Abstract: The invention relates to novel diphenyl-substituted heterocycles with 6-membered ring of general formula (I)
in which A, X and the residues R1, R2, R3, R4 and R5 are as defined in the claims, processes for the preparation thereof and the use thereof as medicaments.
Type:
Grant
Filed:
April 12, 1999
Date of Patent:
May 22, 2001
Assignees:
Boehringer Ingelheim Pharma KG, Boehringer Ingelheim Italia S.p.A.
Inventors:
Michael Brenner, Rainer Palluk, Marion Wienrich, Thomas Weiser, Enzo Cereda, Maura Bignotti, Carlo Maria Pellegrini, Giovanni Battista Schiavi, Raffaele Cesana
Abstract: Pharmacologically active novel esters and amides of di-substituted 1,4 piperidine as 5-HT.sub.4 antagonists of formula (I) ##STR1## wherein A, X, Y and R have the meanings specified in the description, and a process for their preparation, are disclosed.
Abstract: Pharmacologically active benzimidazolone derivatives as 5-HT.sub.1A and 5-HT.sub.2 receptors, useful in the treatment of CNS disorders, of formula: ##STR1## wherein the substituents are defined herein.
Type:
Grant
Filed:
March 23, 1994
Date of Patent:
November 19, 1996
Assignee:
Boehringer Ingelheim Italia S.p.A.
Inventors:
Giuseppe Bietti, Franco Borsini, Marco Turconi, Ettore Giraldo, Maura Bignotti
Abstract: A method for treating a human host suffering from psychosis, which method comprises administering to such host a therapeutically effective amount of a compound of the formula I ##STR1## wherein the radicals are defined in claim 1.
Type:
Grant
Filed:
May 1, 1994
Date of Patent:
September 3, 1996
Assignee:
Boehringer Ingelheim Italia S.p.A.
Inventors:
Marco Turconi, Arturo Donetti, Ernesto Montagna, Massimo Nicola, Annamaria Uberti, Rosamaria Micheletti, Antonio Giachetti
Abstract: Crystalline and pharmacologically active monohydrates of endo-2,3-dihydro-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2-oxo-1H-benzimi dazole-1-carboxamide hydrochloride and of endo-3-ethyl-2,3-dihydro-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2-oxo-1H -benzimidazole-1-carboxamide hydrochloride.
Type:
Grant
Filed:
June 22, 1994
Date of Patent:
November 21, 1995
Assignee:
Boehringer Ingelheim Italia S.p.A.
Inventors:
Enzo Cereda, Antoine Ezhaya, Marco Turconi, Enrica Dubini, Grazia Maffione
Abstract: Pharmacologically active benzimidazoline-2-oxo-1-carboxylic acid compounds which are useful for treating a human host suffering from anxiety.
Type:
Grant
Filed:
March 16, 1993
Date of Patent:
October 25, 1994
Assignee:
Boehringer Ingelheim Italia
Inventors:
Marco Turconi, Arturo Donetti, Ernesto Montagna, Massimo Nicola, Annamaria Uberti, Rosamaria Micheletti, Antonio Giachetti
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.
Type:
Grant
Filed:
March 4, 1992
Date of Patent:
June 29, 1993
Assignee:
Boehringer Ingelheim Italia S.p.A.
Inventors:
Marco Turconi, Arturo Donetti, Ernesto Montagna, Massimo Nicola, Annamaria Uberti, Rosamaria Micheletti, Antonio Giachetti
Abstract: Orally administrable pharmaceutical preparation containing an active ingredient to be released in the lower part of the gastrointestinal tract, i.e. in the large intestine, and especially colon, consisting of a core containing a therapeutically active substance and coated with three protection layers at different solubility. The manufacturing and the use of these preparations are also described.