专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO1992020673A1 ANTIHYPOTENSIVE BENZOFURAN DERIVATIVES WITH N-LINKED 1H-IMIDAZOLYLMETHYL-5-CARBOXAMIDE SUBSTITUENTS 审中-公开
标题翻译：具有N-连接的1H-咪唑啉基甲基-5-羧酰胺取代基的抗真菌苯并呋喃衍生物
公开(公告)号：WO1992020673A1
公开(公告)日：1992-11-26
申请号：PCT/GB1992000889
申请日：1992-05-15
申请人： GLAXO GROUP LIMITED , ROSS, Barry, Clive , MIDDLEMISS, David , SCOPES, David, Ian, Carter , JACK, Torquil, Iain, MacLean , CARDWELL, Kevin, Stuart , DOWLE, Michael, Dennis , JUDD, Duncan, Bruce
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D405/06
CPC分类号： C07D405/06
摘要： The invention provides compounds of general formula (I), or a physiologically acceptable salt or solvate thereof in which Het represents an N-linked imidazolyl group of formula α; R1 represents an ethyl or n-propyl group; R2 represents a chlorine atom or a methyl or ethyl group; and R3 represents a hydrogen atom or a methyl or ethyl group. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

2. 发明申请

WO1992020679A1 BENZOFURAN DERIVATIVES 审中-公开
标题翻译： BENZOFURAN衍生物
公开(公告)号：WO1992020679A1
公开(公告)日：1992-11-26
申请号：PCT/GB1992000887
申请日：1992-05-15
申请人： GLAXO GROUP LIMITED , ROSS, Barry, Clive , MIDDLEMISS, David , SCOPES, David, Ian, Carter , JACK, Torquil, Iain, MacLean , CARDWELL, Kevin, Stuart , DOWLE, Michael, Dennis , MONTANA, John, Gary , PASS, Martin , JUDD, Duncan, Bruce
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D471/04
CPC分类号： C07D405/14 , C07D471/04 , C07D473/00
摘要： The invention provides compounds of general formula (I) or a physiologically acceptable salt, solvate or metabolically labile ester thereof wherein R1 and Ar are as defined in the claims and Het represents the group (a), A represents a variety of 4-membered optionally substituted linkages; R6 represents a hydrogen atom or a group selected from C¿1-6?alkyl, C2-6alkyl, C1-6alkylthio, C1-6alkoxy, C3-7cycloalkyl, or C3-7cycloalkylC1-4alkyl. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

3. 发明申请

WO1992016552A1 1-IMIDAZOLGEMETHYL BENZOFURAN DERIVATIVES AS INHIBITORS OF ANGIOTENSIN II ACTIVITY 审中-公开
标题翻译：作为抗生素II活性抑制剂的1-咪唑烷基苯并呋喃衍生物
公开(公告)号：WO1992016552A1
公开(公告)日：1992-10-01
申请号：PCT/EP1992000627
申请日：1992-03-21
申请人： GLAXO GROUP LIMITED , ROSS, Barry, Clive , MIDDLEMISS, David , SCOPES, David, Ian, Carter , JACK, Torquil, Iain, Maclean , CARDWELL, Kevin, Stuart , DOWLE, Michael, Dennis , WATSON, Stephen, Paul , HIRST, Gavin, Charles
发明人： GLAXO GROUP LIMITED
IPC分类号： C07K05/06
CPC分类号： C07D405/06 , A61K38/00 , C07D405/14 , C07K5/06191
摘要： The invention provides compounds of general formula (I) or a physiologically acceptable salt, solvate or metabolically labile ester thereof wherein: R1 représents a hydrogen atom or a halogen atom or a group selected from C¿1-6?alkyl, C2-6alkenyl, fluoroC1-6alkyl, C1-6alkoxy, -CHO, -CO2H or -COR?2¿; Ar represents the group (II), R2 represents a group selected from C¿1-6?alkyl, C2-6alkenyl, C1-6alkoxy or the group -NR?12R13; R3¿ represents a group selected from -CO¿2?H, -NHSO2CF3 or a C-linked tetrazolyl group; R?4 and R5¿ which may be the same or different each independently represent a hydrogen atom or a halogen atom or a C¿1-6?alkyl group; Het represents the group (III), R?6¿ represents a hydrogen atom or a group selected from C¿1-6?alkyl, C2-6alkenyl, C1-6alkylthio, C1-6alkoxy, C3-7cycloalkyl or C3-7cycloalkylC1-4alkyl; R?7¿ represents a hydrogen atom or a halogen atom or a group selected from C¿1-6?alkyl, C2-6alkenyl or fluoroC1-6alkyl; R?8¿ represents a hydrogen atom or a C¿1-6?alkyl group; R?9¿ represents a hydrogen atom or a group selected from phenyl or C¿1-6?alkyl, optionally substituted by a phenyl, hydroxyphenyl, hydroxyl, amino, guanidino, imidazolyl, indolyl, mercapto, C1-6alkylthio, carboxyl or amido group; or R?8 and R9¿, when taken together, form an alkylene bridge of 2, 3 or 4 carbon atoms; R10 represents a hydrogen atom or a C¿1-6?alkyl group; R?11¿ represents a group selected from hydroxyl, C¿1-6?alkoxy, C2-6alkenoxy or -NR?12R13; R12 and R13¿, which may be the same of different, each independently represent a hydrogen atom or a C¿1-4?alkyl group or -NR?12R13¿ forms a saturated heterocyclic ring which has 5 or 6 ring members and may optionally contain in the ring one oxygen atom; m represents zero or an integer from 1 to 4; and n represents zero or an integer from 1 to 3; with the proviso that when n represents an integer from 1 to 3, R?9 and R10¿ both represent hydrogen atoms. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

