Pfizer Corporation

Infineum International Limited

Mark David Andrews

David Hepworth

Donald Stuart Middleton

Alan Stobie

Alan Daniel Brown

Paul Anthony Stupple

Gavin Alistair Whitlock

Karl Richard Gibson

Geoffrey E Gymer

Paul Vincent Fish

Thomas Ryckmans

Sharanjeet Kaur Bagal

Sarah Elizabeth Skerratt

Kiyoyuki Omoto

Mavis Diane Adam

Mark Ian Lansdell

Benjamin Robert Elvidge

Harry Ralph Howard

Harry R Howard, Jr

Michael J Fray

Christopher Gordon Barber

Julian Blagg

Florian Michel Wakenhut

David Graham Brown

Yogesh Sabnis

Mark Leonard Elliott

Wolfgang Klute

Inaki Morao

R Ian Storer

Paul Brennan

Nicholas William Summerhill

The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.

Pyrrolo[3,2-c]pyridine tropomyosin-related kinase inhibitors

Pyrrolo[2,3-d]pyrimidine tropomysin-related kinase inhibitors

The present invention relates to compounds of formula (I) wherein R, R, R, R, L and n are as defined in the specification. These compounds are useful as MC4 agonists. 

Diazepine and diazocane compounds as MC4 agonists

The present invention relates to a class of melanocortin MCR4 agonists of general formula (I) wherein the variables and substituents are as defined herein and especially to selective MCR4 agonist compounds, to their use in medicine, particularly in the treatment of sexual dysfunction and obesity, to intermediates useful in their synthesis and to compositions containing them.

Melanocortin type 4 receptor agonist piperidinoylpyrrolidines

The present invention provides a compound of formula (I): or a pharmaceutically acceptable salt thereof wherein the variables R, R, R, R, R, R, and Rare as defined herein. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a 5-HTreceptor-mediated disorders with a compound of formula (I) or a pharmaceutical composition comprising a compound of formula (I).

[object Object]

A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein Ris H, Calkyl, &#x2014;C(X)Y, Ccycloalkyl, aryl, het, aryl-Calkyl or het-Calkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from Calkyl, Calkoxy, OH, halo, CF, OCF, SCF, hydroxy-Calkyl, Calkoxy-Calkyl and Calkyl-S&#x2014;Calkyl; Ris aryl or heteroaryl, each optionally substituted by at least one substituent independently selected from Calkyl, Calkoxy, OH, halo, CF, OCF, SCF, hydroxy-Calkyl, Calkoxy-Calkyl and Calkyl-S&#x2014;Calkyl; Ris Calkyl, Ccycloalkyl, Ccycloalkyl-Calkyl, aryl, het, aryl-Calkyl or het-Calkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from Calkyl, Calkoxy, OH, halo, CF, OCF, SCF, hydroxy-Calkyl, Calkoxy &#x2014;Calkyl and Calkyl-S&#x2014;Calkyl; X is S or O; Y is H, Calkyl, aryl, het, aryl-Calkyl or het-Calkyl; and n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral center. The compounds of the invention exhibit activity as both serotonin and noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.

Compounds

The invention relates to compounds of formula I 

Phenyl heterocyclyl ethers

The invention relates to compounds of formula I

Diaryl compounds

The invention provides compounds of general formula (I) wherein R is H or C -C alkyl; R and R , together with the interconnecting atoms form a 4 to 8-membered saturated ring containing one or two heteroatoms (including the nitrogen to which R is attached) wherein a second heteroatom, if present, is selected from oxygen, nitrogen and sulfur, with the proviso that said ring cannot contain two adjacent heteroatoms; Z is CF , OCF , C -C alkylthio or C -C alkoxy; Y is hydrogen, halogen, &mdash;OR , R or C -C alkylthio, and wherein R is C -C alkyl optionally substituted with fluorine atoms; or when Z and Y are attached para and meta to the ether linkage linking rings A and B, Z and Y are linked so that, together with the interconnecting atoms, Z and Y form a fused 5 to 7-membered carbocyclic or heterocyclic ring which may be saturated, unsaturated or aromatic, and wherein when Z and Y form a heterocyclic ring, in addition to carbon atoms, the linkage contains one or two heteroatoms independently selected from oxygen, sulfur and nitrogen; and Z and Y together do not form a fused phenyl ring; R and R , which may be the same or different, are: A&mdash;X, wherein A&equals;&mdash;CH&boxH;CH&mdash; or &mdash;(CH ) &mdash; where p is 0, 1 or 2; X is hydrogen, F, Cl, Br, I, CONR R , SO NR R , SO NHC(&boxH;O)R , OH, C alkoxy, NR SO R , NO , NR R , CN, CO R , CHO, SR , S(O)R or SO R ; or a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O, optionally substituted independently by one or more R ; wherein R is hydroxy, C -C alkoxy, F, C -C alkyl, haloalkyl, haloalkoxy, &mdash;NH , &mdash;NH(C -C alkyl) or &mdash;N(C -C alkyl) .

