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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

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。

3. 发明申请

WO2010059788A1 PYRAZOLOPYRIDINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：吡唑并吡啶PI3K抑制剂化合物及其使用方法
公开(公告)号：WO2010059788A1
公开(公告)日：2010-05-27
申请号：PCT/US2009/065085
申请日：2009-11-19
申请人： GENENTECH, INC. , F. HOFFMANN-LA ROCHE AG , DOTSON, Jennafer , HEFFRON, Tim , OLIVERO, Alan G. , SUTHERLIN, Daniel P. , STABEN, Steven , WANG, Shumei , ZHU, Bing-Yan , CHUCKOWREE, Irina S. , FOLKES, Adrian J. , WAN, Nan Chi
发明人： DOTSON, Jennafer , HEFFRON, Tim , OLIVERO, Alan G. , SUTHERLIN, Daniel P. , STABEN, Steven , WANG, Shumei , ZHU, Bing-Yan , CHUCKOWREE, Irina S. , FOLKES, Adrian J. , WAN, Nan Chi
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04
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 or inflammation 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）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，并用于治疗疾病如癌症或炎症介导通过脂质激酶。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条件中的这种疾病的方法。

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. 发明授权

EP1812446B1 PHARMACEUTICAL COMPOUNDS 有权
公开(公告)号：EP1812446B1
公开(公告)日：2015-11-18
申请号：EP05798278.7
申请日：2005-10-25
申请人： Piramed Limited
发明人： SHUTTLEWORTH, Stephen J. , FOLKES, Adrian J. , CHUCKOWREE, Irina S. , WAN, Nan Chi , HANCOX, Timothy C. , BAKER, Stewart J. , SOHAL, Sukhjit , LATIF, Mohammed A.
IPC分类号： C07D495/04 , A61K31/519
CPC分类号： C07D495/04

8. 发明公开

EP1812446A1 PHARMACEUTICAL COMPOUNDS 有权
标题翻译：药物化合物
公开(公告)号：EP1812446A1
公开(公告)日：2007-08-01
申请号：EP05798278.7
申请日：2005-10-25
申请人： Piramed Limited
发明人： SHUTTLEWORTH, Stephen J. , FOLKES, Adrian J. , CHUCKOWREE, Irina S. , WAN, Nan Chi , HANCOX, Timothy C. , BAKER, Stewart J. , SOHAL, Sukhjit , LATIF, Mohammed A.
IPC分类号： C07D495/04 , A61K31/519
CPC分类号： C07D495/04
摘要： Fused pyrimidines of formula (1); wherein A represents a thiophene or a furan ring; n is 1 or 2; R1 is a group of formula (); wherein m is 0 or 1; R30 is H or C1-C6 alkyl; R4 and R5 form, together with the N atom to which they are attached a 5- or 6- membered saturated N-containing heterocyclic group which includes 0 or 1 additional heteroatoms selected from N, S and O, which may be fused to a benzene ring and which is unsubstituted or substituted; or one of R4 and R5 is alkyl and the other is a 5- Or 6-membered saturated N-containing heterocyclic group as defined above; R2 is selected from a) formula (3) wherein R6 and R7 form, together with the nitrogen atom to which they are attached, a morpholine, thiomorpholine, piperidine, piperazine, oxazepane, or thiazepane group which is unsubstituted or substituted; and b) formula (4) wherein Y is a C2-C4 alkylene chain which contains, between constituent carbon atoms of the chain and/or at one or both ends of the chain, 1 or 2 heteroatoms selected from O, N and S, and which is unsubstituted or substituted; and R3 is selected from: (a) a group of the following formula: (5) wherein B is a phenyl ring which is unsubstituted or substituted and Z is selected from H, -OR, -SR, CH2OR, -CO2R, CF2OH, CH(CF3)OH, C(CF3)2OH, -(CH2)qOR, -(CH2)qNR2, -C(O)N(R)2, -NR2, -NRC(O)R, -S(O)mN(R)2, -OC(O)R, OC(O)N)2, -NRS(O)mR, -NRC(O)N(R)2, CN, halogen and -NO2, wherein each R is independently selected from H, C1-C6 alkyl, C3 - C10 cycloalkyl and a 5- to 12- membered aryl or heteroaryl group, the group being unsubstituted or substituted, m is 1 or 2 and q is 0, 1 or 2; (b) a heteroaryl group which contains, 1, 2, 3 or 4 ring nitrogen atoms and 0, 1 or 2 additional heteroatoms selected from O and S, which group is monocyclic or bicyclic and which is unsubstituted or substituted; and (c) a group comprising a benzene ring which is unsubstituted or substituted and which is fused to a heteroaryl group as defined above; or a pharmaceutically acceptable salt thereof; provided that R3 is not an indole group or an indazole group, which group is unsubstituted or substituted; and the pharmaceutically acceptable salt thereof have activity as inhibitors of P13K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with P13 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（1）的稠合嘧啶; 其中A代表噻吩或呋喃环; n是1或2; R1是一组式（）; 其中m是0或1; R30是H或C1-C6烷基; R 4和R 5与它们所连接的N原子一起形成包含0或1个选自N，S和O的另外的杂原子的5-或6-元饱和的含N杂环基团，所述杂原子可以与苯稠合环并且其未被取代或被取代; 或者R 4和R 5中的一个是烷基，另一个是如上所定义的5或6元饱和含氮杂环基团; R2选自a）式（3）其中R6和R7与它们所连接的氮原子一起形成未取代或取代的吗啉，硫代吗啉，哌啶，哌嗪，氧杂氮杂环庚烷或噻嗪烷基团; 和b）式（4）其中Y是在链的组成碳原子之间和/或在链的一端或两端含有1或2个选自O，N和S的杂原子的C2-C4亚烷基链，并且其未被取代或被取代; （a）下式的基团：（5）其中B为未取代或取代的苯基环，且Z选自H，-OR，-SR，CH 2 OR，-CO 2 R，CF 2 OH，（O）R，-S（O）CH（CF 3）OH，C（CF 3）（R）2，-OC（O）R，OC（O）N）2，-NRS（O）mR，-NRC（O）N（R）2，CN，卤素和-NO 2，独立地选自H，C 1 -C 6烷基，C 3 -C 10环烷基和5至12元芳基或杂芳基，所述基团未被取代或被取代，m为1或2并且q为0,1或2; （b）含有1,2,3或4个环氮原子和0,1或2个选自O和S的另外的杂原子的杂芳基，该基团是单环或双环的并且是未取代的或取代的; 和（c）包含苯环的基团，所述苯环未被取代或被取代并且与如上定义的杂芳基稠合; 或其药学上可接受的盐; 条件是R3不是吲哚基团或吲唑基团，该基团未被取代或被取代; 及其药学上可接受的盐具有作为P13K抑制剂的活性，因此可用于治疗与P13激酶有关的异常细胞生长，功能或行为引起的疾病和病症，例如癌症，免疫病症，心血管疾病，病毒感染，炎症，代谢/内分泌失调和神经疾病。还描述了合成这些化合物的方法。

