JP2015518001A5 - - Google Patents
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- JP2015518001A5 JP2015518001A5 JP2015505958A JP2015505958A JP2015518001A5 JP 2015518001 A5 JP2015518001 A5 JP 2015518001A5 JP 2015505958 A JP2015505958 A JP 2015505958A JP 2015505958 A JP2015505958 A JP 2015505958A JP 2015518001 A5 JP2015518001 A5 JP 2015518001A5
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- JP
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- Prior art date
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- 235000001014 amino acid Nutrition 0.000 claims description 141
- 150000001413 amino acids Chemical group 0.000 claims description 141
- 238000006467 substitution reaction Methods 0.000 claims description 114
- 239000000203 mixture Substances 0.000 claims description 60
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- 239000003814 drug Substances 0.000 claims description 27
- 229940124597 therapeutic agent Drugs 0.000 claims description 27
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 claims description 22
- 150000001875 compounds Chemical class 0.000 claims description 21
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims description 20
- 102100038970 Histone-lysine N-methyltransferase EZH2 Human genes 0.000 claims description 20
- 101000882127 Homo sapiens Histone-lysine N-methyltransferase EZH2 Proteins 0.000 claims description 20
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims description 18
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- 239000004472 Lysine Substances 0.000 claims description 16
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- 206010028980 Neoplasm Diseases 0.000 claims description 15
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 claims description 15
- 201000011510 cancer Diseases 0.000 claims description 15
- ZDXPYRJPNDTMRX-UHFFFAOYSA-N glutamine Natural products OC(=O)C(N)CCC(N)=O ZDXPYRJPNDTMRX-UHFFFAOYSA-N 0.000 claims description 15
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- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims description 13
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims description 13
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- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 claims description 12
- 239000004473 Threonine Substances 0.000 claims description 12
- 230000035772 mutation Effects 0.000 claims description 12
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims description 11
- 235000013922 glutamic acid Nutrition 0.000 claims description 11
- 239000004220 glutamic acid Substances 0.000 claims description 11
- 150000003839 salts Chemical class 0.000 claims description 11
- -1 C 1 -C 6 alkyl Chemical group 0.000 claims description 10
- 239000004471 Glycine Substances 0.000 claims description 10
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 claims description 10
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims description 10
- 125000000217 alkyl group Chemical group 0.000 claims description 10
- AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 claims description 10
- 229960000310 isoleucine Drugs 0.000 claims description 10
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims description 8
- 125000001475 halogen functional group Chemical group 0.000 claims description 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 8
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims description 8
- 229940024606 amino acid Drugs 0.000 claims description 7
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 6
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 6
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims description 6
- 125000003118 aryl group Chemical group 0.000 claims description 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 6
- XOFYZVNMUHMLCC-ZPOLXVRWSA-N prednisone Chemical compound O=C1C=C[C@]2(C)[C@H]3C(=O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 XOFYZVNMUHMLCC-ZPOLXVRWSA-N 0.000 claims description 6
- 229960004618 prednisone Drugs 0.000 claims description 6
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 5
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims description 4
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 claims description 4
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims description 4
- 206010025323 Lymphomas Diseases 0.000 claims description 4
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims description 4
- 108020004485 Nonsense Codon Proteins 0.000 claims description 4
- 208000006994 Precancerous Conditions Diseases 0.000 claims description 4
