JP2015519891A5 - - Google Patents
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- Publication number
- JP2015519891A5 JP2015519891A5 JP2015509097A JP2015509097A JP2015519891A5 JP 2015519891 A5 JP2015519891 A5 JP 2015519891A5 JP 2015509097 A JP2015509097 A JP 2015509097A JP 2015509097 A JP2015509097 A JP 2015509097A JP 2015519891 A5 JP2015519891 A5 JP 2015519891A5
- Authority
- JP
- Japan
- Prior art keywords
- nucleoside
- cet
- modified oligonucleotide
- bicyclic
- methoxyethyl
- 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.)
- Granted
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- 239000002777 nucleoside Substances 0.000 claims 108
- 150000003833 nucleoside derivatives Chemical class 0.000 claims 61
- -1 bicyclic nucleoside Chemical class 0.000 claims 26
- 108091034117 Oligonucleotide Proteins 0.000 claims 23
- 150000001875 compounds Chemical class 0.000 claims 19
- 239000008194 pharmaceutical composition Substances 0.000 claims 17
- 125000003835 nucleoside group Chemical group 0.000 claims 16
- 239000005549 deoxyribonucleoside Substances 0.000 claims 14
- 206010016654 Fibrosis Diseases 0.000 claims 7
- 230000004761 fibrosis Effects 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 108091062762 miR-21 stem-loop Proteins 0.000 claims 5
- 108091041631 miR-21-1 stem-loop Proteins 0.000 claims 5
- 108091044442 miR-21-2 stem-loop Proteins 0.000 claims 5
- RPTUSVTUFVMDQK-UHFFFAOYSA-N Hidralazin Chemical compound C1=CC=C2C(NN)=NN=CC2=C1 RPTUSVTUFVMDQK-UHFFFAOYSA-N 0.000 claims 4
- OPTASPLRGRRNAP-UHFFFAOYSA-N cytosine Chemical compound NC=1C=CNC(=O)N=1 OPTASPLRGRRNAP-UHFFFAOYSA-N 0.000 claims 4
- 239000003112 inhibitor Substances 0.000 claims 4
- LRSASMSXMSNRBT-UHFFFAOYSA-N 5-methylcytosine Chemical compound CC1=CNC(=O)N=C1N LRSASMSXMSNRBT-UHFFFAOYSA-N 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 201000002793 renal fibrosis Diseases 0.000 claims 3
- 239000005541 ACE inhibitor Substances 0.000 claims 2
- 208000022461 Glomerular disease Diseases 0.000 claims 2
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 208000019425 cirrhosis of liver Diseases 0.000 claims 2
- 230000000295 complement effect Effects 0.000 claims 2
- 229940104302 cytosine Drugs 0.000 claims 2
- 230000006870 function Effects 0.000 claims 2
- 229960002474 hydralazine Drugs 0.000 claims 2
- 208000015181 infectious disease Diseases 0.000 claims 2
- 210000000056 organ Anatomy 0.000 claims 2
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 2
- 230000000306 recurrent effect Effects 0.000 claims 2
- RMMXLENWKUUMAY-UHFFFAOYSA-N telmisartan Chemical compound CCCC1=NC2=C(C)C=C(C=3N(C4=CC=CC=C4N=3)C)C=C2N1CC(C=C1)=CC=C1C1=CC=CC=C1C(O)=O RMMXLENWKUUMAY-UHFFFAOYSA-N 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- BIDNLKIUORFRQP-XYGFDPSESA-N (2s,4s)-4-cyclohexyl-1-[2-[[(1s)-2-methyl-1-propanoyloxypropoxy]-(4-phenylbutyl)phosphoryl]acetyl]pyrrolidine-2-carboxylic acid Chemical compound C([P@@](=O)(O[C@H](OC(=O)CC)C(C)C)CC(=O)N1[C@@H](C[C@H](C1)C1CCCCC1)C(O)=O)CCCC1=CC=CC=C1 BIDNLKIUORFRQP-XYGFDPSESA-N 0.000 claims 1
- 208000024985 Alport syndrome Diseases 0.000 claims 1
- 102000005862 Angiotensin II Human genes 0.000 claims 1
- 102000008873 Angiotensin II receptor Human genes 0.000 claims 1
