Patent classifications
C07D413/14
INDOLE COMPOUNDS AS ANDROGEN RECEPTOR MODULATORS
Provided herein are indole compounds that bind to BF3 of an androgen receptor (AR), which can modulate the AR for the treatment of Kennedy's disease
Bicyclic Compounds and their Uses
- Vincent Bordas ,
- Jvan BRUN ,
- Andrea DECKER ,
- Markus Furegati ,
- Geoffrey GOGNIAT ,
- Wanben GONG ,
- Jacques HAMON ,
- Jürgen Hans-Hermann HINRICHS ,
- Philipp Holzer ,
- Fatma LIMAM ,
- Henrik MÖBITZ ,
- Sandro NOCITO ,
- Simone PLATTNER ,
- Niko Schmiedeberg ,
- Joseph Schoepfer ,
- Jessica SOTO ,
- Ross Sinclair STRANG ,
- Shuping YAO ,
- Huangchao YU ,
- Frédéric ZECRI ,
- Sisi ZHANG
The present invention provides a compound, or a pharmaceutically acceptable salt thereof, of formula (I):
##STR00001##
wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.26, R.sub.27, y, R, M, W, L, V, T, Y, J, K and A are as described herein, therapeutic uses of said compounds, uses of said compounds as research chemicals, a pharmaceutical composition and combinations comprising said compounds, and methods for manufacturing the compounds of the invention.
Bicyclic Compounds and their Uses
- Vincent Bordas ,
- Jvan BRUN ,
- Andrea DECKER ,
- Markus Furegati ,
- Geoffrey GOGNIAT ,
- Wanben GONG ,
- Jacques HAMON ,
- Jürgen Hans-Hermann HINRICHS ,
- Philipp Holzer ,
- Fatma LIMAM ,
- Henrik MÖBITZ ,
- Sandro NOCITO ,
- Simone PLATTNER ,
- Niko Schmiedeberg ,
- Joseph Schoepfer ,
- Jessica SOTO ,
- Ross Sinclair STRANG ,
- Shuping YAO ,
- Huangchao YU ,
- Frédéric ZECRI ,
- Sisi ZHANG
The present invention provides a compound, or a pharmaceutically acceptable salt thereof, of formula (I):
##STR00001##
wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.26, R.sub.27, y, R, M, W, L, V, T, Y, J, K and A are as described herein, therapeutic uses of said compounds, uses of said compounds as research chemicals, a pharmaceutical composition and combinations comprising said compounds, and methods for manufacturing the compounds of the invention.
Fluoroalkyl-oxadiazoles and uses thereof
Provided herein are compounds identified as inhibitors of HDAC6 activity having the formula: ##STR00001##
or a pharmaceutically acceptable salt thereof, that can be used to treat various diseases and disorders.
Macrocyclic chelators and methods of use thereof
Macrocyclic chelators for chelation of alpha-emitting radiometal ions, such as actinium-225 are provided. Also provided are radiometal complexes containing an alpha-emitting radiometal ion bound to the macrocyclic chelator via coordinate bonding, and radioimmunoconjugates containing the radiometal complexes covalently linked to a targeting ligand, such as an antibody or antigen binding fragment thereof. The radioimmunoconjugates can be produced by click chemistry reactions. Methods of using the radiocomplexes and radioimmunoconjugates for selectively targeting neoplastic cells for radiotherapy and for treating neoplastic diseases and disorders are also described.
Triazacyclododecansulfonamide (“TCD”)-based protein secretion inhibitors
Provided herein are triazacyclododecansulfonamide (“TCD”)-based protein secretion inhibitors, such as inhibitors of Sec61, methods for their preparation, related pharmaceutical compositions, and methods for using the same. For example, provided herein are compounds of Formula (I) and pharmaceutically acceptable salts and compositions including the same. The compounds disclosed herein may be used, for example, in the treatment of diseases including inflammation and/or cancer. ##STR00001##
Triazacyclododecansulfonamide (“TCD”)-based protein secretion inhibitors
Provided herein are triazacyclododecansulfonamide (“TCD”)-based protein secretion inhibitors, such as inhibitors of Sec61, methods for their preparation, related pharmaceutical compositions, and methods for using the same. For example, provided herein are compounds of Formula (I) and pharmaceutically acceptable salts and compositions including the same. The compounds disclosed herein may be used, for example, in the treatment of diseases including inflammation and/or cancer. ##STR00001##
Heterocyclic RIP1 inhibitory compounds
Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The compounds may have a structure according to Formula I ##STR00001## The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.
Compounds for inhibition of α4 β7 integrin
The present disclosure provides a compound of Formula (I): ##STR00001##
or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), therapeutic methods for treating inflammatory disease.
Compounds for inhibition of α4 β7 integrin
The present disclosure provides a compound of Formula (I): ##STR00001##
or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), therapeutic methods for treating inflammatory disease.