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    • 1. 发明授权
    • Novel substituted polyamides and process for producing them
    • 新型取代聚酰胺及其制备方法
    • US3970597A
    • 1976-07-20
    • US476320
    • 1974-06-04
    • Mordechai SokolovskyAmihay FreemanLeon Goldstein
    • Mordechai SokolovskyAmihay FreemanLeon Goldstein
    • C08G69/48C08G69/50C08G18/00
    • C08G69/48
    • Novel substituted polyamides of the general formula ##EQU1## wherein A and B, which may be identical or different, are the hydrocarbon backbone groups of the formula --(CH.sub.2).sub.n --, where n is an integer, R.sub.2 and R.sub.3 are the residues of an aldehyde R.sub.2 --CHO or of an isocyanide R.sub.3 --N.tbd.C, where R.sub.2 and R.sub.3 are aliphatic, aromatic or heterocyclic residues of the respective aldehyde or isocyanide, or where R.sub.3 is a chromophoric moiety. R.sub.2 and R.sub.3 can be substituted, and amongst the possible substituents there may be R.sub.3 designating --(CH.sub.2).sub.n --NHCO--CHR.sub.2 --N(CO)(R.sub.4)--X, where R.sub.4 is the residue of a monocarboxylic or dicarboxylic acid and X is the lysyl residue of a protein, which may be biologically active, or the residue of a low-molecular weight compound containing a primary amine moiety. Preferred polyamides are various types of nylons. Amongst proteins chemically bound to the polyamide there may be mentioned enzymes, antibodies and peptide hormones. When R.sub.3 is a chromophoric moiety, the product is a chemically dyed polyamide. The invention relates also to a process for the production of such novel substituted polyamides.
    • 通式-CONH-A-CONH-B-CO-NA-CONH-B-CONH-A- | CH-R2 | CO-NH-R3的新型取代聚酰胺其中A和B可以相同或不同, 是式 - (CH 2)n - 的烃主链基团,其中n是整数,R 2和R 3是醛R 2 -CHO或异氰酸酯R 3 -N N BOND C的残基,其中R 2和R 3是脂族基, 相应醛或异氰化物的芳族或杂环残基,或其中R3是发色部分。 R2和R3可以被取代,并且在可能的取代基中可以有R3表示 - (CH 2)n -NHCO-CHR 2 -N(CO)(R 4)-X,其中R 4是一元羧酸或二羧酸的残基,X 是可能是生物活性的蛋白质的赖氨酰残基,或含有伯胺部分的低分子量化合物的残基。 优选的聚酰胺是各种类型的尼龙。 与聚酰胺化学结合的蛋白质中,可以提及酶,抗体和肽激素。 当R3是发色部分时,产物是化学染色的聚酰胺。 本发明还涉及生产这种新型取代的聚酰胺的方法。
    • 3. 发明授权
    • Dihaloisocyanide derivatives of polymers for coupling nucleophiles
    • 用于偶联亲核体的聚合物的二卤代吖啶衍生物
    • US4440903A
    • 1984-04-03
    • US921055
    • 1978-06-30
    • Leon GolsteinMordechai SokolovskyAmihay Freeman
    • Leon GolsteinMordechai SokolovskyAmihay Freeman
    • C08G12/40C08G63/685C08G63/91C08G85/00C12N11/08C07C143/00C07G7/00C12N11/06
    • C08G63/91C08G12/40C08G63/685C08G85/004C12N11/08Y10S525/921
    • The present invention relates to novel key intermediates for the production of biologically active compounds coupled to polymers, of the general formula P--NCX.sub.2, wherein X designates a halogen atom selected from chlorine and bromine, and wherein P designates the polymer backbone of a polymer of the polyamide, polyester and ureaformaldehyde type. The invention further relates to compounds obtained by the reaction of the above compound P--NCX.sub.2 with a bifunctional or polyfunctional nucleophile. Suitable nucleophiles are hydrazides of dicarboxylic acids and amongst these there may be mentioned polyacrylamides partially substituted with acylhydrazide groups; polyfunctional amines selected from alkylamines, aralkylamines, arylamines and macromolecular compounds containing amino groups. The key intermediate PNCX.sub.2 may be coupled directly to biologically active macromolecules and amongst the preferred compounds of this type there are the various biologically active proteins and enzymes. The coupling of the biologically active macromolecules may also be effected via hydrophilic polymer moieties first grafted onto the polymer P via said dihaloisocyanide groups.
