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Showing papers on "Alkoxy group published in 1998"


Patent
02 Apr 1998
TL;DR: In this paper, the authors define compounds having formula (1) wherein: X is cycloalkyl which may be optionally substituted; or is a pyridinyl, pyrimidinyl or phenyl ring; n is 0-1; Y is -NH-, -O-, -S-, or -NR-; R is alkyl of 1-6 carbon atoms; R1, R2, R3, R4 and R4 are each, independently, hydrogen, halogen, alkyyl, alkenyl, alkynyl, and
Abstract: This invention provides compounds having formula (1), wherein: X is cycloalkyl which may be optionally substituted; or is a pyridinyl, pyrimidinyl, or phenyl ring; wherein the pyridinyl, pyrimidinyl, or phenyl ring may be optionally substituted; n is 0-1; Y is -NH-, -O-, -S-, or -NR-; R is alkyl of 1-6 carbon atoms; R1, R2, R3 and R4 are each, independently, hydrogen, halogen, alkyl, alkenyl, alkynyl, alkenyloxy, alkynyloxy, hydroxymethyl, halomethyl, alkanoyloxy, alkenoyloxy, alkynoyloxy, alkanoyloxymethyl, alkenoyloxymethyl, alkynoyloxymethyl, alkoxymethyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylsulfonamido, alkenylsulfonamido, alkynylsulfonamido, hydroxy, trifluoromethyl, cyano, nitro, carboxy, carboalkoxy, carboalkyl, phenoxy, phenyl, thiophenoxy, benzyl, amino, hydroxyamino, alkoxyamino, alkylamino, dialkylamino, aminoalkyl, N-alkylaminoalkyl, N,N-dialkylaminoalkyl, phenylamino, benzylamino, formulae (a, b, c, d, e, f, g, h, i, j, k, l, m, n, o, p, q or r); R5 is alkyl which may be optionally substituted, or phenyl which may be optionally substituted; R6 is hydrogen, alkyl, or alkenyl; R7 is chloro or bromo; R8 is hydrogen, alkyl, aminoalkyl, N-alkylaminoalkyl, N,N-dialkylaminoalkyl, N-cycloalkylaminoalkyl, N-cycloalkyl-N-alkylaminoalkyl, N,N-dicycloalkylaminoalkyl, morpholino-N-alkyl, piperidino-N-alkyl, N-alkyl-piperidino-N-alkyl, azacycloalkyl-N-alkyl, hydroxyalkyl, alkoxyalkyl, carboxy, carboalkoxy, phenyl, carboalkyl +, chloro, fluoro, or bromo; Z is amino, hydroxy, alkoxy, alkylamino, dialkylamino, morpholino, piperazino, N-alkylpiperazino, or pyrrolidino; m = 1-4, q = 1-3, and p = 0-3; any of the substituents R1, R2, R3 or R4 that are located on contiguous carbon atoms can together be the divalent radical -O-C(R8)2-O-; or a pharmaceutically acceptable salt thereof with the proviso that when Y is -NH-, R1, R2, R3 and R4 are hydrogen, and n is O, X is not 2-methylphenyl, which are inhibitors of protein tyrosine kinase.

354 citations


Patent
04 Feb 1998
TL;DR: In this article, a general formula (1) is provided between a pair of electrodes, where one layer containing at least one compound is sandwiched, and the other layer containing an organic electroluminescent element sandwiched.
Abstract: (57) [Summary] SOLUTION: A general formula (1) is provided between a pair of electrodes. At least one layer containing at least one compound An organic electroluminescent element sandwiched. (Wherein, Ar 1 ~ Ar Four Is a substituted or unsubstituted aryl A group represented by Ar 1 And Ar Two And Ar Three And Ar Four Forms a nitrogen-containing heterocyclic ring with the nitrogen atom May represent R 1 And R Two Is a hydrogen atom, Chain, branched or cyclic alkyl group, substituted or unsubstituted Represents an aryl group or an aralkyl group; 1 and Z Two Is a hydrogen atom, halogen atom, straight-chain, branched or cyclic Alkyl group, alkoxy group, or substituted or unsubstituted X represents a substituted aryl group; 1 And X Two Is replaced or not Represents a substituted arylene group) [Effect] Organic electric field emission with long light emission life and excellent durability An optical element is provided.

283 citations


Patent
23 Mar 1998
TL;DR: The novel compounds of formula I: wherein R 1 is hydrogen or methyl; R 2 is hydrogen, or an optionally substituted alkyl, alkenyl, alkynyl, alkadienyl or phenyl group; Hal is halogen; and L 1 through L 5 are each hydrogen, halogen or nitro, provided that at least one of them represents nitro or alkoxy as mentioned in this paper.
Abstract: The novel compounds of formula I: wherein R 1 is hydrogen or methyl; R 2 is hydrogen, or an optionally substituted alkyl, alkenyl, alkynyl, alkadienyl or phenyl group; Hal is halogen; and L 1 through L 5 are each hydrogen, halogen, alkyl, alkoxy or nitro, provided that at least one of L 1 through L 5 represents nitro or alkoxy; show selective fungicidal activity. The new compounds are processed with carriers and adjuvants to fungicidal compositions.

