CA3161509A1 - Preparation of trifarotene and intermediates and polymorphs thereof - Google Patents

Preparation of trifarotene and intermediates and polymorphs thereof Download PDF

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Publication number
CA3161509A1
CA3161509A1 CA3161509A CA3161509A CA3161509A1 CA 3161509 A1 CA3161509 A1 CA 3161509A1 CA 3161509 A CA3161509 A CA 3161509A CA 3161509 A CA3161509 A CA 3161509A CA 3161509 A1 CA3161509 A1 CA 3161509A1
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CA
Canada
Prior art keywords
trifarotene
formula
substituted
polymorph
compound
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
CA3161509A
Other languages
English (en)
French (fr)
Inventor
Ilana Ozer
Yulia KAFTANOV
Elliot Simhon
Andrey DUSHKIN
Shani SHEFFER DEE-NOOR
Hillel Pizem
Avi Avramoff
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.)
Taro Pharmaceutical Industries Ltd
Original Assignee
Taro Pharmaceutical Industries Ltd
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 Taro Pharmaceutical Industries Ltd filed Critical Taro Pharmaceutical Industries Ltd
Publication of CA3161509A1 publication Critical patent/CA3161509A1/en
Pending legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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
    • C07D207/08Heterocyclic 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 hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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
    • C07D207/06Heterocyclic 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 radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • 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
    • A61K31/40Heterocyclic 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
    • A61K31/4021-aryl substituted, e.g. piretanide
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
CA3161509A 2019-12-11 2020-12-10 Preparation of trifarotene and intermediates and polymorphs thereof Pending CA3161509A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962946943P 2019-12-11 2019-12-11
US62/946,943 2019-12-11
PCT/US2020/064365 WO2021119351A1 (en) 2019-12-11 2020-12-10 Preparation of trifarotene and intermediates and polymorphs thereof

Publications (1)

Publication Number Publication Date
CA3161509A1 true CA3161509A1 (en) 2021-06-17

Family

ID=74141909

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3161509A Pending CA3161509A1 (en) 2019-12-11 2020-12-10 Preparation of trifarotene and intermediates and polymorphs thereof

Country Status (9)

Country Link
US (2) US11691946B2 (https=)
EP (2) EP4073035B1 (https=)
JP (3) JP7281016B2 (https=)
CN (1) CN114787129B (https=)
AU (2) AU2020402049B2 (https=)
CA (1) CA3161509A1 (https=)
ES (1) ES3037292T3 (https=)
IL (2) IL293800B2 (https=)
WO (1) WO2021119351A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL293800B2 (en) * 2019-12-11 2024-10-01 Taro Pharma Ind Preparation of trifarotene and intermediates and polymorphs thereof
CN117342993A (zh) * 2022-07-05 2024-01-05 石家庄迪斯凯威医药科技有限公司 一种曲法罗汀盐及其药物组合物和用途
CN115745913B (zh) * 2022-09-16 2024-05-24 南京迈诺威医药科技有限公司 曲法罗汀多晶型及其制备方法
JP2026507122A (ja) * 2023-02-28 2026-02-27 タロー・ファーマシューティカル・インダストリーズ・リミテッド トリファロテンを調製する方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1248869A2 (en) * 2000-01-07 2002-10-16 Transform Pharmaceuticals, Inc. High-throughput formation, identification, and analysis of diverse solid-forms
WO2004083335A2 (en) * 2003-03-21 2004-09-30 University Of Rochester Glassy chiral-nematic liquid crystals and optical devices containing same
US8354427B2 (en) 2004-06-24 2013-01-15 Vertex Pharmaceutical Incorporated Modulators of ATP-binding cassette transporters
DK1817301T3 (da) * 2004-11-22 2012-02-27 Lilly Co Eli Forstærkere af glutamat-receptorer
PL1831149T3 (pl) * 2004-12-23 2012-06-29 Galderma Res & Dev Nowe ligandy, które modulują receptory RAR, i ich zastosowanie w medycynie i kosmetyce
GB2426247A (en) 2005-05-20 2006-11-22 Arrow Int Ltd Methods of preparing purine derivatives such as famciclovir
EP3475312B1 (en) * 2016-06-23 2020-05-27 Galderma S.A. Cyclodextrin-grafted cross-linked hyaluronic acid complexed with active drug substances and uses thereof
IL293800B2 (en) * 2019-12-11 2024-10-01 Taro Pharma Ind Preparation of trifarotene and intermediates and polymorphs thereof

Also Published As

Publication number Publication date
JP2026016786A (ja) 2026-02-03
IL293800A (en) 2022-08-01
JP2022550632A (ja) 2022-12-02
EP4552691A3 (en) 2025-09-10
IL293800B1 (en) 2024-06-01
WO2021119351A1 (en) 2021-06-17
US20230051259A1 (en) 2023-02-16
CN114787129B (zh) 2025-07-04
AU2023222982B2 (en) 2025-01-02
EP4073035B1 (en) 2025-05-07
NZ788464A (en) 2024-07-05
IL293800B2 (en) 2024-10-01
EP4073035A1 (en) 2022-10-19
US11691946B2 (en) 2023-07-04
IL312356A (en) 2024-06-01
JP7281016B2 (ja) 2023-05-24
JP2023100974A (ja) 2023-07-19
EP4552691A2 (en) 2025-05-14
AU2020402049B2 (en) 2023-06-01
CN114787129A (zh) 2022-07-22
AU2023222982A1 (en) 2023-09-21
US20230278956A1 (en) 2023-09-07
AU2020402049A1 (en) 2022-06-09
ES3037292T3 (en) 2025-09-30

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