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21. 发明专利

EA025611B1 АКТИВИРУЮЩИЕ AMPK ГЕТЕРОЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ И СПОСОБЫ ИХ ИСПОЛЬЗОВАНИЯ 未知
公开(公告)号：EA025611B1
公开(公告)日：2017-01-30
申请号：EA201390184
申请日：2011-07-29
申请人： RIGEL PHARMACEUTICALS INC
发明人： GOFF DANE , PAYAN DONALD , SINGH RAJINDER , SHAW SIMON , CARROLL DAVID , HITOSHI YASUMICHI
IPC分类号： C07D213/82 , A61K31/4427 , A61K31/501 , A61K31/5377 , A61P3/10 , A61P9/10 , C07D295/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/10
摘要： Изобретениеотноситсяк соединению, характеризующемусяструктурнойформулой, описаннойниже, илиегофармацевтическиприемлемойсоли, где RпредставляетсобойН; Rпредставляетсобойфенил, замещенный 0, 1, 2 или 3 заместителями, независимовыбраннымииз -(C-C-алкил), -(C-C-галогеналкил), -NHC(О)(C-C-алкил), NRR, -О-(C-C-алкил), -O-(C-C-фторалкил), -C(O)(C-C-алкил), -S(O)(C-C-алкил), -галогена, -CN; Yпредставляетсобой N илиСН; Тпредставляетсобой, где Q представляетсобойодинарнуюсвязь, -СН-, -O-, -СН(СН)-, -С(О)- или -S(O)-; обозначенная "А" кольцеваясистемапредставляетсобойфенил; каждый Rнезависимовыбираютиз -(C-C-алкил), -(C-C-галогеналкил), -NHC(O)(C-C-алкил), -C(O)NRR, -NRR, -O(C-C-алкил), -О(C-C-фторалкил), -C(O)(C-C-алкил), -C(O)(C-C-фторалкил), -S(O)(C-C-алкил), -S(О)(C-C-фторалкил), -галогена, -N, -SF, -NOи -CN; уравно 0, 1, 2 или 3; гдекаждый Rи RнезависимовыбираютизН и -(C-C-алкил); каждый Rнезависимовыбираютиз -Ни -(C-C-алкил). Изобретениетакжеотноситсяк фармацевтическимкомпозициям, содержащимуказанныесоединения. Соединениеактивируетметаболическийпуть AMPK иможетбытьиспользованодлялечениясвязанныхс метаболизмомнарушенийи состояний.

