AU2022271223A1 - Benzimidazoyl glp-1 receptor agonists, pharmaceutical compositions comprising the same, and methods for their use - Google Patents

Benzimidazoyl glp-1 receptor agonists, pharmaceutical compositions comprising the same, and methods for their use Download PDF

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Publication number
AU2022271223A1
AU2022271223A1 AU2022271223A AU2022271223A AU2022271223A1 AU 2022271223 A1 AU2022271223 A1 AU 2022271223A1 AU 2022271223 A AU2022271223 A AU 2022271223A AU 2022271223 A AU2022271223 A AU 2022271223A AU 2022271223 A1 AU2022271223 A1 AU 2022271223A1
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AU
Australia
Prior art keywords
alkyl
methyl
substituted
compound
certain embodiments
Prior art date
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Abandoned
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AU2022271223A
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English (en)
Inventor
Xiaohui Du
Ray FUCINI
Sumanta GARAI
Hiroyuki Kawai
Craig Lee
Xu RAN
Subas Man Sakya
Xiaofang Wang
Chien-Hung Yeh
Xiang Zhou
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Carmot Therapeutics Inc
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Carmot Therapeutics Inc
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Publication date
Application filed by Carmot Therapeutics Inc filed Critical Carmot Therapeutics Inc
Publication of AU2022271223A1 publication Critical patent/AU2022271223A1/en
Abandoned legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2022271223A 2021-05-03 2022-05-03 Benzimidazoyl glp-1 receptor agonists, pharmaceutical compositions comprising the same, and methods for their use Abandoned AU2022271223A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US202163183612P 2021-05-03 2021-05-03
US63/183,612 2021-05-03
US202163282686P 2021-11-24 2021-11-24
US63/282,686 2021-11-24
PCT/US2022/027535 WO2022235717A1 (en) 2021-05-03 2022-05-03 Benzimidazoyl glp-1 receptor agonists, pharmaceutical compositions comprising the same, and methods for their use

Publications (1)

Publication Number Publication Date
AU2022271223A1 true AU2022271223A1 (en) 2023-11-02

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Family Applications (1)

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AU2022271223A Abandoned AU2022271223A1 (en) 2021-05-03 2022-05-03 Benzimidazoyl glp-1 receptor agonists, pharmaceutical compositions comprising the same, and methods for their use

Country Status (8)

Country Link
US (2) US20220396569A1 (https=)
EP (2) EP4334304A1 (https=)
JP (1) JP2024516291A (https=)
AU (1) AU2022271223A1 (https=)
BR (1) BR112023022836A2 (https=)
CA (1) CA3217720A1 (https=)
MX (1) MX2023012918A (https=)
WO (1) WO2022235717A1 (https=)

