Showing papers on "Alkoxy group published in 1982"

1-(Aminoalkylphenyl and aminoalkylbenzyl)-indoles and indolines and analgesic method of use thereof

Abstract: The invention relates to 1-(aminoalkylphenyl and aminoalkylbenzyl)indoles and indolines of the formula: ##STR1## where R 1 and R 2 are the same or different and are hydrogen, lower alkyl, cycloalkyl and acyl of the formula ##STR2## where R 3 is lower alkyl, lower alkoxy, cycloalkyl, phenyl of the formula ##STR3## and Ar lower alkyl of the formula ##STR4## X is hydrogen, halogen, lower alkoxy, Ar lower alkoxy of the formula ##STR5## m and p are independently integers of 0 and 1 and the pharmaceutically acceptable acid addition salts thereof.

Liquid crystal mixtures

Abstract: Liquid crystal mixtures containing a coloring substance which comprise about 5 to about 40 weight % of trans-p-[5-(4-alkylcyclohexyl)-2-pyrimidinyl]benzonitriles, about 10 to about 60 weight % of trans-4-alkylcyclohexane carboxylic acid phenyl esters and about 0.1 to about 15 weight % of one or more coloring substances of the formula ##STR1## wherein m stands for the number 1 and X is alkoxy and Y is nitro; or m stands for the number 1 or 2; and X is p-alkoxyphenyl and Y is nitro or dialkylamino, or X is alkoxy and Y is -p-nitrophenyl or -(dialkylamino)phenyl; or m stands for the number 2, and X is alkoxy and Y is alkoxy, nitro or dialkylamino, or both X and Y are dialkylamino; and wherein the alkoxy denotes a straight-chain group containing 1 to 12 carbon atoms and the alkyl groups in the dialkylamino each denote a straight-chain alkyl group containing 1 to 4 carbon atoms are described.

Process for producing olefin polymers or copolymers and catalyst components used therefor

Abstract: A process for producing olefin polymers or copolymers which comprises polymerizing olefins or copolymerizing olefins with each other or with dienes in the presence of a catalyst system composed of the following components (A), (B) and (C): (A) a solid titanium catalyst component containing magnesium, titanium, halogen and an ester selected from the group consisting of esters of polycarboxylic acids and esters of polyhydroxy compounds, said catalyst component being obtained by contacting a liquid hydrocarbon solution of (i) a magnesium compound with (ii) a titanium compound in the liquid state to form a solid product or first preparing a liquid hydrocarbon solution of the magnesium compound (i) and the titanium compound (ii) and then forming a solid product therefrom, said reaction of forming the solid product being carried out in the presence of (D) at least one electron donor selected form the group consisting of monocarboxylic acid esters, aliphatic carboxylic acids, carboxylic acid anhydrides, ketones, aliphatic ethers, aliphatic carbonates, alkoxy group-containing alcohols, aryloxy group-containing alcohols, organic silicon compounds having an Si-O-C bond and organic phosphorus compounds having a P-O-C bond, and during or after the formation of the solid product, contacting the solid product with (E) and ester selected from the group consisting of esters of polycarboxylic acids and esters of polyhydroxy compounds, (B) and organometallic compound of a metal selected from the group consisting of metals of Groups I to III of the periodic table, and (C) and organic silicon compound having an Si-O-Cbond or Si-N-C bond;and a solid titanium catalyst component used therefor.

Organosilicone coating composition

Abstract: Coating compositions in accordance with the invention are usefully coated on substrates, such as plastic lenses, and cured. The cured coatings provide excellent abrasion resistance and good adherence and weathering properties. The coating compositions comprise an organic solvent and a mixture of at least two components derived by partial hydrolysis from precursor organosilicone compounds. The precursor compounds include a plurality of alkoxy groups, and the at least two components are partially hydrolyzed by greater than 40% of a stoichiometric amount of water required to hydrolyze the alkoxy groups. A first component of the two components is in an imine, aminal or enamine form, which extends working life of the coating compositions.

Derivatives of cis, endo-2-azabicyclo-(3.3.0)-octane-3-carboxylic acid, process for their preparation, medicines containing them and their use

Abstract: of the disclosure: Compounds of the formula I (I) in which the carboxyl group on carbon atom 3 is orienta-ted in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R1 denotes hydro-gen, allyl, vinyl or a side-chain of a naturally occurring ?-aminoacid, which may be protected, R2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and Z denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl or cycloalkyl, or aryl which is optionally mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, di-alkylamino or methylenedioxy, or denotes indol-3-yl, a process for their preparation, agents containing these com-pounds and their use. Compounds of the formula I have a long-lasting intense hypotensive action.

