72486-09-0

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• Synthesis and evaluation of Re/99mTc(I) complexes bearing a somatostatin receptor-targeting antagonist and labeled via a novel [N,S,O] clickable bifunctional chelating agent
• The somatostatin receptor subtype 2 (SSTR2) is often highly expressed on neuroendocrine tumors (NETs), making it a popular in vivo target for diagnostic and therapeutic approaches aimed toward management of NETs. In this work, an antagonist peptide (ssts
• Radford, Lauren L.,Papagiannopoulou, Dionysia,Gallazzi, Fabio,Berendzen, Ashley,Watkinson, Lisa,Carmack, Terry,Lewis, Michael R.,Jurisson, Silvia S.,Hennkens, Heather M.

• p. 492 - 501

  (2019)
• Read Online

• Silver-Catalyzed Cascade Cyclization/1,6-Conjugate Addition of Homopropargyl Sulfonamides to p-Quinone Methides: An Approach to Diverse 3-Diarylmethine Substituted Dihydropyrroles
• A silver-catalyzed cycloisomerization/1,6-conjugate addition of homopropargyl sulfonamides to p-quinone methides to access diverse diarylmethine substituted dihydropyrroles has been disclosed. The reaction pathway involves an intramolecular cascade cyclization of homopropargyl sulfonamides to generate a highly reactive dihydropyrrole intermediate in situ followed by conjugate addition with p-quinone methides. This method provides an efficient and scalable route for the synthesis of 3-diarylmethine substituted dihydropyrroles, in one pot.
• Shirsath, Sachin R.,Ghotekar, Ganesh S.,Bahadur, Vir,Gonnade, Rajesh G.,Muthukrishnan

• p. 15038 - 15050

  (2020)
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• Double Radical Cyclization/β-Fragmentation of Acyclic ω-Yne Vinyl Sulfides. Synthesis of 3-Vinyldihydrothiophene and Dihydrothiopyran Derivatives. A New Example of a 5-endo-trig Radical Cyclization
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• Journet, Michel,Rouillard, Alain,Cai, Dongwei,Larsen, Robert D.

• p. 8630 - 8631

  (1997)
• Read Online

• New polyelectrolytes based on 4-vinyl-1,2,3-triazole and 1-vinylimidazole
• Copolymers of 4-vinyl-1,2,3-triazole and 1-vinylimidazole (VI) were obtained by radical copolymerization of (4-vinyl-1H-1,2,3-triazol-1-yl)methyl pivalate with VI followed by alkali hydrolysis. Reactivity ratios of the triazole and imidazole monomers are 0.51 and 0.30, respectively. Theoretical quantum-chemical calculations by the PM3 semiempirical method give close values, which show that the obtained reactivity ratios reflect the activity of the vinyl groups. Polyelectrolyte properties of the copolymers were studied by potentiometric titration. Hydrogen bonds between the protonated triazole cycle and the triazole or imidazole units were found to considerably influence the solubility and solution properties of the copolymers.
• Danilovtseva, Elena N.,Chafeev, Mikhail A.,Annenkov, Vadim V.

• p. 1539 - 1546

  (2012)
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• A versatile new monomer family: Functionalized 4-vinyl-1,2,3-triazoles via click chemistry
• Using facile, highly modular synthetic approaches, a new monomer family based on a 1,2,3-triazole-4-vinyl building block has been prepared, and various functional derivatives have been obtained. Subsequent homo- and copolymerization of these novel functionalized monomers gives polymeric materials with unique physical properties, combining many attractive features of more traditional monomers, such as styrene, vinylpyridine, and meth/acrylates. Copyright
• Thibault, Raymond J.,Takizawa, Kenichi,Lowenheilm, Peter,Helms, Brett,Mynar, Justin L.,Frechet, Jean M. J.,Hawker, Craig J.

