- Driving the Emission Towards Blue by Controlling the HOMO-LUMO Energy Gap in BF2-Functionalized 2-(Imidazo[1,5-a]pyridin-3-yl)phenols
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Several boron compounds with 2-(imidazo[1,5-a]pyridin-3-yl)phenols, differentiated by the nature of the substituent (R) in the para position of the hydroxy group, have been synthesized and thoroughly characterized both in solution (1H, 13C, 11B, 19F NMR) and in the solid state (X-ray). All derivatives displayed attractive photophysical properties like very high Stokes shift, high fluorescence quantum yields and a good photostability in solution. Time-Dependent Density Functional Theory (TD-DFT) calculations allowed to define the main electronic transitions as intra ligand transitions (1ILT), which was corroborated by the Natural Transition Orbitals (NTOs) shapes. The HOMO-LUMO energy gap was correlated to the electronic properties of the substituent R on the phenolic ring, as quantified by its σp Hammett constant.
- Colombo, Gioele,Attilio Ardizzoia,Furrer, Julien,Therrien, Bruno,Brenna, Stefano
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Read Online
- Preparation of titanium-containing polymeric foam for inertial confinement fusion target
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In the framework of the increasing need for metal-doped polymer materials for inertial confinement fusion targets, we report the preparation of low-density titanium-containing materials. For this purpose, we developed a new monomer based on hydroxyl and o
- Cadra, Stephane,Balland-Longeau, Alexia,Gerard, Jean-Francois,Moreau, Louis,Thibonnet, Jerome
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Read Online
- Schiff bases from TRIS and ortho-hydroxyarenecarbaldehydes: Structures and tautomeric equilibria in the solid state and in solution
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Three Schiff bases generated by conventional condensation of a simple aminopolyol (TRIS) and 5-bromo- and 5-iodosalicylaldehyde, and 2-hydroxy-1-naphthaldehyde, have been fully characterized, both in solution and in the solid state. This study provides a
- Martinez, R. Fernando,Uvalos, Martin,Babiano, Reyes,Cintas, Pedro,Jimenez, Jose L.,Light, Mark E.,Palacios, Juan C.
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Read Online
- Synthesis and electrogenerated chemiluminescence of donor-substituted phenylethynylcoumarins
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Two series of donor-bearing phenylethynylcoumarins have been synthesized, and their photophysical properties have been evaluated. Chemiluminescence was observed through the annihilation of their electrogenerated radical ions and was found to be only sligh
- Elangovan, Arumugasamy,Lin, Jui-Hsien,Yang, Shu-Wen,Hsu, Hsien-Yi,Ho, Tong-Ing
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Read Online
- Two-photon fluorescent probes for biological Mg2+ detection based on 7-substituted coumarin
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Two novel water-soluble coumarin-based compounds (OC7, NC7) were designed and synthesized as two-photon fluorescent probes for biological Mg2+ detection. The compounds feature a β-keto acid as a high selective binding site for Mg2+ a
- Yin, Haijing,Zhang, Buchang,Yu, Haizhu,Zhu, Lin,Feng, Yan,Zhu, Manzhou,Guo, Qingxiang,Meng, Xiangming
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Read Online
- Selectivity control in the reaction between 2-hydroxyarylaldehydes and 4-hydroxycoumarin. Antioxidant activities and computational studies of the formed products
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A series of 6H,7H-7-(4-Hydroxy-3-coumarinyl)[1]benzopyrano[4,3-b][1]benzopyran-6-ones 4a-g and 3-(2-hydroxybenzoyl)-2H-chromen-2-ones 5a-g derivatives were synthesized by reaction of 4-hydroxycoumarin with 2-hydroxyarylaldehydes 2a-f or 2-hydroxynaphtalde
- Lamara, Kamilia Ould,Makhloufi-Chebli, Malika,Benazzouz-Touami, Amina,Terrachet-Bouaziz, Souhila,Hamdi, Nejla,Silva, Artur M.S.,Behr, Jean-Bernard
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- Imine or Enamine? Insights and Predictive Guidelines from the Electronic Effect of Substituents in H-Bonded Salicylimines
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Imine and enamine bonds decorate the skeleton of numerous reagents, catalysts, and organic materials. However, it is difficult to isolate at will a single tautomer, as dynamic equilibria occur easily, even in the solid state, and are sensitive to electronic and steric effect, including π-conjugation and H-bonding. Here, using as model Schiff bases generated from salicylaldehydes and TRIS in a set of linear free energy relationships (LFER), we disclose how the formation of either imines or enamines can be controlled and provide a comprehensive framework that captures the structural underpinning of this prediction. This work highlights the potentiality of tailor-made designs en route to compounds with desirable functionality.