Aldol strategy: coordination of the lithium cation with an alkoxy substituent

Abstract: In Abhangigkeit von der Grose der Substituenten R1 und (insbesondere) R2 verlauft die Enolat-Bildung der Ketone (I) bis zu 100% stereoselektiv zugunsten des Z-Enolats ((II) und (III) werden als Trimethylsilylether bestimmt).

Treatment of diarrhoea

Abstract: A compound of formula (I) wherein (i) P is a bond, oxygen, sulphur, NR4, methylene, ethylene or vinylene and X is and R1 and R2 are each hydrogen, halogen, hydroxy, acyloxy, lower alkyl, lower alkoxy or trifluoromethyl and R3 is hydrogen, lower alkyl, lower aralkyl; aminoethyl or aminopropyl each optionally N-substituted by lower alkyl, or lower alkyl substituted nitrogen-containing heterocyclyl. and R4 is lower alkyl, and R5 is hydrogen, or (ii) P is - CR6R7 and X is wherein the nitrogen is bonded to P. and R1 is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, halogen or trifluoromethyl, and R3 is hydrogen, lower or higher alkyl, lower alkenyl or lower alkynyl, C3-7 cycloalkyl, C3-7 cycloalkenyl or lower alkyi substituted by C3-7 cycloalkyl, hydroxy, amino, mono- or diloweralkylamino, carboxy, lower carbalkoxy, carbamoyl, mono- or di- lower alkyl-carbamoyl, phenyl, lower alkanoyl or phenylcarbonyl and R5, R6 and R7 are each hydrogen or lower alkyl and R8 is hydrogen, lower alkyl, carboxy, lower carbalkoxy, or lower alkyl substituted by hydroxy, amino, mono- or di- lower alkyl amino, or a lower or higher alkanoyl, adamantoyl, carbamoyl, mono- or di- lower alkyl carbamoyl, C3-7 cycloalkyl carbonyl or phenyl carbonyl derivative or a 2-N-oxide, 2-N-lower alkyl or phenyl lower alkyl quaternary derivative or a pharmaceutically acceptable salt thereof, is useful in treating diarrhoea or scours.

1-Aryl 2-aminomethyl cyclopropane carboxyamide (Z) derivatives and their use as useful drugs in the treatment of disturbances of the central nervous system

Abstract: The present invention concerns new derivatives of 1-aryl 2-aminomethyl cyclopropane carboxamides (Z) of general formula I: ##STR1## in which: R represents a hydrogen or halogen atom, a lower alkyl group, a lower alkoxy group, or a hydroxy. nitro or amino group; n represents the value 1 or 2; R 1 and R 2 represent a hydrogen atom, a lower alkyl group, an aryl or lower alkaryl group, possibly substituted, preferably in para position, by a halogen atom, preferably a chlorine atom; R 1 and R 2 may also form a heterocycle having 5 or 6 members with the adjacent nitrogen atom; R 3 and R 4 represent a hydrogen atom or a lower alkyl group; R 3 and R 4 may also form with the adjacent nitrogen atom a heterocycle having 5 or 6 members, possibly containing an additional heteroatom selected from among nitrogen and oxygen, as well as their salts with therapeutically acceptable inorganic or organic acids, and their pharmaceutical compositions and use in the treatment of central nervous system disturbances, e.g., depression.

Substituted 9-(1 or 3-monoacyloxy or 1,3-diacyloxy-2-propoxymethyl) purines as antiviral agent

Abstract: Compounds useful as antiviral agents are defined by the following formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R1 is hydrogen or --C(O)R7 wherein R7 is hydrogen, alkyl of one to nineteen carbon atoms, hydroxyalkyl of one to eight carbon atoms, alkoxyalkyl of two to nine carbon atoms, alkenyl of two to nineteen carbon atoms, phenyl, 1-adamantyl or 2-carboxyethyl and the pharmaceutically acceptable alkali metal salts thereof; R2 is --C(O)R7 wherein R7 is as defined above; R3 is hydrogen, halo, thio, lower alkylthio of one to six carbon atoms, azido, NR9 R10 wherein R9 and R10 are independently hydrogen or lower alkyl of one to six carbon atoms or --NHC(O)R8 wherein R8 is hydrogen, alkyl of one to nineteen carbon atoms or 1-adamantyl; and (a) R6 is hydrogen, halo, lower alkoxy of one to six carbon atoms, azido, thio, lower alkylthio of one to six carbon atoms, --NR9 R10 wherein R9 and R10 are as defined above or --NHC(O)R8 wherein R8 is as defined above and R4 together with R5 is a bond; or (b) R5 together with R6 is a keto group and R4 is hydrogen.

