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1. 发明申请

WO2008078100A3 TRICYCLIC AMINE DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白酪氨酸激酶抑制剂的三元胺衍生物
公开(公告)号：WO2008078100A3
公开(公告)日：2008-11-13
申请号：PCT/GB2007004960
申请日：2007-12-21
申请人： ASTEX THERAPEUTICS LTD , BERDINI VALERIO , BESONG GILBERT EBAI , CALLAGHAN OWEN , CARR MARIA GRAZIA , CONGREVE MILES STUART , GILL ADRIAN LIAM , GRIFFITHS-JONES CHARLOTTE MARY , MADIN ANDREW , MURRAY CHRISTOPHER WILLIAM , NIJJAR RAJDEEP KAUR , O'BRIEN MICHAEL ALISTAIR , PIKE ANDREW , SAXTY GORDON , TAYLOR RICHARD DAVID , VICKERSTAFFE EMMA
发明人： BERDINI VALERIO , BESONG GILBERT EBAI , CALLAGHAN OWEN , CARR MARIA GRAZIA , CONGREVE MILES STUART , GILL ADRIAN LIAM , GRIFFITHS-JONES CHARLOTTE MARY , MADIN ANDREW , MURRAY CHRISTOPHER WILLIAM , NIJJAR RAJDEEP KAUR , O'BRIEN MICHAEL ALISTAIR , PIKE ANDREW , SAXTY GORDON , TAYLOR RICHARD DAVID , VICKERSTAFFE EMMA
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to new bicyclic heterocyclic derivative compounds of Formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. The compounds of Formula (I) are inhibitors of FGFR, VEGFR or PDGFR.
摘要翻译：本发明涉及式（I）的新的双环杂环衍生物化合物，包含所述化合物的药物组合物以及所述化合物在治疗疾病中的用途。癌症。式（I）的化合物是FGFR，VEGFR或PDGFR的抑制剂。

2. 发明申请

WO2008007123A3 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2008007123A3
公开(公告)日：2008-02-28
申请号：PCT/GB2007002655
申请日：2007-07-13
申请人： ASTEX THERAPEUTICS LTD , NOVARTIS AG , CONGREVE MILES STUART , GILL ADRIAN LIAM , HOWARD STEVEN , MORTENSON PAUL NEIL , BESONG GILBERT EBAI
发明人： CONGREVE MILES STUART , GILL ADRIAN LIAM , HOWARD STEVEN , MORTENSON PAUL NEIL , BESONG GILBERT EBAI
IPC分类号： C07D401/12 , A61K31/4155 , A61P25/28 , A61P31/10 , A61P31/12 , A61P35/00 , A61P37/00 , C07D401/14 , C07D417/12 , C07D497/04
CPC分类号： C07D417/12 , C07D401/12 , C07D401/14 , C07D513/04
摘要： The invention provides a cyclin dependent kinase (e.g. cdk-4 kinase) inhibitor of the formula (I) or a salt, tautomer, solvate or N-oxide thereof; wherein R 1 is an optionally substituted monocyclic or bicyclic aryl or heteroaryl group containing 0-2 heteroatoms selected from O, N and S wherein the optional substituents are selected from halogen, C 1-4 alkyl, C 1-4 alkoxy, C 3-4 cycloalkyl and cyano, and wherein the C 1-4 alkyl and C 1-4 alkoxy groups are each optionally further substituted by C 1-2 alkoxy or one or more halogen atoms; and E is a group E1, E2, E3 or E4: formulae E1, E2, E3, E4 wherein n, q, A5 B, T, U, V, W, Z, R 2 , R 5 , R 6 and R 7 are as defined in the claims.
摘要翻译：本发明提供式（I）的细胞周期蛋白依赖性激酶（例如cdk-4激酶）抑制剂或其盐，互变异构体，溶剂化物或N-氧化物; 其中R 1是任选取代的含有0-2个选自O，N和S的杂原子的单环或双环芳基或杂芳基，其中任选的取代基选自卤素，C 1-4烷基，烷基，C 1-4烷氧基，C 3-4环烷基和氰基，并且其中C 1-4烷基和C 1-4烷基 1-4烷氧基各自任选进一步被C 1-2烷氧基或一个或多个卤素原子取代; 和E是基团E1，E2，E3或E4：式E1，E2，E3，E4其中n，q，A5 B，T，U，V，W，Z，R 2，R R5，R6和R7如权利要求中所定义。

