Showing papers on "Alkoxy group published in 1999"

Hepatitis C inhibitor tri-peptides

Abstract: Racemates, diastereoisomers and optical isomers of a compound of formula (I) wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4-C(O)-; a carboxyl of formula R4-O-C(O)-; an amide of formula R4-N(R5)-C(O)-; a thioamide of formula R4-N(R5)-C(S)-;or a sulfonyl of formula R4-SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C?1-8? alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is CH2-R20, NH-R20, O-R20or S-R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or tri-substituted with R21, or R20 is a C6 or C10 aryl or C7-14 aralkyl optionally substituted, or R20 is Het or (lower alkyl)-Het, both optionally substituted, Het or (lower alkyl)-Het; carboxyl; carboxy(lower alkyl); C6 or C10 aryl, C7-14 aralkyl or Het, said aryl, aralkyl or Het being optionally substituted; and R?1? is H; C?1-6? alkyl, C3-7 cycloalkyl, C2-6 alkenyl, or C2-6 alkynyl, all optionally substituted with halogen; or a pharmaceutically acceptable salt or ester thereof.

[Rh2(OCOCF3)4] as an auxiliary chromophore in chiroptical studies on steroidal alcohols

Abstract: The circular dichroism (CD) of in situ formed complexes of steroidal substituted secondary and tertiary alcohols with [Rh2(OCOCF3)4] have been investigated. The applicability of the bulkiness rule, developed for unsubstituted secondary alcohols and connecting the sign of the E band at ca. 350 nm with the absolute stereochemistry of an alcohol, is extended to substituted secondary and tertiary alcohols. The rule works well for secondary and tertiary alcohols containing a double bond, alkoxy, ester or amide groups, halogen substituents as well as additional primary hydroxy groups in a molecule. The influence of other substituents present at the stereogenic center, e.g. a keto-, amino-, azido- or additional hydroxy groups, on CD is also described. It is demonstrated that alcohol molecules bind to the Rh-core at axial positions to form 1:2 adducts of the general formula [Rh2(OCOCF3)4(alcohol)2].

4,4-Diarylbutadienes as water soluble, photostable UV-filters for cosmetic and pharmaceutical preparations

Abstract: 4,4-Diarylbutadienes (I) are new. Diaryl-butadienes of formula (I) (where the diene system is in Z,Z, E,Z, Z,E or E,E configuration, or a mixture of these) are new: R1, R2 = H; 1-20C alkyl, 2-10C alkenyl, 3-10C cycloalkyl, 3-10C cycloalkenyl, 1-12C alkoxy, 1-20C alkoxycarbonyl, mono- or di-(1-12C alkyl)-amino, aryl or heteroaryl (optionally substituted); or water-solubilizing substituents selected from carboxylate, sulfonate and ammonium groups; R3 = H, COOR5, COR5, CONR5R6 or CN; R4 = COOR6, COR6 or CONR5R6; R5 = H, -(X)o-R7 or -(1-6C) alkylene-Q; Q = SO3Y, PO3Y or N ; R6 = as R5 but not H; X = (CH2)pZ, CHMeCH2Z or CH2CHEtZ; p = 2-4; A = Cl, Br, I or SO4R9; Y = H, Na , K , Mg , Ca , Li , Al or N(R8)4 ; Z = O or NH; R7, R8 = H, 1-8C alkyl, 2-6C alkenyl or 1-6C acyl; R9 = H, 1-6C alkyl or 2-6C alkenyl; n = 1-3; and o = 1-150.

Arylphenyl-substituted cyclic keto-enols

Abstract: The invention relates to new arylphenyl-substituted cyclic keto-enols of the formula (I), where X is halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkyl sulfinyl, alkyl sulfonyl, halogen alkyl, halogen alkoxy, halogen alkenyloxy, nitro, cyano, or a phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio which each can possibly be substituted; Y is a cycloalkyl, aryl or hetaryl which each can possibly be substituted; Z is hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogen alkyl, halogen alkoxy, halogen alkenyloxy, nitro or cyano; and CKE is one of groups (1, 2, 3, 4, 5, 6, 7 or 8), where A, B, D, G and Q1 to Q6 have the meanings given in the description. The invention also relates to several method for producing the above cyclic keto-enols and their use as pesticides and herbicides.

