JPWO2020010068A5 - - Google Patents
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- Publication number
- JPWO2020010068A5 JPWO2020010068A5 JP2020572517A JP2020572517A JPWO2020010068A5 JP WO2020010068 A5 JPWO2020010068 A5 JP WO2020010068A5 JP 2020572517 A JP2020572517 A JP 2020572517A JP 2020572517 A JP2020572517 A JP 2020572517A JP WO2020010068 A5 JPWO2020010068 A5 JP WO2020010068A5
- Authority
- JP
- Japan
- Prior art keywords
- crystalline salt
- pharmaceutical composition
- salt according
- subject
- diffraction pattern
- 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
- 150000003839 salts Chemical class 0.000 claims 37
- 239000011780 sodium chloride Substances 0.000 claims 37
- 239000008194 pharmaceutical composition Substances 0.000 claims 25
- 238000000634 powder X-ray diffraction Methods 0.000 claims 8
- 206010045261 Type IIa hyperlipidaemia Diseases 0.000 claims 4
- 235000001014 amino acid Nutrition 0.000 claims 4
- 150000001413 amino acids Chemical group 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 229940079593 drugs Drugs 0.000 claims 4
- 208000000563 Hyperlipoproteinemia Type II Diseases 0.000 claims 3
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 claims 3
- 102100012475 LDLR Human genes 0.000 claims 3
- 108060004326 LDLR Proteins 0.000 claims 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-N acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 3
- 201000001386 familial hypercholesterolemia Diseases 0.000 claims 3
- 201000009846 fatty liver disease Diseases 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 238000006467 substitution reaction Methods 0.000 claims 3
- 239000004475 Arginine Substances 0.000 claims 2
- 206010058108 Dyslipidaemia Diseases 0.000 claims 2
- 229960002885 Histidine Drugs 0.000 claims 2
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 claims 2
- ODKSFYDXXFIFQN-BYPYZUCNSA-N L-arginine Chemical compound OC(=O)[C@@H](N)CCCN=C(N)N ODKSFYDXXFIFQN-BYPYZUCNSA-N 0.000 claims 2
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 2
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims 2
- 206010061227 Lipid metabolism disease Diseases 0.000 claims 2
- 206010053219 Non-alcoholic steatohepatitis Diseases 0.000 claims 2
- 239000004473 Threonine Substances 0.000 claims 2
- 235000004279 alanine Nutrition 0.000 claims 2
- 235000009697 arginine Nutrition 0.000 claims 2
- 230000035772 mutation Effects 0.000 claims 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 2
- -1 3,5-dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazine-3-yl) oxy) phenyl Chemical group 0.000 claims 1
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 1
- 206010003736 Attention deficit/hyperactivity disease Diseases 0.000 claims 1
- 208000003432 Bone Disease Diseases 0.000 claims 1
- 210000000988 Bone and Bones Anatomy 0.000 claims 1
- OEYIOHPDSNJKLS-UHFFFAOYSA-N C[N+](C)(C)CCO Chemical compound C[N+](C)(C)CCO OEYIOHPDSNJKLS-UHFFFAOYSA-N 0.000 claims 1
- 208000008787 Cardiovascular Disease Diseases 0.000 claims 1
- 206010011878 Deafness Diseases 0.000 claims 1
- 206010012426 Dermal cyst Diseases 0.000 claims 1
- 206010012601 Diabetes mellitus Diseases 0.000 claims 1
- ZBCBWPMODOFKDW-UHFFFAOYSA-N Diethanolamine Chemical compound OCCNCCO ZBCBWPMODOFKDW-UHFFFAOYSA-N 0.000 claims 1
- HPNMFZURTQLUMO-UHFFFAOYSA-N Diethylamine Chemical compound CCNCC HPNMFZURTQLUMO-UHFFFAOYSA-N 0.000 claims 1