4. 发明申请

WO1992009600A1 BENZOFURAN AND BENZTHIOPHENE DERIVATIVES 审中-公开
标题翻译：苯并呋喃和苯并噻吩衍生物
公开(公告)号：WO1992009600A1
公开(公告)日：1992-06-11
申请号：PCT/GB1991002114
申请日：1991-11-28
申请人： GLAXO GROUP LIMITED , ROSS, Barry, Clive , SCOPES, David, Ian, Carter , CARDWELL, Kevin, Stuart , ELDRED, Colin, David , MIDDLEMISS, David , JACK, Torquil, Iain, MacLean , DOWLE, Michael, Dennis , MONTANA, John, Gary , SHAH, Pritom
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D405/06
CPC分类号： C07D307/82 , C07D405/06 , C07D405/10 , C07D405/14
摘要： The invention provides compounds of general formula (I) or a physiologically acceptable salt, solvate or metabolically labile ester thereof wherein Q represents an oxygen or sulphur atom; R represents a hydrogen atom or a halogen atom or a group selected from C1-6alkyl, C2-6alkenyl, fluoroC1-6alkyl, -CHO, -CO2H, C1-6alkoxy, or -COR ; Ar represents the group (a); R represents a group selected from C1-6alkyl, C2-6alkenyl, C1-6alkoxy or the group -NR R ; R represents a group selected from -CO2H, -NHSO2CF3 or a C-linked tetrazolyl group; R and R , which may be the same or different, each independently represent a hydrogen atom or a halogen atom or a C1-6alkyl group; Het represents the group (b); X represents N or CH; Y represents N or CR ; Z represents N or CR ; R represents a hydrogen atom or a C1-6alkyl, C2-6alkenyl or a C1-6alkylthio group; R represents a halogen atom or a group selected from cyano, nitro, C1-6alkyl, C2-6alkenyl, fluoroC1-6alkyl, -(CH2)mR , -(CH2)nCOR , or -(CH2)pNR COR ; R represents a hydroxy or C1-6alkoxy group; R represents a hydrogen atom or a group selected from hydroxy, C1-6alkyl, C1-6alkoxy, phenyl, phenoxy or the group -NR R ; R represents a hydrogen atom or a C1-6alkyl group; R represents a hydrogen atom or a group selected from C1-6alkyl, C1-6alkoxy, phenyl, phenoxy or the group -NR R ; R and R , which may be the same or different, each independently represent a hydrogen atom or a C1-4alkyl group or -NR R forms a saturated heterocyclic ring which has 5 or 6 ring members and may optionally contain in the ring one oxygen atom; m represents an integer from 1 to 4; n represents zero or an integer from 1 to 4; and p represents an integer from 1 to 4; with the proviso that at least one of X, Y and Z is a nitrogen atom, and with the further proviso that when X is N at least one of Y and Z is N and when Y is N at least one of X and Z is N. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.
摘要翻译：本发明提供通式（I）的化合物或其生理上可接受的盐，溶剂合物或代谢不稳定的酯，其中Q表示氧或硫原子; R 1表示氢原子或卤素原子或选自C 1-6烷基，C 2-6烯基，氟C 1-6烷基，-CHO，-CO 2 H，C 1-6烷氧基或-COR 2的基团。 Ar表示组（a）; R 2表示选自C 1-6烷基，C 2-6烯基，C 1-6烷氧基或-NR 14 R 13基团。 R 3表示选自-CO 2 H，-NHSO 2 CF 3或C连接的四唑基的基团; R 4和R 5可以相同或不同，各自独立地表示氢原子或卤素原子或C1-6烷基; Het代表组（b）; X表示N或CH; Y表示N或CR 7; Z表示N或CR 7; R 6表示氢原子或C 1-6烷基，C 2-6烯基或C 1-6烷硫基; R 7表示卤素原子或选自氰基，硝基，C 1-6烷基，C 2-6烯基，氟C 1-6烷基， - （CH 2）m R 8， - （CH 2）n COR 9或 - （ CH2）PNR <10> COR <11>; R 8表示羟基或C 1-6烷氧基; R 9表示氢原子或选自羟基，C 1-6烷基，C 1-6烷氧基，苯基，苯氧基或基团-NR 12 R 13的基团。 R 10表示氢原子或C 1-6烷基; R 11表示氢原子或选自C 1-6烷基，C 1-6烷氧基，苯基，苯氧基或基团-NR 12 R 13的基团。 R 12和R 13可以相同或不同，各自独立地表示氢原子或C 1-4烷基或-NR 12 R 13形成饱和杂环，其具有5或6个环成员，并且可以任选地在环中含有一个氧原子; m表示1〜4的整数， n表示0或1至4的整数; p表示1〜4的整数，条件是X，Y和Z中的至少一个是氮原子，另外条件是当X是N时，Y和Z中的至少一个是N，当Y是N时，X和Z中的至少一个是该化合物可用于治疗或预防与认知障碍相关的高血压和疾病。