Lubricious, drug-accommodating coating

Abstract: A coating is provided for a substrate comprising a polyisocyanate; an amine donor and/or hydroxyl donor; an isocyanatosilane adduct having terminal isocyanate groups and at least one hydrolyzable alkoxy group bonded to silicon; and optionally a polymer selected from the group consisting of polyethylene oxide, polyvinyl pyrrolidone, polyvinyl alcohol, polyethylene glycol, and polyacrylic acid. The coating can accommodate a drug so that when the coating is applied to a medical device, the medical device becomes drug-releasing when in contact with aqueous body fluid. A coated article as well as a method for preparing the coating is also provided.

Aryl phenyl substituted cyclic ketoenols

Abstract: The invention relates to new aryl phenyl substituted ketoenols of formula (I), where X is halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkyl sulfinyl, alkyl sulfonyl, halogen alkyl, halogen alkoxy, halogen alkenyloxy, nitro, cyano or possibly substituted phenyl, phenoxy, phenylthio, phenyl alkoxy or phenyl alkylthio; Z is possibly substituted cycloalkyl, aryl or hetaryl; W and Z independently of each other are hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogen alkyl, halogen alkoxy, halogen alkenyloxy, nitro or cyano; and CKE is one of groups (1), (2), (3), (4), (5), (6), (7) or (8), where A, B, D, G and Q1 to Q6 have the meanings assigned in the description. The invention also relates to several methods for producing said ketoenols and to their use as pest control agents and herbicides.

A3 adenosine receptor agonists

Abstract: The present invention provides certain novel pyridine and dihydropyridine derivatives, pharmaceutical compositions comprising one or more of these derivatives, and a method of treating a mammal by selectively blocking an A3 adenosine receptor of the mammal by the administration of a pyridine or dihydropyridine derivative of the present invention. Thus, for example, the present invention provides the following pyridine derivatives of formula (I) or a pharmaceutically acceptable salt thereof; wherein R2 is selected from the group consisting of C1-C6 alkyl, C3-C7 cycloalkyl, and C1-C6 alkoxy C1-C6 alkyl; R3 is selected from the group consisting of C1-C6 alkoxy, C1-C6 alkylsulfanyl, hydroxy, C1-C6 alkoxy C1-C6 alkylsulfanyl, hydroxy C1-C6 alkylsulfanyl, and halo C1-C6 alkylsulfanyl, or R3 together with R4 forms a 3-7 membered heterocyclic ring containing O, N, or S; R4 is selected from the group consisting of C1-C6 alkyl, halo C1-C6 alkyl, hydroxy C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylsulfanyl, C1-C6 alkylamino, C1-C6 alkylcarbonyl sulfanyl C1-C6 alkyl, aryl C2-C6 alkenyl, aryl C2-C6 alkynyl, formyl, and acetal; R5 is selected from the group consisting of C1-C6 alkyl, aryl C1-C6 alkyl, hydroxy C1-C6 alkyl, and halo C1-C6 alkyl; and R6 is selected from the group consisting of aryl, C3-C7 cycloalkyl, and haloaryl; wherein said aryl is a phenyl or naphthyl. The compounds of the present invention can be used for inhibiting the binding of ligands to an adenosine receptor of a substrate. The compounds of the present invention can be used for characterizing an adenosine receptor in a substrate.

Polymerizable polyalkoxylated naphthopyrans

Abstract: Described are novel photochromic polymerizable polyalkoxylated naphthopyran compounds, examples of which are certain 2H-naphtho[1,2-b]pyrans, 3H-naphtho[2,1-b]pyrans and indeno[2,1-f]naphtho[1,2-b]pyrans each having at least one polyalkoxylated substituent of from 1 to 50 alkoxy units per substituent which is end-capped with a polymerizable group. Specific substituents are also present on the naphtho, indeno and pyrano portions of the compounds. These compounds may be represented by graphic formulae (I), (II) or (III). Also described are various substrates, e.g., paper, glass, polymeric organic materials, etc., that contain or that are coated with such compounds. Optically clear articles such as contact lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, indenonaphthopyrans, benzopyrans, oxazine-type compounds, etc., are also described.

