- Charge-tagged polar phosphine ligands in Pd-catalysed reactions in aqueous and ionic media
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A new range of polar imidazolium and phosphate-containing ligands was synthesised from readily available starting materials in high yielding multi-step transformations. These ligands were used to generate Pd catalysts for Suzuki and Heck C–C coupling reac
- van Zyl, Vivien L.,Muller, Alfred,Williams, D. Bradley G.
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Read Online
- N3-Substituted thymidine analogues III: Radiosynthesis of N 3-[(4-[18F]fluoromethyl-phenyl)butyl]thymidine ([ 18F]-FMPBT) and N-[(4-[18F]fluoromethyl-phenyl)pentyl] thymidine ([18F]-FMPPT)
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Radiosyntheses of two N3-substituted thymidine analogues, N 3-[(4[18F]fluoromethyl-phenyl)butyl]thymidine ([ 18F]-FMPBT) and N3-[(4[18F]fluoromethyl-phenyl) pentyl]thymidine ([18
- Ghosh, Pradip,Gelovani, Juri G.,Alauddin, Mian M.
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Read Online
- Iron-Catalyzed Ring Expansion of Cyclobutanols for the Synthesis of 1-Pyrrolines by Using MsONH3OTf
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The synthesis of 1-pyrrolines from cyclobutanol derivatives and an aminating reagent (MsONH3OTf) has been developed. This one-pot procedure achieves C–N bond/C═N bond formation via ring expansion. A series of 1-pyrroline derivatives are synthes
- Zhuang, Daijiao,Gatera, Tharcisse,An, Zhenyu,Yan, Rulong
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supporting information
p. 771 - 775
(2022/01/20)
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- Design, synthesis, in vitro and in vivo evaluation of heterobivalent sifalin-modified peptidic radioligands targeting both integrin αv β3 and the mc1 receptor—suitable for the specific visualization of melanomas?
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Combining two peptides addressing two different receptors to a heterobivalent peptidic ligand (HBPL) is thought to enable an improved tumor-targeting sensitivity and thus tumor visu-alization, compared to monovalent peptide ligands. In the case of melanoma, the Melanocortin-1 receptor (MC1R), which is stably overexpressed in the majority of primary malignant melanomas, and integrin αv β3, which is involved in lymph node metastasis and therefore has an important role in the transition from local to metastatic disease, are important target receptors. Thus, if a radiolabeled HBPL could be developed that was able to bind to both receptor types, the early diagnosis and correct staging of the disease would be significantly increased. Here, we report on the design, synthesis, radiolabeling and in vitro and in vivo testing of different SiFAlin-modified HBPLs (SiFA = silicon fluoride acceptor), consisting of an MC1R-targeting (GG-Nle-c(DHfRWK)) and an integrin αv β3-affine peptide (c(RGDfK)), being connected by a symmetrically branching framework including linkers of differing length and composition. Kit-like18 F-radiolabeling of the HBPLs 1–6 provided the labeled products [18 F]1–[18 F]6 in radiochemical yields of 27–50%, radiochemical purities of ≥95% and non-optimized molar activities of 17–51 GBq/μmol within short preparation times of 25 min. Besides the evaluation of radiotracers regarding logD(7.4) and stability in human serum, the receptor affinities of the HBPLs were investigated in vitro on cell lines overexpressing integrin αv β3 (U87MG cells) or the MC1R (B16F10). Based on these re-sults, the most promising compounds [18 F]2, showing the highest affinity to both target receptors (IC50 (B16F10) = 0.99 ± 0.11 nM, IC50 (U87MG) = 1300 ± 288 nM), and [18 F]4, exhibiting the highest hy-drophilicity (logD(7.4) = ?1.39 ± 0.03), were further investigated in vivo and ex vivo in a xenograft mouse model bearing both tumors. For both HBPLs, clear visualization of B16F10, as well as U87MG tumors, was feasible. Blocking studies using the respective monospecific peptides demon-strated both peptide binders of the HBPLs contributing to tumor uptake. Despite the somewhat lower target receptor affinities (IC50 (B16F10) = 6.00 ± 0.47 nM and IC50 (U87MG) = 2034 ± 323 nM) of [18 F]4, the tracer showed higher absolute tumor uptakes ([18 F]4: 2.58 ± 0.86% ID/g in B16F10 tumors and 3.92 ± 1.31% ID/g in U87MG tumors; [18 F]2: 2.32 ± 0.49% ID/g in B16F10 tumors and 2.33 ± 0.46% ID/g in U87MG tumors) as well as higher tumor-to-background ratios than [18 F]2. Thus, [18 F]4 demonstrates to be a highly potent radiotracer for the sensitive and bispecific imaging of malignant melanoma by PET/CT imaging and impressively illustrates the suitability of the un-derlying concept to develop heterobivalent integrin αv β3-and MC1R-bispecific radioligands for the sensitive and specific imaging of malignant melanoma by PET/CT.