- 108050000824 Angiotensin II receptor Proteins 0.000 claims 1
- 101800000733 Angiotensin-2 Proteins 0.000 claims 1
- 206010003694 Atrophy Diseases 0.000 claims 1
- XPCFTKFZXHTYIP-PMACEKPBSA-N Benazepril Chemical compound C([C@@H](C(=O)OCC)N[C@@H]1C(N(CC(O)=O)C2=CC=CC=C2CC1)=O)CC1=CC=CC=C1 XPCFTKFZXHTYIP-PMACEKPBSA-N 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 239000002083 C09CA01 - Losartan Substances 0.000 claims 1
- 239000002080 C09CA02 - Eprosartan Substances 0.000 claims 1
- 239000004072 C09CA03 - Valsartan Substances 0.000 claims 1
- 239000002947 C09CA04 - Irbesartan Substances 0.000 claims 1
- 239000002053 C09CA06 - Candesartan Substances 0.000 claims 1
- 239000005537 C09CA07 - Telmisartan Substances 0.000 claims 1
- 229940127291 Calcium channel antagonist Drugs 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010009208 Cirrhosis alcoholic Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 102000015225 Connective Tissue Growth Factor Human genes 0.000 claims 1
- 108010039419 Connective Tissue Growth Factor Proteins 0.000 claims 1
- LTMHDMANZUZIPE-AMTYYWEZSA-N Digoxin Natural products O([C@H]1[C@H](C)O[C@H](O[C@@H]2C[C@@H]3[C@@](C)([C@@H]4[C@H]([C@]5(O)[C@](C)([C@H](O)C4)[C@H](C4=CC(=O)OC4)CC5)CC3)CC2)C[C@@H]1O)[C@H]1O[C@H](C)[C@@H](O[C@H]2O[C@@H](C)[C@H](O)[C@@H](O)C2)[C@@H](O)C1 LTMHDMANZUZIPE-AMTYYWEZSA-N 0.000 claims 1
- 108010061435 Enalapril Proteins 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 206010018372 Glomerulonephritis membranous Diseases 0.000 claims 1
- 229920001499 Heparinoid Polymers 0.000 claims 1
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 1
- 208000010159 IgA glomerulonephritis Diseases 0.000 claims 1
- 206010021263 IgA nephropathy Diseases 0.000 claims 1
- CZGUSIXMZVURDU-JZXHSEFVSA-N Ile(5)-angiotensin II Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC=1C=CC=CC=1)C([O-])=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(N)=[NH2+])NC(=O)[C@@H]([NH3+])CC([O-])=O)C(C)C)C1=CC=C(O)C=C1 CZGUSIXMZVURDU-JZXHSEFVSA-N 0.000 claims 1
- 108010007859 Lisinopril Proteins 0.000 claims 1
- 206010067125 Liver injury Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 229910002651 NO3 Inorganic materials 0.000 claims 1
- 108020001621 Natriuretic Peptide Proteins 0.000 claims 1
- 102000004571 Natriuretic peptide Human genes 0.000 claims 1
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 claims 1
- 239000005480 Olmesartan Substances 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010061481 Renal injury Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 206010062129 Tongue neoplasm Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 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 Chemical class 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 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 208000010002 alcoholic liver cirrhosis Diseases 0.000 claims 1
- 229950006323 angiotensin ii Drugs 0.000 claims 1
- 229940127003 anti-diabetic drug Drugs 0.000 claims 1
- 229940124599 anti-inflammatory drug Drugs 0.000 claims 1
- 239000003472 antidiabetic agent Substances 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 230000037444 atrophy Effects 0.000 claims 1
