CN114787129B - 曲法罗汀及其中间体和多晶型物的制备 - Google Patents

曲法罗汀及其中间体和多晶型物的制备 Download PDF

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Publication number
CN114787129B
CN114787129B CN202080085458.5A CN202080085458A CN114787129B CN 114787129 B CN114787129 B CN 114787129B CN 202080085458 A CN202080085458 A CN 202080085458A CN 114787129 B CN114787129 B CN 114787129B
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substituted
formula
faluo
compound
unsubstituted
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Chinese (zh)
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CN114787129A (zh
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I·奥泽尔
Y·卡夫塔诺夫
E·西蒙
A·杜什金
S·谢弗迪诺尔
H·皮泽姆
A·埃弗拉莫夫
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Taro Pharmaceutical Industries Ltd
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Taro Pharmaceutical Industries Ltd
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    • 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
    • C07D207/06—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 radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic 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
    • C07D295/04—Heterocyclic 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
    • C07D295/14—Heterocyclic 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
    • C07D295/155—Heterocyclic 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
    • 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
    • C07D207/08—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 hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • 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
    • A61K31/402—1-aryl substituted, e.g. piretanide
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline 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)
CN202080085458.5A 2019-12-11 2020-12-10 曲法罗汀及其中间体和多晶型物的制备 Active CN114787129B (zh)

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 (2)

Publication Number Publication Date
CN114787129A CN114787129A (zh) 2022-07-22
CN114787129B true CN114787129B (zh) 2025-07-04

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Country Status (9)

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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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004083335A2 (en) * 2003-03-21 2004-09-30 University Of Rochester Glassy chiral-nematic liquid crystals and optical devices containing same
WO2006066978A1 (en) * 2004-12-23 2006-06-29 Galderma Research & Development Novel ligands that modulate rar receptors, and use thereof in human medicine and in cosmetics
CN101061106A (zh) * 2004-11-22 2007-10-24 伊莱利利公司 谷氨酸受体增效剂

Family Cites Families (5)

* 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
US8354427B2 (en) 2004-06-24 2013-01-15 Vertex Pharmaceutical Incorporated Modulators of ATP-binding cassette transporters
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004083335A2 (en) * 2003-03-21 2004-09-30 University Of Rochester Glassy chiral-nematic liquid crystals and optical devices containing same
CN101061106A (zh) * 2004-11-22 2007-10-24 伊莱利利公司 谷氨酸受体增效剂
WO2006066978A1 (en) * 2004-12-23 2006-06-29 Galderma Research & Development Novel ligands that modulate rar receptors, and use thereof in human medicine and in cosmetics

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
CA3161509A1 (en) 2021-06-17
WO2021119351A1 (en) 2021-06-17
US20230051259A1 (en) 2023-02-16
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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