JPWO2021110886A5 - - Google Patents
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- JPWO2021110886A5 JPWO2021110886A5 JP2022532829A JP2022532829A JPWO2021110886A5 JP WO2021110886 A5 JPWO2021110886 A5 JP WO2021110886A5 JP 2022532829 A JP2022532829 A JP 2022532829A JP 2022532829 A JP2022532829 A JP 2022532829A JP WO2021110886 A5 JPWO2021110886 A5 JP WO2021110886A5
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- 206010010774 Constipation Diseases 0.000 claims 14
- 206010008635 Cholestasis Diseases 0.000 claims 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 10
- 230000007870 cholestasis Effects 0.000 claims 9
- 231100000359 cholestasis Toxicity 0.000 claims 9
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 claims 8
- NIXOWILDQLNWCW-UHFFFAOYSA-N 2-Propenoic acid Natural products OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims 8
- 239000003613 bile acid Substances 0.000 claims 8
- 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 7
- 201000010099 disease Diseases 0.000 claims 7
- 201000002150 Progressive familial intrahepatic cholestasis Diseases 0.000 claims 6
- 208000019425 cirrhosis of liver Diseases 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 210000004185 liver Anatomy 0.000 claims 6
- 201000001493 benign recurrent intrahepatic cholestasis Diseases 0.000 claims 5
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 5
- 208000019423 liver disease Diseases 0.000 claims 5
- 150000001875 compounds Chemical class 0.000 claims 4
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 4
- 230000002265 prevention Effects 0.000 claims 4
- 208000011580 syndromic disease Diseases 0.000 claims 4
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 3
- 208000008964 Chemical and Drug Induced Liver Injury Diseases 0.000 claims 3
- 206010010317 Congenital absence of bile ducts Diseases 0.000 claims 3
- 206010010356 Congenital anomaly Diseases 0.000 claims 3
- 206010072268 Drug-induced liver injury Diseases 0.000 claims 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 3
- 206010019708 Hepatic steatosis Diseases 0.000 claims 3
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 3
- 208000004622 abetalipoproteinemia Diseases 0.000 claims 3
- 210000000941 bile Anatomy 0.000 claims 3
- 210000000013 bile duct Anatomy 0.000 claims 3
- 201000005271 biliary atresia Diseases 0.000 claims 3
- 230000015572 biosynthetic process Effects 0.000 claims 3
- 201000001883 cholelithiasis Diseases 0.000 claims 3
- 206010012601 diabetes mellitus Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 238000003786 synthesis reaction Methods 0.000 claims 3
- 238000002054 transplantation Methods 0.000 claims 3
- 201000011374 Alagille syndrome Diseases 0.000 claims 2
- 208000010061 Autosomal Dominant Polycystic Kidney Diseases 0.000 claims 2
- 208000002814 Autosomal Recessive Polycystic Kidney Diseases 0.000 claims 2
- 208000017354 Autosomal recessive polycystic kidney disease Diseases 0.000 claims 2
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 2
- 208000031229 Cardiomyopathies Diseases 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 208000029448 Chylomicron retention disease Diseases 0.000 claims 2
- 206010016654 Fibrosis Diseases 0.000 claims 2
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 2
- 206010020772 Hypertension Diseases 0.000 claims 2
- 201000004408 Hypobetalipoproteinemia Diseases 0.000 claims 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 2
- 206010023126 Jaundice Diseases 0.000 claims 2
- 201000005099 Langerhans cell histiocytosis Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 206010033645 Pancreatitis Diseases 0.000 claims 2
- 208000012347 Parenteral nutrition associated liver disease Diseases 0.000 claims 2
- 208000033147 Parenteral nutrition-associated cholestasis Diseases 0.000 claims 2
- 208000003251 Pruritus Diseases 0.000 claims 2
- 230000002159 abnormal effect Effects 0.000 claims 2
- 208000022185 autosomal dominant polycystic kidney disease Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 230000007882 cirrhosis Effects 0.000 claims 2
- 230000007547 defect Effects 0.000 claims 2
- 230000007812 deficiency Effects 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 201000008220 erythropoietic protoporphyria Diseases 0.000 claims 2
- 201000000544 familial hypobetalipoproteinemia 1 Diseases 0.000 claims 2
- 230000004129 fatty acid metabolism Effects 0.000 claims 2
- 208000001130 gallstones Diseases 0.000 claims 2
- 230000002440 hepatic effect Effects 0.000 claims 2
- 208000006454 hepatitis Diseases 0.000 claims 2
- 231100000283 hepatitis Toxicity 0.000 claims 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 2
- 208000001024 intrahepatic cholestasis Diseases 0.000 claims 2
- 230000007872 intrahepatic cholestasis Effects 0.000 claims 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 2
- 208000030761 polycystic kidney disease Diseases 0.000 claims 2
- 230000035935 pregnancy Effects 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 208000010157 sclerosing cholangitis Diseases 0.000 claims 2
