JP2018538331A5 - - Google Patents
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- Publication number
- JP2018538331A5 JP2018538331A5 JP2018532396A JP2018532396A JP2018538331A5 JP 2018538331 A5 JP2018538331 A5 JP 2018538331A5 JP 2018532396 A JP2018532396 A JP 2018532396A JP 2018532396 A JP2018532396 A JP 2018532396A JP 2018538331 A5 JP2018538331 A5 JP 2018538331A5
- Authority
- JP
- Japan
- Prior art keywords
- degrees
- crystalline form
- diffraction pattern
- ray diffraction
- peaks
- 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.)
- Pending
Links
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 17
- 238000002441 X-ray diffraction Methods 0.000 claims description 15
- ZXERDUOLZKYMJM-ZWECCWDJSA-N obeticholic 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)CCC(O)=O)CC[C@H]21 ZXERDUOLZKYMJM-ZWECCWDJSA-N 0.000 claims description 13
- 239000013078 crystal Substances 0.000 claims description 12
- 239000002253 acid Substances 0.000 claims description 10
- 229960001601 obeticholic acid Drugs 0.000 claims description 10
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims description 9
- 239000012535 impurity Substances 0.000 claims description 6
- 239000000843 powder Substances 0.000 claims description 3
- RUDATBOHQWOJDD-UHFFFAOYSA-N (3beta,5beta,7alpha)-3,7-Dihydroxycholan-24-oic acid Natural products OC1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)CC2 RUDATBOHQWOJDD-UHFFFAOYSA-N 0.000 claims description 2
- 150000007513 acids Chemical class 0.000 claims description 2
- RUDATBOHQWOJDD-BSWAIDMHSA-N chenodeoxycholic acid Chemical compound C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)CC1 RUDATBOHQWOJDD-BSWAIDMHSA-N 0.000 claims description 2
- 229960001091 chenodeoxycholic acid Drugs 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 2
- 238000001953 recrystallisation Methods 0.000 claims 5
- DKPFZGUDAPQIHT-UHFFFAOYSA-N butyl acetate Chemical compound CCCCOC(C)=O DKPFZGUDAPQIHT-UHFFFAOYSA-N 0.000 claims 2
- NTIZESTWPVYFNL-UHFFFAOYSA-N Methyl isobutyl ketone Chemical compound CC(C)CC(C)=O NTIZESTWPVYFNL-UHFFFAOYSA-N 0.000 claims 1
- UIHCLUNTQKBZGK-UHFFFAOYSA-N Methyl isobutyl ketone Natural products CCC(C)C(C)=O UIHCLUNTQKBZGK-UHFFFAOYSA-N 0.000 claims 1
- LYGJENNIWJXYER-UHFFFAOYSA-N nitromethane Chemical compound C[N+]([O-])=O LYGJENNIWJXYER-UHFFFAOYSA-N 0.000 claims 1
- 239000007787 solid Substances 0.000 description 4
- 238000002474 experimental method Methods 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 1
- 238000001938 differential scanning calorimetry curve Methods 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 239000004810 polytetrafluoroethylene Substances 0.000 description 1
- 229920001343 polytetrafluoroethylene Polymers 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 238000001757 thermogravimetry curve Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US14/979,005 | 2015-12-22 | ||
| US14/979,005 US9982008B2 (en) | 2012-06-19 | 2015-12-22 | Preparation and uses of obeticholic acid |
| PCT/US2016/012651 WO2017111979A1 (en) | 2015-12-22 | 2016-01-08 | Polymorphic crystalline forms of obeticholic acid |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018538331A JP2018538331A (ja) | 2018-12-27 |
| JP2018538331A5 true JP2018538331A5 (https=) | 2019-02-14 |
Family
ID=55650649
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018532396A Pending JP2018538331A (ja) | 2015-12-22 | 2016-01-08 | オベチコール酸の多型結晶形態 |
Country Status (15)
| Country | Link |
|---|---|
| EP (1) | EP3394081A1 (https=) |
