TWI837169B - 甲狀腺素受體β促效劑化合物 - Google Patents
甲狀腺素受體β促效劑化合物 Download PDFInfo
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- TWI837169B TWI837169B TW108130298A TW108130298A TWI837169B TW I837169 B TWI837169 B TW I837169B TW 108130298 A TW108130298 A TW 108130298A TW 108130298 A TW108130298 A TW 108130298A TW I837169 B TWI837169 B TW I837169B
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- 150000001875 compounds Chemical class 0.000 title claims abstract description 335
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- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 46
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 44
- 201000010099 disease Diseases 0.000 claims description 37
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims description 33
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- 125000004432 carbon atom Chemical group C* 0.000 claims description 27
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 26
- 125000004429 atom Chemical group 0.000 claims description 25
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims description 23
- 229910052736 halogen Inorganic materials 0.000 claims description 22
- 150000002367 halogens Chemical class 0.000 claims description 22
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- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 13
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- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 10
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- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 8
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- 238000000034 method Methods 0.000 abstract description 55
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- 125000004434 sulfur atom Chemical group 0.000 description 1
- 235000011149 sulphuric acid Nutrition 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 238000001308 synthesis method Methods 0.000 description 1
- 230000006794 tachycardia Effects 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- BCNZYOJHNLTNEZ-UHFFFAOYSA-N tert-butyldimethylsilyl chloride Chemical compound CC(C)(C)[Si](C)(C)Cl BCNZYOJHNLTNEZ-UHFFFAOYSA-N 0.000 description 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- 150000003536 tetrazoles Chemical class 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 description 1
- 125000005323 thioketone group Chemical group 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- 230000037317 transdermal delivery Effects 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
- 150000003852 triazoles Chemical class 0.000 description 1
- 229910052905 tridymite Inorganic materials 0.000 description 1
- 239000001226 triphosphate Substances 0.000 description 1
- 235000011178 triphosphate Nutrition 0.000 description 1
- 125000002264 triphosphate group Chemical group [H]OP(=O)(O[H])OP(=O)(O[H])OP(=O)(O[H])O* 0.000 description 1
- 150000004043 trisaccharides Chemical class 0.000 description 1
- 229930195735 unsaturated hydrocarbon Natural products 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- BFDBKMOZYNOTPK-UHFFFAOYSA-N vonoprazan Chemical compound C=1C=CN=CC=1S(=O)(=O)N1C=C(CNC)C=C1C1=CC=CC=C1F BFDBKMOZYNOTPK-UHFFFAOYSA-N 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
- UGOMMVLRQDMAQQ-UHFFFAOYSA-N xphos Chemical compound CC(C)C1=CC(C(C)C)=CC(C(C)C)=C1C1=CC=CC=C1P(C1CCCCC1)C1CCCCC1 UGOMMVLRQDMAQQ-UHFFFAOYSA-N 0.000 description 1
- 229910052726 zirconium Inorganic materials 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Obesity (AREA)
- Diabetes (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862722312P | 2018-08-24 | 2018-08-24 | |
| US62/722,312 | 2018-08-24 | ||
| US201962867117P | 2019-06-26 | 2019-06-26 | |
| US62/867,117 | 2019-06-26 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW202023560A TW202023560A (zh) | 2020-07-01 |
| TWI837169B true TWI837169B (zh) | 2024-04-01 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW108130298A TWI837169B (zh) | 2018-08-24 | 2019-08-23 | 甲狀腺素受體β促效劑化合物 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US10800767B2 (enExample) |
| EP (1) | EP3840755A4 (enExample) |
| JP (2) | JP7579253B2 (enExample) |
| CN (1) | CN112805005A (enExample) |
| AU (2) | AU2019325656B2 (enExample) |
| CA (1) | CA3110520A1 (enExample) |
| MA (1) | MA53448A (enExample) |
