- NOVEL COMPOUNDS AND THEIR USE
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The present invention provides compounds of the general formula (I) or a pharmaceutically acceptable prodrugs, salts and/or solvates thereof, wherein LHS is selected from the group consisting of LHSa and LHSb And wherein, the asterisk (*) marks the point of attachment; These compounds exhibit antibacterial activity against Gram-negative and Gram-positive bacteria, especially S. aureus, E. coli, K. pneumoniae and A. baumannii. Pharmaceutical compositions containing these compounds, therapeutic uses thereof and methods for manufacturing the same are also provided.
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Page/Page column 113-114
(2021/06/26)
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- Copper(II)-Catalyzed Tandem Reaction: Synthesis of Furo[3,2- c]coumarin Derivatives and Evaluation for Photophysical Properties
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An efficient protocol for synthesizing furo[3,2-c]coumarin derivatives is described. The novel reaction could afford the desired furocoumarins with good to excellent yields in a mild and rapid manner. Large substrate scope screening and scale-up preparation have also been accomplished, and selected compounds were evaluated for their photophysical properties.
- Feng, Xi,Qin, Zhen,Cheng, Xinying,Liu, Dongyu,Peng, Yinghe,Huang, Huidan,Song, Bin,Bian, Jinlei,Li, Zhiyu
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supporting information
p. 12537 - 12548
(2021/09/20)
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- Design, synthesis, and biological activity of a novel series of benzofuran derivatives against oestrogen receptor-dependent breast cancer cell lines
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A docking study of a novel series of benzofuran derivatives with ERα was conducted. In this study, we report the synthesis of a novel series of benzofuran derivatives and evaluation of their anticancer activity in vitro against MCF-7 human breast cancer cells, as well as their potential toxicity to ER-independent MDA-MB-231 breast cancer cells, human renal epithelial HEK-293 cells, and human immortal keratinocytes (HaCaT cells) by using the MTT colorimetric assay. The screening results indicated that the target compounds exhibited anti-breast cancer activity. The target compound 2-benzoyl-3-methyl-6-[2-(morpholin-4-yl)ethoxy]benzofuran hydrochloride (4e) exhibited excellent activity against anti-oestrogen receptor-dependent breast cancer cells and low toxicity. The preliminary structure-activity relationships of the target benzofuran derivatives have been summarised. In conclusion, the novel benzofuran scaffold may be a promising lead for the development of potential oestrogen receptor inhibitors.
- Hu, Chun,Hu, Jian-Shu,Huang, Er-Fang,Jin, Li-Ping,Jin, Zhe,Wan, David Chi-Cheong,Wang, Lin,Xie, Qian,Zhang, Bing-Qi
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- CLASS OF BIFUNCTIONAL COMPOUNDS WITH QUATERNARY AMMONIUM SALT STRUCTURE
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The invention provides a class of compounds represented by formula (I), having bifunctional active quaternary ammonium salt structure of a β2-adrenoreceptor agonist and an M receptor antagonist, a pharmaceutically acceptable salt, solvate, and optical isomer thereof. A pharmaceutical composition comprising such a compound with quaternary ammonium salt structure, a method for preparing such a compound with quaternary ammonium salt structure and an intermediate thereof, and uses thereof in treating pulmonary disorders are also provided. The compounds of the invention have high selectivity to the M receptor subtype, and have less adverse reaction and lower toxic and side effects in the treatment of pulmonary diseases such as COPD and asthma.
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Paragraph 0168
(2019/11/11)
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- 5-[2-hydroxy-3-(alkylamine) propoxy] benzofuran compound and application thereof
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The invention belongs to the technical field of medicines and relates to a 5-[2-hydroxy-3-(alkylamine) propoxy] benzofuran compound and the application thereof. The 5-[2-hydroxy-3-(alkylamine) propoxy] benzofuran compound comprises a stereisomer of the compound and pharmaceutically applicable salt; the general molecular formula of the compound is shown as follows: wherein R is described as the claims and the specification. The 5-[2-hydroxy-3-(alkylamine) propoxy] benzofuran compound and the pharmaceutically applicable acid addition salt of the compound can be combined with the existing drug for use or can be used alone, and are used for preparing a drug for treating a vascular smooth muscle spastic disease.
