CA3181637A1 - Method for preparing a crystalline form of rabeximod - Google Patents

Method for preparing a crystalline form of rabeximod

Info

Publication number
CA3181637A1
CA3181637A1 CA3181637A CA3181637A CA3181637A1 CA 3181637 A1 CA3181637 A1 CA 3181637A1 CA 3181637 A CA3181637 A CA 3181637A CA 3181637 A CA3181637 A CA 3181637A CA 3181637 A1 CA3181637 A1 CA 3181637A1
Authority
CA
Canada
Prior art keywords
chloro
salt
rabeximod
quinoxaline
dimethyl
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
CA3181637A
Other languages
English (en)
French (fr)
Inventor
Ulf Bjorklund
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Cyxone AB
Original Assignee
Cyxone AB
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 Cyxone AB filed Critical Cyxone AB
Publication of CA3181637A1 publication Critical patent/CA3181637A1/en
Pending legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4808—Preparations in capsules, e.g. of gelatin, of chocolate characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/485—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Processes Of Treating Macromolecular Substances (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Cosmetics (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Indole Compounds (AREA)
CA3181637A 2020-06-10 2021-06-10 Method for preparing a crystalline form of rabeximod Pending CA3181637A1 (en)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
EP20179277 2020-06-10
EP20179279.3 2020-06-10
EP20179239 2020-06-10
EP20179239.7 2020-06-10
EP20179279 2020-06-10
EP20179277.7 2020-06-10
EP20180706.2 2020-06-18
EP20180706 2020-06-18
PCT/EP2021/065694 WO2021250197A1 (en) 2020-06-10 2021-06-10 Method for preparing a crystalline form of rabeximod

Publications (1)

Publication Number Publication Date
CA3181637A1 true CA3181637A1 (en) 2021-12-16

Family

ID=76305939

Family Applications (3)

Application Number Title Priority Date Filing Date
CA3181637A Pending CA3181637A1 (en) 2020-06-10 2021-06-10 Method for preparing a crystalline form of rabeximod
CA3181646A Pending CA3181646A1 (en) 2020-06-10 2021-06-10 Oral formulation comprising a crystalline form of rabeximod
CA3181629A Pending CA3181629A1 (en) 2020-06-10 2021-06-10 Rabeximod in the treatment of rheumatoid arthritis

Family Applications After (2)

Application Number Title Priority Date Filing Date
CA3181646A Pending CA3181646A1 (en) 2020-06-10 2021-06-10 Oral formulation comprising a crystalline form of rabeximod
CA3181629A Pending CA3181629A1 (en) 2020-06-10 2021-06-10 Rabeximod in the treatment of rheumatoid arthritis

Country Status (8)

Country Link
US (3) US12594274B2 (enExample)
EP (3) EP4164616A1 (enExample)
JP (3) JP2023529001A (enExample)
KR (3) KR20230022882A (enExample)
CN (4) CN115697308A (enExample)
AU (3) AU2021290174A1 (enExample)
CA (3) CA3181637A1 (enExample)
WO (3) WO2021250199A1 (enExample)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023529001A (ja) 2020-06-10 2023-07-06 シクソン エービー 結晶形のラベキシモドを含む経口製剤
US11643415B1 (en) * 2021-12-09 2023-05-09 Cyxone Ab Rabeximod compounds

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE8600260D0 (sv) 1986-01-21 1986-01-21 Lundblad Leif Substituerade indolokinoxaliner
SE504289C2 (sv) * 1994-06-23 1996-12-23 Leif J I Lundblad Användning av vissa indolo-2,3b-kinoxaliner för framställning av ett läkemedel för inhibering av enzymet HIV-integras
JPH08165278A (ja) 1994-12-14 1996-06-25 Kawaken Fine Chem Co Ltd １−置換トリプタミン化合物の製造方法
SE504862C2 (sv) 1994-12-27 1997-05-20 Leif J I Lundblad Användning av vissa indolo-§2,3b¤-kinoxaliner för framställning av ett läkemedel för skydd av DNA i initieringsfasen och/eller promotionsfasen av karcinogenes och för förhindrande av oxidativ stress i patienter med sjukdomar relaterade till fria radikaler
DE19516804A1 (de) * 1995-05-08 1996-11-14 Hoechst Ag Isoindolinpigmente auf Basis von Aminochinoxalindionen
SE516067C2 (sv) 2000-02-18 2001-11-12 Lundblad Leif J I Användning av en förening för framställning av ett läkemedel
US6333327B2 (en) 2000-02-18 2001-12-25 Leif J. I. Lundblad Method for the treatment of Multiple Sclerosis
TW200410921A (en) * 2002-11-25 2004-07-01 Hoffmann La Roche Mandelic acid derivatives
ATE382623T1 (de) * 2004-06-09 2008-01-15 Hoffmann La Roche Octahydropyrrolo(3,4-c)pyrrolderivate und deren verwendung als antivirale mitteln
SE527639C2 (sv) 2004-06-17 2006-05-02 Oxypharma Ab Alkylsubstituerade indolokinoxaliner
CN101558038B (zh) * 2006-11-30 2013-05-01 国立大学法人东京工业大学 姜黄素衍生物
CN102115457B (zh) 2011-03-05 2012-11-21 太原理工大学 一种n-乙基咔唑的制备方法
WO2013182905A2 (en) * 2012-06-05 2013-12-12 Jonas Axelsson Mechanism, diagnostic, and treatments for complications of renal failure
WO2014140321A1 (en) 2013-03-15 2014-09-18 Vironova Ab Antiviral indolo[2,3-b]quinoxaline
EP3302442B1 (en) 2015-06-03 2024-10-16 Triastek, Inc. Dosage forms and use thereof
CN105061432B (zh) 2015-07-16 2017-09-29 河北大学 6H‑吲哚[2,3‑b]喹喔啉衍生物、药物组合物及其制备和应用
TWI721483B (zh) * 2018-07-13 2021-03-11 美商基利科學股份有限公司 吡咯并[1,2-b]嗒𠯤衍生物
WO2021250196A1 (en) 2020-06-10 2021-12-16 Cyxone Ab New use of rabeximod
JP2023529001A (ja) 2020-06-10 2023-07-06 シクソン エービー 結晶形のラベキシモドを含む経口製剤
US11643415B1 (en) * 2021-12-09 2023-05-09 Cyxone Ab Rabeximod compounds

Also Published As

Publication number Publication date
CN115698010A (zh) 2023-02-03
CN115697308A (zh) 2023-02-03
KR20230022880A (ko) 2023-02-16
JP2023529001A (ja) 2023-07-06
CA3181646A1 (en) 2021-12-16
KR20230022881A (ko) 2023-02-16
EP4164650A1 (en) 2023-04-19
AU2021290173A1 (en) 2023-02-09
EP4165043A1 (en) 2023-04-19
US20220133717A1 (en) 2022-05-05
JP2023533662A (ja) 2023-08-04
AU2021290174A1 (en) 2023-02-09
CN115768431A (zh) 2023-03-07
CA3181629A1 (en) 2021-12-16
US12673056B2 (en) 2026-07-07
US20230227455A1 (en) 2023-07-20
WO2021250197A1 (en) 2021-12-16
WO2021250204A1 (en) 2021-12-16
JP2023529877A (ja) 2023-07-12
EP4164616A1 (en) 2023-04-19
US12594274B2 (en) 2026-04-07
KR20230022882A (ko) 2023-02-16
US20230227456A1 (en) 2023-07-20
CN120383602A (zh) 2025-07-29
AU2021289006A1 (en) 2023-02-09
WO2021250199A1 (en) 2021-12-16

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