272 citations


Patent
06 Jul 1998
TL;DR: In this article, the authors considered the Colchinol derivatives of formula (I) where R1, R2, R3 and R6 are each independently H, optionally substituted alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl and alkanoyl, PO3H2, X is carbonyl (CO), thiocarbonyl, methylene (CH2) or a group CHR4; R4 is OH, O-alkyl or NR8R9; R5 and R7 are
Abstract: Colchinol derivatives of formula (I) wherein R1, R2, R3 and R6 are each independently H, optionally substituted alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, alkanoyl, PO3H2; X is carbonyl (CO), thiocarbonyl (CS), methylene (CH2) or a group CHR4; R4 is OH, O-alkyl or NR8R9; R5 and R7 are each independently H, alkyl, halogen, hydroxy, alkoxy, nitro or amino; R8 is H, optionally substituted alkyl, cycloalkyl, alkanoyl, thioalkanoyl, aryl, heteroaryl, arylcarbonyl, heteroarylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, arylaminocarbonyl, alkylsulfonyl, arylsulfonyl, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl or arylaminosulfonyl; and R9 is H, alkyl or cycloalkyl and the pharmaceutically acceptable salts, solvates, and hydrates thereof have been found to be useful for treatment of diseases involving angiogenesis. Some of these compounds are novel. Particularly preferred are those compounds in which R6 is PO3H2.

220 citations


Patent
06 Oct 1998
TL;DR: In this article, the disclosed solvents for ambient-temperature lithium-sulfur batteries include at least one ethoxy repeating unit compound of the general formula R1(CH2CH2O)nR2, where n ranges between 2 and 10 and R1 and R2 are different or identical alkyl or alkoxy groups.
Abstract: Disclosed are electrolyte solvents for ambient-temperature lithium-sulfur batteries. The disclosed solvents include at least one ethoxy repeating unit compound of the general formula R1(CH2CH2O)nR2, where n ranges between 2 and 10 and R1 and R2 are different or identical alkyl or alkoxy groups (including substituted alkyl or alkoxy groups). Alternatively, R1 and R2 may together with (CH2CH2O)n form a closed ring. Examples of linear solvents include the glymes (CH3O(CH2CH2)nCH3). Some electrolyte solvents include a donor or acceptor solvent in addition to an ethoxy compound as described. Examples of donor solvents include hexamethylphosphoramide, pyridine, N,N-diethylacetamide, N,N-diethylformamide, dimethylsulfoxide, tetramethylurea, N,N-dimethylacetamide, N,N-dimethylformamide, tributylphosphate, trimethylphosphate, N,N,N',N'-tetraethylsulfamide, tetramethylenediamine, tetramethylpropylenediamine, and pentamethyldiethylenetriamine. These assist in solvation of lithium ions. Examples of acceptor solvents include alcohols, glycols, and polyglycols. These assist in solvation of the sulfide and polysulfide anions.

205 citations


Patent
09 Oct 1998
TL;DR: In this paper, the MMP inhibitors are defined as compounds of formula (I) or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R?1 and R 2? are each independently selected from hydrogen, C?1? to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C 1 to C 6 alkenyl.
Abstract: Compounds of formula (I) or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R ?1 and R2? are each independently selected from hydrogen, C?1? to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR?6? or which is optionally benzo-fused; R3 is hydrogen, halo, R?7 or OR7; R4? is hydrogen, C?1? to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R?6? is hydrogen or C?1? to C4 alkyl; R?7? is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin diseases.

200 citations


Patent
05 Sep 1998
TL;DR: In this article, the substituents have the following meanings: R 1 represents difluoromethyl or trifluorsomethymyl, R 2 represents hydrogen or fluorine, R 3 represents cyano substituted with cyano, R 4 represents phenyl- C?1?-C6 alkyl.
Abstract: The invention relates to benzamidoxim derivatives of formula (I) wherein the substituents have the following meanings: R1 represents difluoromethyl or trifluoromethyl, R2 represents hydrogen or fluorine, R3 represents C?1?-C4 alkyl optionally substituted with cyano, C1-C4 halogenalkyl, C1-C4 alkoxy- C1-C4 alkyl, C3-C6 alkenyl, C3-C6 halogenalkenyl, C3-C6 alkinyl, C3-C8 cycloalkyl- C1-C4 alkyl, R?4? represents phenyl- C?1?-C6 alkyl, which can carry one or more substituents selected from the group composed of halogen, C1-C4 alkyl, C1-C4 halogenalkyl, C1-C4 alkoxy or C1-C4 halogenalkoxy on the phenyl ring, or thienyl- C1-C4 alkyl, which can carry one or more substituents selected from the group composed of halogen, C1-C4 alkyl, C1-C4 halogenalkyl, C1-C4 alkoxy or C1-C4 halogenalkoxy on the thienyl ring, or pyrazol- C1-C4 alkyl, which can carry one or more substituents selected from the group composed of halogen, C1-C4 alkyl, C1-C4 halogenalkyl, C1-C4 alkoxy or C1-C4 halogenalkoxy on the pyrazol ring. The invention also relates to intermediate products for the preparation of these derivatives and to their use as fungicides.

