ПРОИЗВОДНЫЕ АМИНОКИСЛОТЫ, СПОСОБ ИХ ПОЛУЧЕНИЯ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ПОДАВЛЕНИЯ МНОЖЕСТВЕННОЙ ЛЕКАРСТВЕННОЙ УСТОЙЧИВОСТИ

Описываются новые соединения формулы I, где В и D независимо друг от друга обозначают водород или Аr-замещенный (C1-С6)-алкил с прямой или разветвленной цепью; R1 - (C1-С6)-алкил с прямой или разветвленной цепью или Аr-замещенный (C1-С6)-алкил с прямой или разветвленной цепью; J обозначает (C1-С6)-алкил с прямой или разветвленной цепью; К обозначает (C1-С6)-алкил с прямой или разветвленной цепью, фенилзамещенный (C1-С6)-алкил с прямой или разветвленной цепью, где фенил может быть замещен галогеном; Х обозначает фенил, замещенный O-(C1-С6)-алкилом; Аr обозначает фенил, или Аr является гетероциклической ароматической группой, выбираемой из группы, включающей 2-пиридил, 3-пиридил, 4-пиридил и имидазолил, причем Аr может быть замещен галогеном, которые могут быть использованы для подавления множественной лекарственной устойчивости. Описывается также способ их получения, фармацевтическая композиция и способ подавления множественной лекарственной устойчивости. 6 c. и 5 з.п. ф-лы, 3 табл.

НОВЫЕ АЦИЛИРОВАННЫЕ ПСЕВДОДИПЕПТИДЫ, СПОСОБ ИХ ПОЛУЧЕНИЯ И СОДЕРЖАЩИЕ ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ

Изобретение относится к N-ацилированным псевдодипептидам, соответствующим общей формуле I в которой R1 и R2 обозначают каждый ацильную группу карбоновой кислоты, имеющей от 2 до 24 атомов углерода, которая может быть насыщенной или ненасыщенной, линейной или разветвленной, незамещенной или имеющей один или несколько заместителей, выбранных из гидроксила, алкила, групп алкокси, ацилокси, амино, ациламино, ацилтио и C1-C24алкилтио; дескрипторы m, р и q могут принимать значения от 1 до 10; дескриптор n может принимать значения от 0 до 10; X и Y каждый обозначают водород или кислотную группу, выбранную из следующих групп: карбокси-С1-С5-алкил, -СН-[(СН2)mСООН][(СН2)nСООН], где m = 0-5 и n = 0-5, фосфоно-С1-С5-алкил, дигидроксифосфорилокси-С1-С5-алкил, диметоксифосфорил, фосфоно, гидроксисульфонил, гидроксисульфонил-С1 -С5-алкил, гидроксисульфонилокси C1-C5-алкил в нейтральной или заряженной форме при условии, что по крайней мере один из заместителей X и Y обозначает определенную выше кислотную ...

АЛЬФА-СПИРАЛЬНЫЕ МИМЕТИКИ И СПОСОБЫ, СВЯЗАННЫЕ С НИМИ

Изобретение относится к соединению формулы (I) или к его фармацевтически приемлемой соли, где А означает -CHR-, где Rозначает водород, Cалкил, необязательно замещенный заместителем, выбранным из -ОН, -OR, где Rозначает Cалкил, -NH, -COOH и -CONH, Cарил-Cалкил, необязательно замещенный 1-3 заместителями, выбранными из -ОН, -ОР(=O)(ОН), -ОР(=O)(ONa)и Cалкила, 5-9-членный гетероарил-Cалкил, Cциклоалкил-Cалкил, Сарил или Cциклоалкил; G означает -NR- или -О-, где Rнезависимо выбирают из Cалкила и Салкенила; Rозначает -Ra-R; где Ra означает Cалкилен и Rозначает нафтил или 9-10-членный бициклический конденсированный гетероарил, необязательно замещенный заместителем, выбранным из -NHи галогена; Rозначает -W-W-Rb-R, где Wозначает -(СО)-; Wозначает -О- или -NH-; Rb означает связь или Cалкилен, необязательно замещенный Cалкилом; и Rозначает Cалкил, Сарил, необязательно замещенный галогеном, 5-6-членный гетероарил или Cциклоалкил; и Rозначает Cалкил; где "гетероарил" означает моноциклический или бициклический ...

ГИДРОХЛОРИД N-(2,6-ДИМЕТИЛФЕНИЛ)АМИДА 2-(β-N,N-ДИЭТИЛАМИНОЭТИЛАМИНО)-4-ОКСО-4-(4-ЭТОКСИФЕНИЛ)-2-БУТЕНОВОЙ КИСЛОТЫ, ПРОЯВЛЯЮЩИЙ МЕСТНОАНЕСТЕЗИРУЮЩУЮ АКТИВНОСТЬ

Гидрохлорид N-(2,6-диметилфенил)амида 2-(β-N,N-диэтиламиноэтиламино)-4-оксо-4-(4-этоксифенил)-2-бутеновой кислоты формулы ! ! проявляющий местноанестезирующую активность.

