JP2019142823A5 - - Google Patents
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- JP2019142823A5 JP2019142823A5 JP2018030208A JP2018030208A JP2019142823A5 JP 2019142823 A5 JP2019142823 A5 JP 2019142823A5 JP 2018030208 A JP2018030208 A JP 2018030208A JP 2018030208 A JP2018030208 A JP 2018030208A JP 2019142823 A5 JP2019142823 A5 JP 2019142823A5
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- Prior art keywords
- pharmaceutical composition
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- group
- kinase
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- -1 -NH 2 Chemical group 0.000 claims 12
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 6
- KOZFSFOOLUUIGY-SOLYNIJKSA-N K-252a Chemical compound C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1[C@H]1C[C@@](C(=O)OC)(O)[C@]4(C)O1 KOZFSFOOLUUIGY-SOLYNIJKSA-N 0.000 claims 5
- 239000002246 antineoplastic agent Substances 0.000 claims 5
- 108091000080 Phosphotransferase Proteins 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 102000020233 phosphotransferase Human genes 0.000 claims 4
- 229940079593 drug Drugs 0.000 claims 3
- GAXOKIHBYAPTSY-LROUJFHJSA-N (15S,16S,18R)-16-(aminomethyl)-16-hydroxy-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaen-3-one Chemical compound C[C@]12O[C@H](C[C@]1(O)CN)n1c3ccccc3c3c4C(=O)NCc4c4c5ccccc5n2c4c13 GAXOKIHBYAPTSY-LROUJFHJSA-N 0.000 claims 2
- MEXUTNIFSHFQRG-UHFFFAOYSA-N 6,7,12,13-tetrahydro-5h-indolo[2,3-a]pyrrolo[3,4-c]carbazol-5-one Chemical compound C12=C3C=CC=C[C]3NC2=C2NC3=CC=C[CH]C3=C2C2=C1C(=O)NC2 MEXUTNIFSHFQRG-UHFFFAOYSA-N 0.000 claims 2
- UAQXZUMECPBOGP-IZKCBNJNSA-N ac1l2zvq Chemical compound C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1[C@@H]1C[C@@](CNCCC)(O)[C@]4(C)O1 UAQXZUMECPBOGP-IZKCBNJNSA-N 0.000 claims 2
- 229940041181 antineoplastic drug Drugs 0.000 claims 2
- HKSZLNNOFSGOKW-UHFFFAOYSA-N ent-staurosporine Natural products C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1C1CC(NC)C(OC)C4(C)O1 HKSZLNNOFSGOKW-UHFFFAOYSA-N 0.000 claims 2
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 2
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 230000035772 mutation Effects 0.000 claims 2
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims 2
- 208000016691 refractory malignant neoplasm Diseases 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- HKSZLNNOFSGOKW-FYTWVXJKSA-N staurosporine Chemical compound C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1[C@H]1C[C@@H](NC)[C@@H](OC)[C@]4(C)O1 HKSZLNNOFSGOKW-FYTWVXJKSA-N 0.000 claims 2
- CGPUWJWCVCFERF-UHFFFAOYSA-N staurosporine Natural products C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1C1CC(NC)C(OC)C4(OC)O1 CGPUWJWCVCFERF-UHFFFAOYSA-N 0.000 claims 2
- OSJFVOAURBIGTC-IFGWQFMBSA-N (2S,3R,4R,6R)-4-hydroxy-3-methoxy-2-methyl-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one Chemical compound C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1[C@H]1C[C@@H](O)[C@@H](OC)[C@]4(C)O1 OSJFVOAURBIGTC-IFGWQFMBSA-N 0.000 claims 1
- OWOHLURDBZHNGG-YFKPBYRVSA-N (8ar)-hexahydropyrrolo[1,2-a]pyrazine-1,4-dione Chemical compound O=C1CNC(=O)[C@@H]2CCCN12 OWOHLURDBZHNGG-YFKPBYRVSA-N 0.000 claims 1