184 citations


Patent
24 Feb 1998
TL;DR: In this article, a herbicidal composition comprising of a herbicidally effective amount of acetochlor and a nonphytotoxic antidotally effective ratio of a compound according to formula (I) is presented.
Abstract: This invention is directed to a herbicidal composition comprising: a) a herbicidally effective amount of acetochlor; and b) a non-phytotoxic antidotally effective amount of a compound according to formula (I), wherein each of R?1 and R2? independently represents one or more substituents selected from hydrogen, (C?1?-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylamino, halo, halo(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkyl and nitro; wherein A is selected from (a) and (b), wherein each of R?3 and R4? is independently selected from hydrogen, (C?1?-C6)alkyl, halo(C1-C6)alkyl, cyano(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, phenyl, nitrophenyl, benzyl, halobenzyl, pyridinyl(C1-C6)alkyl and (C1-C6)alkylammonium; and n is 0 or 1.

156 citations


Patent
15 Oct 1998
TL;DR: In this article, an organic electroluminescenters are coupled directly with an anode and cathode such that the organic ELC emits light upon the application of a voltage across the anodes and cathodes.
Abstract: Organic electroluminescent materials having desirable efficiency, weight, and durability properties, as well as devices made from such materials. In one aspect, an organic electroluminescent material is electroluminescently conductively coupled directly with an anode and cathode such that the organic electroluminescent material emits light upon the application of a voltage across the anode and cathode. The organic electroluminescent material includes an organo-siloxane polymer having a main chain comprising anthracene and/or pentacene. The anthracene or pentacene can be substituted optionally with hydrogen, alkyl, aryl, heteroalkyl, heteroaralkyl, nitro, cyano, hydroxy, alkoxy, aryloxy, thio, alkylthio, arylthio, amino, halogen, dialkylamino, diarylamino, diaralkylamino, arylamino, alkylamino, arylalkylamino, carbonyloxy, carbonylalkoxy, carbonylalkyloxy, alkylcarbonyloxy, arylcarbonyloxy, alkoxylcarbonyloxy, sulfonyl, sulfonyloxy, alkyl bonded to the adjacent silicon atom of the organo-siloxane polymer, aryl bonded to the adjacent silicon atom of the organo-siloxane polymer, or the adjacent silicon atom of said organo-siloxane polymer.

148 citations


Journal ArticleDOI
TL;DR: In this article, the Fourier transform Raman spectra with laser excitation in the near infrared were recorded during the base-catalyzed sol-gel reaction of the system 3-glycidoxypropyl-trimethoxysilane (GPTS)/3-aminopropyl-triethoxylynne (APTS).
Abstract: Fourier transform Raman spectra with laser excitation in the near infrared were recorded during the base-catalyzed sol–gel reaction of the system 3-glycidoxypropyl-trimethoxysilane (GPTS)/3-aminopropyl-triethoxysilane (APTS). This combination of organo-(alkoxy)silanes is used for the synthesis of hybrid polymers. Raman bands of the trimethoxysilyl- and the epoxy-moieties were used to monitor the kinetic behaviour of the hydrolysis reaction and the ring cleavage as a function of temperature. A decrease of the rate of hydrolysis of GPTS at elevated temperatures is attributed to a decrease of the pH caused by temporarily accumulating silanol groups. After the start of the condensation reactions, the pH increases and forces hydrolysis to accelerate. The results indicate the existence of a pentacoordinated transition state with a negative charge at the silicon atom during base catalyzed hydrolysis.

146 citations


Journal ArticleDOI
TL;DR: Results of the crystal structure analysis of the CuII -(bis)oxazoline complex in combination with calculations on model compounds indicate the formation of a reactive intermediate through replacement of the two H2 O ligands with a chelating substrate.
Abstract: Air-stable and recyclable, the CuII -(bis)oxazoline complex 1 efficiently catalyzes diastereo- and enantioselective hetero-Diels-Alder reactions between β,γ-unsaturated α-keto acid derivatives 2 and vinyl ethers for the synthesis of substituted dihydropyrans 3 [Eq. (1)]. Results of the crystal structure analysis of 1 in combination with calculations on model compounds indicate the formation of a reactive intermediate through replacement of the two H2 O ligands with a chelating substrate. X=OEt, N(OMe)Me; R=alkyl, aryl, alkoxy, thiobenzyl.

