CN116981461A - 用于制备杂环甲酮化合物及其氮杂双环中间体的工艺 - Google Patents

用于制备杂环甲酮化合物及其氮杂双环中间体的工艺 Download PDF

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Publication number
CN116981461A
CN116981461A CN202180088882.XA CN202180088882A CN116981461A CN 116981461 A CN116981461 A CN 116981461A CN 202180088882 A CN202180088882 A CN 202180088882A CN 116981461 A CN116981461 A CN 116981461A
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compound
formula
group
reaction
alkyl
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CN202180088882.XA
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English (en)
Chinese (zh)
Inventor
克里斯蒂安·格鲁格尔
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Ray Quality Medical Co ltd
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Ray Quality Medical Co ltd
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Priority claimed from AU2020904060A external-priority patent/AU2020904060A0/en
Application filed by Ray Quality Medical Co ltd filed Critical Ray Quality Medical Co ltd
Publication of CN116981461A publication Critical patent/CN116981461A/zh
Pending legal-status Critical Current

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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06—Oxygen atoms
    • 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
    • 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
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B49/00—Grignard reactions
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN202180088882.XA 2020-11-06 2021-11-05 用于制备杂环甲酮化合物及其氮杂双环中间体的工艺 Pending CN116981461A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
AU2020904060A AU2020904060A0 (en) 2020-11-06 Process for preparing heterocyclic methanone compounds and aza-bicyclo intermediates thereof
AU2020904060 2020-11-06
PCT/AU2021/051310 WO2022094668A1 (en) 2020-11-06 2021-11-05 Process for preparing heterocyclic methanone compounds and aza-bicyclo intermediates thereof

Publications (1)

Publication Number Publication Date
CN116981461A true CN116981461A (zh) 2023-10-31

Family

ID=81458249

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202180088882.XA Pending CN116981461A (zh) 2020-11-06 2021-11-05 用于制备杂环甲酮化合物及其氮杂双环中间体的工艺

Country Status (11)

Country Link
US (1) US20230416243A1 (https=)
EP (1) EP4240740A4 (https=)
JP (1) JP2023548368A (https=)
KR (1) KR20230154789A (https=)
CN (1) CN116981461A (https=)
AU (1) AU2021374232A1 (https=)
CA (1) CA3196642A1 (https=)
CL (1) CL2023001300A1 (https=)
IL (1) IL302671A (https=)
MX (1) MX2023004940A (https=)
WO (1) WO2022094668A1 (https=)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2026509196A (ja) * 2023-03-02 2026-03-17 アクチノゲン メディカル リミテッド アザ二環式ヘテロアリール化合物を調製するための流動化学プロセス
WO2025073002A1 (en) * 2023-10-03 2025-04-10 Actinogen Medical Limited Tablet formulation

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1909906A (zh) * 2004-01-20 2007-02-07 默克公司 作为趋化因子受体活性调节剂的2,6－二取代的哌啶类化合物
CN101395154A (zh) * 2006-03-01 2009-03-25 施万制药 作为μ阿片受体拮抗剂的8-氮杂双环[3.2.1]辛烷化合物
WO2010046445A2 (en) * 2008-10-23 2010-04-29 Boehringer Ingelheim International Gmbh Urea derivatives of substituted nortropanes, medicaments containing such compounds and their use
WO2011033255A1 (en) * 2009-09-16 2011-03-24 The University Of Edinburgh (4-phenyl-piperidin-1-yl)-[5-1h-pyrazol-4yl)-thiophen-3-yl]-methanone compounds and their use
CN102858767A (zh) * 2009-12-17 2013-01-02 默沙东公司 作为syk抑制剂的氨基嘧啶
CN102947295A (zh) * 2010-04-29 2013-02-27 爱丁堡大学 作为11β-HSD1抑制剂的3,3-二取代的-(8-氮杂双环[3.2.1]辛烷-8-基)-[5-(1H-吡唑-4 基)-噻吩-3-基]-甲酮

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY145633A (en) * 2006-03-01 2012-03-15 Theravance Inc 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
EP2525659B1 (en) * 2010-01-19 2019-02-27 Merck Sharp & Dohme Corp. PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS mTOR INHIBITORS

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1909906A (zh) * 2004-01-20 2007-02-07 默克公司 作为趋化因子受体活性调节剂的2,6－二取代的哌啶类化合物
CN101395154A (zh) * 2006-03-01 2009-03-25 施万制药 作为μ阿片受体拮抗剂的8-氮杂双环[3.2.1]辛烷化合物
WO2010046445A2 (en) * 2008-10-23 2010-04-29 Boehringer Ingelheim International Gmbh Urea derivatives of substituted nortropanes, medicaments containing such compounds and their use
WO2011033255A1 (en) * 2009-09-16 2011-03-24 The University Of Edinburgh (4-phenyl-piperidin-1-yl)-[5-1h-pyrazol-4yl)-thiophen-3-yl]-methanone compounds and their use
CN102858767A (zh) * 2009-12-17 2013-01-02 默沙东公司 作为syk抑制剂的氨基嘧啶
CN102947295A (zh) * 2010-04-29 2013-02-27 爱丁堡大学 作为11β-HSD1抑制剂的3,3-二取代的-(8-氮杂双环[3.2.1]辛烷-8-基)-[5-(1H-吡唑-4 基)-噻吩-3-基]-甲酮

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
FISCHER, J. 等: "Application of the modified von Braun demethylation procedure.I.Grignard reactions of aminoketones:preparation of 3-substituted 3-tropanols", 《ACTA CHIMICA ACADEMIAE SCIENTIARUM HUNGARICAE》, vol. 68, no. 3, 31 December 1971 (1971-12-31), pages 253 - 259 *
NOEL M. PAUL 等: "Structure-Activity Relationships for a Novel Series of Dopamine D2-like Receptor Ligands based on N- substituted 3-aryl-8-azabicyclo[3.2.1]octan-3-ol", 《JOURNAL OF MEDICINAL CHEMISTRY》, vol. 51, no. 19, 6 September 2008 (2008-09-06), pages 6095 - 6109 *
SCOTT P WEBSTER 等: "Selection and early clinical evaluation of the brain-penetrant 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor UE2343 (Xanamem™)", 《BRITISH JOURNAL OF PHARMACOLOGY》, vol. 174, no. 5, 23 December 2016 (2016-12-23), pages 396 - 408 *

Also Published As

Publication number Publication date
US20230416243A1 (en) 2023-12-28
WO2022094668A1 (en) 2022-05-12
IL302671A (en) 2023-07-01
MX2023004940A (es) 2023-09-12
CL2023001300A1 (es) 2024-01-05
AU2021374232A1 (en) 2023-06-08
EP4240740A4 (en) 2024-12-11
JP2023548368A (ja) 2023-11-16
KR20230154789A (ko) 2023-11-09
CA3196642A1 (en) 2022-05-12
EP4240740A1 (en) 2023-09-13
AU2021374232A9 (en) 2024-09-26

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CB03 Change of inventor or designer information

Inventor after: Christian Grugel

Inventor after: Tobias Weddell

Inventor before: Christian Grugel

CB03 Change of inventor or designer information