- Preparation method of optically pure 4-(1-amino) ethyl benzoate and salt thereof
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The invention relates to a preparation method of of optically pure 4-(1-amino) ethyl benzoate and salt thereof. The method has the characteristics of low cost, environmental friendliness, high opticalpurity, simplicity and convenience in operation and easiness in industrial production.
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Paragraph 0089-0093
(2021/03/30)
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- Methylpyrazole derivatives as RET inhibitor
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The invention relates to a methylpyrazole derivative as an RET inhibitor, in particular to a compound as shown in a formula (I), a stereoisomer and pharmaceutically acceptable salt thereof, a preparation method and a pharmaceutical composition thereof. The compound of the formula (I) can be used for preventing or treating diseases mediated by abnormal RET activity.
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Paragraph 0817-0822
(2021/07/21)
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- PYRAZOLO[3,4-b]PYRIDINE AND PYRROLO[2,3-b]PYRIDINE INHIBITORS OF BRUTON'S TYROSINE KINASE
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Disclosed are pyrazolo[3,4-b]pyridine and pyrrolo[2,3-b]pyridine inhibitors of Bruton's tyrosine kinase (Btk). Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are described, alone or in combin
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Paragraph 1024-1025
(2018/07/31)
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- Substituent effects on chiral resolutions of derivatized 1-phenylalkylamines by heptakis(2,3-di-O-methyl-6-O-tert-butyldimethylsilyl)-β-cyclodextrin GC stationary phase
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Chiral resolutions of trifluoroacetyl-derivatized 1-phenylalkylamines with different type and position of substituent were investigated by capillary gas chromatography by using heptakis(2,3-di-O-methyl-6-O-tert-butyldimethylsilyl)-β-cyclodextrin diluted in OV-1701 as a chiral stationary phase. The influence of column temperature on retention and enantioselectivity was examined. All enantiomers of meta-substituted analytes as well as fluoro-substituted analytes could be resolved. Temperature had a favorable influence on enantioselectivity for small amines with substituents at the ortho-position. The type of substituent at the stereogenic center of amines also had a crucial effect as the ethyl group led to poor enantioseparation. Among all analytes studied, trifluoroacetyl-derivatized 1-(2′-fluorophenyl)ethylamine exhibited baseline resolution with the shortest analysis time.
- Issaraseriruk, Natthapol,Sritana-anant, Yongsak,Shitangkoon, Aroonsiri
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p. 900 - 906
(2018/05/08)
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- 7-PHENYLETHYLAMINO-4H-PYRIMIDO[4,5-D][1,3]OXAZIN-2-ONE COMPOUNDS AS MUTANT IDH1 AND IDH2 INHIBITORS
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A compound, as defined herein, or pharmaceutical composition containing the compound, for use in treating IDH1 or IDH2 mutant cancer and having the structure: (I).
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Page/Page column 19; 48
(2018/07/05)
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- CYCLOALKYL NITRILE PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS
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The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
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Page/Page column 71
(2014/10/03)
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- CYCLOALKYL NITRILE PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS
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Compounds of formula I are provided, which are JAK inhibitors and are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
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Page/Page column 84
(2014/10/03)
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- SYNTHESIS OF INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1
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Disclosed are syntheses of 11 beta-HSD1 inhibitors and corresponding intermediates that are promising for the treatment of a variety of disease states including diabetes, metabolic syndrome, obesity, glucose intolerance, insulin resistance, hyperglycemia, hypertension, hypertension-related cardiovascular disorders, hyperlipidemia, deleterious gluco-corticold effects on neuronal function (e.g. cognitive impairment, dementia, and/or depression), elevated intra-ocular pressure, various forms of bone disease (e.g., osteoporosis), tuberculosis, leprosy (Hansen's disease), psoriasis, and impaired wound healing (e.g., in patients that exhibit impaired glucose tolerance and/or type 2 diabetes).