- Cheng, Xia,Fricker, Gert,Hübner, Ralph,Schirrmacher, Ralf,W?ngler, Bj?rn,W?ngler, Carmen,von Kiedrowski, Valeska
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- Preparation method 4 - hydroxymethylphenylboronic acid
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The invention relates to the technical field of organic synthesis. The invention specifically discloses a preparation method of 4 -hydroxymethylphenylboronic acid. To the preparation method, bromobenzyl alcohol is taken as a raw material, Grignard reagent
- -
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Paragraph 0055-0058; 0085-0088; 0091-0094
(2021/09/08)
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- Aerobic oxygenation of α-methylene ketones under visible-light catalysed by a CeNi3complex with a macrocyclic tris(salen)-ligand
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A hetero-tetranuclear CeNi3 complex with a macrocyclic ligand catalysed the aerobic oxygenation of a methylene group adjacent to a carbonyl group under visible-light radiation to produce the corresponding α-diketones. The visible-light induced homolysis of the Ce-O bond of a bis(enolate) intermediate is proposed prior to aerobic oxygenation.
- Fujiwara, Sakiko,Kon, Yoshihiro,Mashima, Kazushi,Nagae, Haruki,Okuda, Jun,Sakamoto, Kazutaka,Sato, Kazuhiko,Schindler, Tobias
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supporting information
p. 11169 - 11172
(2021/11/04)
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- SILICON-FLUORIDE ACCEPTOR SUBSTITUTED RADIOPHARMACEUTICALS AND PRECURSORS THEREOF
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A ligand-SiFA conjugate compound represented by formula (1) wherein: RL is a ligand moiety which is capable of binding to prostate-specific membrane antigen (PSMA); RSiFA is a silicon-fluoride acceptor (SiFA) moiety which can be labe
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Page/Page column 74
(2020/08/22)
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- CANCER DIAGNOSTIC IMAGING AGENTS
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The present invention relates to a ligand-SIFA-chelator conjugate, comprising, within a single molecule three separate moieties: (a) one or more ligands which are capable of binding to PSMA, (b) a silicon-fluoride acceptor (SIFA) moiety which comprises a covalent bond between a silicon atom and a fluorine atom, and (c) one or more chelating groups, containing a chelated nonradioactive cation.
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Page/Page column 51-53
(2020/08/22)
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- ANTIMICROBIAL COMPOUNDS AND METHODS
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The invention is directed to compounds that are active as antibacterial agents. The invention compounds are active against gram-positive and gram-negative bacteria and can be used to treat infections caused by gram-positive and gram-negative bacteria. Also disclosed are processes and intermediates for making the compounds.
