Target and Its Patented Drug(s)

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Target General Information
Patent(s) and the Corresponding Patented Drug(s)
References
Target General Information  Top
Target ID T13176 Target Info
Target Name PRKR-like endoplasmic reticulum kinase (PERK)
Synonyms PEK
Target Type Clinical trial Target
Gene Name EIF2AK3
Biochemical Class Kinase
UniProt ID
E2AK3_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2015136463
Title Chemical Compounds Acting As Perk Inhibitors.
Abstract The invention is directed to substituted pyrrolidinone derivatives. Specifically, the invention is directed to compounds according to Formula X: wherein R41, R42, R43, R44, R45, R46, and R47 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, diabetes, Parkinson disease, Huntington's disease, Creutzfeldt- Jakob Disease, and related prion diseases, amyotrophic lateral sclerosis, myocardial infarction, neurodegeneration, cardiovascular disease, atherosclerosis, ocular diseases, and arrhythmias, more specifically cancers of the breast, colon, pancreas 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.
Applicant(s) Glaxosmithkline Intellectual Property (No.2) Limited
Representative Drug(s) D08JII Drug Info pIC50 > 6.4 Click to Show More [1]
2 D0D4FR Drug Info pIC50 > 6.4 [1]
3 D04AMY Drug Info pIC50 = 8 [1]
Patent ID WO2014161808
Title Novel N-(2,3-Dihydro-1H-Pyrrolo[2,3-B]Jpyridin-5-Yl)-4- Quinazolinamine and N-(2,3-Dihydro-1H-Indol-5-Yl)-4- Quinazolinamine Derivatives As Perk Inhibitors.
Abstract The present invention relates to N-(2,3-dihydro-1H-pyrrolo[2,3-b)]pyridin-5-yl)-4-quinazolinamine and N-(2.3-dihydro-1H-indol-5-yl)-4-quinazolinamine derivatives of Formula (I) wherein R1, R2, R3, R4,.
Applicant(s) Janssen Pharmaceutica Nv
Representative Drug(s) D0RX8U Drug Info pIC50 = 6.7 Click to Show More [1]
2 D0G5EI Drug Info pIC50 = 8.1 [1]
3 D0NA2Q Drug Info pIC50 = 8.4 [1]
4 D0H1WN Drug Info pIC50 = 9.4 [1]
Patent ID WO2012013557
Title Isoxazolo-Quinazolines As Modulators of Protein Kinase Activity.
Abstract The present invention relates to substituted isoxazolo-quinazolines which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular human MPS1 and PERK. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
Applicant(s) Nerviano Medical Sciences S.R.L
Representative Drug(s) D0JC8E Drug Info IC50 = 240 nM Click to Show More [1]
2 D06GGI Drug Info IC50 = 400 nM [1]
3 D08HTR Drug Info N.A. [1]
Patent ID WO2011119663
Title Chemical Compounds.
Abstract 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.
Applicant(s) Glaxosmithkline Llc
Representative Drug(s) D0DY3E Drug Info pIC50 >= 7.5 Click to Show More [1]
2 D0KH5D Drug Info N.A. [1]
Patent ID WO2015056180
Title Indoline Derivatives As Inhibitors of Perk.
Abstract The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: (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 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, pancreas 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.
Applicant(s) Glaxosmithkline Intellectual Property (No.2) Limited
Representative Drug(s) D06PIO Drug Info pIC50 = 8.4 Click to Show More [1]
2 D0KH5D Drug Info N.A. [1]
Patent ID WO2016024010
Title Perk Activator for The Treatment of Neurodegenerative Diseases.
Abstract The present invention relates to a novel method for the treatment and/or prophylaxis of a tau-mediated neurodegenerative disease and/or of a tau-mediated neurodegenerative pathological condition, especially of a neurodegenerative disease and/or of a neurodegenerative pathological condition associated with and/or accompanied by tau aggregation, and in particular for the treatment and/or prophylaxis of a tauopathy; compounds and/or agents and compositions for such treatment and/or prophylaxis, and the manufacture of the compounds and/or agents and compositions suitable for the said treatment and/or prophylaxis. In this regard, the present invention relates especially to the use of compounds acting as PERK activator, a prodrug thereof, a derivative thereof and/or a pharmaceutically acceptable salt of any thereof, as a medicament. In contrast to the prior art which addresses mainly PERK inhibition, or occasionally only the apoptotic arm of PERK of activation, the present invention pertains to the effects of indirect or direct PERK activation achieved via the neuroprotective arm of PERK signaling.
Applicant(s) Deutsches Zentrum Fr Neurodegenerative Erkrankungen
References  Top
REF 1 Protein kinase R(PKR)-like endoplasmic reticulum kinase (PERK) inhibitors: a patent review (2010-2015).Expert Opin Ther Pat. 2017 Jan;27(1):37-48.

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