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Publication number Priority date Publication date Assignee Title
CA3192601A1 (en) * 2020-08-21 2022-02-24 Terns Pharmaceuticals, Inc. Compounds as glp-1r agonists
WO2023029380A1 (zh) 2021-08-30 2023-03-09 杭州德睿智药科技有限公司 作为glp1r激动剂的新型芳醚取代杂环类化合物
PT4408840T (pt) 2021-09-27 2025-10-07 Terns Pharmaceuticals Inc Ácidos benzimidazolocarboxílicos como agonistas de glp-1r
CN118401519A (zh) 2021-10-25 2024-07-26 拓臻制药公司 作为glp-1r激动剂的化合物
US20250042882A1 (en) 2021-12-16 2025-02-06 Astrazeneca Ab Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators
WO2023111144A1 (en) 2021-12-16 2023-06-22 Astrazeneca Ab Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators
CN119095843A (zh) 2022-02-23 2024-12-06 拓臻制药公司 作为glp-1r激动剂的化合物
CN117362282B (zh) * 2022-07-07 2026-04-21 杭州德睿智药科技有限公司 Glp-1r激动剂的盐及其制备方法和应用
EP4562006A1 (en) * 2022-07-27 2025-06-04 Carmot Therapeutics, Inc. N-heterocylic gpcr receptor agonists, pharmaceutical compositions comprising the same, and methods for their use
WO2024051700A1 (zh) * 2022-09-05 2024-03-14 德睿智药(苏州)新药研发有限公司 作为glp1r激动剂的新型芳基氘代苄醚取代杂环类化合物
EP4592285A1 (en) 2022-09-22 2025-07-30 Shionogi & Co., Ltd. Fused ring compound having glp-1 receptor agonist effect
KR20250085816A (ko) 2022-11-16 2025-06-12 일라이 릴리 앤드 캄파니 글루카곤-유사 펩티드 1 수용체 효능제
CN116217522B (zh) * 2023-02-22 2025-06-24 广东莱佛士制药技术有限公司 Glp-1受体激动剂关键中间体的手性纯化方法
EP4568664B1 (en) 2023-04-07 2026-04-01 Terns Pharmaceuticals, Inc. Combination comprising a thr-beta agonist and a glp-1r agonist for use in treating obesity
CN120981457A (zh) 2023-09-14 2025-11-18 歌礼制药(中国)有限公司 Glp-1r激动剂及其治疗方法
TW202521534A (zh) 2023-11-24 2025-06-01 香港商歌禮製藥(中國)有限公司 Glp-1r 激動劑及其治療方法
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
TW202600132A (zh) 2024-03-08 2026-01-01 美商安尼波那生物公司 用於治療肥胖症及提高減重之方法
WO2026073030A1 (en) 2024-09-27 2026-04-02 Carmot Therapeutics Inc. Combination therapy of peptide tyrosine-tyrosine (pyy) analogues and glp-1r agonists

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US20060275288A1 (en) 2005-01-20 2006-12-07 Grihalde Nelson D GLP-1 receptor agonist and allosteric modulator monoclonal antibodies and uses thereof
US20120148586A1 (en) 2009-08-27 2012-06-14 Joyce Ching Tsu Chou Glucagon-like protein-1 receptor (glp-1r) agonists for treating autoimmune disorders
US20120021979A1 (en) 2010-06-24 2012-01-26 Vanderbilt University GLP-1 receptor modulation of addiction, neuropsychiatric disorders and erectile dysfunction
KR102314286B1 (ko) * 2016-12-16 2021-10-21 화이자 인코포레이티드 Glp-1 수용체 작용제 및 이의 용도
US10934279B2 (en) * 2018-06-13 2021-03-02 Pfizer Inc. GLP-1 receptor agonists and uses thereof
MA54555A (fr) * 2018-11-22 2021-09-29 Qilu Regor Therapeutics Inc Agonistes de glp-1r et leurs utilisations
EP3953344A4 (en) * 2019-04-12 2023-08-09 Qilu Regor Therapeutics Inc. GLP-IR AGONISTS AND THEIR USES
WO2020234726A1 (en) * 2019-05-20 2020-11-26 Pfizer Inc. Combinations comprising benzodioxol as glp-1r agonists for use in the treatment of nash/nafld and related diseases
TWI751585B (zh) * 2019-06-28 2022-01-01 美商美國禮來大藥廠 類升糖素肽1受體促效劑
WO2021096284A1 (ko) * 2019-11-15 2021-05-20 일동제약(주) Glp-1 수용체 작용제 및 이의 용도
CN114761395B (zh) * 2019-12-02 2024-11-15 现代药品株式会社 Glp-1受体激动剂

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Publication number Publication date
EP4334304A1 (en) 2024-03-13
CA3217720A1 (en) 2022-11-10
WO2022235717A1 (en) 2022-11-10
BR112023022836A2 (pt) 2024-01-16
US20240262811A1 (en) 2024-08-08
EP4461355A3 (en) 2025-01-15
MX2023012918A (es) 2024-03-13
US20220396569A1 (en) 2022-12-15
JP2024516291A (ja) 2024-04-12
EP4461355A2 (en) 2024-11-13

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