- 3,3-DISUBSTITUTED-1-HYDROXYTRIAZ-1-ENE 2-OXIDES AND WOUND-HEALING COMPOSITIONS USING THEM
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Esters, carbonates and imides of 3,3-disubstituted-1-hydroxytriaz-1-ene 2-oxides of the formula I are disclosed. The compounds release nitric oxide (NO) under physiologic conditions, and pharmaceutical compositions containing them are useful to aid in wound healing.
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Paragraph 0045
(2015/08/03)
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- NO-RELEASING NONOATE(OXYGEN-BOUND)CHROMENE CONJUGATES
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The present invention provides NO-releasing NONOate(oxygen bound)chromene conjugates, having the structure of Formula (I): wherein Z, R1, R2, R3, R4, R5, R6, and R7 are as defined in the detailed description; pharmaceutical compositions comprising at least one compound of Formula (I); and methods useful for healing wounds, preventing and treating cancer, or treating actinic keratosis, cystic fibrosis, or acne, using a compound of Formula (I).
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Paragraph 0264
(2015/08/03)
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- 2,3-DIHYDROIMIDAZOL[1,2-C]PYRIMIDIN-5(1H)-ONE BASED LIPOPROTEIN-ASSOCIATED PHOSPHOLIPASE A2 (LP-PLA2) INHIBITORS
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The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
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Page/Page column 32
(2014/08/07)
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- COMPOUNDS
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The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
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Paragraph 0206; 0207; 0208
(2014/08/07)
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- Synthesis of pacidamycin analogues via an Ugi-multicomponent reaction
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The second-generation synthesis of 3′-hydroxypacidamycin D (2) has been accomplished via an Ugi-four component reaction at a late stage of the synthesis. This approach provided ready access to a range of analogues including diastereomers of the diaminobut
- Okamoto, Kazuya,Sakagami, Masahiro,Feng, Fei,Takahashi, Fumiyo,Uotani, Kouichi,Togame, Hiroko,Takemoto, Hiroshi,Ichikawa, Satoshi,Matsuda, Akira
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scheme or table
p. 4810 - 4815
(2012/08/13)
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- Catalytic Hydrogenation of Chiral α-Amino and α-Hydroxy Esters at Room Temperature with Nishimura Catalyst without Racemization
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The hydrogenation of carboxylic acid derivatives at room temperature was investigated. With a mixed Rh/Pt oxide (Nishimura catalyst), low to medium activity was observed for various α-amino and α-hydroxy esters. At 100 bar hydrogen pressure and 10% catalysts loading, high yields of the desired amino alcohols and diols were obtained without racemization. The most suitable α-substituents were NH2, NHR, and OH, whereas β-NH2 were less effective. Usually, aromatic rings were also hydrogenated, but with the free bases of amino acids as substrates, some selectivity was observed. No reaction was found for α-NR2, α-OR, and unfunctionalized esters; acids and amides were also not reduced under these conditions. A working hypothesis for the mode of action of the catalyst is presented.
- Studer, Martin,Burkhardt, Stefan,Blaser, Hans-Ulrich
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p. 802 - 808
(2007/10/03)
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- Enantioselective reduction of aromatic ketones catalysed by chiral ruthenium(II) complexes
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The catalytic enantioselective reduction of aromatic ketones in 2- propanol is carried out by using ruthenium(II) complexes prepared from [Ru(p- cymene)Cl2]2 and a variety of chiral diamines and β-aminoalcohols derived from α-amino acids. Good conversions (>99%) and enantioselectivities (=96%) are observed under mild reaction conditions. (C) 2000 Elsevier Science Ltd.
- Aitali,Allaoud,Karim,Meliet,Mortreux
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p. 1367 - 1374
(2007/10/03)
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- α-Amino Acids as Chiral Educts for Stereoselective Syntheses of Pyrrolidine and Pyrrolizidine Systems
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Homochiral functionalized pyrrolidine and pyrrolizidine systems have been achieved by stereoselective intramolecular 1,3-dipolar cycloaddition of homochiral nitrones, starting from homochiral amino acids, and by subsequent reduction of the obtained cycloadducts.
- Chiacchio, Ugo,Casuscelli, Franco,Corsaro, Antonio,Librando, Vito,Rescifina, Antonio,et al.
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p. 5689 - 5700
(2007/10/02)
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- SYNTHESE D'AMINOPHOSPHINEPHOSPHINITES CHIRAUX. UTILISATION EN REDUCTION ASYMETRIQUE CATALYTIQUE
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The chiral aminophosphinephosphinites ligands (AMPP) are directly synthesized from natural amino alcohols or by reduction of formyl esters of α-amino acids and PPh2Cl. Their cationic rhodium complexes have been found to be excellent catalysts for enantioselective hydrogenation of dehydroamino acids (ee ca. 86percent, yield ca. 100percent) for example.Asymmetric reduction of ketones can also be performed with the new alkyl AMPP* modified rhodium catalyst (ee 50percent).
- Karim, A.,Mortreux, A.,Petit, F.,Buono, G.,Pfeiffer, G.,Siv, C.
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- Chiroptical properties of 2-alkylaziridines and their N-methyl derivatives
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Some optically active 2-alkylaziridines and their N-methyl derivatives have been prepared from the corresponding L-amino acids.Both the ORD and the CD spectra of the aziridines have been determined.From these spectra it is concluded that a cis orientation of the lone pair of the nitrogen, relative to the 2-alkyl substituent, can be correlated with a negative Cotton effect in the 200 nm region.
- Maat, L.,Wulkan, R. W.
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p. 204 - 207
(2007/10/02)
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