- Cintas, Pedro,Martínez, R. Fernando,Matamoros, Esther,Palacios, Juan C.
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p. 5838 - 5862
(2020/05/20)
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- Aryl derivatives of 3H-1,2-benzoxathiepine 2,2-dioxide as carbonic anhydrase inhibitors
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A new series of homosulfocoumarins (3H-1,2-benzoxathiepine 2,2-dioxides) possessing various substitution patterns and moieties in the 7, 8 or 9 position of the heterocylic ring were prepared by original procedures and investigated for the inhibition of four physiologically relevant carbonic anhydrase (CA, EC 4.2.1.1) isoforms, the human (h) hCA I, II, IX and XII. The 8-substituted homosulfocoumarins were the most effective hCA IX/XII inhibitors followed by the 7-substituted derivatives, whereas the substitution pattern in position 9 led to less effective binders for the transmembrane, tumour-associated isoforms IX/XII. The cytosolic isoforms hCA I and II were not inhibited by these compounds, similar to the sulfocoumarins/coumarins investigated earlier. As hCA IX and XII are validated anti-tumour targets, with one sulphonamide (SLC-0111) in Phase Ib/II clinical trials, finding derivatives with better selectivity for inhibiting the tumour-associated isoforms over the cytosolic ones, as the homosulfocoumarins reported here, is of crucial importance.
- Pustenko, Aleksandrs,Nocentini, Alessio,Bala?ova, Anastasija,Alafeefy, Ahmed,Krasavin, Mikhail,?alubovskis, Raivis,Supuran, Claudiu T.
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p. 245 - 254
(2019/12/11)
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- Nitrostyrene-Modified 2-(2-Hydroxyphenyl)benzothiazole: Enol-Emission Solvatochromism by ESICT-ESIPT and Aggregation-Induced Emission Enhancement
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Excited-state intramolecular charge transfer (ESICT) and excited-state intramolecular proton transfer (ESIPT) are two competitive reactions that occur in the excited states of organic dyes that contain intramolecular hydrogen-bonds and electron acceptors and donors. Determining the mechanisms of these processes is key to understanding their multiple emission features, as the manner in which these processes interact can be modulated by modifying the dye structure. In addition, donor–π–acceptor (D–π–A) molecules often suffer from aggregation-induced quenching. Herein, we report the synthesis of three nitrophenyl-modified 2-(2-hydroxyphenyl)benzothiazole (HBT) derivatives, HBT-s-NO2, HBT-d-NO2, and HBT-t-NO2, which have C?C, C=C, and C≡C bonds between their HBT and nitrophenyl moieties, respectively. Compared with the enol emissions from HBT-s-NO2 and HBT-t-NO2, that from HBT-d-NO2 exhibits outstanding solvatochromism owing to consecutive ESICT-ESIPT. In addition, X-ray diffraction reveals that despite the highly planar and polar nature of HBT-d-NO2, which is strongly H-aggregated, it exhibits highly efficient fluorescence. Hence, this study provides new insight into the design of ESICT/ESIPT-coupled systems and for engendering planar dipolar molecules with excellent emission properties in the solid state.
- Niu, Yahui,Wang, Rong,Shao, Panlin,Wang, Yuxiu,Zhang, Yanrong
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supporting information
p. 16670 - 16676
(2018/10/25)
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- Ultrasonically assisted halogenation of aromatic compounds using isoquinolinium bound hypervalent chromium and tetrabutylammonium halides in PEG-600 solutions under acid free and solvent-free conditions
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Isoquinolinium bound Cr(VI) reagents like isoquinolinium dichromate (IQDC) and isoquinolinium chlorochromate (IQCC) have been successfully accomplished as efficient reagents for oxidative halogenation of aromatic compounds using tetrabutylammonium halide (TBAX) as halogenating agents in aqueous polyethylene glycol (PEG-600) under acid free conditions. Tetrabutylammonium bromide (TBAB) has been used for bromination and tetrabutylammonium iodide (TBAI) for iodination. The halogenation reactions that occurred smoothly in 2 to 7 h under conventional conditions are accelerated magnificently under sonication with few minutes (25 to 70 min) of reaction time and fairly good yields. The reactions occurred at moderate temperature under mild and environmentally safe conditions with simple work up.
