AU2014251038A1 - Therapeutic benefit of suboptimally administered chemical compounds - Google Patents
Therapeutic benefit of suboptimally administered chemical compounds Download PDFInfo
- Publication number
- AU2014251038A1 AU2014251038A1 AU2014251038A AU2014251038A AU2014251038A1 AU 2014251038 A1 AU2014251038 A1 AU 2014251038A1 AU 2014251038 A AU2014251038 A AU 2014251038A AU 2014251038 A AU2014251038 A AU 2014251038A AU 2014251038 A1 AU2014251038 A1 AU 2014251038A1
- Authority
- AU
- Australia
- Prior art keywords
- mustard
- alkylating agent
- group
- inhibitors
- drug therapy
- 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.)
- Abandoned
Links
- 230000001225 therapeutic effect Effects 0.000 title claims abstract description 28
- 150000001875 compounds Chemical class 0.000 title claims description 54
- 230000008901 benefit Effects 0.000 title claims description 8
- QKSKPIVNLNLAAV-UHFFFAOYSA-N bis(2-chloroethyl) sulfide Chemical compound ClCCSCCCl QKSKPIVNLNLAAV-UHFFFAOYSA-N 0.000 claims abstract description 364
- 235000003351 Brassica cretica Nutrition 0.000 claims abstract description 358
- 235000003343 Brassica rupestris Nutrition 0.000 claims abstract description 358
- 235000010460 mustard Nutrition 0.000 claims abstract description 358
- 241000219198 Brassica Species 0.000 claims abstract description 357
- 229940100198 alkylating agent Drugs 0.000 claims abstract description 326
- 239000002168 alkylating agent Substances 0.000 claims abstract description 326
- 238000000034 method Methods 0.000 claims abstract description 268
- 239000003814 drug Substances 0.000 claims abstract description 181
- 229940124597 therapeutic agent Drugs 0.000 claims abstract description 141
- IDPUKCWIGUEADI-UHFFFAOYSA-N 5-[bis(2-chloroethyl)amino]uracil Chemical compound ClCCN(CCCl)C1=CNC(=O)NC1=O IDPUKCWIGUEADI-UHFFFAOYSA-N 0.000 claims abstract description 139
- 239000000203 mixture Substances 0.000 claims abstract description 135
- 229960001055 uracil mustard Drugs 0.000 claims abstract description 116
- SHVCSCWHWMSGTE-UHFFFAOYSA-N 6-methyluracil Chemical compound CC1=CC(=O)NC(=O)N1 SHVCSCWHWMSGTE-UHFFFAOYSA-N 0.000 claims abstract description 60
- JKUXMZDHLUUPGG-UHFFFAOYSA-N 6-ethyl-1h-pyrimidine-2,4-dione Chemical compound CCC1=CC(=O)NC(=O)N1 JKUXMZDHLUUPGG-UHFFFAOYSA-N 0.000 claims abstract description 57
- 229940002612 prodrug Drugs 0.000 claims abstract description 47
- 239000000651 prodrug Substances 0.000 claims abstract description 47
- 230000000694 effects Effects 0.000 claims abstract description 45
- 238000002651 drug therapy Methods 0.000 claims description 151
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 132
- 229910052757 nitrogen Inorganic materials 0.000 claims description 130
- 125000001188 haloalkyl group Chemical group 0.000 claims description 107
- OSTGTTZJOCZWJG-UHFFFAOYSA-N nitrosourea Chemical group NC(=O)N=NO OSTGTTZJOCZWJG-UHFFFAOYSA-N 0.000 claims description 105
- 239000003112 inhibitor Substances 0.000 claims description 102
- 239000003795 chemical substances by application Substances 0.000 claims description 72
- 229910052760 oxygen Inorganic materials 0.000 claims description 56
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 55
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 55
- 239000001301 oxygen Substances 0.000 claims description 55
- 230000006872 improvement Effects 0.000 claims description 50
- 238000011282 treatment Methods 0.000 claims description 50
- 125000001424 substituent group Chemical group 0.000 claims description 48
- 206010028980 Neoplasm Diseases 0.000 claims description 38
- 201000010099 disease Diseases 0.000 claims description 35
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 35
- 201000011510 cancer Diseases 0.000 claims description 30
- DFWRZHZPJJAJMX-UHFFFAOYSA-N propanimidamide;hydrochloride Chemical compound Cl.CCC(N)=N DFWRZHZPJJAJMX-UHFFFAOYSA-N 0.000 claims description 29
- 229940079593 drug Drugs 0.000 claims description 27
- IAKHMKGGTNLKSZ-INIZCTEOSA-N (S)-colchicine Chemical compound C1([C@@H](NC(C)=O)CC2)=CC(=O)C(OC)=CC=C1C1=C2C=C(OC)C(OC)=C1OC IAKHMKGGTNLKSZ-INIZCTEOSA-N 0.000 claims description 26
- LGDHWEGQMXIZPI-UHFFFAOYSA-N 3-amino-1h-pyrimidine-2,4-dione Chemical compound NN1C(=O)C=CNC1=O LGDHWEGQMXIZPI-UHFFFAOYSA-N 0.000 claims description 24
- 125000005518 carboxamido group Chemical group 0.000 claims description 24
- ISAKRJDGNUQOIC-UHFFFAOYSA-N Uracil Chemical compound O=C1C=CNC(=O)N1 ISAKRJDGNUQOIC-UHFFFAOYSA-N 0.000 claims description 22
- 230000004048 modification Effects 0.000 claims description 20
- 238000012986 modification Methods 0.000 claims description 20
- -1 bicyclic sulfamides Chemical class 0.000 claims description 19
- 108090000623 proteins and genes Proteins 0.000 claims description 19
- 210000004027 cell Anatomy 0.000 claims description 17
- 239000002552 dosage form Substances 0.000 claims description 17
- 238000002360 preparation method Methods 0.000 claims description 16
- 230000001988 toxicity Effects 0.000 claims description 16
- 231100000419 toxicity Toxicity 0.000 claims description 16
- 230000015572 biosynthetic process Effects 0.000 claims description 14
- 238000012377 drug delivery Methods 0.000 claims description 14
- 229960001338 colchicine Drugs 0.000 claims description 13
- 230000001965 increasing effect Effects 0.000 claims description 13
- 238000007726 management method Methods 0.000 claims description 13
- 239000002904 solvent Substances 0.000 claims description 13
- 238000002560 therapeutic procedure Methods 0.000 claims description 13
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims description 12
- 230000027455 binding Effects 0.000 claims description 12
- 230000002829 reductive effect Effects 0.000 claims description 12
- 150000003839 salts Chemical class 0.000 claims description 12
- ZHSKUOZOLHMKEA-UHFFFAOYSA-N 4-[5-[bis(2-chloroethyl)amino]-1-methylbenzimidazol-2-yl]butanoic acid;hydron;chloride Chemical compound Cl.ClCCN(CCCl)C1=CC=C2N(C)C(CCCC(O)=O)=NC2=C1 ZHSKUOZOLHMKEA-UHFFFAOYSA-N 0.000 claims description 11
- DLGOEMSEDOSKAD-UHFFFAOYSA-N Carmustine Chemical compound ClCCNC(=O)N(N=O)CCCl DLGOEMSEDOSKAD-UHFFFAOYSA-N 0.000 claims description 11
- 239000003085 diluting agent Substances 0.000 claims description 11
- 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 11
- SGDBTWWWUNNDEQ-LBPRGKRZSA-N melphalan Chemical compound OC(=O)[C@@H](N)CC1=CC=C(N(CCCl)CCCl)C=C1 SGDBTWWWUNNDEQ-LBPRGKRZSA-N 0.000 claims description 11
- 230000019491 signal transduction Effects 0.000 claims description 11
- 239000000126 substance Substances 0.000 claims description 11
- IUOVOJHLRFQQNS-UHFFFAOYSA-N 1-(2-chloroethyl)-3-(2-methylsulfonylethyl)-1-nitrosourea Chemical compound CS(=O)(=O)CCNC(=O)N(N=O)CCCl IUOVOJHLRFQQNS-UHFFFAOYSA-N 0.000 claims description 10
- PKUFNWPSFCOSLU-UHFFFAOYSA-N 6-chloro-1h-pyrimidine-2,4-dione Chemical compound ClC1=CC(=O)NC(=O)N1 PKUFNWPSFCOSLU-UHFFFAOYSA-N 0.000 claims description 10
- GQYIWUVLTXOXAJ-UHFFFAOYSA-N Lomustine Chemical compound ClCCN(N=O)C(=O)NC1CCCCC1 GQYIWUVLTXOXAJ-UHFFFAOYSA-N 0.000 claims description 10
- JKMILVOVUWCVPG-UHFFFAOYSA-N n',n'-bis(2-chloroethyl)ethane-1,2-diamine Chemical compound NCCN(CCCl)CCCl JKMILVOVUWCVPG-UHFFFAOYSA-N 0.000 claims description 10
- 229920000642 polymer Polymers 0.000 claims description 10
- 229940035893 uracil Drugs 0.000 claims description 10
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 10
- HZSKRKPZUQECIE-UHFFFAOYSA-N 2-ethoxy-n-[4-[(5-methyl-1,2-oxazol-3-yl)sulfamoyl]phenyl]acetamide Chemical compound C1=CC(NC(=O)COCC)=CC=C1S(=O)(=O)NC1=NOC(C)=C1 HZSKRKPZUQECIE-UHFFFAOYSA-N 0.000 claims description 9
- QNKJFXARIMSDBR-UHFFFAOYSA-N 3-[2-[bis(2-chloroethyl)amino]ethyl]-1,3-diazaspiro[4.5]decane-2,4-dione Chemical compound O=C1N(CCN(CCCl)CCCl)C(=O)NC11CCCCC1 QNKJFXARIMSDBR-UHFFFAOYSA-N 0.000 claims description 9
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims description 9
- HFVNWDWLWUCIHC-GUPDPFMOSA-N Prednimustine Chemical compound O=C([C@@]1(O)CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)[C@@H](O)C[C@@]21C)COC(=O)CCCC1=CC=C(N(CCCl)CCCl)C=C1 HFVNWDWLWUCIHC-GUPDPFMOSA-N 0.000 claims description 9
- AHHFEZNOXOZZQA-ZEBDFXRSSA-N Ranimustine Chemical compound CO[C@H]1O[C@H](CNC(=O)N(CCCl)N=O)[C@@H](O)[C@H](O)[C@H]1O AHHFEZNOXOZZQA-ZEBDFXRSSA-N 0.000 claims description 9
- 238000004458 analytical method Methods 0.000 claims description 9
- 229940126600 bulk drug product Drugs 0.000 claims description 9
- 230000003034 chemosensitisation Effects 0.000 claims description 9
- YAKWPXVTIGTRJH-UHFFFAOYSA-N fotemustine Chemical compound CCOP(=O)(OCC)C(C)NC(=O)N(CCCl)N=O YAKWPXVTIGTRJH-UHFFFAOYSA-N 0.000 claims description 9
- MQXVYODZCMMZEM-ZYUZMQFOSA-N mannomustine Chemical compound ClCCNC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CNCCCl MQXVYODZCMMZEM-ZYUZMQFOSA-N 0.000 claims description 9
- VFEDRRNHLBGPNN-UHFFFAOYSA-N nimustine Chemical compound CC1=NC=C(CNC(=O)N(CCCl)N=O)C(N)=N1 VFEDRRNHLBGPNN-UHFFFAOYSA-N 0.000 claims description 9
- 239000002777 nucleoside Substances 0.000 claims description 9
- 238000004806 packaging method and process Methods 0.000 claims description 9
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims description 8
- 102000004190 Enzymes Human genes 0.000 claims description 8
- 108090000790 Enzymes Proteins 0.000 claims description 8
- 150000002148 esters Chemical class 0.000 claims description 8
- VJJPUSNTGOMMGY-MRVIYFEKSA-N etoposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@H](C)OC[C@H]4O3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 VJJPUSNTGOMMGY-MRVIYFEKSA-N 0.000 claims description 8
- 229960005420 etoposide Drugs 0.000 claims description 8
- 230000003993 interaction Effects 0.000 claims description 8
- 229960001924 melphalan Drugs 0.000 claims description 8
- 238000012544 monitoring process Methods 0.000 claims description 8
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 8
- RJXQSIKBGKVNRT-UHFFFAOYSA-N phosphoramide mustard Chemical compound ClCCN(P(O)(=O)N)CCCl RJXQSIKBGKVNRT-UHFFFAOYSA-N 0.000 claims description 8
- 235000018102 proteins Nutrition 0.000 claims description 8
- 102000004169 proteins and genes Human genes 0.000 claims description 8
- 230000007118 DNA alkylation Effects 0.000 claims description 7
- 206010025323 Lymphomas Diseases 0.000 claims description 7
- 206010033128 Ovarian cancer Diseases 0.000 claims description 7
- 229940122803 Vinca alkaloid Drugs 0.000 claims description 7
- 230000000340 anti-metabolite Effects 0.000 claims description 7
- 230000000692 anti-sense effect Effects 0.000 claims description 7
- 229940100197 antimetabolite Drugs 0.000 claims description 7
- 239000002256 antimetabolite Substances 0.000 claims description 7
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims description 7
- 229960001842 estramustine Drugs 0.000 claims description 7
- 125000003835 nucleoside group Chemical group 0.000 claims description 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 7
- 150000003057 platinum Chemical class 0.000 claims description 7
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 7
- 239000012453 solvate Substances 0.000 claims description 7
- 239000005483 tyrosine kinase inhibitor Substances 0.000 claims description 7
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 claims description 7
- ZTGWXXOUUKHQLW-UHFFFAOYSA-N 1-nitropyrimidine-2,4-dione Chemical compound [O-][N+](=O)N1C=CC(=O)NC1=O ZTGWXXOUUKHQLW-UHFFFAOYSA-N 0.000 claims description 6
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 6
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims description 6
- YTKUWDBFDASYHO-UHFFFAOYSA-N bendamustine Chemical compound ClCCN(CCCl)C1=CC=C2N(C)C(CCCC(O)=O)=NC2=C1 YTKUWDBFDASYHO-UHFFFAOYSA-N 0.000 claims description 6
- 229960002707 bendamustine Drugs 0.000 claims description 6
- 239000000890 drug combination Substances 0.000 claims description 6
- 230000002708 enhancing effect Effects 0.000 claims description 6
- 230000003463 hyperproliferative effect Effects 0.000 claims description 6
- 229950008612 mannomustine Drugs 0.000 claims description 6
- 230000000144 pharmacologic effect Effects 0.000 claims description 6
- 230000005855 radiation Effects 0.000 claims description 6
- 229950006050 spiromustine Drugs 0.000 claims description 6
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims description 5
- CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 claims description 5
- 102000004127 Cytokines Human genes 0.000 claims description 5
- 108090000695 Cytokines Proteins 0.000 claims description 5
- 108010074338 Lymphokines Proteins 0.000 claims description 5
- 102000008072 Lymphokines Human genes 0.000 claims description 5
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims description 5
- 239000002246 antineoplastic agent Substances 0.000 claims description 5
- VSJKWCGYPAHWDS-FQEVSTJZSA-N camptothecin Chemical compound C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-FQEVSTJZSA-N 0.000 claims description 5
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 5
- 229960005243 carmustine Drugs 0.000 claims description 5
- 229960004397 cyclophosphamide Drugs 0.000 claims description 5
- 229960004783 fotemustine Drugs 0.000 claims description 5
- 229960002247 lomustine Drugs 0.000 claims description 5
- 230000007246 mechanism Effects 0.000 claims description 5
- 230000002503 metabolic effect Effects 0.000 claims description 5
- 239000002207 metabolite Substances 0.000 claims description 5
- 201000005962 mycosis fungoides Diseases 0.000 claims description 5
- 229960001420 nimustine Drugs 0.000 claims description 5
- 229960004694 prednimustine Drugs 0.000 claims description 5
- 238000001959 radiotherapy Methods 0.000 claims description 5
- 229960002185 ranimustine Drugs 0.000 claims description 5
- 230000008439 repair process Effects 0.000 claims description 5
- ZIMFQFMUIGMSEQ-UHFFFAOYSA-N 1-hydroxy-5-nitropyrimidine-2,4-dione Chemical compound On1cc([N+]([O-])=O)c(=O)[nH]c1=O ZIMFQFMUIGMSEQ-UHFFFAOYSA-N 0.000 claims description 4
- BXOUFHBYBVNPPU-UHFFFAOYSA-N 5-[bis(2-chloroethyl)aminomethyl]-1,3-dimethylpyrimidine-2,4-dione Chemical compound CN1C=C(CN(CCCl)CCCl)C(=O)N(C)C1=O BXOUFHBYBVNPPU-UHFFFAOYSA-N 0.000 claims description 4
- AVQSJLFYXJNZHI-UHFFFAOYSA-N 5-[bis(2-chloroethyl)aminomethyl]-1-methylpyrimidine-2,4-dione Chemical compound CN1C=C(CN(CCCl)CCCl)C(=O)NC1=O AVQSJLFYXJNZHI-UHFFFAOYSA-N 0.000 claims description 4
- DSNDKLPCPVXPMQ-UHFFFAOYSA-N 5-[bis(2-chloroethyl)aminomethyl]-1h-pyrimidine-2,4-dione Chemical compound ClCCN(CCCl)CC1=CNC(=O)NC1=O DSNDKLPCPVXPMQ-UHFFFAOYSA-N 0.000 claims description 4
- QLCSQGFYPNEMBN-UHFFFAOYSA-N 5-[bis(2-chloroethyl)aminomethyl]-6-methyl-1h-pyrimidine-2,4-dione Chemical compound CC=1NC(=O)NC(=O)C=1CN(CCCl)CCCl QLCSQGFYPNEMBN-UHFFFAOYSA-N 0.000 claims description 4
- AZXCUOMVEXRBFD-UHFFFAOYSA-N 5-[bis(2-chloroethyl)aminomethyl]-6-methyl-2-sulfanylidene-1h-pyrimidin-4-one Chemical compound CC=1NC(=S)NC(=O)C=1CN(CCCl)CCCl AZXCUOMVEXRBFD-UHFFFAOYSA-N 0.000 claims description 4
- XVEFFLYRDVITRB-UHFFFAOYSA-N 5-[bis(2-chloroethyl)aminomethyl]-6-propyl-1h-pyrimidine-2,4-dione Chemical compound CCCC=1NC(=O)NC(=O)C=1CN(CCCl)CCCl XVEFFLYRDVITRB-UHFFFAOYSA-N 0.000 claims description 4
- UPALIKSFLSVKIS-UHFFFAOYSA-N 5-amino-2-[2-(dimethylamino)ethyl]benzo[de]isoquinoline-1,3-dione Chemical class NC1=CC(C(N(CCN(C)C)C2=O)=O)=C3C2=CC=CC3=C1 UPALIKSFLSVKIS-UHFFFAOYSA-N 0.000 claims description 4
- NVKJOXRVEKMMHS-UHFFFAOYSA-N 5-nitro-1,2,4-triazol-3-one Chemical compound [O-][N+](=O)C1=NC(=O)N=N1 NVKJOXRVEKMMHS-UHFFFAOYSA-N 0.000 claims description 4
- JWNSFESVPQPBGS-UHFFFAOYSA-N 5-nitro-1,3-diazinane-2,4-dione Chemical compound [O-][N+](=O)C1CNC(=O)NC1=O JWNSFESVPQPBGS-UHFFFAOYSA-N 0.000 claims description 4
- BUMUBHQTPIIMCO-UHFFFAOYSA-N 5-nitro-1-(4-nitrophenyl)-1,3-diazinane-2,4-dione Chemical compound O=C1NC(=O)C([N+](=O)[O-])CN1C1=CC=C([N+]([O-])=O)C=C1 BUMUBHQTPIIMCO-UHFFFAOYSA-N 0.000 claims description 4
- CYAAFLGWAUCWEF-UHFFFAOYSA-N 5-nitro-1-(4-nitrophenyl)pyrimidine-2,4-dione Chemical compound C1=CC([N+](=O)[O-])=CC=C1N1C(=O)NC(=O)C([N+]([O-])=O)=C1 CYAAFLGWAUCWEF-UHFFFAOYSA-N 0.000 claims description 4
- IMUTYIOWQFQGIC-UHFFFAOYSA-N 6-propyl-1h-pyrimidine-2,4-dione Chemical compound CCCC1=CC(=O)NC(=O)N1 IMUTYIOWQFQGIC-UHFFFAOYSA-N 0.000 claims description 4
- 108010006654 Bleomycin Proteins 0.000 claims description 4
- KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 claims description 4
- 229940123780 DNA topoisomerase I inhibitor Drugs 0.000 claims description 4
- 238000009007 Diagnostic Kit Methods 0.000 claims description 4
- 206010021143 Hypoxia Diseases 0.000 claims description 4
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims description 4
- 239000000365 Topoisomerase I Inhibitor Substances 0.000 claims description 4
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 claims description 4
- 230000009471 action Effects 0.000 claims description 4
- 230000000845 anti-microbial effect Effects 0.000 claims description 4
- 230000006907 apoptotic process Effects 0.000 claims description 4
- 229940127093 camptothecin Drugs 0.000 claims description 4
- VSJKWCGYPAHWDS-UHFFFAOYSA-N dl-camptothecin Natural products C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)C5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-UHFFFAOYSA-N 0.000 claims description 4
- 201000003444 follicular lymphoma Diseases 0.000 claims description 4
- 208000015181 infectious disease Diseases 0.000 claims description 4
- 208000032839 leukemia Diseases 0.000 claims description 4
- 230000004060 metabolic process Effects 0.000 claims description 4
- 230000003285 pharmacodynamic effect Effects 0.000 claims description 4
- 230000009467 reduction Effects 0.000 claims description 4
- 208000029922 reticulum cell sarcoma Diseases 0.000 claims description 4
- 206010065553 Bone marrow failure Diseases 0.000 claims description 3
- 108090000994 Catalytic RNA Proteins 0.000 claims description 3
- 102000053642 Catalytic RNA Human genes 0.000 claims description 3
- 108091023040 Transcription factor Proteins 0.000 claims description 3
- 102000040945 Transcription factor Human genes 0.000 claims description 3
- 208000017733 acquired polycythemia vera Diseases 0.000 claims description 3
- 229960000548 alemtuzumab Drugs 0.000 claims description 3
- OFCNXPDARWKPPY-UHFFFAOYSA-N allopurinol Chemical compound OC1=NC=NC2=C1C=NN2 OFCNXPDARWKPPY-UHFFFAOYSA-N 0.000 claims description 3
- 229960003459 allopurinol Drugs 0.000 claims description 3
- 239000003242 anti bacterial agent Substances 0.000 claims description 3
- 230000000118 anti-neoplastic effect Effects 0.000 claims description 3
- 229960001561 bleomycin Drugs 0.000 claims description 3
- OYVAGSVQBOHSSS-UAPAGMARSA-O bleomycin A2 Chemical compound N([C@H](C(=O)N[C@H](C)[C@@H](O)[C@H](C)C(=O)N[C@@H]([C@H](O)C)C(=O)NCCC=1SC=C(N=1)C=1SC=C(N=1)C(=O)NCCC[S+](C)C)[C@@H](O[C@H]1[C@H]([C@@H](O)[C@H](O)[C@H](CO)O1)O[C@@H]1[C@H]([C@@H](OC(N)=O)[C@H](O)[C@@H](CO)O1)O)C=1N=CNC=1)C(=O)C1=NC([C@H](CC(N)=O)NC[C@H](N)C(N)=O)=NC(N)=C1C OYVAGSVQBOHSSS-UAPAGMARSA-O 0.000 claims description 3