- 229960004530 benazepril Drugs 0.000 claims 1
- 239000002876 beta blocker Substances 0.000 claims 1
- 229940097320 beta blocking agent Drugs 0.000 claims 1
- 239000000480 calcium channel blocker Substances 0.000 claims 1
- 229960000932 candesartan Drugs 0.000 claims 1
- SGZAIDDFHDDFJU-UHFFFAOYSA-N candesartan Chemical compound CCOC1=NC2=CC=CC(C(O)=O)=C2N1CC(C=C1)=CC=C1C1=CC=CC=C1C1=NN=N[N]1 SGZAIDDFHDDFJU-UHFFFAOYSA-N 0.000 claims 1
- 229960000830 captopril Drugs 0.000 claims 1
- FAKRSMQSSFJEIM-RQJHMYQMSA-N captopril Chemical group SC[C@@H](C)C(=O)N1CCC[C@H]1C(O)=O FAKRSMQSSFJEIM-RQJHMYQMSA-N 0.000 claims 1
- 230000009787 cardiac fibrosis Effects 0.000 claims 1
- 208000020832 chronic kidney disease Diseases 0.000 claims 1
- 231100000012 chronic liver injury Toxicity 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- LTMHDMANZUZIPE-PUGKRICDSA-N digoxin Chemical compound C1[C@H](O)[C@H](O)[C@@H](C)O[C@H]1O[C@@H]1[C@@H](C)O[C@@H](O[C@@H]2[C@H](O[C@@H](O[C@@H]3C[C@@H]4[C@]([C@@H]5[C@H]([C@]6(CC[C@@H]([C@@]6(C)[C@H](O)C5)C=5COC(=O)C=5)O)CC4)(C)CC3)C[C@@H]2O)C)C[C@@H]1O LTMHDMANZUZIPE-PUGKRICDSA-N 0.000 claims 1
- 229960005156 digoxin Drugs 0.000 claims 1
- LTMHDMANZUZIPE-UHFFFAOYSA-N digoxine Natural products C1C(O)C(O)C(C)OC1OC1C(C)OC(OC2C(OC(OC3CC4C(C5C(C6(CCC(C6(C)C(O)C5)C=5COC(=O)C=5)O)CC4)(C)CC3)CC2O)C)CC1O LTMHDMANZUZIPE-UHFFFAOYSA-N 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000002500 effect on skin Effects 0.000 claims 1
- 229960000873 enalapril Drugs 0.000 claims 1
- GBXSMTUPTTWBMN-XIRDDKMYSA-N enalapril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(O)=O)CC1=CC=CC=C1 GBXSMTUPTTWBMN-XIRDDKMYSA-N 0.000 claims 1
- 208000028208 end stage renal disease Diseases 0.000 claims 1
- 201000000523 end stage renal failure Diseases 0.000 claims 1
- 229960004563 eprosartan Drugs 0.000 claims 1
- OROAFUQRIXKEMV-LDADJPATSA-N eprosartan Chemical compound C=1C=C(C(O)=O)C=CC=1CN1C(CCCC)=NC=C1\C=C(C(O)=O)/CC1=CC=CS1 OROAFUQRIXKEMV-LDADJPATSA-N 0.000 claims 1
- 201000005206 focal segmental glomerulosclerosis Diseases 0.000 claims 1
- 231100000854 focal segmental glomerulosclerosis Toxicity 0.000 claims 1
- 229960002490 fosinopril Drugs 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 231100000852 glomerular disease Toxicity 0.000 claims 1
- 206010061989 glomerulosclerosis Diseases 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 230000004217 heart function Effects 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 239000002554 heparinoid Substances 0.000 claims 1
- 208000006454 hepatitis Diseases 0.000 claims 1
- 231100000283 hepatitis Toxicity 0.000 claims 1
- 208000003215 hereditary nephritis Diseases 0.000 claims 1
- 239000003018 immunosuppressive agent Substances 0.000 claims 1
- 229940124589 immunosuppressive drug Drugs 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 1
- 229960002198 irbesartan Drugs 0.000 claims 1
- YCPOHTHPUREGFM-UHFFFAOYSA-N irbesartan Chemical compound O=C1N(CC=2C=CC(=CC=2)C=2C(=CC=CC=2)C=2[N]N=NN=2)C(CCCC)=NC21CCCC2 YCPOHTHPUREGFM-UHFFFAOYSA-N 0.000 claims 1
- MOYKHGMNXAOIAT-JGWLITMVSA-N isosorbide dinitrate Chemical compound [O-][N+](=O)O[C@H]1CO[C@@H]2[C@H](O[N+](=O)[O-])CO[C@@H]21 MOYKHGMNXAOIAT-JGWLITMVSA-N 0.000 claims 1