Rubber composition, method of adding and blending the composition and vehicle tire made from the composition

Abstract: A rubber composition which contains a rubber mixture that can be vulcanized with a vulcanizing agent, which includes at least one rubber component, at least one filler having nucleophilic groups, gel particles comprising a rubber, having a particle size between about 3x10-9 and about 1x 10-6 m and a swelling index in toluene of about 1 to about 15 and whose surface has electrophilic centers, and a substance acting as a coupling agent between tile filler having nucleophilic groups and the additional filler, the substance acting as a coupling agent having the following structure: X - R1 -Si - (R2)3, wherein X is a nucleophilic group, R1 is an alkyl group having up to about 6 carbon atoms or a phenyl group, and R2 may be the same as or different from each other and from R1 and is an alkyl or alkoxy group having up to 6 carbon atoms and at least one of R2 is an alkoxy group. The rubber composition has improved hysteresis behavior in the vulcanized state so that with the use of this rubber composition in tires, the rolling resistance is reduced and the wet slippage behavior is improved in relation to conventional rubber compositions. A method of adding and blending the rubber composition as well as a composition useful for tire treads and vehicle tires containing the composition are disclosed.

Material for luminescence element and luminescence element using the same

Abstract: A material for a luminescence element is described, which is a compound having a partial structure represented by the following formula (I): wherein Q 1 represents an atomic group necessary to form a 5- or 6-membered nitrogen-containing aromatic heterocyclic ring; Q 2 represents an atomic group necessary to form a 5- or 6-membered aromatic ring; X and Y each represents a carbon atom or a nitrogen atom; and Z represents SO 2 R 1 , COR 2 or POR 3 (R 4 ) , wherein R 1 , R 2 , R 3 and R 4 each represents an aliphatic hydrocarbon group, an aryl group, a heterocyclic group, an amino group, an alkoxyl group, an aryloxy group or a heterocyclic oxy group.

Benzamide derivatives for the treatment of diseases mediated by cytokines

Abstract: The invention concerns the use of amide derivatives of formula (I) wherein: R?1 and R2? are substituents such as hydroxy, C?1-6?alkoxy, mercapto, C1-6alkylthio, amino, C1-6alkylamino and di-(C1-6alkyl)amino; m and p are independently 0-3; R?3? is C?1-4?alkyl; q is 0-4; and R?4? is aryl or cycloalkyl; or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of diseases or medical conditions mediated by cytokines.

5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3, 4-dihydropyrimidin-4(3H)-ones: novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives.

Abstract: Molecular modeling analysis of compounds belonging to the recently published series of dihydro-alkoxy-benzyl-oxopyrimidines (DABOs), such as S-DABOs and DATNOs, gave support to the design of new 2, 6-disubstituted benzyl-DABO derivatives as highly potent and specific inhibitors of the HIV-1 reverse transcriptase (RT). To follow up on the novel DABO derivatives, we decided to investigate the effect of electron-withdrawing substituents in the benzyl unit of the S-DABO skeleton versus their anti-HIV-1 activity. Such chemical modifications impacted the inhibitory activity, especially when two halogen units were introduced at positions 2 and 6 in the phenyl portion of the benzyl group bound to C-6 of the pyrimidine ring. Various 5-alkyl-2-(alkyl(or cycloalkyl)thio)-6-(2, 6-dichloro(or 2,6-difluoro)phenylmethyl)-3, 4-dihydropyrimidin-4(3H)-ones were then synthesized and tested as anti-HIV-1 agents in both cell-based and enzyme (recombinant reverse transcriptase, rRT) assays. Among the various mono- and disubstituted phenyl derivatives, the most potent were those containing a 6-(2,6-difluorophenylmethyl) substituent (F-DABOs), which showed EC50's ranging between 40 and 90 nM and selectivity indexes up to >/=5000. An excellent correlation was found between EC50 and IC50 values which confirmed that these compounds act as inhibitors of the HIV-1 RT. The structure-activity relationships of the newly synthesized pyrimidinones are presented herein.

