122243-28-1Relevant articles and documents
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.
Inhibition of hypoxia-induced gene transcription by substituted pyrazolyl oxadiazoles: Initial lead generation and structure-activity relationships
Haerter, Michael,Thierauch, Karl-Heinz,Boyer, Stephen,Bhargava, Ajay,Ellinghaus, Peter,Beck, Hartmut,Greschat-Schade, Susanne,Hess-Stumpp, Holger,Unterschemmann, Kerstin
supporting information, p. 61 - 66 (2014/01/17)
The transcription factors hypoxia-inducible factor-1 and -2 (HIF-1 and HIF-2) orchestrate a multitude of processes that allow tumor cells to survive under conditions of low oxygen and nutrients, and that lead to resistance to some apoptotic pathways and facilitate invasion and metastasis. Therefore, inhibition of transactivation by HIF has become an attractive target in cancer research. Herein we present the results of a cell-based screening approach that led to the discovery of substituted 1H-pyrazole-3-carboxamides. Chemical optimization of the hit class with respect to potency and metabolic stability is described; it resulted in novel 5-(1H-pyrazol-3-yl)-1,2,4-oxadiazoles that inhibit the hypoxia-induced accumulation of HIF-1α and HIF-2α. The HIF inhibitory potency in the screening cell system was improved from IC 50 190 to 0.7 nM, and significant parts of the SAR are disclosed. For a key compound, the ability to suppress the hypoxia-induced expression of HIF target genes was studied in A549 human lung adenocarcinoma cells. The same compound shows a favorable pharmacokinetic profile in rats after i.v. and p.o. administration. Suppressing HIF target genes: Substituted 5-(1H-pyrazol-3-yl)-1, 2,4-oxadiazoles are presented as a novel chemotype to specifically inhibit the hypoxia-induced transcription of target genes of the transcription factor hypoxia-inducible factor (HIF). The new chemotype was derived from 1H-pyrazole-3-carboxamides that had been discovered from a cell-based screen. We present the optimization of the potency and metabolic stability of the initial screening hit. Copyright
SUBSTITUTED OXADIAZOLYL PYRIDINONES AND OXADIAZOLYL PYRIDAZINONES AS HIF INHIBITORS
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Paragraph 0485; 0486; 0487; 0488, (2014/11/13)
The present application relates to novel substituted 5-(1,2,4-oxadiazol-5-yl)pyridin-2-ones and 6-(1,2,4-oxadiazol-5-yl)pyridazin-3-ones, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for producing medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be effected in the form of monotherapy or else in combination with other medicaments or further therapeutic measures.
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.