- 229960000201 isosorbide dinitrate Drugs 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 230000003907 kidney function Effects 0.000 claims 1
- 208000037806 kidney injury Diseases 0.000 claims 1
- 229960002394 lisinopril Drugs 0.000 claims 1
- RLAWWYSOJDYHDC-BZSNNMDCSA-N lisinopril Chemical compound C([C@H](N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(O)=O)C(O)=O)CC1=CC=CC=C1 RLAWWYSOJDYHDC-BZSNNMDCSA-N 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 230000003908 liver function Effects 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 229960004773 losartan Drugs 0.000 claims 1
- KJJZZJSZUJXYEA-UHFFFAOYSA-N losartan Chemical compound CCCCC1=NC(Cl)=C(CO)N1CC1=CC=C(C=2C(=CC=CC=2)C=2[N]N=NN=2)C=C1 KJJZZJSZUJXYEA-UHFFFAOYSA-N 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 230000004199 lung function Effects 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000008350 membranous glomerulonephritis Diseases 0.000 claims 1
- 231100000855 membranous nephropathy Toxicity 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000000692 natriuretic peptide Substances 0.000 claims 1
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 1
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 1
- 108020004707 nucleic acids Proteins 0.000 claims 1
- 150000007523 nucleic acids Chemical class 0.000 claims 1
- 102000039446 nucleic acids Human genes 0.000 claims 1
- 229960005117 olmesartan Drugs 0.000 claims 1
- VTRAEEWXHOVJFV-UHFFFAOYSA-N olmesartan Chemical compound CCCC1=NC(C(C)(C)O)=C(C(O)=O)N1CC1=CC=C(C=2C(=CC=CC=2)C=2NN=NN=2)C=C1 VTRAEEWXHOVJFV-UHFFFAOYSA-N 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 229960001455 quinapril Drugs 0.000 claims 1
- JSDRRTOADPPCHY-HSQYWUDLSA-N quinapril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](CC2=CC=CC=C2C1)C(O)=O)CC1=CC=CC=C1 JSDRRTOADPPCHY-HSQYWUDLSA-N 0.000 claims 1
- 229960003401 ramipril Drugs 0.000 claims 1
- HDACQVRGBOVJII-JBDAPHQKSA-N ramipril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](C[C@@H]2CCC[C@@H]21)C(O)=O)CC1=CC=CC=C1 HDACQVRGBOVJII-JBDAPHQKSA-N 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 210000000952 spleen Anatomy 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 229960005187 telmisartan Drugs 0.000 claims 1
- RYYWUUFWQRZTIU-UHFFFAOYSA-K thiophosphate Chemical compound [O-]P([O-])([O-])=S RYYWUUFWQRZTIU-UHFFFAOYSA-K 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 210000001519 tissue Anatomy 0.000 claims 1
- 201000006134 tongue cancer Diseases 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
- 230000008733 trauma Effects 0.000 claims 1
- 210000005239 tubule Anatomy 0.000 claims 1
- 208000037999 tubulointerstitial fibrosis Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 229960004699 valsartan Drugs 0.000 claims 1
- SJSNUMAYCRRIOM-QFIPXVFZSA-N valsartan Chemical compound C1=CC(CN(C(=O)CCCC)[C@@H](C(C)C)C(O)=O)=CC=C1C1=CC=CC=C1C1=NN=N[N]1 SJSNUMAYCRRIOM-QFIPXVFZSA-N 0.000 claims 1
- 229940124549 vasodilator Drugs 0.000 claims 1
- 239000003071 vasodilator agent Substances 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261741783P | 2012-04-25 | 2012-04-25 | |
| US61/741,783 | 2012-04-25 | ||
| US201261717927P | 2012-10-24 | 2012-10-24 | |
