NZ543318A - Combined therapy against tumors comprising substituted acryloyl distamycin derivatives, taxanes and/or antimetabolites - Google Patents
Combined therapy against tumors comprising substituted acryloyl distamycin derivatives, taxanes and/or antimetabolitesInfo
- Publication number
- NZ543318A NZ543318A NZ543318A NZ54331801A NZ543318A NZ 543318 A NZ543318 A NZ 543318A NZ 543318 A NZ543318 A NZ 543318A NZ 54331801 A NZ54331801 A NZ 54331801A NZ 543318 A NZ543318 A NZ 543318A
- Authority
- NZ
- New Zealand
- Prior art keywords
- methyl
- amino
- formula
- group
- antimetabolite
- Prior art date
Links
- 229940100197 antimetabolite Drugs 0.000 title claims abstract description 29
- 239000002256 antimetabolite Substances 0.000 title claims abstract description 29
- 230000000340 anti-metabolite Effects 0.000 title claims abstract description 28
- -1 acryloyl distamycin derivatives Chemical class 0.000 title claims description 52
- 206010028980 Neoplasm Diseases 0.000 title claims description 14
- 229940123237 Taxane Drugs 0.000 title claims description 6
- 238000002648 combination therapy Methods 0.000 title claims description 5
- 229940044684 anti-microtubule agent Drugs 0.000 claims abstract description 19
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 18
- UPBAOYRENQEPJO-UHFFFAOYSA-N n-[5-[[5-[(3-amino-3-iminopropyl)carbamoyl]-1-methylpyrrol-3-yl]carbamoyl]-1-methylpyrrol-3-yl]-4-formamido-1-methylpyrrole-2-carboxamide Chemical class CN1C=C(NC=O)C=C1C(=O)NC1=CN(C)C(C(=O)NC2=CN(C)C(C(=O)NCCC(N)=N)=C2)=C1 UPBAOYRENQEPJO-UHFFFAOYSA-N 0.000 claims abstract description 16
- 108010042747 stallimycin Proteins 0.000 claims abstract description 13
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims abstract description 10
- 229910052801 chlorine Chemical group 0.000 claims abstract description 8
- 150000003839 salts Chemical class 0.000 claims abstract description 8
- 229910052794 bromium Inorganic materials 0.000 claims abstract description 7
- 125000001309 chloro group Chemical group Cl* 0.000 claims abstract description 6
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 3
- 239000004480 active ingredient Substances 0.000 claims abstract 2
- 125000001246 bromo group Chemical group Br* 0.000 claims abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 35
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 31
- 229960005277 gemcitabine Drugs 0.000 claims description 14
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims description 14
- 239000003814 drug Substances 0.000 claims description 10
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 9
- IPKHXIAPPAKHTB-UHFFFAOYSA-N 2-[[4-[[4-[[4-[[4-(2-bromoprop-2-enoylamino)-1-methylpyrrole-2-carbonyl]amino]-1-methylpyrrole-2-carbonyl]amino]-1-methylpyrrole-2-carbonyl]amino]-1-methylpyrrole-2-carbonyl]amino]ethyl-(diaminomethylidene)azanium;chloride Chemical compound Cl.C1=C(C(=O)NCCN=C(N)N)N(C)C=C1NC(=O)C1=CC(NC(=O)C=2N(C=C(NC(=O)C=3N(C=C(NC(=O)C(Br)=C)C=3)C)C=2)C)=CN1C IPKHXIAPPAKHTB-UHFFFAOYSA-N 0.000 claims description 8
- 239000001257 hydrogen Substances 0.000 claims description 8
- 229910052739 hydrogen Inorganic materials 0.000 claims description 8
- 238000002360 preparation method Methods 0.000 claims description 8
- 150000001875 compounds Chemical class 0.000 claims description 7
- 125000000623 heterocyclic group Chemical group 0.000 claims description 7
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims description 6
- 229930012538 Paclitaxel Natural products 0.000 claims description 6
- 229960001842 estramustine Drugs 0.000 claims description 6
