Syntex (u.s.a.) Inc.

Roche Palo Alto LLC

F. Hoffmann-la Roche Ag

Jacob Berger

Robin D Clark

Shu-Hai Zhao

Lee Allen Flippin

Francisco Javier Lopez-Tapia

Klaus Kurt Weinhardt

Joseph M Muchowski

Robert J Greenhouse

Keith Adrian Murray Walker

Saul Jaime-Figueroa

Klaus K Weinhardt

Joan Marie Caroon

John O Gardner

Aubry Kern Miller

David George Putman

Yanzhou Liu

Fang-Ting Chiu

Dov Nitzan

William L Smith

Richard M Eglen

Robert James Weikert

Christine E Brotherton-Pleiss

David Garrett Loughhead

Douglas L Wren

Nancy Elisabeth Krauss

Lee Edwin Lowrie, Jr

Paul E Weller

John Cureton Hunter

David S Carter

Robin Douglas Clark

Jr Lee Edwin Lowrie

The present invention provides a compound of the formula: a pharmaceutically acceptable salt or a prodrug thereof, where R, R, R, R, R, R, R, R, R, Y, Z, m, n, and p are as defined herein. The present invention also provides compositions comprising, methods for using, and methods for preparing Compound of Formula I.

Benzoxazine derivatives and uses thereof

Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R, R, R, R, Rand Rare as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.

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Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, R, R, R, R, Rand Rare as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.

Compounds of the formula I: wherein m, n, p, X, Ar, R, R, R, Rand Rare as defined herein. Methods of making the compounds and using the compounds for treatment of 5-HT6 receptor-mediated diseases are disclosed.

Compounds of the formula I: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein m, n, p, Ar, X, R, R, R, R, Rand Rare as defined herein. Also provided are compositions comprising, methods of preparing, and methods of using the subject compounds.

Arylsulfonyl benzodioxanes, benzoxazines and benzothiazines as 5-HT6 antagonists

Compounds of the formula (I): or pharmaceutically acceptable salts, solvates or prodrugs thereof, where R, R, R, R, R, R, R, R, R, X, Y and m are as defined herein. Also provided are compositions comprising, methods for using, and methods for preparing compound of formula (I).

Compounds of the formula:or pharmaceutically acceptable salts or prodrugs thereof, where each of n and p independently is 2 or 3, Y is &#x2014;SO&#x2014; or &#x2014;SO&#x2014;N(R)&#x2014;, Zis CH or N, and R, R, R, R, R, R, R, R, Rand Rare as defined herein. The compounds have selective 5-HT6 affinity and are useful in the treatment of certain CNS disorders. Also provided are compositions comprising, methods for using, and methods for preparing Compounds of Formula I.

Arylsulfonyl derivatives with 5-HT6 receptor affinity

The aryl pyrimidine derivatives and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, including utility as selective 5HT.sub.2B -antagonists. The 5-HT.sub.2B antagonist is a compound of the formula: ##STR1## wherein: R.sup.1 is hydrogen, alkyl, lower alkoxy, hydroxyalkyl, cycloalkyl, cycloalkyl lower alkyl, alkenyl, lower thioalkoxy, halo, fluoroalkyl, --NR.sup.6 R.sup.7, --CO.sub.2 R.sup.8, --O(CH.sub.2).sub.n R.sup.9, or lower alkyl optionally substituted with hydroxy, alkoxy, halo, or aryl; in which

Aryl pyrimidine derivatives and uses thereof

The aryl pyrimidine derivatives and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, including utility as selective 5HT.sub.2B -antagonists.

Aryl pyrimidine derivatives

The disclosed pyrimidine derivatives, and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, in particular use as selective 5HT.sub.2B -antagonists. The invention is also directed to formulations and methods for treatment.

Heterocyclic compounds of Formula I: ##STR1## in which n is 2, 3, 4, 5 or 6; t is 1, 2, 3 or 4; u is 0 or 1 (provided that t is not 1 when u is 0); X is O or N(R.sup.4); Y and Z are independently C(O), C(S) or CH.sub.2 (provided that Y and Z are not both CH.sub.2); R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as defined in the specification; and their pharmaceutically acceptable salts and N-oxides, formulations containing them, their uses as therapeutic agents, and their synthesis.

1,3,8-triaza- and 3,8-diaza-1-oxaspiro �4,5! decane derivatives

This invention relates to a compound of the Formula I: ##STR1## as a racemic mixture and its individual enantiomers, in particular the (R)-enantiomer, and their pharmaceutically acceptable salts. These compounds are useful as sodium channel blockers, and are particularly useful for the alleviation of neuropathic pain.

Treatment of neuropathic pain

This invention relates to 2-(1'-azabicyclo[2.2.2]oct-3'S-yl)-6-hydroxy-2,4,5,6-tetrahydro-1H-benz[de ]isoquinolin-1-one and 2-(1'-azabicyclo[2.2.2]oct-3'S-yl)-6-hydroxy-2,3,3a,4,5,6-hexahydro-1H-ben z[de]isoquinolin-1-one and their individual stereoisomers and uses and the processes for their making.

Growing community of inventors

Los Altos Hills, CA, United States of America

Jacob Berger