Vernalis Research Limited

Hoffmann-la Roche Inc.

Other

F. Hoffmann-la Roche Ag

Jonathan Mark Bentley

David Reginald Adams

Jonathan Richard Anthony Roffey

Stephan Roever

Paul Hebeisen

Hans G Richter

Howard Langham Mansell

Sven Taylor

James Edward Paul Davidson

Richard John Hamlyn

Ashley Roger George

Patrizio Mattei

Claire Elizabeth Dawson

Nathaniel Monck

Ian Anthony Cliffe

Robert Mark Pratt

Marc Muller

Suneel Gaur

Matthew Alexander James Duncton

Nathaniel Julius Thomas Monck

Jacques Mizrahi

Michael John Bickerdike

Matthias Heinrich Nettekoven

Jean-Marc Plancher

Wolfgang Guba

Henri Stalder

Jean-Luc Specklin

Timothy James Morley

Guy Anthony Kennett

Corinna Dagmar Bodkin

Toby Jonathan Blench

David Bebbington

Kerry Wilkinson

Sean Lightowler

Steven Paul Vickers

Vicki Ruston

The present invention refers to chemical compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein Rto Rhave the significance given in claim. These compounds can be used for the preparation of medicaments.

Morpholine derivatives as 5HT2C receptor agonists for the treatment of obesity

The present invention is directed to 1,2,3,4,10,10a,-hexahydropyrazino[1,2-a]indole derivatives as well as pharmaceutically acceptable salts, solvates and esters thereof, wherein Rto Rhave the significance given in claim 1 be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, obesity and sleep apnea.

Anti-obesity 1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles

The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts, solvates and esters thereof. These compounds can be used to prepare pharmaceutical compositions for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.

1,2,3,4,9,9a-hexahydro-2,4a,5-triaza-fluorene and 1,2,3,4-tetrahydro-2,4a,5-triaza-fluorene derivatives

The present invention is a chemical compound of formula (I)or a pharmaceutically acceptable salts, solvates and esters thereof, wherein Rto R, A, Am and n are as described in the specification.

Piperazine derivatives

The present invention is directed to 1,2,3,4,10,10a-hexahydropyrazino [1,2-a]indole derivatives of formula (I):as well as pharmaceutically acceptable salts, hydrates and esters thereof, wherein the substituents have the meanings provided in the specification. Compounds of the present invention may be used in the treatment or prevention of obesity or Type II diabetes.

A chemical compound of formula (I) wherein: R and R are independently selected from hydrogen and alkyl; R is alkyl; R , R and R are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsufoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; R is selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; A is a 5- or 6-membered partially unsaturated or aromatic heterocyclic ring or a 5- or 6-membered partially unsaturated carbocyclic ring, wherein if A is a 6-membered partially unsaturated carbocyclic ring then at least one of R to R is other than hydrogen, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof, and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinial disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.

Indole derivatives process for their preparation, pharmaceutical compositions containing them and their medicinal application

Fused indole derivatives

Aza- indolyl derivatives for treating obesity

A chemical compound of formula (I) wherein R to R are independently selected from hydrogen and alkyl; R to R are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, monoalkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, arylthio, arylsulfoxyl, arylsulfonyl, alkylsulfoxyl, alkylsulfonyl, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino; and R is selected from alkyl and alkoxy, and pharmaceutically acceptable salts and prodrugs thereof, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.

Indazole derivatives with 5-HT2 receptor activity

The present invention relates to indoline derivatives. These compounds are especially useful for the prevention and treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes, sleep apnea, and especially for the treatment and prevention of obesity.

Indoline derivatives and method of treating obesity

A chemical compound of formula (I), wherein n is 1, 2 or 3; R and R are independently selected from hydrogen and alkyl; R is alkyl; R to R are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, or R and R together form a carbocyclic or heterocyclic ring, and pharmaceutically acceptable salts and prodrugs thereof, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders, diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity

Pyrroloindoles, pyridoindoles and azepinoindoles as 5-ht2c agonists

Indoline derivatives as 5-HT2B and or 5-HTC receptor ligands

 A chemical compound of formula (I), wherein R to R are independently selected from hydrogen and alkyl; R is selected from hydrogen, alkyl, alkoxy, formyl and cyano; X is selected from N and C&mdash;R ; X is selected from N and C&mdash;R ; X is selected from N and C&mdash;R ; X is selected from N and C&mdash;R ; wherein at least one of X , X , X and X is N; and R to R are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus; and sleep apnea, and particularly for the treatment of obesity.

Pyrroloquinolines for treatment of obesity

Growing community of inventors

Wokingham, United Kingdom

Jonathan Mark Bentley