- Design, synthesis and preliminary bioactivity evaluation of bitopic benzopyranomorpholine analogues as selective dopamine D3 receptor ligands as anti-drug addiction therapeutic agents
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Three series of bitopic benzopyranomorpholine analogues were designed, synthesized, and evaluated as a novel class of selective ligands for the dopamine D3 receptor. Binding affinities of target compounds were determined using the method of radioligand binding assay. Most compounds demonstrated considerable binding affinities and selectivity for D3 receptor. Besides, the compounds were screened for their ability to alleviate withdrawal symptoms of opioid addiction in animal behavioral models. The results showed that compound 20h displayed nanomolar affinity for the D3R, and exhibited anti-drug addiction efficacy in the animal model of of naloxone-induced withdrawal symptoms in morphine-dependent mice.
- Cai, Jin,Chen, Xixi,Huang, Mingqi,Ji, Min,Wang, Yuhong
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- Acid activated montmorillonite K-10 mediated intramolecular acylation: Simple and convenient synthesis of 4-chromanones
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3-Aryloxyproionic acids undergo intramolecular cyclization in the presence of AA.Mont.K-10 in toluene under reflux for 30–45 min in good to excellent yields. Phenyl ring bearing various substituents at the ortho, meta, para positions undergo this cyclization reaction. This method involves simple work up and amenable for large scale preparations. The heterogeneous acid treated catalyst can be regenerated and used for up to three cycles with minimum loss of activity.
- Begum, Ayisha F.,Balasubramanian, Kalpattu K.,Shanmugasundaram, Bhagavathy
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- CHROMENE DERIVATIVES AS INHIBITORS OF TCR-NCK INTERACTION
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The present invention provides compounds that modulate the interaction of TCR with Nck, compositions thereof, and methods of treatment using the same.
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Paragraph 0468; 0469
(2019/09/06)
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- Synthesis of Flavanones via Palladium(II)-Catalyzed One-Pot β-Arylation of Chromanones with Arylboronic Acids
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A total of 47 flavanones were expediently synthesized via one-pot β-arylation of chromanones, a class of simple ketones possessing chemically unactivated β sites, with arylboronic acids via tandem palladium(II) catalysis. This reaction provides a novel route to various flavanones, including natural products such as naringenin trimethyl ether, in yields up to 92percent.
- Cho, Yang Yil,Jang, Hyu Jeong,Kim, Dong Hwan,Kim, Nam Yong,Kim, Nam-Jung,Kim, Young Min,Lee, Soo Jin,Lee, Yong Sup,Park, Boyoung Y.,Son, Seung Hwan,Yoo, Hyung-Seok
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supporting information
p. 10012 - 10023
(2019/08/30)
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- METHOD OF TREATING POLYCYSTIC KIDNEY DISEASES WITH CERAMIDE DERIVATIVES
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PROBLEM TO BE SOLVED: To provide a method of treating polycystic kidney diseases with ceramide derivatives. SOLUTION: A pharmaceutical composition for treating polycystic kidney disease in a subject comprises an effective amount of a predetermined compoun
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Paragraph 0182
(2016/10/08)
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- Glucosylceramide synthase inhibition for the treatment of collapsing glomerulopathy and other glomerular disease
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A method of treating a glomerular disease selected from the group consisting of mesangial proliferative glomerulonephritis, collapsing glomerulopathy, proliferative lupus nephritis, crescentic glomerulonephritis and membranous nephropathy in a subject com
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Page/Page column 68
(2016/11/21)
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- Efficient and rapid synthesis of phenolic analogs of 4-phenylbutanoic acid using microwave-assisted Michael addition as a key reaction
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ABSTRACT: The addition of phenols to acrylonitrile in the presence of aqueous benzyltrimethylammonium hydroxide or tetramethylammonium hydroxide under microwave irradiation yielded the corresponding Michael adducts. The obtained adducts were easily transformed to phenolic analogs of 4-phenylbutanoic acids via the hydrolysis of nitrile groups.
