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1. 发明申请

WO2011119663A8 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2011119663A8
公开(公告)日：2012-10-26
申请号：PCT/US2011029511
申请日：2011-03-23
申请人： GLAXOSMITHKLINE LLC , AXTEN JEFFREY MICHAEL , GRANT SETH WILSON , HEERDING DIRK A , MEDINA JESUS RAUL , ROMERIL STUART PAUL , TANG JUN
发明人： AXTEN JEFFREY MICHAEL , GRANT SETH WILSON , HEERDING DIRK A , MEDINA JESUS RAUL , ROMERIL STUART PAUL , TANG JUN
IPC分类号： A01N43/38 , A61K31/405
CPC分类号： C07D487/04 , A61K31/405 , A61K45/06 , C07D403/04 , C07D491/04 , C07D495/04 , A61K2300/00
摘要： The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I wherein R1, R2 and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译：本发明涉及取代的二氢吲哚衍生物。具体地，本发明涉及式I化合物，其中R 1，R 2和R 3在本文中定义。本发明的化合物是PERK的抑制剂，可用于治疗癌症，眼部疾病和与活化的未折叠蛋白反应途径相关的疾病，例如阿尔茨海默病，中风，1型糖尿病帕金森病，亨廷顿病，肌萎缩性侧索硬化症，心肌梗死，心血管疾病，动脉粥样硬化和心律失常，更具体地说是乳腺癌，结肠癌，胰腺癌和肺癌。因此，本发明进一步涉及包含本发明化合物的药物组合物。本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物抑制PERK活性和与之相关疾病的治疗方法。

2. 发明专利

ZA201206746B CHEMICAL COMPOUNDS 未知
公开(公告)号：ZA201206746B
公开(公告)日：2013-05-29
申请号：ZA201206746
申请日：2012-09-10
申请人： GLAXOSMITHKLINE LLC
发明人： AXTEN JEFFREY MICHAEL , GRANT SETH WILSON , HEERDING DIRK A , MEDINA JESUS RAUL , ROMERIL STUART PAUL , TANG JUN
IPC分类号： A01N20060101 , A61K20060101
摘要： The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

3. 发明专利

CA2794153C SUBSTITUTED INDOLINE DERIVATIVES AS PERK INHIBITORS 未知
公开(公告)号：CA2794153C
公开(公告)日：2018-01-02
申请号：CA2794153
申请日：2011-03-23
申请人： GLAXOSMITHKLINE LLC
发明人： AXTEN JEFFREY MICHAEL , GRANT SETH WILSON , HEERDING DIRK A , MEDINA JESUS RAUL , ROMERIL STUART PAUL , TANG JUN
IPC分类号： C07D487/04 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/506 , A61K31/519 , A61P27/02 , A61P35/00 , C07D403/10 , C07D471/04 , C07D491/048 , C07D495/04
摘要： The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I wherein R1, R2 and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

4. 发明专利

CA2794153A1 CHEMICAL COMPOUNDS 未知
公开(公告)号：CA2794153A1
公开(公告)日：2011-09-29
申请号：CA2794153
申请日：2011-03-23
申请人： GLAXOSMITHKLINE LLC
发明人： AXTEN JEFFREY MICHAEL , GRANT SETH WILSON , HEERDING DIRK A , MEDINA JESUS RAUL , ROMERIL STUART PAUL , TANG JUN
IPC分类号： C07D487/04 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/506 , A61K31/519 , A61P27/02 , A61P35/00 , C07D403/10 , C07D471/04 , C07D491/048 , C07D495/04
摘要： The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I wherein R1, R2 and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

