- OXADIAZOLE COMPOUNDS
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The present invention relates to a compound of formula (I) or (II) or a stereoisomer, enantiomer, racemic, or tautomer thereof, (I) (II) wherein R1,R2,R3,L1,L2,L3,L4,L5 and n, have the same meaning as that defined in the claims and the description. The present invention also relates to compositions, in particular pharmaceuticals, comprising such compounds, and to uses of such compounds and compositions for the prevention and/or treatment of metabolic disorders and/or neurodegenerative diseases, and/or protein misfolding disorders.
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Page/Page column 145; 146
(2015/11/11)
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- Condensation of Vilsmeier salts, derived from tetraalkylureas, with amidoximes: a novel approach to access N,N-dialkyl-1,2,4-oxadiazol-5-amines
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A novel approach, consendation of vilsmeier salts and amidoximes, to access N,N-dialkyl-1,2,4-oxadiazol-5-amines has been developed. By this approach, a broad range of N,N-dialkyl-1,2,4-oxadiazol-5-amines, including aromatic, heteroaromatic and alphatic s
- Su, Dongshan,Duan, Haifeng,Wei, Zhonglin,Cao, Jungang,Liang, Dapeng,Lin, Yingjie
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supporting information
p. 6959 - 6963
(2019/04/10)
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- PYRAZOLO [1,5-ALPHA] PYRIMIDINYL DERIVATIVES USEFUL AS CORTICOTROPIN-RELEASING FACTOR (CRF) RECEPTOR ANTAGONISTS
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CRF receptor antagonists are disclosed which may have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in mammals. The CRF receptor antagonists of this invention have the following structure: (I); and pharmaceutically acceptable salts, esters, solvates, stereoisomers and prodrugs thereof, wherein R1, R2a, R2b, Y, Het, n, o, R6, Ar and R7 are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.
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Page/Page column 49
(2008/06/13)
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- 2-(2-Thienyl)-5,6-dihydroxy-4-carboxypyrimidines as inhibitors of the hepatitis C virus NS5B polymerase: Discovery, SAR, modeling, and mutagenesis
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Infections caused by hepatitis C virus (HCV) are a significant world health problem for which novel therapies are in urgent demand. The polymerase of HCV is responsible for the replication of viral RNA. We recently disclosed dihydroxypyrimidine carboxylates 2 as novel, reversible inhibitors of the HCV NS5B polymerase. This series was further developed into 5,6-dihydroxy-2-(2- thienyl)pyrimidine-4-carboxylic acids such as 34 (EC50 9.3 μM), which now show activity in the cell-based HCV replication assay. The structure-activity relationship of these inhibitors is discussed in the context of their physicochemical properties and of the polymerase crystal structure. We also report the results of mutagenesis experiments which support the proposed binding model, which involves pyrophosphate-like chelation of the active site Mg ions.
- Koch, Uwe,Attenni, Barbara,Malancona, Savina,Colarusso, Stefania,Conte, Immacolata,Di Filippo, Marcello,Harper, Steven,Pacini, Barbara,Giomini, Claudia,Thomas, Steven,Incitti, Ilario,Tomei, Licia,De Francesco, Raffaele,Altamura, Sergio,Matassa, Victor G.,Narjes, Frank
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p. 1693 - 1705
(2007/10/03)
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- NOVEL ALKYNYL DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
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The present invention relates to novel compounds of formula (I) wherein W, n, X and W’ are defined in the description; invention compounds are modulators of metabotropic glutamate receptors - subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
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Page/Page column 99
(2008/06/13)
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- Synthesis of various 3-substituted 1,2,4-oxadiazole-containing chiral β3- and α-amino acids from Fmoc-protected aspartic acid
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Various 3-substituted chiral 1,2,4-oxadiazole-containing Fmoc-β 3- and α-amino acids were synthesized from FmoC-(L or D)-Asp(OtBu)-OH and Fmoc-L-Asp-OtBu, respectively, in three steps (i.e., condensation of an aspartyl derivative with different
- Hamze?, Abdallah,Hernandez, Jean-Franc?ois,Fulcrand, Pierre,Martinez, Jean
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p. 7316 - 7321
(2007/10/03)
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- The Syntheses of Triazole, Sulfur-Containing Diazole and N-Phenylthiatriazole Biphenyltetrazoles as Potential Angiotensin II Receptor Antagonists
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The syntheses of triazole, sulfur-containing diazole and N-phenylthiatriazole analogs of imidazole angiotensin II antagonist, DuP 753, are reported. 5-Butyl-3-[(2-trifluoromethyl)phenyl]-2,1,3,4-1H-thiatriazole-2-one biphenyltetrazole (63) is found to hav
- Chou, Shan-Yen,Chen, Su-San,Ho, Chin-Chung,Huang, Shiang-Ling,Huang, Tsai-Mien,Pan, Ohm-Guo,Wang, Chia-Lin,Chen, Ying,Lu, Hsiao-Hwa,Liu, Shih-Hwa,Huang, Shir-Ly,Chiang, Ren-Shou
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- PREPARATION OF A MODEL SYSTEM FOR A CONSTRAINED ANGIOTENSIN II RECEPTOR ANTAGONIST
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An imidazooxazin-8-one system, designed to be a fused ring analog of a potent angiotensin II receptor antagonist, was prepared.
- Boschelli, Diane H.,Connor, David T.
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p. 121 - 124
(2007/10/02)
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- BIPHENYL OXADIAZINONE ANGIOTENSIN II INHIBITORS
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Angiotension II inhibition is exhibited by STR1 wherein: R. sup.1 and R 2 are each independently hydrogen, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, thiophenalkyl, pyridylalkyl, or--R 8 CO. sub.2 R 9 ;R 3 is a single bond,--S--, or--O--;
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- Oxadiazinone substituted indole and benzimidazole derivatives
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Novel compounds having the formula STR1 wherein X, R1, R2, R3, R4 and R5 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
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