• p. 12084 - 12085

  (2006)
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• RET Inhibitor. Pharmaceutical composition and use thereof
• The invention belongs to the field of medicines, and relates to a novel RET inhibitor, a pharmaceutical composition and application thereof. , The present invention relates to a compound represented by formula (I), a stereoisomer, a geometric isomer, a tautomer, an oxynitride, a solvate, a metabolite, a pharmaceutically acceptable salt or prodrug thereof, I, and a pharmaceutical composition thereof in the manufacture of a medicament, in particular for the treatment and prevention and RET of diseases and disorders associated with irritable bowel syndrome.
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• Paragraph 0415-0418

  (2021/11/26)
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• Discovery of a novel family of FKBP12 “reshapers” and their use as calcium modulators in skeletal muscle under nitro-oxidative stress
• The hypothesis of rescuing FKBP12/RyR1 interaction and intracellular calcium homeostasis through molecular “reshaping” of FKBP12 was investigated. To this end, novel 4-arylthioalkyl-1-carboxyalkyl-1,2,3-triazoles were designed and synthesized, and their e
• Aizpurua, Jesus M.,Miranda, José I.,Irastorza, Aitziber,Torres, Endika,Eceiza, Maite,Sagartzazu-Aizpurua, Maialen,Ferrón, Pablo,Aldanondo, Garazi,Lasa-Fernández, Haizpea,Marco-Moreno, Pablo,Dadie, Naroa,López de Munain, Adolfo,Vallejo-Illarramendi, Ainara

• (2021/01/25)
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• Switchable Divergent Synthesis in Gold-Catalyzed Difunctionalizations of o-Alkynylbenzenesulfonamides with Aryldiazonium Salts
• Gold-catalyzed difunctionalizations of o-alkynylbenzenesulfonamides with aryldiazonium salts are reported herein. Upon irradiation with the blue LEDs, benzosultam products were formed via aminoarylation accompanied by the release of N2. Without irradiatio
• Li, Jun,Shi, Hongwei,Zhang, Shan,Rudolph, Matthias,Rominger, Frank,Hashmi, A. Stephen K.
• supporting information

  p. 7713 - 7717

  (2021/10/20)
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• Synthesis of Exo- and Endocyclic Enamides Through Copper-Catalyzed Regioselective Intramolecular N-Halovinylation
• Cross-couplings between amides and 1,2-dihaloalkenes are an efficient and straightforward way to access β-haloenamides which, in turn, can be functionalized into complex, stereodefined enamide motifs. However, the intramolecular version of these cross-couplings, leading to cyclic β-haloenamides, has not been formally studied. In this paper, we report an investigation of factors affecting the efficiency of the reaction and its selectivity between potential exo and endo cyclization products. We demonstrate that exo/endo selectivity is largely determined by ring strain, whether it arises from the size of the resulting ring or from the structure of the starting compound, but that selectivity can also be modulated by varying reaction conditions. Finally, we show that resulting β-haloenamides readily undergo transition metal-catalyzed reactions, making this sequence a viable way to access highly functionalized cyclic enamides.
• Bergeron, Jodrey,Daoust, Benoit,Gilbert, Nicolas,Lambolez, Pierre,Ricard, Simon
• supporting information

  (2020/05/04)
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• ?-LACTAMASE INHIBITOR AND USE THEREOF
• Provided are a β-lactamase inhibitor of formula (I), or an ester, a stereoisomer or a pharmaceutically acceptable salt thereof, and a method of preparing the same. Further provided is a pharmaceutical composition comprising the β-lactamase inhibitor of formula (I), or the ester, the stereoisomer or pharmaceutically acceptable salt thereof. In addition, the present invention relates to a method for treating diseases caused by bacterial infection, which comprises administering the β-lactamase inhibitor of formula (I), or the ester, the stereoisomer or the pharmaceutically acceptable salt thereof to a patient or a subject in need.
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• Paragraph 0222; 0223

  (2020/12/10)
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• Aldehyde-mediated bioconjugation: Via in situ generated ylides
• A technically simple approach for rapid, high-yielding and site-selective bioconjugation has been developed for both in vitro and cellular applications. This method involves the generation of maleimido-phosphonium ylides via 4-nitrophenol catalysis under physiological conditions followed by their Wittig reactions with aldehyde-appended biomolecules.
• Parmar, Sangeeta,Pawar, Sharad P.,Iyer, Ramkumar,Kalia, Dimpy
• supporting information

  p. 14926 - 14929

  (2019/12/24)
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• IRAK DEGRADERS AND USES THEREOF
• The present invention provides compounds, compositions thereof, and methods of using the same.
• -
• Paragraph 3756; 3757