5. 发明专利

ES2530955T3 Compuestos químicos 未知
公开(公告)号：ES2530955T3
公开(公告)日：2015-03-09
申请号：ES11760102
申请日：2011-03-23
申请人： GLAXOSMITHKLINE LLC
发明人： AXTEN JEFFREY MICHAEL , GRANT SETH WILSON , HEERDING DIRK A , MEDINA JESUS RAUL , ROMERIL STUART PAUL , TANG JUN
IPC分类号： C07D403/04 , A61K31/06 , A61K31/405 , A61P35/00 , C07D487/04 , C07D491/04 , C07D495/04
摘要： Un compuesto de acuerdo con la Fórmula (I):**Fórmula** en la que: R1 se selecciona de: bicicloheteroarilo, y bicicloheteroarilo sustituido con 1 a 5 sustituyentes independientemente seleccionados de: halógeno, alquilo C1-6, alquiloxi C1-4, -OH, hidroxialquilo C1-4, -COOH, -CONH2, tetrazol, -CF3, -alquil(C1-4)-O-alquilo(C1-4), -CH2CH2N(H)C(O)OCH2arilo di(alquil C1-4)amino(alquilo C1-4) aminoalquilo(C1-4), -NO2, -NH2, -CN, arilo, arilo sustituido con 1 a 3 sustituyentes independientemente seleccionados de: alquilo C1-4, di(alquil C1- 4)amino(alquilo C1-4), fluoro, cloro, bromo, yodo y -CF3, heterocicloalquilo, heterocicloalquilo sustituido con uno a tres sustituyentes seleccionados independientemente de: alquilo C1-4, di(alquil C1-4)amino(alquilo C1-4), fluoro, cloro, bromo, yodo y -CF3, -(alquil C1-4)-heterocicloalquilo, -(alquil C1-4)-heterocicloalquilo sustituido con 1 a 3 sustituyentes independientemente seleccionados de: alquilo C1-4, di-alquil C1-4-amino-alquilo C1-4, fluoro, cloro, bromo, yodo y -CF3, heteroarilo, y heteroarilo sustituido con uno a tres sustituyentes seleccionados independientemente de: alquilo C1-4, di-(alquil C1-4)-amino-(alquilo C1-4), fluoro, cloro, bromo, yodo y -CF3; R2 se selecciona de: arilo, arilo sustituido con 1 a 5 sustituyentes independientemente seleccionados de: fluoro, cloro, bromo, yodo, alquilo C1-4, alquiloxi C1-4, -OH, -COOH, -CONH2, -CF3, -(alquil C1-4)-O-(alquilo C1-4), -NO2, -NH2 y -CN, heteroarilo, heteroarilo sustituido con 1 a 5 sustituyentes independientemente seleccionados de: fluoro, cloro, bromo, yodo, alquilo C1-4, alquiloxi C1-4, -OH, -COOH, -CONH2, -CF3, -(alquil C1-4)-O-(alquilo C1-4), -NO2, -NH2 y -CN, cicloalquilo, y cicloalquilo sustituido con 1 a 5 sustituyentes independientemente seleccionados de: fluoro, cloro, bromo, yodo, alquilo C1-4, alquiloxi C1-4, -OH, -COOH, -CONH2, -CF3, -(alquil C1-4)-O-(alquilo C1-4), -NO2, -NH2 y -CN; y R3 se selecciona de: hidrógeno, fluoro, cloro, bromo y yodo; o una sal del mismo incluyendo una sal farmacéuticamente aceptable del mismo.

6. 发明专利

AU2011232516B2 Chemical compounds 未知
公开(公告)号：AU2011232516B2
公开(公告)日：2014-08-07
申请号：AU2011232516
申请日：2011-03-23
申请人： GLAXOSMITHKLINE LLC
发明人： AXTEN JEFFREY MICHAEL , GRANT SETH WILSON , HEERDING DIRK A , MEDINA JESUS RAUL , ROMERIL STUART PAUL , TANG JUN
IPC分类号： A01N43/38 , A61K31/405
摘要： The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I wherein R

7. 发明专利

AU2011232516A8 Chemical compounds 未知
公开(公告)号：AU2011232516A8
公开(公告)日：2012-12-13
申请号：AU2011232516
申请日：2011-03-23
申请人： GLAXOSMITHKLINE LLC
发明人： AXTEN JEFFREY MICHAEL , GRANT SETH WILSON , HEERDING DIRK A , MEDINA JESUS RAUL , ROMERIL STUART PAUL , TANG JUN
IPC分类号： A01N43/38 , A61K31/405
摘要： The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I wherein R

