JP2020517618A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2020517618A5 JP2020517618A5 JP2019556647A JP2019556647A JP2020517618A5 JP 2020517618 A5 JP2020517618 A5 JP 2020517618A5 JP 2019556647 A JP2019556647 A JP 2019556647A JP 2019556647 A JP2019556647 A JP 2019556647A JP 2020517618 A5 JP2020517618 A5 JP 2020517618A5
- Authority
- JP
- Japan
- Prior art keywords
- inhibitor
- halo
- alkyl
- optionally substituted
- independently
- 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.)
- Withdrawn
Links
- 239000003112 inhibitor Substances 0.000 claims description 390
- 125000005843 halogen group Chemical group 0.000 claims description 232
- 238000000034 method Methods 0.000 claims description 204
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 185
- -1 photemstin Chemical compound 0.000 claims description 160
- 125000000217 alkyl group Chemical group 0.000 claims description 139
- 125000005842 heteroatom Chemical group 0.000 claims description 115
- 229910052760 oxygen Inorganic materials 0.000 claims description 112
- 229910052717 sulfur Inorganic materials 0.000 claims description 112
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 93
- 125000003118 aryl group Chemical group 0.000 claims description 93
- 102100035042 Histone-lysine N-methyltransferase EHMT2 Human genes 0.000 claims description 91
- 101000877312 Homo sapiens Histone-lysine N-methyltransferase EHMT2 Proteins 0.000 claims description 91
- 229910052799 carbon Inorganic materials 0.000 claims description 91
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 90
- 229910052739 hydrogen Inorganic materials 0.000 claims description 90
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 86
- 125000003545 alkoxy group Chemical group 0.000 claims description 81
- 125000004043 oxo group Chemical group O=* 0.000 claims description 80
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 65
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 65
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 59
- 206010028980 Neoplasm Diseases 0.000 claims description 57
- 229910052757 nitrogen Inorganic materials 0.000 claims description 56
- 150000003839 salts Chemical class 0.000 claims description 55
- 239000003814 drug Substances 0.000 claims description 53
- 150000001875 compounds Chemical class 0.000 claims description 52
- 229940124597 therapeutic agent Drugs 0.000 claims description 48
- 125000005647 linker group Chemical group 0.000 claims description 46
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 43
- 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 43
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 36
- 201000011510 cancer Diseases 0.000 claims description 34
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 32
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 32
- 125000004429 atom Chemical group 0.000 claims description 30
- 239000003795 chemical substances by application Substances 0.000 claims description 24
- 239000000556 agonist Substances 0.000 claims description 23
- 229960005486 vaccine Drugs 0.000 claims description 22
- 108010079944 Interferon-alpha2b Proteins 0.000 claims description 21
- 125000001072 heteroaryl group Chemical group 0.000 claims description 21
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 20
- 230000037361 pathway Effects 0.000 claims description 20
- 210000004027 cell Anatomy 0.000 claims description 18
- 229960005386 ipilimumab Drugs 0.000 claims description 18
- 102100040018 Interferon alpha-2 Human genes 0.000 claims description 17
- 229940043355 kinase inhibitor Drugs 0.000 claims description 14
- 201000001441 melanoma Diseases 0.000 claims description 14
- 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 claims description 13
- 229960005167 everolimus Drugs 0.000 claims description 13
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 13
- 102000000588 Interleukin-2 Human genes 0.000 claims description 12
- 239000005557 antagonist Substances 0.000 claims description 12
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims description 12
- 229940124617 receptor tyrosine kinase inhibitor Drugs 0.000 claims description 12
- 239000005483 tyrosine kinase inhibitor Substances 0.000 claims description 12
- MLDQJTXFUGDVEO-UHFFFAOYSA-N BAY-43-9006 Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=CC(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 MLDQJTXFUGDVEO-UHFFFAOYSA-N 0.000 claims description 11
- 108020004414 DNA Proteins 0.000 claims description 10
- AUZONCFQVSMFAP-UHFFFAOYSA-N disulfiram Chemical compound CCN(CC)C(=S)SSC(=S)N(CC)CC AUZONCFQVSMFAP-UHFFFAOYSA-N 0.000 claims description 10
- 108090000765 processed proteins & peptides Proteins 0.000 claims description 10
- 102000003702 retinoic acid receptors Human genes 0.000 claims description 10
- 108090000064 retinoic acid receptors Proteins 0.000 claims description 10
- 230000011664 signaling Effects 0.000 claims description 10
- 206010011703 Cyanosis Diseases 0.000 claims description 9
- 108010002350 Interleukin-2 Proteins 0.000 claims description 9
- 229940124647 MEK inhibitor Drugs 0.000 claims description 9
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 9
- SHGAZHPCJJPHSC-YCNIQYBTSA-N all-trans-retinoic acid Chemical compound OC(=O)\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-YCNIQYBTSA-N 0.000 claims description 9
- 239000003697 methyltransferase inhibitor Substances 0.000 claims description 9
- 201000000050 myeloid neoplasm Diseases 0.000 claims description 9
- 229960002621 pembrolizumab Drugs 0.000 claims description 9
- 125000004076 pyridyl group Chemical group 0.000 claims description 9
- 238000002560 therapeutic procedure Methods 0.000 claims description 9
- GPXBXXGIAQBQNI-UHFFFAOYSA-N vemurafenib Chemical compound CCCS(=O)(=O)NC1=CC=C(F)C(C(=O)C=2C3=CC(=CN=C3NC=2)C=2C=CC(Cl)=CC=2)=C1F GPXBXXGIAQBQNI-UHFFFAOYSA-N 0.000 claims description 9
- UHDGCWIWMRVCDJ-CCXZUQQUSA-N Cytarabine Chemical compound O=C1N=C(N)C=CN1[C@H]1[C@@H](O)[C@H](O)[C@@H](CO)O1 UHDGCWIWMRVCDJ-CCXZUQQUSA-N 0.000 claims description 8
- IBXPAFBDJCXCDW-MHFPCNPESA-A [Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].Cc1cn([C@H]2C[C@H](O)[C@@H](COP([S-])(=O)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3CO)n3cc(C)c(=O)[nH]c3=O)n3ccc(N)nc3=O)n3cc(C)c(=O)[nH]c3=O)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3cnc4c(N)ncnc34)n3cnc4c3nc(N)[nH]c4=O)n3ccc(N)nc3=O)n3cnc4c3nc(N)[nH]c4=O)n3cc(C)c(=O)[nH]c3=O)n3cnc4c3nc(N)[nH]c4=O)n3ccc(N)nc3=O)n3cnc4c3nc(N)[nH]c4=O)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3cnc4c(N)ncnc34)O2)c(=O)[nH]c1=O Chemical compound [Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].Cc1cn([C@H]2C[C@H](O)[C@@H](COP([S-])(=O)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3COP([O-])(=S)O[C@H]3C[C@@H](O[C@@H]3CO)n3cc(C)c(=O)[nH]c3=O)n3ccc(N)nc3=O)n3cc(C)c(=O)[nH]c3=O)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3cnc4c(N)ncnc34)n3cnc4c3nc(N)[nH]c4=O)n3ccc(N)nc3=O)n3cnc4c3nc(N)[nH]c4=O)n3cc(C)c(=O)[nH]c3=O)n3cnc4c3nc(N)[nH]c4=O)n3ccc(N)nc3=O)n3cnc4c3nc(N)[nH]c4=O)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3cnc4c(N)ncnc34)O2)c(=O)[nH]c1=O IBXPAFBDJCXCDW-MHFPCNPESA-A 0.000 claims description 8
- 230000006907 apoptotic process Effects 0.000 claims description 8
- 125000004432 carbon atom Chemical group C* 0.000 claims description 8
- 239000003102 growth factor Substances 0.000 claims description 8
- 229960003301 nivolumab Drugs 0.000 claims description 8
- 229960004390 palbociclib Drugs 0.000 claims description 8
- AHJRHEGDXFFMBM-UHFFFAOYSA-N palbociclib Chemical compound N1=C2N(C3CCCC3)C(=O)C(C(=O)C)=C(C)C2=CN=C1NC(N=C1)=CC=C1N1CCNCC1 AHJRHEGDXFFMBM-UHFFFAOYSA-N 0.000 claims description 8
- 229940121649 protein inhibitor Drugs 0.000 claims description 8
- 229930002330 retinoic acid Natural products 0.000 claims description 8
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 claims description 8
- STQGQHZAVUOBTE-UHFFFAOYSA-N 7-Cyan-hept-2t-en-4,6-diinsaeure Natural products C1=2C(O)=C3C(=O)C=4C(OC)=CC=CC=4C(=O)C3=C(O)C=2CC(O)(C(C)=O)CC1OC1CC(N)C(O)C(C)O1 STQGQHZAVUOBTE-UHFFFAOYSA-N 0.000 claims description 7
- 239000005511 L01XE05 - Sorafenib Substances 0.000 claims description 7
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims description 7
- 206010039491 Sarcoma Diseases 0.000 claims description 7
- BPEGJWRSRHCHSN-UHFFFAOYSA-N Temozolomide Chemical compound O=C1N(C)N=NC2=C(C(N)=O)N=CN21 BPEGJWRSRHCHSN-UHFFFAOYSA-N 0.000 claims description 7
- 229940100198 alkylating agent Drugs 0.000 claims description 7
- 239000002168 alkylating agent Substances 0.000 claims description 7
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims description 7
- 229960004316 cisplatin Drugs 0.000 claims description 7
- 229960002465 dabrafenib Drugs 0.000 claims description 7
- BFSMGDJOXZAERB-UHFFFAOYSA-N dabrafenib Chemical compound S1C(C(C)(C)C)=NC(C=2C(=C(NS(=O)(=O)C=3C(=CC=CC=3F)F)C=CC=2)F)=C1C1=CC=NC(N)=N1 BFSMGDJOXZAERB-UHFFFAOYSA-N 0.000 claims description 7
- 229960000975 daunorubicin Drugs 0.000 claims description 7
- STQGQHZAVUOBTE-VGBVRHCVSA-N daunorubicin 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(C)=O)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 STQGQHZAVUOBTE-VGBVRHCVSA-N 0.000 claims description 7
- 229960003668 docetaxel Drugs 0.000 claims description 7
- 239000003197 protein kinase B inhibitor Substances 0.000 claims description 7
- 102200055464 rs113488022 Human genes 0.000 claims description 7
- 102220197820 rs121913227 Human genes 0.000 claims description 7
- 229960003787 sorafenib Drugs 0.000 claims description 7
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 6
- 206010006187 Breast cancer Diseases 0.000 claims description 6
- 208000026310 Breast neoplasm Diseases 0.000 claims description 6
- 108010041986 DNA Vaccines Proteins 0.000 claims description 6
- 229940021995 DNA vaccine Drugs 0.000 claims description 6
- 101001059454 Homo sapiens Serine/threonine-protein kinase MARK2 Proteins 0.000 claims description 6
- 229940124640 MK-2206 Drugs 0.000 claims description 6
- 201000010133 Oligodendroglioma Diseases 0.000 claims description 6
- 108091008611 Protein Kinase B Proteins 0.000 claims description 6
- 102100028904 Serine/threonine-protein kinase MARK2 Human genes 0.000 claims description 6
- 206010041067 Small cell lung cancer Diseases 0.000 claims description 6
- 102100033178 Vascular endothelial growth factor receptor 1 Human genes 0.000 claims description 6
- 201000005188 adrenal gland cancer Diseases 0.000 claims description 6
- 208000024447 adrenal gland neoplasm Diseases 0.000 claims description 6
- 210000003169 central nervous system Anatomy 0.000 claims description 6
- 229960002271 cobimetinib Drugs 0.000 claims description 6
- RESIMIUSNACMNW-BXRWSSRYSA-N cobimetinib fumarate Chemical compound OC(=O)\C=C\C(O)=O.C1C(O)([C@H]2NCCCC2)CN1C(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F.C1C(O)([C@H]2NCCCC2)CN1C(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F RESIMIUSNACMNW-BXRWSSRYSA-N 0.000 claims description 6
- 239000002875 cyclin dependent kinase inhibitor Substances 0.000 claims description 6
- 229940043378 cyclin-dependent kinase inhibitor Drugs 0.000 claims description 6
- 229940029030 dendritic cell vaccine Drugs 0.000 claims description 6
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims description 6
- 125000001624 naphthyl group Chemical group 0.000 claims description 6
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 6
- 108010092851 peginterferon alfa-2b Proteins 0.000 claims description 6
- BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Chemical compound [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 claims description 6
- 239000012268 protein inhibitor Substances 0.000 claims description 6
- 235000018102 proteins Nutrition 0.000 claims description 6
- 102000004169 proteins and genes Human genes 0.000 claims description 6
- 108090000623 proteins and genes Proteins 0.000 claims description 6
- 108091008598 receptor tyrosine kinases Proteins 0.000 claims description 6
- 102000027426 receptor tyrosine kinases Human genes 0.000 claims description 6
- 230000019491 signal transduction Effects 0.000 claims description 6
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 6
- YPBKTZBXSBLTDK-PKNBQFBNSA-N (3e)-3-[(3-bromo-4-fluoroanilino)-nitrosomethylidene]-4-[2-(sulfamoylamino)ethylamino]-1,2,5-oxadiazole Chemical compound NS(=O)(=O)NCCNC1=NON\C1=C(N=O)/NC1=CC=C(F)C(Br)=C1 YPBKTZBXSBLTDK-PKNBQFBNSA-N 0.000 claims description 5
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 5
- FDKXTQMXEQVLRF-ZHACJKMWSA-N (E)-dacarbazine Chemical compound CN(C)\N=N\c1[nH]cnc1C(N)=O FDKXTQMXEQVLRF-ZHACJKMWSA-N 0.000 claims description 5
- NMUSYJAQQFHJEW-KVTDHHQDSA-N 5-azacytidine Chemical compound O=C1N=C(N)N=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 NMUSYJAQQFHJEW-KVTDHHQDSA-N 0.000 claims description 5
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 5
- 229940124297 CDK 4/6 inhibitor Drugs 0.000 claims description 5
- 239000012275 CTLA-4 inhibitor Substances 0.000 claims description 5
- 229940045513 CTLA4 antagonist Drugs 0.000 claims description 5
- 230000007067 DNA methylation Effects 0.000 claims description 5
- 102100031480 Dual specificity mitogen-activated protein kinase kinase 1 Human genes 0.000 claims description 5
- 101710146526 Dual specificity mitogen-activated protein kinase kinase 1 Proteins 0.000 claims description 5
- 239000012824 ERK inhibitor Substances 0.000 claims description 5
- 102100038970 Histone-lysine N-methyltransferase EZH2 Human genes 0.000 claims description 5
- 102100039489 Histone-lysine N-methyltransferase, H3 lysine-79 specific Human genes 0.000 claims description 5
- 101000882127 Homo sapiens Histone-lysine N-methyltransferase EZH2 Proteins 0.000 claims description 5
- 101000963360 Homo sapiens Histone-lysine N-methyltransferase, H3 lysine-79 specific Proteins 0.000 claims description 5
- 229940076838 Immune checkpoint inhibitor Drugs 0.000 claims description 5
- 102000007399 Nuclear hormone receptor Human genes 0.000 claims description 5
- 108020005497 Nuclear hormone receptor Proteins 0.000 claims description 5
- 239000012828 PI3K inhibitor Substances 0.000 claims description 5
- 210000001744 T-lymphocyte Anatomy 0.000 claims description 5
- 239000000427 antigen Substances 0.000 claims description 5
- 108091007433 antigens Proteins 0.000 claims description 5
- 102000036639 antigens Human genes 0.000 claims description 5
- 239000003719 aurora kinase inhibitor Substances 0.000 claims description 5
- 229960002756 azacitidine Drugs 0.000 claims description 5
