US 2010/0144716 A1Published application

New CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions

AssigneeBoehringer Ingelheim International GmbH

InventorsStephan Georg MUELLER, Klaus RUDOLF, Philipp LUSTENBERGER, Dirk STENKAMP, Marco SANTAGOSTINO, Fabio PALEARI, Gerhard SCHAENZLE, Kirsten ARNDT, Henri DOODS

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Abstract

The present invention relates to the CGRP-antagonists of general formula I wherein R1, R2, R3, R4 and X are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, mixtures and salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, as well as those compounds of general formula I in which one or more hydrogen atoms are replaced by deuterium, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.

Claims11

Dependent claims

A compound of the formula

wherein
X denotes CH2, NH, C1-3-alkyl-N, O or S,
R1 denotes a moiety selected from the group consisting of
wherein
R1.1 denotes H, halogen, HO, F3C or C1-6-alkyl-O,
R2 denotes a group of the formulae II
wherein
R2.1 denotes H, halogen, C1-3-alkyl-O, C1-3-alkyl or F3C,
R2.2 denotes H, H2N, HO, H3C—O, H—C(O)—O or C1-3-alkyl-C(O)-O,
R2.3 denotes H, halogen, C1-3-alkyl or F3C, or
R2 denotes a moiety selected from the group consisting of
wherein
R2.4 denotes H or H3C,
R3 denotes a group of the formulae III
wherein
R3.1 denotes H, C1-3-alkyl or R3.1.1—(O)C,
R3.1.1 denotes HO or C1-6-alkyl-O,
R3.2 denotes H or C1-3-alkyl and
R3.3 denotes a free pair of electrons or the oxygen atom,
R4 denotes a 4- to 7-membered oxycycloalkyl group optionally substituted by R4.1 and
R4.1 denotes NC, HO, C1-3-alkyl or C1-3-alkyl-O,
or a tautomer or salt thereof.

19 more elements

Dependencies are inferred from the claim text.

Facts

Application: 12/707,890Filed 18 Feb 2010
Priority: AR 05010113923 Mar 2005
Published: 10 Jun 2010
Term ends: Not estimatedThe source records don’t support an estimate.

Classification23 codes

C07D 405/12
Containing two hetero rings: linked by a chain containing hetero atoms as chain links
A61P 1/00
Drugs for disorders of the alimentary tract or the digestive system
A61P 1/02
Drugs for disorders of the alimentary tract or the digestive system: stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
A61P 1/10
Drugs for disorders of the alimentary tract or the digestive system: laxatives

Family

Application11/277,177Division · filed 22 Mar 2006
Application12/363,175Division · filed 30 Jan 2009
Application12/707,890Division
US 2006/0252931 A1Published application
US 2009/0186881 A1Published application
US 7,528,129 B2Related patent
US 7,696,209 B2Related patent
US 2010/0144716 A1This patent

From the US filing history. Foreign family members aren’t listed.