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1. 发明公开

EP1483261A1 PHTHALIMIDE CARBOXYLIC ACID DERIVATIVES 审中-公开
标题翻译：邻苯二甲酸羧酸衍生物
公开(公告)号：EP1483261A1
公开(公告)日：2004-12-08
申请号：EP03743432.1
申请日：2003-03-06
申请人： Oxford GlycoSciences (UK) Ltd,Attn: Mary Gadsden , Scopes, David, Ian, Carter
发明人： COURTNEY, Stephen Martin , HAY, Philip Andrew
IPC分类号： C07D413/10 , A61K31/423 , C07D413/14 , A61P35/00
CPC分类号： C07D413/10 , C07D413/14
摘要： The present invention relates to phthalimide carboxylic acid derivatives of formula (I), methods for their preparation, pharmaceutical compositions containing them and their use in medicine, specifically in the treatment of cancer. (I), wherein X is O or S; R1 is a phthalimide carboxylic acid group of formula (II). R is hydrogen, C1-C6 alkyl, aryl or C1-C3 alkylaryl and R2, R3 and R4 represent various substituents.
摘要翻译：本发明涉及式（I）的邻苯二甲酰亚胺羧酸衍生物，其制备方法，含有它们的药物组合物以及它们在医学中，特别是在癌症治疗中的用途。（I），其中X是O或S; R1是式（II）的邻苯二甲酰亚胺羧酸基团。 R为氢，C1-C6烷基，芳基或C1-C3烷基芳基，R2，R3和R4代表各种取代基。

2. 发明申请

WO2004046122A3 BENZOXAZOLE, BENZTHIAZOLE AND BENZIMIDAZOLE ACID DERIVATIVES AND THEIR USE AS HEPARANASE INHIBITORS 审中-公开
公开(公告)号：WO2004046122A3
公开(公告)日：2004-06-03
申请号：PCT/GB2003/004991
申请日：2003-11-17
申请人： OXFORD GLYCOSCIENCES (UK) LTD , COURTNEY, Stephen, Martin , HAY, Philip, Andrew , SCOPES, David, Ian, Carter
发明人： COURTNEY, Stephen, Martin , HAY, Philip, Andrew , SCOPES, David, Ian, Carter
IPC分类号： C07D263/57
摘要： Compounds of formula (I): wherein R 1 , R 2 and R 3 are independently, hydrogen, halogen, CF 3 , OR 6 , NR 7 R 8 , NR 8 COR 10 , NR 8 SO 2 R 10 or C 1-6 alkyl optionally substituted by hydroxy, C 1-6 alkoxy or NR 7 R 8 ; R 4 is NR 8 CONR 8 R 9 , NR 8 COR 9 , NR 8 SO 2 R 9 , or W-CONR 8 R 9 , where W is a bond, C 1-6 alkylene, C 2-6 alkenylene or C 2-6 alkynylene; and R 5 is Formula (A) methods for their synthesis, pharmaceutical compositions comprising them and their use in medicine, in particular for the treatment of cancer.

3. 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.

