6019-39-2Relevant academic research and scientific papers
Rhodium-catalyzed electrophilic amination of arylboronic acids with secondary hydroxylamines
Yasuhisa, Tomohiro,Hirano, Koji,Miura, Masahiro
supporting information, p. 463 - 465 (2017/04/03)
A rhodium(III)-catalyzed electrophilic amination of arylboronic acids with secondary hydroxylamines has been developed. The rhodium catalysis is compatible with heteroarylboronic acids as well as acyl and alkoxycarbonyl protecting groups on the nitrogen of O-acylhydroxylamines, and the corresponding secondary anilines are obtained in good to excellent yields.
Identification of an indol-based derivative as potent and selective varicella zoster virus (VZV) inhibitor
Musella, Simona,di Sarno, Veronica,Ciaglia, Tania,Sala, Marina,Spensiero, Antonia,Scala, Maria Carmina,Ostacolo, Carmine,Andrei, Graciela,Balzarini, Jan,Snoeck, Robert,Novellino, Ettore,Campiglia, Pietro,Bertamino, Alessia,Gomez-Monterrey, Isabel M.
, p. 773 - 781 (2016/09/28)
We report the synthesis and antiviral activity of a new family of non-nucleoside antivirals, derived from the indole nucleus. Modifications of this template through Mannich and Friedel-Crafts reactions, coupled with nucleophilic displacement and reductive
NOVEL RHO KINASE INHIBITORS AND METHODS OF USE
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Page/Page column 88, (2012/10/18)
The subject invention concerns materials and methods for treating diseases and disorders associated with expression of Rho associated kinases (ROCKs). Examples of diseases and disorders contemplated within the scope of the invention include, but are not limited to, oncological disorders, cardiovascular diseases, CNS disorders, and inflammatory disorders. In one embodiment, a method of the invention comprises administering a therapeutically effective amount of one or more compounds of the present invention, or a composition comprising the compounds, to a person or animal in need of treatment. The subject invention also concerns compounds that inhibit ROCKs, and compositions that comprise the inhibitor compounds of the invention. Compounds contemplated within the scope of the invention include, but are not limited to, those compounds shown in Table (5).
Phenylaminopropanol derivatives and methods of their use
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Page/Page column 71, (2010/11/26)
The present invention is directed to phenylaminopropanol derivatives of formulae I, II, and III: [image] or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, schizophrenia, and combinations thereof.
PHARMACEUTICAL COMPOUNDS
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Page/Page column 39, (2010/02/07)
The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by a p38 MAP kinase such as rheumatoid arthritis and osteoarthritis; the compound being of the general formula (I): wherein U, T, V and W are each a nitrogen atom or a group CR4 provided that no more than three of U, T, V and W are nitrogen atoms; R0 is hydrogen, C1-4 hydrocarbyl, halogen or a group -A-R3; R1 is hydrogen, C1-4 hydrocarbyl or a group -A-R3; provided that only one of R0 and R1 is a group -A-R3; R2 is hydrogen, C1-4 hydrocarbyl or halogen; A is a carbon- or heteroatom-containing linker group having a linking chain length of one or two atoms; R3 is a monocyclic or bicyclic heteroaryl group containing from five to twelve ring members; each group R4 is independently selected from hydrogen, hydroxy, halogen, nitro, cyano, a monocyclic heterocyclic group having up to seven ring members, a group N(R5)2, a group C(O)N(R6)2, a group S02N(R6)2, a group Ra-Rb and a group Y; provided that no more than one group Y is present; Ra is a bond, O, S, SO, S02, NH or N-C1-4 hydrocarbyl; Rb is C1-8 hydrocarbyl optionally interrupted by O, S, SO, SO2, NH or N-C1- 4 hydrocarbyl and optionally substituted by one or more substitutents selected from hydroxy, amino, mono- or di-C1-4 hydrocarbylamino, C1 -4 hydrocarbyloxy, oxo, C1 -4 hydrocarbylthio and halogen; each group R5 is independently selected from hydrogen, C1-4 alkyl, C1-4 acyl and C 1-4 alkylsulphonyl; each group R6 is independently selected from hydrogen and C1-4 hydrocarbyl; Y is a group -N(R7)-C(O)-R8 or -N(R7)_SO2-R8; R7 is hydrogen, C1-4 hydrocarbyl or a group C(O)-R8 or S02-R8; R8 is selected from C1-l0 hydrocarbyl, CI-10hydrocarbylamino, CI-10 hydrocarbylthio, C1-l0 hydrocarbyloxy, and aryl, arylamino, arylthio and aryloxy groups, the aryl moieties of which are carbocyclic or heterocyclic and have from five to twelve ring members, each substituent group R8 being optionally substituted by one or more groups R4 other than Y; or R7 and R8 together with the nitrogen and carbon or sulphur atoms to which they are attached are linked to form a ring structure of 4 to 7 ring members; wherein R0 is other than a 2-(2,4-diamino-6-triazinyl)ethyl group when, in combination, U, T, V and W are all CH, and R1 and R2 are both hydrogen; and provided that when the group -A-R3 contains an acidic substitituent group selected from carboxylic, phosphonic and sulphonic acids and tetrazoles, or contains a -C(O)NSO2- group, or when -A- is -C(O)N- and the nitrogen atom of the group A is linked directly to a furan or thiophene ring, then either R1 is -A-R3 and both R0 and R2 are hydrogen, or R0 is-A-R3 and R1 is hydrogen.
