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31. 发明授权

US06518283B1 Squaric acid derivatives 失效
标题翻译：方酸衍生物
公开(公告)号：US06518283B1
公开(公告)日：2003-02-11
申请号：US09579317
申请日：2000-05-25
申请人： Barry John Langham , Rikki Peter Alexander , John Clifford Head , Janeen Marsha Linsley , John Robert Porter , Sarah Catherine Archibald , Graham John Warrellow
发明人： Barry John Langham , Rikki Peter Alexander , John Clifford Head , Janeen Marsha Linsley , John Robert Porter , Sarah Catherine Archibald , Graham John Warrellow
IPC分类号： A61K31445
CPC分类号： C07D213/79 , C07B2200/07 , C07C229/34 , C07C229/36 , C07C233/55 , C07C233/81 , C07C235/16 , C07C235/56 , C07C235/64 , C07C235/84 , C07C237/40 , C07C255/57 , C07C271/22 , C07C271/28 , C07C271/58 , C07C2601/04 , C07C2603/18 , C07D213/81 , C07D215/42 , C07D217/22 , C07D239/34 , C07D239/42 , C07D241/42 , C07D241/44 , C07D295/135 , C07D333/70 , C07D471/04 , C40B40/00
摘要： Squaric acid Derivatives of formula (1) are described: wherein R1 is an integrin binding group; R2 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic chain; R3 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group: and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune of inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.
摘要翻译：式（1）的方酸描述：其中R1是整联蛋白结合基团; R2是氢原子或C1-6烷基; L1是共价键或连接原子或基团; n是0或整数1; Alk1是任选取代的脂族链; R3是氢原子或任选取代的杂脂族，脂环族，杂脂族，多环脂族，多杂环脂族，芳族或杂芳族基团：及其盐，溶剂合物，水合物和N-氧化物。抑制整联蛋白与其配体的结合，并且可用于预防和治疗炎症性疾病或涉及细胞不适当生长或迁移的疾病的免疫。

32. 发明授权

US5821251A Nitrogen heterocycles 失效
公开(公告)号：US5821251A
公开(公告)日：1998-10-13
申请号：US448452
申请日：1996-04-10
申请人： Roger Crossley , Albert Opalko , Peter Jonathan Meade , Barry John Langham
发明人： Roger Crossley , Albert Opalko , Peter Jonathan Meade , Barry John Langham
IPC分类号： C07C217/74 , C07C229/46 , C07D215/14 , A01N43/42 , C07D215/00 , C07D215/16 , C07D401/00
CPC分类号： C07C229/46 , C07C217/74 , C07D215/14 , C07C2101/14
摘要： This invention concerns a compounds of generic formula: ##STR1## or a pharmaceutically acceptable salt thereof, where the dotted lines represent optional bonds with the nitrogen ring optional bonds being between one adjacent pair on ring atoms, R.sup.3 is an optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl group; said aryl or heteroaryl radicals being optionally substituted by one or more substituents the same or different, R.sup.4 represents hydrogen, or a group of formula --CR.sup.a R.sup.b R.sup.c where R.sup.a, R.sup.b and R.sup.c are independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl, optionally substituted C.sub.6 -C.sub.10 aryl, optionally substituted heteroaryl, C.sub.1 -C.sub.6 alkyl substituted by optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl, R' represents one or more optional substituents the same or different, selected from one or more of the following: halogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkoxycarbonyl, C.sub.1 -C.sub.6 hydroxyalkyl, CN, aminocarbonyl, C.sub.2 -C.sub.7 alkanoyloxy(C.sub.1 -C.sub.6)alkyl, carboxy, C.sub.2 -C.sub.7 alkanoxyamino, optionally substituted C.sub.6 -C.sub.10 or heteroaryl or an optionally substituted (C.sub.6 -C.sub.10 aryl)alkyl or a heteroaryl alkyl radical; said aryl or heteroaryl radicals being optionally substituted by one or more substituents the same or different, and R.sup." represents one or more optional mono- or di- valent substituents in the 5, 7 or 8 positions the same or different: monovalent substituents being selected from the following: C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkanoyloxy, hydroxy, amino, C.sub.2 -C.sub.7 alkanoylamino, C.sub.1 -C.sub.6 alkylamino, C.sub.1 -C.sub.6 hydroxalkyl, R.sup." can also represent hydroxy in the 6 position (when the optional bond is absent); the di-valent substituents being selected from oxo (i.e.dbd.O) and methylene (i.e .dbd.CH.sub.2). which compounds have pharmaceutical uses conferred by their ability to block voltage gated potassium channels.

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