  (2019/07/10)
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• BIS-BENZIMIDAZOLE COMPOUNDS AND METHODS OF USING SAME
• Provided herein are compounds and methods for modulating abnormal repeat expansions of gene sequences. More particularly, provided are inhibitors of RNA and the uses of such inhibitors in regulating nucleotide repeat expansions, e.g., to treat Myotonic Dystrophy Type 1 (DM1 ), Myotonic Dystrophy Type 2 (DM2), Fuchs dystrophy, Huntington Disease, Amyotrophic Lateral Sclerosis, or Frontotemporal Dementia.
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• Paragraph 00767-00769

  (2019/06/05)
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• Multifunctional 1,3-diphenylguanidine for the carboxylative cyclization of homopropargyl amines with CO2 under ambient temperature and pressure
• Herein, we report that 1,3-diphenylguanidine (DPG) could be utilized for the carboxylative cyclization of homopropargyl amines with CO2 under ambient temperature and pressure, in combination with AgSbF6, which enabled the synthesis o
• Gao, Xiao-Tong,Xie, Shi-Liang,Zhou, Feng,Wu, Hai-Hong,Zhou, Jian
• supporting information

  p. 14303 - 14306

  (2019/12/03)
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• Multiheterocyclic Motifs via Three-Component Reactions of Benzynes, Cyclic Amines, and Protic Nucleophiles
• A broadly general, three-component reaction strategy for the construction of compounds containing multiple heterocycles is described. Thermal benzyne formation (by the hexadehydro-Diels-Alder (HDDA) reaction) in the presence of tertiary cyclic amines and a protic nucleophile (HNu) gives, via ring-opening of intermediate ammonium ion/Nu- ion pairs, heterocyclic products. Many reactions are efficient even when the stoichiometric loading of the three reactants approaches unity. Use of HOSO2CF3 as the HNu gives ammonium triflate intermediates, which can then be ring opened by an even wider variety of nucleophiles.
• Ross, Sean P.,Hoye, Thomas R.
• supporting information

  p. 100 - 103

  (2018/01/17)
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• DISUBTITUTED AZETIDINES, PYRROLIDINES, PIPERIDINES AND AZEPANES AS INHIBITORS OF MONOAMINE OXIDASE B FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
• This invention relates to new inhibitors of MAO-Bwith the general formula I, where substituents are described in patent description. Compounds can be in the form of pure enantiomers or as racemic mixtures, or in the form of pharmaceutically acceptable salts. The present invention relates to the use of these inhibitors for the alleviation of symptoms and treatment of acute and chronic neurological disorders, cognitive and neurodegenerative diseases.
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• Page/Page column 19; 80; 81; 82

  (2018/04/20)
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• Controlling Proton and Electron Transfer Rates to Enhance the Activity of an Oxygen Reduction Electrocatalyst
• An electrochemical approach is developed that allows for the control of both proton and electron transfer rates in the O2 reduction reaction (ORR). A dinuclear Cu ORR catalyst was prepared that can be covalently attached to thiol-based self-assembled monolayers (SAMs) on Au electrodes using azide–alkyne click chemistry. Using this architecture, the electron transfer rate to the catalyst is modulated by changing the length of the SAM, and the proton transfer rate to the catalyst is controlled with an appended lipid membrane modified with proton carriers. By tuning the relative rates of proton and electron transfer, the current density of the lipid-covered catalyst is enhanced without altering its core molecular structure. This electrochemical platform will help identify optimal thermodynamic and kinetic parameters for ORR catalysts and catalysts of other reactions that involve the transfer of both protons and electrons.
• Gautam, Rajendra P.,Lee, Yi Teng,Herman, Gabriel L.,Moreno, Cynthia M.,Tse, Edmund C. M.,Barile, Christopher J.

• p. 13480 - 13483

  (2018/09/25)
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• Identification of the Ferric-Acinetobactin Outer Membrane Receptor in Aeromonas salmonicida subsp. salmonicida and Structure-Activity Relationships of Synthetic Acinetobactin Analogues
• Aeromonas salmonicida subsp. salmonicida, the causative agent of furunculosis in several fish species, produces acinetobactin and amonabactin as siderophores. In a previous study, we chemically characterized these siderophores and proposed a biosynthetic
• Balado, Miguel,Segade, Yuri,Rey, Diego,Osorio, Carlos R.,Rodríguez, Jaime,Lemos, Manuel L.,Jiménez, Carlos

