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 T25265 Target Info
Target Name Enhancer of zeste homolog 2 (EZH2)
Synonyms Lysine Nmethyltransferase 6; Lysine N-methyltransferase 6; KMT6; Histonelysine Nmethyltransferase EZH2; Histone-lysine N-methyltransferase EZH2; EZH2; ENX1; ENX-1
Target Type Successful Target
Gene Name EZH2
Biochemical Class Methyltransferase
UniProt ID
EZH2_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2016089804
Title Inhibitors of Ezh2.
Abstract The present invention relates to compounds that inhibit activity of the histone lysine N-methyltransferase, Enhancer of Zeste Homolog 2 (EZH2), pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat cancer, such as hematologic and solid tumors.
Applicant(s) Eli Lilly and Company
Representative Drug(s) D01PZZ Drug Info IC50 = 0.93 nM Click to Show More [1]
2 D0G1JR Drug Info IC50 = 6.45 nM [1]
Patent ID WO2016066697
Title Enhancer of Zeste Homolog 2 Inhibitors.
Abstract This invention relates to novel compounds according to Formula (I) which are inhibitors of Enhancer of Zeste Homo log 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
Applicant(s) Glaxosmithkline Intellectual Property (No.2) Limited
Representative Drug(s) D0FI3A Drug Info IC50 = 20 nM Click to Show More [1]
2 D03MYI Drug Info IC50 = 100 nM [1]
3 D0Z7GN Drug Info IC50 = 100 nM [1]
4 D0RD5P Drug Info IC50 = 316 nM [1]
5 D0M1TG Drug Info IC50 = 500 nM [1]
Patent ID WO2015200650
Title Substituted Benzene and 6,5-Fused Bicyclic Heteroaryl Compounds.
Abstract The present invention relates to substituted benzene compounds and bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
Applicant(s) Epizyme, Inc
Representative Drug(s) D08MXO Drug Info IC50 < 1000 nM Click to Show More [1]
2 D09GFF Drug Info IC50 < 1000 nM [1]
3 D09PQQ Drug Info IC50 < 1000 nM [1]
4 D0M9BY Drug Info IC50 < 1000 nM [1]
5 D0Z0NC Drug Info IC50 < 1000 nM [1]
Patent ID WO2015193768
Title Aryl Fused Lactams As Ezh2 Modulators.
Abstract This invention relates to compounds of Formula (I) in which R1, R2, R3, R4, X and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
Applicant(s) Pfizer Inc
Representative Drug(s) D0B4TX Drug Info IC50 = 2 nM; Ki < 1 nM Click to Show More [1]
2 D0D4UH Drug Info IC50 = 5 nM [1]
3 D0M8AA Drug Info IC50 = 168000 nM [1]
Patent ID WO2015010078
Title Substituted 6,5-Fused Bicyclic Heteroaryl Compounds.
Abstract The present invention relates to substituted bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
Applicant(s) Epizyme, Inc
Representative Drug(s) D0TA4N Drug Info IC50 = 1470 nM Click to Show More [1]
2 D0GT7A Drug Info IC50 = 21900 nM [1]
Patent ID WO2015004618
Title Enhancer of Zeste Homolog 2 Inhibitors.
Abstract This invention relates to novel compounds according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
Applicant(s) Glaxosmithkline Intellectual Property (No.2) Limited
Representative Drug(s) D0MO2X Drug Info IC50 = 16 nM Click to Show More [1]
2 D0MH8G Drug Info IC50 = 100 nM [1]
Patent ID WO2015077193
Title Inhibitors of Lysine Methyl Transferase.
Abstract There are disclosed compounds that are inhibitors of EZH2, pharmaceutical compositions containing said compounds and methods of treating hyperproliferative, inflammatory, infectious, and immunoregulatory disorders and diseases, utilizing the compounds of the invention.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D0A0VH Drug Info IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM Click to Show More [1]
2 D0FC9J Drug Info IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM [1]
3 D0LR5O Drug Info IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM [1]
4 D0PB6T Drug Info IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM [1]
5 D0BT6Y Drug Info N.A. [1]
6 D0QH1J Drug Info N.A. [1]
Patent ID WO2016073956
Title Ezh2 Inhibitors and Uses Thereof.
Abstract The present disclosure provides compounds of any one of Formulae (I) and (II). The compounds described herein are inhibitors of histone methyltransferases (e.g., enhancer of zeste homolog 1 (EZH1) and enhancer of zeste homolog 2 (EZH2)) and are useful in treating and/or preventing a broad range of diseases (e.g., proliferative diseases). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein. Further provided in the present disclosure are methods of identifying EZH1and/or EZH2 inhibitors.