- 210000004369 blood Anatomy 0.000 claims description 3
- 239000008280 blood Substances 0.000 claims description 3
- 229960004679 doxorubicin Drugs 0.000 claims description 3
- 230000007954 hypoxia Effects 0.000 claims description 3
- 201000005296 lung carcinoma Diseases 0.000 claims description 3
- 208000037244 polycythemia vera Diseases 0.000 claims description 3
- 230000001012 protector Effects 0.000 claims description 3
- 239000002534 radiation-sensitizing agent Substances 0.000 claims description 3
- 108091092562 ribozyme Proteins 0.000 claims description 3
- 238000012360 testing method Methods 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
- 229960004528 vincristine Drugs 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
- 208000005045 Interdigitating dendritic cell sarcoma Diseases 0.000 claims description 2
- 206010052178 Lymphocytic lymphoma Diseases 0.000 claims description 2
- 230000033115 angiogenesis Effects 0.000 claims description 2
- JCKYGMPEJWAADB-UHFFFAOYSA-N chlorambucil Chemical compound OC(=O)CCCC1=CC=C(N(CCCl)CCCl)C=C1 JCKYGMPEJWAADB-UHFFFAOYSA-N 0.000 claims description 2
- 229960004630 chlorambucil Drugs 0.000 claims description 2
- 230000002496 gastric effect Effects 0.000 claims description 2
- 230000001394 metastastic effect Effects 0.000 claims description 2
- 206010061289 metastatic neoplasm Diseases 0.000 claims description 2
- OHRURASPPZQGQM-GCCNXGTGSA-N romidepsin Chemical compound O1C(=O)[C@H](C(C)C)NC(=O)C(=C/C)/NC(=O)[C@H]2CSSCC\C=C\[C@@H]1CC(=O)N[C@H](C(C)C)C(=O)N2 OHRURASPPZQGQM-GCCNXGTGSA-N 0.000 claims description 2
- 229960003452 romidepsin Drugs 0.000 claims description 2
- 108010091666 romidepsin Proteins 0.000 claims description 2
- OHRURASPPZQGQM-UHFFFAOYSA-N romidepsin Natural products O1C(=O)C(C(C)C)NC(=O)C(=CC)NC(=O)C2CSSCCC=CC1CC(=O)NC(C(C)C)C(=O)N2 OHRURASPPZQGQM-UHFFFAOYSA-N 0.000 claims description 2
- 238000002054 transplantation Methods 0.000 claims description 2
- 239000003826 tablet Substances 0.000 claims 36
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 claims 18
- DFPAKSUCGFBDDF-UHFFFAOYSA-N Nicotinamide Chemical compound NC(=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-UHFFFAOYSA-N 0.000 claims 16
- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 claims 16
- WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 claims 15
- 108060006633 protein kinase Proteins 0.000 claims 15
- DOUMFZQKYFQNTF-WUTVXBCWSA-N (R)-rosmarinic acid Chemical compound C([C@H](C(=O)O)OC(=O)\C=C\C=1C=C(O)C(O)=CC=1)C1=CC=C(O)C(O)=C1 DOUMFZQKYFQNTF-WUTVXBCWSA-N 0.000 claims 14
- VFLDPWHFBUODDF-FCXRPNKRSA-N curcumin Chemical compound C1=C(O)C(OC)=CC(\C=C\C(=O)CC(=O)\C=C\C=2C=C(OC)C(O)=CC=2)=C1 VFLDPWHFBUODDF-FCXRPNKRSA-N 0.000 claims 14
- 230000014509 gene expression Effects 0.000 claims 14
- 102000001253 Protein Kinase Human genes 0.000 claims 13
- 108090000765 processed proteins & peptides Proteins 0.000 claims 13
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims 12
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 12
- ATHHXGZTWNVVOU-UHFFFAOYSA-N N-methylformamide Chemical compound CNC=O ATHHXGZTWNVVOU-UHFFFAOYSA-N 0.000 claims 12
- 102000004196 processed proteins & peptides Human genes 0.000 claims 12
- 102000001301 EGF receptor Human genes 0.000 claims 10
- 108060006698 EGF receptor Proteins 0.000 claims 10
- 239000002775 capsule Substances 0.000 claims 10
- YBHILYKTIRIUTE-UHFFFAOYSA-N berberine Chemical compound C1=C2CC[N+]3=CC4=C(OC)C(OC)=CC=C4C=C3C2=CC2=C1OCO2 YBHILYKTIRIUTE-UHFFFAOYSA-N 0.000 claims 9
- 229940093265 berberine Drugs 0.000 claims 9
- QISXPYZVZJBNDM-UHFFFAOYSA-N berberine Natural products COc1ccc2C=C3N(Cc2c1OC)C=Cc4cc5OCOc5cc34 QISXPYZVZJBNDM-UHFFFAOYSA-N 0.000 claims 9
- 229920001223 polyethylene glycol Polymers 0.000 claims 9
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 claims 8
- 239000003534 dna topoisomerase inhibitor Substances 0.000 claims 8
- 238000000605 extraction Methods 0.000 claims 8
- ZCOLJUOHXJRHDI-CMWLGVBASA-N genistein 7-O-beta-D-glucoside Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=CC(O)=C2C(=O)C(C=3C=CC(O)=CC=3)=COC2=C1 ZCOLJUOHXJRHDI-CMWLGVBASA-N 0.000 claims 8
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 8
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 8
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 8
- MXWHMTNPTTVWDM-NXOFHUPFSA-N mitoguazone Chemical compound NC(N)=N\N=C(/C)\C=N\N=C(N)N MXWHMTNPTTVWDM-NXOFHUPFSA-N 0.000 claims 8
- 229960003966 nicotinamide Drugs 0.000 claims 8
- 235000005152 nicotinamide Nutrition 0.000 claims 8
- 239000011570 nicotinamide Substances 0.000 claims 8
- 229940044693 topoisomerase inhibitor Drugs 0.000 claims 8
- LPHGQDQBBGAPDZ-UHFFFAOYSA-N Isocaffeine Natural products CN1C(=O)N(C)C(=O)C2=C1N(C)C=N2 LPHGQDQBBGAPDZ-UHFFFAOYSA-N 0.000 claims 7
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 7
- 102000012338 Poly(ADP-ribose) Polymerases Human genes 0.000 claims 7
- 108010061844 Poly(ADP-ribose) Polymerases Proteins 0.000 claims 7
- 229920000776 Poly(Adenosine diphosphate-ribose) polymerase Polymers 0.000 claims 7
- ZZAFFYPNLYCDEP-HNNXBMFYSA-N Rosmarinsaeure Natural products OC(=O)[C@H](Cc1cccc(O)c1O)OC(=O)C=Cc2ccc(O)c(O)c2 ZZAFFYPNLYCDEP-HNNXBMFYSA-N 0.000 claims 7
- 229960001948 caffeine Drugs 0.000 claims 7
- VJEONQKOZGKCAK-UHFFFAOYSA-N caffeine Natural products CN1C(=O)N(C)C(=O)C2=C1C=CN2C VJEONQKOZGKCAK-UHFFFAOYSA-N 0.000 claims 7
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims 7
- 229960004316 cisplatin Drugs 0.000 claims 7
- 229940109262 curcumin Drugs 0.000 claims 7
- 239000004148 curcumin Substances 0.000 claims 7
- 235000012754 curcumin Nutrition 0.000 claims 7
- VFLDPWHFBUODDF-UHFFFAOYSA-N diferuloylmethane Natural products C1=C(O)C(OC)=CC(C=CC(=O)CC(=O)C=CC=2C=C(OC)C(O)=CC=2)=C1 VFLDPWHFBUODDF-UHFFFAOYSA-N 0.000 claims 7
- 235000006539 genistein Nutrition 0.000 claims 7
- 229940045109 genistein Drugs 0.000 claims 7
- TZBJGXHYKVUXJN-UHFFFAOYSA-N genistein Natural products C1=CC(O)=CC=C1C1=COC2=CC(O)=CC(O)=C2C1=O TZBJGXHYKVUXJN-UHFFFAOYSA-N 0.000 claims 7
- 201000005202 lung cancer Diseases 0.000 claims 7
- 208000020816 lung neoplasm Diseases 0.000 claims 7
- 239000002773 nucleotide Substances 0.000 claims 7
- 125000003729 nucleotide group Chemical group 0.000 claims 7
- DOUMFZQKYFQNTF-MRXNPFEDSA-N rosemarinic acid Natural products C([C@H](C(=O)O)OC(=O)C=CC=1C=C(O)C(O)=CC=1)C1=CC=C(O)C(O)=C1 DOUMFZQKYFQNTF-MRXNPFEDSA-N 0.000 claims 7
- TVHVQJFBWRLYOD-UHFFFAOYSA-N rosmarinic acid Natural products OC(=O)C(Cc1ccc(O)c(O)c1)OC(=Cc2ccc(O)c(O)c2)C=O TVHVQJFBWRLYOD-UHFFFAOYSA-N 0.000 claims 7
- 102000008186 Collagen Human genes 0.000 claims 6
- 108010035532 Collagen Proteins 0.000 claims 6
- 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 6
- 239000005517 L01XE01 - Imatinib Substances 0.000 claims 6
- FXHOOIRPVKKKFG-UHFFFAOYSA-N N,N-Dimethylacetamide Chemical compound CN(C)C(C)=O FXHOOIRPVKKKFG-UHFFFAOYSA-N 0.000 claims 6
- 229940127327 Thymidylate Synthetase Inhibitors Drugs 0.000 claims 6
- 230000001062 anti-nausea Effects 0.000 claims 6
- XADJWCRESPGUTB-UHFFFAOYSA-N apigenin Natural products C1=CC(O)=CC=C1C1=CC(=O)C2=CC(O)=C(O)C=C2O1 XADJWCRESPGUTB-UHFFFAOYSA-N 0.000 claims 6
- 235000008714 apigenin Nutrition 0.000 claims 6
- KZNIFHPLKGYRTM-UHFFFAOYSA-N apigenin Chemical compound C1=CC(O)=CC=C1C1=CC(=O)C2=C(O)C=C(O)C=C2O1 KZNIFHPLKGYRTM-UHFFFAOYSA-N 0.000 claims 6
- 229940117893 apigenin Drugs 0.000 claims 6
- 239000011230 binding agent Substances 0.000 claims 6
- 239000011248 coating agent Substances 0.000 claims 6
- 229920001436 collagen Polymers 0.000 claims 6
- 229960000684 cytarabine Drugs 0.000 claims 6
- 229960002949 fluorouracil Drugs 0.000 claims 6
- 238000009472 formulation Methods 0.000 claims 6
- 229960003943 hypromellose Drugs 0.000 claims 6
- KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 claims 6
- 229960002411 imatinib Drugs 0.000 claims 6
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 6
- 229960003539 mitoguazone Drugs 0.000 claims 6
- 230000002018 overexpression Effects 0.000 claims 6
- 235000019445 benzyl alcohol Nutrition 0.000 claims 5
- 230000005764 inhibitory process Effects 0.000 claims 5
- 102000005962 receptors Human genes 0.000 claims 5
- 108020003175 receptors Proteins 0.000 claims 5
- QNOCRUSVMMAKSC-CCEZHUSRSA-N (3e)-1-methyl-3-(2-oxo-1h-indol-3-ylidene)indol-2-one Chemical compound C12=CC=CC=C2N(C)C(=O)\C1=C\1C2=CC=CC=C2NC/1=O QNOCRUSVMMAKSC-CCEZHUSRSA-N 0.000 claims 4
- 229920000623 Cellulose acetate phthalate Polymers 0.000 claims 4
- 229920000858 Cyclodextrin Polymers 0.000 claims 4
- ZBNZXTGUTAYRHI-UHFFFAOYSA-N Dasatinib Chemical compound C=1C(N2CCN(CCO)CC2)=NC(C)=NC=1NC(S1)=NC=C1C(=O)NC1=C(C)C=CC=C1Cl ZBNZXTGUTAYRHI-UHFFFAOYSA-N 0.000 claims 4
- 239000001856 Ethyl cellulose Substances 0.000 claims 4
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims 4
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 4
- 102000003964 Histone deacetylase Human genes 0.000 claims 4
- 108090000353 Histone deacetylase Proteins 0.000 claims 4
- 101000634975 Homo sapiens Tripartite motif-containing protein 29 Proteins 0.000 claims 4
- 239000002067 L01XE06 - Dasatinib Substances 0.000 claims 4
- 239000005536 L01XE08 - Nilotinib Substances 0.000 claims 4
- MWUXSHHQAYIFBG-UHFFFAOYSA-N Nitric oxide Chemical compound O=[N] MWUXSHHQAYIFBG-UHFFFAOYSA-N 0.000 claims 4
- 108700005126 Ornithine decarboxylases Proteins 0.000 claims 4
- 102000052812 Ornithine decarboxylases Human genes 0.000 claims 4
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 4
- 108091000080 Phosphotransferase Proteins 0.000 claims 4
- 239000002202 Polyethylene glycol Substances 0.000 claims 4
- 239000004372 Polyvinyl alcohol Substances 0.000 claims 4
- RADKZDMFGJYCBB-UHFFFAOYSA-N Pyridoxal Chemical compound CC1=NC=C(CO)C(C=O)=C1O RADKZDMFGJYCBB-UHFFFAOYSA-N 0.000 claims 4
- 102100031463 Serine/threonine-protein kinase PLK1 Human genes 0.000 claims 4
- 229920001800 Shellac Polymers 0.000 claims 4
- 102000002689 Toll-like receptor Human genes 0.000 claims 4
- 108020000411 Toll-like receptor Proteins 0.000 claims 4
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims 4
- 230000004075 alteration Effects 0.000 claims 4
- 239000005557 antagonist Substances 0.000 claims 4
- 230000003110 anti-inflammatory effect Effects 0.000 claims 4
- 239000004599 antimicrobial Substances 0.000 claims 4
- 229940034982 antineoplastic agent Drugs 0.000 claims 4
- 229940081734 cellulose acetate phthalate Drugs 0.000 claims 4
- 229960002448 dasatinib Drugs 0.000 claims 4
- 239000008121 dextrose Substances 0.000 claims 4
- 239000000839 emulsion Substances 0.000 claims 4
- 235000019325 ethyl cellulose Nutrition 0.000 claims 4
- 229920001249 ethyl cellulose Polymers 0.000 claims 4
- 239000000499 gel Substances 0.000 claims 4
- HYFHYPWGAURHIV-UHFFFAOYSA-N homoharringtonine Natural products C1=C2CCN3CCCC43C=C(OC)C(OC(=O)C(O)(CCCC(C)(C)O)CC(=O)OC)C4C2=CC2=C1OCO2 HYFHYPWGAURHIV-UHFFFAOYSA-N 0.000 claims 4
- 230000002209 hydrophobic effect Effects 0.000 claims 4
- 229960001438 immunostimulant agent Drugs 0.000 claims 4
- 238000001802 infusion Methods 0.000 claims 4
- AXESYCSCGBQJBL-SZPBEECKSA-N largazole Chemical compound O=C([C@@]1(C)N=C2SC1)N[C@@H](C(C)C)C(=O)O[C@H](/C=C/CCSC(=O)CCCCCCC)CC(=O)NCC1=NC2=CS1 AXESYCSCGBQJBL-SZPBEECKSA-N 0.000 claims 4
- 230000036457 multidrug resistance Effects 0.000 claims 4
- 229960001346 nilotinib Drugs 0.000 claims 4
- HHZIURLSWUIHRB-UHFFFAOYSA-N nilotinib Chemical compound C1=NC(C)=CN1C1=CC(NC(=O)C=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)=CC(C(F)(F)F)=C1 HHZIURLSWUIHRB-UHFFFAOYSA-N 0.000 claims 4
- 229960002230 omacetaxine mepesuccinate Drugs 0.000 claims 4
- HYFHYPWGAURHIV-JFIAXGOJSA-N omacetaxine mepesuccinate Chemical compound C1=C2CCN3CCC[C@]43C=C(OC)[C@@H](OC(=O)[C@@](O)(CCCC(C)(C)O)CC(=O)OC)[C@H]4C2=CC2=C1OCO2 HYFHYPWGAURHIV-JFIAXGOJSA-N 0.000 claims 4
- 239000000816 peptidomimetic Substances 0.000 claims 4
- ZJAOAACCNHFJAH-UHFFFAOYSA-N phosphonoformic acid Chemical compound OC(=O)P(O)(O)=O ZJAOAACCNHFJAH-UHFFFAOYSA-N 0.000 claims 4
- 102000020233 phosphotransferase Human genes 0.000 claims 4
- BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Chemical compound [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 claims 4
- 108010056274 polo-like kinase 1 Proteins 0.000 claims 4
- 239000008389 polyethoxylated castor oil Substances 0.000 claims 4
- 229920002451 polyvinyl alcohol Polymers 0.000 claims 4
- 229940068984 polyvinyl alcohol Drugs 0.000 claims 4
- 210000002307 prostate Anatomy 0.000 claims 4
- 229960004641 rituximab Drugs 0.000 claims 4
- 239000004208 shellac Substances 0.000 claims 4
- 229940113147 shellac Drugs 0.000 claims 4
- 235000013874 shellac Nutrition 0.000 claims 4
- ZLGIYFNHBLSMPS-ATJNOEHPSA-N shellac Chemical compound OCCCCCC(O)C(O)CCCCCCCC(O)=O.C1C23[C@H](C(O)=O)CCC2[C@](C)(CO)[C@@H]1C(C(O)=O)=C[C@@H]3O ZLGIYFNHBLSMPS-ATJNOEHPSA-N 0.000 claims 4
- 239000000454 talc Substances 0.000 claims 4
- 229910052623 talc Inorganic materials 0.000 claims 4
- 229940033134 talc Drugs 0.000 claims 4
- 235000012222 talc Nutrition 0.000 claims 4
- 239000004408 titanium dioxide Substances 0.000 claims 4
- 235000010215 titanium dioxide Nutrition 0.000 claims 4
- 230000000699 topical effect Effects 0.000 claims 4
- 239000008215 water for injection Substances 0.000 claims 4
- 229940124291 BTK inhibitor Drugs 0.000 claims 3
- 101000823298 Homo sapiens Broad substrate specificity ATP-binding cassette transporter ABCG2 Proteins 0.000 claims 3
- GAMYVSCDDLXAQW-AOIWZFSPSA-N Thermopsosid Natural products O(C)c1c(O)ccc(C=2Oc3c(c(O)cc(O[C@H]4[C@H](O)[C@@H](O)[C@H](O)[C@H](CO)O4)c3)C(=O)C=2)c1 GAMYVSCDDLXAQW-AOIWZFSPSA-N 0.000 claims 3
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 claims 3
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 claims 3
- 239000012190 activator Substances 0.000 claims 3
- 238000013270 controlled release Methods 0.000 claims 3
- ZQSIJRDFPHDXIC-UHFFFAOYSA-N daidzein Chemical compound C1=CC(O)=CC=C1C1=COC2=CC(O)=CC=C2C1=O ZQSIJRDFPHDXIC-UHFFFAOYSA-N 0.000 claims 3
- 229930003944 flavone Natural products 0.000 claims 3
- 150000002212 flavone derivatives Chemical class 0.000 claims 3
- 235000011949 flavones Nutrition 0.000 claims 3
- 229930003935 flavonoid Natural products 0.000 claims 3
- 150000002215 flavonoids Chemical class 0.000 claims 3
- 235000017173 flavonoids Nutrition 0.000 claims 3
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims 3
- 239000003022 immunostimulating agent Substances 0.000 claims 3
- 230000003308 immunostimulating effect Effects 0.000 claims 3
- 230000001939 inductive effect Effects 0.000 claims 3
- 230000036210 malignancy Effects 0.000 claims 3
- 230000010534 mechanism of action Effects 0.000 claims 3
- 238000002483 medication Methods 0.000 claims 3
- 239000012730 sustained-release form Substances 0.000 claims 3
- VHBFFQKBGNRLFZ-UHFFFAOYSA-N vitamin p Natural products O1C2=CC=CC=C2C(=O)C=C1C1=CC=CC=C1 VHBFFQKBGNRLFZ-UHFFFAOYSA-N 0.000 claims 3
- WAEXFXRVDQXREF-UHFFFAOYSA-N vorinostat Chemical compound ONC(=O)CCCCCCC(=O)NC1=CC=CC=C1 WAEXFXRVDQXREF-UHFFFAOYSA-N 0.000 claims 3
- 229960000237 vorinostat Drugs 0.000 claims 3
- 230000003442 weekly effect Effects 0.000 claims 3
- FDKXTQMXEQVLRF-ZHACJKMWSA-N (E)-dacarbazine Chemical compound CN(C)\N=N\c1[nH]cnc1C(N)=O FDKXTQMXEQVLRF-ZHACJKMWSA-N 0.000 claims 2
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims 2
- BNZPFJBUHRBLNB-UHFFFAOYSA-N 1-oxido-1,2,4-benzotriazin-1-ium Chemical class C1=CC=C2[N+]([O-])=NC=NC2=C1 BNZPFJBUHRBLNB-UHFFFAOYSA-N 0.000 claims 2
- MQLACMBJVPINKE-UHFFFAOYSA-N 10-[(3-hydroxy-4-methoxyphenyl)methylidene]anthracen-9-one Chemical compound C1=C(O)C(OC)=CC=C1C=C1C2=CC=CC=C2C(=O)C2=CC=CC=C21 MQLACMBJVPINKE-UHFFFAOYSA-N 0.000 claims 2
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 claims 2
- FSPQCTGGIANIJZ-UHFFFAOYSA-N 2-[[(3,4-dimethoxyphenyl)-oxomethyl]amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide Chemical compound C1=C(OC)C(OC)=CC=C1C(=O)NC1=C(C(N)=O)C(CCCC2)=C2S1 FSPQCTGGIANIJZ-UHFFFAOYSA-N 0.000 claims 2
- YZEUHQHUFTYLPH-UHFFFAOYSA-N 2-nitroimidazole Chemical compound [O-][N+](=O)C1=NC=CN1 YZEUHQHUFTYLPH-UHFFFAOYSA-N 0.000 claims 2
- ZZVDXRCAGGQFAK-UHFFFAOYSA-N 2h-oxazaphosphinine Chemical class N1OC=CC=P1 ZZVDXRCAGGQFAK-UHFFFAOYSA-N 0.000 claims 2
- PWMYMKOUNYTVQN-UHFFFAOYSA-N 3-(8,8-diethyl-2-aza-8-germaspiro[4.5]decan-2-yl)-n,n-dimethylpropan-1-amine Chemical compound C1C[Ge](CC)(CC)CCC11CN(CCCN(C)C)CC1 PWMYMKOUNYTVQN-UHFFFAOYSA-N 0.000 claims 2
- MHJBZVSGOZTKRH-IZHYLOQSSA-N 4-Hydroxy-N-desmethyltamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCNC)=CC=1)/C1=CC=C(O)C=C1 MHJBZVSGOZTKRH-IZHYLOQSSA-N 0.000 claims 2
- VVIAGPKUTFNRDU-UHFFFAOYSA-N 6S-folinic acid Natural products C1NC=2NC(N)=NC(=O)C=2N(C=O)C1CNC1=CC=C(C(=O)NC(CCC(O)=O)C(O)=O)C=C1 VVIAGPKUTFNRDU-UHFFFAOYSA-N 0.000 claims 2
- 244000215068 Acacia senegal Species 0.000 claims 2
- 229940121683 Acetylcholine receptor antagonist Drugs 0.000 claims 2
- 102000006772 Acid Ceramidase Human genes 0.000 claims 2
- 108020005296 Acid Ceramidase Proteins 0.000 claims 2
- 229940123786 Adenosine A3 receptor antagonist Drugs 0.000 claims 2
- 108010029445 Agammaglobulinaemia Tyrosine Kinase Proteins 0.000 claims 2
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims 2
- 102100025674 Angiopoietin-related protein 4 Human genes 0.000 claims 2
- 102100021569 Apoptosis regulator Bcl-2 Human genes 0.000 claims 2
- 102000014654 Aromatase Human genes 0.000 claims 2
- 108010078554 Aromatase Proteins 0.000 claims 2
- 102100022718 Atypical chemokine receptor 2 Human genes 0.000 claims 2
- 102100024222 B-lymphocyte antigen CD19 Human genes 0.000 claims 2
- 208000032800 BCR-ABL1 positive blast phase chronic myelogenous leukemia Diseases 0.000 claims 2
- 108091007065 BIRCs Proteins 0.000 claims 2
- 102100026596 Bcl-2-like protein 1 Human genes 0.000 claims 2
- 208000004860 Blast Crisis Diseases 0.000 claims 2
- 102100022595 Broad substrate specificity ATP-binding cassette transporter ABCG2 Human genes 0.000 claims 2
- 102100031650 C-X-C chemokine receptor type 4 Human genes 0.000 claims 2
- 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 2
- 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 2
- 102000014914 Carrier Proteins Human genes 0.000 claims 2
- 102000052052 Casein Kinase II Human genes 0.000 claims 2
- 108010010919 Casein Kinase II Proteins 0.000 claims 2
- 229940121737 Choline kinase inhibitor Drugs 0.000 claims 2
- 101000749287 Clitocybe nebularis Clitocypin Proteins 0.000 claims 2
- 101000767029 Clitocybe nebularis Clitocypin-1 Proteins 0.000 claims 2
- 229920002261 Corn starch Polymers 0.000 claims 2
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 2
- 239000004971 Cross linker Substances 0.000 claims 2
- 101710095468 Cyclase Proteins 0.000 claims 2
