Warner-lambert Company

Other

Pfizer Corporation

Cocensys Inc.

Neurosearch A/s

Christopher Franklin Bigge

Graham Johnson

Sui Xiong Cai

Nancy C Lan

Eckard Weber

Anthony P Guzikowski

Richard Woodward

Zhang-Lin Zhou

Charles Price Taylor, Jr

Devin Franklin Welty

John F Keana

John F W Keana

Thomas C Malone

Chung Stephen Yi

Po-wai Yuen

Gian Luca Araldi

Jeremy John Edmunds

Kevin James Filipski

Agustin Casimiro-Garcia

Jonathan L Wright

Danette Andrea Dudley

Robert Michael Schelkun

Chad Alan Van Huis

Donald Lamunyon

James Jia-He Li

Jeffrey Thomas Kohrt

John S Kiely

Frank Watjen

Mark J Suto

Michael R Pavia

Edward Faith Elslager

James C French

Gerard C Hokanson

Shelly Ann Glase

Daniel Fred Ortwine

Josefino B Tunac

Mark Robert Barvian

Sheryl Jeanne Hays

Corinne E Augelli-Szafran

Tomoyuki Yasunaga

Nancy Sue Barta

Yingjie Lai

Takenori Kimura

Vlad E Gregor

Tim A Smitka

John H Wilton

Blanche D Graham

John Fw Keana

Perry M Novak

Robert Schaum

Shunichiro Hachiya

Annette Theresa Sakkab

Larry Craswell Walker

Nian Zhuang

James T Drummond

Daniel Martin Retz

Gerald David Nordblom

Stephen W Mamber

Nancy F Lan

The present invention provides compounds of Formula (I): wherein A, B, C, G, and Whave any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thrombotic disorders. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.

Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade

The present invention provides compounds of Formula (I):wherein A, B, C, G, and Whave any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thrombotic disorders. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.

The present invention provides a method of treating Alzheimer's disease using a compound of Formula (I). Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of the Formula (I) and a method of imaging amyloid deposits, as well as new compounds of Formula (I).

Method of inhibiting amyloid protein aggregation and imaging amyloid deposits

The present invention provides compounds of Formula (I) and a method of treating Alzheimer's disease using a compound of Formula (I), wherein: Rand Rinclude alkyl and phenylalkyl; Ris hydrogen or alkyl; and Rand Rinclude alkyl, alkoxy, carboxyl, alkoxycarbonyl, and nitro. Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of Formula (I)and a method of imaging amyloid deposits using compounds of Formula (I).

Method of inhibiting amyloid protein aggregation and imaging amyloid deposits using aminoindane derivatives

Quinoxalinedione derivatives, their preparation and use

Antidiabetic agents

Novel 2-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 2-substituted piperidine analogs as selectively active antagonist of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, anxiety, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headaches, chronics pain, glaucoma, CMV retinitis, psychosis, urinary incontinence, opioid tolerance or withdrawal, or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.

2-substituted piperidine analogs and their use as subtype-selective NMDA receptor antagonists

The invention relates to subtype-selective NMDA receptor ligands and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, Parkinson's disease, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.

Subtype-selective NMDA receptor ligands and the use thereof

Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using the 4-substituted piperidine analogs as selectively active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as cerebral ischemia, central nervous system trauma, hypoglycemia, neurodegenerative disorders, anxiety, migraine headaches, convulsions, aminoglycoside antibiotics-induced hearing loss, chronic pain, psychosis, glaucoma, CMV retinitis, opioid tolerance or withdrawal, urinary incontinence and neurodegenerative disorders such as lathyrism, Alzheimers' Disease, Parkinsonism, and Huntington's Disease are described. Also described are novel methods for preparing 4-substituted piperidine analogs and novel intermediates of the 4-substituted piperidine analogs.

4-substituted piperidine analogs and their use as subtype selective NMDA receptor antagonists

The invention relates to subtype-selective NMDA receptor ligands and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neuro-degenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, Parkinson's disease, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.

Novel N-substituted azacycloalkyl ring fused 2,3-quinoxalinediones represented by the formula:

Glutamate (ampa/kainate) receptor antagonists: N-substituted fused azacycloalkylquinoxalinediones

4-substituted piperidine analogs and their use as subtype selective NMDA

2-substituted piperidine analogs and their use as subtype-selective NMDA

Novel N-substituted azacycloalkyl ring fused 2,3-quinoxalinediones are disclosed represented by the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is hydrogen, alkyl or W-alkyl; X and Y are independently hydrogen, halogen, nitro, cyano, trifluoromethyl, SO.sub.2 CF.sub.3, SO.sub.2 R.sup.4, SO.sub.2 NR.sup.4 R.sup.5, alkyl, alkenyl, (CH.sub.2).sub.z CONR.sup.4 R.sup.5, (CH.sub.2).sub.z COOR.sup.4, or NHCOR.sup.4, wherein R.sup.4 and R.sup.5 are independently hydrogen, alkyl having 1 to 6 carbon atoms, cycloalkyl or W-alkyl, and z is an integer from 0 to 4; R.sup.2 is benzoyl, W, W-alkyl, COcycloalkyl, COalkyl-W, CONR.sup.3 alkyl, CONR.sup.3 -W, CONR.sup.3 alkyl-W, CSNR.sup.3 alkyl, CSNR.sup.3 alkyl-W, ##STR2## or a moiety derived from a common amino acid by removal of the --OH from the carboxyl group which is alpha to the amino, wherein --W is aryl, heteroaryl, or the heterocycles piperidinyl, piperazinyl, morpholinyl or pyrrolidinyl, wherein R.sup.3 is hydrogen, alkyl or W-alkyl; and m and n are independently 0, 1 or 2 provided that m+n is &gt;1; provided that when R.sup.2 is benzoyl, ##STR3## or X is nitro, Y and R.sup.1 are H, m is 2 and n is 1; when R.sup.2 is ##STR4## X is nitro, Y and R.sup.1 are H and m is 2 and n is 1; or when R.sup.2 is ##STR5## X is bromo, Y and R.sup.1 are H, m is 1 and n is 2. The novel N-substituted azacycloalkyl ring fused 2,3-quinoxalinediones may be used, for example, as neuroprotective agents, for treatment of chronic neurodegenerative disorders, as anticonvulsants and in the treatment of schizophrenia, epilepsy, anxiety, pain and drug addiction.

Glutamate (ampa/kainate) receptor antagonists: N-substituted fused

Growing community of inventors

Ann Arbor, MI, United States of America

Christopher Franklin Bigge