5. 发明申请

WO1992020674A1 1H-IMIDAZOL-1-YL-METHYL BENZOFURAN DERIVATIVES, WITH THE IMIDAZOLYL MOIETY BEING SUBSTITUTED BY A CYCLOALKYL GROUP 审中-公开
标题翻译： 1H-咪唑烷-1-YL-甲基苯并呋喃衍生物，由环烷基取代的咪唑烷基
公开(公告)号：WO1992020674A1
公开(公告)日：1992-11-26
申请号：PCT/GB1992000888
申请日：1992-05-15
申请人： GLAXO GROUP LIMITED , ROSS, Barry, Clive , MIDDLEMISS, David , SCOPES, David, Ian, Carter , JACK, Torquil, Iain, MacLean , CARDWELL, Kevin, Stuart , DOWLE, Michael, Dennis , JUDO, Duncan, Bruce , WASTON, Stephen, Paul
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D405/14
CPC分类号： C07D249/08 , C07B59/00 , C07D231/12 , C07D233/56 , C07D405/06 , C07D405/14
摘要： The invention provides compounds of general formula (I), or a physiologically acceptable salt, solvate or metabolically labile ester thereof wherein R1 represents a hydrogen atom or a halogen atom or a group selected from C¿1-6?alkyl, C2-6alkenyl, fluoroC1-6alkyl, C1-6alkoxy, -CHO, -CO2H or -COR?2¿; Ar represents the group α; R2 represents a group selected from C¿1-6?alkyl, C2-6alkenyl, C1-6alkoxy or the group -NR?13R14; R3¿ represents a group selected from -CO¿2?H, -NHSO2CF3 or a C-linked tetrazolyl group; R?4 and R5¿ which may be the same or different each independently represent a hydrogen atom or a halogen atom or a C¿1-6?alkyl group; Het represents the group β; R?6¿ represents a hydrogen atom or a group selected from C¿1-6?alkyl, C2-6alkenyl, C1-6alkylthio, C1-6alkoxy, C3-7cycloalkyl or C3-7cycloalkylC1-4alkyl; R?7¿ represents among others and as shown in the examples a group selected from C¿3-7?cycloalkyl or C3-7cycloalkylC1-4alkyl; R?8¿ represents a hydrogen atom or a halogen atom or a group selected from cyano, nitro, C¿1-6?alkyl, C2-6alkenyl, fluoroC1-6alkyl, -(CH2)mR?9¿, -(CH¿2?)nCOR?10¿ or -(CH¿2?)pNR?11COR12; and R9, R10, R11, R12, R13 and R14¿ are a variety of groups and substituents; with the proviso that when R6 represents a hydrogen atom or a group selected from C¿1-6?alkyl; C2-6alkenyl or C1-6alkylthio, R?7¿ represents a group selected from C¿3-7?cycloalkyl or C3-7cycloalkylC1-4alkyl. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

