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公开(公告)号：US06423728B1
公开(公告)日：2002-07-23
申请号：US09864104
申请日：2001-05-23
IPC分类号： A61K3144
CPC分类号： C07D213/82 , C07C327/46 , C07C327/48 , C07C2601/04 , C07C2601/08 , C07D213/56 , C07D233/38 , C07D239/28 , C07D401/06
摘要： It has been discovered that compounds of the formula: and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, inhibit the binding of VCAM-1 to VLA-4 and are usefull in treating inflammation associated with chronic inflammatory diseases such as rheumatoid arthritis (RA), multiple sclerosis, (MS), asthma, and inflammatory bowel disease (IBD).
摘要翻译： 已经发现，下式的化合物及其药学上可接受的盐和酯其中X和Y如下所定义，抑制VCAM-1与VLA-4的结合，并且在治疗与慢性炎性疾病相关的炎症中是有用的，例如 作为类风湿性关节炎（RA），多发性硬化，（MS），哮喘和炎性肠病（IBD）。
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公开(公告)号：US06288267B1
公开(公告)日：2001-09-11
申请号：US09505903
申请日：2000-02-17
IPC分类号： C07C69612
CPC分类号： C07D213/82 , C07C327/46 , C07C327/48 , C07C2601/04 , C07C2601/08 , C07D213/56 , C07D233/38 , C07D239/28 , C07D401/06
摘要： It has been discovered that compounds of the formula: and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, inhibit the binding of VCAM-1 to VLA-4 and are useful in treating inflammation associated with chronic inflammatory diseases such as rheumatoid arthritis (RA), multiple sclerosis, (MS), asthma, and inflammatory bowel disease (I BD).
摘要翻译： 已经发现下式的化合物及其药学上可接受的盐和酯，其中X和Y如下所定义，抑制VCAM-1与VLA-4的结合，并且可用于治疗与慢性炎性疾病相关的炎症，例如 作为类风湿性关节炎（RA），多发性硬化，（MS），哮喘和炎症性肠病（I BD）。
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公开(公告)号：US06806365B2
公开(公告)日：2004-10-19
申请号：US10117616
申请日：2002-04-05
申请人： Li Chen , Robert William Guthrie , Tai-Nang Huang , Achytharao Sidduri , Jefferson Wright Tilley , Kenneth Gregory Hull
发明人： Li Chen , Robert William Guthrie , Tai-Nang Huang , Achytharao Sidduri , Jefferson Wright Tilley , Kenneth Gregory Hull
IPC分类号： C07C22902
CPC分类号： C07D213/81 , C07C233/87 , C07C235/40 , C07C235/64 , C07C235/82 , C07C237/24 , C07C255/41 , C07C255/57 , C07C271/22 , C07C275/18 , C07C275/24 , C07C275/30 , C07C275/60 , C07C317/44 , C07C323/60 , C07C335/08 , C07C2601/08 , C07C2601/14 , C07D211/64 , C07D213/89 , C07D217/26 , C07D231/14 , C07D233/32 , C07D249/06 , C07D257/04 , C07D261/18 , C07D277/14 , C07D295/088 , C07D317/30 , C07D317/68 , C07D401/06 , C07D487/04
摘要： Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.
摘要翻译： 公开了具有作为VCAM-1与表达VLA-4的细胞之间结合的抑制剂的活性的式的化合物。 这些化合物可用于治疗其症状和/或损伤与VCAM-1与表达VLA-4的细胞结合相关的疾病。
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公开(公告)号：US06426348B1
公开(公告)日：2002-07-30
申请号：US09864032
申请日：2001-05-23
IPC分类号： A61K31505
CPC分类号： C07D213/82 , C07C327/46 , C07C327/48 , C07C2601/04 , C07C2601/08 , C07D213/56 , C07D233/38 , C07D239/28 , C07D401/06
摘要： It has been discovered that compounds of the formula: and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, inhibit the binding of VCAM-1 to VLA-4 and are useful in treating inflammation associated with chronic inflammatory diseases such as rheumatoid arthritis (RA), multiple sclerosis, (MS), asthma, and inflammatory bowel disease (I BD).
