KR20040030808A - 에포틸론 포함 조합물 및 그의 제약 용도 - Google Patents
에포틸론 포함 조합물 및 그의 제약 용도 Download PDFInfo
- Publication number
- KR20040030808A KR20040030808A KR10-2004-7000700A KR20047000700A KR20040030808A KR 20040030808 A KR20040030808 A KR 20040030808A KR 20047000700 A KR20047000700 A KR 20047000700A KR 20040030808 A KR20040030808 A KR 20040030808A
- Authority
- KR
- South Korea
- Prior art keywords
- combination
- formula
- hydrogen
- lower alkyl
- cancer
- Prior art date
- 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.)
- Ceased
Links
- HESCAJZNRMSMJG-KKQRBIROSA-N epothilone A Chemical class C/C([C@@H]1C[C@@H]2O[C@@H]2CCC[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 HESCAJZNRMSMJG-KKQRBIROSA-N 0.000 title description 4
- 229930013356 epothilone Natural products 0.000 title description 3
- 150000001875 compounds Chemical class 0.000 claims abstract description 50
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 43
- 201000010099 disease Diseases 0.000 claims abstract description 35
- 230000002062 proliferating effect Effects 0.000 claims abstract description 31
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 29
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract description 26
- 239000001257 hydrogen Substances 0.000 claims abstract description 26
- 229940122361 Bisphosphonate Drugs 0.000 claims abstract description 19
- 239000004480 active ingredient Substances 0.000 claims abstract description 19
- 150000004663 bisphosphonates Chemical class 0.000 claims abstract description 19
- 239000003814 drug Substances 0.000 claims abstract description 17
- 150000003883 epothilone derivatives Chemical class 0.000 claims abstract description 17
- 150000003839 salts Chemical class 0.000 claims abstract description 16
- 241001465754 Metazoa Species 0.000 claims abstract description 15
- 238000000034 method Methods 0.000 claims abstract description 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract description 13
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract description 13
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 11
- 239000003937 drug carrier Substances 0.000 claims abstract description 9
- 150000003058 platinum compounds Chemical class 0.000 claims abstract description 9
- 238000004519 manufacturing process Methods 0.000 claims abstract description 8
- 206010060862 Prostate cancer Diseases 0.000 claims description 19
- YCOYDOIWSSHVCK-UHFFFAOYSA-N vatalanib Chemical compound C1=CC(Cl)=CC=C1NC(C1=CC=CC=C11)=NN=C1CC1=CC=NC=C1 YCOYDOIWSSHVCK-UHFFFAOYSA-N 0.000 claims description 15
- 229950000578 vatalanib Drugs 0.000 claims description 15
- XRASPMIURGNCCH-UHFFFAOYSA-N zoledronic acid Chemical compound OP(=O)(O)C(P(O)(O)=O)(O)CN1C=CN=C1 XRASPMIURGNCCH-UHFFFAOYSA-N 0.000 claims description 13
- 229960004276 zoledronic acid Drugs 0.000 claims description 12
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 11
- 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 description 9
- 210000000988 bone and bone Anatomy 0.000 claims description 9
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 9
- 229960004562 carboplatin Drugs 0.000 claims description 8
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims description 8
- 208000020816 lung neoplasm Diseases 0.000 claims description 8
- 229960001756 oxaliplatin Drugs 0.000 claims description 8
- DWAFYCQODLXJNR-BNTLRKBRSA-L oxaliplatin Chemical compound O1C(=O)C(=O)O[Pt]11N[C@@H]2CCCC[C@H]2N1 DWAFYCQODLXJNR-BNTLRKBRSA-L 0.000 claims description 8
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 7
- 229960004316 cisplatin Drugs 0.000 claims description 7
- 201000005202 lung cancer Diseases 0.000 claims description 7
- 239000000203 mixture Substances 0.000 claims description 7
- 239000005526 vasoconstrictor agent Substances 0.000 claims description 7
- OGSPWJRAVKPPFI-UHFFFAOYSA-N Alendronic Acid Chemical compound NCCCC(O)(P(O)(O)=O)P(O)(O)=O OGSPWJRAVKPPFI-UHFFFAOYSA-N 0.000 claims description 6
- 206010033128 Ovarian cancer Diseases 0.000 claims description 6
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 6
- DKJJVAGXPKPDRL-UHFFFAOYSA-N Tiludronic acid Chemical compound OP(O)(=O)C(P(O)(O)=O)SC1=CC=C(Cl)C=C1 DKJJVAGXPKPDRL-UHFFFAOYSA-N 0.000 claims description 6
- WRUUGTRCQOWXEG-UHFFFAOYSA-N pamidronate Chemical compound NCCC(O)(P(O)(O)=O)P(O)(O)=O WRUUGTRCQOWXEG-UHFFFAOYSA-N 0.000 claims description 6
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 5
- 206010009944 Colon cancer Diseases 0.000 claims description 5
- MPBVHIBUJCELCL-UHFFFAOYSA-N Ibandronate Chemical compound CCCCCN(C)CCC(O)(P(O)(O)=O)P(O)(O)=O MPBVHIBUJCELCL-UHFFFAOYSA-N 0.000 claims description 5
- IIDJRNMFWXDHID-UHFFFAOYSA-N Risedronic acid Chemical compound OP(=O)(O)C(P(O)(O)=O)(O)CC1=CC=CN=C1 IIDJRNMFWXDHID-UHFFFAOYSA-N 0.000 claims description 5
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 5
- 229960004343 alendronic acid Drugs 0.000 claims description 5
- 201000010881 cervical cancer Diseases 0.000 claims description 5
- 208000029742 colonic neoplasm Diseases 0.000 claims description 5
- 238000009472 formulation Methods 0.000 claims description 5
- 229960005236 ibandronic acid Drugs 0.000 claims description 5
- 229960003978 pamidronic acid Drugs 0.000 claims description 5
- 229960005324 tiludronic acid Drugs 0.000 claims description 5
- 206010027476 Metastases Diseases 0.000 claims description 4
- 208000026037 malignant tumor of neck Diseases 0.000 claims description 4
- 230000009401 metastasis Effects 0.000 claims description 4