6. 发明申请

WO1997049698A1 PIPERIDINE ACETIC ACID DERIVATIVES AND THEIR USE IN THE TREATMENT OF THROMBOTIC DISORDERS 审中-公开
标题翻译：哌啶酸酸衍生物及其在治疗血栓性疾病中的应用
公开(公告)号：WO1997049698A1
公开(公告)日：1997-12-31
申请号：PCT/EP1997003194
申请日：1997-06-19
申请人： GLAXO GROUP LIMITED , ALLEN, David, George , ELDRED, Colin, David , JUDKINS, Brian, David , MITCHELL, William, Leonard , SCOPES, David, Ian, Carter
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , C07D413/14 , C07D453/02
摘要： The invention relates to compounds of formula (I) or a salt, solvate, or physiologically functional derivative thereof, in which: X is CH2-CH2, CH=CH, or CC; Y is hydrogen, C1-6 alkyl, C1-6 alkenyl, C1-6 alkynyl, C1-6 haloalkyl, C1-6 hydroxyalkyl, aryl, hetaryl, arylC1-4alkyl, or hetarylC1-4alkyl, wherein the aryl and hetaryl groups are optionally substituted by halo, nitro, C1-6 alkyl, C1-6haloalkyl, hydroxy, C1-6 alkoxy, cyano, -C(O)nR , -NR S(O)nR , -C(O)NR R , or -NR R , wherein R and R are independently selected from hydrogen, C1-4 alkyl and C1-4 haloalkyl, and n is 0, 1, or 2; Z is piperidinyl, piperazinyl, or quinuclidinyl; ring B is a 5- or 6-membered aromatic heterocycle fused to ring A and is optionally substituted by a group -L-R wherein: L is a bond, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6 haloalkoxy, S(O)n, C(O)n, or CONR , wherein n is 0, 1, or 2, and R is selected from hydrogen, C1-4 alkyl, and C1-4 haloalkyl; and R is C1-6 alkyl, C4-7 cycloalkyl, C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 alkoxy, cyano, -NR R , aryl or hetaryl, wherein R and R are independently selected from hydrogen, C1-6 alkyl and C1-6 haloalkyl, or together with the nitrogen to which they are bonded form a piperidinyl, morpholino, or pyrolidinyl group, and the aryl and hetaryl groups are optionally substituted by halo, nitro, C1-4 alkyl, hydroxy, C1-4 alkoxy, cyano, -C(O)NR R or -NR R wherein R and R are as defined for R and R above, to processes for their preparation, to pharmaceutical compositions containing such compounds and to their use in medicine, particularly in the treatment of thrombotic disorders.
摘要翻译：本发明涉及式（I）化合物或其盐，溶剂化物或生理功能衍生物，其中：X为CH 2 -CH 2，CH = CH或CC; Y是氢，C 1-6烷基，C 1-6烯基，C 1-6炔基，C 1-6卤代烷基，C 1-6羟烷基，芳基，杂芳基，芳基C 1-4烷基或杂芳基C 1-4烷基，其中芳基和杂芳基是任选的被卤素，硝基，C 1-6烷基，C 1-6卤代烷基，羟基，C 1-6烷氧基，氰基，-C（O）n R 1，-NR 1 S（O）n R 2，-C （O）NR 1 R 2或-NR 1 R 2，其中R 1和R 2独立地选自氢，C 1-4烷基和C 1-4卤代烷基，和 n为0,1或2; Z是哌啶基，哌嗪基或奎宁环基; 环B是与环A稠合的5或6元芳族杂环，并且任选地被基团-LR取代，其中：L是键，C 1-6烷基，C 1-6烷氧基，C 1-6卤代烷基，C 1-6 卤代烷氧基，S（O）n，C（O）n或CONR 3，其中n为0,1或2，R 3选自氢，C 1-4烷基和C 1-4卤代烷基 ; 和R为C 1-6烷基，C 4-7环烷基，C 1-6卤代烷基，C 1-6卤代烷氧基，C 1-6烷氧基，氰基，-NR 4 R 5，芳基或杂芳基，其中R 4和 R 5独立地选自氢，C 1-6烷基和C 1-6卤代烷基，或与它们键合的氮一起形成哌啶基，吗啉代或吡咯烷基，芳基和杂芳基任选被卤素，硝基，C 1-4烷基，羟基，C 1-4烷氧基，氰基，-C（O）NR 6 R 7或-NR 6 R 7其中R 6和R 7 >如上述R 4和R 5所定义，其制备方法，含有这些化合物的药物组合物及其在医药中的用途，特别是治疗血栓形成障碍。