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Paragraph 00601
(2020/07/31)
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- Manganese-Catalyzed Electrochemical Deconstructive Chlorination of Cycloalkanols via Alkoxy Radicals
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A manganese-catalyzed electrochemical deconstructive chlorination of cycloalkanols has been developed. This electrochemical method provides access to alkoxy radicals from alcohols and exhibits a broad substrate scope, with various cyclopropanols and cyclobutanols converted into synthetically useful β- and γ-chlorinated ketones (40 examples). Furthermore, the combination of recirculating flow electrochemistry and continuous inline purification was employed to access products on a gram scale.
- Allen, Benjamin D. W.,Hareram, Mishra Deepak,Seastram, Alex C.,McBride, Tom,Wirth, Thomas,Browne, Duncan L.,Morrill, Louis C.
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supporting information
p. 9241 - 9246
(2019/11/19)
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- Mild Ring Contractions of Cyclobutanols to Cyclopropyl Ketones via Hypervalent Iodine Oxidation
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An iodine-mediated oxidative ring contraction of cyclobutanols has been developed. The reaction allows the synthesis of a wide range of aryl cyclopropyl ketones under mild and eco-friendly conditions. A variety of functional groups including aromatic or alkyl halides, ethers, esters, ketones, alkenes, and even aldehydes are nicely tolerated in the reaction. This is in contrast with traditional synthetic approaches for which poor functional group tolerance is often a problem. The practicality of the method is also highlighted by the tunability of iodine oxidation system. Specifically, combining the iodine(III) reagent with an appropriate base allows the reaction to accommodate a range of challenging electron-rich arene substrates. The facile scalability of this reaction is also exhibited herein. (Figure presented.).
- Sun, Yan,Huang, Xin,Li, Xiaojin,Luo, Fan,Zhang, Lei,Chen, Mengyuan,Zheng, Shiya,Peng, Bo
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supporting information
p. 1082 - 1087
(2018/01/27)
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- Remote migratory cross-electrophile coupling and olefin hydroarylation reactions enabled by in situ generation of nih
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A highly efficient strategy for remote reductive cross-electrophile coupling has been developed through the ligand-controlled nickel migration/arylation. This general protocol allows the use of abundant and bench-stable alkyl bromides and aryl bromides for the synthesis of a wide range of structurally diverse 1, 1-diarylalkanes in excellent yields and high regioselectivities under mild conditions. We also demonstrated that alkyl bromide could be replaced by the proposed olefin intermediate while using n-propyl bromide/Mn0 as a potential hydride source.
- Chen, Fenglin,Chen, Ke,Zhang, Yao,He, Yuli,Wang, Yi-Ming,Zhu, Shaolin
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supporting information
p. 13929 - 13935
(2017/11/07)
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- Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids
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Pretomanid (PA-824) is an important nitroimidazole antitubercular agent in late stage clinical trials. However, pretomanid is limited by poor solubility and high protein binding, which presents opportunities for improvement in its physiochemical properties. Conversely, the oxazolidinone linezolid has excellent physicochemical properties and has recently shown impressive activity for the treatment of drug resistant tuberculosis. In this study we explore if incorporation of the outer ring elements found in first and second generation oxazolidinones into the nitroimidazole core of pretomanid can be used to improve its physicochemical and antitubercular properties. The synthesis of pretomanid outer oxazolidinone ring hybrids was successfully performed producing hybrids that maintained antitubercular activity and had improved in vitro physicochemical properties. Three lead compounds were identified and evaluated in a chronic model of tuberculosis infection in mice. However, the compounds lacked efficacy suggesting that portions of PA-824 tail not found in the hybrid molecules are required for in vivo efficacy.
- Rakesh,Bruhn, David F.,Scherman, Michael S.,Singh, Aman P.,Yang, Lei,Liu, Jiuyu,Lenaerts, Anne J.,Lee, Richard E.
