TWI769532B - 製造5-(4-((2s,5s)-5-(4-氯芐基)-2-甲基嗎啉基)哌啶-1-基)-1h-1,2,4-三唑-3-胺的方法 - Google Patents

製造5-(4-((2s,5s)-5-(4-氯芐基)-2-甲基嗎啉基)哌啶-1-基)-1h-1,2,4-三唑-3-胺的方法 Download PDF

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TWI769532B
TWI769532B TW109133211A TW109133211A TWI769532B TW I769532 B TWI769532 B TW I769532B TW 109133211 A TW109133211 A TW 109133211A TW 109133211 A TW109133211 A TW 109133211A TW I769532 B TWI769532 B TW I769532B
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Taiwan
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formula
chlorobenzyl
compound
solvent
methylmorpholinyl
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TW109133211A
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English (en)
Chinese (zh)
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TW202126644A (zh
Inventor
格熱戈日 維特科夫斯基
莫塔 梅蒂居
馬格達萊娜 蒂希基維茨
馬辛 扎克熱夫斯基
斯坦尼斯瓦夫 皮庫爾
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波蘭商昂科艾倫迪治療法股份公司
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D211/74—Oxygen atoms
    • 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
    • C07B2200/07—Optical isomers
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
TW109133211A 2019-09-25 2020-09-25 製造5-(4-((2s,5s)-5-(4-氯芐基)-2-甲基嗎啉基)哌啶-1-基)-1h-1,2,4-三唑-3-胺的方法 TWI769532B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201962905494P 2019-09-25 2019-09-25
PL43126919 2019-09-25
PLP-431269 2019-09-25
US62/905,494 2019-09-25

Publications (2)

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TW202126644A TW202126644A (zh) 2021-07-16
TWI769532B true TWI769532B (zh) 2022-07-01

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TW109133211A TWI769532B (zh) 2019-09-25 2020-09-25 製造5-(4-((2s,5s)-5-(4-氯芐基)-2-甲基嗎啉基)哌啶-1-基)-1h-1,2,4-三唑-3-胺的方法
TW111121583A TWI849432B (zh) 2019-09-25 2020-09-25 製造5-(4-((2s,5s)-5-(4-氯芐基)-2-甲基嗎啉基)哌啶-1-基)-1h-1,2,4-三唑-3-胺的方法
TW113127475A TWI892762B (zh) 2019-09-25 2020-09-25 製造5-(4-((2s,5s)-5-(4-氯芐基)-2-甲基嗎啉基)哌啶-1-基)-1h-1,2,4-三唑-3-胺的方法

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TW111121583A TWI849432B (zh) 2019-09-25 2020-09-25 製造5-(4-((2s,5s)-5-(4-氯芐基)-2-甲基嗎啉基)哌啶-1-基)-1h-1,2,4-三唑-3-胺的方法
TW113127475A TWI892762B (zh) 2019-09-25 2020-09-25 製造5-(4-((2s,5s)-5-(4-氯芐基)-2-甲基嗎啉基)哌啶-1-基)-1h-1,2,4-三唑-3-胺的方法

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US (2) US11746107B2 (https=)
EP (1) EP4041726B8 (https=)
JP (1) JP7697933B2 (https=)
KR (1) KR20220069008A (https=)
CN (1) CN114466845B (https=)
AU (1) AU2020356534B2 (https=)
BR (1) BR112022005420A2 (https=)
CA (1) CA3155177A1 (https=)
ES (1) ES3056105T3 (https=)
IL (1) IL291569B2 (https=)
MX (1) MX2022002881A (https=)
PH (1) PH12022550713A1 (https=)
PL (1) PL4041726T3 (https=)
TW (3) TWI769532B (https=)
WO (1) WO2021059220A1 (https=)
ZA (1) ZA202204542B (https=)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2022002881A (es) 2019-09-25 2022-06-08 Oncoarendi Therapeutics Sa Proceso para la produccion de 5-(4-((2s,5s)-5-(4-clorobencil)-2-me tilmorfolino)piperidin-1-il)-1h-1,2,4-triazol-3-amina.

