- Nickel(IV)-Catalyzed C-H Trifluoromethylation of (Hetero)arenes
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This Article describes the development of a stable NiIV complex that mediates C(sp2)-H trifluoromethylation reactions. This reactivity is first demonstrated stoichiometrically and then successfully translated to a NiIV-catalyzed C-H trifluoromethylation of electron-rich arene and heteroarene substrates. Both experimental and computational mechanistic studies support a radical chain pathway involving NiIV, NiIII, and NiII intermediates.
- Meucci, Elizabeth A.,Nguyen, Shay N.,Camasso, Nicole M.,Chong, Eugene,Ariafard, Alireza,Canty, Allan J.,Sanford, Melanie S.
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supporting information
p. 12872 - 12879
(2019/08/26)
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- TRICYCLIC DLK INHIBITORS AND USES THEREOF
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The invention relates to compounds of formula (I) and salts thereof, wherein ring A and R1-R2 have any of the values defined in the specification. The compounds and salts are useful for treating DLK mediated disorders. The invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable salt thereof, as well as methods of using said compounds, salts, or compositions as DLK inhibitors and for treating neurodegeneration diseases and disorders.
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Page/Page column 72
(2016/09/26)
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- 3-SUBSTITUTED PYRAZOLES AND USE AS DLK INHIBITORS
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The present invention provides for compounds of Formula (I) and various embodiments thereof, and compositions comprising compounds of Formula (I) and various embodiments thereof. (I) In compounds of Formula I, the groups R1, R2, R3, R4, R5, R6 and R7 have the meaning as described herein. The present invention also provides for methods of using compounds of Formula I and compositions comprising compounds of Formula (I) as DLK inhibitors and for treating neurodegeneration diseases and disorders.
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Page/Page column 105
(2014/08/06)
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- AZABICYCLO COMPOUND AND SALT THEREOF
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It is intended to provide a novel azabicyclo compound which exhibits both HSP90 inhibitory activity and cell proliferation inhibitory effect. Specifically disclosed is a compound represented by the following general formula (I) or a salt thereof: wherein X1 represents CH or N; any one of X2, X3 and X4 represents N, and the others represent CH; any one or two of Y1, Y2, Y3 and Y4 represent C—R4, and the others are the same or different and represent CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S and O; R2 represents an alkyl group having 1 to 6 carbon atoms, or the like; and R3 and R4 represent —CO—R5 or the like.
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Page/Page column 30
(2012/05/07)
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- Novel Compounds for the Treatment of Diseases Associated with Amyloid or Amyloid-Like Proteins
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The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.
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Page/Page column 80
(2011/11/30)
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- Improved synthesis of the selective rho-kinase inhibitor 6-chloro-n4-{3,5-difluoro-4-[(3-methyl-1h-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl} pyrimidin-2,4-diamine
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A highly potent and selective Rho-kinase inhibitor containing a 7-azaindole moiety has been developed at Bayer Schering Pharma. Herein we disclose details of a significantly improved synthesis of the compound in 8.2% overall yield. Key aspects include cost and safety considerations and the uncommon use of a trifluoromethyl group with controllable reactivity as a masked methyl group.
- Schirok, Hartmut,Paulsen, Holger,Kroh, Walter,Chen, Gang,Gao, Ping
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experimental part
p. 168 - 173
(2010/04/29)
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- Synthesis and derivatization of 3-perfluoroalkyl-substituted 7-azaindoles
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An expedient large-scale synthesis of 3-perfluoroalkyl-7-azaindoles starting from 2-fluoropyridine is presented. The activation as 6-chloro-4-nitro derivative allows the further derivatization by nucleophilic aromatic substitution in the 4-position. Georg
- Schirok, Hartmut,Figueroa-Perez, Santiago,Thutewohl, Michael,Paulsen, Holger,Kroh, Walter,Klewer, Dagmar
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p. 251 - 258
(2007/10/03)
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