- 102000008130 Cyclic AMP-Dependent Protein Kinases Human genes 0.000 claims 2
- 108010049894 Cyclic AMP-Dependent Protein Kinases Proteins 0.000 claims 2
- 108090000266 Cyclin-dependent kinases Proteins 0.000 claims 2
- 102000003903 Cyclin-dependent kinases Human genes 0.000 claims 2
- 229940094664 Cysteine protease inhibitor Drugs 0.000 claims 2
- 102100033189 Diablo IAP-binding mitochondrial protein Human genes 0.000 claims 2
- 101710101225 Diablo IAP-binding mitochondrial protein Proteins 0.000 claims 2
- 206010059866 Drug resistance Diseases 0.000 claims 2
- 108050002772 E3 ubiquitin-protein ligase Mdm2 Proteins 0.000 claims 2
- 102000012199 E3 ubiquitin-protein ligase Mdm2 Human genes 0.000 claims 2
- 102100037024 E3 ubiquitin-protein ligase XIAP Human genes 0.000 claims 2
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims 2
- 102000003688 G-Protein-Coupled Receptors Human genes 0.000 claims 2
- 108090000045 G-Protein-Coupled Receptors Proteins 0.000 claims 2
- 108010010803 Gelatin Proteins 0.000 claims 2
- 229940089838 Glucagon-like peptide 1 receptor agonist Drugs 0.000 claims 2
- 102100041003 Glutamate carboxypeptidase 2 Human genes 0.000 claims 2
- 102000005720 Glutathione transferase Human genes 0.000 claims 2
- 108010070675 Glutathione transferase Proteins 0.000 claims 2
- 229920000084 Gum arabic Polymers 0.000 claims 2
- 101710113864 Heat shock protein 90 Proteins 0.000 claims 2
- 102100034051 Heat shock protein HSP 90-alpha Human genes 0.000 claims 2
- 102100022623 Hepatocyte growth factor receptor Human genes 0.000 claims 2
- 101710184069 Hepatocyte growth factor receptor Proteins 0.000 claims 2
- 101000600756 Homo sapiens 3-phosphoinositide-dependent protein kinase 1 Proteins 0.000 claims 2
- 101000693076 Homo sapiens Angiopoietin-related protein 4 Proteins 0.000 claims 2
- 101000971171 Homo sapiens Apoptosis regulator Bcl-2 Proteins 0.000 claims 2
- 101000678892 Homo sapiens Atypical chemokine receptor 2 Proteins 0.000 claims 2
- 101000980825 Homo sapiens B-lymphocyte antigen CD19 Proteins 0.000 claims 2
- 101000716070 Homo sapiens C-C chemokine receptor type 9 Proteins 0.000 claims 2
- 101000922348 Homo sapiens C-X-C chemokine receptor type 4 Proteins 0.000 claims 2
- 101000892862 Homo sapiens Glutamate carboxypeptidase 2 Proteins 0.000 claims 2
- 101000785063 Homo sapiens Serine-protein kinase ATM Proteins 0.000 claims 2
- 101000777293 Homo sapiens Serine/threonine-protein kinase Chk1 Proteins 0.000 claims 2
- 101000777277 Homo sapiens Serine/threonine-protein kinase Chk2 Proteins 0.000 claims 2
- 101001117146 Homo sapiens [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial Proteins 0.000 claims 2
- 241000701806 Human papillomavirus Species 0.000 claims 2
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims 2
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims 2
- AVXURJPOCDRRFD-UHFFFAOYSA-N Hydroxylamine Chemical class ON AVXURJPOCDRRFD-UHFFFAOYSA-N 0.000 claims 2
- VSNHCAURESNICA-UHFFFAOYSA-N Hydroxyurea Chemical compound NC(=O)NO VSNHCAURESNICA-UHFFFAOYSA-N 0.000 claims 2
- 108060003951 Immunoglobulin Proteins 0.000 claims 2
- 102000008394 Immunoglobulin Fragments Human genes 0.000 claims 2
- 108010021625 Immunoglobulin Fragments Proteins 0.000 claims 2
- 102100024319 Intestinal-type alkaline phosphatase Human genes 0.000 claims 2
- 241000713321 Intracisternal A-particles Species 0.000 claims 2
- 102000015617 Janus Kinases Human genes 0.000 claims 2
- 108010024121 Janus Kinases Proteins 0.000 claims 2
- 102000001291 MAP Kinase Kinase Kinase Human genes 0.000 claims 2
- 108060006687 MAP kinase kinase kinase Proteins 0.000 claims 2
- CERQOIWHTDAKMF-UHFFFAOYSA-N Methacrylic acid Chemical compound CC(=C)C(O)=O CERQOIWHTDAKMF-UHFFFAOYSA-N 0.000 claims 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 2
- 102000002151 Microfilament Proteins Human genes 0.000 claims 2
- 108010040897 Microfilament Proteins Proteins 0.000 claims 2
- HSHXDCVZWHOWCS-UHFFFAOYSA-N N'-hexadecylthiophene-2-carbohydrazide Chemical compound CCCCCCCCCCCCCCCCNNC(=O)c1cccs1 HSHXDCVZWHOWCS-UHFFFAOYSA-N 0.000 claims 2
- 102000019315 Nicotinic acetylcholine receptors Human genes 0.000 claims 2
- 108050006807 Nicotinic acetylcholine receptors Proteins 0.000 claims 2
- 101150056950 Ntrk2 gene Proteins 0.000 claims 2
- 102000007399 Nuclear hormone receptor Human genes 0.000 claims 2
- 108020005497 Nuclear hormone receptor Proteins 0.000 claims 2
- 108010038807 Oligopeptides Proteins 0.000 claims 2
- 102000015636 Oligopeptides Human genes 0.000 claims 2
- 239000012661 PARP inhibitor Substances 0.000 claims 2
- 108091007960 PI3Ks Proteins 0.000 claims 2
- 229930012538 Paclitaxel Natural products 0.000 claims 2
- BUQLXKSONWUQAC-UHFFFAOYSA-N Parthenolide Natural products CC1C2OC(=O)C(=C)C2CCC(=C/CCC1(C)O)C BUQLXKSONWUQAC-UHFFFAOYSA-N 0.000 claims 2
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 claims 2
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 claims 2
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 claims 2
- 229940121906 Poly ADP ribose polymerase inhibitor Drugs 0.000 claims 2
- 229920000954 Polyglycolide Polymers 0.000 claims 2
- 108091008611 Protein Kinase B Proteins 0.000 claims 2
- 102000009516 Protein Serine-Threonine Kinases Human genes 0.000 claims 2
- 108010009341 Protein Serine-Threonine Kinases Proteins 0.000 claims 2
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 2
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 2
- 102000013009 Pyruvate Kinase Human genes 0.000 claims 2
- 108020005115 Pyruvate Kinase Proteins 0.000 claims 2
- 102100033810 RAC-alpha serine/threonine-protein kinase Human genes 0.000 claims 2
- 238000012228 RNA interference-mediated gene silencing Methods 0.000 claims 2
- 229940123690 Raf kinase inhibitor Drugs 0.000 claims 2
- 108091005682 Receptor kinases Proteins 0.000 claims 2
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims 2
- 101710151245 Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims 2
- 108010083644 Ribonucleases Proteins 0.000 claims 2
- 102000006382 Ribonucleases Human genes 0.000 claims 2
- 101150099493 STAT3 gene Proteins 0.000 claims 2
- 239000002262 Schiff base Substances 0.000 claims 2
- 150000004753 Schiff bases Chemical class 0.000 claims 2
- 102100020824 Serine-protein kinase ATM Human genes 0.000 claims 2
- 102100031081 Serine/threonine-protein kinase Chk1 Human genes 0.000 claims 2
- 102100031075 Serine/threonine-protein kinase Chk2 Human genes 0.000 claims 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 2
- 241000700584 Simplexvirus Species 0.000 claims 2
- 241000710960 Sindbis virus Species 0.000 claims 2
- 108010061312 Sphingomyelin Phosphodiesterase Proteins 0.000 claims 2
- 208000031673 T-Cell Cutaneous Lymphoma Diseases 0.000 claims 2
- 229940123237 Taxane Drugs 0.000 claims 2
- 108010017842 Telomerase Proteins 0.000 claims 2
- 108010022394 Threonine synthase Proteins 0.000 claims 2
- 102000004338 Transferrin Human genes 0.000 claims 2
- 108090000901 Transferrin Proteins 0.000 claims 2
- 102100029519 Tripartite motif-containing protein 29 Human genes 0.000 claims 2
- 102100029823 Tyrosine-protein kinase BTK Human genes 0.000 claims 2
- 108010092464 Urate Oxidase Proteins 0.000 claims 2
- 108700031544 X-Linked Inhibitor of Apoptosis Proteins 0.000 claims 2
- 229920002494 Zein Polymers 0.000 claims 2
- DXWGBJJLEDQBKS-LDBVRRDLSA-N [(2r,3s,4s,5r,6s)-3,4,5-trihydroxy-6-[5-hydroxy-3-(4-hydroxyphenyl)-4-oxochromen-7-yl]oxyoxan-2-yl]methyl acetate Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](COC(=O)C)O[C@H]1OC1=CC(O)=C2C(=O)C(C=3C=CC(O)=CC=3)=COC2=C1 DXWGBJJLEDQBKS-LDBVRRDLSA-N 0.000 claims 2
- 239000000205 acacia gum Substances 0.000 claims 2
- 235000010489 acacia gum Nutrition 0.000 claims 2
- 102000010126 acid sphingomyelin phosphodiesterase activity proteins Human genes 0.000 claims 2
- 230000004913 activation Effects 0.000 claims 2
- 239000002580 adenosine A3 receptor antagonist Substances 0.000 claims 2
- 239000000556 agonist Substances 0.000 claims 2
- 235000001014 amino acid Nutrition 0.000 claims 2
- 125000000539 amino acid group Chemical group 0.000 claims 2
- 150000001413 amino acids Chemical class 0.000 claims 2
- 238000004873 anchoring Methods 0.000 claims 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims 2
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 2
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 claims 2
- 239000003963 antioxidant agent Substances 0.000 claims 2
- 230000003078 antioxidant effect Effects 0.000 claims 2
- 235000006708 antioxidants Nutrition 0.000 claims 2
- 239000002221 antipyretic Substances 0.000 claims 2
- 229940125716 antipyretic agent Drugs 0.000 claims 2
- 239000008365 aqueous carrier Substances 0.000 claims 2
- 238000003556 assay Methods 0.000 claims 2
- 239000005441 aurora Substances 0.000 claims 2
- 229960001215 bendamustine hydrochloride Drugs 0.000 claims 2
- 229940049706 benzodiazepine Drugs 0.000 claims 2
- 125000003310 benzodiazepinyl group Chemical class N1N=C(C=CC2=C1C=CC=C2)* 0.000 claims 2
- 108091008324 binding proteins Proteins 0.000 claims 2
- 230000000975 bioactive effect Effects 0.000 claims 2
- 229920013641 bioerodible polymer Polymers 0.000 claims 2
- 229960000074 biopharmaceutical Drugs 0.000 claims 2
- 229960000455 brentuximab vedotin Drugs 0.000 claims 2
- 229940022399 cancer vaccine Drugs 0.000 claims 2
- 238000009566 cancer vaccine Methods 0.000 claims 2
- 229930003827 cannabinoid Natural products 0.000 claims 2
- 239000003557 cannabinoid Substances 0.000 claims 2
- 229940065144 cannabinoids Drugs 0.000 claims 2
- 229960004117 capecitabine Drugs 0.000 claims 2
- 239000001768 carboxy methyl cellulose Substances 0.000 claims 2
- RPKLZQLYODPWTM-KBMWBBLPSA-N cholanoic acid Chemical compound C1CC2CCCC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@@H](CCC(O)=O)C)[C@@]1(C)CC2 RPKLZQLYODPWTM-KBMWBBLPSA-N 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- CCGSUNCLSOWKJO-UHFFFAOYSA-N cimetidine Chemical compound N#CNC(=N/C)\NCCSCC1=NC=N[C]1C CCGSUNCLSOWKJO-UHFFFAOYSA-N 0.000 claims 2
- 229960001380 cimetidine Drugs 0.000 claims 2
- 230000003081 coactivator Effects 0.000 claims 2
- 238000000576 coating method Methods 0.000 claims 2
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims 2
- 239000008120 corn starch Substances 0.000 claims 2
- 229940099112 cornstarch Drugs 0.000 claims 2
- 239000006184 cosolvent Substances 0.000 claims 2
- 229940111134 coxibs Drugs 0.000 claims 2
- 239000006071 cream Substances 0.000 claims 2
- 229960001681 croscarmellose sodium Drugs 0.000 claims 2
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 2
- 201000007241 cutaneous T cell lymphoma Diseases 0.000 claims 2
- 239000002875 cyclin dependent kinase inhibitor Substances 0.000 claims 2
- 229940043378 cyclin-dependent kinase inhibitor Drugs 0.000 claims 2
- 229940097362 cyclodextrins Drugs 0.000 claims 2
- 239000003255 cyclooxygenase 2 inhibitor Substances 0.000 claims 2
- 150000001944 cysteine derivatives Chemical class 0.000 claims 2
- 229960003901 dacarbazine Drugs 0.000 claims 2
- 229940124447 delivery agent Drugs 0.000 claims 2
- 238000012631 diagnostic technique Methods 0.000 claims 2
- 102000004419 dihydrofolate reductase Human genes 0.000 claims 2
- 239000000539 dimer Substances 0.000 claims 2
- 238000006471 dimerization reaction Methods 0.000 claims 2
- 239000002934 diuretic Substances 0.000 claims 2
- 230000001882 diuretic effect Effects 0.000 claims 2
- 230000003828 downregulation Effects 0.000 claims 2
- 239000008298 dragée Substances 0.000 claims 2
- 239000002662 enteric coated tablet Substances 0.000 claims 2
- 230000001973 epigenetic effect Effects 0.000 claims 2
- 210000002950 fibroblast Anatomy 0.000 claims 2
- 239000007941 film coated tablet Substances 0.000 claims 2
- 229960000556 fingolimod Drugs 0.000 claims 2
- KKGQTZUTZRNORY-UHFFFAOYSA-N fingolimod Chemical compound CCCCCCCCC1=CC=C(CCC(N)(CO)CO)C=C1 KKGQTZUTZRNORY-UHFFFAOYSA-N 0.000 claims 2
- VVIAGPKUTFNRDU-ABLWVSNPSA-N folinic acid Chemical compound C1NC=2NC(N)=NC(=O)C=2N(C=O)C1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 VVIAGPKUTFNRDU-ABLWVSNPSA-N 0.000 claims 2
- 235000008191 folinic acid Nutrition 0.000 claims 2
- 239000011672 folinic acid Substances 0.000 claims 2
- 229960005102 foscarnet Drugs 0.000 claims 2
- 239000012458 free base Substances 0.000 claims 2
- 239000008273 gelatin Substances 0.000 claims 2
- 229920000159 gelatin Polymers 0.000 claims 2
- 235000019322 gelatine Nutrition 0.000 claims 2
- 235000011852 gelatine desserts Nutrition 0.000 claims 2
- 230000009368 gene silencing by RNA Effects 0.000 claims 2
- 238000001415 gene therapy Methods 0.000 claims 2
- 150000004676 glycans Chemical class 0.000 claims 2
- OZBAVEKZGSOMOJ-MIUGBVLSSA-N glycitin Chemical compound COC1=CC(C(C(C=2C=CC(O)=CC=2)=CO2)=O)=C2C=C1O[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O OZBAVEKZGSOMOJ-MIUGBVLSSA-N 0.000 claims 2
- 229910001385 heavy metal Inorganic materials 0.000 claims 2
- 229940121372 histone deacetylase inhibitor Drugs 0.000 claims 2
- 239000003276 histone deacetylase inhibitor Substances 0.000 claims 2
- 229920001477 hydrophilic polymer Polymers 0.000 claims 2
- 229960001330 hydroxycarbamide Drugs 0.000 claims 2
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims 2
- 102000018358 immunoglobulin Human genes 0.000 claims 2
- 229940072221 immunoglobulins Drugs 0.000 claims 2
- 239000000367 immunologic factor Substances 0.000 claims 2
- 102000006639 indoleamine 2,3-dioxygenase Human genes 0.000 claims 2
- 108020004201 indoleamine 2,3-dioxygenase Proteins 0.000 claims 2
- 230000000977 initiatory effect Effects 0.000 claims 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 2
- 238000001990 intravenous administration Methods 0.000 claims 2
- GOMNOOKGLZYEJT-UHFFFAOYSA-N isoflavone Chemical compound C=1OC2=CC=CC=C2C(=O)C=1C1=CC=CC=C1 GOMNOOKGLZYEJT-UHFFFAOYSA-N 0.000 claims 2
- CJWQYWQDLBZGPD-UHFFFAOYSA-N isoflavone Natural products C1=C(OC)C(OC)=CC(OC)=C1C1=COC2=C(C=CC(C)(C)O3)C3=C(OC)C=C2C1=O CJWQYWQDLBZGPD-UHFFFAOYSA-N 0.000 claims 2
- 235000008696 isoflavones Nutrition 0.000 claims 2
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 claims 2
- 229960001021 lactose monohydrate Drugs 0.000 claims 2
- 108010039490 largazole Proteins 0.000 claims 2
- GOTYRUGSSMKFNF-UHFFFAOYSA-N lenalidomide Chemical compound C1C=2C(N)=CC=CC=2C(=O)N1C1CCC(=O)NC1=O GOTYRUGSSMKFNF-UHFFFAOYSA-N 0.000 claims 2
- 229960004942 lenalidomide Drugs 0.000 claims 2
- 229960001691 leucovorin Drugs 0.000 claims 2
- 239000002502 liposome Substances 0.000 claims 2
- 239000007788 liquid Substances 0.000 claims 2
- 239000012669 liquid formulation Substances 0.000 claims 2
- 208000019423 liver disease Diseases 0.000 claims 2
- YDDMIZRDDREKEP-HWTBNCOESA-N lurbinectedin Chemical compound C([C@@]1(C(OC2)=O)NCCC3=C1NC1=CC=C(C=C13)OC)S[C@@H]1C3=C(OC(C)=O)C(C)=C4OCOC4=C3[C@H]2N2[C@@H](O)[C@H](CC=3C4=C(O)C(OC)=C(C)C=3)N(C)[C@H]4[C@@H]21 YDDMIZRDDREKEP-HWTBNCOESA-N 0.000 claims 2
- 229940124302 mTOR inhibitor Drugs 0.000 claims 2
- 150000002678 macrocyclic compounds Chemical class 0.000 claims 2
- 229960003511 macrogol Drugs 0.000 claims 2
- 235000019359 magnesium stearate Nutrition 0.000 claims 2
- 229940057948 magnesium stearate Drugs 0.000 claims 2
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims 2
- 238000005259 measurement Methods 0.000 claims 2
- 239000012528 membrane Substances 0.000 claims 2
- 229920000609 methyl cellulose Polymers 0.000 claims 2
- 239000001923 methylcellulose Substances 0.000 claims 2
- 239000000693 micelle Substances 0.000 claims 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 2
- 239000008108 microcrystalline cellulose Substances 0.000 claims 2
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 2
- 239000004005 microsphere Substances 0.000 claims 2
- 238000003032 molecular docking Methods 0.000 claims 2
- 239000000178 monomer Substances 0.000 claims 2
- SUXGLLRPXXXJER-UHFFFAOYSA-N myrsinoic acid A Natural products CC(C)=CCCC(C)=CCC1=CC(C(O)=O)=CC(CC=C(C)C)=C1O SUXGLLRPXXXJER-UHFFFAOYSA-N 0.000 claims 2
- SUXGLLRPXXXJER-LICLKQGHSA-N myrsinoic acid A Chemical compound CC(C)=CCC\C(C)=C\CC1=CC(C(O)=O)=CC(CC=C(C)C)=C1O SUXGLLRPXXXJER-LICLKQGHSA-N 0.000 claims 2
- 239000002159 nanocrystal Substances 0.000 claims 2
- 239000002105 nanoparticle Substances 0.000 claims 2
- 108020004017 nuclear receptors Proteins 0.000 claims 2
- 230000025308 nuclear transport Effects 0.000 claims 2
- 229960003347 obinutuzumab Drugs 0.000 claims 2
- 229960002450 ofatumumab Drugs 0.000 claims 2
- 239000006186 oral dosage form Substances 0.000 claims 2
- 229960001592 paclitaxel Drugs 0.000 claims 2
- 229960005184 panobinostat Drugs 0.000 claims 2
- FWZRWHZDXBDTFK-ZHACJKMWSA-N panobinostat Chemical compound CC1=NC2=CC=C[CH]C2=C1CCNCC1=CC=C(\C=C\C(=O)NO)C=C1 FWZRWHZDXBDTFK-ZHACJKMWSA-N 0.000 claims 2
- 229940069510 parthenolide Drugs 0.000 claims 2
- 230000037361 pathway Effects 0.000 claims 2
- NDTYTMIUWGWIMO-UHFFFAOYSA-N perillyl alcohol Chemical compound CC(=C)C1CCC(CO)=CC1 NDTYTMIUWGWIMO-UHFFFAOYSA-N 0.000 claims 2
- 238000002823 phage display Methods 0.000 claims 2
- ICFJFFQQTFMIBG-UHFFFAOYSA-N phenformin Chemical compound NC(=N)NC(=N)NCCC1=CC=CC=C1 ICFJFFQQTFMIBG-UHFFFAOYSA-N 0.000 claims 2
- 229960003243 phenformin Drugs 0.000 claims 2
- NSFSLUUZQIAOOX-LDCXZXNSSA-N pheophorbide a Chemical compound N1C(C=C2[C@H]([C@H](CCC(O)=O)C(=N2)C2=C3NC(=C4)C(C)=C3C(=O)[C@@H]2C(=O)OC)C)=C(C)C(C=C)=C1C=C1C(C)=C(CC)C4=N1 NSFSLUUZQIAOOX-LDCXZXNSSA-N 0.000 claims 2
- 102000051624 phosphatidylethanolamine binding protein Human genes 0.000 claims 2
- 108700021017 phosphatidylethanolamine binding protein Proteins 0.000 claims 2
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 claims 2
- 150000008299 phosphorodiamidates Chemical class 0.000 claims 2
- XNGIFLGASWRNHJ-UHFFFAOYSA-L phthalate(2-) Chemical compound [O-]C(=O)C1=CC=CC=C1C([O-])=O XNGIFLGASWRNHJ-UHFFFAOYSA-L 0.000 claims 2
- 229910052697 platinum Inorganic materials 0.000 claims 2
- 229920000747 poly(lactic acid) Polymers 0.000 claims 2
- 229940050929 polyethylene glycol 3350 Drugs 0.000 claims 2
- 229940057838 polyethylene glycol 4000 Drugs 0.000 claims 2
- 229920001282 polysaccharide Polymers 0.000 claims 2
- 239000005017 polysaccharide Substances 0.000 claims 2
- 235000019422 polyvinyl alcohol Nutrition 0.000 claims 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 2
- 229960000214 pralatrexate Drugs 0.000 claims 2
- OGSBUKJUDHAQEA-WMCAAGNKSA-N pralatrexate Chemical compound C1=NC2=NC(N)=NC(N)=C2N=C1CC(CC#C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OGSBUKJUDHAQEA-WMCAAGNKSA-N 0.000 claims 2
- XOFYZVNMUHMLCC-ZPOLXVRWSA-N prednisone Chemical compound O=C1C=C[C@]2(C)[C@H]3C(=O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 XOFYZVNMUHMLCC-ZPOLXVRWSA-N 0.000 claims 2
- 229960004618 prednisone Drugs 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 208000025638 primary cutaneous T-cell non-Hodgkin lymphoma Diseases 0.000 claims 2