- ACWZRVQXLIRSDF-UHFFFAOYSA-N binimetinib Chemical compound OCCONC(=O)C=1C=C2N(C)C=NC2=C(F)C=1NC1=CC=C(Br)C=C1F ACWZRVQXLIRSDF-UHFFFAOYSA-N 0.000 claims description 5
- 201000000053 blastoma Diseases 0.000 claims description 5
- 229960003901 dacarbazine Drugs 0.000 claims description 5
- 229960002563 disulfiram Drugs 0.000 claims description 5
- 229940079593 drug Drugs 0.000 claims description 5
- 201000008184 embryoma Diseases 0.000 claims description 5
- 229950006370 epacadostat Drugs 0.000 claims description 5
- 230000012010 growth Effects 0.000 claims description 5
- 229940121372 histone deacetylase inhibitor Drugs 0.000 claims description 5
- 239000003276 histone deacetylase inhibitor Substances 0.000 claims description 5
- 239000012274 immune-checkpoint protein inhibitor Substances 0.000 claims description 5
- GOTYRUGSSMKFNF-UHFFFAOYSA-N lenalidomide Chemical compound C1C=2C(N)=CC=CC=2C(=O)N1C1CCC(=O)NC1=O GOTYRUGSSMKFNF-UHFFFAOYSA-N 0.000 claims description 5
- CMJCXYNUCSMDBY-ZDUSSCGKSA-N lgx818 Chemical compound COC(=O)N[C@@H](C)CNC1=NC=CC(C=2C(=NN(C=2)C(C)C)C=2C(=C(NS(C)(=O)=O)C=C(Cl)C=2)F)=N1 CMJCXYNUCSMDBY-ZDUSSCGKSA-N 0.000 claims description 5
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims description 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 5
- 201000008968 osteosarcoma Diseases 0.000 claims description 5
- 229960001592 paclitaxel Drugs 0.000 claims description 5
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 claims description 5
- 230000035755 proliferation Effects 0.000 claims description 5
- 230000004083 survival effect Effects 0.000 claims description 5
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims description 5
- 229960004964 temozolomide Drugs 0.000 claims description 5
- 229960003862 vemurafenib Drugs 0.000 claims description 5
- 230000035899 viability Effects 0.000 claims description 5
- 229960004528 vincristine Drugs 0.000 claims description 5
- 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 5
- 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 5
- SEGYOKHGGFKMCX-UHFFFAOYSA-N 4-[bis(1,3-benzodioxol-5-yl)-hydroxymethyl]-1-piperidinecarboxylic acid (4-nitrophenyl) ester Chemical compound C=1C=C2OCOC2=CC=1C(C=1C=C2OCOC2=CC=1)(O)C(CC1)CCN1C(=O)OC1=CC=C([N+]([O-])=O)C=C1 SEGYOKHGGFKMCX-UHFFFAOYSA-N 0.000 claims description 4
- 102100036009 5'-AMP-activated protein kinase catalytic subunit alpha-2 Human genes 0.000 claims description 4
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 claims description 4
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 claims description 4
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 claims description 4
- 239000012664 BCL-2-inhibitor Substances 0.000 claims description 4
- 229940124291 BTK inhibitor Drugs 0.000 claims description 4
- 229940123711 Bcl2 inhibitor Drugs 0.000 claims description 4
- 208000017815 Dendritic cell tumor Diseases 0.000 claims description 4
- 108010017213 Granulocyte-Macrophage Colony-Stimulating Factor Proteins 0.000 claims description 4
- 102100039620 Granulocyte-macrophage colony-stimulating factor Human genes 0.000 claims description 4
- 102000003964 Histone deacetylase Human genes 0.000 claims description 4
- 108090000353 Histone deacetylase Proteins 0.000 claims description 4
- 101000783681 Homo sapiens 5'-AMP-activated protein kinase catalytic subunit alpha-2 Proteins 0.000 claims description 4
- 101000578784 Homo sapiens Melanoma antigen recognized by T-cells 1 Proteins 0.000 claims description 4
- 101000616502 Homo sapiens Phosphatidylinositol 3,4,5-trisphosphate 5-phosphatase 1 Proteins 0.000 claims description 4
- 101000932478 Homo sapiens Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims description 4
- 101000851018 Homo sapiens Vascular endothelial growth factor receptor 1 Proteins 0.000 claims description 4
- 102000042838 JAK family Human genes 0.000 claims description 4
- 108091082332 JAK family Proteins 0.000 claims description 4
- RFSMUFRPPYDYRD-CALCHBBNSA-N Ku-0063794 Chemical compound C1=C(CO)C(OC)=CC=C1C1=CC=C(C(=NC(=N2)N3C[C@@H](C)O[C@@H](C)C3)N3CCOCC3)C2=N1 RFSMUFRPPYDYRD-CALCHBBNSA-N 0.000 claims description 4
- 239000003798 L01XE11 - Pazopanib Substances 0.000 claims description 4
- 102100028389 Melanoma antigen recognized by T-cells 1 Human genes 0.000 claims description 4
- 229940123379 Methyltransferase inhibitor Drugs 0.000 claims description 4
- 229940123282 Oncogene inhibitor Drugs 0.000 claims description 4
- YZDJQTHVDDOVHR-UHFFFAOYSA-N PLX-4720 Chemical compound CCCS(=O)(=O)NC1=CC=C(F)C(C(=O)C=2C3=CC(Cl)=CN=C3NC=2)=C1F YZDJQTHVDDOVHR-UHFFFAOYSA-N 0.000 claims description 4
- 101150023417 PPARG gene Proteins 0.000 claims description 4
- 102100021797 Phosphatidylinositol 3,4,5-trisphosphate 5-phosphatase 1 Human genes 0.000 claims description 4
- 108700020978 Proto-Oncogene Proteins 0.000 claims description 4
- 102000052575 Proto-Oncogene Human genes 0.000 claims description 4
- 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 claims description 4
- 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 claims description 4
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims description 4
- 229940096885 Retinoic acid receptor agonist Drugs 0.000 claims description 4
- 102100023606 Retinoic acid receptor alpha Human genes 0.000 claims description 4
- 102100033909 Retinoic acid receptor beta Human genes 0.000 claims description 4
- 102100033912 Retinoic acid receptor gamma Human genes 0.000 claims description 4
- 102100031463 Serine/threonine-protein kinase PLK1 Human genes 0.000 claims description 4
- 102000003425 Tyrosinase Human genes 0.000 claims description 4
- 108060008724 Tyrosinase Proteins 0.000 claims description 4
- GUWXKKAWLCENJA-WGWHJZDNSA-N [(2r,3s,5r)-5-(2-amino-6-oxo-3h-purin-9-yl)-3-hydroxyoxolan-2-yl]methyl [(2r,3s,5r)-5-(4-amino-2-oxo-1,3,5-triazin-1-yl)-2-(hydroxymethyl)oxolan-3-yl] hydrogen phosphate Chemical compound O=C1N=C(N)N=CN1[C@@H]1O[C@H](CO)[C@@H](OP(O)(=O)OC[C@@H]2[C@H](C[C@@H](O2)N2C3=C(C(N=C(N)N3)=O)N=C2)O)C1 GUWXKKAWLCENJA-WGWHJZDNSA-N 0.000 claims description 4
- 230000004913 activation Effects 0.000 claims description 4
- 229930013930 alkaloid Natural products 0.000 claims description 4
- 229960000684 cytarabine Drugs 0.000 claims description 4
- 210000004443 dendritic cell Anatomy 0.000 claims description 4
- 239000003534 dna topoisomerase inhibitor Substances 0.000 claims description 4
- 229950001546 guadecitabine Drugs 0.000 claims description 4
- 239000003481 heat shock protein 90 inhibitor Substances 0.000 claims description 4
- 229940075628 hypomethylating agent Drugs 0.000 claims description 4
- 125000002883 imidazolyl group Chemical group 0.000 claims description 4
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims description 4
- 239000000411 inducer Substances 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 4
- 230000005865 ionizing radiation Effects 0.000 claims description 4
- 210000004698 lymphocyte Anatomy 0.000 claims description 4
- 229940115256 melanoma vaccine Drugs 0.000 claims description 4
- 230000002503 metabolic effect Effects 0.000 claims description 4
- LZWZPGLVHLSWQX-XMMPIXPASA-N n'-(3,5-dimethylbenzoyl)-n'-[(3r)-2,2-dimethylhexan-3-yl]-2-ethyl-3-methoxybenzohydrazide Chemical compound C=1C(C)=CC(C)=CC=1C(=O)N([C@H](CCC)C(C)(C)C)NC(=O)C1=CC=CC(OC)=C1CC LZWZPGLVHLSWQX-XMMPIXPASA-N 0.000 claims description 4
- NSQSAUGJQHDYNO-UHFFFAOYSA-N n-[(4,6-dimethyl-2-oxo-1h-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(morpholin-4-ylmethyl)phenyl]benzamide Chemical compound C=1C(C=2C=CC(CN3CCOCC3)=CC=2)=CC(C(=O)NCC=2C(NC(C)=CC=2C)=O)=C(C)C=1N(CC)C1CCOCC1 NSQSAUGJQHDYNO-UHFFFAOYSA-N 0.000 claims description 4
- 229940127082 non-receptor tyrosine kinase inhibitor Drugs 0.000 claims description 4
- 229960000435 oblimersen Drugs 0.000 claims description 4
- 229960005184 panobinostat Drugs 0.000 claims description 4
- FWZRWHZDXBDTFK-ZHACJKMWSA-N panobinostat Chemical compound CC1=NC2=CC=C[CH]C2=C1CCNCC1=CC=C(\C=C\C(=O)NO)C=C1 FWZRWHZDXBDTFK-ZHACJKMWSA-N 0.000 claims description 4
- 229960000639 pazopanib Drugs 0.000 claims description 4
- CUIHSIWYWATEQL-UHFFFAOYSA-N pazopanib Chemical compound C1=CC2=C(C)N(C)N=C2C=C1N(C)C(N=1)=CC=NC=1NC1=CC=C(C)C(S(N)(=O)=O)=C1 CUIHSIWYWATEQL-UHFFFAOYSA-N 0.000 claims description 4
- 229940106366 pegintron Drugs 0.000 claims description 4
- HYAFETHFCAUJAY-UHFFFAOYSA-N pioglitazone Chemical compound N1=CC(CC)=CC=C1CCOC(C=C1)=CC=C1CC1C(=O)NC(=O)S1 HYAFETHFCAUJAY-UHFFFAOYSA-N 0.000 claims description 4
- 239000013612 plasmid Substances 0.000 claims description 4
- 239000003806 protein tyrosine phosphatase inhibitor Substances 0.000 claims description 4
- 229940126731 protein tyrosine phosphatase inhibitor Drugs 0.000 claims description 4
- 108091008726 retinoic acid receptors α Proteins 0.000 claims description 4
- 108091008761 retinoic acid receptors β Proteins 0.000 claims description 4
- 108091008760 retinoic acid receptors γ Proteins 0.000 claims description 4
- QBIYUDDJPRGKNJ-UHFFFAOYSA-M sepantronium bromide Chemical compound [Br-].O=C1C2=CC=CC=C2C(=O)C2=C1N(CCOC)C(C)=[N+]2CC1=CN=CC=N1 QBIYUDDJPRGKNJ-UHFFFAOYSA-M 0.000 claims description 4
- 230000008054 signal transmission Effects 0.000 claims description 4
- 229950004774 tazemetostat Drugs 0.000 claims description 4
- 229940044693 topoisomerase inhibitor Drugs 0.000 claims description 4
- 150000004917 tyrosine kinase inhibitor derivatives Chemical class 0.000 claims description 4
- SSOORFWOBGFTHL-OTEJMHTDSA-N (4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-5-carbamimidamido-1-[[(2S)-5-carbamimidamido-1-[[(1S)-4-carbamimidamido-1-carboxybutyl]amino]-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-2,6-diaminohexanoyl]amino]-3-methylbutanoyl]amino]propanoyl]amino]-5-oxopentanoic acid Chemical compound CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H](N)CCCCN)C(C)C)C(C)C)C(C)C)C(C)C)C(C)C)C(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O SSOORFWOBGFTHL-OTEJMHTDSA-N 0.000 claims description 3
- 229940123877 Aurora kinase inhibitor Drugs 0.000 claims description 3
- 206010005003 Bladder cancer Diseases 0.000 claims description 3
- 229940124204 C-kit inhibitor Drugs 0.000 claims description 3
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 3
- 206010009944 Colon cancer Diseases 0.000 claims description 3
- 102100032857 Cyclin-dependent kinase 1 Human genes 0.000 claims description 3
- 101710106279 Cyclin-dependent kinase 1 Proteins 0.000 claims description 3
- 108010004651 DAB(486)-interleukin 2 Proteins 0.000 claims description 3
- 229940124087 DNA topoisomerase II inhibitor Drugs 0.000 claims description 3
- 229940124186 Dehydrogenase inhibitor Drugs 0.000 claims description 3
- 108010053187 Diphtheria Toxin Proteins 0.000 claims description 3
- 102000016607 Diphtheria Toxin Human genes 0.000 claims description 3
- 206010061825 Duodenal neoplasm Diseases 0.000 claims description 3
- 208000032612 Glial tumor Diseases 0.000 claims description 3
- 206010018338 Glioma Diseases 0.000 claims description 3
- 229940043367 IDO1 inhibitor Drugs 0.000 claims description 3
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 3
- 239000005517 L01XE01 - Imatinib Substances 0.000 claims description 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 3
- 206010025323 Lymphomas Diseases 0.000 claims description 3
- 206010033128 Ovarian cancer Diseases 0.000 claims description 3
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 3
- 239000012271 PD-L1 inhibitor Substances 0.000 claims description 3
- 229930012538 Paclitaxel Natural products 0.000 claims description 3
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 3
- 229940049937 Pgp inhibitor Drugs 0.000 claims description 3
- 206010060862 Prostate cancer Diseases 0.000 claims description 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 3
- 206010038389 Renal cancer Diseases 0.000 claims description 3
- 206010054184 Small intestine carcinoma Diseases 0.000 claims description 3
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 3
- 208000024313 Testicular Neoplasms Diseases 0.000 claims description 3
- 206010057644 Testis cancer Diseases 0.000 claims description 3
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 3
- 239000000317 Topoisomerase II Inhibitor Substances 0.000 claims description 3
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 3
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 3
- 208000002495 Uterine Neoplasms Diseases 0.000 claims description 3
- JXLYSJRDGCGARV-WWYNWVTFSA-N Vinblastine Natural products O=C(O[C@H]1[C@](O)(C(=O)OC)[C@@H]2N(C)c3c(cc(c(OC)c3)[C@]3(C(=O)OC)c4[nH]c5c(c4CCN4C[C@](O)(CC)C[C@H](C3)C4)cccc5)[C@@]32[C@H]2[C@@]1(CC)C=CCN2CC3)C JXLYSJRDGCGARV-WWYNWVTFSA-N 0.000 claims description 3
- 108010081577 aldehyde dehydrogenase (NAD(P)+) Proteins 0.000 claims description 3
- VSRXQHXAPYXROS-UHFFFAOYSA-N azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OC(=O)C1(C(O)=O)CCC1 VSRXQHXAPYXROS-UHFFFAOYSA-N 0.000 claims description 3
- 230000027455 binding Effects 0.000 claims description 3
- 238000009739 binding Methods 0.000 claims description 3
- 229950003054 binimetinib Drugs 0.000 claims description 3
- 210000000133 brain stem Anatomy 0.000 claims description 3
- 229960004562 carboplatin Drugs 0.000 claims description 3
- 201000010881 cervical cancer Diseases 0.000 claims description 3
- 208000029742 colonic neoplasm Diseases 0.000 claims description 3
- 201000000312 duodenum cancer Diseases 0.000 claims description 3
- 229960005420 etoposide Drugs 0.000 claims description 3
- VJJPUSNTGOMMGY-MRVIYFEKSA-N etoposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@H](C)OC[C@H]4O3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 VJJPUSNTGOMMGY-MRVIYFEKSA-N 0.000 claims description 3
- 208000024519 eye neoplasm Diseases 0.000 claims description 3
- 108020001507 fusion proteins Proteins 0.000 claims description 3
- 102000037865 fusion proteins Human genes 0.000 claims description 3
- 206010017758 gastric cancer Diseases 0.000 claims description 3
- 210000004392 genitalia Anatomy 0.000 claims description 3
- 239000002748 glycoprotein P inhibitor Substances 0.000 claims description 3
- 201000010536 head and neck cancer Diseases 0.000 claims description 3
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 3
- 230000002489 hematologic effect Effects 0.000 claims description 3
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 3
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 3
- KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 claims description 3
- 229960002411 imatinib Drugs 0.000 claims description 3
- 201000010982 kidney cancer Diseases 0.000 claims description 3
