公开(公告)号：USRE39576E1

公开(公告)日：2007-04-17

申请号：US10407204

申请日：1995-06-14

申请人： Harold Francis Hodson ,  Richard Michael John Palmer ,  David Alan Sawyer ,  Richard Graham Knowles ,  Karl Witold Franzmann ,  Martin James Drysdale ,  Patricia Ifeyinwa Davies ,  Helen Alice Rebecca Clark ,  Barry George Shearer ,  Steven Smith

发明人： Harold Francis Hodson ,  Richard Michael John Palmer ,  David Alan Sawyer ,  Richard Graham Knowles ,  Karl Witold Franzmann ,  Martin James Drysdale ,  Patricia Ifeyinwa Davies ,  Helen Alice Rebecca Clark ,  Barry George Shearer ,  Steven Smith

IPC分类号： A61K31/195

CPC分类号： C07C323/60 ,  C07C317/48 ,  Y02P20/55

摘要： A compound of formula (I) wherein R1 is a C1-6 straight or branched chain alkyl group, a C2-6alkenyl group, a C2-6 alkynyl group, a C3-6cycloalkyl group or a C3-6cycloalkylC1-6alkyl group, each optionally substituted by one to three groups independently selected from: —CN; —NO2; a group —COR2 wherein R2 is hydrogen, C1-6 alkyl, —OR3 wherein R3 is hydrogen or C1-6alkyl or NR4R5 wherein R4 and R5 are independently selected from hydrogen or C1-6 alkyl; a group —S(O)mR6 wherein m is 0, 1 or 2, R6 is hydrogen, C1-6 alkyl, hydroxy or NR7R8 wherein R7 and R8 are independently hydrogen or C1-6 alkyl; a group PO(OR9)2 wherein R9 is hydrogen or C1-6 alkyl; a group NR10R11 wherein R10 and R11 are independently selected from hydrogen, C1-6 alkyl, —COR12 wherein R12 is hydrogen or C1-6 alkyl, or —S(O)m′R13 wherein m′ is 0, 1 or 2 and R13 is hydrogen or C1-6 alkyl; halo; or a group —OR14 wherein R14 is hydrogen, C1-6 alkyl optionally substituted by one to three halo atoms, C6-10 aryl or —COR15 wherein R15 is hydrogen or C1-6 alkyl; p is 2 or 3, q is 1 or 2 and n is 0 or 1 and all salts, esters, amides and physiologically acceptable prodrugs thereof; pharmaceutical uses and formulations therefor; and processes for their preparation are disclosed.

摘要翻译： 式的化合物

公开(公告)号：US5889056A

公开(公告)日：1999-03-30

申请号：US750679

申请日：1996-12-27

申请人： Harold Francis Hodson ,  Richard Michael John Palmer ,  David Alan Sawyer ,  Richard Graham Knowles ,  Karl Witold Franzmann ,  Martin James Drysdale ,  Patricia Ifeyinwa Davies ,  Helen Alice Rebecca Clark ,  Barry George Shearer ,  Steven Smith

发明人： Harold Francis Hodson ,  Richard Michael John Palmer ,  David Alan Sawyer ,  Richard Graham Knowles ,  Karl Witold Franzmann ,  Martin James Drysdale ,  Patricia Ifeyinwa Davies ,  Helen Alice Rebecca Clark ,  Barry George Shearer ,  Steven Smith

IPC分类号： A61K31/00 ,  A61K20060101 ,  A61K31/195 ,  A61K31/198 ,  A61P5/00 ,  A61P9/00 ,  A61P43/00 ,  C07C20060101 ,  C07C257/14 ,  C07C315/02 ,  C07C317/02 ,  C07C317/48 ,  C07C317/50 ,  C07C323/60 ,  C07C327/00 ,  C07C327/58

CPC分类号： C07C323/60 ,  C07C317/48 ,  Y02P20/55

摘要： A compound of formula (I) ##STR1## wherein R.sup.1 is a C.sub.1-6 straight or branched chain alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.3-6 cycloalkyl group or a C.sub.3-6 cycloalkylC.sub.1-6 alkyl group, each optionally substituted by one to three groups independently selected from: --CN; --NO.sub.2 ; a group --COR.sup.2 wherein R.sup.2 is hydrogen, C.sub.1-6 alkyl, --OR.sup.3 wherein R.sup.3 is hydrogen or C.sub.1-6 alkyl or NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently selected from hydrogen or C.sub.1-6 alkyl; a group --S(O).sub.m R.sup.6 wherein m is 0, 1 or 2, R.sup.6 is hydrogen, C.sub.1-6 alkyl, hydroxy or NR.sup.7 R.sup.8 wherein R.sup.7 and R.sup.8 are independently hydrogen or C.sub.1-6 alkyl; a group PO(OR.sup.9).sub.2 wherein R.sup.9 is hydrogen or C.sub.1-6 alkyl; a group NR.sup.10 R.sup.11 wherein R.sup.10 and R.sup.11 are independently selected from hydrogen, C.sub.1-6 alkyl, --COR.sup.12 wherein R.sup.12 is hydrogen or C.sub.1-6 alkyl, or --S(O).sub.m' R.sup.13 wherein m' is 0, 1 or 2 and R.sup.13 is hydrogen or C.sub.1-6 alkyl; halo; or a group --OR.sup.14 wherein R.sup.14 is hydrogen, C.sub.1-6 alkyl optionally substituted by one to three halo atoms, C.sub.6-10 aryl or --COR.sup.15 wherein R.sup.15 is hydrogen or C.sub.1-6 alkyl; p is 2 or 3, q is 1 or 2 and n is 0 or 1 and all salts, esters, amides and physiologically acceptable prodrugs thereof; pharmaceutical uses and formulations therefor; and processes for their preparation are disclosed.

摘要翻译： PCT No.PCT / GB95 / 01378 Sec。 371日期1996年12月27日第 102（e）日期1996年12月27日PCT提交1995年6月14日PCT公布。 公开号WO95 / 34534 日期：1995年12月21日一种式（I）化合物其中R 1为C 1-6直链或支链烷基，C 2-6烯基，C 2-6炔基，C 3-6环烷基 或C 3-6环烷基C 1-6烷基，各自任选被一至三个独立地选自：-CN; -NO2; 基团-COR 2，其中R 2是氢，C 1-6烷基，-OR 3，其中R 3是氢或C 1-6烷基或NR 4 R 5，其中R 4和R 5独立地选自氢或C 1-6烷基; 基团-S（O）m R 6，其中m为0,1或2，R 6为氢，C 1-6烷基，羟基或NR 7 R 8，其中R 7和R 8独立地为氢或C 1-6烷基; 基团PO（OR 9）2，其中R 9是氢或C 1-6烷基; 基团NR10R11，其中R10和R11独立地选自氢，C1-6烷基，-COR12，其中R12是氢或C1-6烷基或-S（O）m'R13，其中m'是0,1或2，R13 是氢或C 1-6烷基; 光环; 或-OR 14，其中R 14是氢，任选被一至三个卤素原子取代的C 1-6烷基，C 6-10芳基或-COR 15，其中R 15是氢或C 1-6烷基; p为2或3，q为1或2，n为0或1，所有的盐，酯，酰胺和其生理上可接受的前药; 药用及其制剂; 并公开了其制备方法。