• p. 479 - 493

  (2017/03/01)
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• Structure and Mechanism Revision of a Catalyzed Cyclization of Benzaldehyde Bearing Alkyne-Nitrile
• Pt(II)-catalyzed carbocyclization of benzaldehyde containing a keto-nitrile functionality resulted in the formation, respectively, of isochromenes and spiro-lactones instead of fused lactams and spiro-lactams as was previously reported. The reaction mecha
• ?afá?, Peter,Marchalín, ?tefan,?oral, Michal,Moncol, Ján,Da?ch, Adam
• supporting information

  p. 4742 - 4745

  (2017/09/25)
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• Compound and application of compound to treating colon cancer
• The invention discloses a compound and application of the compound to treating the colon cancer. The structural formula of the compound is shown in the formula I, wherein R1, R2, R3 and R4 in the formula I are respectively independently chosen from alkyl groups and alkoxy groups, the number of hydrogen atoms, halogen, nitro and carbon atoms in the alkyl group is 1-6, the number of carbon atoms in the alkoxy group is 1-6, R5 is chosen from nitro and -NR6R7, wherein R6 and R7 are respectively independently the hydrogen atom or CH2Ar, the Ar represents a phenyl group or an aryl group, the para-position of the aryl group is substituted by R8, the aryl group is a phenyl group, the R8 is an alkoxy group or the following shown groups, and the number of halogen, hydroxyl and carbon atoms in the R8 is 1-6. The compound also has an obvious effect on inhibiting a tumor sphere from a cancer patient with the colon cancer. In addition, the compound also has an obvious effect on inhibiting the migration and the moving ability of a colon cancer cell line. A novel medicine for treating the colon cancer is expected to be developed on the basis of the compound.
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• Paragraph 0159-0161

  (2017/11/04)
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• Iodocarbamation of N-Homopropargyl Carbamates: Mild and Stereoselective Entry to Functionalized Oxazinan-2-ones
• An efficient and general iodocarbamation of benzyl N-homopropargylcarbamates has been developed by using iodine as the electrophilic agent. This regio- and stereoselective cyclization yielded (E)-6-iodomethyleneoxazinan-2-ones, which can be further transformed through palladium cross-coupling reactions followed by hydrogenation to produce 1,3-oxazinan-2-ones.
• Quinodoz, Pierre,Quelhas, Alexandre,Wright, Karen,Drouillat, Bruno,Marrot, Jér?me,Couty, Fran?ois
• supporting information

  p. 2621 - 2626

  (2017/05/19)
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• Routes of Synthesis of Carbapenems for Optimizing Both the Inactivation of l, d -Transpeptidase LdtMt1 of Mycobacterium tuberculosis and the Stability toward Hydrolysis by β-Lactamase BlaC
• Combinations of β-lactams of the carbapenem class, such as meropenem, with clavulanate, a β-lactamase inhibitor, are being evaluated for the treatment of drug-resistant tuberculosis. However, carbapenems approved for human use have never been optimized for inactivation of the unusual β-lactam targets of Mycobacterium tuberculosis or for escaping to hydrolysis by broad-spectrum β-lactamase BlaC. Here, we report three routes of synthesis for modification of the two side chains carried by the β-lactam and the five-membered rings of the carbapenem core. In particular, we show that the azide-alkyne Huisgen cycloaddition reaction catalyzed by copper(I) is fully compatible with the highly unstable β-lactam ring of carbapenems and that the triazole ring generated by this reaction is well tolerated for inactivation of the l,d-transpeptidase LdtMt1 target. Several of our new carbapenems are superior to meropenem both with respect to the efficiency of in vitro inactivation of LdtMt1 and reduced hydrolysis by BlaC.
• Iannazzo, Laura,Soroka, Daria,Triboulet, Sébastien,Fonvielle, Matthieu,Compain, Fabrice,Dubée, Vincent,Mainardi, Jean-Luc,Hugonnet, Jean-Emmanuel,Braud, Emmanuelle,Arthur, Michel,Etheve-Quelquejeu, Mélanie

• p. 3427 - 3438

  (2016/05/19)
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• INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
• The present invention provides compounds of Formula Ia and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
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• Paragraph 0223