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p. 388 - 391
(2016/01/09)
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- SMALL MOLECULE MODULATORS OF PCSK9 AND METHODS OF USE THEREOF
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A compound of Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or racemic mixture or stereoisomer thereof, and methods for preventing or treating an LDL-cholesterol-related disease or disorder using such compound(s), and kits and comp
- -
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Paragraph 0366
(2016/02/22)
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- PYRIDINE DERIVATIVES AS MUSCARINIC M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
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The present invention provides, in part, compounds of Formula I: (I) N-oxides thereof, and pharmaceutically acceptable salts of the compounds or N-oxides; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds,N-oxides, or salts, and their uses for treating M1-mediated (or M1-associated) disorders including, e.g., Alzheimer's disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.
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Page/Page column 136; 137
(2016/02/10)
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- PYRROLIDINE-2-CARBOXYLIC ACID DERIVATIVES AS IGLUR ANTAGONISTS
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The present invention relates to compounds of Formula (I), combinations and use thereof for disease therapy, or pharmaceutically acceptable salt or solvate thereof, including all tautomers, stereoismers and polymorphs thereof, which are iGluR receptor inhibitors, and hence are useful in the treatment of psychiatric diseases or neurological disorders or a disease or disorder associated with abnormal activities of iGluR receptors.
- -
-
Paragraph 0120; 0121
(2014/09/03)
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- Preparation of nano silica supported sodium hydrogen sulfate: As an efficient catalyst for the trimethyl, triethyl and t-butyldimethyl silylations of aliphatic and aromatic alcohols in solution and under solvent-free conditions
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Nano silica supported sodium hydrogen sulfate has been prepared by mixing NaHSO4 with activated Nano silicagel. We wish to report a new method for the synthesis of trimethyl (TMS), triethyl (TES) and t-butyldimethyl silyl (TBS) ethers from benzylic, allylic, propargylic alcohols, phenols, naphtholes and some of phenolic drugs in the solution and under solvent-free conditions.
- Abri, Abdolreza,Ranjdar, Somayeh
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p. 929 - 934
(2014/10/16)
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- NOVEL TARGETING AGENTS FOR DIAGNOSTIC AND THERAPEUTIC INDICATIONS
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The invention relates to compounds and use thereof in the diagnosis and/or in treatment of medical disorders. In some embodiments, the compounds may be used for detecting a cancer. The compound may include a di-acid moiety. In some embodiments the di-acid moiety comprises a di-carboxylic acid and in some embodiments the di- acid moiety comprises a di-tetrazole.
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Paragraph 00112
(2013/10/22)
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- VIRAL REPLICATION INHIBITORS
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The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds.
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Page/Page column 131; 180
(2013/04/13)
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- 2- (TERT - BUTOXY) -2- (7 -METHYLQUINOLIN- 6 - YL) ACETIC ACID DERIVATIVES FOR TREATING AIDS
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The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compound
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Page/Page column 112
(2013/07/19)
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- PYRIMIDONE DERIVATIVES USED AS TAU PROTEIN KINASE 1 INHIBITORS
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A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom or C-X; X represents hydrogen atom or fluorine atom; R1 is hydrogen atom or a C1 -C3 alkyl group; L represents single bond or a C1 -C6 alkylene group which may be substituted; Y represents single bond, sulfur atom, oxygen atom, NH, or the like; R2 represents hydrogen atom or a cyclic group which may be substituted, which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).
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Page/Page column 49
(2011/02/24)
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- Synthesis and biological evaluation of a series of aromatic bisphosphonates
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Geminal bisphosphonates display varied biological activity depending on the nature of the substituents on the central carbon atom. For example, the nitrogenous bisphosphonates zoledronate and risedronate inhibit the enzyme farnesyl diphosphate synthase wh
- Barney, Rocky J.,Wasko, Brian M.,Dudakovic, Amel,Hohl, Raymond J.,Wiemer, David F.
