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

WO2008073785A2 PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：磷酸三辛酯抑制剂化合物及其使用方法
公开(公告)号：WO2008073785A2
公开(公告)日：2008-06-19
申请号：PCT/US2007/086533
申请日：2007-12-05
申请人： GENENTECH, INC. , PIRAMED LIMITED , CASTANEDO, Georgette , DOTSON, Jennafer , GOLDSMITH, Richard , GUNZNER, Janet , HEFFRON, Tim , MATHIEU, Simon , OLIVERO, Alan , STABEN, Steven , SUTHERLIN, Daniel P. , TSUI, Vickie , WANG, Shumei , ZHU, Bing-Yan , BAYLISS, Tracy , CHUCKOWREE, Irina , FOLKES, Adrian , WAN, Nan Chi
发明人： CASTANEDO, Georgette , DOTSON, Jennafer , GOLDSMITH, Richard , GUNZNER, Janet , HEFFRON, Tim , MATHIEU, Simon , OLIVERO, Alan , STABEN, Steven , SUTHERLIN, Daniel P. , TSUI, Vickie , WANG, Shumei , ZHU, Bing-Yan , BAYLISS, Tracy , CHUCKOWREE, Irina , FOLKES, Adrian , WAN, Nan Chi
IPC分类号： C07D491/048 , C07D495/04 , A61K31/519 , A61P35/00
CPC分类号： C07D491/048 , C07D495/04
摘要： Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R 3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. Formula (Ic) and (Id).
摘要翻译：式Ia-d的化合物，其中X是S或O，mor是吗啉基团，R 3是单环杂芳基，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的其盐可用于调节脂质激酶（包括PI3K）的活性，以及用于治疗由脂质激酶介导的癌症等疾病。公开了使用式Ia-d化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种疾病的方法。式（Ic）和（Id）。

2. 发明申请

WO2008070740A1 PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：磷酸三辛酯抑制剂化合物及其使用方法
公开(公告)号：WO2008070740A1
公开(公告)日：2008-06-12
申请号：PCT/US2007/086543
申请日：2007-12-05
申请人： PIRAMED LIMITED , GENENTECH, INC. , BAYLISS, Tracy , CHUCKOWREE, Irina , FOLKES, Adrian , OXENFORD, Sally , WAN, Nan, Chi , CASTANEDO, Georgette , GOLDSMITH, Richard , GUNZNER, Janet , HEFFRON, Tim , MATHIEU, Simon , OLIVERO, Alan , STABEN, Steven , SUTHERLIN, Daniel, P. , ZHU, Bing-Yan
发明人： BAYLISS, Tracy , CHUCKOWREE, Irina , FOLKES, Adrian , OXENFORD, Sally , WAN, Nan, Chi , CASTANEDO, Georgette , GOLDSMITH, Richard , GUNZNER, Janet , HEFFRON, Tim , MATHIEU, Simon , OLIVERO, Alan , STABEN, Steven , SUTHERLIN, Daniel, P. , ZHU, Bing-Yan
IPC分类号： C07D491/04 , C07D495/04 , A61K31/5377 , A61K31/519 , A61P35/00
CPC分类号： A61K31/5377 , A61K31/519 , C07D413/14 , C07D491/04 , C07D495/04
摘要： Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. [Insert Formula Ic and Id]
摘要翻译：式Ia-d的化合物，其中X是S或O，mor是吗啉基团，R3是单环杂芳基，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐可用于调节脂质激酶（包括PI3K）的活性，以及用于治疗脂质激酶介导的疾病如癌症。公开了使用式Ia-d化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种疾病的方法。 [插入公式Ic和Id]

