CN103391939B - 作为表观遗传酶调节剂的经取代的嘌呤和7-氮杂嘌呤化合物 - Google Patents
作为表观遗传酶调节剂的经取代的嘌呤和7-氮杂嘌呤化合物 Download PDFInfo
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- CN103391939B CN103391939B CN201180066760.7A CN201180066760A CN103391939B CN 103391939 B CN103391939 B CN 103391939B CN 201180066760 A CN201180066760 A CN 201180066760A CN 103391939 B CN103391939 B CN 103391939B
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- 0 CC(C1)=*1c1c(C)c(*)c(*)c2c1nc(*)[n]2 Chemical compound CC(C1)=*1c1c(C)c(*)c(*)c2c1nc(*)[n]2 0.000 description 13
- FMUIUKDCXVNYSY-UHFFFAOYSA-N C=Cc1cc(CC(F)(F)F)ccc1F Chemical compound C=Cc1cc(CC(F)(F)F)ccc1F FMUIUKDCXVNYSY-UHFFFAOYSA-N 0.000 description 1
- DEEUQVQRKOISKW-UHFFFAOYSA-N CC(C)(C(C(C1)=C)=CC2C1C2CBr)C#N Chemical compound CC(C)(C(C(C1)=C)=CC2C1C2CBr)C#N DEEUQVQRKOISKW-UHFFFAOYSA-N 0.000 description 1
- JKAKAIMPPQLGGD-RIHRGEQVSA-N CC(C)N(C[C@@H](C1)[C@H]2OC(C)(C)O[C@H]2[C@@H]1[n](cc1)c2c1c(NCc(ccc(OC)c1)c1OC)ncn2)C1CC(CCc2nc(cc(C(F)(F)F)c(Cl)c3)c3[nH]2)C1 Chemical compound CC(C)N(C[C@@H](C1)[C@H]2OC(C)(C)O[C@H]2[C@@H]1[n](cc1)c2c1c(NCc(ccc(OC)c1)c1OC)ncn2)C1CC(CCc2nc(cc(C(F)(F)F)c(Cl)c3)c3[nH]2)C1 JKAKAIMPPQLGGD-RIHRGEQVSA-N 0.000 description 1
- FNLGNKVSVUHWHB-JIZJUJIKSA-N CC(C)N(C[C@H]([C@H]1OC(C)(C)O[C@H]11)OC1[n]1c(ncnc2N)c2nc1)C1CC(CCC(OCc2ccccc2)=O)C1 Chemical compound CC(C)N(C[C@H]([C@H]1OC(C)(C)O[C@H]11)OC1[n]1c(ncnc2N)c2nc1)C1CC(CCC(OCc2ccccc2)=O)C1 FNLGNKVSVUHWHB-JIZJUJIKSA-N 0.000 description 1
- WYYSTUCYZVHACI-FIXISWKDSA-O CC(C)NC[C@H](C[C@H]1OC(C)(C)[OH2+])O[C@H]1[n]1c(ncnc2N)c2nc1 Chemical compound CC(C)NC[C@H](C[C@H]1OC(C)(C)[OH2+])O[C@H]1[n]1c(ncnc2N)c2nc1 WYYSTUCYZVHACI-FIXISWKDSA-O 0.000 description 1
- IHUHMUNRHPNHRN-CCVYWJFASA-N CC(C1C)C1C([C@H](C)C1)=CC[C@H]1N Chemical compound CC(C1C)C1C([C@H](C)C1)=CC[C@H]1N IHUHMUNRHPNHRN-CCVYWJFASA-N 0.000 description 1
- JYJDMCSGYKIVPW-UHFFFAOYSA-N CC1(CCC1)c(cc1)cc([N+]([O-])=O)c1NC(C(F)(F)F)=O Chemical compound CC1(CCC1)c(cc1)cc([N+]([O-])=O)c1NC(C(F)(F)F)=O JYJDMCSGYKIVPW-UHFFFAOYSA-N 0.000 description 1
- QLLOQFCDTDWTNK-UHFFFAOYSA-N CC1=C(C)C(N=C)=CCC1CC(F)(F)F Chemical compound CC1=C(C)C(N=C)=CCC1CC(F)(F)F QLLOQFCDTDWTNK-UHFFFAOYSA-N 0.000 description 1
- VCRGORCCAWNXOD-CUIRVDNCSA-N CCN(C[C@H]([C@H]1O)OC[C@]1([n]1c2ncnc(N)c2nc1)O)[C@H]1C[C@@H](CCc2nc3cc(C(C)(C)C)ccc3[nH]2)C1 Chemical compound CCN(C[C@H]([C@H]1O)OC[C@]1([n]1c2ncnc(N)c2nc1)O)[C@H]1C[C@@H](CCc2nc3cc(C(C)(C)C)ccc3[nH]2)C1 VCRGORCCAWNXOD-CUIRVDNCSA-N 0.000 description 1
- BDXVDQGZGGFUSW-UHFFFAOYSA-N CCOC(CCC(CC1=O)C1(Cl)Cl)=O Chemical compound CCOC(CCC(CC1=O)C1(Cl)Cl)=O BDXVDQGZGGFUSW-UHFFFAOYSA-N 0.000 description 1
- YKHGURVCMYCEGN-UHFFFAOYSA-N FC1C=CC(CC(F)(F)F)CC1 Chemical compound FC1C=CC(CC(F)(F)F)CC1 YKHGURVCMYCEGN-UHFFFAOYSA-N 0.000 description 1
- SSRBPCIJNIBXCQ-UHFFFAOYSA-N Nc1ccc(C2COC2)cc1N Chemical compound Nc1ccc(C2COC2)cc1N SSRBPCIJNIBXCQ-UHFFFAOYSA-N 0.000 description 1
Classifications
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- 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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- 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
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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
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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
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- 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
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- 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
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
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- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Obesity (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Saccharide Compounds (AREA)
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 |
|---|---|
| CN103391939A CN103391939A (zh) | 2013-11-13 |
| CN103391939B true CN103391939B (zh) | 2016-03-09 |
Family
ID=45444712
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201180066760.7A Expired - Fee Related CN103391939B (zh) | 2010-12-03 | 2011-12-02 | 作为表观遗传酶调节剂的经取代的嘌呤和7-氮杂嘌呤化合物 |
