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 PDF

Info

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
reaction
added
compound
independently selected
ethyl acetate
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
Application number
CN202080051869.2A
Other languages
English (en)
Chinese (zh)
Inventor
于涛
张盛彬
吴成德
李婕
黎健
陈曙辉
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Medshine Discovery Inc
Original Assignee
Medshine Discovery Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Medshine Discovery Inc filed Critical Medshine Discovery Inc
Publication of CN114174282A publication Critical patent/CN114174282A/zh
Pending legal-status Critical Current

Links

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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN202080051869.2A 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 Pending CN114174282A (zh)

Applications Claiming Priority (13)

Application Number Priority Date Filing Date Title
CN201910459299X 2019-05-29
CN201910459299 2019-05-29
CN201910741177X 2019-08-12
CN201910741177 2019-08-12
CN201911130068 2019-11-18
CN2019111300680 2019-11-18
CN2020100765259 2020-01-23
CN202010076525 2020-01-23
CN202010188909X 2020-03-17
CN202010188909 2020-03-17
CN202010409420 2020-05-14
CN2020104094200 2020-05-14
PCT/CN2020/093284 WO2020239076A1 (fr) 2019-05-29 2020-05-29 DÉRIVÉS DE PYRIDAZINONE CONSTITUANT DES AGONISTES DU RÉCEPTEUR DE LA THYROXINE DE TYPE β ET LEUR UTILISATION

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 (fr)
WO (1) WO2020239076A1 (fr)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA53868A (fr) 2018-10-12 2021-08-18 Terns Inc Composés agonistes du récepteur bêta des hormones thyroïdiennes
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
AU2021374988A1 (en) 2020-11-06 2023-06-15 Aligos Therapeutics, Inc. Bicyclic pyridazinones as thyroid hormone receptor beta (tr-beta) agonists
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
CA3229539A1 (fr) 2021-08-25 2023-03-02 Xiaoyan Zhang Inhibiteurs de nlrp3
WO2023147779A1 (fr) * 2022-02-07 2023-08-10 四川海思科制药有限公司 Procédé de préparation d'un dérivé de pyridazinone, et intermédiaire de celui-ci

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007009913A1 (fr) * 2005-07-21 2007-01-25 F. Hoffmann-La Roche Ag Derives de pyridazinone utilises comme agonistes du recepteur de l'hormone thyroidienne
WO2014043706A1 (fr) * 2012-09-17 2014-03-20 Madrigal Pharmaceuticals, Inc. Procédé de synthèse d'analogues de l'hormone thyroïdienne et de ses polymorphes
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)

* Cited by examiner, † Cited by third party
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
WO2019240938A1 (fr) * 2018-06-12 2019-12-19 Fronthera U.S. Pharmaceuticals Llc Agonistes du récepteur de l'hormone thyroïdienne et utilisations associées

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007009913A1 (fr) * 2005-07-21 2007-01-25 F. Hoffmann-La Roche Ag Derives de pyridazinone utilises comme agonistes du recepteur de l'hormone thyroidienne
WO2014043706A1 (fr) * 2012-09-17 2014-03-20 Madrigal Pharmaceuticals, Inc. Procédé de synthèse d'analogues de l'hormone thyroïdienne et de ses polymorphes
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)

* Cited by examiner, † Cited by third party
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 (fr) 2020-12-03

Similar Documents

Publication Publication Date Title
CN114174282A (zh) 作为甲状腺素受体-β激动剂的哒嗪酮类衍生物及其应用
CN112533916B (zh) 一种作用于crbn蛋白的三并环类化合物
CN110446712B (zh) 作为A2A受体抑制剂的[1,2,4]三唑并[1,5-c]嘧啶衍生物
CN115702156A (zh) 吡啶酰胺类化合物
AU2017359025A1 (en) Cyclobutane- and azetidine-containing mono and spirocyclic compounds as alpha V integrin inhibitors
CN112654619B (zh) 三环并呋喃取代哌啶二酮类化合物
TW201938556A (zh) 化合物及它們在治療癌症中之用途
CN104812748A (zh) 二氢吡唑gpr40调节剂
CN111344282A (zh) 喹唑啉酮类化合物及其应用
CN114105950A (zh) 吡唑类化合物及其应用
CN115772180A (zh) 戊二酰亚胺类化合物与其应用
WO2021129817A1 (fr) Composé à base de pyrimidine ayant un effet inhibiteur de la cétohexokinase (chk)
WO2023001069A1 (fr) Composés amides macrocycliques et leur application
CN103508931A (zh) 六氢并环戊二烯衍生物、其制备方法及其在医药上的应用
CN117337278A (zh) 烷基羧酸化合物及其应用
CN112601746A (zh) 吡唑并嘧啶衍生物及其作为pi3k抑制剂的应用
WO2023208127A1 (fr) Composé bicyclique substitué par hétéroaryle et son utilisation
JP7299408B2 (ja) ＳＧＬＴｓ／ＤＰＰ４阻害剤およびその使用
CN114096245B (zh) 作为ccr2/ccr5拮抗剂的杂环烷基类化合物
CN111148515A (zh) 2,6-二氧杂螺[4,5]癸烷类衍生物、其制备方法及其在医药上的应用
CN112955453B (zh) 作为选择性Trk抑制剂的吡唑并嘧啶衍生物
CN114555600A (zh) 作为cdk2/4/6三重抑制剂的氨基嘧啶类化合物
TWI814092B (zh) 稠合的三并環衍生物及其在藥學上的應用
CN112752749B (zh) 作为pd-l1免疫调节剂的氟乙烯基苯甲酰胺基化合物
CN115515963A (zh) 嘧啶三并环类化合物及其应用

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination