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1. 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。

2. 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。

3. 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。

4. 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

5. 发明申请

WO2008110846A3 COMPOSITIONS COMPRISING (S)-2-AMINO-1-(4-CHLOROPHENYL)-1-[4-(1H-PYRAZOL-4-YL)-PHENYL]-ETHANOL AS MODULATOR OF PROTEIN KINASES 审中-公开
标题翻译：包含（S）-2-氨基-1-（4-氯苯基）-1- [4-（1H-吡唑-4-基） - 苯基] - 乙醇的组合物作为蛋白激酶的调节剂
公开(公告)号：WO2008110846A3
公开(公告)日：2009-03-05
申请号：PCT/GB2008050180
申请日：2008-03-14
申请人： ASTEX THERAPEUTICS LTD , CANCER RES INST ROYAL , CANCER REC TECH LTD , WOODHEAD STEVEN JOHN , REES DAVID CHARLES , FREDERICKSON MARTYN , GRIMSHAW KYLA MERRIOM
发明人： WOODHEAD STEVEN JOHN , REES DAVID CHARLES , FREDERICKSON MARTYN , GRIMSHAW KYLA MERRIOM
IPC分类号： A61K31/415 , A61P35/00 , C07D231/12 , C07D301/00
CPC分类号： A61K31/415 , C07C215/32 , C07C247/10 , C07C309/30 , C07D231/12 , A61K2300/00
摘要： The invention provides a composition comprising (S) 2-amino-1-(4-chloro-phenyl)- 1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol, wherein the composition is either substantially free of (R) 2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)- phenyl]-ethanol or the composition contains a mixture of the (S) and (R) enantiomers in which the (S) enantiomer predominates. Also provided are processes for the preparation of the (S) 2-amino-1-(4-chloro-phenyl)-1-[4-(1H- pyrazol-4-yl)-phenyl]-ethanol, novel process intermediates and methods for making the novel process intermediates.
摘要翻译：本发明提供了包含（S）2-氨基-1-（4-氯 - 苯基）-1- [4-（1H-吡唑-4-基） - 苯基] - 乙醇的组合物，其中组合物基本上不含的（R）2-氨基-1-（4-氯 - 苯基）-1- [4-（1H-吡唑-4-基） - 苯基] - 乙醇或该组合物含有（S）和（（S）对映异构体占优势。还提供了制备（S）2-氨基-1-（4-氯 - 苯基）-1- [4-（1H-吡唑-4-基） - 苯基] - 乙醇的方法，新工艺中间体和制备新工艺中间体的方法。

6. 发明公开

EP1831170A4 SUBSTITUTED AMINOPYRIDINES AND USES THEREOF 审中-公开
标题翻译：取代的氨基吡啶及其使用
公开(公告)号：EP1831170A4
公开(公告)日：2009-10-14
申请号：EP05815781
申请日：2005-12-12
申请人： ASTRAZENECA AB , ASTEX THERAPEUTICS LTD
发明人： ALBERT JEFFREY SCOTT , CALLAGHAN OWEN , CAMPBELL JAMES , CARR ROBIN ARTHUR ELLIS , CHESSARI GIANNI , COWAN SUZANNA , CONGREVE MILES STUART , EDWARDS PHIL , FREDERICKSON MARTYN , MURRAY CHRISTOPHER WILLIAM , PATEL SAHIL
IPC分类号： C07D213/73 , A61K31/44 , A61P25/16 , A61P25/28
CPC分类号： C07D213/73 , C07D213/74 , C07D213/81 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/10 , C07D409/14 , C07D413/12

