- HETEROCYCLIC COMPOUNDS AS DIHYDROOROTATE DEHYDROGENASE INHIBITORS
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Disclosed are compounds, compositions and methods for treating diseases, disorders, or medical conditions that are affected by the modulation of DHODH. Embodiments of such compounds are represented by Formula (I) and Formula (II) as follows: and wherein R1, R2, R3, R4, R5, R6, R7, R8, X1, X2, X3, X4, Y and Z, are defined herein.
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Page/Page column 90
(2021/08/14)
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- Nucleophilic reactivity of ethers against terminal epoxides in the presence of BF3: A mechanistic study
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In the presence of BF3, a series of symmetrical and unsymmetrical ethers reacted with epichlorohydrin and 2-[(benzyloxy)methyl] oxirane, two terminal epoxides, to afford 1-alkoxy-3-chloropropan-2-ol and 1-alkoxy-3-(benzyloxy)propan-2-ol. The cleavage of unsymmetrical ethers occurred via an SN2 or SN1 mechanism. Secondary epoxides did not give similar ring-opening products. Copyright
- Kose, Aytekin,Altundas, Ramazan,Secen, Hasan,Kara, Yunus
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p. 1325 - 1330
(2013/08/23)
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- COMPOUNDS FOR INHIBITING CELL PROLIFERATION IN EGFR-DRIVEN CANCERS
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The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of Formula (I), wherein the variables are as defined herein.
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Page/Page column 74
(2013/12/03)
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- NOVEL LIPASE INHIBITORS, REPORTER SUBSTRATES AND USES THEREOF
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The invention provides for novel lipase inhibitors, and compositions and devices comprising the same. The invention further provides for methods for treatment o f disorders comprising administration o f novel diacylglycerol lipase inhibitors, and com -positions and devices comprising said inhibitors. In some embodiments, the disorders are pancreatitis, obesity, shock or pancreatic necrosis. The invention further provides for novel ether lipid reporter compounds and methods o f assaying enzymatic activity com -prising contacting a compound with a novel ether lipid reporter compound.
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Paragraph 0159
(2014/01/07)
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- COMPOUNDS FOR INHIBITING CELL PROLIFERATION IN EGFR-DRIVEN CANCERS
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The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of formula (I), wherein the variables are as defined herein.
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Page/Page column 67
(2012/11/14)
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- Assay and inhibition of diacylglycerol lipase activity
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A series of N-formyl-α-amino acid esters of β-lactone derivatives structurally related to tetrahydrolipstatin (THL) and O-3841 were synthesized that inhibit human and murine diacylglycerol lipase (DAGL) activities. New ether lipid reporter compounds were developed for an in vitro assay to efficiently screen inhibitors of 1,2-diacyl-sn-glycerol hydrolysis and related lipase activities using fluorescence resonance energy transfer (FRET). A standardized thin layer chromatography (TLC) radioassay of diacylglycerol lipase activity utilizing the labeled endogenous substrate [1″- 14C]1-stearoyl-2-arachidonoyl-sn-glycerol with phosphorimaging detection was used to quantify inhibition by following formation of the initial product [1″-14C]2-arachidonoylglycerol and further hydrolysis under the assay conditions to [1-14C]arachidonic acid.
- Johnston, Meghan,Bhatt, Shachi R.,Sikka, Surina,Mercier, Richard W.,West, Jay M.,Makriyannis, Alexandros,Gatley, S. John,Duclos Jr., Richard I.
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scheme or table
p. 4585 - 4592
(2012/08/08)
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- Enantioselective ring-opening reaction of epoxides with MeOH catalyzed by homochiral metal-organic framework
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Two new copper metal-organic frameworks containing 2,2′-dihydroxy-1, 1′-binaphthalene-5,5′-dicarboxylic acid (5,5′-H 2BDA) and 2,2′-dihydroxy-1,1′-binaphthalene-4,4′- dicarboxylic acid (4,4′-H2BDA) have been prepared. X-ray structure determination of [Cu2(5,5′-BDA)2(H 2O)2]·MeOH·2H2O (MOF-1) and [Cu2(4,4′-BDA)2(H2O)2] ·4H2O (MOF-2) revealed similar 2D sheet structures, containing square-grid coordination networks, but differences in the stacking motif. The desolvated MOF-1 and -2 were used as Lewis acid catalysts in the asymmetric ring-opening reaction of epoxides with MeOH.
