EA028605B1 - Комбинация озельтамивира и ингибитора mek для лечения вирусных заболеваний - Google Patents
Комбинация озельтамивира и ингибитора mek для лечения вирусных заболеваний Download PDFInfo
- Publication number
- EA028605B1 EA028605B1 EA201590703A EA201590703A EA028605B1 EA 028605 B1 EA028605 B1 EA 028605B1 EA 201590703 A EA201590703 A EA 201590703A EA 201590703 A EA201590703 A EA 201590703A EA 028605 B1 EA028605 B1 EA 028605B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- inhibitor
- oseltamivir
- mek
- virus
- pharmaceutically acceptable
- Prior art date
Links
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 title claims abstract description 88
- 229940124647 MEK inhibitor Drugs 0.000 title claims abstract description 86
- 201000010099 disease Diseases 0.000 title claims abstract description 50
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims abstract description 50
- 238000011282 treatment Methods 0.000 title claims abstract description 44
- 230000003612 virological effect Effects 0.000 title claims abstract description 44
- VSZGPKBBMSAYNT-RRFJBIMHSA-N oseltamivir Chemical compound CCOC(=O)C1=C[C@@H](OC(CC)CC)[C@H](NC(C)=O)[C@@H](N)C1 VSZGPKBBMSAYNT-RRFJBIMHSA-N 0.000 title claims description 77
- 229960003752 oseltamivir Drugs 0.000 title claims description 47
- 239000002911 sialidase inhibitor Substances 0.000 claims abstract description 64
- 229940123424 Neuraminidase inhibitor Drugs 0.000 claims abstract description 58
- 150000003839 salts Chemical class 0.000 claims abstract description 35
- 230000002265 prevention Effects 0.000 claims abstract description 15
- 241000700605 Viruses Species 0.000 claims description 49
- 241000712461 unidentified influenza virus Species 0.000 claims description 33
- 239000003112 inhibitor Substances 0.000 claims description 31
- 229960002194 oseltamivir phosphate Drugs 0.000 claims description 21
- 239000008194 pharmaceutical composition Substances 0.000 claims description 21
- 208000015181 infectious disease Diseases 0.000 claims description 18
- 239000003814 drug Substances 0.000 claims description 17
- 241000712431 Influenza A virus Species 0.000 claims description 10
- 238000011321 prophylaxis Methods 0.000 claims description 10
- 102000004232 Mitogen-Activated Protein Kinase Kinases Human genes 0.000 claims description 8
- 108090000744 Mitogen-Activated Protein Kinase Kinases Proteins 0.000 claims description 5
- 241000713196 Influenza B virus Species 0.000 claims description 4
- 210000004027 cell Anatomy 0.000 description 35
- 238000000034 method Methods 0.000 description 30
- 108091000080 Phosphotransferase Proteins 0.000 description 20
- 102000020233 phosphotransferase Human genes 0.000 description 20
- 150000001875 compounds Chemical class 0.000 description 18
- 229940079593 drug Drugs 0.000 description 15
- 230000000840 anti-viral effect Effects 0.000 description 14
- 230000014509 gene expression Effects 0.000 description 14
- 208000037797 influenza A Diseases 0.000 description 14
- 230000002195 synergetic effect Effects 0.000 description 14
- 239000000725 suspension Substances 0.000 description 13
- 108091032973 (ribonucleotides)n+m Proteins 0.000 description 12
- 108010006232 Neuraminidase Proteins 0.000 description 12
- 230000000694 effects Effects 0.000 description 12
- 239000000203 mixture Substances 0.000 description 12
- 102000005348 Neuraminidase Human genes 0.000 description 11
- 241000282414 Homo sapiens Species 0.000 description 10
- 208000037798 influenza B Diseases 0.000 description 10
- 239000003085 diluting agent Substances 0.000 description 9
- 102100031480 Dual specificity mitogen-activated protein kinase kinase 1 Human genes 0.000 description 8
- 101710146526 Dual specificity mitogen-activated protein kinase kinase 1 Proteins 0.000 description 8
- 108091054455 MAP kinase family Proteins 0.000 description 8
- 102000043136 MAP kinase family Human genes 0.000 description 8
- 230000019491 signal transduction Effects 0.000 description 8
- 239000000243 solution Substances 0.000 description 8
- 241000124008 Mammalia Species 0.000 description 7
- 206010022000 influenza Diseases 0.000 description 7
- 230000005764 inhibitory process Effects 0.000 description 7
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 6
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 6
- 238000002648 combination therapy Methods 0.000 description 6
- 229940042406 direct acting antivirals neuraminidase inhibitors Drugs 0.000 description 6
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 6
- 229940016286 microcrystalline cellulose Drugs 0.000 description 6