- Iida, Hirokazu,Akatsu, Yusuke,Mizukami, Kazushi,Natori, Sho,Matsukawa, Minako,Takahashi, Kie
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supporting information
p. 581 - 585
(2016/07/06)
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- Synthesis, characterization, and antimicrobial activity of novel substituted 2H-chromenyl acrylates
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The present study deals with conventional Witting olefination of 2H-chromene-3-carbaldehydes with stabilized ylide in the presence of dichloromethane to afford (2E)-ethyl-3-(4-chloro-2H-chromen-3-yl) acrylate derivatives. All the products were found to have E-geometry at C=C bond. The synthesized compounds were characterized by spectral data such as IR, 1H NMR and MS. Compounds were screened for antimicrobial activity against strains of gram positive, gram negative bacterial and fungal strains. All compounds showed good antibacterial and antifungal activity.
- Subhashini,Ravi,Cherupally,China Raju,Reddy,Bee
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p. 2900 - 2905
(2017/03/22)
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- Selective catalytic synthesis of unsymmetrical ethers from the dehydrative etherification of two different alcohols
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The cationic ruthenium-hydride complex [(C6H6)(PCy3)(CO)RuH]+BF4- catalyzes selective etherification of two different alcohols to form unsymmetrically substituted ethers. The catalytic method exhibits a broad substrate scope while tolerating a range of heteroatom functional groups in forming unsymmetrical ethers, and it is successfully used to directly synthesize a number of highly functionalized chiral nonracemic ethers.
- Kim, Junghwa,Lee, Dong-Hwan,Kalutharage, Nishantha,Yi, Chae S.
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p. 3881 - 3885
(2015/01/16)
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- 2-ACYLAMINOPROPOANOL-TYPE GLUCOSYLCERAMIDE SYNTHASE INHIBITORS
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A compound for use in treating polycystic kidney disease is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating polycystic kidney disease in a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Methods of treating in polycystic kidney disease in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof
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Page/Page column 90; 91
(2010/04/27)
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- 2-ACYLAMINOPROPOANOL-TYPE GLUCOSYLCERAMIDE SYNTHASE INHIBITORS
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A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating
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Page/Page column 90-91
(2009/01/24)
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- Enantioselective synthesis of the PPARα agonist (R)-K-13675 via (S)-2-hydroxybutyrolactone
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Enantioselective synthesis of enantiomerically pure PPARα agonist (R)-K-13675 can be achieved starting from (S)-2-hydroxybutyrolactone. An important intermediate, 2-(aryloxy)butyrolactone, was prepared by reaction of the phenol with (S)-2-hydroxybutyrolactone in excellent yield without loss of enantiomeric purity using the Mitsunobu reaction, followed by conversion into the 2-(aryloxy)butanoic acid via the 2-(aryloxy)-4-iodobutanoate by cleavage of the lactone on exposure to iodotrimethylsilane, followed by hydrogenolysis and hydrolysis. Georg Thieme Verlag Stuttgart.
- Yamazaki, Yukiyoshi,Araki, Takaaki,Koura, Minoru,Shibuya, Kimiyuki
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p. 1017 - 1022
(2008/12/22)
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- PROCESS FOR PRODUCTION OF OPTICALLY ACTIVE PPAR-ACTIVATING COMPOUND AND INTERMEDIATE OF THE SAME
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A process for obtaining a compound (1) and an intermediate thereof in high yield and high optical yield is provided. A process for producing a compound (4), the process including reacting a compound (2) with a compound (3) in the presence of a base; and a process for producing a compound (1), the process including reacting a compound (2) with a compound (3) in the presence of a base to yield a compound (4) and then deesterifying the compound (4). wherein R represents an alkyl group having 1 to 6 carbon atoms or an aralkyl group having 7 to 8 carbon atoms.
