利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

7 条记录 (耗时 0.012 秒)

    Butadiene derivatives and process for preparing thereof
    4.
    发明授权
    Butadiene derivatives and process for preparing thereof 失效
    丁二烯衍生物及其制备方法

    公开(公告)号：US06248743B1

    公开(公告)日：2001-06-19

    申请号：US09143358

    申请日：1998-08-28

    申请人： Hiroshi Ohmizu ,  Akio Ohtani ,  Tsuyoshi Ohgiku ,  Hiroshi Sai ,  Jun Murakami

    发明人： Hiroshi Ohmizu ,  Akio Ohtani ,  Tsuyoshi Ohgiku ,  Hiroshi Sai ,  Jun Murakami

    IPC分类号： A61K31495

    CPC分类号： C07D207/02 ,  C07C69/734 ,  C07C235/34 ,  C07C2601/08 ,  C07D211/58 ,  C07D213/40 ,  C07D213/55 ,  C07D213/56 ,  C07D213/75 ,  C07D213/89 ,  C07D231/12 ,  C07D231/38 ,  C07D231/40 ,  C07D233/56 ,  C07D239/42 ,  C07D249/08 ,  C07D261/14 ,  C07D317/60 ,  C07D401/06 ,  C07D405/12

    摘要： A novel butadiene derivative of the formula: wherein Ring A is heterocycle, or benzene being optionally substituted by lower alkyl, alkoxy, nitro, hydroxy, substituted or unsubstituted amino or halogen, Ring B is heterocycle, or benzene being optionally substituted by lower alkoxy, lower alkylenedioxy or di-lower alkylamino, R1 and R2 are each H or lower alkyl, one of —COR32 and —COR42 is carboxyl, and the other is carboxyl being optionally esterified, or the corresponding amide or pyrrolidine derivatives, or a pharmaceutically acceptable salt thereof. Said compounds show excellent PAI-1 inhibitory activity and are useful in the prophylaxis or treatment of various thromboses such as myocardial infarction, intra-atrial thrombus in atrial fibrillation, cerebral infarction, angina pectoris, stroke, pulmonary infarction, deep venous thrombus (DVT), disseminated intravascular coagulation syndrome (DIC), diabetic complications, restenosis after percutaneous transluminal coronary angioplasty (PTCA), etc.

    摘要翻译： 一种下式的新型丁二烯衍生物：其中环A是杂环，或任选被低级烷基，烷氧基，硝基，羟基，取代或未取代的氨基或卤素取代的苯，环B是杂环，或任选被低级烷氧基取代的苯， 低级亚烷基二氧基或二低级烷基氨基，R 1和R 2各自为H或低级烷基，-COR 32和-COR 42中的一个为羧基，另一个为任选被酯化的羧基，或相应的酰胺或吡咯烷衍生物或其药学上可接受的盐 其中。 所述化合物显示优异的PAI-1抑制活性，可用于预防或治疗心肌梗死，心房颤动，脑梗死，心绞痛，中风，肺梗死，深静脉血栓（DVT）等心血管栓塞， ，弥漫性血管内凝血综合征（DIC），糖尿病并发症，经皮腔内冠状动脉成形术（PTCA）后再狭窄等。

    Process for preparing acetoxyazetidinone derivative and intermediate thereof
    5.
    发明授权
    Process for preparing acetoxyazetidinone derivative and intermediate thereof 失效
    制备乙酰氧基氮杂环丁酮衍生物及其中间体的方法

    公开(公告)号：US5831091A

    公开(公告)日：1998-11-03

    申请号：US743834

    申请日：1996-11-05

    申请人： Hiroshi Ohmizu ,  Masahiko Seki

    发明人： Hiroshi Ohmizu ,  Masahiko Seki

    IPC分类号： C07D239/88 ,  C07C227/32 ,  C07C229/22 ,  C07D205/08 ,  C07D265/12 ,  C07D265/22 ,  C07D279/08 ,  C07D413/06 ,  C07F7/18 ,  C07D205/00

    CPC分类号： C07D413/06 ,  C07C227/32 ,  C07C229/22 ,  C07D205/08 ,  C07D265/12 ,  C07D265/22 ,  C07F7/1856 ,  C07F7/1892 ,  Y02P20/55

    摘要： An N-�2-(1-hydroxyethyl)-3-oxopropyl!amine compound of the formula �III!: ##STR1## wherein Ring B represents a benzene ring which may be substituted; W represents oxygen atom or sulfur atom; Y represents oxygen atom, sulfur atom or N R.sup.0, R.sup.0 represents hydrogen atom or a substituent; Z represents a substituted methylene group which contains at least one chiral center; R.sup.5 represents an aralkyloxycarbonyl group or an alkoxycarbonyl group; R.sup.6 represents hydrogen atom, an aralkyl group, an acyloxy group, a tri-substituted silyloxy group or an alkoxy group; or both of R.sup.5 and R.sup.6 bond at their termini and combine with the adjacent nitrogen atom to form phthalimido group, and a process thereof are disclosed. Said compound �III! is useful as a starting compound of .beta.-lactam antibacterial agents.

    摘要翻译： 式[III]的N- [2-（1-羟乙基）-3-氧代丙基]胺化合物：其中环B表示可被取代的苯环; W表示氧原子或硫原子; Y表示氧原子，硫原子或N R0，R0表示氢原子或取代基; Z表示含有至少一个手性中心的取代亚甲基; R5表示芳烷氧基羰基或烷氧基羰基; R6代表氢原子，芳烷基，酰氧基，三取代甲硅烷氧基或烷氧基; 或者R 5和R 6两者在其末端键合并与相邻的氮原子结合形成苯二甲酰亚氨基，并且公开了其方法。 所述化合物[III]可用作β-内酰胺抗菌剂的起始化合物。