7. 发明申请

WO1994011369A1 ANTIHYPERTENSIVE 5-[(IMIDAZO[4,5-b]PYRIDIN-3-YL)METHYL]BENZOFURAN DERIVATIVES 审中-公开
标题翻译：抗真菌剂5 - [（咪唑并[4,5-b]吡啶-3-基）甲基]苯并呋喃衍生物
公开(公告)号：WO1994011369A1
公开(公告)日：1994-05-26
申请号：PCT/EP1993003157
申请日：1993-11-11
申请人： GLAXO GROUP LIMITED , JUDD, Duncan, Bruce
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The invention relates to the compounds: N-[2-[3-chloro-5-[(5,7-dimethyl-2-ethyl-3H-imidazo[4,5-b]pyridin-3-yl)methyl]-2-benzofuranyl]phenyl]trifluoromethanesulphonamide; 3-[[3-chloro-2-[2-[[(trifluoromethyl)sulphonyl]amino]phenyl]-5-benzofuranyl]methyl]-2-ethyl-7-methyl-3H-imidazo[4,5-b]pyridine-5-methanol; N-[2-[3-chloro-5-[[2-ethyl-5-[2-(hydroxypropyl)]-7-methyl-3H-imidazo[4,5-b]pyridin-3-yl]methyl]-2-benzofuranyl]phenyl]trifluoromethanesulphonamide; 3-[[3-chloro-2-[2-[[(trifluoromethyl)sulphonyl]amino]phenyl]-5-benzofuranyl]methyl]-7-methyl-2-propyl-3H-imidazo[4,5-b]pyridine-5-methanol; N-[2-[3-chloro-5-[[5-[2-(hydroxypropyl)]-7-methyl-2-propyl-3H-imidazo[4,5-b]pyridin-3-yl]methyl]-2-benzofuranyl]phenyl]trifluoromethanesulphonamide; and physiologically acceptable salts and solvates thereof. The invention further relates to processes for their preparation, pharmaceutical compositions containing them, and to their use in medicine, particularly in the treatment of hypertension.
摘要翻译：本发明涉及化合物：N- [2- [3-氯-5 - [（5,7-二甲基-2-乙基-3H-咪唑并[4,5-b]吡啶-3-基）甲基] -2-苯并呋喃基]苯基] trifluoromethanesulphonamide; 3 - [[3-氯-2- [2 - [[（三氟甲基）磺酰基]氨基]苯基] -5-苯并呋喃基]甲基] -2-乙基-7-甲基-3H-咪唑并[4,5-B] 吡啶-5-甲醇; N- [2- [3-氯-5 - [[2-乙基-5- [2-（羟丙基）] - 7-甲基-3H-咪唑并[4,5-b]吡啶-3-基]甲基] -2-苯并呋喃基]苯基] trifluoromethanesulphonamide; 3 - [[3-氯-2- [2 - [[（三氟甲基）磺酰基]氨基]苯基] -5-苯并呋喃基]甲基] -7-甲基-2-丙基-3H-咪唑并[4,5-B] 吡啶-5-甲醇; N- [2- [3-氯-5 - [[5- [2-（羟丙基）] - 7-甲基-2-丙基-3H-咪唑并[4,5-b]吡啶-3-基]甲基] -2-苯并呋喃基]苯基] trifluoromethanesulphonamide; 及其生理上可接受的盐和溶剂合物。本发明还涉及其制备方法，含有它们的药物组合物及其在医药中的用途，特别是用于治疗高血压。

