- PERK INHIBITING PYRROLOPYRIMIDINE COMPOUNDS
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Provided herein are compounds of formula (I), compositions, and methods useful for inhibiting PERK and for treating related conditions diseases, and disorders.
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Paragraph 0158; 0161; 0162
(2021/03/05)
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- PERK INHIBITING INDOLINYL COMPOUNDS
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Provided herein are compounds of formula (I), compositions, and methods useful for inhibiting PERK and for treating related conditions diseases, and disorders, wherein Q is selected from (Ia), (Ib) ou (Ic).
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Paragraph 0150; 0151
(2021/03/05)
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- PERK INHIBITING PYRROLOPYRIMIDINE COMPOUNDS TO TREAT VIRAL INFECTIONS
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Provided herein are methods for treating a viral infection in a patient, comprising administering to said patient a therapeutically effective amount of a PERK inhibitor selected from a compound having the structure (I):
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Page/Page column 76; 77
(2021/11/20)
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- FGFR INHIBITORS AND METHODS OF USE THEREOF
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The present disclosure relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of FGFR enzymes with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with FGFR signaling with the compounds and compositions of the disclosure.
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Paragraph 0291
(2020/11/30)
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- PHENYL-2-HYDROXY-ACETYLAMINO-2-METHYL-PHENYL COMPOUNDS
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The present invention provides phenyl-2-hydroxy-acetylamino-2-methyl-phenyl compounds, to pharmaceutical compositions comprising the compounds, to methods of using the compounds to treat physiological disorders such as cancer.
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Page/Page column 16
(2018/11/22)
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- A critical evaluation of pyrrolo[2,3-d]pyrimidine-4-amines as Plasmodium falciparum apical membrane antigen 1 (AMA1) inhibitors
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We have determined that a previously reported class of pyrrolo[2,3-d]pyrimidine-4-amines exhibit low binding to apical membrane antigen 1 (AMA1) and suffer from unattractive qualities, such as aggregation. We attempted to remove these traits by generating
- Devine, Shane M.,Lim, San Sui,Chandrashekaran, Indu R.,Macraild, Christopher A.,Drew, Damien R.,Debono, Cael O.,Lam, Raymond,Anders, Robin F.,Beeson, James G.,Scanlon, Martin J.,Scammells, Peter J.,Norton, Raymond S.
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supporting information
p. 1500 - 1506
(2014/12/10)
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- Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro- 1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK)
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Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states. Evidence that PERK is implicated in tumori-genesis and cancer cell survival stim
- Axten, Jeffrey M.,Medina, Jesús R.,Feng, Yanhong,Shu, Arthur,Romeril, Stuart P.,Grant, Seth W.,Li, William Hoi Hong,Heerding, Dirk A.,Minthorn, Elisabeth,Mencken, Thomas,Atkins, Charity,Liu, Qi,Rabindran, Sridhar,Kumar, Rakesh,Hong, Xuan,Goetz, Aaron,Stanley, Thomas,Taylor, J. David,Sigethy, Scott D.,Tomberlin, Ginger H.,Hassell, Annie M.,Kahler, Kirsten M.,Shewchuk, Lisa M.,Gampe, Robert T.
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p. 7193 - 7207
(2012/11/07)
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- CHEMICAL COMPOUNDS
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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.
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Page/Page column 82
(2011/10/13)
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