Imperial Chemical Industries Limited

Pfizer Corporation

Syngenta Corporation

David A. Roberts

Robin Wood

Arnold H. Ratcliffe

Keith Hopkinson Gibson

Simon T. Russell

David A Roberts

Simon F Campbell

Robert Hugh Bradbury

Robert J Pearce

Arnold H Ratcliffe

Martin P Edwards

Simon T Russell

Andrew Peter Thomas

David Waterson

John K Stubbs

David J Brown

Albert A Jaxa-Chamiec

Richard William Luke

David S Morris

The invention concerns pharmaceutically useful novel compounds of the formula I, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, Ra, A, X and Z have the various meanings defined herein, and their non-toxic salts, and pharmaceutical compositions containing them. The novel compounds are of value in treating conditions such as hypertension and congestive heart failure. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment. ##STR1##

Quinoline derivatives and use thereof as angiotensin II antagonists

The invention concerns pharmaceutically useful compounds of the formula I, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X and Z have the various meanings defined herein, and their non-toxic salts, and pharmaceutical compositions containing them. The novel compounds are of value in treating conditions such as hypertension and congestive heart failure. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.

Pyridine compounds which have useful pharmaceutical utility

There are disclosed quinolines of the formula ##STR1## wherein R.sup.1 is hydrogen, or hydrocarbyl. R.sub.3 and R.sub.4 are independently, H, alkyl, various functional groups or alkylenedioxy, X is phenylene optionally bearing a substituent, R.sub.a is (1-4)C alkyl optionally bearing one or more F's, Z is various carboxyl derivatives, useful as angiotensin II antagonists.

Biphenylene branched alkyleneoxy quinolines

Pyridine compounds which are useful as angiotensin II receptor

The invention concerns pharmaceutically useful novel compounds of the formula I, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X, X.sup.1 and Z have the various meanings defined herein, and their non-toxic salts, and pharmaceutical compositions containing them. The novel compounds are of value in treating conditions such as hypertension and congestive heart failure. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.

Angiotensin II antagonizing compounds containing a 1,5-naphthyridine or

The invention concerns pharmaceutically useful compounds of the formula I, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, n, m, X, Y and Z have the various meanings defined herein, and their non-toxic salts, and pharmaceutical compositions containing them. The novel compounds are of value in treating conditions such as hypertension and congestive heart failure. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.

Angiotensin II antagonizing fused pyridinyloxy containing derivatives

The invention concerns pharmaceutically useful novel compounds of the formula I, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X and Z have the various meanings defined herein, and their non-toxic salts, and pharmaceutical compositions containing them. The novel compounds are of value in treating conditions such as hypertension and congestive heart failure. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.

Angiotension II antagonizing pyridine derivatives

The invention concerns novel heterocyclic compounds of the formula I as defined herein and their physiologically acceptable salts, together with pharmaceutical compositions containing them. The heterocyclic compounds antagonize the actions of angiotensin II and are of value in treating diseases or medical conditions such as hypertension and congestive heart failure in warm-blooded animals. The invention further includes processes for the manufacture of the novel compounds and their use in medical treatment.

Benz[4,5]imidazole-containing angiotensin antagonists

Angiotensin II antagonizers which are condensed pyridine derivatives

The invention concerns pharmaceutically useful novel compounds of the formula I, in which ring B, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X and Z have the various meanings defined herein, and their non-toxic salts, and pharmaceutical compositions containing them. The novel compounds are of value in treating conditions such as hypertension and congestive heart failure. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.

Diazine derivatives and pharmaceutical use

This invention concerns novel nitrogen derivatives of the formula I ##STR1## (and their pharmaceutically-acceptable salts), together with pharmaceutical compositions containing them. The nitrogen derivatives are inhibitors of the catalytic action of renin. The invention further concerns novel processes for the manufacture of said inhibitors.