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 6
- 239000008108 microcrystalline cellulose Substances 0.000 description 6
- 230000010076 replication Effects 0.000 description 6
- 239000002904 solvent Substances 0.000 description 6
- 239000000758 substrate Substances 0.000 description 6
- 239000000375 suspending agent Substances 0.000 description 6
- 241000699670 Mus sp. Species 0.000 description 5
- 230000006870 function Effects 0.000 description 5
- PGZUMBJQJWIWGJ-ONAKXNSWSA-N oseltamivir phosphate Chemical compound OP(O)(O)=O.CCOC(=O)C1=C[C@@H](OC(CC)CC)[C@H](NC(C)=O)[C@@H](N)C1 PGZUMBJQJWIWGJ-ONAKXNSWSA-N 0.000 description 5
- 108090000623 proteins and genes Proteins 0.000 description 5
- 230000008054 signal transmission Effects 0.000 description 5
- 239000000126 substance Substances 0.000 description 5
- 239000003826 tablet Substances 0.000 description 5
- 229940061367 tamiflu Drugs 0.000 description 5
- 241000271566 Aves Species 0.000 description 4
- 241001494479 Pecora Species 0.000 description 4
- 241000283216 Phocidae Species 0.000 description 4
- 101000761953 Schizosaccharomyces pombe (strain 972 / ATCC 24843) Protein kinase byr2 Proteins 0.000 description 4
- 208000036142 Viral infection Diseases 0.000 description 4
- 239000011230 binding agent Substances 0.000 description 4
- 239000002775 capsule Substances 0.000 description 4
- 230000003833 cell viability Effects 0.000 description 4
- 238000011161 development Methods 0.000 description 4
- 230000018109 developmental process Effects 0.000 description 4
- 239000002552 dosage form Substances 0.000 description 4
- 239000000945 filler Substances 0.000 description 4
- 235000003599 food sweetener Nutrition 0.000 description 4
- 239000000314 lubricant Substances 0.000 description 4
- 239000007922 nasal spray Substances 0.000 description 4
- 231100000252 nontoxic Toxicity 0.000 description 4
- 230000003000 nontoxic effect Effects 0.000 description 4
- 230000026731 phosphorylation Effects 0.000 description 4
- 238000006366 phosphorylation reaction Methods 0.000 description 4
- 238000002360 preparation method Methods 0.000 description 4
- 239000003765 sweetening agent Substances 0.000 description 4
- 230000001225 therapeutic effect Effects 0.000 description 4
- 230000009385 viral infection Effects 0.000 description 4
- ARAIBEBZBOPLMB-UFGQHTETSA-N zanamivir Chemical compound CC(=O)N[C@@H]1[C@@H](N=C(N)N)C=C(C(O)=O)O[C@H]1[C@H](O)[C@H](O)CO ARAIBEBZBOPLMB-UFGQHTETSA-N 0.000 description 4
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 3
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 description 3
- -1 2-chloro-4-iodophenylamino Chemical group 0.000 description 3
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 3
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 3
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound 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 GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 3
- 235000006576 Althaea officinalis Nutrition 0.000 description 3
- 241001136800 Anas acuta Species 0.000 description 3
- 241000272525 Anas platyrhynchos Species 0.000 description 3
- 241000272814 Anser sp. Species 0.000 description 3
- 241000272517 Anseriformes Species 0.000 description 3
- 241000283690 Bos taurus Species 0.000 description 3
- 241000282836 Camelus dromedarius Species 0.000 description 3
- 241000282465 Canis Species 0.000 description 3
- 241000283707 Capra Species 0.000 description 3
- 241000700199 Cavia porcellus Species 0.000 description 3
- 241000283153 Cetacea Species 0.000 description 3
- 241000699800 Cricetinae Species 0.000 description 3
- 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 description 3
- 235000019739 Dicalciumphosphate Nutrition 0.000 description 3
- 241000283073 Equus caballus Species 0.000 description 3
- 241000282326 Felis catus Species 0.000 description 3
- 241000287828 Gallus gallus Species 0.000 description 3
- 102000003886 Glycoproteins Human genes 0.000 description 3
- 108090000288 Glycoproteins Proteins 0.000 description 3
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 3
- 241000272168 Laridae Species 0.000 description 3
- 241000282560 Macaca mulatta Species 0.000 description 3
- 229930195725 Mannitol Natural products 0.000 description 3
- 241001465754 Metazoa Species 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 241000699666 Mus <mouse, genus> Species 0.000 description 3
- 241000772415 Neovison vison Species 0.000 description 3
- 241000272458 Numididae Species 0.000 description 3
