CA2819648C - Substituted purine and 7-deazapurine compounds - Google Patents

Substituted purine and 7-deazapurine compounds Download PDF

Info

Publication number
CA2819648C
CA2819648C CA2819648A CA2819648A CA2819648C CA 2819648 C CA2819648 C CA 2819648C CA 2819648 A CA2819648 A CA 2819648A CA 2819648 A CA2819648 A CA 2819648A CA 2819648 C CA2819648 C CA 2819648C
Authority
CA
Canada
Prior art keywords
alkyl
amino
compound
halo
cycloalkyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CA2819648A
Other languages
English (en)
French (fr)
Other versions
CA2819648A1 (en
Inventor
Edward James Olhava
Richard Chesworth
Kevin Wayne Kuntz
Victoria Marie Richon
Roy Macfarlane Pollock
Scott Richard Daigle
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Epizyme Inc
Original Assignee
Epizyme Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Epizyme Inc filed Critical Epizyme Inc
Publication of CA2819648A1 publication Critical patent/CA2819648A1/en
Application granted granted Critical
Publication of CA2819648C publication Critical patent/CA2819648C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • 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
    • A61K31/33—Heterocyclic compounds
    • 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
    • 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
    • A61K31/33—Heterocyclic compounds
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/14—Pyrrolo-pyrimidine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • C07H19/167—Purine radicals with ribosyl as the saccharide radical

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Saccharide Compounds (AREA)
CA2819648A 2010-12-03 2011-12-02 Substituted purine and 7-deazapurine compounds Active CA2819648C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US41966110P 2010-12-03 2010-12-03
US61/419,661 2010-12-03
PCT/US2011/063044 WO2012075381A1 (en) 2010-12-03 2011-12-02 Substituted purine and 7 - deazapurine compounds as modulators of epigenetic enzymes

Publications (2)

Publication Number Publication Date
CA2819648A1 CA2819648A1 (en) 2012-06-07
CA2819648C true CA2819648C (en) 2018-05-01

Family

ID=45444712

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2819648A Active CA2819648C (en) 2010-12-03 2011-12-02 Substituted purine and 7-deazapurine compounds

Country Status (18)

Country Link
US (5) US8580762B2 (enExample)
EP (1) EP2646444B1 (enExample)
JP (1) JP5931905B2 (enExample)
KR (1) KR101923746B1 (enExample)
CN (1) CN103391939B (enExample)
AR (1) AR084408A1 (enExample)
AU (1) AU2011336415B2 (enExample)
BR (1) BR112013013659B8 (enExample)
CA (1) CA2819648C (enExample)
DK (1) DK2646444T3 (enExample)
ES (1) ES2577027T3 (enExample)
HR (1) HRP20160655T1 (enExample)
IL (1) IL226651A (enExample)
MX (1) MX2013006251A (enExample)
RU (1) RU2606514C2 (enExample)
SI (1) SI2646444T1 (enExample)
TW (1) TWI537271B (enExample)
WO (1) WO2012075381A1 (enExample)