8. 发明申请

WO1997036903A1 PYRROLOPYRROLONE DERIVATIVES AS INHIBITORS OF NEUTROPHIL ELASTASE 审中-公开
标题翻译：作为中性粒细胞酶抑制剂的吡咯烷酮衍生物
公开(公告)号：WO1997036903A1
公开(公告)日：1997-10-09
申请号：PCT/EP1997001530
申请日：1997-03-26
申请人： GLAXO GROUP LIMITED , DOWLE, Michael, Dennis , FINCH, Harry , HARRISON, Lee, Andrew , INGLIS, Graham, George, Adam , JOHNSON, Martin, Redpath , MACDONALD, Simon, John, Fawcett , SHAH, Pritom , SMITH, Robin, Andrew
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07D207/14
摘要： There are described according to the invention compounds of formula (I) (relative stereochemistry indicated), wherein R1, R2, R3 and X are as defined in the specification, together with processes for preparing them, compositions containing them and their use as pharmaceuticals. Compounds of formula (I) are indicated inter alia for the treatment of chronic bronchitis.
摘要翻译：根据本发明描述了式（I）化合物（所示的相对立体化学），其中R1，R2，R3和X如说明书中所定义，以及其制备方法，含有它们的组合物及其作为药物的用途。式（I）的化合物尤其用于治疗慢性支气管炎。

9. 发明申请

WO1992012157A1 BRIDGED CYCLIC KETAL DERIVATIVES 审中-公开
标题翻译： BRIDGED循环酮衍生物
公开(公告)号：WO1992012157A1
公开(公告)日：1992-07-23
申请号：PCT/EP1992000015
申请日：1992-01-05
申请人： GLAXO GROUP LIMITED , SIDEBOTTOM, Philip, James , LESTER, Michael, George , PROCOPIOU, Panayiotis, Alexandrou , WATSON, Nigel, Stephen , KIRK, Barrie, Edward , ROSS, Barry, Clive
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D493/08
CPC分类号： C07D493/08
摘要： Compounds are described of formula (I), wherein R represents a group selected from (a), (b), (c), (d), -CH2C(CH3)=CHCH(CH2OH)CH2Ph, -CH2C(CH2OH)=CHCH(CH3)CH2Ph, -CH2C(=CH2)CH(OH)CH(CH2OH)CH2Ph, -CH2C(=CH2)CH(NHCOCH3)CH(CH3)CH2Ph, -CH2C(CH2NHCOCH3)=CHCH(CH3)CH2Ph and (e) (where the dotted line represents the absence or presence of a single bond, R represents a hydrogen atom or a hydroxyl, acyloxy, C1-6 alkoxy or C1-4 alkyl group, R represents a hydrogen atom and R represents a hydrogen atom or a hydroxyl, C1-6 alkoxy or acyloxy group or CR R forms a group C=O, R represents a hydrogen atom or a C1-4 alkyl group, R represents a hydrogen atom or a methyl group, m represents 1 or 2 and n represents zero or 1); R , R and R may each independently represent a hydrogen atom or a methyl group; and salts thereof. These compounds inhibit the enzyme squalene synthase and/or are intermediates for the preparation of compounds which inhibit the enzyme squalene synthase. Compounds of the invention may be formulated for use in a variety of conditions where a lowering of the level of blood plasma cholesterol in animals would be beneficial and for use in combating fungal infections in animals.
摘要翻译：式（I）化合物，其中R 1表示选自（a），（b），（c），（d），-CH 2 C（CH 3）= CHCH（CH 2 OH）CH 2 Ph，-CH 2 C（ CH 2 CH（CH 2）CH（CH 2）CH（OH）CH（CH 2 OH）CH 2 Ph，-CH 2 C（= CH 2）CH（NHCOCH 3）CH（CH 3）CH 2 Ph，-CH 2 C（CH 2 NHCOCH 3））CH 2 Ph和（e）（其中虚线表示不存在或不存在单键，R 5表示氢原子或羟基，酰氧基，C 1-6烷氧基或C 1-4烷基，R 6，表示氢原子，R 7表示氢原子或羟基，C 1-6烷氧基或酰氧基或CR 6 R 7形成基团C = O，R 8表示氢原子或 C 1-4烷基，R 9表示氢原子或甲基，m表示1或2，n表示0或1）; R 2，R 3和R 4各自独立地表示氢原子或甲基; 及其盐。这些化合物抑制角鲨烯合成酶和/或用于制备抑制酶角鲨烯合酶的化合物的中间体。本发明的化合物可以配制用于各种病症，其中动物血浆中胆固醇水平的降低将是有益的并且用于抵抗动物中的真菌感染。

