- A novel hydrosoluble near-infrared fluorescent probe for specifically monitoring tyrosinase and application in a mouse model
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A novel hydrosoluble near-infrared (NIR) fluorescent probe that could specifically identify tyrosinase has been successfully constructed and applied for imaging of tyrosinase in living cells and zebrafish. Notably, the probe has been successfully applied to the diagnosis of melanoma in a xenogeneic mouse model.
- Zhang, Jiahang,Li, Zhao,Tian, Xinwei,Ding, Ning
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Read Online
- Highly selective two-photon fluorescent off-on probes for imaging tyrosinase activity in living cells and tissues
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A coumarin-based two-photon (TP) fluorescent off-on probe has been developed for detecting tyrosinase activity. High selectivity, sensitivity and biocompatibility enable the probes to successfully image tyrosinase activity in live cells and tissues using TP microscopy.
- Cui, Yixin,Kim, Hwan Myung,Park, Sang Jun,Qi, Sujie,Wang, Rui,Wu, Xiaofeng,Yoon, Juyoung
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supporting information
p. 6911 - 6914
(2021/07/25)
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- FUNGICIDAL HALOMETHYL KETONES AND HYDRATES AND THEIR MIXTURES
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Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1, including all geometric and stereoisomers, tautomers, A-oxides, and salts thereof, wherein E, L, J, A and T are as defined in the disclosure; and (b) at least one additional fungicidal compound. Also disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of a compound of Formula 1, an A-oxide, or salt thereof (e.g., as a component in the aforesaid composition). Also disclosed is a composition comprising: (a) at least one compound selected from the compounds of Formula 1 described above, A- oxides, and salts thereof; and at least one invertebrate pest control compound or agent.
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Page/Page column 115
(2021/09/17)
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- FUNGICIDAL HALOMETHYL KETONES AND HYDRATES
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Disclosed are compounds of Formulae 1 and 10 including all geometric and stereoisomers, tautomers, N oxides, and salts thereof, wherein E, L, J, A, T, R1, R2a, R2b, X, Y, R6a, R6b and R29 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
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Page/Page column 90-91
(2020/05/07)
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- METHOD TO PREPARE PHENOLICS FROM BIOMASS
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The present invention is directed to a method for preparing a final phenolic product from biomass comprising the steps of providing a furanic compound obtainable from biomass; reacting the furanic compound with a dienophile to obtain a phenolic compound; reacting the phenolic compound further to obtain the final phenolic product.
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Page/Page column 47; 48
(2016/08/10)
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- Monooxygenation of an appended phenol in a model system of tyrosinase: Implications on the enzymatic reaction mechanism
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A new tridentate N-donor ligand and its corresponding copper(i) complex have been synthesized to investigate the tyrosinase-like aromatic hydroxylation of an attached phenol. The results of the oxygenation reactions are compared to related systems having attached phenyl and catechol groups, respectively. The title complex is the first system mediating the monooxygenation of a phenol in the absence of an external base. This journal is
- Hamann, Jessica Nadine,Rolff, Malte,Tuczek, Felix
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p. 3251 - 3258
(2015/03/05)
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- HETEROCYCLIC MODULATORS OF HIF ACTIVITY FOR TREATMENT OF DISEASE
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The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.
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Paragraph 0327; 0328
(2014/03/25)
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- HETEROCYCLIC MODULATORS OF HIF ACTIVITY FOR TREATMENT OF DISEASE
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The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.
