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Epizyme Inc patents


Recent patent applications related to Epizyme Inc. Epizyme Inc is listed as an Agent/Assignee. Note: Epizyme Inc may have other listings under different names/spellings. We're not affiliated with Epizyme Inc, we're just tracking patents.

ARCHIVE: New 2018 2017 2016 2015 2014 2013 2012 2011 2010 2009 | Company Directory "E" | Epizyme Inc-related inventors


Inhibitors of human ezh2, and methods of use thereof

The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase ezh2, the catalytic subunit of the prc2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone h3 (h3-k27). In one embodiment the inhibition is selective for the mutant form of the ezh2, such that trimethylation of h3-k27, which is associated with certain cancers, is inhibited. ... Epizyme Inc

Prmt1 inhibitors and uses thereof

Described herein are compounds of formula (i), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting prmt1 activity. ... Epizyme Inc

Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof

Described herein are compounds of formula (i), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. ... Epizyme Inc

Method for treating cancer

The present disclosure relates to pharmaceutical compositions comprising inhibitor(s) of human histone methyltransferase ezh2, and methods of cancer therapy using the ezh2 inhibitor(s).. . ... Epizyme Inc

Isoxazole carboxamides as irreversible smyd inhibitors

The present disclosure provides substituted isoxazole carboxamides having formula (i), and the pharmaceutically acceptable salts and solvates thereof, wherein r1, r2a, r2b, r3a, r3b, x, n, and m are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of formula i to treat a disorder responsive to the blockade of smyd proteins such as smyd3 or smyd2. ... Epizyme Inc

Substituted 6,5-fused bicyclic heteroaryl compounds

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. ... Epizyme Inc

Prmt5 inhibitors and uses thereof

Described herein are compounds of formula (i), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting prmt5 activity. ... Epizyme Inc

Prmt5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof

Described herein are compounds of formula (a), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting prmt5 activity. ... Epizyme Inc

Methods of synthesizing substituted purine compounds

The present invention provides an efficient process for the synthesis of (2r,3r,4s,5r)-2-(6-amino-9h-purin-9-yl)-5-((((1r,3s)-3-(2-(5-(tert-butyl)-1h-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for treating disorders in which dot1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also provides novel crystalline forms of (2r,3r,4s,5r)-2-(6-amino-9h-purin-9-yl)-5-((((1r,3s)-3-(2-(5-(tert-butyl)-1h-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (form a, form b, and form c), characterized by a unique x-ray diffraction pattern and differential scanning calorimetry profile, as well as a unique crystalline structure.. ... Epizyme Inc

Methods of synthesizing substituted purine compounds

The present invention provides an efficient process for the synthesis of (2r,3r,4s,5r)-2-(6-amino-9h-purin-9-yl)-5-((((1r,3s)-3-(2-(5-(tert-butyl)-1h-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for treating disorders in which dot1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also provides novel crystalline forms of (2r,3r,4s,5r)-2-(6-amino-9h-purin-9-yl)-5-((((1r,3s)-3-(2-(5-(tert-butyl)-1h-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (form a, form b, and form c), characterized by a unique x-ray diffraction pattern and differential scanning calorimetry profile, as well as a unique crystalline structure.. ... Epizyme Inc

1,4-pyridone bicyclic heteroaryl compounds

The present invention relates to 1,4-pyridone 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. ... Epizyme Inc

Method for treating cancer

The present invention provides a method for treating or alleviating a symptom of a disorder, e.g., immune evasion, cancer-cell induced immune dysfunction, reduced immune response, lowered inflammation, decreased expression of a major histocompatibility complex (mhc), or cancer, characterized by aberrant, misregulated, or increased enhancer of zeste homolog 2 (ezh2) activity in a cell or subject in need thereof by contacting the cell or administering to the subject a therapeutically effective amount of an ezh2 inhibitor.. . ... Epizyme Inc

Substituted purine compounds

The present invention relates to substituted purine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which dot1-mediated protein methylation plays a part, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.. ... Epizyme Inc

Arginine methyltransferase inhibitors and uses thereof

Described herein are compounds of formula (i), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting arginine methyltransferase activity. ... Epizyme Inc

04/12/18 / #20180098987

Prmt5 inhibitors and uses thereof

Described herein are compounds of formula (i), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting prmt5 activity. ... Epizyme Inc

03/15/18 / #20180072702

Substituted 6,5-fused bicyclic heteroaryl compounds

The present invention relates to substituted 6,5-fused 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.. ... Epizyme Inc

03/15/18 / #20180071300

Method of treating cancer

The present invention relates to methods of treating cancer by administering an ezh2 inhibitor or a pharmaceutical composition thereof to the subject in need thereof.. . ... Epizyme Inc

