JP2010520881A5 - - Google Patents

Info

Publication number

JP2010520881A5

JP2010520881A5 JP2009552899A JP2009552899A JP2010520881A5 JP 2010520881 A5 JP2010520881 A5 JP 2010520881A5 JP 2009552899 A JP2009552899 A JP 2009552899A JP 2009552899 A JP2009552899 A JP 2009552899A JP 2010520881 A5 JP2010520881 A5 JP 2010520881A5

Authority

JP

Japan

Prior art keywords

melanoma

day

treatment

agent according

wild type

Prior art date

2008-03-07

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
• Global Dossier
• Discuss

• 201000001441 melanoma Diseases 0.000 claims description 11
• 150000001875 compounds Chemical class 0.000 claims description 7
• 239000000203 mixture Substances 0.000 claims description 5
• 239000003795 chemical substances by application Substances 0.000 claims 4
• 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 claims 2
• 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 claims 2
• RJURFGZVJUQBHK-UHFFFAOYSA-N actinomycin D Natural products CC1OC(=O)C(C(C)C)N(C)C(=O)CN(C)C(=O)C2CCCN2C(=O)C(C(C)C)NC(=O)C1NC(=O)C1=C(N)C(=O)C(C)=C2OC(C(C)=CC=C3C(=O)NC4C(=O)NC(C(N5CCCC5C(=O)N(C)CC(=O)N(C)C(C(C)C)C(=O)OC4C)=O)C(C)C)=C3N=C21 RJURFGZVJUQBHK-UHFFFAOYSA-N 0.000 claims 2
• 150000003839 salts Chemical class 0.000 claims 2
• FDKXTQMXEQVLRF-ZHACJKMWSA-N (E)-dacarbazine Chemical compound CN(C)\N=N\c1[nH]cnc1C(N)=O FDKXTQMXEQVLRF-ZHACJKMWSA-N 0.000 claims 1
• UEJJHQNACJXSKW-UHFFFAOYSA-N 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione Chemical compound O=C1C2=CC=CC=C2C(=O)N1C1CCC(=O)NC1=O UEJJHQNACJXSKW-UHFFFAOYSA-N 0.000 claims 1
• DLGOEMSEDOSKAD-UHFFFAOYSA-N Carmustine Chemical compound ClCCNC(=O)N(N=O)CCCl DLGOEMSEDOSKAD-UHFFFAOYSA-N 0.000 claims 1
• 206010073140 Clear cell sarcoma of soft tissue Diseases 0.000 claims 1
• 108010092160 Dactinomycin Proteins 0.000 claims 1
• 241000282324 Felis Species 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
• 102100040018 Interferon alpha-2 Human genes 0.000 claims 1
• 108010079944 Interferon-alpha2b Proteins 0.000 claims 1
• 102100020873 Interleukin-2 Human genes 0.000 claims 1
• 108010002350 Interleukin-2 Proteins 0.000 claims 1
• 206010061252 Intraocular melanoma Diseases 0.000 claims 1
• GQYIWUVLTXOXAJ-UHFFFAOYSA-N Lomustine Chemical compound ClCCN(N=O)C(=O)NC1CCCCC1 GQYIWUVLTXOXAJ-UHFFFAOYSA-N 0.000 claims 1
• ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims 1
• 206010029488 Nodular melanoma Diseases 0.000 claims 1
• 229930012538 Paclitaxel Natural products 0.000 claims 1
• BPEGJWRSRHCHSN-UHFFFAOYSA-N Temozolomide Chemical compound O=C1N(C)N=NC2=C(C(N)=O)N=CN21 BPEGJWRSRHCHSN-UHFFFAOYSA-N 0.000 claims 1
• 201000005969 Uveal melanoma Diseases 0.000 claims 1
• JXLYSJRDGCGARV-WWYNWVTFSA-N Vinblastine Natural products O=C(O[C@H]1[C@](O)(C(=O)OC)[C@@H]2N(C)c3c(cc(c(OC)c3)[C@]3(C(=O)OC)c4[nH]c5c(c4CCN4C[C@](O)(CC)C[C@H](C3)C4)cccc5)[C@@]32[C@H]2[C@@]1(CC)C=CCN2CC3)C JXLYSJRDGCGARV-WWYNWVTFSA-N 0.000 claims 1
• RJURFGZVJUQBHK-IIXSONLDSA-N actinomycin D Chemical compound C[C@H]1OC(=O)[C@H](C(C)C)N(C)C(=O)CN(C)C(=O)[C@@H]2CCCN2C(=O)[C@@H](C(C)C)NC(=O)[C@H]1NC(=O)C1=C(N)C(=O)C(C)=C2OC(C(C)=CC=C3C(=O)N[C@@H]4C(=O)N[C@@H](C(N5CCC[C@H]5C(=O)N(C)CC(=O)N(C)[C@@H](C(C)C)C(=O)O[C@@H]4C)=O)C(C)C)=C3N=C21 RJURFGZVJUQBHK-IIXSONLDSA-N 0.000 claims 1
• 239000004480 active ingredient Substances 0.000 claims 1
• 239000002246 antineoplastic agent Substances 0.000 claims 1
• VSRXQHXAPYXROS-UHFFFAOYSA-N azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OC(=O)C1(C(O)=O)CCC1 VSRXQHXAPYXROS-UHFFFAOYSA-N 0.000 claims 1
• 229960004562 carboplatin Drugs 0.000 claims 1
• 229960005243 carmustine Drugs 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
• 201000000292 clear cell sarcoma Diseases 0.000 claims 1
• 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims 1
• 208000030381 cutaneous melanoma Diseases 0.000 claims 1
• 229960003901 dacarbazine Drugs 0.000 claims 1
• 229960000640 dactinomycin Drugs 0.000 claims 1
• 229960003668 docetaxel Drugs 0.000 claims 1
• 239000003814 drug Substances 0.000 claims 1
• -1 hotemustine Chemical compound 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
• 229960004768 irinotecan Drugs 0.000 claims 1
• 150000003893 lactate salts Chemical class 0.000 claims 1
• 229960002247 lomustine Drugs 0.000 claims 1
• HAWPXGHAZFHHAD-UHFFFAOYSA-N mechlorethamine Chemical compound ClCCN(C)CCCl HAWPXGHAZFHHAD-UHFFFAOYSA-N 0.000 claims 1
• 229960004961 mechlorethamine Drugs 0.000 claims 1
• 230000001394 metastastic effect Effects 0.000 claims 1
• 206010061289 metastatic neoplasm Diseases 0.000 claims 1
• 201000003731 mucosal melanoma Diseases 0.000 claims 1
• 201000000032 nodular malignant melanoma Diseases 0.000 claims 1
• 208000016450 non-cutaneous melanoma Diseases 0.000 claims 1
• 201000002575 ocular melanoma Diseases 0.000 claims 1
• 229960001592 paclitaxel Drugs 0.000 claims 1
• 201000003708 skin melanoma Diseases 0.000 claims 1
• 210000004872 soft tissue Anatomy 0.000 claims 1
• 229960001052 streptozocin Drugs 0.000 claims 1
• ZSJLQEPLLKMAKR-GKHCUFPYSA-N streptozocin Chemical compound O=NN(C)C(=O)N[C@H]1[C@@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O ZSJLQEPLLKMAKR-GKHCUFPYSA-N 0.000 claims 1
• RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims 1
• 229960004964 temozolomide Drugs 0.000 claims 1
• 229960003433 thalidomide Drugs 0.000 claims 1
• 229940124597 therapeutic agent Drugs 0.000 claims 1
• 229960003048 vinblastine Drugs 0.000 claims 1
• JXLYSJRDGCGARV-XQKSVPLYSA-N vincaleukoblastine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-XQKSVPLYSA-N 0.000 claims 1
• 238000006243 chemical reaction Methods 0.000 description 10
• HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 9
• LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 8
• 239000007787 solid Substances 0.000 description 4
• 239000000706 filtrate Substances 0.000 description 3
• 239000003921 oil Substances 0.000 description 3
• 235000019198 oils Nutrition 0.000 description 3
• MWLBMGPQZJDFKZ-UHFFFAOYSA-N 23491-48-7 Chemical compound C1CN(C)CCN1C1=CC=C([N+]([O-])=O)C(N)=C1 MWLBMGPQZJDFKZ-UHFFFAOYSA-N 0.000 description 2
• 235000019502 Orange oil Nutrition 0.000 description 2
• 150000004985 diamines Chemical class 0.000 description 2
• ANQVKHGDALCPFZ-UHFFFAOYSA-N ethyl 2-[6-(4-methylpiperazin-1-yl)-1h-benzimidazol-2-yl]acetate Chemical compound C1=C2NC(CC(=O)OCC)=NC2=CC=C1N1CCN(C)CC1 ANQVKHGDALCPFZ-UHFFFAOYSA-N 0.000 description 2
• HYMXUYQKXCHWDC-UHFFFAOYSA-N ethyl 3-ethoxy-3-iminopropanoate;hydrochloride Chemical compound Cl.CCOC(=N)CC(=O)OCC HYMXUYQKXCHWDC-UHFFFAOYSA-N 0.000 description 2
• 238000001914 filtration Methods 0.000 description 2
• 238000004128 high performance liquid chromatography Methods 0.000 description 2
• 239000000463 material Substances 0.000 description 2
• 238000000034 method Methods 0.000 description 2
• 239000010502 orange oil Substances 0.000 description 2
• 239000000843 powder Substances 0.000 description 2
• 239000011541 reaction mixture Substances 0.000 description 2
• 230000035484 reaction time Effects 0.000 description 2
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
• 241000694440 Colpidium aqueous Species 0.000 description 1
• 230000008034 disappearance Effects 0.000 description 1
• 201000010099 disease Diseases 0.000 description 1
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
• 239000012065 filter cake Substances 0.000 description 1
• 230000007935 neutral effect Effects 0.000 description 1
• 239000002244 precipitate Substances 0.000 description 1
• 239000000047 product Substances 0.000 description 1
• 239000000725 suspension Substances 0.000 description 1
• 238000010626 work up procedure Methods 0.000 description 1