This disclosure relates to new phthalimide and isoindolinone derivatives and other PFKFB3 inhibitors for use in the treatment of diseases. The invention further relates to pharmaceutical compositions containing such PFKFB3 inhibitors, methods of preparation thereof, methods for their use as therapeutic agents, and methods of preparation of a medicament for use in therapy, as well as kits and other inventions comprising such PFKFB3 inhibitors. These PFKFB3 inhibitors are useful for the treatment and prophylaxis of cancer, neurodegenerative diseases, autoimmune diseases, inflammatory disorders, multiple sclerosis, metabolic diseases, inhibition of angiogenesis and other diseases and conditions, where the modulation of PFKFB3 and/or PFKFB4 has beneficial effect as well as neuroprotection.

The present invention relates to compounds of Formula (Ia) or pharmaceutically acceptable salts, hydrates, solvates, clathrates, polymorphs, stereoisomers thereof. It further discloses a pharmaceutical composition comprising compounds of Formula (Ia) and the use of compounds of Formula (Ib), in particular for the use in the treatment of diseases or disorders wherein disrupting Rad51-BRCA2 interaction is beneficial.

##STR00001##

The present invention relates to compounds of Formula (Ia) or pharmaceutically acceptable salts, hydrates, solvates, clathrates, polymorphs, stereoisomers thereof. It further discloses a pharmaceutical composition comprising compounds of Formula (Ia) and the use of compounds of Formula (Ib), in particular for the use in the treatment of diseases or disorders wherein disrupting Rad51-BRCA2 interaction is beneficial.

##STR00001##

Provided herein are compounds of the following Formula (I): or a pharmaceutically acceptable salt thereof. Methods for treating a diseases, disorders, or symptom by antagonizing muscarinic receptors, including specifically antagonizing muscarinic receptor 4 (M4), are also provided.

##STR00001##

Provided herein are compounds of the following Formula (I): or a pharmaceutically acceptable salt thereof. Methods for treating a diseases, disorders, or symptom by antagonizing muscarinic receptors, including specifically antagonizing muscarinic receptor 4 (M4), are also provided.

##STR00001##

The compound represented by formula (I), and racemates, stereoisomers, tautomers, isotopic markers, nitrogen oxides, solvates, polymorphs, metabolites, esters, pharmaceutically acceptable salts, or prodrugs thereof have ROCK inhibitory activity. The compound represented by formula (1) has good safety, good metabolic stability, and a low risk of potential hepatotoxicity. Further, the compound represented by formula (I) has a simple preparation method and is easy to purify, and therefore has good application prospects.

##STR00001##

The compound represented by formula (I), and racemates, stereoisomers, tautomers, isotopic markers, nitrogen oxides, solvates, polymorphs, metabolites, esters, pharmaceutically acceptable salts, or prodrugs thereof have ROCK inhibitory activity. The compound represented by formula (1) has good safety, good metabolic stability, and a low risk of potential hepatotoxicity. Further, the compound represented by formula (I) has a simple preparation method and is easy to purify, and therefore has good application prospects.

##STR00001##

The present invention provides a phenol compound represented by the following Formula (I) or a salt thereof:

##STR00001##

wherein R.sub.1, R.sub.2, R.sub.5, L.sub.1, L.sub.2, L.sub.3, A, X, and m are as described in the specification.

The present invention provides a phenol compound represented by the following Formula (I) or a salt thereof:

##STR00001##

wherein R.sub.1, R.sub.2, R.sub.5, L.sub.1, L.sub.2, L.sub.3, A, X, and m are as described in the specification.

The present invention relates to a compound represented by Formula 1 wherein A, B, L, X, and R.sub.1 to R.sub.6 are as described herein, or a pharmaceutically acceptable salt thereof, which serves as a GLP-1 receptor agonist and may be useful in the prevention or treatment of a disease associated with GLP-1 activity.