4. 发明申请

WO2011144578A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2011144578A1
公开(公告)日：2011-11-24
申请号：PCT/EP2011/057902
申请日：2011-05-16
申请人： SENEXIS LIMITED , HORWELL, David Christopher , SCOPES, David Ian Carter
发明人： HORWELL, David Christopher , SCOPES, David Ian Carter
IPC分类号： C07D413/04 , C07D498/04 , A61K31/538 , A61K31/553 , A61P25/28
CPC分类号： C07D413/04 , C07D498/04
摘要： A compound of formula (I) or a pharmaceutically acceptable salt or prodrug thereof wherein X is N or CH; Q is NR 6 or O; A 1 and A 2 are independently hydrogen or C 1-6 alkyl or may together form a carbonyl group; R 1 and R 2 are independently hydrogen, halogen, CF 3 , CN, OR 7 , OR 8 , NR 8 R 9 , NR 8 COR 10 , NR 8 S0 2 R 10 , S0 2 NR 8 R 9 , SO 2 R 10 or C 1-6 alkyl optionally and independently substituted by one or more of hydroxyl, C 1-6 alkoxy, halogen or NR 8 R 9 ; R 3 is hydrogen, halogen, CF3 or OR 7; R4 is hydrogen, halogen, CF3, OR8, NR8R9, NR8COR10, NR8S02R10 or C1-6 alkyl optionally substituted by hydroxyl, C1-6 alkoxy or NR 8 R 9; or when R 3 and R 4 are positioned ortho and taken together form -0(CH 2 ) m O-, where m is 1-3; R 5 is hydrogen or C 1-6 alkyl optionally substituted by hydroxyl, C 1-6 alkoxy or NR 8 R 9 ; R 6 is hydrogen or C 1-6 alkyl; R 7 is hydrogen or C 1-6 alkyl optionally substituted by OR 8 or NR 8 R 9 ; R 8 is hydrogen, C 1-6 alkyl, optionally substituted by hydroxyl or C 1-6 alkoxy or C 1-3 alkylphenyl wherein said phenyl group is optionally substituted by one or more substituents selected from halogen, C 1-6 alkyl, CF 3 , OR 7 , NR 8 R 9 or OCF 3 ; or the groups R 8 and R 9 when they are attached to a nitrogen atom may together form a 5- or 6-membered ring which optionally contains one further heteroatom selected from NR 7 , S and O said 5 or 6 membered ring being optionally substituted by hydroxyl or C 1-6 alkoxy; or the groups R 8 and R 9 when they are attached to a nitrogen atom may together form an azetidinyl ring optionally substituted by hydroxyl or C 1-6 alkoxy; and R 10 is C 1-6 alkyl or a phenyl group optionally substituted by one or more substituents selected from halogen, C 1-6 alkyl, CF 3 , OCF 3 or OR 7 ; and n is 1 or 2. The use of the compounds in treating amyloid disease is also disclosed.
摘要翻译：式（I）化合物或其药学上可接受的盐或前药，其中X为N或CH; Q是NR6或O; A1和A2独立地是氢或C1-6烷基，或者可以一起形成羰基; R1和R2独立地是氢，卤素，CF3，CN，OR7，OR8，NR8R9，NR8COR10，NR8S02R10，SO2NR8R9，SO2R10或C1-6烷基，任选和独立地被一个或多个羟基，C 1-6烷氧基，卤素或NR 8取代 R9; R 3是氢，卤素，CF 3或OR 7; R4是氢，卤素，CF3，OR8，NR8R9，NR8COR10，NR8S02R10或任选被羟基，C 1-6烷氧基或NR 8 R 9取代的C 1-6烷基; 或当R3和R4相邻并且一起形成-O（CH 2）m O-时，其中m是1-3; R5是氢或任选被羟基取代的C 1-6烷基，C 1-6烷氧基或NR 8 R 9; R6是氢或C1-6烷基; R 7是氢或任选被OR 8或NR 8 R 9取代的C 1-6烷基; R 8是氢，任选地被羟基或C 1-6烷氧基取代的C 1-6烷基或C 1-3烷基苯基，其中所述苯基任选被一个或多个选自卤素，C 1-6烷基，CF 3，OR 7，NR 8 R 9或 OCF 3; 或基团R8和R9可以一起形成5-或6-元环，其任选地含有一个选自NR7，S和O的另外的杂原子，所述5或6元环任选地被羟基或 C 1-6烷氧基或者当基团R8和R9连接到氮原子时可以一起形成任选被羟基或C 1-6烷氧基取代的氮杂环丁烷基环; R 10是C 1-6烷基或任选被一个或多个选自卤素，C 1-6烷基，CF 3，OCF 3或OR 7的取代基取代的苯基; 并且n为1或2.还公开了化合物在治疗淀粉样蛋白病中的用途。

5. 发明申请

WO2004067480A3 SUBSTITUTED PHENYLUREA DERIVATIVES AS HDAC INHIBITORS 审中-公开
标题翻译：取代的苯乙烯衍生物作为HDAC抑制剂
公开(公告)号：WO2004067480A3
公开(公告)日：2004-11-04
申请号：PCT/GB2004000238
申请日：2004-01-22
申请人： OXFORD GLYCOSCIENCES UK LTD , SCOPES DAVID IAN CARTER
发明人： SCOPES DAVID IAN CARTER
IPC分类号： A61K31/423 , A61P35/00 , C07C20060101 , C07D263/56
CPC分类号： C07D263/57
摘要： A series of phenylurea derivatives, further substituted on the phenyl ring by a benzoxazole, benzothiazole or benzimidazole moiety, being inhibitors of histone deacetylase, are accordingly of use in medicine, in particular for the treatment of cancer.