8. 发明公开

EP2549868A4 CHEMICAL COMPOUNDS 有权
公开(公告)号：EP2549868A4
公开(公告)日：2013-08-07
申请号：EP11760102
申请日：2011-03-23
申请人： GLAXOSMITHKLINE LLC
发明人： AXTEN JEFFREY MICHAEL , GRANT SETH WILSON , HEERDING DIRK A , MEDINA JESUS RAUL , ROMERIL STUART PAUL , TANG JUN
IPC分类号： C07D403/04 , A61K31/06 , A61K31/405 , A61P35/00 , C07D487/04 , C07D491/04 , C07D495/04
CPC分类号： C07D487/04 , A61K31/405 , A61K45/06 , C07D403/04 , C07D491/04 , C07D495/04 , A61K2300/00

9. 发明专利

EA022325B1 ПРОИЗВОДНЫЕ ИНДОЛИНА КАК ИНГИБИТОРЫ PERK 未知
公开(公告)号：EA022325B1
公开(公告)日：2015-12-30
申请号：EA201290952
申请日：2011-03-23
申请人： GLAXOSMITHKLINE LLC
发明人： AXTEN JEFFREY MICHAEL , GRANT SETH WILSON , HEERDING DIRK A , MEDINA JESUS RAUL , ROMERIL STUART PAUL , TANG JUN
IPC分类号： A01N43/38
摘要： Изобретениеотноситсяк замещеннымпроизводныминдолина. Соединенияпоизобретениюявляютсяингибиторами PERK имогутбытьиспользованыв лечениирака, глазныхзаболеванийи заболеваний, связанныхс путямиответовнаактивированныенескрученныебелки, такихкакболезньАльцгеймера, инсульт, диабеттипа 1, болезньПаркинсона, болезньГентингтона, боковойамиотрофическийсклероз, инфарктмиокарда, сердечно-сосудистоезаболевание, атеросклерози аритмии, иболееконкретноракмолочнойжелезы, толстойкишки, поджелудочнойжелезыи легкого. Соответственно, изобретениетакжеотноситсяк фармацевтическимкомпозициям, включающимсоединениепоизобретению. Изобретениетакжеотноситсяк способамингибированияактивности PERK илечениянарушений, связанныхс этойактивностью.

10. 发明专利

BR112012024380A2 compostos químicos 未知
公开(公告)号：BR112012024380A2
公开(公告)日：2015-09-15
申请号：BR112012024380
申请日：2011-03-23
申请人： GLAXOSMITHKLINE LLC
发明人： HEERDING DIRK A , AXTEN JEFFREY MICHAEL , MEDINA JESUS RAUL , TANG JUN , GRANT SETH WILSON , ROMERIL STUART PAUL
IPC分类号： A61K31/405 , A01N43/38
摘要： compostos químicos. a invenção é dirigida aos derivados de indolina substituídos. especificamente, a invenção é dirigida aos compostos de acordo com a fórmula i, onde r^ 1^, r^ 2^ e r^ 3^ são definidos neste documento. os compostos da invenção são inibidores da perk e podem ser úteis no tratamento de câncer, doenças oculares, e doenças associadas com as vias de resposta da proteína não dobrada ativadas, tais como a doença de alzheimer, o acidente vascular cerebral, o diabetes tipo 1, a doença de parkinson, a doença de huntington, a esclerose lateral amiotrófica, o infarto do miocárdio, a doença cardiovascular, a aterosclerose, e as arritimias, e mais especificamente os cânceres da mama, cólon, pancreáticos, e pulmão. consequentemente, a invenção é adicionalmente dirigida ás composições farmacêuticas compreendendo um composto da invenção. a invenção é ainda adicionalmente dirigida aos métodos de inibir a atividade da perk e ao tratamento de distúrbios associados com ela usando um composto da invenção ou uma composição farmacêutica compreendendo um composto da invenção.

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