10. 发明申请

WO1992012158A1 CYCLIC KETAL DERIVATIVES 审中-公开
标题翻译：循环牙膏衍生物
公开(公告)号：WO1992012158A1
公开(公告)日：1992-07-23
申请号：PCT/EP1992000016
申请日：1992-01-05
申请人： GLAXO GROUP LIMITED , SIDEBOTTOM, Philip, James , LESTER, Michael, George , PROCOPIOU, Panayiotis, Alexandrou , WATSON, Nigel, Stephen , BIONDI, Stefano , RAMSAY, Michael, Vincent, John , LIVERMORE, David, George, Hubert , ROSS, Barry, Clive
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D493/08
CPC分类号： C07D493/08
摘要： Compounds are described of formula (Ia), (Ib), wherein R represents a hydrogen atom, a hydroxyl group or a group selected from -OCOCH=CHCH(CH3)(CH2)3CH3, -OCOCH=CHC(CH3)=CHCH(CH3)CH2CH3 or -OCO-X-CH2CH(CH3)CH2CH3 [where X is -CH=CHCH(CH3)-, -CH2CH(OH)CH(CH3)-, -CH=CHC(OH)(CH3)-, -CH2CH(OH)CH2- or -CH2CH2CH(CH3)-]; R represents a hydroxyl group, a group -OCOR or a group -OCO2R (where R is a group selected from C1-8alkyl, aryl, arylC1-4alkyl and C3-8cycloalkyl); R represents a group selected from (a) (where R is a hydrogen atom or an acetyl group), -C(CH3)=CHCH(CH2R )CH2Ph (where R is a hydrogen or a hydroxyl group), -C(CH2OH)=CHCH(CH3)CH2Ph, -C(=CH2)CH(OH)CH(CH2OH)CH2Ph, -C(=CH2)CH(NHCOCH3)CH(CH3)CH2Ph, -C(CH2NHCOCH3)=CHCH(CH3)CH2Ph and (b); R , R and R may each independently represent a hydrogen atom or a methyl group; and salts thereof. These compounds inhibit the enzyme squalene synthase and/or are intermediates for the preparation of compounds which inhibit the enzyme squalene synthase. Compounds of the invention may be formulated for use in a variety of conditions where a lowering of the level of blood plasma cholesterol in animals would be beneficial and for use in combating fungal infections in animals.
摘要翻译：化合物描述为式（Ia），（Ib），其中R 1表示氢原子，羟基或选自-OCOCH = CHCH（CH 3）（CH 2）3 CH 3，-OCOCH = CHC（CH 3） = CHCH（CH3）CH2CH3或-OCO-X-CH2CH（CH3）CH2CH3 [其中X为-CH = CHCH（CH3） - ， - CH2CH（OH）CH（CH3） - ， - CH = CHC（OH）） - ，-CH 2 CH（OH）CH 2 - 或-CH 2 CH 2 CH（CH 3） - ]; R 2表示羟基，-OCOR 7基团或-OCO 2 R 7基团（其中R 7是选自C 1-8烷基，芳基，芳基C 1-4烷基和C 3-8环烷基的基团）; R 3表示选自（a）（其中R 8为氢原子或乙酰基），-C（CH 3）= CHCH（CH 2 R 9）CH 2 Ph（其中R 9为氢或羟基），-C（CH2OH）= CHCH（CH3）CH2Ph，-C（= CH2）CH（OH）CH（CH2OH）CH2Ph，-C（= CH2）CH（NHCOCH3）CH（CH3），-C（CH 2 NHCOCH 3）= CHCH（CH 3）CH 2 Ph和（b）; R 4，R 5和R 6各自独立地表示氢原子或甲基; 及其盐。这些化合物抑制角鲨烯合成酶和/或用于制备抑制酶角鲨烯合酶的化合物的中间体。本发明的化合物可以配制用于各种病症，其中动物血浆中胆固醇水平的降低将是有益的并且用于抵抗动物中的真菌感染。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式