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    Process for the preparation of macrocyclic metalloprotease inhibitors
    3.
    发明授权
    Process for the preparation of macrocyclic metalloprotease inhibitors 失效
    制备大环金属蛋白酶抑制剂的方法

    公开(公告)号：US06562963B2

    公开(公告)日：2003-05-13

    申请号：US09919564

    申请日：2001-07-31

    申请人： Roberta L. Dorow ,  Silvio Campagna ,  Pasquale N. Confalone ,  Fuqiang Jin ,  Zhe Wang

    发明人： Roberta L. Dorow ,  Silvio Campagna ,  Pasquale N. Confalone ,  Fuqiang Jin ,  Zhe Wang

    IPC分类号： C07C23101

    CPC分类号： C07C69/007 ,  C07C43/315 ,  C07C59/58 ,  C07C235/28 ,  C07D267/00 ,  C07D273/02

    摘要： The present invention is directed to a process for the preparation of a compound of formula (X-a) or a pharmaceutically acceptable salt form thereof, wherein: R1 is selected from the group consisting of: C1-5 alkyl substituted with 0-5 R1a, —(CH2)r—C3-10 cycloalkyl substituted with 0-5 R1a, and —(CH2)r-aryl substituted with 0-5 R1a. Compounds of Formula (X-a) are macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.

    摘要翻译： 本发明涉及制备式（Xa）化合物或其药学上可接受的盐形式的方法，其中：R 1选自：被0-5个R 1a取代的C 1-5烷基， - （O）R-C3-10环烷基取代有0-5个R 1a和 - （CH 2）r - 被0-5个R 1a取代的芳基。式（Ⅹa）化合物是含有抗琥珀酸残基的大环分子，其抑制金属蛋白酶如 聚集蛋白聚糖酶，以及肿瘤坏死因子（TNF）的产生。 抗琥珀酸盐由爱立信选择性的甲硅烷基乙烯酮缩醛的爱尔兰克莱森重排形成。

    Process for the preparation of macrocyclic metalloprotease inhibitors
    4.
    发明授权
    Process for the preparation of macrocyclic metalloprotease inhibitors 失效
    制备大环金属蛋白酶抑制剂的方法

    公开(公告)号：US06307044B1

    公开(公告)日：2001-10-23

    申请号：US09329674

    申请日：1999-06-10

    申请人： Roberta L. Dorow ,  Silvio Campagna ,  Pasquale N. Confalone ,  Fuqiang Jin ,  Zhe Wang

    发明人： Roberta L. Dorow ,  Silvio Campagna ,  Pasquale N. Confalone ,  Fuqiang Jin ,  Zhe Wang

    IPC分类号： C07D27302

    CPC分类号： C07C69/007 ,  C07C43/315 ,  C07C59/58 ,  C07C235/28 ,  C07D267/00 ,  C07D273/02

    摘要： The present invention is directed to a process for the preparation of a compound of formula (X-a): or a pharmaceutically acceptable salt form thereof, wherein: R1 is selected from the group consisting of: C1-5 alkyl substituted with 0-5 R1a, —(CH2)r—C3-10 cycloalkyl substituted with 0-5 R1a, and —(CH2)r-aryl substituted with 0-5 R1a. Compounds of Formula (X-a) are macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.

    摘要翻译： 本发明涉及制备式（Xa）化合物或其药学上可接受的盐形式的方法，其中：R 1选自：被0-5个R 1a取代的C 1-5烷基， - （CH 2）r -C 3-10环烷基，被0-5个R 1a取代，和 - （CH 2）r - 被0-5个R 1a取代的芳基。式（Xa）化合物是含有抗琥珀酸酯残基的大环分子，其抑制金属蛋白酶 作为聚集蛋白聚糖酶，以及肿瘤坏死因子（TNF）的产生。 抗琥珀酸盐由爱立信选择性的甲硅烷基乙烯酮缩醛的爱尔兰克莱森重排形成。