6. 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.

7. 发明申请

WO2008107677A3 THIADIAZOLE AND OXADIAZOLE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS 审中-公开
标题翻译：用于治疗神经损伤性疾病的噻唑并噻唑衍生物
公开(公告)号：WO2008107677A3
公开(公告)日：2008-10-30
申请号：PCT/GB2008000761
申请日：2008-03-06
申请人： SENEXIS LTD , SCOPES DAVID IAN CARTER , CHEESERIGHT TIMOTHY JOHN , VINTER JEREMY GILBERT
发明人： SCOPES DAVID IAN CARTER , CHEESERIGHT TIMOTHY JOHN , VINTER JEREMY GILBERT
IPC分类号： C07D285/135 , A61K31/433 , A61P25/16 , A61P25/28 , C07D271/113
CPC分类号： C07D285/135 , C07D271/113
摘要： A compound of formula (I) or a pharmaceutically acceptable salt or prodrug thereof: wherein X is an oxygen or sulphur atom A is CH(R 6 )-, -O- or NR 7 or when A is NR 7 , then R 1 and NR 7 can together form a ring such that R 1 and R 7 are (CH 2 ) n , where n is 2-4, preferably 2-3; Y is a bond, CH(R 6 )-, -O- or NR 7 or A and Y together form a single bond between the aromatic group and the carbonyl group but when A is-O- then Y is not -O-; R 1 and R 2 are independently hydrogen, halogen, OR 8 , NR 9 R 10 , NR 9 COR 11 , NR 9 SO 2 R 11 or C 1-6 alkyl optionally substituted by fluorine, hydroxyl, C 1-6 alkoxy or NR 9 R 10 ; R 3 is C 1-6 alkyl, C 3-8 cycloalkyl C 4-10 alkylcycloalkyl optionally substituted by hydroxyl, C 1-6 alkoxy or NR 9 R 10 ; R 4 is hydrogen, halogen, CF 3 , OR 9 , NR 9 R 10 , NR 9 COR 11 , NR 9 SO 2 R 11 or C 1-6 alkyl optionally substituted by hydroxyl, C 1-6 alkoxy or NR 9 R 10 ; R 5 is hydrogen, halogen, CF 3 , OR 8 , COOR 9 , CONR 9 R 10 or SO 2 R 11 ; The compounds find use in the treatment of amyloid related diseases, such as Alzheimer disease.
摘要翻译：式（I）化合物或其药学上可接受的盐或前药：其中X是氧或硫原子A是CH（R 6） - ，-O-或NR 7，或者当A为NR 7时，R 1和NR 7可以一起形成环，使得R 1， R 2和R 7是（CH 2）n N，其中n是2-4，优选2-3; Y是键，CH（R 6） - ，-O-或NR 7或A和Y一起在芳族基团和羰基之间形成单键，但是当A为-O-时，Y不为-O-; R 1和R 2各自独立地为氢，卤素，OR 8，NR 9 R 10， NR 9，NR 9，11，12，12，12，12，12，或任选被氟取代的C 1-6烷基，羟基，C 1-6烷氧基或NR 9 R 10 >; R 3是C 1-6烷基，C 3-8环烷基C 4-10烷基环烷基，任选被羟基，C 1-6烷氧基或NR 9 R 10; R 4是氢，卤素，CF 3或OR 9，NR 9，R 10，或者其他的，或者是它们的结合，或者任选被羟基取代的C 1-6烷基，C 1-6烷氧基或NR 9 R 10; R 5是氢，卤素，CF 3或OR 8，COOR 9，CONR 9，或这些化合物可用于治疗淀粉样蛋白相关疾病，如阿尔茨海默病。