| TW (1) | TWI837169B (enExample) |
| WO (1) | WO2020041741A1 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI840423B (zh) | 2018-10-12 | 2024-05-01 | 美商拓臻股份有限公司 | 甲狀腺素受體β促效劑化合物 |
| CN121081472A (zh) | 2018-12-13 | 2025-12-09 | 拓臻股份有限公司 | 一种THRβ受体激动剂化合物及其制备方法和用途 |
| SG11202111552YA (en) | 2019-05-08 | 2021-11-29 | Aligos Therapeutics Inc | MODULATORS OF THR-ß AND METHODS OF USE THEREOF |
| TW202108556A (zh) * | 2019-05-10 | 2021-03-01 | 大陸商深圳微芯生物科技股份有限公司 | 一種噠嗪酮衍生物及其應用 |
| CN114375193B (zh) | 2019-09-12 | 2024-05-14 | 拓臻制药公司 | 甲状腺激素受体β激动剂化合物 |
| CN114437034A (zh) * | 2020-11-06 | 2022-05-06 | 深圳微芯生物科技股份有限公司 | 一种酞嗪类化合物的可药用盐、晶型及其制备方法 |
| WO2022103960A1 (en) * | 2020-11-13 | 2022-05-19 | Inipharm, Inc. | Dichlorophenol hsd17b13 inhibitors and uses thereof |
| CN114621207B (zh) * | 2020-12-11 | 2025-02-11 | 广东东阳光药业股份有限公司 | 一种作为甲状腺激素β受体激动剂的化合物及其用途 |
| CN117120051A (zh) * | 2021-03-03 | 2023-11-24 | 拓臻制药公司 | 甲状腺激素受体β激动剂化合物 |
| WO2022194287A1 (zh) * | 2021-03-19 | 2022-09-22 | 南京明德新药研发有限公司 | 双环吡啶酮类化合物及其应用 |
| JP7665774B2 (ja) * | 2021-03-19 | 2025-04-21 | メッドシャイン ディスカバリー インコーポレイテッド | 二環式フェノール系化合物及びその使用 |
| TW202506131A (zh) | 2023-04-07 | 2025-02-16 | 美商拓臻製藥公司 | ＧＬＰ－１Ｒ及ＴＨＲβ激動劑之組合以及其使用方法 |
| CN116554063B (zh) * | 2023-05-23 | 2025-03-07 | 江苏省农用激素工程技术研究中心有限公司 | 氟胺磺隆中间体的制备方法 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1471049A1 (en) * | 2002-01-30 | 2004-10-27 | Kissei Pharmaceutical Co., Ltd. | Novel thyroid hormone receptor ligand, medicinal compositions containing the same and use thereof |
| WO2007009913A1 (en) * | 2005-07-21 | 2007-01-25 | F. Hoffmann-La Roche Ag | Pyridazinone derivatives as thyroid hormone receptor agonists |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7572799B2 (en) * | 2003-11-24 | 2009-08-11 | Pfizer Inc | Pyrazolo[4,3-d]pyrimidines as Phosphodiesterase Inhibitors |
| GB0327319D0 (en) * | 2003-11-24 | 2003-12-24 | Pfizer Ltd | Novel pharmaceuticals |
| WO2007132475A1 (en) * | 2006-05-15 | 2007-11-22 | Cadila Healthcare Limited | Selective tr-beta 1 agonist |
| US8394811B2 (en) * | 2007-04-18 | 2013-03-12 | Molsoft Llc | Hydrazide compounds as thyroid hormone receptor modulators and uses thereof |
| CN111646979B (zh) | 2018-01-23 | 2021-08-31 | 深圳市塔吉瑞生物医药有限公司 | 取代的哒嗪酮化合物 |
| JP7181386B2 (ja) | 2018-06-12 | 2022-11-30 | スーチョワン ハイスコ ファーマスーティカル カンパニー リミテッド | 甲状腺ホルモン受容体アゴニスト及びその用途 |
| CN119552152A (zh) | 2018-10-12 | 2025-03-04 | 益方生物科技(上海)股份有限公司 | 甲状腺激素受体激动剂 |
-
2019
- 2019-08-23 EP EP19852050.4A patent/EP3840755A4/en active Pending
- 2019-08-23 MA MA053448A patent/MA53448A/fr unknown
- 2019-08-23 CN CN201980066702.0A patent/CN112805005A/zh active Pending
- 2019-08-23 WO PCT/US2019/047968 patent/WO2020041741A1/en not_active Ceased
- 2019-08-23 CA CA3110520A patent/CA3110520A1/en active Pending
- 2019-08-23 US US16/549,979 patent/US10800767B2/en active Active
- 2019-08-23 JP JP2021533405A patent/JP7579253B2/ja active Active
- 2019-08-23 TW TW108130298A patent/TWI837169B/zh active
- 2019-08-23 AU AU2019325656A patent/AU2019325656B2/en active Active
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2024
- 2024-08-29 US US18/818,705 patent/US20250236615A1/en active Pending
- 2024-10-25 JP JP2024187991A patent/JP2025020206A/ja active Pending
-
2025
- 2025-07-22 AU AU2025206402A patent/AU2025206402A1/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1471049A1 (en) * | 2002-01-30 | 2004-10-27 | Kissei Pharmaceutical Co., Ltd. | Novel thyroid hormone receptor ligand, medicinal compositions containing the same and use thereof |
| WO2007009913A1 (en) * | 2005-07-21 | 2007-01-25 | F. Hoffmann-La Roche Ag | Pyridazinone derivatives as thyroid hormone receptor agonists |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3840755A1 (en) | 2021-06-30 |
| US10800767B2 (en) | 2020-10-13 |
| CN112805005A (zh) | 2021-05-14 |
| JP2021535207A (ja) | 2021-12-16 |
| JP2025020206A (ja) | 2025-02-12 |
| AU2025206402A1 (en) | 2025-08-07 |
| AU2019325656A1 (en) | 2021-03-11 |
| AU2019325656B2 (en) | 2025-04-24 |
| MA53448A (fr) | 2022-04-20 |
| US20250236615A1 (en) | 2025-07-24 |
| WO2020041741A1 (en) | 2020-02-27 |
| CA3110520A1 (en) | 2020-02-27 |
| TW202023560A (zh) | 2020-07-01 |
| JP7579253B2 (ja) | 2024-11-07 |
| EP3840755A4 (en) | 2022-04-20 |
| US20200062742A1 (en) | 2020-02-27 |
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