5-(heterocyclylalkanoyl)amino-4-hydroxypentanamides

A series of novel heterocyclic-substituted 2-(1H)-quinolone compounds have been prepared, including the 3,4-dihydro derivatives thereof, wherein the heterocyclic ring moiety is a pyrrolyl, imidazolyl, pyrazolyl, triazolyl or tetrazolyl group attached by a nitrogen atom of said group to the 5-, 6-, 7- or 8-positions of the quinolone ring. These particular compounds are useful in therapy as highly potent inotropic agents and therefore, are of value in the treatment of various cardiac conditions. Preferred member compounds include 6-(2,4-dimethylimidazol-1-yl)-8-methyl-2-(1H)-quinolone, 6-(2,4-dimethyl-5-nitroimidazol-1-yl)-8-methyl-2-(1H)-quinolone, 8-methyl-6-(tetrazol-1-yl)-2-(1H)-quinolone, 8-methyl-6-(1,2,4-triazol-4-yl)-2-(1H)-quinolone, and 6-(4-cyano-2-methylimidazol-1-yl)-8-methyl-2-(1H)-quinolone, respectively. Methods for preparing these compounds from known starting materials are provided.

precursors to Quinolone inotropic agents

A series of novel heterobicyclic substituted 2-(1H)-quinolone compounds have been prepared, including the 3,4-dihydro derivatives thereof, wherein the heterobicyclic ring moiety is an optionally-substituted indolyl, phthalizinyl, benzimidazolyl, imidazopyridinyl, quinolinyl or isoquinolinyl group attached by an nitrogen or carbon atom of said group to the 6-position of the quinolone ring. The optional substituent is a C.sub.1 -C.sub.14 alkyl group located on either of the two heterobicyclic rings and/or an oxo group situated on the heterocyclic portion of said heterobicyclic ring system. These particular compounds are useful in therapy as cardiac stimulants and therefore, are of value in the treatment of various cardiac conditions. 6-{1(H)-Imidazo[4,5-b]pyridin-6-yl}-8-methyl-2-(1H)-quinolone represents a typical and preferred member compound. Methods for preparing these compounds from known starting materials are provided.

Imidazo[4,5-b]pyridyl quinolone cardiac stimulants

A series of novel heterocyclic-substituted 2-(1H)-quinolone compounds have been prepared, including the 3,4-dihydro derivatives thereof, wherein the heterocyclic ring moiety is a pyrrolyl, imidazolyl, pyrazolyl, triazolyl or tetrazolyl group attached by a nitrogen atom of said group to the 5-, 6-, 7- or 8-positions of the quinolone ring. These particular compounds are useful in therapy as highly potent inotropic agents and therefore, are of value in the treatment of various cardiac conditions. Preferred member compounds include 6-(2,4-dimethylimidazol-1-yl)-8-methyl-2-(1H)-quinolone, 6-(2,4-dimethyl-5-nitroimidazol-1-yl)-8-methyl-2-(1H)-quinolone, 8-methyl-6-(tetrazol-1-yl)-2-(1H)-quinolone, 8-methyl-6-(1,2,4-triazol-4-yl)-2-(1H)-quinolone, and 6-(4-cyano-2-methylimidazol-1-yl)-8-methyl-2-(1H)-quinolone, respectively. Methods for preparing these compounds from known starting material are provided.

Precursors to quinolone inotropic agents

A series of novel heterocyclic-substituted 1,2,3,5-tetrahydroimidazo(2,1-b)quinazolin-2-(1H)-one compounds have been prepared, including their pharmaceutically acceptable salts, wherein the heterocyclic ring moiety is an optionally substituted 5- or 6-membered aromatic heterocyclic group attached to the 6-, 7-, 8- or 9-positions of the aforesaid tetrahydroquinaxolinone ring. These particular compounds are useful in therapy as highly potent inotropic and therefore, are of value in the treatment of various cardiac conditions. Preferred member compounds include 7-(2,4-dimethylimidaxol-1-yl)-9-methyl-1,2,4,5,-tetrahydroimidazo (2,1-b)quinazolin-2-(1H)-one, 3,9-dimethyl-7-(2,4-dimethylimidazol-1-yl) -1,2,3,5-tetrahydroimidazo(2,1-b)quinazolin-2-(1H)-one and 9-methyl-7 -(1,2,4-triazol-4-yl)-1,2,3,5-tetrahydroimidazo(2,1-b)quinazolin-2-(1H)-on e, respectively. Methods for preparing these compounds from known starting materials are provided.

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Congleton, United Kingdom

David A Roberts