摘要翻译： 已经发现下式的化合物及其药学上可接受的盐和酯，其中X和Y如下所定义，抑制VCAM-1与VLA-4的结合，并且可用于治疗与慢性炎性疾病相关的炎症，例如 作为类风湿性关节炎（RA），多发性硬化，（MS），哮喘和炎症性肠病（I BD）。
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公开(公告)号：US06479666B2
公开(公告)日：2002-11-12
申请号：US09863567
申请日：2001-05-23
IPC分类号： C07D23302
CPC分类号： C07D213/82 , C07C327/46 , C07C327/48 , C07C2601/04 , C07C2601/08 , C07D213/56 , C07D233/38 , C07D239/28 , C07D401/06
摘要： It has been discovered that compounds of the formula: and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, inhibit the binding of VCAM-1 to VLA-4 and are useful in treating inflammation associated with chronic inflammatory diseases such as rheumatoid arthritis (RA), multiple sclerosis, (MS), asthma, and inflammatory bowel disease (I BD).
摘要翻译： 已经发现下式的化合物及其药学上可接受的盐和酯，其中X和Y如下所定义，抑制VCAM-1与VLA-4的结合，并且可用于治疗与慢性炎性疾病相关的炎症，例如 作为类风湿性关节炎（RA），多发性硬化，（MS），哮喘和炎症性肠病（I BD）。
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公开(公告)号：US06458844B2
公开(公告)日：2002-10-01
申请号：US09863579
申请日：2001-05-23
IPC分类号： A61K3119
CPC分类号： C07D213/82 , C07C327/46 , C07C327/48 , C07C2601/04 , C07C2601/08 , C07D213/56 , C07D233/38 , C07D239/28 , C07D401/06
摘要： It has been discovered that compounds of the formula: and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, inhibit the binding of VCAM-1 to VLA-4 and are useful in treating inflammation associated with chronic inflammatory diseases such as rheumatoid arthritis (RA), multiple sclerosis, (MS), asthma, and inflammatory bowel disease (I BD).
摘要翻译： 已经发现下式的化合物及其药学上可接受的盐和酯，其中X和Y如下所定义，抑制VCAM-1与VLA-4的结合，并且可用于治疗与慢性炎性疾病相关的炎症，例如 作为类风湿性关节炎（RA），多发性硬化，（MS），哮喘和炎症性肠病（I BD）。
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公开(公告)号：US06455550B1
公开(公告)日：2002-09-24
申请号：US09138353
申请日：1998-08-21
申请人： Li Chen , Robert William Guthrie , Tai-Nang Huang , Achytharao Sidduri , Jefferson Wright Tilley , Kenneth Gregory Hull
发明人： Li Chen , Robert William Guthrie , Tai-Nang Huang , Achytharao Sidduri , Jefferson Wright Tilley , Kenneth Gregory Hull
IPC分类号： A61K314166
CPC分类号： C07D213/81 , C07C233/87 , C07C235/40 , C07C235/64 , C07C235/82 , C07C237/24 , C07C255/41 , C07C255/57 , C07C271/22 , C07C275/18 , C07C275/24 , C07C275/30 , C07C275/60 , C07C317/44 , C07C323/60 , C07C335/08 , C07C2601/08 , C07C2601/14 , C07D211/64 , C07D213/89 , C07D217/26 , C07D231/14 , C07D233/32 , C07D249/06 , C07D257/04 , C07D261/18 , C07D277/14 , C07D295/088 , C07D317/30 , C07D317/68 , C07D401/06 , C07D487/04
摘要： Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.
摘要翻译： 公开了具有作为VCAM-1与表达VLA-4的细胞之间结合的抑制剂的活性的式的化合物。 这些化合物可用于治疗其症状和/或损伤与VCAM-1与表达VLA-4的细胞结合相关的疾病。
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公开(公告)号：US06420600B1
公开(公告)日：2002-07-16
申请号：US09506062
申请日：2000-02-17
IPC分类号： C07C22900
CPC分类号： C07C323/60 , C07B2200/07 , C07C233/80 , C07C2601/08
摘要： It has been discovered that compounds of the formula: and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, are more readily absorbed and more bioavailable than the corresponding carboxylic acids from which they are derived, both of which are effective inhibitors of the binding of VCAM-1 to VLA-4 in vivo and are useful in treating inflammation in inflammatory diseases in which such binding acts to bring on the inflammation.
摘要翻译： 已经发现，其中X和Y如下所定义的下式的化合物及其药学上可接受的盐和酯比它们衍生的相应的羧酸更容易被吸收并且更具生物利用性，两者都是有效的 VCAM-1与VLA-4在体内结合的抑制剂，可用于治疗炎症性疾病中的炎症，其中这种结合会引起炎症。
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