EP4171233A4 - Crystal forms of 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin -1-yl]ethyl pyridine-3-carboxylate and methods of synthesis - Google Patents

Crystal forms of 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin -1-yl]ethyl pyridine-3-carboxylate and methods of synthesis Download PDF

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Publication number
EP4171233A4
EP4171233A4 EP21833175.9A EP21833175A EP4171233A4 EP 4171233 A4 EP4171233 A4 EP 4171233A4 EP 21833175 A EP21833175 A EP 21833175A EP 4171233 A4 EP4171233 A4 EP 4171233A4
Authority
EP
European Patent Office
Prior art keywords
trimethoxyphenyl
piperazin
carboxylate
synthesis
methyl
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
EP21833175.9A
Other languages
German (de)
English (en)
French (fr)
Other versions
EP4171233A1 (en
Inventor
Neil Buckley
Dan BELMONT
Sarah Bethune
Krista DIAZ
Bryan HAUSER
Myoung Goo Kim
Kumar Kannan
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.)
Imbria Pharmaceuticals Inc
Original Assignee
Imbria Pharmaceuticals 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 Imbria Pharmaceuticals Inc filed Critical Imbria Pharmaceuticals Inc
Publication of EP4171233A1 publication Critical patent/EP4171233A1/en
Publication of EP4171233A4 publication Critical patent/EP4171233A4/en
Pending legal-status Critical Current

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Classifications

    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79Acids; Esters
    • C07D213/80Acids; Esters in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material 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)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
EP21833175.9A 2020-06-30 2021-06-28 Crystal forms of 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin -1-yl]ethyl pyridine-3-carboxylate and methods of synthesis Pending EP4171233A4 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063046123P 2020-06-30 2020-06-30
US202063046120P 2020-06-30 2020-06-30
PCT/US2021/039305 WO2022005928A1 (en) 2020-06-30 2021-06-28 Crystal forms of 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin -1-yl]ethyl pyridine-3-carboxylate and methods of synthesis

Publications (2)

Publication Number Publication Date
EP4171233A1 EP4171233A1 (en) 2023-05-03
EP4171233A4 true EP4171233A4 (en) 2024-08-21

Family

ID=79314883

Family Applications (1)

Application Number Title Priority Date Filing Date
EP21833175.9A Pending EP4171233A4 (en) 2020-06-30 2021-06-28 Crystal forms of 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin -1-yl]ethyl pyridine-3-carboxylate and methods of synthesis

Country Status (8)

Country Link
EP (1) EP4171233A4 (https=)
JP (2) JP7792920B2 (https=)
KR (1) KR20230031320A (https=)
CN (1) CN116056711B (https=)
AU (1) AU2021299266A1 (https=)
CA (1) CA3188286A1 (https=)
IL (1) IL299547A (https=)
WO (1) WO2022005928A1 (https=)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023235297A1 (en) * 2022-06-03 2023-12-07 Imbria Pharmaceuticals, Inc. Compounds and methods for increasing efficiency of cardiac metabolism

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020243120A1 (en) * 2019-05-31 2020-12-03 Imbria Pharmaceuticals, Inc. Methods of treating fibrosis using compounds that promote glucose oxidation
WO2020243119A1 (en) * 2019-05-31 2020-12-03 Imbria Pharmaceuticals, Inc. Methods of altering cardiac remodeling using compounds that promote glucose oxidation

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9169279B2 (en) * 2009-07-31 2015-10-27 Thar Pharmaceuticals, Inc. Crystallization method and bioavailability
CN102850296B (zh) * 2012-09-29 2015-01-07 瑞阳制药有限公司 曲美他嗪的制备方法
IL283725B2 (en) * 2017-06-20 2024-04-01 Imbria Pharmaceuticals Inc Compositions and methods for increasing efficiency of cardiac metabolism

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020243120A1 (en) * 2019-05-31 2020-12-03 Imbria Pharmaceuticals, Inc. Methods of treating fibrosis using compounds that promote glucose oxidation
WO2020243119A1 (en) * 2019-05-31 2020-12-03 Imbria Pharmaceuticals, Inc. Methods of altering cardiac remodeling using compounds that promote glucose oxidation

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of WO2022005928A1 *

Also Published As

Publication number Publication date
JP2026027462A (ja) 2026-02-18
JP2023532330A (ja) 2023-07-27
WO2022005928A1 (en) 2022-01-06
AU2021299266A1 (en) 2023-02-02
JP7792920B2 (ja) 2025-12-26
IL299547A (en) 2023-02-01
CN116056711B (zh) 2026-03-31
EP4171233A1 (en) 2023-05-03
CN116056711A (zh) 2023-05-02
KR20230031320A (ko) 2023-03-07
CA3188286A1 (en) 2022-01-06

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