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 T28052 Target Info
Target Name Lysine-specific demethylase 5A (KDM5A)
Synonyms Retinoblastoma-binding protein 2; RBP2; RBBP2; RBBP-2; Jumonji/ARID domain-containing protein 1A; JARID1A; Histone demethylase JARID1A
Target Type Patented-recorded Target
Gene Name KDM5A
Biochemical Class Paired donor oxygen oxidoreductase
UniProt ID
KDM5A_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
United States Patent and Trademark Office (USPTO)
Patent ID US9738637
Title Histone demethylase inhibitors
Abstract The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrrolopyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Applicant(s) Celgene Quantical Research, Inc.
Representative Drug(s) D0PQ5P Drug Info IC50 < 100nM [1]
Patent ID US9725441
Title Histone demethylase inhibitors
Abstract The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Applicant(s) Celgene Quanticel Research, Inc.
Representative Drug(s) D05CCY Drug Info IC50 = 550 nM [2]
Patent ID US9714230
Title Histone demethylase inhibitors
Abstract Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Applicant(s) Celgene Quantical Research, Inc.
Representative Drug(s) D0GH8J Drug Info IC50 < 100nM Click to Show More [3]
2 D00SUC Drug Info IC50 < 100nM [3]
3 D03TKM Drug Info IC50 = 550 nM [3]
Patent ID US9714230
Title Histone demethylase inhibitors
Abstract Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Applicant(s) Celgene Quantical Research, Inc.
Representative Drug(s) D0GH8J Drug Info IC50 < 100nM Click to Show More [3]
2 D00SUC Drug Info IC50 < 100nM [3]
3 D03TKM Drug Info IC50 = 550 nM [3]
Patent ID US9714230
Title Histone demethylase inhibitors
Abstract Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Applicant(s) Celgene Quantical Research, Inc.
Representative Drug(s) D0GH8J Drug Info IC50 < 100nM Click to Show More [3]
2 D00SUC Drug Info IC50 < 100nM [3]
3 D03TKM Drug Info IC50 = 550 nM [3]
Patent ID US9617242
Title Histone demethylase inhibitors
Abstract The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted 3-aminopyridine derivative compounds, substituted 3-aminopyridazine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Applicant(s) CELGENE QUANTICEL RESEARCH, INC.
Representative Drug(s) D01WHH Drug Info IC50 < 100nM [4]
Patent ID US9611221
Title Histone demethylase inhibitors
Abstract The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Applicant(s) Celgene Quanticel Research, Inc.
Representative Drug(s) D09CWB Drug Info IC50 < 100nM Click to Show More [5]
2 D0NG8M Drug Info IC50 = 550 nM [5]
Patent ID US9611221
Title Histone demethylase inhibitors
Abstract The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Applicant(s) Celgene Quanticel Research, Inc.
Representative Drug(s) D09CWB Drug Info IC50 < 100nM Click to Show More [5]
2 D0NG8M Drug Info IC50 = 550 nM [5]
Patent ID US9604961
Title Histone demethylase inhibitors
Abstract Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Applicant(s) Celgene Quanticel Research, Inc.
Representative Drug(s) D0F3TL Drug Info IC50 < 10nM [6]
Patent ID US10179769
Title Histone demethylase inhibitors
Abstract The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted amidopyridine or amidopyridazine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Applicant(s) Celgene Quanticel Research, Inc.
Representative Drug(s) D0HT9Q Drug Info IC50 < 100nM [7]
Patent ID US10174026
Title Histone demethylase inhibitors
Abstract The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrrolopyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Applicant(s) CELGENE QUANTICEL RESEARCH, INC.
Representative Drug(s) D0N9JZ Drug Info IC50 < 100nM Click to Show More [8]
2 D0R2GT Drug Info IC50 = 550 nM [8]
3 D0ZJ0Z Drug Info IC50 = 5500 nM [8]
Patent ID US10174026
Title Histone demethylase inhibitors
Abstract The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrrolopyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Applicant(s) CELGENE QUANTICEL RESEARCH, INC.