Families Citing this family (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9394310B2 (en) 2010-12-03 2016-07-19 Epizyme, Inc. Carbocycle-substituted purine and 7-deazapurine compounds
US9029343B2 (en) 2010-12-03 2015-05-12 Epizyme, Inc. Modulators of histone methyltransferase, and methods of use thereof
RU2606514C2 (ru) * 2010-12-03 2017-01-10 Эпизайм, Инк. Замещенные пуриновые и 7-деазапуриновые соединения
EP2646454B1 (en) 2010-12-03 2015-07-08 Epizyme, Inc. 7-deazapurine modulators of histone methyltransferase, and methods of use thereof
EP2766474B1 (en) 2011-10-14 2020-10-07 Children's Medical Center Corporation Inhibition and enhancement of reprogramming by chromatin modifying enzymes
CN104114568B (zh) 2011-12-22 2017-09-01 艾丽奥斯生物制药有限公司 取代的核苷、核苷酸及其类似物
US9441007B2 (en) 2012-03-21 2016-09-13 Alios Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
USRE48171E1 (en) 2012-03-21 2020-08-25 Janssen Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
EP2882750A4 (en) 2012-08-10 2016-08-17 Epizyme Inc INHIBITORS OF THE PROTEIN METHYLTRANSFERASE DOT1L AND METHOD OF USE THEREOF
CA2883781A1 (en) * 2012-09-06 2014-03-13 Epizyme, Inc. Method of treating leukemia
CA2894220A1 (en) * 2012-12-21 2014-06-26 Epizyme, Inc. Dot1l inhibitors for use in the treatment of leukemia
SI2958921T1 (sl) 2013-02-22 2017-12-29 Pfizer Inc. Derivati pirolo(2,3-d)pirimidina kot inhibitorji Janus kinaz (JAK)
US9365527B2 (en) 2013-03-14 2016-06-14 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9446064B2 (en) * 2013-03-14 2016-09-20 Epizyme, Inc. Combination therapy for treating cancer
US20160045531A1 (en) * 2013-03-14 2016-02-18 Epizyme, Inc. Combination therapy for treating cancer
WO2014153172A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
WO2014152261A1 (en) * 2013-03-14 2014-09-25 Epizyme, Inc. Substituted 7-deazapurine compounds
US9133189B2 (en) 2013-03-14 2015-09-15 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US8952026B2 (en) 2013-03-14 2015-02-10 Epizyme, Inc. PRMT1 inhibitors and uses thereof
EP2970220A2 (en) 2013-03-14 2016-01-20 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9045455B2 (en) 2013-03-14 2015-06-02 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
CA2903264A1 (en) 2013-03-14 2014-11-06 Epizyme, Inc. Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof
ES2837034T3 (es) 2013-03-14 2021-06-29 Epizyme Inc Inhibidores de arginina metiltransferasa y usos de los mismos
WO2014144659A1 (en) 2013-03-14 2014-09-18 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
US20160022725A1 (en) * 2013-03-15 2016-01-28 Epizyme, Inc. Injectable formulations for treating cancer
WO2014152566A2 (en) 2013-03-15 2014-09-25 Epizyme, Inc. Methods of synthesizing substituted purine compounds
US9688714B2 (en) 2013-07-03 2017-06-27 Epizyme, Inc. Substituted purine compounds
US9535067B2 (en) 2013-07-29 2017-01-03 Dana-Farber Cancer Institute, Inc. DOT1L probes
