122243-28-1Relevant academic research and scientific papers
CRYSTAL POLYMORPHISM OF KCNQ2-5 CHANNEL ACTIVATOR
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Paragraph 0107, (2019/05/18)
Crystal polymorphism may exist in a crystalline compound. In the case where crystal polymorphism exists, depending on the crystal form, solubility, dissolution rate, stability against heat, light, humidity, etc. or the like is different. Accordingly, in t
P - [...] mono hydro pell fluoro alkane derivative as a starting material and method for producing a perfluoroalkyl compounds or derivatives [...] p - (by machine translation)
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Paragraph 0031; 0032; 0033, (2018/10/16)
[Problem] to the para position of the benzene ring of the benzaldehyde derivative having a halogen atom or a phenyl ketone carbonyl group with a mono hydro pell fluoro alkane as a starting raw material, an organic material, a pharmaceutical, an agrochemical, a polymeric material such as a function of the important intermediate for the production of perfluoroalkyl compounds is simple. The following reaction schemes are illustrated in schemes [a], (1a) mono hydro pell fluoro alkane basic action, in addition to the benzene ring of the benzaldehyde derivative having a halogen atom or a phenyl ketone carbonyl group in the para position by reaction, and a benzene ring (2a) having a perfluoroalkyl group having a halogen atom at the para position of alcohol production. [Drawing] no (by machine translation)
KCNQ2-5 CHANNEL ACTIVATOR
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Paragraph 0386-0388, (2017/08/26)
The present invention relates to a compound represented by the general formula (I) (wherein the definition of each group has the same meaning as described in the specification). The compound is useful as preventive and/or therapeutic agent for KCNQ2-5 cha
ETHYL N-BOC PIPERIDINYL PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS
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Page/Page column 41; 42, (2016/05/24)
Provided are compounds of Formula I as JAK inhibitors, which are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
SUBSTITUTED 1H-PYRROLOPYRIDINONE DERIVATIVES AS KINASE INHIBITORS
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Page/Page column 28, (2014/09/03)
The present invention provides novel substituted 1H-Pyrrolopyridinone derivatives of formula (1) as protein kinase inhibitors, in which R1, R2, R3, R4, R5, R6 and 'p' have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting kinase enzyme, more particularly BTK enzyme. The present invention also provides methods for synthesizing and administering the kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
CYCLOALKYL NITRILE PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS
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Page/Page column 125, (2014/10/03)
Compounds of formula I are provided, which are JAK inhibitors and are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
N-(2-CYANO HETEROCYCLYL)PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS
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Page/Page column 55, (2014/10/03)
Provided are compounds of Formula I, a JAK inhibitor, and use thereof for the treatment of JAK-mediated diseases by the application.
ACYCLIC CYANOETHYLPYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS
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Page/Page column 43, (2014/10/03)
The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
GEMINALLY SUBSTITUTED CYANOETHYLPYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS
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Page/Page column 99, (2014/10/03)
The instant invention provides compounds of Formula (I) which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept
Ashton, Kate S.,Andrews, Kristin L.,Bryan, Marion C.,Chen, Jie,Chen, Kui,Chen, Michelle,Chmait, Samer,Croghan, Michael,Cupples, Rod,Fotsch, Christopher,Helmering, Joan,Jordan, Steve R.,Kurzeja, Robert J. M.,Michelsen, Klaus,Pennington, Lewis D.,Poon, Steve F.,Sivits, Glenn,Van, Gwyneth,Vonderfecht, Steve L.,Wahl, Robert C.,Zhang, Jiandong,Lloyd, David J.,Hale, Clarence,St. Jean, David J.
, p. 309 - 324 (2014/02/14)
Small molecule activators of glucokinase have shown robust efficacy in both preclinical models and humans. However, overactivation of glucokinase (GK) can cause excessive glucose turnover, leading to hypoglycemia. To circumvent this adverse side effect, we chose to modulate GK activity by targeting the endogenous inhibitor of GK, glucokinase regulatory protein (GKRP). Disrupting the GK-GKRP complex results in an increase in the amount of unbound cytosolic GK without altering the inherent kinetics of the enzyme. Herein we report the identification of compounds that efficiently disrupt the GK-GKRP interaction via a previously unknown binding pocket. Using a structure-based approach, the potency of the initial hit was improved to provide 25 (AMG-1694). When dosed in ZDF rats, 25 showed both a robust pharmacodynamic effect as well as a statistically significant reduction in glucose. Additionally, hypoglycemia was not observed in either the hyperglycemic or normal rats.