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experimental part
p. 7212 - 7220
(2010/11/18)
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- Prenylated Bisphosphonates as Anti-tuberculosis Agents
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The invention provides methods to treat a mycobacterium infection and methods to inhibit mycobacterial polyprenyl pyrophosphate synthesis with a compound of formula I. The invention also provides novel compounds of formula I as well as salts and prodrugs
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Page/Page column 7
(2010/10/03)
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- Syntheses of trans -SCH-A and cis -SCH-A via a stereodivergent cyclopropanation protocol
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(Figure Presented) A highly diastereoselective cyclopropanation protocol has been employed in the syntheses of trans-SCH-A and cis-SCH-A. This strategy encompasses a stereodivergent procedure for the preparation of syn- and anti-cyclopropane diastereoisom
- Csatayova, Kristina,Davies, Stephen G.,Lee, James A.,Ling, Kenneth B.,Roberts, Paul M.,Russell, Angela J.,Thomson, James E.
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supporting information; experimental part
p. 3152 - 3155
(2010/09/05)
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- DIAZACARBAZOLES AND METHODS OF USE
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The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chkl) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
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Page/Page column 158-159
(2010/01/07)
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- NOVEL N-BENZYLAMIDE SUBSTITUTED DERIVATIVES OF 2-(ACYLAMIDO)ACETIC ACID AND 2-(ACYLAMIDO)PROPIONIC ACIDS: POTENT NEUROLOGICAL AGENTS
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A first aspect of the invention is a compound (sometimes also referred to herein as an "active agent" or "active compound") of Formula (I) or ( Ia): or a pharmaceutically acceptable salt or prodrug thereof. Compositions thereof and methods of using the same (e.g. for the treatment of a neurological disease) are also described.
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Page/Page column 62
(2009/12/27)
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- A xerogel-sequestered selenoxide catalyst for brominations with hydrogen peroxide and sodium bromide in an aqueous environment
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(Chemical Equation Presented) 4-(Hydroxymethyl)phenyl benzyl selenoxide (4) sequestered in a halide-permeable, Class II xerogel formed from 10/90 (mol/mol) 3-aminopropyltriethoxysilane/tetraethoxysilane catalyzes the bromination of organic substrates (4-pentenoic acid, 3,5-dihydroxybenzoic acid, 1,3,5-trimethoxybenzene, N-phenylmorpholine, and N,N-dimethylaniline) with NaBr and H2O2. Catalyst performance (reaction rate) when sequestered within the halide-permeable xerogel is 23-fold greater in comparison to xerogel-free catalyst in solution. The catalyst is easily separated from the reaction mixture via filtration and the recovered catalyst can be reused without loss of activity through formation of the first 80 mol of product per mole of catalyst.
- Bennett, Stephanie M.,Tang, Ying,McMaster, Danielle,Bright, Frank V.,Detty, Michael R.
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p. 6849 - 6852
(2008/12/22)
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- Synthesis of soluble oligo- and polymeric pentacene-based materials
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Functionalization of pentacene at the 6- and 13-positions affords versatile building blocks for oligomer and polymer formation. Di- and trimeric materials are synthesized using unsymmetrical building block 18, while symmetrical diol monomer 17 allows for the synthesis of polymers. The materials reported herein are soluble in common organic solvents and air-stable. UV-vis and fluorescence spectroscopic properties have been investigated. Solid-state X-ray crystallography of building blocks 17 and 19 shows that these derivatives can π-stack with significant acene face-to-face interactions with spacing of less than 3.5 A?.
- Lehnherr, Dan,McDonald, Robert,Ferguson, Michael J.,Tykwinski, Rik R.
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supporting information; experimental part
p. 11449 - 11461
(2009/04/11)
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- Trifluoromethyldiazirine: An effective photo-induced cross-linking probe for exploring amyloid formation
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The separative and analytical power of ion mobility spectrometry-mass spectrometry combined with photo-induced cross-linking of site-specifically incorporated trifluoromethyldiazirine provides a powerful approach towards structural characterisation of amy
- Smith, David P.,Anderson, Jon,Plante, Jeffrey,Ashcroft, Alison E.,Radford, Sheena E.,Wilson, Andrew J.,Parker, Martin J.
