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    Production of 2',3'-dideoxy-2',3'-Didehydronucleosides
    2.
    发明公开
    Production of 2',3'-dideoxy-2',3'-Didehydronucleosides 失效
    Herstellung von 2'，3'-二脱氧-2'，3'-二脱氢核糖苷。

    公开(公告)号：EP0334368A2

    公开(公告)日：1989-09-27

    申请号：EP89105269.8

    申请日：1989-03-23

    申请人： Bristol-Myers Squibb Company

    发明人： Starrett, John E., Jr. ,  Mansuri, Muzammil M. ,  Martin, John C. ,  Fuller, Carl E. ,  Howell, Henry G.

    IPC分类号： C07D405/04 ,  A61K31/505

    CPC分类号： C07D405/04 ,  C07H19/04

    摘要： There are disclosed novel processes for producing 2′,3′-dideoxy-2′3′-didehydronucleosides, for example, 2′,3′- dideoxy-2′,3′-didehydrothymidine in high yields and on a large scale. The compounds so-produced are useful as antiviral agents, especially as agents effective against the human immunodeficiency viruses (HIV).

    摘要翻译： 公开了以高产率和大规模生产2分钟，3分钟 - 脱氧-2分钟3分钟 - 二氢核苷的新方法，例如2分钟，3分钟 - 脱氧-2分钟，3分钟 - 二氢胸苷。 如此制备的化合物可用作抗病毒剂，特别是作为有效抵抗人类免疫缺陷病毒（HIV）的药剂。

    Cephalosporin derivatives
    3.
    发明公开
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    公开(公告)号：EP0727426A2

    公开(公告)日：1996-08-21

    申请号：EP96400295.0

    申请日：1996-02-13

    申请人： BRISTOL-MYERS SQUIBB COMPANY

    发明人： Kim, Choung U. ,  Misco, Peter F. ,  Wichtowski, John A. ,  Ueda, Yasutsugu ,  Hudyma, Thomas W. ,  Matiskella, John D. ,  D'Andrea, Stanley W. ,  Hoeft, Shelley E. ,  Miller, Raymond F. ,  Mansuri, Muzammil M. ,  Bronson, Joanne J.

    IPC分类号： C07D501/36 ,  A61K31/545

    CPC分类号： C07D501/00

    摘要： Novel cephem derivatives represented by the general formula

    in which the Acyl substituent is a group of the formula

    wherein Ar is a lipophilic optionally substituted phenyl, naphthyl, pyridyl or benzthiazolyl group; R 1 is selected from certain optionally substituted aliphatic, aromatic, arylaliphatic or sugar moieties and R 2 and R 3 are each independently hydrogen, alkyl or aminoalkylcarbonylamino are gram-positive antibacterial agents, especially useful in the treatment of infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA).

    摘要翻译： 由通式表示的新型头孢烯衍生物，其中酰基取代基是下式的基团其中Ar是亲脂性的任选取代的苯基，萘基，吡啶基或苯并噻唑基; R1选自某些任选取代的脂族，芳族，芳基脂族或糖部分，R2和R3各自独立地为氢，烷基或氨基烷基羰基氨基为革兰氏阳性抗菌剂，特别用于治疗由耐甲氧西林金黄色葡萄球菌引起的感染性疾病 MRSA）。

    3'-Substituted methyl nucleosides as antiviral agents
    10.
    发明公开
    3'-Substituted methyl nucleosides as antiviral agents 失效
    3'-取代的甲基核苷作为抗病毒剂

    公开(公告)号：EP0391411A3

    公开(公告)日：1991-04-10

    申请号：EP90106510.2

    申请日：1990-04-05

    申请人： Bristol-Myers Squibb Company

    发明人： Sterzycki, Roman Z. ,  Mansuri, Muzammil M. ,  Martin, John C.

    IPC分类号： C07H19/073 ,  C07H19/173 ,  A61K31/70

    CPC分类号： C07H19/06 ,  C07H19/16 ,  Y02P20/55

    摘要： Certain 3′-substituted methyl nucleosides are disclosed which are useful in the treatment of viral infections, e.g., infections caused by herpes simplex virus types 1 and 2, and/or are useful as intermediates in the preparation of 3′-substituted methyl nucleosides having antiviral activity. In accordance with one aspect of the invention, there are provided novel 3′-substituted methyl nucleosides represented by Formulas I and II
    wherein:
    B indicates that B can be either alpha or beta;
    B is a member selected from the group consisting of the pyrimidine and purine nucleoside bases connected to the tetrahydrofuran ring through the N¹ heterocyclic nitrogen atom of the pyrimidines and the N⁹ or N⁷ heterocyclic nitrogen atom of the purines including the naturally occurring nucleoside bases and 5-fluoro, 5-bromo, 5-iodo, 5-chloro, 5-trifluoromethyl, 5-ethyl, 5-(2-bromovinyl)­uracil; triazolecarboxamide; 2-aminopurine;
    2,6-diaminopurine; 4-chloropyrimidine; pyrimidine; azapyrimidine; purine; 2,6-dichloropurine; 2-amino-6-­chloropurine; and deazapurine;
    R and Q are either both hydrogen or halogen, especially fluorine, or one is hydrogen and the other one is hydroxy or halogen, especially fluorine; in Formula I at least one of R and Q is halogen; and
    X and Y can be the same or different and are selected from the group consisting of O-alkyl, O-aryl, O-acyl-, halogen, especially fluorine, azido, amino, acylamido, -SH, S-alkyl and S-aryl, or one of X or Y can be hydroxy, or X may be the group R¹O and Y may be the group R²O wherein R¹ and R² are hydrogen or hydroxy-protecting groups. Preferred O-alkyl and S-alkyl groups contain from one to four carbon atoms; preferred O-aryl and S-aryl groups contain from 6 to 10 carbon atoms; and preferred O-acyl groups contain from one to four carbon atoms.