Новые ацилированные псевдодипептиды, способ их получения и содержащие их фармацевтические композиции

... 1. N-ацилированные псевдодипептиды, соответствующие общей формуле I: в которой R1 и R2 обозначают, каждый, ацильную группу карбоновой кислоты, имеющей от 2 до 24 атомов углерода, которая может быть насыщенной или ненасыщенной, линейной или разветвленной, незамещенной или имеющей один или несколько заместителей, выбранных из гидроксила, алкила, групп алкокси, ацилокси, амино, ациламино, ацилтио и C1-C24- алкилтио; m, p и q = 1 - 10; n = 0 - 10; Х и Y, каждый, обозначают водород или кислотную группу, выбранную из следующих групп: карбокси-С1-С5 -алкил, СН-[(СН2)mСООН] [(СН2)nСООН], где m=0-5 и n=0-5, фосфоно-С1-С5-алкил, дигидроксифосфорилокси-С1-С5-алкил, диметоксифосфорил, фосфоно, гидроксисульфонил, гидроксисульфонил-С1-С5-алкил, гидроксисульфонилокси-С1-С5-алкил, в нейтральной или заряженной форме, при условии, что по крайней мере один из заместителей Х и Y обозначает определенную выше кислотную группу в нейтральной или заряженной форме; А и В, независимо один от другого, обозначают атом ...

Способ получения оптически чистых моноэфиров винной кислоты и оптически активных алканоламинов или их солей

Изобретение касается производных оксикислот, в частности моноэфи- ров винной кислоты и алканоламинов общей формулы (1)А - С (OR,) - CH,j - - NHR,, где А - 4 нитрофенШ1, 1-наф- тилок симе тил, 4-индолилоксиметнл феноксильный остаток 4-R,, 2-R -CgHj- -O-CBj-, где R - метоксиэтил, -NHK; К - алканоил С,-С, в котором алкил С,-С 7 или дикарбамоил, в котором алкил С,-Сг; R4-H, СН,-С(0)-; RZ-, водород или разветвленный С,-С -алкил; R,- остаток дизамещенной (R, R)- или ...

Способ получения производных аминокислот или их солей или оптических изомеров

Способ получения производных 1,1-бифенил-2-илалкиламина или их солей

Способ получения производных 1,1-Оифенил-2-илалкиламина общей формулы RI 1Н2- 5Нг-йн-сн2- С он 2 где RI - водород или С -С алкил; R2-C,-C4- алкил, или их солей, отличающийся тем, что 1,2,-эпокск-4-{1,1-бифенил2-ил )-бутан вводят во взаимодействие с амином общей формула ,RI НИ; СО где RJ и R2 имеют указанные значения, при нагревании в органическом растворителе , таком как этанол, и выде- S ляют целевой продукт в свободном виде или в виде соли.

Способ получения ацилированных 2-аминобензофенонов

KATALYTISCHE ASYMMETRISCHE HYDRIERVERFAHREN

Verfahren zur Herstellung von Aminocarbonsaeureamiden, welche die Atomgruppierung ? enthalten

SALZE VON GLYKOSAMINOGLYKANEN, VERFAHREN ZU IHRER HERSTELLUNG UND DIESE SALZE ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSETZUNGEN.

PHARMAZEUTISCH WIRKSAME VERBINDUNGEN UND METHODEN ZU IHRER ANWENDUNG

Verfahren zur Herstellung von antikonvulsivisch wirkenden Carbonsaeureamiden

Verfahren zur Herstellung von beta-Dialkylaminoacylaniliden

2-phenylisopropylaminoacet-2, 6-xylidide - with antiarrhythmic anorectic, antiinflammatory, analgesic and local anaesthetic act

... 2-Phenylisopropylaminoacet-2,6-xylidide and its salts with anti-arrhythmic, local, anaesthetic, anorectic, analgesic and antiinflammatory activity. Prepd. by treating 2,6-xylidine with chloroacetyl chloride to give an intermediate chloracet-2,6-xylidide which is condensed iwth 2-phenylisopropylamine to give the required product.

MITTEL ZUR BEEINFLUSSUNG DES PFLANZENWACHSTUMS

Process for the preparation of N-(2,6-Dialkylphenyl)-N-formylglycine derivatives

Verfahren zum Faerben von Keratinfasern,insbesondere von Haaren,und Mittel zur Durchfuehrung dieses Verfahrens

A process for the manufacture of benzodiazepine derivatives

Compounds of the general formula (wherein R represents an alkyl, alkenyl, hydroxyalkyl or aralkyl group, R1 represents an alkyl or aryl group, R2 represents an alkyl, alkoxy or trifluoromethyl group or a halogen atom, R3 represents a trifluoromethyl, alkyl, alkoxy, alkylthio, hydroxyalkylthio, nitro, amino, alkylsulphinyl, alkylsulphonyl, hydroxy or acylamino group or a halogen atom and R4, which can only be present if R3 is other than a trifluoromethyl group, represents any of the values of R3 except the latter value, and wherein the broken lines denote optional substituents) are prepared by reacting a benzophenone derivative of the general formula (wherein X represents a halogen atom) with ammonia, heating any uncyclized product obtained to effect ring closure and, in the case where R3 and R4 were absent in the benzophenone derivative, subjecting the benzodiazepine formed to one or more of the steps nitration, reduction of the nitro group and acylation ...

