132945-75-6Relevant academic research and scientific papers
ISOQUINOLINE DERIVATIVES AS SIK2 INHIBITORS
-
Paragraph 00256-00257, (2021/05/07)
Provided are compounds of the Formula I, and salts and solvates thereof: (I) wherein R1, R2, R3, R6, X1, X2 and Z are defined in the specification. The compounds are inhibitors of salt-inducible kinase (SIK), particular SIK2, and are useful in therapy, particularly in the treatment of a proliferative disorder, a benign neoplasm, pathological angiogenesis, an inflammatory disease or condition, a musculoskeletal disease or condition, an autoimmune disease, a haematological disease or condition, a neurological disease or condition, a psychiatric disorder, or a metabolic disorder.
ISOQUINOLINE DERIVATIVES AS SIK2 INHIBITORS
-
Paragraph 00137; 00257, (2021/05/07)
Provided are compounds of the Formula I, and salts and solvates thereof: (I) wherein R1, R2, R3, X1, X2, X3 and Z are defined in the specification. The compounds are inhibitors of salt-inducible kinase (SIK), particular SIK2, and are useful in therapy, particularly in the treatment of a proliferative disorder, a benign neoplasm, pathological angiogenesis, an inflammatory disease or condition, a musculoskeletal disease or condition, an autoimmune disease, a haematological disease or condition, a neurological disease or condition, a psychiatric disorder, or a metabolic disorder.
6-HETEROARYLOXY BENZIMIDAZOLES AND AZABENZIMIDAZOLES AS JAK2 INHIBITORS
-
Paragraph 0272; 0276; 0938, (2021/11/13)
The present disclosure provides 6-heteroaryloxy benzimidazole and azabenzimidazole compounds and compositions thereof useful for inhibiting JAK2.
Novel pyrrolidine or piperidine derivatives having activity for T-type calcium channel
-
Paragraph 0379-0382; 0394-0397, (2020/04/23)
A pyrrolidine or piperidine compound having activity for T - type calcium channel, wherein the pyrrolidine or piperidine compound of Formula 1 according to the present invention has an excellent antagonistic activity to, T-type calcium channel, and can be used as a preventive or therapeutic agent, for pain diseases, or cancer related to cancer, or cancer such as, epilepsy and,hepatic pain, angina. (by machine translation)
PYRROLO(PYRAZOLO)PYRIMIDINE DERIVATIVE AS LRRK2 INHIBITOR
-
Paragraph 0119-0120; 0128-0129, (2020/11/23)
The present invention relates to a pyrrolo(pyrazolo)pyrimidine derivative having efficacy as an LRRK2 inhibitor, a preparation method therefor, and a pharmaceutical composition for preventing or treating degenerative brain diseases, containing the same.
RET INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
-
Paragraph 00550, (2020/07/06)
Provided herein are a RET inhibitor, a pharmaceutical composition thereof and uses thereof. In particular, provided is a compound having Formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. Provided is a pharmaceutical composition comprising the compound, and uses of the compound and pharmaceutical composition thereof for the preparation of a medicament, in particular for treatment and prevention of RET-related diseases and conditions, including cancer, irritable bowel syndrome, and/or pain associated with irritable bowel syndrome.
RET INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
-
Paragraph 00230; 00390; 00650, (2020/07/05)
Provided herein are a RET inhibitor, a pharmaceutical composition thereof and uses thereof. In particular, provided is a compound having Formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. Provided is a pharmaceutical composition comprising the compound, and uses of the compound and pharmaceutical composition thereof for the preparation of a medicament, in particular for treatment and prevention of RET-related diseases and conditions, including cancer, irritable bowel syndrome, and/or pain associated with irritable bowel syndrome.
Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype
Wellaway, Christopher R.,Bamborough, Paul,Bernard, Sharon G.,Chung, Chun-Wa,Craggs, Peter D.,Cutler, Leanne,Demont, Emmanuel H.,Evans, John P.,Gordon, Laurie,Karamshi, Bhumika,Lewis, Antonia J.,Lindon, Matthew J.,Mitchell, Darren J.,Rioja, Inmaculada,Soden, Peter E.,Taylor, Simon,Watson, Robert J.,Willis, Rob,Woolven, James M.,Wyspiańska, Beata S.,Kerr, William J.,Prinjha, Rab K.
, p. 9020 - 9044 (2020/08/24)
The bromodomain and extraterminal domain (BET) family of epigenetic regulators comprises four proteins (BRD2, BRD3, BRD4, BRDT), each containing tandem bromodomains. To date, small molecule inhibitors of these proteins typically bind all eight bromodomains of the family with similar affinity, resulting in a diverse range of biological effects. To enable further understanding of the broad phenotype characteristic of pan-BET inhibition, the development of inhibitors selective for individual, or sets of, bromodomains within the family is required. In this regard, we report the discovery of a potent probe molecule possessing up to 150-fold selectivity for the N-terminal bromodomains (BD1s) over the C-terminal bromodomains (BD2s) of the BETs. Guided by structural information, a specific amino acid difference between BD1 and BD2 domains was targeted for selective interaction with chemical functionality appended to the previously developed I-BET151 scaffold. Data presented herein demonstrate that selective inhibition of BD1 domains is sufficient to drive anti-inflammatory and antiproliferative effects.
IRAK DEGRADERS AND USES THEREOF
-
Paragraph 00962; 002243-002245, (2020/06/19)
The present invention provides compounds, compositions thereof, and methods of using the same.
BTK Inhibitors and uses thereof
-
Paragraph 1462-1466, (2020/05/02)
The invention discloses a bruton's tyrosine kinase (BTK) inhibitor and use thereof. Specifically, the invention provides heteroaromatic compounds or stereoisomers, geometrical isomers, tautomers, racemates, nitrogen oxides, hydrates, solvates, metabolites and pharmaceutically acceptable salts or prodrugs thereof, and pharmaceutical compositions containing the heteroaromatic compounds; the invention also discloses use of the heteroaromatic compounds or the pharmaceutical compositions containing the heteroaromatic compounds in preparation of medicines; the medicines can be used for treating autoimmune diseases, inflammatory diseases or proliferative diseases.
