- C(sp2)-H Trifluoromethylation of enamides using TMSCF3: Access to trifluoromethylated isoindolinones, isoquinolinones, 2-pyridinones and other heterocycles
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A method for the direct C(sp2)-H trifluoromethylation of enamides, including biologically relevant isoindolinones, isoquinolinones and 2-pyridinones using TMSCF3 under oxidative conditions is presented. The protocol is convenient, operationally simple and exhibits high tolerance across a multitude of relevant handles and functional groups.
- Krishnamurti, Vinayak,Munoz, Socrates B.,Ispizua-Rodriguez, Xanath,Vickerman, Jeffrey,Mathew, Thomas,Surya Prakash
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supporting information
p. 10574 - 10577
(2018/09/27)
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- ANTIVIRAL COMPOUNDS
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The present invention discloses compounds of Formula (I): wherein the variables in Formula (I) are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formula (I) in the prevention or treatment of HCV infection.
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Page/Page column 97
(2014/09/29)
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- NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE
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The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
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Page/Page column 31
(2009/10/01)
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- Tetrabutylammonium pyridin-2-olate: A new reagent for the efficient synthesis of N-aryl pyridin-2-ones
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A new reagent, tetrabutylammonium pyridin-2-olate, was prepared and its application to the efficient synthesis of N-aryl pyridine-2-ones was demonstrated using CuI-catalyzed coupling reactions with aryl iodides. This coupling reaction is mild, high-yielding, and remarkably chemoselective (N- vs. O-arylation). It is also compatible with substrates containing labile functional groups. Georg Thieme Verlag Stuttgart.
- Zhang, Huiping,Chen, Bang-Chi,Wang, Bei,Chao, Sam T.,Zhao, Rulin,Lim, Ngiapkie,Balasubramanian, Balu
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experimental part
p. 1523 - 1526
(2009/04/06)
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- Preparation of N-aryl pyridones
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A novel process and intermediates thereof for making N-aryl pyridones of the type shown below from appropriate pyridinolates is described. These compounds are useful as intermediates for the synthesis of clinical candidates.
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Page/Page column 11
(2008/06/13)
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- PROLINE DERIVATIVES
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The invention relates to novel compounds of formula (I), wherein X, Y, R1, R2, R3, R4 and n have the meaning cited in claim 1, are inhibitors of the coagulation factor Xa and can be used for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.
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Page/Page column 35, 41
(2008/06/13)
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- TETRAHYDROISOQUINOLINES AS FACTOR XA INHIBITORS
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The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
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Page/Page column 61-62
(2008/06/13)
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- A versatile copper-catalyzed coupling reaction of pyridin-2(1H)-ones with aryl halides
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A robust method has been developed to couple a wide variety of pyridin-2-ones and aryl halides. This C-N bond forming reaction makes use of catalytic copper(I) iodide and the ligand 8-hydroxyquinoline. These conditions tolerate a wide degree of functional
- Filipski, Kevin J.,Kohrt, Jeffrey T.,Casimiro-Garcia, Agustin,Van Huis, Chad A.,Dudley, Danette A.,Cody, Wayne L.,Bigge, Christopher F.,Desiraju, Shrilakshmi,Sun, Shaoyi,Maiti, Samarendra N.,Jaber, Mohamad R.,Edmunds, Jeremy J.
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p. 7677 - 7680
(2007/10/03)
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- Compositions and methods for treatment of epilepsy
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A method of treating a mammal with an epileptic condition, comprising: administering to said mammal a pharmaceutical composition containing an effective amount of an N-phenyl substituted 2-pyridone compound and/or pharmaceutically acceptable salts thereof.
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- TOPICAL ANTISEPTIC COMPOSITIONS AND METHODS
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In a preferred embodiment, a method of treating bacteria, fungi, and/or viruses on the surface of, or within, the layers of the dermis of skin, ears, fingernails, toenails, or hoofs of mammalian species, comprising: applying to the surface or layers a pharmaceutical substance including an effective amount of one or more 2-(1H) pyridone compound(s).
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- CARBONYL COMPOUNDS
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The invention relates to the novel compounds of formula (I), wherein D, E, G, W, X, Y, T, R and R are defined as in claim 1. The inventive compounds inhibit coagulation factor Xa and can be used in the prophylaxis and/or therapy of thrombo-embolic diseases and for treating tumors.