8. 发明申请

WO2004111001A1 2-HYDROXYMETHYL-3,4,5-TRIHYDROXY-1-(4-PENTLYOXYBENZYL) PIPERIDINE AS GLUCOSYLCERAMIDE SYNTHASE (GCS) 审中-公开
标题翻译：作为葡萄糖酸合成酶（GCS）的2-羟基甲基-3,4,5-三羟基-1-（4-戊氧基苯基）哌啶
公开(公告)号：WO2004111001A1
公开(公告)日：2004-12-23
申请号：PCT/GB2004/002450
申请日：2004-06-09
申请人： OXFORD GLYCOSCIENCES (UK) LTD , ORCHARD, Michael, Glen , SCOPES, David, Ian, Carter
发明人： ORCHARD, Michael, Glen , SCOPES, David, Ian, Carter
IPC分类号： C07D211/46
CPC分类号： C07D211/46
摘要： The compound 3,4,5-piperidinetriol, 2-(hydroxymethyl)-1-[(4-(pentyloxy)phenyl)methyl]-, (2S,3S,4R,5S), or a pharmaceutically acceptable salt or prodrug thereof, is useful as an inhibitor of glucosylceramide synthase.
摘要翻译：化合物3,4,5-哌啶三醇，2-（羟甲基）-1 - [（4-（戊氧基）苯基）甲基] - ，（2S，3S，4R，5S）或其药学上可接受的盐或前药，可用作葡萄糖神经酰胺合成酶的抑制剂。

9. 发明申请

WO2004046122A2 BENZOXAZOLE, BENZTHIAZOLE AND BENZIMIDAZOLE ACID DERIVATIVES AND THEIR USE AS HEPARANASE INHIBITORS 审中-公开
标题翻译：苯并唑，苯并噻唑和苯并咪唑酸衍生物及其作为肝素酶抑制剂的用途
公开(公告)号：WO2004046122A2
公开(公告)日：2004-06-03
申请号：PCT/GB0304991
申请日：2003-11-17
申请人： OXFORD GLYCOSCIENCES UK LTD , COURTNEY STEPHEN MARTIN , HAY PHILIP ANDREW , SCOPES DAVID IAN CARTER
发明人： COURTNEY STEPHEN MARTIN , HAY PHILIP ANDREW , SCOPES DAVID IAN CARTER
IPC分类号： A61P35/00 , C07D263/56 , C07D263/57 , C07D413/12 , C07D417/12 , C07D417/14 , C07D263/00
CPC分类号： C07D263/57 , C07D413/12 , C07D417/12 , C07D417/14
摘要： Compounds of formula (I): wherein R , R and R are independently, hydrogen, halogen, CF3, OR , NR R , NR COR , NR SO2R or C1-6 alkyl optionally substituted by hydroxy, C1-6 alkoxy or NR R ; R is NR CONR R , NR COR , NR SO2R , or W-CONR R , where W is a bond, C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene; and R is Formula (A) methods for their synthesis, pharmaceutical compositions comprising them and their use in medicine, in particular for the treatment of cancer.
摘要翻译：式（I）化合物：其中R 1，R 2和R 3独立地为氢，卤素，CF 3，OR 6，NR 7 R 8，NR 8 COR NR 8 SO 2 R 10或任选被羟基，C 1-6烷氧基或NR 7 R 8取代的C 1-6烷基; R 4是NR 8 CONR 8 R 9，NR 8 COR 9，NR 8 SO 2 R 9或W-CONR 8 R 9，其中W 是键，C1-6亚烷基，C2-6亚烯基或C2-6亚炔基; 并且R 5是式（A）的合成方法，包含它们的药物组合物以及它们在医学中的用途，特别是用于治疗癌症。

