KR20240000510A - 소르틸린 활성 조절제 - Google Patents
소르틸린 활성 조절제 Download PDFInfo
- Publication number
- KR20240000510A KR20240000510A KR1020237037613A KR20237037613A KR20240000510A KR 20240000510 A KR20240000510 A KR 20240000510A KR 1020237037613 A KR1020237037613 A KR 1020237037613A KR 20237037613 A KR20237037613 A KR 20237037613A KR 20240000510 A KR20240000510 A KR 20240000510A
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- South Korea
- Prior art keywords
- acid
- halo
- alkyl
- ser
- acetamido
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
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- 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
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- 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
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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- 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
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- 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
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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
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- 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
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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
- C07K5/06—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
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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
- C07K5/06—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
Landscapes
- 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)
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- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
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- Pharmacology & Pharmacy (AREA)
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- Bioinformatics & Cheminformatics (AREA)
- Psychiatry (AREA)
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- 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)
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 |
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| Publication Number | Publication Date |
|---|---|
| KR20240000510A true KR20240000510A (ko) | 2024-01-02 |
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|---|---|
| US (1) | US20240217922A1 (https=) |
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| JP (1) | JP2024517678A (https=) |
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| WO (1) | WO2022223805A1 (https=) |
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| 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 |
| 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 |
| 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 |
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| 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 |
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2021
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2022
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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 |
| CN117677627A (zh) | 2024-03-08 |
| WO2022223805A1 (en) | 2022-10-27 |
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