| 摘要 |
<p>The present invention relates to compounds of the formula
<Chemistry id="chema01" num="0001"><Image id="ia01" he="37" wi="57" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" /></Chemistry> Q is selected from the group consisting of
<Chemistry id="chema02" num="0002"><Image id="ia02" he="21" wi="126" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" /></Chemistry> G is selected from the group consisting of alkyl, substituted alkvl, substituted or unsubstituted aryl, heterocyclo,
<Chemistry id="chema03" num="0003"><Image id="ia03" he="20" wi="129" file="IMGA0003.TIF" imgContent="chem" imgFormat="TIFF" /></Chemistry> W is O or NR<Sub>15</Sub>;
X is O or H,H;
Y is selected from the group consisting of O; H,OR<Sub>16</Sub>; OR<Sub>17</Sub>,OR<Sub>17</Sub>; NOR<Sub>18</Sub>; H,NOR<Sub>19</Sub>; H,NR<Sub>20</Sub>R<Sub>21</Sub>; H,H; or CHR<Sub>22</Sub>; OR<Sub>17</Sub> OR<Sub>17</Sub> can be a cyclic ketal;
Z<Sub>1</Sub>, and Z<Sub>2</Sub> are selected from the group consisting of CH<Sub>2</Sub>, O, NR<Sub>23</Sub>, S, or SO<Sub>2</Sub>, wherein only one of Z and Z<Sub>2</Sub> is a heteroatom;
B<Sub>1</Sub> and B<Sub>2</Sub> are selected from the group consisting of OR<Sub>24</Sub>, or OCOR<Sub>25</Sub>, or O<Sub>2</Sub>CNR<Sub>26</Sub>R<Sub>27</Sub>; when B<Sub>1</Sub> is H and Y is OH, H they can form a six-membered ring ketal or acetal;
D is selected from the group consisting of NR<Sub>28</Sub>R<Sub>29</Sub>, NR<Sub>30</Sub>COR<Sub>31</Sub> or saturated heterocycle
<!-- EPO <DP n="8001"> --> R<Sub>1</Sub>, R<Sub>2</Sub>, R<Sub>3</Sub>, R<Sub>4</Sub>, R<Sub>5</Sub>, R<Sub>6</Sub>, R<Sub>7</Sub>, R<Sub>13</Sub>, R<Sub>14</Sub>, R<Sub>18</Sub>, R<Sub>19</Sub>, R<Sub>20</Sub>, R<Sub>21</Sub>, R<Sub>22</Sub>, R<Sub>26</Sub>, and R<Sub>27</Sub> are selected from the group H, alkyl, substituted alkyl, or aryl and when R<Sub>1</Sub> and R<Sub>2</Sub> are alkyl can be joined to form a cycloalkyl; R<Sub>3</Sub> and R<Sub>4</Sub> are alkyl can be joined to form a cycloalkyl;
R<Sub>9</Sub>, R<Sub>10</Sub>, R<Sub>16</Sub>, R<Sub>17</Sub>, R<Sub>24</Sub>, R<Sub>25</Sub>, and R<Sub>31</Sub> are selected from the group H, alkyl, or substituted alkyl;
R<Sub>8</Sub>, R<Sub>11</Sub>, R<Sub>12</Sub>, R<Sub>28</Sub>, R<Sub>30</Sub>, R<Sub>32</Sub>, R<Sub>33</Sub>, and R<Sub>30</Sub> are selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, or heterocyclo;
R<Sub>15</Sub>, R<Sub>23</Sub> and R<Sub>29</Sub> are selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, heterocyclo, R<Sub>32</Sub>C=O, R<Sub>33</Sub>SO<Sub>2</Sub>, hydroxy, O-alkyl or O-substituted alkyl, the pharmaceutically acceptable salts thereof and any hydrates, solvates or geometric, optical and stereoisomers thereof, with the proviso that compounds wherein
W and X are both O; and
R<Sub>1</Sub>, R<Sub>2</Sub>, R<Sub>7</Sub>, are H; and
R<Sub>3</Sub>, R<Sub>4</Sub>, R<Sub>6</Sub>, are methyl; and
R<Sub>8</Sub>, is H or methyl; and
Z<Sub>1</Sub>, and Z<Sub>2</Sub>, are CH<Sub>2</Sub>; and
G is 1-methyl-2-(substituted-4-thiazolyl)ethenyl; and
Q is as defined above
are excluded.</p> |