    Method for the synthesis of 2′,3′-dideoxy-2′,3′-didehydronucleosides
    7.
    发明授权
    Method for the synthesis of 2′,3′-dideoxy-2′,3′-didehydronucleosides 有权
    2'，3'-二脱氧-2'，3'-二脱氢核苷合成方法

    公开(公告)号：US06927291B2

    公开(公告)日：2005-08-09

    申请号：US10087112

    申请日：2002-03-01

    申请人： Fuqiang Jin ,  Pasquale N. Confalone

    发明人： Fuqiang Jin ,  Pasquale N. Confalone

    IPC分类号： C07H19/067 ,  A61K31/506 ,  A61P31/10 ,  A61P31/18 ,  C07D407/04 ,  C07D407/14 ,  C07H19/00 ,  C07H19/06 ,  C07H19/16 ,  C07D405/04

    CPC分类号： C07H19/06 ,  C07H19/16

    摘要： An efficient synthetic route to antiviral 2′,3′-dideoxy-2′,3′-didehydro-nucleosides, such as 2′,3′-dideoxy and 2′- or 3′-deoxyribo-nucleoside analogs, from available precursors is disclosed, with the option of introducing functionality as needed. In one embodiment, a method for the preparation of β-D and β-L-2′,3′-dideoxy-2′,3′-didehydro-nucleosides is described that includes: activating a compound of structure (1) wherein B is a pyrimidine or purine base and Y is O, S or CH2 with an acyl halide of the formula X—C(═O)R1, X—C(═O)C(R1)2OC(═O)R1 or X—C(═O)OR1 (wherein X is a halogen, and each R1 is independently hydrogen, lower alkyl, alkyl, aryl or phenyl); reducing the resulting compound with a reducing agent to form a 2′,3′-dideoxy-2′,3′-didehydro-nucleoside; and optionally deprotecting the nucleoside. The haloacylation of the first step can form the 2′-acyl-3′-halonucleoside, the 3′-acyl-2′-halonucleoside, or a mixture thereof.

    摘要翻译： 来自可用前体的抗病毒2'，3'-二脱氧-2'，3'-二脱氢核苷如2'，3'-二脱氧和2'-或3'-脱氧核苷类似物的有效合成途径是 披露，可以根据需要引入功能。 在一个实施方案中，描述了制备β-D和β-L-2'，3'-二脱氧-2'，3'-二脱氢核苷的方法，其包括：活化结构（1）的化合物，其中B 是嘧啶或嘌呤碱，Y为O，S或CH 2，与式XC（-O）R 1，XC（-O）C （R 1）2 OC（-O）R 1或XC（-O）OR 1（其中 X是卤素，并且每个R 1独立地是氢，低级烷基，烷基，芳基或苯基）。 用还原剂还原所得化合物以形成2'，3'-二脱氧-2'，3'-二脱氢核苷; 并任选地使核苷脱保护。 第一步的卤代酰化可以形成2'-酰基-3'-卤素核苷，3'-酰基-2'-脱氢核苷或其混合物。

    Cyclic carbamates and isoxazolidines as IIb/IIIa antagonists
    8.
    发明授权
    Cyclic carbamates and isoxazolidines as IIb/IIIa antagonists 有权
    环状氨基甲酸酯和异恶唑烷作为IIb / IIIa拮抗剂

    公开(公告)号：US06265400B1

    公开(公告)日：2001-07-24

    申请号：US09340950

    申请日：1999-06-28

    申请人： Fuqiang Jin ,  Pasquale Nicholas Confalone

    发明人： Fuqiang Jin ,  Pasquale Nicholas Confalone

    IPC分类号： C07D26102

    CPC分类号： C07D261/02 ,  C07D265/10 ,  C07D413/06 ,  C07D413/12

    摘要： The present invention relates generally to cyclic carbamates and isoxazolidines or Formula (I) or their pharmaceutically acceptable salts thereof, which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.