03/08/18 / #20180065954

Substituted 6,5-fused bicyclic heteroaryl compounds

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. ... Epizyme Inc

12/21/17 / #20170362217

Substituted piperidine compounds

The present disclosure provides substituted piperidine compounds having formula (i), and the pharmaceutically acceptable salts and solvates thereof, wherein r1, b, x, and z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of formula i to treat a disorder responsive to the blockade of smyd proteins such as smyd3 or smyd2. ... Epizyme Inc

12/21/17 / #20170362191

Substituted cyclohexylamine compounds

The present disclosure provides substituted cyclohexylamine compounds having formula (i): and the pharmaceutically acceptable salts and solvates thereof, wherein r1, r2a, r2b, r3a, r3b, r4, r5, and r7 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of formula i to treat a disorder responsive to the blockade of smyd proteins such as smyd3 or smyd2. ... Epizyme Inc

12/14/17 / #20170355712

Amine-substituted aryl or heteroaryl compounds

The present disclosure relates to amine-substituted aryl or heteroaryl compounds. The present disclosure also relates to pharmaceutical compositions containing these compounds and methods of treating a disorder (e.g., sickle cell anemia) via inhibition of a methyltransferase enzyme selected from ehmt1 and ehmt2, by administering an amine-substituted aryl or heteroaryl compound disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. ... Epizyme Inc

12/14/17 / #20170355695

Smyd inhibitors

The present disclosure provides carboxamides and sulfonamides having formula (i): and the pharmaceutically acceptable salts and solvates thereof, wherein a, y, b, x, and z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of formula (i) to treat a disorder responsive to the blockade of smyd proteins such as smyd3 or smyd2. ... Epizyme Inc

11/23/17 / #20170334861

Tetrahydro- and dihydro-isoquinoline prmt5 inhibitors and uses thereof

Described herein are compounds of formula (a), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting prmt5 activity. ... Epizyme Inc

10/26/17 / #20170305922

Carm1 inhibitors and uses thereof

. . Provided herein are compounds of formula (i): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein r1, r2a, r2b, r3 and ring b are as defined herein, and ring a is a group of formula (a-i), (a-ii), or (a-iii): wherein r, r, r, r, and r are as defined herein. Compounds of the present invention are useful for inhibiting carm1 activity. ... Epizyme Inc

10/26/17 / #20170305890

Methods of treating cancer

The present invention relates to methods of treating cancer by administering the ezh2 inhibitor 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.. ... Epizyme Inc

10/26/17 / #20170305889

Methods of treating cancer

The present invention relates to methods of treating cancer by administering the ezh2 inhibitor 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.. ... Epizyme Inc

10/12/17 / #20170291905

Arginine methyltransferase inhibitors and uses thereof

Described herein are compounds of formula (s-i), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. ... Epizyme Inc

10/12/17 / #20170291890

Heterocycle substituted amino-pyridine compounds and methods of use thereof

The present disclosure relates to heterocycle substituted amino-pyridine compounds. The present disclosure 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. ... Epizyme Inc

10/12/17 / #20170290837

Substituted benzene compounds

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. ... Epizyme Inc

10/12/17 / #20170290765

Injectable formulations for treating cancer

The present invention provides injectable formulations of (2r,3r,4s,5r)-2-(6-amino-9h-purin-9-yl)-5-((((1r,3s)-3-(2-(5-(tert-butyl)-1h-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for treating disorders in which dot 1-mediated protein methylation plays a part, such as cancer and neurological disorders.. . ... Epizyme Inc

10/05/17 / #20170283440

Carm1 inhibitors and uses thereof

Provided herein are compounds of formula (i): (i) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein x, r1, r2a, r2b, r2c, r2d, are as defined herein, and ring het is an optionally substituted 6,5-bicyclic heteroaryl ring system comprising 2 to 5 nitrogen atoms, inclusive, wherein the point of attachment is provided on the 6-membered ring of the 6,5-bicyclic heteroaryl ring system, and wherein the 6-membered ring is further substituted with a group of formula -l1-r3, wherein l1 and r3 are as defined herein. Compounds of the present invention are useful for inhibiting carm1 activity. ... Epizyme Inc

10/05/17 / #20170283400

Arginine methyltransferase inhibitors and uses thereof

Provided herein are various compounds, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.. ... Epizyme Inc

10/05/17 / #20170280720

Arginine methyltransferase inhibitors and uses thereof

Described herein are compounds of formula (i), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. ... Epizyme Inc

09/21/17 / #20170267642

Arginine methyltransferase inhibitors and uses thereof

Described herein are compounds of formula (i), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. ... Epizyme Inc

09/07/17 / #20170253601

Substituted pyrrolidine compounds

The present disclosure provides substituted pyrrolidine compounds having formula (i): and the pharmaceutically acceptable salts and solvates thereof, wherein r1, b, x, and z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of formula (i) to treat a disorder responsive to the blockade of smyd proteins such as smyd3 or smyd2. ... Epizyme Inc

09/07/17 / #20170252349

Aryl-or heteroaryl-substituted benzene compounds

The present invention relates to aryl- or heteroaryl-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. ... Epizyme Inc

