Pfizer Corporation

Neurogen Corporation

Martin Patrick Allen

Spiros Liras

Alan J Hutchison

Jun Yuan

Kevin S Currie

Scott A Mitchell

Pamela Ann Albaugh

George D Maynard

Yuhpyng Liang Chen

Linda M Gustavson

Robert L Rosati

Guolin Cai

George P Luke

Kyungae Lee

Manuka Ghosh

Guiying Li

Nian Liu

Barbara Eileen Segelstein

Ling Hong Xie

Brian Thomas O'Neill

Jotham Wadsworth Coe

John M Peterson

Christopher John O'Donnell

Thomas Allen Chappie

John Michael Humphrey

William Michael Whalen

Vinod Singh

Xie Ling Hong

This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I. The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAreceptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAreceptors in tissue sections.

Benzimidazole and pyridylimidazole derivatives

The invention provides compounds of Formula I:  wherein R, R, R, R, R, R, Rand A are as defined. Compounds of formula I have activity inhibiting production of A&#x3b2;-peptide. The invention also provides pharmaceutical compositions and methods for treating diseases, for example Alzheimer's disease, in mammals comprising compounds of Formula I.

Pyrazole compounds for treatment of neurodegenerative disorders

The present invention provides a compound having the structure of formula I: wherein Ris hydrogen, (C&#x2013;C) alkyl, unconjugated (C&#x2013;C) alkenyl, benzyl, YC(&#x2550;O)(C&#x2013;C) alkyl or &#x2014;CHCH&#x2014;O&#x2014;(C&#x2013;C) alkyl; X is CHor CHCH; Y is (C&#x2013;C) alkylene; Z is (CH), CF, or C(&#x2550;O), where m is 0, 1 or 2; Rand Rare selected independently from hydrogen, halogen, &#x2014;(C&#x2013;C) alkyl optionally substituted with from 1 to 7 halogen atoms, and &#x2014;O(C&#x2013;C) alkyl optionally substituted with from 1 to 7 halogen atoms, or Rand Reach together with the atom to which it is connected independently form C(&#x2550;O), S&#x2192;O, S(&#x2550;O), or N&#x2192;O; and is a 5- to 7-membered monocyclic heteroaryl group selected from pyridinyl, pyridone, pyridazinyl, imidazolyl, pyrimidinyl, pyrazolyl, triazolyl, pyrazinyl, furyl, thienyl, isoxazolyl, thiazolyl, oxazolyl, isothiazolyl, pyrrolyl, cinnolinyl, triazinyl, oxadiazolyl, thiadiazolyl and furazanyl groups.

Heteroaryl fused azapolycyclic compounds

This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I  The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAreceptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAreceptors in tissue sections.

The invention pertains to substituted quinazoline and isoquinoline compounds that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE-10. The invention also relates to intermediates for preparation of said compounds; pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders.

Tetrahydroisoquinolinyl derivatives of quinazoline and isoquinoline

The invention provides compounds of Formula I: wherein R, R, R, R, R, R, R, and A are as defined. Compounds of formula I have activity inhibiting production of A&#x3b2;-peptide. The invention also provides pharmaceutical compositions and methods for treating diseases, for example Alzheimer's disease, in mammals comprising compounds of Formula I.

3,3-Biarylpiperidine and 2,2-biarylmorpholine derivatives

3,3-biarylpiperidine and 2,2-biarylmorpholine derivatives

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North Stonington, CT, United States of America

Martin Patrick Allen