- 239000003528 protein farnesyltransferase inhibitor Substances 0.000 claims 2
- 239000003909 protein kinase inhibitor Substances 0.000 claims 2
- 108010083755 proto-oncogene proteins pim Proteins 0.000 claims 2
- 229960003581 pyridoxal Drugs 0.000 claims 2
- 235000008164 pyridoxal Nutrition 0.000 claims 2
- 239000011674 pyridoxal Substances 0.000 claims 2
- 150000003223 pyridoxals Chemical class 0.000 claims 2
- 230000009257 reactivity Effects 0.000 claims 2
- 102000027426 receptor tyrosine kinases Human genes 0.000 claims 2
- 108091008598 receptor tyrosine kinases Proteins 0.000 claims 2
- 239000013557 residual solvent Substances 0.000 claims 2
- 201000006845 reticulosarcoma Diseases 0.000 claims 2
- 239000003590 rho kinase inhibitor Substances 0.000 claims 2
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 claims 2
- 239000002002 slurry Substances 0.000 claims 2
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims 2
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims 2
- 238000009494 specialized coating Methods 0.000 claims 2
- 230000009870 specific binding Effects 0.000 claims 2
- 239000002732 sphingomyelin phosphodiesterase inhibitor Substances 0.000 claims 2
- 229950006315 spirogermanium Drugs 0.000 claims 2
- 239000007940 sugar coated tablet Substances 0.000 claims 2
- 231100000617 superantigen Toxicity 0.000 claims 2
- 239000000829 suppository Substances 0.000 claims 2
- 239000000725 suspension Substances 0.000 claims 2
- 229920001059 synthetic polymer Polymers 0.000 claims 2
- 239000006188 syrup Substances 0.000 claims 2
- 235000020357 syrup Nutrition 0.000 claims 2
- 230000008685 targeting Effects 0.000 claims 2
- 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 2
- IQFYYKKMVGJFEH-CSMHCCOUSA-N telbivudine Chemical compound O=C1NC(=O)C(C)=CN1[C@H]1O[C@@H](CO)[C@H](O)C1 IQFYYKKMVGJFEH-CSMHCCOUSA-N 0.000 claims 2
- 229960005196 titanium dioxide Drugs 0.000 claims 2
- 239000012581 transferrin Substances 0.000 claims 2
- 238000005829 trimerization reaction Methods 0.000 claims 2
- 230000003424 uricosuric effect Effects 0.000 claims 2
- 239000013598 vector Substances 0.000 claims 2
- 239000005019 zein Substances 0.000 claims 2
- 229940093612 zein Drugs 0.000 claims 2
- 229930007631 (-)-perillyl alcohol Natural products 0.000 claims 1
- KPLDRYODCDLNHB-UHFFFAOYSA-N 1-ethylpyrimidine-2,4-dione Chemical compound CCN1C=CC(=O)NC1=O KPLDRYODCDLNHB-UHFFFAOYSA-N 0.000 claims 1
- FPIPGXGPPPQFEQ-UHFFFAOYSA-N 13-cis retinol Natural products OCC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-UHFFFAOYSA-N 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- FUXVKZWTXQUGMW-FQEVSTJZSA-N 9-Aminocamptothecin Chemical compound C1=CC(N)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 FUXVKZWTXQUGMW-FQEVSTJZSA-N 0.000 claims 1
- 208000030507 AIDS Diseases 0.000 claims 1
- 102100027211 Albumin Human genes 0.000 claims 1
- 108010088751 Albumins Proteins 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 108010076667 Caspases Proteins 0.000 claims 1
- 102000011727 Caspases Human genes 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000003311 Cytochrome P-450 Enzyme Inhibitors Diseases 0.000 claims 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 1
- GMTUGPYJRUMVTC-UHFFFAOYSA-N Daidzin Natural products OC(COc1ccc2C(=O)C(=COc2c1)c3ccc(O)cc3)C(O)C(O)C(O)C=O GMTUGPYJRUMVTC-UHFFFAOYSA-N 0.000 claims 1
- KYQZWONCHDNPDP-UHFFFAOYSA-N Daidzoside Natural products OC1C(O)C(O)C(CO)OC1OC1=CC=C2C(=O)C(C=3C=CC(O)=CC=3)=COC2=C1 KYQZWONCHDNPDP-UHFFFAOYSA-N 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 108010032035 Desmoglein 3 Proteins 0.000 claims 1
- 102000007577 Desmoglein 3 Human genes 0.000 claims 1
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 claims 1
- 244000133098 Echinacea angustifolia Species 0.000 claims 1
- 108010029961 Filgrastim Proteins 0.000 claims 1
- ZCOLJUOHXJRHDI-FZHKGVQDSA-N Genistein 7-O-glucoside Natural products O([C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](CO)O1)c1cc(O)c2C(=O)C(c3ccc(O)cc3)=COc2c1 ZCOLJUOHXJRHDI-FZHKGVQDSA-N 0.000 claims 1
- CJPNHKPXZYYCME-UHFFFAOYSA-N Genistin Natural products OCC1OC(Oc2ccc(O)c3OC(=CC(=O)c23)c4ccc(O)cc4)C(O)C(O)C1O CJPNHKPXZYYCME-UHFFFAOYSA-N 0.000 claims 1
- XJTZHGNBKZYODI-UHFFFAOYSA-N Glycitin Natural products OCC1OC(Oc2ccc3OC=C(C(=O)c3c2CO)c4ccc(O)cc4)C(O)C(O)C1O XJTZHGNBKZYODI-UHFFFAOYSA-N 0.000 claims 1
- 201000005569 Gout Diseases 0.000 claims 1
- 108010017080 Granulocyte Colony-Stimulating Factor Proteins 0.000 claims 1
- 102000004269 Granulocyte Colony-Stimulating Factor Human genes 0.000 claims 1
- 102000004457 Granulocyte-Macrophage Colony-Stimulating Factor Human genes 0.000 claims 1
- 108010017213 Granulocyte-Macrophage Colony-Stimulating Factor Proteins 0.000 claims 1
- 208000007514 Herpes zoster Diseases 0.000 claims 1
- 108010033040 Histones Proteins 0.000 claims 1
- 206010020880 Hypertrophy Diseases 0.000 claims 1
- 102100023915 Insulin Human genes 0.000 claims 1
- 108090001061 Insulin Proteins 0.000 claims 1
- PWKSKIMOESPYIA-BYPYZUCNSA-N L-N-acetyl-Cysteine Chemical compound CC(=O)N[C@@H](CS)C(O)=O PWKSKIMOESPYIA-BYPYZUCNSA-N 0.000 claims 1
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims 1
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims 1
- 239000002177 L01XE27 - Ibrutinib Substances 0.000 claims 1
- 229930195725 Mannitol Natural products 0.000 claims 1
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 1
- 102100022219 NF-kappa-B essential modulator Human genes 0.000 claims 1
- 101710090077 NF-kappa-B essential modulator Proteins 0.000 claims 1
- 108010049358 Oncogene Protein p65(gag-jun) Proteins 0.000 claims 1
- YCUNGEJJOMKCGZ-UHFFFAOYSA-N Pallidiflorin Natural products C1=CC(OC)=CC=C1C1=COC2=CC=CC(O)=C2C1=O YCUNGEJJOMKCGZ-UHFFFAOYSA-N 0.000 claims 1
- 208000002151 Pleural effusion Diseases 0.000 claims 1
- 208000037062 Polyps Diseases 0.000 claims 1
- 108090000315 Protein Kinase C Proteins 0.000 claims 1
- 102000003923 Protein Kinase C Human genes 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- DWAQJAXMDSEUJJ-UHFFFAOYSA-M Sodium bisulfite Chemical compound [Na+].OS([O-])=O DWAQJAXMDSEUJJ-UHFFFAOYSA-M 0.000 claims 1
- NAVMQTYZDKMPEU-UHFFFAOYSA-N Targretin Chemical compound CC1=CC(C(CCC2(C)C)(C)C)=C2C=C1C(=C)C1=CC=C(C(O)=O)C=C1 NAVMQTYZDKMPEU-UHFFFAOYSA-N 0.000 claims 1
- 102000009618 Transforming Growth Factors Human genes 0.000 claims 1
- 108010009583 Transforming Growth Factors Proteins 0.000 claims 1
- 102000014384 Type C Phospholipases Human genes 0.000 claims 1
- 108010079194 Type C Phospholipases Proteins 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- FPIPGXGPPPQFEQ-BOOMUCAASA-N Vitamin A Natural products OC/C=C(/C)\C=C\C=C(\C)/C=C/C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-BOOMUCAASA-N 0.000 claims 1
- 229930003316 Vitamin D Natural products 0.000 claims 1
- QYSXJUFSXHHAJI-XFEUOLMDSA-N Vitamin D3 Natural products C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C/C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-XFEUOLMDSA-N 0.000 claims 1
- 229930003427 Vitamin E Natural products 0.000 claims 1
- 229960004308 acetylcysteine Drugs 0.000 claims 1
- 238000001467 acupuncture Methods 0.000 claims 1
- 230000002152 alkylating effect Effects 0.000 claims 1
- FPIPGXGPPPQFEQ-OVSJKPMPSA-N all-trans-retinol Chemical compound OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-OVSJKPMPSA-N 0.000 claims 1
- 230000002491 angiogenic effect Effects 0.000 claims 1
- 230000001142 anti-diarrhea Effects 0.000 claims 1
- 230000003474 anti-emetic effect Effects 0.000 claims 1
- 230000002924 anti-infective effect Effects 0.000 claims 1
- 230000001754 anti-pyretic effect Effects 0.000 claims 1
- 239000002111 antiemetic agent Substances 0.000 claims 1
- 229940121375 antifungal agent Drugs 0.000 claims 1
- 239000003429 antifungal agent Substances 0.000 claims 1
- 229940125715 antihistaminic agent Drugs 0.000 claims 1
- 239000000739 antihistaminic agent Substances 0.000 claims 1
- 239000002220 antihypertensive agent Substances 0.000 claims 1
- 229940030600 antihypertensive agent Drugs 0.000 claims 1
- 229960005475 antiinfective agent Drugs 0.000 claims 1
- 239000003096 antiparasitic agent Substances 0.000 claims 1
- 229940125687 antiparasitic agent Drugs 0.000 claims 1
- 239000003443 antiviral agent Substances 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- KLNFSAOEKUDMFA-UHFFFAOYSA-N azanide;2-hydroxyacetic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OCC(O)=O KLNFSAOEKUDMFA-UHFFFAOYSA-N 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
- 229960002938 bexarotene Drugs 0.000 claims 1
- 230000037058 blood plasma level Effects 0.000 claims 1
- 210000001185 bone marrow Anatomy 0.000 claims 1
- 238000010322 bone marrow transplantation Methods 0.000 claims 1
- 238000002725 brachytherapy Methods 0.000 claims 1
- 239000000872 buffer Substances 0.000 claims 1
- 229960004562 carboplatin Drugs 0.000 claims 1
- 230000003197 catalytic effect Effects 0.000 claims 1
- 239000006114 chemosensitizer Substances 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000003246 corticosteroid Substances 0.000 claims 1
- 229960001334 corticosteroids Drugs 0.000 claims 1
- 235000007240 daidzein Nutrition 0.000 claims 1
- KYQZWONCHDNPDP-QNDFHXLGSA-N daidzein 7-O-beta-D-glucoside Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=CC=C2C(=O)C(C=3C=CC(O)=CC=3)=COC2=C1 KYQZWONCHDNPDP-QNDFHXLGSA-N 0.000 claims 1
- 239000003599 detergent Substances 0.000 claims 1
- 235000014134 echinacea Nutrition 0.000 claims 1
- 210000002889 endothelial cell Anatomy 0.000 claims 1
- 230000002255 enzymatic effect Effects 0.000 claims 1
- 229960001433 erlotinib Drugs 0.000 claims 1
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims 1
- 239000002329 esterase inhibitor Substances 0.000 claims 1
- 238000010195 expression analysis Methods 0.000 claims 1
- 239000012530 fluid Substances 0.000 claims 1
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 claims 1
- 229960002584 gefitinib Drugs 0.000 claims 1
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims 1
- DXYUAIFZCFRPTH-UHFFFAOYSA-N glycitein Chemical compound C1=C(O)C(OC)=CC(C2=O)=C1OC=C2C1=CC=C(O)C=C1 DXYUAIFZCFRPTH-UHFFFAOYSA-N 0.000 claims 1
- NNUVCMKMNCKPKN-UHFFFAOYSA-N glycitein Natural products COc1c(O)ccc2OC=C(C(=O)c12)c3ccc(O)cc3 NNUVCMKMNCKPKN-UHFFFAOYSA-N 0.000 claims 1
- 235000008466 glycitein Nutrition 0.000 claims 1
- DUBPGEJGGVZKDD-PFKOEMKTSA-N glycitein 7-(6-O-acetyl-beta-D-glucoside) Chemical compound COC1=CC(C(C(C=2C=CC(O)=CC=2)=CO2)=O)=C2C=C1O[C@@H]1O[C@H](COC(C)=O)[C@@H](O)[C@H](O)[C@H]1O DUBPGEJGGVZKDD-PFKOEMKTSA-N 0.000 claims 1
- 230000000147 hypnotic effect Effects 0.000 claims 1
- 230000001146 hypoxic effect Effects 0.000 claims 1
- 229960001507 ibrutinib Drugs 0.000 claims 1
- XYFPWWZEPKGCCK-GOSISDBHSA-N ibrutinib Chemical compound C1=2C(N)=NC=NC=2N([C@H]2CN(CCC2)C(=O)C=C)N=C1C(C=C1)=CC=C1OC1=CC=CC=C1 XYFPWWZEPKGCCK-GOSISDBHSA-N 0.000 claims 1
- 229940125396 insulin Drugs 0.000 claims 1
- 238000001361 intraarterial administration Methods 0.000 claims 1
- 238000007913 intrathecal administration Methods 0.000 claims 1
- 229960004768 irinotecan Drugs 0.000 claims 1
- UWKQSNNFCGGAFS-XIFFEERXSA-N irinotecan Chemical compound C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 UWKQSNNFCGGAFS-XIFFEERXSA-N 0.000 claims 1
- 229960003350 isoniazid Drugs 0.000 claims 1
- QRXWMOHMRWLFEY-UHFFFAOYSA-N isoniazide Chemical compound NNC(=O)C1=CC=NC=C1 QRXWMOHMRWLFEY-UHFFFAOYSA-N 0.000 claims 1
- 208000002741 leukoplakia Diseases 0.000 claims 1
- 239000003446 ligand Substances 0.000 claims 1
- MTXMHWSVSZKYBT-UHFFFAOYSA-N malonyl daidzin Natural products OC1C(O)C(O)C(COC(=O)CC(O)=O)OC1OC1=CC=C2C(=O)C(C=3C=CC(O)=CC=3)=COC2=C1 MTXMHWSVSZKYBT-UHFFFAOYSA-N 0.000 claims 1
- MTXMHWSVSZKYBT-ASDZUOGYSA-N malonyldaidzin Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](COC(=O)CC(O)=O)O[C@H]1OC1=CC=C2C(=O)C(C=3C=CC(O)=CC=3)=COC2=C1 MTXMHWSVSZKYBT-ASDZUOGYSA-N 0.000 claims 1
- 239000000594 mannitol Substances 0.000 claims 1
- 235000010355 mannitol Nutrition 0.000 claims 1
- 239000003550 marker Substances 0.000 claims 1
- 210000000214 mouth Anatomy 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 229950007221 nedaplatin Drugs 0.000 claims 1
- 229940029345 neupogen Drugs 0.000 claims 1
- 208000004235 neutropenia Diseases 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 235000016709 nutrition Nutrition 0.000 claims 1
- 231100000590 oncogenic Toxicity 0.000 claims 1
- 230000002246 oncogenic effect Effects 0.000 claims 1
- 238000011275 oncology therapy Methods 0.000 claims 1
- 229960001756 oxaliplatin Drugs 0.000 claims 1
- 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 1
- KTEXNACQROZXEV-PVLRGYAZSA-N parthenolide Chemical compound C1CC(/C)=C/CC[C@@]2(C)O[C@@H]2[C@H]2OC(=O)C(=C)[C@@H]21 KTEXNACQROZXEV-PVLRGYAZSA-N 0.000 claims 1
- 125000000810 parthenolide group Chemical group 0.000 claims 1
- 235000005693 perillyl alcohol Nutrition 0.000 claims 1
- 239000008363 phosphate buffer Substances 0.000 claims 1
- 239000003504 photosensitizing agent Substances 0.000 claims 1
- 229950005566 picoplatin Drugs 0.000 claims 1
- IIMIOEBMYPRQGU-UHFFFAOYSA-L picoplatin Chemical compound N.[Cl-].[Cl-].[Pt+2].CC1=CC=CC=N1 IIMIOEBMYPRQGU-UHFFFAOYSA-L 0.000 claims 1
- 230000000750 progressive effect Effects 0.000 claims 1
- 230000002285 radioactive effect Effects 0.000 claims 1
- 239000011347 resin Substances 0.000 claims 1
- 229920005989 resin Polymers 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 claims 1
- 229960005399 satraplatin Drugs 0.000 claims 1
- 190014017285 satraplatin Chemical compound 0.000 claims 1
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 claims 1
- 238000009168 stem cell therapy Methods 0.000 claims 1
- 239000000021 stimulant Substances 0.000 claims 1
- 238000013268 sustained release Methods 0.000 claims 1
- 150000003573 thiols Chemical class 0.000 claims 1
- 206010043554 thrombocytopenia Diseases 0.000 claims 1
- 238000011200 topical administration Methods 0.000 claims 1
- 229960000303 topotecan Drugs 0.000 claims 1
- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 claims 1
- 229950002860 triplatin tetranitrate Drugs 0.000 claims 1
- 190014017283 triplatin tetranitrate Chemical compound 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 230000009452 underexpressoin Effects 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 210000002700 urine Anatomy 0.000 claims 1
- 210000005166 vasculature Anatomy 0.000 claims 1
- 230000024883 vasodilation Effects 0.000 claims 1
- 108700026220 vif Genes Proteins 0.000 claims 1
- 235000019155 vitamin A Nutrition 0.000 claims 1
- 239000011719 vitamin A Substances 0.000 claims 1
- 235000019166 vitamin D Nutrition 0.000 claims 1
- 239000011710 vitamin D Substances 0.000 claims 1
- 150000003710 vitamin D derivatives Chemical class 0.000 claims 1
- 235000019165 vitamin E Nutrition 0.000 claims 1
- 229940046009 vitamin E Drugs 0.000 claims 1
- 239000011709 vitamin E Substances 0.000 claims 1
- 229940045997 vitamin a Drugs 0.000 claims 1
- 229940046008 vitamin d Drugs 0.000 claims 1
- 238000009097 single-agent therapy Methods 0.000 abstract description 4
- 125000000217 alkyl group Chemical group 0.000 description 66
- 229910052739 hydrogen Inorganic materials 0.000 description 45
- 239000001257 hydrogen Substances 0.000 description 44
- 125000003118 aryl group Chemical group 0.000 description 42
- 125000001309 chloro group Chemical group Cl* 0.000 description 32
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 32
- 125000001072 heteroaryl group Chemical group 0.000 description 24
- 125000005842 heteroatom Chemical group 0.000 description 22
- 125000003342 alkenyl group Chemical group 0.000 description 20
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 18
- 125000000304 alkynyl group Chemical group 0.000 description 18
- 125000001246 bromo group Chemical group Br* 0.000 description 17
- 238000006243 chemical reaction Methods 0.000 description 17
- 125000002346 iodo group Chemical group I* 0.000 description 16
- 108020004414 DNA Proteins 0.000 description 14
- 125000000623 heterocyclic group Chemical group 0.000 description 14
- 125000002252 acyl group Chemical group 0.000 description 13
- 125000000753 cycloalkyl group Chemical group 0.000 description 13
- 239000000047 product Substances 0.000 description 13
- 125000003710 aryl alkyl group Chemical group 0.000 description 11
- 125000004122 cyclic group Chemical group 0.000 description 11
- UYTPUPDQBNUYGX-UHFFFAOYSA-N guanine Chemical compound O=C1NC(N)=NC2=C1N=CN2 UYTPUPDQBNUYGX-UHFFFAOYSA-N 0.000 description 11
- 125000004404 heteroalkyl group Chemical group 0.000 description 11
- 238000003786 synthesis reaction Methods 0.000 description 11
- 125000004429 atom Chemical group 0.000 description 10
- 125000003545 alkoxy group Chemical group 0.000 description 9
- 229910052799 carbon Inorganic materials 0.000 description 9
- 125000004432 carbon atom Chemical group C* 0.000 description 8
- 125000005647 linker group Chemical group 0.000 description 8
- 125000002950 monocyclic group Chemical group 0.000 description 8
- 239000012071 phase Substances 0.000 description 8
- 125000002947 alkylene group Chemical group 0.000 description 7
- 125000005843 halogen group Chemical group 0.000 description 7
- 125000004446 heteroarylalkyl group Chemical group 0.000 description 7
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 7
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 7
- 230000004044 response Effects 0.000 description 7
- 229910052717 sulfur Inorganic materials 0.000 description 7
- 230000029936 alkylation Effects 0.000 description 6
- 238000005804 alkylation reaction Methods 0.000 description 6
- 238000013459 approach Methods 0.000 description 6
- 125000002619 bicyclic group Chemical group 0.000 description 6
- 230000000875 corresponding effect Effects 0.000 description 6
- 125000004185 ester group Chemical group 0.000 description 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 6
- 238000002638 palliative care Methods 0.000 description 6
- 229920006395 saturated elastomer Polymers 0.000 description 6
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 5
- 125000002837 carbocyclic group Chemical group 0.000 description 5
- 238000011161 development Methods 0.000 description 5
- 230000018109 developmental process Effects 0.000 description 5
- VILAVOFMIJHSJA-UHFFFAOYSA-N dicarbon monoxide Chemical group [C]=C=O VILAVOFMIJHSJA-UHFFFAOYSA-N 0.000 description 5
- 125000001183 hydrocarbyl group Chemical group 0.000 description 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 5
- 238000012216 screening Methods 0.000 description 5
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 description 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 4
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 4
- 239000002253 acid Substances 0.000 description 4
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 4
