Patent classifications
A61K31/4985
Substituted [1,2,4]triazolo[4,3-a]pyrazines as modulators of mGlu5 receptors
Disclosed are triazole, imidazole and pyrrole condensed piperazine derivatives and their use as allosteric modulators of mGlus receptor activity, pharmaceutical compositions comprising such compounds, and methods of treatment therewith. Compounds of the invention can be used for the treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline, dementia or cognitive impairment, or other pathologies that can be related either directly or indirectly to glutamate dysfunction, i.e., disorders treatable by positive allosteric modulation (PAM) or by negative allosteric modulation (NAM) of mGluR.sub.5. ##STR00001##
Substituted [1,2,4]triazolo[4,3-a]pyrazines as modulators of mGlu5 receptors
Disclosed are triazole, imidazole and pyrrole condensed piperazine derivatives and their use as allosteric modulators of mGlus receptor activity, pharmaceutical compositions comprising such compounds, and methods of treatment therewith. Compounds of the invention can be used for the treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline, dementia or cognitive impairment, or other pathologies that can be related either directly or indirectly to glutamate dysfunction, i.e., disorders treatable by positive allosteric modulation (PAM) or by negative allosteric modulation (NAM) of mGluR.sub.5. ##STR00001##
Bicyclic and tricyclic compounds
Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
Bicyclic and tricyclic compounds
Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-a]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF
The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.
PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-a]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF
The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.
POLYCYCLIC PYRIDOPYRAZINE DERIVATIVE
The present invention provides a compound represented by the following Formula (I):
##STR00001##
wherein ring A is a C5-C7 non-aromatic carbocycle or a 5- to 7-membered non-aromatic heterocycle; ring B is a benzene ring or the like; Q is —NHC(O)— or a 5-membered aromatic heterocycle; R.sup.1 is each independently halogen or the like; R.sup.2a and R.sup.2b are each independently hydrogen, alkyl, or haloalkyl; R.sup.3 is alkyl or the like; R.sup.4 and R.sup.5 are each independently hydrogen or the like; R.sup.6 is each independently halogen, alkyl, haloalkyl, alkyloxy, haloalkyloxy, or alkyloxyalkyl; n is an integer of 1 to 3; and m is an integer of 0 to 3.
MOLECULAR TARGETS FOR ADDICTION
Provided herein are methods and compositions for the treatment or prevention of certain disorders and conditions, for example, addiction using an agent to modulate 5-hydroxytryptamine 1D receptor (HTR1D) activity and/or expression. Also provided are methods for screening a candidate to determine if the candidate is suitable for the therapies disclosed herein.
MOLECULAR TARGETS FOR ADDICTION
Provided herein are methods and compositions for the treatment or prevention of certain disorders and conditions, for example, addiction using an agent to modulate 5-hydroxytryptamine 1D receptor (HTR1D) activity and/or expression. Also provided are methods for screening a candidate to determine if the candidate is suitable for the therapies disclosed herein.
Novel Ferroportin Inhibitors
The invention relates to novel compounds of the general formula (I),
##STR00001##
with Het-2 being an optionally substituted bicyclic heteroaryl of the formula
##STR00002##
pharmaceutical compositions comprising them and the use thereof as medicaments, in particular for the use as ferroportin inhibitors, more particularly for the use in the prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, such as particularly iron overload states such as in particular thalassemia and hemochromatosis.