- Sambashiva Rao,Ramesh, Kola,Rajanna,Chakrvarthi
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p. 1892 - 1896
(2018/07/10)
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- Rapid Access to Benzofuran-Based Natural Products through a Concise Synthetic Strategy
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A concise strategy is described for the synthesis of ailanthoidol (1), egonol (2), homoegonol (3), demethoxyegonol (4), demethoxyhomoegonol (5), and stemofuran A (6). This approach involves a Pd-catalysed domino cyclization/coupling process using triarylbismuth reagents for the generation of the benzofuran core. Subsequent structural modifications then give the final targets. The high yielding synthesis of the recently isolated natural products egonol-9(Z)-12(Z)-linoleate (2a), 7-demethoxyegonol-9(Z)-12(Z)-linoleate (4a), and 7-demethoxy-egonol-9(Z)-oleate (4b) are also reported.
- Rao, Maddali L. N.,Murty, Venneti N.
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p. 2177 - 2186
(2016/05/09)
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- A six bit substituted coumarin derivatives of two-photon fluorescent dye and its preparation method
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The invention discloses hexa-substituted coumarin derivative two-photon fluorescent dye of which the structural general formula is shown in the specification, wherein R is CH3O- or (CH3)2N-. The fluorescent dye prepared by the invention is simple to synth
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Paragraph 0021 - 0023
(2017/02/24)
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- Isoquinolinium Dichromate and Chlorochromate as Efficient Catalysts for Oxidative Halogenation of Aromatic Compounds under Acid-Free Conditions
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Isoquinolinium dichromate and isoquinolinium chlorochromate were found as efficient catalysts to trigger oxidative bromination and iodination of aromatic hydrocarbons with KBr/KI and KHSO4 under acid-free conditions. Reaction times reduced highly significantly under sonication, followed by corresponding mono bromo derivatives in very good yield with high regioselectivity.
- Rao, A. Sambashiva,Rajanna,Reddy, K. Rajendar,Kulkarni, Subhash
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p. 832 - 837
(2016/02/12)
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- Improved and scalable synthesis of building blocks for the modular synthesis of teraryl-based alpha-helix mimetics
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The modular synthesis of teraryl-based alpha-helix mimetics can be accomplished by sequential Suzuki-couplings of arylboronic acid building blocks with 4-iodophenyltriflate core-fragments. We report about new synthetic accesses to core fragments featuring
- Trobe, Melanie,Breinbauer, Rolf
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p. 509 - 521
(2016/03/19)
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- Antioxidant properties in a non-polar environment of difluoromethyl bioisosteres of methyl hydroxycinnamates
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Objectives Many natural antioxidants have poor pharmacokinetic properties that impair their therapeutic use. For hydroxycinnamic acids (HCAs) and other phenolic antioxidants, their major drawback is their low lipophilicity and a rapid metabolism. The difl
- Martínez, Mario D.,Luna, Lorena,Tesio, Alvaro Y.,Feresin, Gabriela E.,Durán, Fernando J.,Burton, Gerardo
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p. 233 - 244
(2016/02/27)
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- Gold(I)-catalyzed iodination of arenes
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A wide variety of electron-rich arenes were efficiently converted into the corresponding iodinated compounds via a gold(I)-catalyzed reaction under mild conditions. Georg Thieme Verlag Stuttgart. New York.
- Leboeuf, David,Ciesielski, Jennifer,Frontier, Alison J.
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supporting information
p. 399 - 402
(2014/03/21)
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- Greener iodination of arenes using sulphated ceria-zirconia catalysts in polyethylene glycol
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An environmentally benign method for the selective monoiodination of diverse aromatic compounds has been developed using reusable sulphated ceria-zirconia under mild conditions. The protocol provides moderate to good yields and selectively introduces iodine at the para/ortho position in monosubstituted arenes. SO42-/Ce0.07Zr 0.93O2 was found to be the best choice for the synthesis of aryl iodides in high yield, presumably due to the maximum number of acid sites (4.23 mmol g-1) among the various compositions of the catalyst system.
- Kahandal, Sandeep S.,Kale, Sandip R.,Gawande, Manoj B.,Zboril, Radek,Varma, Rajender S.,Jayaram, Radha V.