  (2016/10/06)
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• Synthesis of Azabicycles via Cascade Aza-Prins Reactions: Accessing the Indolizidine and Quinolizidine Cores
• The first detailed studies of intramolecular aza-Prins and aza-silyl-Prins reactions, starting from acyclic materials, are reported. The methods allow rapid and flexible access toward an array of [6,5] and [6,6] aza-bicycles, which form the core skeletons of various alkaloids. On the basis of our findings on the aza-Prins and aza-silyl-Prins cyclizations, herein we present simple protocols for the intramolecular preparation of the azabicyclic cores of the indolizidines and quinolizidines using a one-pot cascade process of N-acyliminium ion formation followed by aza-Prins cyclization and either elimination or carbocation trapping. It is possible to introduce a range of different substituents into the heterocycles through a judicial choice of Lewis acid and solvent(s), with halo-, phenyl-, and amido-substituted azabicyclic products all being accessed through these highly diastereoselective processes.
• Chio, Freda K. I.,Guesné, Sébastien J. J.,Hassall, Lorraine,McGuire, Thomas,Dobbs, Adrian P.

• p. 9868 - 9880

  (2015/11/03)
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• USE OF EMICORONS AS SELECTIVE INDUCERS OF DAMAGE TO THE TELOMERE DNA
• The hydrosoluble emicoron derivatives of the general formula (I) are particularly effective as inducers of selective telomere and non- telomere DNA damage in tumour and transformed cells. The damage is measured as the ability to cause a number of TIF foci in transformed cells that is equal to or higher than 4 at a 0.1 uM dose of the compound of the formula (I). Such emicoron derivatives can be used in a kit together with other known anti-tumour drugs, such as, for example, topoisomerase I inhibitors, for the combined, simultaneous, delayed or sequential administration. The emicoron compounds of the formula (I) are particularly useful in the therapy of tumours that do not express p53 protein or express an inactive p53 protein and of tumours that maintain telomeres by mechanisms different from telomere maintenance by telomerase, and in the removal of cancer stem cells. Also, the method for the preparation of emicoron compounds of the formula (I), which envisages the use of intermediates such as the Ν,Ν'-bis [2-(1-piperidino)-ethyl] - 1-(1-piperidinyl)-7- [3-(1-piperidino)- butynyl]-perylene-3,4;9,10-tetracarboxyl diimide, is described.
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• Page/Page column 32

  (2014/05/07)
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• Biogenetically inspired total syntheses of lycopodium alkaloids, (+)-flabellidine and (-)-lycodine
• The first asymmetric total synthesis of (+)-flabellidine (2) and the shortest total synthesis of (-)-lycodine (3) were accomplished by a strategy featuring the one-pot construction of a tetracyclic lycodine skeleton from a linear precursor, which was insp
• Azuma, Masayuki,Yoshikawa, Tetsuya,Kogure, Noriyuki,Kitajima, Mariko,Takayama, Hiromitsu
• supporting information

  p. 11618 - 11621

  (2014/11/08)
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• 1,2,3-triazolium ionic liquids
• The present invention relates to compositions of matter that are ionic liquids, the compositions comprising substituted 1,2,3-triazolium cations combined with any anion. Compositions of the invention should be useful in the separation of gases and, perhap
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• Page/Page column 9

  (2014/12/12)
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• ISOXAZOLE β-LACTAMASE INHIBITORS
• β-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D β-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
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• Page/Page column 75; 76

  (2013/10/21)
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• THIAMINE DERIVATIVES AND THEIR USE AS ANTIBIOTICS
• The present invention relates to compounds according to general formula (I), pharmaceutical compositions comprising compounds according to general formula (I) and the use of the compounds for the treatment of a bacterial infection, particularly for use as
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• Page/Page column 28

  (2013/08/28)
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• Thiamine analogues and their use as antibiotics
• The present invention relates to compounds according to general formula (I), pharmaceutical compositions comprising compounds according to general formula (I) and the use of the compounds for the treatment of a bacterial infection, particularly for use as
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• Paragraph 0083

  (2013/08/28)
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• Copper-catalyzed trifluoromethylation-cyclization of enynes: Highly regioselective construction of trifluoromethylated carbocycles and heterocycles
• Regioselective trifluoromethylation-cyclization: A method for copper-catalyzed trifluoromethylation-cyclization of simple enynes using the C-C triple bond as a nucleophile is reported for the first time (see scheme). The reaction proceeds efficiently in a
• Gao, Pin,Yan, Xiao-Biao,Tao, Tao,Yang, Fan,He, Ting,Song, Xian-Rong,Liu, Xue-Yuan,Liang, Yong-Min
• supporting information

  p. 14420 - 14424

  (2013/11/06)
• 

• INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
• The present invention provides compounds of Formula Ia and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
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• Page/Page column 101

