TWI875776B - 作為d1正向異位調節劑之經取代的四氫異喹啉衍生物及其用途 - Google Patents

作為d1正向異位調節劑之經取代的四氫異喹啉衍生物及其用途 Download PDF

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TWI875776B
TWI875776B TW109122035A TW109122035A TWI875776B TW I875776 B TWI875776 B TW I875776B TW 109122035 A TW109122035 A TW 109122035A TW 109122035 A TW109122035 A TW 109122035A TW I875776 B TWI875776 B TW I875776B
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formula
compound
pharmaceutically acceptable
disease
acceptable salt
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TW109122035A
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Chinese (zh)
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TW202115010A (zh
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亞里 阿苔絲
大衛 斯考爾科
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比利時商優稀美生物醫藥股份有限公司
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/12Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
    • C07D217/14Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
    • C07D217/16Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals substituted by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D261/00Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/20Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Anesthesiology (AREA)
  • Addiction (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
TW109122035A 2019-07-01 2020-06-30 作為d1正向異位調節劑之經取代的四氫異喹啉衍生物及其用途 TWI875776B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP19183643.6 2019-07-01
EP19183643 2019-07-01

Publications (2)

Publication Number Publication Date
TW202115010A TW202115010A (zh) 2021-04-16
TWI875776B true TWI875776B (zh) 2025-03-11

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TW109122035A TWI875776B (zh) 2019-07-01 2020-06-30 作為d1正向異位調節劑之經取代的四氫異喹啉衍生物及其用途
TW114104593A TW202537959A (zh) 2019-07-01 2020-06-30 製備四氫異喹啉衍生物之方法

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TW114104593A TW202537959A (zh) 2019-07-01 2020-06-30 製備四氫異喹啉衍生物之方法

Country Status (23)

Country Link
US (1) US20220259179A1 (https=)
EP (1) EP3993794A1 (https=)
JP (1) JP7510444B2 (https=)
KR (1) KR20220029686A (https=)
CN (2) CN117700395A (https=)
AR (1) AR119318A1 (https=)
AU (1) AU2020299953B2 (https=)
BR (1) BR112021022378A2 (https=)
CA (1) CA3139571A1 (https=)
CL (1) CL2021002946A1 (https=)
CO (1) CO2021018155A2 (https=)
EC (1) ECSP21093559A (https=)
IL (2) IL289314B2 (https=)
MA (1) MA56440A (https=)
MX (2) MX2021015873A (https=)
MY (1) MY210361A (https=)
PE (1) PE20221020A1 (https=)
PH (1) PH12021552825A1 (https=)
SA (1) SA521431279B1 (https=)
SG (1) SG11202112537YA (https=)
TW (2) TWI875776B (https=)
WO (1) WO2021001288A1 (https=)
ZA (1) ZA202109193B (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2976784T3 (es) 2020-10-07 2024-08-08 Lilly Co Eli Derivados de fenil-3,4-dihidroisoquinolin-2(1H)-il-etan-1-ona como moduladores alostéricos positivos del receptor de dopamina D1
US20240083925A1 (en) 2020-12-18 2024-03-14 UCB Biopharma SRL Prodrugs of 2-(3,5-Dichloro-1-methyl-indazol-4-yl)-1-[(1S,3R)-3-(hydroxymethyl)-5-(1-hydroxy-1-methyl-ethyl)-1-methyl-3,4-dihydro-1H-isoquinolin-2-yl]ethanone
JP7798891B2 (ja) 2020-12-18 2026-01-14 ユーシービー バイオファルマ エスアールエル D1陽性アロステリック調節因子としての置換テトラヒドロイソキノリン誘導体
WO2022129267A1 (en) * 2020-12-18 2022-06-23 UCB Biopharma SRL Amorphous solid dispersions
EP4304577A1 (en) * 2021-03-09 2024-01-17 Eli Lilly And Co. Use of mevidalen and other d1 positive allosteric modulators for slowing of parkinson's disease progression
WO2026022198A1 (en) 2024-07-25 2026-01-29 UCB Biopharma SRL Process for the preparation of 2-(3,5-dichloro-1-methyl-indazol-4-yl)-1-[(1 s,3 r)-3-(hydroxymethyl)-5-(1-hydroxy-1-methyl-ethyl)-1-methyl-3,4-dihydro-1 h-isoquinolin-2-yl]ethanone monohydrate

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014193781A1 (en) * 2013-05-30 2014-12-04 Eli Lilly And Company 3,4-dihydroisoquinolin-2(1h)-yl compounds
WO2017178377A1 (en) * 2016-04-13 2017-10-19 Ucb Biopharma Sprl Tetrahydroisoquinoline derivatives

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2679735A1 (en) 2007-03-01 2008-09-12 Janssen Pharmaceutica N.V. Tetrahydroisoquinoline compounds as modulators of the histamine h3 receptor
KR101284796B1 (ko) 2011-10-05 2013-07-10 (주)포인트엔지니어링 캔 패지키 타입의 광 디바이스 제조 방법 및 이에 의해 제조된 광 디바이스
WO2016055479A1 (en) 2014-10-08 2016-04-14 Ucb Biopharma Sprl Tetrahydroisoquinoline derivatives
TWI725408B (zh) 2018-04-20 2021-04-21 美商美國禮來大藥廠 多巴胺d1受體正向異位調節劑

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014193781A1 (en) * 2013-05-30 2014-12-04 Eli Lilly And Company 3,4-dihydroisoquinolin-2(1h)-yl compounds
WO2017178377A1 (en) * 2016-04-13 2017-10-19 Ucb Biopharma Sprl Tetrahydroisoquinoline derivatives

Also Published As

Publication number Publication date
CN113993857B (zh) 2024-01-02
CN117700395A (zh) 2024-03-15
SG11202112537YA (en) 2021-12-30
CL2021002946A1 (es) 2022-07-15
US20220259179A1 (en) 2022-08-18
WO2021001288A1 (en) 2021-01-07
IL289314A (en) 2022-02-01
MX2021015873A (es) 2022-02-03
IL289314B1 (en) 2025-05-01
AU2020299953A1 (en) 2022-01-06
AR119318A1 (es) 2021-12-09
PE20221020A1 (es) 2022-06-16
EP3993794A1 (en) 2022-05-11
JP2022539152A (ja) 2022-09-07
KR20220029686A (ko) 2022-03-08
MY210361A (en) 2025-09-13
ECSP21093559A (es) 2022-02-25
IL289314B2 (en) 2025-09-01
PH12021552825A1 (en) 2022-10-03
TW202115010A (zh) 2021-04-16
WO2021001288A9 (en) 2021-09-02
MX2024015493A (es) 2025-02-10
JP7510444B2 (ja) 2024-07-03
CA3139571A1 (en) 2021-01-07
MA56440A (fr) 2022-05-11
SA521431279B1 (ar) 2024-01-09
IL319939A (en) 2025-05-01
TW202537959A (zh) 2025-10-01
CN113993857A (zh) 2022-01-28
CO2021018155A2 (es) 2022-01-17
AU2020299953B2 (en) 2025-06-05
BR112021022378A2 (pt) 2022-03-08
ZA202109193B (en) 2023-11-29

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