- FRPJXPJMRWBBIH-RBRWEJTLSA-N estramustine Chemical compound ClCCN(CCCl)C(=O)OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 FRPJXPJMRWBBIH-RBRWEJTLSA-N 0.000 claims description 6
- 229960002949 fluorouracil Drugs 0.000 claims description 6
- 229910052757 nitrogen Inorganic materials 0.000 claims description 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 6
- 229910052760 oxygen Inorganic materials 0.000 claims description 6
- 229960001592 paclitaxel Drugs 0.000 claims description 6
- 229910052717 sulfur Inorganic materials 0.000 claims description 6
- 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 description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 5
- 125000003739 carbamimidoyl group Chemical group C(N)(=N)* 0.000 claims description 5
- 239000003795 chemical substances by application Substances 0.000 claims description 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 5
- 208000032839 leukemia Diseases 0.000 claims description 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 5
- 230000002195 synergetic effect Effects 0.000 claims description 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 4
- 229940122803 Vinca alkaloid Drugs 0.000 claims description 4
- 125000000217 alkyl group Chemical group 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 4
- NDMPLJNOPCLANR-UHFFFAOYSA-N 3,4-dihydroxy-15-(4-hydroxy-18-methoxycarbonyl-5,18-seco-ibogamin-18-yl)-16-methoxy-1-methyl-6,7-didehydro-aspidospermidine-3-carboxylic acid methyl ester Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 NDMPLJNOPCLANR-UHFFFAOYSA-N 0.000 claims description 3
- NMUSYJAQQFHJEW-KVTDHHQDSA-N 5-azacytidine Chemical compound 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 description 3
- GAGWJHPBXLXJQN-UORFTKCHSA-N Capecitabine Chemical compound C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1[C@H]1[C@H](O)[C@H](O)[C@@H](C)O1 GAGWJHPBXLXJQN-UORFTKCHSA-N 0.000 claims description 3
- GAGWJHPBXLXJQN-UHFFFAOYSA-N Capecitabine Natural products C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1C1C(O)C(O)C(C)O1 GAGWJHPBXLXJQN-UHFFFAOYSA-N 0.000 claims description 3
- UHDGCWIWMRVCDJ-CCXZUQQUSA-N Cytarabine Chemical compound O=C1N=C(N)C=CN1[C@H]1[C@@H](O)[C@H](O)[C@@H](CO)O1 UHDGCWIWMRVCDJ-CCXZUQQUSA-N 0.000 claims description 3
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims description 3
- 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 description 3
- IVTVGDXNLFLDRM-HNNXBMFYSA-N Tomudex Chemical compound C=1C=C2NC(C)=NC(=O)C2=CC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)S1 IVTVGDXNLFLDRM-HNNXBMFYSA-N 0.000 claims description 3
- 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 description 3
- 230000003432 anti-folate effect Effects 0.000 claims description 3
- 229940127074 antifolate Drugs 0.000 claims description 3
- 229960002756 azacitidine Drugs 0.000 claims description 3
- 229960004117 capecitabine Drugs 0.000 claims description 3
- 229960000684 cytarabine Drugs 0.000 claims description 3
- UHDGCWIWMRVCDJ-ZAKLUEHWSA-N cytidine Chemical class O=C1N=C(N)C=CN1[C@H]1[C@H](O)[C@@H](O)[C@H](CO)O1 UHDGCWIWMRVCDJ-ZAKLUEHWSA-N 0.000 claims description 3
- 229960003668 docetaxel Drugs 0.000 claims description 3
- 229960000961 floxuridine Drugs 0.000 claims description 3
- ODKNJVUHOIMIIZ-RRKCRQDMSA-N floxuridine Chemical compound C1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C(F)=C1 ODKNJVUHOIMIIZ-RRKCRQDMSA-N 0.000 claims description 3
- 239000004052 folic acid antagonist Substances 0.000 claims description 3
- 125000005842 heteroatom Chemical group 0.000 claims description 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 3
- 239000002502 liposome Substances 0.000 claims description 3
