JP2005535608A5 - - Google Patents

Info

Publication number

JP2005535608A5

JP2005535608A5 JP2004510831A JP2004510831A JP2005535608A5 JP 2005535608 A5 JP2005535608 A5 JP 2005535608A5 JP 2004510831 A JP2004510831 A JP 2004510831A JP 2004510831 A JP2004510831 A JP 2004510831A JP 2005535608 A5 JP2005535608 A5 JP 2005535608A5

Authority

JP

Japan

Prior art keywords

combination

administration

epothilone

effect

active ingredient

Prior art date

2003-06-06

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

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• 239000004480 active ingredient Substances 0.000 description 8
• 230000000694 effects Effects 0.000 description 7
• 230000003902 lesion Effects 0.000 description 5
• 150000003883 epothilone derivatives Chemical class 0.000 description 4
• 238000000034 method Methods 0.000 description 4
• 239000000203 mixture Substances 0.000 description 4
• QXRSDHAAWVKZLJ-OXZHEXMSSA-N Epothilone B Natural products O=C1[C@H](C)[C@H](O)[C@@H](C)CCC[C@@]2(C)O[C@H]2C[C@@H](/C(=C\c2nc(C)sc2)/C)OC(=O)C[C@H](O)C1(C)C QXRSDHAAWVKZLJ-OXZHEXMSSA-N 0.000 description 3
• 201000010099 disease Diseases 0.000 description 3
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
• HESCAJZNRMSMJG-HGYUPSKWSA-N epothilone A Natural products O=C1[C@H](C)[C@H](O)[C@H](C)CCC[C@H]2O[C@H]2C[C@@H](/C(=C\c2nc(C)sc2)/C)OC(=O)C[C@H](O)C1(C)C HESCAJZNRMSMJG-HGYUPSKWSA-N 0.000 description 3
• QXRSDHAAWVKZLJ-PVYNADRNSA-N epothilone B Chemical compound C/C([C@@H]1C[C@@H]2O[C@]2(C)CCC[C@@H]([C@@H]([C@@H](C)C(=O)C(C)(C)[C@@H](O)CC(=O)O1)O)C)=C\C1=CSC(C)=N1 QXRSDHAAWVKZLJ-PVYNADRNSA-N 0.000 description 3
• 239000008194 pharmaceutical composition Substances 0.000 description 3
• 238000002360 preparation method Methods 0.000 description 3
• 208000037821 progressive disease Diseases 0.000 description 3
• 230000002195 synergetic effect Effects 0.000 description 3
• 206010012735 Diarrhoea Diseases 0.000 description 2
• 230000001142 anti-diarrhea Effects 0.000 description 2
• 229940125714 antidiarrheal agent Drugs 0.000 description 2
• 239000003793 antidiarrheal agent Substances 0.000 description 2
• 239000002775 capsule Substances 0.000 description 2
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• OROGSEYTTFOCAN-DNJOTXNNSA-N codeine Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)=C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC OROGSEYTTFOCAN-DNJOTXNNSA-N 0.000 description 2
• 150000001875 compounds Chemical class 0.000 description 2
• 238000009472 formulation Methods 0.000 description 2
• 150000003951 lactams Chemical class 0.000 description 2
• RDOIQAHITMMDAJ-UHFFFAOYSA-N loperamide Chemical compound C=1C=CC=CC=1C(C=1C=CC=CC=1)(C(=O)N(C)C)CCN(CC1)CCC1(O)C1=CC=C(Cl)C=C1 RDOIQAHITMMDAJ-UHFFFAOYSA-N 0.000 description 2
• 229960001571 loperamide Drugs 0.000 description 2
• 229940005483 opioid analgesics Drugs 0.000 description 2
• 239000007787 solid Substances 0.000 description 2
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• DEQANNDTNATYII-OULOTJBUSA-N (4r,7s,10s,13r,16s,19r)-10-(4-aminobutyl)-19-[[(2r)-2-amino-3-phenylpropanoyl]amino]-16-benzyl-n-[(2r,3r)-1,3-dihydroxybutan-2-yl]-7-[(1r)-1-hydroxyethyl]-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxa Chemical compound C([C@@H](N)C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC=2C3=CC=CC=C3NC=2)NC(=O)[C@H](CC=2C=CC=CC=2)NC1=O)C(=O)N[C@H](CO)[C@H](O)C)C1=CC=CC=C1 DEQANNDTNATYII-OULOTJBUSA-N 0.000 description 1
• LVRVABPNVHYXRT-BQWXUCBYSA-N 52906-92-0 Chemical compound C([C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(O)=O)C(C)C)C1=CC=CC=C1 LVRVABPNVHYXRT-BQWXUCBYSA-N 0.000 description 1
• 239000005995 Aluminium silicate Substances 0.000 description 1
• 206010006187 Breast cancer Diseases 0.000 description 1
• 208000026310 Breast neoplasm Diseases 0.000 description 1
• 229940121710 HMGCoA reductase inhibitor Drugs 0.000 description 1
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 1
• 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
• 102000002419 Motilin Human genes 0.000 description 1
• 101800002372 Motilin Proteins 0.000 description 1
• 108010016076 Octreotide Proteins 0.000 description 1
• 229920002472 Starch Polymers 0.000 description 1
• 239000013543 active substance Substances 0.000 description 1
• 230000000996 additive effect Effects 0.000 description 1
• 208000037844 advanced solid tumor Diseases 0.000 description 1