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Page/Page column 45-46
(2010/04/03)
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- Novel, tunable, and efficient chiral bisdihydrobenzooxaphosphole ligands for asymmetric hydrogenation
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"Chemical Equation Presented" A series of novel, efficient, air-stable, and tunable chiral bisdihydrobenzooxaphosphole ligands (BIBOPs) were developed for rhodium-catalyzed hydrogenations of various functionalized olefins such as α-ary lenam ides, α-(acylamino)acrylic acid derivatives, β-(acylamino)acrylates, and dimethyl itaconate with excellent enantioselectivities (up to 99% ee) and reactivities (up to 2000 TON)
- Tang, Wenjun,Qu, Bo,Capacci, Andrew G.,Rodriguez, Sonia,Wei, Xudong,Haddad, Nizar,Narayanan, Bikashandarkoil,Ma, Shengli,Grinberg, Nelu,Yee, Nathan K.,Krishnamurthy, Dhileep,Senanayake, Chris H.
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supporting information; experimental part
p. 176 - 179
(2010/03/30)
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- PYRIDYL-AZA(THIO)XANTHONE SENSITIZER COMPRISING LANTHANIDE(III) ION COMPLEXING COMPOUNDS, THEIR LUMINESCENT LANTHANIDE (III) ION COMPLEXES AND USE THEREOF AS FLUORESCENT LABELS.
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Lanthanide (III) Ion completing compound comprising: (1) a sensitizer moiety of Formula (I) in which: a is an integer from 1 to 4; b is an integer equal to 1 or 2; c is an integer equal to 1 or 2; (R1)a, (R2)b, (R3)C are t
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Page/Page column 50; 51
(2010/08/08)
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- Reaction prospecting by 31P NMR: enantioselective rhodium-DuPhos catalysed addition of ZnMe2 to diphenylphosphinoylimines
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Chiral shift 31P NMR spectroscopy allows the identification of ligand leads in asymmetric catalyst systems for ZnMe2 addition to ArCH{double bond, long}NP(O)Ph2. Subsequent GC-based optimisation shows [RhCl(CH2{double bond, long}CH2)2]2 and (R,R)-MeDuPhos to be the optimal pre-catalyst combination (product in 78-93% ee). Transmetallation of [(MeDuPhos)Rh{N(P(O)Ph2-CHMeAr}] with ZnMe2 appears to be the rate limiting step of the catalytic cycle as competing coordination by the imine starting material leads to Ph2P(O)NHCH2Ar via MVP hydrogen-transfer. This limitation can largely be overcome by the slow addition of the imine.
- Crampton, Rosemary H.,Hajjaji, Samir El,Fox, Martin E.,Woodward, Simon
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experimental part
p. 2497 - 2503
(2010/04/05)
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- Enantiomeric impurities in chiral synthons, catalysts, and auxiliaries: Part 3
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The enantiomeric excess of chiral reagents used in asymmetric syntheses directly affects the reaction selectivity and product purity. In this work, 84 of the more recently available chiral compounds were evaluated to determine their actual enantiomeric composition. These compounds are widely used in asymmetric syntheses as chiral synthons, catalysts, and auxiliaries. These include chiral alcohols, amines, amino alcohols, amides, carboxylic acids, epoxides, esters, ketones, and oxolanes among other classes of compounds. All enantiomeric test results were categorized within five impurity levels (i.e., 10%). The majority of the reagents tested were determined to have enantiomeric impurities over 0.01%, and two of them were found to contain enantiomeric impurities exceeding the 10% level. The most effective enantioselective analysis method was a GC approach using a Chiraldex GTA chiral stationary phase (CSP). This method worked exceedingly well with chiral amines and alcohols.
- Huang, Ke,Breitbach, Zachary S.,Armstrong, Daniel W.