Novel trifluoromethyl-benzophenones and the preparation thereof

The invention comprises 2-amino-5-trifluoromethylbenzophenone and 2-amino-21, 5-bis- (trifluoromethyl)-benzophenone, and their preparation by treating the corresponding 2-chlorobenzophenones under pressure with aqueous ammonia in the presence of cuprous chloride. The biscompound is purified via its sulphate. Specification 972,976 also is referred to.

Process for the preparation of aminoacetyl-anilides having alkyl substituents at theamino nitrogen and products thereof

The invention comprises a process for the preparation of amino-acetyl anilides, the benzene nucleus of which contains methyl substituents in the positions 2 and 6, and is either unsubstituted or substituted with a methyl group or an n-butoxy group in the position 4, and the amino group of which contains two alkyl substituents having a total of four carbons at the most, or one alkyl substituent having three carbon atoms, which consists in condensing an amino-acetyl anilide, the benzene nucleus of which contains substituents of the kind above stated, and the amino group of which is either unsubstituted, or, when preparing a dialkyl-substituted compound, may contain an alkyl substituent having three carbon atoms at the most, with an alkylation agent which contains the alkyl group that is to be incorporated in the amino group of the said aminoacetylanilide. Alkylation agents, mentioned include methyl chloride, bromide, iodide, ethyl chloride, bromide, iodide, n-propyl iodide, iso-propyl iodide ...

Improvements in process for the production of aminocarboxylic acids and their n-substituted derivatives

Amino carboxylic acids and their N-substituted derivatives in which a hydrogen of the amino group is substituted by an acyl group are produced by reacting lactones of the formula (in which R1 is a substituted or unsubstituted carbon chain and X is hydrogen or an alkyl radical) with carboxylic acid amides at elevated temperatures, advantageously with the exclusion of moisture, to give N-substituted aminocarboxylic acids which may be saponified with mineral acids or alkali solutions to give amino carboxylic acids. Lactones containing acylatable groups may be used as starting materials, the acylatable groups being unaffected by the reaction. Alternatively when amino carboxylic acids are required as end products lactones which are substituted by groups which can react with ammonia may be used, e.g. if a lactone substituted by halogen is used an aminocarboxylic acid which still contains halogen is obtained. The lactones may be reacted with aliphatic, aromatic, alicyclic ...

PHYSIOLOGICALLY TOLERABLE METAL COMPLEX SALTS FOR USE IN NMR DIAGNOSIS

Novel hydrazine derivatives and a process for the manufacture thereof

The invention comprises compounds of the formula: and their acid addition salts and hydrazones of the general formula wherein R is a hydrogen atom or an amino substituted alkanyol group which may contain a hydroxy group as a further substituent and n is 2 or 3 and the preparation thereof by condensing a hydrazine R-NH-NH2 (wherein the hydrogen atoms of the hydrazine residue not needed for the condensation may be replaced by protecting groups) or a salt thereof with a carbonyl compound of the formula: (wherein R1 is a hydroxy group which may be etherified with a hydrogenolytically removable group) hydrogenating the resulting hydrazone, splitting off any protecting groups and, if desired, alkanoylating and/or converting the resulting hydrazine into a salt. Pharmaceutical compositions comprise the hydrazines of the invention in association with a compatible pharmaceutical carrier. The compositions may be in conventional pharmaceutical ...

Local anesthetic preparations and process of making same

Aqueous anaesthetic solutions, prepared by adding carbon dioxide to an aqueous suspension of a local anaesthetic of the basically substituted acid amide type, e.g. lidocaine, until the anaesthetic base is dissolved, are applied from pressure resistant dispensers in which the propellant may be a mixture of chlorofluorohydrocarbons.ALSO:Aqueous solutions of local anaesthetics of the basically substituted acid amide type are prepared by introducing carbon dioxide, in an amount in excess over that stoichiometrically required for carbonate salt formation, into an aqueous suspension of the anaesthetic, at a temperature not exceeding ambient temperature, until the anaesthetic base has been dissolved. In a modification, an acid addition salt of the anaesthetic base is used together with a water-soluble, acid-neutralizing agent, e.g. sodium bicarbonate, sodium carbonate or sodium hydroxide, in an amount equimolecular to the acid moiety of the addition salt, and carbon dioxide is then introduced ...

Process for the Production of Tertiary-Amino Alkylated Primary Amines

... 1,157,637. Tertiary-amino-alkylated primary amines. STERLING DRUG Inc. 1 July, 1966 [1 July, 1965], No. 29636/66. Heading C2C. Tertiary-amino-alkylated primary amines are obtained by a process which comprises (a) catalytically hydrogenating 2-methylene-glutaronitrile to produce 2-methylglutaronitrile, (b) reductively alkylating 2-methyl-glutaronitrile in the presence of an amine, HNR 1 R 2 , to produce 2-methyl-5-NR 1 R 2 -valeronitrile, (c) hydrolysing 2 - methyl - 5 - NR 1 R 2 - valeronitrile, preferably in an aqueous mineral acid, to produce 2-methyl-5-NR 1 R 2 -valeramide and treating the latter with an aqueous alkaline solution of an alkali metal hypohalite to produce 2-amino-5-NR 1 R 2 -pentane, where NR 1 R 2 is a tertiary amino group and R 1 and R 2 are the same or different and represent lower or higher alkyl, hydroxy lower or higher alkyl, lower alkoxy higher or lower alkyl, di-lower alkylamino lower or higher alkyl, C 3-7 cycloalkyl, phenyl or substituted phenyl, said substituents ...