- 229960000759 risedronic acid Drugs 0.000 claims description 4
- MBJMCOJMDMARNB-UHFFFAOYSA-N O.O.O.O.[Na].[Na].OP(O)(=O)C(Cl)(Cl)P(O)(O)=O Chemical compound O.O.O.O.[Na].[Na].OP(O)(=O)C(Cl)(Cl)P(O)(O)=O MBJMCOJMDMARNB-UHFFFAOYSA-N 0.000 claims description 3
- 229960002286 clodronic acid Drugs 0.000 claims description 3
- 230000003054 hormonal effect Effects 0.000 claims description 2
- 230000002137 anti-vascular effect Effects 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 abstract description 39
- 229940045985 antineoplastic platinum compound Drugs 0.000 abstract description 3
- 210000005166 vasculature Anatomy 0.000 abstract description 2
- 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 32
- 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 31
- 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 31
- 238000011282 treatment Methods 0.000 description 29
- 230000000694 effects Effects 0.000 description 17
- 241000282414 Homo sapiens Species 0.000 description 15
- 241000699660 Mus musculus Species 0.000 description 12
- 238000011580 nude mouse model Methods 0.000 description 12
- 230000009286 beneficial effect Effects 0.000 description 11
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 description 10
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 description 10
- 229940079593 drug Drugs 0.000 description 10
- 241000282412 Homo Species 0.000 description 9
- 238000001802 infusion Methods 0.000 description 9
- 239000002253 acid Substances 0.000 description 8
- 210000004027 cell Anatomy 0.000 description 8
- 238000001990 intravenous administration Methods 0.000 description 8
- 201000001514 prostate carcinoma Diseases 0.000 description 8
- 238000012360 testing method Methods 0.000 description 6
- 230000003442 weekly effect Effects 0.000 description 6
- -1 acryloxy Chemical group 0.000 description 5
- 229940034982 antineoplastic agent Drugs 0.000 description 5
- 239000002246 antineoplastic agent Substances 0.000 description 5
- 238000013461 design Methods 0.000 description 5
- 239000002552 dosage form Substances 0.000 description 5
- 201000001441 melanoma Diseases 0.000 description 5
- 238000002360 preparation method Methods 0.000 description 5
- 239000003981 vehicle Substances 0.000 description 5
- 206010006187 Breast cancer Diseases 0.000 description 4
- 208000026310 Breast neoplasm Diseases 0.000 description 4
- 238000001727 in vivo Methods 0.000 description 4
- 208000024891 symptom Diseases 0.000 description 4
- 241000699666 Mus <mouse, genus> Species 0.000 description 3
- 229940123237 Taxane Drugs 0.000 description 3
- 230000033115 angiogenesis Effects 0.000 description 3
- 239000002775 capsule Substances 0.000 description 3
- 208000035475 disorder Diseases 0.000 description 3
- 239000012467 final product Substances 0.000 description 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 3
- 125000001841 imino group Chemical group [H]N=* 0.000 description 3
- 208000017169 kidney disease Diseases 0.000 description 3
- 206010061289 metastatic neoplasm Diseases 0.000 description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 3
- 230000004048 modification Effects 0.000 description 3
- 238000012986 modification Methods 0.000 description 3
- 238000007911 parenteral administration Methods 0.000 description 3
- 239000000902 placebo Substances 0.000 description 3
- 229940068196 placebo Drugs 0.000 description 3
- 238000009097 single-agent therapy Methods 0.000 description 3
- 230000002195 synergetic effect Effects 0.000 description 3
- 239000003826 tablet Substances 0.000 description 3
- 210000004881 tumor cell Anatomy 0.000 description 3
- 230000004614 tumor growth Effects 0.000 description 3
- NBRQRXRBIHVLGI-OWXODZSWSA-N (4as,5ar,12ar)-1,10,11,12a-tetrahydroxy-3,12-dioxo-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide Chemical compound C1C2=CC=CC(O)=C2C(O)=C(C2=O)[C@@H]1C[C@@H]1[C@@]2(O)C(O)=C(C(=O)N)C(=O)C1 NBRQRXRBIHVLGI-OWXODZSWSA-N 0.000 description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- 208000020084 Bone disease Diseases 0.000 description 2
- 208000007342 Diabetic Nephropathies Diseases 0.000 description 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 description 2
- 206010018364 Glomerulonephritis Diseases 0.000 description 2
- 208000037147 Hypercalcaemia Diseases 0.000 description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 description 2
- 208000034578 Multiple myelomas Diseases 0.000 description 2
- 206010035226 Plasma cell myeloma Diseases 0.000 description 2
- 206010038389 Renal cancer Diseases 0.000 description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 description 2
- 241000534944 Thia Species 0.000 description 2
- 108010053099 Vascular Endothelial Growth Factor Receptor-2 Proteins 0.000 description 2
- 102000009484 Vascular Endothelial Growth Factor Receptors Human genes 0.000 description 2
- 230000009471 action Effects 0.000 description 2
- 125000002947 alkylene group Chemical group 0.000 description 2
- 230000037396 body weight Effects 0.000 description 2
- 201000011510 cancer Diseases 0.000 description 2
- 125000004432 carbon atom Chemical group C* 0.000 description 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 2
- 238000002648 combination therapy Methods 0.000 description 2
- 239000013078 crystal Substances 0.000 description 2
- 208000033679 diabetic kidney disease Diseases 0.000 description 2
- 206010017758 gastric cancer Diseases 0.000 description 2