| US61/717,927 | 2012-10-24 | ||
| US201361779913P | 2013-03-13 | 2013-03-13 | |
| US61/779,913 | 2013-03-13 | ||
| PCT/US2013/037913 WO2013163258A1 (en) | 2012-04-25 | 2013-04-24 | Microrna compounds and methods for modulating mir-21 activity |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015519891A JP2015519891A (ja) | 2015-07-16 |
| JP2015519891A5 true JP2015519891A5 (enExample) | 2016-06-09 |
| JP6322189B2 JP6322189B2 (ja) | 2018-05-09 |
Family
ID=48289681
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015509097A Active JP6322189B2 (ja) | 2012-04-25 | 2013-04-24 | Ｍｉｒ−２１活性を調節するためのマイクロｒｎａ化合物及び方法 |
Country Status (28)
| Country | Link |
|---|---|
| US (5) | US8969317B2 (enExample) |
| EP (1) | EP2841579B1 (enExample) |
| JP (1) | JP6322189B2 (enExample) |
| KR (4) | KR102369722B1 (enExample) |
| CN (1) | CN104254607B (enExample) |
| AR (1) | AR090825A1 (enExample) |
| AU (1) | AU2013251696B2 (enExample) |
| BR (1) | BR112014026639A8 (enExample) |
| CA (1) | CA2869639A1 (enExample) |
| CL (3) | CL2014002844A1 (enExample) |
| CO (1) | CO7111303A2 (enExample) |
| CR (1) | CR20140524A (enExample) |
| DO (1) | DOP2014000233A (enExample) |
| EA (1) | EA030211B1 (enExample) |
| EC (1) | ECSP14028612A (enExample) |
| GT (1) | GT201400221A (enExample) |
| IL (1) | IL234904B (enExample) |
| IN (1) | IN2014DN09134A (enExample) |
| MX (1) | MX353562B (enExample) |
| MY (1) | MY173600A (enExample) |
| NZ (1) | NZ630591A (enExample) |
| PE (1) | PE20142404A1 (enExample) |
| PH (2) | PH12023550488A1 (enExample) |
| SG (1) | SG11201406931XA (enExample) |
| TW (1) | TWI647235B (enExample) |
| UA (1) | UA117098C2 (enExample) |
| WO (1) | WO2013163258A1 (enExample) |
| ZA (1) | ZA201407228B (enExample) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2733708T3 (es) | 2010-02-08 | 2019-12-02 | Ionis Pharmaceuticals Inc | Reducción selectiva de variantes alélicas |
| CA2807552A1 (en) | 2010-08-06 | 2012-02-09 | Moderna Therapeutics, Inc. | Engineered nucleic acids and methods of use thereof |
| EP2857499A1 (en) | 2010-10-01 | 2015-04-08 | Moderna Therapeutics, Inc. | Engineered nucleic acids and methods of use thereof |
| CA2831613A1 (en) | 2011-03-31 | 2012-10-04 | Moderna Therapeutics, Inc. | Delivery and formulation of engineered nucleic acids |
| MX393138B (es) | 2011-04-25 | 2025-03-24 | Sanofi Sa | Compuestos de microarn y metodos para modular la actividad de mir-21. |
| US9464124B2 (en) | 2011-09-12 | 2016-10-11 | Moderna Therapeutics, Inc. | Engineered nucleic acids and methods of use thereof |
| PT3682905T (pt) | 2011-10-03 | 2022-04-07 | Modernatx Inc | Nucleósidos, nucleótidos e ácidos nucleicos modificados e respetivas utilizações |
| ES2923757T3 (es) | 2011-12-16 | 2022-09-30 | Modernatx Inc | Composiciones de ARNm modificado |
| WO2013151664A1 (en) | 2012-04-02 | 2013-10-10 | modeRNA Therapeutics | Modified polynucleotides for the production of proteins |
| US9283287B2 (en) | 2012-04-02 | 2016-03-15 | Moderna Therapeutics, Inc. | Modified polynucleotides for the production of nuclear proteins |
| US10501512B2 (en) | 2012-04-02 | 2019-12-10 | Modernatx, Inc. | Modified polynucleotides |
| US9572897B2 (en) | 2012-04-02 | 2017-02-21 | Modernatx, Inc. | Modified polynucleotides for the production of cytoplasmic and cytoskeletal proteins |
