KR20240000510A - 소르틸린 활성 조절제 - Google Patents

소르틸린 활성 조절제 Download PDF

Info

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
Authority
KR
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.)
Pending
Application number
KR1020237037613A
Other languages
English (en)
Korean (ko)
Inventor
폴 브라이언 리틀
마누엘 야비에르 카세스-토마스
마드스 푸글상 기욀뷔
안데르스 뉘키에르
Original Assignee
인수센스 에이피에스
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by 인수센스 에이피에스 filed Critical 인수센스 에이피에스
Publication of KR20240000510A publication Critical patent/KR20240000510A/ko
Pending legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0821Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic 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
    • C07C237/04Carboxylic 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
    • C07C237/12Carboxylic 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
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/20Radicals 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic 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
    • C07D233/64Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic 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
    • C07D241/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/301,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043Leu-amino acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • C07K5/06147Dipeptides with the first amino acid being heterocyclic and His-amino acid; Derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • C07K5/06156Dipeptides with the first amino acid being heterocyclic and Trp-amino acid; Derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06191Dipeptides 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)
  • 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)
KR1020237037613A 2021-04-23 2022-04-22 소르틸린 활성 조절제 Pending KR20240000510A (ko)

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
KR20240000510A true KR20240000510A (ko) 2024-01-02

Family

ID=75674611

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020237037613A Pending KR20240000510A (ko) 2021-04-23 2022-04-22 소르틸린 활성 조절제

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=)

Families Citing this family (7)

* 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
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

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

Also Published As

Publication number Publication date
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
CA3215848A1 (en) 2022-10-27

Similar Documents

Publication Publication Date Title
KR20240000510A (ko) 소르틸린 활성 조절제
US20240294569A1 (en) Modulators of sortilin activity
TW202136247A (zh) 2-((4-((S)-2-(5-氯吡啶-2-基)-2-甲基苯并〔d〕〔1,3〕二氧呃-4-基)哌啶-1-基)甲基)-1-(((S)-氧呾-2-基)甲基)-1H-苯并〔d〕咪唑-6-羧酸1,3-二羥基-2-(羥基甲基)丙烷-2-胺鹽之固體形式
KR20190005838A (ko) 이중 lsd1/hdac 억제제로서 사이클로프로필-아마이드 화합물
TW202313595A (zh) 2-[(4-{6-[(4-氰基-2-氟芐基)氧基]吡啶-2-基}哌啶-1-基)甲基]-1-[(2s)- 氧雜環丁烷-2-基甲基]-1h-苯并咪唑-6-羧酸,1,3-二羥基-2-(羥甲基)丙-2-胺鹽之固體形式
JP7030776B2 (ja) アミノピリジン誘導体およびそれらの選択的alk-2阻害剤としての使用
CN103896946A (zh) 用于预防及治疗多种自身免疫疾病的新化合物
JP2023500263A (ja) アドレナリン受容体adrac2の阻害剤
CN119866342A (zh) 用于捕获白介素-1β的环肽
JP2025508927A (ja) ソルチリン依存性疾患を治療するためのアミノ酸ベースのカルバメート及び/又は尿素
KR20230135085A (ko) 소르틸린 활성 조절제로서의 피리딘 유도체
EP4428121A1 (en) Modulators of sortilin activity
EP4676917A1 (en) Modulators of sortilin activity
HK40082417A (en) Solid forms of 2-((4-((s)-2-(5-chloropyridin-2-yl)-2-methylbenzo[d] [1,3]dioxol-4-yl)piperidin-1-yl)methyl)-1-(((s)-oxetan-2-yl)methyl)-1h-benzo[d] imidazole-6-carboxylic acid, 1,3-dihydroxy-2-(hydroxymethyl)propan-2-amine salt

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20231031

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
A201 Request for examination
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20250213

Comment text: Request for Examination of Application