- 229960004942 lenalidomide Drugs 0.000 claims description 3
- 208000032839 leukemia Diseases 0.000 claims description 3
- 201000007270 liver cancer Diseases 0.000 claims description 3
- 208000014018 liver neoplasm Diseases 0.000 claims description 3
- 201000005202 lung cancer Diseases 0.000 claims description 3
- 208000020816 lung neoplasm Diseases 0.000 claims description 3
- 229940124302 mTOR inhibitor Drugs 0.000 claims description 3
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 3
- 108091005573 modified proteins Proteins 0.000 claims description 3
- 102000035118 modified proteins Human genes 0.000 claims description 3
- VFEDRRNHLBGPNN-UHFFFAOYSA-N nimustine Chemical compound CC1=NC=C(CNC(=O)N(CCCl)N=O)C(N)=N1 VFEDRRNHLBGPNN-UHFFFAOYSA-N 0.000 claims description 3
- 201000008106 ocular cancer Diseases 0.000 claims description 3
- 201000002528 pancreatic cancer Diseases 0.000 claims description 3
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 3
- 229940121656 pd-l1 inhibitor Drugs 0.000 claims description 3
- 201000008814 placenta cancer Diseases 0.000 claims description 3
- 229910052697 platinum Inorganic materials 0.000 claims description 3
- 229960003876 ranibizumab Drugs 0.000 claims description 3
- 208000000587 small cell lung carcinoma Diseases 0.000 claims description 3
- 229950007213 spartalizumab Drugs 0.000 claims description 3
- 201000011549 stomach cancer Diseases 0.000 claims description 3
- 230000008685 targeting Effects 0.000 claims description 3
- 201000003120 testicular cancer Diseases 0.000 claims description 3
- 229940021747 therapeutic vaccine Drugs 0.000 claims description 3
- 201000002510 thyroid cancer Diseases 0.000 claims description 3
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 3
- 206010046766 uterine cancer Diseases 0.000 claims description 3
- 229960003048 vinblastine Drugs 0.000 claims description 3
- JXLYSJRDGCGARV-XQKSVPLYSA-N vincaleukoblastine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-XQKSVPLYSA-N 0.000 claims description 3
- DOKZLKDGUQWMSX-HKBQPEDESA-N (2S)-2-[[2-(2,3-dihydro-1H-inden-5-yloxy)-9-[(4-phenylphenyl)methyl]-6-purinyl]amino]-3-phenyl-1-propanol Chemical compound C([C@@H](CO)NC=1C=2N=CN(CC=3C=CC(=CC=3)C=3C=CC=CC=3)C=2N=C(OC=2C=C3CCCC3=CC=2)N=1)C1=CC=CC=C1 DOKZLKDGUQWMSX-HKBQPEDESA-N 0.000 claims description 2
- KGWWHPZQLVVAPT-STTJLUEPSA-N (2r,3r)-2,3-dihydroxybutanedioic acid;6-(4-methylpiperazin-1-yl)-n-(5-methyl-1h-pyrazol-3-yl)-2-[(e)-2-phenylethenyl]pyrimidin-4-amine Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O.C1CN(C)CCN1C1=CC(NC2=NNC(C)=C2)=NC(\C=C\C=2C=CC=CC=2)=N1 KGWWHPZQLVVAPT-STTJLUEPSA-N 0.000 claims description 2
- NEHKZPHIKKEMAZ-ZFVKSOIMSA-N (2s)-2-[[(2s,3r)-2-[[(2s)-2-[[(2s,3s)-2-[[2-[[(2s,3s)-2-[[2-[[(2s)-2-[[(2s)-2-azaniumylpropanoyl]amino]propanoyl]amino]acetyl]amino]-3-methylpentanoyl]amino]acetyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-methylb Chemical compound C[C@H](N)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C(C)C)C(O)=O NEHKZPHIKKEMAZ-ZFVKSOIMSA-N 0.000 claims description 2
- NXNQLECPAXXYTR-LCYFTJDESA-N (3z)-3-[(1-methylindol-3-yl)methylidene]-1h-pyrrolo[3,2-b]pyridin-2-one Chemical compound C12=CC=CC=C2N(C)C=C1\C=C/1C2=NC=CC=C2NC\1=O NXNQLECPAXXYTR-LCYFTJDESA-N 0.000 claims description 2
- OYYVWNDMOQPMGE-SDQBBNPISA-N (5z)-5-[[5-(4-fluoro-2-hydroxyphenyl)furan-2-yl]methylidene]-1,3-thiazolidine-2,4-dione Chemical compound OC1=CC(F)=CC=C1C(O1)=CC=C1\C=C/1C(=O)NC(=O)S\1 OYYVWNDMOQPMGE-SDQBBNPISA-N 0.000 claims description 2
- FAYAUAZLLLJJGH-UHFFFAOYSA-N 1-(3-chlorophenyl)-3-[5-[2-(4-thieno[3,2-d]pyrimidinylamino)ethyl]-2-thiazolyl]urea Chemical compound ClC1=CC=CC(NC(=O)NC=2SC(CCNC=3C=4SC=CC=4N=CN=3)=CN=2)=C1 FAYAUAZLLLJJGH-UHFFFAOYSA-N 0.000 claims description 2
- YABJJWZLRMPFSI-UHFFFAOYSA-N 1-methyl-5-[[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]-4-pyridinyl]oxy]-N-[4-(trifluoromethyl)phenyl]-2-benzimidazolamine Chemical compound N=1C2=CC(OC=3C=C(N=CC=3)C=3NC(=CN=3)C(F)(F)F)=CC=C2N(C)C=1NC1=CC=C(C(F)(F)F)C=C1 YABJJWZLRMPFSI-UHFFFAOYSA-N 0.000 claims description 2
- RYJXAZXFWIWTOJ-UHFFFAOYSA-N 1-phenyl-2-pyrrolidin-1-ylnonan-1-one Chemical compound C=1C=CC=CC=1C(=O)C(CCCCCCC)N1CCCC1 RYJXAZXFWIWTOJ-UHFFFAOYSA-N 0.000 claims description 2
- AXNUEXXEQGQWPA-UHFFFAOYSA-N 2,5-dichloro-N-(2-methyl-4-nitrophenyl)benzenesulfonamide Chemical compound CC1=CC([N+]([O-])=O)=CC=C1NS(=O)(=O)C1=CC(Cl)=CC=C1Cl AXNUEXXEQGQWPA-UHFFFAOYSA-N 0.000 claims description 2
- RNAMYOYQYRYFQY-UHFFFAOYSA-N 2-(4,4-difluoropiperidin-1-yl)-6-methoxy-n-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine Chemical compound N1=C(N2CCC(F)(F)CC2)N=C2C=C(OCCCN3CCCC3)C(OC)=CC2=C1NC1CCN(C(C)C)CC1 RNAMYOYQYRYFQY-UHFFFAOYSA-N 0.000 claims description 2
- XRKYMMUGXMWDAO-UHFFFAOYSA-N 2-(4-morpholinyl)-6-(1-thianthrenyl)-4-pyranone Chemical compound O1C(C=2C=3SC4=CC=CC=C4SC=3C=CC=2)=CC(=O)C=C1N1CCOCC1 XRKYMMUGXMWDAO-UHFFFAOYSA-N 0.000 claims description 2
- LQGCAMWQDSYOAY-UHFFFAOYSA-N 2-(oxaloamino)-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-3-carboxylic acid;hydrochloride Chemical compound Cl.C1NCCC2=C1SC(NC(=O)C(=O)O)=C2C(O)=O LQGCAMWQDSYOAY-UHFFFAOYSA-N 0.000 claims description 2
- PDMUGYOXRHVNMO-UHFFFAOYSA-N 2-[4-[3-(6-quinolinylmethyl)-5-triazolo[4,5-b]pyrazinyl]-1-pyrazolyl]ethanol Chemical compound C1=NN(CCO)C=C1C1=CN=C(N=NN2CC=3C=C4C=CC=NC4=CC=3)C2=N1 PDMUGYOXRHVNMO-UHFFFAOYSA-N 0.000 claims description 2
- LHGWWAFKVCIILM-AMZGXZFVSA-N 2-[[(2r)-butan-2-yl]amino]-4-n-[(1s,5r)-8-[5-(cyclopropanecarbonyl)pyridin-2-yl]-8-azabicyclo[3.2.1]octan-3-yl]-5-methylbenzene-1,4-dicarboxamide Chemical compound C1=C(C(N)=O)C(N[C@H](C)CC)=CC(C(=O)NC2C[C@H]3CC[C@H](N3C=3N=CC(=CC=3)C(=O)C3CC3)C2)=C1C LHGWWAFKVCIILM-AMZGXZFVSA-N 0.000 claims description 2
- BDQMCYCLZBSYJZ-UHFFFAOYSA-N 2-[[2-[[2-[[1-[2-[[5-amino-2-[[2-[[2-[(2-amino-3-methylpentanoyl)amino]-4-methylsulfanylbutanoyl]amino]-3-carboxypropanoyl]amino]-5-oxopentanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-met Chemical compound CCC(C)C(N)C(=O)NC(CCSC)C(=O)NC(CC(O)=O)C(=O)NC(CCC(N)=O)C(=O)NC(C(C)C)C(=O)N1CCCC1C(=O)NC(C(=O)NC(CO)C(=O)NC(C(C)C)C(O)=O)CC1=CC=CC=C1 BDQMCYCLZBSYJZ-UHFFFAOYSA-N 0.000 claims description 2
- LAXXPOJCFVMVAX-UHFFFAOYSA-N 2-azaniumyl-4-butylsulfanylbutanoate Chemical compound CCCCSCCC(N)C(O)=O LAXXPOJCFVMVAX-UHFFFAOYSA-N 0.000 claims description 2
- QOECJCJVIMVJGX-UHFFFAOYSA-N 2-cyclohexyl-6-methoxy-N-(1-propan-2-yl-4-piperidinyl)-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine Chemical compound N1=C(C2CCCCC2)N=C2C=C(OCCCN3CCCC3)C(OC)=CC2=C1NC1CCN(C(C)C)CC1 QOECJCJVIMVJGX-UHFFFAOYSA-N 0.000 claims description 2
- WVSBGSNVCDAMCF-UHFFFAOYSA-N 2-cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid Chemical compound OC(=O)C1=CC=C(C=2C3=CC(=CN=C3NC=2)C=2C=CC=CC=2)C=C1C1CCCC1 WVSBGSNVCDAMCF-UHFFFAOYSA-N 0.000 claims description 2
- LIOLIMKSCNQPLV-UHFFFAOYSA-N 2-fluoro-n-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide Chemical compound C1=C(F)C(C(=O)NC)=CC=C1C1=NN2C(CC=3C=C4C=CC=NC4=CC=3)=CN=C2N=C1 LIOLIMKSCNQPLV-UHFFFAOYSA-N 0.000 claims description 2
- NDFKBGWLUHKMFY-UHFFFAOYSA-N 3-[(4-anilino-2-methoxyphenyl)sulfamoyl]-2-thiophenecarboxylic acid methyl ester Chemical compound S1C=CC(S(=O)(=O)NC=2C(=CC(NC=3C=CC=CC=3)=CC=2)OC)=C1C(=O)OC NDFKBGWLUHKMFY-UHFFFAOYSA-N 0.000 claims description 2
- KIWODJBCHRADND-UHFFFAOYSA-N 3-anilino-4-[1-[3-(1-imidazolyl)propyl]-3-indolyl]pyrrole-2,5-dione Chemical compound O=C1NC(=O)C(C=2C3=CC=CC=C3N(CCCN3C=NC=C3)C=2)=C1NC1=CC=CC=C1 KIWODJBCHRADND-UHFFFAOYSA-N 0.000 claims description 2
- QFRLDZGQEZCCJZ-UHFFFAOYSA-N 4-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-[(5-nitro-2-thiazolyl)thio]-1H-1,2,4-triazol-5-one Chemical compound S1C([N+](=O)[O-])=CN=C1SC1=NNC(=O)N1C1=CC=C(OCCO2)C2=C1 QFRLDZGQEZCCJZ-UHFFFAOYSA-N 0.000 claims description 2
- PGXAYGZAIAUNJP-UHFFFAOYSA-N 4-(2,4-dichloro-5-methoxyanilino)-2-[3-(2-pyrrolidin-1-ylethoxy)anilino]pyrimidine-5-carbonitrile Chemical compound C1=C(Cl)C(OC)=CC(NC=2C(=CN=C(NC=3C=C(OCCN4CCCC4)C=CC=3)N=2)C#N)=C1Cl PGXAYGZAIAUNJP-UHFFFAOYSA-N 0.000 claims description 2
- 108010082808 4-1BB Ligand Proteins 0.000 claims description 2
- CTESJDQKVOEUOY-UHFFFAOYSA-N 4-hydroxy-3-[4-(2-hydroxyphenyl)phenyl]-6-oxo-7H-thieno[2,3-b]pyridine-5-carbonitrile Chemical compound OC1=CC=CC=C1C1=CC=C(C=2C=3C(O)=C(C#N)C(=O)NC=3SC=2)C=C1 CTESJDQKVOEUOY-UHFFFAOYSA-N 0.000 claims description 2
- VCWLZDVWHQVAJU-UHFFFAOYSA-N 4-methylidene-2-octyl-5-oxotetrahydrofuran-3-carboxylic acid Chemical compound CCCCCCCCC1OC(=O)C(=C)C1C(O)=O VCWLZDVWHQVAJU-UHFFFAOYSA-N 0.000 claims description 2
- MUOKSQABCJCOPU-UHFFFAOYSA-N 5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxylic acid Chemical compound C=1C(C(=O)O)=CC=C(C2=CN=CC=C22)C=1N=C2NC1=CC=CC(Cl)=C1 MUOKSQABCJCOPU-UHFFFAOYSA-N 0.000 claims description 2
- MYQAUKPBNJWPIE-UHFFFAOYSA-N 5-[[3-methoxy-4-[(4-methoxyphenyl)methoxy]phenyl]methyl]pyrimidine-2,4-diamine Chemical compound C1=CC(OC)=CC=C1COC(C(=C1)OC)=CC=C1CC1=CN=C(N)N=C1N MYQAUKPBNJWPIE-UHFFFAOYSA-N 0.000 claims description 2
- HCZKYSPHMGOMOY-UHFFFAOYSA-N 5-bromo-4-N-(4-fluorophenyl)-2-N-[4-methoxy-3-(2-pyrrolidin-1-ylethoxy)phenyl]pyrimidine-2,4-diamine Chemical compound BrC=1C(=NC(=NC=1)NC1=CC(=C(C=C1)OC)OCCN1CCCC1)NC1=CC=C(C=C1)F HCZKYSPHMGOMOY-UHFFFAOYSA-N 0.000 claims description 2
- QQWUGDVOUVUTOY-UHFFFAOYSA-N 5-chloro-N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine Chemical compound COC1=CC(N2CCC(CC2)N2CCN(C)CC2)=CC=C1NC(N=1)=NC=C(Cl)C=1NC1=CC=CC=C1S(=O)(=O)C(C)C QQWUGDVOUVUTOY-UHFFFAOYSA-N 0.000 claims description 2
- HLXHCNWEVQNNKA-UHFFFAOYSA-N 5-methoxy-2,3-dihydro-1h-inden-2-amine Chemical compound COC1=CC=C2CC(N)CC2=C1 HLXHCNWEVQNNKA-UHFFFAOYSA-N 0.000 claims description 2
- NHHQJBCNYHBUSI-UHFFFAOYSA-N 6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one Chemical compound COC1=C(OC)C(OC)=CC(NC=2N=C(NC=3N=C4NC(=O)C(C)(C)OC4=CC=3)C(F)=CN=2)=C1 NHHQJBCNYHBUSI-UHFFFAOYSA-N 0.000 claims description 2
- FUZYTVDVLBBXDL-UHFFFAOYSA-N 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide Chemical compound N1C2=CC=C(Cl)C=C2C2=C1C(C(=O)N)CCC2 FUZYTVDVLBBXDL-UHFFFAOYSA-N 0.000 claims description 2
- SMMOSUHFGLYTGG-UHFFFAOYSA-N 6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-7-(3-piperidin-1-ylpropoxy)-n-(1-propan-2-ylpiperidin-4-yl)quinazolin-4-amine Chemical compound N1=C(N2CCN(C)CCC2)N=C2C=C(OCCCN3CCCCC3)C(OC)=CC2=C1NC1CCN(C(C)C)CC1 SMMOSUHFGLYTGG-UHFFFAOYSA-N 0.000 claims description 2
- 239000012827 ATM inhibitor Substances 0.000 claims description 2
- 102100022089 Acyl-[acyl-carrier-protein] hydrolase Human genes 0.000 claims description 2
- 208000036832 Adenocarcinoma of ovary Diseases 0.000 claims description 2
- 108010012934 Albumin-Bound Paclitaxel Proteins 0.000 claims description 2
- 102000004400 Aminopeptidases Human genes 0.000 claims description 2
- 108090000915 Aminopeptidases Proteins 0.000 claims description 2
- 229940122531 Anaplastic lymphoma kinase inhibitor Drugs 0.000 claims description 2
- 102100032187 Androgen receptor Human genes 0.000 claims description 2
- 102100022014 Angiopoietin-1 receptor Human genes 0.000 claims description 2
- 102000010565 Apoptosis Regulatory Proteins Human genes 0.000 claims description 2
- 108010063104 Apoptosis Regulatory Proteins Proteins 0.000 claims description 2
- 102000004000 Aurora Kinase A Human genes 0.000 claims description 2
- 108090000461 Aurora Kinase A Proteins 0.000 claims description 2
- 102100032306 Aurora kinase B Human genes 0.000 claims description 2
- 108090000749 Aurora kinase B Proteins 0.000 claims description 2
- 102100026630 Aurora kinase C Human genes 0.000 claims description 2
- 108090000805 Aurora kinase C Proteins 0.000 claims description 2
- DTEKTGDVSARYDS-UHFFFAOYSA-N BI-D1870 Chemical compound N1=C2N(CCC(C)C)C(C)C(=O)N(C)C2=CN=C1NC1=CC(F)=C(O)C(F)=C1 DTEKTGDVSARYDS-UHFFFAOYSA-N 0.000 claims description 2
- CWHUFRVAEUJCEF-UHFFFAOYSA-N BKM120 Chemical compound C1=NC(N)=CC(C(F)(F)F)=C1C1=CC(N2CCOCC2)=NC(N2CCOCC2)=N1 CWHUFRVAEUJCEF-UHFFFAOYSA-N 0.000 claims description 2
- 229940125431 BRAF inhibitor Drugs 0.000 claims description 2
- 102100021663 Baculoviral IAP repeat-containing protein 5 Human genes 0.000 claims description 2
- WPTTVJLTNAWYAO-KPOXMGGZSA-N Bardoxolone methyl Chemical compound C([C@@]12C)=C(C#N)C(=O)C(C)(C)[C@@H]1CC[C@]1(C)C2=CC(=O)[C@@H]2[C@@H]3CC(C)(C)CC[C@]3(C(=O)OC)CC[C@]21C WPTTVJLTNAWYAO-KPOXMGGZSA-N 0.000 claims description 2
- 229940118364 Bcr-Abl inhibitor Drugs 0.000 claims description 2
- 206010061692 Benign muscle neoplasm Diseases 0.000 claims description 2
- KHBQMWCZKVMBLN-UHFFFAOYSA-N Benzenesulfonamide Chemical compound NS(=O)(=O)C1=CC=CC=C1 KHBQMWCZKVMBLN-UHFFFAOYSA-N 0.000 claims description 2
- 102000015735 Beta-catenin Human genes 0.000 claims description 2
- 108060000903 Beta-catenin Proteins 0.000 claims description 2
- 108010006654 Bleomycin Proteins 0.000 claims description 2
- 101001042041 Bos taurus Isocitrate dehydrogenase [NAD] subunit beta, mitochondrial Proteins 0.000 claims description 2
- 102100026008 Breakpoint cluster region protein Human genes 0.000 claims description 2
- 108010029697 CD40 Ligand Proteins 0.000 claims description 2
- 102100032937 CD40 ligand Human genes 0.000 claims description 2
- 229940126074 CDK kinase inhibitor Drugs 0.000 claims description 2
- 229940125888 CDK7 inhibitor Drugs 0.000 claims description 2
- 101150050673 CHK1 gene Proteins 0.000 claims description 2
- QFDQQSFQDXLPRF-UHFFFAOYSA-N COC1=C(C=C(C=C1)C1(NC=CC(=N1)NC1=NNC(=C1)C(C)(C)CC)N)OCCN1CCCC1 Chemical compound COC1=C(C=C(C=C1)C1(NC=CC(=N1)NC1=NNC(=C1)C(C)(C)CC)N)OCCN1CCCC1 QFDQQSFQDXLPRF-UHFFFAOYSA-N 0.000 claims description 2
- 101100220616 Caenorhabditis elegans chk-2 gene Proteins 0.000 claims description 2
- 201000000274 Carcinosarcoma Diseases 0.000 claims description 2
- 206010039499 Cartilage sarcomas Diseases 0.000 claims description 2
- 229940122537 Casein kinase inhibitor Drugs 0.000 claims description 2
- 102000000844 Cell Surface Receptors Human genes 0.000 claims description 2
- 108010001857 Cell Surface Receptors Proteins 0.000 claims description 2
- 101710163595 Chaperone protein DnaK Proteins 0.000 claims description 2
- 229940121977 Checkpoint kinase inhibitor Drugs 0.000 claims description 2
- 208000006332 Choriocarcinoma Diseases 0.000 claims description 2
- 206010073140 Clear cell sarcoma of soft tissue Diseases 0.000 claims description 2
- 208000037845 Cutaneous squamous cell carcinoma Diseases 0.000 claims description 2
- 241001464975 Cutibacterium granulosum Species 0.000 claims description 2
- 108050006400 Cyclin Proteins 0.000 claims description 2
- 102000016736 Cyclin Human genes 0.000 claims description 2