3. 发明申请

WO2007127175A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2007127175A2
公开(公告)日：2007-11-08
申请号：PCT/US2007/009866
申请日：2007-04-24
申请人： PIRAMED LIMITED , GENENTECH, INC. , GOLDSMITH, Richard , FOLKES, Adrian , SHUTTLEWORTH, Stephen , CHUCKOWREE, Irina , OXENFORD, Sally , WAN, Nan Chi , CASTANEDO, Georgette , GUNZNER, Janet , HEFFRON, Tim , MATHIEU, Simon , OLIVERO, Alan , SUTHERLIN, Daniel, P. , ZHU, Bing-Yan
发明人： FOLKES, Adrian , SHUTTLEWORTH, Stephen , CHUCKOWREE, Irina , OXENFORD, Sally , WAN, Nan Chi , CASTANEDO, Georgette , GUNZNER, Janet , HEFFRON, Tim , MATHIEU, Simon , OLIVERO, Alan , SUTHERLIN, Daniel, P. , ZHU, Bing-Yan
CPC分类号： A61K31/5377 , A61K31/551 , A61K45/06 , C07D491/04 , C07D491/048 , C07D495/04
摘要： Compounds of Formulae Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib for in vitro , in situ , and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译：式Ia和Ib化合物及其立体异构体，几何异构体，互变异构体，溶剂化物，代谢物和药学上可接受的盐可用于抑制包括PI3K在内的脂质激酶，以及用于治疗诸如癌症脂质激酶。在体外，原位和体内诊断，预防或治疗这些哺乳动物疾病中使用式Ia和Ib化合物的方法细胞或相关的病理状况，都被公开。

4. 发明申请

WO2009042607A1 THIAZOLOPYRIMIDINE P13K INHIBITOR COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：噻唑吡啶P13K抑制剂化合物及其使用方法
公开(公告)号：WO2009042607A1
公开(公告)日：2009-04-02
申请号：PCT/US2008/077394
申请日：2008-09-23
申请人： GENENTECH, INC. , F. HOFFMANN - LA ROCHE AG , CASTANEDO, Georgette, M. , GUNZNER, Janet, L. , MALESKY, Kimberly , MATHIEU, Simon , OLIVERO, Alan, G. , SUTHERLIN, Daniel, P. , WANG, Shumei , ZHU, Bing-yan , CHUCKOWREE, Irina , FOLKES, Adrian , OXENFORD, Sally , WAN, Nan Chi
发明人： CASTANEDO, Georgette, M. , GUNZNER, Janet, L. , MALESKY, Kimberly , MATHIEU, Simon , OLIVERO, Alan, G. , SUTHERLIN, Daniel, P. , WANG, Shumei , ZHU, Bing-yan , CHUCKOWREE, Irina , FOLKES, Adrian , OXENFORD, Sally , WAN, Nan Chi
IPC分类号： C07D513/04 , A61K31/519 , A61P35/00
CPC分类号： C07D513/04
摘要： Compounds of Formulas (Ia and Ib), and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译：式（Ia和Ib）的化合物，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐可用于抑制脂质激酶（包括PI3K）和用于治疗由脂质激酶介导的癌症等疾病。公开了将式Ia和Ib化合物用于体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

5. 发明申请

WO2009097446A1 PYRAZOLOPYRIMIDINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译： PYRAZOLOPYRIMIDINE PI3K抑制剂化合物及其使用方法
公开(公告)号：WO2009097446A1
公开(公告)日：2009-08-06
申请号：PCT/US2009/032459
申请日：2009-01-29
申请人： GENENTECH, INC. , F. HOFFMANN-LA ROCHE AG , DOTSON, Jennafer , HEFFRON, Tim , OLIVERO, Alan , SUTHERLIN, Daniel P. , WANG, Shumei , ZHU, Bing-yan , CHUCKOWREE, Irina , FOLKES, Adrian , WAN, Nan Chi
发明人： DOTSON, Jennafer , HEFFRON, Tim , OLIVERO, Alan , SUTHERLIN, Daniel P. , WANG, Shumei , ZHU, Bing-yan , CHUCKOWREE, Irina , FOLKES, Adrian , WAN, Nan Chi
IPC分类号： C07D487/04 , C07D519/00 , A61K31/505 , A61P35/00
CPC分类号： C07D487/04 , C07D519/00
摘要： Compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. [Fomula I]
摘要翻译：式I化合物，包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗由脂质激酶介导的癌症等疾病。公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。 [Fomula I]