10. 发明申请

WO2009044160A1 PYRIDINE DERIVATIVES FOR THE TREATMENT OF AMYLOID-RELATED DISEASES 审中-公开
标题翻译：用于治疗类淀粉样相关疾病的吡啶衍生物
公开(公告)号：WO2009044160A1
公开(公告)日：2009-04-09
申请号：PCT/GB2008/003359
申请日：2008-10-06
申请人： SENEXIS LIMITED , SCOPES, David, Ian, Carter , HORWELL, David, Christopher
发明人： SCOPES, David, Ian, Carter , HORWELL, David, Christopher
IPC分类号： A61P25/28 , A61P25/16 , A61P3/10 , A61K31/4412 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/496 , C07D213/63 , C07D401/12
CPC分类号： C07D213/74
摘要： a compound of formula (I) or a pharmaceutically acceptable salt or prodrug thereof: wherein X and Y are independently NR 5 or O; W and Z are independently a bond or (CH2)mCH(R7)(CH2)n; m = 0-1, n = 0-2; R is hydrogen or halogen; R 1 and R 2 are independently selected from hydrogen, halogen, CF 3 , CN, OR 8 , NR 9 R 10 , NR 9 COR 11 , NR 9 SO 2 R 11 or C 1-6 alkyl optionally substituted by hydroxyl, C 1-6 alkoxy or NR 9 R 10 ; R 3 is hydrogen, halogen, CF 3, CN, OR 8 , SR 8 or SO 2 R 11 .; R 4 is hydrogen, halogen, CF 3 , OR 9 , NR 9 R 10 , NR 9 COR 11 , NR 9 SO 2 R 11 or C 1-6 alkyl optionally substituted by hydroxyl, C 1-6 alkoxy or NR 9 R 10 ; R 5 is hydrogen or C 1-6 alkyl optionally substituted by hydroxyl, C 1-6 alkoxy or NR 9 R 10 ;R6 is hydrogen, fluorine, C1-6 alkyl, or C1-6 alkoxy; R 6 is hydrogen, fluorine, C 1-6 alkyl, or C 1-6 alkoxy; R 7 is hydrogen, C 1-6 alkyl, phenyl or C 1-3 alkylphenyl wherein said phenyl groups are optionally substituted by one or more substituents selected from halogen, C 1-6 alkyl, CF 3 , OCF 3 or OR 9 ; R 8 is hydrogen or C 1-6 alkyl optionally substituted by fluorine, C 1-6 alkoxy or NR 9 R 10 ; R 9 is hydrogen, C 1-6 alkyl or C 1-3 alkylphenyl wherein said phenyl group is optionally substituted by one or more substituents selected from halogen, C 1-6 alkyl, CF 3 , OR 8 , NR 9 R 10 Or OCF 3 ; R 10 is hydrogen, C 1-6 alkyl, C 1-6 alkenyl, phenyl or C 1-3 alkylphenyl wherein said phenyl groups are optionally substituted by one or more substituents selected from halogen, C 1-6 alkyl, CF 3 , OR 8 or OCF 3 ; or the groups R 9 and R 10 when they are attached to a nitrogen atom may together form a 5- or 6-membered ring which optionally contains one further heteroatom selected from NR 9 , S and O; and R 11 is C 1-6 alkyl or a phenyl group optionally substituted by one or more substituents selected from halogen, C 1-6 alkyl, CF 3 , OCF 3 or OR 8 is provided. The compounds are useful in treating amyloid related diseases.
摘要翻译：式（I）化合物或其药学上可接受的盐或前药：其中X和Y独立地是NR 5或O; W和Z独立地是键或（CH 2）m CH（R 7）（CH 2）n; m = 0-1，n = 0-2; R是氢或卤素; R 1和R 2独立地选自氢，卤素，CF 3，CN，OR 8，NR 9 R 10，NR 9 COR 11，NR 9 SO 2 R 11或任选被羟基，C 1-6烷氧基或NR 9 R 10取代的C 1-6烷基; R3是氢，卤素，CF3，CN，OR8，SR8或SO2R11。 R4是氢，卤素，CF3，OR9，NR9R10，NR9COR11，NR9SO2R11或任选被羟基，C 1-6烷氧基或NR 9 R 10取代的C 1-6烷基; R5是氢或任选被羟基，C 1-6烷氧基或NR 9 R 10取代的C 1-6烷基; R 6是氢，氟，C 1-6烷基或C 1-6烷氧基; R6是氢，氟，C1-6烷基或C1-6烷氧基; R 7是氢，C 1-6烷基，苯基或C 1-3烷基苯基，其中所述苯基任选被一个或多个选自卤素，C 1-6烷基，CF 3，OCF 3或OR 9的取代基取代; R8是氢或任选被氟取代的C 1-6烷基，C 1-6烷氧基或NR 9 R 10; R9是氢，C1-6烷基或C1-3烷基苯基，其中所述苯基任选被一个或多个选自卤素，C 1-6烷基，CF 3，OR 8，NR 9 R 10 OCF 3的取代基取代; R 10是氢，C 1-6烷基，C 1-6烯基，苯基或C 1-3烷基苯基，其中所述苯基任选被一个或多个选自卤素，C 1-6烷基，CF 3，OR 8或OCF 3的取代基取代; 或当基团连接到氮原子时，基团R 9和R 10可以一起形成5-或6-元环，其任选地含有一个选自NR 9，S和O的另外的杂原子; 并且R 11是C 1-6烷基或任选被一个或多个选自卤素，C 1-6烷基，CF 3，OCF 3或OR 8的取代基取代的苯基。该化合物可用于治疗淀粉样蛋白相关疾病。

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