Torrey Pines Institute for Molecular Studies

University of South Florida

The Burnham Institute

University of California

Trega Biosciences, Inc.

Mixture Sciences, Inc.

Adel Nefzi

Richard Allen Houghten

John M Ostresh

John C Reed

Clemencia Pinilla

Lindsey Neil Shaw

Marcello Angelo Giulianotti

Renee Marie Fleeman

Radleigh G Santos

Kate Welsh

Zhiwei Wang

Colette Dooley

Dmitriy Minond

Oliver Civelli

Hiroshi Nagasaki

Madepalli K Lakshmana

The present disclosure provides compositions including a bis-cyclic guanidine compound, pharmaceutical compositions including a bis-cyclic guanidine compound, methods of treatment of a condition (e.g., bacterial infection) or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.

Bis-cyclic guanidine compound compositions, methods of use and treatment thereof

Embodiments of the present disclosure provide for compositions including a compound, pharmaceutical compositions including the compound, methods of treatment of a disease or related condition (e.g., neurological disease on condition), methods of treatment using compositions or pharmaceutical compositions, and the like.

Compounds and methods of treating neurological disorders

The present disclosure provides compositions including a bis-cyclic guanidine compound, pharmaceutical compositions including a bis-cyclic guanidine compound, methods of treatment of a condition {e.g., bacterial infection) or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.

BIS-cyclic guanidine compound compositions, methods of use and treatment thereof

This invention relates generally to N-benzylamino cyclic thioureas, pharmaceutical compositions containing them, and their use as antagonists of melanin-concentrating hormone receptor (MCH receptor).

Melanin-concentrating hormone receptor antagonists and methods of use

The invention provides isolated agents having novel chemical structures and possessing superior activity as derepressors of IAP inhibited caspase. The invention further provides a method of derepressing an IAP-inhibited caspase. The invention further provides assay methods employing labeled compounds of the invention, especially fluorescent labeled compounds.

Methods and compositions for derepression of IAP-inhibited caspase

The invention provides isolated agents having a core peptide selected from the group consisting of Core peptides 5 through 39 and 42 through 55, wherein the agent derepresses an IAP-inhibited caspase. Also provided is an isolated agent having a core structure selected from any of the structures shown in FIGS.B, andwherein said agent derepresses an IAP-inhibited caspase. The invention further provides a method of derepressing an IAP-inhibited caspase. The method consists of contacting an IAP-inhibited caspase with an effective amount of an agent to derepress an IAP-inhibited caspase, the agent having a core motif selected from the group consisting of a core peptide having a sequence set forth in any of Core peptides 4 through 39 and 42 through 55, and a core structure selected from the group consisting of TPI759, TPI882, TPI914 or TPI927. The methods of the invention also can be used for promoting apoptosis in a cell and for reducing the severity of a pathology characterized by reduced levels of apoptosis. Methods for identifying agents that derepress an IAP-inhibited caspase are also provided.

The synthesis of individual di- and tri-substituted-1,4-diazacyclic compounds having 6- to 8-atoms in the cyclic ring, their corresponding 1,6-diketo-2,5-diazacyclic compounds and similar 1,4-diazacyclic ring compounds having one ring carbonyl gorup and 6-8 atoms in the ring is disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.

Diketodiazacyclic compounds, diazacyclic compounds and combinatorial libraries thereof

The synthesis of individual di- and tri-substituted-1,4-diazacyclic compounds having 6- to 8-atoms in the cyclic ring, their corresponding 1,6-diketo-2,5-diazacyclic compounds and similar 1,4-diazacyclic ring compounds having one ring carbonyl group and 6-8 atoms in the ring is disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.

The invention provides a rapid approach for combinatorial synthesis and screening of libraries of cyclic urea and cyclic thiourea compounds. The present invention further provides the compounds made by the combinatorial synthesis.

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Adel Nefzi