Patent classifications
C07D211/06
Selective FKBP51 ligands for treatment of psychiatric disorders
The present invention relates to compounds of the general formula (I) having a selective FKBP51 ligand scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said selective FKBP51 ligand compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions. ##STR00001##
Prodrugs of fumarates and their use in treating various diseases
The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. ##STR00001##
Prodrugs of fumarates and their use in treating various diseases
The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. ##STR00001##
PIPERIDINYLPYRAZOLOPYRIMIDINONES AND THEIR USE
- Manuel Ellermann ,
- Gaelle Valot ,
- Yolanda Cancho Grande ,
- Jorma HAßFELD ,
- Tom Kinzel ,
- Johannes KÖBBERLING ,
- Kristin BEYER ,
- Susanne RÖHRIG ,
- Michael Sperzel ,
- Jan STAMPFUß ,
- Imke Meyer ,
- Maria KÖLLNBERGER ,
- Nils Burkhardt ,
- Karl-Heinz Schlemmer ,
- Christian Stegmann ,
- Joachim Schuhmacher ,
- Matthias Werner ,
- Jörg HEIERMANN ,
- Willem Jan Hengeveld
The present application relates to novel substituted piperidinylpyrazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired hemostatic disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of heavy menstrual bleeding, postpartum hemorrhage, hemorrhagic shock, hemorrhagic cystitis, gastrointestinal hemorrhage, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.
PIPERIDINYLPYRAZOLOPYRIMIDINONES AND THEIR USE
- Manuel Ellermann ,
- Gaelle Valot ,
- Yolanda Cancho Grande ,
- Jorma HAßFELD ,
- Tom Kinzel ,
- Johannes KÖBBERLING ,
- Kristin BEYER ,
- Susanne RÖHRIG ,
- Michael Sperzel ,
- Jan STAMPFUß ,
- Imke Meyer ,
- Maria KÖLLNBERGER ,
- Nils Burkhardt ,
- Karl-Heinz Schlemmer ,
- Christian Stegmann ,
- Joachim Schuhmacher ,
- Matthias Werner ,
- Jörg HEIERMANN ,
- Willem Jan Hengeveld
The present application relates to novel substituted piperidinylpyrazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired hemostatic disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of heavy menstrual bleeding, postpartum hemorrhage, hemorrhagic shock, hemorrhagic cystitis, gastrointestinal hemorrhage, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.
ArylSulfonamide-based matrix metalloprotease inhibitors
The present invention provides a compound of formula (I): ##STR00001##
said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.
COMPOSITIONS FOR TREATING NEURODEGENERATIVE DISEASES
The present disclosure relates to novel compounds, pharmaceutical compositions containing the compounds and methods of using the compounds and pharmaceutical compositions for treating neurodegerative diseases, including Alzheimer's disease and cognitive decline. Methods for inhibiting synapse number decline or membrane trafficking abnormalities associated with exposure of a neuronal cell to Abeta species are also disclosed.
METHOD FOR THE PREPARATION OF 1-(2-HALOGEN-ETHYL)-4 PIPERIDINE-CARBOXYLIC ACID ETHYL ESTERS
The present invention refers to a process for the preparation of 1-(2-halogen-ethyl)-4-piperidinecarboxylic acid ethyl esters, in particular of 1-(2-chloroethyl)-4 piperidinecarboxylic acid ethyl ester, a versatile synthesis intermediate, particularly useful as an intermediate compound in the synthesis of umeclidinium.
METHOD FOR THE PREPARATION OF 1-(2-HALOGEN-ETHYL)-4 PIPERIDINE-CARBOXYLIC ACID ETHYL ESTERS
The present invention refers to a process for the preparation of 1-(2-halogen-ethyl)-4-piperidinecarboxylic acid ethyl esters, in particular of 1-(2-chloroethyl)-4 piperidinecarboxylic acid ethyl ester, a versatile synthesis intermediate, particularly useful as an intermediate compound in the synthesis of umeclidinium.
PYRIMIDINE COMPOUNDS AS JAK KINASE INHIBITORS
The invention provides compounds of formula (I):
##STR00001##
wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of JAK kinases. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat gastrointestinal and other inflammatory diseases, and processes and intermediates useful for preparing such compounds.