Patent(s) and the Corresponding Patented Drug(s) |
Top |
United States Patent and Trademark Office (USPTO) |
Patent ID |
US9737525 |
Title |
Small molecule activators of NRF2 pathway |
Abstract |
This disclosure relates to compounds that act as activators of the NRF2/KEAP1/ARE pathway. Specifically, the compounds provided herein can act as high affinity reversible bindings for the NRF2 inhibitor, KEAP1. In some cases, NRF2/KEAP1/ARE pathway activation compounds are capable of repressing expression of inflammatory markers and/or reducing levels of TNFa to provide neuroprotective anti-inflammatory effects in the CNS. Such compounds are useful in the treatment of a variety of diseases including Huntington's disease, Parkinson's disease, Alzheimer's disease, inflammation, and cancer. |
Applicant(s) |
The General Hospital Corporation; The Regents of the University of California |
Representative Drug(s) |
D0F6NT |
Drug Info
|
IC50 = 7000 nM |
Click to Show More |
[1] |
2
|
D0Y1WA
|
Drug Info
|
IC50 = 10000 nM
|
[1] |
3
|
D07YHN
|
Drug Info
|
IC50 > 50000000nM
|
[1] |
Patent ID |
US9737525 |
Title |
Small molecule activators of NRF2 pathway |
Abstract |
This disclosure relates to compounds that act as activators of the NRF2/KEAP1/ARE pathway. Specifically, the compounds provided herein can act as high affinity reversible bindings for the NRF2 inhibitor, KEAP1. In some cases, NRF2/KEAP1/ARE pathway activation compounds are capable of repressing expression of inflammatory markers and/or reducing levels of TNFa to provide neuroprotective anti-inflammatory effects in the CNS. Such compounds are useful in the treatment of a variety of diseases including Huntington's disease, Parkinson's disease, Alzheimer's disease, inflammation, and cancer. |
Applicant(s) |
The General Hospital Corporation; The Regents of the University of California |
Representative Drug(s) |
D0F6NT |
Drug Info
|
IC50 = 7000 nM |
Click to Show More |
[1] |
2
|
D0Y1WA
|
Drug Info
|
IC50 = 10000 nM
|
[1] |
3
|
D07YHN
|
Drug Info
|
IC50 > 50000000nM
|
[1] |
Patent ID |
US9737525 |
Title |
Small molecule activators of NRF2 pathway |
Abstract |
This disclosure relates to compounds that act as activators of the NRF2/KEAP1/ARE pathway. Specifically, the compounds provided herein can act as high affinity reversible bindings for the NRF2 inhibitor, KEAP1. In some cases, NRF2/KEAP1/ARE pathway activation compounds are capable of repressing expression of inflammatory markers and/or reducing levels of TNFa to provide neuroprotective anti-inflammatory effects in the CNS. Such compounds are useful in the treatment of a variety of diseases including Huntington's disease, Parkinson's disease, Alzheimer's disease, inflammation, and cancer. |
Applicant(s) |
The General Hospital Corporation; The Regents of the University of California |
Representative Drug(s) |
D0F6NT |
Drug Info
|
IC50 = 7000 nM |
Click to Show More |
[1] |
2
|
D0Y1WA
|
Drug Info
|
IC50 = 10000 nM
|
[1] |
3
|
D07YHN
|
Drug Info
|
IC50 > 50000000nM
|
[1] |
Patent ID |
US9365508 |
Title |
Aroyl thiourea derivatives |
Abstract |
The invention provides compounds according to formula (I): (wherein X, Y, Z1 R1, R2, R3, Ar and Ar are as defined herein), and physiologically acceptable salts, solvates, esters or amides thereof, pharmaceutical compositions comprising these compounds and the compounds for use in medicine, for example for the treatment or prophylaxis of diseases involving cell proliferation, such as cancer, and for the treatment or prophylaxis of other diseases. |
Applicant(s) |
University Court of the University of St Andrews; University Court of the University of Dundee |
Representative Drug(s) |
D07NKC |
Drug Info
|
IC50 = 21200 nM |
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[2] |
2
|
D0V2UZ
|
Drug Info
|
IC50 = 32500 nM
|
[2] |
3
|
D00RNS
|
Drug Info
|
IC50 = 39500 nM
|
[2] |
Patent ID |
US9365508 |
Title |