22. 发明专利

ES2528032T3 Inhibidores de Axl para su uso en terapia de combinación para prevenir, tratar o manejar cáncer metastásico 未知
公开(公告)号：ES2528032T3
公开(公告)日：2015-02-03
申请号：ES10700686
申请日：2010-01-15
申请人： RIGEL PHARMACEUTICALS INC
发明人： HITOSHI YASUMICHI , HOLLAND SACHA , PAYAN DONALD
IPC分类号： A61K31/00
摘要： Inhibidor de Axl y uno o más agentes quimioterápicos, para su uso para prevenir, tratar o manejar cáncer, en el que el inhibidor de Axl es un compuesto de fórmula (I):**Fórmula** en la que: R1, R4 y R5 se seleccionan cada uno independientemente del grupo que consiste en hidrógeno, alquilo, alquenilo, arilo, aralquilo, -C(O)R8, -C(O)N(R6)R7 y -C(>=NR6)N(R6)R7; R2 y R3 son cada uno independientemente un heteroarilo policíclico que contiene más de 14 átomos de anillo opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo que consiste en oxo, tioxo, ciano, nitro, halógeno, haloalquilo, alquilo, cicloalquilo opcionalmente sustituido, cicloalquilalquilo opcionalmente sustituido, arilo opcionalmente sustituido, aralquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heterociclilo opcionalmente sustituido, -R9-OR8, -R9-O-R10-OR8, -R9-O-R10-O-R10-OR8, -R9-O-R10-CN, -R9-O-R10-C(O)OR8, -R9-O-R10-C(O)N(R6)R7, -R9-O-R10-S(O)pR8 (en el que p es 0, 1 ó 2), -R9-O-R10-N(R6)R7, -R9-O-R10-C(NR11)N(R11)H, -R9-OC(O)-R8, -R9-N(R6)R7, -R9-C(O)R8, -R9-C(O)OR8, -R9-C(O)N(R6)R7, -R9-N(R6)C(O)OR8, -R9-N(R6)C(O)R8, -R9-N(R6)S(O)tR8 (en el que t es 1 ó 2), -R9-S(O)tOR8 (en el que t es 1 ó 2), -R9-S(O)pR8 (en el que p es 0, 1 ó 2) y -R9-S(O)tN(R6)R7 (en el que t es 1 ó 2); o R2 es un heteroarilo policíclico que contiene más de 14 átomos de anillo tal como se describió anteriormente y R3 se selecciona del grupo que consiste en arilo y heteroarilo, en el que el arilo y el heteroarilo están cada uno opcionalmente sustituidos independientemente con uno o más sustituyentes seleccionados del grupo que consiste en alquilo, alquenilo, alquinilo, halógeno, haloalquilo, haloalquenilo, haloalquinilo, oxo, tioxo, ciano, nitro, arilo opcionalmente sustituido, aralquilo opcionalmente sustituido, aralquenilo opcionalmente sustituido, aralquinilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, cicloalquilalquilo opcionalmente sustituido, cicloalquilalquenilo opcionalmente sustituido, cicloalquilalquinilo opcionalmente sustituido, heterociclilo opcionalmente sustituido, heterociclilalquilo opcionalmente sustituido, heterociclilalquenilo opcionalmente sustituido, heterociclilalquinilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heteroarilalquilo opcionalmente sustituido, heteroarilalquenilo opcionalmente sustituido, heteroarilalquinilo opcionalmente sustituido, -R13-OR12, -R13- OC(O)-R12, -R13-O-R14-N(R12)2, -R13-N(R12)-R14-N(R12)2, -R13-N(R12)-R14-N(R12)2, -R13-N(R12)2, -R13-C(O)R12, -R13-C(O)OR12, -R13-C(O)N(R12)2, -R13-C(O)N(R12)-R14-N(R12)R13, -R13-C(O)N(R12)-R14-OR12, -R13- N(R12)C(O)OR12, -R13-N(R12)C(O)R12, -R13-N(R12)S(O)tR12 (en el que t es 1 ó 2), -R13-S(O)tOR12 (en el que t es 1 ó 2), -R13-S(O)pR12 (en el que p es 0, 1 ó 2) y -R13-S(O)tN(R12)2 (en el que t es 1 ó 2); o R3 es un heteroarilo policíclico que contiene más de 14 átomos de anillo tal como se describió anteriormente, y R2 se selecciona del grupo que consiste en arilo y heteroarilo, en el que el arilo y el heteroarilo están cada uno opcionalmente sustituidos independientemente con uno o más sustituyentes seleccionados del grupo que consiste en alquilo, alquenilo, alquinilo, halógeno, haloalquilo, haloalquenilo, haloalquinilo, oxo, tioxo, ciano, nitro, arilo opcionalmente sustituido, aralquilo opcionalmente sustituido, aralquenilo opcionalmente sustituido, aralquinilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, cicloalquilalquilo opcionalmente sustituido, cicloalquilalquenilo opcionalmente sustituido, cicloalquilalquinilo opcionalmente sustituido, heterociclilo opcionalmente sustituido, heterociclilalquilo opcionalmente sustituido, heterociclilalquenilo opcionalmente sustituido, heterociclilalquinilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heteroarilalquilo opcionalmente sustituido, heteroarilalquenilo opcionalmente sustituido, heteroarilalquinilo opcionalmente sustituido, -R13-OR12, -R13- OC(O)-R12, -R13-O-R14-N(R12)2, -R13-N(R12)-R14-N(R12)2, -R13-N(R12)-R14-N(R12)2, -R13-N(R12)2, -R13-C(O)R12, -R13-C(O)OR12, -R13-C(O)N(R12)2, -R13-C(O)N(R12)-R14-N(R12)R13, -R13-C(O)N(R12)-R14-OR12, -R13- N(R12)C(O)OR12, -R13-N(R12)C(O)R12, -R13-N(R12)S(O)tR12 (en el que t es 1 ó 2), -R13-S(O)tOR12 (en el que t es 1 ó 2), -R13-S(O)pR12 (en el que p es 0, 1 ó 2) y -R13-S(O)tN(R12)2 (en el que t es 1 ó 2).

