SE544998C2 - Peptide conjugates of melphalan for the treatment of cancer - Google Patents

Peptide conjugates of melphalan for the treatment of cancer

Info

Publication number
SE544998C2
SE544998C2 SE2150017A SE2150017A SE544998C2 SE 544998 C2 SE544998 C2 SE 544998C2 SE 2150017 A SE2150017 A SE 2150017A SE 2150017 A SE2150017 A SE 2150017A SE 544998 C2 SE544998 C2 SE 544998C2
Authority
SE
Sweden
Prior art keywords
methyl
pentan
cyclopropyl
cyclopentyl
cancer
Prior art date
Application number
SE2150017A
Other languages
English (en)
Other versions
SE2150017A1 (en
Inventor
Björn-Olof Klasson
Original Assignee
Bkmdcl 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 Bkmdcl Ab filed Critical Bkmdcl Ab
Priority to SE2150017A priority Critical patent/SE544998C2/en
Publication of SE2150017A1 publication Critical patent/SE2150017A1/en
Publication of SE544998C2 publication Critical patent/SE544998C2/en

Links

Classifications

    • 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
    • C07C237/28Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
    • C07C237/36Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group 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
    • A61P35/00Antineoplastic agents

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Peptides Or Proteins (AREA)

Claims (8)

1. Förening representerad av formel (l): i vilken: R1 är metyl, propanyl, propan-2-yl, pentan-3-yl, cyklopropylmetyl, 2-metylpropan-1-yl, 2- etylbutan-1-yl, 2-propylpentan-1-yl, (2S)-butan-2-y|, (2R)-butan-2-y|, (2S)-pentan-2-y|, (2R)- pentan-2-yl, (2R)-hexan-2-y|, (2S)-hexan-2-y|, cyklopropyl, cyklobutyl, cyklopentyl eller cyklohexyl; och R2 är Br, Cl, I, CN, metyl, etyl, n-propyl, propan-2-yl, cyklopropyl, 1-metyl-1-cyklopropyl, cyklobutyl, 1-metyl-1-cyklobutyl, cyklopentyl, 1-metyl-1-cyklopentyl, Si(CH3)s, C(CHs)s eller CXFz, CX2F eller CXa, där X är Cl eller Br, såväl som farmaceutiskt godtagbara salter och/eller solvat därav.
2. Förening enligt patentkrav 1, i vilken: R1 är propan-2-yl, pentan-3-yl, 2-metylpropan-1-yl, 2-etylbutan-1-yl, 2-propylpentan-1-yl, (2S)-butan-2-y|, (2R)-butan-2-y|, (2S)-pentan-2-y|, (2R)-pentan-2-yl, cyklopropyl eller cyklopentyl; och R2 är Br, Cl, I, CN, metyl, etyl, n-propyl, propan-2-yl, cyklopropyl, 1-metyl-1-cyklopropyl, cyklobutyl, 1-metyl-1-cyklobutyl, cyklopentyl, 1-metyl-1-cyklopentyl, Si(CH3)s, C(CHs)s eller CXF2, CX2F eller CXs där X är Cl eller Br.
3. Förening enligt patentkrav 2, i vilken: R1 är propan-2-yl, pentan-3-yl, (2S)-pentan-2-yl eller (2R)-pentan-2-yl; och R2 är Br, Cl, CN, 1-metyl-1-cyklopropyl, cyklopropyl, Si(CH3)3, eller C(CH3)
4. Förening enligt patentkrav 3, i vilken: 1(2) R1 är pentan-3-yl eller propan-2-yl; och R2 är Br, Si(CH3)3 eller C(CH3)
5. Farmaceutiskt preparat, vilket innefattar en förening såsom definierad i vilket som helst av patentkraven 1-4 i kombination med en farmaceutiskt godtagbar bärare.
6. Förening enligt vilket som helst av patentkraven 1-4 för användning som medikament.
7. Förening enligt vilket som helst av patentkraven 1-4 för användning vid behandling av cancer.
8. Förening för användning enligt patentkrav 7, vilken inkluderar behandling av tumörsjukdomar valda ur den grupp som består av lungcancer, bröstcancer, äggstockscancer, testikelcancer, multipelt myelom och malignt melanom. 2(2)
SE2150017A 2021-01-13 2021-01-13 Peptide conjugates of melphalan for the treatment of cancer SE544998C2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
SE2150017A SE544998C2 (en) 2021-01-13 2021-01-13 Peptide conjugates of melphalan for the treatment of cancer

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
SE2150017A SE544998C2 (en) 2021-01-13 2021-01-13 Peptide conjugates of melphalan for the treatment of cancer

Publications (2)

Publication Number Publication Date
SE2150017A1 SE2150017A1 (en) 2022-07-14
SE544998C2 true SE544998C2 (en) 2023-02-21

Family

ID=82702060

Family Applications (1)

Application Number Title Priority Date Filing Date
SE2150017A SE544998C2 (en) 2021-01-13 2021-01-13 Peptide conjugates of melphalan for the treatment of cancer

Country Status (1)

Country Link
SE (1) SE544998C2 (sv)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011078782A1 (en) * 2009-12-22 2011-06-30 Oncopeptides Ab A composition comprising of melphalan derivatives and gemcitabine or etoposide useful in the treatment of cancer
WO2017093443A1 (en) * 2015-12-01 2017-06-08 Oncopeptides Ab Melflufen dosage regimens for cancer

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011078782A1 (en) * 2009-12-22 2011-06-30 Oncopeptides Ab A composition comprising of melphalan derivatives and gemcitabine or etoposide useful in the treatment of cancer
WO2017093443A1 (en) * 2015-12-01 2017-06-08 Oncopeptides Ab Melflufen dosage regimens for cancer

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Agadzhanyan, Ts. et al, Amino acids and peptides. XIII. Synthesis of asaphan analogs, Armyanskii Khimicheskii Zhurnal (1977), 30(9), 776-80 *

Also Published As

Publication number Publication date
SE2150017A1 (en) 2022-07-14

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