JP2009502920A5 - - Google Patents

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Publication number: JP2009502920A5
Authority: JP; Japan
Prior art keywords: alkyl; ifn; dose; cycloalkyl; subcutaneously
Prior art date: 2006-07-17
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

Application number

JP2008523949A

Other languages

English (en)

Japanese (ja)

Other versions

JP5249028B2 (ja

JP2009502920A (ja

Filing date

2006-07-17

Publication date

2009-10-15

2006-07-17 Application filed filed Critical

2006-07-17 Priority claimed from PCT/US2006/027738 external-priority patent/WO2007015824A2/en

2009-01-29 Publication of JP2009502920A publication Critical patent/JP2009502920A/ja

2009-10-15 Publication of JP2009502920A5 publication Critical patent/JP2009502920A5/ja

2013-07-31 Application granted granted Critical

2013-07-31 Publication of JP5249028B2 publication Critical patent/JP5249028B2/ja

Status Active legal-status Critical Current

2026-07-17 Anticipated expiration legal-status Critical

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125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 140
229910052739 hydrogen Inorganic materials 0.000 claims description 129
229910052799 carbon Inorganic materials 0.000 claims description 113
150000001875 compounds Chemical class 0.000 claims description 113
-1 chloropyridinyl Chemical group 0.000 claims description 99
239000001257 hydrogen Substances 0.000 claims description 20
125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 17
125000001072 heteroaryl group Chemical group 0.000 claims description 16
PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 claims description 13
125000002541 furyl group Chemical group 0.000 claims description 13
125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 7
125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 7
125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 6
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 2
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
125000004076 pyridyl group Chemical group 0.000 claims 3
125000000068 chlorophenyl group Chemical group 0.000 claims 1
125000004188 dichlorophenyl group Chemical group 0.000 claims 1
125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
125000000217 alkyl group Chemical group 0.000 description 371
239000005557 antagonist Substances 0.000 description 167
229940079593 drug Drugs 0.000 description 159
239000003814 drug Substances 0.000 description 159
108010010648 interferon alfacon-1 Proteins 0.000 description 158
125000003545 alkoxy group Chemical group 0.000 description 139
125000001316 cycloalkyl alkyl group Chemical group 0.000 description 135
239000003112 inhibitor Substances 0.000 description 134
125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 description 133
238000000034 method Methods 0.000 description 133
102100040247 Tumor necrosis factor Human genes 0.000 description 118
108010074328 Interferon-gamma Proteins 0.000 description 106
108010047761 Interferon-alpha Proteins 0.000 description 105
102000006992 Interferon-alpha Human genes 0.000 description 105
125000001153 fluoro group Chemical group F* 0.000 description 102
102100037850 Interferon gamma Human genes 0.000 description 99
OHDXDNUPVVYWOV-UHFFFAOYSA-N n-methyl-1-(2-naphthalen-1-ylsulfanylphenyl)methanamine Chemical compound CNCC1=CC=CC=C1SC1=CC=CC2=CC=CC=C12 OHDXDNUPVVYWOV-UHFFFAOYSA-N 0.000 description 99
125000005843 halogen group Chemical group 0.000 description 88
125000004093 cyano group Chemical group *C#N 0.000 description 69
125000003118 aryl group Chemical group 0.000 description 68
229940090438 infergen Drugs 0.000 description 63
230000000670 limiting effect Effects 0.000 description 53
230000037396 body weight Effects 0.000 description 50
125000000753 cycloalkyl group Chemical group 0.000 description 50
RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 description 48
230000002354 daily effect Effects 0.000 description 47
GOZMBJCYMQQACI-UHFFFAOYSA-N 6,7-dimethyl-3-[[methyl-[2-[methyl-[[1-[3-(trifluoromethyl)phenyl]indol-3-yl]methyl]amino]ethyl]amino]methyl]chromen-4-one;dihydrochloride Chemical compound Cl.Cl.C=1OC2=CC(C)=C(C)C=C2C(=O)C=1CN(C)CCN(C)CC(C1=CC=CC=C11)=CN1C1=CC=CC(C(F)(F)F)=C1 GOZMBJCYMQQACI-UHFFFAOYSA-N 0.000 description 46
208000015181 infectious disease Diseases 0.000 description 43
229910052760 oxygen Inorganic materials 0.000 description 41
