JPWO2020044266A5 - - Google Patents
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- JPWO2020044266A5 JPWO2020044266A5 JP2021510174A JP2021510174A JPWO2020044266A5 JP WO2020044266 A5 JPWO2020044266 A5 JP WO2020044266A5 JP 2021510174 A JP2021510174 A JP 2021510174A JP 2021510174 A JP2021510174 A JP 2021510174A JP WO2020044266 A5 JPWO2020044266 A5 JP WO2020044266A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- pharmaceutically acceptable
- composition according
- alcoholic steatohepatitis
- inhibitor
- 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.)
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- 239000008194 pharmaceutical composition Substances 0.000 claims 33
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 26
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 25
- 150000003839 salts Chemical class 0.000 claims 22
- -1 1-isopropyl-7-oxo-1,4,6,7-tetrahydrospiro [indazole-5,4'-piperidine] -1'-carbonyl Chemical group 0.000 claims 20
- 239000003112 inhibitor Substances 0.000 claims 19
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 13
- 208000019425 cirrhosis of liver Diseases 0.000 claims 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 13
- 201000010099 disease Diseases 0.000 claims 12
- 239000007787 solid Substances 0.000 claims 10
- 206010016654 Fibrosis Diseases 0.000 claims 9
- 230000007882 cirrhosis Effects 0.000 claims 9
- 239000005711 Benzoic acid Substances 0.000 claims 7
- 235000010233 benzoic acid Nutrition 0.000 claims 7
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 6
- 239000003795 chemical substances by application Substances 0.000 claims 6
- 229940079593 drug Drugs 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- QDXGKRWDQCEABB-UHFFFAOYSA-N pyrimidine-5-carboxamide Chemical compound NC(=O)C1=CN=CN=C1 QDXGKRWDQCEABB-UHFFFAOYSA-N 0.000 claims 6
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 5
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 5
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 5
- 208000004930 Fatty Liver Diseases 0.000 claims 4
- 206010019708 Hepatic steatosis Diseases 0.000 claims 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 claims 4
- 208000010706 fatty liver disease Diseases 0.000 claims 4
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 4
- 238000000634 powder X-ray diffraction Methods 0.000 claims 4
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 4
- LXZMHBHEXAELHH-UHFFFAOYSA-N 4-[6-methoxy-4-(7-oxo-1-propan-2-ylspiro[4,6-dihydroindazole-5,4'-piperidine]-1'-carbonyl)pyridin-2-yl]benzoic acid Chemical compound N=1C(OC)=CC(C(=O)N2CCC3(CC2)CC(=O)C=2N(C(C)C)N=CC=2C3)=CC=1C1=CC=C(C(O)=O)C=C1 LXZMHBHEXAELHH-UHFFFAOYSA-N 0.000 claims 3
- 201000009030 Carcinoma Diseases 0.000 claims 3
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- 239000003472 antidiabetic agent Substances 0.000 claims 3
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- 229940075993 receptor modulator Drugs 0.000 claims 3
- 102000000452 Acetyl-CoA carboxylase Human genes 0.000 claims 2
- 108010016219 Acetyl-CoA carboxylase Proteins 0.000 claims 2
- 108010018763 Biotin carboxylase Proteins 0.000 claims 2
- FAFWJVRLRTVCCS-UHFFFAOYSA-N C(C)(C)N1N=CC=2CC3(CCN(CC3)C(=O)C3=CC=NC(=C3)OC)CC(C12)=O Chemical compound C(C)(C)N1N=CC=2CC3(CCN(CC3)C(=O)C3=CC=NC(=C3)OC)CC(C12)=O FAFWJVRLRTVCCS-UHFFFAOYSA-N 0.000 claims 2
- 102000002148 Diacylglycerol O-acyltransferase Human genes 0.000 claims 2
- 108010001348 Diacylglycerol O-acyltransferase Proteins 0.000 claims 2
- 102000016622 Dipeptidyl Peptidase 4 Human genes 0.000 claims 2
- 102100025353 G-protein coupled bile acid receptor 1 Human genes 0.000 claims 2
- 101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 claims 2
- 208000002705 Glucose Intolerance Diseases 0.000 claims 2
- 206010019280 Heart failures Diseases 0.000 claims 2
- 101000857733 Homo sapiens G-protein coupled bile acid receptor 1 Proteins 0.000 claims 2
- 102100030643 Hydroxycarboxylic acid receptor 2 Human genes 0.000 claims 2
- 102000004877 Insulin Human genes 0.000 claims 2
- 108090001061 Insulin Proteins 0.000 claims 2
- 108010055717 JNK Mitogen-Activated Protein Kinases Proteins 0.000 claims 2
- 108010015847 Non-Receptor Type 1 Protein Tyrosine Phosphatase Proteins 0.000 claims 2
- 208000018262 Peripheral vascular disease Diseases 0.000 claims 2
- 102000004861 Phosphoric Diester Hydrolases Human genes 0.000 claims 2
- 108090001050 Phosphoric Diester Hydrolases Proteins 0.000 claims 2
- 102100033001 Tyrosine-protein phosphatase non-receptor type 1 Human genes 0.000 claims 2