Active energy ray curing composition and method of its coating film formation

Abstract: PROBLEM TO BE SOLVED: To provide an active energy ray curing compsn. excellent in curing. SOLUTION: This compsn. is provided by compounding the following components: (A) a sulfur-contg. compd. prepared by reacting a compd. (a) contg. at least two average thiol groups (SH group) in a molecule and having an average mol.wt. of 150-1,000, an acrylic silane compd. (b) contg. an acryloyl group and at least two alkoxy siliyl groups in a molecule, and, if necessary, and acrylic compd. (c) contg. an acryloyl group and at least an epoxy group and/or an oxetane ring in a molecule, in such a molar ratio as the acryloly group in the component (b) and component (c)/the thiol group in the component (a) is 0.5-1.2:5-100 pts.wt.; (B) a photo cationic reactive compd.: 0-95 pts.wt.; and (C) a photo cationic polymn. initiator: 0.05-20 pts.wt. per 100 pts.wt. of total component (A) and component (B).

Herbicidal mixtures having a synergistic effect

Abstract: The invention relates to synergistic herbicidal mixtures containing A) at least one 3-heterocyclyl-substituted benzoyl derivative of formula (I) in which the variables have the following meaning: R1, R3 represent hydrogen, halogen, alkyl, alkyl halide, alkoxy, alkoxy halide, alkylthio, alkyl sulfinyl, or alkyl sulfonyl; R2 represents a heterocyclic radical selected from the group: thiazole-2-yl, thiazole-4-yl, thiazole-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, 4,5-dihydroisoxazol-3-yl, 4,5-dihydroisoxazol-4-yl and 4,5-dihydroisoxazol-5-yl, whereby these can be optionally substituted one time or a multiple number of times by halogen, alkyl, alkoxy, alkyl halide, alkoxy halide, alkylthio; R4 represents hydrogen, halogen or alkyl; R5 represents alkyl; R6 represents hydrogen or alkyl; or one of the environmentally compatible salts thereof; and B) a synergistically effective quantity of at least one herbicidal compound from the group of acetyl CoA carboxylase inhibitors (ACC), acetolactate synthase inhibitors (ALS), amides, auxin herbicides, auxin transport inhibitors, carotinoid biosynthesis inhibitors, enolpyruvyl-shikimat-3-phosphate synthase inhibitors (ESPS), glutamine synthetase inhibitors, lipid biosynthesis inhibitors, mitosis inhibitors, protophorphyrinogen-IX-oxidase inhibitors, photosynthesis inhibitors, synergistic agents, growth substances, cell wall biosynthesis inhibitors and various other herbicides. The invention also relates to agents which contain these mixtures, to methods for producing these agents, and to the use thereof for controlling unwanted plants.

Effect of Alkyl Substituents and Ring Size on Alkoxy Radical Cleavage Reactions.

Abstract: The α-cleavage ring-opening reactions of a series of acyclic and cyclic alkoxy radicals are examined computationally with CASSCF/6-31G*, UHF/6-31G*, and UB3LYP/6-31G* methods, to explain the anomalous results obtained by Zhang and Dowd (Tetrahedron 1993, 49, 1965): tricyclic alkoxy radicals were found to cleave to give the less-stable products in several cases; even allylic stabilization of the radical formed by cleavage does not influence the direction of cleavage. The source of this kinetic preference is identified as arising from two factors: (i) through-bond interactions significantly slow the rate of bond cleavage in fused four-membered rings relative to exocyclic cleavage of four-membered rings, and (ii) allylic stabilization is not effective in the early transition state of alkoxy radical cleavage in these strained systems. The relationship between activation energies of cleavage and the energy of the reaction is explored for a variety of cyclic and acyclic alkoxy radicals. Benson's observation t...

Phthalamide derivatives, or salt thereof agrohorticultural insecticide, and method for using the same

Abstract: The present invention provides a phthalamide derivative of the formula (I): [wherein A1 is (substituted) C1-C8 alkylene, (substituted) C3-C8 alkenylene, (substituted) C3-C8 alkynylene, etc., R1 is H, (halo) C3-C6 cycloalkyl, (substituted) phenyl, (substituted) heterocycle, -A2-R4, etc., R2 and R3 are H, C3-C6 cycloalkyl, -A2-R4, etc., A2 is -C(=O)-, -C(=S)- or -C(=NR5)-, R4 is H, alkyl, (substituted) phenyl, (substituted) heterocycle, etc., X and Y are halogen, cyano, nitro, (halo) C1-C6 alkyl, (halo) C1-C6 alkoxy, etc., 1 is 0-4, m is 0-5, n is 0-2]; and an agrohorticultural insecticide containing said compound as active ingredient and exhibiting an excellent insecticidal effect.