- 229910052794 bromium Inorganic materials 0.000 description 4
- 150000001721 carbon Chemical group 0.000 description 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 4
- 230000001413 cellular effect Effects 0.000 description 4
- 239000013043 chemical agent Substances 0.000 description 4
- 239000000460 chlorine Substances 0.000 description 4
- 229910052801 chlorine Inorganic materials 0.000 description 4
- 239000000562 conjugate Substances 0.000 description 4
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 description 4
- WVYXNIXAMZOZFK-UHFFFAOYSA-N diaziquone Chemical compound O=C1C(NC(=O)OCC)=C(N2CC2)C(=O)C(NC(=O)OCC)=C1N1CC1 WVYXNIXAMZOZFK-UHFFFAOYSA-N 0.000 description 4
- 238000011156 evaluation Methods 0.000 description 4
- 229910052736 halogen Inorganic materials 0.000 description 4
- 150000002367 halogens Chemical class 0.000 description 4
- 230000001976 improved effect Effects 0.000 description 4
- 238000001727 in vivo Methods 0.000 description 4
- 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 compound 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 description 4
- 102000039446 nucleic acids Human genes 0.000 description 4
- 108020004707 nucleic acids Proteins 0.000 description 4
- 150000007523 nucleic acids Chemical class 0.000 description 4
- 238000006722 reduction reaction Methods 0.000 description 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 description 3
- 108091032973 (ribonucleotides)n+m Proteins 0.000 description 3
- 125000000041 C6-C10 aryl group Chemical group 0.000 description 3
- 239000012626 DNA minor groove binder Substances 0.000 description 3
- 208000017604 Hodgkin disease Diseases 0.000 description 3
- 208000010747 Hodgkins lymphoma Diseases 0.000 description 3
- XCPGHVQEEXUHNC-UHFFFAOYSA-N amsacrine Chemical compound COC1=CC(NS(C)(=O)=O)=CC=C1NC1=C(C=CC=C2)C2=NC2=CC=CC=C12 XCPGHVQEEXUHNC-UHFFFAOYSA-N 0.000 description 3
- 229960001220 amsacrine Drugs 0.000 description 3
- 230000000259 anti-tumor effect Effects 0.000 description 3
- 239000002585 base Substances 0.000 description 3
- 125000004452 carbocyclyl group Chemical group 0.000 description 3
- 125000004093 cyano group Chemical group *C#N 0.000 description 3
- 125000000262 haloalkenyl group Chemical group 0.000 description 3
- 125000000232 haloalkynyl group Chemical group 0.000 description 3
- 125000003106 haloaryl group Chemical group 0.000 description 3
- 125000005216 haloheteroaryl group Chemical group 0.000 description 3
- 125000004415 heterocyclylalkyl group Chemical group 0.000 description 3
- 125000005020 hydroxyalkenyl group Chemical group 0.000 description 3
- 125000002768 hydroxyalkyl group Chemical group 0.000 description 3
- 125000005016 hydroxyalkynyl group Chemical group 0.000 description 3
- 125000005027 hydroxyaryl group Chemical group 0.000 description 3
- 210000000987 immune system Anatomy 0.000 description 3
- 238000000338 in vitro Methods 0.000 description 3
- HAWPXGHAZFHHAD-UHFFFAOYSA-N mechlorethamine Chemical compound ClCCN(C)CCCl HAWPXGHAZFHHAD-UHFFFAOYSA-N 0.000 description 3
- 229960004961 mechlorethamine Drugs 0.000 description 3
- 208000030159 metabolic disease Diseases 0.000 description 3
- 238000009522 phase III clinical trial Methods 0.000 description 3
- 150000003254 radicals Chemical class 0.000 description 3
- 230000001105 regulatory effect Effects 0.000 description 3
- JVBXVOWTABLYPX-UHFFFAOYSA-L sodium dithionite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])=O JVBXVOWTABLYPX-UHFFFAOYSA-L 0.000 description 3
- 125000004953 trihalomethyl group Chemical group 0.000 description 3
- 229960005486 vaccine Drugs 0.000 description 3
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 description 2
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 description 2
- WNXJIVFYUVYPPR-UHFFFAOYSA-N 1,3-dioxolane Chemical compound C1COCO1 WNXJIVFYUVYPPR-UHFFFAOYSA-N 0.000 description 2
- DPVIABCMTHHTGB-UHFFFAOYSA-N 2,4,6-trichloropyrimidine Chemical compound ClC1=CC(Cl)=NC(Cl)=N1 DPVIABCMTHHTGB-UHFFFAOYSA-N 0.000 description 2
- TUARVSWVPPVUGS-UHFFFAOYSA-N 5-nitrouracil Chemical compound [O-][N+](=O)C1=CNC(=O)NC1=O TUARVSWVPPVUGS-UHFFFAOYSA-N 0.000 description 2
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 description 2
- COVZYZSDYWQREU-UHFFFAOYSA-N Busulfan Chemical compound CS(=O)(=O)OCCCCOS(C)(=O)=O COVZYZSDYWQREU-UHFFFAOYSA-N 0.000 description 2
- 208000035473 Communicable disease Diseases 0.000 description 2
- LVZWSLJZHVFIQJ-UHFFFAOYSA-N Cyclopropane Chemical compound C1CC1 LVZWSLJZHVFIQJ-UHFFFAOYSA-N 0.000 description 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 2
- 208000021519 Hodgkin lymphoma Diseases 0.000 description 2
- KJQFBVYMGADDTQ-CVSPRKDYSA-N L-buthionine-(S,R)-sulfoximine Chemical compound CCCCS(=N)(=O)CC[C@H](N)C(O)=O KJQFBVYMGADDTQ-CVSPRKDYSA-N 0.000 description 2
- MJVAVZPDRWSRRC-UHFFFAOYSA-N Menadione Chemical compound C1=CC=C2C(=O)C(C)=CC(=O)C2=C1 MJVAVZPDRWSRRC-UHFFFAOYSA-N 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 229930192392 Mitomycin Natural products 0.000 description 2
- 101100030361 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) pph-3 gene Proteins 0.000 description 2
- 108091028043 Nucleic acid sequence Proteins 0.000 description 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 2
- 238000004617 QSAR study Methods 0.000 description 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 2
- 102100024219 T-cell surface glycoprotein CD1a Human genes 0.000 description 2
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 description 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 2
- SMPZPKRDRQOOHT-UHFFFAOYSA-N acronycine Chemical compound CN1C2=CC=CC=C2C(=O)C2=C1C(C=CC(C)(C)O1)=C1C=C2OC SMPZPKRDRQOOHT-UHFFFAOYSA-N 0.000 description 2
- 239000013543 active substance Substances 0.000 description 2
- 125000003277 amino group Chemical group 0.000 description 2
- 229940088710 antibiotic agent Drugs 0.000 description 2
- 230000004071 biological effect Effects 0.000 description 2
- 229960002092 busulfan Drugs 0.000 description 2
- 239000011203 carbon fibre reinforced carbon Substances 0.000 description 2
- 238000002512 chemotherapy Methods 0.000 description 2
- 210000000349 chromosome Anatomy 0.000 description 2
- 238000004132 cross linking Methods 0.000 description 2
- 229940127089 cytotoxic agent Drugs 0.000 description 2
- 230000006378 damage Effects 0.000 description 2
- 230000001066 destructive effect Effects 0.000 description 2
- 238000009826 distribution Methods 0.000 description 2
- 238000001647 drug administration Methods 0.000 description 2
- 238000005421 electrostatic potential Methods 0.000 description 2
- CTSPAMFJBXKSOY-UHFFFAOYSA-N ellipticine Chemical compound N1=CC=C2C(C)=C(NC=3C4=CC=CC=3)C4=C(C)C2=C1 CTSPAMFJBXKSOY-UHFFFAOYSA-N 0.000 description 2
- 229940088598 enzyme Drugs 0.000 description 2
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 2
- 229910052731 fluorine Inorganic materials 0.000 description 2
- 239000011737 fluorine Substances 0.000 description 2
- 230000006870 function Effects 0.000 description 2
- 230000004927 fusion Effects 0.000 description 2
- 230000002068 genetic effect Effects 0.000 description 2
- 230000036541 health Effects 0.000 description 2
- 230000001900 immune effect Effects 0.000 description 2
- 208000026278 immune system disease Diseases 0.000 description 2
- 230000002458 infectious effect Effects 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 239000000138 intercalating agent Substances 0.000 description 2
- PNDPGZBMCMUPRI-UHFFFAOYSA-N iodine Chemical compound II PNDPGZBMCMUPRI-UHFFFAOYSA-N 0.000 description 2
- 239000011630 iodine Substances 0.000 description 2
- 229910052740 iodine Inorganic materials 0.000 description 2
- 150000002500 ions Chemical class 0.000 description 2
- 210000004698 lymphocyte Anatomy 0.000 description 2
- 230000003211 malignant effect Effects 0.000 description 2
- 231100000682 maximum tolerated dose Toxicity 0.000 description 2
- 239000002184 metal Chemical class 0.000 description 2
- 229910052751 metal Inorganic materials 0.000 description 2
- 230000001613 neoplastic effect Effects 0.000 description 2
- 230000003389 potentiating effect Effects 0.000 description 2
- 239000003755 preservative agent Substances 0.000 description 2
- GPTFURBXHJWNHR-UHFFFAOYSA-N protopine Chemical compound C1=C2C(=O)CC3=CC=C4OCOC4=C3CN(C)CCC2=CC2=C1OCO2 GPTFURBXHJWNHR-UHFFFAOYSA-N 0.000 description 2
- 230000010076 replication Effects 0.000 description 2
- 238000011160 research Methods 0.000 description 2
- 125000006413 ring segment Chemical group 0.000 description 2
- 108010042747 stallimycin Proteins 0.000 description 2
- 229950009902 stallimycin Drugs 0.000 description 2
- 239000007858 starting material Substances 0.000 description 2
- 238000006467 substitution reaction Methods 0.000 description 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 description 2
- 239000011593 sulfur Substances 0.000 description 2
- 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 description 2
- 239000011701 zinc Substances 0.000 description 2
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 description 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 description 1
- ZGNLFUXWZJGETL-YUSKDDKASA-N (Z)-[(2S)-2-amino-2-carboxyethyl]-hydroxyimino-oxidoazanium Chemical compound N[C@@H](C\[N+]([O-])=N\O)C(O)=O ZGNLFUXWZJGETL-YUSKDDKASA-N 0.000 description 1
- LHGVYNDAWRBWGL-UHFFFAOYSA-O (e)-(5-amino-5-carboxy-2-oxopentylidene)-iminoazanium Chemical compound OC(=O)C(N)CCC(=O)C=[N+]=N LHGVYNDAWRBWGL-UHFFFAOYSA-O 0.000 description 1
- 102000040650 (ribonucleotides)n+m Human genes 0.000 description 1
- KZPYGQFFRCFCPP-UHFFFAOYSA-N 1,1'-bis(diphenylphosphino)ferrocene Chemical compound [Fe+2].C1=CC=C[C-]1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=C[C-]1P(C=1C=CC=CC=1)C1=CC=CC=C1 KZPYGQFFRCFCPP-UHFFFAOYSA-N 0.000 description 1
- 102100025573 1-alkyl-2-acetylglycerophosphocholine esterase Human genes 0.000 description 1
- KHUFHLFHOQVFGB-UHFFFAOYSA-N 1-aminoanthracene-9,10-dione Chemical class O=C1C2=CC=CC=C2C(=O)C2=C1C=CC=C2N KHUFHLFHOQVFGB-UHFFFAOYSA-N 0.000 description 1
- DEEULBIVHZVMHX-UHFFFAOYSA-N 1-nitroacridine Chemical compound C1=CC=C2C=C3C([N+](=O)[O-])=CC=CC3=NC2=C1 DEEULBIVHZVMHX-UHFFFAOYSA-N 0.000 description 1
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 description 1
- YQTCQNIPQMJNTI-UHFFFAOYSA-N 2,2-dimethylpropan-1-one Chemical group CC(C)(C)[C]=O YQTCQNIPQMJNTI-UHFFFAOYSA-N 0.000 description 1
- KPRFMAZESAKTEJ-UHFFFAOYSA-N 2-[1-amino-4-[2,5-dioxo-4-(1-phenylethyl)pyrrolidin-3-yl]-1-oxobutan-2-yl]-5-carbamoylheptanedioic acid;azane Chemical compound [NH4+].[NH4+].C=1C=CC=CC=1C(C)C1C(CCC(C(CCC(CC([O-])=O)C(N)=O)C([O-])=O)C(N)=O)C(=O)NC1=O KPRFMAZESAKTEJ-UHFFFAOYSA-N 0.000 description 1
- JPCHHZXQVHSGGC-UHFFFAOYSA-N 2-[[10-(2-hydroxyethoxy)anthracen-9-yl]methylamino]-2-methylpropane-1,3-diol Chemical compound C1=CC=C2C(CNC(CO)(CO)C)=C(C=CC=C3)C3=C(OCCO)C2=C1 JPCHHZXQVHSGGC-UHFFFAOYSA-N 0.000 description 1
- SEHSPJCWCBQHPF-UHFFFAOYSA-N 2-chloroethyl methylsulfonylmethanesulfonate Chemical compound CS(=O)(=O)CS(=O)(=O)OCCCl SEHSPJCWCBQHPF-UHFFFAOYSA-N 0.000 description 1
- RKEBXTALJSALNU-LDCXZXNSSA-N 3-[(3R,21S,22S)-16-ethenyl-11-ethyl-4-hydroxy-3-methoxycarbonyl-12,17,21,26-tetramethyl-7,23,24,25-tetrazahexacyclo[18.2.1.15,8.110,13.115,18.02,6]hexacosa-1,4,6,8(26),9,11,13(25),14,16,18(24),19-undecaen-22-yl]propanoic acid Chemical compound CCC1=C(C2=NC1=CC3=C(C4=C([C@@H](C(=C5[C@H]([C@@H](C(=CC6=NC(=C2)C(=C6C)C=C)N5)C)CCC(=O)O)C4=N3)C(=O)OC)O)C)C RKEBXTALJSALNU-LDCXZXNSSA-N 0.000 description 1
- KFKRXESVMDBTNQ-UHFFFAOYSA-N 3-[18-(2-carboxylatoethyl)-8,13-bis(1-hydroxyethyl)-3,7,12,17-tetramethyl-22,23-dihydroporphyrin-21,24-diium-2-yl]propanoate Chemical class N1C2=C(C)C(C(C)O)=C1C=C(N1)C(C)=C(C(O)C)C1=CC(C(C)=C1CCC(O)=O)=NC1=CC(C(CCC(O)=O)=C1C)=NC1=C2 KFKRXESVMDBTNQ-UHFFFAOYSA-N 0.000 description 1
- WUIABRMSWOKTOF-OYALTWQYSA-N 3-[[2-[2-[2-[[(2s,3r)-2-[[(2s,3s,4r)-4-[[(2s,3r)-2-[[6-amino-2-[(1s)-3-amino-1-[[(2s)-2,3-diamino-3-oxopropyl]amino]-3-oxopropyl]-5-methylpyrimidine-4-carbonyl]amino]-3-[(2r,3s,4s,5s,6s)-3-[(2r,3s,4s,5r,6r)-4-carbamoyloxy-3,5-dihydroxy-6-(hydroxymethyl)ox Chemical compound OS([O-])(=O)=O.N([C@H](C(=O)N[C@H](C)[C@@H](O)[C@H](C)C(=O)N[C@@H]([C@H](O)C)C(=O)NCCC=1SC=C(N=1)C=1SC=C(N=1)C(=O)NCCC[S+](C)C)[C@@H](O[C@H]1[C@H]([C@@H](O)[C@H](O)[C@H](CO)O1)O[C@@H]1[C@H]([C@@H](OC(N)=O)[C@H](O)[C@@H](CO)O1)O)C=1NC=NC=1)C(=O)C1=NC([C@H](CC(N)=O)NC[C@H](N)C(N)=O)=NC(N)=C1C WUIABRMSWOKTOF-OYALTWQYSA-N 0.000 description 1
- XMIIGOLPHOKFCH-UHFFFAOYSA-N 3-phenylpropionic acid Chemical compound OC(=O)CCC1=CC=CC=C1 XMIIGOLPHOKFCH-UHFFFAOYSA-N 0.000 description 1
- AOJJSUZBOXZQNB-VTZDEGQISA-N 4'-epidoxorubicin 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-VTZDEGQISA-N 0.000 description 1
- JARCFMKMOFFIGZ-UHFFFAOYSA-N 4,6-dioxo-n-phenyl-2-sulfanylidene-1,3-diazinane-5-carboxamide Chemical compound O=C1NC(=S)NC(=O)C1C(=O)NC1=CC=CC=C1 JARCFMKMOFFIGZ-UHFFFAOYSA-N 0.000 description 1
- OGONXIUGGALDIV-UHFFFAOYSA-N 4-[3-[4-(4,6-diamino-2,2-dimethyl-1,3,5-triazin-1-yl)phenyl]propanoylamino]-2-methylbenzenesulfonyl fluoride;ethanesulfonic acid Chemical compound CCS(O)(=O)=O.C1=C(S(F)(=O)=O)C(C)=CC(NC(=O)CCC=2C=CC(=CC=2)N2C(N=C(N)N=C2N)(C)C)=C1 OGONXIUGGALDIV-UHFFFAOYSA-N 0.000 description 1
- GWZMCNGIPHSLLG-UHFFFAOYSA-N 4h-benzo[h]isoquinoline-1,3-dione Chemical class C1=CC=CC2=C(C(=O)NC(=O)C3)C3=CC=C21 GWZMCNGIPHSLLG-UHFFFAOYSA-N 0.000 description 1
- 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 description 1
- WHSIXKUPQCKWBY-IOSLPCCCSA-N 5-iodotubercidin Chemical compound C1=C(I)C=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O WHSIXKUPQCKWBY-IOSLPCCCSA-N 0.000 description 1
- XQQAEEYIUMQDHR-UHFFFAOYSA-N 9-aminoacridine-4-carboxamide Chemical class C1=CC=C2N=C3C(C(=O)N)=CC=CC3=C(N)C2=C1 XQQAEEYIUMQDHR-UHFFFAOYSA-N 0.000 description 1
- 206010000830 Acute leukaemia Diseases 0.000 description 1
- 108010024976 Asparaginase Proteins 0.000 description 1
- 108091008875 B cell receptors Proteins 0.000 description 1
- 102100038080 B-cell receptor CD22 Human genes 0.000 description 1
- 102100022005 B-lymphocyte antigen CD20 Human genes 0.000 description 1
- 241000894006 Bacteria Species 0.000 description 1
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 1
- LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 description 1
- 241000219193 Brassicaceae Species 0.000 description 1
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 description 1
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 1
- 208000005623 Carcinogenesis Diseases 0.000 description 1
- 206010048610 Cardiotoxicity Diseases 0.000 description 1
- 102100021906 Cyclin-O Human genes 0.000 description 1
- 102000053602 DNA Human genes 0.000 description 1
- 230000006820 DNA synthesis Effects 0.000 description 1
- AUGQEEXBDZWUJY-ZLJUKNTDSA-N Diacetoxyscirpenol Chemical compound C([C@]12[C@]3(C)[C@H](OC(C)=O)[C@@H](O)[C@H]1O[C@@H]1C=C(C)CC[C@@]13COC(=O)C)O2 AUGQEEXBDZWUJY-ZLJUKNTDSA-N 0.000 description 1
- AUGQEEXBDZWUJY-UHFFFAOYSA-N Diacetoxyscirpenol Natural products CC(=O)OCC12CCC(C)=CC1OC1C(O)C(OC(C)=O)C2(C)C11CO1 AUGQEEXBDZWUJY-UHFFFAOYSA-N 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- HTIJFSOGRVMCQR-UHFFFAOYSA-N Epirubicin Natural products COc1cccc2C(=O)c3c(O)c4CC(O)(CC(OC5CC(N)C(=O)C(C)O5)c4c(O)c3C(=O)c12)C(=O)CO HTIJFSOGRVMCQR-UHFFFAOYSA-N 0.000 description 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 description 1
- 239000005977 Ethylene Substances 0.000 description 1
- 206010059024 Gastrointestinal toxicity Diseases 0.000 description 1
- 244000303040 Glycyrrhiza glabra Species 0.000 description 1
- ZIXGXMMUKPLXBB-UHFFFAOYSA-N Guatambuinine Natural products N1C2=CC=CC=C2C2=C1C(C)=C1C=CN=C(C)C1=C2 ZIXGXMMUKPLXBB-UHFFFAOYSA-N 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 101000884305 Homo sapiens B-cell receptor CD22 Proteins 0.000 description 1
- 101000897405 Homo sapiens B-lymphocyte antigen CD20 Proteins 0.000 description 1
- 101000897441 Homo sapiens Cyclin-O Proteins 0.000 description 1
- 101000823316 Homo sapiens Tyrosine-protein kinase ABL1 Proteins 0.000 description 1
- MLFKVJCWGUZWNV-UHFFFAOYSA-N L-alanosine Natural products OC(=O)C(N)CN(O)N=O MLFKVJCWGUZWNV-UHFFFAOYSA-N 0.000 description 1
- 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 description 1
- 229940124041 Luteinizing hormone releasing hormone (LHRH) antagonist Drugs 0.000 description 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 1
- 101100490437 Mus musculus Acvrl1 gene Proteins 0.000 description 1
- 150000001204 N-oxides Chemical class 0.000 description 1
- GRYLNZFGIOXLOG-UHFFFAOYSA-N Nitric acid Chemical compound O[N+]([O-])=O GRYLNZFGIOXLOG-UHFFFAOYSA-N 0.000 description 1
- 108091034117 Oligonucleotide Proteins 0.000 description 1
- 229930187135 Olivomycin Natural products 0.000 description 1
- 102000004316 Oxidoreductases Human genes 0.000 description 1
- 108090000854 Oxidoreductases Proteins 0.000 description 1
- 206010035148 Plague Diseases 0.000 description 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 description 1
- 206010060862 Prostate cancer Diseases 0.000 description 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 1
- 229940123573 Protein synthesis inhibitor Drugs 0.000 description 1
- 229930189077 Rifamycin Natural products 0.000 description 1
- SUYXJDLXGFPMCQ-INIZCTEOSA-N SJ000287331 Natural products CC1=c2cnccc2=C(C)C2=Nc3ccccc3[C@H]12 SUYXJDLXGFPMCQ-INIZCTEOSA-N 0.000 description 1
- ZSJLQEPLLKMAKR-UHFFFAOYSA-N Streptozotocin Natural products O=NN(C)C(=O)NC1C(O)OC(CO)C(O)C1O ZSJLQEPLLKMAKR-UHFFFAOYSA-N 0.000 description 1
- 238000006069 Suzuki reaction reaction Methods 0.000 description 1
- 210000001744 T-lymphocyte Anatomy 0.000 description 1
- BPEGJWRSRHCHSN-UHFFFAOYSA-N Temozolomide Chemical compound O=C1N(C)N=NC2=C(C(N)=O)N=CN21 BPEGJWRSRHCHSN-UHFFFAOYSA-N 0.000 description 1
- FOCVUCIESVLUNU-UHFFFAOYSA-N Thiotepa Chemical compound C1CN1P(N1CC1)(=S)N1CC1 FOCVUCIESVLUNU-UHFFFAOYSA-N 0.000 description 1
- 101710183280 Topoisomerase Proteins 0.000 description 1
- 102000007537 Type II DNA Topoisomerases Human genes 0.000 description 1
- 108010046308 Type II DNA Topoisomerases Proteins 0.000 description 1
- 102100022596 Tyrosine-protein kinase ABL1 Human genes 0.000 description 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 description 1
- 241000607479 Yersinia pestis Species 0.000 description 1
- JURAJLFHWXNPHG-UHFFFAOYSA-N [acetyl(methylcarbamoyl)amino] n-methylcarbamate Chemical compound CNC(=O)ON(C(C)=O)C(=O)NC JURAJLFHWXNPHG-UHFFFAOYSA-N 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- QAWIHIJWNYOLBE-OKKQSCSOSA-N acivicin Chemical compound OC(=O)[C@@H](N)[C@@H]1CC(Cl)=NO1 QAWIHIJWNYOLBE-OKKQSCSOSA-N 0.000 description 1
- 229950008427 acivicin Drugs 0.000 description 1
- 229950003478 acodazole Drugs 0.000 description 1
- 229940125665 acridine carboxamide Drugs 0.000 description 1
- 150000001251 acridines Chemical class 0.000 description 1
