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21. 发明申请

WO1996019483A1 LOW MOLECULAR WEIGHT BICYCLIC THROMBIN INHIBITORS 审中-公开
标题翻译：低分子量双分子抑制剂
公开(公告)号：WO1996019483A1
公开(公告)日：1996-06-27
申请号：PCT/CA1995000708
申请日：1995-12-21
申请人： BIOCHEM PHARMA INC. , DIMAIO, John , SIDDIQUI, M., Arshad , GILLARD, John, W. , ST-DENIS, Yves , TARAZI, Micheline , PREVILLE, Patrice , LEVESQUE, Sophie , BACHAND, Benoit
发明人： BIOCHEM PHARMA INC.
IPC分类号： C07D513/04
CPC分类号： C07D487/04 , A61K38/00 , C07D513/04 , C07K5/0202 , C07K5/06078 , C07K5/06139 , C07K5/0812 , C07K5/0821
摘要： This invention relates to the discovery of heterocyclic competitive inhibitors of the enzyme thrombin having formula (I), their preparation, and pharmaceutical compositions thereof. As well, this invention relates to the use of such compounds and compositions in vitro as anticoagulants and in vivo as agents for the treatment and prophylaxis of thrombotic disorders such as venous thrombosis, pulmonary embolism and arterial thrombosis resulting in acute ischemic events such as myocardial infarction or cerebral infarction. Moreover, these compounds and compositions have therapeutic utility for the prevention and treatment of coagulopathies associated with coronary bypass operations as well as restenotic events following transluminal angioplasty.
摘要翻译：本发明涉及具有式（I）的酶凝血酶的杂环竞争性抑制剂的发现，其制备及其药物组合物。此外，本发明还涉及这些化合物和组合物在体外作为抗凝剂和体内作为治疗和预防血栓形成疾病例如静脉血栓形成，肺栓塞和动脉血栓形成作为导致急性缺血事件如心肌梗死的药物的用途或脑梗塞。此外，这些化合物和组合物具有治疗用途，用于预防和治疗与冠状动脉旁路手术相关的凝血病以及经腔血管成形术后的再狭窄事件。

22. 发明申请

WO1994014802A1 PROCESS FOR PREPARING SUBSTITUTED 1,3-OXATHIOLANES WITH ANTIVIRAL PROPERTIES 审中-公开
标题翻译：制备具有抗病性的取代的1,3-氧化物的方法
公开(公告)号：WO1994014802A1
公开(公告)日：1994-07-07
申请号：PCT/CA1992000557
申请日：1992-12-21
申请人： BELLEAU, Pierrette +hf , BIOCHEM PHARMA INC. , MANSOUR, Tarek , TSE, Allan , EVANS, Colleen, A. , JIN, Haolun , ZACHARIE, Boulus , NGUYEN-BA, Nghe
发明人： BELLEAU, Pierrette +hf , BIOCHEM PHARMA INC. , BELLEAU, Bernard +di
IPC分类号： C07D411/04
CPC分类号： C07D327/04 , C07D405/04 , C07D411/04 , C07D411/14 , C07D473/00 , C07D473/40
摘要： Disclosed are processes for preparing compounds of formula (I) and pharmaceutically acceptable salts or esters thereof, wherein R2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S = O or SO2. The invention also relates to intermediates of use in the preparation of these compounds.
摘要翻译：公开了制备式（I）化合物及其药学上可接受的盐或酯的方法，其中R2是嘌呤或嘧啶碱基或其类似物或衍生物; Z为S，S = O或SO 2。本发明还涉及用于制备这些化合物的中间体。

