CR20250437A - Antagonistas del receptor de polipéptido insulinotrópico dependiente de glucosa y usos de estos - Google Patents

Antagonistas del receptor de polipéptido insulinotrópico dependiente de glucosa y usos de estos

Info

Publication number
CR20250437A
CR20250437A CR20250437A CR20250437A CR20250437A CR 20250437 A CR20250437 A CR 20250437A CR 20250437 A CR20250437 A CR 20250437A CR 20250437 A CR20250437 A CR 20250437A CR 20250437 A CR20250437 A CR 20250437A
Authority
CR
Costa Rica
Prior art keywords
glucose
receptor antagonists
polypeptide receptor
dependent insulin
tropic
Prior art date
Application number
CR20250437A
Other languages
English (en)
Inventor
Steven Victor O'neil
Yang Wang
Alsina Luis Angel Martinez
Samuel Michael Levi
Qifang Li
Matthew Richard Reese
Danica Antonia Rankic
Kevin James Filipski
Matthew Forrest Sammons
Advaita Panchagnula
Yanfei Guan
Lei Zhang
Ethan Lawrence Fisher
Original Assignee
Pfizer
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 Pfizer filed Critical Pfizer
Publication of CR20250437A publication Critical patent/CR20250437A/es

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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61P3/08—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

En la presente se describen compuestos de la Fórmula I: I y sus sales aceptables desde el punto de vista farmacéutico, en donde R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, L<sup>1</sup>, T<sup>1</sup>, T<sup>2</sup>, T<sup>3</sup>, T<sup>4</sup>, t1 y t2 se definen en la presente; su uso como antagonistas de GIPR; composiciones farmacéuticas que contienen tales compuestos y sales; y el uso de tales compuestos y sales para tratar o prevenir, por ejemplo, la obesidad, el aumento de peso y/o T2DM.
CR20250437A 2023-04-14 2024-04-11 Antagonistas del receptor de polipéptido insulinotrópico dependiente de glucosa y usos de estos CR20250437A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202363496232P 2023-04-14 2023-04-14
US202363598698P 2023-11-14 2023-11-14
PCT/IB2024/053554 WO2024214038A1 (en) 2023-04-14 2024-04-11 Glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof

Publications (1)

Publication Number Publication Date
CR20250437A true CR20250437A (es) 2025-12-09

Family

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Family Applications (1)

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CR20250437A CR20250437A (es) 2023-04-14 2024-04-11 Antagonistas del receptor de polipéptido insulinotrópico dependiente de glucosa y usos de estos

Country Status (14)

Country Link
US (1) US20240366598A1 (es)
EP (1) EP4695226A1 (es)
KR (1) KR20250172881A (es)
CN (1) CN121311466A (es)
AU (1) AU2024250528A1 (es)
CL (1) CL2025003141A1 (es)
CO (1) CO2025014087A2 (es)
CR (1) CR20250437A (es)
DO (1) DOP2025000260A (es)
IL (1) IL323689A (es)
MX (1) MX2025012216A (es)
PE (1) PE20252756A1 (es)
TW (1) TWI910597B (es)
WO (1) WO2024214038A1 (es)

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WO2025158284A1 (en) * 2024-01-24 2025-07-31 Pfizer Inc. Combination therapy using glucose-dependent insulinotropic polypeptide receptor antagonist compounds and glp-1 receptor agonist peptides
WO2025158275A1 (en) * 2024-01-24 2025-07-31 Pfizer Inc. Combination therapy using glucose-dependent insulinotropic polypeptide receptor antagonist compounds and glp-1 receptor agonist compounds
TW202539633A (zh) * 2024-02-01 2025-10-16 美商輝瑞股份有限公司 葡萄糖依賴性促胰島素多肽受體拮抗劑及其用途
US20250326741A1 (en) * 2024-04-22 2025-10-23 Pfizer Inc. Glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof
WO2026013287A1 (en) 2024-07-12 2026-01-15 Astrazeneca Ab Quinazoline derivatives as gipr antagonists
WO2026042018A1 (en) * 2024-08-21 2026-02-26 Pfizer Inc. 4-{4-[(1-{[4-(propan-2-yl)phenyl]carbamoyl)-d-prolyl)amino]cyclohexyl}benzoic acid derivatives as gipr antagonists for the treatment of diabetes
WO2026078617A1 (en) * 2024-10-11 2026-04-16 Pfizer Inc. Glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof
WO2026078673A1 (en) * 2024-10-13 2026-04-16 Pfizer Inc. Glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof
WO2026078674A1 (en) * 2024-10-13 2026-04-16 Pfizer Inc. Heterocyclic derivatives as glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof
WO2026078672A1 (en) * 2024-10-13 2026-04-16 Pfizer Inc. Glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof
WO2026078671A1 (en) * 2024-10-13 2026-04-16 Pfizer Inc. Heterocyclic compounds as glucose-dependent insulinotropic polypeptide receptor antagonists
WO2026078670A1 (en) * 2024-10-13 2026-04-16 Pfizer Inc. Heterocyclic derivatives as glucose-dependent insulinotropic polypeptide receptor antagonists

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Also Published As

Publication number Publication date
PE20252756A1 (es) 2025-12-05
TWI910597B (zh) 2026-01-01
EP4695226A1 (en) 2026-02-18
CL2025003141A1 (es) 2026-01-16
AU2024250528A1 (en) 2025-10-23
MX2025012216A (es) 2025-11-03
IL323689A (en) 2025-11-01
US20240366598A1 (en) 2024-11-07
DOP2025000260A (es) 2025-11-30
CN121311466A (zh) 2026-01-09
WO2024214038A1 (en) 2024-10-17
TW202446369A (zh) 2024-12-01
CO2025014087A2 (es) 2025-10-30
KR20250172881A (ko) 2025-12-09

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