Representative Drug(s) D0N9JZ Drug Info IC50 < 100nM Click to Show More [8]
2 D0R2GT Drug Info IC50 = 550 nM [8]
3 D0ZJ0Z Drug Info IC50 = 5500 nM [8]
Patent ID US10174026
Title Histone demethylase inhibitors
Abstract The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrrolopyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Applicant(s) CELGENE QUANTICEL RESEARCH, INC.
Representative Drug(s) D0N9JZ Drug Info IC50 < 100nM Click to Show More [8]
2 D0R2GT Drug Info IC50 = 550 nM [8]
3 D0ZJ0Z Drug Info IC50 = 5500 nM [8]
Patent ID US10173996
Title Histone demethylase inhibitors
Abstract Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Applicant(s) Celgene Quanticel Research, Inc.
Representative Drug(s) D0K4LW Drug Info IC50 < 100nM [9]
Patent ID US10040779
Title Histone demethylase inhibitors
Abstract The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted 3-aminopyridine derivative compounds, substituted 3-aminopyridazine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Applicant(s) Celgene Quanticel Research, Inc.
Representative Drug(s) D0VZ5E Drug Info IC50 < 0.1nM Click to Show More [10]
2 D06TKT Drug Info IC50 < 0.1nM [10]
3 D0G8QR Drug Info IC50 < 0.1nM [10]
Patent ID US10040779
Title Histone demethylase inhibitors
Abstract The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted 3-aminopyridine derivative compounds, substituted 3-aminopyridazine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Applicant(s) Celgene Quanticel Research, Inc.
Representative Drug(s) D0VZ5E Drug Info IC50 < 0.1nM Click to Show More [10]
2 D06TKT Drug Info IC50 < 0.1nM [10]
3 D0G8QR Drug Info IC50 < 0.1nM [10]
Patent ID US10040779
Title Histone demethylase inhibitors
Abstract The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted 3-aminopyridine derivative compounds, substituted 3-aminopyridazine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Applicant(s) Celgene Quanticel Research, Inc.
Representative Drug(s) D0VZ5E Drug Info IC50 < 0.1nM Click to Show More [10]
2 D06TKT Drug Info IC50 < 0.1nM [10]
3 D0G8QR Drug Info IC50 < 0.1nM [10]
Patent ID US10022354
Title IRE-1 inhibitors
Abstract Compounds which directly inhibit IRE-1 activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
Applicant(s) GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS INC.
Representative Drug(s) D03POM Drug Info IC50 = 0.065 nM Click to Show More [11]
2 D0T8YT Drug Info IC50 = 0.083 nM [11]
3 D0NM3B Drug Info IC50 = 7.4 nM [11]
Patent ID US10022354
Title IRE-1 inhibitors
Abstract Compounds which directly inhibit IRE-1 activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
Applicant(s) GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS INC.
Representative Drug(s) D03POM Drug Info IC50 = 0.065 nM Click to Show More [11]
2 D0T8YT Drug Info IC50 = 0.083 nM [11]
3 D0NM3B Drug Info IC50 = 7.4 nM [11]
Patent ID US10022354
Title IRE-1 inhibitors
Abstract Compounds which directly inhibit IRE-1 activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
Applicant(s) GENENTECH, INC.; CONSTELLATION PHARMACEUTICALS INC.
Representative Drug(s) D03POM Drug Info IC50 = 0.065 nM Click to Show More [11]
2 D0T8YT Drug Info IC50 = 0.083 nM [11]
3 D0NM3B Drug Info IC50 = 7.4 nM [11]
References  Top
REF 1 Histone demethylase inhibitors. US9738637.
REF 2 Histone demethylase inhibitors. US9725441.
REF 3 Histone demethylase inhibitors. US9714230.
REF 4 Histone demethylase inhibitors. US9617242.
REF 5 Histone demethylase inhibitors. US9611221.
REF 6 Histone demethylase inhibitors. US9604961.
REF 7 Histone demethylase inhibitors. US10179769.
REF 8 Histone demethylase inhibitors. US10174026.
REF 9 Histone demethylase inhibitors. US10173996.
REF 10 Histone demethylase inhibitors. US10040779.
REF 11 IRE-1 inhibitors

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