- JKEBWJSRGQOXNU-TUZCJGOLSA-N 118736-03-1 Chemical compound C12=C3N4C5=CC=C(O)C=C5C3=C3CNC(=O)C3=C2C2=CC(O)=CC=C2N1[C@H]1C[C@H](C(=O)OOC)[C@]4(C)O1 JKEBWJSRGQOXNU-TUZCJGOLSA-N 0.000 claims 1
- 125000001731 2-cyanoethyl group Chemical group [H]C([H])(*)C([H])([H])C#N 0.000 claims 1
- YFYYWLWHOINTHH-UHFFFAOYSA-N 3'-Demethoxy-3'-hydroxystaurosporine Natural products C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1C1CC(NC)C(O)C4(C)O1 YFYYWLWHOINTHH-UHFFFAOYSA-N 0.000 claims 1
- YFYYWLWHOINTHH-FCHZLITKSA-N 3'-demethylstaurosporine Chemical compound C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1[C@H]1C[C@@H](NC)[C@@H](O)[C@]4(C)O1 YFYYWLWHOINTHH-FCHZLITKSA-N 0.000 claims 1
- CCOPBVQTBWBCIK-UHFFFAOYSA-N 4'-demethylamino-4',5'-dihydroxystaurosporine Natural products C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1C1C(O)C(O)C(OC)C4(C)O1 CCOPBVQTBWBCIK-UHFFFAOYSA-N 0.000 claims 1
- HMFXRYBLHSRYJD-IQRRFOAXSA-N 7-o-methyl ucn-01 Chemical compound N([C@@H](C1=C2C3=CC=CC=C3N3C2=C24)OC)C(=O)C1=C2C1=CC=CC=C1N4[C@@H]1C[C@@H](NC)[C@H](OC)[C@]3(C)O1 HMFXRYBLHSRYJD-IQRRFOAXSA-N 0.000 claims 1
- POTTVLREWUNNRO-UGZRAAABSA-N 7-oxostaurosporine Chemical compound C12=C3N4C5=CC=CC=C5C3=C3C(=O)NC(=O)C3=C2C2=CC=CC=C2N1[C@H]1C[C@@H](NC)[C@@H](OC)[C@]4(C)O1 POTTVLREWUNNRO-UGZRAAABSA-N 0.000 claims 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 1
- CCOPBVQTBWBCIK-DYEJEPNJSA-N C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1[C@H]1[C@H](O)[C@H](O)[C@@H](OC)[C@]4(C)O1 Chemical compound C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1[C@H]1[C@H](O)[C@H](O)[C@@H](OC)[C@]4(C)O1 CCOPBVQTBWBCIK-DYEJEPNJSA-N 0.000 claims 1
- ZEOWTGPWHLSLOG-UHFFFAOYSA-N Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F Chemical compound Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F ZEOWTGPWHLSLOG-UHFFFAOYSA-N 0.000 claims 1
- ZBNZXTGUTAYRHI-UHFFFAOYSA-N Dasatinib Chemical compound C=1C(N2CCN(CCO)CC2)=NC(C)=NC=1NC(S1)=NC=C1C(=O)NC1=C(C)C=CC=C1Cl ZBNZXTGUTAYRHI-UHFFFAOYSA-N 0.000 claims 1
- 102100023593 Fibroblast growth factor receptor 1 Human genes 0.000 claims 1
- 101710182386 Fibroblast growth factor receptor 1 Proteins 0.000 claims 1
- 102100023600 Fibroblast growth factor receptor 2 Human genes 0.000 claims 1
- 101710182389 Fibroblast growth factor receptor 2 Proteins 0.000 claims 1
- 102100027842 Fibroblast growth factor receptor 3 Human genes 0.000 claims 1
- 101710182396 Fibroblast growth factor receptor 3 Proteins 0.000 claims 1
- 102100035108 High affinity nerve growth factor receptor Human genes 0.000 claims 1
- 101000596894 Homo sapiens High affinity nerve growth factor receptor Proteins 0.000 claims 1
- 101000579425 Homo sapiens Proto-oncogene tyrosine-protein kinase receptor Ret Proteins 0.000 claims 1
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 claims 1
- 101000823316 Homo sapiens Tyrosine-protein kinase ABL1 Proteins 0.000 claims 1
- QTYMDECKVKSGSM-YMUMJAELSA-N KT 5823 Chemical compound C12=C3N4C5=CC=CC=C5C3=C3CN(C)C(=O)C3=C2C2=CC=CC=C2N1[C@H]1C[C@](OC)(C(=O)OC)[C@]4(C)O1 QTYMDECKVKSGSM-YMUMJAELSA-N 0.000 claims 1
- ZZWAFVPZTZSAEM-RIGQTMPJSA-N KT 5926 Chemical compound C12=CC=CC=C2C2=C(CNC3=O)C3=C3C4=CC(OCCC)=CC=C4N4C3=C2N1[C@]1(C)[C@@](O)(C(=O)OC)C[C@H]4O1 ZZWAFVPZTZSAEM-RIGQTMPJSA-N 0.000 claims 1