    摘要翻译： 本发明一般涉及可用作血小板糖蛋白IIb / IIIa纤维蛋白原受体复合物的拮抗剂的环状氨基甲酸酯和异恶唑烷或式（I）或其药学上可接受的盐，含有这些化合物的药物组合物，制备这些化合物的方法 以及使用这些化合物抑制血小板聚集作为血栓溶解剂和/或治疗血栓栓塞障碍的方法。

    Method for the synthesis of 2',3'-dideoxy-2',3'-didehydronucleosides
    9.
    发明申请
    Method for the synthesis of 2',3'-dideoxy-2',3'-didehydronucleosides 审中-公开
    2'，3'-二脱氧-2'，3'-二脱氢核苷合成方法

    公开(公告)号：US20050250946A1

    公开(公告)日：2005-11-10

    申请号：US11182862

    申请日：2005-07-18

    申请人： Pasquale Confalone ,  Fuqiang Jin

    发明人： Pasquale Confalone ,  Fuqiang Jin

    IPC分类号： C07H19/067 ,  A61K31/506 ,  A61P31/10 ,  A61P31/18 ,  C07D407/04 ,  C07D407/14 ,  C07H19/00 ,  C07H19/06 ,  C07H19/16 ,  A61K31/513 ,  C07D45/04

    CPC分类号： C07H19/06 ,  C07H19/16

    摘要： The present invention is an efficient synthetic route to 2′,3′-dideoxy-2′,3′-didehydro-nucleosides from available precursors with the option of introducing functionality as needed, such as, the 2′,3′-dideoxy and 2′- or 3′-deoxyribo-nucleoside analogs as well as additional derivatives obtained by subsequent functional group manipulations. Briefly, the present invention discloses a method for the preparation of β-D and β-L-2′,3′-dideoxy-2′,3′-didehydro-nucleosides starting from appropriately substituted ribonucleosides in two, optionally three steps: Step (1) a haloacylation, such as haloacetylation, and in particular, bromoacetylation; Step (2) a reductive elimination; and optionally, Step (3) a deprotection. The haloacylation of step (1) can form the 2′-acyl-3′-halonucleoside, the 3′-acyl-2′-halonucleoside, or a mixture thereof.

    摘要翻译： 本发明是从可用前体的2'，3'-二脱氧-2'，3'-二脱氢核苷的有效合成途径，可根据需要引入官能团，例如2'，3'-二脱氧和 2'-或3'-脱氧核苷类似物以及通过随后的官能团操作获得的另外的衍生物。 简言之，本发明公开了一种从适当取代的核糖核苷酸开始制备β-D和β-L-2'，3'-二脱氧-2'，3'-二脱氢核苷的方法，可任选地分三步：步骤 （1）卤代酰化，例如卤代乙酰化，特别是溴乙酰化; 步骤（2）还原消除; 和任选的步骤（3）脱保护。 步骤（1）的卤代酰化可以形成2'-酰基-3'-卤代核苷，3'-酰基-2'-卤代核苷或其混合物。

    Cyclic carbamates and isoxazolidines as IIb/IIIa antagonists
    10.
    发明授权
    Cyclic carbamates and isoxazolidines as IIb/IIIa antagonists 失效
    环状氨基甲酸酯和异恶唑烷作为IIb / IIIa拮抗剂

    公开(公告)号：US6004955A

    公开(公告)日：1999-12-21

    申请号：US133146

    申请日：1998-08-12

    申请人： Fuqiang Jin ,  Pasquale Nicholas Confalone

    发明人： Fuqiang Jin ,  Pasquale Nicholas Confalone

    IPC分类号： C07D261/02 ,  C07D265/10 ,  C07D413/12 ,  A61K31/535 ,  A61K31/42

    CPC分类号： C07D261/02 ,  C07D265/10 ,  C07D413/12

    摘要： ##STR1## This invention relates generally to cyclic carbamates and hydroxylamines which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.

    摘要翻译： 本发明一般涉及可用作血小板糖蛋白IIb / IIIa纤维蛋白原受体复合物的拮抗剂的环状氨基甲酸酯和羟胺，含有这些化合物的药物组合物，制备这些化合物的方法，以及使用这些化合物抑制血小板的方法 聚集，作为溶血栓剂，和/或用于治疗血栓栓塞性疾病。