The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Jun. 29, 1993

Filed:

Mar. 04, 1992
Applicant:
Inventors:

Marco Turconi, Voghera, IT;

Arturo Donetti, Milan, IT;

Ernesto Montagna, San Giuliano Milanese, IT;

Massimo Nicola, Pavia, IT;

Annamaria Uberti, Milan, IT;

Rosamaria Micheletti, Milan, IT;

Antonio Giachetti, Milan, IT;

Assignee:
Attorneys:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C07D / ; A61K / ;
U.S. Cl.
CPC ...
514304 ; 546126 ;
Abstract

New pharmacologically active benzimidazoline-2-oxo-1-carboxylic acid derivatives which are 5-HT receptor antagonists useful as antiemetic agents and as gastric prokinetic agents of the following formula: ##STR1## wherein R is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl; R.sub.1 is hydrogen; R.sub.2 is hydrogen, halogen or C.sub.1-6 alkoxy; Y is oxygen or N--R.sub.3 in which R.sub.3 is hydrogen; A is a group selected from: ##STR2## wherein p is 1; r is 0, 2 or 3: R.sub.4 is hydrogen; R.sub.5 is hydrogen, C.sub.1-6 alkyl, or R.sub.5 is a group of the formula --CR.sub.6 =N--R.sub.7 wherein R.sub.6 is hydrogen, C.sub.1-4 alkyl or amino and R.sub.7 is hydrogen or C.sub.1-6 alkyl; or a pharmaceutically acceptable acid addition salt thereof. The processes for the preparation of the compounds of formula (I) as well as pharmaceutical compositions contained in them are also described.


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