Astrazeneca Ab

Niklas Plobeck

William Brown

Christopher Walpole

Andrew Griffin

Paul Jones

Daniel Pagé

The invention relates to at least one compound of general formula I wherein Ris phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, or pyridine N-oxide, where each Rphenyl and Rheteroaromatic ring may optionally and independently be substituted by 1, 2 or 3 substituents selected from CF, methyl, iodo, bromo, fluoro, and chloro; Ris independently selected from ethyl and isopropyl;Ris hydrogen or fluoro; Ris &#x2014;NHor &#x2014;NHSOR; and Ris hydrogen, &#x2014;CF, or C-Calkyl, or pharmaceutically acceptable salts thereof; at least one process for making at least one compound in accordance with Formula I; at least one method for treating at least one &#x3b4; receptor associated condition with at least one compound in accordance with Formula I; and at least one pharmaceutical composition comprising at least one compound in accordance with Formula I.

4-(phenyl-piperazinyl-methyl)benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestinal disorders

Compounds of general formula: wherein R, Rand Rare as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.

4(phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain or gastrointestinal disorders

The invention relates to at least one compound of general formula I wherein Ris phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, or pyridine N-oxide, where each Rphenyl and Rheteroaromatic ring may optionally and independently be substituted by 1, 2 or 3 substituents selected from CF, methyl, iodo, bromo, fluoro, and chloro; Ris independently selected from ethyl and isopropyl;

Compounds

An asymmetric synthesis of diarylmethylpiperazines is described. The synthetic route enables preparation of a variety of enatiomerically pure amines with different N-alkyl groups. The invention includes an asymmetric addition of organometallic compounds to chiral sulfinimine to give adducts in predominantly one diastereomer can subsequently be transferred into pure enantiomers of by cleavage of the chiral auxilliary which is followed by synthesis of the piperazine ring by alkylation procedures.

Asymmetric process for the preparation of diarylethylpiperazines derivatives and novel asymmetric diarylmethylamines as intermediates

Compounds of general formula: wherein Rand Rare as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.

4(Phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain or gastrointestinal disorders

Compounds of general formula (I) wherein R, Rand Rare as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain 

4(Phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain of gastrointestinal disorders

Compounds of general formula I Ris selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, and pyridine N-oxide; Ris independently selected from ethyl and isopropyl; Ris independently selected from hydrogen and fluoro; Ris independently selected from &#x2014;OH, &#x2014;NHand &#x2014;NHSOR; and Ris independently selected from hydrogen, &#x2014;CFand C&#x2013;Calkyl, or salts thereof or separate enantiomers and salts thereof; where each Rheteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C&#x2013;Calkyl, NO, CF, C&#x2013;Calkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as separate enantiomers of the compounds and salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety and functional gastrointestinal disorders.

Growing community of inventors

Södertälje, Sweden

Niklas Plobeck