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Paragraph 0334
(2014/03/25)
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- The coordination chemistry of pentafluorophenylphosphino pincer ligands to platinum and palladium
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The synthesis of electron-poor PCP pincer ligands 1,3-((C6F 5)2PO)2C6H4, 1,3-((C 6F5)2PCH2)2C 6H4, and 1-((C6F5) 2PO)-3-(tBu2PCH2)C6H4, and their coordination chemistry to platinum and palladium is described. The most electron-poor ligand 1,3-((C6F5)2PO) 2C6H4 (POCOPH) reacts with Group10 metal chloride precursors to form a range of unusual cis, trans-dimers of the type κ2-P,P-[(POCOPH)MCl(L)]2 (M=Pt, Pd; L=Cl, Me), which undergo metallation to form [(POCOP)MCl] pincer complexes only under prolonged thermolysis. The formation of such cis,trans-dimers during pincer complex formation can be mitigated through the use of starting materials with more strongly binding ancillary ligands, improving the overall rate of ligand metallation. Carbonyl complexes of the type [(PCP)M(CO)]+ were synthesised from the pincer chloride complexes by halide abstraction, and displayed large ν(C-O) values, from 2170-2111cm-1, confirming the electron-poor nature of the compounds. The [(PCP)Pd(CO)]+ complexes also demonstrated the ability to reversibly bind carbon monoxide both in solution and the solid state, with the rate of decarbonylation increasing with increasing wavenumber for the C-O stretch. Back and forth: The electron-poor P(C6F5)2 donor group was incorporated into the PCP pincer ligand motif to generate a range of poorly donating ligands. Palladium carbonyl complexes of these ligands demonstrated the ability to reversibly bind CO, with the ease of CO displacement increasing with increasing ν(CO) values (see figure). These ligands also displayed a reluctance to undergo metallation on Pt or Pd, which led to the formation of rare examples of cis,trans-dimers.
- Anderson, Bradley G.,Spencer, John L.
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p. 6421 - 6432
(2014/06/09)
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- Synthesis and structure-activity relationship studies of conformationally flexible tetrahydroisoquinolinyl triazole carboxamide and triazole substituted benzamide analogues as σ2 receptor ligands
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Two novel classes of compounds targeting the sigma-2 (σ2) receptor were synthesized, and their bioactivities to binding σ1 and σ2 receptors were measured. Four novel triazole carboxamide analogues, 24d, 24e, 24f, and 39c, demonstrated high affinity and selectivity for the σ2 receptor. These data suggest 11C-labeled versions of these compounds may be potential σ2-selective radiotracers for imaging the proliferative status of solid tumors.
- Bai, Suping,Li, Shihong,Xu, Jinbin,Peng, Xin,Sai, Kiran,Chu, Wenhua,Tu, Zhude,Zeng, Chenbo,Mach, Robert H.
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supporting information
p. 4239 - 4251
(2014/06/09)
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- NITROXY DERIVATIVES OF SOFT STEROIDS
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A compound of formula (I) or a pharmaceutically acceptable salt thereof, and an ophthalmic composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof. The invention is also directed to the use of the ophthalmic compositions for treating inflammatory conditions of the palpebral or bulbar conjunctiva, cornea and anterior segment of the globe, and to ameliorate inflammation associated with corneal injury.
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Page/Page column 17; 18
(2013/09/26)
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- N-ARYLYLMETHYLINDAZOLE MODULATORS OF PPARG
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The invention provides molecular entities that bind with high affinity to PPARG (PPARy), inhibit cdJk5-mediated phosphorylation of PP ARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes or obesity. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.
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Page/Page column 109; 110
(2013/06/06)
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- NITRIC OXIDE DONOR NEPRILYSIN INHIBITORS
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In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R7, R8, Z, X, b, and c are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are nitric oxide donors and have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
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Paragraph 0384; 0385
(2014/01/07)
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- Rational design of highly active "hybrid" phosphine-phosphinite pincer iridium catalysts for alkane metathesis
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Both the bisphosphine and bisphosphinite pincer complexes ( tBu4PCP)IrH2 and (tBu4POCOP)IrH2 can cocatalyze alkane metathesis in tandem with olefin metathesis catalysts, but the two complexes have different resting states during catalysis, suggesting that different steps are turnover-limiting in each case. This led to the hypothesis that a complex with intermediate properties would be catalytically more active than either of these two species. Accordingly, "hybrid" phosphine-phosphinite pincer ligands (PCOP) and the corresponding iridium complexes were synthesized (3c-e). In tandem with olefin-metathesis catalyst MoF12, (tBu4PCOP)IrH2 displays significantly higher activity for the metathesis of n-hexane than does (tBu4PCP)IrH 2 or (tBu4POCOP)IrH2. (tBu2PCOP iPr2)IrH4 (3d) is even more active (>30-fold more active than (tBu4POCOP)IrH2) and affords nearly 4.6 M alkane products after 8 h at 125 C.