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Paragraph 0036; 0044; 0045
(2018/04/21)
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- 5-[2-hydroxy-3-(isopropylamino)propoxy]benzofuran derivatives and application thereof
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The invention belongs to the technical field of medicines, and relates to 5-[2-hydroxy-3-(isopropylamino)propoxy]benzofuran derivatives and an application thereof. The 5-[2-hydroxy-3-(isopropylamino)propoxy]benzofuran derivatives comprise stereoisomers and pharmaceutically acceptable salts of 5-[2-hydroxy-3-(isopropylamino)propoxy]benzofuran, and the structural formula of the derivatives is shownin the description. The 5-[2-hydroxy-3-(isopropylamino)propoxy]benzofuran derivatives and the pharmaceutically acceptable acid addition formed salts of 5-[2-hydroxy-3-(isopropylamino)propoxy]benzofuran can be used together with existing medicines or individually, and are used for preparing medicines for treating blood vessel smooth muscle spasm diseases.
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Paragraph 0036; 0037; 0038
(2018/06/15)
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- One-pot two-step synthesis of 3-iodo-4-aryloxy coumarins and their Pd/C-catalyzed annulation to coumestans
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An efficient protocol for the synthesis of various coumestans from the intramolecular annulation of 3-iodo-4-aryloxy coumarins through C-H activation has been developed. When 3-iodo-4-aryloxy coumarins were treated with 10% Pd/C (0.3 mol% Pd) in the presence of sodium acetate, the corresponding coumestans were produced in good to excellent yield. Reusability of the palladium catalyst was investigated in up to three consecutive cycles and it was found that the yield of the reaction was almost unaltered. Sequential iodination and O-arylation of 4-hydroxy coumarins leading to the 3-iodo-4-aryloxy coumarins were also achieved in a one-pot two-step process starting from aryl iodides in high yield. Pivalic acid was revealed to be the most effective additive for the later method to produce 3-iodo-4-phenoxy coumarins. Different functional groups bearing electron-donating as well as withdrawing groups are also tolerant to the reaction conditions.
- Panda, Niranjan,Mattan, Irshad
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p. 7716 - 7725
(2018/03/01)
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- COMPOUNDS AND METHODS FOR INHIBITING EMT PATHWAYS TO TREAT CANCER, ORGAN FIBROSIS AND METABOLIC DISORDERS
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A compound, or a pharmaceutically acceptable salt or isomer thereof, of Formula I: wherein R is hydrogen, alkyl, substituted alkyl, alkenyl, or substituted alkenyl; R1 is hydrogen, alkoxy, or substituted alkoxy; R2 is hydrogen, alkyl, or substituted alkyl; and R3 is hydrogen, alkyl, or substituted alkyl.
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Page/Page column 22; 23
(2018/09/19)
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- Benzoxazine compound and its preparation methods and application
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The invention relates to a benzoxazine compound represented in the following formula 1. The benzoxazine compound can serve as a beta 2 receptor agonist. The formula can be seen from the description.
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Paragraph 0051; 0056; 0057
(2017/10/07)
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- The synthesis and evaluation of flavone and isoflavone chimeras of novobiocin and derrubone
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The natural products novobiocin and derrubone have both demonstrated Hsp90 inhibition and structure-activity relationships have been established for each scaffold. Given these compounds share several key structural features, we hypothesized that incorporation of elements from each could provide insight to structural features important for Hsp90 inhibition. Thus, chimeric analogues of novobiocin and derrubone were constructed and evaluated. These studies confirmed that the functionality present at the 3-position of the isoflavone plays a critical role in determining Hsp90 inhibition and suggests that the bicyclic ring system present in both novobiocin and derrubone do not share similar modes of binding.