230000003442 weekly effect Effects 0.000 description 37
MRKKUGDWODATMF-SECBINFHSA-N (2R)-2-[[5-methoxy-2-(methylamino)pyrimidin-4-yl]amino]hexan-1-ol Chemical compound CCCC[C@H](CO)Nc1nc(NC)ncc1OC MRKKUGDWODATMF-SECBINFHSA-N 0.000 description 34
229940124257 Interferon receptor agonist Drugs 0.000 description 34
IWUCXVSUMQZMFG-AFCXAGJDSA-N Ribavirin Chemical compound N1=C(C(=O)N)N=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 IWUCXVSUMQZMFG-AFCXAGJDSA-N 0.000 description 34
229960000329 ribavirin Drugs 0.000 description 34
HZCAHMRRMINHDJ-DBRKOABJSA-N ribavirin Natural products O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1N=CN=C1 HZCAHMRRMINHDJ-DBRKOABJSA-N 0.000 description 34
FCEHBMOGCRZNNI-UHFFFAOYSA-N 1-benzothiophene Chemical compound C1=CC=C2SC=CC2=C1 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 description 32
YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 32
SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 description 32
KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 description 32
JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 32
KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 description 32
SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 description 32
YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 description 32
125000003342 alkenyl group Chemical group 0.000 description 32
IOJUPLGTWVMSFF-UHFFFAOYSA-N benzothiazole Chemical compound C1=CC=C2SC=NC2=C1 IOJUPLGTWVMSFF-UHFFFAOYSA-N 0.000 description 32
XSCHRSMBECNVNS-UHFFFAOYSA-N quinoxaline Chemical compound N1=CC=NC2=CC=CC=C21 XSCHRSMBECNVNS-UHFFFAOYSA-N 0.000 description 32
108010008165 Etanercept Proteins 0.000 description 30
125000004356 hydroxy functional group Chemical group O* 0.000 description 29
IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 29
229910052717 sulfur Inorganic materials 0.000 description 29
238000005303 weighing Methods 0.000 description 28
229960002964 adalimumab Drugs 0.000 description 26
229960000403 etanercept Drugs 0.000 description 26
229960000598 infliximab Drugs 0.000 description 26
101800001838 Serine protease/helicase NS3 Proteins 0.000 description 25
229960003358 interferon alfacon-1 Drugs 0.000 description 25
229910052757 nitrogen Inorganic materials 0.000 description 25
125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 description 24
208000036142 Viral infection Diseases 0.000 description 24
238000002648 combination therapy Methods 0.000 description 24
AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical compound C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 description 24
230000009385 viral infection Effects 0.000 description 24
125000000623 heterocyclic group Chemical group 0.000 description 23
229940077274 Alpha glucosidase inhibitor Drugs 0.000 description 20
101000599940 Homo sapiens Interferon gamma Proteins 0.000 description 20
102000014150 Interferons Human genes 0.000 description 20
108010050904 Interferons Proteins 0.000 description 20
229940099550 actimmune Drugs 0.000 description 20
239000003888 alpha glucosidase inhibitor Substances 0.000 description 20
108010042414 interferon gamma-1b Proteins 0.000 description 20
125000001624 naphthyl group Chemical group 0.000 description 20
229940079322 interferon Drugs 0.000 description 19
0 **C(CCC=CCC=C[C@](C1)C1(C(*)=O)NC(C1N2CC(*)C1)=O)C2=O Chemical compound **C(CCC=CCC=C[C@](C1)C1(C(*)=O)NC(C1N2CC(*)C1)=O)C2=O 0.000 description 18
125000000882 C2-C6 alkenyl group Chemical group 0.000 description 18
125000005842 heteroatom Chemical group 0.000 description 18
108010018844 interferon type III Proteins 0.000 description 17
QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 17
108010077753 type II interferon receptor Proteins 0.000 description 17
HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 description 16
ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 description 16
PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 description 16
WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 description 16
CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 description 16
WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical group C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 16
FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 description 16
150000001413 amino acids Chemical class 0.000 description 16
125000004429 atom Chemical group 0.000 description 16
