CN117677627A - 分拣蛋白活性调节剂 - Google Patents

分拣蛋白活性调节剂 Download PDF

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Publication number
CN117677627A
CN117677627A CN202280030307.9A CN202280030307A CN117677627A CN 117677627 A CN117677627 A CN 117677627A CN 202280030307 A CN202280030307 A CN 202280030307A CN 117677627 A CN117677627 A CN 117677627A
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CN
China
Prior art keywords
acid
acetamido
alkyl
ser
propionylamino
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Pending
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CN202280030307.9A
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English (en)
Chinese (zh)
Inventor
保罗·布莱恩·黎托
曼努埃尔·哈维尔·凯斯-托马斯
麦德斯·富格桑·克约尔比
安德斯·纽易尔
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Innocence Ltd
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Innocence Ltd
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Publication of CN117677627A publication Critical patent/CN117677627A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C237/12—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/20—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals substituted additionally by nitrogen atoms, e.g. tryptophane
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/12—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043—Leu-amino acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06147—Dipeptides with the first amino acid being heterocyclic and His-amino acid; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06156—Dipeptides with the first amino acid being heterocyclic and Trp-amino acid; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biomedical Technology (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Sawing (AREA)
  • Investigating Or Analyzing Materials By The Use Of Electric Means (AREA)
  • Secondary Cells (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN202280030307.9A 2021-04-23 2022-04-22 分拣蛋白活性调节剂 Pending CN117677627A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP21170274.1 2021-04-23
EP21170274.1A EP4079748A1 (en) 2021-04-23 2021-04-23 Modulators of sortilin activity
PCT/EP2022/060742 WO2022223805A1 (en) 2021-04-23 2022-04-22 Modulators of sortilin activity

Publications (1)

Publication Number Publication Date
CN117677627A true CN117677627A (zh) 2024-03-08

Family

ID=75674611

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202280030307.9A Pending CN117677627A (zh) 2021-04-23 2022-04-22 分拣蛋白活性调节剂

Country Status (8)

Country Link
US (1) US20240217922A1 (https=)
EP (2) EP4079748A1 (https=)
JP (1) JP2024517678A (https=)
KR (1) KR20240000510A (https=)
CN (1) CN117677627A (https=)
AU (1) AU2022260554A1 (https=)
CA (1) CA3215848A1 (https=)
WO (1) WO2022223805A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116143648A (zh) * 2022-12-05 2023-05-23 河北远大九孚生物科技有限公司 一种n-乙酰-l-苯丙氨酸的合成方法

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4471047A1 (en) * 2023-05-31 2024-12-04 Insusense ApS Modulators of sortilin activity
EP4361165A1 (en) * 2022-10-24 2024-05-01 Insusense ApS Modulators of sortilin activity
EP4428124A1 (en) * 2023-03-07 2024-09-11 Vesper Bio Aps Modulators of sortilin activity
EP4428121A1 (en) * 2023-03-07 2024-09-11 Vesper Bio Aps Modulators of sortilin activity
EP4719366A1 (en) 2023-05-26 2026-04-08 Bertram Wiedenmann Sortilin inhibitors for treatment of patients with functional neuroendocrine tumors
TW202600557A (zh) * 2024-02-20 2026-01-01 日商大塚製藥股份有限公司 作為sort1抑制劑之哌啶-及嗎啉-羧酸鹽化合物

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DD262583A5 (de) * 1986-10-31 1988-12-07 Pfizer Inc.,Us Verfahren zur herstellung von nor-statin- und nor-cyclostatin-polypeptiden
DE3842067A1 (de) * 1988-12-14 1990-06-21 Hoechst Ag Enzym-hemmende aminosaeurederivate, verfahren zu ihrer herstellung, diese enthaltende mittel und ihre verwendung
JPH05345754A (ja) * 1992-06-15 1993-12-27 Suntory Ltd ジペプチド誘導体およびそれを有効成分とする骨疾患の予防または治療剤
DE19546532C2 (de) * 1995-12-13 2000-04-20 Degussa Verfahren zur Gewinnung von optisch aktiven L-alpha-Aminocarbonsäuren aus entsprechenden racemischen D,L-alpha-Aminocarbonsäuren
WO2004037159A2 (en) * 2002-10-23 2004-05-06 Obetherapy Biotechnology Compounds, compositions and methods for modulating fat metabolism
WO2006050861A2 (en) * 2004-11-10 2006-05-18 Boehringer Ingelheim International Gmbh Statine derivatives for the treatment of alzheimer's disease
CA2617294A1 (en) * 2005-08-03 2007-02-08 Boehringer Ingelheim International Gmbh Substituted ethane-1,2-diamines for the treatment of alzheimer's disease ii
PT3309157T (pt) 2009-05-13 2019-12-02 Gilead Pharmasset Llc Compostos antivirais
GB201011411D0 (en) * 2010-07-06 2010-08-18 St Georges Hosp Medical School Therapeutic compounds and their use
CN104955456B (zh) * 2013-01-28 2018-07-03 H.隆德贝克有限公司 作为分拣蛋白抑制剂的n-取代的-5-取代的邻氨甲酰苯甲酸
WO2015131100A1 (en) 2014-02-28 2015-09-03 The Scripps Research Institute Ligand-controlled c(sp3)-h arylation and olefination in synthesis of unnatural chiral alpha amino acids
US20160331746A1 (en) 2015-05-12 2016-11-17 University Of South Florida Sortilin-Binding Small Molecules for Increasing Glucose Uptake

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116143648A (zh) * 2022-12-05 2023-05-23 河北远大九孚生物科技有限公司 一种n-乙酰-l-苯丙氨酸的合成方法

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US20240217922A1 (en) 2024-07-04
AU2022260554A1 (en) 2023-11-02
EP4079748A1 (en) 2022-10-26
EP4326742A1 (en) 2024-02-28
AU2022260554A9 (en) 2023-11-16
JP2024517678A (ja) 2024-04-23
WO2022223805A1 (en) 2022-10-27
CA3215848A1 (en) 2022-10-27
KR20240000510A (ko) 2024-01-02

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