Patent classifications
C07C215/38
NOVEL COMPOUND USEFUL AS TOLL-LIKE RECEPTOR 7 ACTIVATION INHIBITOR
CB-7 exhibits a weak TLR7 inhibiting effect in normal mice. The present invention provides a novel compound with a stronger TLR7 inhibiting effect than CB-7, a pharmaceutically acceptable salt of said compound, or a prodrug of said compound or salt. The present invention also provides a drug for the prevention or treatment of diseases associated with the activation of TLR7, said drug including the aforementioned TLR7 activation inhibitor.
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.
PROCESS FOR THE SYNTHESIS OF (+) AND (-)-1-(3,4-DICHLOROPHENYL)-3-AZABICYCLO[3.1.0]HEXANE
The present invention is concerned with novel processes for the preparation of (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and (−)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof. These compounds have pharmaceutical utility and are known to be useful for treating e.g., depression, anxiety disorders, eating disorders and urinary incontinence.
Quinolinone or quinazolinone comprising antibiofilm compositions, compounds and methods and uses relating thereto
An antibiofilm composition comprising a compound of formula (A1), (A2) or (A3): ##STR00001##
wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrogen, alkyl, alkenyl, aryl, halo, alkoxy, hydroxyl, amino, nitro, sulfoxy, thiol, carboxy, alkyl carboxy and amido; and X may be O or S, wherein the composition does not comprise a compound of formula (B1) or (B2): ##STR00002##
Quinolinone or quinazolinone comprising antibiofilm compositions, compounds and methods and uses relating thereto
An antibiofilm composition comprising a compound of formula (A1), (A2) or (A3): ##STR00001##
wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrogen, alkyl, alkenyl, aryl, halo, alkoxy, hydroxyl, amino, nitro, sulfoxy, thiol, carboxy, alkyl carboxy and amido; and X may be O or S, wherein the composition does not comprise a compound of formula (B1) or (B2): ##STR00002##
Quinolinone or quinazolinone comprising antibiofilm compositions, compounds and methods and uses relating thereto
An antibiofilm composition comprising a compound of formula (A1), (A2) or (A3): ##STR00001##
wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrogen, alkyl, alkenyl, aryl, halo, alkoxy, hydroxyl, amino, nitro, sulfoxy, thiol, carboxy, alkyl carboxy and amido; and X may be O or S, wherein the composition does not comprise a compound of formula (B1) or (B2): ##STR00002##
Quinolinone or quinazolinone comprising antibiofilm compositions, compounds and methods and uses relating thereto
An antibiofilm composition comprising a compound of formula (A1), (A2) or (A3): ##STR00001##
wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrogen, alkyl, alkenyl, aryl, halo, alkoxy, hydroxyl, amino, nitro, sulfoxy, thiol, carboxy, alkyl carboxy and amido; and X may be O or S, wherein the composition does not comprise a compound of formula (B1) or (B2): ##STR00002##
QUINOLINONE OR QUINAZOLINONE COMPRISING ANTIBIOFILM COMPOSITIONS, COMPOUNDS AND METHODS AND USES RELATING THERETO
An antibiofilm composition comprising a compound of formula (A1), (A2) or (A3):
##STR00001##
wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrogen, alkyl, alkenyl, aryl, halo, alkoxy, hydroxyl, amino, nitro, sulfoxy, thiol, carboxy, alkyl carboxy and amido; and X may be O or S, wherein the composition does not comprise a compound of formula (B1) or (B2):
##STR00002##
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.