Ferring B.v.

Vantia Limited

Michael Bryan Roe

Andrzej Roman Batt

Peter Hudson

Celine Marguerite Simone Heeney

Andrew John Baxter

David Michael Evans

Gary Robert William Pitt

David Philip Rooker

David Raymond Churchley

Valerie Elizabeth Peal

Martin Lee Stockley

Rachel Louisa Charlotte Handy

Rachel Handy

Peter Andrew Robson

Timothy John Kenhardt Gibs

Timothy John Gibbs

Celine Heeney

Roman Batt Andrzej

Timothy John Kenhardt Gibbs

Rachel Louisa Handy

The invention provides cyclopropanecarboxylic acid 4-(6-chloro-3-methyl-4,10-dihydro-3H-2,3,4,9-tetraazabenzo[f]azulene-9-carbonyl)-2-fluoro-benzylamide para-toluenesulphonate, pharmaceutical compositions containing it, and its use in therapy.

Tosylate salt of cyclopropanecarboxylic acid 4-(6-chloro-3-methyl-4, 10-dihydro-3H-2,3,4,9-tetrabenzo[f]azulene-9-carbonyl)-2-fluorobenzylamide

The present invention concerns compounds inter alia according to general formula 1. Compounds according to the invention are vasopressin Vreceptor antagonists. Pharmaceutical compositions of the compounds are useful as treatment of dysmenorrhoea. 

[object Object]

Novel compounds according to general formula 1, wherein Gis NRRor a fused polycyclic group that are specific OT receptor agonists and/or Vreceptor antagonists. Pharmaceutical compositions comprising such compounds are useful in the treatment of, inter alia, primary dysmenorrhoea. 

Benzamide derivatives as oxytocin agonists and vasopressin antagonists

Compounds according to general formula 1, wherein A-Aare selected from Aand Awhere Ais either &#x2550;CR&#x2014; or &#x2550;N&#x2014; and Ais &#x2014;NR&#x2014;, &#x2014;O&#x2014; or &#x2014;S&#x2014;; Ais either a covalent bond or A, provided that when Ais a covalent bond one of A-Amust be Aand the other two must be Aand when Ais Athen all of A-Amust be A; Ris selected from H, NHY' and COY, in which case Ris H, or Rand R2 may both be methyl or together represent &#x2550;O; R, Rand Rare each independently selected from H and lower alkyl groups; R, R, R, R, R, Rand Rare each independently selected from H, lower alkyl groups, NH, halogens (F, Cl and Br) O-alkyl, CHNMand CF; Ris selected from H, F, Cl Br, NO, NH, OH, Me, Et, OMe, NMeand CF; Ris selected from H, methyl and ethyl; W is selected from &#x2550;CH&#x2014; and &#x2550;N&#x2014;; X is selected from CH, O, S, SO, NH and N lower alkyl; Yis selected from CO-lower alkyl, CO(CH)Y, CO(CH)COYand CO(CH)NHCOY, where b is 1-3; Y2 is selected from OR, NRRand NH(CH)COY, where c is 1-3; Yis selected from ORand NRR; Ris selected from H, lower alkyl and (CH)R, where a is 0-4; Rand Rare each independently selected from H, lower alkyl and (CH)Ror together are &#x2014;(CH)-Z-(CH&#x2014;; Ris OH a phenyl group or an aromatic heterocycle selected from pyridyl, pyrimidinyl, pyrazinyl, furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, triazolyl, oxadiazolyl and thiadiazolyl, each of which may optionally have a lower alkyl group substituent; and Z is selected from O, CH, S, SO, NH and N-lower alkyl, are new. They are useful in the treatment of breast and prostate cancer, endometriosis and benign prostate hyperplasia, in the regulation of fertility, and in in vitro fertilisation.

Non-peptide GnRH antagonists

Growing community of inventors

Southampton, United Kingdom

Michael Bryan Roe