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 description 3
- 239000005642 Oleic acid Substances 0.000 description 3
- 241000282577 Pan troglodytes Species 0.000 description 3
- 241000009328 Perro Species 0.000 description 3
- 241000700159 Rattus Species 0.000 description 3
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 3
- 229920002472 Starch Polymers 0.000 description 3
- 241000287181 Sturnus vulgaris Species 0.000 description 3
- 241000282898 Sus scrofa Species 0.000 description 3
- 108091023040 Transcription factor Proteins 0.000 description 3
- 102000040945 Transcription factor Human genes 0.000 description 3
- 230000000996 additive effect Effects 0.000 description 3
- 235000010443 alginic acid Nutrition 0.000 description 3
- 239000000783 alginic acid Substances 0.000 description 3
- 229960001126 alginic acid Drugs 0.000 description 3
- 229920000615 alginic acid Polymers 0.000 description 3
- 150000004781 alginic acids Chemical class 0.000 description 3
- 230000000259 anti-tumor effect Effects 0.000 description 3
- 239000003443 antiviral agent Substances 0.000 description 3
- 230000009286 beneficial effect Effects 0.000 description 3
- 239000001506 calcium phosphate Substances 0.000 description 3
- 238000004113 cell culture Methods 0.000 description 3
- NEFBYIFKOOEVPA-UHFFFAOYSA-K dicalcium phosphate Chemical compound [Ca+2].[Ca+2].[O-]P([O-])([O-])=O NEFBYIFKOOEVPA-UHFFFAOYSA-K 0.000 description 3
- 229940038472 dicalcium phosphate Drugs 0.000 description 3
- 229910000390 dicalcium phosphate Inorganic materials 0.000 description 3
- 235000014113 dietary fatty acids Nutrition 0.000 description 3
- 239000007884 disintegrant Substances 0.000 description 3
- 241001493065 dsRNA viruses Species 0.000 description 3
- 239000000194 fatty acid Substances 0.000 description 3
- 229930195729 fatty acid Natural products 0.000 description 3
- 150000004665 fatty acids Chemical class 0.000 description 3
- 239000012729 immediate-release (IR) formulation Substances 0.000 description 3
- 238000007918 intramuscular administration Methods 0.000 description 3
- 238000001990 intravenous administration Methods 0.000 description 3
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 3
- 229940043355 kinase inhibitor Drugs 0.000 description 3
- 239000008101 lactose Substances 0.000 description 3
- 229960001375 lactose Drugs 0.000 description 3
- 235000019359 magnesium stearate Nutrition 0.000 description 3
- 229940057948 magnesium stearate Drugs 0.000 description 3
- 239000000594 mannitol Substances 0.000 description 3
- 235000010355 mannitol Nutrition 0.000 description 3
- 229920000609 methyl cellulose Polymers 0.000 description 3
- 239000001923 methylcellulose Substances 0.000 description 3
- 235000010981 methylcellulose Nutrition 0.000 description 3
- 230000003020 moisturizing effect Effects 0.000 description 3
- 239000000346 nonvolatile oil Substances 0.000 description 3
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 3
- 230000037361 pathway Effects 0.000 description 3
- 102000004169 proteins and genes Human genes 0.000 description 3
- 239000000661 sodium alginate Substances 0.000 description 3
- 235000010413 sodium alginate Nutrition 0.000 description 3
- 229940005550 sodium alginate Drugs 0.000 description 3
- 239000008107 starch Substances 0.000 description 3
- 235000019698 starch Nutrition 0.000 description 3
- 229940032147 starch Drugs 0.000 description 3
- 239000000829 suppository Substances 0.000 description 3
- 239000007916 tablet composition Substances 0.000 description 3
- 229940126585 therapeutic drug Drugs 0.000 description 3
- 238000002560 therapeutic procedure Methods 0.000 description 3
- 239000002562 thickening agent Substances 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- RCLQNICOARASSR-SECBINFHSA-N 3-[(2r)-2,3-dihydroxypropyl]-6-fluoro-5-(2-fluoro-4-iodoanilino)-8-methylpyrido[2,3-d]pyrimidine-4,7-dione Chemical compound FC=1C(=O)N(C)C=2N=CN(C[C@@H](O)CO)C(=O)C=2C=1NC1=CC=C(I)C=C1F RCLQNICOARASSR-SECBINFHSA-N 0.000 description 2
- 108020004414 DNA Proteins 0.000 description 2
- 241000450599 DNA viruses Species 0.000 description 2
- 238000002965 ELISA Methods 0.000 description 2
- 102000004190 Enzymes Human genes 0.000 description 2
- 108090000790 Enzymes Proteins 0.000 description 2
- 241000283086 Equidae Species 0.000 description 2
- 241000282412 Homo Species 0.000 description 2
- 101001059454 Homo sapiens Serine/threonine-protein kinase MARK2 Proteins 0.000 description 2
- 102000001291 MAP Kinase Kinase Kinase Human genes 0.000 description 2
- 108060006687 MAP kinase kinase kinase Proteins 0.000 description 2