- Nawara-Hultzsch, Agnieszka J.,Hackenberg, Jason D.,Punji, Benudhar,Supplee, Carolyn,Emge, Thomas J.,Bailey, Brad C.,Schrock, Richard R.,Brookhart, Maurice,Goldman, Alan S.
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p. 2505 - 2514
(2013/11/19)
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- AGONISTS OF GPR40
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The present invention relates to compounds that have the ability to modulate the activity of GPR40 and are there-fore useful in the treatment of GPR40 related disorders. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders related to GPR40 activity.
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Page/Page column 70; 71-72
(2012/02/05)
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- Benzylic ligand hydroxylation starting from a dicopper μ- I·2:I·2 peroxo intermediate: Dramatic acceleration of the reaction by hydrogen-atom donors
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Radicals in directed pathways: The μ-I·2: I·2 peroxo CuII2 intermediate 1 shows a much faster benzylic ligand hydroxylation than systems without phenol. This novel reactivity can be further accelerated by addition of external H-atom donors such as TEMPO-H. The results imply initial H-atom transfer leading to the formation of phenoxyl radicals. A highly reactive copper oxyl intermediate is then formed, which inserts oxygen into the benzylic C-H bond. Copyright
- Rolff, Malte,Hamann, Jessica Nadine,Tuczek, Felix
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supporting information; experimental part
p. 6924 - 6927
(2011/08/06)
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- PHENOL DERIVATIVES
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The present invention relates to the use of a compound of the general formula (I): wherein: n is an integer from 1 to 20; R is H, an halogen atom, a linear or branched (C1-C10)- alkoxy group, an hydroxy group, -CF3, -NHR' wherein R' is H or a linear or branched (C1-C10)-alkyl; or a salt thereof for treating inflammatory disease states or disorders, cardiovascular and/or peripheral vascular diseases.
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Page/Page column 7
(2008/06/13)
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- 4-PHENYL-5-OXO-1,4,5,6,7,8-HEXAHYDROQUINOLINE DERIVATIVES THE TREATMENT OF INFERTILITY
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The present invention relates to 4-phenyl-5-oxo-l,4)5,6,7,8-hexahydroquinoline derivatives according to Formula I, Formula I or a pharmaceutically acceptable salt thereof, wherein R1 is (l-6C)alkyl, (2-6C)alkenyl or (2-6C)aDcynyl; R2, R3 are independently halogen, (l-4C)allcyl, (2-4C)alkenyl, (2-4C)- alkynyl, (1 -4C)aBcoxy, (3-4C)alkenyloxy or (3-4C)alkynyloxy; R4 is phenyl or (2-5C)- heteroaryl, both substituted with R7 and optionally substituted on the (hetero)aromatic ring with one or more substituents selected from hydroxy, amino, halogen, nitro, trifluoromethyl, cyano, (l-4C)alkyl, (l-4C)alkoxy , (l-4C)alkylthio and (di)(l-4C)- alkylamino. The invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these 4-phenyl-5-oxo-l, 4,5,6, 7,8-hexahydro- quinoline derivatives in therapy, more specifically for the treatment of infertility
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Page/Page column 40
(2010/11/24)
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- PROSTAGLANDIN NITROOXYDERIVATIVES
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Prostaglandin nitrooxyderivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.