- 229930183665 actinomycin Natural products 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 229950004955 adozelesin Drugs 0.000 description 1
- BYRVKDUQDLJUBX-JJCDCTGGSA-N adozelesin Chemical compound C1=CC=C2OC(C(=O)NC=3C=C4C=C(NC4=CC=3)C(=O)N3C[C@H]4C[C@]44C5=C(C(C=C43)=O)NC=C5C)=CC2=C1 BYRVKDUQDLJUBX-JJCDCTGGSA-N 0.000 description 1
- 229950005033 alanosine Drugs 0.000 description 1
- 150000001336 alkenes Chemical class 0.000 description 1
- 125000005090 alkenylcarbonyl group Chemical group 0.000 description 1
- 125000005092 alkenyloxycarbonyl group Chemical group 0.000 description 1
- 125000005137 alkenylsulfonyl group Chemical group 0.000 description 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 description 1
- 229940045714 alkyl sulfonate alkylating agent Drugs 0.000 description 1
- 150000008052 alkyl sulfonates Chemical class 0.000 description 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 description 1
- 125000001118 alkylidene group Chemical group 0.000 description 1
- 125000005087 alkynylcarbonyl group Chemical group 0.000 description 1
- 125000005225 alkynyloxycarbonyl group Chemical group 0.000 description 1
- 125000005139 alkynylsulfonyl group Chemical group 0.000 description 1
- 229960000473 altretamine Drugs 0.000 description 1
- 150000001412 amines Chemical class 0.000 description 1
- ROBVIMPUHSLWNV-UHFFFAOYSA-N aminoglutethimide Chemical compound C=1C=C(N)C=CC=1C1(CC)CCC(=O)NC1=O ROBVIMPUHSLWNV-UHFFFAOYSA-N 0.000 description 1
- 229960003437 aminoglutethimide Drugs 0.000 description 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 description 1
- 229960004701 amonafide Drugs 0.000 description 1
- 239000003098 androgen Substances 0.000 description 1
- 229940030486 androgens Drugs 0.000 description 1
- 229940045799 anthracyclines and related substance Drugs 0.000 description 1
- 230000001093 anti-cancer Effects 0.000 description 1
- 230000001028 anti-proliverative effect Effects 0.000 description 1
- 229940045687 antimetabolites folic acid analogs Drugs 0.000 description 1
- 239000003080 antimitotic agent Substances 0.000 description 1
- 229940045719 antineoplastic alkylating agent nitrosoureas Drugs 0.000 description 1
- 229940027998 antiseptic and disinfectant acridine derivative Drugs 0.000 description 1
- SGPJMFVJKNVPLI-CJXLBUIWSA-N aphig Chemical compound Cl.C1[C@@]23[C@@]4(C)CC[C@@H](O)[C@@](C)(CO)[C@@H]4CC[C@H]3C[C@H]1[C@](COC(=O)CN)(O)CC2 SGPJMFVJKNVPLI-CJXLBUIWSA-N 0.000 description 1
- 125000005140 aralkylsulfonyl group Chemical group 0.000 description 1
- 239000003886 aromatase inhibitor Substances 0.000 description 1
- 229940046844 aromatase inhibitors Drugs 0.000 description 1
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 description 1
- 125000004391 aryl sulfonyl group Chemical group 0.000 description 1
- 125000004104 aryloxy group Chemical group 0.000 description 1
- 229960005261 aspartic acid Drugs 0.000 description 1
- TWHSQQYCDVSBRK-UHFFFAOYSA-N asulacrine Chemical compound C12=CC=CC(C)=C2N=C2C(C(=O)NC)=CC=CC2=C1NC1=CC=C(NS(C)(=O)=O)C=C1OC TWHSQQYCDVSBRK-UHFFFAOYSA-N 0.000 description 1
- 229960002170 azathioprine Drugs 0.000 description 1
- LMEKQMALGUDUQG-UHFFFAOYSA-N azathioprine Chemical compound CN1C=NC([N+]([O-])=O)=C1SC1=NC=NC2=C1NC=N2 LMEKQMALGUDUQG-UHFFFAOYSA-N 0.000 description 1
- YFUNDTIYMJBNTB-UHFFFAOYSA-N aziridin-1-ylphosphane Chemical class PN1CC1 YFUNDTIYMJBNTB-UHFFFAOYSA-N 0.000 description 1
- 150000001541 aziridines Chemical class 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 description 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 description 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 description 1
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 description 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 description 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 1
- 230000008236 biological pathway Effects 0.000 description 1
- 229940126587 biotherapeutics Drugs 0.000 description 1
- 229950008548 bisantrene Drugs 0.000 description 1
- 229960004395 bleomycin sulfate Drugs 0.000 description 1
- 230000015624 blood vessel development Effects 0.000 description 1
- 230000036952 cancer formation Effects 0.000 description 1
- 229950009338 caracemide Drugs 0.000 description 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 description 1
- 150000003857 carboxamides Chemical class 0.000 description 1
- 231100000504 carcinogenesis Toxicity 0.000 description 1
- 231100000259 cardiotoxicity Toxicity 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 238000006555 catalytic reaction Methods 0.000 description 1
- 230000022131 cell cycle Effects 0.000 description 1
- 230000030833 cell death Effects 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- SMNPLAKEGAEPJD-UHFFFAOYSA-N chembl34922 Chemical compound Cl.Cl.Cl.C1CN(C)CCN1C1=CC=C(NC(=N2)C=3C=C4N=C(NC4=CC=3)C=3C=CC(O)=CC=3)C2=C1 SMNPLAKEGAEPJD-UHFFFAOYSA-N 0.000 description 1
- 230000002925 chemical effect Effects 0.000 description 1
- 150000005829 chemical entities Chemical class 0.000 description 1
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 238000005094 computer simulation Methods 0.000 description 1
- 230000002596 correlated effect Effects 0.000 description 1
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 description 1
- 231100000433 cytotoxic Toxicity 0.000 description 1
- 231100000599 cytotoxic agent Toxicity 0.000 description 1
- 230000001472 cytotoxic effect Effects 0.000 description 1
- 239000002619 cytotoxin Substances 0.000 description 1
- 238000003066 decision tree Methods 0.000 description 1
- 238000006731 degradation reaction Methods 0.000 description 1
- 229960002923 denileukin diftitox Drugs 0.000 description 1
- 108010017271 denileukin diftitox Proteins 0.000 description 1
- 239000005549 deoxyribonucleoside Substances 0.000 description 1
- 238000013461 design Methods 0.000 description 1
- 238000003745 diagnosis Methods 0.000 description 1
- 125000004985 dialkyl amino alkyl group Chemical group 0.000 description 1
- 229950002389 diaziquone Drugs 0.000 description 1
- 230000004069 differentiation Effects 0.000 description 1
- 150000004683 dihydrates Chemical class 0.000 description 1
- 239000001177 diphosphate Substances 0.000 description 1
- 235000011180 diphosphates Nutrition 0.000 description 1
- 208000016097 disease of metabolism Diseases 0.000 description 1
- 231100000371 dose-limiting toxicity Toxicity 0.000 description 1
- 150000002085 enols Chemical class 0.000 description 1
- 229960001904 epirubicin Drugs 0.000 description 1
- 229960005309 estradiol Drugs 0.000 description 1
- 229930182833 estradiol Natural products 0.000 description 1
- 229940011871 estrogen Drugs 0.000 description 1
- 239000000262 estrogen Substances 0.000 description 1
- GBPZYMBDOBODNK-SFTDATJTSA-N ethyl (2s)-2-[[(2s)-2-acetamido-3-[4-[bis(2-chloroethyl)amino]phenyl]propanoyl]amino]-4-methylpentanoate Chemical compound CCOC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)CC1=CC=C(N(CCCl)CCCl)C=C1 GBPZYMBDOBODNK-SFTDATJTSA-N 0.000 description 1
- 239000000284 extract Substances 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 150000005699 fluoropyrimidines Chemical class 0.000 description 1
- 150000002224 folic acids Chemical class 0.000 description 1
- 230000003325 follicular Effects 0.000 description 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 description 1
- 125000002541 furyl group Chemical group 0.000 description 1
- 231100000414 gastrointestinal toxicity Toxicity 0.000 description 1
- 210000003714 granulocyte Anatomy 0.000 description 1
- 125000004438 haloalkoxy group Chemical group 0.000 description 1
- 125000004474 heteroalkylene group Chemical group 0.000 description 1
- 150000004687 hexahydrates Chemical class 0.000 description 1
- VKYKSIONXSXAKP-UHFFFAOYSA-N hexamethylenetetramine Chemical compound C1N(C2)CN3CN1CN2C3 VKYKSIONXSXAKP-UHFFFAOYSA-N 0.000 description 1
- UUVWYPNAQBNQJQ-UHFFFAOYSA-N hexamethylmelamine Chemical compound CN(C)C1=NC(N(C)C)=NC(N(C)C)=N1 UUVWYPNAQBNQJQ-UHFFFAOYSA-N 0.000 description 1
- 230000036571 hydration Effects 0.000 description 1
- 238000006703 hydration reaction Methods 0.000 description 1
- 125000002883 imidazolyl group Chemical group 0.000 description 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 description 1
- 125000001041 indolyl group Chemical group 0.000 description 1
- 230000004968 inflammatory condition Effects 0.000 description 1
- 230000009545 invasion Effects 0.000 description 1
- 125000005956 isoquinolyl group Chemical group 0.000 description 1
- 150000002576 ketones Chemical class 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- 210000001165 lymph node Anatomy 0.000 description 1
- 201000011649 lymphoblastic lymphoma Diseases 0.000 description 1
- 230000000527 lymphocytic effect Effects 0.000 description 1
- 238000009607 mammography Methods 0.000 description 1
- 229960000485 methotrexate Drugs 0.000 description 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 description 1
- QXYYYPFGTSJXNS-UHFFFAOYSA-N mitozolomide Chemical compound N1=NN(CCCl)C(=O)N2C1=C(C(=O)N)N=C2 QXYYYPFGTSJXNS-UHFFFAOYSA-N 0.000 description 1
- 229950005967 mitozolomide Drugs 0.000 description 1
- 150000004682 monohydrates Chemical class 0.000 description 1
- 238000002703 mutagenesis Methods 0.000 description 1
- 231100000350 mutagenesis Toxicity 0.000 description 1
- 206010028537 myelofibrosis Diseases 0.000 description 1
- NJSMWLQOCQIOPE-OCHFTUDZSA-N n-[(e)-[10-[(e)-(4,5-dihydro-1h-imidazol-2-ylhydrazinylidene)methyl]anthracen-9-yl]methylideneamino]-4,5-dihydro-1h-imidazol-2-amine Chemical compound N1CCN=C1N\N=C\C(C1=CC=CC=C11)=C(C=CC=C2)C2=C1\C=N\NC1=NCCN1 NJSMWLQOCQIOPE-OCHFTUDZSA-N 0.000 description 1
- XBGNERSKEKDZDS-UHFFFAOYSA-N n-[2-(dimethylamino)ethyl]acridine-4-carboxamide Chemical compound C1=CC=C2N=C3C(C(=O)NCCN(C)C)=CC=CC3=CC2=C1 XBGNERSKEKDZDS-UHFFFAOYSA-N 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
- 229930014626 natural product Natural products 0.000 description 1
- 229940086322 navelbine Drugs 0.000 description 1
- 238000006396 nitration reaction Methods 0.000 description 1
- 150000003833 nucleoside derivatives Chemical class 0.000 description 1
- JRZJOMJEPLMPRA-UHFFFAOYSA-N olefin Natural products CCCCCCCC=C JRZJOMJEPLMPRA-UHFFFAOYSA-N 0.000 description 1
- CZDBNBLGZNWKMC-MWQNXGTOSA-N olivomycin Chemical class O([C@@H]1C[C@@H](O[C@H](C)[C@@H]1O)OC=1C=C2C=C3C[C@H]([C@@H](C(=O)C3=C(O)C2=C(O)C=1)O[C@H]1O[C@@H](C)[C@H](O)[C@@H](OC2O[C@@H](C)[C@H](O)[C@@H](O)C2)C1)[C@H](OC)C(=O)[C@@H](O)[C@@H](C)O)[C@H]1C[C@H](O)[C@H](OC)[C@H](C)O1 CZDBNBLGZNWKMC-MWQNXGTOSA-N 0.000 description 1
- 229940045681 other alkylating agent in atc Drugs 0.000 description 1
- 125000002971 oxazolyl group Chemical group 0.000 description 1
- 125000004043 oxo group Chemical group O=* 0.000 description 1
- 125000004430 oxygen atom Chemical group O* 0.000 description 1
- 238000009521 phase II clinical trial Methods 0.000 description 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 description 1
- 125000000286 phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 description 1
- 229910052698 phosphorus Inorganic materials 0.000 description 1
- 239000013612 plasmid Substances 0.000 description 1
- 125000003367 polycyclic group Chemical group 0.000 description 1
- 102000040430 polynucleotide Human genes 0.000 description 1
- 108091033319 polynucleotide Proteins 0.000 description 1
- 239000002157 polynucleotide Substances 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- 231100001271 preclinical toxicology Toxicity 0.000 description 1
- CPTBDICYNRMXFX-UHFFFAOYSA-N procarbazine Chemical compound CNNCC1=CC=C(C(=O)NC(C)C)C=C1 CPTBDICYNRMXFX-UHFFFAOYSA-N 0.000 description 1
- 229960000624 procarbazine Drugs 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 239000000007 protein synthesis inhibitor Substances 0.000 description 1
- 125000003373 pyrazinyl group Chemical group 0.000 description 1
- 125000003226 pyrazolyl group Chemical group 0.000 description 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 125000005344 pyridylmethyl group Chemical group [H]C1=C([H])C([H])=C([H])C(=N1)C([H])([H])* 0.000 description 1
- 229940083082 pyrimidine derivative acting on arteriolar smooth muscle Drugs 0.000 description 1
- 150000003230 pyrimidines Chemical class 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 125000000168 pyrrolyl group Chemical group 0.000 description 1
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 description 1
- 125000005493 quinolyl group Chemical group 0.000 description 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 description 1
- UOWVMDUEMSNCAV-WYENRQIDSA-N rachelmycin Chemical compound C1([C@]23C[C@@H]2CN1C(=O)C=1NC=2C(OC)=C(O)C4=C(C=2C=1)CCN4C(=O)C1=CC=2C=4CCN(C=4C(O)=C(C=2N1)OC)C(N)=O)=CC(=O)C1=C3C(C)=CN1 UOWVMDUEMSNCAV-WYENRQIDSA-N 0.000 description 1
- 238000011363 radioimmunotherapy Methods 0.000 description 1
- 238000012827 research and development Methods 0.000 description 1
- BTVYFIMKUHNOBZ-QXMMDKDBSA-N rifamycin s Chemical class O=C1C(C(O)=C2C)=C3C(=O)C=C1NC(=O)\C(C)=C/C=C\C(C)C(O)C(C)C(O)C(C)C(OC(C)=O)C(C)C(OC)\C=C/OC1(C)OC2=C3C1=O BTVYFIMKUHNOBZ-QXMMDKDBSA-N 0.000 description 1
- 229940081192 rifamycins Drugs 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 210000003491 skin Anatomy 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 238000007614 solvation Methods 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 239000003270 steroid hormone Substances 0.000 description 1
- 229960001052 streptozocin Drugs 0.000 description 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 description 1
- 125000000547 substituted alkyl group Chemical group 0.000 description 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 description 1
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-N sulfuric acid Substances OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 1
- 230000008093 supporting effect Effects 0.000 description 1
- 230000004083 survival effect Effects 0.000 description 1
- 230000009897 systematic effect Effects 0.000 description 1
- 238000011521 systemic chemotherapy Methods 0.000 description 1
- 238000009121 systemic therapy Methods 0.000 description 1
- 229960001603 tamoxifen Drugs 0.000 description 1
- 229960004964 temozolomide Drugs 0.000 description 1
- 229960001278 teniposide Drugs 0.000 description 1
- NRUKOCRGYNPUPR-QBPJDGROSA-N teniposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@@H](OC[C@H]4O3)C=3SC=CC=3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 NRUKOCRGYNPUPR-QBPJDGROSA-N 0.000 description 1
- 125000005247 tetrazinyl group Chemical group N1=NN=NC(=C1)* 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 229940036565 thiouracil antithyroid preparations Drugs 0.000 description 1
- 229950002376 tirapazamine Drugs 0.000 description 1
- ORYDPOVDJJZGHQ-UHFFFAOYSA-N tirapazamine Chemical compound C1=CC=CC2=[N+]([O-])C(N)=N[N+]([O-])=C21 ORYDPOVDJJZGHQ-UHFFFAOYSA-N 0.000 description 1
- 238000013518 transcription Methods 0.000 description 1
- 230000035897 transcription Effects 0.000 description 1
- 238000011269 treatment regimen Methods 0.000 description 1
- 150000004654 triazenes Chemical class 0.000 description 1
- 125000004306 triazinyl group Chemical group 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- 150000004684 trihydrates Chemical class 0.000 description 1
- 229960003048 vinblastine Drugs 0.000 description 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 description 1
- CILBMBUYJCWATM-PYGJLNRPSA-N vinorelbine ditartrate Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O.OC(=O)[C@H](O)[C@@H](O)C(O)=O.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 CILBMBUYJCWATM-PYGJLNRPSA-N 0.000 description 1
- 210000001835 viscera Anatomy 0.000 description 1
- 235000012711 vitamin K3 Nutrition 0.000 description 1
- 239000011652 vitamin K3 Substances 0.000 description 1
- 229940041603 vitamin k 3 Drugs 0.000 description 1
Classifications
-
- 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
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- 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
- A61K31/133—Amines having hydroxy groups, e.g. sphingosine
-
- 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
- A61K31/4164—1,3-Diazoles
- A61K31/417—Imidazole-alkylamines, e.g. histamine, phentolamine
-
- 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
- A61K31/56—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
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
- A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Oncology (AREA)
- Hematology (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)
Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2019240599A AU2019240599A1 (en) | 2013-04-08 | 2019-10-01 | Therapeutic benefit of suboptimally administered chemical compounds |
| AU2021257978A AU2021257978A1 (en) | 2013-04-08 | 2021-10-27 | Therapeutic benefit of suboptimally administered chemical compounds |
| AU2024200650A AU2024200650A1 (en) | 2013-04-08 | 2024-02-02 | Therapeutic benefit of suboptimally administered chemical compounds |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361809627P | 2013-04-08 | 2013-04-08 | |
| US61/809,627 | 2013-04-08 | ||
| PCT/US2014/033391 WO2014168986A1 (en) | 2013-04-08 | 2014-04-08 | Therapeutic benefit of suboptimally administered chemical compounds |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2019240599A Division AU2019240599A1 (en) | 2013-04-08 | 2019-10-01 | Therapeutic benefit of suboptimally administered chemical compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AU2014251038A1 true AU2014251038A1 (en) | 2015-11-26 |
Family
ID=51689967
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2014251038A Abandoned AU2014251038A1 (en) | 2013-04-08 | 2014-04-08 | Therapeutic benefit of suboptimally administered chemical compounds |
| AU2019240599A Abandoned AU2019240599A1 (en) | 2013-04-08 | 2019-10-01 | Therapeutic benefit of suboptimally administered chemical compounds |
| AU2021257978A Abandoned AU2021257978A1 (en) | 2013-04-08 | 2021-10-27 | Therapeutic benefit of suboptimally administered chemical compounds |
| AU2024200650A Abandoned AU2024200650A1 (en) | 2013-04-08 | 2024-02-02 | Therapeutic benefit of suboptimally administered chemical compounds |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2019240599A Abandoned AU2019240599A1 (en) | 2013-04-08 | 2019-10-01 | Therapeutic benefit of suboptimally administered chemical compounds |
| AU2021257978A Abandoned AU2021257978A1 (en) | 2013-04-08 | 2021-10-27 | Therapeutic benefit of suboptimally administered chemical compounds |
| AU2024200650A Abandoned AU2024200650A1 (en) | 2013-04-08 | 2024-02-02 | Therapeutic benefit of suboptimally administered chemical compounds |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US11491154B2 (enExample) |
| EP (1) | EP2983674A4 (enExample) |
| JP (2) | JP2016519684A (enExample) |
| KR (1) | KR20160061911A (enExample) |
