OA13140A - Non-nucleosidic inhibitors of reverse transcripta se as antagonists of cell proliferation and inducers of cell differentiation. - Google Patents
Non-nucleosidic inhibitors of reverse transcripta se as antagonists of cell proliferation and inducers of cell differentiation. Download PDFInfo
- Publication number
- OA13140A OA13140A OA1200400180A OA1200400180A OA13140A OA 13140 A OA13140 A OA 13140A OA 1200400180 A OA1200400180 A OA 1200400180A OA 1200400180 A OA1200400180 A OA 1200400180A OA 13140 A OA13140 A OA 13140A
- Authority
- OA
- OAPI
- Prior art keywords
- nevirapine
- tumors
- compound
- cells
- cell
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title claims abstract description 18
- 230000024245 cell differentiation Effects 0.000 title abstract description 3
- 239000005557 antagonist Substances 0.000 title description 3
- 239000000411 inducer Substances 0.000 title description 3
- 230000004663 cell proliferation Effects 0.000 title description 2
- NQDJXKOVJZTUJA-UHFFFAOYSA-N nevirapine Chemical compound C12=NC=CC=C2C(=O)NC=2C(C)=CC=NC=2N1C1CC1 NQDJXKOVJZTUJA-UHFFFAOYSA-N 0.000 claims abstract description 155
- 229960000689 nevirapine Drugs 0.000 claims abstract description 73
- 206010028980 Neoplasm Diseases 0.000 claims abstract description 51
- 102100034343 Integrase Human genes 0.000 claims abstract description 40
- 108010092799 RNA-directed DNA polymerase Proteins 0.000 claims abstract description 40
- XPOQHMRABVBWPR-ZDUSSCGKSA-N efavirenz Chemical compound C([C@]1(C2=CC(Cl)=CC=C2NC(=O)O1)C(F)(F)F)#CC1CC1 XPOQHMRABVBWPR-ZDUSSCGKSA-N 0.000 claims abstract description 33
- XPOQHMRABVBWPR-UHFFFAOYSA-N Efavirenz Natural products O1C(=O)NC2=CC=C(Cl)C=C2C1(C(F)(F)F)C#CC1CC1 XPOQHMRABVBWPR-UHFFFAOYSA-N 0.000 claims abstract description 28
- 229960003804 efavirenz Drugs 0.000 claims abstract description 27
- 150000001875 compounds Chemical class 0.000 claims abstract description 24
- WHBIGIKBNXZKFE-UHFFFAOYSA-N delavirdine Chemical compound CC(C)NC1=CC=CN=C1N1CCN(C(=O)C=2NC3=CC=C(NS(C)(=O)=O)C=C3C=2)CC1 WHBIGIKBNXZKFE-UHFFFAOYSA-N 0.000 claims abstract description 19
- 230000007170 pathology Effects 0.000 claims abstract description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 7
- 229960005319 delavirdine Drugs 0.000 claims abstract description 3
- 150000003839 salts Chemical class 0.000 claims abstract 2
- 230000000694 effects Effects 0.000 claims description 21
- 206010006187 Breast cancer Diseases 0.000 claims description 10
- 208000026310 Breast neoplasm Diseases 0.000 claims description 10
- 201000008275 breast carcinoma Diseases 0.000 claims description 10
- 208000032839 leukemia Diseases 0.000 claims description 9
- 201000008808 Fibrosarcoma Diseases 0.000 claims description 7
- 201000008968 osteosarcoma Diseases 0.000 claims description 7
- 239000000203 mixture Substances 0.000 claims description 6
- 208000001608 teratocarcinoma Diseases 0.000 claims description 6
- 208000032612 Glial tumor Diseases 0.000 claims description 5
- 206010018338 Glioma Diseases 0.000 claims description 5
- 206010061311 nervous system neoplasm Diseases 0.000 claims description 4
- 239000000243 solution Substances 0.000 claims description 4
- 238000002347 injection Methods 0.000 claims description 3
- 239000007924 injection Substances 0.000 claims description 3
- 201000008806 mesenchymal cell neoplasm Diseases 0.000 claims description 3
- 206010053317 Hydrophobia Diseases 0.000 claims description 2
- 239000000969 carrier Substances 0.000 claims description 2
- 230000001413 cellular effect Effects 0.000 claims description 2