  (2013/03/26)
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• ANTICANCER DERIVIATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF
• The invention relates to nicotinamide derivatives which can be used as anticancer drugs.
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• Page/Page column 14

  (2012/04/23)
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• Design and synthesis of novel bis-thiazolone derivatives as micromolar CDC25 phosphatase inhibitors: Effect of dimerisation on phosphatase inhibition
• CDC25 phosphatases are involved in deregulated cell cycle progression and tumor development with poor prognosis. Among the most potent CDC25 inhibitors, quinonoid-based derivatives have been extensively studied. Dimerisation of heterocyclic quinones has led to IRC-083864, a bis-quinone compound with increased CDC25B inhibitory activity. Thirty-one bis-thiazolone derivatives were synthesized and assayed for CDC25 inhibitory activity. Most of the dimers displayed enhanced inhibitory activities with micromolar IC50 values lower than that observed for each thiazolone scaffold separately. Moreover, most of these compounds were selective CDC25 inhibitors. Dimer 40 showed an IC 50 value of 2.9 μM and could inhibit CDC25 activity without generating reactive oxygen species which is likely to occur with quinone-based inhibitors. Molecular docking studies suggested that the dimers could bind simultaneously to the active site and the inhibitor binding pocket.
• Sarkis, Manal,Tran, Diem Ngan,Kolb, Stephanie,Miteva, Maria A.,Villoutreix, Bruno O.,Garbay, Christiane,Braud, Emmanuelle

• p. 7345 - 7350

  (2013/02/23)
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• Total synthesis of RNA-polymerase inhibitor ripostatin B and 15-deoxyripostatin A
• Keep me skipped: A highly convergent total synthesis of ripostatin B, an inhibitor of the bacterial RNA polymerase, is described. The key steps to construct and avoid isomerization of the skipped triene are a double Stille cross-coupling reaction and a ring-closing metathesis. Furthermore, 15-deoxyripostatin A, a stable and conformationally locked analogue of ripostatin A (see scheme, 15-OH group red), was prepared and tested in vivo. Copyright
• Tang, Wufeng,Prusov, Evgeny V.
• supporting information; experimental part

  p. 3401 - 3404

  (2012/06/29)
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• Influence of the acetylenic substituent on the intramolecular carbolithiation of alkynes
• The intramolecular carbolithiation of a series of propargylic ethers has been performed to evaluate the influence of the terminal substituent on the efficiency and the stereochemical outcome of the cyclization. Our results show that only 5-exo-dig cyclizations are observed, and dihydrobenzofurans are obtained exclusively. Depending on the nature of the terminal substituent, two cases can be considered. If the terminal substituent carried by the acetylenic carbon atom is itself a carbon atom, the cyclization can occur provided the terminal propargylic position bears a coordinating element and is at least disubstituted. When the cyclization occurs, it follows an anti-carbolithiation pathway and thus leads to the E isomer of the exocyclic double bond. Only in one case (Ph) was a mixture of the E and Z isomers of the resulting olefin recovered. The cyclization can also take place if the alkyne is directly substituted by S or Si, provided the cyclization conditions are tuned. In the case of the trimethylsilyl substituent, a syn-carbolithiation was observed. If the double bond is recovered, in most cases, in the exocyclic position, the products can aromatize directly for SPh-substituted substrate 24. Furthermore, in the two latter cases, when alkylation of the vinyllithium intermediate is performed, isomerization of the double bond seems instantaneous. Copyright
• Girard, Anne-Lise,Lhermet, Rudy,Fressigne, Catherine,Durandetti, Muriel,Maddaluno, Jacques
• scheme or table

  p. 2895 - 2905

  (2012/06/29)
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• ARACHIDONIC ACID ANALOGS AND METHODS FOR ANALGESIC TREATMENT USING SAME
• The present invention provides arachidonic acid (AA) analogs and compositions containing those analogs as active agents for use in analgesic treatments. Various methods of r manufacturing the inventive compounds are provided and pharmaceutical formulations, including injectable and oral dosages, are described. The analogs are additionally useful as antipyretic compositions and in related fever reducing treatments.
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• Page/Page column 39; 40

