152170-30-4Relevant academic research and scientific papers
BICYCLIC HETEROARYL SUBSTITUTED COMPOUNDS
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Page/Page column 307, (2018/03/25)
Disclosed are compounds of Formula (I) to (VIII): (I) (II) (III) (IV) (V) (VI) (VII) (VIII); or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein R3 is a bicyclic heteroaryl group substituted with zero to 3 R3a; and R1, R2, R3a, R4, and n are defined herein. Also disclosed are methods of using such compounds as PAR4 inhibitors, and pharmaceutical compositions comprising such compounds. These compounds are useful in inhibiting or preventing platelet aggregation, and are useful for the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder.
BICYCLIC HETEROCYCLIC DERIVATIVES AND METHODS OF USE THEREOF
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Page/Page column 50, (2010/08/05)
The present invention relates to novel Bicyclic Heterocyclic Derivatives, pharmaceutical compositions comprising the Bicyclic Heterocyclic Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a cognitive disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
Synthesis and structure-activity relationships of 2-(1,4′-bipiperidin-1′-yl)thiazolopyridine as H3 receptor antagonists
Rao, Ashwin U.,Palani, Anandan,Chen, Xiao,Huang, Ying,Aslanian, Robert G.,West Jr., Robert E.,Williams, Shirley M.,Wu, Ren-Long,Hwa, Joyce,Sondey, Christopher,Lachowicz, Jean
scheme or table, p. 6176 - 6180 (2010/06/16)
A series of 2-(1,4′-bipiperidine-1′-yl)thiazolopyridines was synthesized and evaluated as a new lead of non-imidazole histamine H3 receptor antagonists. Introduction of diversity at the 6-position of the pyridine ring was designed to enhance in vitro potency and decrease hERG activity. The structure-activity relationships for these new thiazolopyridine antagonists are discussed.
NOVEL PIPERAZINES, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF
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Page/Page column 92, (2008/06/13)
Disclosed are novel piperazine derivatives that act as agonists of the α7 nAChR. Also disclosed are phannaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds.
PREPARATION AND USE OF BIPHENYL-4-YL-CARBONYLAMINO ACID DERIVATIVES FOR THE TREATMENT OF OBESITY
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Page/Page column 65, (2010/11/08)
This invention relates to certain biphenyl-4-yl carbonylamino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.
Deoxygenation of polyphenols by ascomycetes : kinetic behaviour of the NADPH-dependent naphthol dehydrogenase and inhibition by tricyclazole and its analogues
Viviani, F.,Vors, J. P.,Gaudry, M.,Marquet, A.
, p. 395 - 404 (2007/10/02)
The mode of action of tricyclazole, a systemic fungicide that specifically inhibits the biosynthesis of fungal melanins, has been studied with the purified naphthol reductase from Pyricularia oryzae.The NADPH-dependent naphthol reductase transforms 1,3,6,8-tetrahydroxy-naphthalene (T4HN) into (+)scytalone and 1,3,8-trihydroxynaphthalene (T3HN) into (-)vermelone, and is very strongly inhibited by tricyclazole.Kinetic analysis reveals that the inhibition is noncompetitive with respect to T4HN or T3HN, and uncompetitive with respect to NADPH.An aza-analogue of tricyclazole has been synthesized and tested.Unexpectedly, it appears to be a competitive inhibitor of T4HN in spite of its similarity to tricyclazole. Keywords: melanin biosynthesis / polyphenol deoxygenation / naphthol dehydrogenase