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims 1
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims 1
- 239000002067 L01XE06 - Dasatinib Substances 0.000 claims 1
- 101100490437 Mus musculus Acvrl1 gene Proteins 0.000 claims 1
- 101100335081 Mus musculus Flt3 gene Proteins 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 101150038994 PDGFRA gene Proteins 0.000 claims 1
- 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 claims 1
- 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 claims 1
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 claims 1
- 108060006706 SRC Proteins 0.000 claims 1
- 102000001332 SRC Human genes 0.000 claims 1
- 102100022596 Tyrosine-protein kinase ABL1 Human genes 0.000 claims 1
- XQJTZEAYPSXVTH-XNZIZSAOSA-N ac1l2vdo Chemical compound C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1[C@@H]1C[C@](CN(C)C)(O)[C@]4(C)O1 XQJTZEAYPSXVTH-XNZIZSAOSA-N 0.000 claims 1
- XRPFUJUZOIDJFP-DOYMOWJKSA-N ac1l2vdr Chemical compound C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1[C@@H]1C[C@@](CNC)(O)[C@]4(C)O1 XRPFUJUZOIDJFP-DOYMOWJKSA-N 0.000 claims 1
- YYDZNUMDZXMMCI-ZEMYHKRKSA-N ac1l315s Chemical compound C12=C3N4C5=CC=CC=C5C3=C3C(=O)NC(=O)C3=C2C2=CC=CC=C2N1[C@@H]1C[C@@H](N(C)C(=O)OCC)[C@H](OC)[C@]4(C)O1 YYDZNUMDZXMMCI-ZEMYHKRKSA-N 0.000 claims 1
- 229960001686 afatinib Drugs 0.000 claims 1
- ULXXDDBFHOBEHA-CWDCEQMOSA-N afatinib Chemical compound N1=CN=C2C=C(O[C@@H]3COCC3)C(NC(=O)/C=C/CN(C)C)=CC2=C1NC1=CC=C(F)C(Cl)=C1 ULXXDDBFHOBEHA-CWDCEQMOSA-N 0.000 claims 1
- KIZWKTROWIIMNN-FYTWVXJKSA-N afn941 Chemical compound C1CCCC(N2C3=C45)=C1C3=C1C(=O)NCC1=C5C1=CC=CC=C1N4[C@@]1(C)O[C@@H]2C[C@@H](NC)[C@H]1OC KIZWKTROWIIMNN-FYTWVXJKSA-N 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 229950008356 becatecarin Drugs 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- JSKFWUPVIZYJMR-UDOAKELVSA-N bmy-27557 Chemical compound O=C1N(CCN(CC)CC)C(=O)C(C2=C3[CH]C=CC(Cl)=C3NC2=C23)=C1C2=C1C=CC=C(Cl)[C]1N3[C@@H]1O[C@H](CO)[C@@H](OC)[C@H](O)[C@H]1O JSKFWUPVIZYJMR-UDOAKELVSA-N 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- NMMGUHANGUWNBN-OGLOGDKOSA-N cep-751 Chemical compound C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1C1C[C@](OC)(CO)[C@]4(C)O1 NMMGUHANGUWNBN-OGLOGDKOSA-N 0.000 claims 1
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims 1
- 229960004316 cisplatin Drugs 0.000 claims 1
- 229960002448 dasatinib Drugs 0.000 claims 1
- 125000006222 dimethylaminomethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 229960001433 erlotinib Drugs 0.000 claims 1
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 125000006351 ethylthiomethyl group Chemical group [H]C([H])([H])C([H])([H])SC([H])([H])* 0.000 claims 1
- 229960002584 gefitinib Drugs 0.000 claims 1
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims 1
- 229960005277 gemcitabine Drugs 0.000 claims 1
- 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 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 1
- 239000000693 micelle Substances 0.000 claims 1
