thereof which are inhibitors of selectin-mediated cellular adhesion and are useful in the treatment or prevention of inflammatory diseases and other pathological conditions in mammals.

    摘要翻译: 提供了式Ⅰ的新型硫酸化α-糖脂化合物,其中R是脂肪酸的酰基残基; R 1是 - (CH = CH)m - (CH 2)n -CH 3; R2,R3,R4和R6独立地为至少两个-SO3H; R2,R3,R4 R5和R6各自独立地为氢,未取代或取代的烷酰基,芳基烷基或芳基羰基,其中所述取代基选自卤素,C 1-4烷基,三氟甲基,羟基和C 1-4烷氧基; m为0或1的整数; n为5〜14的整数,包括端值; 或其选择素介导的细胞粘附的抑制剂的无毒的药学上可接受的盐,溶剂化物或水合物,并且可用于治疗或预防哺乳动物的炎性疾病和其它病理状况。

    Sulfated .beta.-glycolipid derivatives as cell adhesion inhibitors
    2.
    发明授权
    Sulfated .beta.-glycolipid derivatives as cell adhesion inhibitors 失效
    硫酸化β-糖脂衍生物作为细胞粘附抑制剂

    公开(公告)号:US5565433A

    公开(公告)日:1996-10-15

    申请号:US600558

    申请日:1996-02-12

    CPC分类号: C07H15/10

    摘要: There is provided novel sulfated p-glycolipid compounds of the formula ##STR1## wherein R is an acyl residue of a fatty acid;R.sup.1 is --(CH.dbd.CH).sub.m --(CH.sub.2).sub.n --CH.sub.3 ;R.sup.2, R.sup.3, R.sup.4 and R.sup.6 each are independently --SO.sub.3 H, hydrogen, unsubstituted or substituted alkanoyl, arylalkyl or arylcarbonyl wherein said substituent is selected from the group consisting of halogen, C.sub.1-4 alkyl, trifluoromethyl, hydroxy and C.sub.1-4 alkoxy; or R.sub.4 and R.sub.6, taken together are isopropylidene; provided at least two of R.sup.2, R.sup.3, R.sup.4 and R.sup.6 are --SO.sub.3 H;R.sup.5 is hydrogen, unsubstituted or substituted alkanoyl, arylalkyl or arylcarbonyl wherein said substituent is selected from the group consisting of halogen, C.sub.1-4 alkyl, trifluoromethyl, hydroxy and C.sub.1-4 alkoxy;m is an integer of 0 or 1;n is an integer of from 5 to 14, inclusive;or a non-toxic pharmaceutically acceptable salt, solvate or hydrate thereof which are inhibitors of selectin-mediated cellular adhesion and are useful in the treatment or prevention of inflammatory diseases and other pathological conditions in mammals.

    摘要翻译: 提供了式Ⅰ的新型硫酸化p-糖脂化合物,其中R是脂肪酸的酰基残基; R 1是 - (CH = CH)m - (CH 2)n -CH 3; R 2,R 3,R 4和R 6各自独立地为-SO 3 H,氢,未取代或取代的烷酰基,芳烷基或芳基羰基,其中所述取代基选自卤素,C 1-4烷基,三氟甲基,羟基和C 1-4烷氧基; 或R4和R6一起为异丙叉; 提供R 2,R 3,R 4和R 6中的至少两个是-SO 3 H; R5是氢,未取代或取代的烷酰基,芳基烷基或芳基羰基,其中所述取代基选自卤素,C 1-4烷基,三氟甲基,羟基和C 1-4烷氧基; m为0或1的整数; n为5〜14的整数,包括端值; 或其选择素介导的细胞粘附的抑制剂的无毒的药学上可接受的盐,溶剂化物或水合物,并且可用于治疗或预防哺乳动物的炎性疾病和其它病理状况。

    CD40 receptor ligands
    4.
    发明授权
    CD40 receptor ligands 失效
    CD40受体配体

    公开(公告)号:US06472510B1

    公开(公告)日:2002-10-29

    申请号:US08338975

    申请日:1994-11-14

    IPC分类号: C07K14705

    摘要: The present invention relates to a counter-receptor, termed CD40CR, for the CD40 B-cell antigen, and to soluble ligands for this receptor, including fusion molecules comprising at least a portion of CD40 protein. It is based, at least in part, on the discovery that a soluble CD40/immunoglobulin fusion protein was able to inhibit helper T-cell mediated B-cell activation by binding to a novel 39 kD protein receptor on helper T-cell membranes. The present invention provides for a substantially purified CD40CR receptor; for soluble ligands of CD40CR, including antibodies as well as fusion molecules comprising at least a portion of CD40 protein; and for methods of controlling B-cell activation which may be especially useful in the treatment of allergy or autoimmune disease.

    摘要翻译: 本发明涉及用于CD40B细胞抗原的称为CD40CR的反受体,以及该受体的可溶性配体,包括至少包含一部分CD40蛋白的融合分子。 至少部分基于这样一个发现,即可溶性CD40 /免疫球蛋白融合蛋白能够通过结合辅助性T细胞膜上的新型39kD蛋白受体来抑制辅助T细胞介导的B细胞活化。 本发明提供了基本纯化的CD40CR受体; 用于CD40CR的可溶性配体,包括抗体以及包含至少一部分CD40蛋白的融合分子; 以及用于控制B细胞活化的方法,其可能特别可用于治疗过敏或自身免疫性疾病。

    Artificial proteoglycans
    8.
    发明授权
    Artificial proteoglycans 失效
    人造蛋白多糖

    公开(公告)号:US06559287B1

    公开(公告)日:2003-05-06

    申请号:US09235230

    申请日:1999-01-21

    IPC分类号: C07K1400

    摘要: Novel articifial proteoglycans containing a GAG assembly site and a control sequence required for assembly, method for enhancing the biological activity of a glycosaminoglycan binding protein using artificial proteoglycans, DNA constructs of artificial proteoglycans. The artificial proteoglycans of the present invention are useful for preparations of adjuvants for vaccination, for targeting of chemokines to non-immunogenic tumor cells to enhance cellular anti-tumor response, for preparations designed to help promote wound healing, and for treatment of immunological disorders,including rheumatoid arthritis, asthma, chronic obstructive pulmonary disorder, Lupus, inflammatory bowel disease, psoriasis, osteoarthritis, and HIV infection.

    摘要翻译: 含有GAG组装位点和组装所需的控制序列的新颖的克隆蛋白聚糖,使用人造蛋白聚糖增强糖胺聚糖结合蛋白的生物活性的方法,人造蛋白聚糖的DNA构建体。 本发明的人造蛋白聚糖可用于疫苗接种佐剂的制备,将趋化因子靶向非免疫原性肿瘤细胞以增强细胞抗肿瘤反应,用于帮助促进伤口愈合的制剂和用于治疗免疫疾病, 包括类风湿关节炎,哮喘,慢性阻塞性肺病,狼疮,炎性肠病,牛皮癣,骨关节炎和HIV感染。