- 208000004930 Fatty Liver Diseases 0.000 claims 1
- 208000004559 Hearing Loss Diseases 0.000 claims 1
- 206010011879 Hearing loss Diseases 0.000 claims 1
- 206010019708 Hepatic steatosis Diseases 0.000 claims 1
- 208000006454 Hepatitis Diseases 0.000 claims 1
- 208000009576 Hypercholesterolemia Diseases 0.000 claims 1
- 206010062060 Hyperlipidaemia Diseases 0.000 claims 1
- 208000003532 Hypothyroidism Diseases 0.000 claims 1
- 235000019766 L-Lysine Nutrition 0.000 claims 1
- 235000014852 L-arginine Nutrition 0.000 claims 1
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 claims 1
- 239000004472 Lysine Substances 0.000 claims 1
- MBBZMMPHUWSWHV-BDVNFPICSA-N Meglumine Chemical compound CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO MBBZMMPHUWSWHV-BDVNFPICSA-N 0.000 claims 1
- 206010027378 Mental retardation Diseases 0.000 claims 1
- LJMFFFZEUKITIM-UHFFFAOYSA-N N#CC1=CNCNN1 Chemical compound N#CC1=CNCNN1 LJMFFFZEUKITIM-UHFFFAOYSA-N 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010037211 Psychomotor hyperactivity Diseases 0.000 claims 1
- 208000001871 Tachycardia Diseases 0.000 claims 1
- 210000001685 Thyroid Gland Anatomy 0.000 claims 1
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Tris Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 claims 1
- 230000001476 alcoholic Effects 0.000 claims 1
- 150000001483 arginine derivatives Chemical class 0.000 claims 1
- 201000006287 attention deficit hyperactivity disease Diseases 0.000 claims 1
- 230000003111 delayed Effects 0.000 claims 1
- HZAXFHJVJLSVMW-UHFFFAOYSA-N ethanolamine Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 claims 1
- 231100000888 hearing loss Toxicity 0.000 claims 1
- 231100000283 hepatitis Toxicity 0.000 claims 1
- 230000002989 hypothyroidism Effects 0.000 claims 1
- 201000006347 intellectual disability Diseases 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 229960003646 lysine Drugs 0.000 claims 1
- 230000003340 mental Effects 0.000 claims 1
- 230000000926 neurological Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 230000001568 sexual Effects 0.000 claims 1
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 239000005495 thyroid hormone Substances 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024076310A JP2024105460A (ja) | 2018-07-02 | 2024-05-09 | ２－（３，５－ジクロロ－４－（（５－イソプロピル－６－オキソ－１，６－ジヒドロピリダジン－３－イル）オキシ）フェニル）－３，５－ジオキソ－２，３，４，５－テトラヒドロ－１，２，４－トリアジン－６－カルボニトリルの固体形態 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862692914P | 2018-07-02 | 2018-07-02 | |
| US62/692,914 | 2018-07-02 | ||
| PCT/US2019/040276 WO2020010068A1 (en) | 2018-07-02 | 2019-07-02 | Solid forms of 2-(3,5-dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yl)oxy)phenyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024076310A Division JP2024105460A (ja) | 2018-07-02 | 2024-05-09 | ２－（３，５－ジクロロ－４－（（５－イソプロピル－６－オキソ－１，６－ジヒドロピリダジン－３－イル）オキシ）フェニル）－３，５－ジオキソ－２，３，４，５－テトラヒドロ－１，２，４－トリアジン－６－カルボニトリルの固体形態 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2021530456A JP2021530456A (ja) | 2021-11-11 |
| JPWO2020010068A5 true JPWO2020010068A5 (es) | 2022-07-08 |
Family
ID=67441642
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020572517A Pending JP2021530456A (ja) | 2018-07-02 | 2019-07-02 | ２−（３，５−ジクロロ−４−（（５−イソプロピル−６−オキソ−１，６−ジヒドロピリダジン−３−イル）オキシ）フェニル）−３，５−ジオキソ−２，３，４，５−テトラヒドロ−１，２，４−トリアジン−６−カルボニトリルの固体形態 |