- 238000001990 intravenous administration Methods 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 239000002904 solvent Substances 0.000 claims description 2
- 239000000725 suspension Substances 0.000 claims description 2
- 201000009030 Carcinoma Diseases 0.000 claims 2
- POXWDTQUDZUOGP-UHFFFAOYSA-N 1h-1,4-diazepine Chemical class N1C=CC=NC=C1 POXWDTQUDZUOGP-UHFFFAOYSA-N 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000006187 pill Substances 0.000 claims 1
- 230000002209 hydrophobic effect Effects 0.000 abstract 1
- 210000004027 cell Anatomy 0.000 description 61
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 33
- 241000700159 Rattus Species 0.000 description 20
- SHGAZHPCJJPHSC-YCNIQYBTSA-N all-trans-retinoic acid Chemical compound OC(=O)\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-YCNIQYBTSA-N 0.000 description 13
- 230000014509 gene expression Effects 0.000 description 13
- 229930002330 retinoic acid Natural products 0.000 description 13
- 229960001727 tretinoin Drugs 0.000 description 13
- 241001529936 Murinae Species 0.000 description 12
- 238000011081 inoculation Methods 0.000 description 12
- 230000012010 growth Effects 0.000 description 11
- 206010073071 hepatocellular carcinoma Diseases 0.000 description 9
- 108090000623 proteins and genes Proteins 0.000 description 9
- 239000003814 drug Substances 0.000 description 8
- 238000011534 incubation Methods 0.000 description 8
- 238000003556 assay Methods 0.000 description 7
- 229940079593 drug Drugs 0.000 description 7
- 230000006698 induction Effects 0.000 description 7
- 238000000034 method Methods 0.000 description 7
- 239000002777 nucleoside Substances 0.000 description 7
- 108091032973 (ribonucleotides)n+m Proteins 0.000 description 6
- 229940063627 rescriptor Drugs 0.000 description 6
- 210000001519 tissue Anatomy 0.000 description 6
- 210000004881 tumor cell Anatomy 0.000 description 6
- 206010003445 Ascites Diseases 0.000 description 5
- 206010009944 Colon cancer Diseases 0.000 description 5
- 101000946889 Homo sapiens Monocyte differentiation antigen CD14 Proteins 0.000 description 5
- 102100035877 Monocyte differentiation antigen CD14 Human genes 0.000 description 5
- 230000007423 decrease Effects 0.000 description 5
- 210000003098 myoblast Anatomy 0.000 description 5
- 230000001225 therapeutic effect Effects 0.000 description 5
- 238000002560 therapeutic procedure Methods 0.000 description 5
- 208000030507 AIDS Diseases 0.000 description 4
- 102100035248 Alpha-(1,3)-fucosyltransferase 4 Human genes 0.000 description 4
- 101001022185 Homo sapiens Alpha-(1,3)-fucosyltransferase 4 Proteins 0.000 description 4
- 101001046686 Homo sapiens Integrin alpha-M Proteins 0.000 description 4
- 102100022338 Integrin alpha-M Human genes 0.000 description 4
- 241000699670 Mus sp. Species 0.000 description 4
- 108091034117 Oligonucleotide Proteins 0.000 description 4
- 238000004458 analytical method Methods 0.000 description 4
- 239000000427 antigen Substances 0.000 description 4
- 108091007433 antigens Proteins 0.000 description 4
- 102000036639 antigens Human genes 0.000 description 4
- 239000013592 cell lysate Substances 0.000 description 4
- 238000002474 experimental method Methods 0.000 description 4
- 238000001727 in vivo Methods 0.000 description 4
- -1 nucleoside compounds Chemical class 0.000 description 4
- 150000003833 nucleoside derivatives Chemical class 0.000 description 4
- 210000004940 nucleus Anatomy 0.000 description 4
- 230000008569 process Effects 0.000 description 4
- 230000004044 response Effects 0.000 description 4
- 229940054565 sustiva Drugs 0.000 description 4
- 230000004614 tumor growth Effects 0.000 description 4
