- TETRAHYDROPYRAZOLO-PYRAZINYL-DIHYDROIMIDAZOLONE OR TETRAHYDROPYRAZOLO-PYRIDINYL-DIHYDROIMIDAZOLONE COMPOUNDS AND METHODS OF USING SAME
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The application relates to a compound of Formula (I) : or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of GLP-1 receptor, a pharmaceutical composition comprising a compound of Formula (I), and a method of treating or preventing a disease in which GLP-1 receptor plays a role.
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Paragraph 00564
(2022/02/05)
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- Synthesis and pharmacology of glutamate receptor ligands: New isothiazole analogues of ibotenic acid
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The naturally occurring heterocyclic amino acid ibotenic acid (Ibo) and the synthetic analogue thioibotenic acid (Thio-Ibo) possess interesting but dissimilar pharmacological activity at ionotropic and metabotropic glutamate receptors (iGluRs and mGluRs).
- J?rgensen, Charlotte G.,Clausen, Rasmus P.,Hansen, Kasper B.,Br?uner-Osborne, Hans,Nielsen, Birgitte,Bj?rn Metzler,Kehler, Jan,Krogsgaard-Larsen, Povl,Madsen, Ulf
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p. 463 - 471
(2008/03/27)
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- Regioselective lithiation and functionalization of 3-(benzyloxy)isothiazole: Application to the synthesis of thioibotenic acid
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Direct functionalization of the 3-oxygenated isothiazole heteroaromatic parental system has not yet been reported in the literature. Here, we report the first regioselective lithiation of the 5-position of 3-(benzyloxy)isothiazole (4) using LDA in diethyl ether. The versatility of the methodology was explored by quenching with a variety of electrophiles to give the desired products 7a,b,d-g in 54-68% yield. Only benzoylation aiming at the synthesis of 7c was unsuccessful. Furthermore, a highly convergent synthesis of thioibotenic acid (1), the sulfur analogue of the neurotoxic natural product ibotenic acid, was carried out.
- Bunch, Lennart,Krogsgaard-Larsen, Povl,Madsen, Ulf
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p. 2375 - 2377
(2007/10/03)
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