6. 发明申请

WO2009146406A1 PURINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译： PURINE PI3K抑制剂化合物及其使用方法
公开(公告)号：WO2009146406A1
公开(公告)日：2009-12-03
申请号：PCT/US2009/045603
申请日：2009-05-29
申请人： GENENTECH, INC. , F. HOFFMANN-LA ROCHE AG , CASTANEDO, Georgette , CHUCKOWREE, Irina , FOLKES, Adrian , SUTHERLIN, Daniel, P. , WAN, Nan Chi
发明人： CASTANEDO, Georgette , CHUCKOWREE, Irina , FOLKES, Adrian , SUTHERLIN, Daniel, P. , WAN, Nan Chi
IPC分类号： C07D473/32 , A61P35/00 , A61K31/52
CPC分类号： C07D473/32
摘要： Purine compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译：式I的嘌呤化合物，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和其药学上可接受的盐可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗诸如由脂质激酶介导的癌症。公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

7. 发明申请

WO2009066084A1 2 -MORPHOLINOPYRIMIDINES AND THEIR USE AS PI3 KINASE INHIBITORS 审中-公开
标题翻译： 2-吗啉酰亚胺及其作为PI3激酶抑制剂的用途
公开(公告)号：WO2009066084A1
公开(公告)日：2009-05-28
申请号：PCT/GB2008/003910
申请日：2008-11-21
申请人： F. HOFFMANN-LA ROCHE AG , GENENTECH, INC. , CHUCKOWREE, Irina , FOLKES, Adrian , OXENFORD, Sally , OLIVERO, Alan , SUTHERLIN, Daniel, P. , ZHU, Bing-Yan
发明人： CHUCKOWREE, Irina , FOLKES, Adrian , OXENFORD, Sally , OLIVERO, Alan , SUTHERLIN, Daniel, P. , ZHU, Bing-Yan
IPC分类号： C07D239/42 , C07D239/47 , C07D239/48 , C07D401/14 , C07D403/14 , A61K31/506 , A61P35/00
CPC分类号： C07D239/48 , C07D239/42 , C07D239/47 , C07D401/14 , C07D403/14 , C07D413/14
摘要： Morpholino pyrimidines of formula (I): wherein R 1 is selected from -Y-R 6 and -NR 4 R 5 ; R 2 is a N-containing monocyclic heteroaryl group which is selected from pyridyl, isoxazolyl, imidazolyl, pyrazolyl, pyrrolyl, thiazolyl, pyridazinyl, pyrimidinyl, pyrazinyl, oxazolyl, furanyl, thienyl, triazolyl and tetrazolyl and which is unsubstituted or substituted by halo, -CN, -NR 10 R 11 , -OR 10 , -C(O)R 10 , -NR 10 C(O)R 11 , - N(C(O)R 11 ) 2 , -NR 10 C(O)NR 10 R 11 , -SO 2 R 10 R 11 , -SO 2 NR 10 R 11 , -C(=O)OR 10 , -C(=O)NR 10 R 11 , halo-C 1 -C 6 alkyl and unsubstituted C 1 -C 12 alkyl; R 3 is selected from H, C 1 -C 6 alkyl and C 1 -C 6 alkoxy; Y is selected from a direct bond, -(CR 2 ) m -, C 2 -C 6 alkenylene, C 2 -C 6 alkynylene, -(CR 2 ) p -O-(CR 2 ) t -, -(CR 2 ) p -NR-(CR 2 ) t , -(CR 2 ) p -NR-(CR 2 ) n -C(O)-, -(CR 2 ) p -NR-C(O)- (CR 2 ) n -, -(CR 2 ) p -C(O)-NR-(CR 2 ) t , -(CR 2 ) p -C(O)-(CR 2 ) n -NR-(CR 2 ) t ,- and -(CR 2 ) p - C(O)-(CR 2 ) n -; R 6 is selected