9. 发明专利

MY168159A BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY 未知
公开(公告)号：MY168159A
公开(公告)日：2018-10-11
申请号：MYPI2013003401
申请日：2012-04-20
申请人： ASTEX THERAPEUTICS LTD
发明人： JOHNSON CHRISTOPHER NORBERT , GRIFFITHS-JONES CHARLOTTE MARY , CHESSARI GIANNI , TAMANINI EMILIANO , WOOLFORD ALISON JO-ANNE , HOWARD STEVEN , BUCK ILDIKO MARIA , DAY JAMES EDWARD HARVEY , CHIARPARIN ELISABETTA , HEIGHTMAN THOMAS DANIEL , FREDERICKSON MARTYN
IPC分类号： C07D401/06 , A61K31/497 , A61K31/501 , C07D403/04 , C07D403/14 , C07D419/00
摘要： OR TAUTOMERIC OR STEREOCHEMICALLY ISORNERIC FORMS, N-OXIDES, PHARMACEUTICALLY ACCEPTABLE SALTS OR THE SOLVATES THEREOF; WHEREIN R1, R2A, R2B, R3, R3B, R5, R6, R7, R8, R9, P AND E ARE AS DEFINED HEREIN; TO PHARMACEUTICAL COMPOSITIONS COMPRISING SAID COMPOUNDS AND TO THE USE OF SAID COMPOUNDS IN THE TREATMENT OF DISEASES, E.G. CANCER.

10. 发明专利

CY1115797T1 ΠΑΡΑΓΩΓΑ ΥΔΡΟΞΥΒΕΝΖΑΜΙΔΙΟΥ ΚΑΙ Η ΧΡΗΣΗ ΤΟΥΣ ΩΣ ΑΝΑΣΤΟΛΕIΣ ΤΗΣ HSP90 未知
公开(公告)号：CY1115797T1
公开(公告)日：2017-01-25
申请号：CY141100993
申请日：2014-11-27
申请人： ASTEX THERAPEUTICS LTD
发明人： CHESSARI GIANNI , CONGREVE MILES STUART , NAVARRO EVA FIGUEROA , FREDERICKSON MARTYN , MURRAY CHRISTOPHER , WOOLFORD ALISON JO-ANN , 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
摘要： Ηεφεύρεσηπαρέχειενώσειςτουτύπου (I): ήάλατα, ταυτομερή, διαλυτώματακαιΝ-οξείδιααυτής, όπουτο R1 είναιυδροξύλιοή υδρογόνο, το R2 είναιυδροξυ, μεθόξυή υδρογόνο, υπότηνπροϋπόθεσηότιτουλάχιστονένααπότα R1 και R2 είναιυδρόξυ. To R3 επιλέγεταιαπόυδρογόνο, αλογόνο, κυανό, προαιρετικάυποκατεστημένο C1-5 υδροκαρβύλιοκαιπροαιρετικάυποκατεστημένο C1-5 υδροκαρβυλοξυ. To R4 επιλέγεταιαπόυδρογόνο, μιαομάδα - (Ο) n-R 7, όπουτο n είναι 0 ή 1 καιτο R7 είναιμίαπροαιρετικάυποκατεστημένηακυκλική C1-5 ομάδαυδροκαρβυλίουή μίαμονοκυκλικήκαρβοκυκλικήή ετεροκυκλικήομάδαπουέχει 3 έως 7 μέληδακτυλίου, αλογόνο, κυανό, υδροξυ, αμινο, καιπροαιρετικώςυποκατεστημένομονο- ήδι-C1-5 υδροκαρβυλαμινο, ήτα R3 και R4 μαζίσχηματίζουνέναμονοκυκλικόκαρβοκυκλικόή ετεροκυκλικόδακτύλιομε 5 έως 7 μέληδακτυλίουκαιτο NR5R6 σχηματίζειμίαπροαιρετικώςυποκατεστημένηδικυκλικήετεροκυκλικήομάδαπουέχει 8 έως 12 μέληδακτυλίουεκτωνοποίωνέως 5 μέληδακτυλίουείναιετεροάτομαπουεπιλέγονταιαπόοξυγόνο, άζωτοκαιθείο. Οιενώσειςέχουνδραστικότηταωςαναστολείςτης HSP90.

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