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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- 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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- 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
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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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- A61K31/395—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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- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
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- 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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- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
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- 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)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (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)
- Diabetes (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (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 |
|---|---|---|---|---|
| US8580762B2 (en) * | 2010-12-03 | 2013-11-12 | Epizyme, Inc. | Substituted purine and 7-deazapurine compounds |
| CA2819620A1 (en) | 2010-12-03 | 2012-06-21 | Epizyme, Inc. | Modulators of histone methyltransferase, and methods of use thereof |
| CA2819625A1 (en) | 2010-12-03 | 2012-06-07 | Epizyme, Inc. | 7-deazapurine modulators of histone methyltransferase, and methods of use thereof |
| AU2011336264A1 (en) | 2010-12-03 | 2013-06-20 | Epizyme, Inc. | Carbocycle-substituted purine and 7-deazapurine compounds |
| WO2013055397A1 (en) | 2011-10-14 | 2013-04-18 | Children's Medical Center Corporation | Inhibition and enhancement of reprogramming by chromatin modifying enzymes |
| SI2794627T1 (sl) | 2011-12-22 | 2019-02-28 | Alios Biopharma, Inc. | Substituirani nukleozidi, nukleotidi in njihovi analogi |
| 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 |
| WO2014100662A1 (en) * | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | Dot1 l inhibitors for use in the treatment of leukemia |
| EP2958921B1 (en) | 2013-02-22 | 2017-09-20 | Pfizer Inc | Pyrrolo [2, 3 -d]pyrimidine derivatives as inhibitors of janus kinases (jak) |
| US9394258B2 (en) | 2013-03-14 | 2016-07-19 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| AU2014260433A1 (en) | 2013-03-14 | 2015-09-10 | Epizyme, Inc. | Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof |
| US9120757B2 (en) | 2013-03-14 | 2015-09-01 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| EP2970136A1 (en) | 2013-03-14 | 2016-01-20 | Epizyme, Inc. | Arginine methyl transferase inhibtors and uses thereof |
| EP2970133B1 (en) | 2013-03-14 | 2018-10-24 | Epizyme, Inc. | Pyrazole derivatives as prmt1 inhibitors and uses thereof |
| SG11201506972PA (en) | 2013-03-14 | 2015-10-29 | Epizyme Inc | Arginine methyltransferase inhibitors and uses thereof |
| WO2014153208A1 (en) | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| EP2970134B1 (en) | 2013-03-14 | 2018-02-28 | Epizyme, Inc. | Pyrazole derivatives as prmt1 inhibitors and uses thereof |
| US9446064B2 (en) * | 2013-03-14 | 2016-09-20 | Epizyme, Inc. | Combination therapy for treating cancer |
| 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 |
| US20160031839A1 (en) | 2013-03-14 | 2016-02-04 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| WO2014152261A1 (en) * | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Substituted 7-deazapurine compounds |
| WO2014144659A1 (en) | 2013-03-14 | 2014-09-18 | Epizyme, Inc. | Pyrazole derivatives as prmt1 inhibitors and uses thereof |
| AU2014239516B2 (en) * | 2013-03-15 | 2019-01-24 | Epizyme, Inc. | Injectable formulations for treating cancer |
| CA2903303A1 (en) | 2013-03-15 | 2014-09-25 | Epizyme, Inc. | Methods of synthesizing substituted purine compounds |
| WO2015003131A1 (en) * | 2013-07-03 | 2015-01-08 | Epizyme, Inc. | Substituted purine compounds |
| US9535067B2 (en) | 2013-07-29 | 2017-01-03 | Dana-Farber Cancer Institute, Inc. | DOT1L probes |
| US10407732B2 (en) | 2013-08-02 | 2019-09-10 | 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 |
| EP3180344B1 (en) | 2014-08-12 | 2019-09-18 | Pfizer Inc | Pyrrolo[2,3-d]pyrimidine derivatives useful for inhibiting janus kinase |
| WO2016025635A2 (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 |
| AU2015317509A1 (en) * | 2014-09-17 | 2017-03-16 | Epizyme, Inc. | Injectable formulations for treating cancer |
| WO2016043874A2 (en) * | 2014-09-17 | 2016-03-24 | Epizyme, Inc. | Combination therapy 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 |
| CA3012649A1 (en) | 2016-01-26 | 2017-08-03 | Memorial Sloan-Kettering Cancer Center | Targeting chromatin regulators inhibits leukemogenic gene expression in npm1 mutant leukemia |
| KR102646126B1 (ko) | 2016-03-15 | 2024-03-11 | 오리존 지노믹스 에스.에이. | 혈액 악성 종양의 치료를 위한 lsd1 억제제의 조합물 |
| AU2017233898B2 (en) | 2016-03-15 | 2022-12-15 | Oryzon Genomics, S.A. | Combinations of LSD1 inhibitors for use in the treatment of solid tumors |
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