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1. 发明授权

US06818638B2 Melvinolin derivatives 失效
标题翻译：梅尔文林衍生物
公开(公告)号：US06818638B2
公开(公告)日：2004-11-16
申请号：US10192888
申请日：2002-07-11
申请人： Rolf Baenteli , Wilfried Bauer , Sylvain Cottens , Claus Ehrhardt , Ulrich Hommel , Jörg Kallen , Josef Gottfried Meingassner , François Nuninger , Gabriele Weitz Schmidt
发明人： Rolf Baenteli , Wilfried Bauer , Sylvain Cottens , Claus Ehrhardt , Ulrich Hommel , Jörg Kallen , Josef Gottfried Meingassner , François Nuninger , Gabriele Weitz Schmidt
IPC分类号： A61K3133
CPC分类号： C07C271/12 , C07C235/26 , C07C235/30 , C07C237/18 , C07C2602/28 , C07D211/76 , C07D265/10
摘要： Mevinolin derivatives wherein the lactone ring is modified have interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1 interactions.
摘要翻译：其中内酯环被修饰的美维林衍生物具有令人感兴趣的药物性质，特别是在预防或治疗由LFA-1 / ICAM-1相互作用介导的疾病或疾病中。

2. 发明授权

US06642225B2 Diazacycloalkanedione derivatives 失效
标题翻译：二氮杂环烷二酮衍生物
公开(公告)号：US06642225B2
公开(公告)日：2003-11-04
申请号：US09968389
申请日：2001-10-02
申请人： Rainer Albert , Janet Dawson , Claus Ehrhardt , Sompong Wattanasin , Gabriele Weitz-Schmidt , Karl Welzenbach
发明人： Rainer Albert , Janet Dawson , Claus Ehrhardt , Sompong Wattanasin , Gabriele Weitz-Schmidt , Karl Welzenbach
IPC分类号： C07D24100
CPC分类号： C07D401/06 , A61K31/4965 , A61K31/551 , C07D241/08 , C07D243/08 , C07D401/12
摘要： Compounds of formula I wherein R is carboxy, esterified carboxy or amidated carboxy; R1 and R3 are independently lower alkyl, (hydroxy, lower alkoxy, amino, acylamino, mono- or di-lower alkylamino or mercapto)-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, cycloalkyl, aryl, biaryl, (cycloalkyl, aryl or biaryl)-lower alkyl, or (carboxy, esterified carboxy or amidated carboxy)-lower alkyl; R2 is hydrogen, lower alkyl, cycloalkyl, aryl, biaryl, arylaminocarbonyl, or aryl-(oxy, thio or amino); n is 1 or 2; Y is lower-alkylene or lower alkenylene; and pharmaceutically acceptable salts thereof; which are useful as LFA-1 antagonists.
摘要翻译：式I化合物，其中R是羧基，酯化的羧基或酰胺化的羧基; R 1和R 3独立地是低级烷基，（羟基，低级烷氧基，氨基，酰氨基，一或二低级烷基氨基或巯基） - 低级烷基，低级烷基 - （（环烷基，芳基或联芳基） - 低级烷基，或（羧基，酯化的羧基或酰胺基羧基） - 低级烷基; R2是氢，低级烷基，环烷基，芳基，联芳基，芳基氨基羰基或芳基 - （氧基，硫代或氨基）; n为1或2; Y为低级亚烷基或低级亚烯基;及其药学上可接受的盐; 其作为LFA-1拮抗剂是有用的。

