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54 条记录 (耗时 0.192 秒)

    Cholesteryl ester transfer protein inhibitors
    21.
    发明授权
    Cholesteryl ester transfer protein inhibitors 有权
    胆固醇酯转移蛋白抑制剂

    公开(公告)号：US08865707B2

    公开(公告)日：2014-10-21

    申请号：US12087189

    申请日：2006-12-29

    申请人： Amjad Ali ,  Peter J. Sinclair ,  Gayle E. Taylor

    发明人： Amjad Ali ,  Peter J. Sinclair ,  Gayle E. Taylor

    IPC分类号： C07D265/10 ,  C07D413/06 ,  A61K31/5355 ,  A61K31/535

    CPC分类号： C07D265/10 ,  C07D413/06

    摘要： Compounds of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), A1 is a cyclic group, and B is a cyclic group which is attached to the heterocyclic ring directly or through a methylene group.

    摘要翻译： 包括化合物的药学上可接受的盐的式（I）化合物是CETP抑制剂，可用于升高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。 在式（I）的化合物中，A1是环状基团，B是直接或通过亚甲基与杂环连接的环状基团。

    Cholesteryl Ester Transfer Protein Inhibitors
    22.
    发明申请
    Cholesteryl Ester Transfer Protein Inhibitors 审中-公开
    胆固醇酯转移蛋白抑制剂

    公开(公告)号：US20100167986A1

    公开(公告)日：2010-07-01

    申请号：US11992816

    申请日：2006-09-28

    申请人： Amjad Ali ,  Peter J. Sinclair

    发明人： Amjad Ali ,  Peter J. Sinclair

    IPC分类号： A61K38/28 ,  C07D257/00 ,  A61K31/41 ,  C07D249/04 ,  A61K31/4192 ,  C07D261/14 ,  A61K31/42 ,  A61P9/10 ,  A61K38/16 ,  A61P3/04 ,  A61P9/12

    CPC分类号： C07D257/06 ,  C07D249/04 ,  C07D261/14 ,  C07D401/12

    摘要： Compounds of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), A1 and A2 are each an aromatic ring, a 5-6-membered heterocyclic ring, an aromatic ring fused to a heterocyclic ring, a phenyl ring fused to a heterocyclic ring, or a cycloalkyl ring, and Z is an aromatic or heterocyclic ring.

    摘要翻译： 包括化合物的药学上可接受的盐的式（I）化合物是CETP抑制剂，可用于升高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。 在式（I）的化合物中，A1和A2各自为芳香环，5-6元杂环，稠合于杂环的芳环，稠合于杂环的苯环或环烷基环， Z为芳香环或杂环。

    Amino O-aryl macrolides having immunosuppressive activity
    25.
    发明授权
    Amino O-aryl macrolides having immunosuppressive activity 失效
    具有免疫抑制活性的氨基O-芳基大环内酯类

    公开(公告)号：US5262533A

    公开(公告)日：1993-11-16

    申请号：US876634

    申请日：1992-05-06

    申请人： Peter J. Sinclair ,  Helen M. Organ ,  Matthew J. Wyvratt

    发明人： Peter J. Sinclair ,  Helen M. Organ ,  Matthew J. Wyvratt

    IPC分类号： C07D498/18 ,  C07D491/16 ,  A61K31/395

    CPC分类号： C07D498/18

    摘要： Amino O-aryl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by arylation and amination at C-3"/C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses. Also, these macrolides are useful in the treatment of reversible obstructive airways disease, particularly asthma; as hair revitalizing agents, especially in the treatment of male pattern alopecia or alopecia senilis; in the reversal of multidrug resistance of tumor cells; in treatment of inflammation of mucosa and blood vessels, gastric ulcers, vascular damage, ischemic bowel disease, inflammatory bowel disease, necrotizing enterocolitis, intestinal lesions associated with thermal burns; in the treatment of cytomegalovirus infection; and in the treatment of idiopathic thrombocytopenic purpura and Basedow's disease.

    摘要翻译： 一般结构式I的氨基O-芳基大环内酯是通过在环己基环的C-3“/ C-4”处的芳基化和胺化由合适的前体制备的。 这些大环内酯类免疫抑制剂可用于哺乳动物宿主用于治疗自身免疫性疾病，感染性疾病和/或预防外来器官移植排斥反应。 此外，这些大环内酯类免疫抑制剂可用于局部治疗炎性和过度增生性皮肤病以及免疫介导疾病的皮肤表现。 此外，这些大环内酯可用于治疗可逆性阻塞性气道疾病，特别是哮喘; 作为头发活化剂，特别是在治疗男性脱发或脱发性秃发症中， 在逆转肿瘤细胞的多药耐药性; 治疗粘膜和血管的炎症，胃溃疡，血管损伤，缺血性肠病，炎性肠病，坏死性小肠结肠炎，与热灼伤相关的肠道损伤; 在治疗巨细胞病毒感染; 并在治疗特发性血小板减少性紫癜和基诺病。

    O-aryl, O-alkyl, O-alkenyl and O-alkynylmacrolides having immunosuppressive activity
    27.
    发明授权
    O-aryl, O-alkyl, O-alkenyl and O-alkynylmacrolides having immunosuppressive activity 失效
    具有免疫抑制活性的O-芳基，O-烷基，O-烯基和O-炔基大环内酯

    公开(公告)号：US5250678A

    公开(公告)日：1993-10-05

    申请号：US875036

    申请日：1992-05-01

    申请人： Mark Goulet ,  Frederick Wong ,  Peter J. Sinclair ,  Matthew J. Wyvratt

    发明人： Mark Goulet ,  Frederick Wong ,  Peter J. Sinclair ,  Matthew J. Wyvratt

    IPC分类号： A61K31/41 ,  A61K31/40 ,  A61K31/445 ,  A61P17/00 ,  A61P29/00 ,  A61P31/12 ,  A61P37/06 ,  C07D498/18 ,  C07D491/16 ,  A61K31/435

    CPC分类号： C07D498/18

    摘要： O-Aryl, O-alkyl, O-alkenyl and O-alkynyl-macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-3" and/or C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses. Also, these macrolides are useful in the treatment of reversible obstructive airways disease, particularly asthma; as hair revitalizing agents, especially in the treatment of male pattern alopecia or alopecia senilis; in the reversal of multidrug resistance of tumor cells; in treatment of inflammation of mucosa and blood vessels, gastric ulcers, vascular damage, ischemic bowel disease, necrotizing enterocolitis, intestinal lesions associated with thermal burns; in the treatment of cytomegalovirus infection; and in the treatment of idiopathic thrombocytopenic purpura and Basedow's disease.