- Mays, Jared R.,Hill, Stephanie A.,Moyers, Justin T.,Blagg, Brian S.J.
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experimental part
p. 249 - 266
(2010/04/05)
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- PROCESS FOR THE MANUFACTURING OF BETA MIMETICS
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The invention relates to a method for producing betamimetics of formula (1), wherein in which n represents 1 or 2; R1 represents hydrogen, halogen, C1-4-alkyl or O—C1-4-alkyl; R2 represents hydrogen, halogen, C
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Page/Page column 5-6
(2010/02/17)
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- Discovery of olodaterol, a novel inhaled β2-adrenoceptor agonist with a 24 h bronchodilatory efficacy
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Compound 4p was identified from a series of 6-hydroxy-4H-benzo[1,4]oxazin-3-ones as potent agonist of the human β2-adrenoceptor with a high β1/β2-selectivity. A complete reversal of acetylcholine-induced bronchoconstrictio
- Bouyssou, Thierry,Hoenke, Christoph,Rudolf, Klaus,Lustenberger, Philipp,Pestel, Sabine,Sieger, Peter,Lotz, Ralf,Heine, Claudia,Büttner, Frank H.,Schnapp, Andreas,Konetzki, Ingo
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scheme or table
p. 1410 - 1414
(2010/07/10)
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- Synthesis and evaluation of [2-(4-quinolyloxy)phenyl]methanone derivatives: Novel selective inhibitors of transforming growth factor-β kinase
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We synthesized and evaluated various [2-(4-quinolyloxy)phenyl]methanone derivatives. These compounds had novel chemical structures that were distinct from those of previously reported inhibitors. Biological data suggested that these compounds inhibited transforming growth factor-β signaling by interacting with the ATP-binding pocket of the transforming growth factor-β type I receptor kinase domain. Here, we report on the synthesis and structure-activity relationships of the compounds in this series.
- Shimizu, Toshiyuki,Kimura, Kaname,Sakai, Teruyuki,Kawakami, Kazuki,Miyazaki, Tetsuko,Nakouji, Masayoshi,Ogawa, Akira,Ohuchi, Hitomi,Shimizu, Kiyoshi
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supporting information; experimental part
p. 3326 - 3329
(2009/04/06)
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- PROCESS FOR THE MANUFACTURING OF BETAMIMETICS
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The present invention relates to a process for preparing betamimetics of formula 1, wherein n denotes 1 or 2; R1 denotes hydrogen, halogen, C1-4-alkyl or O—C1-4-alkyl; R2 denotes hydrogen, halogen, C1-4/su
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Page/Page column 10-11
(2008/06/13)
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- Structure-activity relationships of a novel class of endothelin-A receptor antagonists and discovery of potent and selective receptor antagonist, 2-(benzo[1,3]dioxol-5-yl)-6-isopropyloxy-4- (4-methoxyphenyl)-2H-chromene-3-carboxylic acid (S-1255). 1. Study on structure-activity relationships and basic structure crucial for ETA antagonism
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A novel series of endothelin-A (ETA) selective receptor antagonists having a 2H-chromene skeleton are described. A lead compound, 2-(benzo[1,3] dioxol-5-yl)-2H-chromene-3-carboxylic acid (3), was found by modifications of our own angiotensin II antagonist. A structure-activity relationship (SAR) study of 3 reveals that the structural requirements essential for potent and selective ETA receptor binding affinity are the m,p-methylenedioxyphenyl, carboxyl, and isopropoxy groups at the 2-, 3-,and 6-positions, respectively, on the (R)-2H-chromene skeleton. The substituent at the 4-position is also important for improving the activity, and various hydrophobic functional groups of 6-9 ? such as liner, branched, and cyclic aliphatic groups, unsubstituted and substituted aryl groups, and even halogen atoms were acceptable. These results suggest that (R)-2-(benzo[1,3]dioxol-5-yl)-6-isopropoxy-2H-chromene-3-carboxylic acid, formula 108, is the crucial basic structure to be recognized by the ETA receptor. The most potent compound is (R)-48 (S-1255), which binds to the ETA receptor with an IC50 value of 0.19 nM and is 630-fold selective for the ETA receptor than for the ETB receptor. This compound has 55% oral bioavailability in rats. On the basis of the SAR, the roles of each substituent in the receptor binding are discussed.
