- Sustainable organophosphorus-catalysed Staudinger reduction
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A highly efficient and sustainable catalytic Staudinger reduction for the conversion of organic azides to amines in excellent yields has been developed. The reaction displays excellent functional group tolerance to functionalities that are otherwise prone to reduction, such as sulfones, esters, amides, ketones, nitriles, alkenes, and benzyl ethers. The green nature of the reaction is exemplified by the use of PMHS, CPME, and a lack of column chromatography.
- Lenstra, Danny C.,Lenting, Peter E.,Mecinovi?, Jasmin
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supporting information
p. 4418 - 4422
(2018/10/17)
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- MATRIX METALLOPROTEINASE INHIBITORS
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This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, pulmonary inflammation, acute respiratory distress syndrome, periodontitis, multiple sclerosis, gingivitis, gingivitis, atherosclerosis, dry eye, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and pounds.
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Paragraph 0395; 0396
(2014/06/11)
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- 1, 2, 4-TRIAZOLONE DERIVATIVE
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The present invention provides a 1,2,4-triazolone derivative represented by Formula (1A) having an antagonistic activity on the arginine-vasopressin 1b receptor or a pharmaceutically acceptable salt thereof and provides a pharmaceutical composition comprising the compound or the salt as an active ingredient, in particular, a therapeutic or preventive agent exhibiting favorable pharmacokinetics in a disease such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, or alopecia.
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Paragraph 0411; 0412; 0413
(2013/08/14)
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- MATRIX METALLOPROTEINASE INHIBITORS
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This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, dry eye, neointimal proliferation, which leads to restenosis and ischemic heart faliure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by over-expression and over-activation of matrix metalloproteinase using the compounds.
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Page/Page column 46
(2012/04/10)
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- Scalable synthesis of the VEGF-R2 kinase inhibitor JNJ-17029259 using ultrasound-mediated addition of MeLi-CeCl3 to a nitrile
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(Chemical Equation Presented) The preparation of the selective VEGF-R2 kinase inhibitor 10 (JNJ-17029259) is described in which the key precursor, 4-(5-isoxazolyl)benzonitrile, undergoes clean transformation to the corresponding cumylamine derivative with
- Reuman, Michael,Beish, Sandra,Davis, Jeremy,Batchelor, Mark J.,Hutchings, Martin C.,Moffat, David F. C.,Connolly, Peter J.,Russell, Ronald K.
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p. 1121 - 1123
(2008/09/18)
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- In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: Trends across multiple chemical series
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Structure-activity relationships (SAR) were analyzed within a library of diverse yet simple compounds prepared as histamine H3 antagonists. The libraries were constructed with a variety of low molecular weight pyrrolidines, selected from (R)-2-methylpyrrolidine, (S)-2-methylpyrrolidine, and pyrrolidine.
- Nersesian, Diana L.,Black, Lawrence A.,Miller, Thomas R.,Vortherms, Timothy A.,Esbenshade, Timothy A.,Hancock, Arthur A.,Cowart, Marlon D.
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p. 355 - 359
(2008/04/03)
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- PROCESS FOR THE SYNTHESIS OF DERIVATIVES OF 3-AMINO-TETRAHYDROFURAN-3-CARBOXYLIC ACID AND USE THEREOF AS MEDICAMENTS
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The present invention relates to a process for the manufacturing of substituted 3- amino-tetrahydrofuran-3-carboxylic acid amides of general formula (I) and their precursors in high optical purity to the precursors of the synthesis of substituted S-Amino-tetrahydrofuran-S-carboxylic acid amides of general formula (I) in high optical purity, and to the tautomers, enantiomers, diastereomers, mixtures and salts of substituted 3-amino- tetrahydrofuran-3-carboxylic acid amides of general formula (I) in high optical purity, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
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Page/Page column 96; 97-98
(2008/12/07)
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- DNA-directed alkylating agents. 2. Synthesis and biological activity of platinum complexes linked to 9-anilinoacridine
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Two different classes of cis-diaminedichloroplatinum(II) complexes linked to the DNA-intercalating chromophore 9-anilinoacridine have been synthesized and evaluated as DNA-targeted antitumor agents. Two different Pt chelating ligands were investigated (based on 1,2-ethanediamine and 1,3-propanediamine), designed to deliver the Pt in an orientation likely to respectively enhance either intrastrand or interstrand cross-linking. Although both sets of ligands were somewhat unstable under neutral or basic conditions with respect to disproportionation, the corresponding Pt complexes, once prepared, appeared to be quite stable. All the Pt complexes were monitored for purity by TLC, HPLC, and FAB mass spectra, and the mode of Pt coordination was established by 195Pt NMR spectroscopy. The complexes appeared to cause simultaneous platination and intercalative unwinding of plasmid DNA. In vitro studies were carried out with both wild-type and cisplatin-resistant P388 cell lines. Whereas cisplatin itself and the ethylenediamine and 1,3-propanediamine complexes used as standards were about 10-fold less active against the resistant line, the ethylenediamine-linked Pt complexes showed no differential toxicity between the two lines and the propanediamine-linked complexes showed significant differentials (up to 8-fold) in favor of the cisplatin-resistant line. However, these were no greater than those shown by the unplatinated ligands themselves. The majority of the acridine complexes were inactive in vivo against the wild-type P388 leukemia. They were very insoluble, and although a suitable formulation was found, this may have been a factor. It is also possible that these compounds bind in such a way as to direct the Pt away from the major groove.
- Palmer,Lee,Johnson,Baguley,Wickham,Wakelin,McFadyen,Denny
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p. 3008 - 3014
(2007/10/02)
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