RFRXIWQYSOIBDI-UHFFFAOYSA-N benzarone Chemical compound CCC=1OC2=CC=CC=C2C=1C(=O)C1=CC=C(O)C=C1 RFRXIWQYSOIBDI-UHFFFAOYSA-N 0.000 description 16
PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 description 16
RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 description 16
ZLTPDFXIESTBQG-UHFFFAOYSA-N isothiazole Chemical compound C=1C=NSC=1 ZLTPDFXIESTBQG-UHFFFAOYSA-N 0.000 description 16
CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 description 16
PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical compound C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 description 16
UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 16
JUJWROOIHBZHMG-UHFFFAOYSA-O pyridinium Chemical compound C1=CC=[NH+]C=C1 JUJWROOIHBZHMG-UHFFFAOYSA-O 0.000 description 16
229920006395 saturated elastomer Polymers 0.000 description 16
229930192474 thiophene Natural products 0.000 description 16
OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 15
235000001014 amino acid Nutrition 0.000 description 15
229940024606 amino acid Drugs 0.000 description 15
125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 description 15
125000002757 morpholinyl group Chemical group 0.000 description 15
125000004193 piperazinyl group Chemical group 0.000 description 15
125000003386 piperidinyl group Chemical group 0.000 description 15
125000000719 pyrrolidinyl group Chemical group 0.000 description 15
125000006546 (C4-C10) cycloalkyl group Chemical group 0.000 description 14
108060008682 Tumor Necrosis Factor Proteins 0.000 description 14
230000003993 interaction Effects 0.000 description 14
101800001530 Thymosin alpha Proteins 0.000 description 13
230000004048 modification Effects 0.000 description 13
238000012986 modification Methods 0.000 description 13
125000005119 alkyl cycloalkyl group Chemical group 0.000 description 12
125000003710 aryl alkyl group Chemical group 0.000 description 12
229940002988 pegasys Drugs 0.000 description 12
108010092853 peginterferon alfa-2a Proteins 0.000 description 12
108010092851 peginterferon alfa-2b Proteins 0.000 description 12
229940106366 pegintron Drugs 0.000 description 12
125000000335 thiazolyl group Chemical group 0.000 description 12
125000001544 thienyl group Chemical group 0.000 description 12
125000002971 oxazolyl group Chemical group 0.000 description 11
ISWRGOKTTBVCFA-UHFFFAOYSA-N pirfenidone Chemical class C1=C(C)C=CC(=O)N1C1=CC=CC=C1 ISWRGOKTTBVCFA-UHFFFAOYSA-N 0.000 description 11
OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 10
208000019425 cirrhosis of liver Diseases 0.000 description 10
125000005647 linker group Chemical group 0.000 description 10
125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 description 10
238000007920 subcutaneous administration Methods 0.000 description 10
GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 description 10
XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 9
150000001408 amides Chemical class 0.000 description 9
125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 description 9
229960003073 pirfenidone Drugs 0.000 description 9
MZOFCQQQCNRIBI-VMXHOPILSA-N (3s)-4-[[(2s)-1-[[(2s)-1-[[(1s)-1-carboxy-2-hydroxyethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-[[2-[[(2s)-2,6-diaminohexanoyl]amino]acetyl]amino]-4-oxobutanoic acid Chemical compound OC[C@@H](C(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@@H](N)CCCCN MZOFCQQQCNRIBI-VMXHOPILSA-N 0.000 description 8
NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 8
QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 8
125000000000 cycloalkoxy group Chemical group 0.000 description 8
125000004446 heteroarylalkyl group Chemical group 0.000 description 8
239000001301 oxygen Substances 0.000 description 8
108090000765 processed proteins & peptides Proteins 0.000 description 8
125000003373 pyrazinyl group Chemical group 0.000 description 8
239000000758 substrate Substances 0.000 description 8
239000011593 sulfur Substances 0.000 description 8
206010016654 Fibrosis Diseases 0.000 description 7
125000000539 amino acid group Chemical group 0.000 description 7
238000006243 chemical reaction Methods 0.000 description 7
230000003203 everyday effect Effects 0.000 description 7
125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 7
238000003786 synthesis reaction Methods 0.000 description 7
QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 6
