- Application of Vinamidinium Salt Chemistry for a Palladium Free Synthesis of Anti-Malarial MMV048: A bottom-Up Approach
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MMV390048 (1) is a clinical compound under investigation for antimalarial activity. A new synthetic route was developed which couples two aromatic fragments while forming the central pyridine ring over two steps. This sequence takes advantage of raw materials used in the existing etoricoxib supply chain and eliminates the need for palladium catalysts, which were projected to be major cost-drivers.
- Paymode, Dinesh J.,Chang, Le,Chen, Dan,Wang, Binglin,Kashinath, Komirishetty,Gopalsamuthiram, Vijayagopal,McQuade, D. Tyler,Vasudevan,Ahmad, Saeed,Snead, David R.
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p. 5400 - 5404
(2021/07/26)
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- NITROGEN-CONTAINING HETEROCYCLIC ALKENYL COMPOUND, ORGANIC SEMICONDUCTOR MATERIAL AND ORGANIC SEMICONDUCTOR DEVICE
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PROBLEM TO BE SOLVED: To provide a compound that is high in charge transfer and atmosphere stability and is suitable for an organic semiconductor material, provide an organic semiconductor material comprising the compound, and provide an organic semiconductor element comprising the organic semiconductor material. SOLUTION: The present invention provides a compound represented by formula (1), specifically a compound represented by formula (2) (Ar1 is an unsaturated cyclic hydrocarbon group or the like; Ar2 is an unsaturated heterocyclic group containing nitrogen with an unshared electron pair, or the like; B is -CH=CH- or -C≡C-; X11-X13 independently represent C-R or N; at least one of X12 and X13 is N). SELECTED DRAWING: Figure 1 COPYRIGHT: (C)2018,JPOandINPIT
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Paragraph 0135; 0136
(2017/12/27)
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- COMPOUNDS USEFUL AS CSF1 MODULATORS
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This invention relates to novel compounds and to pharmaceutical compositions comprising the novel compounds. More specifically, the invention relates to compounds useful as Colony Stimulating Factor 1 Receptor (cFMS) modulators (e.g. cFMS inhibitors). This invention also relates to processes for preparing the compounds, uses of the compounds in treatment and methods of treatment employing the compounds. Specifically, the invention relates to the use of the compounds for the treatment of cancer and autoimmune diseases.
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Paragraph 00383; 00384; 00385
(2016/04/26)
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- INDOLE CARBOXAMIDE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS
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The invention relates to indole carboxamide derivatives of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.
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- Benzamides
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The present invention is directed to benzamide containing compounds which inhibit the P2X7 receptor
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Paragraph 0117
(2014/05/07)
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- NOVEL TRPV3 MODULATORS
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Disclosed herein are modulators of TRPV3 of formula (II): wherein G1, X1, X2, X3, X4, X5, G2, Ra, Rb, and u are as defined in the specification. Composition
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Paragraph 1576; 1577
(2013/06/04)
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- NOVEL TRPV3 MODULATORS
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Disclosed herein are modulators of TRPV3 of formula (II): wherein G1, X1, X2, X3, X4, X5, G2, Ra, Rb, and u are as defined in the specification. Composition
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Paragraph 103; 104
(2013/05/21)
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- Efficient methods for the synthesis of arylacetonitriles
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Various approaches to [2-fluoro-4-(trifluoromethyl)phenyl]acetonitrile were investigated. Two of these methods were selected and applied to a variety of electron-deficient substrates, thereby expanding the scopes of the procedures.
- Stazi, Federica,Maton, William,Castoldi, Damiano,Westerduin, Pieter,Curcuruto, Ornella,Bacchi, Sergio
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experimental part
p. 3332 - 3338
(2010/11/20)
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- HETEROAROMATIC MONOAMIDES AS OREXININ RECEPTOR ANTAGONISTS
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The present invention is concerned with novel sulfonamides of formula wherein R1, R2, R3, R4, R5, Ar, Ar1, Ar2, n, o and p are as described in the description and claims. The compounds are orexin receptor antagonists that may be useful in the treatment of disorders, in which orexin pathways are involved.
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Page/Page column 14; 22-23; 40
(2009/12/27)
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