- Synthesis and antileukemic activity of 16E-[4-(2-carboxy)ethoxybenzylidene] -androstene amides
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In order to determine the structural requirements for cytotoxicity against various tumor cell lines, a new series of 16E-arylidene androstene amides with varying degrees of unsaturation in ring A has been synthesized. Characterization and in vitro cytotox
- Bansal, Ranju,Acharya, Pratap Chandra
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Read Online
- Phosphatase Binding Compounds and Methods of Using Same
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The present invention provides bifunctional compounds that efficiently dephosphorylate certain phospho-activated target proteins. Such target proteins can be any protein involved in the pathway of a disease or disorder, such as but not limited to cancer, neurodegeneration, metabolic disease, diabetes, insulin resistance, and so forth.
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Page/Page column 232; 251-252
(2020/07/25)
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- INHIBITORS OF SHORT-CHAIN DEHYDROGENASE ACTIVITY FOR PROMOTING NEUROGENESIS AND INHIBITING NERVE CELL DEATH
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A method of promoting neuroprotection in a subject from axonal degeneration, neuronal cell death, and/or glia cell damage after injury, augmenting neuronal signaling underlying learning and memory, stimulating neuronal regeneration after injury, and/or treating a disease, disorder, and/or condition of the nervous system in a subject in need thereof includes administering to the subject a therapeutically effective amount of a 15-PGDH inhibitor.
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Paragraph 00285
(2018/02/27)
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- Boosting Self-Assembly Diversity in the Solid-State by Chiral/Non-Chiral ZnII-Porphyrin Crystallization
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A chiral ZnII porphyrin derivative 1 and its achiral analogue 2 were studied in the solid state. Considering the rich molecular recognition of designed metalloporphyrins 1 and 2 and their tendency to crystallize, they were recrystallized from t
- Qian, Wenjie,González-Campo, Arántzazu,Pérez-Rodríguez, Ana,Rodríguez-Hermida, Sabina,Imaz, Inhaz,Wurst, Klaus,Maspoch, Daniel,Ruiz, Eliseo,Ocal, Carmen,Barrena, Esther,Amabilino, David B.,Aliaga-Alcalde, Núria
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supporting information
p. 12950 - 12960
(2018/08/11)
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- INHIBITORS OF SHORT-CHAIN DEHYDROGENASE ACTIVITY FOR TREATING FIBROSIS
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A method of treating or preventing a fibrotic disease, disorder or condition includes administering to a subject in need of treatment a 15-PGDH inhibitor.
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Paragraph 00296
(2016/09/26)
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- A process for the preparation of intermediates palestinian multi-past fragrance acetate
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The invention discloses a method for preparing a bazedoxifene acetate intermediate. The preparation method comprises the following steps: 1, condensing 4-hydroxybenzaldehyde S01 and alkylate S02 to prepare a 4-formyl phenoxy derivative M01; 2, performing
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Paragraph 0100-0103
(2017/01/31)
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- Synthesis and pharmacological characterization of novel xanthine carboxylate amides as A2A adenosine receptor ligands exhibiting bronchospasmolytic activity
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The carboxylate amides of 8-phenyl-1,3-dimethylxanthine described herein represent a new series of selective ligands of the adenosine A2A receptors exhibiting bronchospasmolytic activity. The effects of location of 8-phenyl substitutions on the
- Yadav, Rakesh,Bansal, Ranju,Rohilla, Suman,Kachler, Sonja,Klotz, Karl-Norbert
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- COMPOSITIONS AND METHODS OF MODULATING SHORT-CHAIN DEHYDROGENASE ACTIVITY
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Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors described herein.
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Paragraph 00490
(2015/05/19)
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- Selection and development of a route for cholesterol absorption inhibitor AZD4121
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The development of a synthetic route to the cholesterol absorption inhibitor AZD4121 is presented. Key steps are a highly enantioselective CBS reduction, a stereospecific Staudinger reaction, an amine/lithium chloride mediated ester hydrolysis, and a resolution of a 50:50 diastereomeric mixture by recrystallization. The synthesis was accomplished in 10 linear steps, and the overall yield, when compared with the lead optimization (LO) route, was improved from 1% to 20%. All purifications of intermediates through preparative HPLC or silica gel chromatography were avoided. This was possible since many of the intermediates along the route could be used as such in the next step until an intermediate with suitable crystalline properties could be identified and purified through crystallization.