Phenoxyphenylheterocyclyl derivatives as SSRIs

A compound of general formula (I) wherein R and R are H, C -C alkyl or (CH ) (C -C cycloalkyl) wherein d&equals;0, 1, 2 or 3; or R and R together with the nitrogen to which they are attached form an azetidine ring; Z or Y is &mdash;SR and the other Z or Y is halogen or &mdash;R ; wherein R is C -C alkyl optionally substituted with fluorine; except that R is not CF ; or Z and Y are linked so that, together with the interconnecting atoms, Z and Y form a fused 5 to 7-membered carbocyclic or heterocyclic ring, and wherein when Z and Y form a heterocyclic ring, in addition to carbon atoms, the linkage contains one or two heteroatoms independently selected from oxygen, sulfur and nitrogen; R and R , which may be the same or different, are: A&mdash;X, wherein A&equals;&mdash;CH&boxH;CH&mdash; or &mdash;(CH ) &mdash; where p is 0, 1 or 2; X is hydrogen, F, Cl, Br, I, CONR R , SO NR R , SO NHC(&boxH;O)R , OH, C alkoxy, NR SO R , NO , NR R , CN, CO R , CHO, SR , S(O)R or SO R ; or a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O, optionally substituted independently by one or more R ; wherein R is hydroxy, C -C alkoxy, F, C -C alkyl, haloalkyl, haloalkoxy, &mdash;NH , &mdash;NH(C -C alkyl) or &mdash;N(C -C alkyl) .

Phenoxybenzylamine derivatives as SSRIs

A compound of general formula (I), or pharmaceutically acceptable salts, solvates or polymorphs thereof; wherein; R and R , which may be the same or different, are hydrogen, C -C alkyl, (CH ) (C -C cycloalkyl) wherein m &equals;0, 1, 2 or 3, or R and R together with the nitrogen to which they are attached form an azetidine ring; each R is independently CF , OCF , C alkylthio or C -C alkoxy; n is 1, 2 or 3; and R and R , which may be the same or different, are: A&mdash;X, wherein A &equals;&mdash;CH&equals;CH&mdash; or &mdash;(CH )p&mdash; where p is 0, 1 or 2; X is hydrogen, F, Cl, Br, I, CONR R , SO NR R , SO NHC(&equals;O)R , OH, C alkoxy, NR SO R , NO , NR R , CN, CO R , CHO, SR , S(O)R or SO R ; R , R , R and R which may be the same or different, are hydrogen or C alkyl optionally substituted independently by one or more R ; R is C alkyl optionally substituted independently by one or more R ; R is hydrogen, C alkyl optionally substituted independently by one or more R , C(O)R , CO R , C(O)NHR or SO NR R ; R is F, OH, CO H, C cycloalkyl, NH , CONH , C alkoxy, C alkoxycarbonyl or a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O optionally substituted independently by one or more R ; or R and R , together with the nitrogen to which they are attached, form a 4-, 5- or 6-membered heterocyclic ring optionally substituted independently by one or more R ; or a 5- or 6-membered heterocyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O, optionally substituted independently by one or more R ; wherein R is hydroxy, C -C alkoxy, F, C -C alkyl, haloalkyl, haloalkoxy, &mdash;NH , &mdash;NH(C -C alkyl) or &mdash;N(C -C alkyl) ; wherein when R and R are methyl, R and R are hydrogen and n is 1, R is not a &mdash;SMe group para to the ether linkage linking rings A and B.

Diphenyl ether compounds useful in therapy

Growing community of inventors

Sandwich, United Kingdom

Mark David Andrews