Patent
14 Dec 1998
TL;DR: In this article, double prodrugs containing polymeric-based transport forms are defined and a method for their preparation and treatment is described, and methods of preparing the compounds and methods for treatment are also disclosed.
Abstract: The present invention is directed to double prodrugs containing polymeric-based transport forms. These polymeric prodrugs are preferably of formula (I) wherein: L1 is a bifunctional linking moiety; in formula (a) B is H, a leaving group, a residue of an amine-containing moiety, or a residue of a hydroxyl-containing moiety; Y1-4 are independently O, S, or NR12; R1, R4, R9, R10 and R12, are independently selected from the group consisting of hydrogen C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls; R2, R3, R5 and R6 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C1-6 alkoxy, phenoxy, C1-8 heteroalkyls, C1-8 heteroalkoxy, substituted C1-6 alkyls, C3-8 cycloalkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, halo-, nitro-, cyano-, carboxy-, C1-6 carboxyalkyls and C1-6 alkyl carbonyls; Ar is a moiety which when included in Formula (I) forms a multi-substituted aromatic hydrocarbon or a multi-substituted heterocyclic group; (m), (r), (s), (t), (u) and (v) are independently zero or one; (p) is zero or a positive integer; and R11 is a substantially non-antigenic polymer. The first prodrug is generated when the polymeric portion of the double prodrug is cleaved and the parent molecule is generated rapidly thereafter in vivo, preferably as a result of a 1,6 or 1,4 benzyl elimination-reaction. Methods of preparing the compounds and methods of treatment are also disclosed.

Journal ArticleDOI
TL;DR: Appropriately substituted 2,3-dihydro-7H-thiazolo[3,2-a]pyrimidin-7-ones 9-12 and 18 were considered as annulated analogues of HEPT (1-[(2-hydroxyethoxyethoxy)methyl]-6-(phenylthio)-thymine), and some of these compounds were also found active against HIV-1.
Abstract: Appropriately substituted 2,3-dihydro-7H-thiazolo[3,2-a]pyrimidin-7-ones 9−12 and 18 were considered as annulated analogues of HEPT (1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine), and some of these compounds were also found active against HIV-1, the most active one being 2,3-dihydro-5-[(3,5-dimethylphenyl)methyl]-3-ethoxy-6-ethyl-7H-thiazolo[3,2-a]pyrimidin-7-one (10b). S-Alkylation of 5-alkyl-6-(arylmethyl)-2-thiouracils 1−4 was performed with 2-bromoacetaldehyde acetals to furnish the S-[bis(alkoxy)ethyl] derivatives 5−8 and with allyl bromide to furnish S-allyl derivatives 17. The target compounds 9−12 were obtained by an N1 regioselective intramolecular cyclization reaction of silylated 5−8 using trimethylsilyl trifluoromethanesulfonate (TMS triflate) as the catalyst. Treatment of the S-allyl derivatives 17 with bromine in dry methylene chloride afforded the 3-(bromomethyl) derivatives 18.

Journal ArticleDOI
TL;DR: In this article, the structural properties and applications of hetero(bi-and tri-)metallic alkoxides with halides and cyclopentadienyl ligands are discussed.

Patent
18 Sep 1998
TL;DR: In this paper, a class of aromatic-substituted xanthene compounds useful as fluorescent dyes is disclosed, the compounds having general structure (I), where Y1 and Y2 taken separately are selected from the group consisting of hydroxyl, oxygen, imminium, linking group and amine, or Y1 taken together with R2 is cyclic imine, and Y 2 taken together together with cyclic amine.
Abstract: A class of aromatic-substituted xanthene compounds useful as fluorescent dyes is disclosed, the compounds having general structure (I), where Y1 and Y2 taken separately are selected from the group consisting of hydroxyl, oxygen, imminium, linking group and amine, or Y1 taken together with R2 is cyclic imine, or Y2 taken together with R3 is cyclic amine; R2, R3, R5, and R7 taken separately are selected from the group consisting of hydrogen, fluorine, chlorine, lower alkyl, lower alkene, lower alkyne, sulfonate, sulfone, amino, imminium, amido, nitrile, lower alkoxy, phenyl, and linking group; R1 taken separately is selected from the group consisting of phenyl, substituted phenyl, polycyclic aromatic, substituted polycyclic aromatic, linking group and electron-rich heterocycle, or when taken together with R7 is selected from the group consisting of electron-rich heterocycle and indene; R4 taken separately is selected from the group consisting of amino, amido, phenyl, substituted phenyl, polycyclic aromatic, substituted polycyclic aromatic, indene, linking group and electron-rich heterocycle, or when taken together with R5 is selected from the group consisting of phenyl, substituted phenyl, polycyclic aromatic, substituted polycyclic aromatic, indene, and electron-rich heterocycle; and R6 is selected from the group consisting of acetylene, lower alkyl, lower alkene, cyano, phenyl, substituted phenyl, and heterocyclic aromatic. In another aspect, the invention includes methods for synthesizing the above dye compounds and intermediates. In yet another aspect, the present invention includes reagents labeled with the asymmetric benzoxanthene dye compounds, including deoxynucleotides, dideoxynucleotides, phosphoramidites, and polynucleotides. In an additional aspect, the invention includes methods utilizing such dye compounds and reagents including dideoxy polynucleotide sequencing and fragment analysis methods.