| US9193971B2 (en) * | 2012-04-10 | 2015-11-24 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Methods for the treatment of nonalcoholic steatohepatitis |
| MY173600A (en) | 2012-04-25 | 2020-02-08 | Sanofi Sa | Microrna compounds and methods for modulating mir-21 activity |
| UA116639C2 (uk) | 2012-10-09 | 2018-04-25 | Рег'Юлес Терап'Ютікс Інк. | Способи лікування синдрому альпорта |
| EP4086347A3 (en) * | 2012-10-12 | 2023-01-11 | Ionis Pharmaceuticals, Inc. | Selective antisense compounds and uses thereof |
| PT2922554T (pt) | 2012-11-26 | 2022-06-28 | Modernatx Inc | Arn modificado nas porções terminais |
| US8980864B2 (en) | 2013-03-15 | 2015-03-17 | Moderna Therapeutics, Inc. | Compositions and methods of altering cholesterol levels |
| US10023626B2 (en) | 2013-09-30 | 2018-07-17 | Modernatx, Inc. | Polynucleotides encoding immune modulating polypeptides |
| KR20160067219A (ko) | 2013-10-03 | 2016-06-13 | 모더나 세라퓨틱스, 인코포레이티드 | 저밀도 지단백질 수용체를 암호화하는 폴리뉴클레오타이드 |
| WO2015061536A1 (en) | 2013-10-25 | 2015-04-30 | Regulus Therapeutics Inc. | Microrna compounds and methods for modulating mir-21 activity |
| TW201610152A (zh) * | 2013-11-22 | 2016-03-16 | 國立臺灣大學 | 微ｒｎａ１４６－ａ及其於診斷、治療及預防小核醣核酸病毒感染之用途及微ｒｎａ１４６－ａ拮抗劑 |
| JP2017511694A (ja) * | 2014-02-12 | 2017-04-27 | トーマス・ジェファーソン・ユニバーシティ | マイクロｒｎａ阻害剤を使用するための組成物および方法 |
| WO2015154002A1 (en) * | 2014-04-04 | 2015-10-08 | Ohio State Innovation Foundation | Oligonucleotide lipid nanoparticle compositions, methods of making and methods of using the same |
| CN105087477A (zh) * | 2015-05-21 | 2015-11-25 | 王松灵 | miR-21反义核苷酸修饰的骨髓间充质干细胞的用途 |
| US11236337B2 (en) | 2016-11-01 | 2022-02-01 | The Research Foundation For The State University Of New York | 5-halouracil-modified microRNAs and their use in the treatment of cancer |
| US20180193270A1 (en) | 2016-11-29 | 2018-07-12 | PureTech Health LLC | Exosomes for delivery of therapeutic agents |
| EP3618838A1 (en) * | 2017-05-04 | 2020-03-11 | Sanofi | Methods for treatment of alport syndrome |
| EP3841220A1 (en) | 2018-08-23 | 2021-06-30 | Roche Innovation Center Copenhagen A/S | Microrna-134 biomarker |
| TW202031268A (zh) * | 2018-11-13 | 2020-09-01 | 美商雷格勒斯治療公司 | 用於調節mir-10b 活性之微小rna 化合物及方法 |
| MX2021015552A (es) | 2019-06-14 | 2022-10-13 | Cardior Pharmaceuticals Gmbh | Tratamiento de la insuficiencia cardiaca en individuos humanos. |
| JP7692829B2 (ja) | 2019-07-30 | 2025-06-16 | 塩野義製薬株式会社 | Ｍｕｒｆ１を標的とする核酸医薬 |
| KR102293777B1 (ko) * | 2019-12-31 | 2021-08-25 | 연세대학교 산학협력단 | 신규한 UQCRB-관련 순환 miRNA 바이오 마커 및 이를 이용한 대장암의 진단 방법 |
| MX2022012544A (es) * | 2020-04-09 | 2022-11-07 | Univ Muenchen Tech | Liberacion dirigida de un inhibidor de mir-21 a macrofagos para el tratamiento de la fibrosis pulmonar. |
| US11965162B2 (en) | 2020-04-16 | 2024-04-23 | The Johns Hopkins University | MicroRNA and inhibitors thereof and methods of treatment |
| KR102328770B1 (ko) * | 2020-06-01 | 2021-11-19 | 고려대학교 산학협력단 | 비알코올 지방간염 진단용 바이오마커 miRNA-4449 |
| WO2021262919A2 (en) | 2020-06-26 | 2021-12-30 | The Research Foundation For The State University Of New York | 5-halouracil-modified micrornas and their use in the treatment of cancer |