- BMGQWWVMWDBQGC-IIFHNQTCSA-N midostaurin Chemical compound CN([C@H]1[C@H]([C@]2(C)O[C@@H](N3C4=CC=CC=C4C4=C5C(=O)NCC5=C5C6=CC=CC=C6N2C5=C43)C1)OC)C(=O)C1=CC=CC=C1 BMGQWWVMWDBQGC-IIFHNQTCSA-N 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- NJFTXXMZGIINOF-RIGRGULHSA-N n,n-dimethylstaurosporine Chemical compound C12=C3N4C5=CC=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1[C@H]1C[C@@H](N(C)C)[C@H](OC)[C@]4(C)O1 NJFTXXMZGIINOF-RIGRGULHSA-N 0.000 claims 1
- 229960003278 osimertinib Drugs 0.000 claims 1
- DUYJMQONPNNFPI-UHFFFAOYSA-N osimertinib Chemical compound COC1=CC(N(C)CCN(C)C)=C(NC(=O)C=C)C=C1NC1=NC=CC(C=2C3=CC=CC=C3N(C)C=2)=N1 DUYJMQONPNNFPI-UHFFFAOYSA-N 0.000 claims 1
- 150000002923 oximes Chemical class 0.000 claims 1
- 229960005079 pemetrexed Drugs 0.000 claims 1
- QOFFJEBXNKRSPX-ZDUSSCGKSA-N pemetrexed Chemical compound C1=N[C]2NC(N)=NC(=O)C2=C1CCC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 QOFFJEBXNKRSPX-ZDUSSCGKSA-N 0.000 claims 1
- 125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 claims 1
- NVSJOASGKCGXBZ-SYLNULQMSA-N sch-47112 Chemical compound C12=C3N4C5=CC=CC=C5C3=C3C(=O)NC(=O)C3=C2C2=CC=CC=C2N1[C@@H]1C[C@H](CO)[C@H]4O1 NVSJOASGKCGXBZ-SYLNULQMSA-N 0.000 claims 1
- ZXQPCJUWQQAWKY-UHFFFAOYSA-N tan 999 Chemical compound C12=C3N4C5=CC(OC)=CC=C5C3=C3CNC(=O)C3=C2C2=CC=CC=C2N1C1CC(=NC)C(OC)C4(C)O1 ZXQPCJUWQQAWKY-UHFFFAOYSA-N 0.000 claims 1
- 0 C*(*)C(C)(C(**)(*(C)*)C1(C)C)OC1(C)*=C Chemical compound C*(*)C(C)(C(**)(*(C)*)C1(C)C)OC1(C)*=C 0.000 description 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2018030208A JP7223502B6 (ja) | 2018-02-22 | 2018-02-22 | 医薬組成物 |
| PCT/JP2019/006780 WO2019163943A1 (ja) | 2018-02-22 | 2019-02-22 | 医薬組成物 |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2018030208A JP7223502B6 (ja) | 2018-02-22 | 2018-02-22 | 医薬組成物 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2019142823A JP2019142823A (ja) | 2019-08-29 |
| JP2019142823A5 true JP2019142823A5 (https=) | 2021-01-14 |
| JP7223502B2 JP7223502B2 (ja) | 2023-02-16 |
| JP7223502B6 JP7223502B6 (ja) | 2024-02-08 |
Family
ID=67688423
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018030208A Active JP7223502B6 (ja) | 2018-02-22 | 2018-02-22 | 医薬組成物 |
Country Status (2)
| Country | Link |
|---|---|
| JP (1) | JP7223502B6 (https=) |
| WO (1) | WO2019163943A1 (https=) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111303164B (zh) * | 2019-09-19 | 2021-03-23 | 杭州科兴生物化工有限公司 | 一类星孢菌素类衍生物及其制备方法和应用 |
| CN116041371B (zh) * | 2023-01-29 | 2024-04-19 | 杭州科兴生物化工有限公司 | 7-羰基星孢菌素衍生物及其制备方法和应用 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2565795A (en) * | 1994-06-01 | 1995-12-21 | Ciba-Geigy Ag | Carbazole derivatives as agents against multi-drug resistance |
| WO2007022999A1 (en) | 2005-08-25 | 2007-03-01 | Creabilis Therapeutics S.P.A. | Polymer conjugates of k-252a and derivatives thereof |
| WO2016024595A1 (ja) | 2014-08-11 | 2016-02-18 | 国立大学法人東京大学 | エピルビシン複合化ブロック共重合体と、抗癌剤とを含むミセル、及び当該ミセルを含む癌又は耐性癌、転移癌の治療に適用可能な医薬組成物 |
| EP3971227A1 (en) * | 2016-08-23 | 2022-03-23 | Kawasaki Institute of Industrial Promotion | Polymer, method for producing polymer, and drug conjugate |
-
2018
- 2018-02-22 JP JP2018030208A patent/JP7223502B6/ja active Active
-
2019
- 2019-02-22 WO PCT/JP2019/006780 patent/WO2019163943A1/ja not_active Ceased
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