Patent classifications
C07D237/34
Inhibiting G protein coupled receptor 6 kinase polypeptides
This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.
PHTHALAZINONE DERIVATES AS NLRP3 INFLAMMASOME INHIBITORS
Provided are novel compounds for use as inhibitors of NLRP3 inflammasomeproduction, wherein such compounds are as defined by compounds of formula (I) wherein, R.sup.1, R.sup.2 and R.sup.3a and R.sup.3b are as defined in the description, and where the compounds may be useful as medicaments, for instance for use in the treatment of a disease or disorder that is associated with NLRP3 inflammasome activity.
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PHTHALAZINONE DERIVATES AS NLRP3 INFLAMMASOME INHIBITORS
Provided are novel compounds for use as inhibitors of NLRP3 inflammasomeproduction, wherein such compounds are as defined by compounds of formula (I) wherein, R.sup.1, R.sup.2 and R.sup.3a and R.sup.3b are as defined in the description, and where the compounds may be useful as medicaments, for instance for use in the treatment of a disease or disorder that is associated with NLRP3 inflammasome activity.
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INHIBITORS OF NLRP3
- XIAOYAN ZHANG ,
- TIANYI ZHENG ,
- SCOTT j BARRAZA ,
- LAUREN BEJCEK ,
- BRADLEY B GILBERT ,
- HUA GONG ,
- HANDOKO HANDOKO ,
- SEYEDMORTEZA HOSSEYNI ,
- EDUARDO HUARTE ,
- WOOHYUNG JEON ,
- JING LI ,
- YAO LIU ,
- KYLE NIEDERER ,
- MEENU PILLAI ,
- ERICA N PARKER ,
- ETTORE RASTELLI ,
- NADIYA SYDORENKO ,
- ANTHONY TURPOFF ,
- MATTHEW G WOLL ,
- NANJING ZHANG ,
- YAN ZHANG ,
- RAUFUL ALAM
The present invention relates to novel compounds of Formulae I-XI: wherein each A, A, Q, Q, W, Rw, Y, and Z, and -- are as defined herein, which inhibit NOD-like receptor protein 3 (NLRP3) inflammasome activity. The invention further relates to the processes for their preparation, pharmaceutical compositions and medicaments containing them, and their use in the treatment of diseases and disorders mediated by NLRP3.
##STR00001##
INHIBITORS OF NLRP3
- XIAOYAN ZHANG ,
- TIANYI ZHENG ,
- SCOTT j BARRAZA ,
- LAUREN BEJCEK ,
- BRADLEY B GILBERT ,
- HUA GONG ,
- HANDOKO HANDOKO ,
- SEYEDMORTEZA HOSSEYNI ,
- EDUARDO HUARTE ,
- WOOHYUNG JEON ,
- JING LI ,
- YAO LIU ,
- KYLE NIEDERER ,
- MEENU PILLAI ,
- ERICA N PARKER ,
- ETTORE RASTELLI ,
- NADIYA SYDORENKO ,
- ANTHONY TURPOFF ,
- MATTHEW G WOLL ,
- NANJING ZHANG ,
- YAN ZHANG ,
- RAUFUL ALAM
The present invention relates to novel compounds of Formulae I-XI: wherein each A, A, Q, Q, W, Rw, Y, and Z, and -- are as defined herein, which inhibit NOD-like receptor protein 3 (NLRP3) inflammasome activity. The invention further relates to the processes for their preparation, pharmaceutical compositions and medicaments containing them, and their use in the treatment of diseases and disorders mediated by NLRP3.
##STR00001##
Therapeutic compounds and uses thereof
The present invention relates to methods for treating PCAF and GCN5 mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR00001##
wherein ring A, R.sup.1, R.sup.3, R.sup.4, R.sup.5, and each R.sup.e have any of the values defined in the specification. Also included are novel compounds of Formula (I) and salts thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.
Therapeutic compounds and uses thereof
The present invention relates to methods for treating PCAF and GCN5 mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR00001##
wherein ring A, R.sup.1, R.sup.3, R.sup.4, R.sup.5, and each R.sup.e have any of the values defined in the specification. Also included are novel compounds of Formula (I) and salts thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.
KRAS G12C INHIBITORS AND METHODS OF USING THE SAME
Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
KRAS G12C INHIBITORS AND METHODS OF USING THE SAME
Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
NLRP3 INFLAMMASOME INHIBITOR AND APPLICATION THEREOF
The present invention belongs to the technical field of medicines, relates to an NLRP3 inflammasome inhibitor and use thereof, and particularly relates to a compound of general formula (I), or a pharmaceutically acceptable salt, a stereoisomer or a tautomer thereof, wherein each group is defined in the specification. Researches show that the compound of general formula (I), or pharmaceutically acceptable salt, the stereoisomer or the tautomer thereof has relatively high biological activity on NLRP3 inflammasomes and has an important clinical development value for the treatment of NLRP3-associated diseases.
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