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1. 发明申请

WO1997044337A1 BENZOFURAN CARBOXAMIDES AND THEIR THERAPEUTIC USE 审中-公开
标题翻译：苯并呋喃类抗坏血酸及其治疗用途
公开(公告)号：WO1997044337A1
公开(公告)日：1997-11-27
申请号：PCT/GB1997001361
申请日：1997-05-20
申请人： CHIROSCIENCE LIMITED , DYKE, Hazel, Joan , LOWE, Christopher , MONTANA, John, Gary , KENDALL, Hannah, Jayne , SABIN, Verity, Jayne
发明人： CHIROSCIENCE LIMITED
IPC分类号： C07D307/79
CPC分类号： C07D405/12 , C07D307/86 , C07D405/14 , C07D417/14
摘要： A compound of general formula (i) wherein Z is CO or CS; R1 represents alkoxy optionally substituted with one or more halogens, OH or thioalkyl; R2 and R3 are the same or different and are each H, R6, OR10, COR6, C(=NOR6)R6, alkyl-C(=NOR6)R6, alkyl-C(=NOH)R6, C(=NOH)R6, halogen, NR8R9, CF3, CN, CO2H, CO2R10, CONH2, CONHR6 or CON(R6)2; R4 represents H, arylalkyl, heteroarylalkyl, heterocycloalkyl, S(O)mR10 or alkyl optionally substituted with one or more substituents chosen from hydroxy, alkoxy, CO2R7, SO2NR11R12, CONR11R12, CN, carbonyl oxygen, NR8R9, COR10 and S(O)nR10; R5 represents aryl, heteroaryl, heterocyclo, arylalkyl, heteroarylalkyl or heterocycloalkyl; in R4 and/or R5 the aryl/heteroaryl/heterocyclo portion is optionally substituted with one or more substituents alkyl-R13 or R13; R6 represents R10 optionally substituted at any position with R14; R7 represents H, alkyl, arylalkyl, heteroarylalkyl or heterocycloalkyl; R8 represents H, aryl, heteroaryl, heterocyclo, alkyl, cycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkyl, alkylcarbonyl, alkoxycarbonyl, arylsulphonyl, heteroarylsulphonyl, heterocyclosulphonyl, arylcarbonyl, heteroarylcarbonyl, heterocyclocarbonyl or alkylsulphonyl; R10 represents alkyl, cycloalkyl, aryl, heteroaryl, heterocyclo, arylalkyl, heteroarylalkyl or heterocycloalkyl; R9, R11 and R12 are the same or different and are each H or R10; R13 represents alkyl optionally substituted with halogen, alcoxy optionally substituted by halogen, aryl, heteroaryl, heterocyclo, hydroxy, aryloxy, heteroaryloxy, heterocyclooxy, arylalkyloxy, heteroarylalkyloxy, heterocycloalkoxy, CO2R7, CONR11R12, SO2NR11R12, halogen, -CN, -NR8R9, COR10, S(O)nR10 or carbonyl oxygen; R14 represents OH, carbonyl oxygen, OR10, NR8R9, CN, CO2H, CO2R10, CON11R12 or COR10; m is an integer of up to 2; and n represents 0.2, or a pharmaceutically acceptable salt thereof.
摘要翻译：通式（ⅰ）的化合物，其中Z为CO或CS; R 1表示任选被一个或多个卤素OH或硫代烷基取代的烷氧基; R2和R3相同或不同，分别为H，R6，OR10，COR6，C（= NOR6）R6，烷基-C（= NOR6）R6，烷基-C（= NOH）R6，C（= NOH）R6 ，卤素，NR8R9，CF3，CN，CO2H，CO2R10，CONH2，CONHR6或CON（R6）2; R4代表H，芳基烷基，杂芳基烷基，杂环烷基，S（O）mR10或任选被一个或多个选自羟基，烷氧基，CO 2 R 7，SO 2 NR 11 R 12，CONR 11 R 12，CN，羰基氧，NR 8 R 9，COR 10和S（O）n R 10 ; R5表示芳基，杂芳基，杂环基，芳基烷基，杂芳基烷基或杂环烷基; 在R 4和/或R 5中，芳基/杂芳基/杂环部分任选被一个或多个取代基烷基-R 13或R 13取代; R 6表示R 10任选在任何位置被R 14取代; R 7表示H，烷基，芳基烷基，杂芳基烷基或杂环烷基; R8代表H，芳基，杂芳基，杂环基，烷基，环烷基，芳基烷基，杂芳基烷基，杂环烷基，烷基羰基，烷氧基羰基，芳基磺酰基，杂芳基磺酰基，杂环磺酰基，芳基羰基，杂芳基羰基，杂环羰基或烷基磺酰基。 R10表示烷基，环烷基，芳基，杂芳基，杂环基，芳基烷基，杂芳基烷基或杂环烷基; R9，R11和R12相同或不同，分别为H或R10; R13表示任选被卤素取代的烷基，任选被卤素，芳基，杂芳基，杂环基，羟基，芳氧基，杂芳氧基，杂环氧基，芳基烷氧基，杂芳烷氧基，杂环烷氧基，CO 2 R 7，CONR 11 R 12，SO 2 NR 11 R 12，卤素，-CN，-NR 8 R 9，COR 10， S（O）nR 10或羰基氧; R14表示OH，羰基氧，OR10，NR8R9，CN，CO2H，CO2R10，CON11R12或COR10; m是最多2的整数; 和n表示0.2，或其药学上可接受的盐。