Solid-phase synthesis with tris(alkoxy)benzyl backbone amide linkage (BAL)

Abstract: The novel and general BAL concept allows for solid-phase synthesis of C-terminal-modified and cyclic peptides, small organic molecules, and modified amino sugars, as single species or as part of combinatorial chemistry applications. A BAL anchor attached to resin is depicted.

High Molecular Weight Poly(p-phenyleneethynylene)s by Alkyne Metathesis Utilizing “Instant” Catalysts: A Synthetic Study

Abstract: In this contribution, alkyne metathesis of 1,4-dipropynylated benzenes 3 is reported. High-molecular weight poly(p-phenyleneethynylenes) 4 form from 3 under concomitant evolution of butyne. The highly active catalyst system employed in this polymerization reaction forms from commercially available Mo(CO)6 and 4-chlorophenol or 4-trifluoromethylphenol in situ at 140 °C in off-the-shelf quality 1,2-dichlorobenzene. Introduction of dry nitrogen into the reaction vessel serves to remove the byproduct, 2-butyne. Several dipropynylated benzenes 3 carrying solubilizing alkyl (hexyl, nonyl, dodecyl, 2-(ethyl)hexyl, ethylbutyl, isopentyl, 3,7-dimethyloctyl, 2,5,5-trimethylhexyl, cyclohexyl, isopentyloxy) or alkoxy substituents were prepared starting from 1,4-dichlorobenzene (alkyl substituted) or hydroquinone (alkoxy substituted). Polymerization of the monomers 3 furnished the yellow and highly fluorescent poly(p-phenyleneethynylene)s 4 in excellent to quantitative yields and high purity. For soluble derivatives, ...

Aminopropyl-functional siloxane oligomers

Abstract: Mixtures of linear and cyclic amino-functional siloxane oligomers containing: (i) 3-aminopropyl, N-(2-aminoethyl)-3-aminopropyl or N'-(2-aminoethyl)-N-(2-aminoethyl)-3-aminopropyl groups; (ii) optional alkoxy groups; and (iii) (cyclo)alkyl, alkenyl or aryl groups. Mixtures of chain-type and cyclic siloxane oligomers of formula (I) and (II): R = (i) groups of formula -(CH2)3-NH2, -(CH2)3-NHR', -(CH2)3-NH-(CH2)2-NH2 or -(CH2)3-NH-(CH2)2-NH-(CH2)2-NH2, with not more than one aminopropyl-functional group of this type attached to a silicon atom, (ii) methoxy, ethoxy, 2-methoxyethoxy and/or propoxy groups, with a silicon/alkoxy group mol ratio of at least 0.5 and optionally (iii) 1-18C alkyl, alkenyl, iso-alkyl or cycloalkyl, or 6-12C aryl; R' = linear, branched or cyclic 1-18C alkyl, or 6-12C aryl; m = more than 2 and less than 30; n = 3-30 An Independent claim is also included for a process for the production of these mixtures from mixtures of: (A) aminopropyl-functional trialkoxy- or methyldialkoxy-silanes; optionally (B) 1-18C alkyl-, alkenyl-, isoalkyl- or cycloalkyl-trialkoxysilanes and/or phenyl-trialkoxysilanes and/or corresponding methyldialkoxy silanes; and optionally (C) a tetra-alkoxysilane, by hydrolysis and condensation (in succession or as a mixture) at 10-95 degrees C with 0.6-1.2 mols water per 1 mol silicon and 0.1-5 times the weight of methanol or ethanol (based on alkoxysilanes), followed by distillation of alcohol at up to 120 degrees C under normal or reduced pressure.