Journal ArticleDOI
TL;DR: In the proposed mechanism the alkoxy anion of the hexosamine formed in a base-catalyzed reaction at C-1 carbon is subjected to an electrophilic rate-limiting attack by Cl(+) of the oxidant.
Abstract: Oxidation of D-mannosamine (1), D-glucosamine (2), and D-galctosamine (3) by sodium N-chlorobenzenesulfonamide or chloramine-B (CAB) at 313 K is followed by a shortening of carbon chain and obeys the rate law, rate = k[CAB][sugar][HO(-)](x)(), where x is less than unity. The products are arabinonic acid, ribonic acid, and erythronic acid for 1 and 2 with smaller amounts of glyceric and hexonic acids, while lyxonic and threonic acids are predominant in the oxidation of 3 with smaller amounts of glyceric and hexonic acids. Proton inventory studies made in a H(2)O-D(2)O mixture point toward a single transition state. In the proposed mechanism the alkoxy anion (S(-)) of the hexosamine formed in a base-catalyzed reaction at C-1 carbon is subjected to an electrophilic rate-limiting attack by Cl(+) of the oxidant. The hexonic acid formed is decarboxylated with loss of ammonia to form the respective pentose, which is further converted into the corresponding pentonic acid. The breaking of the bond between C-1 and C-2 carbons in pentose yields tetronic acids. The thermodynamic parameters for sugar alkoxy anion formation and activation parameters for the rate-limiting step have been evaluated.

Patent
26 Aug 1998
TL;DR: In this article, the compounds of formula (I), wherein R is methyl or ethyl; R 1 is chloro or fluoro; R 2 is hydrogen or fluoros; R 3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R 4 is hydrogen/fluoro; and R 5 is chlorone, fluoromethyl or methyl; pharmaceutically acceptable salts thereof; and pharmaceutic acceptable prodrug esters thereof; as selective COX-2 cyclooxygenase inhibitors.
Abstract: Disclosed are the compounds of formula (I), wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; pharmaceutically acceptable salts thereof; and pharmaceutically acceptable prodrug esters thereof; as selective COX-2 cyclooxygenase inhibitors.

Journal ArticleDOI
TL;DR: The expanded structure-activity relationship around the phenyl alkyl ether moiety is reported by pursuing both a classical medicinal chemistry approach and a solid-phase chemistry approach for analogue synthesis to provide valuable insight on the requirements for PPARgamma binding, functional activity, selectivity, and aqueous solubility.
Abstract: We previously reported the identification of (2S)-((2-benzoylphenyl)amino)-3-{4-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]phenyl}propanoic acid (2) (PPARγ pKi = 8.94, PPARγ pEC50 = 9.47) as a potent and selective PPARγ agonist. We now report the expanded structure−activity relationship around the phenyl alkyl ether moiety by pursuing both a classical medicinal chemistry approach and a solid-phase chemistry approach for analogue synthesis. The solution-phase strategy focused on evaluating the effects of oxazole and phenyl ring replacements of the 2-(5-methyl-2-phenyloxazol-4-yl)ethyl side chain of 2 with several replacements providing potent and selective PPARγ agonists with improved aqueous solubility. Specifically, replacement of the phenyl ring of the phenyloxazole moiety with a 4-pyridyl group to give 2(S)-((2-benzoylphenyl)amino)-3-{4-[2-(5-methyl-2-pyridin-4-yloxazol-4-yl)ethoxy]phenyl}propionic acid (16) (PPARγ pKi = 8.85, PPARγ pEC50 = 8.74) or a 4-methylpiperazine to give 2(S)-((2-benzoylphenyl)amin...

