Kalvista Pharmaceuticals Limited

Ferring B.v.

David Philip Rooker

David Michael Evans

Rebecca Louise Davie

Hannah Joy Edwards

Simon Teanby Hodgson

Gary Robert William Pitt

Andrzej Roman Batt

Michael Bryan Roe

Stephen John Pethen

Steven John Hewison

Hanna Joy Edwards

The present invention provides a selection of compounds of formula (I): (I) compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein R5, R6, R7, A, B, W, X, Y and Z are as defined herein. 

Pyrazole derivatives as plasma kallikrein inhibitors

The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein A, B, W, X and Y are as defined herein. 

Bicyclic inhibitors

The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein Rto Rare as defined herein.

Benzylamine derivatives as inhibitors of plasma kallikrein

The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein Rto Rare as defined herein. 

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.

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Salisbury, United Kingdom

David Philip Rooker