Asterand UK Limited

Novartis Ag

Glaxo Group Limited

Pharmagene Laboratories Limited

Garry Fenton

Alexander W Oxford

George Hynd

Jonathan Mark Sutton

David Edward Clark

Kenneth Lyle Clark

Robert Alexander Coleman

Neil Victor Harris

Richard Jon Davis

Keith Alfred James Stuttle

Edward Andrew Boyd

Mark Richard Ashton

Shirley Ann Brunton

Keith A J Stuttle

Christopher G Newton

Richard Sedrani

Nils Ostermann

Christine Edwards

Daniel Baeschlin

Simon John Fawcett MacDonald

Gordon G Weingarten

Kenji Namoto

Finton Sirockin

A compound of formula (III): or a salt, solvate and chemically protected form thereof, wherein: Ris an optionally substituted Caryl or Calkyl group; L' is a single bond, &#x2014;O&#x2014; or &#x2014;C(&#x2550;O)&#x2014;; A is selected from the group consisting of: formula (i) (ii) (iii) wherein X and Y are selected from the group consisting of: O and CR; S and CR; NH and CR; NH and N; O and N; S and N; N and S; and N and O, and where the dotted lines indicate a double bond in the appropriate location, and where Q is either N or CH; D is selected from: formula (i) (ii) (iii) (iv) (v) (vii) (viii) (ix) B is selected from the group consisting of: formula (A) (B) where Ris selected from fluoro and chloro; and Ris either: (i) &#x2014;COH; (ii) &#x2014;CONH; (iii) &#x2014;CH&#x2014;OH; or (iv) tetrazol-5-yl. 

[object Object]

The present invention is directed to compounds of formula (I): whereinR represents a methyl or an ethyl groupX represents N, C&#x2014;H or C&#x2014;CHwhen X represents C&#x2014;H or C&#x2014;CH, Y represents Nwhen X represents N, Y represents C&#x2014;Hand physiologically functional derivatives thereof, pharmaceutical compositions comprising the compounds, the use of the compounds for the manufacture of medicaments particularly for the treatment of inflammatory and/or allergic conditions, processes for the preparation of the compounds, and chemical intermediates in the processes for the manufacture of the compounds.

Tetrahydro-naphthalene derivatives as glucocorticoid receptor modulators

The present invention relates to compounds of the formula; and their use in therapy.

Organic compounds

Compounds of formula (I): wherein: Ris H or an optionally substituted Calkyl group; Y is either &#x2014;(CH)&#x2014;X&#x2014;, where n is 1 or 2 and X is O, S, S(&#x2550;O), S(&#x2550;O), or NR, where Ris selected from H or optionally substituted Calkyl, or Y is &#x2014;C(&#x2550;O)NR&#x2014;, where Ris selected from H, and optionally substituted Calkyl or Caryl; Ris an optionally substituted Caryl group linked to a further optionally substituted Caryl group, wherein if both Caryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a Calkylene group; and Ris either: or wherein R is optionally substituted Calkyl, Caryl or NRR, where Rand Rare independently selected from optionally substituted alkyl;

The disclosure provides EPreceptor agonist compounds and methods for using the compounds for treating conditions which can be alleviated by agonism of an EPreceptor.

A compound of formula (I): or a salt, or chemically protected form thereof, wherein: Ris an optionally substituted phenyl;   Where Ris selected from H and Calkyl; where one of Rand Ris &#x2014;C-alkylene-Rand the other of Rand Ris H, m and n can be 0 or 1, and m+n=1 or 2; and additionally, when Ris &#x2014;C-alkylene-R, m can also be 2 or 3, and m+n=1, 2, 3 or 4, and when Ris tetrazol-5-yl, m+n may be 0; or where one of Rand Ris &#x2014;O&#x2014;CH&#x2014;R, and the other of Rand Ris H, n is 0; Ris H or optionally substituted Calkyl; Ris either: (i) &#x2014;COH; (ii) &#x2014;CONH; (iii) &#x2014;CH&#x2014;OH; or (iv) tetrazol-5-yl.

EP2 receptor agonists

Compounds of formula (I): wherein: Ris H or an optionally substituted Calkyl group; Y is either &#x2014;(CH)&#x2014;X&#x2014;, where n is 1 or 2 and X is O, S, S(&#x2550;O), S(&#x2550;O), or NR, where Ris selected from H or optionally substituted Calkyl, or Y is &#x2014;C(&#x2550;O)NR&#x2014;, where Ris selected from H, and optionally substituted Calkyl or Caryl; Ris an optionally substituted Caryl group linked to a further optionally substituted Caryl group, wherein if both Caryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a Calkylene group; and Ris either:  wherein R is optionally substituted Calkyl, Caryl or NRR, where Rand Rare independently selected from optionally substituted Calkyl;

A compound of formula (I): or a salt, solvate and chemically protected form thereof, wherein one of Rand Ris:  wherein R is optionally substituted Calkyl, Caryl, or NRR, where Rand Rare independently selected from optionally substituted Calkyl; or

A compound of formula (I): or a salt, solvate and chemically protected form thereof, wherein: wherein X and Y are selected from the group consisting of:  

Compounds of formula (I): wherein: Ris H or an optionally substituted Calkyl group; Y is either &#x2014;(CH)&#x2014;X&#x2014;, where n is 1 or 2 and X is O, S, S(&#x2550;O), S(&#x2550;O), or NR, where Ris selected from H or optionally substituted Calkyl, or Y is &#x2014;C(&#x2550;O)NR&#x2014;, where Ris selected from H, and optionally substituted Calkyl or Caryl; Ris an optionally substituted Caryl group linked to a further optionally substituted Caryl group, wherein if both Caryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a Calkylene group; and Ris either: or &#x2003;wherein R is optionally substituted Calkyl, Caryl or NRR, where Rand Rare independently selected from optionally substituted Calkyl;

Growing community of inventors

Harlow, United Kingdom

Garry Fenton