- SUBSTITUTED ARYLMETHYLUREAS AND HETEROARYLMETHYLUREAS, ANALOGUES THEREOF, AND METHODS USING SAME
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The present invention includes substituted arylmethyl ureas and heteroarylmethyl-ureas, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) infections in a patient.
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- NOVEL NICOTINAMIDE DERIVATIVES OR SALTS THEREOF
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An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. Th e present invention provides a nicotinamide derivative represented by the follo wing formula (I) (wherein R 1 represents a halogen atom; R 2 represents a C 1-12 alkyl group, a C 2-12 alkenyl group, a C 2-12 alkynyl group, a C 3-8 cycloalkyl g roup, an aryl group, an ar-C 1-6 alkyl group or a heterocyclic group, each opti onally having at least one substituent; R 3 represents an aryl group or a hetero cyclic group each optionally having at least one substituent; and R 4 and R 5 e ach independently represent a hydrogen atom; and R 2 and R 4 may form a cyc lic amino group optionally having at least one substituent together with the ni trogen atom to which they bind) or a salt thereof, and a pharmaceutical comp osition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.
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Paragraph 0894; 0895; 0898
(2018/09/08)
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- Iridium-Catalyzed, Silyl-Directed, peri-Borylation of C?H Bonds in Fused Polycyclic Arenes and Heteroarenes
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peri-Disubstituted naphthalenes exhibit interesting physical properties and unique chemical reactivity, due to the parallel arrangement of the bonds to the two peri-disposed substituents. Regioselective installation of a functional group at the position peri to 1-substituted naphthalenes is challenging due to the steric interaction between the existing substituent and the position at which the second one would be installed. We report an iridium-catalyzed borylation of the C?H bond peri to a silyl group in naphthalenes and analogous polyaromatic hydrocarbons. The reaction occurs under mild conditions with wide functional group tolerance. The silyl group and the boryl group in the resulting products are precursors to a range of functional groups bound to the naphthalene ring through C?C, C?O, C?N, C?Br and C?Cl bonds.
- Su, Bo,Hartwig, John F.
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supporting information
p. 10163 - 10167
(2018/07/31)
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- Simple synthesis of 4-substituted 1(2H)-isoquinolinones via electrophilic trapping of lithiated mono- and dianion precursors
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Synthetic routes have been developed to access 4-substituted 1(2H)-isoquinolinones from readily available precursors. This is achieved via electrophilic trapping of di- and monolithium anions derived from alkyllithium exchange of 4-bromo-1(2H)-isoquinolinones and corresponding 4-bromo-1- methoxyisoquinolines, respectively. Products derived from the latter are then hydrolyzed to the target 4-substituted 1(2H)-isoquinolinones. The methodology has potential application to access 4-substituted 1(2H)-isoquinolinones with additional substituents in either ring. Copyright Taylor & Francis Group, LLC.
- Sercel, Anthony D.,Sanchez, Joseph P.,Showalter, H. D. Hollis
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p. 4199 - 4208
(2008/03/13)
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- PYRAZOLES AND METHODS OF MAKING AND USING THE SAME
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The invention is based on the discovery that compounds of formula I possess unexpectedly high affinity for Alk 5 and/or Alk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders. In one embodiment, the invention features a compound of formula I (I).
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