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Page/Page column 112
(2008/06/13)
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- Treatment of cytokine growth factor caused disorders
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In preferred embodiments, a method of prevention and treatment of disorders caused by enhanced proliferation and enhanced biosynthesis caused by cytokine growth factors in humans and other animals, the method including: administering to a human or other animal an effective dose of a pharmaceutical substance including an N-substituted 2(1H) pyridone and/or an N-substituted 3(1H) pyridone; and a composition for prevention and treatment of disorders caused by enhanced proliferation and enhanced biosynthesis caused by cytokine growth factors in humans and other animals, the composition including: a pharmaceutical preparation including an effective dose of an N-substituted 2(1H) pyridone and/or an N-substituted 3(1H) pyridone.
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- Compositions and method for treatment of lymphomas, leukemias, and leiomyomas
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In a preferred embodiment, drugs having chemotherapeutic properties which are useful against certain neoplastic disorders with wide safety margins as evidenced by their low toxicity, and molecular actions. Such drugs include as active ingredient(s) one or more N-substituted 2-(1H) pyridone(s) and/or N-substituted 3-(1H) pyridone(s). The compositions of this invention are novel as anti-neoplastic drugs, namely as an agent for treating leukemias, lymphomas, and leiomyomas.
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- Inhibition of tumor necrosis factor α
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In a preferred embodiment, a method for the inhibition of the synthesis and release of tumor necrosis factor from various cells, comprising: administering to a human or other mammal an effective dose of one or more pharmaceutical substances selected from the group consisting of N-substituted 2(1H)pyridones, N-substituted 3(1H)pyridones, and pharmaceutically acceptable salts thereof.
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- Compositions and methods for reparation and prevention of fibrotic lesions
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In a preferred embodiment, drugs having pharmacological properties which are useful in the medicinal therapy of fibrotic disease for the reparation and prevention of fibrotic lesional tissues, such drugs including as active ingredient(s) one or more N-substituted 2-(1H) pyridone(s) and/or N-substituted 3-(1H) pyridones. The composition of this invention is novel as an anti-fibrotic drug, namely, as an agent for treating fibrosis. Any existing compounds have not been shown to be effective for the reparation and prevention of fibrotic lesions.
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- A facile copper-catalyzed Ullmann condensation: N-arylation of heterocyclic compounds containing an -NHCO- moiety
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N-Aryl heterocyclic compounds were synthesized from aryl halides and heterocyclic compounds containing an -NHCO- moiety by using a catalytic amount (1-10 mol%) of a commercially available copper catalyst in satisfactory yields. This catalytic reaction was applicable to the synthesis of N-aryl-2-pyridone, -2-pyrrolidone, -1(2H)-isoquinolone, -1(2H)- phthalazinone, -4(3H)-quinazolinone and -1,2,3-benzotriazin-4(3H)-one derivatives.
- Sugahara, Masakatsu,Ukita, Tatsuzo
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p. 719 - 721
(2007/10/03)
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- Compositions and methods for reparation and prevention of fibrotic lesions
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In a preferred embodiment, drugs having pharmacological properties which are useful in the medicinal therapy of fibrotic disease for the reparation and prevention of fibrotic lesional tissues, such drugs including as the active ingredient one or more N-substituted 2-(1H) pyridone(s). The composition of this invention is novel as an anti-fibrotic drug, namely, as an agent for treating fibrosis. Any existing compounds have not been shown to be effective for the reparation and prevention of fibrotic lesions.
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- 5-Methyl-1-phenyl-2-(1H)-pyridone compositions and methods of use
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Novel analgesic, anti-pyretic, anti-inflammatory compositions containing as the active ingredient the compound, 5-methyl-1-phenyl-2-(1H)-pyridone are described. Such compositions have also been found to cause significant lowering of serum uric acid and glucose levels and to be effective in the treatment of a number of upper respiratory ailments in humans and other mammals. Skin conditions such as dermatitis and poison ivy are also alleviated by this agent. The compositions containing 5-methyl-1-phenyl-2-(1H)-pyridone caused no irritation on oral administration or when applied to specific target tissues showed no significant irritation or other sequelae.
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