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    Method of determining a site of inflammation utilizing elam-1 ligands
    2.
    发明授权
    Method of determining a site of inflammation utilizing elam-1 ligands 失效
    使用elam-1配体测定炎症部位的方法

    公开(公告)号：US5143712A

    公开(公告)日：1992-09-01

    申请号：US637868

    申请日：1991-01-07

    申请人： Brian K. Brandley ,  Michael Tiemeyer ,  Stuart J. Swiedler ,  Margaret Moreland ,  Hans Schweingruber

    发明人： Brian K. Brandley ,  Michael Tiemeyer ,  Stuart J. Swiedler ,  Margaret Moreland ,  Hans Schweingruber

    IPC分类号： A61K31/70 ,  A61K51/08 ,  C07H13/04 ,  C07K14/705 ,  G01N33/569

    CPC分类号： C07H13/04 ,  A61K31/70 ,  A61K47/48092 ,  C07K14/70564 ,  G01N33/56972 ,  A61K2123/00

    摘要： Ligands in the form of N-acetyllactosamines which bind to endothelial leukocyte adhesion molecule-1 (ELAM-1) are disclosed. The ligand compounds can be formulated into pharmaceutical compositions and/or assay compositions used to alleviate inflammation and assay for the presence of (qualitative) and amount of (quantitative) ELAM-1 and thereby determine the presence, location and degree of inflammation. The ligands are encompassed by general structural formula I as follows: ##STR1## wherein one of A and B is hydrogen and one is an N-acetyl neuraminic acid residue; D and E are each independently hydrogen or a fucose residue; n is an integer of from 0 to 10 with the proviso that if n is 0, E is a fucose residue; F is hydrogen, a lactosylceramide residue or a linking group; and molecules equivalent to a compound of formula I regarding its ability to bind to an ELAM-1 receptor to the same degree as a compound of formula I.

    摘要翻译： 公开了结合内皮白细胞粘附分子-1（ELAM-1）的N-乙酰乳糖胺形式的配体。 配体化合物可以配制成药物组合物和/或用于缓解炎症和测定（定性）和量的（定量）ELAM-1的存在的药物组合物和/或测定组合物，从而确定炎症的存在，位置和程度。 配体由通式结构式I包括如下：其中A和B之一是氢，一个是N-乙酰神经氨酸残基; D和E各自独立地为氢或岩藻糖残基; n为0至10的整数，条件是如果n为0，则E为岩藻糖残基; F是氢，乳糖神经酰胺残基或连接基团; 以及与式I化合物相当于其与式I化合物相同程度结合ELAM-1受体的能力的分子。

    Method of treating inflammation by blocking ELAM-1 receptor sites
    4.
    发明授权
    Method of treating inflammation by blocking ELAM-1 receptor sites 失效
    通过阻断ELAM-1受体位点治疗炎症的方法

    公开(公告)号：US5428025A

    公开(公告)日：1995-06-27

    申请号：US844101

    申请日：1992-03-02

    申请人： Brian K. Brandley ,  Michael Tiemeyer ,  Stuart J. Swiedler ,  Margaret Moreland ,  Hans Schweingruber

    发明人： Brian K. Brandley ,  Michael Tiemeyer ,  Stuart J. Swiedler ,  Margaret Moreland ,  Hans Schweingruber

    IPC分类号： A61K31/70 ,  A61K51/08 ,  C07H13/04 ,  C07K14/705 ,  G01N33/569 ,  A01N43/04 ,  A61K31/73

    CPC分类号： C07H13/04 ,  A61K31/70 ,  A61K47/48092 ,  A61K51/08 ,  C07K14/70564 ,  G01N33/56972 ,  A61K2123/00

    摘要： Ligands in the form of N-acetyllactosamines which bind to endothelial leukocyte adhesion molecule-1 (ELAM-1) are disclosed. The ligand compounds can be formulated into pharmaceutical compositions and/or assay compositions used to alleviate inflammation and assay for the presence of (qualitative) and amount of (quantitative) ELAM-1 and thereby determine the presence, location and degree of inflammation. The ligands are encompassed by general structural formula I as follows: ##STR1## wherein one of F and G is hydrogen and one is an N-acetyl neuraminic acid residue on the terminal unit and are both hydrogen on any other unit; J is hydrogen, a lactosylceramide or a linking group and K is hydrogen or a fucose residue and n is an integer of from 1 to 10 (preferably 3 or 4) with the proviso that n and K are defined such that at least one K is a fucose residue.