- 108010025468 Cyclin-Dependent Kinase 6 Proteins 0.000 claims description 2
- 108010016788 Cyclin-Dependent Kinase Inhibitor p21 Proteins 0.000 claims description 2
- 102000000578 Cyclin-Dependent Kinase Inhibitor p21 Human genes 0.000 claims description 2
- 229940083347 Cyclin-dependent kinase 4 inhibitor Drugs 0.000 claims description 2
- 102100026804 Cyclin-dependent kinase 6 Human genes 0.000 claims description 2
- 102100024457 Cyclin-dependent kinase 9 Human genes 0.000 claims description 2
- 102100034770 Cyclin-dependent kinase inhibitor 3 Human genes 0.000 claims description 2
- CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 claims description 2
- 102000004127 Cytokines Human genes 0.000 claims description 2
- 108090000695 Cytokines Proteins 0.000 claims description 2
- 230000006429 DNA hypomethylation Effects 0.000 claims description 2
- 229940123780 DNA topoisomerase I inhibitor Drugs 0.000 claims description 2
- 101000953655 Danio rerio Vascular endothelial growth factor receptor kdr-like Proteins 0.000 claims description 2
- 108010002156 Depsipeptides Proteins 0.000 claims description 2
- 102100037024 E3 ubiquitin-protein ligase XIAP Human genes 0.000 claims description 2
- 101150029707 ERBB2 gene Proteins 0.000 claims description 2
- 208000001976 Endocrine Gland Neoplasms Diseases 0.000 claims description 2
- 102100030011 Endoribonuclease Human genes 0.000 claims description 2
- 101710199605 Endoribonuclease Proteins 0.000 claims description 2
- 241000289669 Erinaceus europaeus Species 0.000 claims description 2
- 208000006168 Ewing Sarcoma Diseases 0.000 claims description 2
- 229940124783 FAK inhibitor Drugs 0.000 claims description 2
- 229940125830 FGFR1 inhibitor Drugs 0.000 claims description 2
- 229940125832 FGFR3 inhibitor Drugs 0.000 claims description 2
- KPBNHDGDUADAGP-VAWYXSNFSA-N FK-866 Chemical compound C=1C=CN=CC=1/C=C/C(=O)NCCCCC(CC1)CCN1C(=O)C1=CC=CC=C1 KPBNHDGDUADAGP-VAWYXSNFSA-N 0.000 claims description 2
- 108010039731 Fatty Acid Synthases Proteins 0.000 claims description 2
- 102100023593 Fibroblast growth factor receptor 1 Human genes 0.000 claims description 2
- 102100037813 Focal adhesion kinase 1 Human genes 0.000 claims description 2
- HWVNEWGKWRGSRK-UHFFFAOYSA-N GW 0742 Chemical compound CC=1N=C(C=2C=C(F)C(=CC=2)C(F)(F)F)SC=1CSC1=CC=C(OCC(O)=O)C(C)=C1 HWVNEWGKWRGSRK-UHFFFAOYSA-N 0.000 claims description 2
- DNTSIBUQMRRYIU-UHFFFAOYSA-N GW 9662 Chemical compound [O-][N+](=O)C1=CC=C(Cl)C(C(=O)NC=2C=CC=CC=2)=C1 DNTSIBUQMRRYIU-UHFFFAOYSA-N 0.000 claims description 2
- RVAQIUULWULRNW-UHFFFAOYSA-N Ganetespib Chemical compound C1=C(O)C(C(C)C)=CC(C=2N(C(O)=NN=2)C=2C=C3C=CN(C)C3=CC=2)=C1O RVAQIUULWULRNW-UHFFFAOYSA-N 0.000 claims description 2
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 claims description 2
- 102000002254 Glycogen Synthase Kinase 3 Human genes 0.000 claims description 2
- 108010014905 Glycogen Synthase Kinase 3 Proteins 0.000 claims description 2
- 229940125497 HER2 kinase inhibitor Drugs 0.000 claims description 2
- 108010035452 HLA-A1 Antigen Proteins 0.000 claims description 2
- 101710178376 Heat shock 70 kDa protein Proteins 0.000 claims description 2
- 101710152018 Heat shock cognate 70 kDa protein Proteins 0.000 claims description 2
- 108010004889 Heat-Shock Proteins Proteins 0.000 claims description 2
- 102000002812 Heat-Shock Proteins Human genes 0.000 claims description 2
- 108010036115 Histone Methyltransferases Proteins 0.000 claims description 2
- 102000011787 Histone Methyltransferases Human genes 0.000 claims description 2
- 101000753291 Homo sapiens Angiopoietin-1 receptor Proteins 0.000 claims description 2
- 101000980930 Homo sapiens Cyclin-dependent kinase 9 Proteins 0.000 claims description 2
- 101000945639 Homo sapiens Cyclin-dependent kinase inhibitor 3 Proteins 0.000 claims description 2
- 101000827746 Homo sapiens Fibroblast growth factor receptor 1 Proteins 0.000 claims description 2
- 101000878536 Homo sapiens Focal adhesion kinase 1 Proteins 0.000 claims description 2
- 101000960234 Homo sapiens Isocitrate dehydrogenase [NADP] cytoplasmic Proteins 0.000 claims description 2
- 101000599886 Homo sapiens Isocitrate dehydrogenase [NADP], mitochondrial Proteins 0.000 claims description 2
- 101000916644 Homo sapiens Macrophage colony-stimulating factor 1 receptor Proteins 0.000 claims description 2
- 101000741790 Homo sapiens Peroxisome proliferator-activated receptor gamma Proteins 0.000 claims description 2
- 101000688606 Homo sapiens Phosphatidylinositol 3,4,5-trisphosphate 5-phosphatase 2 Proteins 0.000 claims description 2
- 101000692455 Homo sapiens Platelet-derived growth factor receptor beta Proteins 0.000 claims description 2
- 101000878540 Homo sapiens Protein-tyrosine kinase 2-beta Proteins 0.000 claims description 2
- 101000944909 Homo sapiens Ribosomal protein S6 kinase alpha-1 Proteins 0.000 claims description 2
- 101000944921 Homo sapiens Ribosomal protein S6 kinase alpha-2 Proteins 0.000 claims description 2
- 101000945090 Homo sapiens Ribosomal protein S6 kinase alpha-3 Proteins 0.000 claims description 2
- 101000606090 Homo sapiens Tyrosinase Proteins 0.000 claims description 2
- 101000760175 Homo sapiens Zinc finger protein 35 Proteins 0.000 claims description 2
- 239000003458 I kappa b kinase inhibitor Substances 0.000 claims description 2
- RFAXLXKIAKIUDT-UHFFFAOYSA-N IPA-3 Chemical compound C1=CC=C2C(SSC3=C4C=CC=CC4=CC=C3O)=C(O)C=CC2=C1 RFAXLXKIAKIUDT-UHFFFAOYSA-N 0.000 claims description 2
- 102100040061 Indoleamine 2,3-dioxygenase 1 Human genes 0.000 claims description 2
- UGQMRVRMYYASKQ-KQYNXXCUSA-N Inosine Chemical compound O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1C2=NC=NC(O)=C2N=C1 UGQMRVRMYYASKQ-KQYNXXCUSA-N 0.000 claims description 2
- 108010078049 Interferon alpha-2 Proteins 0.000 claims description 2
- 108010047761 Interferon-alpha Proteins 0.000 claims description 2
- 102000006992 Interferon-alpha Human genes 0.000 claims description 2
- 102000003996 Interferon-beta Human genes 0.000 claims description 2
- 108090000467 Interferon-beta Proteins 0.000 claims description 2
- 108010050904 Interferons Proteins 0.000 claims description 2
- 102000014150 Interferons Human genes 0.000 claims description 2
- 102100039905 Isocitrate dehydrogenase [NADP] cytoplasmic Human genes 0.000 claims description 2
- 102100037845 Isocitrate dehydrogenase [NADP], mitochondrial Human genes 0.000 claims description 2
- 230000004163 JAK-STAT signaling pathway Effects 0.000 claims description 2
- 108010055717 JNK Mitogen-Activated Protein Kinases Proteins 0.000 claims description 2
- 239000012825 JNK inhibitor Substances 0.000 claims description 2
- 229940118135 JNK inhibitor Drugs 0.000 claims description 2
- 229940116839 Janus kinase 1 inhibitor Drugs 0.000 claims description 2
- 229940121730 Janus kinase 2 inhibitor Drugs 0.000 claims description 2
- 229940123241 Janus kinase 3 inhibitor Drugs 0.000 claims description 2
- QIVBCDIJIAJPQS-VIFPVBQESA-N L-tryptophane Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-VIFPVBQESA-N 0.000 claims description 2
- 239000002136 L01XE07 - Lapatinib Substances 0.000 claims description 2
- 239000002146 L01XE16 - Crizotinib Substances 0.000 claims description 2
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims description 2
- 229940113306 Ligase inhibitor Drugs 0.000 claims description 2
- 229940086609 Lipase inhibitor Drugs 0.000 claims description 2
- 102000043136 MAP kinase family Human genes 0.000 claims description 2
- 108091054455 MAP kinase family Proteins 0.000 claims description 2
- 108010010995 MART-1 Antigen Proteins 0.000 claims description 2
- 102000016200 MART-1 Antigen Human genes 0.000 claims description 2
- 229940083338 MDM2 inhibitor Drugs 0.000 claims description 2
- 239000012819 MDM2-Inhibitor Substances 0.000 claims description 2
- 108010058398 Macrophage Colony-Stimulating Factor Receptor Proteins 0.000 claims description 2
- 102100028198 Macrophage colony-stimulating factor 1 receptor Human genes 0.000 claims description 2
- 102000008135 Mechanistic Target of Rapamycin Complex 1 Human genes 0.000 claims description 2
- 108010035196 Mechanistic Target of Rapamycin Complex 1 Proteins 0.000 claims description 2
- 102000009308 Mechanistic Target of Rapamycin Complex 2 Human genes 0.000 claims description 2
- 108010034057 Mechanistic Target of Rapamycin Complex 2 Proteins 0.000 claims description 2
- 229940122357 Monoacylglycerol lipase inhibitor Drugs 0.000 claims description 2
- 101100262328 Mus musculus Dct gene Proteins 0.000 claims description 2
- 201000004458 Myoma Diseases 0.000 claims description 2
- OUSFTKFNBAZUKL-UHFFFAOYSA-N N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)piperidine-4-carboxamide Chemical compound O1C(C(C)(C)C)=CN=C1CSC(S1)=CN=C1NC(=O)C1CCNCC1 OUSFTKFNBAZUKL-UHFFFAOYSA-N 0.000 claims description 2
- CHILCFMQWMQVAL-UHFFFAOYSA-N N-[3,5-bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxybenzamide Chemical compound OC1=CC=C(Cl)C=C1C(=O)NC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1 CHILCFMQWMQVAL-UHFFFAOYSA-N 0.000 claims description 2
- IDYONDYEKGSZDQ-UHFFFAOYSA-N N-[[[4-(3-piperidin-1-ylpropyl)pyrimidin-2-yl]amino]methyl]benzamide Chemical compound O=C(NCNC1=NC(CCCN2CCCCC2)=CC=N1)C1=CC=CC=C1 IDYONDYEKGSZDQ-UHFFFAOYSA-N 0.000 claims description 2
- MZDKLVOWGIOKTN-UHFFFAOYSA-N N-methyl-N-[3-[[[2-[(2-oxo-1,3-dihydroindol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]-2-pyridinyl]methanesulfonamide Chemical compound CS(=O)(=O)N(C)C1=NC=CC=C1CNC1=NC(NC=2C=C3CC(=O)NC3=CC=2)=NC=C1C(F)(F)F MZDKLVOWGIOKTN-UHFFFAOYSA-N 0.000 claims description 2
- 102100031455 NAD-dependent protein deacetylase sirtuin-1 Human genes 0.000 claims description 2
- 101150111783 NTRK1 gene Proteins 0.000 claims description 2
- 229940038430 NY-ESO-1 vaccine Drugs 0.000 claims description 2
- 206010029260 Neuroblastoma Diseases 0.000 claims description 2
- 230000005913 Notch signaling pathway Effects 0.000 claims description 2
- BDUHCSBCVGXTJM-IZLXSDGUSA-N Nutlin-3 Chemical compound CC(C)OC1=CC(OC)=CC=C1C1=N[C@H](C=2C=CC(Cl)=CC=2)[C@H](C=2C=CC(Cl)=CC=2)N1C(=O)N1CC(=O)NCC1 BDUHCSBCVGXTJM-IZLXSDGUSA-N 0.000 claims description 2
- YULUCECVQOCQFQ-UHFFFAOYSA-N OSU-03012 Chemical compound C1=CC(NC(=O)CN)=CC=C1N1C(C=2C=C3C(C4=CC=CC=C4C=C3)=CC=2)=CC(C(F)(F)F)=N1 YULUCECVQOCQFQ-UHFFFAOYSA-N 0.000 claims description 2
- 206010061328 Ovarian epithelial cancer Diseases 0.000 claims description 2
- 239000012826 P38 inhibitor Substances 0.000 claims description 2
- 239000012661 PARP inhibitor Substances 0.000 claims description 2
- 101150117945 PDGFB gene Proteins 0.000 claims description 2
- 229940124611 PDK1 inhibitor Drugs 0.000 claims description 2
- 102000038030 PI3Ks Human genes 0.000 claims description 2
- 108091007960 PI3Ks Proteins 0.000 claims description 2
- 102100038825 Peroxisome proliferator-activated receptor gamma Human genes 0.000 claims description 2
- 229940122907 Phosphatase inhibitor Drugs 0.000 claims description 2
- 102100024242 Phosphatidylinositol 3,4,5-trisphosphate 5-phosphatase 2 Human genes 0.000 claims description 2
- 235000008331 Pinus X rigitaeda Nutrition 0.000 claims description 2
- 235000011613 Pinus brutia Nutrition 0.000 claims description 2
- 241000018646 Pinus brutia Species 0.000 claims description 2
- 102100026547 Platelet-derived growth factor receptor beta Human genes 0.000 claims description 2
- 229940121906 Poly ADP ribose polymerase inhibitor Drugs 0.000 claims description 2
- 229940079156 Proteasome inhibitor Drugs 0.000 claims description 2
- 102000009516 Protein Serine-Threonine Kinases Human genes 0.000 claims description 2
- 108010009341 Protein Serine-Threonine Kinases Proteins 0.000 claims description 2
- 102100024923 Protein kinase C beta type Human genes 0.000 claims description 2
- 101710094033 Protein kinase C beta type Proteins 0.000 claims description 2
- 102100037787 Protein-tyrosine kinase 2-beta Human genes 0.000 claims description 2
- 108010029869 Proto-Oncogene Proteins c-raf Proteins 0.000 claims description 2
- 102100028286 Proto-oncogene tyrosine-protein kinase receptor Ret Human genes 0.000 claims description 2
- 229940122106 Pyruvate dehydrogenase kinase inhibitor Drugs 0.000 claims description 2
- 102100033479 RAF proto-oncogene serine/threonine-protein kinase Human genes 0.000 claims description 2
- 229960005565 RO4929097 Drugs 0.000 claims description 2
- 101710100969 Receptor tyrosine-protein kinase erbB-3 Proteins 0.000 claims description 2
- 101710100963 Receptor tyrosine-protein kinase erbB-4 Proteins 0.000 claims description 2
- 102000034527 Retinoid X Receptors Human genes 0.000 claims description 2
- 108010038912 Retinoid X Receptors Proteins 0.000 claims description 2
- 102100033536 Ribosomal protein S6 kinase alpha-1 Human genes 0.000 claims description 2
- 102100033534 Ribosomal protein S6 kinase alpha-2 Human genes 0.000 claims description 2
- 102100033643 Ribosomal protein S6 kinase alpha-3 Human genes 0.000 claims description 2
- LOGJQOUIVKBFGH-UHFFFAOYSA-N SU6656 Chemical compound C1CCCC(N2)=C1C=C2C=C1C(=O)NC2=CC=C(S(=O)(=O)N(C)C)C=C21 LOGJQOUIVKBFGH-UHFFFAOYSA-N 0.000 claims description 2
- 229940124639 Selective inhibitor Drugs 0.000 claims description 2
- 229940121742 Serine/threonine kinase inhibitor Drugs 0.000 claims description 2
- 101710113029 Serine/threonine-protein kinase Proteins 0.000 claims description 2
- 101710183160 Serine/threonine-protein kinase PLK1 Proteins 0.000 claims description 2
- 102100030070 Serine/threonine-protein kinase Sgk1 Human genes 0.000 claims description 2
- 108010041191 Sirtuin 1 Proteins 0.000 claims description 2
- DMWVGXGXHPOEPT-UHFFFAOYSA-N Src Inhibitor-1 Chemical compound C=12C=C(OC)C(OC)=CC2=NC=NC=1NC(C=C1)=CC=C1OC1=CC=CC=C1 DMWVGXGXHPOEPT-UHFFFAOYSA-N 0.000 claims description 2
- 229940122924 Src inhibitor Drugs 0.000 claims description 2
- 102000005262 Sulfatase Human genes 0.000 claims description 2
- 108010002687 Survivin Proteins 0.000 claims description 2
- 108010008038 Synthetic Vaccines Proteins 0.000 claims description 2
- 108700012920 TNF Proteins 0.000 claims description 2
- NAVMQTYZDKMPEU-UHFFFAOYSA-N Targretin Chemical compound CC1=CC(C(CCC2(C)C)(C)C)=C2C=C1C(=C)C1=CC=C(C(O)=O)C=C1 NAVMQTYZDKMPEU-UHFFFAOYSA-N 0.000 claims description 2
- 239000004012 Tofacitinib Substances 0.000 claims description 2
- 239000000365 Topoisomerase I Inhibitor Substances 0.000 claims description 2
- QIVBCDIJIAJPQS-UHFFFAOYSA-N Tryptophan Natural products C1=CC=C2C(CC(N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-N 0.000 claims description 2
- 108060008683 Tumor Necrosis Factor Receptor Proteins 0.000 claims description 2
