JP2018501286A5 - - Google Patents
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- JP2018501286A5 JP2018501286A5 JP2017536293A JP2017536293A JP2018501286A5 JP 2018501286 A5 JP2018501286 A5 JP 2018501286A5 JP 2017536293 A JP2017536293 A JP 2017536293A JP 2017536293 A JP2017536293 A JP 2017536293A JP 2018501286 A5 JP2018501286 A5 JP 2018501286A5
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- Prior art keywords
- alkyl
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- optionally substituted
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- Prior art date
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- 125000000217 alkyl group Chemical group 0.000 claims description 154
- -1 carbocycle Chemical group 0.000 claims description 110
- 125000005843 halogen group Chemical group 0.000 claims description 110
- 210000000130 stem cell Anatomy 0.000 claims description 104
- 150000001875 compounds Chemical class 0.000 claims description 98
- 206010028980 Neoplasm Diseases 0.000 claims description 92
- 201000011510 cancer Diseases 0.000 claims description 92
- 150000003839 salts Chemical class 0.000 claims description 68
- 125000003118 aryl group Chemical group 0.000 claims description 65
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 58
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 49
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 47
- 125000000623 heterocyclic group Chemical group 0.000 claims description 42
- 239000000203 mixture Substances 0.000 claims description 39
- 229910052799 carbon Inorganic materials 0.000 claims description 31
- 125000000304 alkynyl group Chemical group 0.000 claims description 29
- 125000004043 oxo group Chemical group O=* 0.000 claims description 28
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 27
- 241000124008 Mammalia Species 0.000 claims description 25
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 24
- 125000001054 5 membered carbocyclic group Chemical group 0.000 claims description 22
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 22
- 125000003545 alkoxy group Chemical group 0.000 claims description 22
- 125000003342 alkenyl group Chemical group 0.000 claims description 20
- 125000001072 heteroaryl group Chemical group 0.000 claims description 20
- 239000003112 inhibitor Substances 0.000 claims description 20
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 19
- 229910052757 nitrogen Inorganic materials 0.000 claims description 18
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims description 17
- 230000000694 effects Effects 0.000 claims description 16
- 229910052739 hydrogen Inorganic materials 0.000 claims description 16
- 101100073171 Drosophila melanogaster Kdm2 gene Proteins 0.000 claims description 15
- 230000004069 differentiation Effects 0.000 claims description 14
- YLPCXVWMHNNQGI-UHFFFAOYSA-N 1,2-diazabicyclo[3.2.1]octane Chemical compound C1C2CCN1NCC2 YLPCXVWMHNNQGI-UHFFFAOYSA-N 0.000 claims description 12
