- Using weak interactions to control C-H mono-nitration of indolines
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An unprecedented C-H mononitration of indolines either at the -C5 or -C7 positions under mild condition is reported here. The roles of multiple weak interactions and factors such as steric factors, electronic effects, cation-π interactions, and solvent polarity were established, and we achieved a 100% regioselective electrophilic aromatic (EArS) nitration using Cu(NO3)2 or AgNO3.
- Bose, Anima,Mal, Prasenjit
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supporting information
p. 11368 - 11371
(2017/10/19)
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- BROMODOMAIN INHIBITOR
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The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.
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Paragraph 0245
(2016/10/31)
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- HETEROCYCLIC COMPOUNDS AND USES THEREOF
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The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder, a cancer, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, dry eye or an immunologically related disease, and in some embodiments diseases or disorders related to the dysregulation of kinase such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, FLT3(D835Y), ITK, TEC, TXK, BTK, or JAK, and the respective pathways.
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Paragraph 00404
(2015/02/02)
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- IMIDAZOPYRIDINES AS A NOVEL SCAFFOLD FOR MULTI-TARGETED KINASE INHIBITION
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Compounds that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed. Formula (I).
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Page/Page column 190
(2011/05/11)
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- NOVEL PROTEIN TYROSINE PHOSPHATASE - IB INHIBITORS
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The present invention relates to the novel compounds of the general formula (I), wherein the symbols are same as described in specification, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, to process and intermediates for the preparation of the above said compounds, having the utility of these compounds in medicine and to methods for their therapeutic use, and their use in the treatment of metabolic disorders.
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Page/Page column 77
(2009/10/22)
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- HETEROCYCLE-SUBSTITUTED CYCLIC UREA DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF AS KINASE INHIBITORS
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The invention relates to the novel products of formula (I), in which V represents a heterocyclic radical, as protein kinases inhibitors.
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Page/Page column 76
(2010/02/15)
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- Synthesis of substituted benzoindolinothiazepines using 5- And 6-nitroindolines
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The synthesis of benzoindolothiazepine compounds was investigated using Friedel-Crafts reactions conditions from indolines. The amine function of indolinic identity was protected to avoid an alkylation of this function by methyl iodide. It was observed that the treatment of the desired amines with commercially available methyl chlorosulfanoylbenzonate resulted in the formation of sulfonamide compounds. It was also observed that the cyclization of the carboxylic acid under Friedel-Crafts conditions resulted in the formation of the desired tetracycles.
- Laconde,Depreux,Berthelot,Henichart
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- INHIBITORS OF 11-BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1 AND TYPE 2
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There is provided a compound having Formula (I): wherein one of R1 and R2 is a group of the Formula (a), wherein R4 is selected from H and hydrocarbyl, R5 is a hydrocarbyl group and L is an optional linker group, or R1 and R2 together form a ring substituted with the group (Formula (a)) wherein R3 is H or a substituent, and wherein X is selected from S, O, NR6 and C(R7)(R8), wherein R6 is selected from H and hydrocarbyl groups, wherein each of R7 and R8 are independently selected from H and hydrocarbyl groups.
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Page/Page column 110; 111
(2010/02/06)
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- Regioselectivity in electrophilic substitution of 5-aminoindoles and 5-aminoindolines: Synthesis of pyrrolo[3,2-e]indoles and isomeric pyrrolo[2,3-f]indoles
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An FMO Theory prediction that 5-aminoindoles, 5, should react with electrophiles preferentially at C4 rather than at C6 whereas N1-acyl-5-aminoindolones, 6, should react preferentially at C6 rather than C4 is borne out experimentally by the synthesis of a pyrrolo[3,2-e]indole from 5 and pyrrolo[2,3-f]indoles from 6.
- Prasad,Burchat,Weeratunga,Watts,Dmitrienko
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p. 5035 - 5038
(2007/10/02)
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