from an unsaturated 5- to 12-membered carbocyclic or heterocyclic ring, a saturated 5-, 6- or 7- membered N-containing heterocyclic group which is unsubstituted or substituted, C 1 -C 6 alkyl, -NR 2 , -OR, -NR(CO)R and - C(O)NR 2 ; R 4 and R 5 , which are the same or different, are both C 1 -C 6 alkyl which is unsubstituted or substituted, or R 4 and R 5 together form, with the nitrogen atom to which they are attached, a saturated 5-, 6- or 7- membered N-containing heterocyclic group which is unsubstituted or substituted; each R, which are the same or different when more than one is present in a given group, is independently H, C 1 -C 6 alkyl which is unsubstituted or substituted or a 5- to 12-membered aryl or heteroaryl group which is unsubstituted or substituted; R 10 and R 11 , which are the same or different, are independently selected from H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl and C 3 -C 8 cycloalkyl; n is 0 or an integer of 1 to 6; m is an integer of 1 to 6; p is 0 or an integer of 1 to 6; and t is 0 or an integer of 1 to 6, with the proviso that t is an integer of 2 to 6 when R 6 is linked to Y through a constituent O or N atom of R 6 ; and the pharmaceutically acceptable salts thereof, subject to various provisos, have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour, particularly that associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.
摘要翻译：式（I）的吗啉代嘧啶：其中R1选自-Y-R6和-NR4R5; R2是选自吡啶基，异恶唑基，咪唑基，吡唑基，吡咯基，噻唑基，哒嗪基，嘧啶基，吡嗪基，恶唑基，呋喃基，噻吩基，三唑基和四唑基中的含氮单环杂芳基，其未被取代或被卤素取代， CN，-NR10R11，-OR10，-C（O）R10，-NR10C（O）R11，-N（C（O）R11）2，-NR10C（O）NR10R11，-SO2R10R11，-SO2NR10R11，-C（= O）OR 10，-C（= O）NR 10 R 11，卤代-C 1 -C 6烷基和未取代的C 1 -C 12烷基; R 3选自H，C 1 -C 6烷基和C 1 -C 6烷氧基; Y选自直接键， - （CR2）m-，C2-C6亚烯基，C2-C6亚炔基， - （CR2）pO-（CR2）t-， - （CR2）p-NR-（CR2） - （CR2）p-NR-（CR2）nC（O） - ， - （CR2）p-NR-C（O） - （CR2）n - ， - （CR2）pC（O）-NR-（CR2）（CR2）pC（O） - （CR2）n-NR-（CR2）t， - 和 - （CR2）p- C（O） - （CR2） R 6选自不饱和的5至12元碳环或杂环，未取代或取代的饱和的5-，6-或7-元含氮杂环基，C 1 -C 6烷基，-NR 2，-OR， -NR（CO）R和-C（O）NR 2; R 4和R 5相同或不同，为未取代或取代的C 1 -C 6烷基，或者R 4和R 5与它们所连接的氮原子一起形成饱和的5-，6-或7- 未取代或取代的N，N元杂环基; 当在给定基团中存在多于一个时，各R相同或不同，独立地为H，未取代或取代的C 1 -C 6烷基或未被取代或取代的5至12元芳基或杂芳基 ; R10和R11相同或不同，独立地选自H，C1-C6烷基，C2-C6烯基，C2-C6炔基和C3-C8环烷基; n为0或1〜6的整数， m为1〜6的整数。 p为0或1〜6的整数; 并且当R 6通过R6的组分O或N原子连接到Y时，t为0或1-6的整数，条件是t为2至6的整数; 和其药学上可接受的盐，具有各种条件，具有作为PI3K抑制剂的活性，因此可用于治疗由异常细胞生长，功能或行为引起的疾病和障碍，特别是与PI3激酶如癌症，免疫疾病心血管疾病，病毒感染，炎症，代谢/内分泌紊乱和神经障碍。还描述了合成化合物的方法。

