摘要 |
Novel melatonin ligands of Formula (I) or pharmaceutically acceptable salts thereof wherein: n is 1 or 2; m is 0, 1 or 2; p is 0, 1, 2, 3, 4, 5, 6, 7 or 8; v is 2 or 3; A is aryl or heteroaryl; Z is O, S or NR<SUB>8</SUB>;Y is selected from the group consisting of hydrogen, aryl, heteroaryl, C<SUB>r</SUB>C<SUB>6</SUB> alkyl, C<SUB>3</SUB>-C<SUB>6</SUB> cycloalkyl, and R is selected from the group consisting of hydrogen, hydroxyl, -OCF<SUB>3</SUB>, CF<SUB>3</SUB>, C<SUB>1</SUB>-C<SUB>8 </SUB>alkyl, C<SUB>1</SUB>C<SUB>8</SUB> alkyloxy, C<SUB>1</SUB>C<SUB>8</SUB> alkylthio, halogen and -Z-(CH<SUB>2</SUB>)<SUB>P</SUB>-A; R<SUB>1</SUB> is selected from the group consisting of C<SUB>1</SUB>C<SUB>4</SUB> alkyl, C<SUB>3</SUB>-C<SUB>6</SUB> cycloalkyl, CF<SUB>3</SUB>, hydroxy-substituted C<SUB>1</SUB>C<SUB>4</SUB> alkyl, hydroxy-substituted C<SUB>3</SUB>-C<SUB>6</SUB> cycloalkyl, and NHR<SUB>5</SUB>, wherein R<SUB>5</SUB> is C<SUB>1</SUB>C<SUB>3</SUB> alkyl or C<SUB>3</SUB>-C<SUB>6</SUB> cycloalkyl; R<SUB>2</SUB> is selected from the group consisting of: hydrogen, C<SUB>1</SUB>C<SUB>4</SUB> alkyl, C<SUB>1</SUB>C<SUB>4</SUB> alkyloxy, OCF<SUB>3</SUB>, CF<SUB>3</SUB>, hydroxyl, and halogen; R<SUB>3 </SUB>is selected from the group consisting of hydrogen, C<SUB>1</SUB>C<SUB>4</SUB> alkyl, C<SUB>1</SUB>C<SUB>4</SUB> alkyloxy, OCF<SUB>3</SUB>, CF<SUB>3</SUB>, hydroxyl, and halogen; R and R<SUB>3</SUB> may be connected together to form an -0-(CH<SUB>2</SUB>)<SUB>v</SUB> bridge representing with the carbon atoms to which they are attached a 5- or 6-membered heterocyclic ring system; R<SUB>4</SUB> is selected from the group consisting of hydrogen, C<SUB>1</SUB>C<SUB>4</SUB> alkyl, C<SUB>1</SUB>C<SUB>4</SUB> alkyloxy, OCF<SUB>3</SUB>, CF<SUB>3</SUB>, hydroxyl, and halogen; R<SUB>6</SUB> is selected from the group consisting of hydrogen and C<SUB>1</SUB>C<SUB>6 </SUB>alkyl; R<SUB>7</SUB> is selected from the group consisting of hydrogen, C<SUB>1</SUB>C<SUB>4</SUB> alkyl, C<SUB>1</SUB>C<SUB>4 </SUB>alkyloxy, OCF<SUB>3</SUB>, CF<SUB>3</SUB>, hydroxyl, and halogen; and R<SUB>8</SUB> is selected from the group consisting of hydrogen and C<SUB>1</SUB>C<SUB>4</SUB> alkyl. |
申请人 |
MCGILL UNIVERSITY;UNIVERSITA DEGLI STUDI DI PARMA;UNIVERSITA DEGLI STUDI DI MILANO;UNIVERSITA DEGLI STUDI DI URBINO;GOBBI, GABRIELLA;MOR, MARCO;RIVARA, SILVIA;FRASCHINI, FRANCO;TARZIA, GIORGIO;BEDINI, ANNALIDA;SPADONI, GILBERTO;LUCINI, VALERIA |
发明人 |
GOBBI, GABRIELLA;MOR, MARCO;RIVARA, SILVIA;FRASCHINI, FRANCO;TARZIA, GIORGIO;BEDINI, ANNALIDA;SPADONI, GILBERTO;LUCINI, VALERIA |