2. 发明申请

WO1997044036A1 QUINOLINE CARBOXAMIDES AS TNF INHIBITORS AND AS PDE-IV INHIBITORS 审中-公开
标题翻译：喹啉羧酰胺作为TNF抑制剂和PDE-IV抑制剂
公开(公告)号：WO1997044036A1
公开(公告)日：1997-11-27
申请号：PCT/GB1997001359
申请日：1997-05-20
申请人： CHIROSCIENCE LIMITED , DYKE, Hazel, Joan , MONTANA, John, Gary , LOWE, Christopher , KENDALL, Hannah, Jayne , SABIN, Verity, Margaret
发明人： CHIROSCIENCE LIMITED
IPC分类号： A61K31/47
CPC分类号： C07D401/12 , A61K45/06 , C07D215/48 , C07D401/14 , C07D417/12
摘要： A compound of general formula (i), wherein X is CO or CS; R is H, halogen or alkyl; R1 represents OH, alkoxy optionally substituted with one or more halogens, or thioalkyl; R2, R3 and R4 are the same or different and are each H, R7, OR11, COR7, C(=NOR7)R7, alkyl-C(=NOR7)R7, halogen CF3, alkyl-C(=NOH)R7, C(=NOH)R7, CN, CO2H, CO2R11, CONH2, CONHR7, CON(R7)2, NR9R10 or CONR12R13 where NR12R13 is a heterocyclic ring optionally substituted with one or more R15; R5 represents H, arylalkyl, heteroarylalkyl, heterocycloalkyl, S(O)mR11 or alkyl optionally substituted with one or more substituents chosen from hydroxy, alkoxy, CO2R8, SO2NR12R13, CONR12R13, CN, carbonyl oxygen, NR9R10, COR11 and S(O)nR11; R6 represents aryl, heteroaryl, heterocyclo, arylalkyl, heteroarylalkyl or heterocycloalkyl; in R5 and/or R6, the aryl/heteroaryl/heterocyclo portion is optionally substituted with one or more substituents alkyl-R14 or R14. The compounds can be used to treat disease states, for example disease states associated with proteins that mediate cellular activity, for example by inhibiting tumour necrosis factor and/or by inhibiting phosphodiesterase IV.
摘要翻译：通式（i）的化合物，其中X为CO或CS; R是H，卤素或烷基; R1表示OH，任选被一个或多个卤素取代的烷氧基或硫代烷基; R2，R3和R4相同或不同，分别为H，R7，OR11，COR7，C（= NOR7）R7，烷基-C（= NOR7）R7，卤素CF3，烷基-C（= NOH）R7，C （= NOH）R 7，CN，CO 2 H，CO 2 R 11，CONH 2，CONHR 7，CON（R 7）2，NR 9 R 10或CONR 12 R 13，其中NR 12 R 13是任选被一个或多个R 15取代的杂环; R 5表示H，芳基烷基，杂芳基烷基，杂环烷基，S（O）m R 11或任选被一个或多个选自羟基，烷氧基，CO 2 R 8，SO 2 NR 12 R 13，CONR 12 R 13，CN，羰基氧，NR 9 R 10，COR 11和S（O）n R 11 ; R 6表示芳基，杂芳基，杂环基，芳基烷基，杂芳基烷基或杂环烷基; 在R 5和/或R 6中，芳基/杂芳基/杂环部分任选被一个或多个烷基-R 14或R 14取代基取代。该化合物可用于治疗疾病状态，例如与介导细胞活性的蛋白质相关的疾病状态，例如通过抑制肿瘤坏死因子和/或通过抑制磷酸二酯酶IV。

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