JP2017537061A5 - - Google Patents
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- JP2017537061A5 JP2017537061A5 JP2017519487A JP2017519487A JP2017537061A5 JP 2017537061 A5 JP2017537061 A5 JP 2017537061A5 JP 2017519487 A JP2017519487 A JP 2017519487A JP 2017519487 A JP2017519487 A JP 2017519487A JP 2017537061 A5 JP2017537061 A5 JP 2017537061A5
- Authority
- JP
- Japan
- Prior art keywords
- crystalline
- liver
- dihydrate
- anhydride
- erobixibat
- 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.)
- Granted
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- 150000004683 dihydrates Chemical class 0.000 claims 12
- 150000008064 anhydrides Chemical class 0.000 claims 10
- 201000010099 disease Diseases 0.000 claims 7
- 210000004185 Liver Anatomy 0.000 claims 6
- 238000000634 powder X-ray diffraction Methods 0.000 claims 6
- 206010008635 Cholestasis Diseases 0.000 claims 5
- 206010010774 Constipation Diseases 0.000 claims 5
- 206010019708 Hepatic steatosis Diseases 0.000 claims 4
- 231100000359 cholestasis Toxicity 0.000 claims 4
- 201000009673 liver disease Diseases 0.000 claims 4
- 206010023126 Jaundice Diseases 0.000 claims 3
- 206010053219 Non-alcoholic steatohepatitis Diseases 0.000 claims 3
- 230000001684 chronic Effects 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 3
- 206010004661 Biliary cirrhosis primary Diseases 0.000 claims 2
- 206010008609 Cholangitis sclerosing Diseases 0.000 claims 2
- 208000004930 Fatty Liver Diseases 0.000 claims 2
- 206010016654 Fibrosis Diseases 0.000 claims 2
- 208000008338 Non-alcoholic Fatty Liver Disease Diseases 0.000 claims 2
- 208000003251 Pruritus Diseases 0.000 claims 2
- 239000003613 bile acid Substances 0.000 claims 2
- 230000004761 fibrosis Effects 0.000 claims 2
- 230000001771 impaired Effects 0.000 claims 2
- 200000000011 liver disorder Diseases 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 230000035935 pregnancy Effects 0.000 claims 2
- 201000002728 primary biliary cirrhosis Diseases 0.000 claims 2
- 201000000742 primary sclerosing cholangitis Diseases 0.000 claims 2
- 208000004624 progressive familial intrahepatic 1 Cholestasis Diseases 0.000 claims 2
- 201000002150 progressive familial intrahepatic cholestasis Diseases 0.000 claims 2
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 2
- 102100012868 ATP8B1 Human genes 0.000 claims 1
- 101710012000 ATP8B1 Proteins 0.000 claims 1
- 201000011374 Alagille syndrome Diseases 0.000 claims 1
- 208000002353 Alcoholic Hepatitis Diseases 0.000 claims 1
- 206010003827 Autoimmune hepatitis Diseases 0.000 claims 1
- 206010004637 Bile duct stone Diseases 0.000 claims 1
- 210000003445 Biliary Tract Anatomy 0.000 claims 1
- 206010053684 Cerebrohepatorenal syndrome Diseases 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N D-Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- 206010012735 Diarrhoea Diseases 0.000 claims 1
- 206010072268 Drug-induced liver injury Diseases 0.000 claims 1
- 206010058108 Dyslipidaemia Diseases 0.000 claims 1
- 208000009866 Extrahepatic Cholestasis Diseases 0.000 claims 1
- 208000001130 Gallstone Diseases 0.000 claims 1
- 206010003820 Hepatic autoimmune disease Diseases 0.000 claims 1
- 208000006454 Hepatitis Diseases 0.000 claims 1
- 206010019728 Hepatitis alcoholic Diseases 0.000 claims 1
