JP2016216465A5 - - Google Patents

Info

Publication number

JP2016216465A5

JP2016216465A5 JP2016114725A JP2016114725A JP2016216465A5 JP 2016216465 A5 JP2016216465 A5 JP 2016216465A5 JP 2016114725 A JP2016114725 A JP 2016114725A JP 2016114725 A JP2016114725 A JP 2016114725A JP 2016216465 A5 JP2016216465 A5 JP 2016216465A5

Authority

JP

Japan

Prior art keywords

composition

pharmaceutically active

active compound

composition according

polymer

Prior art date

2016-06-08

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.)

Pending

Links

• Espacenet
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• 239000000203 mixture Substances 0.000 claims 25
• 150000001875 compounds Chemical class 0.000 claims 17
• 229920000642 polymer Polymers 0.000 claims 10
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 7
• 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 6
• 239000011159 matrix material Substances 0.000 claims 5
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
• 229940127089 cytotoxic agent Drugs 0.000 claims 4
• 239000002254 cytotoxic agent Substances 0.000 claims 4
• 231100000599 cytotoxic agent Toxicity 0.000 claims 4
• 229910052739 hydrogen Inorganic materials 0.000 claims 4
• 239000001257 hydrogen Substances 0.000 claims 4
• 239000004005 microsphere Substances 0.000 claims 4
• 239000000178 monomer Substances 0.000 claims 3
• 229940124638 COX inhibitor Drugs 0.000 claims 2
• AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin 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(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims 2
• 206010028980 Neoplasm Diseases 0.000 claims 2
• 239000004372 Polyvinyl alcohol Substances 0.000 claims 2
• 125000000129 anionic group Chemical group 0.000 claims 2
• 229940045799 anthracyclines and related substance Drugs 0.000 claims 2
• 229910052799 carbon Inorganic materials 0.000 claims 2
• 125000004432 carbon atom Chemical group C* 0.000 claims 2
• 230000003073 embolic effect Effects 0.000 claims 2
• 229910052736 halogen Inorganic materials 0.000 claims 2
• 150000002367 halogens Chemical class 0.000 claims 2
• 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
• 229920002451 polyvinyl alcohol Polymers 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
• BUROJSBIWGDYCN-GAUTUEMISA-N AP 23573 Chemical compound C1C[C@@H](OP(C)(C)=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 BUROJSBIWGDYCN-GAUTUEMISA-N 0.000 claims 1
• KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 claims 1
• 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 1
• HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 claims 1
• ABLZXFCXXLZCGV-UHFFFAOYSA-N Phosphorous acid Chemical class OP(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 claims 1
• CBPNZQVSJQDFBE-FUXHJELOSA-N Temsirolimus Chemical compound C1C[C@@H](OC(=O)C(C)(CO)CO)[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 CBPNZQVSJQDFBE-FUXHJELOSA-N 0.000 claims 1
• 125000002252 acyl group Chemical group 0.000 claims 1
• 125000004423 acyloxy group Chemical group 0.000 claims 1
• 125000003545 alkoxy group Chemical group 0.000 claims 1
• 125000000217 alkyl group Chemical group 0.000 claims 1
• 150000001412 amines Chemical class 0.000 claims 1
• 125000003277 amino group Chemical group 0.000 claims 1
• 150000001450 anions Chemical class 0.000 claims 1
• 229940127093 camptothecin Drugs 0.000 claims 1
• -1 camptothecin compound Chemical class 0.000 claims 1
• 125000002837 carbocyclic group Chemical group 0.000 claims 1
• 150000004649 carbonic acid derivatives Chemical class 0.000 claims 1
• 150000007942 carboxylates Chemical class 0.000 claims 1
• 125000002091 cationic group Chemical group 0.000 claims 1
• 230000000295 complement effect Effects 0.000 claims 1
• 239000003431 cross linking reagent Substances 0.000 claims 1
• 239000008367 deionised water Substances 0.000 claims 1
• 229910021641 deionized water Inorganic materials 0.000 claims 1
• VSJKWCGYPAHWDS-UHFFFAOYSA-N dl-camptothecin Natural products C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)C5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-UHFFFAOYSA-N 0.000 claims 1
• 229960004679 doxorubicin Drugs 0.000 claims 1
• 229960005167 everolimus Drugs 0.000 claims 1
• 125000001153 fluoro group Chemical group F* 0.000 claims 1
• 125000000623 heterocyclic group Chemical group 0.000 claims 1
• 229960001680 ibuprofen Drugs 0.000 claims 1
• 125000003010 ionic group Chemical group 0.000 claims 1
• 229960004768 irinotecan Drugs 0.000 claims 1
• 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 1
• 229960001156 mitoxantrone Drugs 0.000 claims 1
• KKZJGLLVHKMTCM-UHFFFAOYSA-N mitoxantrone Chemical group O=C1C2=C(O)C=CC(O)=C2C(=O)C2=C1C(NCCNCCO)=CC=C2NCCNCCO KKZJGLLVHKMTCM-UHFFFAOYSA-N 0.000 claims 1
• 230000007935 neutral effect Effects 0.000 claims 1
• 150000002823 nitrates Chemical class 0.000 claims 1
• 229910052757 nitrogen Inorganic materials 0.000 claims 1
• 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
• 239000008194 pharmaceutical composition Substances 0.000 claims 1
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
• 150000003016 phosphoric acids Chemical class 0.000 claims 1
• 239000002244 precipitate Substances 0.000 claims 1
• 238000010526 radical polymerization reaction Methods 0.000 claims 1
• 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 1
• 150000003839 salts Chemical class 0.000 claims 1
• 229960002930 sirolimus Drugs 0.000 claims 1
• 150000003871 sulfonates Chemical class 0.000 claims 1
• 150000003467 sulfuric acid derivatives Chemical class 0.000 claims 1
• 229960000235 temsirolimus Drugs 0.000 claims 1
• QFJCIRLUMZQUOT-UHFFFAOYSA-N temsirolimus Natural products C1CC(O)C(OC)CC1CC(C)C1OC(=O)C2CCCCN2C(=O)C(=O)C(O)(O2)C(C)CCC2CC(OC)C(C)=CC=CC=CC(C)CC(C)C(=O)C(OC)C(O)C(C)=CC(C)C(=O)C1 QFJCIRLUMZQUOT-UHFFFAOYSA-N 0.000 claims 1
• 238000002560 therapeutic procedure Methods 0.000 claims 1
• YYSFXUWWPNHNAZ-PKJQJFMNSA-N umirolimus Chemical compound C1[C@@H](OC)[C@H](OCCOCC)CC[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 YYSFXUWWPNHNAZ-PKJQJFMNSA-N 0.000 claims 1
• CGTADGCBEXYWNE-JUKNQOCSSA-N zotarolimus Chemical compound N1([C@H]2CC[C@@H](C[C@@H](C)[C@H]3OC(=O)[C@@H]4CCCCN4C(=O)C(=O)[C@@]4(O)[C@H](C)CC[C@H](O4)C[C@@H](/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)C3)OC)C[C@H]2OC)C=NN=N1 CGTADGCBEXYWNE-JUKNQOCSSA-N 0.000 claims 1
• 229950009819 zotarolimus Drugs 0.000 claims 1