AU2013361076B2 - DOT1 L inhibitors for use in the treatment of leukemia - Google Patents
DOT1 L inhibitors for use in the treatment of leukemia Download PDFInfo
- Publication number
- AU2013361076B2 AU2013361076B2 AU2013361076A AU2013361076A AU2013361076B2 AU 2013361076 B2 AU2013361076 B2 AU 2013361076B2 AU 2013361076 A AU2013361076 A AU 2013361076A AU 2013361076 A AU2013361076 A AU 2013361076A AU 2013361076 B2 AU2013361076 B2 AU 2013361076B2
- Authority
- AU
- Australia
- Prior art keywords
- cancer
- compound
- alkyl
- methyl
- amino
- 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.)
- Ceased
Links
- 0 C*(*)C(C)(*)*(C)C(C1)CC1*(C)C(*)(*)C(C)(C)N(*)C[C@@](*[C@]([C@@]1O)N(C(C)*2)C3=C2C(N)NCN3)[C@@]1O Chemical compound C*(*)C(C)(*)*(C)C(C1)CC1*(C)C(*)(*)C(C)(C)N(*)C[C@@](*[C@]([C@@]1O)N(C(C)*2)C3=C2C(N)NCN3)[C@@]1O 0.000 description 11
- PWAQAONRANKJSV-UHFFFAOYSA-N Cc([nH]c1cc(Cl)c2)nc1c2Cl Chemical compound Cc([nH]c1cc(Cl)c2)nc1c2Cl PWAQAONRANKJSV-UHFFFAOYSA-N 0.000 description 2
- SDHYGAUOCHFYSR-UHFFFAOYSA-N CC(C)Cc1cccc(C)c1 Chemical compound CC(C)Cc1cccc(C)c1 SDHYGAUOCHFYSR-UHFFFAOYSA-N 0.000 description 1
- CAZGGIPSNSFVGU-UHFFFAOYSA-N CC(C)c(cc1[nH]c(C)nc1c1)c1F Chemical compound CC(C)c(cc1[nH]c(C)nc1c1)c1F CAZGGIPSNSFVGU-UHFFFAOYSA-N 0.000 description 1
- PVOWNFODJAQZIQ-UHFFFAOYSA-N CC(C)c1cccc(OC(F)F)c1 Chemical compound CC(C)c1cccc(OC(F)F)c1 PVOWNFODJAQZIQ-UHFFFAOYSA-N 0.000 description 1
- JXOLTWIALSFLTO-UHFFFAOYSA-N CC(C)c1cccc(SC)c1 Chemical compound CC(C)c1cccc(SC)c1 JXOLTWIALSFLTO-UHFFFAOYSA-N 0.000 description 1
- HTYWOQURPXQMFA-UHFFFAOYSA-N CCc1nc2c(C(F)(F)F)cccc2[nH]1 Chemical compound CCc1nc2c(C(F)(F)F)cccc2[nH]1 HTYWOQURPXQMFA-UHFFFAOYSA-N 0.000 description 1
- BSROJRWZJKELNS-UHFFFAOYSA-N Cc([nH]c1c2)nc1ccc2OC(F)(F)F Chemical compound Cc([nH]c1c2)nc1ccc2OC(F)(F)F BSROJRWZJKELNS-UHFFFAOYSA-N 0.000 description 1
- CMXLWMLABMJODV-UHFFFAOYSA-N Cc(cc1C(F)(F)F)ccc1Cl Chemical compound Cc(cc1C(F)(F)F)ccc1Cl CMXLWMLABMJODV-UHFFFAOYSA-N 0.000 description 1
- NWESJZZPAJGHRZ-UHFFFAOYSA-N Cc(cc1[N+]([O-])=O)ccc1Cl Chemical compound Cc(cc1[N+]([O-])=O)ccc1Cl NWESJZZPAJGHRZ-UHFFFAOYSA-N 0.000 description 1
- QSSXJPIWXQTSIX-UHFFFAOYSA-N Cc1ccccc1Br Chemical compound Cc1ccccc1Br QSSXJPIWXQTSIX-UHFFFAOYSA-N 0.000 description 1
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
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
- C12Q1/68—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
- C12Q1/6876—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes
- C12Q1/6883—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
- C12Q1/6886—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q2600/00—Oligonucleotides characterized by their use
- C12Q2600/136—Screening for pharmacological compounds
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q2600/00—Oligonucleotides characterized by their use
- C12Q2600/158—Expression markers
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pathology (AREA)
- Zoology (AREA)
- Wood Science & Technology (AREA)
- Epidemiology (AREA)
- Analytical Chemistry (AREA)
- Genetics & Genomics (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Biophysics (AREA)
- Biotechnology (AREA)
- Microbiology (AREA)
- Physics & Mathematics (AREA)
- Hospice & Palliative Care (AREA)
- Biochemistry (AREA)
- General Engineering & Computer Science (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261745294P | 2012-12-21 | 2012-12-21 | |
| US61/745,294 | 2012-12-21 | ||
| PCT/US2013/077082 WO2014100662A1 (en) | 2012-12-21 | 2013-12-20 | Dot1 l inhibitors for use in the treatment of leukemia |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2013361076A1 AU2013361076A1 (en) | 2015-06-25 |
| AU2013361076B2 true AU2013361076B2 (en) | 2018-08-30 |
Family
ID=49956460
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2013361076A Ceased AU2013361076B2 (en) | 2012-12-21 | 2013-12-20 | DOT1 L inhibitors for use in the treatment of leukemia |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US20150342979A1 (https=) |
| EP (1) | EP2934550A1 (https=) |
| JP (2) | JP2016510316A (https=) |
| AU (1) | AU2013361076B2 (https=) |
| CA (1) | CA2894220A1 (https=) |
| WO (1) | WO2014100662A1 (https=) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20150284422A1 (en) | 2012-08-10 | 2015-10-08 | Epizyme, Inc. | Inhibitors of protein methyltransferase dot1l and methods of use thereof |