- 210000002966 serum Anatomy 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 206010067092 AIDS cholangiopathy Diseases 0.000 claims 1
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 206010002388 Angina unstable Diseases 0.000 claims 1
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010003658 Atrial Fibrillation Diseases 0.000 claims 1
- 206010003827 Autoimmune hepatitis Diseases 0.000 claims 1
- 208000023514 Barrett esophagus Diseases 0.000 claims 1
- 208000023665 Barrett oesophagus Diseases 0.000 claims 1
- 208000019256 Benign recurrent intrahepatic cholestasis type 2 Diseases 0.000 claims 1
- 206010004593 Bile duct cancer Diseases 0.000 claims 1
- 206010051341 Bile duct stenosis Diseases 0.000 claims 1
- 206010004637 Bile duct stone Diseases 0.000 claims 1
- 102100028282 Bile salt export pump Human genes 0.000 claims 1
- 208000015163 Biliary Tract disease Diseases 0.000 claims 1
- 208000002177 Cataract Diseases 0.000 claims 1
- 206010053684 Cerebrohepatorenal syndrome Diseases 0.000 claims 1
- 206010008609 Cholangitis sclerosing Diseases 0.000 claims 1
- 201000009331 Choledocholithiasis Diseases 0.000 claims 1
- 208000032170 Congenital Abnormalities Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 208000008960 Diabetic foot Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- 208000004930 Fatty Liver Diseases 0.000 claims 1
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 1
- 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
- 108010010234 HDL Lipoproteins Proteins 0.000 claims 1
- 102000015779 HDL Lipoproteins Human genes 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 208000027761 Hepatic autoimmune disease Diseases 0.000 claims 1
- 208000005176 Hepatitis C Diseases 0.000 claims 1
- 206010019728 Hepatitis alcoholic Diseases 0.000 claims 1
- 206010019799 Hepatitis viral Diseases 0.000 claims 1
- 101000724352 Homo sapiens Bile salt export pump Proteins 0.000 claims 1
- 101000955481 Homo sapiens Phosphatidylcholine translocator ABCB4 Proteins 0.000 claims 1
- 101000671676 Homo sapiens U3 small nucleolar RNA-associated protein 4 homolog Proteins 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 206010020915 Hypervitaminosis Diseases 0.000 claims 1
- 108060003951 Immunoglobulin Proteins 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 206010065973 Iron Overload Diseases 0.000 claims 1
- 101150072399 LSC1 gene Proteins 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 208000015924 Lithiasis Diseases 0.000 claims 1
- 206010025282 Lymphoedema Diseases 0.000 claims 1
- 206010054805 Macroangiopathy Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010028289 Muscle atrophy Diseases 0.000 claims 1
- 206010051606 Necrotising colitis Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010030216 Oesophagitis Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 102100039032 Phosphatidylcholine translocator ABCB4 Human genes 0.000 claims 1
- 206010063985 Phytosterolaemia Diseases 0.000 claims 1
- 235000017284 Pometia pinnata Nutrition 0.000 claims 1
- 240000007653 Pometia tomentosa Species 0.000 claims 1
- 206010057969 Reflux gastritis Diseases 0.000 claims 1
- 208000001647 Renal Insufficiency Diseases 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 208000002227 Sitosterolemia Diseases 0.000 claims 1
- 208000007718 Stable Angina Diseases 0.000 claims 1
- 102100036325 Sterol 26-hydroxylase, mitochondrial Human genes 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 1
- 206010042953 Systemic sclerosis Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 102100040072 U3 small nucleolar RNA-associated protein 4 homolog Human genes 0.000 claims 1
- 208000007814 Unstable Angina Diseases 0.000 claims 1
- 201000004525 Zellweger Syndrome Diseases 0.000 claims 1
- 208000036813 Zellweger spectrum disease Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 230000005856 abnormality Effects 0.000 claims 1
- 208000002353 alcoholic hepatitis Diseases 0.000 claims 1
- 208000006682 alpha 1-Antitrypsin Deficiency Diseases 0.000 claims 1
- 206010002022 amyloidosis Diseases 0.000 claims 1
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 1
- 210000001367 artery Anatomy 0.000 claims 1
- 230000003190 augmentative effect Effects 0.000 claims 1
- 201000001490 benign recurrent intrahepatic cholestasis 1 Diseases 0.000 claims 1
- 201000001488 benign recurrent intrahepatic cholestasis 2 Diseases 0.000 claims 1
- 208000026586 benign recurrent intrahepatic cholestasis type 1 Diseases 0.000 claims 1
- 208000026900 bile duct neoplasm Diseases 0.000 claims 1
- 208000006766 bile reflux Diseases 0.000 claims 1
- 210000003445 biliary tract Anatomy 0.000 claims 1
- 230000036765 blood level Effects 0.000 claims 1
- 210000001185 bone marrow Anatomy 0.000 claims 1
- 230000000747 cardiac effect Effects 0.000 claims 1
- 208000001088 cerebrotendinous xanthomatosis Diseases 0.000 claims 1
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 1
- 208000003167 cholangitis Diseases 0.000 claims 1
- 208000020832 chronic kidney disease Diseases 0.000 claims 1