- 108010040002 Tumor Suppressor Proteins Proteins 0.000 claims description 2
- 102000001742 Tumor Suppressor Proteins Human genes 0.000 claims description 2
- 102100032101 Tumor necrosis factor ligand superfamily member 9 Human genes 0.000 claims description 2
- 229940123371 Tyrosine kinase 2 inhibitor Drugs 0.000 claims description 2
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 claims description 2
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 claims description 2
- 229940091171 VEGFR-2 tyrosine kinase inhibitor Drugs 0.000 claims description 2
- 108010053096 Vascular Endothelial Growth Factor Receptor-1 Proteins 0.000 claims description 2
- 108010053100 Vascular Endothelial Growth Factor Receptor-3 Proteins 0.000 claims description 2
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 claims description 2
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 claims description 2
- 102100033179 Vascular endothelial growth factor receptor 3 Human genes 0.000 claims description 2
- 229930003316 Vitamin D Natural products 0.000 claims description 2
- QYSXJUFSXHHAJI-XFEUOLMDSA-N Vitamin D3 Natural products C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C/C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-XFEUOLMDSA-N 0.000 claims description 2
- 102000013814 Wnt Human genes 0.000 claims description 2
- 108050003627 Wnt Proteins 0.000 claims description 2
- 108700031544 X-Linked Inhibitor of Apoptosis Proteins 0.000 claims description 2
- KLGQSVMIPOVQAX-UHFFFAOYSA-N XAV939 Chemical compound N=1C=2CCSCC=2C(O)=NC=1C1=CC=C(C(F)(F)F)C=C1 KLGQSVMIPOVQAX-UHFFFAOYSA-N 0.000 claims description 2
- 102100024672 Zinc finger protein 35 Human genes 0.000 claims description 2
- 239000002253 acid Substances 0.000 claims description 2
- 230000033289 adaptive immune response Effects 0.000 claims description 2
- 229950009557 adavosertib Drugs 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 238000011226 adjuvant chemotherapy Methods 0.000 claims description 2
- 238000011467 adoptive cell therapy Methods 0.000 claims description 2
- 150000003797 alkaloid derivatives Chemical class 0.000 claims description 2
- 229960005521 allovectin-7 Drugs 0.000 claims description 2
- 108010080146 androgen receptors Proteins 0.000 claims description 2
- 230000003302 anti-idiotype Effects 0.000 claims description 2
- RQNWIZPPADIBDY-UHFFFAOYSA-N arsenic atom Chemical class [As] RQNWIZPPADIBDY-UHFFFAOYSA-N 0.000 claims description 2
- 229960003852 atezolizumab Drugs 0.000 claims description 2
- 239000005441 aurora Substances 0.000 claims description 2
- 229940030547 autologous tumor cell vaccine Drugs 0.000 claims description 2
- 229960000190 bacillus calmette–guérin vaccine Drugs 0.000 claims description 2
- 229960002938 bexarotene Drugs 0.000 claims description 2
- 230000015572 biosynthetic process Effects 0.000 claims description 2
- 229960001561 bleomycin Drugs 0.000 claims description 2
- OYVAGSVQBOHSSS-UAPAGMARSA-O bleomycin A2 Chemical compound N([C@H](C(=O)N[C@H](C)[C@@H](O)[C@H](C)C(=O)N[C@@H]([C@H](O)C)C(=O)NCCC=1SC=C(N=1)C=1SC=C(N=1)C(=O)NCCC[S+](C)C)[C@@H](O[C@H]1[C@H]([C@@H](O)[C@H](O)[C@H](CO)O1)O[C@@H]1[C@H]([C@@H](OC(N)=O)[C@H](O)[C@@H](CO)O1)O)C=1N=CNC=1)C(=O)C1=NC([C@H](CC(N)=O)NC[C@H](N)C(N)=O)=NC(N)=C1C OYVAGSVQBOHSSS-UAPAGMARSA-O 0.000 claims description 2
- 210000004556 brain Anatomy 0.000 claims description 2
- 229950003628 buparlisib Drugs 0.000 claims description 2
- 229960001573 cabazitaxel Drugs 0.000 claims description 2
- BMQGVNUXMIRLCK-OAGWZNDDSA-N cabazitaxel Chemical compound O([C@H]1[C@@H]2[C@]3(OC(C)=O)CO[C@@H]3C[C@@H]([C@]2(C(=O)[C@H](OC)C2=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=3C=CC=CC=3)C[C@]1(O)C2(C)C)C)OC)C(=O)C1=CC=CC=C1 BMQGVNUXMIRLCK-OAGWZNDDSA-N 0.000 claims description 2
- 230000012820 cell cycle checkpoint Effects 0.000 claims description 2
- 230000024245 cell differentiation Effects 0.000 claims description 2
- 239000013592 cell lysate Substances 0.000 claims description 2
- 238000002659 cell therapy Methods 0.000 claims description 2
- QUWFSKKBMDKAHK-SBOJBMMISA-A chembl2103793 Chemical compound [Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(N=C(N)C=C2)=O)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(NC(=O)C(C)=C2)=O)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(N=C(N)C=C2)=O)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(NC(=O)C(C)=C2)=O)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(NC(=O)C(C)=C2)=O)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(NC(=O)C(C)=C2)=O)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(NC(=O)C(C)=C2)=O)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(NC(=O)C(C)=C2)=O)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(N=C(N)C=C2)=O)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(NC(=O)C(C)=C2)=O)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(NC(=O)C(C)=C2)=O)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(NC(=O)C(C)=C2)=O)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(NC(=O)C(C)=C2)=O)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(NC(=O)C(C)=C2)=O)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(N=C(N)C=C2)=O)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(NC(=O)C(C)=C2)=O)COP([O-])(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(NC(=O)C(C)=C2)=O)CO)[C@@H](O)C1 QUWFSKKBMDKAHK-SBOJBMMISA-A 0.000 claims description 2
- ZWVZORIKUNOTCS-OAQYLSRUSA-N chembl401930 Chemical compound C1([C@H](O)CNC2=C(C(NC=C2)=O)C=2NC=3C=C(C=C(C=3N=2)C)N2CCOCC2)=CC=CC(Cl)=C1 ZWVZORIKUNOTCS-OAQYLSRUSA-N 0.000 claims description 2
- 208000009060 clear cell adenocarcinoma Diseases 0.000 claims description 2
- 201000000292 clear cell sarcoma Diseases 0.000 claims description 2
- 229940001442 combination vaccine Drugs 0.000 claims description 2
- 239000013256 coordination polymer Substances 0.000 claims description 2
- 229960005061 crizotinib Drugs 0.000 claims description 2
- KTEIFNKAUNYNJU-GFCCVEGCSA-N crizotinib Chemical compound O([C@H](C)C=1C(=C(F)C=CC=1Cl)Cl)C(C(=NC=1)N)=CC=1C(=C1)C=NN1C1CCNCC1 KTEIFNKAUNYNJU-GFCCVEGCSA-N 0.000 claims description 2
- 229960004397 cyclophosphamide Drugs 0.000 claims description 2
- 229960001251 denosumab Drugs 0.000 claims description 2
- 230000001419 dependent effect Effects 0.000 claims description 2
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims description 2
- UWBXIFCTIZXXLS-UHFFFAOYSA-L disodium;2,3,4,5-tetrachloro-6-(2,4,5,7-tetraiodo-3-oxido-6-oxoxanthen-9-yl)benzoate Chemical compound [Na+].[Na+].[O-]C(=O)C1=C(Cl)C(Cl)=C(Cl)C(Cl)=C1C1=C2C=C(I)C(=O)C(I)=C2OC2=C(I)C([O-])=C(I)C=C21 UWBXIFCTIZXXLS-UHFFFAOYSA-L 0.000 claims description 2
- 229940056913 eftilagimod alfa Drugs 0.000 claims description 2
- BKJIXTWSNXCKJH-UHFFFAOYSA-N elesclomol Chemical compound C=1C=CC=CC=1C(=S)N(C)NC(=O)CC(=O)NN(C)C(=S)C1=CC=CC=C1 BKJIXTWSNXCKJH-UHFFFAOYSA-N 0.000 claims description 2
- 210000002308 embryonic cell Anatomy 0.000 claims description 2
- 201000011523 endocrine gland cancer Diseases 0.000 claims description 2
- 201000003908 endometrial adenocarcinoma Diseases 0.000 claims description 2
- 208000029382 endometrium adenocarcinoma Diseases 0.000 claims description 2
- 230000001973 epigenetic effect Effects 0.000 claims description 2
- PJMPHNIQZUBGLI-UHFFFAOYSA-N fentanyl Chemical compound C=1C=CC=CC=1N(C(=O)CC)C(CC1)CCN1CCC1=CC=CC=C1 PJMPHNIQZUBGLI-UHFFFAOYSA-N 0.000 claims description 2
- 229960002428 fentanyl Drugs 0.000 claims description 2
- 201000003444 follicular lymphoma Diseases 0.000 claims description 2
- 230000004927 fusion Effects 0.000 claims description 2
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims description 2
- 229960005277 gemcitabine Drugs 0.000 claims description 2
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims description 2
- 229950006304 gilteritinib Drugs 0.000 claims description 2
- GYQYAJJFPNQOOW-UHFFFAOYSA-N gilteritinib Chemical compound N1=C(NC2CCOCC2)C(CC)=NC(C(N)=O)=C1NC(C=C1OC)=CC=C1N(CC1)CCC1N1CCN(C)CC1 GYQYAJJFPNQOOW-UHFFFAOYSA-N 0.000 claims description 2
- 229950009672 glembatumumab vedotin Drugs 0.000 claims description 2
- 230000002518 glial effect Effects 0.000 claims description 2
- 230000002519 immonomodulatory effect Effects 0.000 claims description 2
- 230000028993 immune response Effects 0.000 claims description 2
- 230000036039 immunity Effects 0.000 claims description 2
- 238000009169 immunotherapy Methods 0.000 claims description 2
- MOFVSTNWEDAEEK-UHFFFAOYSA-M indocyanine green Chemical compound [Na+].[O-]S(=O)(=O)CCCCN1C2=CC=C3C=CC=CC3=C2C(C)(C)C1=CC=CC=CC=CC1=[N+](CCCCS([O-])(=O)=O)C2=CC=C(C=CC=C3)C3=C2C1(C)C MOFVSTNWEDAEEK-UHFFFAOYSA-M 0.000 claims description 2
- 229960004657 indocyanine green Drugs 0.000 claims description 2
- 102000006639 indoleamine 2,3-dioxygenase Human genes 0.000 claims description 2
- 108020004201 indoleamine 2,3-dioxygenase Proteins 0.000 claims description 2
- 229940090044 injection Drugs 0.000 claims description 2
- 238000002347 injection Methods 0.000 claims description 2
- 239000007924 injection Substances 0.000 claims description 2
- 230000000266 injurious effect Effects 0.000 claims description 2
- 229940079322 interferon Drugs 0.000 claims description 2
- 108700038251 interferon-alfa-1b Proteins 0.000 claims description 2
- 229960001388 interferon-beta Drugs 0.000 claims description 2
- 229960004768 irinotecan Drugs 0.000 claims description 2
- UWKQSNNFCGGAFS-XIFFEERXSA-N irinotecan Chemical compound C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 UWKQSNNFCGGAFS-XIFFEERXSA-N 0.000 claims description 2
- 229960004891 lapatinib Drugs 0.000 claims description 2
- BCFGMOOMADDAQU-UHFFFAOYSA-N lapatinib Chemical compound O1C(CNCCS(=O)(=O)C)=CC=C1C1=CC=C(N=CN=C2NC=3C=C(Cl)C(OCC=4C=C(F)C=CC=4)=CC=3)C2=C1 BCFGMOOMADDAQU-UHFFFAOYSA-N 0.000 claims description 2
- 239000000436 ligase inhibitor Substances 0.000 claims description 2
- 239000002502 liposome Substances 0.000 claims description 2
- 229940123729 mTOR kinase inhibitor Drugs 0.000 claims description 2
- 230000036244 malformation Effects 0.000 claims description 2
- 230000003211 malignant effect Effects 0.000 claims description 2
- 239000012528 membrane Substances 0.000 claims description 2
- OKKJLVBELUTLKV-UHFFFAOYSA-N methanol Natural products OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 2
- 238000002625 monoclonal antibody therapy Methods 0.000 claims description 2
- SGIWFELWJPNFDH-UHFFFAOYSA-N n-(2,2,2-trifluoroethyl)-n-{4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl}benzenesulfonamide Chemical compound C1=CC(C(O)(C(F)(F)F)C(F)(F)F)=CC=C1N(CC(F)(F)F)S(=O)(=O)C1=CC=CC=C1 SGIWFELWJPNFDH-UHFFFAOYSA-N 0.000 claims description 2
- HCUKSDBNBZMFKP-UHFFFAOYSA-N n-[(3,5-difluorophenyl)methyl]-2-(3-pyrrolidin-1-ylpropyl)pyrimidin-4-amine Chemical compound FC1=CC(F)=CC(CNC=2N=C(CCCN3CCCC3)N=CC=2)=C1 HCUKSDBNBZMFKP-UHFFFAOYSA-N 0.000 claims description 2
- VQQFFMMTRRTHKH-UHFFFAOYSA-N n-[2-[[2-[3-(dimethylamino)propyl]pyrimidin-4-yl]amino]ethyl]benzamide Chemical compound CN(C)CCCC1=NC=CC(NCCNC(=O)C=2C=CC=CC=2)=N1 VQQFFMMTRRTHKH-UHFFFAOYSA-N 0.000 claims description 2
- OBJNFLYHUXWUPF-IZZDOVSWSA-N n-[3-[[5-chloro-4-(1h-indol-3-yl)pyrimidin-2-yl]amino]phenyl]-4-[[(e)-4-(dimethylamino)but-2-enoyl]amino]benzamide Chemical compound C1=CC(NC(=O)/C=C/CN(C)C)=CC=C1C(=O)NC1=CC=CC(NC=2N=C(C(Cl)=CN=2)C=2C3=CC=CC=C3NC=2)=C1 OBJNFLYHUXWUPF-IZZDOVSWSA-N 0.000 claims description 2
- YAABRYJGVFZZBL-UHFFFAOYSA-N n-naphthalen-2-yl-2-(piperidin-1-ylmethoxy)pyrimidin-4-amine Chemical compound N=1C=CC(NC=2C=C3C=CC=CC3=CC=2)=NC=1OCN1CCCCC1 YAABRYJGVFZZBL-UHFFFAOYSA-N 0.000 claims description 2
- 229950004847 navitoclax Drugs 0.000 claims description 2
- JLYAXFNOILIKPP-KXQOOQHDSA-N navitoclax Chemical compound C([C@@H](NC1=CC=C(C=C1S(=O)(=O)C(F)(F)F)S(=O)(=O)NC(=O)C1=CC=C(C=C1)N1CCN(CC1)CC1=C(CCC(C1)(C)C)C=1C=CC(Cl)=CC=1)CSC=1C=CC=CC=1)CN1CCOCC1 JLYAXFNOILIKPP-KXQOOQHDSA-N 0.000 claims description 2
- 208000023833 nerve sheath neoplasm Diseases 0.000 claims description 2
- 230000001272 neurogenic effect Effects 0.000 claims description 2
- 229940080607 nexavar Drugs 0.000 claims description 2
- 108020004017 nuclear receptors Proteins 0.000 claims description 2
- UHGIMQLJWRAPLT-UHFFFAOYSA-N octadecyl dihydrogen phosphate Chemical compound CCCCCCCCCCCCCCCCCCOP(O)(O)=O UHGIMQLJWRAPLT-UHFFFAOYSA-N 0.000 claims description 2
- 230000002611 ovarian Effects 0.000 claims description 2
- 208000013371 ovarian adenocarcinoma Diseases 0.000 claims description 2
- 201000006588 ovary adenocarcinoma Diseases 0.000 claims description 2
- 101710135378 pH 6 antigen Proteins 0.000 claims description 2
- 201000008129 pancreatic ductal adenocarcinoma Diseases 0.000 claims description 2
- 230000009996 pancreatic endocrine effect Effects 0.000 claims description 2
- 208000003154 papilloma Diseases 0.000 claims description 2
- 229960005489 paracetamol Drugs 0.000 claims description 2
- 229940023041 peptide vaccine Drugs 0.000 claims description 2
- 230000010412 perfusion Effects 0.000 claims description 2
- 210000003819 peripheral blood mononuclear cell Anatomy 0.000 claims description 2
- JGWRKYUXBBNENE-UHFFFAOYSA-N pexidartinib Chemical compound C1=NC(C(F)(F)F)=CC=C1CNC(N=C1)=CC=C1CC1=CNC2=NC=C(Cl)C=C12 JGWRKYUXBBNENE-UHFFFAOYSA-N 0.000 claims description 2
- 229960005095 pioglitazone Drugs 0.000 claims description 2
- 229940068196 placebo Drugs 0.000 claims description 2
- 239000000902 placebo Substances 0.000 claims description 2
- 108010056274 polo-like kinase 1 Proteins 0.000 claims description 2
- 239000003207 proteasome inhibitor Substances 0.000 claims description 2
- 239000003528 protein farnesyltransferase inhibitor Substances 0.000 claims description 2
- 239000003909 protein kinase inhibitor Substances 0.000 claims description 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
- 238000001959 radiotherapy Methods 0.000 claims description 2
- 229940044601 receptor agonist Drugs 0.000 claims description 2
- 239000000018 receptor agonist Substances 0.000 claims description 2
- 229940044551 receptor antagonist Drugs 0.000 claims description 2
- 239000002464 receptor antagonist Substances 0.000 claims description 2
- 102000005962 receptors Human genes 0.000 claims description 2
- 108020003175 receptors Proteins 0.000 claims description 2
- 239000011435 rock Substances 0.000 claims description 2
- OHRURASPPZQGQM-GCCNXGTGSA-N romidepsin Chemical compound O1C(=O)[C@H](C(C)C)NC(=O)C(=C/C)/NC(=O)[C@H]2CSSCC\C=C\[C@@H]1CC(=O)N[C@H](C(C)C)C(=O)N2 OHRURASPPZQGQM-GCCNXGTGSA-N 0.000 claims description 2
- 230000001568 sexual effect Effects 0.000 claims description 2