9. 发明公开

EP1812444A1 PHARMACEUTICAL COMPOUNDS 有权
标题翻译：药物化合物
公开(公告)号：EP1812444A1
公开(公告)日：2007-08-01
申请号：EP05796680.6
申请日：2005-10-25
申请人： Piramed Limited
发明人： SHUTTLEWORTH, Stephen J. , FOLKES, Adrian J. , CHUCKOWREE, Irina S. , WAN, Nan Chi , HANCOX, Timothy C. , BAKER, Stewart J. , SOHAL, Sukhjit , LATIF, Mohammed A.
IPC分类号： C07D495/04 , A61K31/519
CPC分类号： C07D495/04
摘要： Fused pyrimidines of formula (I); wherein A represents a thiophene or furan ring; n is 1 or 2; R1 is a group of formula (1); wherein m is 0 or 1; R30 is H or C1-C6 alkyl; R4 and R5 form, together with the N atom to which they are attached, a 5- or 6- membered saturated N-containing heterocyclic group which includes 0 or 1 additional heteroatoms selected from N, S and O, which may be fused to a benzene ring and which is unsubstituted or substituted; or one of R4 and R5 is alkyl and the other is a 5- or 6- membered saturated N-containing heterocyclic group as defined above or an alkyl group which is substituted by a 5- or 6- membered saturated N- containing heterocyclic group as defined above; R2 is selected from formula (a); wherein R6 and R7 form, together with the nitrogen atom to which they are attached, a morpholine, thiomorpholine, piperidine, piperazine, oxazepane or thiazepane group which is unsubstituted or substituted; and formula (b); wherein Y is a C2-C4 alkylene chain which contains, between constituent carbon atoms of the chain and/or at one or both ends of the chain, 1 or 2 heteroatoms selected from O, N and S, and which is unsubstituted or substituted ; and R3 in an indole group which is unsubstituted or substituted ; and the pharmaceutically acceptable salt thereof have activity as inhibitors of PI3K and may thus be used to treat diseased and disorders arising from abnormal cell growth, function or behaviour 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）的稠合嘧啶; 其中A代表噻吩或呋喃环; n是1或2; R1是式（1）的基团; 其中m是0或1; R30是H或C1-C6烷基; R 4和R 5与它们所连接的N原子一起形成包含0或1个选自N，S和O的另外的杂原子的5-或6-元饱和的含N杂环基团，所述杂原子可以与苯环并且其是未取代的或取代的; 或者R 4和R 5之一是烷基，另一个是如上定义的5或6元饱和含氮杂环基或被5或6元饱和含氮杂环基取代的烷基为以上定义; R2选自式（a）; 其中R6和R7与它们所连接的氮原子一起形成未被取代或被取代的吗啉，硫代吗啉，哌啶，哌嗪，氧氮杂环庚烷或噻嗪烷基团; 和公式（b）; 其中Y是C2-C4亚烷基链，其在链的组成碳原子之间和/或链的一端或两端含有1或2个选自O，N和S的杂原子并且其未被取代或被取代; R3是未取代或取代的吲哚基团; 及其药学上可接受的盐具有作为PI3K抑制剂的活性，因此可用于治疗与PI3激酶有关的异常细胞生长，功能或行为（例如癌症，免疫紊乱，心血管疾病，病毒感染，炎症等）引起的疾病和病症。代谢/内分泌失调和神经疾病。还描述了合成这些化合物的方法。

10. 发明授权

EP1812445B1 PHARMACEUTICAL COMPOUNDS 有权
公开(公告)号：EP1812445B1
公开(公告)日：2015-12-30
申请号：EP05797514.6
申请日：2005-10-25
申请人： Piramed Limited
发明人： SHUTTLEWORTH, Stephen J. , FOLKES, Adrian J. , CHUCKOWREE, Irina S. , WAN, Nan Chi , HANCOX, Timothy C. , BAKER, Stewart J. , SOHAL, Sukhjit , LATIF, Mohammed A.
IPC分类号： C07D495/04 , A61K31/519
CPC分类号： C07D495/04

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