- 239000003246 corticosteroid Substances 0.000 claims 1
- 230000006378 damage Effects 0.000 claims 1
- 230000003111 delayed effect Effects 0.000 claims 1
- 235000014113 dietary fatty acids Nutrition 0.000 claims 1
- 201000008865 drug-induced hepatitis Diseases 0.000 claims 1
- 208000006881 esophagitis Diseases 0.000 claims 1
- 208000009866 extrahepatic cholestasis Diseases 0.000 claims 1
- 229930195729 fatty acid Natural products 0.000 claims 1
- 239000000194 fatty acid Substances 0.000 claims 1
- 150000004665 fatty acids Chemical class 0.000 claims 1
- 208000010706 fatty liver disease Diseases 0.000 claims 1
- 230000001434 glomerular Effects 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- 230000014101 glucose homeostasis Effects 0.000 claims 1
- 208000005252 hepatitis A Diseases 0.000 claims 1
- 208000002672 hepatitis B Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 1
- 201000008980 hyperinsulinism Diseases 0.000 claims 1
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 1
- 206010021198 ichthyosis Diseases 0.000 claims 1
- 102000018358 immunoglobulin Human genes 0.000 claims 1
- 208000016245 inborn errors of metabolism Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 208000015978 inherited metabolic disease Diseases 0.000 claims 1
- 201000004332 intermediate coronary syndrome Diseases 0.000 claims 1
- 210000003228 intrahepatic bile duct Anatomy 0.000 claims 1
- 201000002161 intrahepatic cholestasis of pregnancy Diseases 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 201000006370 kidney failure Diseases 0.000 claims 1
- 230000003902 lesion Effects 0.000 claims 1
- 208000002502 lymphedema Diseases 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 230000004060 metabolic process Effects 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 201000000585 muscular atrophy Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 208000004995 necrotizing enterocolitis Diseases 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 208000002865 osteopetrosis Diseases 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 201000006195 perinatal necrotizing enterocolitis Diseases 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 208000007232 portal hypertension Diseases 0.000 claims 1
- 208000000876 primary bile acid malabsorption Diseases 0.000 claims 1
- 230000000750 progressive effect Effects 0.000 claims 1
- 238000010992 reflux Methods 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 230000033764 rhythmic process Effects 0.000 claims 1
- 201000000306 sarcoidosis Diseases 0.000 claims 1
- 230000001568 sexual effect Effects 0.000 claims 1
- 210000002027 skeletal muscle Anatomy 0.000 claims 1
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
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- 210000001519 tissue Anatomy 0.000 claims 1
- 231100000419 toxicity Toxicity 0.000 claims 1
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- 230000002792 vascular Effects 0.000 claims 1
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Claims (8)
- 式(I)の化合物
又は医薬として許容されるその塩:
- (Z)-3-((3,3-ジブチル-5-(4-フルオロフェニル)-7-(メチルチオ)-1,1-ジオキシド-2,3,4,5-テトラヒドロ-1,5-ベンゾチアゼピン-8-イル)オキシ)-2-フルオロアクリル酸;
(Z)-3-((3-ブチル-7-(ジメチルアミノ)-3-エチル-1,1-ジオキシド-5-フェニル-2,3,4,5-テトラヒドロ-1,2,5-ベンゾチアジアゼピン-8-イル)オキシ)-2-フルオロアクリル酸;
(S)-(Z)-3-((3-ブチル-7-(ジメチルアミノ)-3-エチル-1,1-ジオキシド-5-フェニル-2,3,4,5-テトラヒドロ-1,2,5-ベンゾチアジアゼピン-8-イル)オキシ)-2-フルオロアクリル酸;
(R)-(Z)-3-((3-ブチル-7-(ジメチルアミノ)-3-エチル-1,1-ジオキシド-5-フェニル-2,3,4,5-テトラヒドロ-1,2,5-ベンゾチアジアゼピン-8-イル)オキシ)-2-フルオロアクリル酸;
(Z)-3-((3-ブチル-3-エチル-5-(4-フルオロフェニル)-7-(メチルチオ)-1,1-ジオキシド-2,3,4,5-テトラヒドロ-1,5-ベンゾチアゼピン-8-イル)オキシ)-2-フルオロアクリル酸;
(S)-(Z)-3-((3-ブチル-3-エチル-5-(4-フルオロフェニル)-7-(メチルチオ)-1,1-ジオキシド-2,3,4,5-テトラヒドロ-1,5-ベンゾチアゼピン-8-イル)オキシ)-2-フルオロアクリル酸;
(R)-(Z)-3-((3-ブチル-3-エチル-5-(4-フルオロフェニル)-7-(メチルチオ)-1,1-ジオキシド-2,3,4,5-テトラヒドロ-1,5-ベンゾチアゼピン-8-イル)オキシ)-2-フルオロアクリル酸;
(E)-3-((3-ブチル-3-エチル-5-(4-フルオロフェニル)-7-(メチルチオ)-1,1-ジオキシド-2,3,4,5-テトラヒドロ-1,5-ベンゾチアゼピン-8-イル)オキシ)アクリル酸;
(S)-(E)-3-((3-ブチル-3-エチル-5-(4-フルオロフェニル)-7-(メチルチオ)-1,1-ジオキシド-2,3,4,5-テトラヒドロ-1,5-ベンゾチアゼピン-8-イル)オキシ)アクリル酸;
(R)-(E)-3-((3-ブチル-3-エチル-5-(4-フルオロフェニル)-7-(メチルチオ)-1,1-ジオキシド-2,3,4,5テトラヒドロ-1,5-ベンゾチアゼピン-8-イル)オキシ)アクリル酸;
(E)-3-((3-エチル-7-(メチルチオ)-1,1-ジオキシド-5-フェニル-3-プロピル-2,3,4,5-テトラヒドロ-1,5-ベンゾチアゼピン-8-イル)オキシ)アクリル酸;
(Z)-3-((3-エチル-7-(メチルチオ)-1,1-ジオキシド-5-フェニル-3-プロピル-2,3,4,5-テトラヒドロベンゾ-1,5-チアゼピン-8-イル)オキシ)-2-フルオロアクリル酸;
(S)-(Z)-3-((3-エチル-7-(メチルチオ)-1,1-ジオキシド-5-フェニル-3-プロピル-2,3,4,5-テトラヒドロ-1,5-ベンゾチアゼピン-8-イル)オキシ)-2-フルオロアクリル酸;
(R)-(Z)-3-((3-エチル-7-(メチルチオ)-1,1-ジオキシド-5-フェニル-3-プロピル-2,3,4,5-テトラヒドロ-1,5-ベンゾチアゼピン-8-イル)オキシ)-2-フルオロアクリル酸;
(E)-3-((3-ブチル-7-(ジメチルアミノ)-3-エチル-1,1-ジオキシド-5-フェニル-2,3,4,5-テトラヒドロ-1,2,5-ベンゾチアジアゼピン-8-イル)オキシ)アクリル酸;
(S)-(E)-3-((3-ブチル-7-(ジメチルアミノ)-3-エチル-1,1-ジオキシド-5-フェニル-2,3,4,5-テトラヒドロ-1,2,5-ベンゾチアジアゼピン-8-イル)オキシ)アクリル酸;
(R)-(E)-3-((3-ブチル-7-(ジメチルアミノ)-3-エチル-1,1-ジオキシド-5-フェニル-2,3,4,5-テトラヒドロ-1,2,5-ベンゾチアジアゼピン-8-イル)オキシ)アクリル酸;
(E)-3-((3-エチル-3-イソプロピル-7-(メチルチオ)-1,1-ジオキシド-5-フェニル-2,3,4,5-テトラヒドロ-1,5-ベンゾチアゼピン-8-イル)オキシ)アクリル酸;及び
(Z)-3-((3-エチル-3-イソプロピル-7-(メチルチオ)-1,1-ジオキシド-5-フェニル-2,3,4,5-テトラヒドロ-1,5-ベンゾチアゼピン-8-イル)オキシ)-2-フルオロアクリル酸;
からなる群から選択される、請求項1に記載の化合物又は医薬として許容されるその塩。 - 治療的有効量の請求項1又は2に記載の化合物と、1つ又は複数の医薬として許容される賦形剤とを含む医薬組成物。
