30766-12-2Relevant academic research and scientific papers
Novel indirect AMP-activated protein kinase activators: Identification of a second-generation clinical candidate with improved physicochemical properties and reduced hERG inhibitory activity
Kuramoto, Kazuyuki,Sawada, Yuki,Yamada, Tomohiro,Nagashima, Takeyuki,Ohnuki, Kei,Shin, Takashi
, p. 452 - 465 (2020/09/09)
This study reports the synthesis and evaluation of novel indirect AMP-activated protein kinase (AMPK) activators. The series of compounds selectively inhibited cell growth in several human breast cancer cell lines by activating AMPK. We performed back-up medicinal chemistry synthetic research on ASP4132, a previously reported as a compound for clinical development that acts as an indirect AMPK activator. This led to the successful identification of 4-({4-[5-({1-[(5-ethoxypyrazin-2-yl)methyl]-4-fluoropiperidin-4-yl}methoxy)-3-methylpyridine-2-carbonyl]piperazin-1-yl}methyl)benzonitrile succinate (27b), a potent, highly aqueous soluble and metabolically stable compound in human hepatocytes. Compound 27b also showed weaker human Ether-a-go-go Related Gene (hERG) inhibitory activity than that of compound 13 and ASP4132. Therefore, 27b was a promising AMPK activator and a second-generation clinical candidate for treatment for human cancer.
HETEROCYCLIC COMPOUNDS AND THEIR USE FOR TREATMENT OF HELMINTHIC INFECTIONS AND DISEASES
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Paragraph 00314, (2020/11/03)
Provided herein are Heterocyclic compounds of formula (I): and pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein W, X, Y, R1, R2, and RN are as defined herein, compositions comprising an effective amount of a Heterocyclic Compound, and methods for treating or preventing animal and human filarial worm infections and diseases.
As neuroprotective agents of pharmaceutical compounds
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Paragraph 0314; 0315; 0316; 0317, (2019/06/26)
The invention discloses a medicinal compound as a neuroprotective agent. The medicinal compound is a neuronal nitric oxide synthase-postsynaptic density protein 95 (nNOS-PSD95) decoupling agent. The medicinal compound is a benzene ring derivative shown in the general formula (I) or its pharmaceutically acceptable salt. The invention further discloses a preparation method of the medicinal compound and a use of the medicinal compound in prevention and treatment on neuronal damage influence-caused diseases.
MODIFIED COMPOUND OF ANDROGRAPHOLIDE
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Paragraph 0260-0262, (2019/01/04)
The present disclosure discloses a modified compound of andrographolide, and particularly discloses a compound shown in formula (I) and (II) or a pharmaceutically acceptable salt thereof.
PYRIDINEAMINE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS
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Page/Page column 71-72, (2016/12/22)
The present disclosure describes pyridineamine compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer, immune disorders and other diseases. Formula (I).
QUINOLINE AND QUINAZOLINE COMPOUNDS
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Paragraph 00306, (2016/05/02)
In some embodiments, the invention relates to quinazoline and quinoline compounds of Formula I: (I) or a pharmaceutically acceptable salt thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, in some embodiments, the present invention relates to quinazoline and quinoline compounds, pharmaceutical compositions thereof, and the use of the compounds and pharmaceutical compositions in the treatment of Bruton's tyrosine kinase (BTK) mediated disorders.
BICYCLIC HETEROAROMATIC CARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS
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Page/Page column 96-97, (2016/02/26)
The present disclosure describes bicyclic heteroaromatic carboxamide derivatives of formula (I), as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
THIAZALOPYRROLIDINE INHIBITORS OF ROR-GAMMA
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Paragraph 00198, (2014/11/13)
Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by ROR?. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I) and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.
COMPOUNDS AND METHODS
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Page/Page column 62, (2013/03/26)
The present invention relates to novel retinoid-reiated orphan receptor gamma (RORy) modulators and their use in the treatment of diseases mediated by RORy.
THERAPEUTIC METHODS
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Page/Page column 52, (2013/06/27)
The present invention relates to methods of treatment of diseases mediated by ROR?.