- Karlsson, Staffan,Soerensen, J. Henrik
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experimental part
p. 586 - 594
(2012/07/03)
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- Synthesis of pH-activatable red fluorescent BODIPY dyes with distinct functionalities
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A series of tunable pH-dependent BODIPY dyes were synthesized and further functionalized in a Knoevenagel condensation reaction with various aldehydes. In this fashion, monofunctional dyes containing an alkyne, azide, or carboxylic acid (masked as its met
- Hoogendoorn, Sascha,Blom, Annet E. M.,Willems, Lianne I.,Van Der Marel, Gijsbert A.,Overkleeft, Herman S.
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supporting information; experimental part
p. 5656 - 5659
(2011/12/04)
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- Discovery of histone deacetylase 8 selective inhibitors
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We have developed an efficient method for synthesizing candidate histone deacetylase (HDAC) inhibitors in 96-well plates, which are used directly in high-throughput screening. We selected building blocks having hydrazide, aldehyde and hydroxamic acid functionalities. The hydrazides were coupled with different aldehydes in DMSO. The resulting products have the previously identified 'cap/linker/biasing element' structure known to favor inhibition of HDACs. These compounds were assayed without further purification. HDAC8-selective inhibitors were discovered from this novel collection of compounds.
- Tang, Weiping,Luo, Tuoping,Greenberg, Edward F.,Bradner, James E.,Schreiber, Stuart L.
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supporting information; experimental part
p. 2601 - 2605
(2011/06/22)
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- Novel Compounds
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The present invention provides compounds of formula (I): wherein Ra, Rb, Rc, R1, R2, R3, X1, Y1, Z1, A, n and m are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
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Page/Page column 33
(2011/06/24)
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- Flexible porphyrin tetracarboxylic acids for crystal engineering
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Tetrakis[4-(carboxymethyleneoxy)phenyl]porphyrin, a flexible tetraacid ligand, is a new attractive building block for the formulation of coordination polymers and hydrogen bonding supramolecular assemblies in the solid state.
- Karmakar, Anirban,Goldberg, Israel
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body text
p. 4095 - 4100
(2011/06/26)
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- Synthesis and biological evaluation of novel 4-hydroxybenzaldehyde derivatives as tyrosinase inhibitors
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A series of novel 4-hydroxybenzaldehyde derivatives were synthesized and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were investigated. Most of target compounds had more potent inhibitory activities than the parent compound 4-hydroxybenzaldehyde (IC50 = 1.22 mM). Interestingly, compound 3c bearing a dimethoxyl phosphate was found to be the most potent inhibitor with IC50 value of 0.059 mM. The inhibition kinetics analyzed by Lineweaver-Burk plots revealed that compound 3c was a non-competitive inhibitor (KI = 0.0368 mM). In particular, compound 3c showed no side effects at dose of 1600 mg/kg in mice. These results suggested that such compounds might be served as lead compounds for further designing new potential tyrosinase inhibitors.
- Yi, Wei,Cao, Rihui,Peng, Wenlie,Wen, Huan,Yan, Qin,Zhou, Binhua,Ma, Lin,Song, Huacan
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scheme or table
p. 639 - 646
(2010/04/02)
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- FUNCTIONALIZED PHENOLIC COMPOUNDS AND POLYMERS THEREFROM
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The present invention relates to compounds of formula I, which are functionalized phenolic compounds, and polymers formed from the same. Ar—[O—(X)p—R′]q??I Polymers formed from the functionalized phenolics are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
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Page/Page column 28
(2009/07/17)
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- RADIATION-SENSITIVE COMPOSITION
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A radiation-sensitive composition containing a resist compound having a high sensitivity, a high resolution, a high etching resistance, and a low outgas which forms a resist pattern with a good shape is described. Further described is a method of forming a resist pattern using the radiation-sensitive composition. Still further described are a novel composition for forming a photoresist under coat film which is excellent in optical properties and etching resistance and contains substantially no sublimable substance and an under coat film formed by the composition. Still further described are a radiation-sensitive composition containing a solvent and a cyclic compound having a specific structure, for example, a cyclic compound (A) having a molecular weight of 700 to 5000 which is synthesized by the condensation reaction of a compound having 2 to 59 carbon atoms and 1 to 4 formyl groups (aldehyde compound (A1)) with a compound having 6 to 15 carbon atoms and 1 to 3 phenolic hydroxyl groups (phenol compound (A2)), and a cyclic compound for use in the radiation-sensitive composition.
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Page/Page column 112
(2009/08/14)
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- Conformationally restricted dipyrromethene boron difluoride (BODIPY) dyes: Highly fluorescent, multicolored probes for cellular imaging
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Novel fluorescent, conformationally restricted dipyrromethene boron difluoride (BODIPY) dyes have been prepared by introducing a naphthalenyl group at the meso position of the BODIPY core. These BODIPY dyes exhibit increased fluorescence quantum yields co
- Zheng, Qingdong,Xu, Gaixia,Prasad, Paras N.