- 請求項1又は2に記載の化合物を含む医薬。
- 循環器疾患又は脂肪酸代謝の障害又はグルコース利用障害、例えば、高コレステロール血症;脂肪酸代謝の障害;1型及び2型真性糖尿病;糖尿病の合併症、例えば、白内障、細小及び大血管疾患、網膜症、神経障害、腎症、及び創傷治癒の遅延、組織虚血、糖尿病性足病変、動脈硬化症、心筋梗塞、急性冠症候群、不安定狭心症、安定狭心症、脳卒中、末梢動脈閉塞性疾患、心筋症、心不全、心拍障害、及び血管再狭窄;糖尿病関連疾患、例えば、インスリン抵抗性(グルコース恒常性の障害)、高血糖、高インスリン血症、脂肪酸又はグリセロールの血中レベルの上昇、肥満、脂質異常症、高脂血症、例えば、高トリグリセリド血症、メタボリック症候群(X症候群)、アテローム性動脈硬化症、及び高血圧;並びに高密度リポタンパク質レベルの増加の治療又は予防における使用のための、請求項4に記載の医薬。
- 胃腸疾患又は障害、例えば、便秘(慢性便秘、機能性便秘、慢性特発性便秘(CIC)、断続的/散発性便秘、真性糖尿病に続発する便秘、脳卒中に続発する便秘、慢性腎臓病に続発する便秘、多発性硬化症に続発する便秘、パーキンソン病に続発する便秘、全身性硬化症に続発する便秘、薬物性便秘、便秘型過敏性腸症候群(IBS-C)、混合型過敏性腸症候群(IBS-M)、小児機能性便秘、及びオピオイド誘発性便秘が含まれる);クローン病;一次胆汁酸吸収不良;過敏性腸症候群(IBS);炎症性腸疾患(IBD);回腸の炎症;並びに逆流症及びその合併症、例えば、バレット食道、胆汁逆流食道炎、及び胆汁逆流胃炎の治療又は予防における使用のための、請求項4に記載の医薬。
- 肝疾患若しくは障害、例えば、肝臓の遺伝性代謝障害;胆汁酸合成の先天性異常;先天性胆管走行異常;胆道閉鎖;葛西手術後の胆道閉鎖;肝臓移植後の胆道閉鎖;新生児肝炎;新生児胆汁うっ滞;遺伝形式の胆汁うっ滞;脳腱黄色腫症;BA合成の二次的欠陥;ツェルウェガー症候群;嚢胞性線維症に関連する肝疾患;α1アンチトリプシン欠損症;アラジール症候群(ALGS);バイラー症候群;胆汁酸(BA)合成の一次的欠陥;進行性家族性肝内胆汁うっ滞(PFIC)、例えば、PFIC-1、PFIC-2、PFIC-3、及び非特定PFIC、胆汁分流後のPFIC、並びに肝臓移植後のPFIC;良性反復性肝内胆汁うっ滞(BRIC)、例えば、BRIC1、BRIC2、及び非特定BRIC、胆汁分流後のBRIC、並びに肝臓移植後のBRIC;自己免疫性肝炎;原発性胆汁性肝硬変(PBC);肝線維症;非アルコール性脂肪性肝疾患(NAFLD);非アルコール性脂肪性肝炎(NASH);門脈圧亢進症;胆汁うっ滞;ダウン症候群の胆汁うっ滞;薬物性胆汁うっ滞;妊娠の肝内胆汁うっ滞(妊娠中の黄疸);肝内胆汁うっ滞;肝外胆汁うっ滞;経静脈栄養に関連する胆汁うっ滞(PNAC);低リン脂質に関連する胆汁うっ滞;リンパ浮腫胆汁うっ滞症候群1(LSC1);原発性硬化性胆管炎(PSC);免疫グロブリンG4に関連する胆管炎;原発性胆汁性胆管炎;胆石症(胆石);胆道結石症(biliary lithiasis);総胆管結石症;胆石性膵炎;カロリー病;胆管の悪性腫瘍;胆樹の閉塞を引き起こす悪性腫瘍;胆管狭窄;AIDS胆管症;虚血性胆管症;胆汁うっ滞若しくは黄疸によるそう痒;膵臓炎;進行性胆汁うっ滞に至る慢性自己免疫性肝疾患;肝脂肪変性;アルコール性肝炎;急性脂肪肝;妊娠の脂肪肝;薬物性肝炎;鉄過剰症;先天性胆汁酸代謝異常症1型(BAS1型);薬物性肝障害(DILI);肝線維症;先天性肝線維症;肝硬変;ランゲルハンス細胞組織球症(LCH);新生児魚鱗癬硬化性胆管炎(NISCH);骨髄性プロトポルフィリン症(EPP);特発性成人胆管減少(IAD);突発性新生児肝炎(INH);非症候性肝内胆管減少症(NS PILBD);常染色体劣性遺伝性肝内胆汁うっ滞(North American Indian childhood cirrhosis)(NAIC);肝サルコイドーシス;アミロイドーシス;壊死性腸炎;血清中胆汁酸が引き起こす毒性、例えば、異常な血清中胆汁酸プロファイルの状況での心律動障害(例えば、心房細動)、肝硬変に関連する心筋症(「コレカルディア(cholecardia)」)、及び胆汁うっ滞性肝疾患に関連する骨格筋消耗;多発性肝嚢胞性疾患;ウイルス性肝炎(A型肝炎、B型肝炎、C型肝炎、D型肝炎、及びE型肝炎が含まれる);肝細胞癌(肝細胞腫);胆管癌;胆汁酸に関係する胃腸癌;並びに肝臓、胆道、及び膵臓の腫瘍及び新生物によって引き起こされる胆汁うっ滞の治療若しくは予防における使用のための;又は肝疾患におけるコルチコステロイド療法の増強における使用のための、請求項4に記載の医薬。
- 過吸収症候群(無βリポタンパク血症、家族性低βリポタンパク血症(FHBL)、カイロミクロン停滞病(CRD)、及びシトステロール血症が含まれる);ビタミン過剰症及び大理石骨病;高血圧;糸球体過剰濾過;多発性嚢胞腎(PKD)、例えば、常染色体優性多発性嚢胞腎(ADPKD)及び常染色体劣性多発性嚢胞腎(ARPKD);並びに腎不全のそう痒の治療若しくは予防における使用のための;又は肝臓若しくは代謝疾患に関連する腎臓傷害に対する保護における使用のための、請求項4に記載の医薬。
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Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE030062T2 (en) | 2010-11-08 | 2017-04-28 | Albireo Ab | IBAT inhibitors for the treatment of liver diseases |
| KR20220082931A (ko) | 2014-06-25 | 2022-06-17 | 이에이 파마 가부시키가이샤 | 고형 제제 및 그의 착색 방지 또는 착색 감소 방법 |
| WO2019234077A1 (en) | 2018-06-05 | 2019-12-12 | Albireo Ab | Benzothia(di)azepine compounds and their use as bile acid modulators |
| PE20210182A1 (es) | 2018-06-20 | 2021-01-29 | Albireo Ab | Modificaciones de cristales de odexibat |
| US11801226B2 (en) | 2018-06-20 | 2023-10-31 | Albireo Ab | Pharmaceutical formulation of odevixibat |
| US10975045B2 (en) | 2019-02-06 | 2021-04-13 | Aibireo AB | Benzothiazepine compounds and their use as bile acid modulators |
| US10941127B2 (en) | 2019-02-06 | 2021-03-09 | Albireo Ab | Benzothiadiazepine compounds and their use as bile acid modulators |
| CN114761080A (zh) | 2019-12-04 | 2022-07-15 | 阿尔比里奥公司 | 苯并硫杂(二)氮杂环庚三烯化合物及其作为胆汁酸调节剂的用途 |
| CN114761018A (zh) | 2019-12-04 | 2022-07-15 | 阿尔比里奥公司 | 苯并硫杂二氮杂环庚三烯化合物及其作为胆汁酸调节剂的用途 |
| EP4069359B1 (en) * | 2019-12-04 | 2024-01-03 | Albireo AB | Benzothia(di)azepine compounds and their use as bile acid modulators |
| KR20220109450A (ko) | 2019-12-04 | 2022-08-04 | 알비레오 에이비 | 벤조티아(디)아제핀 화합물 및 담즙산 조절제로서의 이의 용도 |
| JP2023537285A (ja) | 2020-08-03 | 2023-08-31 | アルビレオ・アクチボラグ | ベンゾチア（ジ）アゼピン化合物及び胆汁酸モジュレータとしてのそれらの使用 |
| JP2023549226A (ja) | 2020-11-12 | 2023-11-22 | アルビレオ エービー | 進行性家族性肝内胆汁うっ滞症（ｐｆｉｃ）を処置するためのオデビキシバット |
| BR112023010799A2 (pt) | 2020-12-04 | 2023-10-03 | Albireo Ab | Compostos de benzotia(di)azepina e seus usos como moduladores de ácidos biliares |
Family Cites Families (162)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3539380A (en) | 1968-01-08 | 1970-11-10 | Upjohn Co | Methylcellulose and polyalkylene glycol coating of solid medicinal dosage forms |
| GB1573487A (en) | 1977-05-23 | 1980-08-28 | Bristol Myers Co | Bile acid binding composition |
| EP0049500B1 (de) | 1979-04-30 | 1984-02-22 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Tyrosinderivate, Verfahren zu ihrer Herstellung und ihre Verwendung bei der Synthese von Peptiden |
| CA1313135C (en) | 1987-02-09 | 1993-01-26 | The Dow Chemical Company | Cholestyramine composition and process for its preparation |
| US5167965A (en) | 1987-02-09 | 1992-12-01 | The Dow Chemical Company | Palatable cholestyramine granules, tablets and methods for preparation thereof |
| US4900757A (en) | 1988-12-08 | 1990-02-13 | Merrell Dow Pharmaceuticals Inc. | Hypocholesterolemic and antiatherosclerotic uses of bix(3,5-di-tertiary-butyl-4-hydroxyphenylthio)methane |
| JP2800242B2 (ja) | 1989-03-30 | 1998-09-21 | 大正製薬株式会社 | 粒剤の製造方法 |
| DE3930168A1 (de) | 1989-09-09 | 1991-03-14 | Knoll Ag | Verbesserte verabreichungsform fuer colestyramin |