- 229950006898 silmitasertib Drugs 0.000 claims description 2
- 201000010106 skin squamous cell carcinoma Diseases 0.000 claims description 2
- IVDHYUQIDRJSTI-UHFFFAOYSA-N sorafenib tosylate Chemical compound [H+].CC1=CC=C(S([O-])(=O)=O)C=C1.C1=NC(C(=O)NC)=CC(OC=2C=CC(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 IVDHYUQIDRJSTI-UHFFFAOYSA-N 0.000 claims description 2
- 229960000487 sorafenib tosylate Drugs 0.000 claims description 2
- 239000007921 spray Substances 0.000 claims description 2
- 210000004500 stellate cell Anatomy 0.000 claims description 2
- 125000001424 substituent group Chemical group 0.000 claims description 2
- 108060007951 sulfatase Proteins 0.000 claims description 2
- 238000003786 synthesis reaction Methods 0.000 claims description 2
- 229950007866 tanespimycin Drugs 0.000 claims description 2
- AYUNIORJHRXIBJ-TXHRRWQRSA-N tanespimycin Chemical compound N1C(=O)\C(C)=C\C=C/[C@H](OC)[C@@H](OC(N)=O)\C(C)=C\[C@H](C)[C@@H](O)[C@@H](OC)C[C@H](C)CC2=C(NCC=C)C(=O)C=C1C2=O AYUNIORJHRXIBJ-TXHRRWQRSA-N 0.000 claims description 2
- 230000001225 therapeutic effect Effects 0.000 claims description 2
- 125000000335 thiazolyl group Chemical group 0.000 claims description 2
- 229950009158 tipifarnib Drugs 0.000 claims description 2
- PLHJCIYEEKOWNM-HHHXNRCGSA-N tipifarnib Chemical compound CN1C=NC=C1[C@](N)(C=1C=C2C(C=3C=C(Cl)C=CC=3)=CC(=O)N(C)C2=CC=1)C1=CC=C(Cl)C=C1 PLHJCIYEEKOWNM-HHHXNRCGSA-N 0.000 claims description 2
- 229960001350 tofacitinib Drugs 0.000 claims description 2
- UJLAWZDWDVHWOW-YPMHNXCESA-N tofacitinib Chemical compound C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)C1=NC=NC2=C1C=CN2 UJLAWZDWDVHWOW-YPMHNXCESA-N 0.000 claims description 2
- 230000009261 transgenic effect Effects 0.000 claims description 2
- 210000004881 tumor cell Anatomy 0.000 claims description 2
- 239000002451 tumor necrosis factor inhibitor Substances 0.000 claims description 2
- 102000003298 tumor necrosis factor receptor Human genes 0.000 claims description 2
- 239000000225 tumor suppressor protein Substances 0.000 claims description 2
- 229950005972 urelumab Drugs 0.000 claims description 2
- 238000002255 vaccination Methods 0.000 claims description 2
- 239000002525 vasculotropin inhibitor Substances 0.000 claims description 2
- 229950004051 veledimex Drugs 0.000 claims description 2
- 235000019166 vitamin D Nutrition 0.000 claims description 2
- 239000011710 vitamin D Substances 0.000 claims description 2
- 150000003710 vitamin D derivatives Chemical class 0.000 claims description 2
- QYSXJUFSXHHAJI-YRZJJWOYSA-N vitamin D3 Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C\C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-YRZJJWOYSA-N 0.000 claims description 2
- 229940046008 vitamin d Drugs 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 10
- 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 claims 5
- AQHHHDLHHXJYJD-UHFFFAOYSA-N propranolol Chemical compound C1=CC=C2C(OCC(O)CNC(C)C)=CC=CC2=C1 AQHHHDLHHXJYJD-UHFFFAOYSA-N 0.000 claims 2
- 239000000835 fiber Substances 0.000 claims 1
- 229960003712 propranolol Drugs 0.000 claims 1
- DRYRBWIFRVMRPV-UHFFFAOYSA-N quinazolin-4-amine Chemical compound C1=CC=C2C(N)=NC=NC2=C1 DRYRBWIFRVMRPV-UHFFFAOYSA-N 0.000 claims 1
- 125000005415 substituted alkoxy group Chemical group 0.000 claims 1
- 150000001345 alkine derivatives Chemical class 0.000 description 17
- 238000011282 treatment Methods 0.000 description 13
- 230000002265 prevention Effects 0.000 description 10
- 0 CCC1(C)C(*)=NC(N(*)c2nc(N(*)*)c(*)c(*)n2)=CC=C1 Chemical compound CCC1(C)C(*)=NC(N(*)c2nc(N(*)*)c(*)c(*)n2)=CC=C1 0.000 description 5
- 125000000304 alkynyl group Chemical group 0.000 description 4
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 description 4
- 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 3
- 229960003603 decitabine Drugs 0.000 description 3
- 229950001969 encorafenib Drugs 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- PVCULFYROUOVGJ-UHFFFAOYSA-N 1-[2-chloroethyl(methylsulfonyl)amino]-3-methyl-1-methylsulfonylurea Chemical compound CNC(=O)N(S(C)(=O)=O)N(S(C)(=O)=O)CCCl PVCULFYROUOVGJ-UHFFFAOYSA-N 0.000 description 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 description 2
- FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 description 2
- 201000003793 Myelodysplastic syndrome Diseases 0.000 description 2
- OGQICQVSFDPSEI-UHFFFAOYSA-N Zorac Chemical compound N1=CC(C(=O)OCC)=CC=C1C#CC1=CC=C(SCCC2(C)C)C2=C1 OGQICQVSFDPSEI-UHFFFAOYSA-N 0.000 description 2
- FPIPGXGPPPQFEQ-OVSJKPMPSA-N all-trans-retinol Chemical compound OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-OVSJKPMPSA-N 0.000 description 2
- 229960000397 bevacizumab Drugs 0.000 description 2
- 125000002619 bicyclic group Chemical group 0.000 description 2
- 125000006580 bicyclic heterocycloalkyl group Chemical group 0.000 description 2
- 238000002648 combination therapy Methods 0.000 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 description 2
- 238000001727 in vivo Methods 0.000 description 2
- 229960000485 methotrexate Drugs 0.000 description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 2
- 125000006574 non-aromatic ring group Chemical group 0.000 description 2
- 229960000565 tazarotene Drugs 0.000 description 2
- 229960001727 tretinoin Drugs 0.000 description 2
- HJTAZXHBEBIQQX-UHFFFAOYSA-N 1,5-bis(chloromethyl)naphthalene Chemical compound C1=CC=C2C(CCl)=CC=CC2=C1CCl HJTAZXHBEBIQQX-UHFFFAOYSA-N 0.000 description 1
- FPIPGXGPPPQFEQ-UHFFFAOYSA-N 13-cis retinol Natural products OCC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-UHFFFAOYSA-N 0.000 description 1
- AANFHDFOMFRLLR-IBGZPJMESA-N 3-fluoro-4-[2-hydroxy-2-(5,5,8,8-tetramethyl-5,6,7,8,-tetrahydro-naphtalen-2-yl)-acetylamino]-benzoic acid Chemical compound O=C([C@@H](O)C=1C=C2C(C)(C)CCC(C2=CC=1)(C)C)NC1=CC=C(C(O)=O)C=C1F AANFHDFOMFRLLR-IBGZPJMESA-N 0.000 description 1
- HXBKPYIEQLLNBK-UHFFFAOYSA-N 4-(4-octylphenyl)benzoic acid Chemical compound C1=CC(CCCCCCCC)=CC=C1C1=CC=C(C(O)=O)C=C1 HXBKPYIEQLLNBK-UHFFFAOYSA-N 0.000 description 1
- AKJHMTWEGVYYSE-AIRMAKDCSA-N 4-HPR Chemical compound C=1C=C(O)C=CC=1NC(=O)/C=C(\C)/C=C/C=C(C)C=CC1=C(C)CCCC1(C)C AKJHMTWEGVYYSE-AIRMAKDCSA-N 0.000 description 1
- KFBPBWUZXBYJDG-UHFFFAOYSA-N 4-[(1,1,3,3-tetramethyl-2-oxoindene-5-carbonyl)amino]benzoic acid Chemical compound C=1C=C2C(C)(C)C(=O)C(C)(C)C2=CC=1C(=O)NC1=CC=C(C(O)=O)C=C1 KFBPBWUZXBYJDG-UHFFFAOYSA-N 0.000 description 1
- HSAOETBFVAWNRP-UHFFFAOYSA-N 4-[4-(2-butoxyethoxy)-5-methyl-1,3-thiazol-2-yl]-2-fluorobenzoic acid Chemical compound S1C(C)=C(OCCOCCCC)N=C1C1=CC=C(C(O)=O)C(F)=C1 HSAOETBFVAWNRP-UHFFFAOYSA-N 0.000 description 1
- VCQGNUWOMLYNNG-UHFFFAOYSA-N 4-[7-(1-adamantyl)-6-hydroxynaphthalen-2-yl]benzoic acid Chemical compound C1=CC(C(=O)O)=CC=C1C1=CC=C(C=C(O)C(=C2)C34CC5CC(CC(C5)C3)C4)C2=C1 VCQGNUWOMLYNNG-UHFFFAOYSA-N 0.000 description 1
- SZWKGOZKRMMLAJ-UHFFFAOYSA-N 4-{[(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)carbonyl]amino}benzoic acid Chemical compound C=1C=C2C(C)(C)CCC(C)(C)C2=CC=1C(=O)NC1=CC=C(C(O)=O)C=C1 SZWKGOZKRMMLAJ-UHFFFAOYSA-N 0.000 description 1
- URUSABQSUCBGGJ-UHFFFAOYSA-N 5-(5,5,8,8-tetramethyl-6,7-dihydroanthracen-2-yl)thiophene-3-carboxylic acid Chemical compound C=1C=C2C=C3C(C)(C)CCC(C)(C)C3=CC2=CC=1C1=CC(C(O)=O)=CS1 URUSABQSUCBGGJ-UHFFFAOYSA-N 0.000 description 1
- PMHNIDJCQQOZAE-UHFFFAOYSA-N 6-methoxy-7-(3-piperidin-1-ylpropoxy)-2-(4-propan-2-yl-1,4-diazepan-1-yl)-n-(1-propan-2-ylpiperidin-4-yl)quinazolin-4-amine Chemical compound N1=C(N2CCN(CCC2)C(C)C)N=C2C=C(OCCCN3CCCCC3)C(OC)=CC2=C1NC1CCN(C(C)C)CC1 PMHNIDJCQQOZAE-UHFFFAOYSA-N 0.000 description 1
- RHXHGRAEPCAFML-UHFFFAOYSA-N 7-cyclopentyl-n,n-dimethyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N1CCNCC1 RHXHGRAEPCAFML-UHFFFAOYSA-N 0.000 description 1
- SHGAZHPCJJPHSC-ZVCIMWCZSA-N 9-cis-retinoic acid Chemical compound OC(=O)/C=C(\C)/C=C/C=C(/C)\C=C\C1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-ZVCIMWCZSA-N 0.000 description 1
- 229940126638 Akt inhibitor Drugs 0.000 description 1
- YCADIXLLWMXYKW-CMDGGOBGSA-N BMS-493 Chemical compound C12=CC(\C=C\C=3C=CC(=CC=3)C(O)=O)=CC=C2C(C)(C)CC=C1C#CC1=CC=CC=C1 YCADIXLLWMXYKW-CMDGGOBGSA-N 0.000 description 1
- LXFOLMYKSYSZQS-LURJZOHASA-N CC(C)N(C[C@H]1O[C@H]([C@H](O)[C@@H]1O)n1cnc2c(N)ncnc12)[C@@H]1C[C@H](CCc2nc3cc(ccc3[nH]2)C(C)(C)C)C1 Chemical group CC(C)N(C[C@H]1O[C@H]([C@H](O)[C@@H]1O)n1cnc2c(N)ncnc12)[C@@H]1C[C@H](CCc2nc3cc(ccc3[nH]2)C(C)(C)C)C1 LXFOLMYKSYSZQS-LURJZOHASA-N 0.000 description 1
- PTOAARAWEBMLNO-KVQBGUIXSA-N Cladribine Chemical compound C1=NC=2C(N)=NC(Cl)=NC=2N1[C@H]1C[C@H](O)[C@@H](CO)O1 PTOAARAWEBMLNO-KVQBGUIXSA-N 0.000 description 1
- 101100216108 Homo sapiens PRMT1 gene Proteins 0.000 description 1
- XDXDZDZNSLXDNA-TZNDIEGXSA-N Idarubicin Chemical compound C1[C@H](N)[C@H](O)[C@H](C)O[C@H]1O[C@@H]1C2=C(O)C(C(=O)C3=CC=CC=C3C3=O)=C3C(O)=C2C[C@@](O)(C(C)=O)C1 XDXDZDZNSLXDNA-TZNDIEGXSA-N 0.000 description 1
- XDXDZDZNSLXDNA-UHFFFAOYSA-N Idarubicin Natural products C1C(N)C(O)C(C)OC1OC1C2=C(O)C(C(=O)C3=CC=CC=C3C3=O)=C3C(O)=C2CC(O)(C(C)=O)C1 XDXDZDZNSLXDNA-UHFFFAOYSA-N 0.000 description 1
- SHGAZHPCJJPHSC-NUEINMDLSA-N Isotretinoin Chemical compound OC(=O)C=C(C)/C=C/C=C(C)C=CC1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-NUEINMDLSA-N 0.000 description 1
- 102100022985 Protein arginine N-methyltransferase 1 Human genes 0.000 description 1
- 101100178218 Schizosaccharomyces pombe (strain 972 / ATCC 24843) hmt2 gene Proteins 0.000 description 1
- 229940123237 Taxane Drugs 0.000 description 1
- 229940122803 Vinca alkaloid Drugs 0.000 description 1
- 229960005339 acitretin Drugs 0.000 description 1
- LZCDAPDGXCYOEH-UHFFFAOYSA-N adapalene Chemical compound C1=C(C(O)=O)C=CC2=CC(C3=CC=C(C(=C3)C34CC5CC(CC(C5)C3)C4)OC)=CC=C21 LZCDAPDGXCYOEH-UHFFFAOYSA-N 0.000 description 1
- 229960002916 adapalene Drugs 0.000 description 1
- 108700025316 aldesleukin Proteins 0.000 description 1
- 229960005310 aldesleukin Drugs 0.000 description 1
- 229960001445 alitretinoin Drugs 0.000 description 1
- 125000003342 alkenyl group Chemical group 0.000 description 1
- IHUNBGSDBOWDMA-AQFIFDHZSA-N all-trans-acitretin Chemical compound COC1=CC(C)=C(\C=C\C(\C)=C\C=C\C(\C)=C\C(O)=O)C(C)=C1C IHUNBGSDBOWDMA-AQFIFDHZSA-N 0.000 description 1
- 230000000340 anti-metabolite Effects 0.000 description 1
- 229940100197 antimetabolite Drugs 0.000 description 1
- 239000002256 antimetabolite Substances 0.000 description 1
- FOIVPCKZDPCJJY-JQIJEIRASA-N arotinoid acid Chemical compound C=1C=C(C(CCC2(C)C)(C)C)C2=CC=1C(/C)=C/C1=CC=C(C(O)=O)C=C1 FOIVPCKZDPCJJY-JQIJEIRASA-N 0.000 description 1
- GOLCXWYRSKYTSP-UHFFFAOYSA-N arsenic trioxide Inorganic materials O1[As]2O[As]1O2 GOLCXWYRSKYTSP-UHFFFAOYSA-N 0.000 description 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 1
- 239000011203 carbon fibre reinforced carbon Substances 0.000 description 1
- 229960002436 cladribine Drugs 0.000 description 1
- WDDPHFBMKLOVOX-AYQXTPAHSA-N clofarabine Chemical compound C1=NC=2C(N)=NC(Cl)=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@@H]1F WDDPHFBMKLOVOX-AYQXTPAHSA-N 0.000 description 1
- 229960000928 clofarabine Drugs 0.000 description 1
- 206010013023 diphtheria Diseases 0.000 description 1
- 229950003662 fenretinide Drugs 0.000 description 1
- 229960000390 fludarabine Drugs 0.000 description 1
- GIUYCYHIANZCFB-FJFJXFQQSA-N fludarabine phosphate Chemical compound C1=NC=2C(N)=NC(F)=NC=2N1[C@@H]1O[C@H](COP(O)(O)=O)[C@@H](O)[C@@H]1O GIUYCYHIANZCFB-FJFJXFQQSA-N 0.000 description 1
- 229960004783 fotemustine Drugs 0.000 description 1
- YAKWPXVTIGTRJH-UHFFFAOYSA-N fotemustine Chemical compound CCOP(=O)(OCC)C(C)NC(=O)N(CCCl)N=O YAKWPXVTIGTRJH-UHFFFAOYSA-N 0.000 description 1
- XXSMGPRMXLTPCZ-UHFFFAOYSA-N hydroxychloroquine Chemical compound ClC1=CC=C2C(NC(C)CCCN(CCO)CC)=CC=NC2=C1 XXSMGPRMXLTPCZ-UHFFFAOYSA-N 0.000 description 1
- 229960004171 hydroxychloroquine Drugs 0.000 description 1
- 229960000908 idarubicin Drugs 0.000 description 1
- 239000002955 immunomodulating agent Substances 0.000 description 1
- 229940121354 immunomodulator Drugs 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000011065 in-situ storage Methods 0.000 description 1
- 229940065638 intron a Drugs 0.000 description 1
- 229960005280 isotretinoin Drugs 0.000 description 1
- SGDBTWWWUNNDEQ-LBPRGKRZSA-N melphalan Chemical compound OC(=O)[C@@H](N)CC1=CC=C(N(CCCl)CCCl)C=C1 SGDBTWWWUNNDEQ-LBPRGKRZSA-N 0.000 description 1
- 229960001924 melphalan Drugs 0.000 description 1
- GLVAUDGFNGKCSF-UHFFFAOYSA-N mercaptopurine Chemical compound S=C1NC=NC2=C1NC=N2 GLVAUDGFNGKCSF-UHFFFAOYSA-N 0.000 description 1
- 229960001428 mercaptopurine Drugs 0.000 description 1
- KKZJGLLVHKMTCM-UHFFFAOYSA-N mitoxantrone Chemical compound O=C1C2=C(O)C=CC(O)=C2C(=O)C2=C1C(NCCNCCO)=CC=C2NCCNCCO KKZJGLLVHKMTCM-UHFFFAOYSA-N 0.000 description 1
- 229960001156 mitoxantrone Drugs 0.000 description 1
- 229960001420 nimustine Drugs 0.000 description 1
- 229950006101 pinometostat Drugs 0.000 description 1
- 229950001626 quizartinib Drugs 0.000 description 1
- CVWXJKQAOSCOAB-UHFFFAOYSA-N quizartinib Chemical compound O1C(C(C)(C)C)=CC(NC(=O)NC=2C=CC(=CC=2)C=2N=C3N(C4=CC=C(OCCN5CCOCC5)C=C4S3)C=2)=N1 CVWXJKQAOSCOAB-UHFFFAOYSA-N 0.000 description 1
- 229960003471 retinol Drugs 0.000 description 1
- 235000020944 retinol Nutrition 0.000 description 1
- 239000011607 retinol Substances 0.000 description 1
- 229950003687 ribociclib Drugs 0.000 description 1
- 229960004641 rituximab Drugs 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 229950010130 tamibarotene Drugs 0.000 description 1
- MUTNCGKQJGXKEM-UHFFFAOYSA-N tamibarotene Chemical compound C=1C=C2C(C)(C)CCC(C)(C)C2=CC=1NC(=O)C1=CC=C(C(O)=O)C=C1 MUTNCGKQJGXKEM-UHFFFAOYSA-N 0.000 description 1
- DKPFODGZWDEEBT-QFIAKTPHSA-N taxane Chemical class C([C@]1(C)CCC[C@@H](C)[C@H]1C1)C[C@H]2[C@H](C)CC[C@@H]1C2(C)C DKPFODGZWDEEBT-QFIAKTPHSA-N 0.000 description 1
- 229960000303 topotecan Drugs 0.000 description 1
- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 description 1
- 229960004066 trametinib Drugs 0.000 description 1
- LIRYPHYGHXZJBZ-UHFFFAOYSA-N trametinib Chemical group CC(=O)NC1=CC=CC(N2C(N(C3CC3)C(=O)C3=C(NC=4C(=CC(I)=CC=4)F)N(C)C(=O)C(C)=C32)=O)=C1 LIRYPHYGHXZJBZ-UHFFFAOYSA-N 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022184887A JP2023009301A (ja) | 2017-04-21 | 2022-11-18 | Ehmt2阻害剤との併用療法 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762488679P | 2017-04-21 | 2017-04-21 | |
| US62/488,679 | 2017-04-21 | ||
| US201762574147P | 2017-10-18 | 2017-10-18 | |
| US62/574,147 | 2017-10-18 | ||