- 230000012010 growth Effects 0.000 description 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 description 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 description 2
- 230000000148 hypercalcaemia Effects 0.000 description 2
- 208000030915 hypercalcemia disease Diseases 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- 201000010982 kidney cancer Diseases 0.000 description 2
- 150000003951 lactams Chemical class 0.000 description 2
- 239000003475 metalloproteinase inhibitor Substances 0.000 description 2
- 230000001394 metastastic effect Effects 0.000 description 2
- 239000003607 modifier Substances 0.000 description 2
- 239000000825 pharmaceutical preparation Substances 0.000 description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 2
- 238000011160 research Methods 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 239000012453 solvate Substances 0.000 description 2
- 201000011549 stomach cancer Diseases 0.000 description 2
- DKPFODGZWDEEBT-QFIAKTPHSA-N taxane Chemical class C([C@]1(C)CCC[C@@H](C)[C@H]1C1)C[C@H]2[C@H](C)CC[C@@H]1C2(C)C DKPFODGZWDEEBT-QFIAKTPHSA-N 0.000 description 2
- RCINICONZNJXQF-XAZOAEDWSA-N taxol® Chemical compound O([C@@H]1[C@@]2(CC(C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3(C21)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-XAZOAEDWSA-N 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 210000002303 tibia Anatomy 0.000 description 2
- GTXSRFUZSLTDFX-HRCADAONSA-N (2s)-n-[(2s)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]-4-methyl-2-[[(2s)-2-sulfanyl-4-(3,4,4-trimethyl-2,5-dioxoimidazolidin-1-yl)butanoyl]amino]pentanamide Chemical compound CNC(=O)[C@H](C(C)(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](S)CCN1C(=O)N(C)C(C)(C)C1=O GTXSRFUZSLTDFX-HRCADAONSA-N 0.000 description 1
- BJHCYTJNPVGSBZ-YXSASFKJSA-N 1-[4-[6-amino-5-[(Z)-methoxyiminomethyl]pyrimidin-4-yl]oxy-2-chlorophenyl]-3-ethylurea Chemical compound CCNC(=O)Nc1ccc(Oc2ncnc(N)c2\C=N/OC)cc1Cl BJHCYTJNPVGSBZ-YXSASFKJSA-N 0.000 description 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 description 1
- SGOOQMRIPALTEL-UHFFFAOYSA-N 4-hydroxy-N,1-dimethyl-2-oxo-N-phenyl-3-quinolinecarboxamide Chemical compound OC=1C2=CC=CC=C2N(C)C(=O)C=1C(=O)N(C)C1=CC=CC=C1 SGOOQMRIPALTEL-UHFFFAOYSA-N 0.000 description 1
- 102400000068 Angiostatin Human genes 0.000 description 1
- 108010079709 Angiostatins Proteins 0.000 description 1
- 206010051113 Arterial restenosis Diseases 0.000 description 1
- 201000001320 Atherosclerosis Diseases 0.000 description 1
- 208000023275 Autoimmune disease Diseases 0.000 description 1
- 206010005003 Bladder cancer Diseases 0.000 description 1
- 208000010392 Bone Fractures Diseases 0.000 description 1
- 208000018084 Bone neoplasm Diseases 0.000 description 1
- 206010006002 Bone pain Diseases 0.000 description 1
- 101100381481 Caenorhabditis elegans baz-2 gene Proteins 0.000 description 1
- 206010007275 Carcinoid tumour Diseases 0.000 description 1
- 206010012689 Diabetic retinopathy Diseases 0.000 description 1
- 206010059866 Drug resistance Diseases 0.000 description 1
- 102400001047 Endostatin Human genes 0.000 description 1
- 108010079505 Endostatins Proteins 0.000 description 1
- BEFZAMRWPCMWFJ-JRBBLYSQSA-N Epothilone C Natural products O=C1[C@H](C)[C@@H](O)[C@@H](C)CCC/C=C\C[C@@H](/C(=C\c2nc(C)sc2)/C)OC(=O)C[C@H](O)C1(C)C BEFZAMRWPCMWFJ-JRBBLYSQSA-N 0.000 description 1
- XOZIUKBZLSUILX-SDMHVBBESA-N Epothilone D Natural products O=C1[C@H](C)[C@@H](O)[C@@H](C)CCC/C(/C)=C/C[C@@H](/C(=C\c2nc(C)sc2)/C)OC(=O)C[C@H](O)C1(C)C XOZIUKBZLSUILX-SDMHVBBESA-N 0.000 description 1
- DBVJJBKOTRCVKF-UHFFFAOYSA-N Etidronic acid Chemical compound OP(=O)(O)C(O)(C)P(O)(O)=O DBVJJBKOTRCVKF-UHFFFAOYSA-N 0.000 description 1
- 206010016654 Fibrosis Diseases 0.000 description 1
- 208000032612 Glial tumor Diseases 0.000 description 1
- 206010018338 Glioma Diseases 0.000 description 1
- LLEUXCDZPQOJMY-AAEUAGOBSA-N Glu-Trp Chemical compound C1=CC=C2C(C[C@H](NC(=O)[C@H](CCC(O)=O)N)C(O)=O)=CNC2=C1 LLEUXCDZPQOJMY-AAEUAGOBSA-N 0.000 description 1
- 208000032759 Hemolytic-Uremic Syndrome Diseases 0.000 description 1
- 206010055171 Hypertensive nephropathy Diseases 0.000 description 1
- 208000007766 Kaposi sarcoma Diseases 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 206010027452 Metastases to bone Diseases 0.000 description 1
- 208000037848 Metastatic bone disease Diseases 0.000 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 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 description 1
- 150000001204 N-oxides Chemical class 0.000 description 1
- 208000003788 Neoplasm Micrometastasis Diseases 0.000 description 1
- MSHZHSPISPJWHW-PVDLLORBSA-N O-(chloroacetylcarbamoyl)fumagillol Chemical compound C([C@H]([C@H]([C@@H]1[C@]2(C)[C@H](O2)CC=C(C)C)OC)OC(=O)NC(=O)CCl)C[C@@]21CO2 MSHZHSPISPJWHW-PVDLLORBSA-N 0.000 description 1
- 229930012538 Paclitaxel Natural products 0.000 description 1
- 208000027067 Paget disease of bone Diseases 0.000 description 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 description 1
- 206010034156 Pathological fracture Diseases 0.000 description 1
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 description 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 description 1
- 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 description 1
- 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 description 1
- 201000004681 Psoriasis Diseases 0.000 description 1
- 101100372762 Rattus norvegicus Flt1 gene Proteins 0.000 description 1
- 208000017442 Retinal disease Diseases 0.000 description 1