  (2011/06/23)
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• Conjugate addition of vinylic organocuprates generated via transmetalation of phenylseleno-substituted vinylzirconates: Functionalization at the 4-position of enones
• Hydrozirconation of propargylic selenides (1) or 4-phenylseleno-1-butyne (2) with Cp2ZrHCl, followed by in situ transmetalation to cuprate (Me2Cu(CN)Li2) and addition of enones, led to the formation of 1,4-adducts in good
• Segi, Masahito,Suzuki, Masahiro,Shintaku, Kazuki,Maeda, Hajime
• experimental part

  p. 545 - 552

  (2012/01/05)
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• Stereospecific synthesis and structure-activity relationships of unsymmetrical 4,4-diphenylbut-3-enyl derivatives of nipecotic acid as GAT-1 inhibitors
• Two complementary stereospecific synthetic approaches for the preparation of unsymmetrical ortho-substituted N-(4,4-diphenylbut-3-enyl) derivatives of nipecotic acid are described. Determination of the activity of the prepared compounds at the GAT-1 trans
• Pizzi, Domenica A.,Leslie, Colin P.,Fabio, Romano Di,Seri, Catia,Bernasconi, Giovanni,Squaglia, Michela,Carnevale, Gennaro,Falchi, Alessandro,Greco, Elisabetta,Mangiarini, Laura,Negri, Michele
• scheme or table

  p. 602 - 605

  (2011/02/27)
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• Regioselective cobalt-catalyzed formation of bicyclic 3- and 4-aminopyridines
• Bimolecular cobalt-catalyzed [2+2+2] cycloadditions between yne-ynamides and nitriles afford bicyclic 3- or 4-aminopyridines in up to 100% yield. The high regioselectivity observed depends on the substitution pattern at the starting ynamide. Aminopyridines bearing TMS and Ts groups are efficiently deprotected in an orthogonal fashion.
• Garcia, Pierre,Evanno, Yannick,George, Pascal,Sevrin, Mireille,Ricci, Gino,Malacria, Max,Auber, C. Torinne,Gandon, Vincent
• supporting information; experimental part

  p. 2030 - 2033

  (2011/06/23)
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• Synthesis of α-CN and α-CF3 N-heterocycles through tandem nucleophilic additions
• Using a readily available secondary aminoalkyne as starting material, a powerful strategy was discovered to prepare precursors of biologically important unnatural cyclic aminoacids and fluorinated N-heterocycles with important ring sizes (e.g., 5-7) in a
• Han, Junbin,Xu, Bo,Hammond, Gerald B.
• supporting information; experimental part

  p. 3450 - 3453

  (2011/08/07)
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• Palladium-catalysed cyclisation of N-alkynyl aminomalonates
• Go around in (hetero)cycles! The palladium-catalysed tandem cyclisation/coupling reaction of alkynyl- and alkenyl-substituted aminomalonates leads to highly functionalised pyrrolidines and piperidines in good yield (see scheme). The reaction allows efficient access to a broad range of synthetically valuable building blocks.
• Hess, Wilfried,Burton, Jonathan W.
• supporting information; experimental part

  p. 12303 - 12306

  (2011/02/23)
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• Synthesis and biological evaluation of a triazole-based library of pyrido[2,3-d]pyrimidines as FGFR3 tyrosine kinase inhibitors
• A library of pyrido[2,3-d]pyrimidines was designed as inhibitors of FGFR3 tyrosine kinase allowing possible interactions with an unexploited region of the ATP binding-site. This library was built-up with an efficient step of click-chemistry giving easy access to triazole-based compounds bearing a large panel of substituents. Among the 27 analogues synthesized, more than half exhibited 55-89% inhibition of in vitro FGFR3 kinase activity at 2 μM and one (19g) was able to inhibit auto-phosphorylation of mutant FGFR3-K650M in transfected HEK cells.
• Le Corre, Laurent,Girard, Anne-Lise,Aubertin, Johannes,Radvanyi, Franois,Benoist-Lasselin, Catherine,Jonquoy, Aurelie,Mugniery, Emilie,Legeai-Mallet, Laurence,Busca, Patricia,Le Merrer, Yves
• scheme or table

  p. 2164 - 2173

  (2010/07/04)
• 

• ANTI-HYPERCHOLESTEROLEMIC COMPOUNDS
• One object of the instant invention is to provide novel cholesterol absorption inhibitors of Formula I or pharmaceutically acceptable salts thereof.
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• Page/Page column 46-47

