C07D403/08

PROTEASE-ACTIVATED CONTRAST AGENTS FOR IN VIVO IMAGING

Compounds useful as contrast agents in image-guided surgery are provided. The compounds comprise a latent cationic lysosomotropic fragment that is detectable upon cleavage by lysosomal proteases within treated tissues, particularly within tumors and other diseased tissues. Also provided are compositions comprising the compounds and methods for using the compounds, for example in dynamically monitoring protease activity in vivo during image-guided tumor resection surgery.

Monoacylglycerol lipase modulators

3.1.0 and 4.1.0 Azabicycle compounds of Formula (I), pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, bipolar disorder), cancers and eye conditions. ##STR00001##
wherein X, Y, R.sup.1, R.sup.2a, and R.sup.2b are defined herein.

INDENE DERIVATIVES USEFUL IN TREATING PAIN AND INFLAMMATION

Compounds of formula (I) wherein, R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b and R.sup.5 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 are useful in treating inflammation and/or pain. Compositions comprising a compound of the invention are also disclosed, as are methods of using the compounds to treat inflammation and/or pain.

INDENE DERIVATIVES USEFUL IN TREATING PAIN AND INFLAMMATION

Compounds of formula (I) wherein, R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b and R.sup.5 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 are useful in treating inflammation and/or pain. Compositions comprising a compound of the invention are also disclosed, as are methods of using the compounds to treat inflammation and/or pain.

5-membered heteroaryl carboxamide compounds for treatment of HBV

The present disclosure provides, in part, 5-membered heteroaryl carboxamide compounds, and pharmaceutical compositions thereof, useful for disruption of HBV core protein assembly, and methods of treating Hepatitis B (HBV) infection.

5-membered heteroaryl carboxamide compounds for treatment of HBV

The present disclosure provides, in part, 5-membered heteroaryl carboxamide compounds, and pharmaceutical compositions thereof, useful for disruption of HBV core protein assembly, and methods of treating Hepatitis B (HBV) infection.

COMPOUND AND LABELED BIOLOGICAL SUBSTANCE USING THE SAME

There are provided a compound of Formula (1) and a labeled biological substance having the compound.

##STR00001##

Z.sup.1 and Z.sup.2 represent a specific 6-membered ring. However, at least one of Z.sup.1 or Z.sup.2 is a benzene ring having a specific substituent at an ortho position with respect to a nitrogen atom to which L.sup.1 or L.sup.2 is bonded, or a specific nitrogen-containing 6-membered ring in which a ring-constituting atom located at the ortho position is a nitrogen atom.

R.sup.1 to R.sup.4, R.sup.11 to R.sup.13, L.sup.1, L.sup.2, and R.sup.21 represents specific groups, and n, α1, α2, and m represent specific numbers.

The compound has at least one structure represented by —(CH.sub.2—CH.sub.2—O).sub.m-R.sup.21 on a heterocyclic ring and has at least one substituent capable of being bonded to a carboxy group or a biological substance at a specific position, and in a case where at least one of Z.sup.1 or Z.sup.2 is the specific nitrogen-containing 6-membered ring, the specific substituents may be bonded to each other to form a ring.

COMPOUND AND LABELED BIOLOGICAL SUBSTANCE USING THE SAME

There are provided a compound of Formula (1) and a labeled biological substance having the compound.

##STR00001##

Z.sup.1 and Z.sup.2 represent a specific 6-membered ring. However, at least one of Z.sup.1 or Z.sup.2 is a benzene ring having a specific substituent at an ortho position with respect to a nitrogen atom to which L.sup.1 or L.sup.2 is bonded, or a specific nitrogen-containing 6-membered ring in which a ring-constituting atom located at the ortho position is a nitrogen atom.

R.sup.1 to R.sup.4, R.sup.11 to R.sup.13, L.sup.1, L.sup.2, and R.sup.21 represents specific groups, and n, α1, α2, and m represent specific numbers.

The compound has at least one structure represented by —(CH.sub.2—CH.sub.2—O).sub.m-R.sup.21 on a heterocyclic ring and has at least one substituent capable of being bonded to a carboxy group or a biological substance at a specific position, and in a case where at least one of Z.sup.1 or Z.sup.2 is the specific nitrogen-containing 6-membered ring, the specific substituents may be bonded to each other to form a ring.

ISOTRYPTAMINE PSYCHOPLASTOGENS AND USES THEREOF

Disclosed herein are compounds, compositions, and methods for promoting neuronal growth and/or improving neuronal structure with the compounds and compositions disclosed herein. Also described are methods of treating diseases or disorders that are mediated by the loss of synaptic connectivity and/or plasticity, such as neurological diseases and disorders, with non-hallucinogenic psychoplastogens.

ISOTRYPTAMINE PSYCHOPLASTOGENS AND USES THEREOF

Disclosed herein are compounds, compositions, and methods for promoting neuronal growth and/or improving neuronal structure with the compounds and compositions disclosed herein. Also described are methods of treating diseases or disorders that are mediated by the loss of synaptic connectivity and/or plasticity, such as neurological diseases and disorders, with non-hallucinogenic psychoplastogens.