Ici Americas, Inc.

Zeneca Limited

Imperial Chemical Industries Limited

Ying K Yee

Frederick J Brown

Peter R Bernstein

Victor G Matassa

Cyrus J Ohnmacht

Diane A Trainor

Joseph J Lewis

Thomas P Maduskuie, Jr

The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R.sup.1, R.sup.2, L, X, Y, Z, A.sup.1, Q, A.sup.2 and M have the meanings set out in the specification. The invention also includes pharmaceutical compositions incorporating a formula I compound or a salt thereof, a process for the manufacture of the said compound, together with intermediates for use in the latter process. ##STR1##

Method for treating vasospastic cardiovascular diseases heterocyclic

Compounds of formula I, Ia or Ib and pharmaceutically acceptable salts thereof, useful in the treatment of neuropsychiatric disorders such as psychoses; pharmaceutical compositions comprising a compound of formula I and a pharmaceutically acceptable diluent or carrier; and methods of treating neuropschiatric disorders comprising administering to a mammal (including man) in need of such treatment an effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof.

Piperidine derivatives

Heterocyclic amide derivatives

Heterocyclic amide derivatives and pharmaceutical use thereof

Compounds of formula I, Ia or Ib and pharmaceutically acceptable salts thereof, useful in the treatment of neuropsychiatric disorders such as psychoses; pharmaceutical compositions comprising a compound of formula I and a pharmaceutically acceptable diluent or carrier; and methods of treating neuropschiatric disorders comprising administering to a mammal (including man) in need of such treatment an effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof; ##STR1##

Piperidine derivatives, compositions and use

The invention provides a series of novel heterocyclic amides of the formula I in which the group A; CRa can be --CRb.dbd.CRa--, --CHRb--CHRa-- or --N.dbd.CRa--, the amidic group Re.L can be Rd.X.CO.NH, Re.X.CS.NH or Re.NH.CO attached to position 4, 5 or 6 of the benzenoid moiety, z is an acid group selected from the group consisting of carboxy, an acylsulphonamide residue of the formula CO.NH.SO.sub.n Rg and a tetrazolyl residue of the formula II and the radicals Ra, Rb, Rc, Rd, Re, Rf, Rg, Rh, n, X, G.sup.1,Q and G.sup.2 have the meanings defined in the following specification. The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compounds, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.

Heterocyclic amides and leucotriene antagonistic use thereof

Heterocyclic amide derivatives and pharmaceutical use

This invention comprises novel carbocyclic compounds of formula I (wherein A, Z, R.sup.11 and R.sup.12 are defined in the specification) derived from acylsulfonamide derivatives of .alpha.-carbocyclyltoluic acids wherein said compounds of formula I antagonize the actions of one or more of the arachidonic acid metabolites known as leukotrienes. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compound, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.

Carbocyclic compounds useful as leukotriene antagonists

This invention provides a series of novel heterocyclic amides of formula I in which the group &gt;X--Y--Z&lt; is selected from &gt;C.dbd.CH--N&lt;, &gt;C.dbd.N--N&lt;, &gt;N--(CH.sub.2)--N&lt;, &gt;CH--CH.sub.2 --N&lt; and &gt;N--N.dbd.C&lt; and the other radicals have the meanings defined in the following specification. The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compounds, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.

Carboxamide derivatives

Heterocyclic amide derivatives and use

The invention provides a series of novel heterocyclic amides of the formula I in which the group A CRa can be --CRb.dbd.CRa--, --CHRb--CHRa-- or --N.dbd.CRa--, the amidic group Re.L can be Re.X.CO.NH, Re.X.CS.NH or Re.NH.CO attached at position 4, 5 or 6 of the benzenoid moiety, Z is an acid group selected from the group consisting of carboxy, an acylsulphonamide residue of the formula CO.NH.SO.sub.n Rg and a tetrazolyl residue of the formula II, and the radicals Ra, Rb, Rc, Rd, Re, Rf, Rg, Rh, n, X, G.sup.1, Q and G.sup.2 have the meanings defined in the following specification. The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compounds, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.

Indazole compounds, pharmaceutical compositions and use

This invention provides a series of novel heterocyclic amides of formula I in which the group &gt;X-Y-Z&lt; is selected from &gt;C.dbd.CH--N&lt;, &gt;C.dbd.N--N&lt;, &gt;N--(CH.sub.2)--N&lt;, &gt;CH--CH.sub.2 --N&lt; and &gt;N--N.dbd.C&lt; and the other radicals have the meanings defined in the following specification.

Carboxamide derivatives of indoles and leucotriene antagonizing use

This invention provides a series of novel heterocyclic carboxamides of formula I in which the group --Y--Z&lt; is selected from --C(Ra).dbd.C&lt;, --N.dbd.C&lt;, and --CH(Ra)--CH&lt; and the other radicals have the meanings defined in the following specification. The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compound, or their salts, for use in the treatment of, for example, allergic or inflammatory diseasxes, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.

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Kennett Square, PA, United States of America

Ying K Yee