- 241000701076 Macacine alphaherpesvirus 1 Species 0.000 description 2
- 102000016397 Methyltransferase Human genes 0.000 description 2
- 108060004795 Methyltransferase Proteins 0.000 description 2
- 206010028980 Neoplasm Diseases 0.000 description 2
- 102000001708 Protein Isoforms Human genes 0.000 description 2
- 108010029485 Protein Isoforms Proteins 0.000 description 2
- 102000001253 Protein Kinase Human genes 0.000 description 2
- 108090000315 Protein Kinase C Proteins 0.000 description 2
- 102000003923 Protein Kinase C Human genes 0.000 description 2
- 102100028904 Serine/threonine-protein kinase MARK2 Human genes 0.000 description 2
- 230000004913 activation Effects 0.000 description 2
- 230000002411 adverse Effects 0.000 description 2
- 230000003281 allosteric effect Effects 0.000 description 2
- 229940125528 allosteric inhibitor Drugs 0.000 description 2
- DKNWSYNQZKUICI-UHFFFAOYSA-N amantadine Chemical compound C1C(C2)CC3CC2CC1(N)C3 DKNWSYNQZKUICI-UHFFFAOYSA-N 0.000 description 2
- 229960003805 amantadine Drugs 0.000 description 2
- 238000004458 analytical method Methods 0.000 description 2
- SQVRNKJHWKZAKO-UHFFFAOYSA-N beta-N-Acetyl-D-neuraminic acid Natural products CC(=O)NC1C(O)CC(O)(C(O)=O)OC1C(O)C(O)CO SQVRNKJHWKZAKO-UHFFFAOYSA-N 0.000 description 2
- 201000011510 cancer Diseases 0.000 description 2
- 230000003915 cell function Effects 0.000 description 2
- 230000004663 cell proliferation Effects 0.000 description 2
- 230000001413 cellular effect Effects 0.000 description 2
- 230000033077 cellular process Effects 0.000 description 2
- 230000004069 differentiation Effects 0.000 description 2
- 239000000890 drug combination Substances 0.000 description 2
- 230000001747 exhibiting effect Effects 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 239000003102 growth factor Substances 0.000 description 2
- 238000011534 incubation Methods 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 210000004072 lung Anatomy 0.000 description 2
- 239000008176 lyophilized powder Substances 0.000 description 2
- 244000005700 microbiome Species 0.000 description 2
- 230000035772 mutation Effects 0.000 description 2
- 238000011275 oncology therapy Methods 0.000 description 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 2
- 239000000651 prodrug Substances 0.000 description 2
- 229940002612 prodrug Drugs 0.000 description 2
- 230000035755 proliferation Effects 0.000 description 2
- 108060006633 protein kinase Proteins 0.000 description 2
- 230000001105 regulatory effect Effects 0.000 description 2
- SQVRNKJHWKZAKO-OQPLDHBCSA-N sialic acid Chemical compound CC(=O)N[C@@H]1[C@@H](O)C[C@@](O)(C(O)=O)OC1[C@H](O)[C@H](O)CO SQVRNKJHWKZAKO-OQPLDHBCSA-N 0.000 description 2
- 230000011664 signaling Effects 0.000 description 2
- UCSJYZPVAKXKNQ-HZYVHMACSA-N streptomycin Chemical compound CN[C@H]1[C@H](O)[C@@H](O)[C@H](CO)O[C@H]1O[C@@H]1[C@](C=O)(O)[C@H](C)O[C@H]1O[C@@H]1[C@@H](NC(N)=N)[C@H](O)[C@@H](NC(N)=N)[C@H](O)[C@H]1O UCSJYZPVAKXKNQ-HZYVHMACSA-N 0.000 description 2
- 239000006188 syrup Substances 0.000 description 2
- 235000020357 syrup Nutrition 0.000 description 2
- 230000007704 transition Effects 0.000 description 2
- 238000011144 upstream manufacturing Methods 0.000 description 2
- 229960001028 zanamivir Drugs 0.000 description 2
- 102000040650 (ribonucleotides)n+m Human genes 0.000 description 1
- LNWRKPWPMUWTGU-UHFFFAOYSA-N 2-(cyclopropylmethoxy)-3,4-difluorobenzamide Chemical compound NC(=O)C1=CC=C(F)C(F)=C1OCC1CC1 LNWRKPWPMUWTGU-UHFFFAOYSA-N 0.000 description 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 description 1
- 208000010507 Adenocarcinoma of Lung Diseases 0.000 description 1
- 241000539677 Berant virus Species 0.000 description 1
- 108091003079 Bovine Serum Albumin Proteins 0.000 description 1
- 208000009079 Bronchial Spasm Diseases 0.000 description 1
- 208000014181 Bronchial disease Diseases 0.000 description 1
- 206010006482 Bronchospasm Diseases 0.000 description 1
- 206010009944 Colon cancer Diseases 0.000 description 1
- 206010013710 Drug interaction Diseases 0.000 description 1
- 206010059866 Drug resistance Diseases 0.000 description 1
- 102100023266 Dual specificity mitogen-activated protein kinase kinase 2 Human genes 0.000 description 1
- 101710146529 Dual specificity mitogen-activated protein kinase kinase 2 Proteins 0.000 description 1
- 208000000059 Dyspnea Diseases 0.000 description 1
- 206010013975 Dyspnoeas Diseases 0.000 description 1
- 102400000719 Endokinin-C Human genes 0.000 description 1
- 208000010201 Exanthema Diseases 0.000 description 1
