- 6-HETEROARYLOXY BENZIMIDAZOLES AND AZABENZIMIDAZOLES AS JAK2 INHIBITORS
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The present disclosure provides 6-heteroaryloxy benzimidazole and azabenzimidazole compounds and compositions thereof useful for inhibiting JAK2.
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Paragraph 0890
(2021/11/13)
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- SUBSTITUTED HETEROARYL COMPOUNDS AND METHODS OF USE
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The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof. They are useful in preventing, managing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.
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Paragraph 0468
(2017/04/14)
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- Substituted heteroaryl compound and composition thereof, and uses of substituted heteroaryl compound and composition thereof
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The present invention provides a substituted heteroaryl compound and a composition thereof, and uses of the substituted heteroaryl compound and the composition, wherein the compound is a compound represented by a formula (I) or a stereoisomer, a tautomer, a nitrogen oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug of the compound represented by the formula (I). The present invention further provides a pharmaceutical composition containing the compound, wherein the pharmaceutical composition can regulate activity of protein kinases, particularly Aurora kinases and JAK kinases, and can be used for prevention, treatment, therapy and alleviation of protein kinases, particularly Aurora kinases and JAK kinase activity mediated diseases or disorders.
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Paragraph 1055; 1056; 1057; 1058
(2017/04/29)
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- DIHYDROPYRONE COMPOUNDS AND HERBICIDES COMPRISING THE SAME
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The present invention provides a compound having an excellent efficacy for controlling weeds. A dihydropyrone compound of formula (I): wherein m is 1, 2 or 3; n is an integer of any one of 1 to 5; X represents O, S, S(O) or S(O)2; R1 /sup
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Paragraph 0088
(2014/06/23)
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- N-SUBSTITUTED PIPERIDINE DERIVATIVES AS SEROTONIN RECEPTOR AGENTS
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Disclosed herein are substantially pure forms of the compounds of Formula (I), (II), (III), (IV) and (V), or a pharmaceutically acceptable salt, prodrug, hydrate, solvate, polymorph, stereoisomer or ester thereof. Also disclosed are methods of inhibiting an activity of a serotonin receptor, methods inhibiting an activation of a serotonin receptor, and methods of alleviating or treating various disease conditions and side effects.
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Page/Page column 79-80
(2010/11/04)
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- Total synthesis of (-)-baconipyrone C
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A highly stereoselective asymmetric total synthesis of marine polypropionate (-)-baconipyrone C has been achieved. Utilization of desymmetrization technique to create five stereogenic centres, Sharpless epoxidation, Gilman's reaction and resolution of met
- Yadav,Sathaiah,Srinivas
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scheme or table
p. 3545 - 3552
(2009/09/25)
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- PIPERIDINES AND RELATED COMPOUNDS FOR TREATMENT OF ALZHEIMER’S DISEASE
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Compounds of formula (I) are modulators of gamma-secretase, and hence are useful in treatment of Alzheimer’s disease.
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Page/Page column 42-43
(2008/06/13)
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- Chemoenzymatic Approach toward the Pure Enantiomers of 2-Methyl-1,3-propanediol Mono(p-Methoxybenzyl Ether)
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In a route towards the enantiomerically pure 2-methylpropane-1,3-diol mono(p-methoxybenzyl ether), which is an important starting material for natural product synthesis, a kinetic resolution approach by means of lipase-catalyzed hydrolysis as well as acyl
- Akeboshi, Tomohiro,Ohtsuka, Yoshikazu,Ishihara, Takashi,Sugai, Takeshi
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p. 624 - 637
(2007/10/03)
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- A new and general synthesis of chiral β-ketosulfoxides by reaction of (+)-(R)-methyl p-tolyl sulfoxide with nitriles
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The nitrile functional group is efficiently transformed into the β-ketosulfoxide moiety by reaction with the anion formed from (+)-(R)-methyl p-tolyl sulfoxide and aqueous acidic work-up of the reaction.
- Vleggaar, Robert,Zeevaart, Jacob G.
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p. 9301 - 9303
(2007/10/03)
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- Microwave thermolysis IV: Selective deprotection of MPM ethers using clay supported ammonium nitrate 'clayan' in dry media
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Selective deprotection of (4-methoxyphenyl)-methyl (MPM) ethers using clay supported ammonium nitrate under microwave irradiation is described. The use of expensive reagents and problems associated with slurry reactions are avoided.
- Yadav,Meshram,Sudershan Reddy,Sumithra
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p. 3043 - 3046
(2007/10/03)
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- Resin type can have important effects on solid phase asymmetric alkylation reactions
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A new N-propionylated oxazolidinone 1 is prepared; asymmetric alkylations of this auxiliary proceed with varying yields and enantioselectivities when supported on Merrifield, Wang and TentaGel R PHB resins.
- Burgess, Kevin,Lim, Dongyeol
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p. 785 - 786
(2007/10/03)
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- 3(1-hydoxyethyl)azetidinone compounds and their production
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An amino acid compound of the formula: STR1 wherein R is a lower alkyl group, R1 is a hydrogen atom or a protecting group for carboxyl, R2 is a hydrogen atom, a protecting group for amino, an optionally substituted allyl group of the formula: STR2 (wherein R3 and R4 are each a hydrogen atom, a lower alkyl group or an aryl group), a beta-hydroxyethyl group in which the hydroxyl group is optionally protected, a formylmethyl group in which the formyl group is optionally protected, a carboxymethyl group in which the carboxyl group is protected or a 2-furylmethyl group and X is an optionally protected carboxyl group, a hydroxymethyl group in which the hydroxyl group is optionally protected or a substituted mercaptomethyl group of the formula: (wherein R5 is an aryl group or an ar(lower)alkyl group), which is a useful intermediate in the synthesis of 1-alkylcarbapenem compounds.