3. 发明申请

WO2006123165A3 PYRIMIDINE DERIVATIVES AS HSP90 INHIBITORS 审中-公开
标题翻译：吡嗪衍生物作为HSP90抑制剂
公开(公告)号：WO2006123165A3
公开(公告)日：2007-10-11
申请号：PCT/GB2006001851
申请日：2006-05-19
申请人： ASTEX THERAPEUTICS LTD , CHESSARI GIANNI , CONGREVE MILES STUART , CALLAGHAN OWEN , COWAN SUZANNA RUTH , MURRAY CHRISTOPHER WILLIAM , WOOLFORD ALISON JO-ANNE , O'BRIEN MICHAEL ALISTAIR , WOODHEAD ANDREW JAMES
发明人： CHESSARI GIANNI , CONGREVE MILES STUART , CALLAGHAN OWEN , COWAN SUZANNA RUTH , MURRAY CHRISTOPHER WILLIAM , WOOLFORD ALISON JO-ANNE , O'BRIEN MICHAEL ALISTAIR , WOODHEAD ANDREW JAMES
IPC分类号： C07D239/42 , C07D251/18 , C07D401/04 , C07D403/04
CPC分类号： C07D413/04 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/04 , C07D409/04
摘要： The invention provides a compound for use as an inhibitor of Hsp90, the compound having the formula (I): or salts, tautomers, solvates or N-oxides thereof; wherein: A is N or a group CR 3 ; R 1 is a monocyclic or bicyclic carbocyclic or heterocyclic ring of 5 to 10 ring members of which up to two ring members may be heteroatoms selected from N, O and S and the remainder are carbon atoms, the carbocyclic or heterocyclic ring being optionally substituted by one or more substituent groups independently selected from R 10 ; and R 2 , R 3 and R 10 are as defined in the claims.
摘要翻译：本发明提供了用作Hsp90抑制剂的化合物，具有式（I）的化合物：或其盐，互变异构体，溶剂合物或N-氧化物; 其中：A为N或基团CR 3; R 1是5至10个环成员的单环或双环碳环或杂环，其中多至两个环成员可以是选自N，O和S的杂原子，其余是碳原子，碳环或杂环任选被一个或多个独立地选自R 10的取代基取代; R 2，R 3和R 10如权利要求中所定义。

4. 发明申请

WO2006109085A8 HYDROXYBENZAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF HSP90 审中-公开
标题翻译：羟基苯甲酸衍生物及其作为HSP90的抑制剂
公开(公告)号：WO2006109085A8
公开(公告)日：2007-05-18
申请号：PCT/GB2006001382
申请日：2006-04-13
申请人： ASTEX THERAPEUTICS LTD , CHESSARI GIANNI , CONGREVE MILES STUART , NAVARRO EVA FIGUEROA , FREDERICKSON MARTYN , MURRAY CHRISTOPHER , WOOLFORD ALISON JO-ANNE , CARR MARIA GRAZIA , DOWNHAM ROBERT , O'BRIEN MICHAEL ALISTAIR , PHILLIPS THERESA RACHEL , WOODHEAD ANDREW JAMES
发明人： CHESSARI GIANNI , CONGREVE MILES STUART , NAVARRO EVA FIGUEROA , FREDERICKSON MARTYN , MURRAY CHRISTOPHER , WOOLFORD ALISON JO-ANNE , CARR MARIA GRAZIA , DOWNHAM ROBERT , O'BRIEN MICHAEL ALISTAIR , PHILLIPS THERESA RACHEL , WOODHEAD ANDREW JAMES
IPC分类号： C07D209/44 , A61K31/403 , A61K31/438 , A61K31/439 , C07D209/08 , C07D215/08 , C07D401/04 , C07D401/12 , C07D471/04 , C07D471/10 , C07D491/08 , C07D491/10
CPC分类号： C07D401/12 , C07C65/21 , C07D209/08 , C07D209/44 , C07D215/08 , C07D217/06 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D471/04 , C07D471/10 , C07D491/08 , C07D491/10
摘要： The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R 1 is hydroxy or hydrogen; R 2 is hydroxy; methoxy or hydrogen; provided that at least one of R 1 and R 2 is hydroxy; R 3 is selected from hydrogen; halogen; cyano; optionally substituted C 1-5 hydrocarbyl and optionally substituted C 1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group -(O)n-R 7 where n is 0 or 1 and R 7 is an optionally substituted acyclic C 1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C 1-5 hydrocarbyl- amino; or R 3 and R 4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR 5 R 6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.
摘要翻译：本发明提供式（I）的化合物：或其盐，互变异构体，溶剂合物和N-氧化物; 其中R 1是羟基或氢; R 2是羟基; 甲氧基或氢; 条件是R 1和R 2中的至少一个是羟基; R 3选自氢; 卤素; 氰基; 任选取代的C 1-5烃基和任选取代的C 1-5 - 烃氧基; R4选自氢; 其中n为0或1且R 7为 - 任选取代的无环C 1-5 - 烃基的基团 - （O）n R 7，或具有3-7个环成员的单环碳环或杂环基; 卤素; 氰基; 羟基; 氨基; 和任选取代的单或二-C 1-5烃基 - 氨基; 或R 3和R 4一起形成5至7个环成员的单环碳环或杂环; 并且NR 5 R 6形成具有8至12个环成员的任选取代的双环杂环基，其中多达5个环成员是选自氧，氮和硫的杂原子。该化合物具有作为Hsp90抑制剂的活性。