| IL95574A (en) | 1989-09-09 | 1994-11-11 | Knoll Ag | Colstiramine preparation |
| JP2542122B2 (ja) | 1990-04-18 | 1996-10-09 | 旭化成工業株式会社 | 球状核、球形顆粒およびその製造方法 |
| DE59108326D1 (de) | 1990-12-06 | 1996-12-12 | Hoechst Ag | Gallensäurederivate, Verfahren zu ihrer Herstellung und Verwendung dieser Verbindung als Arzneimittel |
| FI108451B (fi) | 1991-12-20 | 2002-01-31 | Hoechst Ag | Menetelmõ polymeeristen ja oligomeeristen sappihappojohdannaisten valmistamiseksi |
| JPH05186357A (ja) | 1991-12-31 | 1993-07-27 | Shigeo Ochi | 飲食物消化分解産物吸収抑制手段 |
| GB9203347D0 (en) | 1992-02-17 | 1992-04-01 | Wellcome Found | Hypolipidaemic compounds |
| DK0573848T3 (da) | 1992-06-12 | 1998-08-10 | Hoechst Ag | Galdesyrederivater, fremgangsmåde til deres fremstilling og anvendelse af disse forbindelser som lægemidler |
| US5350584A (en) | 1992-06-26 | 1994-09-27 | Merck & Co., Inc. | Spheronization process using charged resins |
| IL108633A (en) | 1993-02-15 | 1998-07-15 | Wellcome Found | History of Benzothiazepine Hypolipidemic Preparation and Pharmaceutical Preparations Containing Them |
| IL108634A0 (en) | 1993-02-15 | 1994-05-30 | Wellcome Found | Hypolipidaemic heterocyclic compounds, their prepatation and pharmaceutical compositions containing them |
| TW289020B (ja) | 1993-05-08 | 1996-10-21 | Hoechst Sktiengesellschaft | |
| EP0624593A3 (de) | 1993-05-08 | 1995-06-07 | Hoechst Ag | Gallensäurederivate, Verfahren zu ihrer Herstellung und Verwendung dieser Verbindungen als Arzneimittel. |
| TW289757B (ja) | 1993-05-08 | 1996-11-01 | Hoechst Ag | |
| TW289021B (ja) | 1993-05-08 | 1996-10-21 | Hoechst Ag | |
| ZA956647B (en) | 1994-08-10 | 1997-02-10 | Wellcome Found | Hypolipidaemic compounds. |
| AU700557B2 (en) | 1994-09-13 | 1999-01-07 | Monsanto Company | Novel benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake |
| US6262277B1 (en) | 1994-09-13 | 2001-07-17 | G.D. Searle And Company | Intermediates and processes for the preparation of benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake |
| US5994391A (en) | 1994-09-13 | 1999-11-30 | G.D. Searle And Company | Benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake |
| US6642268B2 (en) | 1994-09-13 | 2003-11-04 | G.D. Searle & Co. | Combination therapy employing ileal bile acid transport inhibiting benzothipines and HMG Co-A reductase inhibitors |
| GB9423172D0 (en) * | 1994-11-17 | 1995-01-04 | Wellcom Foundation The Limited | Hypolipidemic benzothiazepines |
| US5811388A (en) | 1995-06-07 | 1998-09-22 | Cibus Pharmaceutical, Inc. | Delivery of drugs to the lower GI tract |
| CA2242991C (en) | 1996-01-16 | 2007-07-24 | University Technology Corporation | Use of antioxidant agents to treat cholestatic liver disease |
| DE19608592A1 (de) | 1996-03-06 | 1997-09-11 | Hoechst Ag | Antikörper zur selektiven immunologischen Bestimmung von Gallensäuren in biologischen Matrices |
| CN1110494C (zh) | 1996-03-11 | 2003-06-04 | G·D·瑟尔公司 | 具有作为回肠胆汁酸转运和牛磺胆酸盐吸收抑制剂活性的新的苯并噻庚因 |
| JP2000510858A (ja) | 1996-05-23 | 2000-08-22 | ノバルティス アクチエンゲゼルシャフト | ６―フルオロウルソデオキシコール酸（６―ｆｕｄｃａ）による結腸直腸癌の予防および治療 |
| ATE197842T1 (de) | 1996-07-24 | 2000-12-15 | Zumtobel Staff Gmbh | Adapter für ein haltemittel, welches zum befestigen einer einbauleuchte in einer einbauöffnung bestimmt ist, oder haltemittel oder einbauleuchte mit einem solchen adapter |
| DE19633268A1 (de) | 1996-08-19 | 1998-02-26 | Hoechst Ag | Polymere Gallensäure-Resorptionsinhibitoren mit gleichzeitiger Gallensäure-Adsorberwirkung |
| GB9704208D0 (en) | 1997-02-28 | 1997-04-16 | Glaxo Group Ltd | Chemical compounds |
| NZ337830A (en) | 1997-03-11 | 2001-07-27 | G | Combination therapy employing ileal bile acid transport inhibiting benzothiepines and HMG Co-A reductase inhibitors |
| EP0864582B1 (en) | 1997-03-14 | 2003-06-04 | Aventis Pharma Deutschland GmbH | Hypolipidemic 1,4-benzothiazepine-1,-dioxides |
| EP0998271B3 (en) | 1997-06-06 | 2014-10-29 | Depomed, Inc. | Gastric-retentive oral drug dosage forms for controlled release of highly soluble drugs |
| US6635280B2 (en) | 1997-06-06 | 2003-10-21 | Depomed, Inc. | Extending the duration of drug release within the stomach during the fed mode |
| AU7552198A (en) | 1997-06-11 | 1998-12-30 | Sankyo Company Limited | Benzylamine derivatives |
| AUPO763197A0 (en) | 1997-06-30 | 1997-07-24 | Sigma Pharmaceuticals Pty Ltd | Health supplement |
| US5900233A (en) | 1997-10-16 | 1999-05-04 | Day; Charles E. | Epichlorohydrin and 1-(3-aminopropyl) imidazole copolymer and its use in treating irritable bowel syndrome |
| US20030153541A1 (en) | 1997-10-31 | 2003-08-14 | Robert Dudley | Novel anticholesterol compositions and method for using same |
| WO1999032478A1 (en) | 1997-12-19 | 1999-07-01 | G.D. Searle & Co. | Method of preparing enantiomerically-enriched tetrahydrobenzothiepine oxides |
| GB9800428D0 (en) * | 1998-01-10 | 1998-03-04 | Glaxo Group Ltd | Chemical compounds |
| WO1999055690A1 (en) | 1998-04-24 | 1999-11-04 | Fujisawa Pharmaceutical Co., Ltd. | Guanidine derivatives |
