JP2018501286A5 - - Google Patents
Download PDFInfo
- Publication number
- 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
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- independently selected
- halo
- optionally substituted
- group
- 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.)
- Granted
Links
- 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 (enExample) | 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 (enExample) |
| EP (1) | EP3242875B1 (enExample) |
| JP (1) | JP6889661B2 (enExample) |
| CN (1) | CN107406418B (enExample) |
| WO (1) | WO2016112251A1 (enExample) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3242875B1 (en) | 2015-01-09 | 2022-02-23 | Genentech, Inc. | 4,5-dihydroimidazole derivatives and their use as histone demethylase (kdm2b) inhibitors |
| CN107690429B (zh) * | 2015-04-07 | 2022-02-25 | Ela制药有限公司 | 用于治疗和/或预防细胞或组织坏死的组合物，其特异性靶向组织蛋白酶c和/或cela1和/或cela3a和/或与其结构相关的酶 |
| WO2018132825A2 (en) * | 2017-01-16 | 2018-07-19 | Memorial Sloan Kettering Cancer Center | Treatment of sarcoma |
Family Cites Families (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CU22545A1 (es) | 1994-11-18 | 1999-03-31 | Centro Inmunologia Molecular | Obtención de un anticuerpo quimérico y humanizado contra el receptor del factor de crecimiento epidérmico para uso diagnóstico y terapéutico |
| 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 |
| CA2066428C (en) | 1989-09-08 | 2000-11-28 | Bert Vogelstein | 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 |
| ES2166368T3 (es) | 1993-12-24 | 2002-04-16 | Merck Patent Gmbh | Inmunoconjugados. |
| IL112248A0 (en) | 1994-01-25 | 1995-03-30 | Warner Lambert Co | Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them |
| IL112249A (en) | 1994-01-25 | 2001-11-25 | Warner Lambert Co | Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds |
| US5679683A (en) | 1994-01-25 | 1997-10-21 | Warner-Lambert Company | Tricyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family |
| EP0772609B1 (en) | 1994-07-21 | 1999-02-24 | Akzo Nobel N.V. | Cyclic ketone peroxide formulations |
| US5804396A (en) | 1994-10-12 | 1998-09-08 | Sugen, Inc. | Assay for agents active in proliferative disorders |
| EP0817775B1 (en) | 1995-03-30 | 2001-09-12 | Pfizer Inc. | Quinazoline derivatives |
| GB9508565D0 (en) | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quiazoline derivative |
| GB9508538D0 (en) | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
| US5747498A (en) | 1996-05-28 | 1998-05-05 | Pfizer Inc. | Alkynyl and azido-substituted 4-anilinoquinazolines |
| CA2222231A1 (en) | 1995-06-07 | 1996-12-19 | Imclone Systems Incorporated | Antibody and antibody fragments for inhibiting the growth of tumors |
| NZ312665A (en) | 1995-07-06 | 1999-08-30 | Novartis Ag | Rrolopyrimidines(7h-pyrrolo[2,3-d]pyrimidine and preparation of these |
| US5760041A (en) | 1996-02-05 | 1998-06-02 | American Cyanamid Company | 4-aminoquinazoline EGFR Inhibitors |
| GB9603095D0 (en) | 1996-02-14 | 1996-04-10 | Zeneca Ltd | Quinazoline derivatives |
| CN1145614C (zh) | 1996-04-12 | 2004-04-14 | 沃尼尔·朗伯公司 | 酪氨酸激酶的不可逆抑制剂，其制药用途及药物组合物 |
| ES2186908T3 (es) | 1996-07-13 | 2003-05-16 | Glaxo Group Ltd | Compuestos heterociciclos condensados como inhibidores de pproteina-tirosina-quinasas. |
| ID18494A (id) | 1996-10-02 | 1998-04-16 | Novartis Ag | Turunan pirazola leburan dan proses pembuatannya |
| UA73073C2 (uk) | 1997-04-03 | 2005-06-15 | Уайт Холдінгз Корпорейшн | Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція |
| US6002008A (en) | 1997-04-03 | 1999-12-14 | American Cyanamid Company | Substituted 3-cyano quinolines |