a-aryl-a,a bis (w-disubstituted amino)alkyl-acetamides and related compoundss

A compound corresponding to the following general formula: wherein R<1> represents C1-C7 alkyl or C5 or C6 cycloalkyl; R<2> represents C1-C7 alkyl; or R<1> and R<2>, together with the nitrogen atom to which they are attached, complete on azamonocyclic ring which may contain at least one further heteroatom and which may be substituted once or twice by phenyl or C1-C4 alkyl; Ar represent pyridyl, trifluoromethylphenyl, biphenylyl, phenyl which may be substituted once or twice by halogen or C1-C4 alkyl, 1- or 2- naphthyl which may be substituted by halogen or C1-C4 alkyl, or C3-C6 cycloalkyl which may be substituted by C1-C4 alkyl or cyclohexyl; and Alk<1> and Alk<2> each independently represents C2-C4 alkylene; or a non- toxic pharmacologically acceptable acid addition salt thereof. Such compounds may be prepared by reacting an appropriate disubstituted acetonitrile with an appropriate haloalkylamine and subsequently hydrolyzing the resulting nitrile using concentrated sulphuric acid ...

PREPARATION OF AN ASPARAGINE OR A GLUTAMINE

... 1467587 Asparagines and glutamines NESTLE SA 18 June 1975 [11 July 1974 18 Sept 1974] 25923/75 Heading C2C Compounds of formula (where n is 1 or 2, and X and Y are hydrogen atoms or C 1-6 alkyl or acyl groups, except that when n = 2 not more than one of X and Y are hydrogen atoms) are made by reacting a compound of formula (where M(+) is a cation and R is an aliphatic group containing 1-3 carbon atoms) with ammonia in an aqueous medium and thereafter acidifying the reaction medium. Examples describe the production of (1) and (2) L-asparagine; (3) -(N-acetyl)-L-asparagine; (4) and (5) -(N-acetyl)-L-glutamine.

Substituted anilides

The invention comprises compounds of the formula : <FORM:0856385/IV(b)/1> (wherein R, R1 and R2 are alkyl groups, or-NR1R2 is a saturated heterocyclic residue) and salts thereof, and their preparation by reacting an amine NHR1 R2 with the appropriate crotonanilide. An excess of the secondary amine is preferably used and the reaction is advantageously performed at the boiling point of this amine under pressure. Examples describe the preparation of N-(b -pyrrolidino)-butyryl-p-amino-benzoic acid n-butyl ester, the corresponding piperidino compound, the corresponding iso-propyl esters and N-(b -diethylamino)-butyryl-p-amino-benzoic acid n-propyl ester. Crotonic acid anilides of the formula : <FORM:0856385/IV(b)/2> are prepared by reacting crotonyl chloride with the appropriate p-amino-benzoic acid ester. The preparation of the n-butyl and iso-propyl esters is described. In the Provisional Specification it is stated that the phenyl group in compounds of the above formulae may be further substituted, for example by free or esterified carboxyl groups or alkyl, alkoxy or aryl groups.ALSO:Therapeutic compositions comprise one or more compounds of the formula: <FORM:0856385/VI/1> (wherein R, R1 and R2 are alkyl groups or -NR1R2 is a saturated heterocyclic residue) or non-toxic salts thereof e.g. hydrochloride, sulphate, phosphate, tartrate and citrate together with a non-toxic pharmaceutical carrier.

Improvement in the preparation of aminoacyl anilides and related compounds

A process for the preparation of a chemical compound of the general formula in which R1 and R2 each represents a lower alkyl group or a halogen atom, R3 represents hydrogen, a lower alkyl group (i.e. an alkyl group containing not more than 5 carbon atoms) or a halogen atom, R3 represents hydrogen, a lower alkyl group or a halogen atom, R4 and R5 each represents a lower alkyl group and n is 1 or 2 comprising heating a phenyl isocyanate of the general formula with a carboxylic acid of the general formula HOOC.CnH2n.Y in which Y represents a halogen atom or the amino group so as to split off CO2 and form a compound of the general formula which, when Y is a halogen atom, is heated with an amine of the formula HNR4R5 to form said chemical compound. In a modification of the process for the preparation of a halide salt of the corresponding betaine anilide, Y is a halogen atom and the halogeno-acyl halide ...

Basically substituted butyric acid amides and a process for their manufacture

The invention comprises amides of the general formula in which R1 represents hydrogen or an alkyl radical containing at most 4 carbon atoms and R2 stands for a phenyl radical which may be substituted by alkyl or alkoxy groups containing up to 2 carbon atoms, or halogen, e.g. chlorine, atoms, or R1 and R2 together with the nitrogen atom may form a heterocyclic ring system. The amides are made by reacting a compound of the general formula with formaldehyde in the presence of formic acid or by catalytic hydrogenation in the presence of formaldehyde. Suitable starting materials include the phenetidide, anilide, p-anisidide, N - methyl - p - phenetidide, N-ethylp-phenetidide, m-anisidide, N-isopropylanilide, N - n - butyl - p - anisidide, N - isobutyl - anilide, o-anisidide, p-toluidide, xylidide, N-propyl-p-phenetidide, 1:2:3:4 - tetrahydroquinolide and 1:2:3:4 - tetrahydro - 6 - methoxy - quinolide of a -amino-b -hydroxy-butyric acid. The compounds ...

