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Adenosine A1 agonists for the treatment of glaucoma and ocular hypertension
专利权人:
Bayer Intellectual Property GmbH
发明人:
KLAR, Jürgen,VON DEGENFELD, Georges,LERCHEN, Hans-Georg,ALBRECHT-KÜPPER, Barbara,KNORR, Andreas,SANDNER, Peter,MEIBOM, Daniel
申请号:
ES11752517
公开号:
ES2570659T3
申请日:
2011.08.29
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
Compound of formula (I) ** Formula ** in which A is oxygen or sulfur, R1 is hydrogen or a group of formula ** Formula ** or in which it is the binding to the oxygen atom, L1 is alkanediyl (C2 -C4) linear, L2 is linear (C1-C3) alkanediyl, R5 and R8 are identical or different and are independently selected from the group consisting of hydrogen, methyl, propan-2-yl, propan-1-yl, 2- methylpropan-1-yl, 1-methylpropan-1-yl, butan-1-yl, tert-butyl, phenyl, benzyl, p-hydroxybenzyl, indole-3-ylmethyl, imidazol-4-ylmethyl, hydroxymethyl, 2-hydroxyethyl, 1-hydroxyethyl, mercaptomethyl, methylthiomethyl, 2-mercaptoethyl, 2-methylthioethyl, carbamoylmethyl, 2-carbamoyllethyl, carboxymethyl, 2-carboxyethyl, 4-aminobutan-1-yl, 4-amino-3-hydroxybutan-1-yl, 3- aminopropan-1-yl, 2- aminoethyl, aminomethyl, 3-guanidinopropan-1-yl, 3-ureidopropan-1-yl, R6 and R9 are independently selected from hydrogen or methyl, R7 is hydrogen or (C1-C4) alkyl, or R7 and R5 form, together with the atoms to which they are attached, a pyrrolidine or piperidine ring, R10 and R11 are identical or different and are independently selected from hydrogen or (C1-C4) alkyl, in which the (C1-C4) alkyl may be substituted with a group selected from hydroxy, (C1-C4) alkoxy, amino, mono-C1-C4 alkylamino or di-C1-C4 alkylamino, or R10 and R8 form, together with the atoms to which they are attached, a pyrrolidine or piperidine ring, and R12 is hydrogen or hydroxycarbonyl, R2 is hydrogen or a group of formula -CH2OR1, wherein R1 is as defined above, R3 is hydrogen, methyl or ethyl, R4 is hydrogen, methyl or ethyl, or R3 and R4 form together with the nitrogen atom, to which they are attached, an azetidine, pyrrolidine or piperidine ring, in which the azetidine, pyrrolidine or piperidine ring may be substituted with one or 2 substituents independently selected from the fluorine, trifluoromethyl, methyl, ethyl, methoxy and etho group xi, or its salts, solvates and solvates of the salts for use in a procedure for the treat
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