| DE19825804C2 (de) | 1998-06-10 | 2000-08-24 | Aventis Pharma Gmbh | 1,4-Benzothiepin-1,1-dioxidderivate, Verfahren zu deren Herstellung und diese Verbindungen enthaltende Arzneimittel |
| US6221897B1 (en) | 1998-06-10 | 2001-04-24 | Aventis Pharma Deutschland Gmbh | Benzothiepine 1,1-dioxide derivatives, a process for their preparation, pharmaceuticals comprising these compounds, and their use |
| EP1103552A4 (en) | 1998-08-07 | 2003-01-15 | Takeda Chemical Industries Ltd | BENZOTHIEPINE DERIVATIVES, METHOD FOR THEIR PRODUCTION AND THEIR USE |
| CN1338945A (zh) | 1998-12-23 | 2002-03-06 | G·D·瑟尔有限公司 | 适用于心血管疾病的回肠胆汁酸转运抑制剂和胆汁酸螯合剂组合 |
| CZ20012342A3 (cs) | 1998-12-23 | 2001-12-12 | G. D. Searle Llc | Kombinace inhibitorů transportu ľlučové kyseliny v ileu a derivátů kyseliny fibrové pro kardiovaskulární indikace |
| HUP0201972A3 (en) | 1998-12-23 | 2005-06-28 | G D Searle Llc Chicago | Combinations of ileal bile acid transport inhibitors and cholesteryl ester transfer protein inhibitors for cardiovascular indications |
| NZ512532A (en) | 1998-12-23 | 2003-12-19 | G | Combinations for treating cardiovascular diseases like hypercholesterolemia and atherosclerosis |
| AU776952B2 (en) | 1998-12-23 | 2004-09-30 | G.D. Searle Llc | Combinations of ileal bile acid transport inhibitors and nicotinic acid derivatives for cardiovascular indications |
| HUP0105409A3 (en) | 1999-02-12 | 2004-11-29 | G D Searle Llc Chicago | 1,2-benzothiazepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake, use thereof and pharmaceutical compositions containing them |
| DE19916108C1 (de) | 1999-04-09 | 2001-01-11 | Aventis Pharma Gmbh | Mit Zuckerresten substituierte 1,4-Benzothiazepin-1,1-dioxidderivate, Verfahren zu deren Herstellung und deren Verwendung |
| SE9901387D0 (sv) | 1999-04-19 | 1999-04-19 | Astra Ab | New pharmaceutical foromaulations |
| US6287609B1 (en) | 1999-06-09 | 2001-09-11 | Wisconsin Alumni Research Foundation | Unfermented gel fraction from psyllium seed husks |
| WO2001034570A1 (fr) | 1999-11-08 | 2001-05-17 | Sankyo Company, Limited | Derives heterocycliques azotes |
| GB9927088D0 (en) | 1999-11-17 | 2000-01-12 | Secr Defence | Use of poly(diallylamine) polymers |
| WO2001060807A1 (en) | 2000-02-18 | 2001-08-23 | Merck & Co. Inc. | Aryloxyacetic acids for diabetes and lipid disorders |
| SE0000772D0 (sv) | 2000-03-08 | 2000-03-08 | Astrazeneca Ab | Chemical compounds |
| JP2003528830A (ja) | 2000-03-10 | 2003-09-30 | ファルマシア・コーポレーション | テトラヒドロベンゾチエピン類の製造方法 |
| WO2001068096A2 (en) | 2000-03-10 | 2001-09-20 | Pharmacia Corporation | Combination therapy for the prophylaxis and treatment of hyperlipidemic conditions and disorders |
| US6638498B2 (en) | 2000-06-30 | 2003-10-28 | Semorex Inc. | Molecularly imprinted polymers for the treatment and diagnosis of medical conditions |
| US20020183307A1 (en) | 2000-07-26 | 2002-12-05 | Tremont Samuel J. | Novel 1,4-benzothiazephine and 1,5-benzothiazepine compounds as inhibitors of apical sodium co-dependent bile acid transport and taurocholate uptake |
| FR2812886B1 (fr) | 2000-08-08 | 2002-11-08 | Assist Publ Hopitaux De Paris | Depistage d'un nouveau syndrome hepatique et ses applications |
| SE0003766D0 (sv) | 2000-10-18 | 2000-10-18 | Astrazeneca Ab | Novel formulation |
| EG26979A (en) | 2000-12-21 | 2015-03-01 | Astrazeneca Ab | Chemical compounds |
| WO2002053548A1 (en) | 2000-12-27 | 2002-07-11 | Banyu Pharmaceutical Co.,Ltd. | Benzothiazepine derivatives |
| US6506921B1 (en) | 2001-06-29 | 2003-01-14 | Virginia Tech Intellectual Properties, Inc. | Amine compounds and curable compositions derived therefrom |
| US20040077625A1 (en) * | 2001-07-25 | 2004-04-22 | Tremont Samuel J. | Novel 1,4-benzothiazepine and 1,5-benzothiazepine compounds as inhibitors of apical sodium codependent bile acid transport abd taurocholate uptake |
| US20040038862A1 (en) | 2001-07-30 | 2004-02-26 | Goodwin Bryan James | Identification of new therapeutic targets for modulating bile acid synthesis |
| GB0121337D0 (en) | 2001-09-04 | 2001-10-24 | Astrazeneca Ab | Chemical compounds |
| GB0121621D0 (en) | 2001-09-07 | 2001-10-31 | Astrazeneca Ab | Chemical compounds |
| GB0121622D0 (en) | 2001-09-07 | 2001-10-31 | Astrazeneca Ab | Chemical compounds |
| ATE349214T1 (de) | 2001-09-08 | 2007-01-15 | Astrazeneca Ab | Benzothiazepin und benzothiadiazepin derivative mit hemmender wirkung auf den säuretransport in den gallengängen zur behandlung von hyperlipidaemia |
| BR0212495A (pt) | 2001-09-12 | 2004-08-24 | Searle Llc | Método para a preparação de tetraidrobenzotiepinas cristalinas |
| WO2003040127A1 (en) | 2001-11-02 | 2003-05-15 | G.D. Searle Llc | Novel mono- and di-fluorinated benzothiepine compounds as inhibitors of apical sodium co-dependent bile acid transport (asbt) and taurocholate uptake |
| TW200300349A (en) | 2001-11-19 | 2003-06-01 | Sankyo Co | A 4-oxoqinoline derivative |
| GB0314079D0 (en) | 2003-06-18 | 2003-07-23 | Astrazeneca Ab | Therapeutic agents |
| GB0229931D0 (en) | 2002-12-21 | 2003-01-29 | Astrazeneca Ab | Therapeutic agents |