    摘要翻译： 公开了结合内皮白细胞粘附分子-1（ELAM-1）的N-乙酰乳糖胺形式的配体。 配体化合物可以配制成药物组合物和/或用于缓解炎症和测定（定性）和量的（定量）ELAM-1的存在的药物组合物和/或测定组合物，从而确定炎症的存在，位置和程度。 配体由通式结构式I包括如下：其中F和G中的一个是氢，一个是末端单元上的N-乙酰神经氨酸残基，并且在任何其它单元上都是氢; J是氢，乳糖神经酰胺或连接基团，K是氢或岩藻糖残基，n是1至10（优选3或4）的整数，条件是n和K被定义为至少一个K是 岩藻糖残基。

    Method of determining a cite of inflammation utilizing elam-1 ligands site
    6.
    发明授权
    Method of determining a cite of inflammation utilizing elam-1 ligands site 失效
    确定使用ELAM-1配置站点的使用方法

    公开(公告)号：US5211936A

    公开(公告)日：1993-05-18

    申请号：US559836

    申请日：1990-07-30

    申请人： Brian K. Brandley ,  Michael Tiemeyer ,  Stuart J. Swiedler ,  Margaret Moreland ,  Hans Schweingruber

    发明人： Brian K. Brandley ,  Michael Tiemeyer ,  Stuart J. Swiedler ,  Margaret Moreland ,  Hans Schweingruber

    IPC分类号： A61K31/70 ,  A61K51/08 ,  C07H13/04 ,  C07K14/705 ,  G01N33/569

    CPC分类号： C07H13/04 ,  A61K31/70 ,  A61K47/48092 ,  A61K51/08 ,  C07K14/70564 ,  G01N33/56972 ,  A61K2123/00

    摘要： Ligands in the form of N-acetyllactosamines which bind to endothelial leukocyte adhesion molecule-1 (ELAM-1) are disclosed. The ligand compounds can be formulated into pharmaceutical compositions and/or assay compositions used to alleviate inflammation and assay for the presence of (qualitative) and amount of (quantitative) ELAM-1 and thereby determine the presence, location and degree of inflammation. The ligands are encompassed by general structural formula I as follows: ##STR1## wherein one of F and G is hydrogen and one is an N-acetyl neuraminic acid residue on the terminal unit and are both hydrogen on any other unit; J is hydrogen, a lactosylceramide or a linking group and K is hydrogen or a fucose residue and n is an integer of from 1 to 10 (preferably 3 or 4) with the proviso that n and K are defined such that at least one K is a fucose residue.

    摘要翻译： 公开了结合内皮白细胞粘附分子-1（ELAM-1）的N-乙酰乳糖胺形式的配体。 配体化合物可以配制成药物组合物和/或用于缓解炎症和测定（定性）和量的（定量）ELAM-1的存在的药物组合物和/或测定组合物，从而确定炎症的存在，位置和程度。 配体由通式结构式I包括如下：其中F和G中的一个是氢，一个是末端单元上的N-乙酰神经氨酸残基，并且在任何其它单元上都是氢; J是氢，乳糖神经酰胺或连接基团，K是氢或岩藻糖残基，n是1至10（优选3或4）的整数，条件是n和K被定义为至少一个K是 岩藻糖残基。

    Novel cross-linking agents
    8.
    发明授权
    Novel cross-linking agents 失效
    新型交联剂

    公开(公告)号：US5034514A

    公开(公告)日：1991-07-23

    申请号：US256723

    申请日：1988-10-12

    申请人： Danute E. Nitecki ,  Margaret Moreland

    发明人： Danute E. Nitecki ,  Margaret Moreland

    IPC分类号： C07D213/71 ,  G01N33/543

    CPC分类号： G01N33/54353 ,  C07D213/71

    摘要： Bifunctional chemicals useful for linking aldehyde containing moieties to moieties containing functionalities which are or can be reactive with sulfhydryl are claimed and have the formula:L--S--(CH.sub.2).sub.n1 --CONH--SPACER--NH--XwhereinL is a leaving group selected from --H or --S--Ar, wherein Ar represents optionally substituted phenyl or pyridyl;n.sub.1 =2-4;X is selected from: --CO--Y--CONHNH.sub.2, a hydrazide; ##STR1## a hydrazine; ##STR2## a hydrazine; --CO--Y--NH--CONHNH.sub.2, a semicarbazide; and --CO--Z--NH--CSNHNH.sub.2, a thiosemicarbazide;wherein Y is alkylene or oxaalkylene and Z is alkylene or a polypeptide residue briding the N-terminal amino group and C-terminal carboxy group thereof;the SPACER is oxaalkylene or oxaalkylene substituted with hydroxyl and specifically includes residues having formulas selected froma) --(CH.sub.2).sub.n2 --O--(CH.sub.2).sub.n2 --O--(CH.sub.2).sub.n2 -- wherein each n2 is independently 2-4 andb) ##STR3## wherein n3 is 2-6. Also claimed are hydrazides, semicarbazides, and thiosemicarbazides of .omega.-mercaptocarboxylic acids which lack SPACER diamine.