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supporting information; experimental part
p. 5728 - 5730
(2009/04/13)
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- COMPOUND CONTAINING BASIC GROUP AND USE THEREOF
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The present invention relates to a compound represented by formula (I): wherein all symbols are as defined here, a salt thereof, a solvate thereof, or a prodrug thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, rejection of transplanted organ, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.
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Page/Page column 63
(2008/12/06)
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- Pentacene oligomers and polymers: Functionalization of pentacene to afford mono-, di-, tri-, and polymeric materials
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(Chemical Equation Presented) The synthesis and characterization of defined-length di- and trimeric pentacenes and the corresponding polymers are described. The synthesis is divergent from two common pentacene building blocks, 1 and 2, allowing for structural diversity. The resulting materials are air stable and exhibit good solubility in common organic solvents.
- Lehnherr, Dan,Tykwinski, Rik R.
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p. 4583 - 4586
(2008/03/12)
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- Optimized catalytic enantioselective aryl transfer process gives access to mGlu2 receptor potentiators
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An asymmetric enantioselective aryl transfer reaction was developed to give access to the diarylmethanol 7 and ultimately acetate 2 which is useful for the preparation of mGlu2 receptor potentiators (Scheme 3). The aryl transfer chemistry involved the pre
- Magnus, Nicholas A.,Anzeveno, Peter B.,Coffey, D. Scott,Hay, David A.,Laurila, Michael E.,Schkeryantz, Jeffrey M.,Shaw, Bruce W.,Staszak, Michael A.
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supporting information
p. 560 - 567
(2012/12/31)
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- Synthesis of photoactive α-mannosides and mannosyl peptides and their evaluation for lectin labeling
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Adhesion to the glycosylated surface of eukaryotic cells, mediated by lectins for example, plays an important role in inflammation and other cellular processes of living organisms. To elucidate the mechanisms involved in the adhesion to cell surfaces and
- Wiegand, Michaela,Lindhorst, Thisbe K.
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p. 4841 - 4851
(2007/10/03)
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- PREVENTIVE AND/OR THERAPEUTIC AGENT FOR NEUTROPHILIC INFLAMMATION DISEASE
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The present invention provides a preventive and/or therapeutic agent for neutrophilic inflammatory diseases which comprises, as an active ingredient, a bicyclic heterocyclic compound represented by formula (I): [wherein R 1 represents a hydrogen atom, substituted or unsubstituted alkyl, or the like, A 1 -A 2 -A 3 -A 4 represents N=CR 3 -CR 4 =CR 5 (wherein R 3 , R 4 , and R 5 are the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, and the like), Q represents substituted or unsubstituted phenylene, and the like, and T represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aroyl, and the like].
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Page/Page column 65-66
(2010/11/24)
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- Synthesis and characterization of photo-cross-linkable hole-conducting polymers
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The synthesis and characterization of side-chain polymers functionalized with hole-transporting units and photo-cross-linkable groups, which can be used for solution-based preparation of multilayer organic light-emitting devices (OLEDs), are discussed. The concept deals with triarylamine and oxetane-functionalized styrenes, which are copolymerized by radical polymerization. Four different types of hole-transporting monomers were combined with one cross-linkable monomer in two different ratios, yielding two groups of each four polymers (P1A...P4A and P1B...P4B). The polymers were investigated by NMR spectroscopy, molecular weights were determined by GPC with light scattering, and the thermal properties were measured with differential scanning calorimetry (DSC). Optical characterization by UV-vis and fluorescence spectroscopy was performed. Electrochemical and cross-linking characteristics of the copolymers were investigated to proove this strategy's potential in application for modern multilayer polymer OLEDs. Finally, hole-only devices were prepared for evaluation of the semiconductive performance of the materials.