| PCT/US2018/028609 WO2018195450A1 (en) | 2017-04-21 | 2018-04-20 | Combination therapies with ehmt2 inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022184887A Division JP2023009301A (ja) | 2017-04-21 | 2022-11-18 | Ehmt2阻害剤との併用療法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020517618A JP2020517618A (ja) | 2020-06-18 |
| JP2020517618A5 true JP2020517618A5 (enExample) | 2021-05-27 |
Family
ID=63856173
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019556647A Withdrawn JP2020517618A (ja) | 2017-04-21 | 2018-04-20 | Ehmt2阻害剤との併用療法 |
| JP2022184887A Pending JP2023009301A (ja) | 2017-04-21 | 2022-11-18 | Ehmt2阻害剤との併用療法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022184887A Pending JP2023009301A (ja) | 2017-04-21 | 2022-11-18 | Ehmt2阻害剤との併用療法 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US11672800B2 (enExample) |
| EP (1) | EP3612181A4 (enExample) |
| JP (2) | JP2020517618A (enExample) |
| CN (2) | CN118021814A (enExample) |
| AU (1) | AU2018254577B2 (enExample) |
| CA (1) | CA3060416A1 (enExample) |
| WO (1) | WO2018195450A1 (enExample) |
Families Citing this family (90)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10729669B2 (en) | 2015-07-28 | 2020-08-04 | University Of Iowa Research Foundation | Compositions and methods for treating cancer |
| US10980797B2 (en) | 2016-03-01 | 2021-04-20 | Corcept Therapeutics Incorporated | Use of glucocorticoid receptor modulators to potentiate checkpoint inhibitors |
| CN110099898B (zh) | 2016-10-24 | 2023-07-25 | 优曼尼蒂治疗公司 | 化合物及其用途 |
| WO2018129403A1 (en) | 2017-01-06 | 2018-07-12 | Yumanity Therapeutics | Methods for the treatment of neurological disorders |
| US11452727B2 (en) * | 2017-09-05 | 2022-09-27 | Epizyme, Inc. | Combination therapy for treating cancer |
| EP3697419A4 (en) * | 2017-10-17 | 2021-08-18 | Epizyme, Inc. | AMINE SUBSTITUTION HETEROCYCLIC COMPOUNDS USED AS AND DERIVATIVES OF EHMT2 |
| CN111315371A (zh) * | 2017-10-18 | 2020-06-19 | 埃皮兹姆公司 | 使用ehmt2抑制剂治疗或预防血液障碍的方法 |
| EP3697420A4 (en) * | 2017-10-18 | 2021-11-24 | Epizyme, Inc. | METHODS OF USING EHMT2 INHIBITORS IN IMMUNOTHERAPIES |
| CA3083000A1 (en) | 2017-10-24 | 2019-05-02 | Yumanity Therapeutics, Inc. | Compounds and uses thereof |
| KR102867888B1 (ko) | 2018-01-31 | 2025-10-13 | 데시페라 파마슈티칼스, 엘엘씨 | 비만 세포증의 치료를 위한 병용 요법 |
| SG11202007198WA (en) | 2018-01-31 | 2020-08-28 | Deciphera Pharmaceuticals Llc | Combination therapy for the treatment of gastrointestinal stromal tumors |
| CN112105602A (zh) * | 2018-03-01 | 2020-12-18 | 反应生物公司 | 基于喹啉和异喹啉的hdac抑制剂及其使用方法 |
| CA3094527A1 (en) | 2018-03-23 | 2019-09-26 | Yumanity Therapeutics, Inc. | Compounds and uses thereof |
| CN117281803A (zh) | 2018-07-31 | 2023-12-26 | 罗索肿瘤学公司 | 喷雾干燥的分散体和制剂 |
| WO2020036852A1 (en) | 2018-08-13 | 2020-02-20 | Beijing Percans Oncology Co. Ltd. | Biomarkers for cancer therapy |
| US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
| US11476430B2 (en) * | 2018-10-15 | 2022-10-18 | Universal Display Corporation | Organic electroluminescent materials and devices |
| US12415816B2 (en) | 2018-11-07 | 2025-09-16 | Dana-Farber Cancer Institute, Inc. | Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof |
| US12509455B2 (en) | 2018-11-07 | 2025-12-30 | Dana-Farber Cancer Institute, Inc. | Imidazopyridine derivatives and aza-imidazopyridine derivatives as Janus kinase 2 inhibitors and uses thereof |
| KR20220007845A (ko) | 2019-01-24 | 2022-01-19 | 유마니티 테라퓨틱스, 인크. | 화합물 및 이의 용도 |
| US11384083B2 (en) | 2019-02-15 | 2022-07-12 | Incyte Corporation | Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors |
| US11472791B2 (en) | 2019-03-05 | 2022-10-18 | Incyte Corporation | Pyrazolyl pyrimidinylamine compounds as CDK2 inhibitors |
| WO2020185812A1 (en) | 2019-03-11 | 2020-09-17 | Teva Pharmaceuticals International Gmbh | Solid state forms of ripretinib |
| MX2021011488A (es) * | 2019-03-22 | 2021-11-17 | Yumanity Therapeutics Inc | Compuestos y usos de estos. |
| US11919904B2 (en) | 2019-03-29 | 2024-03-05 | Incyte Corporation | Sulfonylamide compounds as CDK2 inhibitors |
| WO2020216669A1 (de) | 2019-04-23 | 2020-10-29 | Bayer Aktiengesellschaft | Phenylsubstituierte imidazopyridinamide und ihre verwendung |
| WO2020223469A1 (en) | 2019-05-01 | 2020-11-05 | Incyte Corporation | N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer |
| WO2020223558A1 (en) | 2019-05-01 | 2020-11-05 | Incyte Corporation | Tricyclic amine compounds as cdk2 inhibitors |
| FI3985000T3 (fi) * | 2019-06-28 | 2024-12-17 | Chengdu Zenitar Biomedical Tech Co Ltd | 2,4-disubstituoitu pyrimidiinijohdannainen, sen valmistusmenetelmä sekä sen käyttöjä |
| WO2021007499A1 (en) * | 2019-07-11 | 2021-01-14 | Emory University | Combination therapies for managing cancer |
| WO2021007512A1 (en) * | 2019-07-11 | 2021-01-14 | Emory University | Platinum-based chemotherapy, mast binding agents, glucocorticoid receptor (gr) binding agents, and/or hsp90 binding agents for uses in treating cancer |
| MX2022001863A (es) | 2019-08-12 | 2022-05-30 | Deciphera Pharmaceuticals Llc | Metodos para tratar los tumores del estroma gastrointestinal. |
| TWI878335B (zh) | 2019-08-12 | 2025-04-01 | 美商迪賽孚爾製藥有限公司 | 治療胃腸道基質瘤方法 |
| CR20220066A (es) | 2019-08-14 | 2022-11-28 | Incyte Corp | Compuestos de imidazolil pirimidinilamina como inhibidores de cdk2 |
| CN110623942B (zh) * | 2019-09-30 | 2020-09-22 | 武汉大学 | 一种全反式维甲酸纳米药物制剂、其制备方法及应用 |
| WO2021064142A1 (en) | 2019-10-02 | 2021-04-08 | Tolremo Therapeutics Ag | Heterocyclic derivatives, pharmaceutical compositions and their use in the treatment or amelioration of cancer |
| CN119930610A (zh) | 2019-10-11 | 2025-05-06 | 因赛特公司 | 作为cdk2抑制剂的双环胺 |
| PH12022551091A1 (en) * | 2019-11-05 | 2024-06-24 | Abbvie Deutschland | Dosing regimens for use in treating myelofibrosis and mpn-related disorders with navitoclax |
| EA202192047A1 (ru) | 2019-11-13 | 2021-12-08 | Юманити Терапьютикс, Инк. | Соединения и их применение |
| US12064507B2 (en) | 2019-11-19 | 2024-08-20 | Provectus Pharmatech, Inc. | Composition and method for oral treatment of leukemia |
| WO2021102674A1 (zh) * | 2019-11-26 | 2021-06-03 | 深圳先进技术研究院 | 靶向AMPK的抑制剂/siRNA与蛋白酶体抑制剂组合在抗肿瘤中的应用 |
| DK4069691T3 (da) | 2019-12-06 | 2024-10-28 | Vertex Pharma | Substituerede tetrahydrofuraner som modulatorer af natriumkanaler |
| KR20250057151A (ko) | 2019-12-30 | 2025-04-28 | 데시페라 파마슈티칼스, 엘엘씨 | 1-(4-브로모-5-(1-에틸-7-(메틸아미노)-2-옥소-1,2-디히드로-1,6-나프티리딘-3-일)-2-플루오로페닐)-3-페닐우레아의조성물 |
| IL293866A (en) | 2019-12-30 | 2022-08-01 | Deciphera Pharmaceuticals Llc | Compositions of amorphous kinase inhibitors and methods of using them |
| JP2023516885A (ja) * | 2020-01-29 | 2023-04-21 | コーセプト セラピューティクス, インコーポレイテッド | 選択的グルココルチコイド受容体モジュレーター(sgrm)及び抗体チェックポイント阻害剤による副腎皮質がん腫の処置 |
| US20230149295A1 (en) * | 2020-03-09 | 2023-05-18 | University Of Houston System | Inflammatory bowel disease stem cells, agents which target ibd stem cells, and uses related thereto |
| CN113372364B (zh) * | 2020-03-10 | 2024-05-31 | 明慧医药(上海)有限公司 | 一类jak激酶抑制剂及其制备和应用 |
| PE20230609A1 (es) | 2020-05-04 | 2023-04-13 | Amgen Inc | Compuestos heterociclicos como agonistas del receptor de activacion expresado en las celulas mieloides 2 y metodos de uso |
| TW202208355A (zh) | 2020-05-04 | 2022-03-01 | 美商安進公司 | 作為骨髓細胞觸發受體2促效劑之雜環化合物及使用方法 |
| BR112022022409A2 (pt) | 2020-05-06 | 2023-02-07 | Ajax Therapeutics Inc | 6-heteroarilóxi benzimidazóis e azabenzimidazóis como inibidores de jak2 |
| JP2023527116A (ja) * | 2020-05-28 | 2023-06-27 | エピザイム インコーポレイテッド | がんを治療するためのezh2阻害剤の使用 |
| JP7619575B2 (ja) * | 2020-06-11 | 2025-01-22 | 養生堂有限公司 | Hbvウイルスに対する治療におけるパロバロテンの使用 |
| CN115701996B (zh) * | 2020-06-25 | 2024-12-24 | 托雷莫治疗股份公司 | 用于治疗EGFR突变型NSCLC的CBP/p300溴结构域抑制剂和EGFR抑制剂的组合 |
| CA3184076A1 (en) | 2020-06-25 | 2021-12-30 | Stefanie Fluckiger-Mangual | Combination of a cbp/p300 bromodomain inhibitor and a kras inhibitor for the treatment of cancer |
| IL299732A (en) * | 2020-07-10 | 2023-03-01 | Blossomhill Therapeutics Inc | Macrocycles and their use |
| US11529335B2 (en) * | 2020-07-31 | 2022-12-20 | University Of Iowa Research Foundation | Compositions and methods for treating cancer |
| AR123185A1 (es) | 2020-08-10 | 2022-11-09 | Novartis Ag | Compuestos y composiciones para inhibir ezh2 |
| KR102695540B1 (ko) * | 2020-09-21 | 2024-08-14 | 재단법인 아산사회복지재단 | 퀴나졸린-2,4-다이아민 유도체 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물 |
| CN112274517A (zh) * | 2020-10-30 | 2021-01-29 | 江苏大学 | 一种治疗套细胞淋巴瘤的药物组合物 |
| CN116761607A (zh) * | 2020-12-11 | 2023-09-15 | 阿尔维纳斯运营股份有限公司 | 治疗前列腺癌的方法 |
| US12043632B2 (en) | 2020-12-23 | 2024-07-23 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors |
| KR20230159421A (ko) | 2021-02-19 | 2023-11-21 | 수도 바이오사이언시즈 리미티드 | Tyk2 억제제 및 이의 용도 |
| TWI823255B (zh) * | 2021-02-19 | 2023-11-21 | 大陸商微境生物醫藥科技(上海)有限公司 | 作為Wee-1抑制劑的稠環化合物 |
| WO2022175747A1 (en) | 2021-02-19 | 2022-08-25 | Sudo Biosciences Limited | Tyk2 inhibitors and uses thereof |
| KR20230171854A (ko) * | 2021-04-16 | 2023-12-21 | 프로벡투스 파마테크 인코포레이티드 | 백혈병의 경구 치료를 위한 조성물 및 방법 |
| CN113288871B (zh) * | 2021-05-28 | 2022-09-16 | 华中科技大学 | 用于调控表观遗传与免疫检查点的药物组合物脂质体制剂 |
| US11827627B2 (en) | 2021-06-04 | 2023-11-28 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamides as modulators of sodium channels |
| US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
| CN113425851B (zh) * | 2021-07-09 | 2021-12-17 | 南京市儿童医院 | 修饰bix-01294的金纳米星制备方法及其应用 |
| CN113735859A (zh) * | 2021-08-12 | 2021-12-03 | 安徽医科大学 | 一种激酶抑制剂 |
| EP4134077A1 (en) * | 2021-08-13 | 2023-02-15 | ScandiEdge Therapeutics AB | Small molecule treatment of fatty liver disease and hcc |
| US20230062911A1 (en) * | 2021-09-02 | 2023-03-02 | Rutgers, The State University Of New Jersey | Compositions and methods for treating, preventing, and/or ameliorating chemotherapy-induced premature ovarian failure (pof) |
| WO2023064586A1 (en) * | 2021-10-15 | 2023-04-20 | Tango Therapeutics, Inc. | Novel modulators of ehmt1 and ehmt2 and therapeutic use thereof |
| TW202334089A (zh) | 2021-11-02 | 2023-09-01 | 美商夫雷爾醫療公司 | Pparg反向激動劑及其用途 |
| US12162881B2 (en) | 2021-11-09 | 2024-12-10 | Ajax Therapeutics, Inc. | Forms and compositions of inhibitors of JAK2 |
| CA3234638A1 (en) | 2021-11-09 | 2023-05-19 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| WO2023092394A1 (en) * | 2021-11-25 | 2023-06-01 | Guo Dagang | Methods and compositions for treating ewing family of tumors |
| US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| WO2023107705A1 (en) | 2021-12-10 | 2023-06-15 | Incyte Corporation | Bicyclic amines as cdk12 inhibitors |
| JP2025502748A (ja) | 2021-12-30 | 2025-01-28 | バイオメア フュージョン,インコーポレイテッド | Flt3の阻害剤としてのピラジン化合物 |
| MX2024008868A (es) | 2022-01-18 | 2024-09-23 | Maze Therapeutics Inc | Inhibidores de la apolipoproteína l1 (apol1) y métodos de uso. |
| CN115137731B (zh) * | 2022-05-19 | 2023-11-21 | 上海交通大学医学院附属新华医院 | Flt3抑制剂及其药学上可接受的盐在制备治疗皮肤t细胞淋巴瘤药物中的应用 |
| CN115300493A (zh) * | 2022-07-12 | 2022-11-08 | 厦门大学 | 核受体RXRα配体的应用及抗肿瘤药物 |
| CN116675653B (zh) * | 2022-07-22 | 2024-10-01 | 中国药科大学 | 氨基烷基取代的1,2,4-噻二唑烷-3,5-二酮化合物及其制备方法和应用 |
| US11779572B1 (en) | 2022-09-02 | 2023-10-10 | Deciphera Pharmaceuticals, Llc | Methods of treating gastrointestinal stromal tumors |
| CN117800894A (zh) * | 2022-09-30 | 2024-04-02 | 苏州阿尔脉生物科技有限公司 | 饱和环类衍生物、包含其的药物组合物及其医药用途 |
| CN115487185A (zh) * | 2022-10-18 | 2022-12-20 | 四川大学华西医院 | G007-lk在治疗小细胞肺癌中的应用 |
| TW202517642A (zh) * | 2023-07-11 | 2025-05-01 | 美商梅斯治療股份有限公司 | Apol1抑制劑及其使用方法 |
| WO2025043183A1 (en) * | 2023-08-23 | 2025-02-27 | Eigen Therapeutics Inc. | Methods and compositions for treating hematological cancers |
| KR20250088371A (ko) * | 2023-12-08 | 2025-06-17 | 인제대학교 산학협력단 | Ezh2 저해제 및 jak3 억제제를 포함하는 암의 예방 또는 치료용 약학적 조성물 |
Family Cites Families (118)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2443305A (en) | 1948-06-15 | Pyrimidine derivatives | ||
| US4522811A (en) | 1982-07-08 | 1985-06-11 | Syntex (U.S.A.) Inc. | Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides |
| SE8604566D0 (sv) | 1986-10-27 | 1986-10-27 | Haessle Ab | Novel compunds |
| GB8820231D0 (en) | 1988-08-25 | 1988-09-28 | Fujisawa Pharmaceutical Co | New benzazole compounds processes for preparation thereof & pharmaceutical composition comprising same |
| US5247083A (en) | 1992-07-10 | 1993-09-21 | Syntex (U.S.A.) Inc. | Direct esterification of mycophenolic acid |
| EP0585500A1 (en) | 1992-09-04 | 1994-03-09 | Merrell Dow Pharmaceuticals Inc. | Diaryl piperazineacetamides as antimuscarinic agents |
| GB9523675D0 (en) | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| US5763263A (en) | 1995-11-27 | 1998-06-09 | Dehlinger; Peter J. | Method and apparatus for producing position addressable combinatorial libraries |
| US6025379A (en) | 1996-03-11 | 2000-02-15 | Eli Lilly And Company | Methods of treating or preventing interstitial cystitis |
| ES2361146T3 (es) | 1998-03-27 | 2011-06-14 | Janssen Pharmaceutica Nv | Derivados de la piramidina inhibitatoria de vih. |
| EP1126843A4 (en) | 1998-10-29 | 2005-06-15 | Bristol Myers Squibb Co | AMINO-CELL DERIVATIVE COMPOUNDS INHIBITORS OF ENZYME IMPDH |
| US6596747B2 (en) | 1998-10-29 | 2003-07-22 | Bristol-Myers Squibb Company | Compounds derived from an amine nucleus and pharmaceutical compositions comprising same |
| US6355648B1 (en) | 1999-05-04 | 2002-03-12 | American Home Products Corporation | Thio-oxindole derivatives |
| US6391907B1 (en) | 1999-05-04 | 2002-05-21 | American Home Products Corporation | Indoline derivatives |
| US20020065270A1 (en) | 1999-12-28 | 2002-05-30 | Moriarty Kevin Joseph | N-heterocyclic inhibitors of TNF-alpha expression |
| US6906067B2 (en) | 1999-12-28 | 2005-06-14 | Bristol-Myers Squibb Company | N-heterocyclic inhibitors of TNF-α expression |
| EP1255738B1 (en) | 2000-01-25 | 2012-03-07 | Neurocrine Biosciences, Inc. | Gonadotropin-releasing hormone receptor antagonists and methods relating thereto |
| TW593278B (en) | 2001-01-23 | 2004-06-21 | Wyeth Corp | 1-aryl-or 1-alkylsulfonylbenzazole derivatives as 5-hydroxytryptamine-6 ligands |
| ES2292830T3 (es) | 2001-02-21 | 2008-03-16 | Astrazeneca Ab | Compuestos heteropoliciclicos y su uso como antagonistas del receptor metabotropico de glutamato. |
| WO2003040141A1 (en) | 2001-09-28 | 2003-05-15 | Bayer Pharmaceuticals Corporation | Oxazolyl-phenyl-2,4-diamino-pyrimidine compounds and methods for treating hyperproliferative disorders |
| EP1453516A2 (de) | 2001-10-17 | 2004-09-08 | Boehringer Ingelheim Pharma GmbH & Co.KG | 5-substituierte 4-amino-2-phenylamino-pyrimdinderivate und ihre verwendung als beta-amyloid modulatoren |
| FR2833948B1 (fr) | 2001-12-21 | 2004-02-06 | Sod Conseils Rech Applic | Nouveaux derives de benzimidazole et leur utilisation en tant que medicament |
