Imperial Chemical Industries Limited

Zeneca Limited

Imperial Chemical House

Ici Pharma

Keith H Gibson

Cyrus J Ohnmacht

Keith Russell

Robert J Pearce

Robin Wood

Arnold H Ratcliffe

Brian B Masek

Pierre A Bruneau

James Roy Empfield

Frank Carey

Christian R Delvare

Russell Keith

Rodger M McMillan

The invention concerns quinazoline derivatives of the formula I ##STR1## wherein n is 1,2 or 3 and each R.sup.2 is independently halogeno, trifluoromethyl or (1-4C)alkyl;

Quinazoline derivatives

Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the aides and pharmaceutical compositions containing them.

Method of preparing therapeutic amides

Therapeutic amides

Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the amides and pharmaceutical compositions containing them.

Compounds of formula I ##STR1## wherein X, A, B, R.sup.1 and R.sup.2 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable ester thereof, processes for preparing the compounds and pharmaceutical compositions comprising them. The compounds are useful as potassium channel openers and as therapeutic agents in the treatment of urinary incontinence.

Therapeutic alcohols

Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolyzable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the amides and pharmaceutical compositions containing them.

The invention concerns pharmaceutically useful compounds of the formula I, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, Ra, Rb, 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.

1,6-naphthyridinone derivatives having angiotension II antagonist

1,6-naphthyridone derivatives having angiotensin II antagonist activity

The invention concerns pharmaceutical compositions containing a 1,2-dihydro-3H-indazol-3-one derivative of the formula I ##STR1## wherein Ra is hydrogen, halogeno, nitro, hydroxy, (2-6C)alkanoyloxy, (1-6C)alkyl, (1-6C)alkoxy, fluoro-(1-4C)alkyl, (2-6C)alkanoyl, amino, (1-6C)alkylamino, di-[(1-4C)alkyl]amino, (2-6C)alkanoylamino or hydroxy-(1-6C)alkyl; Rb is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy; and Y is a group of the formula --A.sup.1 --X--A.sup.2 --Q in which A.sup.1 is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene, or A.sup.1 is phenylene; X is oxy, thio, sulphinyl, sulphonyl, imino, (1-6C)alkylimino, (1-6C)alkanoylimino, iminocarbonyl or phenylene, or X is a direct link to A.sup.2 ; A.sup.2 is (1-6C)alkylene, (3-6C)alkenylene or (3-6C)alkynylene or A.sup.2 is cyclo(3-6C)alkylene or is a direct link to Q, or the group --A.sup.1 --X--A.sup.2 -- is a direct link to Q; or Y is (2-10)alkyl, (3-10C)alkenyl or (3-6C)alkynyl; and Q is aryl or heteroaryl. The invention also provides novel 1,2-dihydro-3H-indazol-3-ones, processes for their production and the use of 1,2-dihydro-3H-indazol-3-ones for the manufacture of medicaments for the treatment of various allergic and inflammatory diseases.

Therapeutic preparations containing indazole derivatives

This application describes novel 17-(optionally substituted)phenyl-18,19,20-trinorprosta-16-ynoic acid derivatives of the F, E and A series, for example methyl 9.alpha.,11.alpha.,15-trihydroxy-17-phenyl-18,19,20-trinorprosta-5-cis,13- trans-dien-16-ynoate, together with processes for their manufacture, pharmaceutical or veterinary compositions containing them, and a method of luteolysis in a mammalian host.

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Macclesfield, United Kingdom

Keith H Gibson