| KR102360963B1 (ko) * | 2020-07-28 | 2022-02-09 | 고려대학교 산학협력단 | microRNA조합을 이용한 비알코올 지방간염 진단용 바이오마커 |
| WO2022072336A1 (en) * | 2020-10-01 | 2022-04-07 | University Of Washington | Drug-like molecules and methods for the therapeutic targeting of microrna-21 |
| JP2024535445A (ja) * | 2021-10-08 | 2024-09-30 | レグルス セラピューティクス インコーポレイテッド | オフターゲット効果を回避するための方法及び組成物 |
| CN122295113A (zh) * | 2023-11-22 | 2026-06-26 | 国立大学法人东海国立大学机构 | 囊性肾病的预防和/或治疗剂 |
| EP4741501A1 (en) * | 2024-11-11 | 2026-05-13 | RNATICS GmbH | Dosing of oligonucleotide drugs targeting mir-21 for inhalation |
| EP4740935A1 (en) * | 2024-11-11 | 2026-05-13 | RNATICS GmbH | Formulation of oligonucleotide drugs for inhalation |
Family Cites Families (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2285841T3 (es) | 1998-05-22 | 2007-11-16 | Boys Town National Research Hospital | Uso de inhibidores del receptor de integrina alfa1beta1 e inhibidores de tgf-beta1 en el tratamiento de la enfermedad renal. |
| US20060008817A1 (en) | 2000-12-08 | 2006-01-12 | Invitrogen Corporation | Methods and compositions for generating recombinant nucleic acid molecules |
| EP2428570B1 (en) | 2001-09-28 | 2018-05-23 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Microrna molecules |
| CA2504694C (en) | 2002-11-05 | 2013-10-01 | Isis Pharmaceuticals, Inc. | Polycyclic sugar surrogate-containing oligomeric compounds and compositions for use in gene modulation |
| US20050124591A1 (en) | 2003-07-29 | 2005-06-09 | Jin Tian | Use of vitamin Ds to treat kidney disease |
| WO2005013901A2 (en) | 2003-07-31 | 2005-02-17 | Isis Pharmaceuticals, Inc. | Oligomeric compounds and compositions for use in modulation of small non-coding rnas |
| DK1661905T3 (da) | 2003-08-28 | 2012-07-23 | Takeshi Imanishi | Hidtil ukendte syntetiske nukleinsyrer af N-O-krydsbindingstype |
| EP2471924A1 (en) | 2004-05-28 | 2012-07-04 | Asuragen, INC. | Methods and compositions involving microRNA |
| EP2990410A1 (en) | 2004-08-10 | 2016-03-02 | Alnylam Pharmaceuticals Inc. | Chemically modified oligonucleotides |
| US20080187508A1 (en) | 2004-09-08 | 2008-08-07 | Boys Town National Research Hospital | Treatment of Golmerular Basement Membrane Disease Involving Matrix Metalloproteinase-12 |
| ES2534300T3 (es) | 2004-11-12 | 2015-04-21 | Asuragen, Inc. | Procedimientos y composiciones que implican miARN y moléculas inhibidoras de miARN |
| US20070099196A1 (en) | 2004-12-29 | 2007-05-03 | Sakari Kauppinen | Novel oligonucleotide compositions and probe sequences useful for detection and analysis of micrornas and their target mRNAs |
| US6995235B1 (en) | 2005-05-02 | 2006-02-07 | Univation Technologies, Llc | Methods of producing polyolefins and films therefrom |
| WO2007027894A2 (en) | 2005-08-29 | 2007-03-08 | Isis Pharmaceuticals, Inc. | Antisense compounds having enhanced anti-microrna activity |
| DE602007009487D1 (de) | 2006-01-27 | 2010-11-11 | Isis Pharmaceutical Inc | 6-modifizierte bicyclische nukleinsäureanaloga |
| EP2388328A1 (en) | 2006-01-27 | 2011-11-23 | Isis Pharmaceuticals, Inc. | Oligomeric compounds and compositions for the use in modulation of micrornas |
| EA201100811A1 (ru) | 2006-04-03 | 2012-06-29 | Сантарис Фарма А/С | Фармацевтическая композиция |
