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15 条记录 (耗时 0.017 秒)

    Process for preparing piperazinepentaneamide HIV protease inhibitors
    6.
    发明授权
    Process for preparing piperazinepentaneamide HIV protease inhibitors 失效

    公开(公告)号：US06649761B2

    公开(公告)日：2003-11-18

    申请号：US10158527

    申请日：2002-05-30

    申请人： Norihiro Ikemoto ,  Jinchu Liu

    发明人： Norihiro Ikemoto ,  Jinchu Liu

    IPC分类号： C07D41306

    CPC分类号： C07D413/14

    摘要： A process for preparing &ggr;-hydroxy-4-[[2-oxazolyl]alkyl]-&agr;-[(cyclo)alkyl- or aryl- or heteroaryl-substituted methyl]-2-[[(un)substituted alkyl]aminocarbonyl]-1-piperazinepentanamides is disclosed. The piperazinepentanamides are useful as HIV protease inhibitors. A process for making a 4-[[2-oxazolyl]alkyl]-2-[[(un)substituted alkyl]aminocarbonyl]piperazine by treating a ketoamide precursor with fuming sulfuric acid in the presence of polyphosphoric acid is also disclosed. In addition, a process for enhancing the optical purity of 4-[[2-oxazolyl]alkyl]-2-[[(un)substituted alkyl]aminocarbonyl]-piperazines via the formation 2-naphthalenesulfonic acid crystal salts thereof is disclosed, as well as a method for purifying 2-naphthalenesulfonic acid.

    Thiazolidinone compounds useful as chemokine inhibitors
    7.
    发明授权
    Thiazolidinone compounds useful as chemokine inhibitors 有权
    可用作趋化因子抑制剂的噻唑烷酮化合物

    公开(公告)号：US06506751B1

    公开(公告)日：2003-01-14

    申请号：US09705219

    申请日：2000-11-02

    申请人： Stephanie Elizabeth Ault Justus ,  Helen Tsenwhei Lee ,  Jason Keith Pontrello ,  Bruce David Roth ,  Karen Elaine Sexton ,  Michael William Wilson

    发明人： Stephanie Elizabeth Ault Justus ,  Helen Tsenwhei Lee ,  Jason Keith Pontrello ,  Bruce David Roth ,  Karen Elaine Sexton ,  Michael William Wilson

    IPC分类号： C07D41306

    CPC分类号： C07D417/04 ,  C07D277/34 ,  C07D417/06

    摘要： Disclosed are compounds of the Formula I wherein: Z is C or nothing, provided that when Z is nothing, R3 and R4 are nothing; A is S, S═O or O═S═O; R1 and R2 are independently hydrogen, lower alkyl, halogen, hydroxy or lower alkoxy, (un)substituted aryl, (un)substituted arylalkyl, (un)substituted heteroaryl or(un)substituted heteroarylakyl; R3 and R4 independently represent hydrogen, lower alkyl, cycloalkyl, aminoalkyl, mono- or dialkylaminoalkyl, (un)substituted aryl or (un)substituted heteroaryl; R5 represents a (un)substituted carbocyclic group containing from 3-7 members, up to two of which members are optionally hetero atoms; or R5 is (CR6R7)—(CH2)n—XR8R9; X is S or N; R6, R7, R8, R9, and n are as defined in the specification. The compounds are useful in the treatment and prevention of the AIDS virus. Intermediates useful in the preparation of the final products, pharmaceutical compositions containing the final products are also taught.

    摘要翻译： 公开了式I的化合物，其中Z为C或无，条件是当Z不为任何时，R 3和R 4不为任何; A为S，S = O或O = S = O; R 1和R 2独立地为氢，低级烷基 ，卤素，羟基或低级烷氧基，（未）取代的芳基，（未）取代的芳基烷基，（未）取代的杂芳基或（未）取代的杂芳基; R3和R4独立地表示氢，低级烷基，环烷基，氨基烷基， ，（un）取代的芳基或（未）取代的杂芳基; R 5表示含有3-7个成员的（未）取代的碳环基，其中至多两个为任意的杂原子; 或R 5是（CR 6 R 7） - （CH 2）n -XR 8 R 9; X是S或N; R 6，R 7，R 8，R 9和n如说明书中所定义。该化合物可用于治疗和预防艾滋病毒。 还教导了用于制备最终产品的中间体，含有最终产品的药物组合物。

    Compounds for inhibition of ceramide-mediated signal transduction
    8.
    发明授权
    Compounds for inhibition of ceramide-mediated signal transduction 失效
    用于抑制神经酰胺介导的信号转导的化合物

    公开(公告)号：US06323201B1

    公开(公告)日：2001-11-27

    申请号：US08858778

    申请日：1997-05-19

    申请人： Dennis A. Carson ,  Howard Cottam

    发明人： Dennis A. Carson ,  Howard Cottam

    IPC分类号： C07D41306

    CPC分类号： C07D239/545 ,  C07D213/76 ,  C07D217/24 ,  C07D239/96 ,  C07D473/06 ,  C07D473/10 ,  C07D475/02 ,  C07D513/04

    摘要： Novel, heterocyclic compounds having at least one ring nitrogen, disclosed side chains and, in some embodiments, an oxygen ortho to the ring nitrogen inhibit inflammatory responses associated with TNF-&agr; and fibroblast proliferation in vivo and in vitro. The compounds of the invention neither appreciably inhibit the activity of cAMP phosphodiesterase nor the hydrolysis of phosphatidic acid, and are neither cytotoxic nor cytostatic. Preferred compounds of the invention are esters. Methods for the use of the novel compounds to inhibit ceramide-mediated intracellular responses in stimuli in vivo (particularly TN-&agr;) are also described. The methods are expected to be of use in reducing inflammatory responses (for example, after angioplasty), in limiting fibrosis (for example, of the liver in cirrhosis), in inhibiting cell senescence, cell apoptosis and UV induced cutaneous immune suppression. Compounds having enhanced water solubility are also described.

    摘要翻译： 新颖的，具有至少一个环氮的杂环化合物，在一些实施方案中，环氮原子上的氧被抑制与体内和体外TNF-α和成纤维细胞增殖相关的炎性反应。 本发明的化合物既不明显地抑制cAMP磷酸二酯酶的活性也不抑制磷脂酸的水解，既不是细胞毒性的也不是细胞抑制的。 本发明优选的化合物是酯。 还描述了使用新化合物抑制体内刺激中神经酰胺介导的细胞内应答的方法（特别是TN-α）。 预期这些方法可用于减少炎症反应（例如血管成形术后），限制纤维化（例如肝硬化），抑制细胞衰老，细胞凋亡和UV诱导的皮肤免疫抑制。 还描述了具有增强的水溶性的化合物。

    Synthesis of heteroarylamine intermediate compounds
    9.
    发明授权
    Synthesis of heteroarylamine intermediate compounds 有权
    杂芳基胺中间体化合物的合成

    公开(公告)号：US06822093B2

    公开(公告)日：2004-11-23

    申请号：US10313666

    申请日：2002-12-06

    申请人： Jinhua J. Song ,  Nathan K. Yee

    发明人： Jinhua J. Song ,  Nathan K. Yee

    IPC分类号： C07D41306

    CPC分类号： C07D213/61 ,  C07D213/38

    摘要： Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.

    摘要翻译： 公开了新的2-（5-卤代吡啶基）和2-（5-卤代嘧啶基）卤化镁，其制备方法及其在各自的5-卤代-2-取代的吡啶和嘧啶中的有效合成中的用途。