- Ishizuka, Natsuki,Matsumura, Ken-Ichi,Sakai, Katsunori,Fujimoto, Masafumi,Mihara, Shin-Ichi,Yamamori, Teru
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p. 2041 - 2055
(2007/10/03)
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- Chromene-3-carboxylate derivatives
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The present invention provides a compound of the formula (I): wherein R1, R2, R3and R4are each independently hydrogen, optionally substituted alkyl, hydroxy, optionally substituted alkoxy or the like, R5/s
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- The asymmetric synthesis of 2-benzopyrans and their quinones through intramolecular diastereoselective ring-closure of titanium phenolates of phenolic aldehydes
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Treatment of the phenolic aldehyde (a′5,25)-2-(5′-hydroxy-2′-methoxy-a′-methylbenzyloxy) propanal 15 with titanium tetraisopropoxide followed by ultrasonication led to its completely diastereoselective cyclisation in high yield to afford (lS,3S′,4.R)-3,4-
- Giles, Robin G. F.,Joli, Cynthia A.
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p. 3039 - 3048
(2007/10/03)
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- Alkylbenzyl ethers of hydroquinones as monoamine oxidase B inhibitors
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A series of alkylbenzylethers of substituted hydroquinone analogs of 4-(3-chlorophenyl methyloxy)-phenoxybutyronitrile I, and alcohol II were synthesized as monoamine oxidase (MAO) inhibitors. Incorporation of electron-withdrawing groups on the hydroquinone afforded compounds with higher levels of activity and selectivity than I or II for MAO B inhibition.
- Arvanitis, Argyrios G.,Scholfield, Everett L.,Grigoriadis, Dimitri,Heytler, Peter G.,Bowdle, Jack,Chorvat, Robert J.
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p. 115 - 120
(2007/10/03)
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- Substituted 1-[3-(heteroarylmethoxy)phenyl]alkanols and related compounds in the treatment of asthma
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Substituted 1-[3-(heteroarylmethoxy)phenyl]-alkanols and related compounds which, by inhibiting 5-lipoxygenase enzyme and/or blocking leukotriene receptors, are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction, stroke and related disease states in mammals; pharmaceutical compositions thereof; and a method of treatment therewith.
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- Substituted 2-alkynylphenols with anti-inflammatory action, a process for their preparation and pharmaceutical compositions thereof
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There are described new compounds of formula wherein, R and R1 are chosen independently from: hydrogen, hydroxyl, halogen, (C1 - C6) alkyl, (C1 - C4) alkoxy, benzyloxy, -COOR4;, R2 is : hydrogen, hydr
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- Studies on the metabolism of propafenone. 1st comm.: Synthesis and chromatographic/mass spectrometric properties of the labelled compound and of the reference substances
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The synthesis of 14C-propafenone and 2H-propafenone (propafenone: 2-(2'-hydroxy-3'-propylamino-propoxy)-ω-phenyl-propiophenone hydrochloride) and some reference compounds is described. The thin-layer chromatographic, high-performance liquid and gas chromatographic properties of the substances are described. Propafenone and the reference substances were studied by mass spectrometry and compared with each other, with respect to structural elucidation of the metabolites. The chromatographic and mass spectrometric data (key ions) enables the metabolites of propafenone to be identified in biological material.
- Hege,Weymann,Lietz
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p. 843 - 849
(2007/10/02)
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