| SE0104334D0 (sv) | 2001-12-19 | 2001-12-19 | Astrazeneca Ab | Therapeutic agents |
| JP2005518408A (ja) | 2001-12-29 | 2005-06-23 | ノボ ノルディスク アクティーゼルスカブ | 異常脂肪血症を治療するための、ｇｌｐ−１化合物と他の薬物との組み合わせ使用 |
| GB0201850D0 (en) | 2002-01-26 | 2002-03-13 | Astrazeneca Ab | Therapeutic treatment |
| US20040014806A1 (en) | 2002-03-08 | 2004-01-22 | Pharmacia Corporation | Methods and compositions for lowering levels of blood lipids |
| GB0209467D0 (en) | 2002-04-25 | 2002-06-05 | Astrazeneca Ab | Chemical compounds |
| GB0213669D0 (en) | 2002-06-14 | 2002-07-24 | Astrazeneca Ab | Chemical compounds |
| GB0216321D0 (en) | 2002-07-13 | 2002-08-21 | Astrazeneca Ab | Therapeutic treatment |
| US7312208B2 (en) | 2002-08-28 | 2007-12-25 | Asahi Kasei Pharma Corporation | Quaternary ammonium compounds |
| ATE531701T1 (de) | 2002-08-28 | 2011-11-15 | Asahi Kasei Pharma Corp | Neue quaternüre ammoniumverbindungen |
| GB0304194D0 (en) | 2003-02-25 | 2003-03-26 | Astrazeneca Ab | Chemical compounds |
| CA2517245C (en) | 2003-02-28 | 2009-01-20 | Mcgill University | Cell and enzyme compositions for modulating bile acids, cholesterol and triglycerides |
| GB0307918D0 (en) | 2003-04-05 | 2003-05-14 | Astrazeneca Ab | Therapeutic use |
| CA2584188C (en) | 2003-10-16 | 2014-03-18 | Techcom Group, Llc | Reduced digestible carbohydrate food having reduced blood glucose response |
| US7973030B2 (en) | 2004-02-27 | 2011-07-05 | Asahi Kasei Pharma Corporation | Benzothiazepine and benzothiepine compounds |
| US20050197376A1 (en) | 2004-03-02 | 2005-09-08 | Fujisawa Pharmaceutical Co. Ltd. | Concomitant drugs |
| EP1593671A1 (en) | 2004-03-05 | 2005-11-09 | Graffinity Pharmaceuticals AG | DPP-IV inhibitors |
| US20050215882A1 (en) | 2004-03-23 | 2005-09-29 | The Regents Of The University Of Michigan | Noninvasive method to determine fat content of tissues using MRI |
| TWI354569B (en) | 2004-05-28 | 2011-12-21 | Bristol Myers Squibb Co | Coated tablet formulation and method |
| US20050287178A1 (en) | 2004-06-23 | 2005-12-29 | Steed Barrie L | Diagnosis and treatment of heavy gallbladder densities |
| EP1877373A2 (en) | 2005-05-05 | 2008-01-16 | Microbia, Inc. | Biphenylazetidinone cholesterol absorption inhibitors |
| DE102005033099A1 (de) | 2005-07-15 | 2007-01-18 | Sanofi-Aventis Deutschland Gmbh | Neues 1,4-Benzothiazepin-1,1-Dioxidderivat mit verbesserten Eigenschaften, Verfahren zu dessen Herstellung, diese Verbindung enthaltende Arzneimittel und dessen Verwendung |
| DE102005033100B3 (de) | 2005-07-15 | 2007-01-25 | Sanofi-Aventis Deutschland Gmbh | Neues 1,4-Benzothiazepin-1,1-Dioxidderivat mit verbesserten Eigenschaften, diese Verbindung enthaltene Arzneimittel und Verfahren zu deren Herstellung |
| US8143217B2 (en) | 2005-09-20 | 2012-03-27 | Novartis Ag | Use of DPP-IV inhibitor to reduce hypoglycemic events |
| AU2007238896A1 (en) | 2006-04-10 | 2007-10-25 | Merck Sharp & Dohme Corp. | CGRP antagonist salt |
| US8048413B2 (en) | 2006-05-17 | 2011-11-01 | Helene Huguet | Site-specific intestinal delivery of adsorbents, alone or in combination with degrading molecules |
| DE102006053635B4 (de) | 2006-11-14 | 2011-06-30 | Sanofi-Aventis Deutschland GmbH, 65929 | Neue mit Benzylresten substituierte 1,4-Benzothiepin-1,1-Dioxidderivate, diese Verbindungen enthaltende Arzneimittel und deren Verwendung |
| DE102006053637B4 (de) | 2006-11-14 | 2011-06-30 | Sanofi-Aventis Deutschland GmbH, 65929 | Neue mit Fluor substituierte 1,4-Benzothiepin-1,1-Dioxidderivate, diese Verbindungen enthaltende Arzneimittel und deren Verwendung |
| DE502007006208D1 (de) | 2006-11-14 | 2011-02-17 | Sanofi Aventis Deutschland | Neue 1,4-benzothiepin-1,1-dioxidderivate mit verbesserten eigenschaften, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
| DE102006053636B4 (de) | 2006-11-14 | 2008-09-18 | Sanofi-Aventis Deutschland Gmbh | Neue mit Cyclohexylresten substituierte 1,4-Benzothiepin-1,1-Dioxidderivate und deren Verwendung |
| JP5292310B2 (ja) | 2007-01-19 | 2013-09-18 | インターセプト ファーマシューティカルズ， インコーポレイテッド | Ｔｇｒ５調節剤としての２３−置換胆汁酸およびその使用方法 |
| AU2008223091B2 (en) | 2007-03-02 | 2014-04-24 | Farnam Companies, Inc. | Sustained release pellets comprising wax-like material |
| US9295677B2 (en) | 2008-02-26 | 2016-03-29 | Qing Bile Therapeutics Inc. | Polyhydroxylated bile acids for treatment of biliary disorders |
| RU2011112694A (ru) | 2008-09-02 | 2012-10-10 | Юсв Лимитед (In) | Сшитые полимеры |
| CA2744817C (en) | 2008-11-26 | 2020-07-07 | Satiogen Pharmaceuticals, Inc. | Bile acid recycling inhibitors for treatment of obesity and diabetes |
| US20110152204A1 (en) | 2009-12-18 | 2011-06-23 | Satiogen Pharmaceuticals, Inc. | Treatment of Obesity or Diabetes with Bile Acid Sequestrants |
| JO3131B1 (ar) | 2010-04-27 | 2017-09-20 | Glaxosmithkline Llc | مركبات كيميائية |
| WO2011150286A2 (en) | 2010-05-26 | 2011-12-01 | Satiogen Pharmaceuticals,Inc. | Bile acid recycling inhibitors and satiogens for treatment of diabetes, obesity, and inflammatory gastrointestinal conditions |