Piperidine and pyrrolidine derivatives comprising a nitric oxide donor for treating stress

Abstract: The present invention relates to chemical compounds comprising a nitric oxide (NO) donor and a superoxide ion (O2-) scavenger, their preparation and their use in the treatment of conditions associated with oxidative stress or endothelial dysfunction. In particular, the present invention relates to chemical compounds of formula (I) wherein: R1 may be the same or different and are independently selected from hydrogen, alkoyl, alkoxy, carboxy, hydroxy, amino, amido, cyano, nitro, thio, sulphonyl, sulphoxide alkyl goups comprising an NO-donor, provided that at least one R1 is a group comprising an NO-donor, R2 may be the same or different and are independently selected from alkyl groups; n is an integer 1, 2 or 3; or a salt thereof.

New peptide aldehyde and boronic acid derivatives are proteinase inhibitors useful for treatment of viral infections, especially hepatitis

Abstract: Peptide aldehydes and boronic acid derivatives (I) and their base salts are new. They are prepared from new peptide acetals (II) and peptide-substituted dioxaborolanes (III). Peptide aldehydes and boronic acid derivatives (I) and their base salts are new: E = CHO or B(OH)2; R = 1-7C alkyl (optionally substituted with halo, CN, 1-7C alkylthio, aryl-1-7C alkylthio, aryl or heteroaryl); 2-7C alkenyl; or 2-7C alkynyl; R = R2a or R2b; R2a = 1-7C alkyl (optionally substituted with OH, COOH, aryl, CONH2 or 3-7C cycloalkyl); R2b = aryl-1-7C alkoxy-1-7C alkyl or heteroaryl-1-7C alkyl; R = H or 1-7C alkyl; or R +R = di- or trimethylene optionally substituted with OH; R = 1-7C alkyl (optionally substituted with OH, 3-7C cycloalkyl, COOH, aryl, 1-7C alkylthio, cyano-1-7C alkylthio or aryl-1-7C alkylthio); 2-7C alkenyl; aryl; or 3-7C cycloalkyl; R = R5a or R5b; R5a = 1-7C alkyl (optionally substituted with OH, 1-7C alkylthio, aryl, aryl-1-7C alkylthio or cyano-1-7C alkylthio); or 3-7C cycloalkyl; R5b = 3-7C cycloalkyl-1-7C alkyl; R = H or 1-7C alkyl; R = R7a or R7b; R7a = 1-7C alkyl (optionally substituted with OH, COOH, aryl or 3-7C cycloalkyl); or 3-7C cycloalkyl; R7b = 1-7C alkyl (which is substituted with aryl-1-7C alkylthio, aryl-1-7C alkoxy-aryl, aryl-1-7C alkoxycarbonyl, aryl-1-7C alkylcarbonyl, nitroguanidino, arylsulfonylguanidino, 1-7C alkylsulfonyl or acetamidomethylthio or heteroaryl); or is aryl; R = R8a or R8b; R8a = 1-7C alkyl (which is substituted with OH, COOH or aryl); R8b = 1-7C alkyl which is substituted with SH, 1-7C alkylsulfonyl, aryl-1-7C alkoxy or aryl-heteroaryl; R = R9a or R9b; R9a = 1-7C alkylcarbonyl; COOH-1-7C alkylcarbonyl; arylcarbonyl; 1-7C alkylsulfonyl; arylsulfonyl; 1-7C alkoxycarbonyl; or aryl-1-7C alkoxycarbonyl; R9b = 1-7C alkylcarbonyl (which is substituted with aryl, heteroaryl, arylaminocarbonyl, heteroarylthio, heteroarylcarbonyl, 1-7C alkoxy, arylcarbonyl, 1-7C alkoxy-1-7C alkoxy-1-7C alkoxy, arylcarbonylamino, 3-7C cycloalkyl, 1-7C alkylcarbonyl-3-7C cycloalkyl, 1-7C alkylcarbonylamino, 1-7C alkylcarbonyloxy, 1-7C alkoxycarbonyl or aryloxy); or is heteroarylcarbonyl; hydroxyfluorenylcarbonyl; heterocyclylcarbonyl; 2-7C alkynylcarbonyl; or 3-7C cycloalkylcarbonyl; provided that R , R , R , R and R are not simultaneously R2a, R5a, R7a, R8a and R9a. Independent claims are also included for: (a) the preparation of the compounds (I); (b) peptide acetals of formula (II); and (c) peptide-substituted dioxaborolanes of formula (III). R and R = 1-7C alkyl; Q = group of formula (a) or (b): R - R = H or 1-7C alkyl; any COOH, OH and/or CONH2 groups present in (II) and (III) are protected.