- 125000004193 piperazinyl group Chemical group 0.000 claims description 12
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims description 10
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 10
- 239000003814 drug Substances 0.000 claims description 10
- 125000004011 3 membered carbocyclic group Chemical group 0.000 claims description 8
- 125000001845 4 membered carbocyclic group Chemical group 0.000 claims description 8
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims description 8
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims description 8
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 8
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 8
- 206010025323 Lymphomas Diseases 0.000 claims description 8
- 239000001257 hydrogen Substances 0.000 claims description 8
- 150000002431 hydrogen Chemical class 0.000 claims description 8
- 230000001939 inductive effect Effects 0.000 claims description 8
- 208000032839 leukemia Diseases 0.000 claims description 8
- 201000005202 lung cancer Diseases 0.000 claims description 8
- 208000020816 lung neoplasm Diseases 0.000 claims description 8
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 8
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 8
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims description 7
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims description 6
- 230000000779 depleting effect Effects 0.000 claims description 6
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims description 6
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims description 5
- 125000001617 2,3-dimethoxy phenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C(OC([H])([H])[H])=C1[H] 0.000 claims description 4
- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims description 4
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims description 4
- 125000004860 4-ethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])C([H])([H])[H] 0.000 claims description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
- 230000006698 induction Effects 0.000 claims description 4
- 125000000040 m-tolyl group Chemical group [H]C1=C([H])C(*)=C([H])C(=C1[H])C([H])([H])[H] 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 125000003261 o-tolyl group Chemical group [H]C1=C([H])C(*)=C(C([H])=C1[H])C([H])([H])[H] 0.000 claims description 4
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims description 4
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 4
- 125000002112 pyrrolidino group Chemical group [*]N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 4
- 238000011282 treatment Methods 0.000 claims description 4
- 125000006276 2-bromophenyl group Chemical group [H]C1=C([H])C(Br)=C(*)C([H])=C1[H] 0.000 claims description 2
- 125000005809 3,4,5-trimethoxyphenyl group Chemical group [H]C1=C(OC([H])([H])[H])C(OC([H])([H])[H])=C(OC([H])([H])[H])C([H])=C1* 0.000 claims description 2
