28313-42-0Relevant academic research and scientific papers
Transition-metal-free alkoxycarbonylation of aryl halides
Zhang, Hua,Shi, Renyi,Ding, Anxing,Lu, Lijun,Chen, Borui,Lei, Aiwen
supporting information, p. 12542 - 12545 (2013/02/23)
Transitions: The title reaction has been developed for the synthesis of a variety of tert-butyl benzoates by employing 1,10-phenanthroline as an additive. Various functional groups were tolerated and heteroaryl iodides were also suitable substrates. Preli
Optically active compound and photosensitive resin composition
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, (2008/06/13)
A photoactive compound is used in combination with a photosensitizer, represented by the following formula (1): A?[(J)m?(X-Pro)]n ??(1) wherein A represents a hydrophobic unit comprising at least one kind of hydrophobic groups selected from a hydrocarbon group and a heterocyclic group, J represents a connecting group, X-Pro represents a hydrophilic group protected by a protective group Pro which is removable by light exposure, m represents 0 or 1, and n represents an integer of not less than 1. The protective group Pro may be removable by light exposure in association with the photosensitizer (especially, a photo acid generator), or may be a hydrophobic protective group. The hydrophilic group may be a hydroxyl group or a carboxyl group. The photoactive compound has high sensitivity to a light source of short wavelength beams, for resist application, therefore, the photoactive compound is advantageously used for forming a pattern with high resolution.
Computational predictions of binding affinities to dihydrofolate reductase: Synthesis and biological evaluation of methotrexate analogues
Graffner-Nordberg,Marelius,Ohlsson,Persson,Swedberg,Andersson,Andersson,Aqvist,Hallberg
, p. 3852 - 3861 (2007/10/03)
The relative binding affinities to human dihydrofolate reductase of four new potential antifolates, containing ester linkages between the two aromatic systems, were estimated by free energy perturbation simulations. The ester analogue, predicted to exhibi
Zinc promoted mild and efficient method for the esterification of acid chlorides with alcohols
Yadav,Reddy, Gondi Sudershan,Srinivas, Dale,Himabindu, Konuru
, p. 2337 - 2342 (2007/10/03)
The esterification of variety of acid chlorides with alcohols in the presence of zinc is described. The easy formation of t-butyl and pivaloyl esters are the additional importance of this procedure.
Retinoid-like compounds
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, (2008/06/13)
The present invention relates to a compound of formula I STR1 or a nontoxic pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof, in whichX is --O--CO--, --NH--CO--, --CS--NH--, --CO--O--, --CO--NH--, --COS--, --SCO--, --SCH 2 --, --CH 2 --CH 2 --, --C C--, --CH 2 --NH--, --COCH 2 --, --NHCS--, --CH 2 S--, --CH 2 O--, --OCH 2 --, --NHCH 2 -- or --CR 5 CR 6 --;R m and R k are independently hydrogen, halogen, C 1-6 alkyl, hydroxy, C 1-6 alkyloxy or nitro;n is zero or one;R 4 is --(CH 2) t --Y, C 1-6 alkyl, or C 3-6 cycloalkyl;R 1 is --CO 2 Z, C 1-6 alkyl, CH 2 OH, --CONHR y, or CHO;R 2 and R 3 are independently hydrogen or C 1-6 alkyl;R a and R b are independently hydrogen or C 1-6 alkyl; but when n is one, R a and R b together can form a radical of the formula STR2 Y is naphthyl or phenyl, both radicals can be optionally substituted with one to three same or different C 1-6 alkyl or halogen;Z is hydrogen or C 1-6 alkyl;R 5, R 6 and R y are independently hydrogen or C 1-6 alkyl; andt is zero to six.
Retinoid-like compounds
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, (2008/06/13)
The present invention relates to a compound of formula STR1 or a nontoxic pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof, in which X is --O--CO--, --NH--CO--, --CS--NH--, --CO--O--, --CO--NH--, --COS--, --SCO--, --SCH2 --, --CH2 --CH2 --, --C C--, --CH2 --NH--, --COCH2 --, --NHCS--, --CH2 S--, --CH2 O--, --OCH2 --, --NHCH2 -- or --CR5 =CR6 --; Rm and Rk are independently hydrogen, halogen, C1-6 alkyl, hydroxy, C1-6 alkyloxy or nitro; n is zero or one; R4 is --(CH2)t --Y, C1-6 alkyl, or C3-6 cycloalkyl; R1 is --CO2 Z, C1-6 alkyl, CH2 OH, --CONHRy, or CHO; R2 and R3 are independently hydrogen or C1-6 alkyl; Ra and Rb are independently hydrogen or C1-6 alkyl; but when n is one, Ra and Rb together can form a radical of the formula STR2 Y is naphthyl or phenyl, both radicals can be optionally substituted with one to three same or different C1-6 alkyl or halogen; Z is hydrogen or C1-6 alkyl; R5, R6 and Ry are independently hydrogen or C1-6 alkyl; and t is zero to six.