Arylating agents

Method of preparation of derived from benzamide.

New anilide with basic substituent and its preparation.

Anti viral and anti cancer agents

Anti viral and anti cancer agents.

... 2-chloro-5-nitrobenzoic acid and various other chloro ...

Amino acid derivatives with multi-drug resistance activity, compositions and uses thereof and processes for preparing said derivatives.

The present invention relates to compounds of formula Compounds of formula (I) are useful in maintaining, increasing or restoring drug-sensitivity of mult-drug resistant cells.This invention also relates to pharmaceutical compositions comprising compounds of formula (I) and the use of these compounds for treating and preventing multi-drug resistant cells, particularly in multi-drug resistant cancer therapy. This invention also relates to processes for preparing compounds of formula (I).

4-Acylaminobenzamides and their use as fungicides.

A fungicidal compound having the formula wherein either a and b are both fluoro; w is oxygen; z is nr'r ...

Novel amino acid derivatives with improved multi-drug resistance activity

New compounds benzodiazepines.

Process for the preparation of derived from 1,4-benzodiapine.

Process for the preparation of derived from 1,4-benzodiazepine.

Process for the preparation of derived from 1,4-benzodiazepine.

Arylating medicaments

Process for the preparation of derived from 1,4-benzodiazepine.

New weedkillers, their preparation and use.

Process for the preparation of derived from benzodiazepine.

Process for the preparation of derived from 1,4-benzodiazepine.

Derived from acid-animated, their preparation and use as well as the compositions containing these derivatives.

New useful derivatives of aniline like agents microbicides and their method of preparation.

Anti-viral and anti-cancer agents

New growth regulators of the plants containing anilides of acids quaternary-alcanoïques ammonium.

Process for the preparation of derived from 1,4-benzodiazepine.

New derivatives of aniline, their process of preparation and their application like agents microbicides and of regulation of the growth.

Process for the preparation of derived from 1,4-benzodiazepine.

(2-hydroxy-2-(4-hydroxy-3-hydroxymethylphenyl)-ethylamino)-propyl-phenyl derivatives as beta2 agonists.

Novel amino acid derivatives with improved multi-drug resistance activity

FUNGICIDES

Compounds useful for the treatment of diseases

Entry inhibitors of the HIV virus.

ABIOTI HEPARINANTAGONISTEN

PROCEDURE FOR THE PRODUCTION OF NEW SYMMETRICAL ALPHA ARYL ALPHA, ALPHA DI (OMEGA (DIISOPROPYLAMINO) ALKYL) ACETAMIDE

PROCEDURE FOR THE PRODUCTION OF NEW GLYCINE AMIDE DERIVATIVES

Procedure for the production of new n (1-Aryloxy-2-hydroxypropyl) - amino acids and their derivatives

PROCEDURE FOR the PRODUCTION OF NEW RACEMI OR OPTICAL ACTIVE N, N' TO - (3-SUBST. PHENOXY-2-HYDROXY - 1 - PROPYL) - ALFA, OMEGA - DIAMINOALKANEN AS WELL AS THEIR ACID ADDITION SALTS

PROCEDURE FOR the PRODUCTION OF NEW ONE 2-AMINO-3 - BENZOYL PHENYLACETAMID DERIVATIVES

MITTEL ZUR BEEINFLUSSUNG DES PFLANZENWACHSTUMS

VERFAHREN ZUR HERSTELLUNG VON 1-PHENYL-2-GLYCINAMIDOATHANOLEN-(1) UND VON DEREN SALZEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN BENZOPHENON-DERIVATEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN 2-AMINOALKANOYLAMIDOBENZOPHENONEN

FLUOROBENZAMIDE FOR THE TREATMENT OF ALZHEIMER'S OR SENILE DEMENTIA

PRODUCTION OF POLYMERS

ATOMIC POSITION LAYER (ALD) BY METALLAMIDINATEN

MODULAR STAND FOR THE ORGANIZATION FROM SPECIFIC MOLECULES TO THE USE AS PEPITMIMETIKA AND HEMMER FOR THE PROTEIN INTERACTION

VERFAHREN ZUR HERSTELLUNG VON NEUEN N,N-DIALKYLAMINOESSIGSAURE-2,6-XYLIDIDEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN ALPHA-ARYL-ALPHA,ALPHA-BIS-(OMEGA(DISUBSTITUIER - AMINO)-ALKYL)ACETAMIDEN

9-SUBSTITUIERTE MINOCYCLINVERBINDUNGEN

PROCEDURE FOR THE PRODUCTION OF NEW AMINO ACID, AMIDES, YOUR SALTS AND OPTICAL ACTIVE ANTIPODES

PROCEDURE FOR THE REGULATION OF DELTA GLUTAMYLTRANSPEPTIDASE ONES

PROCEDURE FOR the PRODUCTION OF NEW RACEMI OR OPTICAL ACTIVE N, N' UNTIL (3-SUBST. PHENOXY-2-HYDROXY-1-PROPYL) - ALPHA, W-DIAMINOALKANEN AS WELL AS THEIR SAEUREADDITIONSSALZEN