- 206010019799 Hepatitis viral Diseases 0.000 claims 1
- 208000009576 Hypercholesterolemia Diseases 0.000 claims 1
- 206010022489 Insulin resistance Diseases 0.000 claims 1
- 208000001024 Intrahepatic Cholestasis Diseases 0.000 claims 1
- 206010065973 Iron overload Diseases 0.000 claims 1
- 208000002551 Irritable Bowel Syndrome Diseases 0.000 claims 1
- 102000006832 Jagged-1 Protein Human genes 0.000 claims 1
- 108010047319 Jagged-1 Protein Proteins 0.000 claims 1
- 206010061227 Lipid metabolism disease Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 230000036740 Metabolism Effects 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 108009000135 Nonalcoholic fatty liver disease Proteins 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 208000007232 Portal Hypertension Diseases 0.000 claims 1
- 102100011656 SLC10A2 Human genes 0.000 claims 1
- 101710036999 SLC10A2 Proteins 0.000 claims 1
- 210000002435 Tendons Anatomy 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 208000001072 Type 2 Diabetes Mellitus Diseases 0.000 claims 1
- 201000004525 Zellweger syndrome Diseases 0.000 claims 1
- 238000005299 abrasion Methods 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 230000002490 cerebral Effects 0.000 claims 1
- 201000009331 choledocholithiasis Diseases 0.000 claims 1
- 201000001883 cholelithiasis Diseases 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 201000003883 cystic fibrosis Diseases 0.000 claims 1
- 201000008286 diarrhea Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 201000008865 drug-induced hepatitis Diseases 0.000 claims 1
- 231100000595 drug-induced hepatitis Toxicity 0.000 claims 1
- 229940079593 drugs Drugs 0.000 claims 1
- 230000004129 fatty acid metabolism Effects 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- 231100000283 hepatitis Toxicity 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 201000004044 liver cirrhosis Diseases 0.000 claims 1
- 230000004060 metabolic process Effects 0.000 claims 1
- 230000035786 metabolism Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 230000000414 obstructive Effects 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 230000000750 progressive Effects 0.000 claims 1
- 201000002162 progressive familial intrahepatic cholestasis 1 Diseases 0.000 claims 1
- 239000002002 slurry Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 201000010874 syndrome Diseases 0.000 claims 1
- 238000003786 synthesis reaction Methods 0.000 claims 1
- 230000002194 synthesizing Effects 0.000 claims 1
- 201000001862 viral hepatitis Diseases 0.000 claims 1
- 239000011800 void material Substances 0.000 claims 1
Claims (17)
- 実質的に化学量論量の水を含有可能な空隙容量を含むエロビキシバットの結晶形態であって、ただし、前記化学量論量の水はエロビキシバットの１モルあたり1モルではない、エロビキシバットの結晶形態。
- エロビキシバットの結晶性無水物であって、前記無水物は、20℃の温度で10％の相対湿度で安定である、エロビキシバットの結晶性無水物。
- 6.1±0.2及び5.9±0.2の°2θ位置にピークを有する、CuKα1線によって得たXRPDパターンを有する、請求項1又は2に記載の無水物。
- 12.4±0.2及び5.8±0.2の°2θ位置にピークを有する、CuKα1線によって得たXRPDパターンを有する、請求項1又は2に記載の無水物。
- 6.4±0.2及び12.7±0.2の°2θ位置にピークを有する、CuKα1線によって得たXRPDパターンを有する、請求項1又は2に記載の無水物。
- エロビキシバットの結晶性二水和物。
- 水と接触して安定である、請求項6に記載の二水和物。
- スラリーから直接結晶化可能である、請求項6又は7に記載の二水和物。
- 6.1±0.2及び12.0±0.4の°2θ位置にピークを有する、CuKα1線によって得たXRPDパターンを有する、請求項6に記載の二水和物。
- 6.1±0.2、8.0±0.2、及び12.0±0.2の°2θ位置にピークを有する、CuKα1線によって得たXRPDパターンを有する、請求項6に記載の二水和物。
- 6.1±0.2、12.1±0.2、及び20.9±0.2の°2θ位置にピークを有する、CuKα1線によって得たXRPDパターンを有する、請求項6に記載の二水和物。
