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1. 发明申请

WO2014100071A2 SUBSTITUTED PYRROLOPYRIMIDINES AS HDM2 INHIBITORS 审中-公开
标题翻译：取代的吡咯烷酮作为HDM2抑制剂
公开(公告)号：WO2014100071A2
公开(公告)日：2014-06-26
申请号：PCT/US2013075917
申请日：2013-12-18
申请人： MERCK SHARP & DOHME , DINSMORE CHRISTOPHER , FRADERA LLINAS FRANCESC XAVIER , KUDALE AMIT ASHOKRAO , MACHACEK MICHELLE , REUTERSHAN MICHAEL HALE , THOMPSON CHRISTOPHER FRANCIS , TROTTER B WESLEY , YANG LIPING , ALTMAN MICHAEL D , BOGEN STEPHANE L , DOLL RONALD J , VOSS MATTHEW E
发明人： DINSMORE CHRISTOPHER , FRADERA LLINAS FRANCESC XAVIER , KUDALE AMIT ASHOKRAO , REUTERSHAN MICHAEL HALE , THOMPSON CHRISTOPHER FRANCIS , YANG LIPING , ALTMAN MICHAEL D , BOGEN STEPHANE L , DOLL RONALD J , VOSS MATTHEW E
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： The present invention provides substituted pyrrolopyrimidines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
摘要翻译：本发明提供如本文所述的取代吡咯并嘧啶或其药学上可接受的盐或溶剂化物。代表性化合物可用作HDM2蛋白的抑制剂。还公开了包含上述化合物的药物组合物和使用其治疗癌症的潜在方法。

2. 发明专利

CA2895504A1 SUBSTITUTED IMIDAZOPYRIDINES AS HDM2 INHIBITORS 未知
公开(公告)号：CA2895504A1
公开(公告)日：2014-06-26
申请号：CA2895504
申请日：2013-12-18
申请人： MERCK SHARP & DOHME
发明人： BOLISETTI RAGHU , CAMMARANO CAROLYN MICHELE , CHRISTOPHER MATTHEW P , FRADERA LLINAS FRANCESC XAVIER , GHOSH PARTHA , MACHACEK MICHELLE , MARTINEZ MICHELLE , PANDA JAGANNATH , REUTERSHAN MICHAEL HALE , SAMALA JAYA PRAKASH , SHIZUKA MANAMI , SUN BINYUAN , THOMPSON CHRISTOPHER FRANCIS , TONY KURISSERY ANTHAPPAN , TROTTER B WESLEY , VOSS MATTHEW E , YANG LIPING , ALTMAN MICHAEL D , BOGEN STEPHANE L , DOLL RONALD J
IPC分类号： C07D471/04 , A61K31/437 , A61K31/498 , A61K31/5377 , A61K31/538 , A61K31/5383 , A61K31/541 , A61K31/553 , A61P35/00 , C07D519/00
摘要： The present invention provides substituted imidazopyridines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.

3. 发明专利

AU2013361694A1 Substituted imidazopyridines as HDM2 inhibitors 未知
公开(公告)号：AU2013361694A1
公开(公告)日：2015-06-18
申请号：AU2013361694
申请日：2013-12-18
申请人： MERCK SHARP & DOHME
发明人： BOLISETTI RAGHU , CAMMARANO CAROLYN MICHELE , CHRISTOPHER MATTHEW P , FRADERA LLINAS FRANESC XAVIER , GHOSH PARTHA , MACHACEK MICHELLE , MARTINEZ MICHELLE , PANDA JAGANNATH , REUTERSHAN MICHAEL HALE , SAMALA JAYA PRAKASH , SHIZUKA MANAMI , SUN BINYUAN , THOMPSON CHRISTOPHER FRANCIS , TONY KURISSERY ANTHAPPAN , TROTTER B WESLEY , VOSS MATTHEW E , YANG LIPING , ALTMAN MICHAEL D , BOGEN STEPHANE L , DOLL RONALD J
IPC分类号： C07D471/04 , A61K31/437 , A61K31/498 , A61K31/5377 , A61K31/538 , A61K31/5383 , A61K31/541 , A61K31/553 , A61P35/00 , C07D519/00
摘要： The present invention provides substituted imidazopyridines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.

