- A convenient synthesis of gimeracil
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A practical three-step synthetic approach to gimeracil in a 68% overall yield is described, using 2,4-dimethoxypyridine as the starting material with 3,5-dichloro-2,4-dimethoxypyridine and 3,5-dichloro-2,4-dihydroxypyridine as intermediates. The advantages of this procedure include short reaction steps, simple operation and good yield.
- Li, Xiao-Lin,Zhu, Hao-Ting,Zhan, Li,Liu, Ting,Cheng, Guang,Liu, Ning,Yu, Shan-Bao,Li, Hui,Luo, Yu,Yang, Fan,Tang, Jie
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- ANTI-FIBROTIC PYRIDINONES
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This application relates to polycyclic compounds with a pyridinone or pyridinone derivative core including, substituted pyridinones, 5,6- and 6,6- bicyclic heterocycles and substituted pyridine-thiones. This application also discloses methods of preparing these polycyclic compounds, pharmaceutical compositions and medicaments comprising said compounds and methods to treat, prevent or diagnose diseases, disorders or conditions associated with fibrosis.
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Paragraph 0677
(2015/11/02)
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- ANTI-FIBROTIC PYRIDINONES
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Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
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Paragraph 0883-0884
(2014/04/17)
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- CHEMICAL COMPOUNDS AND PROCESSES
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The present invention relates generally to chemical compounds and methods for their use and preparation. In particular, the invention relates to chemical compounds which may possess useful therapeutic activity, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds.
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Page/Page column 74
(2008/12/06)
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- NOVEL PYRIDINONE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2-RECEPTORS
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The present invention relates to novel compounds, in particular novel pyridinone derivat ives according to Formula (I) X R1 N Y (I) R2 R3 wherein all radicals are defined in the application. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subt ype 2 ("mGluR2") which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved. "
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Page/Page column 114
(2010/10/20)
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- Rearrangaments of Azabiphenylenes. The Impact of Nitrogen Number and Position
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4-Methoxy-1-azabiphenylene and 1-methoxy-2-azabiphenylene have been synthesized from the appropriate precursor diethynylmethoxypyridines via cobalt-catalyzed cooligomerization with bis(trimethylsilyl)acetylene.When 4-methoxy-1,3-diazabiphenylene was transformed into 1,3-dimethoxyisoquinoline in methanolic sodium methoxide at reflux overnight, 1-methoxy-2-azabiphenylene required longer reflux time and 4-methoxy-1-azabiphenylene required forcing conditions for transformations to occur.The transformations product from the latter was shown to be 1,5-dimethoxy-2-benzazocine and that from the former was established by independent synthesis to be 3-methoxy-1-((E)-2-methoxyethenyl)isoquinoline.The impressive disparity in the products obtained from the methoxydiazabiphenylene and the two methoxyazabiphenylenes can be rationalized by consideration of the locus of methanol addition and sequential electrocyclic reactions.
- Gibson, Katharine J.,d'Alarcao, Marc,Leonard, Nelson J.
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p. 2462 - 2468
(2007/10/02)
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