WO2015017863A1 (en) 2013-08-02 2015-02-05 Memorial Sloan-Kettering Cancer Center Methods for the detection and treatment of leukemias that are responsive to dot1l inhibition
WO2015073706A1 (en) * 2013-11-13 2015-05-21 Epizyme, Inc. Methods for treating cancer
US20170198006A1 (en) * 2014-06-25 2017-07-13 Epizyme, Inc. Prmt5 inhibitors and uses thereof
JP6585158B2 (ja) 2014-08-12 2019-10-02 ファイザー・インク ヤヌスキナーゼの阻害に有用なピロロ［２，３−ｄ］ピリミジン誘導体
US20170232030A1 (en) * 2014-08-13 2017-08-17 Epizyme, Inc. Combination therapy for treating cancer
US9458165B2 (en) 2014-08-27 2016-10-04 Dana-Farber Cancer Institute, Inc. DOT1L inhibitors
EP3193884A4 (en) * 2014-09-17 2018-06-20 Epizyme, Inc. Combination therapy for treating cancer
US20170290765A1 (en) * 2014-09-17 2017-10-12 Epizyme, Inc. Injectable formulations for treating cancer
EP3200826B1 (en) * 2014-09-30 2021-04-21 Vecht-lifshitz, Susan Eve Pharmaceutical compositions for treating ebola virus disease
US20180028552A1 (en) * 2015-01-30 2018-02-01 Epizyme, Inc. Combination therapy for treating cancer
US11453697B1 (en) 2015-08-13 2022-09-27 Merck Sharp & Dohme Llc Cyclic di-nucleotide compounds as sting agonists
ES3044036T3 (en) 2016-01-26 2025-11-26 Memorial Sloan Kettering Cancer Center Targeting chromatin regulators for inhibiting leukemogenic gene expression in npm1
EA201892075A1 (ru) 2016-03-15 2019-04-30 Оризон Дженомикс, С.А. Комбинации ингибиторов lsd1 для применения для лечения солидных опухолей
CA3253937A1 (en) * 2016-03-15 2025-03-04 Oryzon Genomics, S.A. Combinations of Lysine-Specific Demethylase 1 Inhibitors for the Treatment of Hematological Maligna
CN106432095B (zh) * 2016-09-09 2019-04-16 东南大学 匹莫苯丹关键中间体6-(3,4-二氨基苯基)-5-甲基-4,5-二氢哒嗪-3(2h)-酮的制备
WO2018175746A1 (en) 2017-03-24 2018-09-27 Kura Oncology, Inc. Methods for treating hematological malignancies and ewing's sarcoma
CN109748943A (zh) * 2017-11-03 2019-05-14 中国科学院上海药物研究所 2’-c-甲基取代核苷类化合物及其制备与用途
CN109748944B (zh) * 2017-11-03 2021-12-10 中国科学院上海药物研究所 5’-脱氧-5’-异丙基取代氨基核苷类化合物、其制备方法和用途
CN111741964A (zh) * 2017-12-05 2020-10-02 安杰斯制药公司 作为prmt5抑制剂的杂环化合物
KR102118891B1 (ko) 2018-10-04 2020-06-04 성균관대학교산학협력단 매소니아노사이드 b를 유효성분으로 포함하는 혼합 직계성 백혈병 유전자 재배열 동반 백혈병 예방 및 치료용 약학적 조성물
JP2022516745A (ja) * 2019-01-09 2022-03-02 ダナ－ファーバー キャンサー インスティテュート，インコーポレイテッド Ｄｏｔ１ｌ分解剤およびその使用
BR112021017831A2 (pt) * 2019-03-11 2021-11-30 Collaborative Medicinal Dev Llc Derivados heteroaromáticos e aromáticos heterobicíclicos para o tratamento de distúrbios relacionados com ferroptose
CN110092804A (zh) * 2019-03-29 2019-08-06 广州盈升生物科技有限公司 一种含双环基团的嘌呤化合物及其制备方法
KR20210145787A (ko) 2019-04-02 2021-12-02 알리고스 테라퓨틱스 인코포레이티드 Prmt5를 표적으로 하는 화합물
CN113024620B (zh) * 2021-03-11 2023-02-28 沈阳药科大学 一种嘌呤衍生物及其制备方法和用途
WO2022271540A1 (en) * 2021-06-21 2022-12-29 Mayo Foundation For Medical Education And Research Inhibitors of dot1l
KR20240035820A (ko) 2021-07-09 2024-03-18 플렉시움 인코포레이티드 Ikzf2를 조절하는 아릴 화합물 및 약학 조성물
CA3221819A1 (en) * 2021-07-19 2023-01-26 Jun Qi Targeting dot1l and smarca4/2 for the treatment of mllr leukemia