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p. 6267 - 6274
(2014/01/23)
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- Polymerizable coordination complexes and polymeric materials obtained from said monomers
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Coordination complexes of at least one metal element with at least one aromatic monomer are provided. The at least one aromatic monomer may comprise at least one aromatic ring, which ring comprising at least one ethylenic group, at least one hydroxide gro
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Paragraph 8; 9
(2014/09/16)
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- A family of enantiopure FeIII4 single molecule magnets: Fine tuning of energy barrier by remote substituent
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A new family of enantiopure star-shaped FeIII4 single-molecule magnets (SMMs) with the general formula [Fe4(L K)6] (H2L = (R or S)-2-((2-hydroxy-1- phenylethylimino methyl)phenol); K = H (1), Cl (2), Br (3), I (4), and t-Bu (5)), were structurally and magnetically characterized. Complex 1 was reported in our previous paper (Chem. Commun., 2011, 47, 8049-8051). Detailed magnetic measurements and a systematic magneto-structural correlation study revealed that the SMM properties of this series of compounds can be finely tuned by the remote substituent of the ligands. Although the change in the coordination environment of the central Fe3+ ions is very small, the properties of SMM behavior are changed considerably. All five complexes display frequency dependence of the ac susceptibility. However, the χ′′ac peaks of complexes 2 and 5 cannot be observed down to 0.5 K. The fitted anisotropy energy barriers (Ueff) of complexes 1, 3, and 4 were 5.9, 7.1, and 11.0 K, respectively. Moreover, the hysteresis loops of these three complexes can be also observed around 0.5 K. Magneto-structural correlation analyses revealed that the coordination symmetry of the central Fe3+ ion and the intermolecular interaction are two key factors affecting the SMM properties. Deviation to a trigonal prism coordination environment and the existence of intermolecular interactions between neighboring clusters may both reduce the anisotropy energy barriers. This journal is the Partner Organisations 2014.
- Zhu, Yuan-Yuan,Cui, Chang,Qian, Kang,Yin, Ji,Wang, Bing-Wu,Wang, Zhe-Ming,Gao, Song
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supporting information
p. 11897 - 11907
(2014/08/05)
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- A modular synthesis of teraryl-based α-helix mimetics, part 1: Synthesis of core fragments with two electronically differentiated leaving groups
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Teraryl-based α-helix mimetics have proven to be useful compounds for the inhibition of protein-protein interactions (PPI). We have developed a modular and flexible approach for the synthesis of teraryl-based α-helix mimetics. Central to our strategy is the use of a benzene core unit featuring two leaving groups of differentiated reactivity in the Pd-catalyzed cross-coupling used for terphenyl assembly. With the halogen/diazonium route and the halogen/triflate route, two strategies have successfully been established. The synthesis of core building blocks with aliphatic (Ala, Val, Leu, Ile), aromatic (Phe), polar (Cys, Lys), hydrophilic (Ser, Gln), and acidic (Glu) amino acid side chains are reported. Turn on: Teraryl-based α-helix mimetics can be effectively produced by sequential Suzuki coupling of a central core fragment featuring electronically differentiated leaving groups with aryl boronic pinacol esters (see scheme; dppf=1,1′-bis(diphenylphosphino) ferrocene, DME=dimethoxyethane, Pin=pinacol, Tf=trifluoromethanesulfonyl). With a set of only 2×18 building blocks, all permutations of α-helix mimetics can be produced. Copyright
- Peters, Martin,Trobe, Melanie,Tan, Hao,Kleineweischede, Rolf,Breinbauer, Rolf
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supporting information
p. 2442 - 2449
(2013/04/24)
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- Synthesis of luminescent ethynyl-extended regioisomers of borate complexes based on 2-(2′-hydroxyphenyl)benzoxazole
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A series of thirteen luminescent tetrahedral borate complexes based on the 2-(2′-hydroxyphenyl)benzoxazole (HBO) core is presented. Their synthesis includes the incorporation of an ethynyl fragment by Sonogashira cross-coupling reaction, with the goal of
- Massue, Julien,Frath, Denis,Retailleau, Pascal,Ulrich, Gilles,Ziessel, Raymond
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p. 5375 - 5386
(2013/05/21)
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- POLYMERIZABLE COORDINATION COMPLEXES AND POLYMERIC MATERIALS OBTAINED FROM SAID MONOMERS
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Coordination complexes of at least one metal element with at least one aromatic monomer are provided. The at least one aromatic monomer may comprise at least one aromatic ring, which ring comprising at least one ethylenic group, at least one hydroxide gro
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- HETEROCYCLYL-SUBSTITUTED ANTI-HYPERCHOLESTEROLEMIC COMPOUNDS
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This invention provides cholesterol absorption inhibitors of Formula I: and the pharmaceutically acceptable salts thereof, wherein R12 is a hydroxylated alkyl group and R9 contains a heterocyclic ring. 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 80
(2008/12/05)
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- Aminostyrylbenzofuran derivatives as potent inhibitors for Aβ fibril formation
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The synthesis of a novel series of aminostyrylbenzofuran derivatives 1a-w and their inhibitory activities for Aβ fibril formation were described. All the synthesized compounds were evaluated by thioflavin T (ThT) assay and displayed potent inhibitory activities for Aβ fibril formation. Among them, compounds 1i and 1q exhibited excellent inhibitory activities (IC50 = 0.07 and 0.08 μM, respectively) than those of Curcumin (IC50 = 0.80 μM) and IMSB (IC50 = 8.00 μM) as reference compounds. Both compounds were selected as promising candidates for further biological evaluation.
