Anilide derivative, production and use thereof

A compound selected from the group consisting of

• N-methyl-N-[4-[[[2-(4-methylphenyl)-6,7-dihydro-5H-benzocyclohepten-8-yl]ca rbonyl]amino]benzyl]piperidinium iodide,
• N-methyl-N-[4-[[[7-(4-methylphenyl)-2,3-dihydro-1-benzoxepin-4-yl]carbonyl] amino]benzyl]piperidinium iodide,
• N-[4-[N-methyl-N-(tetrahydropyran-4-yl)aminomethyl]phenyl]-7-(4-methylpheny l)-2,3-dihydro-1-benzoxepine-4-carboxmide,
• N-[4-[N-methyl-N-(tetrahydropyran-4-yl)aminomethyl]phenyl]-7-(4-morpholinop henyl)-2,3-dihydro-1-benzoxepine-4-carboxmide,
• 7-(4-ethoxyphenyl)-N-[4-[N-methyl-N-(tetrahydropyran-4-yl)aminomethyl]pheny l]-2,3-dihydro-1-benzoxepine-4-carboxmide,
• N,N-dimethyl-N-[4-[[[2-(4-methylphenyl)-6,7-dihydro-5H-benzocyclohepten-8-y l]carbonyl]amino]benzyl]-N-(tetrahydropyran-4-yl)ammonium iodide and
• N-methyl-N-[4-[[[7-(4-methylphenyl)-3,4-dihydronaphthalen-2-yl]carbonyl]ami no]benzyl]piperidinium iodide,
• or a salt thereof.

A pharmaceutical composition for antagonizing MCP-1 receptor, which comprises a compound of the formula:

• ##STR48## wherein R.sup.1 is an optionally substituted 5- to 6-membered ring, W is a divalent group of the formula:
• ##STR49## wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted carbon atom, an optionally substituted nitrogen atom, sulfur atom or oxygen atom, the ring B is an optionally substituted 5- to 7-membered ring, Z is a chemical bond or a divalent group, R.sup.2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, (2) an optionally substituted nitrogen-containing heterocyclic ring group which may contain a sulfur atom or an oxygen atom as ring constituting atoms and wherein a nitrogen atom may form a quaternary ammonium, (3) a group binding through a sulfur atom or (4) a group of the formula:
• ##STR50## wherein k is 0 or 1, and when k is 0, a phosphorus atom may form a phosphonium;
• and R.sup.5 ' and R.sup.6 ' are independently an optionally substituted hydrocarbon group, an optionally substituted hydroxy group or an optionally substituted amino group, and R.sup.5 ' and R.sup.6 ' may bind to each other to form a cyclic group together with the adjacent phosphorus atom, or a salt thereof.

A method for antagonizing MCP-1 receptor which comprises administering to a mammal in need thereof an effective amount of a compound of the formula:

• ##STR51## wherein R.sup.1 is an optionally substituted 5- to 6-membered ring;
• W is a divalent group of the formula:
• ##STR52## wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted carbon atom, an optionally substituted nitrogen atom, sulfur atom or oxygen atom, and the ring B is an optionally substituted 5- to 7-membered ring;
• Z is a chemical bond or a divalent group;
• R.sup.2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, (2) an optionally substituted nitrogen-containing heterocyclic ring group which may contain a sulfur atom or an oxygen atom as ring constituting atoms and wherein a nitrogen atom may form a quaternary ammonium, (3) a group binding through a sulfur atom or (4) a group of the formula:
• ##STR53## wherein k is 0 or 1, and when k is 0, a phosphorus atom may form a phosphonium;
• and R.sup.5 ' and R.sup.6 ' are independently an optionally substituted hydrocarbon group, an optionally substituted hydroxy group or an optionally substituted amino group, and R.sup.5 ' and R.sup.6 ' may bind to each other to form a cyclic group together with the adjacent phosphorus atom, or a salt thereof.

A method of making a medicament for antagonizing MCP-1 receptor comprising using a compound of the formula:

• ##STR54## wherein R.sup.1 is an optionally substituted 5- to 6-membered ring;
• W is a divalent group of the formula:
• ##STR55## wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted carbon atom, an optionally substituted nitrogen atom, sulfur atom or oxygen atom, and the ring B is an optionally substituted 5- to 7-membered ring;
• Z is a chemical bond or a divalent group;
• R.sup.2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, (2) an optionally substituted nitrogen-containing heterocyclic ring group which may contain a sulfur atom or an oxygen atom as ring constituting atoms and wherein a nitrogen atom may form a quaternary ammonium, (3) a group binding through a sulfur atom or (4) a group of the formula:
• ##STR56## wherein k is 0 or 1, and when k is 0, a phosphorus atom may form a phosphonium;
• and R.sup.5 ' and R.sup.6 ' are independently an optionally substituted hydrocarbon group, an optionally substituted hydroxy group or an optionally substituted amino group, and R.sup.5 ' and R.sup.6 ' may bind to each other to form a cyclic group together with the adjacent phosphorus atom, or a salt thereof.