JPWO2020161217A5 - - Google Patents

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JPWO2020161217A5
JPWO2020161217A5 JP2021545897A JP2021545897A JPWO2020161217A5 JP WO2020161217 A5 JPWO2020161217 A5 JP WO2020161217A5 JP 2021545897 A JP2021545897 A JP 2021545897A JP 2021545897 A JP2021545897 A JP 2021545897A JP WO2020161217 A5 JPWO2020161217 A5 JP WO2020161217A5
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disease
liver
constipation
cholestasis
syndrome
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求項1から9のいずれか一項に記載の化合物を含む医薬 A medicament comprising a compound according to any one of claims 1-9. 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用の、請求項11に記載の医薬Cardiovascular disease or disorders of fatty acid metabolism or glucose utilization disorders such as hypercholesterolemia; disorders of fatty acid metabolism; diabetes mellitus type 1 and type 2; complications of diabetes such as cataracts, micro- and macrovascular disease, retinopathy , neuropathy, nephropathy, and delayed wound healing, tissue ischemia, diabetic foot, arteriosclerosis, myocardial infarction, acute coronary syndrome, unstable angina, stable angina, stroke, peripheral arterial occlusive disease diseases, cardiomyopathy, heart failure, heart failure, and vascular restenosis; diabetes-related diseases such as insulin resistance (impaired glucose homeostasis), hyperglycemia, hyperinsulinemia, elevated blood levels of fatty acids or glycerol; Claims for the treatment or prevention of obesity, dyslipidemia, hyperlipidemia, e.g., hypertriglyceridemia, metabolic syndrome (Syndrome X), atherosclerosis, and hypertension; and increased levels of high-density lipoprotein 12. The medicine according to Item 11 . 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用の、請求項11に記載の医薬Gastrointestinal disease or disorder, e.g., constipation (chronic constipation, functional constipation, chronic idiopathic constipation (CIC), intermittent/sporadic constipation, constipation secondary to diabetes mellitus, constipation secondary to stroke, secondary to chronic kidney disease) Constipation, constipation secondary to multiple sclerosis, constipation secondary to Parkinson's disease, constipation secondary to systemic sclerosis, drug-induced constipation, irritable bowel syndrome with constipation (IBS-C), mixed irritable bowel syndrome ( IBS-M), childhood functional constipation, and opioid-induced constipation); Crohn's disease; primary bile acid malabsorption; irritable bowel syndrome (IBS); inflammatory bowel disease (IBD); 12. A medicament according to claim 11 for the treatment or prevention of reflux disease and its complications such as Barrett's esophagus, bile reflux esophagitis and bile reflux gastritis. 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;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用の;又は肝疾患におけるコルチコステロイド療法の増強用の、請求項11記載の医薬Liver diseases or disorders, such as inherited metabolic disorders of the liver; congenital anomalies of bile acid synthesis; congenital anomalies of bile duct running; biliary atresia; stasis; hereditary forms of cholestasis; cerebrotendinous xanthomatosis; secondary defects in BA synthesis; Zellweger syndrome; liver disease associated with cystic fibrosis; syndrome; primary defect in bile acid (BA) synthesis; progressive familial intrahepatic cholestasis (PFIC), e.g., PFIC-1, PFIC-2, PFIC-3, and non-specific PFIC, PFIC after bile diversion , and PFIC after liver transplantation; benign recurrent intrahepatic cholestasis (BRIC), such as BRIC1, BRIC2, and unspecified BRIC, BRIC after bile diversion, and BRIC after liver transplantation; autoimmune hepatitis; liver fibrosis; non-alcoholic fatty liver disease (NAFLD); non-alcoholic steatohepatitis (NASH); portal hypertension; cholestasis; Down's syndrome cholestasis; drug-induced cholestasis; intrahepatic cholestasis of pregnancy (jaundice in pregnancy); intrahepatic cholestasis; extrahepatic cholestasis; parenteral nutrition-associated cholestasis (PNAC); lymphedema cholestasis syndrome 1 (LSC1); primary sclerosing cholangitis (PSC); immunoglobulin G4-associated cholangitis; primary cholangitis; cholelithiasis (gallstones); biliary lithiasis; choledocholithiasis; cholelithic pancreatitis; Calorie's disease; malignant tumor of the bile duct; malignant tumor causing obstruction of the bile tree; pruritus; pancreatitis; chronic autoimmune liver disease leading to progressive cholestasis; liver steatosis; alcoholic hepatitis; acute fatty liver; fatty liver of pregnancy; Dysfunction type 1 (BAS type 1); drug-induced liver injury (DILI); liver fibrosis; congenital liver fibrosis; cirrhosis; Langerhans cell histiocytosis (LCH); idiopathic adult cholangiocytopenia (IAD); idiopathic neonatal hepatitis (INH); non-syndromic intrahepatic cholangiocytopenia (NS PILBD); autosomal recessive intrahepatic cholestasis (North American Indian childhood cirrhosis) (NAIC); hepatic sarcoidosis amyloidosis; necrotizing enterocolitis; serum bile acid-induced toxicities, e.g., cardiac rhythm disturbances in the setting of abnormal serum bile acid profiles (e.g., atrial fibrillation); (cholecardia)”), and skeletal muscle wasting associated with cholestatic liver disease; viral hepatitis (including hepatitis A, hepatitis B, hepatitis C, hepatitis D, and hepatitis E); liver cholangiocarcinoma; gastrointestinal cancer associated with bile acids; and for the treatment or prevention of cholestasis caused by tumors and neoplasms of the liver, biliary tract and pancreas; or cortico in liver disease 12. A medicament according to claim 11 for augmenting steroid therapy. 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;並びに腎不全のそう痒の治療若しくは予防用の;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用の、請求項11に記載の医薬hyperabsorption syndrome (including abetalipoproteinemia, familial hypobetalipoproteinemia (FHBL), chylomicron retention disease (CRD), and sitosterolemia); hypervitaminosis and osteopetrosis; hypertension; 12. A medicament according to claim 11 for glomerular hyperfiltration; and for the treatment or prevention of pruritus of renal failure; or for protection against renal injury associated with hepatic or metabolic disease.
JP2021545897A 2019-02-06 2020-02-06 Benzothiadiazepine compounds and their use as bile acid modulators - Patents.com Active JP7504109B2 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
IN201911004690 2019-02-06
IN201911004690 2019-02-06
SE1950464 2019-04-12
SE1950464-6 2019-04-12
IN201911049981 2019-12-04
IN201911049981 2019-12-04
PCT/EP2020/052942 WO2020161217A1 (en) 2019-02-06 2020-02-06 Benzothiadiazepine compounds and their use as bile acid modulators

Publications (3)

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JP2022519370A JP2022519370A (en) 2022-03-23
JPWO2020161217A5 true JPWO2020161217A5 (en) 2023-02-01
JP7504109B2 JP7504109B2 (en) 2024-06-21

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