23. 发明专利

SG186850A1 AMPK-ACTIVATING HETEROCYCLIC COMPOUNDS AND METHODS FOR USING THE SAME 未知
公开(公告)号：SG186850A1
公开(公告)日：2013-02-28
申请号：SG2012095964
申请日：2011-07-29
申请人： RIGEL PHARMACEUTICALS INC
发明人： GOFF DANE , PAYAN DONALD , SINGH RAJINDER , SHAW SIMON , CARROLL DAVID , HITOSHI YASUMICHI
摘要： Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by "B", T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

24. 发明专利

HK1164146A1 AXL INHIBITORS FOR USE IN COMBINATION THERAPY FOR PREVENTING, TREATING OR MANAGING METASTATIC CANCER AXL 未知
公开(公告)号：HK1164146A1
公开(公告)日：2012-09-21
申请号：HK12104971
申请日：2012-05-22
申请人： RIGEL PHARMACEUTICALS INC
发明人： HITOSHI YASUMICHI , HOLLAND SACHA , PAYAN DONALD G
IPC分类号： A61K20060101
摘要： This invention is directed to methods of preventing, treating or managing cancer, preferably metastatic cancer, in a patient. The methods comprise administering an effective amount of an Axl inhibitor in combination with the administration of an effective amount of one or more chemotherapeutic agents.

25. 发明专利

AU2002332441A8 Mre11: modulation of cellular proliferation 未知
公开(公告)号：AU2002332441A8
公开(公告)日：2010-02-11
申请号：AU2002332441
申请日：2002-07-31
申请人： RIGEL PHARMACEUTICALS INC
发明人： HITOSHI YASUMICHI , DEMO SUSAN , JENKINS YONCHU
IPC分类号： C12Q1/68 , A61K38/43 , A61K48/00 , C12N9/00 , C12N9/22 , C12Q1/34 , G01N33/50 , G01N33/573
摘要： The present invention relates to regulation of cellular proliferation. More particularly, the present invention is directed to nucleic acids encoding MRE11, which is a protein involved in modulation of cellular proliferation. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions, antibodies, peptides, cyclic peptides, nucleic acids, antisense nucleic acids, and ribozymes, that modulate cellular proliferation via modulation of MRE11; as well as to the use of expression profiles and compositions in diagnosis and therapy related to modulation of cellular proliferation.

26. 发明专利

DE60230684D1 未知
公开(公告)号：DE60230684D1
公开(公告)日：2009-02-12
申请号：DE60230684
申请日：2002-07-31
申请人： RIGEL PHARMACEUTICALS INC
发明人： DEMO SUSAN , HITOSHI YASUMICHI , JENKINS YONCHU
IPC分类号： C12Q1/68 , A61K38/00 , A61K39/395 , A61K48/00 , C12Q1/48 , G01N33/53 , G01N33/574
摘要： The present invention relates to regulation of cellular proliferation. More particularly, the present invention is directed to nucleic acids encoding SAK, which is a protein kinase involved in modulation of cellular proliferation and cell cycle regulation. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions, antibodies, peptides, cyclic peptides, nucleic acids, RNAi, antisense nucleic acids, and ribozymes, that modulate cell cycle regulation and cellular proliferation via modulation of SAK; as well as to the use of expression profiles and compositions in diagnosis and therapy related to cell cycle regulation and modulation of cellular proliferation, e.g., for treatment of cancer and other diseases of cellular proliferation.

