- Electricity Driven 1,3-Oxohydroxylation of Donor-Acceptor Cyclopropanes: a Mild and Straightforward Access to β-Hydroxy Ketones
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An unprecedented external oxidant-free electrochemical protocol for 1, 3-oxohydroxylation of donor-acceptor cyclopropane is disclosed. The strategy encompasses the activation of the labile π-electron cloud of the aryl ring to cleave the strained Csp3?Csp3 bond of cyclopropane to afford the β-hydroxy ketones via insertion of molecular oxygen. More significantly, based on the detailed mechanistic investigations and cyclic voltammetry experiments, a plausible mechanism is proposed.
- Banerjee, Prabal,Maajid Taily, Irshad,Saha, Debarshi
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supporting information
p. 5053 - 5057
(2021/09/30)
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- Amide compound and pharmaceutical composition containing same and preparation method of amide compound and application of amide compound or pharmaceutical composition
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The invention relates to an amide compound of a formula (I) shown in the description, a pharmaceutical composition containing with the same, a preparation method of the amide compound and applicationof the amide compound or the pharmaceutical composition, and specifically, the amide compound or the pharmaceutical composition can be used to prevent or treat retinoic acid receptor related orphan nuclear receptor gamma (ROR[gamma]) mediated diseases or symptoms.
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Paragraph 0283; 0284; 0285; 0286
(2020/02/14)
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- Preparation method of methyl 5-formyl-2-methoxybenzoate
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The invention discloses a preparation method of methyl 5-formyl-2-methoxybenzoate. The preparation method comprises following steps: (1), preparation of methyl-2-methoxybenzoate; (2), preparation of methyl 5-formyl-2-methoxybenzoate. With the adoption of the method for loading an aldehyde group by urotropine after ester formation, the total yield can be increased to about 90%, the utilization rateof the raw materials is greatly increased, the cost is low, the operation is simple and convenient, and industrialization is facilitated.
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Paragraph 0038; 0040; 0042; 0044
(2019/01/16)
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- Synthesis and biological activity of 5-(4-methoxyphenyl)-oxazole derivatives
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5-(4′-Methoxyphenyl)-oxazole (MPO), originally reported as a synthetic compound, was isolated from fungal culture broth as an inhibitor of hatch and growth of Caenorhabditis elegans. Nineteen MPO derivatives were chemically synthesized, but showed no effect on C. elegans hatch and growth. These findings strongly suggested that the whole structure of MPO is essential for anti-C. elegans activity.
- Yamamuro, Daisuke,Uchida, Ryuji,Ohtawa, Masaki,Arima, Shiho,Futamura, Yushi,Katane, Masumi,Homma, Hiroshi,Nagamitsu, Tohru,Osada, Hiroyuki,Tomoda, Hiroshi
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supporting information
p. 313 - 316
(2015/04/13)
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- SPIRO-SUBSTITUTED OXINDOLE DERIVATIVES HAVING AMPK ACTIVITY
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The present invention relates to compounds of formula (I), which have valuable pharmacological properties, in particular are activators of AMPK and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
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- OLEFIN SUBSTITUTED OXINDOLES HAVING AMPK ACTIVITY
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The present invention relates to compounds of formula (I), which have valuable pharmacological properties, in particular are activators of AMPK and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
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- 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOL DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS
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Compounds of formula (I) described herein are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and are useful for the prevention and/or treatment of an allergic disease state or a disease of the respiratory tract characterized by airway obstruction.
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- SHORT ACTING PHENYLALKYLAMINE CALCIUM CHANNEL BLOCKERS AND USES THEREOF
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The present invention relates to the use of a pharmaceutically effective amount of an short-acting calcium channel blocking compound to treat ischemic heart conditions, cardiac arrhythmias, hypertensive crisis in an emergency room setting, hypertension before, during, or after surgery, no- reflow phenomenon following reperfusion, and diseases associated with decreased skeletal muscle blood flow. The invention also relates to pharmaceutical compositions formulated for use in such methods and to kits for such methods.
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Page/Page column 61
(2009/01/23)
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- Polyfluorinated bis-styrylbenzene β-amyloid plaque binding ligands
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β-Amyloid (Aβ) binding affinities and specificities for six bis-styrylbenzenes with multiple magnetically equivalent fluorine atoms in the form of a tetrafluorophenyl core or symmetrical trifluoromethyl and trifluoromethoxy groups were determined by means of fluorescence titrations with amyloid peptide Aβ1-40 and a novel in vitro fluorescence-based assay using APP/PS1 transgenic mouse brain sections. Bisstyrylbenzenes with a tetrafluorophenyl core had increased Aβ binding affinities compared to their monofluorophenyl or phenyl counterparts. Bis-styrylbenzenes with carboxylic acid functional groups had lower Aβ binding affinities than their neutral counterparts. Selected bis-styrylbenzenes were demonstrated to have good blood - brain barrier penetration capabilities. These data extend the SAR of bis-styrylbenzene Aβ binding and provide direction for the development of a noninvasive probe for early detection of Alzheimer's disease using 19F MRI.