- 206010038923 Retinopathy Diseases 0.000 description 1
- 206010041067 Small cell lung cancer Diseases 0.000 description 1
- 206010041549 Spinal cord compression Diseases 0.000 description 1
- 208000005250 Spontaneous Fractures Diseases 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 208000034841 Thrombotic Microangiopathies Diseases 0.000 description 1
- 206010052779 Transplant rejections Diseases 0.000 description 1
- 102000004243 Tubulin Human genes 0.000 description 1
- 108090000704 Tubulin Proteins 0.000 description 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 description 1
- 108091008605 VEGF receptors Proteins 0.000 description 1
- 108010073929 Vascular Endothelial Growth Factor A Proteins 0.000 description 1
- 102000016549 Vascular Endothelial Growth Factor Receptor-2 Human genes 0.000 description 1
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 229940037127 actonel Drugs 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 208000038016 acute inflammation Diseases 0.000 description 1
- 230000006022 acute inflammation Effects 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 206010064930 age-related macular degeneration Diseases 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
- 125000004644 alkyl sulfinyl group Chemical group 0.000 description 1
- 125000004414 alkyl thio group Chemical group 0.000 description 1
- 238000005804 alkylation reaction Methods 0.000 description 1
- 230000000202 analgesic effect Effects 0.000 description 1
- 239000002870 angiogenesis inducing agent Substances 0.000 description 1
- 230000001028 anti-proliverative effect Effects 0.000 description 1
- 230000000259 anti-tumor effect Effects 0.000 description 1
- FZCSTZYAHCUGEM-UHFFFAOYSA-N aspergillomarasmine B Natural products OC(=O)CNC(C(O)=O)CNC(C(O)=O)CC(O)=O FZCSTZYAHCUGEM-UHFFFAOYSA-N 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 208000016738 bone Paget disease Diseases 0.000 description 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 description 1
- 125000001589 carboacyl group Chemical group 0.000 description 1
- 150000001720 carbohydrates Chemical group 0.000 description 1
- 208000002458 carcinoid tumor Diseases 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 239000006285 cell suspension Substances 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 238000002512 chemotherapy Methods 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 229950009003 cilengitide Drugs 0.000 description 1
- AMLYAMJWYAIXIA-VWNVYAMZSA-N cilengitide Chemical compound N1C(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)N(C)C(=O)[C@H]1CC1=CC=CC=C1 AMLYAMJWYAIXIA-VWNVYAMZSA-N 0.000 description 1
- 230000007882 cirrhosis Effects 0.000 description 1
- 208000019425 cirrhosis of liver Diseases 0.000 description 1
- ACSIXWWBWUQEHA-UHFFFAOYSA-N clodronic acid Chemical compound OP(O)(=O)C(Cl)(Cl)P(O)(O)=O ACSIXWWBWUQEHA-UHFFFAOYSA-N 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 238000002425 crystallisation Methods 0.000 description 1
- 230000008025 crystallization Effects 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 230000002074 deregulated effect Effects 0.000 description 1
- BEFZAMRWPCMWFJ-UHFFFAOYSA-N desoxyepothilone A Natural products O1C(=O)CC(O)C(C)(C)C(=O)C(C)C(O)C(C)CCCC=CCC1C(C)=CC1=CSC(C)=N1 BEFZAMRWPCMWFJ-UHFFFAOYSA-N 0.000 description 1
- XOZIUKBZLSUILX-UHFFFAOYSA-N desoxyepothilone B Natural products O1C(=O)CC(O)C(C)(C)C(=O)C(C)C(O)C(C)CCCC(C)=CCC1C(C)=CC1=CSC(C)=N1 XOZIUKBZLSUILX-UHFFFAOYSA-N 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 229960004679 doxorubicin Drugs 0.000 description 1
- 239000008298 dragée Substances 0.000 description 1
- 210000005069 ears Anatomy 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- BEFZAMRWPCMWFJ-QJKGZULSSA-N epothilone C Chemical compound O1C(=O)C[C@H](O)C(C)(C)C(=O)[C@H](C)[C@@H](O)[C@@H](C)CCC\C=C/C[C@H]1C(\C)=C\C1=CSC(C)=N1 BEFZAMRWPCMWFJ-QJKGZULSSA-N 0.000 description 1
- XOZIUKBZLSUILX-GIQCAXHBSA-N epothilone D Chemical compound O1C(=O)C[C@H](O)C(C)(C)C(=O)[C@H](C)[C@@H](O)[C@@H](C)CCC\C(C)=C/C[C@H]1C(\C)=C\C1=CSC(C)=N1 XOZIUKBZLSUILX-GIQCAXHBSA-N 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 230000003176 fibrotic effect Effects 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000013355 food flavoring agent Nutrition 0.000 description 1
- 229940001490 fosamax Drugs 0.000 description 1
- 238000004108 freeze drying Methods 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 230000014509 gene expression Effects 0.000 description 1
- 150000002334 glycols Chemical class 0.000 description 1
- 239000003979 granulating agent Substances 0.000 description 1
- 229910052736 halogen Inorganic materials 0.000 description 1
- 150000002367 halogens Chemical class 0.000 description 1
- 201000010536 head and neck cancer Diseases 0.000 description 1
- 201000002222 hemangioblastoma Diseases 0.000 description 1
- 201000011066 hemangioma Diseases 0.000 description 1
- 150000004677 hydrates Chemical class 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 230000003907 kidney function Effects 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000012669 liquid formulation Substances 0.000 description 1
- 230000003908 liver function Effects 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 208000037841 lung tumor Diseases 0.000 description 1
- 210000001165 lymph node Anatomy 0.000 description 1
- 208000002780 macular degeneration Diseases 0.000 description 1
