Pfizer Corporation

Other

David Alker

Peter E. Cross

Robert J. Bass

Peter E Cross

Roger P Dickinson

Simon F Campbell

John E Arrowsmith

Ian T Barnish

John C Danilewicz

Alexander Roderick MacKenzie

John K Stubbs

Geoffrey N Thomas

Malcolm Morville

Brian Gadsby

John Edward Kemp

Robert M Wallis

Kenneth Richardson

Kelvin Cooper

Alan Stobie

Michael J Fray

Robert J Bass

Michael G Page

Kevin Neil Dack

John Steele

Michael J Parry

A compound of the formula: or a pharmaceutically acceptable salt thereof, wherein Y is a direct link, --(CH.sub.2 --, --(CH.sub.2).sub.2 --, --CH.sub.2 O-- or CH.sub.2 S--; R is --CN or --CONH.sub.2 ; and R.sup.1 is a group of the formula: ##STR1## where R.sup.2 and R.sup.3 are each independently H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, --(CH.sub.2).sub.n OH, halo, trifluoromethyl, cyano, --(CH.sub.2).sub.n NR.sup.4 R.sup.5, --CO(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.4 alkyl), --CH(OH) (C.sub.1 -C.sub.4 alkyl), --C(OH) (C.sub.1 -C.sub.4 alkyl).sub.2, --SO.sub.2 NH.sub.2, --(CH.sub.2).sub.n CONR.sup.4 R.sup.5 or --(CH.sub.2).sub.n COO(C.sub.1 -C.sub.4 alkyl; R.sub.4 and R.sup.5 are each independently H or C.sub.1 -C.sub.4 alkyl; n is 0, 1 or 2; and 'Het' is pyridyl, pyrazinyl or thienyl. The compounds are muscarinic receptor antagonists usedful in the treatment of diseases associated with the altered motility and/or tone of smooth muscle, especially irritable bowel syndrome.

Muscarinic receptor antagonists

Indole derivatives thromboxane A2 antagonists

The invetion is a method of treating irritable bowel syndrome with a compound selected from the formula ##STR1## wherein R, R.sup.1, m, n p are as defined in the specification, or a pharmaceutically acceptable salt thereof.

Quinuclidine esters process and intermediate for their preparation and

Synthetic intermediates of 1-arylethyl-3-substituted piperidines. The Intermediates include the 3R,S- and 3R-forms of the compounds having the following formulae: ##STR1##

1-arylethyl-3-substituted piperidines

Selective muscarinic receptor antagonists of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are both optionally substituted phenyl, the broken line is an optional bond, X is &gt;COH--, &gt;SiOH-- or CH-- when the double bond is absent or is &gt;C.dbd. when the double bond is present, X being attached to a carbon atom of A, A is selected from certain piperidine and pyrrolidine groups, n is 1 to 3 and R.sup.3 is optionally substituted phenyl or thienyl, pyridyl or pyrazinyl.

Anticholinergic agents

A compound of the formula ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup..sup.4, Y, m and n are defined herein are useful as muscarinic receptor antagonists.

Synthetic intermediates of 1-arylethyl-3-substituted piperidines. The Intermediates includes the 3R,S- and 3R-forms of the compounds having the following formulae: ##STR1##

Certain 1-azabicyclo[2.2.1]heptanes useful as muscarinic receptor

Piperidine and pyrrolidine derivatives

Compounds of the formula I ##STR1## wherein X, Y and v are as defined below, novel intermediates used in their synthesis, and the pharmaceutically acceptable salts of such compounds and intermediates. The compounds of formula I and the novel intermediates used in their synthesis are muscarinic receptor antagonists that are selected for smooth muscle muscarinic sites and are useful in the prevention and treatment of diseases associated with altered motility or tone of smooth muscle, such as irritable bowel syndrome, diverticular disease, urinary incontinence, aesophageal achalasia, and chronic obstructive airways disease.

Growing community of inventors

Canterbury, United Kingdom

Peter E Cross