27. 发明专利

AU2002318934A8 Sak: modulation of cellular proliferation for treatment of cancer 未知
公开(公告)号：AU2002318934A8
公开(公告)日：2005-11-17
申请号：AU2002318934
申请日：2002-07-31
申请人： RIGEL PHARMACEUTICALS INC
发明人： JENKINS YONCHU , DEMO SUSAN , HITOSHI YASUMICHI
IPC分类号： A61K38/00 , G01N33/574 , C12Q1/68 , A61K39/395 , G01N33/53 , C12Q1/48 , A61K48/00 , A61K7/46
摘要： The present invention relates to regulation of cellular proliferation. More particularly, the present invention is directed to nucleic acids encoding SAK, which is a protein kinase involved in modulation of cellular proliferation and cell cycle regulation. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions, antibodies, peptides, cyclic peptides, nucleic acids, RNAi, antisense nucleic acids, and ribozymes, that modulate cell cycle regulation and cellular proliferation via modulation of SAK; as well as to the use of expression profiles and compositions in diagnosis and therapy related to cell cycle regulation and modulation of cellular proliferation, e.g., for treatment of cancer and other diseases of cellular proliferation.

28. 发明专利

AU2002318934A1 Sak: modulation of cellular proliferation for treatment of cancer 未知
公开(公告)号：AU2002318934A1
公开(公告)日：2003-02-17
申请号：AU2002318934
申请日：2002-07-31
申请人： RIGEL PHARMACEUTICALS INC
发明人： JENKINS YONCHU , DEMO SUSAN , HITOSHI YASUMICHI
IPC分类号： A61K38/00 , G01N33/574
摘要： The present invention relates to regulation of cellular proliferation. More particularly, the present invention is directed to nucleic acids encoding SAK, which is a protein kinase involved in modulation of cellular proliferation and cell cycle regulation. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions, antibodies, peptides, cyclic peptides, nucleic acids, RNAi, antisense nucleic acids, and ribozymes, that modulate cell cycle regulation and cellular proliferation via modulation of SAK; as well as to the use of expression profiles and compositions in diagnosis and therapy related to cell cycle regulation and modulation of cellular proliferation, e.g., for treatment of cancer and other diseases of cellular proliferation.

29. 发明公开

EP1549760A4 SAK: MODULATION OF CELLULAR PROLIFERATION FOR TREATMENT OF CANCER 有权
标题翻译： SAK：调制癌症治疗的细胞增殖
公开(公告)号：EP1549760A4
公开(公告)日：2006-04-26
申请号：EP02750377
申请日：2002-07-31
申请人： RIGEL PHARMACEUTICALS INC
发明人： DEMO SUSAN , HITOSHI YASUMICHI , JENKINS YONCHU
IPC分类号： A61K38/00 , G01N33/574 , C12Q1/68 , A61K7/46 , A61K39/395 , A61K48/00 , C12Q1/48 , G01N33/53
CPC分类号： G01N33/57484 , A61K38/00 , A61K2039/505 , G01N2333/912

30. 发明专利

AU2010204578B2 AXL inhibitors for use in combination therapy for preventing, treating or managing metastatic cancer 未知
公开(公告)号：AU2010204578B2
公开(公告)日：2016-05-12
申请号：AU2010204578
申请日：2010-01-15
申请人： RIGEL PHARMACEUTICALS INC
发明人： HITOSHI YASUMICHI , HOLLAND SACHA , PAYAN DONALD G
IPC分类号： A61K31/4196 , A61K31/00 , A61P35/00
摘要： This invention is directed to methods of preventing, treating or managing cancer, preferably metastatic cancer, in a patient. The methods comprise administering an effective amount of an AxI inhibitor in combination with the administation of an effective amount of one or more chemotherapeutic agents.

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