8. 发明申请

WO2004111052A1 PYRROLOPYRIMIDINE DERIVATIVES AS MODULATORS OF MULTI-DRUG RESISTANCE (MDR) 审中-公开
标题翻译：作为多药耐药（MDR）的调节剂的吡咯烷酮衍生物
公开(公告)号：WO2004111052A1
公开(公告)日：2004-12-23
申请号：PCT/GB2004/002523
申请日：2004-06-11
申请人： XENOVA LIMITED , WANG, Shouming , HANCOX, Timothy , MILLER, Warren , HARRISON, John , CHUCKOWREE, Irina , BAKER, Stewart , FOLKES, Adrian , WAN, Nan, Chi
发明人： WANG, Shouming , HANCOX, Timothy , MILLER, Warren , HARRISON, John , CHUCKOWREE, Irina , BAKER, Stewart , FOLKES, Adrian , WAN, Nan, Chi
IPC分类号： C07D487/04
CPC分类号： C07D471/14 , C07D487/04
摘要： A compound which is a pyrrolopyrimidine of formula (I) wherein R 1 is selected from H, C l -C 6 alkyl which is unsubstituted or substituted, (CH 2 ) n Ar 1 , (CH 2 ) p NR 4 R 5 , halogen and (CH 2 ) p X; R 2 is CH 2 ) p Ar l ; R 3 is selected from H, C l -C 6 alkyl which is unsubstituted or substituted, (CH 2 ) p Z and (CH 2 ) p Ar l ; P is an unsaturated 5, 6, or 7 membered carbocyclic or heterocyclic ring which is unsubstituted or substituted; R 4 and R 5 which are the same or different are selected from H, C l -C 6 alkyl which is unsubstituted or substituted, (CH 2 ) n C 3 -C 10 cycloalkyl, (CH 2 ) n Ar 1 , and (CH 2 ) n OR 6 , or R 4 and R 5 together with the nitrogen atom to which they are attached, form a saturated five or six membered nitrogen containing heterocyclic ring which may contain one extra heteroatom selected from 0, N and S and which is unsubstituted or substituted; R 6 is selected from H, C l -C 6 alkyl which is unsubstituted or substituted, C 3 -C 10 cycloalkyl, (CH 2 ) n OC 1 -C 6 alkyl which is unsubstituted or substituted, (CH 2 ) n O(CH 2 ) n Ar 1 , (CH 2 ) n CO 2 C 1 -C 6 ,alkyl which is unsubstituted or substituted and (CH 2 ) n Ar 1 ; X is selected from CN, azide, (CH 2 ) n NHSO 2 R 6 and (CH 2 ) n NHCOR 6 ; Z is selected from CN, CO 2 R 6 and CONR 4 R 5 ; Ar 1 is the same or different when more than one is present within a given substituent group and is an unsaturated C 6 -C 10 membered carbocylic group or an unsaturated 5-11 membered heterocycle, either of which is unsubstituted or substituted; p is an integer of 1 to 6; n is the same or different when more than one is present within a given substituent group and is 0 or an integer of 1 to 6; with the proviso that the pyrrolepyrimidine compound of formula (I) is other than 1-(4-benzyl-piperazin-1-yl)-9H-2,4,9-triaza-fluorene; and the pharmaceutically acceptable salts thereof, have activity as inhibitors of MRP (multidrug resistant protein) and may thus be used to modulate multidrug resistance, for instance in potentiating the cytotoxicity of a chemotherapeutic agent.
摘要翻译：化合物，其是式（I）的吡咯并嘧啶，其中R 1选自H，未取代或取代的C 1 -C 6烷基，（CH 2）n Ar 1，（CH 2）p NRR 5 R 5，，卤素和（CH 2）pX; R 2是CH 2）pAr 1; R 3选自H，未被取代或取代的C 1 -C 6烷基，（CH 2）pZ和（CH 2）p Ar 1; P是未取代或取代的不饱和5,6或7元碳环或杂环; （CH 2）n C 3 -C 10环烷基，（CH 2）n Ar 1和（CH 2）n C 3 -C 10环烷基，C 1 -C 4烷基， nOR 6或R 4和R 5与它们所连接的氮原子一起形成饱和的五或六元含氮杂环，其可含有一个选自0，N和S的杂原子并且其是未取代或取代的; R 6选自未取代或取代的C 1 -C 6烷基，C 3 -C 10环烷基，未取代或取代的（CH 2）n O（CH 2）n Ar 1（CH 2）n OC 1 -C 6烷基，）nCO2C1-C6，未取代或取代的烷基和（CH2）nAr 1; X选自CN，叠氮化物，（CH 2）n NHSO 2 R 6和（CH 2）n NHCOR 6; Z选自CN，CO 2 R 6和CONR 4 R 5; 当在给定的取代基中存在多于一个时，Ar 1是相同或不同的，并且是不饱和的C 6 -C 10元碳环基或不饱和5-11元杂环，其中任一个是未取代的或取代的; p为1〜6的整数。当给定取代基中存在多于一个时，n相同或不同，为0或1〜6的整数; 条件是式（I）的吡咯嘧啶化合物不是1-（4-苄基 - 哌嗪-1-基）-9H- 2,4,9-三氮杂芴; 和其药学上可接受的盐具有作为MRP（多药耐药性蛋白）的抑制剂的活性，因此可用于调节多药耐药性，例如增强化学治疗剂的细胞毒性。

