TWI874616B - Taar1促效劑的鹽類及結晶形式 - Google Patents

Taar1促效劑的鹽類及結晶形式 Download PDF

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Publication number
TWI874616B
TWI874616B TW110109520A TW110109520A TWI874616B TW I874616 B TWI874616 B TW I874616B TW 110109520 A TW110109520 A TW 110109520A TW 110109520 A TW110109520 A TW 110109520A TW I874616 B TWI874616 B TW I874616B
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TW
Taiwan
Prior art keywords
methyl
ethyl
pyrazole
phenyl
carboxamide
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TW110109520A
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English (en)
Chinese (zh)
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TW202140466A (zh
Inventor
克里斯藤 安卓 葛雷瑟
厄爾 舒維特
法蘭克 史都瓦舍
芙洛恩斯 妮可 安東妮爾特 提克斯恩特
蕾尼 楚莎迪
Original Assignee
瑞士商赫孚孟拉羅股份公司
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    • 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
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
TW110109520A 2020-03-19 2021-03-17 Taar1促效劑的鹽類及結晶形式 TWI874616B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP20164069 2020-03-19
EP20164069.5 2020-03-19

Publications (2)

Publication Number Publication Date
TW202140466A TW202140466A (zh) 2021-11-01
TWI874616B true TWI874616B (zh) 2025-03-01

Family

ID=69846246

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TW110109520A TWI874616B (zh) 2020-03-19 2021-03-17 Taar1促效劑的鹽類及結晶形式

Country Status (13)

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US (1) US20230120311A1 (https=)
EP (1) EP4121428B1 (https=)
JP (2) JP2023517729A (https=)
KR (1) KR20220155575A (https=)
CN (1) CN115279752A (https=)
AU (1) AU2021238632A1 (https=)
BR (1) BR112022016746A2 (https=)
CA (1) CA3166331A1 (https=)
ES (1) ES3044409T3 (https=)
IL (1) IL294301A (https=)
MX (1) MX2022010794A (https=)
TW (1) TWI874616B (https=)
WO (1) WO2021185878A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2023323858A1 (en) * 2022-08-12 2024-11-21 F. Hoffmann-La Roche Ag Pharmaceutical compositions comprising 5-ethyl-4-methyl- n-[4-[(2 s) morpholin-2-yl]phenyl]-1h-pyrazole-3-carboxamide
WO2024222860A1 (zh) * 2023-04-28 2024-10-31 江苏豪森药业集团有限公司 一种吗啉杂环类化合物的盐及其制备方法和应用
CN117903050B (zh) * 2024-03-15 2024-05-17 中国药科大学 阿立哌唑共晶及其药物组合物和应用

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017157873A1 (en) * 2016-03-17 2017-09-21 F. Hoffmann-La Roche Ag 5-ethyl-4-methyl-pyrazole-3-carboxamide derivative having activity as agonist of taar

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5323907A (en) 1992-06-23 1994-06-28 Multi-Comp, Inc. Child resistant package assembly for dispensing pharmaceutical medications

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017157873A1 (en) * 2016-03-17 2017-09-21 F. Hoffmann-La Roche Ag 5-ethyl-4-methyl-pyrazole-3-carboxamide derivative having activity as agonist of taar

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
專書 Caira M.R. et al. "Crystalline Polymorphism of Organic Compounds." vol 198:163-208, In: Weber E. et al. (eds) Design of Organic Solids. Topics in Current Chemistry.Springer, Berlin, Heidelberg. First Online: 01 January 1999.; *
期刊 Richard J. Bastin, et al. " Salt Selection and Optimisation Procedures for Pharmaceutical New Chemical Entities." Org. Proc. Res. 4, 5, Dev. 2000, 427-435. *

Also Published As

Publication number Publication date
JP2023517729A (ja) 2023-04-26
CA3166331A1 (en) 2021-09-23
EP4121428A1 (en) 2023-01-25
BR112022016746A2 (pt) 2022-10-11
WO2021185878A1 (en) 2021-09-23
KR20220155575A (ko) 2022-11-23
US20230120311A1 (en) 2023-04-20
EP4121428B1 (en) 2025-08-13
IL294301A (en) 2022-08-01
AU2021238632A1 (en) 2022-07-14
TW202140466A (zh) 2021-11-01
ES3044409T3 (en) 2025-11-26
EP4121428C0 (en) 2025-08-13
CN115279752A (zh) 2022-11-01
MX2022010794A (es) 2022-09-27
JP2025166092A (ja) 2025-11-05

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