- 治療用の請求項1から11のいずれか一項に記載のエロビキシバットの結晶形態、結晶性無水物、または結晶性二水和物。
- 医薬として許容される希釈剤又は担体とともに、請求項1から11のいずれか一項に記載のエロビキシバットの結晶形態、結晶性無水物、または結晶性二水和物を含む、医薬組成物。
- 結晶形態、結晶性無水物、または結晶性二水和物の化学的純度は、>99％である、請求項13に記載の医薬組成物。
- 高コレステロール血症、脂質異常症、代謝症候群、肥満、脂肪酸代謝の障害、グルコース利用率障害、インスリン抵抗性が関与する障害、1型糖尿病及び2型糖尿病、肝臓疾患、IBAT阻害剤化合物を含む治療中の下痢、慢性便秘を含めた便秘、例えば、慢性便秘及び便秘型過敏性腸症候群(IBS-C)を含めた機能的便秘からなる群より選択される疾患の処置又は予防のための、請求項1から11のいずれか一項に記載のエロビキシバットの結晶形態、結晶性無水物、または結晶性二水和物。
- 肝実質、肝臓の先天性代謝異常、バイラー症候群、脳腱黄色腫瘍症等の胆汁酸(BA)合成に関する一次性欠損症、ツェルウェガー症候群等の二次性欠損症、新生児肝炎、嚢胞性線維症(肝臓における発現)、ALGS(アラジール症候群)、進行性家族性肝内胆汁うっ滞(PFIC)、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肝疾患、NAFLD／NASH、門脈圧亢進症、薬物に起因した黄疸又は妊娠中の黄疸等の一般的な胆汁うっ滞、遺伝型の胆汁うっ滞、例えばPFIC1等の肝内胆汁うっ滞及び肝外胆汁うっ滞、原発性硬化性胆管炎(PSC)、胆石及び総胆管結石症、胆管系の閉塞を引き起こす悪性腫瘍、胆汁うっ滞／黄疸に起因した症状(擦過傷、そう痒症)、膵炎、進行性胆汁うっ滞に帰結する慢性自己免疫性肝臓疾患、胆汁うっ滞性肝臓疾患に関するそう痒症、並びに、高脂質症の疾患に付随する疾患状態からなる群より選択される疾患の処置又は予防のための、請求項1から11のいずれか一項に記載のエロビキシバットの結晶形態、結晶性無水物、または結晶性二水和物。
- 肝臓障害及び肝臓障害に関連した疾患、脂肪肝、肝脂肪症、非アルコール性脂肪性肝炎(NASH)、アルコール性肝炎、急性脂肪肝、妊娠による脂肪肝、薬物によって誘導される肝炎、鉄過剰症障害、肝線維症、肝硬変、肝癌、ウイルス性肝炎、並びに、肝臓、胆道及び膵臓の腫瘍及び新生物に関連した問題からなる群より選択される疾患の処置又は予防のための、請求項1から11のいずれか一項に記載のエロビキシバットの結晶形態、結晶性無水物、または結晶性二水和物。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14190290.8 | 2014-10-24 | ||
| EP14190290.8A EP3012252A1 (en) | 2014-10-24 | 2014-10-24 | Crystal modifications of elobixibat |
| PCT/EP2015/074573 WO2016062848A1 (en) | 2014-10-24 | 2015-10-23 | Crystal modifications of elobixibat |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017537061A JP2017537061A (ja) | 2017-12-14 |
| JP2017537061A5 true JP2017537061A5 (ja) | 2018-10-18 |
| JP6700263B2 JP6700263B2 (ja) | 2020-05-27 |
Family
ID=51786891
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017519487A Active JP6700263B2 (ja) | 2014-10-24 | 2015-10-23 | エロビキシバットの結晶変態 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US10183920B2 (ja) |
| EP (3) | EP3012252A1 (ja) |
| JP (1) | JP6700263B2 (ja) |
| KR (1) | KR102498539B1 (ja) |
| CN (2) | CN107001301A (ja) |
| AU (1) | AU2015334883B2 (ja) |
| CA (1) | CA2959760C (ja) |
| ES (1) | ES2874573T3 (ja) |
| RU (1) | RU2017114109A (ja) |
| WO (1) | WO2016062848A1 (ja) |
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| BR112013010157B1 (pt) | 2010-11-08 | 2020-02-04 | Albireo Ab | iinibidores do ibat, seus usos, e composição e combinações farmacêuticas |
| CN106659726A (zh) | 2014-06-25 | 2017-05-10 | Ea制药株式会社 | 固体制剂及其着色防止或着色减少方法 |
| US10441604B2 (en) | 2016-02-09 | 2019-10-15 | Albireo Ab | Cholestyramine pellets and methods for preparation thereof |
| US10786529B2 (en) | 2016-02-09 | 2020-09-29 | Albireo Ab | Oral cholestyramine formulation and use thereof |
| US10441605B2 (en) | 2016-02-09 | 2019-10-15 | Albireo Ab | Oral cholestyramine formulation and use thereof |
| KR101844184B1 (ko) * | 2017-07-21 | 2018-04-02 | 씨제이헬스케어 주식회사 | 아미노알킬벤조티아제핀 유도체의 용도 |
| JP2020530448A (ja) | 2017-08-09 | 2020-10-22 | アルビレオ・アクチボラグ | コレスチラミン顆粒、経口コレスチラミン製剤、及びそれらの使用 |
| US10428109B1 (en) | 2018-03-09 | 2019-10-01 | Elobix Ab | Process for the preparation of 1,5-benzothiazepine compounds |
| MX2020009332A (es) | 2018-03-09 | 2020-10-08 | Elobix Ab | Proceso para la preparacion de elobixibat. |
| ES2942443T3 (es) | 2018-06-05 | 2023-06-01 | Albireo Ab | Compuestos de benzotia(di)azepina y su uso como moduladores de ácidos biliares |