08/31/17 / #20170247326

Substituted pyrrolidine carboxamide compounds

The present disclosure provides pyrrolidine carboxamide compounds having formula i and the pharmaceutically acceptable salts and solvates thereof, wherein a, b, x, y, and z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of formula i to treat a disorder responsive to the blockade of smyd proteins such as smyd3 or smyd2. ... Epizyme Inc

08/24/17 / #20170240537

Prmt5 inhibitors and uses thereof

Described herein are compounds of formula (a), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting prmt5 activity. ... Epizyme Inc

08/17/17 / #20170233347

Prmt1 inhibitors and uses thereof

Described herein are compounds of formula (i), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting prmt1 activity. ... Epizyme Inc

08/03/17 / #20170217941

Substituted benzene and 6,5-fused bicyclic heteroaryl compounds

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. ... Epizyme Inc

08/03/17 / #20170216300

Ezh2 inhibitors for treating lymphoma

The present invention relates to compositions comprising inhibitors of human histone methyltransferase ezh2 and their use for the treatment of cancer.. . ... Epizyme Inc

07/27/17 / #20170210751

Prmt5 inhibitors and uses thereof

Described herein are compounds of formula (a), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof: wherein y1 is of formula (x) or formula (y):ring y is a 5- to 6-membered heteroaryl ring; and v4, v5, rx, x, y, and n are as defined herein. Compounds of the present invention are useful for inhibiting prmt5 activity. ... Epizyme Inc

07/13/17 / #20170198006

Prmt5 inhibitors and uses thereof

Described herein are compounds of formula (i)-(xiii), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting prmt5 activity. ... Epizyme Inc

07/06/17 / #20170190676

Isoxazole carboxamide compounds

The present disclosure provides substituted isoxazole carboxamide compounds having formula (i) and the pharmaceutically acceptable salts and solvates thereof, wherein r1, r2, a, x, and z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of formula i to treat a disorder responsive to the blockade of smyd proteins such as smyd3 or smyd2. ... Epizyme Inc

06/29/17 / #20170182005

Prmt1 inhibitors and uses thereof

Described herein are compounds of formula (i-a) and (i-b), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting prmt1 activity. ... Epizyme Inc

06/15/17 / #20170165288

Method of treating leukemia

The present invention relates to methods of treating disorders in which dot1l-mediated protein methylation plays a part, such as cancer, by administering dot1l inhibitor compounds and pharmaceutical compositions to subjects in need thereof.. . ... Epizyme Inc

05/18/17 / #20170137455

Inhibitors of protein methyltransferase dot1l and methods of use thereof

The present invention relates to dot1l inhibitors and methods of identifying, designing, or optimizing them. The present invention also relates to crystals of dot1l-inhibitor complexes, the crystal structures thereof, and the use of the crystal structures. ... Epizyme Inc

05/04/17 / #20170119780

Aryl- or heteroaryl-substituted benzene compounds

The present invention relates to aryl- or heteroaryl-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. ... Epizyme Inc

05/04/17 / #20170119735

Arginine methyltransferase inhibitors and uses thereof

Described herein are compounds of formula (i), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting arginine methyltransferase activity. ... Epizyme Inc

04/27/17 / #20170114061

Prmt5 inhibitors and uses thereof

Described herein are compounds of formula (i), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting prmt5 activity. ... Epizyme Inc

03/30/17 / #20170088541

Prmt5 inhibitors and uses thereof

Described herein are compounds of formula (i), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting prmt5 activity. ... Epizyme Inc

03/30/17 / #20170088529

Arginine methyltransferase inhibitors and uses thereof

Described herein are compounds of formula (i), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting arginine methyltransferase activity. ... Epizyme Inc

03/23/17 / #20170080010

Combination therapy for treating cancer

The present invention relates to compositions comprising inhibitors of human histone methyltransferase dot1l and one or more therapeutic agents, particularly anticancer agents, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.. . ... Epizyme Inc

03/09/17 / #20170065628

Inhibitors of human ezh2, and methods of use thereof

The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase ezh2, the catalytic subunit of the prc2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone h3 (h3-k27). In one embodiment the inhibition is selective for the mutant form of the ezh2, such that trimethylation of h3-k27, which is associated with certain cancers, is inhibited. ... Epizyme Inc

03/09/17 / #20170065600

Inhibitors of human ezh2, and methods of use thereof

The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase ezh2, the catalytic subunit of the prc2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone h3 (h3-k27). In one embodiment the inhibition is selective for the mutant form of the ezh2, such that trimethylation of h3-k27, which is associated with certain cancers, is inhibited. ... Epizyme Inc

03/02/17 / #20170057926

Arginine methyltransferase inhibitors and uses thereof

. . Described herein are compounds of formula (i), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. ... Epizyme Inc

02/02/17 / #20170027935

Prmt5 inhibitors and uses thereof

Described herein are compounds of formula (i), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting prmt5 activity. ... Epizyme Inc








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