| US6235883B1 (en) | 1997-05-05 | 2001-05-22 | Abgenix, Inc. | Human monoclonal antibodies to epidermal growth factor receptor |
| PT980244E (pt) | 1997-05-06 | 2003-10-31 | Wyeth Corp | Utilizacao de compostos de quinazolina para o tratamento da doenca policistica renal |
| ZA986729B (en) | 1997-07-29 | 1999-02-02 | Warner Lambert Co | Irreversible inhibitors of tyrosine kinases |
| ZA986732B (en) | 1997-07-29 | 1999-02-02 | Warner Lambert Co | Irreversible inhibitiors of tyrosine kinases |
| TW436485B (en) | 1997-08-01 | 2001-05-28 | American Cyanamid Co | Substituted quinazoline derivatives |
| KR20010031813A (ko) | 1997-11-06 | 2001-04-16 | 윌리암 에이취 캘넌, 에곤 이 버그 | 결장 폴립 치료용 티로신 키나제 억제제로서의 퀴나졸린유도체의 용도 |
| NZ512189A (en) | 1998-11-19 | 2003-10-31 | Warner Lambert Co | N-[4-(3-chloro-4-fluoro-phenylamino)-7-(3-morpholin-4- yl-propoxy)-quinazolin-6-yl]-acrylamide useful as an irreversible inhibitor of tyrosine kinases |
| CN101316823B (zh) * | 2005-12-01 | 2013-05-22 | 霍夫曼-拉罗奇有限公司 | 用作抗癌剂的作为p53和MDM2蛋白之间相互作用的抑制剂的2,4,5-三苯基咪唑啉衍生物 |
| CA2670105A1 (en) * | 2006-11-27 | 2008-06-05 | Novartis Ag | Substituted dihydroimidazoles and their use in the treatment of tumors |
| US7897602B2 (en) * | 2009-01-12 | 2011-03-01 | Development Center For Biotechnology | Indolinone compounds as kinase inhibitors |
| EP2698367A1 (en) * | 2012-08-14 | 2014-02-19 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Benzimidazoles for the treatment of cancer |
| CA2903081A1 (en) * | 2013-03-14 | 2014-09-25 | Quanticel Pharmaceuticals, Inc. | Histone demethylase inhibitors |
| HRP20171609T1 (hr) * | 2013-03-15 | 2017-12-15 | Quanticel Pharmaceuticals Inc | Inhibitori histon demetilaze |
| EP3242875B1 (en) | 2015-01-09 | 2022-02-23 | Genentech, Inc. | 4,5-dihydroimidazole derivatives and their use as histone demethylase (kdm2b) inhibitors |
-
2016
- 2016-01-08 EP EP16702999.0A patent/EP3242875B1/en active Active
- 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 CN CN201680014129.5A patent/CN107406418B/zh not_active Expired - Fee Related
-
2017
- 2017-07-07 US US15/643,805 patent/US10202354B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| TWI579284B (zh) | 咪唑并吡咯啶酮化合物 | |
| RU2403247C2 (ru) | Модуляторы никотиновых ацетилхолиновых рецепторов альфа 7 и их терапевтические применения | |
| RU2006135111A (ru) | Производные тиазола | |
| RU2018106453A (ru) | Соединения | |
| RU2014152790A (ru) | Пирролопиразоновые ингибиторы танкиразы | |
| RU2018111439A (ru) | Новое пиразоло[3, 4-d]пиримидиновое соединение или его соль | |
| RU2004121161A (ru) | Замещенные 2-тио-3,5-дициано-4-фенил-6-аминопиридины и их применение | |
| PE20231441A1 (es) | Cocristal de un inhibidor de cdk | |
| JP2011509309A5 (enExample) | ||
| JP2009536620A5 (enExample) | ||
| RU2005113168A (ru) | Производные 2-пиридона в качестве ингибитора нейтрофильной эластазы | |
| CA2416274A1 (en) | N-phenyl-2-pyrimidine-amine derivatives | |
| RU2007116119A (ru) | Производные циклоспорина, замещенные 3-эфиром и 3-тиоэфиром, для лечения и профилактики инфекционного гепатита с | |
| JP2016506387A5 (enExample) | ||
| JP2017507122A5 (enExample) | ||
| JP2022141835A5 (enExample) | ||
| RU2007101309A (ru) | Боросодержащее соединение и способы применения | |
| RU2014141674A (ru) | 3,5-диаминопиразоловые ингибиторы киназы | |
| RU2019141734A (ru) | Терапевтические соединения и композиции и способы их применения | |
| JP2011516511A5 (enExample) | ||
| RU2015150120A (ru) | Соединение дикарбоновой кислоты | |
| RU2017117566A (ru) | Активатор kcnq2-5 каналов | |
| JP2001516718A5 (enExample) | ||
| JP2018501286A5 (enExample) | ||
| RU2012108423A (ru) | Ацилгуанидиновые производные с азотсодержащим циклом |