Patent
Ralph P. Robinson1
21 Jul 1998
TL;DR: A compound of formula (I) or the pharmaceutically acceptable salts thereof, wherein R1 is (C?1?-C6)alkyl; R?2? is (c?1/C6)-alkyl, or R?1 and R2? taken together with the carbon atom to which they are attached form a ring selected from (C?5/C7)cycloalkyl and 4-tetrahydropyranyl, 4-piperidinyl, independently selected from hydrogen, fluoro, chloro, trif
Abstract: A compound of formula (I) or the pharmaceutically acceptable salts thereof, wherein R1 is (C?1?-C6)alkyl; R?2? is (C?1?-C6)alkyl; or R?1 and R2? taken together with the carbon atom to which they are attached form a ring selected from (C?5?-C7)cycloalkyl, 4-tetrahydropyranyl and 4-piperidinyl; R?3? is hydrogen or (C?1?-C6)alkyl; and Y is a substituent of any of the carbon atoms of the phenyl ring capable of supporting an additional bond, preferably from 1 to 2 substituents (more preferably one substituent, most preferably one substituent in the 4-position) on the phenyl ring, independently selected from hydrogen, fluoro, chloro, trifluoromethyl, (C1-C6)alkoxy, trifluoromethoxy, difluoromethoxy and (C1-C6)alkyl.

Journal ArticleDOI
TL;DR: Valuable substrates for the synthesis of natural products, compounds 3 are formed from β,γ-unsaturated α-keto esters 1 and vinyl ethers 2 by the title reaction.
Abstract: Valuable substrates for the synthesis of natural products, compounds 3 (R1 =alkyl, aryl, alkoxy; R2 , R3 =alkyl) are formed from β,γ-unsaturated α-keto esters 1 and vinyl ethers 2 by the title reaction [Eq. (1)]. Copper(II) bisoxazolines act as catalysts, and in many cases enantiomeric excesses higher than 99.5 % are achieved.

Patent
15 Oct 1998
TL;DR: In this article, the precursor materials useful for making organic electroluminescent devices such as anthracene derivatives having the structure: ##STR1## R40 -R43 and R44 -R47 are selected independently from the group consisting of hydrogen, alkyl, aryl, heteroalkyl, heterosynthetic, nitro, cyano, hydroxy, alkoxy, ayrloxy, thio, alkoxy, amino, halogen, dialkylamino, diaralkylamino and sulfonyl,
Abstract: Precursor materials useful for making organic electroluminescent devices such as anthracene derivatives having the structure: ##STR1## R40 -R43 and R44 -R47 are selected independently from the group consisting of hydrogen, alkyl, aryl, heteroalkyl, heteroaralkyl, nitro, cyano, hydroxy, alkoxy, aryloxy, thio, alkylthio, arylthio, amino, halogen, dialkylamino, diarylamino, diaralkylamino, arylamino, alkylamino, arylalkylamino, carbonyloxy, carbonylalkoxy, carbonylalkyloxy, alkylcarbonyloxy, arylcarbonyloxy, alkoxylcarbonyloxy, sulfonyl, sulfonyloxy. R48 and R49 are selected independently from the group consisting of trialkoxysilyl, dialkoxysilyl, trichlorosilyl, dichlorosilyl, heptachlorotrisiloxy, and pentachlorodisiloxy.

Patent
30 Apr 1998
TL;DR: In this paper, the authors present a non-corrosive photoresist stripping and cleaning composition, comprising: (a) about 5 % to about 50 % solvent selected from the group consisting of N-methyl-2-pyrrolidinone, N-hydroxyethyl-2pyrrinone, 1,3-dimethyl 2-imidazolidinone and dimethylsulfoxide, N,Ndimethylacetamide, diacetone alcohol, ethylene glycol, propane glycol and admixtures thereof; (b)
Abstract: The present invention is directed to a non-corrosive photoresist stripping and cleaning composition, comprising: (a) about 5 % to about 50 % solvent selected from the group consisting of N-methyl-2-pyrrolidinone, N-hydroxyethyl-2-pyrrolidinone, 1,3-dimethyl-2-imidazolidinone, dimethylsulfoxide, N,N-dimethylacetamide, diacetone alcohol, ethylene glycol, propylene glycol and admixtures thereof; (b) about 10 % to about 90 % of an alkanolamine selected from the group consisting of diethyleneglycolamine, monoethanolamine, diethanolamine, triethanolamine, 2-(2-aminoethylamino)ethanol, and admixtures thereof; (c) about 0.1 % to about 4 % of Formula (I) where R1-R4 are individually selected from the group consisting of hydrogen, alkyl groups having 1-4 carbon atoms, alkoxy groups having 1-4 carbon atoms, halogen groups, amino groups, hydroxyl groups, carboxyl groups or combinations thereof; and (d) about 0.1 % to about 40 % of water, all percentages by weight of the total stripping and cleaning composition.