5. 发明申请

WO2006109075A3 HYDROXYBENZAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF HSP90 审中-公开
标题翻译：羟基苯甲酸衍生物及其作为HSP90的抑制剂
公开(公告)号：WO2006109075A3
公开(公告)日：2006-11-30
申请号：PCT/GB2006001358
申请日：2006-04-13
申请人： ASTEX THERAPEUTICS LTD , CHESSARI GIANNI , CONGREVE MILES STUART , NAVARRO EVA FIGUEROA , FREDERICKSON MARTYN , MURRAY CHRISTOPHER , WOOLFORD ALISON JO-ANNE , CARR MARIA GRAZIA , O'BRIEN MICHAEL ALISTAIR , WOODHEAD ANDREW JAMES
发明人： CHESSARI GIANNI , CONGREVE MILES STUART , NAVARRO EVA FIGUEROA , FREDERICKSON MARTYN , MURRAY CHRISTOPHER , WOOLFORD ALISON JO-ANNE , CARR MARIA GRAZIA , O'BRIEN MICHAEL ALISTAIR , WOODHEAD ANDREW JAMES
IPC分类号： A61K31/401 , A61K31/166 , A61K31/445 , A61K31/5375 , C07C233/65 , C07C233/66 , C07D207/10 , C07D211/22 , C07D211/34 , C07D211/42 , C07D211/56 , C07D265/30 , C07D295/02 , C07D295/18 , C07D309/14
CPC分类号： C07D401/12 , C07C65/21 , C07D209/08 , C07D209/44 , C07D215/08 , C07D217/06 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D471/04 , C07D471/10 , C07D491/08 , C07D491/10
摘要： The invention provides a compound for use as an inhibitor of Hsp90, the compound having the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R 1 is hydroxy or hydrogen; R 2 is hydroxy; methoxy or hydrogen; provided that at least one of R 1 and R 2 is hydroxy; R 3 is selected from hydrogen; halogen; cyano; C 1-5 hydrocarbyl and C 1-5 hydrocarbyloxy; wherein the C 1-5 hydrocarbyl and C 1-5 hydrocarbyloxy moieties are each optionally substituted by one or more substituents selected from hydroxy, halogen, C 1-2 alkoxy, amino, mono- and di-C 1-2 alkylamino, and aryl and heteroaryl groups of 5 to 12 ring members; R 4 is selected from hydrogen; a group -(O) n -R 7 where n is 0 or 1 and R 7 is an acyclic C 1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and mono- or di-C 1-5 hydrocarbyl-amino, wherein the acyclic Ci-5 hydrocarbyl group and the mono and di-C 1-5 hydrocarbylamino moieties in each instance are optionally substituted by one or more substituents selected from hydroxy, halogen, C 1-2 alkoxy, amino, mono- and di-C 1-2 alkylamino, and aryl and heteroaryl groups of 5 to 12 ring members; or R 3 and R 4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and R 5 and R 6 are as defined in the claims.
摘要翻译：本发明提供用作Hsp90抑制剂的化合物，具有式（I）的化合物：或其盐，互变异构体，溶剂化物和N-氧化物; 其中R 1是羟基或氢; R 2是羟基; 甲氧基或氢; 条件是R 1和R 2中的至少一个是羟基; R 3选自氢; 卤素; 氰基; C 1-5烃基和C 1-5氢烃氧基; 其中C 1-5烷基和C 1-5 - 烃基氧基部分各自任选被一个或多个选自羟基，卤素，C 1-2 烷氧基，氨基，单和二-C 1-12烷基氨基，以及5至12个环成员的芳基和杂芳基; R 4选自氢; 其中n为0或1且R 7为无环C 1-5的基团 - （O）N - ， - R 7 具有3〜7个环成员的单环碳环或杂环基; 卤素; 氰基; 羟基; 氨基; 和单 - 或二-C 1-5烃基 - 氨基，其中每个中的非环式C 1-5烃基和单和二-C 1-5烃基氨基部分实例任选被一个或多个选自羟基，卤素，C 1-12烷氧基，氨基，单和二-C 1-2烷基氨基的取代基取代，和芳基和5-12个环成员的杂芳基; 或R 3和R 4一起形成5至7个环成员的单环碳环或杂环; R 5和R 6如权利要求中所定义。

