Patent classifications
A61K31/423
OX2R Compounds
Methods and compositions for agonizing a type-2 orexin receptor (OX2R) in a cell determined to be in need thereof, including the general method of (a) administering to a subject a cyclic guanidinyl OX2R agonist and (b) detecting a resultant enhanced wakefulness or increased resistance to diet-induced accumulation of body fat, or abbreviated recovery from general anesthesia or jet lag.
OX2R Compounds
Methods and compositions for agonizing a type-2 orexin receptor (OX2R) in a cell determined to be in need thereof, including the general method of (a) administering to a subject a cyclic guanidinyl OX2R agonist and (b) detecting a resultant enhanced wakefulness or increased resistance to diet-induced accumulation of body fat, or abbreviated recovery from general anesthesia or jet lag.
USE OF FXR AGONISTS FOR TREATING AN INFECTION BY HEPATITIS D VIRUS
The present invention relates to the use of a farnesoid X receptor (FXR) agonist for the treatment of hepatitis D infection.
USE OF FXR AGONISTS FOR TREATING AN INFECTION BY HEPATITIS D VIRUS
The present invention relates to the use of a farnesoid X receptor (FXR) agonist for the treatment of hepatitis D infection.
INHIBITORS OF CBL-B AND METHODS OF USE THEREOF
- Paul A. BARSANTI ,
- Neil F. BENCE ,
- Jennifa GOSLING ,
- Anjanabha SAHA ,
- Asad M TAHERBHOY ,
- Christoph W. ZAPF ,
- Kathleen BOYLE ,
- Mario CARDOZO ,
- Jeffrey MIHALIC ,
- Morgan LAWRENZ ,
- Mark GALLOP ,
- Jilliane BRUFFEY ,
- Thomas CUMMINS ,
- Daniel ROBBINS ,
- Hiroko TANAKA ,
- Chenbo WANG ,
- Frederick Cohen ,
- Wylie PALMER ,
- Arthur T. SANDS ,
- Hunter SHUNATONA
Compounds, compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo.
INHIBITORS OF CBL-B AND METHODS OF USE THEREOF
- Paul A. BARSANTI ,
- Neil F. BENCE ,
- Jennifa GOSLING ,
- Anjanabha SAHA ,
- Asad M TAHERBHOY ,
- Christoph W. ZAPF ,
- Kathleen BOYLE ,
- Mario CARDOZO ,
- Jeffrey MIHALIC ,
- Morgan LAWRENZ ,
- Mark GALLOP ,
- Jilliane BRUFFEY ,
- Thomas CUMMINS ,
- Daniel ROBBINS ,
- Hiroko TANAKA ,
- Chenbo WANG ,
- Frederick Cohen ,
- Wylie PALMER ,
- Arthur T. SANDS ,
- Hunter SHUNATONA
Compounds, compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo.
NEW COMPOUNDS AND THEIR USE AS THERAPEUTICALLY ACTIVE SUBSTANCES IN THE TREATMENT AND/OR REDUCING SIGNS OR SYMPTOMS OF DISEASES INVOLVING THE RETINAL PIGMENT EPITHELIUM
A method of treating and/or preventing disease wherein retinal pigment epithelium, including administering compound of formula (I)
##STR00001##
or pharmaceutically acceptable salt, racemic mixture, corresponding enantiomer or, if applicable, corresponding diastereomer, wherein: X is either NH or O, R.sub.11, R.sub.12 and R.sub.13 are independently selected from consisting hydrogen group, fluoro, chloro, trifluoromethyl, methyl and difluoromethoxy, A is selected from consisting residue group of formula (II)-(VII) or (VIII)
##STR00002##
“*” denotes point of attachment to molecule remainder, and R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.2.sup.I, R.sub.3.sup.I, R.sub.4.sup.I, R.sub.5.sup.I, R.sub.2.sup.II, R.sub.3.sup.II, R.sub.4.sup.II, R.sub.5.sup.II, R.sub.2.sup.III, R.sub.3.sup.III, R.sub.4.sup.III, R.sub.5.sup.III, R.sub.2.sup.IV, R.sub.3.sup.IV, R.sub.4.sup.IV, R.sub.5.sup.IV, R.sub.2.sup.V, R.sub.3.sup.V, R.sub.4.sup.V, R.sub.5.sup.V, R.sub.2.sup.VI, R.sub.3.sup.VI, R.sub.4.sup.VI and R.sub.5.sup.VI are independently selected from hydrogen consisting group, linear or branched alkyl having 1-3 carbon atoms, fluoro, chloro, bromo, methoxy, ethoxy, propoxy, trifluoromethyl, 2,2,2-trifluoroethyl and difluoromethoxy and R.sub.6 is selected from hydrogen consisting group, linear or branched alkyl having 1-3 carbon atoms, trifluoromethyl, and 2,2,2-trifluoroethyl.