4. 发明专利

ES2707305T3 Imidazopiridinas sustituidas como inhibidores de HDM2 未知
公开(公告)号：ES2707305T3
公开(公告)日：2019-04-03
申请号：ES13818899
申请日：2013-12-18
申请人： MERCK SHARP & DOHME
发明人： BOLISETTI RAGHU , CAMMARANO CAROLYN MICHELE , CHRISTOPHER MATTHEW , FRADERA LLINAS FRANCESC XAVIER , GHOSH PARTHA , MACHACEK MICHELLE , MARTINEZ MICHELLE , PANDA JAGANNATH , REUTERSHAN MICHAEL HALE , SAMALA JAYA PRAKASH , SHIZUKA MANAMI , SUN BINYUAN , THOMPSON CHRISTOPHER FRANCIS , TONY KURISSERY ANTHAPPAN , TROTTER B WESLEY , VOSS MATTHEW , YANG LIPING , ALTMAN MICHAEL , BOGEN STEPHANE , DOLL RONALD
IPC分类号： C07D471/08 , A61K31/437 , A61K31/498 , A61K31/5377 , A61K31/538 , A61K31/5383 , A61K31/541 , A61K31/553 , A61P35/00 , C07D471/04 , C07D498/04 , C07D519/00
摘要： Un compuesto representado por la Fórmula I: **Fórmula** En donde R1 es COOH, C(O)ORc, C(O)NRcRc, C(O)NRcSO2Rc, C(O)NRcSO2NRcRc, NRcSO2Rc, **Fórmula** en donde Rd es metilo o H. R2 es **Fórmula** Rj es H o metilo, Rh es independientemente halo, NRcRc, hidroxialquilo C1-C4, hidroxialcoxi C1-C4, -Oalquil C1-C3Oalquilo C1-C3, alquilo C1-C4 o alcoxi C1-C4; a es 0, 1 o 2; R3 es **Fórmula** X es O, S, NR16, CR162, o SO2,. R15 se selecciona independientemente entre el grupo que consiste en fenilo, heteroarilo de 5 o 6 miembros, heterocíclico, haloalquilo C1-C3, halo, haloalcoxi C1-C3alquilo C0-C3, alcoxi C1-C3, alcoxi C1-C3alquilo C1-C3, alcoxi C1-C3alcoxi C1-C3, alcoxi C1-C3cicloalquilo C3-C5, alquilo C1-C6, cicloalquilo C3-C6, C(O)Rf, C(O)NRc2 e hidroxialquilo C1-C3; dos R15 no adyacentes forman un puente alquileno C2-C3; dos R15 adyacentes forman un cicloalquilo C3-C6 condensado o un anillo heterocíclico de 4, 5 o 6 miembros; o dos R15 unidos al mismo carbono forman =O, un cicloalquilo C3-C6 o un anillo heterocíclico de 5 o 6 miembros, en donde el sustituyente fenilo, heteroarilo, cicloalquilo o heterocíclico puede estar opcionalmente sustituido con halo o alquilo C1-C3; R16 se selecciona independientemente entre el grupo que consiste en H, haloalquilo C1-C8, halo, haloalcoxi C1- C3alquilo C0-C3, alcoxi C1-C3, alcoxi C1-C3alquilo C1-C3, alquilo C1-C6, cicloalquilo C3-C6, C(O)Rf, C(O)NRc2, S(O)2Rc, C(O)OR10 e hidroxialquilo C1-C3; Rc es independientemente H o alquilo C1-C3 opcionalmente sustituido con halo o alcoxi C1-C3; R10 es independientemente alquilo C1-C3 opcionalmente sustituido con halo; Rf es independientemente H, alquilo C1-C3 o cicloalquilo C3-C4, en donde el alquilo o el cicloalquilo están opcionalmente sustituido con halo, alcoxi C1-C3 o heterocíclico de 4-6 miembros; f es 0, 1 o 2; g es 0 o 1; j es independientemente 0, 1 o 2; o R3 es NR8Rc, T-alquilo C1-C6, -T-arilo, -T-heteroarilo, T-heterocíclico, T-cicloalquilo C3-C7, en donde alquilo, arilo, heteroarilo, heterocíclico y cicloalquilo pueden estar opcionalmente sustituidos con halo, ORc, SRc, SO2Rc, haloalquilo C1-C3, haloalcoxi C1-C3 o alquilo C1-C3; R8 es H, alquilo C1-C6, arilalquilo C1-C6 o heterocíclico, en donde alquilo, arilo o heterocíclico están opcionalmente sustituidos con alcoxi C1-C3 o haloalquilo C1-C3; T es independientemente -(CRa2)-, -C(=CH2)- o -C(O)-; Ra es independientemente H, ORc, halo o alquilo C1-C3, dicho alquilo está opcionalmente sustituido con OH, alcoxi C1-C3, halo o haloalquilo C1-C3; R4 es **Fórmula** Rb y Rs son independientemente H, halo, haloalquilo C1-C3 o alquilo C1-C3; Rg es H, C(O)NHRc, o metilo; R17 se selecciona independientemente entre el grupo que consiste en H, halo, COOH, oxadiazolona, alquilo C1-C6, alcoxi C1-C6, NRcRc, -(CRc2)zcicloalquilo C3-C8, -(CRc2)zheteroarilo, -(CRc2)zarilo y -(CRc2)zheterocíclico en donde heteroarilo, arilo, heterocíclico, cicloalquilo y alquilo pueden estar opcionalmente sustituidos con alquilo C1-C6, OH, halo o haloalquilo C1-C6; i y I son independientemente 0, 1, 2, 3, 4 o 5; y e es 0, 1 o 2. o una sal farmacéuticamente aceptable del mismo.