- 210000004027 cell Anatomy 0.000 claims description 4
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- 229930182817 methionine Natural products 0.000 claims description 4
- 230000011987 methylation Effects 0.000 claims description 4
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- 230000037434 nonsense mutation Effects 0.000 claims description 4
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 claims description 4
- 229960005205 prednisolone Drugs 0.000 claims description 4
- OIGNJSKKLXVSLS-VWUMJDOOSA-N prednisolone Chemical compound O=C1C=C[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 OIGNJSKKLXVSLS-VWUMJDOOSA-N 0.000 claims description 4
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims description 4
- 125000003588 lysine group Chemical class [H]N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 claims description 3
- 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 claims description 2
- PYRKKGOKRMZEIT-UHFFFAOYSA-N 2-[6-(2-cyclopropylethoxy)-9-(2-hydroxy-2-methylpropyl)-1h-phenanthro[9,10-d]imidazol-2-yl]-5-fluorobenzene-1,3-dicarbonitrile Chemical compound C1=C2C3=CC(CC(C)(O)C)=CC=C3C=3NC(C=4C(=CC(F)=CC=4C#N)C#N)=NC=3C2=CC=C1OCCC1CC1 PYRKKGOKRMZEIT-UHFFFAOYSA-N 0.000 claims description 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 2
- CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 claims description 2
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- QIVBCDIJIAJPQS-UHFFFAOYSA-N Tryptophan Natural products C1=CC=C2C(CC(N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-N 0.000 claims description 2
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- 229960004316 cisplatin Drugs 0.000 claims description 2
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims description 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 229960004397 cyclophosphamide Drugs 0.000 claims description 2
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- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 claims description 2
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims description 2
- 229960004679 doxorubicin Drugs 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 201000003444 follicular lymphoma Diseases 0.000 claims description 2
- 230000037433 frameshift Effects 0.000 claims description 2
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- 238000003780 insertion Methods 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 230000001404 mediated effect Effects 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 150000007523 nucleic acids Chemical group 0.000 claims description 2
- 239000002773 nucleotide Substances 0.000 claims description 2
- 125000003729 nucleotide group Chemical group 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 125000003386 piperidinyl group Chemical group 0.000 claims description 2
- 235000018102 proteins Nutrition 0.000 claims description 2
- 102000004169 proteins and genes Human genes 0.000 claims description 2
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- 102220105330 rs146675823 Human genes 0.000 claims description 2
- 125000001424 substituent group Chemical group 0.000 claims description 2
- 239000000758 substrate Substances 0.000 claims description 2
- 229960004528 vincristine Drugs 0.000 claims description 2
- OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 claims description 2
- OGWKCGZFUXNPDA-UHFFFAOYSA-N vincristine Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(OC(C)=O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-UHFFFAOYSA-N 0.000 claims description 2
- 230000002265 prevention Effects 0.000 claims 5
- PBUUPFTVAPUWDE-UGZDLDLSSA-N 2-[[(2S,4S)-2-[bis(2-chloroethyl)amino]-2-oxo-1,3,2lambda5-oxazaphosphinan-4-yl]sulfanyl]ethanesulfonic acid Chemical compound OS(=O)(=O)CCS[C@H]1CCO[P@](=O)(N(CCCl)CCCl)N1 PBUUPFTVAPUWDE-UGZDLDLSSA-N 0.000 claims 1
- 230000006806 disease prevention Effects 0.000 claims 1
- 125000000291 glutamic acid group Chemical class N[C@@H](CCC(O)=O)C(=O)* 0.000 claims 1
- 125000000404 glutamine group Chemical group N[C@@H](CCC(N)=O)C(=O)* 0.000 claims 1
- 229950000547 mafosfamide Drugs 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 238000000034 method Methods 0.000 description 28
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 6
- 125000003545 alkoxy group Chemical group 0.000 description 2
- 150000003680 valines Chemical class 0.000 description 2
- XAUDJQYHKZQPEU-KVQBGUIXSA-N 5-aza-2'-deoxycytidine Chemical compound O=C1N=C(N)N=CN1[C@@H]1O[C@H](CO)[C@@H](O)C1 XAUDJQYHKZQPEU-KVQBGUIXSA-N 0.000 description 1
- HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 description 1
- COBBNRKBTCBWQP-UHFFFAOYSA-N Graveoline Chemical compound C1=C2OCOC2=CC(C=2N(C3=CC=CC=C3C(=O)C=2)C)=C1 COBBNRKBTCBWQP-UHFFFAOYSA-N 0.000 description 1
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- 229960003603 decitabine Drugs 0.000 description 1
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Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261624194P | 2012-04-13 | 2012-04-13 | |
| US61/624,194 | 2012-04-13 | ||
| US201361785169P | 2013-03-14 | 2013-03-14 | |
| US61/785,169 | 2013-03-14 | ||
| PCT/US2013/036452 WO2013155464A1 (en) | 2012-04-13 | 2013-04-12 | Combination therapy for treating cancer |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017141119A Division JP2017190337A (ja) | 2012-04-13 | 2017-07-20 | がんを処置するための組合せ治療 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015518001A JP2015518001A (ja) | 2015-06-25 |
| JP2015518001A5 true JP2015518001A5 (enExample) | 2016-06-09 |
| JP6340361B2 JP6340361B2 (ja) | 2018-06-06 |
Family
ID=49328220
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015505958A Active JP6340361B2 (ja) | 2012-04-13 | 2013-04-12 | がんを処置するための組合せ治療 |
| JP2017141119A Withdrawn JP2017190337A (ja) | 2012-04-13 | 2017-07-20 | がんを処置するための組合せ治療 |
| JP2019134563A Withdrawn JP2019196386A (ja) | 2012-04-13 | 2019-07-22 | がんを処置するための組合せ治療 |
| JP2021079088A Withdrawn JP2021119191A (ja) | 2012-04-13 | 2021-05-07 | がんを処置するための組合せ治療 |
| JP2023072566A Active JP7759910B2 (ja) | 2012-04-13 | 2023-04-26 | がんを処置するための組合せ治療 |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017141119A Withdrawn JP2017190337A (ja) | 2012-04-13 | 2017-07-20 | がんを処置するための組合せ治療 |
| JP2019134563A Withdrawn JP2019196386A (ja) | 2012-04-13 | 2019-07-22 | がんを処置するための組合せ治療 |
| JP2021079088A Withdrawn JP2021119191A (ja) | 2012-04-13 | 2021-05-07 | がんを処置するための組合せ治療 |
| JP2023072566A Active JP7759910B2 (ja) | 2012-04-13 | 2023-04-26 | がんを処置するための組合せ治療 |
Country Status (15)
| Country | Link |
|---|---|
| US (5) | US10301290B2 (enExample) |
| EP (2) | EP2836216B1 (enExample) |
| JP (5) | JP6340361B2 (enExample) |
| KR (5) | KR102747818B1 (enExample) |
| CN (2) | CN104768555B (enExample) |
| AU (3) | AU2013245661B2 (enExample) |
| BR (1) | BR112014025506B1 (enExample) |
| CA (1) | CA2870010C (enExample) |
| ES (1) | ES2925312T3 (enExample) |
| IL (6) | IL319364A (enExample) |
| MX (2) | MX392752B (enExample) |
| NZ (2) | NZ700759A (enExample) |
| RU (1) | RU2699546C2 (enExample) |
| SG (3) | SG10201912111TA (enExample) |
| WO (1) | WO2013155464A1 (enExample) |
Families Citing this family (60)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2841142C (en) | 2010-06-23 | 2020-12-15 | Ryan D. Morin | Biomarkers for non-hodgkin lymphomas and uses thereof |
| PL2614369T3 (pl) | 2010-09-10 | 2016-08-31 | Epizyme Inc | Sposób określania przydatności inhibitorów ludzkiego ezh2 w leczeniu |
| JO3438B1 (ar) | 2011-04-13 | 2019-10-20 | Epizyme Inc | مركبات بنزين مستبدلة بأريل أو أريل غير متجانس |
| EP2780013A4 (en) | 2011-11-18 | 2015-07-01 | Constellation Pharmaceuticals Inc | MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF |
| US9085583B2 (en) | 2012-02-10 | 2015-07-21 | Constellation—Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| PL3628670T3 (pl) | 2012-04-13 | 2023-02-20 | Epizyme, Inc. | Postać soli dla inhibicji ezh2 |
| CN104768555B (zh) | 2012-04-13 | 2018-10-30 | Epizyme股份有限公司 | 用于治疗癌症的联合治疗 |
| MX376008B (es) * | 2012-10-15 | 2025-03-07 | Epizyme Inc | Inhibidor de ezh2 para usarse en el tratamiento de sarcoma epiteloide. |
| SG10201705989YA (en) * | 2012-10-15 | 2017-08-30 | Epizyme Inc | Substituted benzene compounds |
| BR112015014090A2 (pt) | 2012-12-13 | 2017-07-11 | Glaxosmithkline Llc | intensificador de inibidores de zeste homólogo 2 |
| WO2014153030A2 (en) * | 2013-03-14 | 2014-09-25 | Genentech, Inc. | Methods of treating cancer and preventing cancer drug resistance |
| EP2970305B1 (en) | 2013-03-15 | 2017-02-22 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| CN105473580A (zh) | 2013-07-10 | 2016-04-06 | 葛兰素史密斯克莱知识产权（第2号）有限公司 | Zeste同源物增强子2抑制剂 |
| WO2015023915A1 (en) | 2013-08-15 | 2015-02-19 | Constellation Pharmaceuticals, Inc. | Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof |
| SI3057962T1 (sl) | 2013-10-16 | 2024-01-31 | Epizyme, Inc. | Oblika hidrokloridne soli za ezh2 inhibicijo |
| AU2014337121A1 (en) * | 2013-10-18 | 2016-04-14 | Epizyme, Inc. | Method of treating cancer |
| KR20220165809A (ko) * | 2013-12-06 | 2022-12-15 | 에피자임, 인코포레이티드 | 암 치료를 위한 병용 요법 |
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