Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.

Disclosed herein are compounds that can inhibit 15-hydroxyprostaglandin dehydrogenase. Such compounds may be administered to subjects that may benefit from modulation of prostaglandin levels.

The present invention relates to novel depot formulations (prodrugs) comprising an immobility promoting unit linked via an ester to an active pharmaceutical ingredient, i.a. common NSAIDs. The novel depot formulations are suitable for intra-articular injections and are soluble at slightly acidic pH to facilitate ease of injection, and sparingly soluble at physiological pH thereby precipitating at the site of administration. The precipitate will slowly dissolve and the active drug is released from dissolved depot formulation following esterase mediated cleavage of the ester link between the immobility promoting unit and the active pharmaceutical agent.

The present invention relates to novel depot formulations (prodrugs) comprising an immobility promoting unit linked via an ester to an active pharmaceutical ingredient, i.a. common NSAIDs. The novel depot formulations are suitable for intra-articular injections and are soluble at slightly acidic pH to facilitate ease of injection, and sparingly soluble at physiological pH thereby precipitating at the site of administration. The precipitate will slowly dissolve and the active drug is released from dissolved depot formulation following esterase mediated cleavage of the ester link between the immobility promoting unit and the active pharmaceutical agent.

A compound represented by General Formula (I), a tautomer, a stereoisomer, or a pharmaceutically acceptable salt of the compound, or a solvate thereof is used as a voltage-dependent T-type calcium channel inhibitor, ##STR00001## in the formula, A represents a benzene ring which may have a substituent or the like; B represents a hetero-fused ring consisting of a 5- or 6-membered heteroaryl ring having one to three same or different heteroatoms selected from an oxygen atom, a sulfur atom, and a nitrogen atom, and a carbon atom, as a ring-constituting atom, and a benzene ring, or the like, and the hetero-fused ring may have a substituent, and is bonded to a cyclopropyl group via a carbon atom constituting these rings; R.sup.1 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like; R.sup.2 and R.sup.3 may be the same as or different from each other, and each represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like, or R.sup.2 and R.sup.3 together form CH.sub.2CH.sub.2 or the like; R.sup.4 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like; m represents 0, 1, or 2; and n represents 0 or 1.

A compound represented by General Formula (I), a tautomer, a stereoisomer, or a pharmaceutically acceptable salt of the compound, or a solvate thereof is used as a voltage-dependent T-type calcium channel inhibitor, ##STR00001## in the formula, A represents a benzene ring which may have a substituent or the like; B represents a hetero-fused ring consisting of a 5- or 6-membered heteroaryl ring having one to three same or different heteroatoms selected from an oxygen atom, a sulfur atom, and a nitrogen atom, and a carbon atom, as a ring-constituting atom, and a benzene ring, or the like, and the hetero-fused ring may have a substituent, and is bonded to a cyclopropyl group via a carbon atom constituting these rings; R.sup.1 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like; R.sup.2 and R.sup.3 may be the same as or different from each other, and each represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like, or R.sup.2 and R.sup.3 together form CH.sub.2CH.sub.2 or the like; R.sup.4 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like; m represents 0, 1, or 2; and n represents 0 or 1.

The present invention relates to a crystalline, two dimensional polymer of Formula I and a process for the preparation thereof.

##STR00001##

The present invention relates to a crystalline, two dimensional polymer of Formula I and a process for the preparation thereof.

##STR00001##

Disclosed herein are compounds that can inhibit 15-hydroxyprostaglandin dehydrogenase. Such compounds may be administered to subjects that may benefit from modulation of prostaglandin levels.

The present invention provides compounds of general Formula I and I′: ##STR00001## ##STR00002##
compositions thereof, and methods of using same to treat Rheb-mediated disorders.