- PHARMACEUTICAL COMPOUNDS
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Benzodiazepine derivatives of formula (I): (I) wherein: each of R1 and R2 is independently H or halo; either (i) T is N, Z is C, ---a--- and ---c--- are bonds, and ---b--- and ---d--- are absent; or (ii) T is C, Z is N, ---b--- and ---d--- are bonds, and ---a--- and ---c--- are absent; each of R3 and R4 is independently halo, -OR6, -NR6R7, -COR8, -C(O)OR8, -CON(R8)2 or -R6; R5 is H or halo; each of R6 and R7 is independently H or a group selected from C1-C6 alkyl, C3-C10 cycloalkyl, C6-C10 aryl, 4- to 10-membered heterocyclyl and 4- to 10-membered heteroaryl, the group being unsubstituted or substituted; R8 is H or C1-C6 alkyl, each R8 being the same or different when two are present; n is 0 or 1; and one of V, W, X and Y is N or CH and the other three are CH; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.
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Page/Page column 61; 62
(2021/02/26)
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- ISOXAZOLE DERIVATIVE AS MUTATED ISOCITRATE DEHYDROGENASE 1 INHIBITOR
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It has been found that a compound of the general formula (I) having an isoxazole skeleton has excellent inhibitory activity against mutant IDH1 protein and inhibits the production of 2-HG by this protein, while the compound is also capable of effectively inhibiting the growth of various tumors expressing the protein. In the formula, R1, R2, R3, Y, and Z are as defined in claim 1.
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Paragraph 0157; 0158; 0159
(2018/02/06)
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- Reformatsky and Blaise reactions in flow as a tool for drug discovery. One pot diversity oriented synthesis of valuable intermediates and heterocycles
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The application of Reformatsky and Blaise reactions for the preparation of a diverse set of valuable intermediates and heterocycles in a one-pot protocol is described. To achieve this goal, a greener activation protocol for zinc in flow conditions has been developed to introduce this metal efficiently into α-bromoacetates. The organozinc compounds were added to a diverse set of ketones and nitriles to obtain a wide range of functional groups and heterocyclic systems.
- Huck,Berton,De La Hoz,Díaz-Ortiz,Alcázar
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supporting information
p. 1420 - 1424
(2017/05/12)
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- PRODUCTION PROCESS OF 2,3'-BIPYRIDYL-6'-ONE
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A production process where 2,3′-bipyridyl-6′-one can be produced in high purity at low cost on an industrial scale without using an expensive catalyst or special equipment is provided. A process for producing 2,3′-bipyridyl-6′-one comprises reacting an acetylpyridine derivative with at least one of compounds represented by formulae (II) to (V) to synthesize a bipyridine derivative and hydrolyzing the bipyridine derivative by one-pot preparation. In formulae (II) to (V), each of R2 to R8, X and Y represents a given group.
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Page/Page column 9
(2010/02/17)
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- PROCESS FOR PRODUCTION OF 2,3'-BIPYRIDYL-6'-ONE
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A production process where 2,3'-bipyridyl-6'-one can be produced in high purity at low cost on an industrial scale without using an expensive catalyst or special equipment is provided. A process for producing 2,3'-bipyridyl-6'-one comprises reacting an acetylpyridine derivative with at least one of compounds represented by formulae (II) to (V) to synthesize a bipyridine derivative and hydrolyzing the bipyridine derivative by one-pot preparation. In formulae (II) to (V), each of R2 to R8, X and Y represents a given group.
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Page/Page column 13
(2009/12/07)
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- ANTIVIRAL AGENTS
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The present invention is directed to compounds that are antiviral agents. Specificially the compounds of the present invention inhibit replication of HCV and are therefore useful in treating hepatitis C infections. The present invention is also directed t
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Page/Page column 38
(2010/11/25)
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- Simple synthesis of (±)-epibatidine
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Concise synthesis of racemic epibatidine (1), a non-opioid analgesic alkaloid, was accomplished starting from 6-chloropyridyl-3-carbaldehyde (6) via Robinson annulation for the construction of the skeleton, by introduction of amino group through Curtius r
- Roy, Balaram,Watanabe, Hidenori,Kitahara, Takeshi
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p. 861 - 871
(2007/10/03)
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