    • 本发明涉及用于生产与通式为P-NCX2的聚合物偶联的生物活性化合物的新型关键中间体,其中X表示选自氯和溴的卤素原子,其中P表示聚合物的聚合物主链 聚酰胺,聚酯和脲甲醛型。 本发明还涉及通过上述化合物P-NCX2与双官能或多官能亲核试剂的反应获得的化合物。 合适的亲核试剂是二羧酸的酰肼,其中可以提及部分被酰基酰肼基团取代的聚丙烯酰胺; 选自烷基胺,芳烷基胺,芳基胺和含有氨基的高分子化合物的多官能胺。 关键的中间体PNCX2可以直接与生物活性大分子偶联,并且在这种类型的优选化合物中存在各种生物活性蛋白质和酶。 生物活性大分子的偶联也可以通过首先通过所述二卤代吖啶基接枝到聚合物P上的亲水性聚合物部分来实现。
    • 10. 发明授权
    • Controlled enzymatic removal and retrieval of cells
    • 控制细胞的酶促去除和回收
    • US07364565B2
    • 2008-04-29
    • US10768749
    • 2004-01-27
    • Amihay Freeman
    • Amihay Freeman
    • A61N1/30
    • A61M3/0258A61B10/0035A61B10/02A61B17/545A61B2017/00761A61B2017/00769A61B2017/00774A61B2017/22082A61B2017/3411A61K38/48A61K38/4886A61M1/0088A61M3/0241A61M3/0283A61M3/0287A61M27/00C12M45/09C12N5/0629C12N2509/00
    • Method and device, including a uniquely operative applicator, and pharmaceutical compositions, for the controlled, non-surgical removal and retrieval of cells from a variety of skin lesions and tissue surfaces are disclosed. A synergistic effect of proteolytic digestion of the intracellular matrix and “stripping” flow is achieved by treating a defined area with a controlled, continuous stream of proteolytic enzyme solution, causing gentle but effective tissue erosion. Isolated cells from the skin lesion and/or tissue surface may be collected from the protease solution stream for histological analysis and/or cell culture, affording a method of “enzymatic biopsy”. The protease solution may be supplemented with anesthetics, coagulants, anticoagulants and antibiotics to decrease the discomfort, erythema, bleeding, risk of infection and scarring traditionally associated with surgical treatment of skin lesions. Delivery of precise levels of catalytic activity is ensured by controlled activation of stable, inactivated enzyme stock solutions and powders shortly prior to application.
    • 公开了包括独特操作的施用器和药物组合物的方法和装置,用于从各种皮肤损伤和组织表面控制,非手术移除和取回细胞。 通过用受控的连续的蛋白水解酶溶液处理限定区域来实现细胞内基质的蛋白水解消化和“剥离”流的协同效应,引起温和但有效的组织侵蚀。 可以从蛋白酶溶液流中收集来自皮肤病变和/或组织表面的分离的细胞用于组织学分析和/或细胞培养,提供“酶活检”的方法。 蛋白酶溶液可以用麻醉剂,凝结剂,抗凝剂和抗生素补充,以减少传统上与皮肤损伤手术治疗相关的不适,红斑,出血,感染风险和瘢痕。 通过在施用前不久稳定的灭活酶储备溶液和粉末的控制活化来确保提供精确水平的催化活性。