|Abstract:||Compounds of the formula ##STR1## wherein R, Y and R.sup.1 are as defined in the specification. These compounds are muscarinic receptor antagonists which are selective for smooth muscle muscarinic sites over cardiac muscarinic sites, and are useful in the treatment of diseases associated with altered motility on tone of smooth muscle, including irritable bowel syndrome, diverticular disease, urinary incontinence, oesophageal achalasia and chronic obstructive airways disease.|
|Inventor(s):||Cross; Peter E. (Canterbury, GB2), MacKenzie; Alexander R. (Deal, GB2)|
|Assignee:||Pfizer Inc. (New York, NY)|
1. A compound of the formula: ##STR43## 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
R is --CONH.sub.2 ; and
R.sup.1 is a group of the formula: ##STR44## where X and X.sup.1 are each independently O or CH.sub.2 ;
m is 1, 2 or 3; and
"Het" is pyridyl, pyrazinyl or thienyl.
2. A compound as claimed in claim 1 in which R.sup.1 is a group of the formula: ##STR45## where X, X.sup.1, "Het" and m are as defined in claim 1.
3. A compound as claimed in claim 2, in which R.sup.1 is a group of the formula: ##STR46##
4. A compound as claimed in claim 1, in which Y is a direct link or --CH.sub.2 --.
5. A compound as claimed in claim 4, in which Y is --CH.sub.2 --.
6. A compound as claimed in claim 1, which is in the 3R,S-(racemic) or 3S-form.
7. 3-(R,S )-(1-carbamoyl-1,1-diphenylmethyl)-1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl]p yrrolidine or 3-(S)-(-)-(1-carbamoyl-1,1-diphenylmethyl)-1-[2-(2,3-dihydrobenzofuran-5-y l)ethyl]pyrrolidine.
8. A pharmaceutical composition comprising muscarinic receptor antagonizing effective amount of a compound according to claim 1 and a pharmaceutically acceptable diluent or carrier.
9. A method of treating a disease associated with altered motility or tone of smooth muscle in a mammal comprising administering to said mammal a muscarinic receptor antagonizing amount of a compound according to claim 1.
10. A method according to claim 9, wherein the disease is irritable bowel syndrome.
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.