Family Cites Families (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US5763263A (en) 1995-11-27 1998-06-09 Dehlinger; Peter J. Method and apparatus for producing position addressable combinatorial libraries
US20020127598A1 (en) 2000-03-27 2002-09-12 Wenqiang Zhou Solution-phase combinatorial library synthesis and pharmaceutically active compounds produced thereby
EP1138689A1 (en) 2000-03-28 2001-10-04 Roche Diagnostics GmbH N8- and C8-linked purine bases as universal nucleosides used for oligonucleotide hybridization
EP1138688A1 (en) 2000-03-28 2001-10-04 Roche Diagnostics GmbH N8- and C8- linked purine bases as universal nucleosides used for oligonucleotide hybridization
US6534651B2 (en) 2000-04-06 2003-03-18 Inotek Pharmaceuticals Corp. 7-Substituted isoindolinone inhibitors of inflammation and reperfusion injury and methods of use thereof
US20040043959A1 (en) 2002-03-04 2004-03-04 Bloom Laura A. Combination therapies for treating methylthioadenosine phosphorylase deficient cells
AU2003269902A1 (en) * 2002-07-16 2004-02-02 Isis Pharmaceuticals, Inc. Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase
AU2002951247A0 (en) * 2002-09-06 2002-09-19 Alchemia Limited Compounds that interact with kinases
JP2006505537A (ja) 2002-09-30 2006-02-16 ジェネラブス テクノロジーズ，インコーポレイテッド Ｃ型肝炎ウイルスの感染を治療するためのヌクレオシド誘導体
GB0301450D0 (en) * 2003-01-22 2003-02-19 Medical Res Council Protein crystal structure
RU2354655C2 (ru) * 2003-12-19 2009-05-10 Ф.Хоффманн-Ля Рош Аг Ингибиторы сомт
WO2006015357A2 (en) 2004-08-02 2006-02-09 University Of Virginia Patent Foundation 2-propynyl adenosine analogs with modified 5'-ribose groups having a2a agonist activity
WO2006028618A1 (en) * 2004-08-02 2006-03-16 University Of Virginia Patent Foundation 2-polycyclic propynyl adenosine analogs with modified 5'-ribose groups having a2a agonist activity
US8058762B2 (en) * 2005-01-19 2011-11-15 Daikin Industries, Ltd. Rotor, axial gap type motor, method of driving motor, and compressor
EP1844062A2 (en) 2005-01-21 2007-10-17 Methylgene, Inc. Inhibitors of dna methyltransferase
ES2390803T3 (es) 2005-02-04 2012-11-16 Millennium Pharmaceuticals, Inc. Inhibidores de las enzimas activadoras E1
US20060235037A1 (en) 2005-04-15 2006-10-19 Purandare Ashok V Heterocyclic inhibitors of protein arginine methyl transferases
US8461128B2 (en) 2005-04-15 2013-06-11 Sloan-Kettering Institute For Cancer Research Anti-microbial agents and uses thereof
EA024006B1 (ru) 2006-02-02 2016-08-31 Миллениум Фармасьютикалз, Инк. Ингибиторы е1 активирующих ферментов
EP2522352B1 (en) 2006-03-02 2017-01-11 Agency for Science, Technology and Research Methods for stem cells modulation
GB0607953D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
US8188063B2 (en) 2006-06-19 2012-05-29 University Of Virginia Patent Foundation Use of adenosine A2A modulators to treat spinal cord injury
US20080132525A1 (en) 2006-12-04 2008-06-05 Methylgene Inc. Inhibitors of DNA Methyltransferase
WO2008124150A1 (en) 2007-04-09 2008-10-16 University Of Virginia Patent Foundation Method of treating enteritis, intestinal damage, and diarrhea from c. difficile with an a2a adenosine receptor agonist
CN101417967A (zh) 2007-10-26 2009-04-29 浙江海正药业股份有限公司 组蛋白去乙酰酶抑制剂、其组合物及其应用
AR069165A1 (es) 2007-11-05 2010-01-06 Novartis Ag Derivados de 4-bencilamino-1-carboxacilpiperidina como inhibidores de cetp utiles para el tratamiento de hiperlipidemia
CN101938904A (zh) 2008-01-09 2011-01-05 PGx健康有限责任公司 用a2ar激动剂鞘内治疗神经性疼痛
WO2010015643A1 (en) 2008-08-06 2010-02-11 Novartis Ag New antiviral modified nucleosides
US20110171192A1 (en) 2008-09-05 2011-07-14 Hiroshi Tomiyama Substituted amine derivative and medicinal composition comprising same as the active ingredient
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
MX2012002317A (es) 2009-08-24 2012-06-25 Ascepion Pharmaceuticals Inc Compuestos de urea que contienen heteroarilo 5,6-biciclicos como inhibidores de cinasa.
EP2646454B1 (en) 2010-12-03 2015-07-08 Epizyme, Inc. 7-deazapurine modulators of histone methyltransferase, and methods of use thereof
US9029343B2 (en) 2010-12-03 2015-05-12 Epizyme, Inc. Modulators of histone methyltransferase, and methods of use thereof
RU2606514C2 (ru) * 2010-12-03 2017-01-10 Эпизайм, Инк. Замещенные пуриновые и 7-деазапуриновые соединения
US9394310B2 (en) 2010-12-03 2016-07-19 Epizyme, Inc. Carbocycle-substituted purine and 7-deazapurine compounds
CA2883781A1 (en) * 2012-09-06 2014-03-13 Epizyme, Inc. Method of treating leukemia
US9446064B2 (en) * 2013-03-14 2016-09-20 Epizyme, Inc. Combination therapy for treating cancer
WO2014152566A2 (en) 2013-03-15 2014-09-25 Epizyme, Inc. Methods of synthesizing substituted purine compounds
WO2015017863A1 (en) * 2013-08-02 2015-02-05 Memorial Sloan-Kettering Cancer Center Methods for the detection and treatment of leukemias that are responsive to dot1l inhibition
WO2015073706A1 (en) * 2013-11-13 2015-05-21 Epizyme, Inc. Methods for treating cancer

