Patent classifications
C07D209/52
1-aryl-3-azabicyclo[3.1.0]hexanes: preparation and use to treat neuropsychiatric disorders
The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.
COMPOUNDS USEFUL FOR TREATING GASTROINTESTINAL TRACT DISORDERS
The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.
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.
BENZENECARBOTHIOCCYCLOPENTA[C] PYRROLE-1,3-DIONE COMPOUNDS AND PROCESS FOR SYNTHESIS THEREOF
The present invention relates to a novel analogues of benzenecarbothioccyclopenta[c]pyrrole-1,3-dione of formula (I) useful for treating various viral infections and process for synthesis thereof.
##STR00001##
The present invention provides a novel process for synthesis of nitrosporeusinesA(1) and B(2). More particularly, the present invention provides a synthetic route for synthesis of nitrosporeusinesA(1) and B(2). Said process is simple, industrially scalable, cost effective and eco-friendly.
BENZENECARBOTHIOCCYCLOPENTA[C] PYRROLE-1,3-DIONE COMPOUNDS AND PROCESS FOR SYNTHESIS THEREOF
The present invention relates to a novel analogues of benzenecarbothioccyclopenta[c]pyrrole-1,3-dione of formula (I) useful for treating various viral infections and process for synthesis thereof.
##STR00001##
The present invention provides a novel process for synthesis of nitrosporeusinesA(1) and B(2). More particularly, the present invention provides a synthetic route for synthesis of nitrosporeusinesA(1) and B(2). Said process is simple, industrially scalable, cost effective and eco-friendly.
INHIBITORS OF HISTONE DEACETYLASE
The present invention relates to compounds of formula (I):
##STR00001##
or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R.sup.1a, R.sup.2b, R.sup.2c, R.sup.5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
INHIBITORS OF HISTONE DEACETYLASE
The present invention relates to compounds of formula (I):
##STR00001##
or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R.sup.1a, R.sup.2b, R.sup.2c, R.sup.5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
Polymorphs of azabicyclohexane
The invention provides polymorphic crystalline forms of acid addition salts of (+)-1-(3, 4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane designated as polymorph form A, polymorph form B and polymorph form C, where polymorph form A is more thermodynamically stable than the other forms, methods for preparing and using such polymorph forms and pharmaceutical compositions containing such polymorph forms.
Polymorphs of azabicyclohexane
The invention provides polymorphic crystalline forms of acid addition salts of (+)-1-(3, 4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane designated as polymorph form A, polymorph form B and polymorph form C, where polymorph form A is more thermodynamically stable than the other forms, methods for preparing and using such polymorph forms and pharmaceutical compositions containing such polymorph forms.
Coferons and methods of making and using them
The present invention is directed to a monomer useful in preparing therapeutic compounds. The monomer includes one or more pharmacophores which potentially binds to a target molecule with a dissociation constant of less than 300 μM and a linker element connected to the pharmacophore. The linker element has a molecular weight less than 500 daltons, is connected, directly or indirectly through a connector, to the pharmacophore.