- Synthesis of N-benzyl substituted 1,4-imino-L-lyxitols with a basic functional group as selective inhibitors of Golgi α-mannosidase IIb
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Inhibition of the biosynthesis of complex N-glycans in the Golgi apparatus is one of alternative ways to suppress growth of tumor tissue. Eight N-benzyl substituted 1,4-imino-L-lyxitols with basic functional groups (amine, amidine, guanidine), hydroxyl an
- Klunda, Tomá?,?esták, Sergej,Kóňa, Juraj,Poláková, Monika
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p. 424 - 431
(2018/11/23)
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- AMINOETHYLAROMATIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR
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The present invention relates to aromatic compounds of the formula (I) wherein Ar is phenyl or an aromatic 5-or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; E is CR6R7 or NR3;R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated Cl-C4--alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C 4-cycloalkylmethyl, fluorinated C3-C4--alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H, C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1--C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C 3-C4-cycloalkylmethyl, fluorinated C3--C 4-alkenyl, or R1a and R2 together are (CH 2)n with n being 2, 3 or 4, or R1a and R 2a together are (CH2)n with n being 2, 3 or 4; R2 and R2a are independently of each other H, C1-C4-alkyl or fluorinated C1-C 4-alkyl or R2a and R2 together are (CH 2)m with m being 1, 2, 3, 4 or 5; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, fluorine, C1-C4-alkyl and fluorinated C1-C4-alkyl or together form a moiety (CH2)p with p being 2, 3, 4 or 5; and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.
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Page/Page column 123
(2010/11/08)
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