Bioassay for thrombogenesis and rabbit model
    4.
    发明授权
    Bioassay for thrombogenesis and rabbit model 失效
    血栓形成和兔模型的生物测定

    公开(公告)号:US5675058A

    公开(公告)日:1997-10-07

    申请号:US116845

    申请日:1993-09-07

    CPC分类号: A61K49/0008 G01N33/4905

    摘要: An in vivo assay for determining the potential thrombogenic activity of a test compound entails pre-treating an animal with both a hepatoxin and either a bacterial agent (whole bacteria or bacterial toxins, including endotoxins) or a bacterial agent-induced cytokine, which pre-treatment enhances sensitivity to thrombogenic substances. The sensitized animal can be used in identifying a thrombogenic substance even when it is a weak potentiator of thrombogenesis, and in detecting smaller amounts of a strong potentiator.

    摘要翻译: 用于确定测试化合物的潜在血栓形成活性的体内测定需要用肝毒素和细菌剂(全细菌或细菌毒素,包括内毒素)或细菌剂诱导的细胞因子来预处理动物, 治疗增强对血栓形成物质的敏感性。 致敏动物即使是血栓形成的弱增强剂也可用于鉴定血栓形成物质,并且用于检测较小量的强增效剂。

    Prevention and treatment of ischemic events and reperfusion injury
resulting therefrom using lys-plasminogen
    6.
    发明授权
    Prevention and treatment of ischemic events and reperfusion injury resulting therefrom using lys-plasminogen 失效
    使用lys-plasminogen预防和治疗由此导致的缺血事件和再灌注损伤

    公开(公告)号:US5520912A

    公开(公告)日:1996-05-28

    申请号:US257626

    申请日:1994-06-08

    CPC分类号: A61K38/484 Y10S514/802

    摘要: A treatment of ischemia and the attendant reperfusion injury entails the administration plasmin and plasmin-forming proteins, including lys-plasminogen and similar substances. Lys-plasminogen, which can be obtained from the proteolytic cleavage of glu-plasminogen, has been found to have a protective effect on tissue that has been injured by ischemic conditions. The administration of lys-plasminogen can used to treat subjects during the time of reperfusion and after reperfusion has already occurred. Lys-plasminogen also can be administered in conjunction with clot lysis therapies, such as those that employ tissue plasminogen activator and the like.

    摘要翻译: 缺血和伴随的再灌注损伤的治疗需要施用纤溶酶和纤溶酶形成蛋白,包括溶酶原纤溶酶原和类似物质。 已经发现,可以从葡萄糖分解纤维蛋白溶酶原的蛋白水解切割中获得的Lys-plasminogen对缺血条件损伤的组织具有保护作用。 溶血纤溶酶原的施用可以在再灌注期间和再灌注已经发生后用于治疗受试者。 Lys-纤溶酶原也可以与凝块溶解疗法结合使用,例如使用组织纤溶酶原激活剂等的那些。

    Tetrahydro-benzthiazoles, the preparation thereof and their use as
intermediate products or as pharmaceuticals
    7.
    发明授权
    Tetrahydro-benzthiazoles, the preparation thereof and their use as intermediate products or as pharmaceuticals 失效
    四氢 - 苯并噻唑,其制备方法及其作为中间产物或药物的用途

    公开(公告)号:US4843086A

    公开(公告)日:1989-06-27

    申请号:US124197

    申请日:1987-11-23

    IPC分类号: A61K31/425 C07D277/82

    CPC分类号: C07D277/82

    摘要: This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nuclei may each be substituted by 1 or 2 halogen atoms.R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by fluorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.3 represent an acyl group are valuable intermediate products for preparing the other compounds of general formula I which have valuable pharmacological properties. The new compounds may be prepared using methods known per se.

    摘要翻译: 本发明涉及通式为(I)的新的四氢苯并噻唑,其中R 1表示氢原子,烷基,烯基或炔基,烷酰基,苯基烷基或苯基烷酰基,而上述苯基核 可各自被1或2个卤素原子取代。 R2表示氢原子或烷基,R3表示氢原子,烷基,环烷基,烯基或炔基,烷酰基,苯基烷基或苯基烷酰基,而苯基核可以被氟取代 ,氯或溴原子,R4表示氢原子,烷基,烷基或烯基或R3和R4以及它们之间的氮原子表示吡咯烷子基,哌啶子基,六亚甲基亚氨基或吗啉代基,对映体和酸加成 的盐。 上述通式I的化合物,其中R1或R3基团或R1和R3两个基团之一表示酰基,是制备其它具有有价值的药理学性质的通式I化合物的有价值的中间产物。 新化合物可以使用本身已知的方法制备。

    2-Phenylimino-imidazolidines and salts thereof
    10.
    发明授权
    2-Phenylimino-imidazolidines and salts thereof 失效
    2-苯基亚氨基 - 咪唑烷及其盐

    公开(公告)号:US4213995A

    公开(公告)日:1980-07-22

    申请号:US11074

    申请日:1979-02-12

    CPC分类号: C07D233/50

    摘要: Compounds of the formula ##STR1## wherein R is 2,6-dichloro-4-hydroxymethyl-phenyl; 2-chloro-4-methyl-5-amino-phenyl; 2,5-dichloro-4-methyl-phenyl; 2-chloro-4-methyl-5-nitro-phenyl; 2,3-dichloro-4-methyl-phenyl; 2-chloro-4-methyl-6-nitro-phenyl; 2-chloro-4-methyl-6-amino-phenyl; 2,4,6-trifluorophenyl; tetrafluoro-phenyl; or 3-bromo-4-fluoro-phenyl; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as hypotensives.

    摘要翻译: 其中R为2,6-二氯-4-羟甲基 - 苯基的式IMA化合物; 2-氯-4-甲基-5-氨基 - 苯基; 2,5-二氯-4-甲基 - 苯基; 2-氯-4-甲基-5-硝基 - 苯基; 2,3-二氯-4-甲基 - 苯基; 2-氯-4-甲基-6-硝基 - 苯基; 2-氯-4-甲基-6-氨基 - 苯基; 2,4,6-三氟苯基; 四氟苯基; 或3-溴-4-氟 - 苯基; 和无毒的,药学上可接受的酸加成盐。 化合物及其盐可用作低渗剂。