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- Asymmetric catalysis. Production of chiral diols by enantioselective catalytic intramolecular hydrosilation of olefins
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Rhodium(I) chiral diphosphine complexes efficiently and rapidly catalyze the intramolecular hydrosilation of silyl ethers derived from allylic alcohols. The efficiency and rates of intramolecular hydrosilations were determined for a variety of silyl and olefin substituents. The catalysts were found to tolerate a wide variety of silyl substituents, although terminal alkyl olefin substituents were found to retard catalysis. Terminal aryl olefin substituents were found to be hydrosilated efficiently and at reasonable rates. One of the chiral catalysts is highly enantioselective for terminal aryl olefin substituents. Almost quantitative ee's are obtained. Moreover, the ee's are only slightly sensitive to aryl and olefin substituents, suggesting that this enantioselective catalysis can provide a wide range of chiral species. Oxidative cleavage of the hydrosilation products gives chiral diols.
- Bergens, Steven H.,Noheda, Pedro,Whelan, John,Bosnich
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p. 2121 - 2128
(2007/10/02)
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- Enantioselective transesterification of 2-methyl-1,3-propanediol derivatives catalyzed by Pseudomonas fluorescens lipase in an organic solvent
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The irreversible transesterification of racemic 2-methyl-1,3-propanediol derivatives, the monoethers 3a, 3b, 5a, and the monobenzoate 5b, with vinyl acetate catalyzed by Pseudomonas fluorescens lipase in chloroform affords enantiomerically pure chiral synthons.
- Grisenti,Ferraboschi,Manzocchi,Santaniello
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p. 3827 - 3834
(2007/10/02)
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- Synthesis of Polypropionate Subunits by SN2'Addition of Cuprates to Nonracemic Acyclic Vinyloxiranes
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Synthetic sequences have been devised for conversion of the chiral pool ester 1 to differentially protected polypropionate subunit polyols 11, 13, 18, and 20.The following stereochemically significant steps were employed: (1) reagent directed Sharpless ep
- Marshall, James A.,Blough, Bruce E.
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p. 1540 - 1547
(2007/10/02)
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- DEPROTECTION OF BENZYL TYPE PROTECTING GROUPS FOR HYDROXY FUNCTIONS BY A PHOTOINDUCED SINGLE ELECTRON TRANSFER REACTION
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DMPM ethers were cleaved by a photo-induced single electron transfer reaction using dicyanoanthracene and anthraquinone as electron acceptors.A similar reaction occured when dimethoxynaphthylmethyl (DMNM) ethers were irradiated in the presence of dicyanob
- Nishida, Atsushi,Oishi, Satoshi,Yonemitsu, Osamu
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p. 2266 - 2268
(2007/10/02)
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- Neighboring Group Participation by Oxygen in the Solvolysis of Acyclic γ-Alkoxy Substituted p-Toluenesulfonates
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Methanolysis of branched 3-(benzyloxy)propyl p-toluenesulfonates, PhCH2OCR1R2CR3R4CHR5OTs (R1 = Me, R2-R5 = H; R1 = R2 = Me, R3-R
- Eliel, Ernest L.,Clawson, Leigh,Knox, David E.
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p. 2707 - 2711
(2007/10/02)
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- ACYLOXYKETONE SUBSTITUTED IMINO AND AMINO ACIDS
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Acyloxyketone substituted imino and amino acids of the formula STR1 are disclosed. These compounds are useful hypotensive agents due to their angiotensin converting enzyme inhibition activity.
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- Acyclic Stereoselection. 22. Diastereofacial Selectivity in the Lewis Acid Mediated Reactions of Allylsilanes with Chiral Aldehydes and Enones
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The Lewis acid mediated reactions of chiral aldehydes 1-4 and enones 5-8 with allylsilanes 9 and 10 have been investigated.With aldehyde 1 and enones 5-7, modest diastereofacial preferences are seen, in the sense predicted by application of Felkin's model for asymmetric induction.Aldehydes 2-4 and enone 8 appear to react by way of chelated intermediates.With these four compounds, the diastereofacial preferences are rather large and are in the sense that is consistend with attack of the allylsilane on the least hindered face of the chelated intermediate.In the reaction of the trans and cis enones 6 and 8 with allyltrimethylsilane, a dramatic reversal of diastereofacial preference is observed; enone 6 gives a 84:14 ratio of products, while enone 8 provides a 10:90 mixture of the same products.
- Heathcock, Clayton H.,Kiyooka, Syun-ichi,Blumenkopf, Todd A.
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p. 4214 - 4223
(2007/10/02)
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- STUDIES IN MACROLIDE SYNTHESIS: AN EFFICIENT SYNTHESIS OF TWO CHIRAL FRAGMENTS OF ERYTHRONOLIDE A
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An efficient asymmetric synthesis of the C1-C5 fragment (3) together with the epimeric C7-C11 fragment (4) used in the Stork approach to the synthesis of erythronolide A is described.
- Paterson, Ian,Patel, Shailesh K.,Porter, John R.
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p. 3395 - 3396
(2007/10/02)
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- Synthesis of 2,6,10-trimethyl-undecan-1-ol
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A synthesis of 2,6,10-trimethyl-undecan-1-ol, an intermediate for producing vitamin E, from methacrolein, crotonaldehyde, β-hydroxy-isobutyric acid including intermediates in this synthesis.
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- Intermediates in the synthesis of vitamin E
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A synthesis of vitamin E in racemic or optically active forms from methacryolein or beta-hydroxyisobutyric acid including intermediates in this synthesis.
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