PROCEDURE FOR THE PRODUCTION OF NEW SALTS AND COMPLEXES ADDITION DERIVATIVES OF TETRACYCLINEN

FUNGICIDES MEANS

PROCEDURE FOR THE PRODUCTION OF THE D-CAMPHORATS OF L-CARNITINAMID

PROCEDURE FOR THE PRODUCTION OF NEW ACYLAMINOSAUREAMIDEN

PROCEDURE FOR THE PRODUCTION OF NEW AMINOALKANSAUREANILIDEN AND THEIR SALTS

PROCEDURE FOR THE PRODUCTION OF NEW PHENYLOETHANOLAMINEN AND OF SALTS OF IT

ANTIMICROBIAL AND/OR ALGIZIDE MEANS

PROCEDURE FOR THE PRODUCTION OF NEW RACEMI OR OPTICAL ACTIVE ONE PHENYLESSIGSAEUREAMIDEN

PROCEDURE FOR THE PRODUCTION OF NEW NITRILOTRIESSIGSAEUREAMIDEN

PROCEDURE FOR THE PRODUCTION OF NEW ALPHA ARYL ALPHA, ALPHA-BIS (OMEGA (OF DISUBSTITUIERTES AMINO) ALKYL) ACETAMIDEN

PROCEDURE FOR THE PRODUCTION OF THE NEW ONE N-METHIONINOMETHYLDERIVATS OF ALFA-6-DEOXY-5-OXYTETRACYCLIN AND ITS SALTS

DIAGNOSTIC MEANS

PROCEDURE FOR THE PRODUCTION OF NEW AMINO ACID OF DERIVATIVES

PROCEDURE FOR THE PRODUCTION OF Z-L-ASPARAGINSÄURE-DINATRIUMSALZ FROM FUMARIC ACID

PROCEDURE FOR the PRODUCTION OF NEW ONE 2-AMINOALKANOYLAMIDOBENZOPHENONEN

PROCEDURE FOR the PRODUCTION OF 1-PHENYL-2-GLYCINAMIDOATHANOLEN (1) AND OF THEIR SALTS

PROCEDURE FOR the PRODUCTION OF n (DIATHYLAMINOATHYL) - 2-METHOXY-4-AMINO-5-CHLORBENZAMID

USE OF SUBSTITUTED GLYCINE AMIDES AS ANTIDOTA IN HERBICIDES MEANS AND HERBICIDES MEANS

Atomic layer deposition using metal amidinates

金属薄膜在均匀厚度和优良阶梯覆盖下沉积。铜金属薄膜通过交替量的N，N′-二异丙基乙脒铜(I)和氢气的反应沉积在加热的底材上。钴金属薄膜通过交替量的N，N′-二异丙基乙脒钴(II)和氢气的反应沉积在加热的底材上。这种金属的氮化物和氧化物可分别用氨或水蒸气代替氢气形成。细孔中的薄膜具有非常均匀的厚度和良好的阶梯覆盖。合适的应用包括微电子器件中和磁信息存储器件中磁致电阻的电连接。

Atomic Layer Deposition Using Metal Amidinates

금속 필름이 균일한 두께 및 우수한 스텝 커버리지로 증착된다. 구리 금속 필름을 가열된 기판에 구리(I) N, N'-디이소프로필아세트아미디네이트 증기와 수소 가스를 교대로 반응시켜서 증착시킨다. 코발트 금속 필름을 가열된 기판에 코발트(II) 비스(N, N'-디이소프로필아세트아미디네이트) 증기와 수소 가스를 교대로 반응시켜서 증착시킨다. 이들 금속의 질화물 및 산화물을 수소를 암모니아 또는 수증기로 각각 교체함으로써 형성할 수가 있다. 필름은 좁은 홀에도 매우 균일한 두께 및 우수한 스텝 커버리지를 갖는다. 적당한 응용분야로는 자기정보 저장장치에서의 마이크로전자 및 자기저항 층의 전기적 상호연결에 사용된다.

Method of obtaining carnitineamidchloride

Patent DE3347867C2

Atomic layer deposition using metal amidinates

Metal films are deposited with uniform thickness and excellent step coverage. Copper metal films were deposited on heated substrates by the reaction of alternating doses of copper(I) NN'-diisopropylacetamidinate vapor and hydrogen gas. Cobalt metal films were deposited on heated substrates by the reaction of alternating doses of cobalt(II) bis(N,N'-diisopropylacetamidinate) vapor and hydrogen gas. Nitrides and oxides of these metals can be formed by replacing the hydrogen with ammonia or water vapor, respectively. The films have very uniform thickness and excellent step coverage in narrow holes. Suitable applications include electrical interconnects in microelectronics and magnetoresistant layers in magnetic information storage devices.

Patent FR4734M

O-AMINO ACID AMIDE DERIVATIVES, THEIR PREPARATION, THEIR USE IN THE TREATMENT OF CONDITIONS OF THE CENTRAL NERVOUS SYSTEM AND CARDIOVASCULAR DISORDERS, AND COMPOSITIONS CONTAINING THEM

Process for obtaining combinations of monoquaternary ammonium, derived from amino- (dialoylamino-acet) anilides

Patent FR2062873B1

Process for preparing anilides

Process for the preparation of omega-alkylamino-acetylamino-benzenes

Process for the production of basic substituted amides of alpha-acylamino-acrylic acids

N- (beta-cyclohexylamino-butyric) 2-trifluoromethyl-4-chloranilide.

