MRGX receptor antagonists
AssigneesRheinische Friedrich-Wilhelms-Universität Bonn, Katholieke Universiteit Leuven of KU Leuven Research & Development
InventorsChrista Müller, Mohamad Wessam Alnouri, Yvonne Riedel, Dominik Thimm, Daniel Marx, Vigneshwaran Namasivayam, Susanne Gattner, Piet Herdewyn, Steven De Jonghe, Piotr Leonczak, Sven Verdonck
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Abstract
The invention relates to a method for preventing or treating a disease or disorder that is associated with the MrgX2 receptor. The invention also relates to MrgX2 antagonists and physiologically acceptable salts thereof. The invention also relates to pharmaceutical compositions and dosage forms comprising an MrgX2 antagonist.
Claims7
A method for treating a disease or disorder that is associated with the MrgX2 receptor, comprising administering to a subject in need thereof a therapeutically effective amount of an MrgX2 antagonist according to general formulas (II), (III), and (VII):
- wherein
- R1 means C1-3 alkyl, linear or branched, saturated or unsaturated, either unsubstituted or monosubstituted with —OH;
- R2 means CH(CH3)2, —CH2CH(CH3)2, —C(CH3)3, -cyclopropyl, -para-methoxyphenyl, -2-thienyl, —CH2C(═O)OH, —C(═O)OCH3, —CH2C(═O)OCH3, —CH2C(═O)OCH2CH3, —C(CH3)2(OH), —CH2OCH3, —SCH3, or —NH2;
- or
- R1 and R2 together with the atoms to which they are attached form a six membered saturated unsubstituted alicyclic ring;
- R3, and R4 means —H;
- —C1-6-alkyl;
- —C1-6-cycloalkyl;
- -phenyl;
- —C1-6-alkyl-phenyl;
- -heteroaryl selected from the group consisting of thienyl, furanyl and pyrrolyl;
- —C(═O)OH;
- —C(═O)O—C1-6-alkyl;
- —CN;
- —OH;
- —O—C1-6-alkyl, —NH2, —S—C1-6-alkyl, —F, —Cl, —Br, or —I;
- R5, R6, R7 and R8 independently of one another mean, —C1-6-alkyl, —CN, —OH, —O—C1-6-alkyl, —F, —Cl, —Br, or —I;
- or
- R6 and R7 together with the carbon atoms to which they are attached form an unsubstituted phenyl ring;
- wherein in each case the “C1-6-alkyl” may be linear or branched, saturated or unsaturated, unsubstituted or monosubstituted with a substituent selected from —CN, —C(═O)OH, —C(═O)O—C1-6-alkyl, —OH, —O—C1-6-alkyl, —NH2, —NH—C1-6-alkyl, —N(C1-6-alkyl) 2, —N3, —F, —Cl, —Br, or —I;
- wherein in each case the “C1-6-cycloalkyl” may be linear or branched, saturated or unsaturated, unsubstituted or monosubstituted with a substituent selected from —CN, —C(═O)OH, —C(═O)O—C1-6-alkyl, —OH, —O—C1-6-alkyl, —NH2, —NH—C1-6-alkyl, —N(C1-6-alkyl) 2, —N3, —F, —Cl, —Br, or —I;
- wherein in each case the “phenyl” may be unsubstituted, mono- or disubstituted with a substituent independently selected from —CN, —C(═O)OH, —C(═O)O—C1-6-alkyl, —OH, —O—C1-6-alkyl, —NH2, —NH—C1-6-alkyl, —N(C1-6-alkyl) 2, —N3, —F, —Cl, —Br, or —I;
- wherein in each case the “heteroaryl” may be linear or branched, saturated or unsaturated, unsubstituted or monosubstituted with a substituent selected from —CN, —C(═O)OH, —C(═O)O—C1-6-alkyl, —OH, —O—C1-6-alkyl, —NH2, —NH—C1-6-alkyl, —N(C1-6-alkyl) 2, —N3, —F, —Cl, —Br, or —I;
- or
- a physiologically acceptable salt thereof.
Dependencies are inferred from the claim text.