- 102000006311 Cyclin D1 Human genes 0.000 description 3
- 108010058546 Cyclin D1 Proteins 0.000 description 3
- 102000004190 Enzymes Human genes 0.000 description 3
- 108090000790 Enzymes Proteins 0.000 description 3
- 208000010454 Experimental Liver Neoplasms Diseases 0.000 description 3
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 description 3
- JLCPHMBAVCMARE-UHFFFAOYSA-N [3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-[[3-[[3-[[3-[[3-[[3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-hydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methyl [5-(6-aminopurin-9-yl)-2-(hydroxymethyl)oxolan-3-yl] hydrogen phosphate Polymers Cc1cn(C2CC(OP(O)(=O)OCC3OC(CC3OP(O)(=O)OCC3OC(CC3O)n3cnc4c3nc(N)[nH]c4=O)n3cnc4c3nc(N)[nH]c4=O)C(COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3CO)n3cnc4c(N)ncnc34)n3ccc(N)nc3=O)n3cnc4c(N)ncnc34)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cc(C)c(=O)[nH]c3=O)n3cc(C)c(=O)[nH]c3=O)n3ccc(N)nc3=O)n3cc(C)c(=O)[nH]c3=O)n3cnc4c3nc(N)[nH]c4=O)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)O2)c(=O)[nH]c1=O JLCPHMBAVCMARE-UHFFFAOYSA-N 0.000 description 3
- 230000009471 action Effects 0.000 description 3
- 230000022131 cell cycle Effects 0.000 description 3
- 230000010261 cell growth Effects 0.000 description 3
- 238000006243 chemical reaction Methods 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 239000000284 extract Substances 0.000 description 3
- 210000005260 human cell Anatomy 0.000 description 3
- 238000010166 immunofluorescence Methods 0.000 description 3
- 210000001161 mammalian embryo Anatomy 0.000 description 3
- 230000000877 morphologic effect Effects 0.000 description 3
- 230000001105 regulatory effect Effects 0.000 description 3
- 230000008521 reorganization Effects 0.000 description 3
- 239000011550 stock solution Substances 0.000 description 3
- 229940098802 viramune Drugs 0.000 description 3
- 238000001262 western blot Methods 0.000 description 3
- NHBKXEKEPDILRR-UHFFFAOYSA-N 2,3-bis(butanoylsulfanyl)propyl butanoate Chemical compound CCCC(=O)OCC(SC(=O)CCC)CSC(=O)CCC NHBKXEKEPDILRR-UHFFFAOYSA-N 0.000 description 2
- 102000007469 Actins Human genes 0.000 description 2
- 108010085238 Actins Proteins 0.000 description 2
- 102000004266 Collagen Type IV Human genes 0.000 description 2
- 108010042086 Collagen Type IV Proteins 0.000 description 2
- 108010058545 Cyclin D3 Proteins 0.000 description 2
- 102100037859 G1/S-specific cyclin-D3 Human genes 0.000 description 2
- 241000282412 Homo Species 0.000 description 2
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical class C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 102000003505 Myosin Human genes 0.000 description 2
- 108060008487 Myosin Proteins 0.000 description 2
- 102100033254 Tumor suppressor ARF Human genes 0.000 description 2
- 230000001154 acute effect Effects 0.000 description 2
- 230000000259 anti-tumor effect Effects 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 238000004113 cell culture Methods 0.000 description 2
- 238000009109 curative therapy Methods 0.000 description 2
- 230000003247 decreasing effect Effects 0.000 description 2
- 231100000673 dose–response relationship Toxicity 0.000 description 2
- 210000002950 fibroblast Anatomy 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 239000003550 marker Substances 0.000 description 2
- 230000007246 mechanism Effects 0.000 description 2
- 210000003205 muscle Anatomy 0.000 description 2
- 239000002243 precursor Substances 0.000 description 2
- 102000004169 proteins and genes Human genes 0.000 description 2
- 230000002829 reductive effect Effects 0.000 description 2
