C07D221/16

TRICYCLIC COMPOUNDS, PREPARATION METHOD AND MEDICAL USE THEREOF

The present invention provides a tricyclic compound, its preparation method and medical use. The tricyclic compound is a compound having the structure of the following formula (I), and its pharmaceutically acceptable salt, prodrug, tautomer, stereoisomers or mixtures of stereoisomers. The compound of the present invention has significant activity of antagonizing histamine H1 receptor, and has lower anti-M-choline side effects and lower hERG toxicity,

##STR00001##

Wherein the group is defined as described in the specification.

TRICYCLIC COMPOUNDS, PREPARATION METHOD AND MEDICAL USE THEREOF

The present invention provides a tricyclic compound, its preparation method and medical use. The tricyclic compound is a compound having the structure of the following formula (I), and its pharmaceutically acceptable salt, prodrug, tautomer, stereoisomers or mixtures of stereoisomers. The compound of the present invention has significant activity of antagonizing histamine H1 receptor, and has lower anti-M-choline side effects and lower hERG toxicity,

##STR00001##

Wherein the group is defined as described in the specification.

Cyclooctynes for click chemistry

Provided herein are dibenzocyclooctyne compounds useful as reagents in 1,3-dipolar cycloaddition reactions, and methods for their preparation.

Cyclooctynes for click chemistry

Provided herein are dibenzocyclooctyne compounds useful as reagents in 1,3-dipolar cycloaddition reactions, and methods for their preparation.

ArylSulfonamide-based matrix metalloprotease inhibitors

The present invention provides a compound of formula (I): ##STR00001##
said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.

SHIP1 MODULATORS AND METHODS RELATED THERETO

Compounds of formula (II):

##STR00001##

wherein

##STR00002##

R.sup.1, R.sup.2, R.sup.5 and R.sup.13 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds have activity as SHIP1 modulators, and thus may be useful in treating a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of the invention are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.

SHIP1 MODULATORS AND METHODS RELATED THERETO

Compounds of formula (II):

##STR00001##

wherein

##STR00002##

R.sup.1, R.sup.2, R.sup.5 and R.sup.13 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds have activity as SHIP1 modulators, and thus may be useful in treating a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of the invention are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.

NLRP MODULATORS

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein, useful to treat connected to the modulation of NRLP3.

##STR00001##

NLRP MODULATORS

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein, useful to treat connected to the modulation of NRLP3.

##STR00001##

Ligands for Alpha-7 Nicotinic Acetylcholine Receptors and Methods of Treating Neurological and Inflammatory Conditions

Compounds are provided which bind to an allosteric site on the mammalian alpha-7 nicotinic acetylcholine receptor (alpha-7 nAChR) and act as positive allosteric modulators with or without allosteric agonist activity. The compounds are useful in diagnosing, preventing, or treating a variety of disorders involving cognition, learning, memory, neurodegeneration, drug addiction, inflammation, chronic pain, and neuropathic pain. The compounds also can be used to enhance memory and learning in normal individuals.