  (2010/06/15)
• 

• 4 ( 1H) -PYRIDINONE DERIVATIVES AND THEIR USE AS ANTIMALARIA AGENTS
• 4-pyridone (4-pyridinone) derivatives of Formula (I) and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations thereof and their use in chemotherapy of certain parasitic infections such as malaria, are provided.
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• Page/Page column 50

  (2010/08/08)
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• N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS
• The present invention relates to N-(hetero)aryl-pyrrolidine derivatives of Formula I: which are JAK inhibitors, such as selective JAK1 inhibitors, useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
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• Page/Page column 82

  (2010/12/29)
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• A click chemistry mediated in vivo activity probe for dimethylarginine dimethylaminohydrolase
• (Chemical Equation Presented) Asymmetric Nω,N ω-dimethyl-L-arginine (ADMA) is an endogenously produced inhibitor of human nitric oxide synthase and an emerging biomarker for cardiovascular disease. Concentrations of ADMA are controlled by two isoforms of its catabolic enzyme dimethylarginine dimethylaminohydrolase (DDAH), the dysregulation of which has been studied as a mediating factor for endothelial dysfunction. A two-part, click-chemistry mediated activity-based probe, N-but-3-ynyl-2-chloroacetamidine, is shown to label myc-tagged DDAH-1 expressed in HEK 293T cells, but not an inactive mutant or inhibited enzyme. A two-color Western blotting technique is used to determine the in vivo IC50 value for a reversible inhibitor of DDAH-1, N5-(1-iminopropyl)-L- ornithine, indicating this compound's bioavailability and its competition for binding to the active site. This probe provides a novel tool for the analysis of DDAH-1 activity in normal and pathophysiological states and should allow more meaningful studies of the etiology of endothelial dysfunction.
• Yun, Wang,Shougang, Hu,Fast, Walter
• supporting information; experimental part

  p. 15096 - 15097

  (2010/01/16)
• 

• UREA GLUCOKINASE ACTIVATORS
• This application relates to novel urea glucokinase activators and use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes. Further encompassed is a pharmaceutic
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• Page/Page column 127

  (2008/12/07)
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• C8-alkynyl- and alkylamino substituted 2′-deoxyguanosines: a universal linker for nucleic acids modification
• Incorporation of modified nucleosides with a flexible universal linker is of great value for post-synthetic modification of nucleic acids. Thus, C8-alkynyl- and alkylamino substituted 2′-deoxyguanosines were synthesized for the first time and incorporated into short oligonucleotide sequences. The preference for syn conformation of these C8-substituted 2′-deoxyguanosines and the stability of the duplexes were discussed. The stabilizing effect of Z-DNA has also been examined.
• Saito, Yoshio,Matsumoto, Katsuhiko,Bag, Subhendu Sekhar,Ogasawara, Shinzi,Fujimoto, Kenzo,Hanawa, Kazuo,Saito, Isao

• p. 3578 - 3588

  (2008/09/21)
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• WATER-SOLUBLE CORONENE DERIVATIVES ACTIVE AS INHIBITORS OF HUMAN TELOMERASE BY INDUCTION OF G-QUADRUPLEX STRUCTURES AND THEIR USE AS ANTICANCER AGENTS
• The coronene derivatives of general formula: (I); wherein R1, R2, R2', R3, R4 and R4', when present and different from H, represent hydrophilic chains, constitute a new family of compounds that can selectively induce the formation of G-quadruplex structures in the telomeric DNA, and can thus act as inhibitors of the telomerase enzyme, thereby inhibiting tumour proliferation. These compounds proved to have a strong anticancer activity in vitro, which was assessed with many human tumour cell lines. Preparations including the coronene derivatives of formula (I) as active ingredients are proposed as medicament for use in anticancer treatments.
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• Page/Page column 15; 24-25

  (2008/12/08)
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• Anti-hypercholesterolemic biaryl azetidinone compounds
• This invention provides cholesterol absorption inhibitors of Formula I: and the pharmaceutically acceptable salts thereof, wherein R12 is an alkyl, alkeny or alkynyl group mono- or poly-substituted with —OH, —COOH or a combination of —OH and —COOH, and R9 contains an alkyl, alkeny or alkynyl group substituted with a heterocyclic ring, amino or sulfonyl. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating atherosclerosis and preventing atherosclerotic disease events.
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• Page/Page column 24

  (2008/12/08)
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• ANTI-HYPERCHOLESTEROLEMIC COMPOUNDS
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• Page/Page column 36

  (2008/12/07)
•