3. 发明授权

US06399599B1 Substituted 2-oxo-1,4-diazacycloalkanes 失效
标题翻译：取代的2-氧代-1,4-二氮杂环烷烃
公开(公告)号：US06399599B1
公开(公告)日：2002-06-04
申请号：US09686511
申请日：2000-10-11
申请人： Rainer Albert , Josef G. Meingassner , Sompong Wattanasin , Gabriele Weitz-Schmidt , Karl Welzenbach , Ulrich Hommel , Claus Ehrhardt , Didier Roche , Joerg Kallen
发明人： Rainer Albert , Josef G. Meingassner , Sompong Wattanasin , Gabriele Weitz-Schmidt , Karl Welzenbach , Ulrich Hommel , Claus Ehrhardt , Didier Roche , Joerg Kallen
IPC分类号： C07D40106
CPC分类号： C07K5/06034 , A61K38/00 , C07D243/08 , C07K5/02 , C07K5/06078
摘要： Compounds of formula I wherein n is 1, 2 or 3; R1 is H, C1-4alkyl, aryl, or aryl-C1-4alkyl; Y is C1-4alkylene, —CO—C1-4alkylene, —CO—C2-5alkenylene, —CO—NH—, —CO—C1-3alkylene-NH—, or —CO—O—; R2 is an aromatic or heteroaromatic residue, each being optionally substituted by CF3, halogen, OH, C1-4alkoxy, amino, mono- or di-C1-4alkyl substituted amino, phenyl, benzyl or C1-4alkyl optionally substituted by amino; R3is the side chain present on the C&agr; of an &agr;-amino acid; R4 is biphenylyl, benzyl, hydroxy-benzyl, &agr;- or &bgr;-naphthyl-methyl, 5,6,7,8-tetrahydro-&bgr;-naphthyl-methyl or indolyl-methyl, each being optionally substituted on the ring by CF3, halogen, OH, C1-4alkoxy, amino, mono- or di-C1-4alkyl substituted amino, phenyl, benzyl or C1-4alkyl optionally substituted by amino; and X is —CN, —NR5R6 or —O—R8 wherein R5 is H, C1-6alkyl, aryl or aryl-C1-4alkyl; R6 is H or C1-6alkyl; and R8 is H, C1-4alkyl, aryl or aryl-C1-4alkyl; in free form or in salt form; which are useful in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1, -ICAM-2 or -ICAM-3 interactions.
摘要翻译：其中n为1,2或3的式I化合物; R 1是H，C 1-4烷基，芳基或芳基-C 1-4烷基; Y是C1-4亚烷基，-CO-C1-4亚烷基，-CO-C2-5亚烯基，-CO-NH-，-CO-C1-3亚烷基-NH-或-CO-O-; R 2是芳族或杂芳族残基，其各自任选被CF 3，卤素，OH，C 1-4烷氧基，氨基，单或二C 1-4烷基取代的氨基，苯基，苄基或任选被氨基取代的C 1-4烷基取代; R3是存在于α-氨基酸的Calpha上的侧链; R4是联苯基，苄基，羟基 - 苄基，α-或β-萘基 - 甲基，5,6,7,8-四氢-β-萘基 - 甲基或吲哚基 - 甲基，其各自在环上被CF 3任选取代，卤素，OH，C 1-4烷氧基，氨基，单或二-C 1-4烷基取代的氨基，苯基，苄基或任选被氨基取代的C 1-4烷基; 并且X是-CN，-NR 5 R 6或-O-R 8，其中R 5是H，C 1-6烷基，芳基或芳基-C 1-4烷基; R6是H或C1-6烷基; 且R 8为H，C 1-4烷基，芳基或芳基-C 1-4烷基; 以游离形式或盐形式; 其可用于预防或治疗由LFA-1 / ICAM-1，-ICAM-2或-ICAM-3相互作用介导的疾病或疾病。

4. 发明授权

US5837862A Sialyl Lewis X mimetics incorporating mannopeptides 失效
标题翻译：掺入甘露肽的唾液酸Lewis X模拟物
公开(公告)号：US5837862A
公开(公告)日：1998-11-17
申请号：US764315
申请日：1996-12-12
申请人： Chi-Huey Wong , Thomas G. Marron , Thomas J. Woltering , Gabriele Weitz-Schmidt
发明人： Chi-Huey Wong , Thomas G. Marron , Thomas J. Woltering , Gabriele Weitz-Schmidt
IPC分类号： C07H7/02 , C07H15/00 , A61K31/70 , C07H7/06
CPC分类号： C07H7/02 , C07H15/00
摘要： Sialyl Lewis X mimetics based on mannose glycosides are synthesized and shown to mimic the configuration and essential functional groups of sialyl Lewis X in space. The mannose based mimetics exhibit comparable biological activity as sialyl Lewis X in the E- selectin binding assay and can be employed for blocking neutrophil inflamatory conditions.
摘要翻译：合成了基于甘露糖苷的唾液酸路易斯X模拟物，并显示出模拟空间中唾液酸路易斯X的构型和必需官能团。基于甘露糖的模拟物在E-选择素结合测定中表现出与唾液酸基路易斯X相当的生物学活性，并且可用于阻断嗜中性粒细胞炎症病症。