- 239000001301 oxygen Substances 0.000 claims description 3
- 229960004432 raltitrexed Drugs 0.000 claims description 3
- 229920006395 saturated elastomer Polymers 0.000 claims description 3
- 125000004434 sulfur atom Chemical group 0.000 claims description 3
- NOYPYLRCIDNJJB-UHFFFAOYSA-N trimetrexate Chemical compound COC1=C(OC)C(OC)=CC(NCC=2C(=C3C(N)=NC(N)=NC3=CC=2)C)=C1 NOYPYLRCIDNJJB-UHFFFAOYSA-N 0.000 claims description 3
- 229960001099 trimetrexate Drugs 0.000 claims description 3
- 229960003048 vinblastine Drugs 0.000 claims description 3
- 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 description 3
- 229960004528 vincristine Drugs 0.000 claims description 3
- OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 claims description 3
- OGWKCGZFUXNPDA-UHFFFAOYSA-N vincristine Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(OC(C)=O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-UHFFFAOYSA-N 0.000 claims description 3
- 229960004355 vindesine Drugs 0.000 claims description 3
- UGGWPQSBPIFKDZ-KOTLKJBCSA-N vindesine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(N)=O)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1N=C1[C]2C=CC=C1 UGGWPQSBPIFKDZ-KOTLKJBCSA-N 0.000 claims description 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims description 2
- 150000005727 5-fluoropyrimidines Chemical class 0.000 claims description 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 2
- 206010027476 Metastases Diseases 0.000 claims description 2
- 125000003545 alkoxy group Chemical group 0.000 claims description 2
- 210000000481 breast Anatomy 0.000 claims description 2
- 210000001072 colon Anatomy 0.000 claims description 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 2
- 210000003734 kidney Anatomy 0.000 claims description 2
- 210000004185 liver Anatomy 0.000 claims description 2
- 210000004072 lung Anatomy 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- 230000009401 metastasis Effects 0.000 claims description 2
- 230000014399 negative regulation of angiogenesis Effects 0.000 claims description 2
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- 231100000331 toxic Toxicity 0.000 claims description 2
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- 229960002066 vinorelbine Drugs 0.000 claims description 2
- GBABOYUKABKIAF-GHYRFKGUSA-N vinorelbine Chemical compound C1N(CC=2C3=CC=CC=C3NC=22)CC(CC)=C[C@H]1C[C@]2(C(=O)OC)C1=CC([C@]23[C@H]([C@]([C@H](OC(C)=O)[C@]4(CC)C=CCN([C@H]34)CC2)(O)C(=O)OC)N2C)=C2C=C1OC GBABOYUKABKIAF-GHYRFKGUSA-N 0.000 claims description 2
- FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 claims 2
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- 241000699670 Mus sp. Species 0.000 claims 2
- 230000000719 anti-leukaemic effect Effects 0.000 claims 2
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- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims 2
- 230000004083 survival effect Effects 0.000 claims 2
- 229960001674 tegafur Drugs 0.000 claims 2
- WFWLQNSHRPWKFK-ZCFIWIBFSA-N tegafur Chemical compound O=C1NC(=O)C(F)=CN1[C@@H]1OCCC1 WFWLQNSHRPWKFK-ZCFIWIBFSA-N 0.000 claims 2
- 241000699666 Mus <mouse, genus> Species 0.000 claims 1
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- YYZVQYVIRZSNMJ-UHFFFAOYSA-N 1-methylpyrrole-2-carboxamide;hydrochloride Chemical compound Cl.CN1C=CC=C1C(N)=O YYZVQYVIRZSNMJ-UHFFFAOYSA-N 0.000 description 2
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 description 2
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 2
- 230000001946 anti-microtubular Effects 0.000 description 2
- 239000002246 antineoplastic agent Substances 0.000 description 2