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- OPTICALLY ACTIVE PPAR-ACTIVATING COMPOUND INTERMEDIATE AND METHOD FOR PRODUCING SAME
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The present invention provides a production intermediate for compound (A-1) and a method for producing the intermediate at high yield and high optical yield. The present invention provides a method for producing compound (3) characterized in that compound
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Page/Page column 7; 8-9
(2008/06/13)
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- Design and synthesis of highly potent and selective human peroxisome proliferator-activated receptor α agonists
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A combination of benzoxazole, phenoxyalkyl side chain, and phenoxybutyric acids was identified as a highly potent and selective human peroxisome proliferator-activated receptor α (PPARα) agonist. The synthesis, structure-activity relationship (SAR) studies, and in vivo activities of the representative compounds are described.
- Yamazaki, Yukiyoshi,Abe, Kazutoyo,Toma, Tsutomu,Nishikawa, Masahiro,Ozawa, Hidefumi,Okuda, Ayumu,Araki, Takaaki,Oda, Soichi,Inoue, Keisuke,Shibuya, Kimiyuki,Staels, Bart,Fruchart, Jean-Charles
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p. 4689 - 4693
(2008/02/11)
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- PROCESS FOR PRODUCTION OF OPTICALLY ACTIVE PPAR-ACTIVATING COMPOUND AND INTERMEDIATE OF THE SAME
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A process for producing a compound (4) comprising the step of reacting a compound (2) with a compound (3) in the presence of a base; and a process for producing a compound (1) comprising the step of reacting a compound (2) with a compound (3) in the prese
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Page/Page column 8-9
(2008/06/13)
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- Substituted heterocyclic compounds, method for preparing and compositions containing same
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The invention relates to compounds of formula (I): wherein: R1, R2and R3are as defined in the description, X is as defined in the description, Y represents an oxygen atom, a sulphur atom, a C(H)qgroup, SO or SO2, n is equal to from 0 to 5, A represents a NR5R6group, and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.
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- Substituted tetralins, chromans and related compounds in the treatment of asthma
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PCT No. PCT/US87/02734 Sec. 371 Date Apr. 11, 1990 Sec. 102(e) Date Apr. 11, 1990 PCT Filed Oct. 19, 1987Substituted tetralins, chromans 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 and related disease states in mammals; pharmaceutical compositions comprising said compounds; a method of treatment with said compounds; and intermediates useful in the synthesis of said compounds.
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- SUBSTITUTED CHROMANS AND THEIR USE IN THE TREATMENT OF ASTHMA, ARTHRITIS AND RELATED DISEASES
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Substituted chromans which by inhibiting 5-lipoxygenase enzyme are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction, stroke and related disease states in mammals, pharmaceutical compositions thereof, a m
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- Substituted tetralins, chromans and related compounds in the treatment of asthma, arthritis and related diseases
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Substituted tetralins, chromans 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 and related disease states in mammals, pharmaceutical compositions thereof, a method of treatment therewith, and to intermediates useful in the synthesis thereof.
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- Synthesis and Dopamine Agonist Properties of (+/-)-trans-3,4,4a,10b-Tetrahydro-4-propyl-2H,5H-benzopyrano-1,4-oxazin-9-ol and Its Enantiomers
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The dopamine agonist profile of (+/-)-trans-3,4,4a,10b-tetrahydro-4-propyl-2H,5H-benzopyrano-1,4-oxazin-9-ol (16a) and its enantiomers (16b-c) was examined.Racemic 16a exhibited moderate affinity for the dopamine (DA) D2 receptor labe
- DeWald, Horace A.,Heffner, Thomas G.,Jaen, Juan C.,Lustgarten, David M.,McPhail, Andrew T.,et al.
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p. 445 - 450
(2007/10/02)
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- A NEW SYNTHETIC APPROACH TO THE ROTENOID RING SYSTEM
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The (+)-cis-chromanochromanones (2) and (3), respresenting the basic ring system of the natural insecticide rotenone, have been synthesised by a general procedure; the key step is 4-aroylation of the 4-(phenyl-sulphonyl)chromans (7; Z=SO2Ph).
- Lai, Steven M. F.,Orchison, Jack J. A.,Whiting, Donald A.
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p. 5895 - 5906
(2007/10/02)
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