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p. 2821 - 2832
(2007/10/03)
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- Efficient synthesis of chiral phenethylamines: preparation, asymmetric hydrogenation, and mild deprotection of ene-trifluoroacetamides
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A mild and efficient route to enantioenriched aryl alkyl amines from ketones has been developed. The first successful synthesis and asymmetric hydrogenation of ene-trifluoroamides from oximes gave highly enantioenriched trifluoroacetamides (94-98% ee). The corresponding phenethyl amides are liberated under mild conditions (K2CO3, MeOH/H2O). In addition, a new application of Josiphos ligands toward the asymmetric hydrogenation of both ene-acetamides and ene-trifluoroacetamides was discovered.
- Allwein, Shawn P.,McWilliams, J. Christopher,Secord, Elizabeth A.,Mowrey, Dale R.,Nelson, Todd D.,Kress, Michael H.
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p. 6409 - 6412
(2007/10/03)
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- Triaryl bis-sulfones as cannabinoid-2 receptor ligands: SAR studies
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We recently reported that compound 1 is a potent inhibitor of the CB2 receptor with high selectivity over CB1. This paper describes the SAR development for this class of compounds. Variation of the substitution pattern on the aromatic rings, as well as th
- Shankar, Bandarpalle B.,Lavey, Brian J.,Zhou, Guowei,Spitler, James A.,Tong, Ling,Rizvi, Razia,Yang, De-Yi,Wolin, Ronald,Kozlowski, Joseph A.,Shih, Neng-Yang,Wu, Jie,Hipkin, R. William,Gonsiorek, Waldemar,Lunn, Charles A.
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p. 4417 - 4420
(2007/10/03)
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- Cannabinoid receptor ligands
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The invention relates to compounds of the formula a prodrug thereof, or a pharmaceutically acceptable salt, solvate or stereoisomer of the compound or of said prodrug; which exhibit anti-inflammatory and immunodulatory activity. Also disclosed are pharmac
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- CANNABINOID RECEPTOR AGONISTS
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A compound of the formula (I) or a pharmaceutically acceptable salt thereof, wherein: R1, R2, R3, R4, R5, R6, L1, L2, M, n, p, X, Y and Z are as described in the specification; pharmaceutical compositions thereof, methods of making said pharmaceutical compositions; and methods of use thereof.
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- Synthesis and structure-Activity relationships of M2-Selective muscarinic receptor ligands in the 1-[4-(4-Arylsulfonyl)-phenylmethyl]-4-(4-piperidinyl)-piperazine family
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The synthesis and muscarinic binding properties of compounds based on the 1-[4-(4-arylsulfonyl)phenylmethyl]-4-(1-aroyl-4-piperidinyl)-piperazine skeleton are described. For compounds, substituted with appropriately configured methyl groups at the benzylic center and at the piperazine 2-position, high levels of selective, M2 subtype affinity could be obtained, particularly when the terminal N-aroyl residue was ortho-substituted.
- McCombie, Stuart W.,Lin, Sue-Ing,Tagat, Jayaram R.,Nazareno, Dennis,Vice, Susan,Ford, Jennifer,Asberom, Theodros,Leone, Daria,Kozlowski, Joseph A.,Zhou, Guowei,Ruperto, Vilma B.,Duffy, Ruth A.,Lachowicz, Jean E.
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p. 795 - 798
(2007/10/03)
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- Substituted 2-(R)-Methyl piperazines as muscarinic M2 selective ligands
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A novel series of 2-(R)-methyl-substituted piperazines (e.g., 2) is described. They are potent M2 selective ligands that have > 100-fold selectivity versus the M1 receptor. In the rat microdialysis assay, compound 14 showed significantly enchanced levels of acetylcholine after oral administration.
- Kozlowski, Joseph A,Zhou, Guowei,Tagat, Jayaram R.,Lin, Sue-Ing,McCombie, Stuart W.,Ruperto, Vilma B.,Duffy, Ruth A.,McQuade, Robert A.,Crosby Jr., Gordon,Taylor, Lisa A.,Billard, William,Binch III, Herbert,Lachowicz, Jean E.
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p. 791 - 794
(2007/10/03)
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