3,4-Dihydro-thiaoxo-1-pyrrolidinyl-or piperidinyl-ZH-benzo[b]pyrons.

摘要

A compound of formula (I):
<Chemistry id="chema01" num="0001"><Image id="ia01" he="43" wi="62" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein:

either one of Ri and R<Sub>2</Sub> is hydrogen and the other is selected from the class of C<Sub>1-6</Sub> alkylcarbonyl, C<Sub>1-6</Sub> alkoxycarbonyl, C<Sub>1-6</Sub> alkylcarbonyloxy, C<Sub>1-6</Sub> alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C<Sub>1-6</Sub> alkylsulphinyl, C<Sub>1-6</Sub> alkylsulphonyl, C<Sub>1-6</Sub> alkoxysulphinyl, Ci-6 alkoxysulphonyl, C<Sub>1-6</Sub> alkylcarbonylamino, C<Sub>1-6</Sub> alkoxycarbonylamino, C<Sub>1-6</Sub> alkyl-thiocarbonyl, C<Sub>1-6</Sub> alkoxy-thiocarbonyl, C<Sub>1-6</Sub> alkyl-thiocarbonyloxy, 1-mercapto-C2-7 alkyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C<Sub>1-6</Sub> alkyl groups, or C<Sub>1-6</Sub> alkysulphinylamino, C<Sub>1-6</Sub> alkylsulphonylamino C<Sub>1-6</Sub> alkoxysulphinylamino or C<Sub>1-6</Sub> alkoxysulphonylamino or ethylenyl terminally substituted by C<Sub>1-6</Sub>alkylcarbonyl, nitro or cyano, or -C(C<Sub>1-6</Sub>alkyl) NOH or -C(C<Sub>1-6</Sub>alkyl) N NH<Sub>2</Sub>, or one of R<Sub>1</Sub> and R<Sub>2</Sub> is nitro, cyano or Ci-3 alkylcarbonyl and the other is methoxy or amino optionally substituted by one or two C<Sub>1-6</Sub> alkyl groups or by C<Sub>2-7</Sub>alkanoyl;

one or R<Sub>3</Sub> and R<Sub>4</Sub> is hydrogen or C<Sub>1-4</Sub> alkyl and the other is C<Sub>1-4</Sub> alkyl or R<Sub>3</Sub> and R<Sub>4</Sub> together are C<Sub>2-5</Sub> polymethylene.

Rsis hydrogen, C<Sub>1-3</Sub> alkyl or C<Sub>1-8</Sub>acyl; and n is 1 or 2; the thiolactam group being trans to the ORs group; or, when one orthe other of R<Sub>1</Sub> and R<Sub>2 </Sub>is an amino or an amino-containing group capable of forming an acid addition salt, a pharmaceutically acceptable saltthereof, having useful pharmacological activity, a process for preparing them, pharmaceutical compositions containing them, and their use in the treatment of mammals.