- 229930186217 Glycolipid Natural products 0.000 description 1
- 102000005744 Glycoside Hydrolases Human genes 0.000 description 1
- 108010031186 Glycoside Hydrolases Proteins 0.000 description 1
- 101000838579 Homo sapiens Serine/threonine-protein kinase TAO1 Proteins 0.000 description 1
- 102000004157 Hydrolases Human genes 0.000 description 1
- 108090000604 Hydrolases Proteins 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- 108010052285 Membrane Proteins Proteins 0.000 description 1
- 102000018697 Membrane Proteins Human genes 0.000 description 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 description 1
- 206010028735 Nasal congestion Diseases 0.000 description 1
- 208000012902 Nervous system disease Diseases 0.000 description 1
- 208000025966 Neurological disease Diseases 0.000 description 1
- 229930040373 Paraformaldehyde Natural products 0.000 description 1
- 229930182555 Penicillin Natural products 0.000 description 1
- JGSARLDLIJGVTE-MBNYWOFBSA-N Penicillin G Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)CC1=CC=CC=C1 JGSARLDLIJGVTE-MBNYWOFBSA-N 0.000 description 1
- 108010015355 RAP kinase Proteins 0.000 description 1
- 206010062237 Renal impairment Diseases 0.000 description 1
- 241000831652 Salinivibrio sharmensis Species 0.000 description 1
- 229940124639 Selective inhibitor Drugs 0.000 description 1
- 102100028948 Serine/threonine-protein kinase TAO1 Human genes 0.000 description 1
- 102100028755 Sialidase-2 Human genes 0.000 description 1
- 241000282887 Suidae Species 0.000 description 1
- 208000024780 Urticaria Diseases 0.000 description 1
- 108010067390 Viral Proteins Proteins 0.000 description 1
- 206010047700 Vomiting Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 230000006978 adaptation Effects 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 238000013459 approach Methods 0.000 description 1
- 230000008033 biological extinction Effects 0.000 description 1
- 230000005540 biological transmission Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 125000002837 carbocyclic group Chemical group 0.000 description 1
- 230000020411 cell activation Effects 0.000 description 1
- 230000034303 cell budding Effects 0.000 description 1
- 230000030833 cell death Effects 0.000 description 1
- 230000024245 cell differentiation Effects 0.000 description 1
- 210000003855 cell nucleus Anatomy 0.000 description 1
- 238000003570 cell viability assay Methods 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 229940112822 chewing gum Drugs 0.000 description 1
- 235000015218 chewing gum Nutrition 0.000 description 1
- 230000002860 competitive effect Effects 0.000 description 1
- 231100000135 cytotoxicity Toxicity 0.000 description 1
- 230000003013 cytotoxicity Effects 0.000 description 1
- 230000007850 degeneration Effects 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 230000002900 effect on cell Effects 0.000 description 1
- 239000012636 effector Substances 0.000 description 1
- 210000002919 epithelial cell Anatomy 0.000 description 1
- 125000004494 ethyl ester group Chemical group 0.000 description 1
- 201000005884 exanthem Diseases 0.000 description 1
- 230000029142 excretion Effects 0.000 description 1
- 239000012894 fetal calf serum Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 230000012010 growth Effects 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 230000002458 infectious effect Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000007972 injectable composition Substances 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- 230000003834 intracellular effect Effects 0.000 description 1
- 238000010255 intramuscular injection Methods 0.000 description 1
- 239000007927 intramuscular injection Substances 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- 238000002955 isolation Methods 0.000 description 1
- 231100001231 less toxic Toxicity 0.000 description 1
- 201000005249 lung adenocarcinoma Diseases 0.000 description 1
- 230000003211 malignant effect Effects 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 201000001441 melanoma Diseases 0.000 description 1
- 230000005012 migration Effects 0.000 description 1
- 238000013508 migration Methods 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 238000010172 mouse model Methods 0.000 description 1
- 210000004400 mucous membrane Anatomy 0.000 description 1
- 229940097496 nasal spray Drugs 0.000 description 1
- 239000006225 natural substrate Substances 0.000 description 1
- 230000017066 negative regulation of growth Effects 0.000 description 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 description 1