    摘要翻译： 要求具有下式的LS-（CH2）n1-CONH-SPACER-NH-X，其中L是选自以下的离去基团 - H或-S-Ar，其中Ar表示任选取代的苯基或吡啶基; n1 = 2-4; X选自：-CO-Y-CONHNH 2，酰肼; 肼; 肼; -CO-Y-NH-CONHNH 2，氨基脲; 和-CO-Z-NH-CSNHNH 2，硫代氨基脲; 其中Y是亚烷基或氧杂亚烷基并且Z是亚烷基，或多肽残基支持其N-末端氨基和C-末端羧基; SPACER是被羟基取代的氧杂亚烷基或氧杂亚烷基，具体包括具有选自a） - （CH 2）n 2 -O-（CH 2）n 2 -O-（CH 2）n 2-的式的残基，其中每个n2独立地为2-4，和b） 其中n3为2-6。 还要求的是缺乏SPACER二胺的ω-巯基羧酸的酰肼，氨基脲和氨基硫脲。

    Compound 1-(3-(2-pyridyldithio)propionamido)-12-(5-hydrazidoglutaramido)-4,9-diox adodecane
    10.
    发明授权
    Compound 1-(3-(2-pyridyldithio)propionamido)-12-(5-hydrazidoglutaramido)-4,9-diox adodecane 失效
    化合物1-（3-（2-吡啶基二硫代）丙酰胺基）-12-（5-酰氨基戊酰氨基）-4,9-二氧代十二烷

    公开(公告)号：US4797491A

    公开(公告)日：1989-01-10

    申请号：US840604

    申请日：1986-03-17

    申请人： Danute E. Nitecki ,  Margaret Moreland

    发明人： Danute E. Nitecki ,  Margaret Moreland

    IPC分类号： C08G69/48 ,  C07C67/00 ,  C07C313/00 ,  C07C323/60 ,  C07C323/62 ,  C07D213/71 ,  C07K1/113 ,  C07K14/415 ,  C07K16/00 ,  C07K17/06 ,  G01N33/543 ,  G01N33/547

    CPC分类号： C07D213/71 ,  G01N33/54353

    摘要： Bifunctional chemicals useful for linking aldehyde containing moieties to moieties containing functionalities which are or can be reactive with sulfhydryl are claimed and have the formula:L--S--(CH.sub.2).sub.n1 --CONH--SPACER--NH--Xwherein L is a leaving group selected from --H or --S--Ar, wherein Ar represents optionally substituted phenyl or pyridyl;n.sub.1 =2-4;X is selected from:--CO--Y--CONHNH.sub.2, a hydrazide; ##STR1## a hydrazine; ##STR2## a hydrazine; --CO--Y--NH--CONHNH.sub.2, a semicarbazide; and--CO--Z--NH--CSNHNH.sub.2, a thiosemicarbazide;wherein Y is alkylene or oxaalkylene and Z is alkylene or a polypeptide residue bridging the N-terminal amino group and C-terminal carboxy group thereof;the SPACER is oxaalkylene or oxaalkylene substituted with hydroxyl and specifically includes residues having formulas selected from--(CH.sub.2).sub.n2 --O--(CH.sub.2).sub.n2 --O--(CH.sub.2).sub.n2 --(a)wherein each n2 is independently 2-4 and ##STR3## wherein n3 is 2-6. Also claimed are hydrazides, semicarbazides, and thiosemicarbazides of .omega.-mercaptocarboxylic acids which lack SPACER diamine.

    摘要翻译： 要求具有下式的LS-（CH2）n1-CONH-SPACER-NH-X，其中L是选自以下的离去基团 - H或-S-Ar，其中Ar表示任选取代的苯基或吡啶基; n1 = 2-4; X选自：-CO-Y-CONHNH 2，酰肼; 肼; 肼; -CO-Y-NH-CONHNH 2，氨基脲; 和-CO-Z-NH-CSNHNH 2，硫代氨基脲; 其中Y是亚烷基或氧杂亚烷基，Z是亚烷基或桥接其N末端氨基和C末端羧基的多肽残基; SPACER是被羟基取代的氧杂亚烷基或氧杂亚烷基，具体包括具有选自 - （CH 2）n 2 -O-（CH 2）n 2 -O-（CH 2）n 2-（a）的式的残基，其中每个n2独立地为2-4， （b）其中n3为2-6。 还要求的是缺乏SPACER二胺的ω-巯基羧酸的酰肼，氨基脲和氨基硫脲。