- Byun, Ji Hun,Kim, HyeYun,Kim, YoungSoo,Mook-Jung, Inhee,Kim, Dong Jin,Lee, Won Koo,Yoo, Kyung Ho
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scheme or table
p. 5591 - 5593
(2009/06/18)
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- Total synthesis of paliurine F
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A couple of coppers: An efficient, asymmetric synthesis of the sedative cyclopeptide alkaloid paliurine F has been achieved. The strategy employs two copper(I)-mediated coupling reactions as key steps to install the aryl ether linkage as well as to form t
- Toumi, Mathieu,Couty, Francois,Evano, Gwilherm
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p. 572 - 575
(2008/02/02)
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- Antibacterial amide macrocycles
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The invention relates to antibacterial amide macrocycles, to methods for the production thereof, and to the use of the same for producing pharmaceuticals for the treatment and/or prophylaxis of illness, especially bacterial infections.
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Page/Page column 23
(2010/11/27)
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- Efficient and selective reduction protocols of the 2,2-dimethyl-1,3- benzodioxan-4-one functional group to readily provide both substituted salicylaldehydes and 2-hydroxybenzyl alcohols
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Two complementary procedures have been developed that selectively allow for the synthesis of either substituted salicylaldehydes or the corresponding 2-hydroxylbenzyl alcohols upon treatment of the 2,2-dimethyl-1,3-benzodioxan-4- one functional group with DIBAL-H or LAH, respectively.
- Bajwa, Naval,Jennings, Michael P.
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p. 3646 - 3649
(2007/10/03)
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- One-pot synthesis of ortho-hydroxycinnamate esters
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Phenols are converted to salicylaldehydes with paraformaldehyde, MgCl 2-Et3N in THF, and subsequent treatment with methyl (triphenylphosphoranylidene)acetate gave the corresponding methyl ortho-hydroxycinnamate derivatives. The sequence is conveniently carried out as a one-pot procedure.
- Anwar, Hany F.,Skatteb?l, Lars,Skramstad, Jan,Hansen, Trond Vidar
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p. 5285 - 5287
(2007/10/03)
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- BENZOPYRAN COMPOUNDS USEFUL FOR TREATING INFLAMMATORY CONDITIONS
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The subject invention concerns methods and compounds that have utility in the treatment of a condition associated with cyclooxygenase-2 mediated disorders. Compounds of particular interest are benzopyrans and their analogs defined by formula (1). Wherein Z, X, R1, R2, R3, and R4 are as described in specification.
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- CHROMENE DERIVATIVES AS ANTI-INFLAMMATORY AGENTS
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The subject invention concerns methods and compounds that have utility in the treatment of a condition associated with cyclooxygenase-2 mediated disorders. Compounds of particular interest are benzopyrans and their analogs defined by formula (I). Wherein Z, X, R1, R2, R3, and R4 are as described in the specification.
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- Efficient halogenation of aromatic systems using N-halosuccinimides in ionic liquids
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A simple, rapid and highly regioselective green protocol has been developed for the halogenation of aromatic systems with N-halosuccinimides using room temperature ionic liquids (ILs) as novel and recyclable reaction media to produce the corresponding halogenated aromatic compounds in high to quantitative yields. N-Halosuccinimides show enhanced reactivity in ionic liquids thereby reducing the reaction times dramatically and improving the yields substantially.
