56962-04-0Relevant articles and documents
KINASE INHIBITORS
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Paragraph 0683; 0684, (2015/01/06)
Compounds of formula (I) described herein are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract
KINASE INHIBITORS
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Page/Page column 217, (2015/01/06)
This invention relates to compounds and compositions that are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
Practical one-pot C-H activation/borylation/oxidation: Preparation of 3-bromo-5-methylphenol on a multigram scale
Norberg, A. Monica,Smith III, Milton R.,Maleczka Jr., Robert E.
, p. 857 - 859 (2011/05/02)
A practical one-pot C-H activation/borylation/oxidation sequence for the generation of 3,5-disubstituted phenols is presented. Specifically, 3-bromo-5-methylphenol is prepared from 3-bromotoluene, without isolation of intermediates, on a multigram scale, and in high yield. The process proceeds under mild conditions and can be completed within one day. Georg Thieme Verlag Stuttgart - New York.
A synthesis of 3,5-disubstituted phenols
Davidson, James P.,Sarma, Keshab,Fishlock, Dan,Welch, Michael H.,Sukhtankar, Sunil,Lee, Gary M.,Martin, Michael,Cooper, Gary F.
, p. 477 - 480 (2011/04/22)
Robust and scalable syntheses of some synthetically useful 3,5- disubstituted phenols are presented. The process involves the selective displacement of a halogen by nucleophilic aromatic substitution using a preformed mixture of potassium tert-butoxide and p-methoxybenzyl alcohol (PMB-OH), followed by deprotection of the PMB ether with acid in the presence of 1,3-dimethoxybenzene. These processes have been demonstrated on kilogramscale, providing crystalline phenols in good yield and high purity.
ARYLSULFONYL PYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS
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Page/Page column 44-45, (2009/10/22)
This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5- HT6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, Irritable Bowel Syndrome, obesity and type-2 diabetes. The compounds have the general formula (1) wherein the symbols have the meanings given in the description.
CHEMICAL COMPOUNDS
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, (2009/01/23)
The present invention relates to compounds that are a non-nucleoside reverse transcriptase inhibitors, and to processes for the preparation and use of the same. Specifically, the present invention includes methods of using such compounds in the treatment of human immunodeficiency virus infection.
CHEMICAL COMPOUNDS
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, (2009/01/23)
The present invention relates to compounds that are a non-nucleoside reverse transcriptase inhibitors, and to processes for the preparation and use of the same. Specifically, the present invention includes methods of using such compounds in the treatment of human immunodeficiency virus infection.
Heterocyclic antiviral compounds
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Page/Page column 16-17, (2010/02/15)
The present invention relates to a compounds according to formula I, methods for treating diseases mediated by human immunodeficieny virus by administration of a compound according to formula I and pharmaceutical compositions for treating diseases mediated by human immunodeficieny virus containing a compound according to formula I where R1, R2, R3, R4, R5, are as defined herein.
Non-nucleoside reverse transcriptase inhibitors
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Page/Page column 41-42, (2008/06/13)
The present invention provides compounds for treating or preventing an HIV infection, or treating AIDS or ARC comprising administering a compound according to formula I where Ar, R1-R5, R7a, R7b, R7c, R8-R10, X1, X2 m, n, o and p are as defined herein.
Process for the synthesis of phenols from arenes
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Page 4; 16, (2008/06/13)
A process to synthesize substituted phenols such as those of the general formula RR′R″Ar(OH) wherein R, R′, and R″ are each independently hydrogen or any group which does not interfere in the process for synthesizing the substituted phenol including, but not limited to, halo, alkyl, alkoxy, carboxylic ester, amine, amide; and Ar is any variety of aryl or hetroaryl by means of oxidation of substituted arylboronic esters is described. In particular, a metal-catalyzed C—H activation/borylation reaction is described, which when followed by direct oxidation in a single or separate reaction vessel affords phenols without the need for any intermediate manipulations. More particularly, a process wherein Ir-catalyzed borylation of arenes using pinacolborane (HBPin) followed by oxidation of the intermediate arylboronic ester by OXONE is described.