CN114174282A - 作为甲状腺素受体-β激动剂的哒嗪酮类衍生物及其应用 - Google Patents
作为甲状腺素受体-β激动剂的哒嗪酮类衍生物及其应用 Download PDFInfo
- Publication number
- CN114174282A CN114174282A CN202080051869.2A CN202080051869A CN114174282A CN 114174282 A CN114174282 A CN 114174282A CN 202080051869 A CN202080051869 A CN 202080051869A CN 114174282 A CN114174282 A CN 114174282A
- Authority
- CN
- China
- Prior art keywords
- beta agonists
- pyridazinone derivatives
- thyroxine receptor
- thyroxine
- receptor
- 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
- XUIIKFGFIJCVMT-GFCCVEGCSA-N D-thyroxine Chemical compound IC1=CC(C[C@@H](N)C(O)=O)=CC(I)=C1OC1=CC(I)=C(O)C(I)=C1 XUIIKFGFIJCVMT-GFCCVEGCSA-N 0.000 title abstract 3
- 229940125388 beta agonist Drugs 0.000 title abstract 3
- 229940034208 thyroxine Drugs 0.000 title abstract 3
- XUIIKFGFIJCVMT-UHFFFAOYSA-N thyroxine-binding globulin Natural products IC1=CC(CC([NH3+])C([O-])=O)=CC(I)=C1OC1=CC(I)=C(O)C(I)=C1 XUIIKFGFIJCVMT-UHFFFAOYSA-N 0.000 title abstract 3
- AAILEWXSEQLMNI-UHFFFAOYSA-N 1h-pyridazin-6-one Chemical class OC1=CC=CN=N1 AAILEWXSEQLMNI-UHFFFAOYSA-N 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
- A61P5/16—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D237/14—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
作为甲状腺素受体‑β激动剂的哒嗪酮类衍生物，及其在制备甲状腺素受体‑β激动剂相关疾病的药物中的应用。具体公开了式(I)所示化合物或其药学上可接受的盐。
Description
PCT国内申请，说明书已公开。
Claims (20)
- PCT国内申请，权利要求书已公开。
Applications Claiming Priority (13)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910459299 | 2019-05-29 | ||
| CN201910459299X | 2019-05-29 | ||
| CN201910741177X | 2019-08-12 | ||
| CN201910741177 | 2019-08-12 | ||
| CN2019111300680 | 2019-11-18 | ||
| CN201911130068 | 2019-11-18 | ||
| CN2020100765259 | 2020-01-23 | ||
| CN202010076525 | 2020-01-23 | ||
| CN202010188909 | 2020-03-17 | ||
| CN202010188909X | 2020-03-17 | ||
| CN2020104094200 | 2020-05-14 | ||
| CN202010409420 | 2020-05-14 | ||
| PCT/CN2020/093284 WO2020239076A1 (zh) | 2019-05-29 | 2020-05-29 | 作为甲状腺素受体-β激动剂的哒嗪酮类衍生物及其应用 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN114174282A true CN114174282A (zh) | 2022-03-11 |
Family
ID=73553497
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202080051869.2A Pending CN114174282A (zh) | 2019-05-29 | 2020-05-29 | 作为甲状腺素受体-β激动剂的哒嗪酮类衍生物及其应用 |
Country Status (2)
| Country | Link |
|---|---|
| CN (1) | CN114174282A (zh) |
| WO (1) | WO2020239076A1 (zh) |
Families Citing this family (10)
| 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 |
| CN111320609A (zh) | 2018-12-13 | 2020-06-23 | 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 |
| WO2020227549A1 (en) | 2019-05-08 | 2020-11-12 | Aligos Therapeutics, Inc. | MODULATORS OF THR-β AND METHODS OF USE THEREOF |
| CN116723844A (zh) | 2020-11-06 | 2023-09-08 | 阿利戈斯治疗公司 | 作为甲状腺激素受体β (TR-β)激动剂的双环哒嗪酮 |
| CN115073429A (zh) * | 2021-03-15 | 2022-09-20 | 昆药集团股份有限公司 | 一种1，2，4-三嗪-3，5-二酮类化合物的盐型、晶型及其制备方法 |
| WO2023028534A1 (en) | 2021-08-25 | 2023-03-02 | Ptc Therapeutics, Inc. | Inhibitors of nlrp3 |
| US20250115559A1 (en) * | 2022-02-07 | 2025-04-10 | Xizang Haisco Pharmaceutical Co., Ltd. | Preparation method of pyridazinone derivative, and intermediate thereof |
| CN116178479A (zh) * | 2022-09-09 | 2023-05-30 | 上海博璞诺科技发展有限公司 | 山海棠素甲醚的制备方法 |
| WO2024143235A1 (ja) * | 2022-12-26 | 2024-07-04 | 国立大学法人東海国立大学機構 | 甲状腺ホルモン受容体β選択的な甲状腺ホルモンアナログとして有用な化合物 |
| TWI872856B (zh) * | 2023-02-17 | 2025-02-11 | 大陸商凱思凱迪(上海)醫藥科技有限公司 | 一種多環類甲狀腺激素β受體激動劑及其用途 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007009913A1 (en) * | 2005-07-21 | 2007-01-25 | F. Hoffmann-La Roche Ag | Pyridazinone derivatives as thyroid hormone receptor agonists |
| WO2014043706A1 (en) * | 2012-09-17 | 2014-03-20 | Madrigal Pharmaceuticals, Inc. | Method of synthesizing thyroid hormone analogs and polymorphs thereof |
| CN111320609A (zh) * | 2018-12-13 | 2020-06-23 | 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 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8076334B2 (en) * | 2007-09-20 | 2011-12-13 | Hoffmann-La Roche Inc. | Prodrugs of thyroid hormone analogs |
| PT3807267T (pt) * | 2018-06-12 | 2025-05-22 | Xizang Haisco Pharmaceutical Co Ltd | Agonistas do recetor da hormona da tiroide e usos dos mesmos |
-
2020
- 2020-05-29 CN CN202080051869.2A patent/CN114174282A/zh active Pending
- 2020-05-29 WO PCT/CN2020/093284 patent/WO2020239076A1/zh active Application Filing
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007009913A1 (en) * | 2005-07-21 | 2007-01-25 | F. Hoffmann-La Roche Ag | Pyridazinone derivatives as thyroid hormone receptor agonists |
| WO2014043706A1 (en) * | 2012-09-17 | 2014-03-20 | Madrigal Pharmaceuticals, Inc. | Method of synthesizing thyroid hormone analogs and polymorphs thereof |
| CN111320609A (zh) * | 2018-12-13 | 2020-06-23 | 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 |
Non-Patent Citations (1)
| Title |
|---|
| MARTHA J. KELLY等: "Discovery of 2-[3, 5-Dichloro-4-(5-isopropyl-6-oxo-1, 6-dihydropyridazin-3-yloxy)phenyl]-3, 5-dioxo-2, 3, 4, 5-tetrahydro[1, 2, 4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β Agonist in Clinical Trials for the Treatment of Dyslipidemia", JOURNAL OF MEDICINAL CHEMISTRY, vol. 57, no. 10, pages 3912, XP055436939, DOI: 10.1021/jm4019299 * |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2020239076A1 (zh) | 2020-12-03 |
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| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20220311 |
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