Patent(s) and the Corresponding Patented Drug(s) |
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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 |
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[1] |
2
|
D0D4FR
|
Drug Info
|
pIC50 > 6.4
|
[1] |
3
|
D0U8IL
|
Drug Info
|
pIC50 > 6.4
|
[1] |
4
|
D04AMY
|
Drug Info
|
pIC50 = 8
|
[1] |
5
|
D0Z5NP
|
Drug Info
|
pIC50 > 8.3
|
[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 |
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[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] |
5
|
D0YF7Q
|
Drug Info
|
N.A.
|
[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 |
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[1] |
2
|
D06GGI
|
Drug Info
|
IC50 = 400 nM
|
[1] |
3
|
D0WK2S
|
Drug Info
|
IC50 = 510 nM
|
[1] |
4
|
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 |
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[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 |
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[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 |