Abstract: Compounds of general formula (I)
wherein R1, R2, R3, and R4 denote hydrogen or hydroxy with the proviso that R1, R2, R3, and R4 cannot simultaneously represent hydrogen, processes for their preparation of the compounds of general formula (I), and their use as pharmaceuticals.
Type:
Grant
Filed:
August 8, 2000
Date of Patent:
August 28, 2001
Assignee:
Ingelheim Italia S.p.A.
Inventors:
Enzo Cereda, Maura Bignotti, Giovanni Battista Schiavi
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: 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.