Also Published As

Publication number Publication date
US8580762B2 (en) 2013-11-12
TWI537271B (zh) 2016-06-11
US20120142625A1 (en) 2012-06-07
KR101923746B1 (ko) 2018-11-29
US20150366893A1 (en) 2015-12-24
RU2013130250A (ru) 2015-01-10
EP2646444A1 (en) 2013-10-09
AU2011336415B2 (en) 2016-08-11
WO2012075381A1 (en) 2012-06-07
BR112013013659A2 (pt) 2016-09-06
TW201307348A (zh) 2013-02-16
BR112013013659B1 (pt) 2022-06-21
KR20130125379A (ko) 2013-11-18
MX2013006251A (es) 2013-10-01
CN103391939A (zh) 2013-11-13
IL226651A (en) 2016-11-30
RU2606514C2 (ru) 2017-01-10
ES2577027T3 (es) 2016-07-12
JP5931905B2 (ja) 2016-06-08
US20180280422A1 (en) 2018-10-04
AR084408A1 (es) 2013-05-15
AU2011336415A1 (en) 2013-06-20
US20140051654A1 (en) 2014-02-20
BR112013013659B8 (pt) 2024-02-27
HRP20160655T1 (hr) 2016-09-23
US20210252035A1 (en) 2021-08-19
HK1189596A1 (zh) 2014-06-13
CA2819648A1 (en) 2012-06-07
CN103391939B (zh) 2016-03-09
JP2013544846A (ja) 2013-12-19
DK2646444T3 (da) 2016-06-27
EP2646444B1 (en) 2016-03-16
SI2646444T1 (sl) 2016-09-30
US9096634B2 (en) 2015-08-04

Similar Documents

Publication Publication Date Title
CA2819648C (en) Substituted purine and 7-deazapurine compounds
EP2646441B1 (en) Carbocycle-substituted purine and 7-deazapurine compounds
US9029343B2 (en) Modulators of histone methyltransferase, and methods of use thereof
AU2013361076B2 (en) DOT1 L inhibitors for use in the treatment of leukemia
AU2013361076A1 (en) DOT1 L inhibitors for use in the treatment of leukemia
US11753433B2 (en) Methods of synthesizing substituted purine compounds
HK1189596B (en) Substituted purine and 7-deazapurine compounds as modulators of epigenetic enzymes
WO2014152261A1 (en) Substituted 7-deazapurine compounds

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20160809