9. 发明申请

WO2007129161A3 THIENO [3, 2-D] PYRIMIDINE DERIVATIVE USEFUL AS PI3K INHIBITOR 审中-公开
公开(公告)号：WO2007129161A3
公开(公告)日：2007-11-15
申请号：PCT/IB2007/001058
申请日：2007-04-24
申请人： PIRAMED LIMITED , CHUCKOWREE, Irina , FOLKES, Adrian , HANCOX, Tim , SHUTTLEWORTH, Stephen
发明人： CHUCKOWREE, Irina , FOLKES, Adrian , HANCOX, Tim , SHUTTLEWORTH, Stephen
IPC分类号： C07D495/04 , A61K31/519 , A61P35/00
摘要： A thienopyrimidine of formula (I) and the pharmaceutically acceptable salts thereof have activity as inhibitors of PI3K with selectivity for the P110α subtype, and may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour, particularly those associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.

10. 发明申请

WO2004065389A1 PYRROLOPYRIMIDINE DERIVATIVES USEFUL AS MODULATORS OF MULTIDRUG RESISTANCE 审中-公开
标题翻译：用作多抗电荷调节剂的吡咯烷酮衍生物
公开(公告)号：WO2004065389A1
公开(公告)日：2004-08-05
申请号：PCT/GB2004/000274
申请日：2004-01-23
申请人： XENOVA LIMITED , MILTON, John , WREN, Stephen , WANG, Shouming , FOLKES, Adrian , CHUCKOWREE, Irina , HANCOX, Timothy , MILLER, Warren , SOHAL, Sukhjit
发明人： MILTON, John , WREN, Stephen , WANG, Shouming , FOLKES, Adrian , CHUCKOWREE, Irina , HANCOX, Timothy , MILLER, Warren , SOHAL, Sukhjit
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A compound which is a pyrrolopyrimidine of formula (I) wherein: R 1 is selected from R 9 and halogen; R 2 is NR 6 R 7 ; R 3 is selected from H, C 1 -C 6 alkyl which is unsubstituted or substituted and -(CH2) n Ar; R 4 is selected from H, C 1 -C 6 alkyl and -(CH 2 )„ Ar; or R 3 and R 4 form, together with the N and C atoms to which they are attached, a fused five-, six-, seven- or eight-membered N-containing saturated ring which is unsubstituted or substituted; R 5 is selected from CN, C0 2 R 9 , C(O)NR 10 R 11 , -(CH 2 ) n OH, -(CH 2 ) n R 10 R n , -C = CH, -C(S)NR 10 R 11 , -C(NH 2 )=NOR 9 , -C(R 9 )=NOR 9 , -C(NH 2 )NH, -C(O)R 9 and an unsaturated 5- or 6-membered heterocyclic group which contains 1, 2 or 3 heteroatoms selected from N, O and S and which is unsubstituted or substituted; R 6 and R 7 , which are the same or different, are selected from C 1 -C 6 alkyl which is unsubstituted or substituted, -(CH 2 ) n X and -(CH 2 ) n Ar; or R 6 and R 7 form, together with the nitrogen atom to which they are attached, a saturated five-, six-, seven- or eight-membered heterocyclic group which contains one nitrogen atom and 0 or from 1 to 3 additional heteroatoms selected from N, O and S, which is unsubstituted or substituted and which optionally contains one or two