- Bacher, Erwin,Bayerl, Michael,Rudati, Paula,Reckefuss, Nina,Mueller, C.David,Meerholz, Klaus,Nuyken, Oskar
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p. 1640 - 1647
(2007/10/03)
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- Vitamin D analogues
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The invention concerns novel bi-aromatic compounds having the formula: which are analogs of vitamin D, the process of preparing them, as well as their use in pharmaceutical compositions in human or veterinary medicine, particularly in dermatology, cancer treatment, treatment of auto-immune diseases, and in organ or tissue transplants. Cosmetic compositions and methods of use are also included.
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Page column 44
(2010/02/05)
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- Benzopyran or thiobenzopyran derivatives
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The present invention provides novel benzopyran compounds, pharmaceutically acceptable salts thereof and stereoisomers thereof where the benzopyran compounds of the invention are compounds according to Formula I: The present invention further provides pharmaceutical compositions which possess anti-estrogenic activity and comprise at least one benzopyran compound of the invention and a method of treating breast cancer by administration of an effective amount of a benzopyran compound provided by the present invention.
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Page/Page column 294
(2010/01/31)
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- A convergent asymmetric synthesis of a growth hormone secretagogue
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Described herein is a convergent asymmetric synthesis of growth hormone secretagogue (GHS) suitable for large-scale preparations. Key features include: (1) an improved method for α-iodination of a lactam; (2) a novel synthesis of a disubstituted urea usin
- Zheng, Nan,Armstrong III, Joseph D.,Eng, Kan K.,Keller, Jennifer,Liu, Tom,Purick, Robert,Lynch, Joseph,Hartner, Frederick W.,Volante
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p. 3435 - 3446
(2007/10/03)
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- Substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benzopyrans
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This invention is directed to substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benzopyrans that inhibit Factor Xa, pharmaceutical compositions comprising these compounds and their use for inhibiting Factor Xa or treating pathological conditions in a patient that may be ameliorated by administration of such compounds. This invention is also is also directed to substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benzopyrans which directly inhibit both Factor Xa and Factor IIa (thrombin), to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds and to a method of simultaneously directly inhibiting both Factor Xa and Factor IIa (thrombin).
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-
-
- Use of precipitons for copper removal in atom transfer radical polymerization [1]
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The use of precipitons for copper removal in atom transfer radical polymerization (ATRP) was discussed. Nitrogen ligands bearing precipitons were prepared and used to mediate ATRP. The results showed that the precipiton-bound ligands successfully mediated
- Honigfort, Mical E.,Brittain, William J.,Bosanac, Todd,Wilcox, Craig S.
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p. 4849 - 4851
(2007/10/03)
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- Fluorous-tethered amine bases for organic and parallel synthesis: Scope and limitations
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The synthesis of fluorous-tethered amine bases is described. These novel fluorous-tethered reagents promote reactions, remove acidic by-products, and scavenge electrophiles. They are readily separated from the reaction mixture by solid phase extraction on a novel mixed sorbent SPE (SCX/fluorous silica gel) delivering products in high yields and purities.
- Lindsley, Craig W,Zhao, Zhijian,Leister, William H,Strauss, Kimberly A
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p. 6319 - 6323
(2007/10/03)
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- Preparation and characterization of poly[2,3-dimethyl-1-(4-thien-3-ylbenzyl)-1H-imidazol-3-ium] bis((trifluoromethyl)sulfonyl)imide
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A new 3-fluorophenylthiophene derivative bearing a cationic imidazolium group in the para position of the phenyl ring was synthesized by a multistep procedure which involves, in a key step, the reaction of 3-[4-(bromomethyl)phenyl]thiophene with 1,2-dimet
- Naudin, Eric,Ho, Hoang Anh,Bonin, Marc-Andre,Breau, Livain,Belanger, Daniel
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p. 4983 - 4987
(2007/10/03)
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- A Novel Electroneutral Anion Host Based on Organoboron Betaines
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Host-guest binding of anions in organic solvents may find attractive applications in ion sensing and transport, if the host can extract the negatively charged guest species from its solvation sphere. The most powerful means to dismantle the anionic guest
- Cattani, Anna,Schmidtchen, Franz P.