- 210000000130 stem cell Anatomy 0.000 description 2
- 238000003786 synthesis reaction Methods 0.000 description 2
- JXYPNRIYAMXJSE-UHFFFAOYSA-N 1,4-diazepin-6-one Chemical compound O=C1C=NC=CN=C1 JXYPNRIYAMXJSE-UHFFFAOYSA-N 0.000 description 1
- ASOMNDIOOKDVDC-UHFFFAOYSA-N 1h-indol-2-yl-[4-[3-(propan-2-ylamino)pyridin-2-yl]piperazin-1-yl]methanone Chemical compound CC(C)NC1=CC=CN=C1N1CCN(C(=O)C=2NC3=CC=CC=C3C=2)CC1 ASOMNDIOOKDVDC-UHFFFAOYSA-N 0.000 description 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 description 1
- 102100021569 Apoptosis regulator Bcl-2 Human genes 0.000 description 1
- 101000719121 Arabidopsis thaliana Protein MEI2-like 1 Proteins 0.000 description 1
- 206010004173 Basophilia Diseases 0.000 description 1
- 235000014698 Brassica juncea var multisecta Nutrition 0.000 description 1
- 102000008186 Collagen Human genes 0.000 description 1
- 108010035532 Collagen Proteins 0.000 description 1
- 102000016736 Cyclin Human genes 0.000 description 1
- 108050006400 Cyclin Proteins 0.000 description 1
- 238000000116 DAPI staining Methods 0.000 description 1
- 108020004414 DNA Proteins 0.000 description 1
- 108020004437 Endogenous Retroviruses Proteins 0.000 description 1
- 108700039887 Essential Genes Proteins 0.000 description 1
- 102100038595 Estrogen receptor Human genes 0.000 description 1
- 229930183217 Genin Natural products 0.000 description 1
- 102100031181 Glyceraldehyde-3-phosphate dehydrogenase Human genes 0.000 description 1
- 208000031886 HIV Infections Diseases 0.000 description 1
- 101000971171 Homo sapiens Apoptosis regulator Bcl-2 Proteins 0.000 description 1
- 101000857677 Homo sapiens Runt-related transcription factor 1 Proteins 0.000 description 1
- 101000733249 Homo sapiens Tumor suppressor ARF Proteins 0.000 description 1
- 101900297506 Human immunodeficiency virus type 1 group M subtype B Reverse transcriptase/ribonuclease H Proteins 0.000 description 1
- 206010061598 Immunodeficiency Diseases 0.000 description 1
- 208000029462 Immunodeficiency disease Diseases 0.000 description 1
- 102100029604 Interferon alpha-inducible protein 27, mitochondrial Human genes 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 101710145242 Minor capsid protein P3-RTD Proteins 0.000 description 1
- 241000699666 Mus <mouse, genus> Species 0.000 description 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 description 1
- 101000986989 Naja kaouthia Acidic phospholipase A2 CM-II Proteins 0.000 description 1
- 238000012408 PCR amplification Methods 0.000 description 1
- 238000010222 PCR analysis Methods 0.000 description 1
- 238000010240 RT-PCR analysis Methods 0.000 description 1
- 241000251184 Rajiformes Species 0.000 description 1
- 101100439111 Rattus norvegicus Cebpd gene Proteins 0.000 description 1
- 108700005075 Regulator Genes Proteins 0.000 description 1
- 102100025373 Runt-related transcription factor 1 Human genes 0.000 description 1
- 102000004243 Tubulin Human genes 0.000 description 1
- 108090000704 Tubulin Proteins 0.000 description 1
- 241000700605 Viruses Species 0.000 description 1
- 238000010817 Wright-Giemsa staining Methods 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- 208000009956 adenocarcinoma Diseases 0.000 description 1
- 208000036878 aneuploidy Diseases 0.000 description 1
- 231100001075 aneuploidy Toxicity 0.000 description 1
- 230000003042 antagnostic effect Effects 0.000 description 1
- 230000001640 apoptogenic effect Effects 0.000 description 1
- 230000006907 apoptotic process Effects 0.000 description 1
- 108700042656 bcl-1 Genes Proteins 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 230000003197 catalytic effect Effects 0.000 description 1