| JP (1) | JP2018538331A (https=) |
| KR (1) | KR20180095070A (https=) |
| CN (1) | CN108495858A (https=) |
| AU (1) | AU2016375566A1 (https=) |
| BR (1) | BR112018012590A2 (https=) |
| CA (1) | CA3009149A1 (https=) |
| CL (1) | CL2018001720A1 (https=) |
| CO (1) | CO2018006701A2 (https=) |
| EA (1) | EA201891491A1 (https=) |
| IL (1) | IL259998A (https=) |
| MX (1) | MX2018007776A (https=) |
| PH (1) | PH12018501318A1 (https=) |
| SG (1) | SG11201805235XA (https=) |
| WO (1) | WO2017111979A1 (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105801653B (zh) * | 2014-12-30 | 2018-04-17 | 苏州晶云药物科技有限公司 | 奥贝胆酸的晶型a及其制备方法 |
| WO2018211413A1 (en) * | 2017-05-15 | 2018-11-22 | Dr. Reddy’S Laboratories Limited | Solid forms of obeticholic acid and process for preparation |
| CN109280071A (zh) * | 2017-07-19 | 2019-01-29 | 东莞东阳光药物研发有限公司 | 奥贝胆酸的晶型及其制备方法 |
| CN107383139A (zh) * | 2017-08-09 | 2017-11-24 | 杭州和泽医药科技有限公司 | 一种3α‑羟基‑7‑氧代‑5β‑胆烷酸新衍生物制备奥贝胆酸的方法 |
| CZ31099U1 (cs) * | 2017-09-05 | 2017-10-17 | Zentiva, K.S. | Krystalické formy (3a,5B,6a,7a)-6-ethyl-3,7- dihydroxycholan-24-ové kyseliny |
| CN109485687A (zh) * | 2017-09-12 | 2019-03-19 | 成都弘达药业有限公司 | 奥贝胆酸的晶型j及其制备方法 |
| WO2019106043A1 (en) | 2017-11-29 | 2019-06-06 | Hexal Ag | Pharmaceutical composition comprising obeticholic acid |
| GB201812382D0 (en) | 2018-07-30 | 2018-09-12 | Nzp Uk Ltd | Compounds |
| CN113264972B (zh) * | 2020-02-14 | 2024-07-12 | 四川科伦药物研究院有限公司 | 一种制备奥贝胆酸的方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ITMI20050912A1 (it) * | 2005-05-19 | 2006-11-20 | Erregierre Spa | Processo di preparazione di acidi 3-a-ya(b)-diidrossi-6-a(b)-alchil-5b-colanici |
| SI3336097T1 (sl) * | 2012-06-19 | 2021-07-30 | Intercept Pharmaceuticals, Inc. | Priprava nekristalinične oblike obetiholne kisline |
| CN106459136B (zh) * | 2014-09-28 | 2018-06-26 | 江苏盛迪医药有限公司 | 一种奥贝胆酸的制备方法 |
| CN107207559B (zh) * | 2014-11-19 | 2019-10-25 | Nzp英国有限公司 | 作为制备类固醇fxr调节剂的中间体的6-烷基-7-羟基-4-烯-3-酮类固醇 |
| KR102527821B1 (ko) * | 2014-11-19 | 2023-05-02 | 엔제트피 유케이 리미티드 | 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 6α-알킬-6,7-다이온 스테로이드 |
| KR102546748B1 (ko) * | 2014-11-19 | 2023-06-22 | 엔제트피 유케이 리미티드 | 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 6α-알킬-3,7-다이온 스테로이드 |
| EA033445B1 (ru) * | 2014-11-19 | 2019-10-31 | Nzp Uk Ltd | 5-бета-6-алкил-7-гидрокси-3-оновые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr |
-
2016
- 2016-01-08 JP JP2018532396A patent/JP2018538331A/ja active Pending
- 2016-01-08 CN CN201680079793.8A patent/CN108495858A/zh active Pending
- 2016-01-08 EA EA201891491A patent/EA201891491A1/ru unknown
- 2016-01-08 CA CA3009149A patent/CA3009149A1/en not_active Abandoned
- 2016-01-08 AU AU2016375566A patent/AU2016375566A1/en not_active Abandoned
- 2016-01-08 KR KR1020187020850A patent/KR20180095070A/ko not_active Withdrawn
- 2016-01-08 SG SG11201805235XA patent/SG11201805235XA/en unknown
- 2016-01-08 BR BR112018012590A patent/BR112018012590A2/pt not_active Application Discontinuation
- 2016-01-08 WO PCT/US2016/012651 patent/WO2017111979A1/en not_active Ceased
- 2016-01-08 EP EP16714049.0A patent/EP3394081A1/en not_active Withdrawn
- 2016-01-08 MX MX2018007776A patent/MX2018007776A/es unknown
-
2018
- 2018-06-13 IL IL259998A patent/IL259998A/en unknown
- 2018-06-20 PH PH12018501318A patent/PH12018501318A1/en unknown
- 2018-06-22 CL CL2018001720A patent/CL2018001720A1/es unknown
- 2018-06-27 CO CONC2018/0006701A patent/CO2018006701A2/es unknown
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