CR20220371A - Agonistas heterocíclicos de glp-1 - Google Patents

Agonistas heterocíclicos de glp-1

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Publication number
CR20220371A
CR20220371A CR20220371A CR20220371A CR20220371A CR 20220371 A CR20220371 A CR 20220371A CR 20220371 A CR20220371 A CR 20220371A CR 20220371 A CR20220371 A CR 20220371A CR 20220371 A CR20220371 A CR 20220371A
Authority
CR
Costa Rica
Prior art keywords
glp
agonists
heterocyclic
solvates
formula
Prior art date
Application number
CR20220371A
Other languages
English (en)
Inventor
Xichen Lin
Weiqiang Xing
Andrew John Jennings
Haizhen Zhang
Qinghua Meng
Hui Lei
Original Assignee
Gasherbrum Bio 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 Gasherbrum Bio Inc filed Critical Gasherbrum Bio Inc
Publication of CR20220371A publication Critical patent/CR20220371A/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • 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
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/26—Glucagons
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6568—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus atoms as the only ring hetero atoms
    • C07F9/65685—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus atoms as the only ring hetero atoms the ring phosphorus atom being part of a phosphine oxide or thioxide
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6581—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
    • C07F9/6584—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Esta divulgacion se refiere a agonistas de GLP-1 de la Formula (<strong>I</strong>): Formula (<strong>I</strong>), <img src="data:image/png;base64,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 (***)
CR20220371A 2020-02-07 2021-02-05 Agonistas heterocíclicos de glp-1 CR20220371A (es)

Applications Claiming Priority (3)

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CN2020074537 2020-02-07
CN2020109304 2020-08-14
PCT/CN2021/075488 WO2021155841A1 (en) 2020-02-07 2021-02-05 Heterocyclic glp-1 agonists

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CR20220371A true CR20220371A (es) 2022-10-27

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US (2) US11492365B2 (es)
EP (1) EP4097099B1 (es)
JP (1) JP2023513272A (es)
KR (1) KR20220156535A (es)
CN (1) CN115698003B (es)
AU (1) AU2021216324A1 (es)
CA (1) CA3169975A1 (es)
CL (1) CL2022002105A1 (es)
CO (1) CO2022011065A2 (es)
CR (1) CR20220371A (es)
DK (1) DK4097099T3 (es)
DO (1) DOP2022000158A (es)
FI (1) FI4097099T3 (es)
IL (1) IL295281A (es)
MX (1) MX2022009524A (es)
PE (1) PE20231066A1 (es)
PT (1) PT4097099T (es)
RS (1) RS65877B1 (es)
TW (1) TW202142538A (es)
WO (1) WO2021155841A1 (es)

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CR20220371A (es) 2020-02-07 2022-10-27 Gasherbrum Bio Inc Agonistas heterocíclicos de glp-1
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WO2022202864A1 (ja) 2021-03-24 2022-09-29 塩野義製薬株式会社 縮合環を有するｇｌｐ－１受容体作動薬を含有する医薬組成物
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WO2024125602A1 (en) 2022-12-15 2024-06-20 Gasherbrum Bio, Inc. Salts and solid forms of a compound having glp-1 agonist activity
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