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- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 2
- 125000000981 3-amino-3-oxopropyl group Chemical group [H]C([*])([H])C([H])([H])C(=O)N([H])[H] 0.000 description 1
- COVZYZSDYWQREU-UHFFFAOYSA-N Busulfan Chemical compound CS(=O)(=O)OCCCCOS(C)(=O)=O COVZYZSDYWQREU-UHFFFAOYSA-N 0.000 description 1
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- 125000002837 carbocyclic group Chemical group 0.000 description 1
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- SFZULDYEOVSIKM-UHFFFAOYSA-N chembl321317 Chemical compound C1=CC(C(=N)NO)=CC=C1C1=CC=C(C=2C=CC(=CC=2)C(=N)NO)O1 SFZULDYEOVSIKM-UHFFFAOYSA-N 0.000 description 1
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- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 1
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/409—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having four such rings, e.g. porphine derivatives, bilirubin, biliverdine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/475—Quinolines; Isoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
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- A—HUMAN NECESSITIES
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Gastroenterology & Hepatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Epoxy Compounds (AREA)
- Pyrrole Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0015446.8A GB0015446D0 (en) | 2000-06-23 | 2000-06-23 | Combined therapy against tumors comprising substituted acryloyl distamycin derivates,taxanes and/or antimetabolites |
| NZ523001A NZ523001A (en) | 2000-06-23 | 2001-06-20 | Combined therapy against tumors comprising substituted acryloyl distamycin derivatives, taxanes and/or antimetabolites |
Publications (1)
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|---|---|
| NZ543318A true NZ543318A (en) | 2007-11-30 |
Family
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| Application Number | Title | Priority Date | Filing Date |
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| NZ543318A NZ543318A (en) | 2000-06-23 | 2001-06-20 | Combined therapy against tumors comprising substituted acryloyl distamycin derivatives, taxanes and/or antimetabolites |
| NZ523001A NZ523001A (en) | 2000-06-23 | 2001-06-20 | Combined therapy against tumors comprising substituted acryloyl distamycin derivatives, taxanes and/or antimetabolites |
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| Application Number | Title | Priority Date | Filing Date |
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| NZ523001A NZ523001A (en) | 2000-06-23 | 2001-06-20 | Combined therapy against tumors comprising substituted acryloyl distamycin derivatives, taxanes and/or antimetabolites |
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|---|---|
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| EP (2) | EP1889624B1 (enExample) |
| JP (1) | JP2003535874A (enExample) |
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| AT (2) | ATE491457T1 (enExample) |
| AU (2) | AU6755301A (enExample) |
| BR (1) | BR0111814A (enExample) |
| CA (1) | CA2412054A1 (enExample) |
| CZ (1) | CZ20024107A3 (enExample) |
| DE (2) | DE60143681D1 (enExample) |
| EA (1) | EA006709B1 (enExample) |
| EE (1) | EE05359B1 (enExample) |
| ES (1) | ES2317913T3 (enExample) |
| GB (1) | GB0015446D0 (enExample) |
| HK (1) | HK1054506B (enExample) |
| HU (1) | HUP0301334A3 (enExample) |
| IL (2) | IL153178A0 (enExample) |
| MX (1) | MXPA02012165A (enExample) |
| NO (1) | NO329967B1 (enExample) |
| NZ (2) | NZ543318A (enExample) |
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| SK (1) | SK287398B6 (enExample) |
| WO (1) | WO2001097618A2 (enExample) |