6. 发明申请

WO2008044027A3 PHARMACEUTICAL COMPOUNDS HAVING HSP90 INHIBITORY OR MODULATING ACTIVITY 审中-公开
标题翻译：具有HSP90抑制或调节活性的药物化合物
公开(公告)号：WO2008044027A3
公开(公告)日：2008-06-19
申请号：PCT/GB2007003860
申请日：2007-10-12
申请人： ASTEX THERAPEUTICS LTD , CONGREVE MILES STUART , FAZAL LYNDSEY HELEN , FREDERICKSON MARTYN , MURRAY CHRISTOPHER WILLIAM , O'BRIEN MICHAEL ALISTAIR , WOODHEAD ANDREW JAMES , LYONS JOHN FRANCIS , THOMPSON NEIL THOMAS
发明人： CONGREVE MILES STUART , FAZAL LYNDSEY HELEN , FREDERICKSON MARTYN , MURRAY CHRISTOPHER WILLIAM , O'BRIEN MICHAEL ALISTAIR , WOODHEAD ANDREW JAMES , LYONS JOHN FRANCIS , THOMPSON NEIL THOMAS
IPC分类号： C07D209/08 , A61K31/438 , C07D209/44 , C07D215/08 , C07D401/04 , C07D401/12 , C07D419/10 , C07D471/04 , C07D471/10 , C07D491/08 , C07D491/10
CPC分类号： C07D403/06 , C07D209/08 , C07D209/44 , C07D215/08 , C07D215/14 , C07D217/06 , C07D401/04 , C07D401/12 , C07D401/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D491/08 , C07D491/10 , C07D491/107 , C07D491/18
摘要： The invention provides a compound for use in medicine, the compound being a compound of the formula (Vl 0 ) or a salt, solvate, tautomer or N-oxide thereof: wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n is 0, 1, 2 or 3; R 1 : is" hydrogen, hydroxy, or O-R z; R 2a is hydroxy, methoxy or O-R z; provided that at least one of R 1 and R 2a is O-R z; R z is L p -R p1 ; SO 3 H; a glucuronide residue; a mono-, di- or tripeptide residue; or; L p is a bond, C=O, (C=O)O, (C=O)NR p1 or S(O) x NR p1 ; x is 1 or 2; R p1 is hydrogen or a an optionally substituted C 1-25 hydrocarbyl group containing 0, 1 or 2 carbocyclic rings and 0, 1, 2, 3, 4, 5 or 6 carbon-carbon multiple bonds, provided that R p1 is not hydrogen when L p is a bond, C=O or (C=O)O; and provided also that O-R z does not contain an 0-0 moiety; and excluding compounds wherein R1 is hydroxy and R2a is methoxy; Rp2 and Rp3 are the same or different and each is a group R p1; and R 3 , R 4a , R 8 and R 10 are defined in the claims. The compounds of formula (Vl0) are pro-drugs of parent compounds wherein R 1 and/or R 2a are hydroxy, wherein the parent compounds have Hsp90 inhibiting activity.
摘要翻译：本发明提供了一种用于医药的化合物，该化合物为下式化合物：其盐，溶剂化物，互变异构体或N-氧化物：其中双环基团选自：结构C1，C5和C6：其中n为0,1,2或3; R 1是氢，羟基或OR z; R 2是羟基，甲氧基或OR z; O / O >条件是R 1和R 2 2中的至少一个是OR z; R z是L SUP > p p> SO 3 H;葡糖苷酸残基;单 - ，二 - 或三肽残基;或●L < / SUP>是键，C = O，（C = O）O，（C = O）NR P1或S（O）x NR 6 x为1或2; R p1为氢或任选取代的含0,1或2个碳环的C 1-25烃基和0 ，1,2,3,4,5或6个碳 - 碳多重键，条件是当P = O时，R p2不是氢，C = O或（C = O）O;并且也提供OR 0不含0-0部分;并且不包括其中R 1是羟基并且R 2a是甲氧基的化合物; Rp2和Rp3相同或不同，每个是基团R p1; R 3和R 3，R 4a，R 8和R 10 是定义在权利要求中。式（V10）化合物是其中R 1和/或R 2a的羟基的母体化合物的前体药物，其中母体化合物具有Hsp90抑制活性。

