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classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D207-08
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D207-08
filingDate 1987-03-18-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c01dc55ce2bb83fc70abc10d0a09ebc3
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publicationDate 1987-09-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-0238319-A1
titleOfInvention Pyrrolidine derivatives
abstract Pyrrolidine derivatives which have inhibitory action for proline-specific endopeptidase and are useful as anti-amnesic agents, have the formula:wherein R<sup>1</sup>R3, R<sup>4</sup>, and R<sup>5</sup> are each independently hydrogen, hydroxy, halogen, lower alkyl, phenyl, substituted phenyl, -CH<sub>2</sub>R<sup>14</sup>, -X-R<sup>15</sup>,or{in which R<sup>14</sup> is phenyl or substituted phenyl. X is oxygen atom or sulfur atom. R<sup>15</sup> is lower alkyl, phenyl or substituted phenyl or -CH<sub>2</sub>R<sup>20</sup> (in which R<sup>20</sup> is phenyl or substituted phenyl). R<sup>16</sup> is lower alkyl, phenyl, substituted phenyl or -CH<sub>2</sub>R<sup>21</sup> (in which R<sup>21</sup> is phenyl or substituted phenyl). R<sup>17</sup> is lower alkyl, five or six-membered cycloalkyl, phenyl, substituted phenyl, -CH<sub>2</sub>R<sup>22</sup> (in which R<sup>22</sup> is phenyl or substituted phenyl)(in which R<sup>23</sup> is lower alkyl, phenyl or substituted phenyl). R<sup>18</sup> and R<sup>19</sup> are each independently lower alkyl or -CH<sub>2</sub>R<sup>24</sup> (in which R<sup>24</sup> is phenyl or subsubstituted phenyl)}. R<sup>6</sup> is hydrogen or lower alkyl. R<sup>7</sup> is hydrogen, lower alkyl, benzyl,or -(CH<sub>2</sub>)<sub>n</sub>-R<sup>25</sup> {in which n is an integer of 0 to 4. R<sup>25</sup> is -OH, -SH, -NH<sub>2</sub>, -SCH<sub>3</sub>,heterocyclic group, or -C0<sub>2</sub>R<sup>26</sup> (in which R<sup>26</sup> is hydrogen or lower alkyl or benzyl)}. R<sup>8</sup> is hydrogen or, when R<sup>8</sup> and R<sup>7</sup> are taken together with the adjacent nitrogen atom and carbon atom to which they are attached, they represent five-membered heterocyclic group. R<sup>9</sup> is hydrogen, lower alkyl, phenyl, substituted phenyl. R<sup>10</sup> is hydrogen, lower alkyl, lower alkoxy or halogen. m is an integer of 0 to 3. R<sup>11</sup> is hydrogen, lower alkyl, phenyl, substituted phenyl or-CH<sub>2</sub>R<sup>27</sup> (in which R<sup>27</sup> is phenyl or substituted phenyl). R<sup>12</sup> is lower alkyl or, when R<sup>12</sup> and R<sup>12</sup> are each taken together, they represent lower alkylene. R<sup>13</sup> is lower alkyl, phenyl, substituted phenyl or CH<sub>2</sub>R<sup>28</sup> (in which R<sup>28</sup> is phenyl or substituted phenyl) and their production and use.
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Total number of triples: 525.