- Yadav,Reddy,Reddy,Basak,Narsaiah
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- Fischer's base as a protecting group: Protection and deprotection of 2- hydroxybenzaldehydes
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The hydroxyl and aldehyde groups of 2-hydroxybenzaldehydes were protected by the reaction with Fischer's base and deprotected by the ozonolysis in methanol at -78°C to give the corresponding 2- hydroxybenzaldehydes in good to high yields. (C) 2000 Elsevier Science Ltd.
- Cho, Young Jin,Lee, Seung Hwan,Bae, Jong Woo,Pyun, Hyung-Jung,Yoon, Cheol Min
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p. 3915 - 3917
(2007/10/03)
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- Substituted benzopyran derivatives for the treatment of inflammation
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A class of benzopyran, derivatives is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I'wherein X, A1, A2, A3, A4, R, R'', R1 and R2 are as described in the specification.
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- Substituted benzopyran analogs for the treatment of inflammation
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A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I'wherein X, A1, A2, A3, A4, R, R'', R1 and R2 are as described in the specification.
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- Substituted sulfonic acid N-[(aminoiminomethyl)phenylalkyl]-azaheterocyclylamide compounds
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The compounds of formula I exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
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- Sulfonamidopyrrolidinone factor Xa inhibitors: Potency and selectivity enhancements via P-1 and P-4 optimization
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Sulfonamidopyrrolidinones were previously disclosed as a selective class of factor Xa (fXa) inhibitors, culminating in the identification of RPR120844 as a potent member with efficacy in vivo. Recognizing the usefulness of the central pyrrolidinone template for the presentation of ligands to the S-1 and S-4 subsites of fXa, studies to optimize the P-1 and P-4 groups were initiated. Sulfonamidopyrrolidinones containing 4-hydroxy- and 4- aminobenzamidines were discovered to be effective inhibitors of fXa. X-ray crystallographic experiments in trypsin and molecular modeling studies suggest that our inhibitors bind by insertion of the 4-hydroxybenzamidine moiety into the S-1 subsite of the fXa active site. Of the P-4 groups examined, the pyridylthienyl sulfonamides were found to confer excellent potency and selectivity especially in combination with 4-hydroxybenzamidine. Compound 20b (RPR130737) was shown to be a potent fXa inhibitor (K1 = 2 nM) with selectivity against structurally related serine proteinases (> 1000 times). Preliminary biological evaluation demonstrates the effectiveness of this inhibitor in common assays of thrombosis in vitro (e.g. activated partial thromboplastin time) and in vivo (e.g. rat FeCl2-induced carotid artery thrombosis model).
- Choi-Sledeski, Yong Mi,McGarry, Daniel G.,Green, Daniel M.,Mason, Helen J.,Becker, Michael R.,Davis, Roderick S.,Ewing, William R.,Dankulich, William P.,Manetta, Vincent E.,Morris, Robert L.,Spada, Alfred P.,Cheney, Daniel L.,Brown, Karen D.,Colussi, Dennis J.,Valeria, Chu,Heran, Christopher L.,Morgan, Suzanne R.,Bentley, Ross G.,Leadley, Robert J.,Maignan, Sebastien,Guilloteau, Jean-Pierre,Dunwiddie, Christopher T.,Pauls, Henry W.
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p. 3572 - 3587
(2007/10/03)
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- Synthesis of conjugated spiropyran dyes via palladium-catalyzed coupling reaction
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Spiropyrans (5a-h) conjugated at 6 position have been conveniently and efficiently prepared by palladium-catalyzed coupling of 6-iodospiropyran (4a, 4b) with olefins or alkynes in moderate to high yield. This method might be a particularly very important
- Cho, Young Jin,Rho, Kee Yoon,Keum, Sam Rok,Kim, Sung Hoon,Yoon, Cheol Min
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p. 2061 - 2068
(2007/10/03)
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- SUBSTITUTED SULFONIC ACID N-[(AMINOIMINOMETHYL)PHENYLALKYL]-AZAHETEROCYCLAMIDE COMPOUNDS
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The compounds of formula I exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
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- The design and synthesis of substituted biphenyl libraries
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A novel scaffold system for the generation of diversity libraries has been designed which allows for rapid modification not only of functional groups, but their spatial arrangements as well. The biphenyl scaffold allows for display of three or four divers
- Pavia, Michael R.,Cohen, Michael P.,Dilley, Garrett J.,Dubuc, Gloria R.,Durgin, Tracy L.,Forman, Frank W.,Hediger, Mark E.,Milot, Guy,Powers, Timothy S.,Sucholeiki, Irving,Zhou, Shulan,Hangauer, David G.
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p. 659 - 666
(2007/10/03)
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