Aroyl thiourea derivatives |
Abstract |
The invention provides compounds according to formula (I): (wherein X, Y, Z1 R1, R2, R3, Ar and Ar are as defined herein), and physiologically acceptable salts, solvates, esters or amides thereof, pharmaceutical compositions comprising these compounds and the compounds for use in medicine, for example for the treatment or prophylaxis of diseases involving cell proliferation, such as cancer, and for the treatment or prophylaxis of other diseases. |
Applicant(s) |
University Court of the University of St Andrews; University Court of the University of Dundee |
Representative Drug(s) |
D07NKC |
Drug Info
|
IC50 = 21200 nM |
Click to Show More |
[2] |
2
|
D0V2UZ
|
Drug Info
|
IC50 = 32500 nM
|
[2] |
3
|
D00RNS
|
Drug Info
|
IC50 = 39500 nM
|
[2] |
Patent ID |
US9365508 |
Title |
Aroyl thiourea derivatives |
Abstract |
The invention provides compounds according to formula (I): (wherein X, Y, Z1 R1, R2, R3, Ar and Ar are as defined herein), and physiologically acceptable salts, solvates, esters or amides thereof, pharmaceutical compositions comprising these compounds and the compounds for use in medicine, for example for the treatment or prophylaxis of diseases involving cell proliferation, such as cancer, and for the treatment or prophylaxis of other diseases. |
Applicant(s) |
University Court of the University of St Andrews; University Court of the University of Dundee |
Representative Drug(s) |
D07NKC |
Drug Info
|
IC50 = 21200 nM |
Click to Show More |
[2] |
2
|
D0V2UZ
|
Drug Info
|
IC50 = 32500 nM
|
[2] |
3
|
D00RNS
|
Drug Info
|
IC50 = 39500 nM
|
[2] |
Patent ID |
US9359293 |
Title |
Methods of treatment using modulators of SIRT2 |
Abstract |
The instant application describes novel compounds that modulate (in particular, inhibit) Sirt2 , with structures according to Formulas (1) and (2) provided herein. The invention is also directed to pharmaceutical compositions thereof, methods of treatment (i.e., cancer and neurodegenerative disease) by administration of the modulating compounds, assay methods for finding modulators of Sirt2 , and kits for practicing the assay method. |
Applicant(s) |
CORNELL UNIVERSITY |
Representative Drug(s) |
D0MW0K |
Drug Info
|
IC50 = 50 nM |
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[3] |
2
|
D0X9SE
|
Drug Info
|
IC50 = 3000 nM
|
[3] |
3
|
D0PL1I
|
Drug Info
|
IC50 = 105000 nM
|
[3] |
Patent ID |
US9359293 |
Title |
Methods of treatment using modulators of SIRT2 |
Abstract |
The instant application describes novel compounds that modulate (in particular, inhibit) Sirt2 , with structures according to Formulas (1) and (2) provided herein. The invention is also directed to pharmaceutical compositions thereof, methods of treatment (i.e., cancer and neurodegenerative disease) by administration of the modulating compounds, assay methods for finding modulators of Sirt2 , and kits for practicing the assay method. |
Applicant(s) |
CORNELL UNIVERSITY |
Representative Drug(s) |
D0MW0K |
Drug Info
|
IC50 = 50 nM |
Click to Show More |
[3] |
2
|
D0X9SE
|
Drug Info
|
IC50 = 3000 nM
|
[3] |
3
|
D0PL1I
|
Drug Info
|
IC50 = 105000 nM
|
[3] |
Patent ID |
US9359293 |
Title |
Methods of treatment using modulators of SIRT2 |
Abstract |
The instant application describes novel compounds that modulate (in particular, inhibit) Sirt2 , with structures according to Formulas (1) and (2) provided herein. The invention is also directed to pharmaceutical compositions thereof, methods of treatment (i.e., cancer and neurodegenerative disease) by administration of the modulating compounds, assay methods for finding modulators of Sirt2 , and kits for practicing the assay method. |
Applicant(s) |
CORNELL UNIVERSITY |
Representative Drug(s) |
D0MW0K |
Drug Info
|
IC50 = 50 nM |
Click to Show More |
[3] |
2
|
D0X9SE
|
Drug Info
|
IC50 = 3000 nM
|
[3] |
3
|
D0PL1I
|
Drug Info
|
IC50 = 105000 nM
|
[3] |