JP2016501838A5 - - Google Patents

Info

Publication number

JP2016501838A5

JP2016501838A5 JP2015539952A JP2015539952A JP2016501838A5 JP 2016501838 A5 JP2016501838 A5 JP 2016501838A5 JP 2015539952 A JP2015539952 A JP 2015539952A JP 2015539952 A JP2015539952 A JP 2015539952A JP 2016501838 A5 JP2016501838 A5 JP 2016501838A5

Authority

JP

Japan

Prior art keywords

medicament according

formula

independently

cancer

medicament

Prior art date

2013-10-30

Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Granted

Links

• Espacenet
• Global Dossier
• Discuss

• 239000003814 drug Substances 0.000 claims 24
• 201000011510 cancer Diseases 0.000 claims 11
• NMUSYJAQQFHJEW-KVTDHHQDSA-N 5-azacytidine Chemical group 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 10
• 229960002756 azacitidine Drugs 0.000 claims 10
• 150000001875 compounds Chemical class 0.000 claims 10
• 239000003112 inhibitor Substances 0.000 claims 10
• 230000007067 DNA methylation Effects 0.000 claims 9
• 206010028980 Neoplasm Diseases 0.000 claims 8
• 125000000217 alkyl group Chemical group 0.000 claims 7
• 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 6
• -1 R 21 Chemical compound 0.000 claims 6
• NMUSYJAQQFHJEW-UHFFFAOYSA-N 5-Azacytidine Natural products O=C1N=C(N)N=CN1C1C(O)C(O)C(CO)O1 NMUSYJAQQFHJEW-UHFFFAOYSA-N 0.000 claims 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 claims 4
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
• 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 3
• 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
• 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 3
• 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
• 125000004093 cyano group Chemical group *C#N 0.000 claims 3
• 229960003603 decitabine Drugs 0.000 claims 3
• 125000003709 fluoroalkyl group Chemical group 0.000 claims 3
• 230000003394 haemopoietic effect Effects 0.000 claims 3
• 125000004404 heteroalkyl group Chemical group 0.000 claims 3
• 125000002768 hydroxyalkyl group Chemical group 0.000 claims 3
• 208000032839 leukemia Diseases 0.000 claims 3
• PVHLMTREZMEJCG-GDTLVBQBSA-N Ile(5)-angiotensin II (1-7) Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N1[C@@H](CCC1)C([O-])=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(N)=[NH2+])NC(=O)[C@@H]([NH3+])CC([O-])=O)C(C)C)C1=CC=C(O)C=C1 PVHLMTREZMEJCG-GDTLVBQBSA-N 0.000 claims 2
• 108010021281 angiotensin I (1-7) Proteins 0.000 claims 2
• 238000002512 chemotherapy Methods 0.000 claims 2
• 201000010099 disease Diseases 0.000 claims 2
• 208000035475 disorder Diseases 0.000 claims 2
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
• 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
• 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 2
• 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
• GOTYRUGSSMKFNF-UHFFFAOYSA-N lenalidomide Chemical compound C1C=2C(N)=CC=CC=2C(=O)N1C1CCC(=O)NC1=O GOTYRUGSSMKFNF-UHFFFAOYSA-N 0.000 claims 2
• 229960004942 lenalidomide Drugs 0.000 claims 2
• 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims 2
• 229940002612 prodrug Drugs 0.000 claims 2
• 239000000651 prodrug Substances 0.000 claims 2
• 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
• 150000003839 salts Chemical class 0.000 claims 2
• 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 1
• 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
• 102000003964 Histone deacetylase Human genes 0.000 claims 1
• 108090000353 Histone deacetylase Proteins 0.000 claims 1
• 208000028018 Lymphocytic leukaemia Diseases 0.000 claims 1
• 206010025323 Lymphomas Diseases 0.000 claims 1
• 208000033833 Myelomonocytic Chronic Leukemia Diseases 0.000 claims 1
• 208000014767 Myeloproliferative disease Diseases 0.000 claims 1
• 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
• 208000009527 Refractory anemia Diseases 0.000 claims 1
• 206010072684 Refractory cytopenia with unilineage dysplasia Diseases 0.000 claims 1
• 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 1
• 239000003146 anticoagulant agent Substances 0.000 claims 1
• 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 1
• 229940079593 drug Drugs 0.000 claims 1
• 230000008482 dysregulation Effects 0.000 claims 1
• 125000003187 heptyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
• 238000001990 intravenous administration Methods 0.000 claims 1
• 208000003747 lymphoid leukemia Diseases 0.000 claims 1
• 230000011987 methylation Effects 0.000 claims 1
• 238000007069 methylation reaction Methods 0.000 claims 1
• 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
• 125000002347 octyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
• 239000008194 pharmaceutical composition Substances 0.000 claims 1
• MFDFERRIHVXMIY-UHFFFAOYSA-N procaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 MFDFERRIHVXMIY-UHFFFAOYSA-N 0.000 claims 1
• 229960004919 procaine Drugs 0.000 claims 1
• 208000016691 refractory malignant neoplasm Diseases 0.000 claims 1
• 238000011476 stem cell transplantation Methods 0.000 claims 1
• 238000007920 subcutaneous administration Methods 0.000 claims 1
• 208000011580 syndromic disease Diseases 0.000 claims 1
• 230000002537 thrombolytic effect Effects 0.000 claims 1