- Flaherty, Daniel P.,Walsh, Shannon M.,Kiyota, Tomomi,Dong, Yuxiang,Ikezu, Tsuneya,Vennerstrom, Jonathan L.
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p. 4986 - 4992
(2008/03/12)
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- NK-1 AND SEROTONIN TRANSPORTER INHIBITORS
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The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating disorders associated with an excess or imbalance of tachykinins or serotonin or both.
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Page/Page column 65; 67; 69
(2010/11/28)
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- Helicity induction in hydrogen-bonding-driven zinc porphyrin foldamers by chiral C60-incorporating histidines
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(Chemical Equation Presented) High chiral amplification is exhibited by a new series of zinc porphyrin appended, hydrogen-bonded foldamers on binding with C60-incorporating chiral histidines as a result of the cooperation of two discrete noncovalent interactions: zinc porphyrin/ imidazole coordination and zinc porphyrin/C6 π-π stacking (see picture).
- Hou, Jun-Li,Yi, Hui-Ping,Shao, Xue-Bin,Li, Chuang,Wu, Zong-Quan,Jiang, Xi-Kui,Wu, Li-Zhu,Tung, Chen-Ho,Li, Zhan-Ting
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p. 796 - 800
(2007/10/03)
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- Fluoro-substituted and 13C-labeled styrylbenzene derivatives for detecting brain amyloid plaques
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Two styrylbenzene derivatives, (E,E)-1-fluoro-2,5-bis-(3-hydroxycarbonyl-4- hydroxy)styrylbenzene (FSB) and (E,E)-1-bromo-2,5-bis(3-hydroxycarbonyl-4- hydroxy)styrylbenzene-α,α′-13C2 ([ 13C]BSB), were synthesized for use as a histochemical stain to detect amyloid plaques of Alzheimer's disease (AD) brain sections. An analysis of fluorescence spectra demonstrated that FSB shows approximately twofold fluorescence intensity relative to the conventional styrylbenzene derivative, (E,E)-1-bromo-2,5-bis-(3-hydroxycarbonyl-4-hydroxy)styrylbenzene (BSB). Moreover, FSB was found to stain amyloid plaques and neurofibrillary tangles of AD brains with greater fluorescence intensity and a lower level of background signals compared to BSB. These finding indicate that FSB can be an excellent fluorescent compound to label human amyloid lesions with high sensitivity and specificity. Because of the possession of a nuclide with a quantized angular momentum, both FSB and [13C]BSB are also potential contrast agents for magnetic resonance imaging to locate AD pathologies in vivo.
- Sato, Kumi,Higuchi, Makoto,Iwata, Nobuhisa,Saido, Takaomi C.,Sasamoto, Kazumi
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p. 573 - 578
(2007/10/03)
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- Thiazolidine derivatives and its use as antifungal agent
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Compounds of formula (I) or salts thereof are provided wherein X is O or S, A and B are OR2 or Y—NR3R4 wherein when A is OR2. B is Y—NR3R4 and vice versa, or when one of A or B is OR2. then the other can be CO2R7. Y is CH2 or C=Q. Q is (CH2)m—CH(R1)—(CH2)n, R is OR6 or NHR7. and with the other definitions as set out in claim 1, a process for its preparation and its use in the prophylaxis or treatment of fungal infections. 1
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- SUBSTITUTED 4-(1H-BENZIMIDAZOL-2-YL)[1,4]DIAZEPANES USEFUL FOR THE TREATMENT ALLERGIC DISEASES
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The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4] diazepane derivatives of formula (1): and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
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- Novel substituted 4-(1H-benzimidazol-2-yl) [1,4]diazepanes useful for the treatment of allergic diseases
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The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4]diazepane derivatives of formula and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
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- Substituted 4-(1H-benzimidazol-2-yl)[1,4]diazepanes useful for the treatment of allergic disease
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The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4]diazepane derivatives of formula (1): and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
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- Substituted 4-(1H-benzimidazol-2-yl-amino)piperidines useful for the treatment of allergic diseases
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The present invention relates to novel substituted piperidine derivatives of formula (1), stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
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- Synthesis of fluorovinylsalicylic acids and their derivatives
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Palladium-catalyzed cross-coupling of iodosalicylic acid derivatives with polyfluorovinyl zinc reagents provided the corresponding fluorovinyl-substituted salicylates.Methyl-5-(β,β)-difluorovinyl methyl salicylate was prepared by a Wittig reaction of the 5-formyl compound with the strongly nucleophilic ylide, .In one sequence, a fluorine-free benzofuran was obtained, instead of a difluorovinylsalicylate. - Keywords: Fluorovinylsalicylic acids; Wittig reaction; Benzofuran
- Filler, Robert,Lin, Shan,Zhang, Zhaoxu
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