PE20211788A1 - Compuesto agonista de receptor thrb y metodo de preparacion y uso del mismo - Google Patents
Compuesto agonista de receptor thrb y metodo de preparacion y uso del mismoInfo
- Publication number
- PE20211788A1 PE20211788A1 PE2021000858A PE2021000858A PE20211788A1 PE 20211788 A1 PE20211788 A1 PE 20211788A1 PE 2021000858 A PE2021000858 A PE 2021000858A PE 2021000858 A PE2021000858 A PE 2021000858A PE 20211788 A1 PE20211788 A1 PE 20211788A1
- Authority
- PE
- Peru
- Prior art keywords
- substituted
- unsubstituted
- halogen
- alkyl
- compound
- Prior art date
Links
Classifications
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- 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
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- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- 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
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C07D237/30—Phthalazines
- C07D237/32—Phthalazines with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Gastroenterology & Hepatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
La presente invencion describe un compuesto de formula (I) y una sal farmaceuticamente aceptable del mismo; en donde, R1 se selecciona de ciano, C1-6 alquilo sustituido o no sustituido o C3-6 cicloalquilo sustituido o no sustituido; R2 y R3 se seleccionan independientemente de halogeno o C1-6 alquilo sustituido o no sustituido, en donde el sustituyente se selecciona de halogeno, hidroxi y C1-6 alcoxi; el anillo A es un C5-10 anillo alifatico saturado o insaturado sustituido o no, o un C5-10 anillo aromatico sustituido o no, donde el sustituyente es seleccionado de hidrogeno, halogeno, hidroxi, -OCF3, -NH2, -NHC1-4 alquilo, -N(C1-4 alquilo)2, entre otros, y cuando se contienen dos sustituyentes, pueden formar una estructura de anillo junto con el carbono conectado a los mismos. Un compuesto seleccionado es 2-(3,5-dicloro-4-((4-oxo-3,4,5,6,7,8-hexahidroftalazin1-il)oxi)fenil)-3,5-dioxo-2,3,4,5-tetrahidro-1,2,4-triazina-6-nitrilo. Dichos compuestos mejoran la selectividad de THRalfa en tanto que mantienen una buena actividad agonista de THRbeta, siendo utiles para el tratamiento de una enfermedad relacionada con el metabolismo, tales como obesidad, hiperlipidemia, hipercolesterolemia, diabetes y esteatohepatitis no alcoholica (NASH), esteatosis de higado, aterosclerosis, hipotiroidismo y cancer de tiroides.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811527414.4A CN111320609A (zh) | 2018-12-13 | 2018-12-13 | 一种THRβ受体激动剂化合物及其制备方法和用途 |
| PCT/US2019/066013 WO2020123827A1 (en) | 2018-12-13 | 2019-12-12 | Thrβ receptor agonist compound and preparation method and use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20211788A1 true PE20211788A1 (es) | 2021-09-09 |
Family
ID=71071432
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2021000858A PE20211788A1 (es) | 2018-12-13 | 2019-12-12 | Compuesto agonista de receptor thrb y metodo de preparacion y uso del mismo |
Country Status (19)
| Country | Link |
|---|---|
| US (5) | US11084802B2 (es) |
| EP (3) | EP3893889A4 (es) |
| JP (2) | JP7532371B2 (es) |
| KR (2) | KR20250133486A (es) |
| CN (4) | CN121081472A (es) |
| AR (1) | AR117694A1 (es) |
| AU (2) | AU2019398339C1 (es) |
| BR (1) | BR112021010871A2 (es) |
| CA (1) | CA3120880A1 (es) |
| CL (1) | CL2021001521A1 (es) |
| CO (1) | CO2021008817A2 (es) |
| IL (2) | IL283362B2 (es) |
| MA (1) | MA54471A (es) |
| MX (2) | MX2021006908A (es) |
| MY (1) | MY207657A (es) |
| PE (1) | PE20211788A1 (es) |
| SG (1) | SG11202106194TA (es) |
| TW (1) | TWI837244B (es) |
| WO (1) | WO2020123827A1 (es) |
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| 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 |
| AU2020267576B2 (en) | 2019-05-08 | 2025-03-13 | Aligos Therapeutics, Inc. | Modulators of THR-β and methods of use thereof |
| WO2020228577A1 (zh) * | 2019-05-10 | 2020-11-19 | 深圳微芯生物科技股份有限公司 | 一种哒嗪酮衍生物及其应用 |
| CN114174282A (zh) * | 2019-05-29 | 2022-03-11 | 南京明德新药研发有限公司 | 作为甲状腺素受体-β激动剂的哒嗪酮类衍生物及其应用 |
| CA3154391A1 (en) | 2019-09-12 | 2021-03-18 | Terns Pharmaceuticals, Inc. | Thyroid hormone receptor beta agonist compounds |
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