CR20220050A - Métodos sintéticos mejorados para la elaboración de compuestos de (2h-1,2,3-triazol-2-il)fenilo como moduladores del receptor de orexina - Google Patents

Métodos sintéticos mejorados para la elaboración de compuestos de (2h-1,2,3-triazol-2-il)fenilo como moduladores del receptor de orexina

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Publication number
CR20220050A
CR20220050A CR20220050A CR20220050A CR20220050A CR 20220050 A CR20220050 A CR 20220050A CR 20220050 A CR20220050 A CR 20220050A CR 20220050 A CR20220050 A CR 20220050A CR 20220050 A CR20220050 A CR 20220050A
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CR
Costa Rica
Prior art keywords
triazol
making
orexin receptor
synthetic methods
receptor modulators
Prior art date
Application number
CR20220050A
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English (en)
Inventor
Dominique Paul M Depré
Kiran Matcha
Cheng Yi Chen
Pieter Westerduin
Florian Damien Medina
Original Assignee
Janssen Pharmaceutica Nv
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Publication date
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of CR20220050A publication Critical patent/CR20220050A/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C249/00—Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton
    • C07C249/16—Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton of hydrazones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C251/00—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
    • C07C251/72—Hydrazones
    • C07C251/74—Hydrazones having doubly-bound carbon atoms of hydrazone groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C251/76—Hydrazones having doubly-bound carbon atoms of hydrazone groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of a saturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C251/00—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
    • C07C251/72—Hydrazones
    • C07C251/74—Hydrazones having doubly-bound carbon atoms of hydrazone groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C251/78—Hydrazones having doubly-bound carbon atoms of hydrazone groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of an unsaturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/48—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups having nitrogen atoms of sulfonamide groups further bound to another hetero atom
    • C07C311/49—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups having nitrogen atoms of sulfonamide groups further bound to another hetero atom to nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring 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
    • C07D295/22—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 hetero atoms directly attached to ring nitrogen atoms
    • C07D295/28—Nitrogen atoms
    • C07D295/30—Nitrogen atoms non-acylated

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Se describen procesos para preparar (((3a<em>R</em>,6a<em>S</em>)-5-(4,6-dimetilpirimidin-2-il)hexahidropirrolo[3,4-c]pirrol-2(1<em>H</em>)-il)(2-fluoro-6-(2<em>H</em>-1,2,3-triazol-2-il)fenil)metanona <img src="data:image/png;base64,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" />, que son útiles para la fabricación comercial. Dicho compuesto es un modulador del receptor de orexina y puede ser útil en composiciones farmacéuticas y métodos para el tratamiento de estados de enfermedad, trastornos y afecciones mediadas por la actividad de la orexina, tales como el insomnio y la depresión.
CR20220050A 2019-08-07 2020-08-06 Métodos sintéticos mejorados para la elaboración de compuestos de (2h-1,2,3-triazol-2-il)fenilo como moduladores del receptor de orexina CR20220050A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962883857P 2019-08-07 2019-08-07
US202062971265P 2020-02-07 2020-02-07
PCT/EP2020/072192 WO2021023843A1 (en) 2019-08-07 2020-08-06 Improved synthetic methods of making (2h-1,2,3-triazol-2-yl)phenyl compounds as orexin receptor modulators

Publications (1)

Publication Number Publication Date
CR20220050A true CR20220050A (es) 2022-04-20

Family

ID=72139573

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Application Number Title Priority Date Filing Date
CR20220050A CR20220050A (es) 2019-08-07 2020-08-06 Métodos sintéticos mejorados para la elaboración de compuestos de (2h-1,2,3-triazol-2-il)fenilo como moduladores del receptor de orexina

Country Status (15)

Country Link
US (1) US20220289754A1 (es)
EP (1) EP4010325A1 (es)
JP (1) JP2022543286A (es)
KR (1) KR20220044323A (es)
CN (1) CN114555603A (es)
AU (1) AU2020324552A1 (es)
BR (1) BR112022002128A2 (es)
CA (1) CA3149689A1 (es)
CR (1) CR20220050A (es)
EC (1) ECSP22016630A (es)
IL (1) IL290362A (es)
JO (1) JOP20220031A1 (es)
MX (1) MX2022001615A (es)
PE (1) PE20220842A1 (es)
WO (1) WO2021023843A1 (es)

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4826833A (en) * 1984-01-30 1989-05-02 Pfizer Inc. 6-(Substituted)methylene-penicillanic and 6-(substituted)hydroxymethylpenicillanic acids and derivatives thereof
DK2491038T3 (da) * 2009-10-23 2016-07-18 Janssen Pharmaceutica Nv Disubstituerede octahydropyrrolo [3,4-c]pyrroler som orexin receptormodulatorer
US8299117B2 (en) * 2010-06-16 2012-10-30 Metabolex Inc. GPR120 receptor agonists and uses thereof
JP6464190B2 (ja) * 2014-04-01 2019-02-06 バイエル・クロップサイエンス・アクチェンゲゼルシャフト 複素環化合物の線虫防除のための使用

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Publication number Publication date
KR20220044323A (ko) 2022-04-07
JOP20220031A1 (ar) 2023-01-30
EP4010325A1 (en) 2022-06-15
ECSP22016630A (es) 2022-04-29
WO2021023843A1 (en) 2021-02-11
PE20220842A1 (es) 2022-05-24
JP2022543286A (ja) 2022-10-11
CN114555603A (zh) 2022-05-27
CA3149689A1 (en) 2021-02-11
MX2022001615A (es) 2022-05-26
AU2020324552A1 (en) 2022-03-24
US20220289754A1 (en) 2022-09-15
IL290362A (en) 2022-04-01
BR112022002128A2 (pt) 2022-06-07

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