Organophotoreceptors for electrophotography featuring novel charge transport compounds

Abstract: Organic photoreceptors that include a charge transport compound, a charge generating compound, and an electroconductive support in which the charge transport compound is a novel aryl hydrazone-functional carbazole compound.

Conformationally Mobile Wide Rim Carbamoylmethylphosphine Oxide (CMPO)-Calixarenes.

Abstract: Six new calix[4]arene derivatives 2a–f have been synthesised, bearing CMPO-like functions (-NH–C(O)–CH2–P(O)Ph2) at their wide rim. They differ by their alkoxy groups at the narrow rim, comprising all possible combinations of methoxy and syn-propoxy groups including the conformationally mobile tetramethyl ether 2e and the tetrapropyl ether 2f fixed in the cone conformation. Their extraction behaviour for thorium(IV) and several lanthanides(III) from 1M HNO3 to dichloromethane has been studied and compared also to non cyclic calixarene analogues 6a–e. Surprisingly the best extraction results were found for the 1,2-dimethoxy-3,4-dipropoxy derivative 2c among the calixarenes and for the tetramer 6d among the linear compounds. Extraction of americium(III) in comparison to curium(III) and various lanthanides(LaIII), Ce(III), Nd(III), Sm(III), Eu(III)) from 0.1– 3M HNO3 to NPHE (o-nitrophenyl hexyl ether) was most effective again for 2c. Among these cations, the highest distribution coefficients were found for Am(III) and the lowest for Ce(III) with a maximum generally in the range of 1–2M HNO3.

Amide derivatives which are useful as cytokine inhibitors

Abstract: The invention concerns amide derivatives of the Formula (I) wherein R3 is (1-6C)alkyl or halogeno; Q is aryl or heteroaryl which optionally bears 1, 2, 3 or 4 substituents such as hydroxy, halogeno, trifluoromethyl, cyano, (1-6C)alkyl, (1-6C)alkoxy, halogeno-(1-6C)alkyl, hydroxy-(1-6C)alkyl, di-[(1-6C)aklyl]amino-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, (1-6C)alkoxy-(2-6C)alkoxy, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, amino-(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, aryl-(1-6C)alkoxy, heteroaryl, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyl-(1-6C)alkyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; p is 0-2 and R2 is a substituent such as hydroxy and halogeno; q is 0-4; and R4 includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatement of diseases or medical conditions mediated by cytokines.

Acryloxypropyl- or methacryloxypropyl-functional siloxane oligomers

Abstract: Mixtures of catenate and cyclic siloxane oligomers of formula I and II ##STR1## wherein the substituents R consist of 3-methacryloxypropyl or 3-acryloxypropyl groups and methoxy, ethoxy and/or propoxy groups alone or together with C 1 -C 18 alkyl, fluoroalkyl, isoalkyl or cycloalkyl groups and/or C 6 -C 12 aryl groups and where not more than one 3-methacryloxypropyl or 3-acryloxypropyl group is attached to one silicon atom and the degree of oligomerization of compounds of the formula I is within the range 2

Benzothiophenes, benzofurans, and indoles useful in the treatment of insulin resistance and hyperglycemia

