Ici Americas, Inc.

Zeneca Limited

Frederick J Brown

Ying K Yee

Peter R Bernstein

Victor G Matassa

Keith Russell

Paul James Warwick, Jr

Thomas P Maduskuie, Jr

Compounds of formula I ##STR1## wherein X.sup.a, X.sup.b, R, R.sup.1 and R.sup.2 have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful as potassium channel openers for the treatment of urinary incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Methods for using benzoxazines for treating asthma

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

2-fluoroalkyl-1,4-benzoxaxines as potassium channel mediators

Heterocyclic amide derivatives

Heterocyclic amide derivatives and pharmaceutical use thereof

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.

Heterocyclic carboxamides

This invention provides a series of novel heterocyclic aliphatic carboxamides of formula I in which the group &gt;Z--Y--X&lt; is selected from &gt;C.dbd.CH--N&lt;, &gt;N--CH.dbd.C&lt;, &gt;C.dbd.N--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 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.

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Newark, DE, United States of America

Frederick J Brown