• 150000001298 alcohols Chemical class 0.000 description 1
• 125000000217 alkyl group Chemical group 0.000 description 1
• 235000012211 aluminium silicate Nutrition 0.000 description 1
• 239000005557 antagonist Substances 0.000 description 1
• 239000003908 antipruritic agent Substances 0.000 description 1
• YBHILYKTIRIUTE-UHFFFAOYSA-N berberine Chemical compound C1=C2CC[N+]3=CC4=C(OC)C(OC)=CC=C4C=C3C2=CC2=C1OCO2 YBHILYKTIRIUTE-UHFFFAOYSA-N 0.000 description 1
• 229940093265 berberine Drugs 0.000 description 1
• QISXPYZVZJBNDM-UHFFFAOYSA-N berberine Natural products COc1ccc2C=C3N(Cc2c1OC)C=Cc4cc5OCOc5cc34 QISXPYZVZJBNDM-UHFFFAOYSA-N 0.000 description 1
• 239000011230 binding agent Substances 0.000 description 1
• ZREIPSZUJIFJNP-UHFFFAOYSA-K bismuth subsalicylate Chemical compound C1=CC=C2O[Bi](O)OC(=O)C2=C1 ZREIPSZUJIFJNP-UHFFFAOYSA-K 0.000 description 1
• 229960000782 bismuth subsalicylate Drugs 0.000 description 1
• 239000000969 carrier Substances 0.000 description 1
• 229960004126 codeine Drugs 0.000 description 1
• 239000003086 colorant Substances 0.000 description 1
• 238000002648 combination therapy Methods 0.000 description 1
• UFIVBRCCIRTJTN-UHFFFAOYSA-N difenoxin Chemical compound C1CC(C(=O)O)(C=2C=CC=CC=2)CCN1CCC(C#N)(C=1C=CC=CC=1)C1=CC=CC=C1 UFIVBRCCIRTJTN-UHFFFAOYSA-N 0.000 description 1
• 239000003085 diluting agent Substances 0.000 description 1
• 229960004192 diphenoxylate Drugs 0.000 description 1
• HYPPXZBJBPSRLK-UHFFFAOYSA-N diphenoxylate Chemical compound C1CC(C(=O)OCC)(C=2C=CC=CC=2)CCN1CCC(C#N)(C=1C=CC=CC=1)C1=CC=CC=C1 HYPPXZBJBPSRLK-UHFFFAOYSA-N 0.000 description 1
• 230000008034 disappearance Effects 0.000 description 1
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• 239000002552 dosage form Substances 0.000 description 1
• 239000008298 dragée Substances 0.000 description 1
• 230000002708 enhancing effect Effects 0.000 description 1
• 229930013356 epothilone Natural products 0.000 description 1
• 239000000796 flavoring agent Substances 0.000 description 1
• 235000013355 food flavoring agent Nutrition 0.000 description 1
• 150000002334 glycols Chemical class 0.000 description 1
• 239000003979 granulating agent Substances 0.000 description 1
• OROGSEYTTFOCAN-UHFFFAOYSA-N hydrocodone Natural products C1C(N(CCC234)C)C2C=CC(O)C3OC2=C4C1=CC=C2OC OROGSEYTTFOCAN-UHFFFAOYSA-N 0.000 description 1
• 229910052739 hydrogen Inorganic materials 0.000 description 1
• 239000001257 hydrogen Substances 0.000 description 1
• 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 description 1
• 238000000338 in vitro Methods 0.000 description 1
• 238000001727 in vivo Methods 0.000 description 1
• NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 description 1
• 210000003734 kidney Anatomy 0.000 description 1
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• 239000007788 liquid Substances 0.000 description 1
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• 239000000314 lubricant Substances 0.000 description 1
• 229940016286 microcrystalline cellulose Drugs 0.000 description 1
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• 239000000472 muscarinic agonist Substances 0.000 description 1
• 231100000252 nontoxic Toxicity 0.000 description 1
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• 229960002700 octreotide Drugs 0.000 description 1
• 239000003921 oil Substances 0.000 description 1
• 229940127240 opiate Drugs 0.000 description 1
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• 229940069533 paregoric Drugs 0.000 description 1
• 239000008414 paregoric Substances 0.000 description 1
• 238000007911 parenteral administration Methods 0.000 description 1
• 239000001814 pectin Substances 0.000 description 1
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• 229920001277 pectin Polymers 0.000 description 1
• 229940068196 placebo Drugs 0.000 description 1
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• 230000002062 proliferating effect Effects 0.000 description 1
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• 238000005932 reductive alkylation reaction Methods 0.000 description 1
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• 235000019698 starch Nutrition 0.000 description 1
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• 229940098465 tincture Drugs 0.000 description 1
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1