- 230000018486 cell cycle phase Effects 0.000 description 1
- 230000010428 chromatin condensation Effects 0.000 description 1
- 229920001436 collagen Polymers 0.000 description 1
- 210000001072 colon Anatomy 0.000 description 1
- 239000002299 complementary DNA Substances 0.000 description 1
- 238000012258 culturing Methods 0.000 description 1
- 230000001086 cytosolic effect Effects 0.000 description 1
- XCLDDDHMRBWEKC-UHFFFAOYSA-N dapi staining Chemical compound C1=CC(C(=N)N)=CC=C1C1=CC2=CC=C(C(N)=N)[CH]C2=N1 XCLDDDHMRBWEKC-UHFFFAOYSA-N 0.000 description 1
- 150000004908 diazepines Chemical class 0.000 description 1
- 210000001840 diploid cell Anatomy 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 230000001804 emulsifying effect Effects 0.000 description 1
- 230000002255 enzymatic effect Effects 0.000 description 1
- 108010038795 estrogen receptors Proteins 0.000 description 1
- MHMNJMPURVTYEJ-UHFFFAOYSA-N fluorescein-5-isothiocyanate Chemical compound O1C(=O)C2=CC(N=C=S)=CC=C2C21C1=CC=C(O)C=C1OC1=CC(O)=CC=C21 MHMNJMPURVTYEJ-UHFFFAOYSA-N 0.000 description 1
- 238000001943 fluorescence-activated cell sorting Methods 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000012634 fragment Substances 0.000 description 1
- 108020004445 glyceraldehyde-3-phosphate dehydrogenase Proteins 0.000 description 1
- 210000003714 granulocyte Anatomy 0.000 description 1
- 230000009036 growth inhibition Effects 0.000 description 1
- 239000003966 growth inhibitor Substances 0.000 description 1
- 230000007813 immunodeficiency Effects 0.000 description 1
- 230000002163 immunogen Effects 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 description 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 230000000977 initiatory effect Effects 0.000 description 1
- 230000002452 interceptive effect Effects 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 229940043355 kinase inhibitor Drugs 0.000 description 1
- 230000000670 limiting effect Effects 0.000 description 1
- 238000011068 loading method Methods 0.000 description 1
- 239000006166 lysate Substances 0.000 description 1
- 210000004962 mammalian cell Anatomy 0.000 description 1
- 238000002844 melting Methods 0.000 description 1
- 230000008018 melting Effects 0.000 description 1
- 108020004999 messenger RNA Proteins 0.000 description 1
- 238000000386 microscopy Methods 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 230000004660 morphological change Effects 0.000 description 1
- 230000001338 necrotic effect Effects 0.000 description 1
- 108091008819 oncoproteins Proteins 0.000 description 1
- 102000027450 oncoproteins Human genes 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 1
- INAAIJLSXJJHOZ-UHFFFAOYSA-N pibenzimol Chemical compound C1CN(C)CCN1C1=CC=C(N=C(N2)C=3C=C4NC(=NC4=CC=3)C=3C=CC(O)=CC=3)C2=C1 INAAIJLSXJJHOZ-UHFFFAOYSA-N 0.000 description 1
- 239000013641 positive control Substances 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 238000002203 pretreatment Methods 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 230000008672 reprogramming Effects 0.000 description 1
- 238000003757 reverse transcription PCR Methods 0.000 description 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 description 1
- 230000011218 segmentation Effects 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 210000001057 smooth muscle myoblast Anatomy 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 230000036962 time dependent Effects 0.000 description 1
- 230000005945 translocation Effects 0.000 description 1
- 230000001960 triggered effect Effects 0.000 description 1
- 230000005748 tumor development Effects 0.000 description 1