| CN (1) | CN105492011A (enExample) |
| AU (4) | AU2014251038A1 (enExample) |
| WO (1) | WO2014168986A1 (enExample) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NO2686520T3 (enExample) | 2011-06-06 | 2018-03-17 | ||
| WO2014179528A2 (en) * | 2013-05-01 | 2014-11-06 | Brown Dennis M | Compositions and methods to improve the therapeutic benefit of suboptimally administered chemical compounds including substituted naphthalimides such as amonafide for the treatment of immunological, metabolic, infectious, and benign or neoplastic hyperproliferative disease conditions |
| NZ714963A (en) | 2013-06-13 | 2020-07-31 | Akebia Therapeutics Inc | Compositions and methods for treating anemia |
| US20160303242A1 (en) | 2013-12-09 | 2016-10-20 | Durect Corporation | Pharmaceutically Active Agent Complexes, Polymer Complexes, and Compositions and Methods Involving the Same |
| JP2018502882A (ja) | 2015-01-23 | 2018-02-01 | アケビア セラピューティクス インコーポレイテッドＡｋｅｂｉａ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｉｎｃ． | ２−（５−（３−フルオロフェニル）−３−ヒドロキシピコリンアミド）酢酸の固体形態、その組成物及び使用 |
| UA123308C2 (uk) * | 2015-04-01 | 2021-03-17 | Екебіа Терапьютікс, Інк. | Композиції і способи для лікування анемії |
| EP3118621A1 (en) * | 2015-07-14 | 2017-01-18 | Fundació Institut d'Investigació Biomèdica de Bellvitge (IDIBELL) | Methods and compositions for the diagnosis and for the treatment of adrenoleukodystrophy |
| WO2018003857A1 (ja) | 2016-06-29 | 2018-01-04 | 株式会社セラバイオファーマ | 非経口投与用医薬組成物 |
| US10449269B2 (en) * | 2016-08-29 | 2019-10-22 | Yale University | Particle conjugated prosthetic patches and methods of making and using thereof |
| CN110944638A (zh) | 2017-03-27 | 2020-03-31 | 特沙诺有限公司 | 尼拉帕尼组合物 |
| KR20200052349A (ko) | 2017-09-11 | 2020-05-14 | 아토사 테라퓨틱스, 인크. | 엔독시펜을 제조 및 사용하는 방법 |
| BR112020006039A2 (pt) * | 2017-09-26 | 2020-10-06 | Tesaro, Inc. | formulações de niraparibe |
| EP3773502A4 (en) * | 2018-04-06 | 2022-05-18 | UCAR Health GmbH | TREATMENT OF CANCER BY GUANIDINIUM DERIVATIVES |
| AU2019265629B2 (en) | 2018-05-09 | 2024-09-12 | Akebia Therapeutics, Inc. | Process for preparing 2-((5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl)amino)acetic acid |
| CN108754160B (zh) * | 2018-07-26 | 2020-05-08 | 江苏理工学院 | 一种吡哆醛含锰废水的回收利用方法 |
| EP3616725A1 (en) * | 2018-08-27 | 2020-03-04 | SmartDyeLivery GmbH | Pkc inhibitors for the treatment of septic cholestasis with polymethine dye targeting |
| CN109628570A (zh) * | 2018-12-07 | 2019-04-16 | 南方医科大学南方医院 | 一种检测TRIM29基因Tyr544Cys突变的试剂盒及其用途 |
| CN109394692B (zh) * | 2018-12-12 | 2020-09-25 | 中国药科大学 | 达沙替尼接枝型聚合物胶束、其冻干粉针剂及制备方法和应用 |
| EP3993898B1 (en) | 2019-07-01 | 2025-10-15 | Oakwood Laboratories, Llc | System and method for making microspheres and emulsions |
| KR20220042352A (ko) | 2019-07-03 | 2022-04-05 | 아토사 테라퓨틱스, 인크. | 엔독시펜의 서방성 조성물 |
| CN110491443B (zh) * | 2019-07-23 | 2022-04-01 | 华中师范大学 | 一种基于投影邻域非负矩阵分解的lncRNA蛋白质关联预测方法 |
| CA3168632A1 (en) * | 2020-01-30 | 2021-08-05 | Purcann Pharma Inc. | Method for preventing or reducing cannabaceae biomass decomposition |
| CN113045550A (zh) * | 2021-03-12 | 2021-06-29 | 深圳济康医药科技有限公司 | 一种三氮唑类衍生物及其制备方法和应用 |
| MX2024002060A (es) * | 2021-09-08 | 2024-03-01 | Eisai R&D Man Co Ltd | Composicion farmaceutica para tratar tumores solidos. |
| CN113929081B (zh) * | 2021-10-13 | 2023-04-14 | 西南大学 | 上下转换双发射全色光谱碳点及其合成方法和应用 |
| CN114425054A (zh) * | 2022-01-20 | 2022-05-03 | 中国人民解放军军事科学院军事医学研究院 | 一种蛋白酶体抑制剂Bortezomib在抗辐射损伤中的用途 |
| CN117205225B (zh) * | 2023-09-12 | 2024-05-31 | 湖南普瑞玛药物研究中心有限公司 | 栀子苷在制备治疗骨髓增殖性肿瘤药物中的应用 |
| CN117860948B (zh) * | 2024-03-12 | 2024-06-04 | 江西永通科技股份有限公司 | 一种医用复合功能型抗菌敷料及其制备方法 |
Family Cites Families (236)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2969364A (en) | 1957-12-26 | 1961-01-24 | Upjohn Co | Derivatives of 5-amino uracil |
| US3008491A (en) | 1959-05-04 | 1961-11-14 | Chapman Valve Mfg Co | Valve for concentric pipe lines |
| US3012976A (en) | 1959-11-02 | 1961-12-12 | Miles Lab | Specific test composition for occult blood |
| US3008281A (en) | 1960-07-14 | 1961-11-14 | Nat Dairy Prod Corp | Conveyor |
| US3299104A (en) | 1963-04-09 | 1967-01-17 | Leo Ab | Certain steroid nu-bis-(haloethyl)-carbamates |
| JPS59186924A (ja) | 1983-04-08 | 1984-10-23 | Kureha Chem Ind Co Ltd | ヒト免疫グロブリン結合抗腫瘍剤 |
| US5093330A (en) | 1987-06-15 | 1992-03-03 | Ciba-Geigy Corporation | Staurosporine derivatives substituted at methylamino nitrogen |
| US5035878A (en) | 1988-09-12 | 1991-07-30 | University Of Rochester | Use of dithiocarbamates to counteract myelosuppression |
| US5542935A (en) | 1989-12-22 | 1996-08-06 | Imarx Pharmaceutical Corp. | Therapeutic delivery systems related applications |
| US5395855A (en) | 1990-05-07 | 1995-03-07 | Ciba-Geigy Corporation | Hydrazones |
| US5484612A (en) | 1993-09-22 | 1996-01-16 | The Board Of Trustees Of The Leland Stanford Junior University | Method of treating a mammal having a solid tumor susceptible to treatment with cisplatin |
| US6326469B1 (en) | 1994-04-22 | 2001-12-04 | Sugen, Inc. | Megakaryocytic protein tyrosine kinases |
| US5747498A (en) | 1996-05-28 | 1998-05-05 | Pfizer Inc. | Alkynyl and azido-substituted 4-anilinoquinazolines |
| CA2224435C (en) | 1995-07-06 | 2008-08-05 | Novartis Ag | Pyrrolopyrimidines and processes for the preparation thereof |
| US6011069A (en) | 1995-12-26 | 2000-01-04 | Nisshin Flour Milling Co., Ltd. | Multidrug resistance inhibitors |
| US20020077461A1 (en) | 1996-04-24 | 2002-06-20 | Soren Bjorn | Pharmaceutical formulation |
| EP0923941B1 (en) | 1996-06-27 | 2006-05-17 | Chugai Seiyaku Kabushiki Kaisha | Remedies for myeloma to be used together with nitrogen mustard antitumor agents |
| US6121245A (en) | 1997-01-29 | 2000-09-19 | Firshein; Richard N. | Method of treating cancer using alkylglycerols in conjunction with chemotherapy |
| CO4950519A1 (es) | 1997-02-13 | 2000-09-01 | Novartis Ag | Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion |
| US20040072889A1 (en) | 1997-04-21 | 2004-04-15 | Pharmacia Corporation | Method of using a COX-2 inhibitor and an alkylating-type antineoplastic agent as a combination therapy in the treatment of neoplasia |
| CA2294247C (en) | 1997-07-01 | 2004-10-26 | Atherogenics, Inc. | Antioxidant enhancement of therapy for hyperproliferative conditions |
| GB9721069D0 (en) | 1997-10-03 | 1997-12-03 | Pharmacia & Upjohn Spa | Polymeric derivatives of camptothecin |
| AU745880B2 (en) | 1998-05-21 | 2002-04-11 | Isis Pharmaceuticals, Inc. | Compositions and methods for non-parenteral delivery of oligonucleotides |
| AU4543899A (en) | 1998-06-08 | 1999-12-30 | Advanced Medicine, Inc. | Multibinding inhibitors of microsomal triglyceride transferase protein |
| KR20000011247A (ko) * | 1998-07-23 | 2000-02-25 | 김윤 | 다당류를이용한대장선택성약물전달조성물및약학제제 |
| BR9912938B1 (pt) | 1998-08-11 | 2011-06-28 | derivados de isoquinolina, composição que os compreende, processo para preparação e uso dos mesmos. | |
| US6326390B1 (en) | 1998-08-25 | 2001-12-04 | King Pharmaceuticals Reseach And Development, Inc. | Use of adenosine A3 receptor antagonists to inhibit tumor growth |
| EP1165085B1 (en) | 1999-03-30 | 2006-06-14 | Novartis AG | Phthalazine derivatives for treating inflammatory diseases |
| US7534866B2 (en) | 2005-10-19 | 2009-05-19 | Ibc Pharmaceuticals, Inc. | Methods and compositions for generating bioactive assemblies of increased complexity and uses |
| US6635677B2 (en) | 1999-08-13 | 2003-10-21 | Case Western Reserve University | Methoxyamine combinations in the treatment of cancer |
| WO2008109417A1 (en) | 2007-03-02 | 2008-09-12 | Case Western Reserve University | Mgmt inhibitor combinations for the treatment of neoplastic disorders |
| US7811981B2 (en) | 1999-08-30 | 2010-10-12 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Methods of and compositions for inhibiting the proliferation of mammalian cells |
| US20030072794A1 (en) | 2000-06-09 | 2003-04-17 | Teni Boulikas | Encapsulation of plasmid DNA (lipogenes™) and therapeutic agents with nuclear localization signal/fusogenic peptide conjugates into targeted liposome complexes |
| DE60141963D1 (de) | 2000-06-23 | 2010-06-10 | Mitsubishi Tanabe Pharma Corp | Antitumoreffekt-verstärker |
| PE20020354A1 (es) | 2000-09-01 | 2002-06-12 | Novartis Ag | Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda) |
| US6733783B2 (en) | 2000-10-30 | 2004-05-11 | Euro-Celtique S.A. | Controlled release hydrocodone formulations |
| ITMI20002358A1 (it) | 2000-10-31 | 2002-05-01 | Flavio Moroni | Derivati di tieno ,2, 3-c|isochinolin-3-one come inibitori della poli(a dp-ribosio)polimerasi |
| US7619005B2 (en) | 2000-11-01 | 2009-11-17 | Cognition Pharmaceuticals Llc | Methods for treating cognitive impairment in humans with Multiple Sclerosis |
| US20100098691A1 (en) | 2001-01-24 | 2010-04-22 | S'bio Pte Ltd | Combination of benzimidazole anti-cancer agent and a second anti-cancer agent |
| TWI238824B (en) | 2001-05-14 | 2005-09-01 | Novartis Ag | 4-amino-5-phenyl-7-cyclobutyl-pyrrolo[2,3-d]pyrimidine derivatives |
| US7318931B2 (en) | 2001-06-21 | 2008-01-15 | Genentech, Inc. | Sustained release formulation |
| US20030158118A1 (en) | 2001-11-26 | 2003-08-21 | Weidner Morten Sloth | Combination of cimetidine and cysteine derivatives for treating cancer |
| US7045534B2 (en) | 2002-02-12 | 2006-05-16 | The Board Of Trustees Of The Leland Stanford Junior University | Methods of reducing angiogenesis |
| WO2003070823A2 (en) | 2002-02-20 | 2003-08-28 | The General Hospital Corporation | Conjugates comprising a biodegradable polymer and uses therefor |
| US8580782B2 (en) | 2002-09-04 | 2013-11-12 | Merck Sharp & Dohme Corp. | Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors |
| AU2003280191A1 (en) | 2002-11-12 | 2004-06-03 | Raquel Silvia Aloyz | Combination of a nitrogen mustard analogue and imatinib for the treatment of chronic lymphocytic leukemia |
| WO2004060313A2 (en) | 2002-12-30 | 2004-07-22 | Celgene Corporation | Fluoroalkoxy-substituted 1, 3-dihydro-isoindolyl compounds and their pharmaceutical uses |
| ES2502490T3 (es) | 2003-02-26 | 2014-10-03 | Sugen, Inc. | Compuestos aminoheteroarílicos como inhibidores de proteín quinasas |
| US20070207952A1 (en) | 2003-03-24 | 2007-09-06 | Sequoia Pharmaceuticals | Long Acting Biologically Active Conjugates |
| EP1613308A4 (en) | 2003-03-27 | 2008-02-20 | Lankenau Inst Medical Res | CANCER TREATMENT METHODS |
| ZA200507752B (en) | 2003-03-28 | 2007-01-31 | Threshold Pharmaceuticals Inc | Compositions and methods for treating cancer |
| WO2004103958A2 (en) | 2003-05-19 | 2004-12-02 | Michigan State University | Preparation of hymenialdisine derivatives and use thereof |
| US7842835B2 (en) | 2003-07-07 | 2010-11-30 | Georgetown University | Histone deacetylase inhibitors and methods of use thereof |
| MXPA06001483A (es) | 2003-08-07 | 2006-05-15 | Schering Corp | Inhibidores novedosos de la proteina farnesil transferasa como agentes antitumorales. |
| WO2005023246A1 (en) | 2003-09-04 | 2005-03-17 | Aventis Pharmaceuticals Inc. | Substituted indoles as inhibitors of poly (adp-ribose) polymerase (parp) |
| HUP0303313A2 (hu) | 2003-10-09 | 2005-07-28 | Richter Gedeon Vegyészeti Gyár Rt. | Transzdermális gyógyszerkészítmények |
| US7491725B2 (en) | 2004-02-06 | 2009-02-17 | Bristol-Myers Squibb Company | Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors |
| US8435539B2 (en) | 2004-02-13 | 2013-05-07 | Immunomedics, Inc. | Delivery system for cytotoxic drugs by bispecific antibody pretargeting |
| US8652484B2 (en) | 2004-02-13 | 2014-02-18 | Immunomedics, Inc. | Delivery system for cytotoxic drugs by bispecific antibody pretargeting |
| WO2005092326A1 (en) | 2004-03-22 | 2005-10-06 | The Regents Of The University Of Michigan | Small molecule antagonists of xiap family proteins |
| US7754897B2 (en) | 2005-06-15 | 2010-07-13 | Cardiome Pharma Corp. | Synthetic processes for the preparation of aminocyclohexyl ether compounds |
| AU2005230682B2 (en) | 2004-04-05 | 2010-10-21 | Merck Hdac Research, Llc | Histone deacetylase inhibitor prodrugs |
| TW200538149A (en) | 2004-05-20 | 2005-12-01 | Telik Inc | Sensitization to another anticancer therapy and/or amelioration of a side effect of another anticancer therapy by treatment with a GST-activated anticancer compound |
| TW200600091A (en) | 2004-05-21 | 2006-01-01 | Telik Inc | Sulfonylethyl phosphorodiamidates |
| CA2569826C (en) | 2004-06-30 | 2013-07-16 | Janssen Pharmaceutica N.V. | Substituted 2-alkyl quinazolinone derivatives as parp inhibitors |
| ATE456579T1 (de) | 2004-07-20 | 2010-02-15 | Genentech Inc | Angiopoietin-like 4 protein hemmer kombinationen und deren verwendung |
| SE0402025D0 (sv) | 2004-08-13 | 2004-08-13 | Active Biotech Ab | Treatment of hyperproliferative disease with superantigens in combination with another anticancer agent |
| US20060100226A1 (en) | 2004-09-10 | 2006-05-11 | Sikorski James A | 2-Thiopyrimidinones as therapeutic agents |
| CN101223175B (zh) | 2005-01-19 | 2013-03-27 | 卫材有限公司 | 二氮杂苯并[de]蒽-3-酮化合物及抑制PARP的方法 |
| US7884094B2 (en) | 2005-02-17 | 2011-02-08 | Synta Pharmaceuticals Corp. | Compounds for the treatment of proliferative disorders |
| US7872050B2 (en) | 2005-03-14 | 2011-01-18 | Yaupon Therapeutics Inc. | Stabilized compositions of volatile alkylating agents and methods of using thereof |
| EP1907444B1 (en) | 2005-04-01 | 2009-08-19 | Intezyne Technologies Incorporated | Polymeric micelles for drug delivery |
| US20060229277A1 (en) | 2005-04-08 | 2006-10-12 | Orbus Pharma, Inc. | Stabilized pharmaceutical compositions comprising an HMG-CoA reductase inhibitor |
| US7728026B2 (en) | 2005-04-11 | 2010-06-01 | Abbott Laboratories, Inc. | 2-substituted-1 h-benzimidazile-4-carboxamides are PARP inhibitors |
| WO2006123185A2 (en) | 2005-05-19 | 2006-11-23 | Merck Sharp & Dohme Limited | Sulphamides for treatment of cancer |
| CA2609343C (en) | 2005-06-07 | 2015-03-31 | Yale University | Methods of treating cancer and other conditions or disease states using lfmau and ldt |
| DK1896421T3 (da) | 2005-06-23 | 2012-01-09 | Merck Sharp & Dohme | Benzocyclohetapyridiner som hæmmere af receptoren tyrosinkinase MET |
| LT1912671T (lt) | 2005-07-18 | 2017-12-11 | Seattle Genetics, Inc. | Vaisto konjugatai, turintys gliukoronido linkerį |
| CN101300233A (zh) | 2005-09-09 | 2008-11-05 | 先灵公司 | 氮杂稠合的细胞周期蛋白依赖性激酶抑制剂 |
| US8378117B2 (en) | 2005-09-23 | 2013-02-19 | Janssen Pharmaceutica N.V. | Hexahydro-cycloheptapyrazole cannabinoid modulators |
| CA2626016A1 (en) | 2005-10-21 | 2007-06-21 | Panacea Biotec Limited | Pharmaceutical composition comprising at least one anticancer drug and at least one polymer |
| US7528142B2 (en) | 2005-11-03 | 2009-05-05 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| AU2006322314A1 (en) | 2005-11-18 | 2007-06-14 | Synthon B.V. | Zolpidem tablets |
| US8324262B2 (en) | 2005-12-20 | 2012-12-04 | The Brigham And Women's Hospital, Inc. | Tricyclic necrostatin compounds |
| WO2007081751A2 (en) | 2006-01-05 | 2007-07-19 | The Johns Hopkins University | Compositions and methods for the treatment of cancer |
| US7910607B2 (en) * | 2006-03-10 | 2011-03-22 | The Trustees Of California State University | Nitroxide free radical synergized antineoplastic agents |
| WO2007106555A2 (en) | 2006-03-14 | 2007-09-20 | Neuren Pharmaceuticals Limited | Oral formulations of glycyl-2-methylprolyl-glutamate |
| ATE470665T1 (de) | 2006-03-22 | 2010-06-15 | Janssen Pharmaceutica Nv | Cycloalkylaminderivate als inhibitoren der wechselwirkung zwischen mdm2 und p53 |
| US20100261758A1 (en) | 2006-03-28 | 2010-10-14 | Novartis Ag | Heterocyclic amides for use as pharmaceuticals |
| CN102671196B (zh) | 2006-04-05 | 2014-12-03 | 诺华股份有限公司 | 用于治疗癌症的治疗剂的组合 |
| AU2007243519A1 (en) | 2006-04-26 | 2007-11-08 | Merck Sharp & Dohme Corp. | Disubstituted aniline compounds |
| GB0609378D0 (en) | 2006-05-11 | 2006-06-21 | Novartis Ag | Organic compounds |
| EP2023924B1 (en) | 2006-05-18 | 2016-08-03 | Merck Sharp & Dohme Corp. | Aryl-fused spirocyclic compounds |
| US8034834B2 (en) | 2006-05-25 | 2011-10-11 | Synta Pharmaceuticals Corp. | Method for treating proliferative disorders with HSP90 inhibitors |
| TWI490212B (zh) | 2006-05-25 | 2015-07-01 | Synta Pharmaceuticals Corp | 調節ｈｓｐ９０活性之三唑化合物 |
| WO2007149907A2 (en) | 2006-06-20 | 2007-12-27 | Abbott Laboratories | Pyrazoloquinazolinones as parp inhibitors |
| US7964728B2 (en) | 2006-07-06 | 2011-06-21 | Solvay Pharmaceuticals B.V. | Azaindole derivatives with a combination of partial nicotinic acetyl-choline receptor agonism and dopamine reuptake inhibition |
| US20080213249A1 (en) | 2006-07-07 | 2008-09-04 | The Scripps Research Insitute | Use of Retro-Aldol Reaction to Generate Reactive Vinyl Ketone for Attachment to Antibody Molecules by Michael Addition Reaction for Use in Immunostaining and Immunotargeting |
| TW200813021A (en) | 2006-07-10 | 2008-03-16 | Merck & Co Inc | Tyrosine kinase inhibitors |
| WO2008009407A2 (en) | 2006-07-17 | 2008-01-24 | Novartis Ag | Sulphonylaminocarbonyl derivatives of bile acid amides for use as immunomodulators |
| AU2007276760B2 (en) | 2006-07-24 | 2012-01-19 | Tetralogic Pharmaceuticals Corporation | Dimeric IAP antagonists |
| TW200817410A (en) | 2006-08-07 | 2008-04-16 | Incyte Corp | Triazolotriazines as kinase inhibitors |
| PT2068930E (pt) | 2006-08-07 | 2012-10-23 | Abbott Biotherapeutics Corp | Composições e métodos utilizando anticorpos anti-cs1 para tratar mieloma múltiplo |
| WO2008021364A2 (en) | 2006-08-17 | 2008-02-21 | Synta Pharmaceuticals Corp. | Triazole compounds that modulate hsp90 activity |
| US20080085882A1 (en) * | 2006-08-18 | 2008-04-10 | University Of North Texas Health Science Center At Fort Worth | Compositions and Methods for Potentiation of Cancer Agents |
| WO2008022771A1 (en) | 2006-08-23 | 2008-02-28 | Novartis Ag | Amides as sphingomyeline inhibitors |
| JP5190365B2 (ja) | 2006-08-23 | 2013-04-24 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | フェノキシピリジン誘導体の塩またはその結晶およびそれらの製造方法 |
| ES2528316T3 (es) | 2006-09-01 | 2015-02-06 | Senhwa Biosciences, Inc. | Moduladores de la serina-treonina proteína quinasa y de PARP |
| WO2008030408A2 (en) | 2006-09-05 | 2008-03-13 | Yale University | Proteomimetic compounds as inhibitors of the interaction of a nuclear receptor with coactivator peptides |
| DK2529622T3 (en) | 2006-09-22 | 2018-05-07 | Pharmacyclics Llc | INHIBITORS OF BRUTON-TYROSINKINASE |
| WO2008044029A1 (en) | 2006-10-12 | 2008-04-17 | Astex Therapeutics Limited | Pharmaceutical combinations |
| US8242080B2 (en) | 2006-10-13 | 2012-08-14 | The Regents Of The University Of California | Inhibitors of the EGFR kinase targeting the asymmetric activating dimer interface |
| UY30639A1 (es) | 2006-10-17 | 2008-05-31 | Kudos Pharm Ltd | Derivados sustituidos de 2h-ftalazin-1-ona, sus formas cristalinas, proceso de preparacion y aplicaciones |
| US7842278B2 (en) | 2006-10-27 | 2010-11-30 | Natural Pharmacia International, Inc. | Hypoxia-selective, weakly basic 2-nitroimidazole delivery agents and methods of use thereof |