- 229920001542 oligosaccharide Polymers 0.000 description 1
- 150000002482 oligosaccharides Chemical class 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 210000003300 oropharynx Anatomy 0.000 description 1
- 229920002866 paraformaldehyde Polymers 0.000 description 1
- 244000052769 pathogen Species 0.000 description 1
- 230000001717 pathogenic effect Effects 0.000 description 1
- 230000007918 pathogenicity Effects 0.000 description 1
- 229940049954 penicillin Drugs 0.000 description 1
- XRQDFNLINLXZLB-CKIKVBCHSA-N peramivir Chemical compound CCC(CC)[C@H](NC(C)=O)[C@@H]1[C@H](O)[C@@H](C(O)=O)C[C@H]1NC(N)=N XRQDFNLINLXZLB-CKIKVBCHSA-N 0.000 description 1
- 229960001084 peramivir Drugs 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000012660 pharmacological inhibitor Substances 0.000 description 1
- 238000009521 phase II clinical trial Methods 0.000 description 1
- 210000002381 plasma Anatomy 0.000 description 1
- 231100000857 poor renal function Toxicity 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 239000003909 protein kinase inhibitor Substances 0.000 description 1
- 206010037844 rash Diseases 0.000 description 1
- 229940061374 relenza Drugs 0.000 description 1
- 230000033458 reproduction Effects 0.000 description 1
- 210000002345 respiratory system Anatomy 0.000 description 1
- 229950010746 selumetinib Drugs 0.000 description 1
- CYOHGALHFOKKQC-UHFFFAOYSA-N selumetinib Chemical compound OCCONC(=O)C=1C=C2N(C)C=NC2=C(F)C=1NC1=CC=C(Br)C=C1Cl CYOHGALHFOKKQC-UHFFFAOYSA-N 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 208000013220 shortness of breath Diseases 0.000 description 1
- 125000005629 sialic acid group Chemical group 0.000 description 1
- 238000009097 single-agent therapy Methods 0.000 description 1
- 238000010186 staining Methods 0.000 description 1
- 229960005322 streptomycin Drugs 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 230000009044 synergistic interaction Effects 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 229960004066 trametinib Drugs 0.000 description 1
- LIRYPHYGHXZJBZ-UHFFFAOYSA-N trametinib Chemical compound CC(=O)NC1=CC=CC(N2C(N(C3CC3)C(=O)C3=C(NC=4C(=CC(I)=CC=4)F)N(C)C(=O)C(C)=C32)=O)=C1 LIRYPHYGHXZJBZ-UHFFFAOYSA-N 0.000 description 1
- 238000013518 transcription Methods 0.000 description 1
- 230000035897 transcription Effects 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 108091005703 transmembrane proteins Proteins 0.000 description 1
- 102000035160 transmembrane proteins Human genes 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 description 1
- 229960005486 vaccine Drugs 0.000 description 1
- 229960003862 vemurafenib Drugs 0.000 description 1
- GPXBXXGIAQBQNI-UHFFFAOYSA-N vemurafenib Chemical compound CCCS(=O)(=O)NC1=CC=C(F)C(C(=O)C=2C3=CC(=CN=C3NC=2)C=2C=CC(Cl)=CC=2)=C1F GPXBXXGIAQBQNI-UHFFFAOYSA-N 0.000 description 1
- 230000035899 viability Effects 0.000 description 1
- 230000029812 viral genome replication Effects 0.000 description 1
- 210000000605 viral structure Anatomy 0.000 description 1
- 210000002845 virion Anatomy 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/18—Sulfonamides
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
-
- 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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
-
- 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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
- A61K31/24—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
- A61K31/245—Amino benzoic acid types, e.g. procaine, novocaine
-
- 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
- A61K31/325—Carbamic acids; Thiocarbamic acids; Anhydrides or salts thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
- A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
-
- 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
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4458—Non condensed piperidines, e.g. piperocaine only substituted in position 2, e.g. methylphenidate
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- Emergency Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Pulmonology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261711136P | 2012-10-08 | 2012-10-08 | |
| US61/711,136 | 2012-10-08 | ||
| PCT/EP2013/070917 WO2014056894A1 (en) | 2012-10-08 | 2013-10-08 | Mek inhibitors in the treatment of virus diseases |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201590703A1 EA201590703A1 (ru) | 2015-07-30 |
| EA028605B1 true EA028605B1 (ru) | 2017-12-29 |
Family
ID=49552318