- Tanaka, Koichi,Otani, Ken-Ichi,Murase, Takanori,Nishihote, Shyota,Urbanczyk-Lipkowska, Zofia
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experimental part
p. 709 - 714
(2012/08/08)
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- Ring-opening reactions of epoxides catalyzed by molybdenum(VI) dichloride dioxide
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Transformation of epoxides to β-alkoxy alcohols, acetonides, and α-alkoxy ketones is achieved by using molybdenum(VI) dichloride dioxide (MoO2Cl2) as a catalyst. Alcohol, aldehyde, oxime, tosyl, and tert-butyldimethylsilyl functional groups are tolerated during the methanolysis and acetonidation of the functionalized epoxides. No polymerization product is observed with any of the epoxides. Direct conversion of epoxides devoid of sensitive functional groups into the corresponding α-methoxy ketone is achieved in a single step by using the MoO2Cl 2/Oxone system. Georg Thieme Verlag Stuttgart.
- Jeyakumar, Kandasamy,Chand, Dillip Kumar
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p. 807 - 819
(2008/09/21)
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- Synthesis of 2,5-dihydrofurans via alkylidene carbene insertion reactions
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The insertion reaction of alkylidene carbenes is demonstrated to be an effective method for the synthesis of 2,5-dihydrofuran ring systems. The best results have been obtained on substrates containing electron-withdrawing substituents, which appear less prone to the competing rearrangement reaction. This insight has led to the development of a new method for the synthesis of the core structure of the squalestatin-zaragozic acid natural products.
- Walker, Louise F.,Bourghida, Ahmed,Connolly, Stephen,Wills, Martin
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p. 965 - 981
(2007/10/03)
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- Novel oxepane formation by TiCl4-catalyzed nucleophilic cleavage of 1- alkoxymethyl-6,8-dioxabicyclo[3.2.1]octanes
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Introduction of an alkoxymethyl group at the C1 position in the 6,8- dioxabicyclo[3.2.1]octane system enabled novel formation of oxepane compounds in TiCl-4-catalyzed acetal cleavage reactions. (C) 2000 Elsevier Science Ltd.
- Fujiwara, Kenshu,Amano, Arika,Tokiwano, Tetsuo,Murai, Akio
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p. 1065 - 1080
(2007/10/03)
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- Enzymatic resolution of butanoic esters of 1-phenyl, 1-phenylmethyl, 1-[2-phenylethyl] and 1-[2-phenoxyethyl] ethers of 3-methoxy-1,2-propanediol
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The enzymatic hydrolysis of butanoic esters of 1-phenyl-, 1-phenylmethyl-, 1-[2-phenylethyl] and 1-[2-phenoxyethyl] ethers of 3-methoxy-1,2-propanediol has been studied by using lipases. Highest enantioselectivity E was obtained with amano PS lipase for the phenyl ether E ~ 55, and with lipase B from Candida antarctica for the other derivatives, E ~ 20, >100 and >55 respectively. The absolute configurations of the products were verified from comparison with reference compounds synthesised from (S)-epichlorohydrin or (S)-glycidol.
- Waagen,Hollingsaeter,Partali,Thorstad,Anthonsen
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p. 2265 - 2274
(2007/10/02)
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- A synthetically useful regioselective epoxide ring-opening procedure
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The reaction of alcohols with epoxides in the presence of boron trifluoride etherate has been investigated and found to proceed with variable regioselectivity depending on the substituents attached to the oxirane ring.
- Liu,Chu,Engel
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p. 2367 - 2371
(2007/10/02)
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- Selective monoalkylation of acyclic diols by means of dibutyltin oxide and fluoride salts
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Fluoride anion was found to promote monoalkylation reaction of diols by the stannylene acetal method, and selective monoalkylation of various acyclic diols was accomplished in good yields under mild conditions by employing this new method. Functional groups such as carboxylic acid ester, carboxamide, carbamate, nitrile, alkyl chloride, and ether were not affected under the reaction conditions.
- Nagashima,Ohno
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p. 1972 - 1982
(2007/10/02)
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