| US10793534B2 (en) | 2018-06-05 | 2020-10-06 | Albireo Ab | Benzothia(di)azepine compounds and their use as bile acid modulators |
| CN112262130A (zh) | 2018-06-20 | 2021-01-22 | 阿尔比里奥公司 | 奥德昔巴特的结晶修饰物 |
| US11801226B2 (en) | 2018-06-20 | 2023-10-31 | Albireo Ab | Pharmaceutical formulation of odevixibat |
| US10722457B2 (en) | 2018-08-09 | 2020-07-28 | Albireo Ab | Oral cholestyramine formulation and use thereof |
| US11007142B2 (en) | 2018-08-09 | 2021-05-18 | Albireo Ab | Oral cholestyramine formulation and use thereof |
| US11549878B2 (en) | 2018-08-09 | 2023-01-10 | Albireo Ab | In vitro method for determining the adsorbing capacity of an insoluble adsorbant |
| 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 |
| CN115175918A (zh) * | 2019-09-09 | 2022-10-11 | 埃洛比克斯股份公司 | 用于制造1,5-苯并硫氮杂䓬化合物的方法 |
| CN114786772B (zh) | 2019-12-04 | 2024-04-09 | 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 |
| JP2023504644A (ja) | 2019-12-04 | 2023-02-06 | 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 |
| US11014898B1 (en) | 2020-12-04 | 2021-05-25 | Albireo Ab | Benzothiazepine compounds and their use as bile acid modulators |
| PL4069360T3 (pl) | 2019-12-04 | 2024-04-29 | Albireo Ab | Związki benzotio(di)azepinowe i ich zastosowanie jako modulatory kwasów żółciowych |
| CA3158181A1 (en) | 2019-12-04 | 2021-06-10 | Albireo Ab | Benzothia(di)azepine compounds and their use as bile acid modulators |
| EP4188541A1 (en) | 2020-08-03 | 2023-06-07 | Albireo AB | Benzothia(di)azepine compounds and their use as bile acid modulators |
| WO2022101379A1 (en) | 2020-11-12 | 2022-05-19 | Albireo Ab | Odevixibat for treating progressive familial intrahepatic cholestasis (pfic) |
| AU2021379076A1 (en) | 2020-11-12 | 2023-06-08 | Albireo Ab | Odevixibat for treating progressive familial intrahepatic cholestasis (pfic) |
| AU2021390172A1 (en) | 2020-12-04 | 2023-06-22 | Albireo Ab | Benzothia(di)azepine compounds and their use as bile acid modulators |
| CN117980295A (zh) * | 2022-08-02 | 2024-05-03 | 上海皓元医药股份有限公司 | 一种依洛西巴特晶型ii及其制备方法 |
| WO2024094841A1 (en) | 2022-11-03 | 2024-05-10 | Albireo Ab | Treating alagille syndrome (algs) |
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-
2014
- 2014-10-24 EP EP14190290.8A patent/EP3012252A1/en not_active Withdrawn
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2015
- 2015-10-23 CA CA2959760A patent/CA2959760C/en active Active
- 2015-10-23 CN CN201580055918.9A patent/CN107001301A/zh active Pending
- 2015-10-23 KR KR1020177012754A patent/KR102498539B1/ko active IP Right Grant
- 2015-10-23 CN CN202011101686.5A patent/CN112375044A/zh active Pending
- 2015-10-23 US US15/519,808 patent/US10183920B2/en active Active
- 2015-10-23 ES ES15784385T patent/ES2874573T3/es active Active
- 2015-10-23 AU AU2015334883A patent/AU2015334883B2/en active Active
- 2015-10-23 RU RU2017114109A patent/RU2017114109A/ru unknown
- 2015-10-23 EP EP15784385.5A patent/EP3209649B1/en active Active
- 2015-10-23 EP EP21167339.7A patent/EP3904344A1/en not_active Withdrawn
- 2015-10-23 JP JP2017519487A patent/JP6700263B2/ja active Active
- 2015-10-23 WO PCT/EP2015/074573 patent/WO2016062848A1/en active Application Filing
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2018
- 2018-12-27 US US16/234,364 patent/US10519120B2/en active Active
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