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201590703A EA028605B1 (ru) | 2012-10-08 | 2013-10-08 | Комбинация озельтамивира и ингибитора mek для лечения вирусных заболеваний |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US9566281B2 (enExample) |
| EP (1) | EP2903649A1 (enExample) |
| JP (2) | JP6294889B2 (enExample) |
| KR (1) | KR102174576B1 (enExample) |
| CN (2) | CN109276716B (enExample) |
| AU (1) | AU2013328824B2 (enExample) |
| BR (1) | BR112015007616B1 (enExample) |
| CA (1) | CA2886138C (enExample) |
| EA (1) | EA028605B1 (enExample) |
| WO (1) | WO2014056894A1 (enExample) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9181329B2 (en) * | 2007-08-31 | 2015-11-10 | The University Of Chicago | Methods and compositions related to immunizing against Staphylococcal lung diseases and conditions |
| CN109276716B (zh) * | 2012-10-08 | 2021-06-08 | 归属疗法有限公司 | 用在病毒性疾病的治疗中的mek抑制剂 |
| EP3142658B1 (en) | 2014-05-16 | 2020-01-15 | Atriva Therapeutics GmbH | Novel anti-infective strategy against influenza virus and s. aureus coinfections |
| JPWO2018030534A1 (ja) * | 2016-08-10 | 2019-06-13 | 国立研究開発法人理化学研究所 | Ｂ型肝炎治療用組成物、及びｂ型肝炎ウイルスの複製活性の評価方法 |
| CA3041561A1 (en) * | 2016-11-25 | 2018-05-31 | Jiangsu Hengrui Medicine Co., Ltd. | Pyridone derivative pharmaceutical composition and preparation method thereof |
| US11040027B2 (en) | 2017-01-17 | 2021-06-22 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| SI3697405T1 (sl) * | 2017-10-17 | 2021-11-30 | Atriva Therapeutics Gmbh | Novi zaviralec MEK za zdravljenje virusnih in bakterijskih okužb |
| US20190298669A1 (en) * | 2018-03-29 | 2019-10-03 | Atriva Therapeutics Gmbh | Ci-1040 for the treatment of viral diseases |
| WO2020070390A1 (en) | 2018-10-03 | 2020-04-09 | Jyväskylän Yliopisto | Vemurafenib and salts thereof for use in the treatment of enteroviral infections |
| CN109765324B (zh) * | 2018-11-27 | 2021-03-30 | 苏州科技大学 | 一种mek1蛋白潜在抑制剂的筛选方法 |
| KR20210142125A (ko) | 2019-03-19 | 2021-11-24 | 아트리바 테라퓨틱스 게엠베하 | 바이러스 질환의 치료에서의 ｒｓｋ 억제제 |
| LU101183B1 (en) | 2019-04-16 | 2020-10-16 | Atriva Therapeutics Gmbh | Novel mek-inhibitor for the treatment of viral and bacterial infections |
| US20220370384A1 (en) | 2019-08-27 | 2022-11-24 | Atriva Therapeutics Gmbh | Combinations of mek inhibitors with cap-dependent endonuclease inhibitors |
| EP4041212B1 (en) | 2019-10-08 | 2025-07-23 | Atriva Therapeutics GmbH | Mek inhibitors for the treatment of hantavirus infections |
| WO2021214296A1 (en) * | 2020-04-24 | 2021-10-28 | Johann Wolfgang Goethe-Universität Frankfurt am Main | Treatment of corona virus infections |
| CN111494620A (zh) * | 2020-05-05 | 2020-08-07 | 华中科技大学同济医学院附属协和医院 | 曲美替尼在制备疫苗中的应用 |
| CN111529532A (zh) * | 2020-05-05 | 2020-08-14 | 华中科技大学同济医学院附属协和医院 | 曲美替尼在制备治疗肺部炎症性疾病药物及促进Tfh细胞分化药物中的应用 |
| CN112137994B (zh) * | 2020-09-15 | 2022-10-14 | 中山大学 | 小分子化合物在制备抗丝状病毒药物中的应用 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009140853A1 (en) * | 2008-05-23 | 2009-11-26 | The University Of Hong Kong | Combination therapy for the treatment of influenza |
| US20100137431A1 (en) * | 2000-04-07 | 2010-06-03 | Stephan Ludwig | Use of substances that act as cascade inhibitors of the raf/mek/erk signal cascade, for producing a medicament to treat dna and rna viruses |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE185133T1 (de) | 1990-07-30 | 1999-10-15 | Procyon Pharm Inc | Proteinkinase-c-modulatoren mit entzündungshemmender und antiviraler aktivität |
| US5866601A (en) | 1995-02-27 | 1999-02-02 | Gilead Sciences, Inc. | Carbocyclic compounds |
| US5763483A (en) | 1995-12-29 | 1998-06-09 | Gilead Sciences, Inc. | Carbocyclic compounds |
| JP2002534381A (ja) * | 1999-01-07 | 2002-10-15 | ワーナー−ランバート・カンパニー | Ｍｅｋ阻害剤を用いた抗ウィルス法 |
| DE10138912A1 (de) | 2001-08-08 | 2003-02-27 | Medinnova Ges Med Innovationen | Verwendung von Wirksubstanzen zur Prophylaxe und/oder Therapie von Viruserkrankungen sowie Testsystem zum Auffinden solcher Wirksubstanzen |
| MY153898A (en) * | 2005-06-22 | 2015-04-15 | Plexxikon Inc | Compounds and methods for kinase modulation, and indications therefor |
| CN109276716B (zh) * | 2012-10-08 | 2021-06-08 | 归属疗法有限公司 | 用在病毒性疾病的治疗中的mek抑制剂 |
-
2013
- 2013-10-08 CN CN201810617076.7A patent/CN109276716B/zh active Active
- 2013-10-08 BR BR112015007616-5A patent/BR112015007616B1/pt active IP Right Grant
- 2013-10-08 JP JP2015535058A patent/JP6294889B2/ja not_active Expired - Fee Related
- 2013-10-08 EP EP13788684.2A patent/EP2903649A1/en not_active Withdrawn
- 2013-10-08 KR KR1020157010311A patent/KR102174576B1/ko not_active Expired - Fee Related