| JP2024076310A Pending JP2024105460A (ja) | 2018-07-02 | 2024-05-09 | ２－（３，５－ジクロロ－４－（（５－イソプロピル－６－オキソ－１，６－ジヒドロピリダジン－３－イル）オキシ）フェニル）－３，５－ジオキソ－２，３，４，５－テトラヒドロ－１，２，４－トリアジン－６－カルボニトリルの固体形態 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024076310A Pending JP2024105460A (ja) | 2018-07-02 | 2024-05-09 | ２－（３，５－ジクロロ－４－（（５－イソプロピル－６－オキソ－１，６－ジヒドロピリダジン－３－イル）オキシ）フェニル）－３，５－ジオキソ－２，３，４，５－テトラヒドロ－１，２，４－トリアジン－６－カルボニトリルの固体形態 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20210122740A1 (es) |
| EP (1) | EP3818057A1 (es) |
| JP (2) | JP2021530456A (es) |
| KR (1) | KR20210027454A (es) |
| CN (1) | CN112638904A (es) |
| AR (1) | AR115666A1 (es) |
| AU (1) | AU2019298236A1 (es) |
| CA (1) | CA3104860A1 (es) |
| IL (1) | IL279700A (es) |
| MX (2) | MX2021000107A (es) |
| TW (1) | TW202019914A (es) |
| WO (1) | WO2020010068A1 (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20200023528A (ko) | 2012-09-17 | 2020-03-04 | 마드리갈 파마슈티칼스, 인크. | 갑상선 호르몬 유사체 및 이의 다형의 합성 방법 |
| US11090308B2 (en) | 2016-10-18 | 2021-08-17 | Madrigal Pharmaceuticals, Inc. | Methods of treating liver disorders or lipid disorders with a THR-beta agonist |
| JP7445996B2 (ja) | 2019-02-21 | 2024-03-08 | ナンジン・ルイジェ・ファーマ・カンパニー・リミテッド | 新規化合物及び甲状腺ホルモン受容体アゴニストとしてのそれらの使用 |
| KR20220017917A (ko) | 2019-05-08 | 2022-02-14 | 알리고스 테라퓨틱스 인코포레이티드 | Thr-베타의 조절제 및 이의 사용 방법 |
| WO2021063367A1 (zh) * | 2019-09-30 | 2021-04-08 | 苏州科睿思制药有限公司 | 一种Resmetirom晶型及其制备方法和用途 |
| WO2021129465A1 (zh) * | 2019-12-26 | 2021-07-01 | 苏州科睿思制药有限公司 | 一种Resmetirom晶型及其制备方法和用途 |
| CN116171275A (zh) | 2020-09-10 | 2023-05-26 | 苏州科睿思制药有限公司 | Resmetirom的晶型及其制备方法和用途 |
| CA3195789A1 (en) | 2020-10-19 | 2022-04-28 | Teva Pharmaceuticals International Gmbh | Solid state forms of resmetirom |
| CN114907327A (zh) * | 2021-02-10 | 2022-08-16 | 杭州领业医药科技有限公司 | Resmetirom的晶型及其制备方法和用途 |
| WO2022225827A1 (en) * | 2021-04-21 | 2022-10-27 | Merck Sharp & Dohme Llc | Novel forms of cyclic dinucleotide compounds |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1919878E (pt) * | 2005-07-21 | 2010-11-02 | Hoffmann La Roche | Derivados de piridazinona como agonistas do receptor da hormona da tiróide |
| KR20200023528A (ko) * | 2012-09-17 | 2020-03-04 | 마드리갈 파마슈티칼스, 인크. | 갑상선 호르몬 유사체 및 이의 다형의 합성 방법 |
| US11090308B2 (en) * | 2016-10-18 | 2021-08-17 | Madrigal Pharmaceuticals, Inc. | Methods of treating liver disorders or lipid disorders with a THR-beta agonist |
-
2019
- 2019-07-01 TW TW108123112A patent/TW202019914A/zh unknown
- 2019-07-01 AR ARP190101846A patent/AR115666A1/es unknown
- 2019-07-02 EP EP19745399.6A patent/EP3818057A1/en active Pending
- 2019-07-02 JP JP2020572517A patent/JP2021530456A/ja active Pending
- 2019-07-02 US US17/257,070 patent/US20210122740A1/en active Pending
- 2019-07-02 CN CN201980056826.0A patent/CN112638904A/zh active Pending
- 2019-07-02 KR KR1020217003360A patent/KR20210027454A/ko not_active Application Discontinuation
- 2019-07-02 CA CA3104860A patent/CA3104860A1/en active Pending
- 2019-07-02 WO PCT/US2019/040276 patent/WO2020010068A1/en unknown
- 2019-07-02 AU AU2019298236A patent/AU2019298236A1/en active Pending
- 2019-07-02 MX MX2021000107A patent/MX2021000107A/es unknown
-
2020
- 2020-12-23 IL IL279700A patent/IL279700A/en unknown
-
2021
- 2021-01-06 MX MX2023009701A patent/MX2023009701A/es unknown
-
2024
- 2024-05-09 JP JP2024076310A patent/JP2024105460A/ja active Pending
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