NEW COMPOUNDS AND THEIR USE AS THERAPEUTICALLY ACTIVE SUBSTANCES IN THE TREATMENT AND/OR REDUCING SIGNS OR SYMPTOMS OF DISEASES INVOLVING THE RETINAL PIGMENT EPITHELIUM
A method of treating and/or preventing disease wherein retinal pigment epithelium, including administering compound of formula (I)
##STR00001##
or pharmaceutically acceptable salt, racemic mixture, corresponding enantiomer or, if applicable, corresponding diastereomer, wherein: X is either NH or O, R.sub.11, R.sub.12 and R.sub.13 are independently selected from consisting hydrogen group, fluoro, chloro, trifluoromethyl, methyl and difluoromethoxy, A is selected from consisting residue group of formula (II)-(VII) or (VIII)
##STR00002##
“*” denotes point of attachment to molecule remainder, and R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.2.sup.I, R.sub.3.sup.I, R.sub.4.sup.I, R.sub.5.sup.I, R.sub.2.sup.II, R.sub.3.sup.II, R.sub.4.sup.II, R.sub.5.sup.II, R.sub.2.sup.III, R.sub.3.sup.III, R.sub.4.sup.III, R.sub.5.sup.III, R.sub.2.sup.IV, R.sub.3.sup.IV, R.sub.4.sup.IV, R.sub.5.sup.IV, R.sub.2.sup.V, R.sub.3.sup.V, R.sub.4.sup.V, R.sub.5.sup.V, R.sub.2.sup.VI, R.sub.3.sup.VI, R.sub.4.sup.VI and R.sub.5.sup.VI are independently selected from hydrogen consisting group, linear or branched alkyl having 1-3 carbon atoms, fluoro, chloro, bromo, methoxy, ethoxy, propoxy, trifluoromethyl, 2,2,2-trifluoroethyl and difluoromethoxy and R.sub.6 is selected from hydrogen consisting group, linear or branched alkyl having 1-3 carbon atoms, trifluoromethyl, and 2,2,2-trifluoroethyl.
MONOACYLGLYCEROL LIPASE MODULATORS FOR USE IN AUTISM SPECTRUM DISORDERS
The disclosure relates to certain uses and methods of use of 3.1.0 and 4.1.0 azabicycle compounds of Formula (I), wherein X, Y, R.sup.1, R.sup.2a, and R.sup.2b are defined herein, and pharmaceutical compositions containing them, in the treatment of autism spectrum disorder, including Asperger's syndrome.
##STR00001##
MONOACYLGLYCEROL LIPASE MODULATORS FOR USE IN AUTISM SPECTRUM DISORDERS
The disclosure relates to certain uses and methods of use of 3.1.0 and 4.1.0 azabicycle compounds of Formula (I), wherein X, Y, R.sup.1, R.sup.2a, and R.sup.2b are defined herein, and pharmaceutical compositions containing them, in the treatment of autism spectrum disorder, including Asperger's syndrome.
##STR00001##