Warner-lambert Company

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Neurosearch A/s

Thomas C Malone

Jagadish C Sircar

Graham Johnson

Michael Francis Rafferty

Christopher Franklin Bigge

Yuntao Song

Lain-Yen Hu

Robert Michael Schelkun

David T Connor

Bruce D Roth

Po-wai Yuen

Todd Robert Ryder

Laszlo Nadasdi

Balazs G Szoke

Laszlo Urge

Chung Stephen Yi

Diego F Silva

Frank Watjen

Louis Brogley

Harriet W Hamilton

Richard John Booth

Wayne Livingston Cody

Anthony Denver Sercel

John Xiaoqiang He

Perry M Novak

Leonard Joseph Lescosky

Quinoxalinedione derivatives, their preparation and use

Substituted diarylalkyl amides as calcium channel antagonists

Peptidyl calcium channel blockers

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

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

Substituted phenols as novel calcium channel blockers

Substituted peptidylamine calcium channel blockers

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

Processes for the preparation of a series of tetracyclic amines useful in the treatment and/or prevention of cerebrovascular disorders are disclosed.

Process for preparing tetracyclic amines useful as cerebrovascular agents

The present invention is novel substituted .alpha.-amino acids, pharmaceutical compositions, methods of use, and preparations therefore having utility for treating disorders which benefit from blockade of aspartate and glutamate receptors.

Substituted .alpha.-amino acids having selected acidic moieties for use

The present invention relates to novel compounds, which are derivatives of ureas, thioureas, carbamates, sulfonylureas, sulfonamides, amides, and thioamides of 2-carboxyindoles as illustrated by the formula ##STR1## The invention also relates to methods for the preparation of the novel compounds, as well as to pharmaceutical compositions or methods of use for the novel compounds. More specifically, the compounds of the present invention are useful in the treatment of neurodegenerative disorders including cerebrovascular disorders as well as in the treatment of schizophrenia or epilepsy; and as analgesics and anxiolytics.

Substituted 2-carboxylindoles having pharmaceutical activity

The present invention relates to novel tetracyclic amines and derivatives thereof useful as pharmaceutical agents, to methods for their production, to pharmaceutical compositions which include these compounds and a pharmaceutically acceptable carrier, and to pharmaceutical methods of treatment. The compounds of the present invention are useful in the treatment of neurodegenerative disorders including cerebrovascular disorders.

Tetracyclic amines having pharmaceutical activity

A novel series of tetracyclic amines, methods of preparation, compositions containing the amines, and methods for using them in the treatment and/or prevention of cerebrovascular disorders are disclosed.

Tetracyclic amines useful as cerebrovascular agents

The present invention is various 7-deazaguanines having activity as immunomodulators. Also included are pharmaceutical compositions and methods of use thereof.

7-deazaguanines as immunomodulators

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Canton, MI, United States of America

Thomas C Malone