| CA2473510A1 (en) | 2002-01-23 | 2003-07-31 | Bayer Pharmaceuticals Corporation | Pyrimidine derivatives as rho-kinase inhibitors |
| AR039540A1 (es) | 2002-05-13 | 2005-02-23 | Tibotec Pharm Ltd | Compuestos microbicidas con contenido de pirimidina o triazina |
| WO2004000820A2 (en) | 2002-06-21 | 2003-12-31 | Cellular Genomics, Inc. | Certain aromatic monocycles as kinase modulators |
| JP2006514989A (ja) | 2002-07-29 | 2006-05-18 | ライジェル ファーマシューティカルズ | 2,4−ピリミジンジアミン化合物による自己免疫疾患の治療および予防方法 |
| US7419984B2 (en) | 2002-10-17 | 2008-09-02 | Cell Therapeutics, Inc. | Pyrimidines and uses thereof |
| US20050014753A1 (en) | 2003-04-04 | 2005-01-20 | Irm Llc | Novel compounds and compositions as protein kinase inhibitors |
| US20050113398A1 (en) | 2003-08-07 | 2005-05-26 | Ankush Argade | 2,4-pyrimidinediamine compounds and uses as anti-proliferative agents |
| US20070105839A1 (en) | 2003-09-18 | 2007-05-10 | Patricia Imbach | 2, 4-Di (phenylamino) pyrimidines useful in the treatment of proliferative disorders |
| MXPA06004236A (es) | 2003-10-16 | 2006-06-28 | Chiron Corp | Benzazoles sustituidos y su uso como inhibidores de raf-cinasa. |
| EP1753750A1 (en) | 2004-05-20 | 2007-02-21 | Sugen, Inc. | Thiophene heteroaryl amines |
| GB0512324D0 (en) | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
| US20060058525A1 (en) | 2004-09-01 | 2006-03-16 | Rajinder Singh | Synthesis of 2,4-pyrimidinediamine compounds |
| US20070032493A1 (en) | 2005-05-26 | 2007-02-08 | Synta Pharmaceuticals Corp. | Method for treating B cell regulated autoimmune disorders |
| EP1746096A1 (en) | 2005-07-15 | 2007-01-24 | 4Sc Ag | 2-Arylbenzothiazole analogues and uses thereof in the treatment of cancer |
| WO2007019345A1 (en) | 2005-08-04 | 2007-02-15 | Sirtris Pharmaceuticals, Inc. | Imidazopyridine derivatives as sirtuin modulating agents |
| WO2007038387A2 (en) | 2005-09-23 | 2007-04-05 | Yale University | Compounds and methods for the treatment of viruses and cancer |
| US8604042B2 (en) | 2005-11-01 | 2013-12-10 | Targegen, Inc. | Bi-aryl meta-pyrimidine inhibitors of kinases |
| MY167260A (en) | 2005-11-01 | 2018-08-14 | Targegen Inc | Bi-aryl meta-pyrimidine inhibitors of kinases |
| TW200736232A (en) | 2006-01-26 | 2007-10-01 | Astrazeneca Ab | Pyrimidine derivatives |
| FR2897061B1 (fr) | 2006-02-03 | 2010-09-03 | Sanofi Aventis | Derives de n-heteroaryl-carboxamides tricycliques contenant un motif benzimidazole, leur preparation et leur application en therapeutique. |
| AR065015A1 (es) | 2007-01-26 | 2009-05-13 | Smithkline Beecham Corp | Derivados de antranilamida, composiciones farmaceuticas que los contienen, y usos para el tratamiento del cancer |
| ES2415163T3 (es) | 2007-04-30 | 2013-07-24 | Prometic Biosciences Inc. | Derivados de triazina, composiciones que contienen tales derivados, y métodos de tratamiento de cáncer y enfermedades autoinmunitarias usando tales derivados |
| AU2008247592A1 (en) | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Thiazoles and pyrazoles useful as kinase inhibitors |
| JP5710251B2 (ja) | 2007-06-07 | 2015-04-30 | イントラ−セルラー・セラピーズ・インコーポレイテッドIntra−Cellular Therapies, Inc. | 新規ヘテロ環化合物およびその使用 |
| CN101903357A (zh) | 2007-07-17 | 2010-12-01 | 里格尔药品股份有限公司 | 作为pkc抑制剂的环状胺取代的嘧啶二胺 |
| JP5328816B2 (ja) | 2008-02-22 | 2013-10-30 | エフ.ホフマン−ラ ロシュ アーゲー | アミロイドβの調節薬 |
| WO2009126537A1 (en) | 2008-04-07 | 2009-10-15 | Syndax Pharmaceuticals, Inc. | Administration of an inhibitor of hdac and an hmt inhibitor |
| JP5802127B2 (ja) | 2008-04-16 | 2015-10-28 | ポートラ ファーマシューティカルズ, インコーポレイテッド | Syk又はjakキナーゼ阻害剤としての2,6−ジアミノ−ピリミジン−5−イル−カルボキサミド類 |
| US8680113B2 (en) | 2008-07-01 | 2014-03-25 | Ptc Therapeutics, Inc. | BMI-1 protein expression modulators |
| UY31982A (es) | 2008-07-16 | 2010-02-26 | Boehringer Ingelheim Int | Derivados de 1,2-dihidropiridin-3-carboxamidas n-sustituidas |
| CN102112131A (zh) | 2008-08-05 | 2011-06-29 | 塔格根公司 | 治疗地中海贫血的方法 |
| US20110230478A1 (en) | 2008-09-03 | 2011-09-22 | Bayer ScienceCrop AG | 4-Alkyl-substituted diaminopyrimidines |
| WO2010083240A2 (en) | 2009-01-14 | 2010-07-22 | Rigel Pharmaceuticals, Inc. | Methods for treating inflammatory disorders using 2,4-pyrimidinediamine compounds |
| EP2389373B1 (en) | 2009-01-21 | 2017-05-17 | Rigel Pharmaceuticals, Inc. | Derivatives of n2-(3-pyridyl or phenyl)-n4-(4-piperidyl)-2,4-pyrimidinediamine useful in the treatment of inflammatory, autoimmune or proliferative diseases |
| EA022802B1 (ru) | 2009-01-23 | 2016-03-31 | Райджел Фармасьютикалз, Инк. | Соединения, композиции и способы для лечения заболеваний, опосредованных jak-киназой |
| WO2010127246A2 (en) | 2009-04-30 | 2010-11-04 | Burnham Institute For Medical Research | Hnf4 modulators and methods of use |
| WO2010129802A1 (en) | 2009-05-06 | 2010-11-11 | Portola Pharmaceuticals, Inc. | Inhibitors of jak |
| JP2012197231A (ja) | 2009-08-06 | 2012-10-18 | Oncotherapy Science Ltd | Ttk阻害作用を有するピリジンおよびピリミジン誘導体 |
| EP2477625A4 (en) | 2009-09-14 | 2012-10-24 | Phusis Therapeutics Inc | PHARMACEUTICAL COMPOSITIONS AND FORMULATIONS COMPRISING PLECKSTRINE HOMOLOGY DOMAIN INHIBITORS AND METHODS OF USE |
| AT509266B1 (de) | 2009-12-28 | 2014-07-15 | Univ Wien Tech | Substituierte pyridine und pyrimidine |
| JP2013523657A (ja) | 2010-03-26 | 2013-06-17 | グラクソ グループ リミテッド | キナーゼ阻害剤としてのインダゾリル‐ピリミジン |
| CN102242146B (zh) | 2010-05-10 | 2015-11-25 | 高丽大学校产学协力团 | 组合物和用其产生诱导全能干细胞的方法 |
| WO2012023285A1 (en) | 2010-08-20 | 2012-02-23 | Oncotherapy Science, Inc. | Ehmt2 as a target gene for cancer therapy and diagnosis |
| AU2011298987B2 (en) | 2010-09-10 | 2017-09-28 | Epizyme, Inc. | Inhibitors of human EZH2, and methods of use thereof |
| WO2012038417A1 (en) | 2010-09-20 | 2012-03-29 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Substituted amino - benzoic acid derivatives as inhibitors of dna methyltransferases |
| WO2012044936A1 (en) | 2010-09-30 | 2012-04-05 | Portola Pharmaceuticals, Inc. | Combination therapy with 4-(3-(2h-1,2,3-triazol-2-yl)phenylamino)-2-((1r,2s)-2-aminocyclohexylamino)pyrimidine-5-carboxamide |
| US9714427B2 (en) | 2010-11-11 | 2017-07-25 | The University Of North Carolina At Chapel Hill | Methods and compositions for unsilencing imprinted genes |
| US20130310379A1 (en) | 2010-11-19 | 2013-11-21 | Constellation Pharmaceuticals | Modulators of methyl modifying enzymes, compositions and uses thereof |
| KR101682417B1 (ko) | 2011-02-25 | 2016-12-06 | 주식회사유한양행 | 다이아미노피리미딘 유도체 및 그의 제조방법 |
| JO3438B1 (ar) * | 2011-04-13 | 2019-10-20 | Epizyme Inc | مركبات بنزين مستبدلة بأريل أو أريل غير متجانس |
| TW201733984A (zh) * | 2011-04-13 | 2017-10-01 | 雅酶股份有限公司 | 經取代之苯化合物 |
| PT2755483T (pt) | 2011-09-14 | 2019-02-18 | Samumed Llc | Indazol-3-carboxamidas e sua utilização como inibidores da via de sinalização de wnt/β-catenina |
| US9458131B2 (en) | 2011-11-08 | 2016-10-04 | Emory University | Compounds and compositions used to epigenetically transform cells and methods related thereto |
| WO2013078468A1 (en) | 2011-11-23 | 2013-05-30 | Portola Pharmaceuticals, Inc. | Selective kinase inhibitors |
| KR101452235B1 (ko) | 2012-02-03 | 2014-10-22 | 서울대학교산학협력단 | 신규한 피리미딘계 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 포함하는 rage 수용체 관련 질환의 예방 또는 치료용 약학적 조성물 |
| AU2013237226A1 (en) | 2012-03-19 | 2014-10-09 | Emory University | Quinazoline compounds and their use in therapy |
| GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| EP2863913B1 (en) | 2012-06-20 | 2018-09-12 | Merck Sharp & Dohme Corp. | Imidazolyl analogs as syk inhibitors |
| WO2014058921A2 (en) | 2012-10-08 | 2014-04-17 | Portola Pharmaceuticals, Inc. | Substituted pyrimidinyl kinase inhibitors |
| US9145412B2 (en) | 2012-11-02 | 2015-09-29 | Acetylon Pharmaceuticals, Inc. | Selective HDAC1 and HDAC2 inhibitors |
| CA2892677A1 (en) | 2012-12-04 | 2014-06-12 | Rigel Pharmaceuticals, Inc. | Protein kinase c inhibitors and uses thereof |
| EP2953457B1 (en) | 2013-02-08 | 2020-04-08 | Celgene CAR LLC | Erk inhibitors and uses thereof |
| CN103172637B (zh) | 2013-03-13 | 2015-05-27 | 上海大学 | 嘧啶并[1,2-a]苯并咪唑类化合物及其制备方法 |
| WO2014151900A1 (en) | 2013-03-14 | 2014-09-25 | Rigel Pharmaceuticals, Inc. | Protein kinase c inhibitors and uses thereof |
| US20150087673A1 (en) | 2013-09-26 | 2015-03-26 | Rigel Pharmaceuticals, Inc. | Methods for using and biomarkers for ampk-activating compounds |
| SG11201604821YA (en) | 2013-12-20 | 2016-07-28 | Signal Pharm Llc | Substituted diaminopyrimidyl compounds, compositions thereof, and methods of treatment therewith |
| US20150250824A1 (en) | 2014-03-07 | 2015-09-10 | The Research Foundation For The State University Of New York | Methods and compositions for expansion of stem cells and other cells |
| US9284272B2 (en) * | 2014-03-28 | 2016-03-15 | Abbvie Inc. | Inhibitors of histone methyltransferase G9a |
| AU2015276537B2 (en) | 2014-06-16 | 2019-03-14 | Fundacion Para La Investigacion Medica Aplicada | Novel compounds as dual inhibitors of histone methyltransferases and dna methyltransferases |
| CA2952474A1 (en) | 2014-06-23 | 2015-12-30 | Genentech, Inc. | Methods of treating cancer and preventing cancer drug resistance |
| EP3885343A1 (en) | 2014-11-06 | 2021-09-29 | Dana-Farber Cancer Institute, Inc. | Indole compounds as ezh2 inhibitors and uses thereof |
| JP2018534276A (ja) | 2015-10-09 | 2018-11-22 | エイジェンシー・フォー・サイエンス,テクノロジー・ア | 癌治療及びエピジェネティクスのための化合物 |
| WO2017085053A1 (en) | 2015-11-16 | 2017-05-26 | Fundación Para La Investigación Médica Aplicada | Novel compounds as inhibitors of dna methyltransferases |
| WO2017090719A1 (ja) | 2015-11-27 | 2017-06-01 | 大鵬薬品工業株式会社 | 縮環ピリミジン化合物又はその塩 |
| WO2017102677A1 (en) | 2015-12-14 | 2017-06-22 | Fundación Para La Investigación Médica Aplicada | 2,4,6,7-tetrasubstituted quinoline compounds as inhibitors of dna methyltransferases |
| EP3416963B1 (en) | 2016-02-17 | 2021-07-28 | Global Blood Therapeutics, Inc. | Histone methyltransferase inhibitors |
| HRP20200728T1 (hr) | 2016-04-15 | 2020-07-24 | Abbvie Inc. | Inhibitori bromodomene |
| KR102426043B1 (ko) | 2016-04-15 | 2022-07-27 | 블루프린트 메디신즈 코포레이션 | 액티빈 수용체 유사 키나아제의 저해제 |
| KR102571679B1 (ko) * | 2016-04-15 | 2023-08-29 | 에피자임, 인코포레이티드 | Ehmt1 및 ehmt2 저해제로서의 아민-치환된 아릴 또는 헤테로아릴 화합물 |
| CN109071545B (zh) | 2016-04-15 | 2021-08-03 | 拜耳动物保健有限责任公司 | 新的吡唑并嘧啶衍生物 |
| MX2018012303A (es) | 2016-04-15 | 2019-01-14 | Syngenta Participations Ag | Compuestos de piridazinona herbicida. |
| RU2748294C2 (ru) | 2016-06-03 | 2021-05-21 | Зе Трастис Оф Коламбия Юниверсити Ин Зе Сити Оф Нью-Йорк | Способ лечения синдрома прадера-вилли |
| WO2017214395A1 (en) | 2016-06-10 | 2017-12-14 | Enanta Pharmaceuticals, Inc. | Hepatitis b antiviral agents |
| CN109563094B (zh) | 2016-06-10 | 2022-03-18 | 法国施维雅药厂 | 新的(杂)芳基取代的哌啶基衍生物、它们的制备方法和含有它们的药物组合物 |
| FR3052452B1 (fr) | 2016-06-10 | 2018-06-22 | Les Laboratoires Servier | Nouveaux derives de piperidinyle, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| US10537590B2 (en) | 2016-09-30 | 2020-01-21 | Boehringer Ingelheim International Gmbh | Cyclic dinucleotide compounds |
| JP7187449B2 (ja) | 2016-09-30 | 2022-12-12 | エピザイム,インコーポレイティド | Ehmt2阻害剤としての置換された融合二環式または三環式複素環化合物 |
| LT3555070T (lt) | 2016-12-19 | 2023-09-11 | Epizyme, Inc. | Aminu pakeisti heterocikliniai junginiai, kaip ehmt2 inhibitoriai, ir jų panaudojimo būdai |
| WO2018119208A1 (en) | 2016-12-22 | 2018-06-28 | Global Blood Therapeutics, Inc. | Histone methyltransferase inhibitors |
| WO2018119263A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Heterocyclic compounds derivatives as pd-l1 internalization inducers |
| WO2018183923A1 (en) | 2017-03-31 | 2018-10-04 | Epizyme, Inc. | Methods of using ehmt2 inhibitors |
| SG11202001090WA (en) | 2017-08-15 | 2020-03-30 | Global Blood Therapeutics Inc | Tricyclic compounds as histone methyl-transferase inhibitors |
| EP3697419A4 (en) | 2017-10-17 | 2021-08-18 | Epizyme, Inc. | AMINE SUBSTITUTION HETEROCYCLIC COMPOUNDS USED AS AND DERIVATIVES OF EHMT2 |
| MA50418A (fr) | 2017-10-18 | 2021-04-07 | Epizyme Inc | Composés hétérocycliques substitués par une amine, utilisés comme inhibiteurs de l'ehmt2, sels de ceux-ci, et leurs méthodes de synthèse |
| EP3697420A4 (en) | 2017-10-18 | 2021-11-24 | Epizyme, Inc. | METHODS OF USING EHMT2 INHIBITORS IN IMMUNOTHERAPIES |
| CN111315371A (zh) | 2017-10-18 | 2020-06-19 | 埃皮兹姆公司 | 使用ehmt2抑制剂治疗或预防血液障碍的方法 |
-
2018
- 2018-04-20 AU AU2018254577A patent/AU2018254577B2/en not_active Ceased
- 2018-04-20 CN CN202410032276.1A patent/CN118021814A/zh active Pending
- 2018-04-20 CA CA3060416A patent/CA3060416A1/en active Pending
- 2018-04-20 CN CN201880028882.9A patent/CN110621316B/zh active Active
- 2018-04-20 US US16/606,833 patent/US11672800B2/en active Active
- 2018-04-20 EP EP18788629.6A patent/EP3612181A4/en active Pending
- 2018-04-20 JP JP2019556647A patent/JP2020517618A/ja not_active Withdrawn
- 2018-04-20 WO PCT/US2018/028609 patent/WO2018195450A1/en not_active Ceased
-
2022
- 2022-11-18 JP JP2022184887A patent/JP2023009301A/ja active Pending
-
2023
- 2023-03-23 US US18/188,691 patent/US20230364086A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2020517618A5 (enExample) | ||
| US20230364086A1 (en) | Combination therapies with ehmt2 inhibitors | |
| ES3001984T3 (en) | Diacylglycerol kinase modulating compounds | |
| CN115698009B (zh) | 抑制cd73的2,4-二氧代嘧啶化合物 | |
| CN105683166B (zh) | 取代的嘧啶Bmi-1抑制剂 | |
| JP7686091B2 (ja) | ジアシルグリセロールキナーゼ調節化合物 | |
| KR102705821B1 (ko) | 항암제 | |
| CN111712494A (zh) | Pd-1/pd-l1抑制剂 | |
| JP7641894B2 (ja) | がん治療におけるentファミリートランスポーター阻害剤の使用及びそのアデノシン受容体アンタゴニストとの組み合わせ | |
| AU2014219256B2 (en) | Heteroaromatic compounds as PI3 kinase modulators | |
| AU2014317119A1 (en) | Combination of a MEK inhibitor and an ERK inhibitor for use in treatment of hyperproliferative diseases | |
| JP2024520593A (ja) | ジアシルグリエルコール(diacylglyercol)キナーゼ調節化合物 | |
| ES2688809T3 (es) | Combinaciones de compuestos inhibidores de AKT y MEK para tratar el cáncer | |
| US20050171182A1 (en) | Methods and compositions for use in the treatment of mutant receptor tyrosine kinase driven cellular proliferative diseases | |
| JP2025000796A (ja) | がん治療におけるentファミリートランスポーター阻害剤の使用及びそのアデノシン受容体アンタゴニストとの組み合わせ | |
| RU2830439C1 (ru) | Фармацевтическая комбинация на основе ингибиторов prmt5 | |
| HK40068336B (zh) | 用於治疗激酶依赖性病症的化合物 | |
| HK40106161A (zh) | 二酰基甘油激酶调节化合物 | |
| HK40108161A (zh) | Pd-1/pd-l1抑制剂 | |
| HK40108704A (zh) | Pd-1/pd-l1抑制剂 | |
| HK40040233B (zh) | Pd-1/pd-l1抑制剂 | |
| HK40031561A (en) | Pd-1/pd-l1 inhibitors | |
| HK1226057B (zh) | 取代的嘧啶bmi-1抑制剂 | |
| BR112016004511B1 (pt) | Composto, composto ou uma forma do mesmo, uso de um composto ou forma do mesmo, e composição farmacêutica para uso no tratamento de um câncer mediado por bmi-1 |