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| US20070249651A1 (en) * | 2001-06-20 | 2007-10-25 | Nerviano Medical Sciences S.R.I. | Combined therapy against tumors comprising substituted acryloyl distamycin derivatives and topoisomerase I and II inhibitors |
| MD36Z (ro) * | 2008-12-02 | 2010-01-31 | Василе ЖОВМИР | Metodă de tratament diferenţiat al carcinomului ductal in situ neinvaziv al glandei mamare |
| MD23Z (ro) * | 2008-12-02 | 2010-01-31 | Василе ЖОВМИР | Metodă de tratament diferenţiat al carcinomului lobular in situ neinvaziv al glandei mamare |
| MD35Z (ro) * | 2008-12-02 | 2010-01-31 | Василе ЖОВМИР | Metodă de apreciere a riscului dezvoltării carcinomului neinvaziv in situ al glandei mamare |
| MD24Z (ro) * | 2008-12-02 | 2010-01-31 | Василе ЖОВМИР | Metodă de tratament diferenţiat al carcinomului neinvaziv al glandei mamare |
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| SE468642B (sv) | 1985-07-16 | 1993-02-22 | Erba Farmitalia | Poly-4-aminopyrrol-2-karboxamidoderivat och foerfarande foer deras framstaellning och en farmaceutisk komposition |
| GB8612218D0 (en) | 1986-05-20 | 1986-06-25 | Erba Farmitalia | Site specific alkylating agents |
| DE3768419D1 (de) | 1986-10-07 | 1991-04-11 | Boehringer Biochemia Srl | Pharmazeutische zusammensetzungen mit antineoplastischer wirkung. |
| GB8906709D0 (en) | 1989-03-23 | 1989-05-10 | Creighton Andrew M | Acryloyl substituted pyrrole derivatives |
| JP2919867B2 (ja) | 1989-09-27 | 1999-07-19 | 千寿製薬株式会社 | 抗腫瘍剤 |
| EP1145715A3 (en) * | 1992-07-07 | 2004-05-19 | Sepracor Inc. | Methods of using (-) cisapride for the treatment of gastro-esophageal reflux disease and other disorders |
| US5633274A (en) * | 1993-02-18 | 1997-05-27 | President And Fellows Of Harvard College | Cancer treatments |
| IT1272234B (it) * | 1994-05-02 | 1997-06-16 | Consiglio Nazionale Ricerche | Derivati glutationici delle antracicline e procedimento per ottenerli. |
| GB9416005D0 (en) | 1994-08-08 | 1994-09-28 | Erba Carlo Spa | Peptidic compounds analogous to distamycin a and process for their preparation |
| US5597830A (en) * | 1994-12-20 | 1997-01-28 | Warner-Lambert Company | Combination chemotherapy |
| US5880097A (en) * | 1996-01-04 | 1999-03-09 | Terrapin Techologies, Inc. | Tethered prodrugs |
| JP2000503999A (ja) | 1996-02-02 | 2000-04-04 | フアルマシア・エ・アツプジヨン・エツセ・ピー・アー | ジスタマイシン誘導体、その調製方法、および抗腫瘍および抗ウイルス剤としてのその使用 |
| GB9610079D0 (en) | 1996-05-14 | 1996-07-17 | Pharmacia Spa | Distamycin deriratives process for preparing them and their use as antitumor and antiviral agents |
| GB9615692D0 (en) * | 1996-07-25 | 1996-09-04 | Pharmacia Spa | Acryloyl substituted distamycin derivatives, process for preparing them, and their use as antitumor and antiviral agents |
| GB9623522D0 (en) * | 1996-11-11 | 1997-01-08 | Pharmacia & Upjohn Spa | Benzoheterocycle distamycin derivatives process for preparing them and their use as antitumour and antiviral agents |
| GB9727524D0 (en) * | 1997-12-31 | 1998-02-25 | Pharmacia & Upjohn Spa | Synergistic antitumor composition containing a biologically active ureido compound |
| GB9806689D0 (en) | 1998-03-27 | 1998-05-27 | Pharmacia & Upjohn Spa | Acryloyl derivatives analogous to distamycin,process for preparing them,and their use as antitumour and antiviral agents |
| GB9806692D0 (en) | 1998-03-27 | 1998-05-27 | Pharmacia & Upjohn Spa | Benzoheterocyclic distamycin derivatives, process for preparing them and their use as antitumour agents |
| GB9816653D0 (en) | 1998-07-30 | 1998-09-30 | Pharmacia & Upjohn Spa | Oxidised sulfurated distamycin derivatives process for preparing them and their use as antitumor agents |
