28121-73-5Relevant academic research and scientific papers
PROSTAGLANDIN E2 (PGE2) EP4 RECEPTOR ANTAGONISTS
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Page/Page column 78; 131, (2021/04/10)
The present invention relates to novel compounds of formula (I) and pharmaceutical compositions containing these compounds. The compounds provided herein can act as prostaglandin E2 (PGE2) EP4 receptor antagonists, which renders them highly advantageous for use in therapy, particularly in the treatment or prevention of cancer, a neovascular eye disease, inflammatory pain, or an inflammatory disease, such as, e.g., multiple sclerosis, rheumatoid arthritis or endometriosis.
With the biological activity of the 1, 3, 8 - triazaspiro [4, 5] decane - 2 - guanidine - 4 - ketone compound and its preparation method and application
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Paragraph 0019; 0020, (2017/08/25)
The present invention discloses a 1,3,8-triazaspiro[4,5]decane-2-guanidine-4-ketone compound with biological activity, a preparation method therefor and application thereof, and belongs to the technical field of pesticide synthesis. A technical solution of the present invention is that: the 1,3,8-triazaspiro[4,5]decane-2-guanidine-4-ketone compound with biological activity has the formula shown in the specification, wherein R is ethyl, propyl, isopropyl or phenyl. The present invention also discloses a preparation method of the 1,3,8-triazaspiro[4,5]decane-2-guanidine-4-ketone compound with biological activity, and application thereof in preparing pesticides. According to the invention, by a new method, a series of 1,3,8-triazaspiro[4,5]decane-2-guanidine-4-ketone compounds with biological activity are synthesized. The invention has the advantages of simple and easy operation in a reaction process, easy access to cheap raw materials, higher reaction efficiency, better repeatability, and remarkable bioactive effects, and has better prospects for application in the field of pesticide preparation.
SUBSTITUTED SPIROCYDIC INHIBITORS OF AUTOTAXIN
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Page/Page column 80, (2015/11/17)
The present invention relates to compounds according to Formula 1 and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancer, lymphocyte homing, chronic inflammation, neuropathic pain, fibrotic diseases, thrombosis, and cholestatic pruritus, mediated at least in part by ATX.
INHIBITORS OF UNDECAPRENYL PYROPHOSPHATE SYNTHASE
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Page/Page column 145, (2008/06/13)
The present invention relates to compounds that are selective and/or potent inhibitors of UPPS. In addition to compounds which inhibit UPPS, the invention also provides pharmaceutical compositions comprising these compounds and methods of using these comp
New Spiropiperidines as Potent and Selective Non-Peptide Tachykinin NK2 Receptor Antagonists
Smith, Paul W.,Cooper, Anthony W. J.,Bell, Richard,Beresford, Isabel J. M.,Gore, Paul M.,et al.
, p. 3772 - 3779 (2007/10/03)
The synthesis of a series of 2-(5-fluoro-1H-indol-3-yl)ethyl spiropiperidines is described together with their tachykinin NK2 receptor affinities measured in a rat colon binding assay.Equivalent NK2 receptor binding affinity was observed for the spirooxalidinone 3-benzyl-8--1-oxa-3,8-diazaspirodecan-2-one (3a), the imidazolidinone 3-benzyl-8--1,3,8-triazaspirodecan-2-one (3s), and the pyrrolidinone 2-benzyl-8--2,8-diazaspirodecan-3-one (3t).Substitution in the phenyl ring of compound 3a produced no significant enhancement in NK2 binding affinity.Replacement of the phenyl ring in 3a with other aromatic rings resulted in a significant loss in binding affinity.Compound 3a was shown to be a potent NK2 receptor antagonist in guinea pig trachea where it also demonstrated 1000-fold selectivity for NK2 receptors over NK1.In the anesthesized guinea pig, compound 3a administered by the intravenous or oral route displayed potent and long-lasting antagonist activity against NK2 receptor agonist induced bronchoconstriction.