- 2013-10-08 WO PCT/EP2013/070917 patent/WO2014056894A1/en not_active Ceased
- 2013-10-08 CA CA2886138A patent/CA2886138C/en active Active
- 2013-10-08 AU AU2013328824A patent/AU2013328824B2/en not_active Ceased
- 2013-10-08 US US14/434,328 patent/US9566281B2/en not_active Expired - Fee Related
- 2013-10-08 EA EA201590703A patent/EA028605B1/ru active IP Right Revival
- 2013-10-08 CN CN201380064116.5A patent/CN105101999B/zh active Active
-
2017
- 2017-02-09 US US15/428,693 patent/US20170209450A1/en not_active Abandoned
-
2018
- 2018-02-16 JP JP2018025712A patent/JP2018118971A/ja active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20100137431A1 (en) * | 2000-04-07 | 2010-06-03 | Stephan Ludwig | Use of substances that act as cascade inhibitors of the raf/mek/erk signal cascade, for producing a medicament to treat dna and rna viruses |
| WO2009140853A1 (en) * | 2008-05-23 | 2009-11-26 | The University Of Hong Kong | Combination therapy for the treatment of influenza |
Non-Patent Citations (4)
| Title |
|---|
| "Vemurafenib B-raf Kinase Inhibitor Oncolytic", DRUGS OF THE FUTURE, PROUS SCIENCE, ES, vol. 36, no. 3, 1 January 2011 (2011-01-01), ES, pages 191 - 199, XP007922458, ISSN: 0377-8282, DOI: 10.1358/dof.2011.36.3.1590788 * |
| HSING-PANG HSIEH, JOHN HSU: "Strategies of Development of Antiviral Agents Directed Against Influenza Virus Replication", CURRENT PHARMACEUTICAL DESIGN, BENTHAM SCIENCE PUBLISHERS, vol. 13, no. 34, 1 December 2007 (2007-12-01), pages 3531 - 3542, XP055093630, ISSN: 13816128, DOI: 10.2174/138161207782794248 * |
| KAROLINE DROEBNER; STEPHAN PLESCHKA; STEPHAN LUDWIG; OLIVER PLANZ;: "Antiviral activity of the MEK-inhibitor U0126 against pandemic H1N1v and highly pathogenic avian influenza virusand", ANTIVIRAL RESEARCH, ELSEVIER BV, NL, vol. 92, no. 2, 3 August 2011 (2011-08-03), NL, pages 195 - 203, XP028325598, ISSN: 0166-3542, DOI: 10.1016/j.antiviral.2011.08.002 * |
| S. LUDWIG: "Targeting cell signalling pathways to fight the flu: towards a paradigm change in anti-influenza therapy", JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, OXFORD UNIVERSITY PRESS, vol. 64, no. 1, 1 July 2009 (2009-07-01), pages 1 - 4, XP055093636, ISSN: 03057453, DOI: 10.1093/jac/dkp161 * |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2015534562A (ja) | 2015-12-03 |
| EP2903649A1 (en) | 2015-08-12 |
| AU2013328824B2 (en) | 2018-04-05 |
| CN109276716B (zh) | 2021-06-08 |
| CN105101999A (zh) | 2015-11-25 |
| US9566281B2 (en) | 2017-02-14 |
| JP2018118971A (ja) | 2018-08-02 |
| KR102174576B1 (ko) | 2020-11-06 |
| BR112015007616B1 (pt) | 2022-08-09 |
| AU2013328824A1 (en) | 2015-04-30 |
| CN105101999B (zh) | 2018-07-17 |
| CA2886138C (en) | 2021-10-12 |
| BR112015007616A2 (pt) | 2017-08-08 |
| KR20150097464A (ko) | 2015-08-26 |
| WO2014056894A1 (en) | 2014-04-17 |
| US20170209450A1 (en) | 2017-07-27 |
| US20150224103A1 (en) | 2015-08-13 |
| CA2886138A1 (en) | 2014-04-17 |
| EA201590703A1 (ru) | 2015-07-30 |
| CN109276716A (zh) | 2019-01-29 |
| JP6294889B2 (ja) | 2018-03-14 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| KR102174576B1 (ko) | 바이러스 질환 치료에서의 ｍｅｋ 억제제 | |
| WO2021214033A1 (en) | Vidofludimus for use in the treatment or prevention of viral diseases | |
| WO2012136851A1 (en) | Methods and pharmaceutical compositions for inhibiting influenza viruses replication | |
| KR20210120891A (ko) | 유행성 rna 바이러스 감염질환의 예방 또는 치료용 약제학적 조성물 | |
| WO2013131496A1 (zh) | 治疗病毒疾病的成分和方法 | |
| US20220370384A1 (en) | Combinations of mek inhibitors with cap-dependent endonuclease inhibitors | |
| WO2014123680A1 (en) | Antimicrobial methods using inhibitors of exchange proteins directly activated by camp (epac) | |
| US20240009213A1 (en) | Treatment for viral infection | |
| US10864210B2 (en) | Composition and combined medication method for treating enterovirus infection | |
| HK40003862B (en) | Mek inhibitors in the treatment of virus diseases | |
| HK40003862A (en) | Mek inhibitors in the treatment of virus diseases | |
| CN121466087A (zh) | Pha-767491在制备防治h1n1亚型猪流感药物中的应用 | |
| Hewedy | Broad-Spectrum Antivirals to Combat COVID-19: the Reality and Challenges | |
| CN121445739A (zh) | Pha-767491作为h3n2亚型猪流感病毒复制抑制剂的应用 | |
| CA2999670A1 (en) | Ci-1040 for the treatment of viral diseases | |
| AU2018202283A1 (en) | Ci-1040 for the treatment of viral diseases | |
| HK1237643A1 (en) | Therapy for inhibition of single-stranded rna virus replication |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG TJ TM RU |
|
| NF4A | Restoration of lapsed right to a eurasian patent |
Designated state(s): AM AZ BY KZ TJ RU |