Saturated and Unsaturated Wax Esters Produced by Acinetobacter sp. HO1-N Grown on C16-C20n-Alkanes

Abstract: The wax ester compositions produced by the action of Acinetobacter sp. HO1-N on n-alkanes (C16 through C20) were analyzed using capillary gas chromatography/mass spectrometry (GC/MS). The wax esters contained, surprisingly, a large percentage of mono-and diunsaturated components. The acyl and alkoxy segments are reported for each wax ester component. Also, the positions of the carbon-carbon double bonds in the wax esters produced from the C16 and C20 n-alkanes are reported. These microbial-produced wax ester mixtures bear a close chemical similarity to those of sperm whale and jojoba oils.

Synthesis of benzyl and benzyloxycarbonyl base-blocked 2'-deoxyribonucleosides

Abstract: Acylimidazoles have been alkylated with trialkyloxonium tetrafluoroborates to form acylimidazolium salts. These salts, particularly (benzyloxycarbonly)imidazolium salts, are shown to be effective agents for the direct, mono-N-protection of deoxynucleosides as their acyl derivatives. These acyl nucleosides are also available via thiocarbamate intermediates. Thus 3',5'-bis(tert-butyldimethylsilyl)-2'-deoxyguanosine, on treatment with phenyl chlorothioformate, gave the 6-thiophenyl-substituted purine (1). The thiophenyl group of (1) can be replaced by hydrogen, amino, and alkoxy groups to give a variety of substituted purine deoxyribonucleosides.

Long-chain alpha, omega-dicarboxylic acids and derivatives thereof and pharmaceutical compositions containing them

Abstract: Long-chain .alpha.,.omega.-dicarboxylic acids of formula I' I' and in vivo hydrolyzable functional derivatives of the carboxylic groups thereof, wherein R1 and R2 each independently represents lower alkyl;lower alkyl substituted by hydroxy, lower alkoxy, halogen or phenyl which may be substituted one or more times by hydroxy, lower alkoxy, lower alkyl or halogen; lower alkenyl; lower alkynyl; C3 - C7 cycloalkyl; phenyl or phenyl substituted by hydroxy, halogen, lower alkyl or lower alkoxy; X and Y indepen-dently represents hydrogen, lower alkyl, lower alkoxy, cyano, halogen carboxyl, lower alkoxy-carbonyl, carbamoyl or hydroxy and Q represents a linear, satu-rated or unsaturated alkylene chain of 8 to 14 carbon atoms which may be -(a) substituted by oxygen, halogen, hydroxy or lower alkoxy, (b) interrupted by one or more heteroatoms and/or (c) of which 1 - 4 chain members may be part of a C3 - C7 cycloalkyl or phenyl ring pro-vided that when Q represents a linear saturated alkylene chain of 8 to 14 carbon atoms, R1 and R2 represents methyl and Y hydrogen, then X is not hydrogen, ethoxycarbonyl, bromo, cyano or methyl or when R1 and R2 represents methyl, X and Y are hydrogen, then Q is not the group provide a significant lipid-lowering effect as well as an antidiabetic effect.

Studies on 2-Aziridinecarboxylic Acid. VI. Synthesis of β-Alkoxy-α-Amino Acids via Ring-opening Reaction of Aziridine

Abstract: The reaction of aziridine derivatives having a urethane-type protecting group with several alcohols in the presence of boron trifluoride etherate afford the corresponding optically pure O-alkylserine and O-alkylthreonine derivatives via a ring-opening reaction of aziridine in good yield.