New alpha-amino-beta-hydroxy-carboxylic acid amides and their preparation

New alpha-amino-beta-hydroxy-carboxylic acid amides and their preparation

Process for the preparation of benzophenone derivatives

Butyric acid amides and their preparation

Amides of amino-propionic acid, usable in particular for the treatment of textile fibers

Process for preparing alpha-n-propylamino-2-methyl propionanilide

Production of beta-alaninamide sulfate and free beta-alaninamide

Patent FR2055700A5

2-phenylisopropylaminoacet-2, 6-xylidide - with antiarrhythmic anorectic, antiinflammatory, analgesic and local anaesthetic act

2-Phenylisopropylaminoacet-2,6-xylidide and its salts with anti-arrhythmic, local, anaesthetic, anorectic, analgesic and antiinflammatory activity. Prepd. by treating 2,6-xylidine with chloroacetyl chloride to give an intermediate chloracet-2,6-xylidide which is condensed iwth 2-phenylisopropylamine to give the required product.

Basically substituted acid amides and process for their manufacture

The invention comprises compounds of the general formula <FORM:0788936/IV (b)/1> in which R1 is an alkylene group of 1-4 carbon atoms, and R2 and R3 are each hydrogen atoms or alkyl radicals of 1-4 carbon atoms or together with the nitrogen atom form a saturated heterocyclic ring, and their acid addition salts. The compounds are made by acylating a 2-nitro-6-chloro-aniline with an amino-alkyl carboxylic acid and reducing the product, if necessary after alkylation at the amino group of the amino-acid residue. They are also prepared by acylating the 2-nitro-6-chloro-aniline with a halogeno-alkyl carboxylic acid, condensing the resulting halogeno-acylamide with ammonia or a primary or secondary amine and reducing the amino-acylamide obtained. The acylation reactions are suitably carried out using the acid chlorides of the amino- or halogeno-alkyl carboxylic acids, in the presence of a solvent and in the presence of an acid binding agent which may be sodium hydroxide or sodium acetate or may be an excess of the 2-nitro-6-chloroaniline itself. In the absence of an acid binding agent hydrogen halide liberated during the acylation is removed by heating. Specified amino-alkyl carboxylic acids include amino, monoalkylamino and dialkylamino acetic, propionic and butyric acids, a -piperidinoacetic acid, b -piperidinopropionic acid and a -pyrrolidinoacetic acid. The reduction of the nitro group to the amino group may be effected by means of tin and hydrochloric acid, sodium dithionite or by catalytic reduction using Raney nickel as a catalyst. Where it is necessary to alkylate a primary or secondary amine prior to reduction, this may be effected for example by means of alkyl halides. The free bases may be converted into their salts with hydrohalic, sulphuric, phosphoric, acetic, lactic, maleic, malic, amidosulphonic, phenol-sulphonic, oxalic, succinic, hydroxyethane sulphonic or aceturic acid. In examples: (1) 2-nitro-6-chloroaniline is acetylated with chloracetyl ...

Process for the preparation of pharmacologically active 2-amino-N- (1,2-diphenylethyl) acetamide derivatives

PROCESS FOR PREPARING AN ASPARAGINE OR A GLUTAMINE

Atomic layer deposition using metal amidinates

Metal films are deposited with uniform thickness and excellent step coverage. Copper metal films were deposited on heated substrates by the reaction of alternating doses of copper(I) NN′-diisopropylacetamidinate vapor and hydrogen gas. Cobalt metal films were deposited on heated substrates by the reaction of alternating doses of cobalt(II) bis(N,N′-diisopropylacetamidinate) vapor and hydrogen gas. Nitrides and oxides of these metals can be formed by replacing the hydrogen with ammonia or water vapor, respectively. The films have very uniform thickness and excellent step coverage in narrow holes. Suitable applications include electrical interconnects in microelectronics and magnetoresistant layers in magnetic information storage devices.

Process for the preparation of substituted beta-alkyl and beta-cycloalkyl-amino-propionamides

Process for the production of a new basic substituted fatty acid amide.

Method for preparing N-benzyloxycarbonyl amino acids containing additional functionality

Crown ethers and silacrown ethers are employed as phase-transfer reagents in blocking primary amino functionality of alkali metal salts of amino acids with a benzyloxycarbonyl group.