230000015572 biosynthetic process Effects 0.000 description 6
125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 6
150000002431 hydrogen Chemical group 0.000 description 6
229940044601 receptor agonist Drugs 0.000 description 6
239000000018 receptor agonist Substances 0.000 description 6
241000894007 species Species 0.000 description 6
IAZDPXIOMUYVGZ-UHFFFAOYSA-N DMSO Substances CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 5
108010086140 Interferon alpha-beta Receptor Proteins 0.000 description 5
102000007438 Interferon alpha-beta Receptor Human genes 0.000 description 5
230000006870 function Effects 0.000 description 5
239000000203 mixture Substances 0.000 description 5
230000037452 priming Effects 0.000 description 5
239000000243 solution Substances 0.000 description 5
125000004169 (C1-C6) alkyl group Chemical group 0.000 description 4
125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 description 4
125000006704 (C5-C6) cycloalkyl group Chemical group 0.000 description 4
QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 description 4
BPYKTIZUTYGOLE-IFADSCNNSA-N Bilirubin Chemical compound N1C(=O)C(C)=C(C=C)\C1=C\C1=C(C)C(CCC(O)=O)=C(CC2=C(C(C)=C(\C=C/3C(=C(C=C)C(=O)N\3)C)N2)CCC(O)=O)N1 BPYKTIZUTYGOLE-IFADSCNNSA-N 0.000 description 4
DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 4
JHRWWRDRBPCWTF-OLQVQODUSA-N captafol Chemical compound C1C=CC[C@H]2C(=O)N(SC(Cl)(Cl)C(Cl)Cl)C(=O)[C@H]21 JHRWWRDRBPCWTF-OLQVQODUSA-N 0.000 description 4
150000001732 carboxylic acid derivatives Chemical class 0.000 description 4
HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 4
230000007882 cirrhosis Effects 0.000 description 4
229940073621 enbrel Drugs 0.000 description 4
229910052736 halogen Inorganic materials 0.000 description 4
230000000004 hemodynamic effect Effects 0.000 description 4
229940048921 humira Drugs 0.000 description 4
230000002401 inhibitory effect Effects 0.000 description 4
230000003908 liver function Effects 0.000 description 4
230000004060 metabolic process Effects 0.000 description 4
239000012044 organic layer Substances 0.000 description 4
UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 description 4
150000003254 radicals Chemical class 0.000 description 4
102000005962 receptors Human genes 0.000 description 4
108020003175 receptors Proteins 0.000 description 4
229940116176 remicade Drugs 0.000 description 4
SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 description 4
239000002904 solvent Substances 0.000 description 4
229910052721 tungsten Inorganic materials 0.000 description 4
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 4
102100040018 Interferon alpha-2 Human genes 0.000 description 3
108010079944 Interferon-alpha2b Proteins 0.000 description 3
102000008070 Interferon-gamma Human genes 0.000 description 3
OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 description 3
PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 description 3
108010078233 Thymalfasin Proteins 0.000 description 3
239000004480 active ingredient Substances 0.000 description 3
239000012267 brine Substances 0.000 description 3
230000004761 fibrosis Effects 0.000 description 3
230000000977 initiatory effect Effects 0.000 description 3
229960003130 interferon gamma Drugs 0.000 description 3
230000006320 pegylation Effects 0.000 description 3
229910052698 phosphorus Inorganic materials 0.000 description 3
239000011574 phosphorus Substances 0.000 description 3
239000000651 prodrug Substances 0.000 description 3
229940002612 prodrug Drugs 0.000 description 3
230000009467 reduction Effects 0.000 description 3
150000003839 salts Chemical class 0.000 description 3
238000009097 single-agent therapy Methods 0.000 description 3
229910052938 sodium sulfate Inorganic materials 0.000 description 3
235000011152 sodium sulphate Nutrition 0.000 description 3
HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 3
239000007787 solid Substances 0.000 description 3
125000003107 substituted aryl group Chemical group 0.000 description 3
238000013268 sustained release Methods 0.000 description 3
239000012730 sustained-release form Substances 0.000 description 3
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JP2008523949A 2005-07-25 2006-07-17 Ｃ型肝炎ウイルス複製の新規大環状阻害剤 Active JP5249028B2 (ja)

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US78980006P	2006-04-06	2006-04-06
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