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US 2003/0166922 A1Published application
Novel cephalosporin compounds and process for preparing the same
OwnerYang-Rae Cho, Chang-Seok Lee +6inventors
InventorsYang-Rae Cho, Chang-Seok Lee, Seong-Ho Oh, Eun-Jung Ryu, Kyoung-Sook Paek, Ha-Sik Youn, Yong-Jin Jang, Geun-Tae Kim
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Abstract
The present invention relates to a novel cephalosporin compound in which thiomethylthio chain is introduced into C-3 position of cephem ring and pharmaceutically acceptable non-toxic salt, physiologically hydrolysable ester, hydrate, solvate or isomer thereof. The present invention also relates to a pharmaceutical composition containing the compound and to a process for preparing the compound.
Claims6
A cephalosporin compound represented by the following formula (I):
- 17
- in which
- R1 and R2 each independently represent hydrogen, halogen, C1-6 alkyl, C1-6 alkylthio, aryl, arylthio, or C5-6 heteroaryl containing one or two hetero atoms selected from the group consisting of nitrogen atom and oxygen atom;
- R3 represents hydrogen or a carboxy-protecting group;
- Q represents S, O, CH2, NH or NR wherein R is hydrogen, C1-6 alkyl or benzyl;
- Z represents CH or N;
- n denotes an integer of 1 or 2;
- and
- Ar represents a heteroaryl group represented by one of the following formulas:
- 18
- wherein X, Y, W, A, B, D, E, G and I independently of one another represent N or C (or CH), provided that the six-membered ring forms a pyrimidine structure;
- R4 represents hydrogen, C1-4 alkyl, or amino substituted or unsubstituted with a substitutent selected from the group consisting of C1-6 alkyl and C1-6 hydroxyalkyl;
- R5 and R6 each independently represent hydrogen, hydroxy, C1-4 alkyl, C1-6 alkylthio substituted or unsubstituted with a substitutent selected from the group consisting of C1-6 alkyl, C1-6 hydroxyalkyl and C1-6 aminoalkyl, or amino substituted or unsubstituted with a substitutent selected from the group consisting of C1-6 alkyl, C1-6 hydroxyalkyl and C1-6 aminoalkyl;
- R7, R8, R9, R10 and R11 independently of one another represent hydrogen, C1-6 alkyl, or amino substituted or unsubstituted with a substitutent selected from the group consisting of C1-6 alkyl, C1-6 hydroxyalkyl and C1-6 aminoalkyl;
- and
- denotes a single bond or a double bond;
- or pharmaceutically acceptable non-toxic salt, physiologically hydrolysable ester, hydrate, solvate or isomer thereof.
14 more elements
Dependencies are inferred from the claim text.