Inhibition of human leukocyte elastase (HLE) by N-substituted peptidyl trifluoromethyl ketones
Skiles,Fuchs,Miao,Sorcek,Grozinger,Mauldin,Vitous,Mui,Jacober,Chow,Matteo,Skoog,Weldon,Possanza,Keirns,Letts,Rosenthal
, p. 641 - 662 (2007/10/02)
A series of tripeptides possessing trifluoromethyl or aryl ketone residues at P1 were prepared and evaluated both in vitro and in vivo as potential inhibitors of human leukocyte elastase (HLE). Tripeptides containing non naturally occurring N-substituted glycine residues at the P2-position have been demonstrated to be potent in vitro inhibitors of HLE, with IC50 values in the submicromolar range. Sterically demanding substituents on the P2- nitrogen have no detrimental effect on in vitro potency. The inhibition process presumably acts via hemiketal formation with the active site Ser195 of HLE, and is facilitated by the strongly electron withdrawing trifluoromethyl functionality. Deletion of the amino acid at the P3-subsite region affords inactive compounds. Valine is the preferred residue at the P1-position, whereas the corresponding glycine, alanine, α,α- dimethylglycine, or phenylalanine analogues are all inactive. The compounds described herein all confer a high degree of in vitro specificity when tested against representative cysteine, aspartyl, metallo, and other serine proteases. One of the most potent in vitro inhibitors is (3RS)-N-[4[[[(4- chlorophenyl)sulfonyl]amino]carbonyl]phenyl]oxomethyl]-L-valyl-N-(2,3- dihydro-1H-inden-2-yl)glycine N-[3-(1,1,1-trifluoro-4-methyl-2- oxopentyl)amide (20i; BI-RA-260) (IC50 = 0.084 μM). Compound 20i was also tested in hamsters in an elastase-induced pulmonary hemorrhage (EPH) model. In this model, intratracheal (it.) administration of 20i, 5 min prior to HLE challenge, effectively inhibited hemorrhage in a dose-dependent manner with an ED50 of 4.8 μg. The inhibitor 20i, 20 μg administered it. 24, 48, and 72 h prior to HLE challenge, exhibits significant inhibition against hemorrhage at all time points (97%, 64% and 49%, respectively). In a 21-day chronic model of emphysema in hamsters, 200 μg of HLE administered it. caused an elastase-induced emphysema in the lungs which can be quantitated histologically utilizing image analysis. In this assay, 20i significantly inhibited pulmonary lesions associated with septal destruction and increased alveolar spaces, when dosed at 20 μg it. 5 min prior to challenge with HLE.
PREPARATION AND PROPERTIES OF OLIGOMERS OF DEFINED CHAIN LENGTH AND STRUCTURE AS MODELS FOR TECHNICAL COPOLYMERS
Seliger, H.,Bitar, M. B.,Goeldner, E.,Kittel, I.,Kilian, H. G.
, p. 171 - 186 (2007/10/03)
Oligomeric segments of the macromolecules with defined structure have been prepared in an attempt to answer the question whether the thermal and mechanical properties of the elastomers (polyester) are mainly influenced by the segregation or by the structu
N-substituted amides
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, (2013/12/16)
Compounds of the formula are inhibitors of human leukocyte elastase.
SELECTED DIFLUORO DERIVATIVES
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, (2008/06/13)
The invention discloses a series of difluoroketone, mono-di-and tri-peptide derivatives of formula Ia, Ib and Ic: ______________________________________ (Formula set out on pages following Examples) Ia (Formula set out on pages following Examples) Ib (Formula set out on pages following Examples) Ic ______________________________________ and salts thereof where appropriate, and wherein the radicals are defined hereafter in the specification. The derivatives are useful in inhibiting the action of human leukocyte elastase. There are also disclosed methods and intermediates for the manufacture of, and pharmaceutical compositions comprising, the said derivatives.