7. 发明申请

WO03087087A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO03087087A2
公开(公告)日：2003-10-23
申请号：PCT/GB0301507
申请日：2003-04-08
申请人： ASTEX TECHNOLOGY LTD , FREDERICKSON MARTYN , GILL ADRIAN LIAM , PADOVA ALESSANDRO , CONGREVE MILES STUART
发明人： FREDERICKSON MARTYN , GILL ADRIAN LIAM , PADOVA ALESSANDRO , CONGREVE MILES STUART
IPC分类号： A61K31/404 , A61K31/437 , A61K31/4439 , A61K31/506 , A61K31/5377 , A61P1/04 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/14 , A61P19/02 , A61P19/06 , A61P19/08 , A61P21/00 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/06 , A61P31/18 , A61P33/06 , A61P35/00 , A61P37/06 , A61P43/00 , C07D209/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D471/04
CPC分类号： C07D401/06 , A61K31/404 , C07D209/08 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12
摘要： The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by a p38 MAP kinase such as rheumatoid arthritis and osteoarthritis; the compound being of the general formula (I): wherein U, T, V and W are each a nitrogen atom or a group CR provided that no more than three of U, T, V and W are nitrogen atoms; R is hydrogen, C1-4 hydrocarbyl, halogen or a group -A-R ; R is hydrogen, C1-4 hydrocarbyl or a group -A-R ; provided that only one of R and R is a group -A-R ; R is hydrogen, C1-4 hydrocarbyl or halogen; A is a carbon- or heteroatom-containing linker group having a linking chain length of one or two atoms; R is a monocyclic or bicyclic heteroaryl group containing from five to twelve ring members; each group R is independently selected from hydrogen, hydroxy, halogen, nitro, cyano, a monocyclic heterocyclic group having up to seven ring members, a group N(R )2, a group C(O)N(R )2, a group S02N(R )2, a group R -R and a group Y; provided that no more than one group Y is present; R is a bond, O, S, SO, S02, NH or N-C1-4 hydrocarbyl; R is C1-8 hydrocarbyl optionally interrupted by O, S, SO, SO2, NH or N-C1- 4 hydrocarbyl and optionally substituted by one or more substitutents selected from hydroxy, amino, mono- or di-C1-4 hydrocarbylamino, C1 -4 hydrocarbyloxy, oxo, C1 -4 hydrocarbylthio and halogen; each group R is independently selected from hydrogen, C1-4 alkyl, C1-4 acyl and C 1-4 alkylsulphonyl; each group R is independently selected from hydrogen and C1-4 hydrocarbyl; Y is a group -N(R )-C(O)-R or -N(R )_SO2-R ; R is hydrogen, C1-4 hydrocarbyl or a group C(O)-R or S02-R ; R is selected from C1-l0 hydrocarbyl, CI-10 hydrocarbylamino, CI-10 hydrocarbylthio, C1-l0 hydrocarbyloxy, and aryl, arylamino, arylthio and aryloxy groups, the aryl moieties of which are carbocyclic or heterocyclic and have from five to twelve ring members, each substituent group R being optionally substituted by one or more groups R other than Y; or R and R together with the nitrogen and carbon or sulphur atoms to which they are attached are linked to form a ring structure of 4 to 7 ring members; wherein R is other than a 2-(2,4-diamino-6-triazinyl)ethyl group when, in combination, U, T, V and W are all CH, and R and R are both hydrogen; and provided that when the group -A-R contains an acidic substitituent group selected from carboxylic, phosphonic and sulphonic acids and tetrazoles, or contains a -C(O)NSO2- group, or when -A- is -C(O)N- and the nitrogen atom of the group A is linked directly to a furan or thiophene ring, then either R is -A-R and both R
摘要翻译：本发明提供了一种用于预防或治疗p38 MAP激酶介导的疾病状态或病症的化合物，例如类风湿性关节炎和骨关节炎; 所述化合物为通式（I）：其中U，T，V和W各自为氮原子或基团CR 4，条件是U，T，V和W中不超过三个为氮原子; R 0是氢，C 1-4烃基，卤素或基团-A-R 3; R 1是氢，C 1-4烃基或基团-A-R 3; 条件是R 0和R 1中仅有一个为-A-R 3基团; R 2是氢，C 1-4烃基或卤素; A是具有一个或两个原子的连接链长度的含碳或杂原子的连接基团; R 3是含有5至12个环成员的单环或双环杂芳基; 每个基团R 4独立地选自氢，羟基，卤素，硝基，氰基，具有至多七个环成员的单环杂环基，基团N（R 5）2，基团C（O）N（ R 6）2，SO 2 N（R 6）2，基团R a -R b和基团Y; 只要不存在不止一个Y组; R a是键，O，S，SO，SO 2，NH或N-C 1-4烃基; R b是任选地被O，S，SO，SO 2，NH或N-C 1-4烃基中断的C 1-8烃基，并任选被一个或多个选自羟基，氨基，单或二-C 1-4的取代基取代烃基氨基，C 1-4烃氧基，氧代，C 1-4烃基硫基和卤素; 每个基团R 5独立地选自氢，C 1-4烷基，C 1-4酰基和C 1-4烷基磺酰基; 每个基团R 6独立地选自氢和C 1-4烃基; Y是基团-N（R 7）-C（O）-R 8或-N（R 7）SO 2 -R 8; R 7是氢，C 1-4烃基或C（O）-R 8或SO 2 -R 8; R 8选自C 1-10烃基，C 1-10烃基氨基，C 1-10烃基硫代，C 1-10烃氧基和芳基，芳基氨基，芳硫基和芳氧基，其芳基部分是碳环或杂环的并具有五至12个环成员，每个取代基R 8任选被一个或多个除Y以外的R 4基团取代; 或R 7和R 8与它们所连接的氮原子和碳原子一起连接形成4至7个环成员的环结构; 当组合U，T，V和W均为CH时，R 0不是2-（2,4-二氨基-6-三嗪基）乙基，R 1和R 2均为都是氢; 并且条件是当基团-AR 3含有选自羧酸，膦酸和磺酸和四唑的酸性取代基时，或含有-C（O）NSO 2 - 基团，或当-A-是-C（O） N-和氮原子的基团A直接连接到呋喃或噻吩环，那么R 1是-AR 3，并且两个R