5. 发明专利

AU2013361694B2 Substituted imidazopyridines as HDM2 inhibitors 未知
公开(公告)号：AU2013361694B2
公开(公告)日：2017-10-26
申请号：AU2013361694
申请日：2013-12-18
申请人： MERCK SHARP & DOHME
发明人： BOLISETTI RAGHU , CAMMARANO CAROLYN MICHELE , CHRISTOPHER MATTHEW P , FRADERA LLINAS FRANESC XAVIER , GHOSH PARTHA , MACHACEK MICHELLE , MARTINEZ MICHELLE , PANDA JAGANNATH , REUTERSHAN MICHAEL HALE , SAMALA JAYA PRAKASH , SHIZUKA MANAMI , SUN BINYUAN , THOMPSON CHRISTOPHER FRANCIS , TONY KURISSERY ANTHAPPAN , TROTTER B WESLEY , VOSS MATTHEW E , YANG LIPING , ALTMAN MICHAEL D , BOGEN STEPHANE L , DOLL RONALD J
IPC分类号： C07D471/04 , A61K31/437 , A61K31/498 , A61K31/5377 , A61K31/538 , A61K31/5383 , A61K31/541 , A61K31/553 , A61P35/00 , C07D519/00
摘要： The present invention provides substituted imidazopyridines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.

6. 发明专利

MX2015008196A IMIDAZOPIRIDINAS SUSTITUIDAS COMO INHIBIDORES DE DOBLE MINUTO 2 HUMANA. 未知
公开(公告)号：MX2015008196A
公开(公告)日：2015-09-16
申请号：MX2015008196
申请日：2013-12-18
申请人： MERCK SHARP & DOHME
发明人： DOLL RONALD J , TROTTER B WESLEY , YANG LIPING , SHIZUKA MANAMI , ALTMAN MICHAEL D , MARTINEZ MICHELLE , CHRISTOPHER MATTHEW P , FRADERA LLINAS FRANCESC XAVIER , BOGEN STEPHANE L , BOLISETTI RAGHU , CAMMARANO CAROLYN MICHELE , GHOSH PARTHA , MACHACEK MICHELLE , PANDA JAGANNATH , REUTERSHAN MICHAEL HALE , SAMALA JAYA PRAKASH , SUN BINYUAN , THOMPSON CHRISTOPHER FRANCIS , TONY KURISSERY ANTHAPPAN , VOSS MATTHEW E
IPC分类号： C07D471/04 , A61K31/437 , A61K31/498 , A61K31/5377 , A61K31/538 , A61K31/5383 , A61K31/541 , A61K31/553 , A61P35/00 , C07D519/00
摘要： La presente invención proporciona imidazopiridinas sustituidas como se describen en el presente documento o una sal farmacéuticamente aceptable o solvato de las mismas; los compuestos representativos son útiles como inhibidores de la proteína HDM2; también se describen composiciones farmacéuticas que comprenden los compuestos anteriores y métodos potenciales para el tratamiento del cáncer que usan los mismos.