23. 发明申请

WO1994011382A1 ANTINEOPLASTIC HETERONAPHTHOQUINONES 审中-公开
标题翻译： ANTINEOPLOSTIC HETERONAPHTHOQUINONES
公开(公告)号：WO1994011382A1
公开(公告)日：1994-05-26
申请号：PCT/CA1993000463
申请日：1993-11-05
申请人： BIOCHEM PHARMA INC. , ATTARDO, Giorgio , BREINING, Tibor , COURCHESNE, Marc , KRAUS, Jean-Louis , LAMOTHE, Serge , LAVALLEE, Jean-François , LEBEAU, Elaine , NGUYEN, Dieu , REJ, Rabindra , ST-DENIS, Yves , WANG, Wuyi , XU, Yao-Chang , BARBEAU, France
发明人： BIOCHEM PHARMA INC.
IPC分类号： C07H17/00
CPC分类号： C07H15/252 , C07D311/76 , C07D311/92 , C07D335/08 , C07H17/00 , C07H17/04
摘要： Tricyclic heteronaphthoquinone derivatives, that have antineoplastic activity, are disclosed, together with processes for their synthesis. Some of these anti-neoplastics compounds have a saccharide moiety. Some members of this structurally distinct group exhibit activity against multiple drug resistant cancer cells.
摘要翻译：公开了具有抗肿瘤活性的三环杂萘醌衍生物及其合成方法。这些抗肿瘤化合物中的一些具有糖部分。该结构不同组的一些成员表现出抗多种耐药性癌细胞的活性。

24. 发明申请

WO1994005300A1 USE OF RAPAMYCIN IN THE TREATMENT OF AIDS 审中-公开
标题翻译： RAPAMYCIN在治疗艾滋病方面的应用
公开(公告)号：WO1994005300A1
公开(公告)日：1994-03-17
申请号：PCT/CA1993000384
申请日：1993-09-02
申请人： BIOCHEM PHARMA INC. , VEZINA, Claude
发明人： BIOCHEM PHARMA INC.
IPC分类号： A61K31/71
CPC分类号： A61K31/70
摘要： The present invention relates to the use of rapamycin or an analog of rapamycin in the manufacture of a medicament for treating, arresting the development or retarding the progression of an HIV infection in an amount sufficient to achieve a reduction in the level of serum p24 antigen; and to the use of rapamycin or analog of rapamycin for treating, arresting the development or retarding the progression of AIDS in a mammal. The invention also relates to a method for treating, arresting the development or retarding the progression of AIDS in a mammal in need thereof by administering to the mammal an amount of rapamycin or analog of rapamycin sufficient to achieve a reduction in the level of serum p24 antigen.
摘要翻译：本发明涉及雷帕霉素或雷帕霉素类似物在制备用于以足以实现血清p24抗原水平降低的量治疗，阻止HIV感染发展或延缓进展的药物中的用途; 以及雷帕霉素或雷帕霉素类似物用于治疗，阻止发展或延缓哺乳动物中AIDS进展的用途。本发明还涉及通过向哺乳动物施用足以实现血清p24抗原水平降低的雷帕霉素或雷帕霉素类似物来治疗，阻止发展或延缓有需要的哺乳动物发展或延缓艾滋病进展的方法。

25. 发明申请

WO1992017493A2 PEPTIDES AND MIXTURES THEREOF FOR DETECTING ANTIBODIES TO HEPATITIS C VIRUS (HCV) 审中-公开
标题翻译：检测丙型肝炎病毒（HCV）的抗体的肽和混合物
公开(公告)号：WO1992017493A2
公开(公告)日：1992-10-15
申请号：PCT/CA1992000137
申请日：1992-04-03
申请人： BIOCHEM PHARMA INC.
发明人： BIOCHEM PHARMA INC. , LACROIX, Martial
IPC分类号： C07K07/10
CPC分类号： C07K14/005 , A61K39/00 , C07K16/109 , C12N2770/24222
摘要： This invention relates to novel peptides from the hepatitis C virus polyprotein amino acid regions 1-81, 101-127 and 210-231 and mixtures thereof useful for detecting HCV infections. These peptides are also useful as active ingredients in vaccines against HCV infection.

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