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experimental part
p. 5812 - 5819
(2009/06/05)
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- Heterocyclic analogs of prostaglandines: IV. Synthesis of 3,7-interphenylene 3,10(11)-dioxa-13-azaprostanoids and 9-oxa-7-azaprostanoids based on tetronic acid and aromatic aldehydes
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An approach was developed to the synthesis of stable in metabolism 3,7-interphenylene 3,10-dioxa-13-aza-and 3,11-dioxa-13-azaprostanoids, and also 9-oxa-7-azaprostanoids with interphenylene and terminal phenyl fragments in the ω-chain based on 3-(alkoxybenzylidene)-and 3-(3-phenylallylidene) tetrahydrofuran-2,4-diones obtained by Knoevenagel condensation of tetronic acid with alkoxy-substituted aromatic aldehydes and cinnamic aldehyde.
- Pashkovskii,Shchukina,Gribovskii,Lakhvich
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experimental part
p. 657 - 670
(2009/04/07)
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- Methyl 2-(2-(4-formylphenoxy)acetamido)-2-substituted acetate derivatives: A new class of acetylcholinesterase inhibitors
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A new class of inhibitors of acetylcholinesterase (methyl 2-(2-(4-formylphenoxy)acetamido)-2-substituted acetate derivatives) is described. Compounds 4b and 4i were found to be more potent than galanthamine in inhibiting acetylcholinesterase.
- Wen, Huan,Zhou, Yayao,Lin, Chonglan,Ge, Hui,Ma, Lin,Wang, Zihou,Peng, Wenlie,Song, Huacan
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p. 2123 - 2125
(2008/02/03)
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- Raf inhibitor compounds and methods of use thereof
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Compounds of Formula I are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formula I, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
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Page/Page column 25
(2008/06/13)
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- ARYL DICARBOXAMIDES
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The present invention is related to aryl dicarboxamides of formula (I) and use thereof for the treatment and/or prevention of obesity and/or metabolic disorders mediated by insulin resistance or hyperglycernia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholes-terolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of aryl dicarboxamides of formula (I) to modulate, notably to inhibit the activity of PTPs. A is an airninocarbonyl moiety; Cy is an aryl, heteroaryl, aryl-heteroaryl, heteroaryl-aryl, aryl-aryl, cycloalkyl or heterocycle group; n is either 0 or 1; R1 and R2 are independently from each other is selected from the group consisting of hydrogen or C1-C6-alkyl; R4 and R5 are each independently from each other selected from the group consisting of H, hydroxy, C1-C6 alkyl, carboxy, C1-C6 alkoxy, C1-C3 alkyl carboxy, C2-C3 alkenyl carboxy, C2-C3 alkynyl carboxy, amino or R4 and R5 may form an unsaturated or saturated heterocyclic ring, whereby at least one of R4 or R5 is not a hydrogen or C1-C6 alkyl.
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Page/Page column 43-44
(2010/02/10)
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- ALKYNYL ARYL CARBOXAMIDES
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The present invention is related to alkynyl aryl carboxamides of Formula (I’) and use thereof for the treatment and/or prevention of an inflammatory disorder, obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance. insulin resistance, hyperlipidemia, hypertriglyceridemia- hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of alkynyl aryl carboxamides of Formula (I’) to modulate, notably to inhibit the activity of PTPs. (I’) A is a C2-C15 alkynyl, C2-C6-alkynyl aryl, C2-C6-alkynyl heteroaryl. Cy is an aryl, heteroaryl, cycloalkyl or heterocycle group; n is either 0 or 1. Cy' is an aryl., which may optionally be fused by a 3-8 membered cycloalkyl. R1and R2 are independently from each other is selected from the group consisting of hydrogen or (CI-C6)alkyl. R4and R5 are each independently from each other selected from the group consisting of H, hydroxy. C1 -C6 alkyl, carboxy, C1-C6 alkoxy, C1 -C3 alkyl carboxy, C2-C3 alkenyl carboxy, C2-C3 alkynyl carboxy, amino or R4 and R5 may form an unsaturated or saturated heterocyclic ring, whereby at least one of R4 or R5 is not a hydrogen or C1-C6 alkyl.
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Page/Page column 48-49
(2008/06/13)
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- Microwave-Accelerated SPOT-synthesis on cellulose supports
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Equation presented. We demonstrate that microwave irradiation can dramatically accelerate reaction rates for spatially addressable library synthesis on planar membrane supports. The development of a robust support/linker system, microwave-assisted synthesis of small molecule test libraries, and methods for solid-phase scale-up on cellulose are described.