Applicant(s) Dana-Farber Cancer Institute, Inc
Representative Drug(s) D0CH4O Drug Info IC50 = 80 nM Click to Show More [1]
2 D07CZI Drug Info N.A. [1]
Patent ID WO2015077194
Title Inhibitors of Lysine Methyl Transferase.
Abstract There are disclosed compounds that are inhibitors of EZH2, pharmaceutical compositions containing said compounds and methods of treating hyperproliferative, inflammatory, infectious, and immunoregulatory disorders and diseases utilizing the compounds of the invention.
Applicant(s) Bristol-Myers Squibb Company
Representative Drug(s) D0H4HR Drug Info N.A. Click to Show More [1]
2 D0PI5O Drug Info N.A. [1]
3 D0U9OH Drug Info N.A. [1]
Patent ID WO2015010049
Title Substituted Benzene Compounds.
Abstract The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
Applicant(s) Epizyme, Inc
Representative Drug(s) D0BL8W Drug Info N.A. Click to Show More [1]
2 D0KR2T Drug Info N.A. [1]
3 D0SQ1R Drug Info N.A. [1]
4 D0SY6P Drug Info N.A. [1]
5 D0T8QL Drug Info N.A. [1]
6 D0UG5O Drug Info N.A. [1]
7 D0VF0M Drug Info N.A. [1]
8 D0Z0QS Drug Info N.A. [1]
Patent ID WO2014144747
Title Substituted 6,5-Fused Bicyclic Heteroaryl Compounds.
Abstract The present invention relates to azole bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
Applicant(s) Epizyme, Inc
Representative Drug(s) D04PCW Drug Info N.A. Click to Show More [1]
2 D0R2TQ Drug Info N.A. [1]
3 D0W4MW Drug Info N.A. [1]
Patent ID WO2014124418
Title Preparation of Methyloxodihydropyridinylmethylcarbamoylmethylindole Derivatives and Analogs for Use As Histone Methyl Modifying Enzyme Modulators.
Representative Drug(s) D0D1QD Drug Info N.A. Click to Show More [1]
2 D0DQ6N Drug Info N.A. [1]
3 D0W2KL Drug Info N.A. [1]
Patent ID WO2016102493
Title Imidazopyridine Ezh2 Inhibitors.
Abstract The present invention relates to imidazopyridines of general formula (I), to a method for their preparation, to intermediates for their preparation, to pharmaceutical compositions comprising at least one of those compounds, and to the use thereof.
Applicant(s) Bayer Pharma Aktiengesellschaft the Broad Institute Inc
Representative Drug(s) D0M4LK Drug Info IC50 = 8.13 nM [1]
Patent ID WO2015132765
Title Enhancer of Zeste Homolog 2 Inhibitors.
Abstract This invention relates to novel compounds according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers. (I).
Applicant(s) Glaxosmithkline Intellectual Property (No.2) Limited
Representative Drug(s) D0S4OP Drug Info IC50 = 32 nM [1]
Patent ID WO2016130396
Title Modulators of Methyl Modifying Enzymes, Compositions and Uses Thereof.
Abstract Provided are novel compounds of Formula (I): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with methyl modifying enzymes. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with methyl modifying enzymes.
Applicant(s) Constellation Pharmaceuticals, Inc
Representative Drug(s) D0MZ8D Drug Info N.A. [1]
Patent ID WO2014193930
Title Method for Inhibiting Ezh2 Expression In Breast Cancer Cells.
Abstract The present invention is directed to a method for inhibiting the overexpression of EZH2 in breast cancer cells. The method comprises administering to breast cancer cells an effective amount of YC-1 (3-(5'-hydroxymethyl-2'-furyl)-1-benzyl indazole), YC-1-succinate (succinic acid mono-[5-(1-benzyl-1H-indazol-3-yl)-furan-2-ylmethyl] ester), or a pharmaceutically acceptable salt thereof. The present invention is also directed to treating breast cancer comprising administering to a subject an effective amount of YC-1-succinate.
Applicant(s) Yung Shin Pharm. Ind. Co., Ltd
Representative Drug(s) D0L1TA Drug Info N.A. [2]
United States Patent and Trademark Office (USPTO)
Patent ID US20140107122
Title Preparation of Substituted Benzene Compounds As Anticancer Agents.
Representative Drug(s) D0H8VN Drug Info IC50 < 10 nM [1]
References  Top
REF 1 EZH2 inhibitors: a patent review (2014-2016).Expert Opin Ther Pat. 2017 Jul;27(7):797-813.
REF 2 Hypoxia-inducible factor (HIF) inhibitors: a patent survey (2011-2015).Expert Opin Ther Pat. 2016;26(3):309-22.

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