| JP5103604B2 (ja) | 2006-10-31 | 2012-12-19 | メルク・シャープ・アンド・ドーム・コーポレーション | プロテインキナーゼ阻害剤としての２−アミノチアゾール−４−カルボン酸アミド |
| MY146474A (en) | 2006-11-06 | 2012-08-15 | Supergen Inc | Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors |
| US20120164075A1 (en) | 2006-11-21 | 2012-06-28 | Jina Pharmaceuticals, Inc. | Endoxifen methods and compositions in the treatment of mammalian diseases |
| US20080125397A1 (en) | 2006-11-28 | 2008-05-29 | Telik, Inc. | 2 (SULFONYL)ETHYL N,N,N',N' tetrakis(2 chloroethyl)phosphorodia |
| US7655799B2 (en) | 2006-11-29 | 2010-02-02 | Telik, Inc. | 2{[2-(substituted amino)ethyl]sulfonyl}ethyl N,N,N',N'-tetrakis(2-chloroethyl)phosphorodiamidates |
| US8536113B2 (en) | 2006-12-21 | 2013-09-17 | Janssen Biotech, Inc. | EGFR binding peptides and uses thereof |
| US8834920B2 (en) | 2006-12-21 | 2014-09-16 | Alza Corporation | Liposome composition for targeting egfr receptor |
| US20080293648A1 (en) | 2007-01-05 | 2008-11-27 | Saha Pharmaceuticals, Inc. | Compositions and Methods for Cancer Treatment |
| US8470323B2 (en) | 2007-01-09 | 2013-06-25 | The Trustees Of The University Of Pennsylvania | Drug delivery to human tissues by single chain variable region antibody fragments cloned by phage display |
| US8398956B2 (en) | 2007-01-11 | 2013-03-19 | Immunomedics, Inc. | In vivo copper-free click chemistry for delivery of therapeutic and/or diagnostic agents |
| ATE483685T1 (de) | 2007-02-06 | 2010-10-15 | Novartis Ag | 1-benzensulfonyl-1h-indol-derivate als hemmer der ccr9-aktivität |
| EP2120900A2 (en) | 2007-02-15 | 2009-11-25 | Novartis AG | Combination of lbh589 with other therapeutic agents for treating cancer |
| AU2008221358A1 (en) | 2007-02-28 | 2008-09-04 | Inotek Pharmaceuticals Corporation | Indenoisoquinolinone analogs and methods of use thereof |
| CA2678248C (en) | 2007-03-08 | 2016-06-28 | Janssen Pharmaceutica Nv | Quinolinone derivatives as parp and tank inhibitors |
| AU2008226532B2 (en) | 2007-03-09 | 2011-09-22 | The Regents Of The University Of Michigan | Compositions and methods relating to novel compounds and targets thereof |
| WO2008112277A2 (en) | 2007-03-13 | 2008-09-18 | Wake Forest University | Compositions and methods for treating cancer |
| WO2008116053A2 (en) | 2007-03-20 | 2008-09-25 | Trustees Of Tufts College | Fap-activated chemotherapeutic compounds, and methods of use thereof |
| DK2139484T3 (da) | 2007-04-10 | 2013-10-21 | Exelixis Inc | Fremgangsmåder til behandling af cancer ved brug af pyridopyrimidinon-inhibitorer af PI3K-alfa |
| CA2681311A1 (en) | 2007-04-13 | 2008-10-23 | Novartis Ag | Pyridazine-, pyridine- and pyrane-derivatives as gpbar1 agonisis |
| JP5498936B2 (ja) | 2007-04-18 | 2014-05-21 | メルク・シャープ・アンド・ドーム・コーポレーション | Ｓｍｏアンタゴニストであるトリアゾール誘導体 |
| TWI448284B (zh) | 2007-04-24 | 2014-08-11 | Theravance Inc | 雙效抗高血壓劑 |
| AT505225A1 (de) | 2007-04-26 | 2008-11-15 | Sanochemia Pharmazeutika Ag | 0erfahren zur herstellung von hoch reinem 2,4'-dimethyl-3-piperidino-propiophenon (tolperison), dieses enthaltende pharmazeutische zusammensetzungen, sowie tolperison enthaltende wirkstoffformulierungen |
| US7838495B2 (en) | 2007-04-27 | 2010-11-23 | University Of Maryland, Baltimore | Compositions and methods of use of EPB1, and ErbB3 binding protein |
| WO2008137619A2 (en) | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Thiazoles and pyrazoles useful as kinase inhibitors |
| HRP20130920T1 (hr) | 2007-05-15 | 2013-11-08 | Otsuka Pharmaceutical Co., Ltd. | Postupak uporabe antagonista vazopresina s kemoterapijom antraciklina radi snižavanja kardiotoksiäśnosti i/ili poboljšanja stope preživljavanja |
| US20110021440A1 (en) | 2007-05-16 | 2011-01-27 | University Of Maryland, Baltimore | Apoptotic pathway targeting for the diagnosis and treatment of cancer |
| US20110288023A1 (en) | 2007-06-08 | 2011-11-24 | The Regents Of The University Of California Office Of Technology Transfer | Cancer drug delivery using modified transferrin |
| WO2009003911A1 (en) | 2007-06-29 | 2009-01-08 | 4Sc Ag | Thiophene-imidazopyridines |
| JP2010532756A (ja) | 2007-07-06 | 2010-10-14 | オーエスアイ・ファーマスーティカルズ・インコーポレーテッド | ｍＴＯＲＣ１及びｍＴＯＲＣ２の両方の阻害剤を含む組み合わせ抗癌療法 |
| ES2776406T3 (es) | 2007-07-12 | 2020-07-30 | Gitr Inc | Terapias de combinación que emplean moléculas de enlazamiento a GITR |
| ES2411907T3 (es) | 2007-08-03 | 2013-07-09 | Facet Biotech Corporation | Uso terapéutico de anticuerpos antirreceptor TWEAK |
| WO2009022642A1 (ja) | 2007-08-10 | 2009-02-19 | Mitsubishi Tanabe Pharma Corporation | 新規なイソキノリン化合物の塩及びその結晶 |
| HRP20160949T1 (hr) | 2007-09-10 | 2016-10-07 | Boston Biomedical, Inc. | Novi sastavi i metode za liječenje karcinoma |
| SI2209375T1 (sl) | 2007-10-03 | 2014-12-31 | Eisai Inc. | Spojine inhibitorja PARP in metode uporabe |
| WO2009045504A1 (en) | 2007-10-04 | 2009-04-09 | President And Fellows Of Harvard College | Methods and compositions for treating cancer and modulating signal transduction and metabolism pathways |
| SI2211904T1 (sl) | 2007-10-19 | 2016-12-30 | Seattle Genetics, Inc. | CD19 vezavna sredstva in njihove uporabe |
| AU2008317406B2 (en) | 2007-10-25 | 2013-07-18 | Merck Sharp & Dohme Corp. | Therapeutic compounds |
| CN102112492B (zh) | 2007-11-14 | 2015-02-25 | 中外制药株式会社 | 使用抗gpr49抗体的癌症的诊断和治疗 |
| ES2524787T3 (es) | 2007-11-15 | 2014-12-12 | Msd Italia S.R.L. | Derivados de piridazinona como inhibidores de PARP |
| WO2009076629A2 (en) | 2007-12-12 | 2009-06-18 | The Regents Of The University Of Michigan | Compositions and methods for treating cancer |
| EP2240172B1 (en) | 2007-12-21 | 2014-03-19 | Novartis AG | Combination of nilotinib and chlorambucil for the treatment of chronic lymphocytic leukemia |
| US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
| JP2011511078A (ja) | 2008-02-06 | 2011-04-07 | レアド トヘラペウトイクス，インコーポレーテッド | ポリ（ａｄｐリボース）ポリメラーゼ（ｐａｒｐ）のベンズオキサゾールカルボキサミド阻害剤 |
| JP2011511076A (ja) | 2008-02-08 | 2011-04-07 | エイルロン セラピューティクス，インコーポレイテッド | 治療用ペプチド模倣大環状分子 |
| WO2009102707A2 (en) | 2008-02-11 | 2009-08-20 | Auspex Pharmaceuticals, Inc. | Substituted oxazaphosphorines |
| US20110046071A1 (en) | 2008-03-05 | 2011-02-24 | Tel Hashomer Medical Research Infrastructure And Services Ltd. | GLP-1 Receptor Agonists And Related Active Pharmaceutical Ingredients For Treatment Of Cancer |
| BRPI0909040B8 (pt) | 2008-03-11 | 2021-05-25 | Incyte Holdings Corp | derivados de azetidina e ciclobutano, seus usos, e composição |
| WO2009123971A1 (en) | 2008-03-31 | 2009-10-08 | Genentech, Inc. | Benzopyran and benzoxepin pi3k inhibitor compounds and methods of use |
| EP2110377A1 (en) | 2008-04-15 | 2009-10-21 | DAC S.r.l. | Spirocyclic derivatives as histone deacetylase inhibitors |
| KR101764927B1 (ko) | 2008-04-30 | 2017-08-03 | 이뮤노젠 아이엔씨 | 가교제 및 그 용도 |
| WO2009143018A2 (en) | 2008-05-19 | 2009-11-26 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
| EP2303269B1 (en) | 2008-06-03 | 2014-07-30 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| GB2475183B (en) | 2008-06-04 | 2011-11-23 | Gw Pharma Ltd | Cannabinoids in combination with non-cannabinoid chemotherapeutic agent that are selective estrogen receptor modulators |
| EP2133334A1 (en) | 2008-06-09 | 2009-12-16 | DAC S.r.l. | Heterocyclic derivatives as HDAC inhibitors |
| US8207195B2 (en) | 2008-06-26 | 2012-06-26 | Inspire Pharmaceuticals, Inc. | Method for treating neurological and neuropathic diseases using rho kinase inhibitor compounds |
| MX2011000235A (es) | 2008-07-08 | 2011-02-23 | Incyte Corp | 1,2,5-oxadiazoles como inhibidores de indolamina 2,3-dioxigenasa. |
| EP2307027A4 (en) | 2008-07-11 | 2012-08-15 | Neumedics | TETRACYCLINE DERIVATIVES WITH REDUCED ANTIBIOTIC ACTIVITY AND NEUROPROTECTIVE PROPERTIES |
| CA2726460C (en) | 2008-07-15 | 2017-02-21 | F. Hoffmann-La Roche Ag | Novel phenyl-imidazopyridines and pyridazines |
| US20110224235A1 (en) | 2008-07-16 | 2011-09-15 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors |
| WO2010009334A1 (en) | 2008-07-17 | 2010-01-21 | Colorado State University Research Foundation | Method for preparing largazole analogs and uses thereof |
| US20120230991A1 (en) | 2008-07-29 | 2012-09-13 | Douglas Kim Graham | Methods and compounds for enhancing anti-cancer therapy |
| WO2010021822A2 (en) | 2008-07-30 | 2010-02-25 | The Regents Of The University Of California | Discovery of candidate biomarkers of in vivo apoptosis by global profiling of caspase cleavage sites |
| ES2438496T3 (es) | 2008-08-01 | 2014-01-17 | Ventirx Pharmaceuticals, Inc. | Formulaciones de agonistas de receptores de tipo toll y su uso |
| EP2326650B9 (en) | 2008-08-06 | 2014-09-10 | BioMarin Pharmaceutical Inc. | Dihydropyridophthalazinone inhibitors of poly(adp-ribose)polymerase (parp) |
| CN102186857A (zh) | 2008-08-26 | 2011-09-14 | 贝林格尔·英格海姆国际有限公司 | 用于药物组合物的噻吩并嘧啶 |
| US20100068302A1 (en) | 2008-09-17 | 2010-03-18 | Traslational Cancer Drugs Pharma, S.L. | Methods and compositions for the treatment of cancer |
| EP2346836B1 (en) | 2008-10-08 | 2018-03-07 | Cephalon, Inc. | Processes for the preparation of bendamustine |
| US8476282B2 (en) | 2008-11-03 | 2013-07-02 | Intellikine Llc | Benzoxazole kinase inhibitors and methods of use |
| US20100111901A1 (en) | 2008-11-03 | 2010-05-06 | Auspex Pharmaceuticals, Inc. | Triazole inhibitors of aromatase |
| UY32240A (es) | 2008-11-14 | 2010-06-30 | Boeringer Ingelheim Kg | Nuevas 2,4-diaminopirimidinas, sus sales farmacéuticamente aceptables, composiciones conteniéndolas y aplicaciones. |
| US20100150896A1 (en) | 2008-12-12 | 2010-06-17 | Auspex Pharmaceuticals, Inc. | Diaminoquinazoline inhibitors of dihydrofolate reductase |
| US20110318430A1 (en) | 2008-12-18 | 2011-12-29 | New York University | Tumor therapy with antitumor agents in combination with sindbis virus-based vectors |
| US20100173013A1 (en) | 2009-01-08 | 2010-07-08 | Denis Drygin | Treatment of neoplastic disorders using combination therapies |
| SG172885A1 (en) | 2009-01-23 | 2011-08-29 | Rigel Pharmaceuticals Inc | Compositions and methods for inhibition of the jak pathway |
| BRPI1007358A2 (pt) | 2009-01-23 | 2018-03-06 | Takeda Pharmaceutical Company Limited | inibidores de poli (adp-ribose) polimerase (parp) |
| CN102405044A (zh) | 2009-02-06 | 2012-04-04 | 南加利福尼亚大学 | 含有单萜的治疗组合物 |
| US8299077B2 (en) | 2009-03-02 | 2012-10-30 | Roche Palo Alto Llc | Inhibitors of Bruton's tyrosine kinase |
| KR101663339B1 (ko) | 2009-03-11 | 2016-10-06 | 플렉시콘 인코퍼레이티드 | Ｒａｆ 키나제의 억제를 위한 피롤로［２,３-ｂ］피리딘 유도체 |
| AU2010234916A1 (en) | 2009-03-30 | 2011-10-13 | Cerulean Pharma Inc. | Polymer-agent conjugates, particles, compositions, and related methods of use |
| WO2010114805A1 (en) | 2009-03-31 | 2010-10-07 | The Trustees Of The University Of Pennsylvania | Methods of treating cancer with phenformin |
| WO2010114881A1 (en) | 2009-04-01 | 2010-10-07 | Progenra Inc. | Anti-neoplastic compounds, compositions and methods |
| CN102448951B (zh) | 2009-04-06 | 2017-05-10 | 安吉奥斯医药品有限公司 | 丙酮酸激酶m2调节剂、治疗组合物和相关使用方法 |
| WO2010118078A1 (en) | 2009-04-08 | 2010-10-14 | Idenix Pharmaceuticals, Inc. | Macrocyclic serine protease inhibitors |
| US20100291025A1 (en) | 2009-04-13 | 2010-11-18 | Auspex Pharmaceuticals, Inc. | Indazole inhibitors of tyrosine kinase |
| JP5497152B2 (ja) | 2009-04-24 | 2014-05-21 | エフ．ホフマン−ラ ロシュ アーゲー | ブルトン型チロシンキナーゼの阻害薬 |
| US20110053968A1 (en) | 2009-06-09 | 2011-03-03 | Auspex Pharmaceuticals, Inc. | Aminopyrimidine inhibitors of tyrosine kinase |
| US9151762B2 (en) | 2009-06-12 | 2015-10-06 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Identification of DSG-3 as a biomarker for the detection of metastasis in lymph nodes |
| TWI491606B (zh) | 2009-07-13 | 2015-07-11 | Gilead Sciences Inc | 調節細胞凋亡信號之激酶的抑制劑 |
| US8232318B2 (en) | 2009-07-31 | 2012-07-31 | The General Hospital Corporation | Approaches to treat cancer using HB-EGF inhibitors |
| MY161541A (en) * | 2009-07-31 | 2017-04-28 | Shin Maeda | Cancer metastasis inhibitor |
| PL2470546T3 (pl) | 2009-08-28 | 2013-12-31 | Takeda Pharmaceuticals Co | Związki heksahydrooksazynopterydynowe do zastosowania jako inhibitory MTOR |
| BR112012005550A2 (pt) | 2009-09-11 | 2015-09-08 | Cylene Pharmaceuticals Inc | lactamas heterociclo-substituídas farmaceuticamente úteis |
| BR112012005970A2 (pt) | 2009-09-16 | 2015-09-08 | Cylene Pharmaceuticals Inc | moduladores tricíclicos de proteína quinase |
| RU2600927C2 (ru) | 2009-09-28 | 2016-10-27 | Ф.Хоффманн-Ля Рош Аг | Бензоксазепиновые ингибиторы pi3k и способы применения |
| US7718662B1 (en) | 2009-10-12 | 2010-05-18 | Pharmacyclics, Inc. | Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase |
| CN110054692A (zh) | 2009-10-23 | 2019-07-26 | 米伦纽姆医药公司 | 抗gcc抗体分子及其相关组合物和方法 |
| CA3063465C (en) | 2009-11-18 | 2023-01-03 | Nektar Therapeutics | Acid salt forms of polymer-drug conjugates and alkoxylation methods |
| AU2010326268B2 (en) | 2009-12-04 | 2016-11-03 | Senhwa Biosciences, Inc. | Pyrazolopyrimidines and related heterocycles as CK2 inhibitors |
| US20110195066A1 (en) | 2010-02-05 | 2011-08-11 | Auspex Pharmaceuticals, Inc. | Quinoline inhibitors of tyrosine kinase |
| WO2011100550A2 (en) | 2010-02-12 | 2011-08-18 | Alexander Vuckovic, M.D., Llc | Compositions and methods for treating depression |
| CA2790199A1 (en) | 2010-02-24 | 2011-09-01 | Auspex Pharmaceuticals, Inc. | Trimethoxyphenyl inhibitors of tyrosine kinase |
| UY33241A (es) | 2010-02-26 | 2011-09-30 | Boehringer Ingelheim Int | ?Tienopirimidinas que contienen heterocicloalquilo para composiciones farmacéuticas?. |
| TW201141483A (en) | 2010-02-26 | 2011-12-01 | Boehringer Ingelheim Int | Thienopyrimidines containing a substituted alkyl group for pharmaceutical compositions |
| WO2011109799A1 (en) | 2010-03-05 | 2011-09-09 | Karyopharm Therapeutics, Inc. | Nuclear transport modulatiors and uses thereof |
| MX2012012225A (es) | 2010-04-23 | 2013-08-27 | Piramal Entpr Ltd | Profármacos de agentes tearapéuticos de liberación de óxido nítrico. |
| MX2012013082A (es) | 2010-05-12 | 2013-05-09 | Vertex Pharma | Derivados de 2-aminopiridina utiles como iinhibidores de cinasa atr. |
| CA2800595C (en) | 2010-05-26 | 2018-04-24 | Shriners Hospitals For Children | Compositions comprising the nc2 domain of collagen ix and methods of using same |
| KR101580714B1 (ko) | 2010-06-03 | 2016-01-04 | 파마싸이클릭스 엘엘씨 | 브루톤 티로신 인산화효소(ｂｔｋ)의 억제제의 용도 |
| WO2012047339A2 (en) | 2010-06-28 | 2012-04-12 | The General Hospital Corporation | Anti-cxcr4 as a sensitizer to cancer therapeutics |
| SG10201802116RA (en) * | 2010-08-18 | 2018-04-27 | Del Mar Pharmaceuticals | Compositions and methods to improve the therapeutic benefit of suboptimally administered chemical compounds including substituted hexitols such as dianhydrogalactitol and diacetyldianhydrogalactitol |
| US20120213854A1 (en) | 2010-09-30 | 2012-08-23 | Fetzer Oliver S | Methods of treating a subject and related particles, polymers and compositions |
| EP2632939A4 (en) | 2010-10-25 | 2014-05-14 | Academia Sinica Taiwan | CANCER-TREATED PEPTIDES AND THEIR USE IN CANCER TREATMENT AND DIAGNOSIS |
| EP2637669A4 (en) | 2010-11-10 | 2014-04-02 | Infinity Pharmaceuticals Inc | Heterocyclic compounds and their use |
| BR122017028566B1 (pt) | 2010-11-12 | 2022-03-03 | Pharma Mar, S.A. | Uso de pm01183, ou um sal farmaceuticamente aceitável do mesmo, em combinação sinérgica com um antibiótico anticâncer e kit |
| US20140088021A1 (en) | 2011-05-27 | 2014-03-27 | Nektar Therapeutics | Water-Soluble Polymer-Linked Binding Moiety and Drug Compounds |
| US8637490B2 (en) | 2011-07-01 | 2014-01-28 | Uwm Research Foundation, Inc. | Anti-cancer agents |
| WO2013012894A1 (en) | 2011-07-18 | 2013-01-24 | The Ohio State University | Fty720 increases cd74 expression and sensitizes cancer cells to anti-cd74 antibody-mediated cell death |
| US10201521B2 (en) * | 2012-01-20 | 2019-02-12 | Del Mar Pharmaceuticals (Bc) Ltd. | Use of substituted hexitols including dianhydrogalactitol and analogs to treat neoplastic disease and cancer stem and cancer stem cells including glioblastoma multiforme and medulloblastoma |
| KR101374820B1 (ko) | 2012-01-30 | 2014-03-17 | 광주과학기술원 | 페오포르바이드-α 컨쥬게이트 및 그의 용도 |
| US8501724B1 (en) | 2012-01-31 | 2013-08-06 | Pharmacyclics, Inc. | Purinone compounds as kinase inhibitors |
| KR20250151610A (ko) | 2012-06-04 | 2025-10-21 | 파마싸이클릭스 엘엘씨 | 브루톤 타이로신 키나아제 저해제의 결정 형태 |
| US20140005148A1 (en) | 2012-06-29 | 2014-01-02 | Coldstream Laboratories Inc. | Stable liquid formulations of nitrogen mustards |
-
2014
- 2014-04-08 AU AU2014251038A patent/AU2014251038A1/en not_active Abandoned
- 2014-04-08 EP EP14782363.7A patent/EP2983674A4/en not_active Ceased
- 2014-04-08 WO PCT/US2014/033391 patent/WO2014168986A1/en not_active Ceased
- 2014-04-08 KR KR1020157032123A patent/KR20160061911A/ko not_active Ceased
- 2014-04-08 CN CN201480032586.8A patent/CN105492011A/zh active Pending
- 2014-04-08 US US14/783,137 patent/US11491154B2/en active Active
- 2014-04-08 JP JP2016507620A patent/JP2016519684A/ja active Pending
-
2019
- 2019-05-28 JP JP2019099028A patent/JP2019135268A/ja active Pending
- 2019-10-01 AU AU2019240599A patent/AU2019240599A1/en not_active Abandoned
-
2021
- 2021-10-27 AU AU2021257978A patent/AU2021257978A1/en not_active Abandoned
-
2022
- 2022-11-07 US US17/982,233 patent/US12336993B2/en active Active
-
2024
- 2024-02-02 AU AU2024200650A patent/AU2024200650A1/en not_active Abandoned
-
2025
- 2025-06-19 US US19/243,604 patent/US20250312347A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| AU2021257978A1 (en) | 2021-11-25 |
| US20160045502A1 (en) | 2016-02-18 |
| EP2983674A1 (en) | 2016-02-17 |
| JP2019135268A (ja) | 2019-08-15 |
| US11491154B2 (en) | 2022-11-08 |
| JP2016519684A (ja) | 2016-07-07 |
| AU2019240599A1 (en) | 2019-10-17 |
| US20250312347A1 (en) | 2025-10-09 |
| US20230133044A1 (en) | 2023-05-04 |
| EP2983674A4 (en) | 2017-05-10 |
| AU2024200650A1 (en) | 2024-02-22 |
| KR20160061911A (ko) | 2016-06-01 |
| WO2014168986A1 (en) | 2014-10-16 |
| CN105492011A (zh) | 2016-04-13 |
| US12336993B2 (en) | 2025-06-24 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US12336993B2 (en) | Therapeutic benefit of suboptimally administered chemical compounds | |
| AU2019283893B2 (en) | Use of dianhydrogalactitol and analogs and derivatives thereof to treat recurrent malignant glioma or progressive secondary brain tumor | |
| US20200206188A1 (en) | Compositions and methods to improve the therapeutic benefit of indirubin and analogs thereof, including meisoindigo | |
| AU2013280644B2 (en) | Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or AHI1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof | |
| AU2024200718A1 (en) | Compositions and methods to improve the therapeutic benefit of suboptimally administered chemical compounds including substituted hexitols such as dibromodulcitol |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MK5 | Application lapsed section 142(2)(e) - patent request and compl. specification not accepted |