Pfizer Corporation

Alan Stobie

Donald Stuart Middleton

Michael J Fray

Mark David Andrews

David Hepworth

Geoffrey E Gymer

Charles Eric Mowbray

Thomas Ryckmans

Justin Stephen Bryans

Patrick Stephen Johnson

Peter E Cross

Gavin Alistair Whitlock

Chikara Uchida

Paul Vincent Fish

David Cameron Pryde

Florian Michel Wakenhut

Andrew Simon Cook

Adam Gillmore

Stephen Challenger

David John Bull

Elisabeth Colette Louise Gautier

Mavis Diane Adam

Christopher Lee Carr

Simon F Campbell

Alan Daniel Brown

Harry Ralph Howard

Mark Edward Bunnage

John Paul Mathias

Seiji Nukui

Harry R Howard, Jr

Kiyoshi Kawamura

Mikio Morita

Lee Richard Roberts

Hirohide Noguchi

Julian Blagg

Michael John Humphrey

Sachiko Mihara

Robert James Crook

Mark Leonard Elliott

Mark Ian Lansdell

David Charles Waite

Mark Llewellyn Lewis

Mark Henryk Stefaniak

David Fenwick

Toby James Underwood

Malcolm Christian Mackenny

Helen Janet Mason

Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein:

Triazole derivatives which inhibit vasopressin antagonistic activity

A compound of formula (I), or a pharmaceutically acceptable derivative, wherein A, B, V, W, X, Y, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof.

Triazole compounds useful in therapy

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

A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein:

Amides useful as monoamine re-uptake inhibitors

A compound of formula (I), or a pharmaceutically acceptable derivative thereof, wherein A, B, V, W, X, Y, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof.

Compounds of the formula (I): or a pharmaceutically acceptable salt, prodrug, solvate or polymorph thereof, wherein R, R, and Z are as defined herein, are useful in treating or preventing a condition for which an NKantagonist is efficacious.

Lactams as tachykinin antagonists

This invention provides compounds of the formula (I) and (II):or the pharmaceutically acceptable esters thereof, and the pharmaceutically acceptable salts thereof: wherein Ris hydrogen or halo; Rand Rare independently hydrogen or Calkyl; Rand Rare independently hydrogen or Calkyl; Ris hydrogen, Calkyl, Calkoxy (C)alkyl or Calkyl substituted by up to 3 substituents selected from the groups consisting of Ccycloalkyl, aryl, heteroaryl and heterocyclic; Rand Rare hydrogen or taken together may form alkylene chain having one or two carbon atoms; Ris Calkyl or Ccycloalkyl; Ris Calkyl or NRR; L is (CRR)or NR; M is NRor (CRR); Rand Rare independently hydrogen or Calkyl; n is an integer from 0 to 5; and m is an integer from 0 to 2; said heterocyclic, aryl and heteroaryl are unsubstituted or are substituted by at least one substituent selected from the group consisting of halo and Calkyl; with the proviso that when Ris Calkyl, L is not NR. These compounds have 5-HTreceptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

Oxo or oxy-pyridine compounds as 5-HT4 receptor modulators

Compounds of formula (I):or pharmaceutically acceptable salts or solvates thereof, wherein

Quinazolinone compounds useful in therapy

The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein Ris optionally substituted Calkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, Calkoxy, &#x2014;NRRor &#x2014;NRSOR; X is the linkage &#x2014;(CH)&#x2014; or &#x2014;(CH)&#x2014;O&#x2014; (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by Calkoxy; hydroxy; hydroxy(Calkyl); Ccycloalkyl; carbocyclyl; heterocyclyl; or by Calkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two Rgroups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.

N-phenpropylcyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase

The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R is optionally substituted C alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C alkoxy, &mdash;NR R or &mdash;NR SO R ; X is the linkage &mdash;(CH ) &mdash; or &mdash;(CH ) &mdash;O&mdash; (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C alkoxy; hydroxy; hydroxy(C alkyl); C cycloalkyl; carbocyclyl; heterocyclyl; or by C alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.

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

Imidazopyridine compounds as 5-HT4 receptor modulators

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

Alan Stobie