| CA3042781C (en) | 2006-04-03 | 2021-10-19 | Roche Innovation Center Copenhagen A/S | Pharmaceutical composition comprising anti-mirna antisense oligonucleotides |
| CA3144493A1 (en) | 2006-10-03 | 2008-04-10 | Arbutus Biopharma Corporation | Lipid containing formulations |
| JP2010505427A (ja) | 2006-10-09 | 2010-02-25 | ジュリアス−マキシミリアンズ−ユニベルシタット ワーズブルグ | 心疾患の診断及び治療用マイクロＲＮＡ（ｍｉＲＮＡ） |
| EP2104735A2 (en) | 2006-12-08 | 2009-09-30 | Asuragen, INC. | Mir-21 regulated genes and pathways as targets for therapeutic intervention |
| WO2008086807A2 (en) | 2007-01-19 | 2008-07-24 | Exiqon A/S | Mediated cellular delivery of lna oligonucleotides |
| DK2170917T3 (da) | 2007-05-30 | 2012-10-08 | Isis Pharmaceuticals Inc | N-Substituerede bicycliske nukleinsyreanaloge med aminomethylenbro |
| WO2008154401A2 (en) | 2007-06-08 | 2008-12-18 | Isis Pharmaceuticals, Inc. | Carbocyclic bicyclic nucleic acid analogs |
| US20100261175A1 (en) | 2007-06-15 | 2010-10-14 | Exiqon A/S | Use of short oligonucleotides for reagent redundancy experiments in rna functional analysis |
| AU2008272918B2 (en) | 2007-07-05 | 2012-09-13 | Isis Pharmaceuticals, Inc. | 6-disubstituted bicyclic nucleic acid analogs |
| DK2205737T3 (da) * | 2007-10-04 | 2013-05-21 | Santaris Pharma As | Mikromirer |
| CN101980712B (zh) * | 2007-10-29 | 2015-02-18 | 雷古拉斯治疗公司 | 用于肝癌治疗的靶向微小rna |
| WO2009091972A2 (en) | 2008-01-18 | 2009-07-23 | Alnylam Pharmaceuticals, Inc. | Chemically modified oligonucleotides and small molecules for use in reducing micro rna activity levels and uses thereof |
| JP2011510678A (ja) | 2008-02-08 | 2011-04-07 | プロセンサ ホールディング ビーブイ | Ｄｎａ反復不安定性関連遺伝性障害を治療するための方法及び手段 |
| EP2096171A1 (en) * | 2008-02-27 | 2009-09-02 | Julius-Maximilians-Universität Würzburg | MicroRNA (miRNA) and down-stream targets for diagnostic and therapeutic purposes |
| EP2268811A1 (en) | 2008-03-07 | 2011-01-05 | Santaris Pharma A/S | Pharmaceutical compositions for treatment of microrna related diseases |
| JP2012518997A (ja) * | 2009-02-26 | 2012-08-23 | ジ・オハイオ・ステイト・ユニバーシティ・リサーチ・ファウンデイション | 喫煙未経験者におけるマイクロｒｎａ、ならびに関連する材料および方法 |
| MA33488B1 (fr) * | 2009-06-08 | 2012-08-01 | Miragen Therapeutics | Motifs de modification chimique pour des inhibiteurs et mimétiques de miarn |
| WO2011126842A2 (en) | 2010-03-30 | 2011-10-13 | Regulus Therapeutics Inc. | Targeting micrornas for the treatment of cardiac disorders |
| MX393138B (es) | 2011-04-25 | 2025-03-24 | Sanofi Sa | Compuestos de microarn y metodos para modular la actividad de mir-21. |
| WO2013013165A2 (en) | 2011-07-21 | 2013-01-24 | The Trustees Of The University Of Pennsylvania | Use of lna compounds for therapeutic inhibition of mir-21 in systemic lupus erythematosus |
| MY173600A (en) | 2012-04-25 | 2020-02-08 | Sanofi Sa | Microrna compounds and methods for modulating mir-21 activity |
| EP2864482A4 (en) | 2012-06-21 | 2016-02-10 | Miragen Therapeutics Inc | OLIGONUCLEOTIDE INHIBITORS COMPRISING A BLOCKED NUCLEIC ACID PATTERN |
| CN104955950B (zh) | 2012-09-26 | 2019-04-26 | 米尔克斯治疗学公司 | 具有改善的脱靶特征谱的寡核苷酸 |
| UA116639C2 (uk) | 2012-10-09 | 2018-04-25 | Рег'Юлес Терап'Ютікс Інк. | Способи лікування синдрому альпорта |
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