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    • 3. 发明授权
    • Cyclic hydroxamic acids
    • 循环羟基酸
    • US5234933A
    • 1993-08-10
    • US785927
    • 1991-10-31
    • Lawrence J. MarnettKenneth V. HonnCarl R. JohnsonYung-fa ChenKatsu-ichi Shimoji
    • Lawrence J. MarnettKenneth V. HonnCarl R. JohnsonYung-fa ChenKatsu-ichi Shimoji
    • C07D211/94
    • C07D211/94
    • Novel cyclic hydroxamic acids of the general formula: ##STR1## wherein ring A is 5- or 6-membered; R.sup.1, R.sup.2 and R.sup.3 each, ipendently, is hydrogen, C1-24 alkyl, C2-24 alkenyl or a group of the formula: ##STR2## wherein R.sup.4, R.sup.5, R.sup.7 and R.sup.8 each, independently is hydrogen,C1-4 alkyl, C1-4 alkoxy, trifluoromethyl, halogen or nitro; l is 1-3; m is 1-3; n is 1-3; k is 1-3;R.sup.6 and R.sup.9 each, independently is C1-24 alkylene or C2-24 alkenylene;With the proviso that, more than one of R.sup.1, R.sup.2 and R.sup.3 are not hydrogen at the same time; and the pharmaceutically acceptable salts thereof possesses an inhibitory activity against 12-lipoxygenase, and therefore, may be useful for treating and/or preventing inflammation, immune diseases, psoriasis, arteriosclerosis and/or ischaemic cardiovascular diseases and also for suppressing metastasis of cancer.
    • 新型环状异羟肟酸,其通式为:其中环A为5-或6-元; R1,R2和R3各自独立地是氢,C1-24烷基,C2-24链烯基或下式的基团:其中R4,R5,R7和R8各自独立地是氢,C1- 4烷基,C 1-4烷氧基,三氟甲基,卤素或硝基; l为1-3; m为1-3; n为1-3; k为1-3; R6和R9各自独立地为C1-24亚烷基或C2-24亚烯基; 条件是,R1,R2和R3中的一个以上不是同时为氢; 其药学上可接受的盐具有对12-脂肪氧合酶的抑制活性,因此可用于治疗和/或预防炎症,免疫疾病,牛皮癣,动脉硬化和/或缺血性心血管疾病,也可用于抑制癌转移。
    • 9. 发明授权
    • Method for measuring blood procoagulant activity of human leukocyte
antigens
    • 测定人白细胞抗原血液促凝血活性的方法
    • US5529934A
    • 1996-06-25
    • US737441
    • 1991-07-29
    • Mohanathasan ChelladuraiKenneth V. HonnDaniel A. Walz
    • Mohanathasan ChelladuraiKenneth V. HonnDaniel A. Walz
    • A61K38/16A61K39/00A61M1/36C12Q1/00A01N37/18A61K39/085C07K1/00
    • A61M1/3672A61K38/164A61K39/001A61K39/0011
    • Thromboembolic complications have been documented in cancer patients and mismatched organ transplant recipients. Procoagulants have been implicated in these processes and may play an additional role in tumor metastases. Two proteins displaying procoagulant activity, with molecular weights of 35,000 and 28,000 daltons, were isolated from human ovarian carcinoma extracts. The amino terminal sequence of the first 12 amino acids of the 35,000 dalton protein was determined to be IKEEHVIIQAEF. This sequence displays 100% homology to the major histocompatibility (MHC) antigen HLA-DR which exists as an heterodimer composed of a 35 kDa and 28 kDa protein. The procoagulant activity was further purified through immunoaffinity column chromatography involving a monoclonal antibody to HLA-DR. The immunoaffinity purified protein enhanced thrombin generation in recalcified normal plasma approximately 20-fold. HLA-DR procoagulant activity was completely abrogated by the addition of Staphylcoccal aureus enterotoxin A (SEA).
    • 血栓栓塞并发症已经在癌症患者和错配的器官移植受者中得到记录。 促凝剂已经涉及这些过程,并且可能在肿瘤转移中起另外的作用。 从人卵巢癌提取物中分离出两种显示促凝活性的蛋白质,分子量为35,000和28,000道尔顿。 35,000道尔顿蛋白的前12个氨基酸的氨基末端序列被确定为IKEEHVIIQAEF。 该序列与作为由35kDa和28kDa蛋白质组成的异二聚体存在的主要组织相容性(MHC)抗原HLA-DR显示100%同源性。 通过涉及HLA-DR的单克隆抗体的免疫亲和柱色谱进一步纯化促凝血活性。 免疫亲和纯化蛋白增强了重新钙化正常血浆中凝血酶的产生约20倍。 通过添加金黄色葡萄球菌肠毒素A(SEA),HLA-DR促凝血活性被完全消除。