- 230000003211 malignant effect Effects 0.000 description 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 description 1
- OCSMOTCMPXTDND-OUAUKWLOSA-N marimastat Chemical compound CNC(=O)[C@H](C(C)(C)C)NC(=O)[C@H](CC(C)C)[C@H](O)C(=O)NO OCSMOTCMPXTDND-OUAUKWLOSA-N 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- BMGQWWVMWDBQGC-IIFHNQTCSA-N midostaurin Chemical compound CN([C@H]1[C@H]([C@]2(C)O[C@@H](N3C4=CC=CC=C4C4=C5C(=O)NCC5=C5C6=CC=CC=C6N2C5=C43)C1)OC)C(=O)C1=CC=CC=C1 BMGQWWVMWDBQGC-IIFHNQTCSA-N 0.000 description 1
- 229950010895 midostaurin Drugs 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 230000035772 mutation Effects 0.000 description 1
- 230000017074 necrotic cell death Effects 0.000 description 1
- 230000003227 neuromodulating effect Effects 0.000 description 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 125000004433 nitrogen atom Chemical group N* 0.000 description 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- 230000002018 overexpression Effects 0.000 description 1
- 125000004430 oxygen atom Chemical group O* 0.000 description 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 description 1
- 229960001592 paclitaxel Drugs 0.000 description 1
- 201000002528 pancreatic cancer Diseases 0.000 description 1
- 208000008443 pancreatic carcinoma Diseases 0.000 description 1
- 230000007170 pathology Effects 0.000 description 1
- 229940043138 pentosan polysulfate Drugs 0.000 description 1
- 208000033808 peripheral neuropathy Diseases 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 description 1
- HRGDZIGMBDGFTC-UHFFFAOYSA-N platinum(2+) Chemical compound [Pt+2] HRGDZIGMBDGFTC-UHFFFAOYSA-N 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 238000001959 radiotherapy Methods 0.000 description 1
- 230000008261 resistance mechanism Effects 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
- 229960003522 roquinimex Drugs 0.000 description 1
- 230000019491 signal transduction Effects 0.000 description 1
- 229940112726 skelid Drugs 0.000 description 1
- 208000000587 small cell lung carcinoma Diseases 0.000 description 1
- 150000003384 small molecules Chemical class 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 238000001228 spectrum Methods 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 208000003265 stomatitis Diseases 0.000 description 1
- 125000001424 substituent group Chemical group 0.000 description 1
- 125000000547 substituted alkyl group Chemical group 0.000 description 1
- 125000003107 substituted aryl group Chemical group 0.000 description 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 239000007940 sugar coated tablet Substances 0.000 description 1
- 238000009495 sugar coating Methods 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- FIAFUQMPZJWCLV-UHFFFAOYSA-N suramin Chemical compound OS(=O)(=O)C1=CC(S(O)(=O)=O)=C2C(NC(=O)C3=CC=C(C(=C3)NC(=O)C=3C=C(NC(=O)NC=4C=C(C=CC=4)C(=O)NC=4C(=CC=C(C=4)C(=O)NC=4C5=C(C=C(C=C5C(=CC=4)S(O)(=O)=O)S(O)(=O)=O)S(O)(=O)=O)C)C=CC=3)C)=CC=C(S(O)(=O)=O)C2=C1 FIAFUQMPZJWCLV-UHFFFAOYSA-N 0.000 description 1
- 229960005314 suramin Drugs 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 230000004083 survival effect Effects 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 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 description 1
- 229940063683 taxotere Drugs 0.000 description 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 229960003433 thalidomide Drugs 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000002110 toxicologic effect Effects 0.000 description 1
- 231100000027 toxicology Toxicity 0.000 description 1
- 230000005747 tumor angiogenesis Effects 0.000 description 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 description 1
- 201000005112 urinary bladder cancer Diseases 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
- 230000003639 vasoconstrictive effect Effects 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 230000004580 weight loss Effects 0.000 description 1
- 229940002005 zometa Drugs 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/24—Heavy metals; Compounds thereof
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
- A61K31/663—Compounds having two or more phosphorus acid groups or esters thereof, e.g. clodronic acid, pamidronic acid
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
-
- 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
- A61K31/555—Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/24—Heavy metals; Compounds thereof
- A61K33/243—Platinum; Compounds thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Inorganic Chemistry (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Biomedical Technology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Gastroenterology & Hepatology (AREA)
- Neurosurgery (AREA)
- Neurology (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)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30655901P | 2001-07-19 | 2001-07-19 | |
| US30657101P | 2001-07-19 | 2001-07-19 | |
| US30656001P | 2001-07-19 | 2001-07-19 | |
| US60/306,560 | 2001-07-19 | ||
| US60/306,559 | 2001-07-19 | ||
| US60/306,571 | 2001-07-19 | ||
| PCT/EP2002/008020 WO2003007924A2 (en) | 2001-07-19 | 2002-07-18 | Combinations comprising epothilones and pharmaceutical uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020097006647A Division KR20090040925A (ko) | 2001-07-19 | 2002-07-18 | 에포틸론 포함 조합물 및 그의 제약 용도 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20040030808A true KR20040030808A (ko) | 2004-04-09 |
Family
ID=27405180