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI289554B (en) * 1999-12-17 2007-11-11 Sanofi Aventis Novel branched substituted amino derivatives of 3-amino-1-phenyl-H[1,2,4]triazole, process for their preparation and pharmaceutical compositions comprising them
TW201402564A (zh) * 2012-05-30 2014-01-16 Hoffmann La Roche 三唑化合物
WO2017037670A1 (en) * 2015-09-04 2017-03-09 OncoArendi Therapeutics Sp. z o.o. Substituted amino triazoles useful as human chitinase inhibitors

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE354568T1 (de) * 2000-08-08 2007-03-15 Ortho Mcneil Pharm Inc Nicht-imidazol aryloxypiperidine als h3 rezeptor liganden
EP3082805B1 (en) * 2013-12-20 2020-02-05 Institute for Drug Discovery, LLC Substituted amino triazoles, and methods using same
US9440953B2 (en) 2014-12-19 2016-09-13 OncoArendi Therapeutics Sp. z o.o. Substituted amino triazoles useful as acidic mammalian chitinase inhibitors
GB201513740D0 (en) * 2015-08-03 2015-09-16 Heptares Therapeutics Ltd Muscarinic agonist
MX2022000306A (es) 2019-07-15 2022-03-11 Oncoarendi Therapeutics Sa Amino triazoles sustituidos utiles como inhibidores de quitinasa.
MX2022002881A (es) 2019-09-25 2022-06-08 Oncoarendi Therapeutics Sa Proceso para la produccion de 5-(4-((2s,5s)-5-(4-clorobencil)-2-me tilmorfolino)piperidin-1-il)-1h-1,2,4-triazol-3-amina.

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI289554B (en) * 1999-12-17 2007-11-11 Sanofi Aventis Novel branched substituted amino derivatives of 3-amino-1-phenyl-H[1,2,4]triazole, process for their preparation and pharmaceutical compositions comprising them
TW201402564A (zh) * 2012-05-30 2014-01-16 Hoffmann La Roche 三唑化合物
WO2017037670A1 (en) * 2015-09-04 2017-03-09 OncoArendi Therapeutics Sp. z o.o. Substituted amino triazoles useful as human chitinase inhibitors

Also Published As

Publication number Publication date
JP2022549863A (ja) 2022-11-29
PL4041726T3 (pl) 2026-02-23
ZA202204542B (en) 2023-01-25
EP4041726B1 (en) 2025-09-17
EP4041726A1 (en) 2022-08-17
CN114466845B (zh) 2024-12-17
IL291569B1 (en) 2024-12-01
EP4041726C0 (en) 2025-09-17
TW202448877A (zh) 2024-12-16
IL291569A (en) 2022-05-01
PH12022550713A1 (en) 2024-02-12
IL291569B2 (en) 2025-04-01
JP7697933B2 (ja) 2025-06-24
WO2021059220A1 (en) 2021-04-01
CA3155177A1 (en) 2021-04-01
EP4041726B8 (en) 2025-11-26
US20210147401A1 (en) 2021-05-20
CN114466845A (zh) 2022-05-10
TW202126644A (zh) 2021-07-16
US20240025889A1 (en) 2024-01-25
BR112022005420A2 (pt) 2022-06-21
AU2020356534A1 (en) 2022-05-19
TWI849432B (zh) 2024-07-21
ES3056105T3 (en) 2026-02-18
US11746107B2 (en) 2023-09-05
US12319677B2 (en) 2025-06-03
MX2022002881A (es) 2022-06-08
AU2020356534B2 (en) 2026-04-09
KR20220069008A (ko) 2022-05-26
TWI892762B (zh) 2025-08-01
TW202237594A (zh) 2022-10-01

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