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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2011336272A1 (en) | 2010-12-03 | 2013-06-20 | Epizyme, Inc. | 7-deazapurine modulators of histone methyltransferase, and methods of use thereof |
| CA2819620A1 (en) | 2010-12-03 | 2012-06-21 | Epizyme, Inc. | Modulators of histone methyltransferase, and methods of use thereof |
| JP5931905B2 (ja) * | 2010-12-03 | 2016-06-08 | エピザイム，インコーポレイティド | 置換プリン及び７‐デアザプリン化合物 |
| US9394310B2 (en) | 2010-12-03 | 2016-07-19 | Epizyme, Inc. | Carbocycle-substituted purine and 7-deazapurine compounds |
| US9670463B2 (en) | 2011-10-14 | 2017-06-06 | Children's Medical Center Corporation | Inhibition and enhancement of reprogramming by chromatin modifying enzymes |
| SG10201610936RA (en) | 2011-12-22 | 2017-02-27 | 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 |
| US9441007B2 (en) | 2012-03-21 | 2016-09-13 | Alios Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| WO2014026198A1 (en) | 2012-08-10 | 2014-02-13 | Epizyme, Inc. | Inhibitors of protein methyltransferase dot1l and methods 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 |
| EP3290421B1 (en) | 2013-02-22 | 2019-01-02 | Pfizer Inc | Combination of pyrrolo [2, 3 -d]pyrimidine derivatives with one or more additional agents as inhibitors of janus- related kinases (jak) |
| US9023883B2 (en) | 2013-03-14 | 2015-05-05 | Epizyme, Inc. | PRMT1 inhibitors and uses thereof |
| US9447079B2 (en) | 2013-03-14 | 2016-09-20 | Epizyme, Inc. | PRMT1 inhibitors and uses thereof |
| WO2014152261A1 (en) * | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Substituted 7-deazapurine compounds |
| US9120757B2 (en) | 2013-03-14 | 2015-09-01 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| WO2014153226A1 (en) | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| JP2016517434A (ja) * | 2013-03-14 | 2016-06-16 | エピザイム，インコーポレイティド | 癌を処置するための併用療法 |
| EP2970181B1 (en) | 2013-03-14 | 2017-06-07 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| US20160039767A1 (en) | 2013-03-14 | 2016-02-11 | Epizyme, Inc. | Pyrazole derivatives as prmt1 inhibitors and uses thereof |
| EP2970136A1 (en) | 2013-03-14 | 2016-01-20 | Epizyme, Inc. | Arginine methyl transferase inhibtors and uses thereof |
| JP2016514164A (ja) | 2013-03-14 | 2016-05-19 | エピザイム，インコーポレイティド | アルギニンメチルトランスフェラーゼ阻害剤としてのピラゾール誘導体およびその使用 |
| EP2970131B1 (en) | 2013-03-14 | 2017-11-15 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| US9446064B2 (en) | 2013-03-14 | 2016-09-20 | Epizyme, Inc. | Combination therapy for treating cancer |
| US9394258B2 (en) | 2013-03-14 | 2016-07-19 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| JP2016513699A (ja) * | 2013-03-15 | 2016-05-16 | エピザイム，インコーポレイティド | 癌の治療のための注射製剤 |
| EP2968387A4 (en) | 2013-03-15 | 2017-04-05 | Epizyme, Inc. | Methods of synthesizing substituted purine compounds |
| US9688714B2 (en) | 2013-07-03 | 2017-06-27 | Epizyme, Inc. | Substituted purine compounds |
| CA2919072A1 (en) * | 2013-07-29 | 2015-02-05 | 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 |
| WO2015200680A2 (en) * | 2014-06-25 | 2015-12-30 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| EP3180344B1 (en) | 2014-08-12 | 2019-09-18 | Pfizer Inc | Pyrrolo[2,3-d]pyrimidine derivatives useful for inhibiting janus kinase |
| CA2956962A1 (en) * | 2014-08-13 | 2016-02-18 | Epizyme, Inc. | Combination therapy for treating cancer |
| US9458165B2 (en) | 2014-08-27 | 2016-10-04 | Dana-Farber Cancer Institute, Inc. | DOT1L inhibitors |
| CA2960287A1 (en) * | 2014-09-17 | 2016-03-24 | Epizyme, Inc. | Injectable formulations for treating cancer |
| AU2015318593A1 (en) * | 2014-09-17 | 2017-02-23 | Epizyme, Inc. | Combination therapy for treating cancer |
| US10369166B2 (en) * | 2014-09-30 | 2019-08-06 | Susan Eve VECHT-LIFSHITZ | 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 |
| EP3407884B1 (en) | 2016-01-26 | 2025-07-09 | Memorial Sloan-Kettering Cancer Center | Targeting chromatin regulators for inhibiting leukemogenic gene expression in npm1 |
| ES3057783T3 (en) | 2016-03-15 | 2026-03-04 | Oryzon Genomics Sa | Combinations of lsd1 inhibitors for use in the treatment of neoplastic diseases |
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| 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 |
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