- 125000004207 3-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(OC([H])([H])[H])=C1[H] 0.000 claims description 2
- 101000614013 Homo sapiens Lysine-specific demethylase 2B Proteins 0.000 claims description 2
- 101000615488 Homo sapiens Methyl-CpG-binding domain protein 2 Proteins 0.000 claims description 2
- 102100040584 Lysine-specific demethylase 2B Human genes 0.000 claims description 2
- 102100021299 Methyl-CpG-binding domain protein 2 Human genes 0.000 claims description 2
- 102000005650 Notch Receptors Human genes 0.000 claims description 2
- 108010070047 Notch Receptors Proteins 0.000 claims description 2
- ZUSWDTWYONAOPH-UHFFFAOYSA-N [2-(trifluoromethyl)phenyl]hydrazine;hydrochloride Chemical group [Cl-].[NH3+]NC1=CC=CC=C1C(F)(F)F ZUSWDTWYONAOPH-UHFFFAOYSA-N 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 125000000118 dimethyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 238000013160 medical therapy Methods 0.000 claims description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 2
- 238000011321 prophylaxis Methods 0.000 claims description 2
- 230000011664 signaling Effects 0.000 claims description 2
- 230000001225 therapeutic effect Effects 0.000 claims description 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 241001024304 Mino Species 0.000 claims 1
- 230000003247 decreasing effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 24
- 0 *C(*)(C1(*)N)N=C(*)N1C(*)=O Chemical compound *C(*)(C1(*)N)N=C(*)N1C(*)=O 0.000 description 4
- PZBPWAVSDAFKKR-UHFFFAOYSA-N C(C1)CC1N(CC1)CCN1C1=NC2(CCCC2)CN1 Chemical compound C(C1)CC1N(CC1)CCN1C1=NC2(CCCC2)CN1 PZBPWAVSDAFKKR-UHFFFAOYSA-N 0.000 description 2
- GGJMDVULWOPZFJ-UHFFFAOYSA-N CC(C)c(cc1)ccc1S(N1C(N(CC2)CCN2C2CC(C)C2)=NCC1)(O)=O Chemical compound CC(C)c(cc1)ccc1S(N1C(N(CC2)CCN2C2CC(C)C2)=NCC1)(O)=O GGJMDVULWOPZFJ-UHFFFAOYSA-N 0.000 description 2
- DGZAKXCWCBQAJB-KRWDZBQOSA-N CC(C)c(cc1)ccc1S(N1C(N(CC2)C[C@H](C)N2C2CCC2)=NCC1)(=O)=O Chemical compound CC(C)c(cc1)ccc1S(N1C(N(CC2)C[C@H](C)N2C2CCC2)=NCC1)(=O)=O DGZAKXCWCBQAJB-KRWDZBQOSA-N 0.000 description 2
- NDELGZAEHZEGGT-UHFFFAOYSA-N CC(C)c(cc1)ccc1S=O Chemical compound CC(C)c(cc1)ccc1S=O NDELGZAEHZEGGT-UHFFFAOYSA-N 0.000 description 2
- IKDOSGHNSMKIPF-INIZCTEOSA-N CCN(CC1)CCN1C1=N[C@@H](C)CN1S(c1ccc(C(C)C)cc1)(=O)=O Chemical compound CCN(CC1)CCN1C1=N[C@@H](C)CN1S(c1ccc(C(C)C)cc1)(=O)=O IKDOSGHNSMKIPF-INIZCTEOSA-N 0.000 description 2
- IKDOSGHNSMKIPF-MRXNPFEDSA-N CCN(CC1)CCN1C1=N[C@H](C)CN1S(c1ccc(C(C)C)cc1)(=O)=O Chemical compound CCN(CC1)CCN1C1=N[C@H](C)CN1S(c1ccc(C(C)C)cc1)(=O)=O IKDOSGHNSMKIPF-MRXNPFEDSA-N 0.000 description 2
- DEOQQQJGUNGFJA-UHFFFAOYSA-N N#Cc(cc1)cc(cc2)c1cc2S(N1C(N(CC2)CCN2C2CCC2)=NCC1)(=O)=O Chemical compound N#Cc(cc1)cc(cc2)c1cc2S(N1C(N(CC2)CCN2C2CCC2)=NCC1)(=O)=O DEOQQQJGUNGFJA-UHFFFAOYSA-N 0.000 description 2
- NFIMKBZSGOEJID-UHFFFAOYSA-N O=S(c1cc(C2CC2)ccc1)(N1C(N(CC2)CCN2C2CCC2)=NCC1)=O Chemical compound O=S(c1cc(C2CC2)ccc1)(N1C(N(CC2)CCN2C2CCC2)=NCC1)=O NFIMKBZSGOEJID-UHFFFAOYSA-N 0.000 description 2