Journal ArticleDOI
TL;DR: In this article, a Suzuki coupling reaction of 1,4-dibromo-2,5-bis(3-sulfonatopropoxy)benzene sodium salt with 1, 4-phenylenediboronic acid or 4,4‘-biphenyldiyldiboric acid 2,2‘ -dimethylpropyl diester using a water soluble Pd(0) catalyst was investigated.
Abstract: Water soluble poly(p-phenylene) derivatives, poly[2,5-bis(3-sulfonatopropoxy)-1,4-phenylene-alt-1,4-phenylene] sodium salt (PPP−OPSO3) and poly[2,5-bis(3-sulfonatopropoxy)-1,4-phenylene-alt-4,4‘-biphenylene] sodium salt (PPBP−OPSO3), have been synthesized through a Suzuki coupling reaction of 1,4-dibromo-2,5-bis(3-sulfonatopropoxy)benzene sodium salt with 1,4-phenylenediboronic acid or 4,4‘-biphenyldiyldiboronic acid 2,2‘-dimethylpropyl diester using a water soluble Pd(0) catalyst or Pd(OAc)2. The pH dependence of the coupling reaction was investigated and resulted in pH independence at pH levels greater than 10.0. End group analysis of PPP−OPSO3 via 1H NMR of tert-butyl end-capped polymers indicates degrees of polymerization in excess of 40 (ca. 80 rings per chain). Viscometric analysis of PPP−OPSO3 in water shows a behavior comparable to sodium poly(styrenesulfonate) (PSS) of molecular weight 8000. In addition, the polyelectrolyte effect is observed at low polymer concentrations. The λmax of the π → π* ...

Patent
Ah-Mee Hor1, Nan-Xing Hu1, Beng S. Ong1, Zoran B. Popović1, Shuan Xie1 
03 Sep 1998
TL;DR: An organic electroluminescent device member comprised of a charge transport component of an indolocarbazole represented by Formulas (I), (II), (III), (IV), (V), or (VI); or optionally mixtures thereof is defined in this article.
Abstract: An organic electroluminescent device member comprised of a charge transport component of an indolocarbazole represented by Formulas (I), (II), (III), (IV), (V), or (VI); or optionally mixtures thereof ##STR1## wherein R and R' are independently selected from the group consisting of a hydrogen atom, halogen atom, alkyl, alkoxyl, and aryl; m and n are numbers of 0 to 4; R 1 and R 2 are independently selected from the group consisting of alkyl, aryl, and vinyl; R 3 and R 4 are independently selected from the group consisting of a hydrogen atom, halogen atom, alkyl, alkoxy, and aryl, and p is a number from 1 to 3.

Journal ArticleDOI
TL;DR: In this article, the adsorption and reaction of methanol, ethanol, and 2,2,2-trifluoroethanol on silica at 300 K were studied by combining microcalorimetric and infrared spectroscopic (FTIR) measurements with quantum-chemical calculations based on density-functional theory.

Patent
08 Jan 1998
TL;DR: In this paper, a method of preventing corrosion of metals using silanes is proposed, where the first treatment solution contains at least one multi-functional silane having at least two trisubstituted silyl groups, and the substituents are individually chosen from the group consisting of alkoxy and acetoxy.
Abstract: A method of preventing corrosion of metals using silanes. The method comprises applying a first treatment solution directly onto the surface of the metal, wherein the first treatment solution contains at least one multi-functional silane having at least two trisubstituted silyl groups, and wherein the substituents are individually chosen from the group consisting of alkoxy and acetoxy. An optional second treatment solution containing an organofunctional silane may also be employed, particularly if the metal is to be painted.

Journal ArticleDOI
TL;DR: In contrast to their hydrocarbon analogues which exhibit only nematic mesophases, poly{5-[[[2,5]-bis[(n-(dimethylsiloxyl)alkoxy)benzoyl)oxy]benzyl]oxy]carbonyl]bicyclo[2.2.1]hept-2-ene}s and their low-molar-mass model compounds exhibit smectic C mesomorphism as mentioned in this paper.
Abstract: In contrast to their hydrocarbon analogues which exhibit only nematic mesophases, poly{5-[[[2‘,5‘-bis[(4‘‘-(n-(dimethylsiloxyl)alkoxy)benzoyl)oxy]benzyl]oxy]carbonyl]bicyclo[2.2.1]hept-2-ene}s and their low-molar-mass model compounds exhibit smectic C mesophases. Since nematic liquid crystals can be forced into layers by terminating their hydrocarbon substituents not only with fluorocarbon segments but also with flexible siloxane segments, this supports the hypothesis that the smectic mesomorphism of amphiphilic molecules containing linear fluorocarbon segments is due primarily to the immiscibility of the hydrocarbon and fluorocarbon segments, rather than to a shape persistence of “mesogenic perfluoroalkyl rods”. The 2,5-bis[(4‘-(n-(oligodimethylsiloxyl)alkoxy)benzoyl)oxy]toluenes mimic both the phases formed by the polymers and the general temperatures of their transitions and are thereforeexcellent models of the polymers. The 5-{[[2‘,5‘-bis[(4‘‘-(n-(oligodimethylsiloxyl)alkoxy)benzoyl)oxy]benzyl]oxy]car...

