Roche Palo Alto LLC

Syntex (u.s.a.) Inc.

Cv Therapeutics, Inc.

F. Hoffmann-La Roche Ag

Chris Richard Melville

David Mark Rotstein

Xiaoming Zhang

Cyrus K Becker

Eun Kyung Lee

Fernando Padilla

Jürg Roland Pfister

Joan Marie Caroon

Jeff A Zablocki

Venkata Poornapragnacharyulu Palle

Counde O'Yang

Jim W Li

Francisco Javier Lopez-Tapia

Terrence Joseph Connolly

Brent K Blackburn

Klaus K Weinhardt

Dov Nitzan

Paul Francis Keitz

Jutta Wanner

Remy Lemoine

Elfaith O Elzein

Lisa Wang

J&uuml;rg Pfister

Patrick Finbar McGarry

Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are alleviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula I. 

Heterocyclic antiviral compounds

This invention relates to piperidine derivatives of formula I wherein R, R, Rand Rare as defined herein useful in the treatment of a variety of disorders, including those in which the modulation of CCR5 receptors is implicated. Disorders that may be treated or prevented by the present derivatives include HIV and genetically related retroviral infections (and the resulting acquired immune deficiency syndrome, AIDS), rheumatoid arthritis, solid organ transplant reject (graft vs. host disease), asthma and COPD. 

Heterocylic antiviral compounds

Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) wherein R-Rand Ar are as defined herein are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are alleviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula I. 

Octahydro-pyrrolo[3,4-c]pyrrole CCR5 receptor antagonists

Compounds represented by Formula I: which are useful as are alpha-1A/B adrenoceptor antagonists, to methods of treating conditions associated with the activity of alpha-1A/B adrenoceptors, and to methods of making said compounds, wherein Ar, Z, R, R', Rand Rare as defined herein.

Arylamine-substituted quinazolinone compounds useful as alpha 1A/B adrenergic receptor antagonists

Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are allieviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula I. 

This invention relates to compounds which are generally alpha-1A/B adrenoceptor antagonists and which are represented by Formula I: 

Quinazolone derivatives as alpha 1A/B adrenergic receptor antagonists

This invention relates to compounds which are generally alpha-1A/B adrenoceptor antagonists and which are represented by Formula I:wherein Z is &#x2014;C(O)&#x2014; or &#x2014;S(O)&#x2014;, X is carbon or nitrogen, Y is carbon, and X&#x2014;Y considered together are two adjoining atoms of the ring A, said ring being a fused aromatic ring of five to six atoms per ring optionally incorporating one to two heteroatoms per ring, chosen from N, O, or S; and the other substituents are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

Orally active A1 adenosine receptor agonists

Quinazoline derivatives as alpha-1 adrenergic antagonists

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Palo Alto, CA, United States of America

Chris Richard Melville