8. 发明申请

WO2007058602A2 NEW COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：WO2007058602A2
公开(公告)日：2007-05-24
申请号：PCT/SE2006001317
申请日：2006-11-20
申请人： ASTRAZENECA AB , ASTEX THERAPEUTICS LTD , BERG STEFAN , BURROWS JEREMY , CHESSARI GIANNI , CONGREVE MILES STUART , HEDSTROEM JOHAN , HELLBERG SVEN , HOEGDIN KATHARINA , KIHLSTROEM JACOB , KOLMODIN KARIN , LINDSTROEM JOHAN , MURRAY CHRISTOPHER , PATEL SAHIL
发明人： BERG STEFAN , BURROWS JEREMY , CHESSARI GIANNI , CONGREVE MILES STUART , HEDSTROEM JOHAN , HELLBERG SVEN , HOEGDIN KATHARINA , KIHLSTROEM JACOB , KOLMODIN KARIN , LINDSTROEM JOHAN , MURRAY CHRISTOPHER , PATEL SAHIL
IPC分类号： C07D233/88 , A61K31/4168 , A61K31/4174 , A61K31/4178 , A61K31/427 , A61K31/4439 , A61K31/4725 , A61K31/497 , A61K31/506 , A61K31/538 , A61P25/16 , A61P25/28 , C07D233/86 , C07D401/04 , C07D401/10 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/10 , C07D413/10 , C07D417/04
CPC分类号： C07D233/88 , C07C25/22 , C07C25/24 , C07C39/373 , C07C43/1747 , C07C43/23 , C07C47/575 , C07C49/792 , C07C49/813 , C07C49/83 , C07C49/84 , C07D209/08 , C07D217/06 , C07D233/86 , C07D265/36 , C07D307/79 , C07D339/08 , C07D401/04 , C07D401/10 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/10 , C07D409/06 , C07D409/10 , C07D413/06 , C07D413/10 , C07D417/04 , C07F7/1856
摘要： This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
摘要翻译：本发明涉及具有以下结构式I的新化合物及其药学上可接受的盐，组合物和使用方法。这些新化合物提供了认知障碍，阿尔茨海默病，神经变性和痴呆症的治疗或预防。

