KR102267502B1 - 인간 ｅｚｈ2의 억제제 및 이의 사용 방법 - Google Patents

인간 ｅｚｈ2의 억제제 및 이의 사용 방법 Download PDF

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KR102267502B1
KR102267502B1 KR1020147028560A KR20147028560A KR102267502B1 KR 102267502 B1 KR102267502 B1 KR 102267502B1 KR 1020147028560 A KR1020147028560 A KR 1020147028560A KR 20147028560 A KR20147028560 A KR 20147028560A KR 102267502 B1 KR102267502 B1 KR 102267502B1
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alkyl
seq
alkylamino
cycloalkyl
wild
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KR20140147836A (ko
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케빈 웨인 쿤츠
사라 캐슬린 넛슨
티모시 제임스 넬슨 위글
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에피자임, 인코포레이티드
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Priority to KR1020217018417A priority Critical patent/KR102453519B1/ko
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
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    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A—HUMAN NECESSITIES
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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KR1020147028560A 2012-03-12 2013-03-12 인간 ｅｚｈ2의 억제제 및 이의 사용 방법 Expired - Fee Related KR102267502B1 (ko)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1020217018417A KR102453519B1 (ko) 2012-03-12 2013-03-12 인간 ｅｚｈ2의 억제제 및 이의 사용 방법

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US13/418,242 2012-03-12
US13/418,242 US9175331B2 (en) 2010-09-10 2012-03-12 Inhibitors of human EZH2, and methods of use thereof
PCT/US2013/030565 WO2013138361A1 (en) 2012-03-12 2013-03-12 Inhibitors of human ezh2, and methods of use thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020217018417A Division KR102453519B1 (ko) 2012-03-12 2013-03-12 인간 ｅｚｈ2의 억제제 및 이의 사용 방법

Publications (2)

Publication Number Publication Date
KR20140147836A KR20140147836A (ko) 2014-12-30
KR102267502B1 true KR102267502B1 (ko) 2021-06-24

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Family Applications (4)

Application Number Title Priority Date Filing Date
KR1020147028560A Expired - Fee Related KR102267502B1 (ko) 2012-03-12 2013-03-12 인간 ｅｚｈ2의 억제제 및 이의 사용 방법
KR1020227034498A Active KR102587175B1 (ko) 2012-03-12 2013-03-12 인간 ｅｚｈ2의 억제제 및 이의 사용 방법
KR1020217018417A Active KR102453519B1 (ko) 2012-03-12 2013-03-12 인간 ｅｚｈ2의 억제제 및 이의 사용 방법
KR1020237033924A Ceased KR20230145531A (ko) 2012-03-12 2013-03-12 인간 ｅｚｈ2의 억제제 및 이의 사용 방법

Family Applications After (3)

Application Number Title Priority Date Filing Date
KR1020227034498A Active KR102587175B1 (ko) 2012-03-12 2013-03-12 인간 ｅｚｈ2의 억제제 및 이의 사용 방법
KR1020217018417A Active KR102453519B1 (ko) 2012-03-12 2013-03-12 인간 ｅｚｈ2의 억제제 및 이의 사용 방법
KR1020237033924A Ceased KR20230145531A (ko) 2012-03-12 2013-03-12 인간 ｅｚｈ2의 억제제 및 이의 사용 방법

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EP (2) EP2825161B1 (https=)
JP (2) JP6321619B2 (https=)
KR (4) KR102267502B1 (https=)
CN (2) CN104540500B (https=)
AU (4) AU2013232229B2 (https=)
CA (2) CA2867282C (https=)
DK (1) DK2825161T3 (https=)
ES (1) ES2718900T3 (https=)
HU (1) HUE042271T2 (https=)
PL (1) PL2825161T3 (https=)
PT (1) PT2825161T (https=)
RU (2) RU2704445C2 (https=)
TR (1) TR201904660T4 (https=)
WO (1) WO2013138361A1 (https=)

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US9051269B2 (en) 2011-11-18 2015-06-09 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
JP5989805B2 (ja) 2012-02-10 2016-09-07 コンステレーション・ファーマシューティカルズ・インコーポレイテッドＣｏｎｓｔｅｌｌａｔｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． メチル基変更酵素の調節物質、組成物及びその使用
US9394283B2 (en) 2012-04-13 2016-07-19 Epizyme, Inc. Salt form of a human histone methyltransferase EZH2 inhibitor
SG10201608579UA (en) * 2012-04-13 2016-12-29 Epizyme Inc Combination therapy for treating cancer
CA2884848C (en) * 2012-09-28 2017-08-22 Pfizer Inc. Benzamide and heterobenzamide compounds
CA2887243C (en) 2012-10-15 2024-04-09 Epizyme, Inc. Methods of treating cancer
PE20150887A1 (es) 2012-10-15 2015-06-04 Epizyme Inc Compuestos de benceno sustituidos
US9745305B2 (en) 2013-03-15 2017-08-29 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
US9969716B2 (en) 2013-08-15 2018-05-15 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
KR102142177B1 (ko) 2013-10-16 2020-08-07 에피자임, 인코포레이티드 Ezh2 억제용 하이드로클로라이드 염 형태
EP3057594A4 (en) * 2013-10-18 2017-06-07 Epizyme, Inc. Method of treating cancer
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US20160361309A1 (en) * 2014-02-26 2016-12-15 Glaxosmithkline Intellectual Property (No.2) Limited Methods of treating cancer patients responding to ezh2 inhibitor gsk126
IL285201B2 (en) * 2014-06-17 2024-05-01 Epizyme Inc EZH2 inhibitors for the treatment of lymphoma
EP3158086B1 (en) 2014-06-19 2021-03-24 Memorial Sloan-Kettering Cancer Center Biomarkers for response to ezh2 inhibitors
IL310279A (en) * 2014-10-16 2024-03-01 Epizyme Inc Method for treating cancer
WO2016073956A1 (en) 2014-11-06 2016-05-12 Dana-Farber Cancer Institute, Inc. Ezh2 inhibitors and uses thereof
HUE062159T2 (hu) * 2014-11-17 2023-10-28 Epizyme Inc Módszer a rák kezelésére N-((4,6-dimetil-2-oxo-l,2-dihidropiridin-3-il)metil)-5-(etil(tetrahidro-2H -pirán-4-il)amino)-4-metil-4'-(morfolinmetil)-[1,1'-bifenil]-3-karboxamiddal
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