7. 发明公开

EP2951180A4 2,6,7,8 SUBSTITUTED PURINES AS HDM2 INHIBITORS 有权转让
标题翻译： 2,6,7,8-SUBSTITUIERTE PURINE ALS HDM2-INHIBITOREN
公开(公告)号：EP2951180A4
公开(公告)日：2016-06-15
申请号：EP14745870
申请日：2014-01-29
申请人： MERCK SHARP & DOHME
发明人： CAMMARANO CAROLYN MICHELE , CHRISTOPHER MATTHEW P , DINSMORE CHRISTOPHER , DOLL RONALD J , FRADERA LLINAS FRANCESC XAVIER , LI CHAOMIN , MACHACEK MICHELLE , MARTINEZ MICHELLE , NAIR LATHA G , PAN WEIDONG , REUTERSHAN MICHAEL HALE , SHIZUKA MANAMI , STEINHUEBEL DIETRICH P , SUN BINYUAN , THOMPSON CHRISTOPHER FRANCIS , TROTTER B WESLEY , VOSS MATTHEW ERNST , WANG YAOLIN , YANG LIPING , PANDA JAGANNATH , KURISSERY ANTHAPPAN TONY , BOGEN STEPHANE L
IPC分类号： C07D473/00 , A61K31/52 , A61P35/00 , C07D473/16 , C07D473/30 , C07D473/34
CPC分类号： C07D473/00 , C07D473/16 , C07D473/30 , C07D473/34
摘要： The present invention provides 2,6,7,8 Substituted Purines as described herein or a pharmaceutically acceptable salt thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
摘要翻译：本发明提供如本文所述的2,6,7,8取代的嘌呤或其药学上可接受的盐。代表性化合物可用作HDM2蛋白的抑制剂。还公开了包含上述化合物的药物组合物和使用其治疗癌症的潜在方法。

8. 发明公开

EP2953470A4 2,6,7 SUBSTITUTED PURINES AS HDM2 INHIBITORS 有权转让
标题翻译： 2,6,7-取代的嘌呤ALS抑制剂HDM2
公开(公告)号：EP2953470A4
公开(公告)日：2016-08-03
申请号：EP14749379
申请日：2014-02-04
申请人： MERCK SHARP & DOHME
发明人： CHRISTOPHER MATTHEW P , FRADERA LLINAS FRANCESC XAVIER , MACHACEK MICHELLE , MARTINEZ MICHELLE , REUTERSHAN MICHAEL HALE , SHIZUKA MANAMI , SUN BINYUAN , THOMPSON CHRISTOPHER FRANCIS , TROTTER B WESLEY , VOSS MATTHEW E , YANG LIPING
IPC分类号： A01N43/90 , A61K31/52 , A61K31/535 , C07D413/00
CPC分类号： C07D473/34 , C07D473/00 , C07D473/30
摘要： The present invention provides 2,6,7 substituted purines as described herein or a pharmaceutically acceptable salt thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.

9. 发明公开

EP2934535A4 SUBSTITUTED PYRROLOPYRIMIDINES AS HDM2 INHIBITORS 有权转让
标题翻译：取代的吡咯并HDM2抑制剂
公开(公告)号：EP2934535A4
公开(公告)日：2016-06-29
申请号：EP13865881
申请日：2013-12-18
申请人： MERCK SHARP & DOHME
发明人： DINSMORE CHRISTOPHER , FRADERA LLINAS FRANCESC XAVIER , KUDALE AMIT ASHOKRAO , REUTERSHAN MICHAEL HALE , THOMPSON CHRISTOPHER FRANCIS , YANG LIPING , ALTMAN MICHAEL D , BOGEN STEPHANE L , DOLL RONALD J , VOSS MATTHEW E
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention provides substituted pyrrolopyrimidines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.

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