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR10-2004-7000700A Ceased KR20040030808A (ko) | 2001-07-19 | 2002-07-18 | 에포틸론 포함 조합물 및 그의 제약 용도 |
| KR1020097006647A Ceased KR20090040925A (ko) | 2001-07-19 | 2002-07-18 | 에포틸론 포함 조합물 및 그의 제약 용도 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020097006647A Ceased KR20090040925A (ko) | 2001-07-19 | 2002-07-18 | 에포틸론 포함 조합물 및 그의 제약 용도 |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US20040235796A1 (https=) |
| EP (2) | EP2210643A3 (https=) |
| JP (2) | JP2005501825A (https=) |
| KR (2) | KR20040030808A (https=) |
| CN (2) | CN1283248C (https=) |
| AU (2) | AU2002328921B2 (https=) |
| BR (1) | BR0211271A (https=) |
| CA (1) | CA2453108A1 (https=) |
| CO (1) | CO5560565A2 (https=) |
| EC (2) | ECSP084948A (https=) |
| HU (1) | HUP0401153A3 (https=) |
| IL (2) | IL159517A0 (https=) |
| MX (1) | MXPA04000567A (https=) |
| NO (1) | NO20040214L (https=) |
| NZ (2) | NZ550174A (https=) |
| PL (1) | PL365030A1 (https=) |
| RU (1) | RU2375058C2 (https=) |
| TW (1) | TWI315982B (https=) |
| WO (1) | WO2003007924A2 (https=) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6867305B2 (en) | 1996-12-03 | 2005-03-15 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| CA2273083C (en) | 1996-12-03 | 2012-09-18 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
| US6204388B1 (en) | 1996-12-03 | 2001-03-20 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| IL157443A0 (en) | 2001-03-14 | 2004-03-28 | Bristol Myers Squibb Co | Pharmaceutical compositions for the treatment of cancer including an epothilone analog and a chemotherapeutic agent |
| TWI315982B (en) * | 2001-07-19 | 2009-10-21 | Novartis Ag | Combinations comprising epothilones and pharmaceutical uses thereof |
| US6921769B2 (en) | 2002-08-23 | 2005-07-26 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| US20050171167A1 (en) * | 2003-11-04 | 2005-08-04 | Haby Thomas A. | Process and formulation containing epothilones and analogs thereof |
| CN101693031A (zh) | 2003-11-18 | 2010-04-14 | 诺瓦提斯公司 | Kit突变形式的抑制剂 |
| US20050215604A1 (en) * | 2004-03-26 | 2005-09-29 | Kosan Biosciences, Inc. | Combination therapies with epothilones and carboplatin |
| EP1640004A1 (en) * | 2004-09-24 | 2006-03-29 | Schering Aktiengesellschaft | Use of epothilones in the treatment of bone metastases and bone tumors or cancers |
| US20060121511A1 (en) | 2004-11-30 | 2006-06-08 | Hyerim Lee | Biomarkers and methods for determining sensitivity to microtubule-stabilizing agents |
| CA2606716C (en) | 2005-05-02 | 2013-07-23 | Novartis Ag | Use of pyrimidylaminobenzamide derivatives for the treatment of systematic mastocytosis |
| CN100384419C (zh) * | 2005-12-02 | 2008-04-30 | 菏泽睿鹰制药集团有限公司 | 一种埃坡霉素缓释植入组合物及应用 |
| US20110300150A1 (en) | 2010-05-18 | 2011-12-08 | Scott Eliasof | Compositions and methods for treatment of autoimmune and other disease |
| RU2478407C1 (ru) * | 2011-09-05 | 2013-04-10 | Федеральное государственное бюджетное учреждение Министерства здравоохранения и социального развития Российской Федерации "Медицинский радиологический научный центр" (ФГБУ МРНЦ Минздравсоцразвития России) | Способ комбинированного лечения местно-распространенного рака желудка |
Family Cites Families (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2409754A (en) * | 1946-10-22 | Method for obtaining hydantoins | ||
| US3475486A (en) * | 1966-09-12 | 1969-10-28 | Monsanto Co | Process for preparing phosphonic acids |
| NL7304882A (https=) | 1972-04-10 | 1973-10-12 | ||
| CH605550A5 (https=) | 1972-06-08 | 1978-09-29 | Research Corp | |
| DE2405254C2 (de) * | 1974-02-04 | 1982-05-27 | Henkel KGaA, 4000 Düsseldorf | Verwendung von 3-Amino-1-Hydroxypropan-1, 1-diphosphonsäure oder ihrer wasserlöslichen Salze bei der Beeinflußung von Calciumstoffwechselstörungen im menschlichen oder tierischen Körper |
| FR2531088B1 (fr) * | 1982-07-29 | 1987-08-28 | Sanofi Sa | Produits anti-inflammatoires derives de l'acide methylenediphosphonique et leur procede de preparation |
| IL77243A (en) * | 1984-12-21 | 1996-11-14 | Procter & Gamble | Pharmaceutical compositions containing geminal diphosphonic acid compounds and certain such novel compounds |
| IT1187828B (it) * | 1985-05-24 | 1987-12-23 | Gentili Ist Spa | Composizione farmaceutica a base di difosfonati per il trattamento dell aretrosi |
| DE3623397A1 (de) * | 1986-07-11 | 1988-01-14 | Boehringer Mannheim Gmbh | Neue diphosphonsaeurederivate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel |
| DE4138042C2 (de) | 1991-11-19 | 1993-10-14 | Biotechnolog Forschung Gmbh | Epothilone, deren Herstellungsverfahren sowie diese Verbindungen enthaltende Mittel |
| FR2694558B1 (fr) * | 1992-08-05 | 1994-10-28 | Sanofi Elf | Monohydrate du sel disodique de l'acide 4-chlorophénylthiométhylène bisphosphonique, sa préparation, les compositions pharmaceutiques en contenant. |
| AU687727B2 (en) | 1992-10-28 | 1998-03-05 | Genentech Inc. | Vascular endothelial cell growth factor antagonists |
| EP0675723A4 (en) | 1992-12-23 | 1998-08-05 | Merck & Co Inc | THERAPY USING BISPHOSPHONATES AND STROGENS TO TREAT AND PREVENT BONE RESORPTION. |
| AU2989695A (en) | 1994-08-08 | 2000-03-07 | Debiopharm S.A. | Pharmaceutically stable oxaliplatinum preparation |
| ATE289199T1 (de) * | 1995-06-06 | 2005-03-15 | Merck & Co Inc | Formulierungen mit dem wasserfreien mononatriumsalz von alendronat und deren verwendung zur behandlung von knochenkrankheiten |
| US5880141A (en) | 1995-06-07 | 1999-03-09 | Sugen, Inc. | Benzylidene-Z-indoline compounds for the treatment of disease |