Process for the curing of stoving lacquers

Abstract: Quinolinium sulfonates of the formula I ##STR1## wherein R1 is C1 -C8 -alkyl, C1 -C4 -alkyl substituted by halogen, hydroxyl or C1 -C4 -alkoxy, or it is C2 -C8 -alkenyl, C7 -C9 -phenylalkyl or C5 -C8 -cycloalkyl, R2, R3, R4 and R5 independently of one another are each hydrogen, C1 -C4 -alkyl, halogen, --CN, --COO(C1 -C4 -alkyl), --CHO, hydroxyl, C1 -C4 -alkoxy, an acyloxy group R7 COO--, a group R8 --CH═CH--, C7 -C9 -phenylalkyl or phenyl, R6 is C1 -C12 -alkyl, C6 -C10 -aryl which is unsubstituted or mono- or polysubstituted by C1 -C12 -alkyl, C1 -C4 -alkoxy, halogen or a group R7 CONH--, or it is fluorine, NH2 or CF3, and R7 and R8 independently of one another are each C1 -C4 -alkyl or phenyl, are suitable as latent curing catalysts for acid-curable stoving lacquers. There is formed by irradiation with UV light the actual acid catalyst, which renders possible curing at relatively low stoving temperatures.

An improved procedure for the synthesis of choline phospholipids via 2-bromoethyl dichlorophosphate.

Abstract: Choline phospholipids can be conveniently synthesized by reaction of a lipophilic alcohol, such as diacylglycerol, with 2-bromoethyl dichlorophosphate followed by nucleophilic displacement of the bromine with trimethylamine. We found that the low yields often encountered in the initial phosphorylation step are particularly due to exchange of both chlorines for alkoxy functions (triester formation) and to chlorination of the alcohol by 2-bromoethyl dichlorophosphate. However, these drawbacks can be overcome by proper choice of the reaction medium and by optimizing other reaction conditions. The procedure described is efficient and most versatile, and it lends itself to the preparation of a wide range of choline phospholipids containing a glycerol, diol, or long-chain alkyl backbone and bearing various aliphatic functions. Proton and carbon-13 nuclear magnetic resonance spectroscopy proved useful in establishing the homogeneity and structures of the synthetic intermediates and byproducts and of the choline phospholipids synthesized.

Water and oil repellent for glass surface

Abstract: PURPOSE: To provide the titled water and oil repellent capable of imprating a glass surface with water-repellency, oil-repellency and stain resistance for a long period, by mixing water glass to a silane compound containing polyfluoroalkyl group. CONSTITUTION: The objective water and oil repellent is prepared in the form of a solvent solution, etc. by mixing (A) a compound having polyfluoroalkyl group (hereinafter called as Rf group) and represented by the formula (Rf is 4W16C perfluoroalkyl containing one or more ether bonds; Q is bivalent orgnaic group; Z is 1W4C lower alkyl; Y is halogen, alkoxy or RCOO-), e.g. RfCH 2 CH 2 SiCl 3 , or the partial hydrolytic condensate of said compound, and (B) water glass (e.g. sodium metasilicate) with (C) an organic solvent (e.g. tetrahydrofuran). The weight ratios of the Rf group-containing silane compound to water glass is preferably 1:0.1W5. USE: Treatment of glass plate, mirror, etc. COPYRIGHT: (C)1983,JPO&Japio

Colorless liquid crystalline compounds

Abstract: A colorless liquid crystalline compound having at least one 6-membered ring and non-cyclic end groups in the molecular skeleton, said 6-membered ring containing two or more carbon atoms, at least one of which is directly bonded to a methylene group of a non-cyclic group having an alkoxy group at another end has a wide mesomorphic range. When said colorless liquid crystalline compound is mixed with a liquid crystal composition, the resulting mixture also has an enlarged mesomorphic range and in almost all cases has a reduced viscosity.

Fate of oxygen free radicals in extracellular fluids.

Abstract: 1. Oxygen radicals in biological systems and the importance of iron Oxygen radicals can be either organic or inorganic. The organic radicals such as the peroxy (ROO') and alkoxy (RO') are those derived from complex molecules like the polyunsaturated fatty acids. The inorganic oxygen radicals are the superoxide radical (O,-*) and the hydroxyl radical (OH'). Formation of the highly reactive hydroxyl radical appears to be due to either ionizing radiation or to the simultaneous presence of superoxide and hydrogen peroxide with suitable iron catalysis, i.e. 20,-' + 2H+ + H,O, + 0,

Sulphonamidophenylcarboxylic acid compounds and pharmaceutical compositions containing them

Abstract: The invention provides sulphonamides of the formula ##STR1## wherein R is a hydrogen atom or a lower alkyl radical; R 1 is alkyl, aryl, aralkyl or aralkenyl, the aryl moiety of which in each case can be optionally substituted one or more times by hydroxyl, halogen, trifluoromethyl, lower alkyl or alkoxy or by acyl, carboxy or alkoxycarbonyl; n is 1, 2 or 3; and W is a valence bond or a divalent aliphatic hydrocarbon linkage and the physiologically acceptable salts, esters and amides of such compound. These compounds have excellent pharmacological lipid depressing activity and inhibit thrombocyte aggregation.

