US 6,147,071 A · Cyclic compounds, their production and use

Abstract

Novel compounds of the following general formula or salts thereof. ##STR1## wherein Ring M is a heterocyclic ring having --N.dbd.CC<, --CO--N< or --CS--N< as the partial structure --X . . . . . Y<; R.sup.a and R.sup.b are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, and at least one of them is optionally substituted heterocyclic ring; Ring C is optionally substituted homocyclic or heterocyclic ring; Ring Z is an optionally substituted ring; and n represents an integer of from 1 to 6, or a salt thereof, which has an excellent tachykinin receptor antagonistic effect, and their production, and pharmaceutical compositions.

A compound of the formula:

##STR53## wherein ring M is a heterocyclic ring wherein --X. . . . . Y<is --N.dbd.C<;
and n is an integer from 1 to 6, or a salt thereof;
R.sup.a and R.sup.b are the same or different and represent, independently,
(1) a hydrogen atom,
(2) a C.sub.1-6 alkyl group optionally having from 1 to 5 substituents selected from
(a) a hydroxyl group,
(b) a C.sub.1-6 alkoxy group,
(c) a C.sub.1-6 alkylthio group,
(d) an amino group,
(e) a C.sub.1-7 acylamino group,
(f) a carboxyl group,
(g) a nitro group,
(h) a mono- or di-C.sub.1-6 alkylamino group,
(i) a mono- or di-C.sub.1-6 cycloalkylamino group,
(j) a C.sub.6-10 arylamino group,
(k) a 5-membered to 9-membered cyclicamino group which may have 1 to 3 hetero atoms selected from nitrogen, oxygen and sulfur atoms in addition to the nitrogen atom in the amino group,
(l) a 5-membered to 6-membered aromatic heterocyclic group having from 1 to 3 hetero atoms selected from nitrogen, oxygen and sulfur atoms, in addition to carbon atoms,
(m) a 5-membered to 9-membered non-aromatic heterocyclic ring having from 1 to 3 hetero atoms selected from nitrogen, oxygen and sulfur atoms, in addition to carbon atoms,
(n) a C.sub.1-4 alkylsulfonylamino group,
(o) a C.sub.1-6 alkyl-carbonyloxy group and
(p) a halogen atom,
(3) an optionally halogenated C.sub.1-6 alkoxy group,
(4) an optionally halogenated C.sub.1-6 alkylthio group,
(5) a C.sub.3-10 cycloalkyl group,
(6) a C.sub.6-10 aryl group,
(7) a C.sub.1-7 acylamino group,
(8) a C.sub.1-3 acyloxy group,
(9) a hydroxy group,
(10) a nitro group,
(11) a cyano group,
(12) an amino group,
(13) a mono- or di-C.sub.1-6 alkylamino group,
(14) a 5-membered to 9-membered cyclicamino group which may have 1 to 3 hetero atoms selected from nitrogen, oxygen and sulfur atoms, in addition to the nitrogen atom in the amino group,
(15) a C.sub.1-6 alkylcarbonylamino group,
(16) a C.sub.1-6 alkylsulfonylamino group,
(17) a C.sub.1-6 alkoxycarbonyl group,
(18) a carboxyl group,
(19) a C.sub.1-6 alkylcarbonyl group,
(20) a carbamoyl group,
(21) a mono- or di-C.sub.1-6 alkylcarbamoyl group,
(22) C.sub.1-6 alkylsulfonyl group;
the Ring B is a benzene ring which may have 1 to 4 substituents selected from
(1) a halogen atom,
(2) a C.sub.1-6 alkyl group optionally having from 1 to 5 substituents selected from
(a) a hydroxyl group,
(b) an amino group,
(c) a carboxyl group,
(d) a nitro group,
(e) a mono- or di-C.sub.1-6 alkylamino group,
(f) a C.sub.1-6 alkyl-carbonyloxy group and
(g) a halogen atom,
(3) an optionally halogenated C.sub.1-6 alkoxy group,
(4) an optionally halogenated C.sub.1-6 alkylthio group,
(5) a C.sub.6-10 aryl group,
(6) a C.sub.1-7 acylamino group,
(7) a C.sub.1-3 acyloxy group,
(8) a hydroxy group,
(9) a nitro group,
(10) a cyano group,
(11) an amino group,
(12) a mono- or di-C.sub.1-6 alkylamino group,
(13) a 5-membered to 9-membered cyclicamino group which may have 1 to 3 hetero atoms selected from nitrogen, oxygen and sulfur atoms, in addition to the nitrogen atom in the amino group,
(14) a C.sub.1-6 alkylcarbonylamino group,
(15) a C.sub.1-6 alkylsulfonylamino group,
(16) a C.sub.1-6 alkoxycarbonyl group,
(17) a carboxyl group,
(18) a C.sub.1-6 alkylcarbonyl group,
(19) a carbamoyl group,
(20) a mono- or di-C.sub.1-6 alkylcarbamoyl group,
(21) a C.sub.1-6 alkylsulfonyl group;
the Ring C is a benzene ring optionally having 1 to 5 substituents selected from
(1) a halogen atom,
(2) an optionally halogenated C.sub.1-10 alkyl group,
(3) an amino-substituted C.sub.1-4 alkyl group,
(4) a mono- or di-C.sub.1-4 alkylamino-substituted C.sub.1-4 alkyl group,
(5) a carboxyl-substituted C.sub.1-4 alkyl group,
(6) a hydroxy-substituted C.sub.1-4 alkyl group,
(7) a C.sub.1-4 alkoxy-carbonyl-substituted C.sub.1-4 alkyl group,
(8) a C.sub.3-10 cycloalkyl group,
(9) a nitro group,
(10) a cyano group,
(11) a hydroxyl group,
(12) an optionally-halogenated C.sub.1-10 alkoxy group,
(13) an optionally-halogenated C.sub.1-4 alkylthio group,
(14) an amino group,
(15) a mono- or di-C.sub.1-4 alkylamino group,
(16) a 5-membered to 9-membered cyclic amino group optionally having 1 to 3 hetero atoms selected from nitrogen, oxygen and sulfur atoms, in addition to the nitrogen atom in the amino group,
(17) a C.sub.1-4 alkyl-carbonylamino group,
(18) an aminocarbonyloxy group,
(19) a mono- or di-C.sub.1-4 alkylaminocarbonyloxy group,
(20) a C.sub.1-4 alkylsulfonylamino group,
(21) a C.sub.1-4 alkoxy-carbonyl group,
(22) an aralkyloxycarbonyl group,
(23) a carboxyl group,
(24) a C.sub.1-6 alkyl-carbonyl group,
(25) a C.sub.3-6 cycloalkyl-carbonyl group,
(26) a carbamoyl group,
(27) a mono- or di-C.sub.1-4 alkylcarbamoyl group,
(28) a C.sub.1-6 alkylsulfonyl group and
(29) a 5-membered or 6-membered aromatic monocyclic heterocyclic group having 1 to 4 hetero atoms selected from nitrogen, oxygen and sulfur atoms, which may have 1 to 3 substituents selected from an optionally halogenated C.sub.1-4 alkyl;
the Ring Z is ##STR54## wherein p is an integer of from 2 to 5 and Z.sub.2 is a hydrogen atom, an C.sub.1-4 alkyl group or a hydroxyl group.

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Cyclic compounds, their production and use

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Cyclic compounds, their production and use

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Abstract

Claims11