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p. 291 - 296
(2007/10/03)
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- Orally active antimalarial 3-substituted trioxanes: New synthetic methodology and biological evaluation
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On the basis of a mechanistic understanding of the mode of action of artemisinin-like antimalarials, a series of structurally simple 3-aryl- 1,2,4-trioxanes 5 was designed and was prepared in three to five operations from commercial reactants. The 3-aryl group was attached in each case as a nucleophile. In an electronically complementary fashion, 3-(fluoroalkyl)- trioxanes 6 were prepared via attachment of electrophilic fluoroalkyl esters. Both in vitro and in vivo antimalarial evaluations of these new trioxanes showed 12β-methoxy-3-aryltrioxanes 5g, 5j, 5k, and 5l to be highly potent, with crystalline fluorobenzyl ether trioxane 5k especially potent even when administered to rodents orally. As shown by rearrangement of hexamethyl Dewar benzene into hexamethylbenzene, iron-induced degradation of some of these 3- aryltrioxanes 5 involves generation of high-valent iron oxo species that might kill malaria parasites.
- Posner, Gary H.
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p. 940 - 951
(2007/10/03)
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- Fibrinogen receptor antagonists
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Novel fibrinogen receptor antagonists of the formula: are provided in which the claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating thrombus formation.
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- Benzo-fused lactams promote release of growth hormone
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There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such bezno-fused lactams as the active ingredient thereof are also disclosed. STR1 where L is STR2
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- Photoinduced energy transfer in associated but noncovalently linked photosynthetic model systems
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The synthesis and photophysical characterization of nucleobase-substituted porphyrins designed to form rigid hydrogen-bonded ensembles, and to allow for energy transfer within the resulting complexes, is reported. Watson-Crick nucleobase-pairing interacti
- Sessler, Jonathan L.,Wang, Bing,Harriman, Anthony
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p. 704 - 714
(2007/10/02)
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- An efficient route to S-N-(9-fluorenylmethoxycarbonyl)-4′-(1-azi-2,2,2-trifluoroethyl) phenylalanine
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An extremely efficient synthesis of optically pure photoactivatable phenylalanine derivative 1 is described. The key step involves a highly diastereoselective alkylation of a chiral glycine equivalent.
- Fishwick, Colin W. G.,Sanderson, John M.,Findlay, John B. C.
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p. 4611 - 4614
(2007/10/02)
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- Synthesis of a fluorescent steroid derivative with high affinities for the glucocorticoid and progesterone receptors
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The synthesis of RU 45196, an 11β-substituted 19-norsteroid of the estra- 4,9-diene series, incorporating the nitrobenzoxadiazole (NBD) fluorophore, is reported. The highly fluorescent target compound displayed remarkable affinity for both the progesteron
- Teutsch, Georges,Klich, Michel,Bouchoux, Francoise,Cerede, Evelyne,Philibert, Daniel
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- Synthesis of 2,6-Diaryl-4H-thiopyran-4-ones
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A novel synthesis of 2,6-diaryl-4H-thiopyran-4-ones has been developed.The title compounds were prepared by two sequential thio-Claisen condensations of a dialkyl ketone and two dithioesters.The intermediate β-thioxo ketone from the first condensation was converted to the corresponding β-(methylthio)enone for both protection and reactivity purposes.Facile addition-elimination of the methylthio moiety by a β-thioxo ketone enolate generated in the second thio-Claisen condensation afforded the desired heterocycle.This new method is rapid and simple with the only requirement being moderate substituent alkaline stability.
- Boaz, Neil W.,Fox, Kristine M.
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p. 3042 - 3045
(2007/10/02)
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