| GB9816652D0 (en) | 1998-07-30 | 1998-09-30 | Pharmacia & Upjohn Spa | Sulfurated distamycin derivatives process for preparing them and their use as antitumor agents |
| GB9928703D0 (en) | 1999-12-03 | 2000-02-02 | Pharmacia & Upjohn Spa | Acryloyl peptidic derivatives,process for their preparation and their use as antitumour agents |
| GB0011059D0 (en) * | 2000-05-08 | 2000-06-28 | Pharmacia & Upjohn Spa | Use of substituted acryloyl distamycin derivatives in the treatment of tumours associated with high levels of glutathione |
| US6576612B1 (en) * | 2000-10-02 | 2003-06-10 | Pharmacia Italia S.P.A. | Antitumor therapy comprising distamycin derivatives |
| US6887851B2 (en) * | 2001-09-18 | 2005-05-03 | Bioexpertise, Llc | IGF-binding protein-derived peptide |
| PL373998A1 (en) * | 2002-04-02 | 2005-09-19 | Pharmacia Italia Spa | Combined therapy against tumors comprising substituted acryloyl distamycin derivatives and radiotherapy |
-
2000
- 2000-06-23 GB GBGB0015446.8A patent/GB0015446D0/en not_active Ceased
-
2001
- 2001-06-20 BR BR0111814-5A patent/BR0111814A/pt not_active Application Discontinuation
- 2001-06-20 EP EP07122497A patent/EP1889624B1/en not_active Expired - Lifetime
- 2001-06-20 EA EA200300059A patent/EA006709B1/ru not_active IP Right Cessation
- 2001-06-20 DE DE60143681T patent/DE60143681D1/de not_active Expired - Lifetime
- 2001-06-20 EE EEP200200688A patent/EE05359B1/xx not_active IP Right Cessation
- 2001-06-20 HK HK03106774.6A patent/HK1054506B/zh not_active IP Right Cessation
- 2001-06-20 EP EP01945297A patent/EP1299110B1/en not_active Expired - Lifetime
- 2001-06-20 US US10/297,620 patent/US7642229B2/en not_active Expired - Fee Related
- 2001-06-20 CN CNB018116078A patent/CN100479824C/zh not_active Expired - Fee Related
- 2001-06-20 KR KR1020027017409A patent/KR100861668B1/ko not_active Expired - Fee Related
- 2001-06-20 AU AU6755301A patent/AU6755301A/xx active Pending
- 2001-06-20 MX MXPA02012165A patent/MXPA02012165A/es active IP Right Grant
- 2001-06-20 HU HU0301334A patent/HUP0301334A3/hu unknown
- 2001-06-20 DE DE60136706T patent/DE60136706D1/de not_active Expired - Lifetime
- 2001-06-20 NZ NZ543318A patent/NZ543318A/en unknown
- 2001-06-20 IL IL15317801A patent/IL153178A0/xx unknown
- 2001-06-20 AU AU2001267553A patent/AU2001267553B2/en not_active Ceased
- 2001-06-20 CZ CZ20024107A patent/CZ20024107A3/cs unknown
- 2001-06-20 WO PCT/EP2001/007060 patent/WO2001097618A2/en not_active Ceased
- 2001-06-20 AT AT07122497T patent/ATE491457T1/de not_active IP Right Cessation
- 2001-06-20 ES ES01945297T patent/ES2317913T3/es not_active Expired - Lifetime
- 2001-06-20 PL PL363696A patent/PL200504B1/pl not_active IP Right Cessation
- 2001-06-20 NZ NZ523001A patent/NZ523001A/en unknown
- 2001-06-20 JP JP2002503104A patent/JP2003535874A/ja not_active Withdrawn
- 2001-06-20 AT AT01945297T patent/ATE415165T1/de not_active IP Right Cessation
- 2001-06-20 CA CA002412054A patent/CA2412054A1/en not_active Abandoned
- 2001-06-20 SK SK1829-2002A patent/SK287398B6/sk not_active IP Right Cessation
-
2002
- 2002-11-28 IL IL153178A patent/IL153178A/en not_active IP Right Cessation
- 2002-12-04 ZA ZA200209835A patent/ZA200209835B/xx unknown
- 2002-12-18 NO NO20026076A patent/NO329967B1/no not_active IP Right Cessation
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Legal Events
| Date | Code | Title | Description |
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| S23 | Proceedings under section 23: mention of inventor as such in patent |
Inventor name: COZZI, PAOLO Inventor name: GERONI, MARIA CRISTINA ROSA Inventor name: BERIA, ITALO |
|
| PSEA | Patent sealed | ||
| RENW | Renewal (renewal fees accepted) |