Sulfonate derivatives, process for preparing same and antilipemic compositions containing the derivative

Abstract: A sulfonate derivative represented by the formula ##STR1## wherein R1 is lower alkyl, lower alkoxy or halogen, l is an integer of from 0 to 3, n is 0 or 1, A is straight-chain or branched-chain alkylene having 1 to 4 carbon atoms, and R2 is hydrogen or lower alkyl but, when n is 0 or 1 and A is straight-chain alkylene with 1 to 4 carbon atoms, is not hydrogen and the method for preparing the same.

Antimalarials. 13. 5-Alkoxy analogues of 4-methylprimaquine.

Abstract: A series of nuclear and side-chain analogues of 4-methylprimaquine incorporating an alkoxy group in the 5-position of the quinoline nucleus has been prepared. The compounds were tested for suppressive antimalarial activity against Plasmodium berghei in mice and for radical curative antimalarial activity against Plasmodium cynomolgi in the rhesus monkey. Although the toxicity problems characteristic of the 8-aminoquinolines were not overcome, several of the compounds, surprisingly, were highly effective as both blood and tissue schizonticidal agents.

Phospholipid derivatives, processes for preparation thereof and pharmaceutical composition of the same

Abstract: New phospholipid derivatives represented by the formula: ##STR1## wherein R1 is alkyl, alkoxy, alkylthio or alkylsulfonyl; R2 is hydrogen, hydroxy, alkoxy, lower alkanoyloxy or lower alkylcarbamoyloxy; n is 0 or 1; R3 is hydroxy or protected hydroxy; and R4 is lower alkoxy or lower alicyclic-oxy group which is substituted with 2 or more hydroxy or protected hydroxy groups, and may be substituted with lower alkoxy or another alicyclic-oxy group having two or more hydroxy or protected hydroxy groups, in which the alicyclic ring may contain an oxygen atom; and pharmaceutically acceptable salt thereof, which exhibit antitumor activity.

Pharmaceutical amides, and preparation, formulations and use thereof

Abstract: Compounds of the general formula ##STR1## wherein Ph is a phenyl group which is optionally substituted by one or more substituents selected from halo (i.e. fluoro, chloro, bromo or iodo), C1-4 alkyl, amino, C1-4 alkylamino, di-C1-4 alkylamino, nitro, sulphonyl, aminosulphonyl, trihalomethyl, carboxy, C1-4 alkoxycarbonyl, amido, C1-4 alkylamido C1-4 alkoxy, C2-4 alkenyl, cyano, aminomethyl or methylsulphonyl; Ra and Rb, which may be the same or different, each represents a hydrogen or alkali metal (e.g. sodium or lithium) atom or a C1-4 (e.g. ethyl) group; m is 0 or 1; Y is a group of formula: --NH--CH2 --CO-- or a group of formula: ##STR2## where R1 is hydrogen or methyl; R2 is alkyl of 1 to 3 carbon atoms or is methylthiomethyl; and Z is --OR3 or --NR4 R5 where R3, R4 and R5 are each hydrogen or alkyl of 1 to 4 carbon atoms (i.e. methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, or t-butyl) and R3 can further be phenylalkyl having 1 to 3 carbon atoms in the alkylene moiety thereof, or phenyl; and basic salts thereof. These compounds have an advantageous enkephalinase inhibitory activity which renders the compounds useful in medical therapy, e.g. to prolong and/or potentiate in a mammal, the effects of endogenous or exogenous enkephalins. The latter includes synthetic enkepalin analogues.

Succinimide derivatives, compositions and method of use

Abstract: Succinimide derivatives representable by the following formula: ##STR1## wherein X and Y are combined to form a group of the formula: ##STR2## (wherein A is an oxygen atom, a methylene group or an ethylene group and a full line accompanying a broken line ( ) is a single bond or a double bond) and Z is a hydrogen atom or, X and Z are combined to form a group of the formula: ##STR3## (wherein A and a full line are each as defined above) and Y is a hydrogen atom, R is a phenyl group, optionally substituted with halogen, C1 -C4 alkyl, C1 -C4 alkoxy or trifluoromethyl, a 2-pyridyl group or a 2-pyrimidinyl group and n is an integer of 3 or 4, and pharmaceutically acceptable acid addition salts thereof, which are useful as antianxious substances.