- Bowman, Matthew D.,Jeske, Ryan C.,Blackwell, Helen E.
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p. 2019 - 2022
(2007/10/03)
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- Process for the preparation of thiazolidine-2,4-dione derivatives
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An improved process for the preparation of 5-[4-[[3-Methyl-4-oxo-3,4-dihydroquinazolin-2-yl]methoxy]benzyl]thiazolidine-2,4-dione of formula (1) which comprises: reducing the compound of formula (2′) where R represents a (C1-C4)alkyl
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- Synthesis and in vitro evaluation of a series of diketopiperazine inhibitors of plasminogen activator inhibitor-1
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We have synthesized and evaluated a series of diketopiperazine-based inhibitors of PAI-1. These studies resulted in the identification of 34 which inhibited PAI-1 in vitro with an IC50 = 0.2 μM. The synthesis and SAR of these compounds are desc
- Folkes, Adrian,Roe, Michael B.,Sohal, Sukhjit,Golec, Julian,Faint, Richard,Brooks, Teresa,Charlton, Peter
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p. 2589 - 2592
(2007/10/03)
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- Designing of resorcinol-p-hydroxybenzaldehyde tetramer for uranophilic activity
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Resorcinol-p-hydroxybenzaldehyde tetramer (1) has been obtained under acidic conditions, separated into its conformations and characterized by 1H NMR and 13C NMR spectra and through the preparation of its octaacetate. The direct carboxymethylation of 1 has been attempted with chloroacetic acid under basic conditions but due to steric repulsions, the tetramer 2a could not be obtained. Using the reverse approach p-hydroxybenzaldehyde is carboxymethylated first to get 6 which is then cyclized under acidic conditions to yield the tetramer 2b. Compound 2a has been characterized as its acetylated ethyl ester 3 by 1H NMR spectral data and elemental analysis. The two conformations of 3 have been separated by repeated recrystallization from acetonitrile and their purity has been checked by 1H NMR spectra. The tetramer 2a is obtained by hydrolysis of 3 with NaOH (1N). The coplanar arrangement of carboxylate groups in 2a is utilized to bind uranyl ion. The binding as shown by Job's plot does not show 1:1 (2a: UO22+) ratio due to fourth carboxylate group, but it acts as a good uranophile as indicated by an increase in the intensity of UO22+ ions in UV absorption in the presence of 3.
- Singh, Harmit,Singh, Serjinder
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p. 409 - 412
(2007/10/03)
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- Porphyrin synthesis in surfactant solution: Multicomponent assembly in micelles
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A synthesis of meso-substituted porphyrins in anionic sodium dodecyl sulfate micelles has been developed. Polar, functionalized aromatic aldehydes condense reversibly with pyrrole in the micellar phase. Oxidation of the porphyrinogen then provides functionalized porphyrins in yields of 10-48%. Hydrophobic aldehydes condense irreversibly to give low yields at practical substrate concentrations. Synthesis in D2O solution results in per-β-deuterated porphyrins. A two-phase model is used to rationalize the dependence of porphyrin yield on reactant and surfactant concentration. Micelles are viewed as potential wells which promote porphyrinogen assembly by binding products more tightly than reactants.
- Bonar-Law, Richard P.
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p. 3623 - 3634
(2007/10/03)
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- Synthesis of Aryloxy Analogues of Arachidonic Acid via Wittig and Palladium Catalysed Cross-coupling Reactions
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The synthesis of o- and p-phenoxy analogues of arachidonic acid is described.In particular, the Wittig olefination reaction of hydroxy and alkyloxy benzaldehydes has been investigated and the products shown to be highly dependent on the solvent used.E/Z isomer control was difficult to achieve in most cases, although there was a tendency towards Z-isomer formation in dimethyl sulphoxide compared to tetrahydrofuran, particularly for the phenolic compounds.Specific Z-isomer formation was achieved by the partial reduction of alkynes derived from appropriately protected bromophenols via Heck or palladium catalysed cross-coupling reactions.
- Buckle, Derek R.,Fenwick, Ashley E.,Outred, D. James,Rockell, Caroline J. M.
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p. 3144 - 3177
(2007/10/02)
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- Novel compounds
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A compound of formula (I): STR1 or a salt, ester or amide thereof, in which Y is a group --O(CH2)m --, --(CH2)m -- or --CH=CH-- where m is an integer of from 1 to 5 n is an integer of from 4 to 14 X represents a double or triple bond, and each of A and B represents hydrogen when X is a double bond, or both A and B are absent when X is a triple bond, is useful in the treatment of allergic diseases.
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