JP2021107447A5 - - Google Patents

Info

Publication number

JP2021107447A5

JP2021107447A5 JP2021075883A JP2021075883A JP2021107447A5 JP 2021107447 A5 JP2021107447 A5 JP 2021107447A5 JP 2021075883 A JP2021075883 A JP 2021075883A JP 2021075883 A JP2021075883 A JP 2021075883A JP 2021107447 A5 JP2021107447 A5 JP 2021107447A5

Authority

JP

Japan

Prior art keywords

composition

use according

formula

gvhd

group

Prior art date

2021-04-28

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
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• 239000000203 mixture Substances 0.000 claims 35
• 150000001875 compounds Chemical class 0.000 claims 14
• 239000003795 chemical substances by application Substances 0.000 claims 12
• 150000003839 salts Chemical class 0.000 claims 8
• 230000000735 allogeneic effect Effects 0.000 claims 6
• 230000001028 anti-proliverative effect Effects 0.000 claims 6
• 230000003409 anti-rejection Effects 0.000 claims 6
• 229940079593 drug Drugs 0.000 claims 5
• 239000003814 drug Substances 0.000 claims 5
• 241000124008 Mammalia Species 0.000 claims 4
• 238000010322 bone marrow transplantation Methods 0.000 claims 4
• 210000004027 cell Anatomy 0.000 claims 4
• 238000011134 hematopoietic stem cell transplantation Methods 0.000 claims 4
• 239000000825 pharmaceutical preparation Substances 0.000 claims 3
• 229940127557 pharmaceutical product Drugs 0.000 claims 3
• PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
• QJJXYPPXXYFBGM-LFZNUXCKSA-N Tacrolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1\C=C(/C)[C@@H]1[C@H](C)[C@@H](O)CC(=O)[C@H](CC=C)/C=C(C)/C[C@H](C)C[C@H](OC)[C@H]([C@H](C[C@H]2C)OC)O[C@@]2(O)C(=O)C(=O)N2CCCC[C@H]2C(=O)O1 QJJXYPPXXYFBGM-LFZNUXCKSA-N 0.000 claims 2
• 230000001154 acute effect Effects 0.000 claims 2
• 210000002798 bone marrow cell Anatomy 0.000 claims 2
• 229940046731 calcineurin inhibitors Drugs 0.000 claims 2
• 230000001684 chronic effect Effects 0.000 claims 2
• 239000003246 corticosteroid Substances 0.000 claims 2
• 229960001334 corticosteroids Drugs 0.000 claims 2
• 229910052731 fluorine Inorganic materials 0.000 claims 2
• 239000011737 fluorine Substances 0.000 claims 2
• 210000003958 hematopoietic stem cell Anatomy 0.000 claims 2
• 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
• ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims 2
• QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[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 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims 2
• 229960002930 sirolimus Drugs 0.000 claims 2
• 229960001967 tacrolimus Drugs 0.000 claims 2
• QJJXYPPXXYFBGM-SHYZHZOCSA-N tacrolimus Natural products CO[C@H]1C[C@H](CC[C@@H]1O)C=C(C)[C@H]2OC(=O)[C@H]3CCCCN3C(=O)C(=O)[C@@]4(O)O[C@@H]([C@H](C[C@H]4C)OC)[C@@H](C[C@H](C)CC(=C[C@@H](CC=C)C(=O)C[C@H](O)[C@H]2C)C)OC QJJXYPPXXYFBGM-SHYZHZOCSA-N 0.000 claims 2
• 238000002054 transplantation Methods 0.000 claims 2
• 150000001204 N-oxides Chemical class 0.000 claims 1
• 238000009472 formulation Methods 0.000 claims 1
• 238000004519 manufacturing process Methods 0.000 claims 1
• 238000002360 preparation method Methods 0.000 claims 1
• 230000002265 prevention Effects 0.000 claims 1
• 230000006641 stabilisation Effects 0.000 claims 1
• 238000011105 stabilization Methods 0.000 claims 1
• 230000000087 stabilizing effect Effects 0.000 claims 1
• UHIXWXSSDNZPPY-OWOJBTEDSA-N C(COc1cccc(-c2nc(N3)ncc2)c1)/C=C/CCOc1cccc3c1 Chemical compound C(COc1cccc(-c2nc(N3)ncc2)c1)/C=C/CCOc1cccc3c1 UHIXWXSSDNZPPY-OWOJBTEDSA-N 0.000 description 1
• WVCWTIZSQNCNBU-IWQZZHSRSA-N C(COc1cccc(-c2nc(N3)ncc2)c1)/C=C\COc1cccc3c1 Chemical compound C(COc1cccc(-c2nc(N3)ncc2)c1)/C=C\COc1cccc3c1 WVCWTIZSQNCNBU-IWQZZHSRSA-N 0.000 description 1
• MKNXYIWTSQKVRR-ARJAWSKDSA-N CN(CC1)CCN1c(cc1)c(COC/C=C\COCc(cc-2cc3)c3OC)cc1Nc1nccc-2n1 Chemical compound CN(CC1)CCN1c(cc1)c(COC/C=C\COCc(cc-2cc3)c3OC)cc1Nc1nccc-2n1 MKNXYIWTSQKVRR-ARJAWSKDSA-N 0.000 description 1
• AGYXJMYZYFWGOU-YQUAQSPQSA-N CNCCNc(cc1)c(COC/C=C/CCO2)cc1NC/N=C(\C=C/NC)/c1cc2ccc1 Chemical compound CNCCNc(cc1)c(COC/C=C/CCO2)cc1NC/N=C(\C=C/NC)/c1cc2ccc1 AGYXJMYZYFWGOU-YQUAQSPQSA-N 0.000 description 1
• 0 Nc(cc1)cc(COCC=CC*Cc2cc(F)cc(-c3n[n]cc3)c2)c1OCCN1CCCC1 Chemical compound Nc(cc1)cc(COCC=CC*Cc2cc(F)cc(-c3n[n]cc3)c2)c1OCCN1CCCC1 0.000 description 1