bridgehead atoms; R 10 and R 11 , which are the same or different, are selected from H, C 1 -C 6 alkyl which is unsubstituted or substituted, -(CH 2 ) n C 3 -C 10 cycloalkyl and -(CH 2 ) n Ar; or R 10 and R 11 form, together with the nitrogen atom to which they are attached, a saturated five or six membered heterocyclic group which contains a nitrogen atom and 0 or from to 3 additional heteroatoms selected from O, S and N, which is unsubstituted or substituted and which is optionally fused to a benzene ring which is unsubstituted or substituted; n is the same or different when more than one is present within a given substituent group and is 0 or an integer of from 1 to 6; X is selected from -CN, -C0 2 R 9 and -NR 10 R 11 ; R 9 is the same or different when more than one is present within a given substituent group and is selected from -H, -QAr, -(CH 2 ) n Ar, C 1 -C 6 alkyl which is unsubstituted or substituted and -(CH 2 ) n C 3 -C 10 cycloalkyl, wherein the cycloalkyl moiety is optionally fused to a benzene ring which is unsubstituted or substituted; Q is C 2 -C 6 alkenylene or alkynylene; and Ar is an unsaturated C 6 -C 10 membered carbocyclic group or an unsaturated 5-11 membered heterocyclic group, which groups are unsubstituted or substituted; or a pharmaceutically acceptable salt thereof. These compounds have activity as inhibitors of MRP (multidrug resistant protein) and may thus be used to modulate multidrug resistance, for instance in potentiating the cytotoxicity of a chemotherapeutic agent.
摘要翻译：化合物，其是式（I）的吡咯并嘧啶，其中：R 1选自R 9和卤素; R 2是NR 6 R 7; R 3选自H，未取代或取代的C 1 -C 6烷基和 - （CH 2）n Ar; R 4选自H，C 1 -C 6烷基和 - （CH 2）“Ar;或R 3和R 4形式，与它们所连接的N和C原子一起，未取代或取代的六元，七元或八元的含N饱和环; R 5选自CN，CO 2 R 9，C（O）NR 10 R 11， - （ CH 2）n OH， - （CH 2）n R 10 R n，-C = CH，-C（S）NR 10 R 11，-C（NH 2）= NOR 9，-C（ R 9）= NOR 9，-C（NH 2）NH，-C（O）R 9和不饱和的5-或6-元杂环基，其含有1,2或3个选自N， O和S是未取代或取代的; R 6和R 7相同或不同，选自未取代或取代的C 1 -C 6烷基， - （CH 2）n X和 - （CH 2） nAr;或R 6和R 7与它们所连接的氮原子一起形成饱和的五元，六元，七元或八元杂环基，其含有一个氮原子且为0或从 1至3个选自N，O和S的杂原子，其是未取代的或取代的并且其任选地包含一个或两个桥头原子; R 10和R 11相同或不同，选自H，未取代或取代的C 1 -C 6烷基， - （CH 2）n C 3 -C 10环烷基和 - （CH 2）n Ar; 或R 10和R 11与它们所连接的氮原子一起形成饱和的五或六元杂环基，其含有氮原子和0或至少3个选自O，S的另外的杂原子， N是未取代或取代的，并且任选地与未被取代或取代的苯环稠合; 当给定的取代基中存在多于一个时，n相同或不同，为0或1-6的整数; X选自-CN，-CO 2 R 9和-NR 10 R 11; R 9在给定的取代基中存在多于一个且选自-H，-QAr， - （CH 2）nAr，未取代或取代的C 1 -C 6烷基和 - （CH 2） nC 3 -C 10环烷基，其中环烷基部分任选地与未被取代或取代的苯环稠合; Q是C 2 -C 6亚烯基或亚炔基; 和Ar是不饱和的C 6 -C 10的碳环基团或不饱和的5-11元杂环基团，这些基团是未取代的或取代的; 或其药学上可接受的盐。这些化合物具有作为MRP（多药耐药蛋白）的抑制剂的活性

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