5. 发明申请

US20100120865A1 Organic compounds 失效
标题翻译：有机化合物
公开(公告)号：US20100120865A1
公开(公告)日：2010-05-13
申请号：US12308338
申请日：2007-06-25
申请人： Ian Bruce , Gabriele Weitz Schmidt
发明人： Ian Bruce , Gabriele Weitz Schmidt
IPC分类号： A61K31/427 , C07D417/14 , C07D417/04 , C07D417/12 , A61K31/4439 , A61P11/00 , A61P11/06 , A61P29/00 , A61P17/00 , A61P27/00 , A61P37/00 , A61P25/00 , A61P19/00 , A61P13/00
CPC分类号： C07D401/14 , C07D417/14
摘要： The present invention concerns a compound of formula (I), or a pharmaceutically acceptable salt, or solvate thereof, wherein the groups Ri-Rs are defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐或溶剂合物，其中R 1 -R 3基团在描述中定义为化合物在治疗通过抑制作用而变态化的疾病的组合物和用途磷脂酰肌醇3-激酶。

6. 发明授权

US07799810B2 Organic compounds 失效
标题翻译：有机化合物
公开(公告)号：US07799810B2
公开(公告)日：2010-09-21
申请号：US12308338
申请日：2007-06-25
申请人： Ian Bruce , Gabriele Weitz Schmidt
发明人： Ian Bruce , Gabriele Weitz Schmidt
IPC分类号： A01N43/40 , A61K31/44
CPC分类号： C07D401/14 , C07D417/14
摘要： The present invention concerns a compound of formula (I), or a pharmaceutically acceptable salt, or solvate thereof, wherein the groups Ri- Rs are defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐或溶剂化物，其中R 1 -R基定义在本说明书中，该化合物在治疗通过抑制磷脂酰肌醇3-激酶。

7. 发明授权

US06630492B1 Lymphocyte function antigen-1 antagonists 失效
标题翻译：淋巴细胞功能抗原-1拮抗剂
公开(公告)号：US06630492B1
公开(公告)日：2003-10-07
申请号：US09486244
申请日：2000-02-24
申请人： Wilfried Bauer , Sylvain Cottens , Dieter Geyl , Gabriele Weitz-Schmidt , Jörg Kallen , Ulrich Hommel
发明人： Wilfried Bauer , Sylvain Cottens , Dieter Geyl , Gabriele Weitz-Schmidt , Jörg Kallen , Ulrich Hommel
IPC分类号： A61K31351
CPC分类号： C07D213/64 , A61K31/00 , A61K31/222 , A61K31/366 , C07C219/24 , C07C235/30 , C07C237/18 , C07C237/22 , C07C2601/08 , C07C2602/28 , C07D207/16 , C07D295/13 , C07D295/145 , C07D295/205 , C07D307/52 , C07D309/10 , C07D309/30 , C07D405/12 , C07D491/10
摘要： Mevinolin compounds for use in the treatment or prevention of autoimmune diseases, inflammation, ischemia/reperfusion injury and graft rejection. Such compounds bind to the LFA-1 I-domain and thereby inhibit LFA-1/ICAM-1 or LFA-1/ICAM-3 interactions.
摘要翻译：美维林化合物，用于治疗或预防自身免疫性疾病，炎症，缺血/再灌注损伤和移植排斥反应。这些化合物结合LFA-1 I结构域，从而抑制LFA-1 / ICAM-1或LFA-1 / ICAM-3相互作用。

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