| US9597348B2 (en) | 2012-09-06 | 2017-03-21 | Epizyme, Inc. | Method of treating leukemia |
| US9446064B2 (en) | 2013-03-14 | 2016-09-20 | Epizyme, Inc. | Combination therapy for treating cancer |
| US9738679B2 (en) | 2013-03-15 | 2017-08-22 | Epizyme, Inc. | Methods of synthesizing substituted purine compounds |
| US20170166976A1 (en) * | 2014-07-18 | 2017-06-15 | The Regents Of The University Of Colorado, A Body Corporate | Dot1l inhibition in patients with mn1-high aml |
| EP3180348A4 (en) * | 2014-08-08 | 2018-02-07 | Baylor College of Medicine | Dot1l inhibitors and uses thereof |
| WO2016029127A1 (en) * | 2014-08-22 | 2016-02-25 | The Regents Of The University Of Colorado, A Body Corporate | Dot1l inhibitors and uses thereof |
| WO2016044649A1 (en) * | 2014-09-17 | 2016-03-24 | Epizyme, Inc. | Injectable formulations for treating cancer |
| WO2016051396A1 (en) * | 2014-09-30 | 2016-04-07 | Susan Eve Vecht-Lifshitz | Pharmaceutical compositions for treating ebola virus disease |
| GB201519573D0 (en) | 2015-11-05 | 2015-12-23 | King S College London | Combination |
| EP4643952A3 (en) * | 2016-01-26 | 2026-01-14 | Memorial Sloan Kettering Cancer Center | Targeting chromatin regulators for inhibiting leukemogenic gene expression in npm1 |
| CN110691779B (zh) | 2017-03-24 | 2023-10-10 | 库拉肿瘤学公司 | 治疗血液系统恶性肿瘤和尤因肉瘤的方法 |
| GB201901817D0 (en) | 2019-02-11 | 2019-04-03 | Phoremost Ltd | Methods |
| 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 |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| IL326136A (en) | 2023-08-07 | 2026-03-01 | Revolution Medicines Inc | RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012075381A1 (en) * | 2010-12-03 | 2012-06-07 | Epizyme, Inc. | Substituted purine and 7 - deazapurine compounds as modulators of epigenetic enzymes |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008041767A1 (en) * | 2006-10-05 | 2008-04-10 | Banyu Pharmaceutical Co., Ltd. | Gene/protein marker for prediction or diagnosis of pharmacological efficacy of aurora a inhibitor |
| CA2598893C (en) * | 2006-10-11 | 2012-04-10 | Astellas Pharma Inc. | Eml4-alk fusion gene |
| JP2010046057A (ja) * | 2008-07-22 | 2010-03-04 | Akita Univ | 癌細胞の治療感受性増強剤、癌細胞の治療感受性の判定方法、および癌細胞の治療感受性判定キット |
| US9597348B2 (en) * | 2012-09-06 | 2017-03-21 | Epizyme, Inc. | Method of treating leukemia |
| US9446064B2 (en) * | 2013-03-14 | 2016-09-20 | Epizyme, Inc. | Combination therapy for treating cancer |
| WO2015073706A1 (en) * | 2013-11-13 | 2015-05-21 | Epizyme, Inc. | Methods for treating cancer |
-
2013
- 2013-12-20 JP JP2015549801A patent/JP2016510316A/ja active Pending
- 2013-12-20 WO PCT/US2013/077082 patent/WO2014100662A1/en not_active Ceased
- 2013-12-20 US US14/654,125 patent/US20150342979A1/en not_active Abandoned
- 2013-12-20 EP EP13821345.9A patent/EP2934550A1/en not_active Withdrawn
- 2013-12-20 AU AU2013361076A patent/AU2013361076B2/en not_active Ceased
- 2013-12-20 CA CA2894220A patent/CA2894220A1/en not_active Abandoned
-
2018
- 2018-10-11 JP JP2018192426A patent/JP2019031525A/ja active Pending
-
2019
- 2019-09-19 US US16/575,957 patent/US20200113923A1/en not_active Abandoned
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012075381A1 (en) * | 2010-12-03 | 2012-06-07 | Epizyme, Inc. | Substituted purine and 7 - deazapurine compounds as modulators of epigenetic enzymes |
Non-Patent Citations (3)
| Title |
|---|
| BASAVAPATHRUNI, A. et al. "Conformational Adaptation Drives Potent, Selective and Durable Inhibition of the Human Protein Methyltransferase DOT1L" Chemical Biology and Drug Design (Oct 2012) Vol.80 No.6, pages 971 to 980 * |
| CHEN, L. et al. "Abrogation of MLL-AF10 and CALM-AF10 Mediated Transformation Through Genetic Inactivation or Pharmacological Inhibition of the H3K79 Methyltransferase DOT1L" Blood (Nov 2012) Vol.120 No.21, Abstract 2384 * |
| DAIGLE, S.R. et al. "Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor" Cancer Cell (2011) Vol.20 No.1, pages 53 to 65 * |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2016510316A (ja) | 2016-04-07 |
| CA2894220A1 (en) | 2014-06-26 |
| EP2934550A1 (en) | 2015-10-28 |
| WO2014100662A1 (en) | 2014-06-26 |
| JP2019031525A (ja) | 2019-02-28 |
| US20200113923A1 (en) | 2020-04-16 |
| US20150342979A1 (en) | 2015-12-03 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FGA | Letters patent sealed or granted (standard patent) | ||
| MK14 | Patent ceased section 143(a) (annual fees not paid) or expired |