Patent
22 Dec 1998
TL;DR: In this paper, a compound of formula I is defined where at least one of R4', R5' or R6' is -X-Y, or two adjacent R3-R6 can together be an aryl or hetaryl ring with 5-12 atoms, with the proviso that if X is -O- or -S-, R 3' and R 6' are H, and Y is pyridyl, then R 6 is alkoxy.
Abstract: The invention relates to a compound of formula I: (see formula I) wherein A is (see formula II), (see formula III) or (see formula IV) R3, R4, R5 and R6 are each, independently, H, halogen, NO2, C1-10-alkyl, C1-10-alkoxy, C6-12 aryl, or C5-12 hetaryl of 1-3 rings, and one of R3-R6 can be -X-Y; or two adjacent R3-R6 can together be an aryl or hetaryl ring with 5-12 atoms; R4' , R5' and R6' are independently H; halogen; C1-C10 alkyl, C1-C10 alkoxy or -X-Y, with the proviso that at least one of R4' , R5' or R6' is -X-Y, or that two adjacent of R4' , R5' and R6' together are a hetaryl ring with 5-12 atoms; R3' is H, halogen, C1-C10 alkyl, or C1-C10 alkoxy; X is -CH2-, -S-, -N(CH3)-, -NHC(O)-, -CH2-S-, -S-CH2; -C(O)-, or -O-; and X is additionally a single bond where Y is pyridyl; and Y is phenyl, pyridyl, naphthyl, pyridone, pyrazine, pyrimidine, benzodioxane, benzopyridine, or benzothiazole; or a pharmaceutically acceptable salt thereof, with the proviso that if X is -O- or -S-, R3' and R6' are H, and Y is phenyl unsubstituted by OH, then R6 is alkoxy.

Patent
Frost Philip1
04 Nov 1998
TL;DR: In this paper, a method of treating or inhibiting colonic polyps in a mammal in need thereof is described, which comprises administering to said mammal a compound having formula (I), wherein X is phenyl which is optionally substituted; R and R 1 are each independently, hydrogen, halogen, alkyl, alkoxy, hydroxy or trifluoromethyl; R 2 is hydrogen, alkoxy, acidoxy, and tetrifluoric acid; Y is a radical selected from the group consisting of formulae (II, (
Abstract: This invention provides a method of treating or inhibiting colonic polyps in a mammal in need thereof which comprises administering to said mammal a compound having formula (I), wherein X is phenyl which is optionally substituted; R and R1 are each independently, hydrogen, halogen, alkyl, alkoxy, hydroxy or trifluoromethyl; R2 is hydrogen, alkyl, alkoxy, hydroxy or trifluoromethyl; Y is a radical selected from the group consisting of formulae (II), (III), (IV), (V), (VI), (VII) and (VIII). R3 is independently hydrogen, alkyl, carboxy, carboalkoxy, phenyl, or carboalkyl; n = 2-4; or a pharmaceutically acceptable salt thereof, with the proviso that each R3 of Y may be the same or different.

Patent
18 Aug 1998
TL;DR: In this paper, a nonaqueous electrolyte for a lithium secondary battery is proposed, where the electrolytic salt is dissolved in a non-aqueous solvent and the battery performance is maintained for a long period.
Abstract: PROBLEM TO BE SOLVED: To provide a nonaqueous electrolyte which is excellent on battery characteristics such as electric capacity, cycle characteristics, and preservation characteristics and maintaining battery performance for a long period, and a lithium secondary battery using the nonaqueous electrolyte. SOLUTION: In the nonaqueous electrolyte wherein electrolytic salt is dissolved in a nonaqueous solvent, the nonaqueous electrolyte for a lithium secondary battery includes 0.1-10 wt.% ethylene carbonate derivative expressed by formula (I), and 0.01-10 wt.% pentafluorophenyloxy compound expressed by a triple-bond containing compound and/or formula (X), and the lithium secondary battery uses the nonaqueous electrolyte. Here, R 1 -R 3 in formula (I) independently show a hydrogen atom, a halogen atom, 2C-12C alkenyl group, 2C-12C alkynyl group, or 6C-18C aryl group, respectively, however, ethylene carbonate is excluded. R 15 in formula (X) shows 2-12C alkyl carbonyl group, 2C-12C alkoxy carbonyl group, 7C-18C aryloxy carbonyl group, or 1C-12C alkane sulfonyl group. However, at least one of hydrogen atoms held by R 15 may be replaced by a halogen atom or 6C-18C aryl group. COPYRIGHT: (C)2010,JPO&INPIT