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Page/Page column 39-40
(2008/06/13)
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- NITRIC OXIDE RELEASING PRODRUGS OF DIARYL-2-(5H)-FURANONES AS CYCLOOXYGENASE-2 INHIBITORS
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The invention encompasses novel compounds of Formula I, which are nitric oxide-releasing prodrugs of diaryl-2-(5H) furanones useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions and methods for treatment of cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula I. The above compounds may be used as a combination therapy with low-dose aspirin to treat chronic cyclooxygenase-2 mediated diseases or conditions while simultaneously reducing the risk of thrombotic cardiovascular events.
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- INDOLES HAVING ANTI-DIABETIC ACTIVITY
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Indoles having aryloxyalkanoic acid substituents or arylalkanoic acid substituents are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
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- Novel unsymmetrical PCP′ pincer ligands and their palladium(II) complexes
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Synthetic routes towards novel PCP′ pincer ligands were devised. Ligand 1-(Pr2iPOCH2) -3-(Bu2tPCH2) (C6H4) is prepared in a three step synthesis from 1,3-benzenedimethanol and 1-(Pr2iPO)-3- (Bu2tPCH2)(C6H4) is accessible in three steps from 3-hydroxybenzylalcohol. Both their palladium(II) complexes are prepared in good yields but are distinctly different since [PdCl{(C6H3) (OPPr2i)-2-(CH2PBu2 t)-6}] possesses two five-membered palladacycles, whereas [PdCl{(C6H3)(CH2PBu2 t)-2-(CH2OPPr2i)-6}] is unusual for a pincer complex in that it contains both five- and six-membered palladacycles. Both compounds also represent the first examples of pincer complexes where one donor is a phosphinite and the other is a phosphine. The X-ray structures of these complexes were solved and are discussed. The data reveal that an increase in the metallacycle ring-size leads to changes in bond lengths, but more importantly to significant increases in the bond angles.
- Eberhard, Michael R.,Matsukawa, Shiro,Yamamoto, Yohsuke,Jensen, Craig M.
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p. 185 - 189
(2007/10/03)
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- Helical and Planar-chiral Pyridinophanes - A New Synthesis and Structure/Chiroptic Relationships
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A new two-step synthesis for the strained helical oxaphanes 1-5 and for a systematic series of novel structural isomeric (2,4)-pyridinophanes (6-10) is presented.The energy barriers for ring inversion of some intermediate phanes and the kinetics of racemization of the phanes are determined.Separation and enrichment of enantiomers is achieved by HPLC on cellulose tris(3,5-dimethylphenyl)carbamate and poly(triphenylmethyl-methacrylate), resp.The circular dichroism curves of the isomers are compared with those of the corresponding protonated pyridinium compounds.The influence of the chromophor orientation on the circular dichroism is discussed. - Keywords: Circular dichroism/ Helical molecules/ Metacyclophanes/ Oxametacyclophane/ Pyridinophanes
- Przybilla, Klaus Juergen,Voegtle, Fritz
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p. 347 - 356
(2007/10/02)
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- Reduction of carbonyl compounds promoted by silicon hydrides under the influence of trimethylsilyl-based reagents
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The synthetic utility of hydrosilanes under the influence of trimethylsilyl-based reagents as new reducing systems is described. 1,1,3,3-Tetramethyldisiloxane (TMDS) reagent in combination with iodotrimethylsilane or bromotrimethylsilane produces alkyl halides from aldehydes in good to excellent yields.Polymethylhydrosiloxane (PMS) in the presence of iodotrimethylsilane also produces benzyl iodides in excellent yields.On the contrary, PMS reagent was found unsuitable for the synthesis of benzyl bromides.Similary, TMDS reagent in combination with trimethylsilyl triflate produces symmetrical ethers from aldehydes without concomitant formation of competitive products.Under similar conditions, PMS reagent failed to provide the expected symmetrical ethers and Friedel-Crafts products were formed.Reduction of quinones to hydroquinones is also described.
- Aizpurua, Jesus M.,Lecea, Begona,Palomo, Claudio
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p. 2342 - 2347
(2007/10/02)
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