- 239000012190 activator Substances 0.000 claims 2
- 229960004733 albiglutide Drugs 0.000 claims 2
- OGWAVGNOAMXIIM-UHFFFAOYSA-N albiglutide Chemical compound O=C(O)C(NC(=O)CNC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)CNC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)CNC(=O)C(NC(=O)CNC(=O)C(N)CC=1(N=CNC=1))CCC(=O)O)C(O)C)CC2(=CC=CC=C2))C(O)C)CO)CC(=O)O)C(C)C)CO)CO)CC3(=CC=C(O)C=C3))CC(C)C)CCC(=O)O)CCC(=O)N)C)C)CCCCN)CCC(=O)O)CC4(=CC=CC=C4))C(CC)C)C)CC=6(C5(=C(C=CC=C5)NC=6)))CC(C)C)C(C)C)CCCCN)CCCNC(=N)N OGWAVGNOAMXIIM-UHFFFAOYSA-N 0.000 claims 2
- 239000003888 alpha glucosidase inhibitor Substances 0.000 claims 2
- 229940125708 antidiabetic agent Drugs 0.000 claims 2
- 235000012000 cholesterol Nutrition 0.000 claims 2
- 208000029078 coronary artery disease Diseases 0.000 claims 2
- 229940124828 glucokinase activator Drugs 0.000 claims 2
- 229940125396 insulin Drugs 0.000 claims 2
- 150000002632 lipids Chemical class 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 201000009104 prediabetes syndrome Diseases 0.000 claims 2
- 108700027806 rGLP-1 Proteins 0.000 claims 2
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical class OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 claims 2
- HSINOMROUCMIEA-FGVHQWLLSA-N (2s,4r)-4-[(3r,5s,6r,7r,8s,9s,10s,13r,14s,17r)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methylpentanoic acid Chemical compound C([C@@]12C)C[C@@H](O)C[C@H]1[C@@H](CC)[C@@H](O)[C@@H]1[C@@H]2CC[C@]2(C)[C@@H]([C@H](C)C[C@H](C)C(O)=O)CC[C@H]21 HSINOMROUCMIEA-FGVHQWLLSA-N 0.000 claims 1
- ZFXCIWPVPUPDMF-UHFFFAOYSA-N 1-propan-2-ylspiro[4,6-dihydroindazole-5,4'-piperidine]-7-one Chemical compound C1C(=O)C=2N(C(C)C)N=CC=2CC21CCNCC2 ZFXCIWPVPUPDMF-UHFFFAOYSA-N 0.000 claims 1
- ROJNYKZWTOHRNU-UHFFFAOYSA-N 2-chloro-4,5-difluoro-n-[[2-methoxy-5-(methylcarbamoylamino)phenyl]carbamoyl]benzamide Chemical compound CNC(=O)NC1=CC=C(OC)C(NC(=O)NC(=O)C=2C(=CC(F)=C(F)C=2)Cl)=C1 ROJNYKZWTOHRNU-UHFFFAOYSA-N 0.000 claims 1
- IGRCWJPBLWGNPX-UHFFFAOYSA-N 3-(2-chlorophenyl)-n-(4-chlorophenyl)-n,5-dimethyl-1,2-oxazole-4-carboxamide Chemical compound C=1C=C(Cl)C=CC=1N(C)C(=O)C1=C(C)ON=C1C1=CC=CC=C1Cl IGRCWJPBLWGNPX-UHFFFAOYSA-N 0.000 claims 1
- DGENZVKCTGIDRZ-UHFFFAOYSA-N 3-[4-[(3-phenoxyphenyl)methylamino]phenyl]propanoic acid Chemical compound C1=CC(CCC(=O)O)=CC=C1NCC1=CC=CC(OC=2C=CC=CC=2)=C1 DGENZVKCTGIDRZ-UHFFFAOYSA-N 0.000 claims 1
- COYPLDIXZODDDL-UHFFFAOYSA-N 3h-benzimidazole-5-carboxylic acid Chemical class OC(=O)C1=CC=C2N=CNC2=C1 COYPLDIXZODDDL-UHFFFAOYSA-N 0.000 claims 1
- MPLLLQUZNJSVTK-UHFFFAOYSA-N 5-[3-[4-[2-(4-fluorophenyl)ethoxy]phenyl]propyl]furan-2-carboxylic acid Chemical compound O1C(C(=O)O)=CC=C1CCCC(C=C1)=CC=C1OCCC1=CC=C(F)C=C1 MPLLLQUZNJSVTK-UHFFFAOYSA-N 0.000 claims 1
- 241000208140 Acer Species 0.000 claims 1
- 208000010444 Acidosis Diseases 0.000 claims 1
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 102100022089 Acyl-[acyl-carrier-protein] hydrolase Human genes 0.000 claims 1
- 229940123324 Acyltransferase inhibitor Drugs 0.000 claims 1
- 102000016912 Aldehyde Reductase Human genes 0.000 claims 1
- 108010053754 Aldehyde reductase Proteins 0.000 claims 1
- 229940077274 Alpha glucosidase inhibitor Drugs 0.000 claims 1
- 101710171801 Alpha-amylase inhibitor Proteins 0.000 claims 1
- 229940123208 Biguanide Drugs 0.000 claims 1
- XNCOSPRUTUOJCJ-UHFFFAOYSA-N Biguanide Chemical compound NC(N)=NC(N)=N XNCOSPRUTUOJCJ-UHFFFAOYSA-N 0.000 claims 1
- 102100031151 C-C chemokine receptor type 2 Human genes 0.000 claims 1
- 101710149815 C-C chemokine receptor type 2 Proteins 0.000 claims 1
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- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 102000002666 Carnitine O-palmitoyltransferase Human genes 0.000 claims 1
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- 208000002177 Cataract Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 229940122502 Cholesterol absorption inhibitor Drugs 0.000 claims 1
- 208000030808 Clear cell renal carcinoma Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 108010011459 Exenatide Proteins 0.000 claims 1
- HTQBXNHDCUEHJF-XWLPCZSASA-N Exenatide Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)CNC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 HTQBXNHDCUEHJF-XWLPCZSASA-N 0.000 claims 1
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- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
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- 101000843810 Homo sapiens Hydroxycarboxylic acid receptor 1 Proteins 0.000 claims 1
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