- QLKHAYOVBMNNDH-UHFFFAOYSA-N O=S(c1ccc(C2CC2)cc1)(N1C(N(CC2)CCN2C2CCC2)=NCC1)=O Chemical compound O=S(c1ccc(C2CC2)cc1)(N1C(N(CC2)CCN2C2CCC2)=NCC1)=O QLKHAYOVBMNNDH-UHFFFAOYSA-N 0.000 description 2
- ZOQOPXVJANRGJZ-UHFFFAOYSA-N 2-(trifluoromethyl)phenol Chemical compound OC1=CC=CC=C1C(F)(F)F ZOQOPXVJANRGJZ-UHFFFAOYSA-N 0.000 description 1
- OYWRUFONTHFTPV-UHFFFAOYSA-N CC(C)(C)c(cc1)ccc1-c1cc(O)ccc1 Chemical compound CC(C)(C)c(cc1)ccc1-c1cc(O)ccc1 OYWRUFONTHFTPV-UHFFFAOYSA-N 0.000 description 1
- SXARRWWXCNNPHR-UHFFFAOYSA-N CC(C)(C)c(cc1)ccc1-c1cccc(C(F)(F)F)c1 Chemical compound CC(C)(C)c(cc1)ccc1-c1cccc(C(F)(F)F)c1 SXARRWWXCNNPHR-UHFFFAOYSA-N 0.000 description 1
- LNHMZPLJAKHRAF-UHFFFAOYSA-N CC(C)c(cc1)ccc1/S(/N1C(N2CCN(CC3C(C)C3)CC2)=NCC1)=C(\C)/O Chemical compound CC(C)c(cc1)ccc1/S(/N1C(N2CCN(CC3C(C)C3)CC2)=NCC1)=C(\C)/O LNHMZPLJAKHRAF-UHFFFAOYSA-N 0.000 description 1
- JCZZXBBNDUHTEO-QFIPXVFZSA-N CC(C)c(cc1)ccc1S(N(C1)C(N(CC2)CCN2C2CCC2)=N[C@@H]1C1CC1)(=O)=O Chemical compound CC(C)c(cc1)ccc1S(N(C1)C(N(CC2)CCN2C2CCC2)=N[C@@H]1C1CC1)(=O)=O JCZZXBBNDUHTEO-QFIPXVFZSA-N 0.000 description 1
- FXTAEGNWBKAXQS-UHFFFAOYSA-N CC(C)c(cc1)ccc1S(N1C(N(CC2)CCN2C(C2)CC2F)=NCC1)(=O)=O Chemical compound CC(C)c(cc1)ccc1S(N1C(N(CC2)CCN2C(C2)CC2F)=NCC1)(=O)=O FXTAEGNWBKAXQS-UHFFFAOYSA-N 0.000 description 1
- XLEPOKYVAIYKGC-UHFFFAOYSA-N CC(C)c(cc1)ccc1S(N1C(N(CC2)CCN2C(C2)CC2F)=NCC1)(OC)=O Chemical compound CC(C)c(cc1)ccc1S(N1C(N(CC2)CCN2C(C2)CC2F)=NCC1)(OC)=O XLEPOKYVAIYKGC-UHFFFAOYSA-N 0.000 description 1
- AGYQXVAHSOSUQM-UHFFFAOYSA-N CC(C)c(cc1)ccc1SN1C(N2CCN(CC3C(C)C3)CC2)=NCC1 Chemical compound CC(C)c(cc1)ccc1SN1C(N2CCN(CC3C(C)C3)CC2)=NCC1 AGYQXVAHSOSUQM-UHFFFAOYSA-N 0.000 description 1
- CODOLAGGHAFSES-UHFFFAOYSA-N CCN(CC1)CCN1C1=NCCN1S(C1=CC(C(F)(F)F)=CCC1)(O)=O Chemical compound CCN(CC1)CCN1C1=NCCN1S(C1=CC(C(F)(F)F)=CCC1)(O)=O CODOLAGGHAFSES-UHFFFAOYSA-N 0.000 description 1
- CIVJDIMNCLSVNQ-UHFFFAOYSA-N CCN(CC1)CC[N-]1C1=NCCN1S(c1cccc(OC(F)(F)F)c1)=O Chemical compound CCN(CC1)CC[N-]1C1=NCCN1S(c1cccc(OC(F)(F)F)c1)=O CIVJDIMNCLSVNQ-UHFFFAOYSA-N 0.000 description 1
- DDZACMDGXVXOOH-UHFFFAOYSA-N Cc(cc1)ccc1-c(cc1)ccc1O Chemical compound Cc(cc1)ccc1-c(cc1)ccc1O DDZACMDGXVXOOH-UHFFFAOYSA-N 0.000 description 1
- ZZFKRTRYOSBWQY-UHFFFAOYSA-N Cc(cc1)ccc1-c(cccc1)c1O Chemical compound Cc(cc1)ccc1-c(cccc1)c1O ZZFKRTRYOSBWQY-UHFFFAOYSA-N 0.000 description 1
- DBGGJDWYVIWOIA-UHFFFAOYSA-N Cc(cc1)ccc1-c1ccc(C(F)(F)F)cc1 Chemical compound Cc(cc1)ccc1-c1ccc(C(F)(F)F)cc1 DBGGJDWYVIWOIA-UHFFFAOYSA-N 0.000 description 1
- GVVICDFSXZKAPO-UHFFFAOYSA-N Cc(cc1)ccc1-c1ccccc1C(F)(F)F Chemical compound Cc(cc1)ccc1-c1ccccc1C(F)(F)F GVVICDFSXZKAPO-UHFFFAOYSA-N 0.000 description 1
- KUZNURGIXXKBEJ-UHFFFAOYSA-N Cc(cc1)ccc1-c1cccnc1 Chemical compound Cc(cc1)ccc1-c1cccnc1 KUZNURGIXXKBEJ-UHFFFAOYSA-N 0.000 description 1
- MRAIVJPPOXSJNG-UHFFFAOYSA-N Cc(cc1)ccc1-c1ccncc1 Chemical compound Cc(cc1)ccc1-c1ccncc1 MRAIVJPPOXSJNG-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562101933P | 2015-01-09 | 2015-01-09 | |