- 231100000588 tumorigenic Toxicity 0.000 description 1
- 230000000381 tumorigenic effect Effects 0.000 description 1
- 210000000689 upper leg Anatomy 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/536—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ITRM20010767 ITRM20010767A1 (it) | 2001-12-24 | 2001-12-24 | Uso di 5.11-diidro-6h-dipirido1/4 3,2-b:2',3'-e|1/4 1.4|diazepine per la preparazione di composizioni farmaceutiche antitumorali. |
| ITMI20021833 ITMI20021833A1 (it) | 2002-08-19 | 2002-08-19 | Inibitori non nucleosidici della trascrittasi inversa come induttori del differenziamento cellulare. |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| OA13140A true OA13140A (en) | 2006-12-13 |
Family
ID=26332794
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| OA1200400180A OA13140A (en) | 2001-12-24 | 2002-12-23 | Non-nucleosidic inhibitors of reverse transcripta se as antagonists of cell proliferation and inducers of cell differentiation. |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US10507207B2 (de) |
| EP (1) | EP1469858B1 (de) |
| JP (1) | JP4336584B2 (de) |
| CN (1) | CN100450487C (de) |
| AP (1) | AP1958A (de) |
| AT (1) | ATE400276T1 (de) |
| AU (1) | AU2002358793B2 (de) |
| CA (1) | CA2471543C (de) |
| CY (1) | CY1108396T1 (de) |
| DE (1) | DE60227563D1 (de) |
| DK (1) | DK1469858T3 (de) |
| EA (1) | EA007004B1 (de) |
| ES (1) | ES2309222T3 (de) |
| HU (1) | HU229522B1 (de) |
| IL (2) | IL162680A0 (de) |
| MX (1) | MXPA04006205A (de) |
| NZ (1) | NZ534257A (de) |
| OA (1) | OA13140A (de) |
| PL (1) | PL211565B1 (de) |
| PT (1) | PT1469858E (de) |
| SI (1) | SI1469858T1 (de) |
| WO (1) | WO2003055493A1 (de) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2387405A2 (de) | 2009-01-13 | 2011-11-23 | ProteoSys AG | Pirenzepin als mittel für die krebstherapie |
| CA2796620A1 (en) * | 2010-06-04 | 2011-12-08 | North-West University | Injectable formulation |
| MX2015009546A (es) * | 2013-01-23 | 2015-11-25 | Alienor Farma | Dosificacion aumentada de efavirenz para el tratamiento de cancer. |
| WO2016156557A1 (en) | 2015-04-03 | 2016-10-06 | Alienor Farma | Monoclonal antibody to human line-1 orf2 protein and method for early detection of transforming cells in pre-neoplastic tissues of a human subject |
| CN113384585A (zh) * | 2021-04-16 | 2021-09-14 | 蓝龙药业(北京)有限公司 | 依法韦仑在制备治疗小细胞肺癌的药物中的应用 |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6258839B1 (en) * | 1997-12-24 | 2001-07-10 | Peter Mashava | Isolation of naturally occuring isoflavanone and some clinical uses thereof |
-
2002
- 2002-12-23 US US10/500,270 patent/US10507207B2/en not_active Expired - Fee Related
- 2002-12-23 CN CNB028260538A patent/CN100450487C/zh not_active Expired - Lifetime
- 2002-12-23 DK DK02793112T patent/DK1469858T3/da active
- 2002-12-23 ES ES02793112T patent/ES2309222T3/es not_active Expired - Lifetime
- 2002-12-23 HU HU0600841A patent/HU229522B1/hu not_active IP Right Cessation
- 2002-12-23 MX MXPA04006205A patent/MXPA04006205A/es active IP Right Grant
- 2002-12-23 WO PCT/EP2002/014727 patent/WO2003055493A1/en not_active Ceased
- 2002-12-23 NZ NZ534257A patent/NZ534257A/en not_active IP Right Cessation
- 2002-12-23 AP APAP/P/2004/003088A patent/AP1958A/en active
- 2002-12-23 OA OA1200400180A patent/OA13140A/en unknown
- 2002-12-23 AT AT02793112T patent/ATE400276T1/de active
- 2002-12-23 PL PL374038A patent/PL211565B1/pl unknown
- 2002-12-23 DE DE60227563T patent/DE60227563D1/de not_active Expired - Lifetime
- 2002-12-23 JP JP2003556070A patent/JP4336584B2/ja not_active Expired - Fee Related
- 2002-12-23 PT PT02793112T patent/PT1469858E/pt unknown