9. 发明申请

WO2007058583A3 NOVEL 2-AMINO-HETEROCYCLES USEFUL IN THE TREATMENT OF ABETA-RELATED PATHOLOGIES 审中-公开
标题翻译：用于治疗与ABETA相关的病理学的新型2-氨基 - 杂环化合物
公开(公告)号：WO2007058583A3
公开(公告)日：2007-07-05
申请号：PCT/SE2006001283
申请日：2006-11-13
申请人： ASTRAZENECA AB , ASTEX THERAPEUTICS LTD , ALBERT JEFFREY , CHESSARI GIANNI , CONGREVE MILES STUART , EDWARDS PHIL , MURRAY CHRISTOPHER , PATEL SAHIL , SYLVESTER MARK
发明人： ALBERT JEFFREY , CHESSARI GIANNI , CONGREVE MILES STUART , EDWARDS PHIL , MURRAY CHRISTOPHER , PATEL SAHIL , SYLVESTER MARK
IPC分类号： C07D217/22 , A61K31/4365 , A61K31/472 , A61K31/517 , A61K31/536 , A61P25/28 , C07D239/94 , C07D265/20 , C07D401/10 , C07D513/04
CPC分类号： C07D217/22 , C07D239/94 , C07D265/20 , C07D401/04 , C07D495/04
摘要： This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
摘要翻译：本发明涉及具有以下结构式I的新化合物及其药学上可接受的盐，组合物和使用方法。这些新化合物提供认知障碍，阿尔茨海默病，神经变性和痴呆症的治疗或预防。

10. 发明申请

WO02055496A8 ARYL PIPERIDINE AND PIPERAZINE DERIVATIVES AS INDUCERS OF LDL-RECEPTOR EXPRESSION 审中-公开
标题翻译：作为低密度脂蛋白受体表达的诱导剂的ARYL PIPERIDINE AND PIPERAZINE DERIVATIVES
公开(公告)号：WO02055496A8
公开(公告)日：2003-07-17
申请号：PCT/GB0100158
申请日：2001-01-15
申请人： GLAXO GROUP LTD , BOUILLOT ANNE MARIE JEANNE , BOMBRUN AGNES , DUMAITRE BERNARD ANDRE , GOSMINI ROMAIN LUC MARIE , RAMSDEN NIGEL GRAHAME , CONGREVE MILES STUART
发明人： BOUILLOT ANNE MARIE JEANNE , BOMBRUN AGNES , DUMAITRE BERNARD ANDRE , GOSMINI ROMAIN LUC MARIE , RAMSDEN NIGEL GRAHAME , CONGREVE MILES STUART
IPC分类号： C07D295/12 , A61K31/445 , A61K31/4468 , A61K31/451 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/495 , A61K31/551 , A61P1/18 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P43/00 , C07D211/14 , C07D211/20 , C07D211/22 , C07D211/46 , C07D211/58 , C07D295/13 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D417/12
CPC分类号： C07D295/13 , A61K31/451 , A61K31/495 , C07D211/14 , C07D211/22 , C07D211/46 , C07D211/58 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12
摘要： The invention concerns Use of a compound of formula (I) or a physiologically acceptable salt, solvate or derivative thereof, in the manufacture of a medicament for the treatment of diseases ameliorated by LDL-r upregulation, to novel compounds and pharmaceutical compositions within the scope of formula (I).
摘要翻译：本发明涉及式（I）化合物或其生理上可接受的盐，溶剂合物或衍生物在制备用于治疗LDL-r上调改善的疾病的药物中的用途，涉及范围内的新化合物和药物组合物的式（I）化合物。

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