| JP4183099B2 (ja) * | 1995-11-17 | 2008-11-19 | ゲゼルシャフト・フュア・ビオテヒノロジッシェ・フォルシュング・ミット・ベシュレンクテル・ハフツング（ゲー・ベー・エフ） | エポチロンｃおよびｄ、製造法ならびに組成物 |
| AU716610B2 (en) | 1996-08-30 | 2000-03-02 | Novartis Ag | Method for producing epothilones, and intermediate products obtained during the production process |
| DE19638745C2 (de) | 1996-09-11 | 2001-05-10 | Schering Ag | Monoklonale Antikörper gegen die extrazelluläre Domäne des menschlichen VEGF - Rezeptorproteins (KDR) |
| ES2312695T3 (es) | 1996-11-18 | 2009-03-01 | Gesellschaft Fur Biotechnologische Forschung Mbh (Gbf) | Epotilones e y f. |
| CA2273083C (en) * | 1996-12-03 | 2012-09-18 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
| US6441186B1 (en) | 1996-12-13 | 2002-08-27 | The Scripps Research Institute | Epothilone analogs |
| CO4950519A1 (es) | 1997-02-13 | 2000-09-01 | Novartis Ag | Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion |
| US6605599B1 (en) | 1997-07-08 | 2003-08-12 | Bristol-Myers Squibb Company | Epothilone derivatives |
| TR200002299T2 (tr) * | 1998-02-05 | 2000-11-21 | Novartis Ag | Epotilon kompozisyonları. |
| US6194181B1 (en) | 1998-02-19 | 2001-02-27 | Novartis Ag | Fermentative preparation process for and crystal forms of cytostatics |
| US6302838B1 (en) * | 1998-02-25 | 2001-10-16 | Novartis Ag | Cancer treatment with epothilones |
| CA2322157C (en) | 1998-02-25 | 2012-05-29 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| FR2775187B1 (fr) * | 1998-02-25 | 2003-02-21 | Novartis Ag | Utilisation de l'epothilone b pour la fabrication d'une preparation pharmaceutique antiproliferative et d'une composition comprenant l'epothilone b comme agent antiproliferatif in vivo |
| WO2000000485A1 (de) * | 1998-06-30 | 2000-01-06 | Schering Aktiengesellschaft | Epothilon-derivate, verfahren zu deren herstellung, zwischenprodukte und ihre pharmazeutische verwendung |
| PT1107964E (pt) | 1998-08-11 | 2010-06-11 | Novartis Ag | Derivados de isoquinolina com actividade inibidora da angiogénese |
| DE19845798A1 (de) * | 1998-09-29 | 2000-04-13 | Schering Ag | Verwendung von Neoangiogenese-Markern für Diagnose und Therapie von Tumoren, diese enthaltende Mittel, sowie Verfahren zu deren Herstellung |
| GB9824579D0 (en) | 1998-11-10 | 1999-01-06 | Novartis Ag | Organic compounds |
| UA71587C2 (uk) | 1998-11-10 | 2004-12-15 | Шерінг Акцієнгезелльшафт | Аміди антранілової кислоти та їхнє застосування як лікарських засобів |
| WO2000031247A2 (en) | 1998-11-20 | 2000-06-02 | Kosan Biosciences, Inc. | Recombinant methods and materials for producing epothilone and epothilone derivatives |
| DK1140173T4 (da) | 1998-12-22 | 2013-06-10 | Genentech Inc | Vaskulære endothelcellevækstfaktorantagonister og anvendelser deraf |
| EP1156823B1 (en) | 1999-02-12 | 2008-10-29 | The Scripps Research Institute | Methods for treatment of tumors and metastases using a combination of anti-angiogenic and immuno therapies |
| DE19908760A1 (de) * | 1999-02-18 | 2000-08-24 | Schering Ag | Neue Epothilon-Derivate, Verfahren zu deren Herstellung und ihre pharmazeutische Verwendung |
| CN1660840A (zh) | 1999-03-30 | 2005-08-31 | 诺瓦提斯公司 | 治疗炎性疾病的酞嗪衍生物 |
| GB9907908D0 (en) * | 1999-04-07 | 1999-06-02 | Bataille Regis | Organic compounds |
| KR100763064B1 (ko) * | 1999-05-21 | 2007-10-04 | 노파르티스 아게 | 제약 조성물 및 용도 |
| EP1267888A4 (en) * | 2000-01-04 | 2005-12-28 | Univ California | USE OF LOW DOSE BISPHOSPHONATES TO INHIBIT CARDIAC AND ARTERIAL CALCIFICATION |
| GB0001930D0 (en) | 2000-01-27 | 2000-03-22 | Novartis Ag | Organic compounds |
| PT1254138E (pt) | 2000-02-09 | 2005-09-30 | Novartis Ag | Derivados de piridina que inibem a angiogenese e/ou o receptor de tirosina cinase do vegf |
| IL157443A0 (en) | 2001-03-14 | 2004-03-28 | Bristol Myers Squibb Co | Pharmaceutical compositions for the treatment of cancer including an epothilone analog and a chemotherapeutic agent |
| TWI315982B (en) * | 2001-07-19 | 2009-10-21 | Novartis Ag | Combinations comprising epothilones and pharmaceutical uses thereof |
-
2002
- 2002-07-17 TW TW091115929A patent/TWI315982B/zh not_active IP Right Cessation
- 2002-07-18 CN CNB028144147A patent/CN1283248C/zh not_active Expired - Fee Related
- 2002-07-18 JP JP2003513533A patent/JP2005501825A/ja not_active Withdrawn
- 2002-07-18 CA CA002453108A patent/CA2453108A1/en not_active Abandoned
- 2002-07-18 NZ NZ550174A patent/NZ550174A/en not_active IP Right Cessation
- 2002-07-18 IL IL15951702A patent/IL159517A0/xx unknown
- 2002-07-18 KR KR10-2004-7000700A patent/KR20040030808A/ko not_active Ceased
- 2002-07-18 AU AU2002328921A patent/AU2002328921B2/en not_active Ceased
- 2002-07-18 HU HU0401153A patent/HUP0401153A3/hu unknown
- 2002-07-18 MX MXPA04000567A patent/MXPA04000567A/es active IP Right Grant
- 2002-07-18 PL PL02365030A patent/PL365030A1/xx not_active IP Right Cessation
- 2002-07-18 WO PCT/EP2002/008020 patent/WO2003007924A2/en not_active Ceased
- 2002-07-18 BR BR0211271-0A patent/BR0211271A/pt not_active Application Discontinuation
- 2002-07-18 EP EP10157876A patent/EP2210643A3/en not_active Withdrawn
- 2002-07-18 RU RU2004105144/15A patent/RU2375058C2/ru not_active IP Right Cessation
- 2002-07-18 US US10/484,482 patent/US20040235796A1/en not_active Abandoned
- 2002-07-18 NZ NZ530572A patent/NZ530572A/en not_active IP Right Cessation
- 2002-07-18 KR KR1020097006647A patent/KR20090040925A/ko not_active Ceased
- 2002-07-18 EP EP02764726A patent/EP1412029A2/en not_active Withdrawn