- 2002-12-23 SI SI200230724T patent/SI1469858T1/sl unknown
- 2002-12-23 CA CA2471543A patent/CA2471543C/en not_active Expired - Fee Related
- 2002-12-23 EA EA200400861A patent/EA007004B1/ru not_active IP Right Cessation
- 2002-12-23 AU AU2002358793A patent/AU2002358793B2/en not_active Ceased
- 2002-12-23 IL IL16268002A patent/IL162680A0/xx unknown
- 2002-12-23 EP EP02793112A patent/EP1469858B1/de not_active Expired - Lifetime
-
2004
- 2004-06-22 IL IL162680A patent/IL162680A/en not_active IP Right Cessation
-
2008
- 2008-10-06 CY CY20081101102T patent/CY1108396T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2005513147A (ja) | 2005-05-12 |
| PL211565B1 (pl) | 2012-05-31 |
| US20060166970A1 (en) | 2006-07-27 |
| AP1958A (en) | 2009-02-20 |
| IL162680A (en) | 2010-11-30 |
| CN1607953A (zh) | 2005-04-20 |
| US10507207B2 (en) | 2019-12-17 |
| EP1469858B1 (de) | 2008-07-09 |
| WO2003055493A1 (en) | 2003-07-10 |
| DK1469858T3 (da) | 2008-09-29 |
| ES2309222T3 (es) | 2008-12-16 |
| AP2004003088A0 (en) | 2004-09-30 |
| MXPA04006205A (es) | 2005-07-25 |
| CN100450487C (zh) | 2009-01-14 |
| AU2002358793A1 (en) | 2003-07-15 |
| EP1469858A1 (de) | 2004-10-27 |
| DE60227563D1 (de) | 2008-08-21 |
| EA007004B1 (ru) | 2006-06-30 |
| CA2471543A1 (en) | 2003-07-10 |
| IL162680A0 (en) | 2005-11-20 |
| PL374038A1 (en) | 2005-09-19 |
| HUP0600841A3 (en) | 2012-09-28 |
| AU2002358793B2 (en) | 2008-04-24 |
| NZ534257A (en) | 2008-03-28 |
| HUP0600841A2 (en) | 2007-05-02 |
| CY1108396T1 (el) | 2014-02-12 |
| HU229522B1 (en) | 2014-01-28 |
| ATE400276T1 (de) | 2008-07-15 |
| SI1469858T1 (sl) | 2008-10-31 |
| EA200400861A1 (ru) | 2004-12-30 |
| CA2471543C (en) | 2011-03-22 |
| PT1469858E (pt) | 2008-10-01 |
| JP4336584B2 (ja) | 2009-09-30 |
| HK1074998A1 (zh) | 2005-12-02 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AU2024200650A1 (en) | Therapeutic benefit of suboptimally administered chemical compounds | |
| US20090170862A1 (en) | Use of c-kit inhibitors for the treatment of myeloma | |
| KR20220034739A (ko) | Tead 억제제 및 이의 용도 | |
| US20090054415A1 (en) | Combinations, methods and compositions for treating cancer | |
| JP7109919B2 (ja) | Usp7阻害剤化合物及び使用方法 | |
| US20120028917A1 (en) | Use Of N-(4-((3-(2-Amino-4-Pyrimidinyl)-2-Pyridinyl)Oxy)Phenyl)-4-(4-Methyl-2-Thienyl)-1-Phthalazinamine In The Treatment Of Antimitotic Agent Resistant Cancer | |
| Chaisuparat et al. | Dual inhibition of PI3Kα and mTOR as an alternative treatment for Kaposi's sarcoma | |
| US20030162740A1 (en) | Strategy for leukemia therapy | |
| KR20210027382A (ko) | 접히지 않은 단백질 반응의 활성화제 | |
| JP2002512962A (ja) | プロテインキナーゼ活性を有する置換三環式ピラゾール誘導体 | |
| Hartman et al. | The Continuing Evolution of HIV‐1 Therapy: Identification and Development of Novel Antiretroviral Agents Targeting Viral and Cellular Targets | |
| EP1469858B1 (de) | Nicht-nukleosidische reverse transcriptase inhibitoren als antagonisten der zellproliferation und induktoren der zell differenzierung | |
| CN112439067B (zh) | Sglt2抑制剂在制备改善抗肿瘤药物敏感性的产品中的应用 | |
| US10906876B2 (en) | Tetrahydroisoquinolines as selective NADPH oxidase 2 inhibitors | |
| US6787573B2 (en) | Antiviral therapy | |
| CN108030777B (zh) | 氯胍在制备抗肿瘤药物中的应用 | |
| Levitzki | Targeting signal transduction for disease therapy | |
| US20220071955A1 (en) | Methods of Treatment, Prevention and Diagnosis | |
| EA048235B1 (ru) | Соединения, модулирующие диацилглицеринкиназу | |
| CN108721299A (zh) | 成纤维细胞生长因子fgfr1抑制剂pp2的应用 | |
| KR20220147511A (ko) | 사이클린 의존성 키나아제 억제용 조성물 및 이의 의학적 용도 | |
| WO2011041512A2 (en) | Compositions and methods for treating mlv-infection, and preventing and treating mlv-initiated diseases |