| US62/101,933 | 2015-01-09 | ||
| PCT/US2016/012588 WO2016112251A1 (en) | 2015-01-09 | 2016-01-08 | 4,5-dihydroimidazole derivatives and their use as histone demethylase (kdm2b) inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018501286A JP2018501286A (ja) | 2018-01-18 |
| JP2018501286A5 true JP2018501286A5 (OSRAM) | 2019-02-14 |
| JP6889661B2 JP6889661B2 (ja) | 2021-06-18 |
Family
ID=55300775
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017536293A Active JP6889661B2 (ja) | 2015-01-09 | 2016-01-08 | ４，５−ジヒドロイミダゾール誘導体およびヒストンジメチラーゼ（ｋｄｍ２ｂ）インヒビターとしてのその使用 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US10202354B2 (OSRAM) |
| EP (1) | EP3242875B1 (OSRAM) |
| JP (1) | JP6889661B2 (OSRAM) |
| CN (1) | CN107406418B (OSRAM) |
| WO (1) | WO2016112251A1 (OSRAM) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016112251A1 (en) | 2015-01-09 | 2016-07-14 | Genentech, Inc. | 4,5-dihydroimidazole derivatives and their use as histone demethylase (kdm2b) inhibitors |
| DK3280401T3 (da) * | 2015-04-07 | 2021-11-15 | Ela Pharma Ltd | Sammensætninger til behandling og/eller forebyggelse af celle- eller vævsnekrose specielt rettet mod kathepsin c og/eller cela1 og/eller cela3a og/eller strukturelt relaterede enzymer dertil |
| WO2018132825A2 (en) * | 2017-01-16 | 2018-07-19 | Memorial Sloan Kettering Cancer Center | Treatment of sarcoma |
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| US4943533A (en) | 1984-03-01 | 1990-07-24 | The Regents Of The University Of California | Hybrid cell lines that produce monoclonal antibodies to epidermal growth factor receptor |
| WO1991003489A1 (en) | 1989-09-08 | 1991-03-21 | The Johns Hopkins University | Structural alterations of the egf receptor gene in human gliomas |
| AU661533B2 (en) | 1992-01-20 | 1995-07-27 | Astrazeneca Ab | Quinazoline derivatives |
| GB9314893D0 (en) | 1993-07-19 | 1993-09-01 | Zeneca Ltd | Quinazoline derivatives |
| ATE207366T1 (de) | 1993-12-24 | 2001-11-15 | Merck Patent Gmbh | Immunokonjugate |
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| US9133166B2 (en) * | 2013-03-14 | 2015-09-15 | Quanticel Pharmaceuticals, Inc. | Histone demethylase inhibitors |
| PL2970211T3 (pl) * | 2013-03-15 | 2018-01-31 | Quanticel Pharmaceuticals Inc | Inhibitory demetylazy histonowej |
| WO2016112251A1 (en) | 2015-01-09 | 2016-07-14 | Genentech, Inc. | 4,5-dihydroimidazole derivatives and their use as histone demethylase (kdm2b) inhibitors |
-
2016
- 2016-01-08 WO PCT/US2016/012588 patent/WO2016112251A1/en not_active Ceased
- 2016-01-08 JP JP2017536293A patent/JP6889661B2/ja active Active
- 2016-01-08 EP EP16702999.0A patent/EP3242875B1/en active Active
- 2016-01-08 CN CN201680014129.5A patent/CN107406418B/zh not_active Expired - Fee Related
-
2017
- 2017-07-07 US US15/643,805 patent/US10202354B2/en active Active
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