| US20120114588A1 (en) | 2010-11-08 | 2012-05-10 | Albireo Ab | Ibat inhibitors for treatment of metabolic disorders and related conditions |
| PT2637646T (pt) | 2010-11-08 | 2016-08-17 | Albireo Ab | Uma combinação farmacêutica que compreende um inibidor do ibat e um sequestrador de ácido biliar |
| CA2815941A1 (en) | 2010-11-08 | 2012-05-18 | Albireo Ab | Ibat inhibitors for treatment of metabolic disorders and related conditions |
| HUE030062T2 (en) | 2010-11-08 | 2017-04-28 | Albireo Ab | IBAT inhibitors for the treatment of liver diseases |
| AU2012328453B2 (en) | 2011-10-28 | 2017-05-04 | Shire Human Genetic Therapies, Inc. | Bile acid recycling inhibitors for treatment of hypercholemia and cholestatic liver disease |
| CN104023727B (zh) | 2011-10-28 | 2017-04-05 | 鲁美纳医药公司 | 用于治疗小儿胆汁淤积性肝病的胆汁酸再循环抑制剂 |
| KR101868991B1 (ko) | 2012-05-07 | 2018-06-19 | 깃세이 야쿠힌 고교 가부시키가이샤 | 피라졸 유도체 및 그 의약용도 |
| US20140275090A1 (en) | 2013-03-15 | 2014-09-18 | Lumena Pharmaceuticals, Inc. | Bile acid recycling inhibitors for treatment of primary sclerosing cholangitis and inflammatory bowel disease |
| JO3301B1 (ar) | 2013-04-26 | 2018-09-16 | Albireo Ab | تعديلات بلورية على إيلوبيكسيبات |
| SG11201607075TA (en) | 2014-02-27 | 2016-09-29 | Nusirt Sciences Inc | Compositions and methods for the reduction or prevention of hepatic steatosis |
| KR102296314B1 (ko) | 2014-06-25 | 2021-09-01 | 이에이 파마 가부시키가이샤 | 고형 제제 및 그의 안정화 방법 |
| KR20220082931A (ko) | 2014-06-25 | 2022-06-17 | 이에이 파마 가부시키가이샤 | 고형 제제 및 그의 착색 방지 또는 착색 감소 방법 |
| KR101674806B1 (ko) | 2014-10-20 | 2016-11-10 | 씨제이헬스케어 주식회사 | 신규한 아미노알킬벤조티아제핀 유도체 및 이의 용도 |
| EP3012252A1 (en) | 2014-10-24 | 2016-04-27 | Ferring BV | Crystal modifications of elobixibat |
| US9684018B2 (en) | 2014-11-19 | 2017-06-20 | Texas Instruments Incorporated | Current sense circuit that operates over a wide range of currents |
| KR20160061492A (ko) | 2014-11-21 | 2016-06-01 | 삼성디스플레이 주식회사 | 휴대용 먼지 센서 및 이를 이용한 휴대전화 |
| WO2017138876A1 (en) | 2016-02-09 | 2017-08-17 | Albireo Ab | Cholestyramine pellets and methods for preparation thereof |
| CA3011565C (en) | 2016-02-09 | 2024-01-02 | Albireo Ab | Oral cholestyramine formulation and use thereof |
| RU2750937C2 (ru) | 2016-02-09 | 2021-07-06 | Альбирео Аб | Пероральный состав холестирамина и его применение |
| US11350844B2 (en) | 2016-11-23 | 2022-06-07 | Mayo Foundation For Medical Education And Research | System and method for generating nonalcoholic fatty liver disease activity score (NAS) using magnetic resonance elastography |
| KR101844184B1 (ko) | 2017-07-21 | 2018-04-02 | 씨제이헬스케어 주식회사 | 아미노알킬벤조티아제핀 유도체의 용도 |
| CA3071285A1 (en) | 2017-08-09 | 2019-02-14 | Albireo Ab | Cholestyramine granules, oral cholestyramine formulations and use thereof |
| WO2019032027A1 (en) | 2017-08-09 | 2019-02-14 | Albireo Ab | CHOLESTYRAMINE TABLETS, ORAL FORMULATIONS OF CHOLESTYRAMINE AND THEIR USE |
| EP3762370A1 (en) | 2018-03-09 | 2021-01-13 | Elobix Ab | Process for the preparation of elobixibat |
| US10428109B1 (en) | 2018-03-09 | 2019-10-01 | Elobix Ab | Process for the preparation of 1,5-benzothiazepine compounds |
| WO2019234077A1 (en) | 2018-06-05 | 2019-12-12 | Albireo Ab | Benzothia(di)azepine compounds and their use as bile acid modulators |
| US10793534B2 (en) | 2018-06-05 | 2020-10-06 | Albireo Ab | Benzothia(di)azepine compounds and their use as bile acid modulators |
| US11801226B2 (en) | 2018-06-20 | 2023-10-31 | Albireo Ab | Pharmaceutical formulation of odevixibat |
| PE20210182A1 (es) | 2018-06-20 | 2021-01-29 | Albireo Ab | Modificaciones de cristales de odexibat |
| US10941127B2 (en) | 2019-02-06 | 2021-03-09 | Albireo Ab | Benzothiadiazepine compounds and their use as bile acid modulators |
| MX2021008981A (es) | 2019-02-06 | 2021-09-08 | Albireo Ab | Compuestos de benzotiadiazepina y su uso como moduladores del acido biliar. |
| CN113453753A (zh) | 2019-02-06 | 2021-09-28 | 阿尔比里奥公司 | 苯并硫氮杂环庚三烯化合物及其用作胆汁酸调节剂的用途 |
| US10975045B2 (en) | 2019-02-06 | 2021-04-13 | Aibireo AB | Benzothiazepine compounds and their use as bile acid modulators |
| US11014898B1 (en) | 2020-12-04 | 2021-05-25 | Albireo Ab | Benzothiazepine compounds and their use as bile acid modulators |
| EP4069359B1 (en) * | 2019-12-04 | 2024-01-03 | Albireo AB | Benzothia(di)azepine compounds and their use as bile acid modulators |
| KR20220109450A (ko) | 2019-12-04 | 2022-08-04 | 알비레오 에이비 | 벤조티아(디)아제핀 화합물 및 담즙산 조절제로서의 이의 용도 |
| CN114761080A (zh) * | 2019-12-04 | 2022-07-15 | 阿尔比里奥公司 | 苯并硫杂(二)氮杂环庚三烯化合物及其作为胆汁酸调节剂的用途 |
| CN114761018A (zh) | 2019-12-04 | 2022-07-15 | 阿尔比里奥公司 | 苯并硫杂二氮杂环庚三烯化合物及其作为胆汁酸调节剂的用途 |
| JP2023537285A (ja) | 2020-08-03 | 2023-08-31 | アルビレオ・アクチボラグ | ベンゾチア（ジ）アゼピン化合物及び胆汁酸モジュレータとしてのそれらの使用 |
| JP2023549226A (ja) | 2020-11-12 | 2023-11-22 | アルビレオ エービー | 進行性家族性肝内胆汁うっ滞症（ｐｆｉｃ）を処置するためのオデビキシバット |
| BR112023010799A2 (pt) | 2020-12-04 | 2023-10-03 | Albireo Ab | Compostos de benzotia(di)azepina e seus usos como moduladores de ácidos biliares |
| TW202313579A (zh) | 2021-06-03 | 2023-04-01 | 瑞典商艾爾比瑞歐公司 | 苯并噻(二)氮呯(benzothia(di)azepine)化合物及其作為膽酸調節劑之用途 |
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