Abstract: This invention provides compounds of Formula I having the structure A is hydrogen, halogen, or OH; B and D are each, independently, hydrogen, halogen, CN, alkyl of 1-6 carbon atoms, aryl, aralkyl of 6-12 carbon atoms, hydroxyalkyl of 1-6 carbon atoms, hydroxyaralkyl of 6-12 carbon atoms, cycloalkyl of 3-8 carbon atoms, nitro, amino, —NR1R1a, —NR1COR1a, —NR1CO2R1a, cycloalkylamino of 3-8 carbon atoms, morpholino, furan-2-yl, furan-3-yl, thiophen-2-yl, thiophen-3-yl, —COR1b or OR; R is hydrogen, alkyl of 1-6 carbon atoms, —COR1, —(CH2)nCO2R1, —CH(R1a)CO2R1, —SO2R1, —(CH2)mCH(OH)CO2R1, —(CH2)mCOCO2R1, —(CH2)mCH═CHCO2R1, or —(CH2)mO(CH2)CO2R1; R1 is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, aryl, or CH2CO2R1; R1′ is hydrogen or alkyl of 1-6 carbon atoms E is S, SO, SO2, O, or NR1c; X is hydrogen, halogen, alkyl of 1-6 carbon atoms, alkenyl of 2-7 carbon atoms, CN, aryl, aralkyl of 6-12 carbon atoms, hydroxyalkyl of 1-6 carbon atoms, hydroxyaralkyl of 6-12 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, aryloxy; arylalkoxy, nitro, amino, NR2R2a, NR2COR2a, cycloalkylamino of 3-8 carbon atoms, morpholino, alkylsulfanyl of 1-6 carbon atoms, arylsulfanyl, pyridylsulfanyl, 2-N,N-dimethylaminoethylsulfanyl, —OCH2CO2R2b or —COR2c; Y is hydrogen, halogen, alkyl of 1-6 carbon atoms, aryl, aralkyl of 6-12 carbon atoms, hydroxyalkyl of 1-6 carbon atoms, hydroxyaralkyl of 6-12 carbon atoms, —OR3, SR3, NR3R3a, —COR3b, morpholine or piperidine; R1a, R1c, R2, R2a R3, R3a are each, independently, hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, or aryl; R1b is alkyl of 1-6 carbon atoms or aryl; R2b is hydrogen, alkyl of 1-6 carbon atoms; R2c and R3b are each, independently, alkyl of 1-6 carbon atoms, aryl, or aralkyl of 6-12 carbon atoms; C is hydrogen, halogen or OR4; R4 is hydrogen, alkyl of 1-6 carbon atoms, —CH(R5)W, —C(CH3)2CO2R6, 5-thiazolidine-2,4-dione, —CH(R7)(CH2)mCO2R6, —COR6, —PO3(R6)2, —SO2R6, —(CH2)pCH(OH)CO2R6, —(CH2)pCOCO2R6, —(CH2)pCH═CHCO2R6, or —(CH2)pO(CH2)qCO2R6; R5 is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, aryl, —CH2(1H-imidazol-4-yl), —CH2(3-1H-indolyl), —CH2CH2(1,3-dioxo-1,3-dihydro-isoindol-2-yl), —CH2CH2(1-oxo-1,3-dihydro-isoindol-2-yl), —CH2(3-pyridyl), —CH2CO2H, or —(CH2)nG; G is NR6aR7a, NR6aCOR7a, W is CO2R6, CONH2, CONHOH, CN, CONH(CH2)2CN, 5-tetrazole, —PO3(R6)2, —CH2OH, —CONR6bCHR7b, —CH2NR6bCHR7bCO2R6, —CH2OCHR7bCO2R6 —CH2Br, or —CONR6bCHR7bCO2R6; R6, R6a, R7, R7a are each, independently, is hydrogen, alkyl of 1-6 carbon atoms, or aryl; R6b is hydrogen or —COR6c; R6c is alkyl of 1-6 carbon atoms or aryl; R7b is hydrogen, alkyl of 1-6 carbon atoms, or hydroxyalkyl of 1-6 carbon atoms; Z1 and Z2 are each, independently, hydrogen, halogen, CN, alkyl of 1-6 carbon atoms, aryl, aralkyl of 6-12 carbon atoms, cycloalkyl of 3-8 carbon atoms, nitro, amino, —NR1R1a, —NR1COR1a, cycloalkylamino of 3-8 carbon atoms, morpholino, or OR8, or Z1 and Z2 may be taken together as a diene unit having the formula —CH═CR9—CR10═CR11—; R8 is hydrogen, alkyl of 1-6 carbon atoms, or aryl; R9, R10, and R11 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, aryl, halogen, hydroxy, or alkoxy of 1-6 carbon atoms m is 1 to 4 n is 1 or 2; p is 1 to 4; q is 1 to 4; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.