- 2002-07-18 CN CN200910168406A patent/CN101791308A/zh active Pending
-
2003
- 2003-12-22 IL IL159517A patent/IL159517A/en not_active IP Right Cessation
-
2004
- 2004-01-16 NO NO20040214A patent/NO20040214L/no not_active Application Discontinuation
- 2004-02-11 CO CO04011525A patent/CO5560565A2/es not_active Application Discontinuation
-
2005
- 2005-12-20 AU AU2005246964A patent/AU2005246964B2/en not_active Ceased
-
2008
- 2008-01-24 US US12/019,294 patent/US7612052B2/en not_active Expired - Fee Related
- 2008-07-04 EC EC2008004948A patent/ECSP084948A/es unknown
-
2009
- 2009-08-28 US US12/549,947 patent/US8008330B2/en not_active Expired - Fee Related
- 2009-11-19 EC EC2009004948A patent/ECSP094948A/es unknown
-
2010
- 2010-03-01 JP JP2010044000A patent/JP2010159271A/ja active Pending
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US8008330B2 (en) | Combinations comprising epothilones and pharmaceutical uses thereof | |
| RU2508110C2 (ru) | КОМБИНАЦИЯ (А) ИНГИБИТОРА ФОСФОИНОЗИТ-3-КИНАЗЫ И (Б) МОДУЛЯТОРА ПУТИ Ras/Raf/Mek | |
| ZA200307665B (en) | Combination comprising N-{5-[4-(4-methyl-piperazinomethyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine and a chemotherapeutic agent. | |
| AU2002328921A1 (en) | Combinations comprising epothilones and pharmaceutical uses thereof | |
| RU2469721C2 (ru) | Комбинация, включающая комплексон железа и противоопухолевый агент, и ее применение | |
| EP1455823A2 (en) | Anti-t cell immunotoxin fusion protein and its therapeutic use | |
| AU2008203233B2 (en) | Combinations comprising epothilones and pharmaceutical uses thereof | |
| HUP0202120A2 (hu) | Daganatellenes kombináció | |
| ZA200309898B (en) | Combinations comprising epothilones and pharmaceutical use thereof. | |
| US20070219115A1 (en) | Pharmaceutical Uses of Bisphosphonates | |
| JP2007513118A5 (https=) | ||
| CN100355423C (zh) | 用于治疗肿瘤的包含血管抑制化合物和烷化剂的组合 | |
| JP2005507410A (ja) | Ｂｃｒ／ａｂｌキナーゼ活性のＡＴＰ競合的阻害剤とチロホスチンアナログとの組合せ剤 | |
| EP1545534A1 (en) | Use of 4-pyridylmethyl-phthalazine derivatives for the manufacture of a medicament for the treatment of myelodysplastic syndromes | |
| CN1911218A (zh) | 包含埃坡霉素的组合及其药学应用 | |
| MXPA06006278A (en) | Pharmaceutical uses of bisphosphonates |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0105 | International application |
Patent event date: 20040116 Patent event code: PA01051R01D Comment text: International Patent Application |
|
| PG1501 | Laying open of application | ||
| A201 | Request for examination | ||
| PA0201 | Request for examination |
Patent event code: PA02012R01D Patent event date: 20070718 Comment text: Request for Examination of Application |
|
| E902 | Notification of reason for refusal | ||
| PE0902 | Notice of grounds for rejection |
Comment text: Notification of reason for refusal Patent event date: 20080331 Patent event code: PE09021S01D |
|
| AMND | Amendment | ||
| E601 | Decision to refuse application | ||
| PE0601 | Decision on rejection of patent |
Patent event date: 20090212 Comment text: Decision to Refuse Application Patent event code: PE06012S01D Patent event date: 20080331 Comment text: Notification of reason for refusal Patent event code: PE06011S01I |
|
| AMND | Amendment | ||
| J201 | Request for trial against refusal decision | ||
| PJ0201 | Trial against decision of rejection |
Patent event date: 20090316 Comment text: Request for Trial against Decision on Refusal Patent event code: PJ02012R01D Patent event date: 20090212 Comment text: Decision to Refuse Application Patent event code: PJ02011S01I Appeal kind category: Appeal against decision to decline refusal Decision date: 20101206 Appeal identifier: 2009101002371 Request date: 20090316 |
|
| A107 | Divisional application of patent | ||
| PA0104 | Divisional application for international application |
Comment text: Divisional Application for International Patent Patent event code: PA01041R01D Patent event date: 20090331 |
|
| PB0901 | Examination by re-examination before a trial |
Comment text: Amendment to Specification, etc. Patent event date: 20090316 Patent event code: PB09011R02I Comment text: Request for Trial against Decision on Refusal Patent event date: 20090316 Patent event code: PB09011R01I Comment text: Amendment to Specification, etc. Patent event date: 20080930 Patent event code: PB09011R02I |
|
| E801 | Decision on dismissal of amendment | ||
| PE0801 | Dismissal of amendment |
Patent event code: PE08012E01D Comment text: Decision on Dismissal of Amendment Patent event date: 20090515 Patent event code: PE08011R01I Comment text: Amendment to Specification, etc. Patent event date: 20090316 Patent event code: PE08011R01I Comment text: Amendment to Specification, etc. Patent event date: 20080930 |
|
| B601 | Maintenance of original decision after re-examination before a trial | ||
| PB0601 | Maintenance of original decision after re-examination before a trial | ||
| J121 | Written withdrawal of request for trial | ||
| PC1202 | Submission of document of withdrawal before decision of registration |
Comment text: [Withdrawal of Procedure relating to Patent, etc.] Withdrawal (Abandonment) Patent event code: PC12021R01D Patent event date: 20101206 |
|
| PJ1201 | Withdrawal of trial |
Patent event code: PJ12011R01D Patent event date: 20101206 Comment text: Written Withdrawal of Request for Trial Appeal identifier: 2009101002371 Request date: 20090316 Appeal kind category: Appeal against decision to decline refusal Decision date: 20101206 |
|
| WITB | Written withdrawal of application |