N-camphoryl-amino acetamides

Acylxylidide local anaesthetics

A procedure for preparing acyl-xylidide compounds of the structural formula ** (See formula) ** in optically active or racemic form, in which formula R1 is ethyl, propyl or butyl; R2 and R3 are each selected from the group consisting of methyl, ethyl, propyl, and butyl; R2 together with R3 is tetramethylene; the total sum of carbon atoms in R1, R2 and R3 is at least six; and its pharmaceutically acceptable salts; characterized in that a compound of the formula is reacted ** (See formula) ** wherein R1 and Y have the meaning set forth above, with a compound of the formula H2 - N - R2 wherein R2 has the meaning set forth above, for the formation of a compound of formula ** (See formula) ** after which this compound is reacted with an alcoholizing agent to form a compound of formula I, and the compound of formula I thus formed is reacted, if desired, with a pharmaceutically acceptable acid. (Machine-translation by Google Translate, not legally binding)

Method of producing diamine derivatives

A compound of the following general formula or a salt thereof (where R, and R 2 which may be the same or different are each an alkyl group having 1 to 3 carbon atoms; R3 is a hydrogen atom or an alkyl group having 1 to 3 carbon atoms; R 4 and R 5 which may be the same or different are each a hydrogen atom or an alkyl group having 1 to 8 carbon atoms or a cycloalkyl group having 3 to 8 carbon atoms; m and n which may be the same or different are each an integer of 1 to 7; provided that R4 and R 5 are not a hydrogen atom at the same time), and a process of preparing the same are disclosed. The compound is useful in the treatment of arrythmias because it exhibits desirably strong effects for treating arrythmias and minimum undesirable side effects.

Process for preparing compounds of the aminoacylaniline type

Process for preparing 4-amino-butyric acid amide hydrochloride.

4-aminobutyramide hydrochloride is produced by hydrogenation of 3-cyanopropionamide in the presence of a solvent inert under the reaction conditions, a noble metal catalyst and hydrogen chloride at a temperature between 5 DEG and 80 DEG C. The hydrochloride can be easily converted into 4-aminobutyramide which as such or in the form of derivatives has significance as a neurotransmitter.

Process for manufacturing N-acyl derivatives of hydroxy-arylglycines

Condensation of the addition product of glyoxylic acid and amides with hydroxyaryl compounds is effected by a first step, wherein the reaction is carried out hot, at a temperature below 60° C, of an aliphatic amide having at the most 4 carbon atoms selected from the group of acetamide, chloracetamide, propionamide, acrylamide and butyramide, on an aqueous solution of glyoxylic acid. Then in a second step, after the addition of acetic acid and gaseous hydrochloric acid, condensation is effected at a temperature below 35° C of the carboxamidoglycolic acid with an excess reaching 500% of hydroxyaryl compound selected from the group comprising phenol and its alkyl derivatives, their halogen derivatives, polyphenols and their ethers and betanaphthol. After the condensation of said second step, the volatile products are removed by vacuum distillation. When the hydroxyaryl compound is phenol, the crude product resulting from this distillation is taken up in nitromethane or water, which are a non-solvent of the N-acyl derivative of parahydroxyphenylglycine but a solvent of the corresponding ortho derivative; the proportion of the para derivative in the resulting compound is then of the order of 100%.

Acylxylidide local anaesthetics

THE 2-ALKYL-2-ALKYLAMINO - 2'',6'' - ACETOXYLIDIDE COMPOUNDS ARE USEFUL AS LONG LASTING LOCAL ANAESTHETICS.

1,6-Hexanediamides from 3-pentenamides

A process for making a diamide of the formula by reacting a monoamide compound of the formula with CO and an amine or ammonia of the formula R 7 R 8 NH in the liquid phase under essentially anhydrous conditions at a temperature in the range from 120 to 210° C, where each of R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 is selected independently from H and a C, to C 12 hydrocarbyl containing no ethylenic or acetylenic unsaturation.

Patent FR2323680B1

Patent GR77444B

Process for the preparation of a pharmacologically active product based on chloral hydrate

Hair care products

Improvements in or relating to pharmaceutically active anilide

The invention comprises b -diethylaminobutyric acid N-methylanilide, acid addition salts thereof, and their preparation by reacting crotonic acid N-methylanilide with diethylamine, preferably at elevated temperature and pressure, and, if desired, salifying. The compounds of the invention may be employed as stimulants for the central nervous system or as psychoanaleptics, and may be used in combination with a pharmaceutically inert carrier in forms suitable for oral or parenteral administration, e.g. as tablets, drag<\>aees or injectable solutions.

Preparation of an asparagine or a glutamine

A B S T R A C T A process for the preparation of compounds of the general formula (I) (in which n is an integer equal to 1 or 2 and X and Y which may be the same or different are hydrogen atoms or organic groups, except that when n=2 not more than one of X and Y may re-present a hydrogen atom) in which a compound of the general formula

Electric time switches for washing machines

826,140. Timing switches. HOLZER, W. Feb. 20, 1956 [Feb. 18, 1955; March 31, 1955], No. 5166/56. Class 38 (5). [Also in Group XXXV] A timing switch for washing-machines comprises disc cams 4, 5, 6a, 6b on a rotatable shaft 12 which actuates contacts 7, 8, 9, 10, the speed of the shaft being controlled by an eddy current brake 16. As shown in Fig. 1 the shaft is driven by a spring which is wound by a handle 14. The brake magnet may be an electromagnet as shown or a pivotable permanent magnet. Different resistances may be introduced in series with the electromagnet windings 17, 18 to vary the speed of the shaft. In Fig. 4 a motor-driven shaft carries discs operating contacts 53-56 for controlling the motor, heater and valves, and contacts 49-52 which complete circuits for including resistances 44-47 in series with the windings of the electromagnet to control the speed of the shaft. The resistors 44-47 may be replaced by other resistors when different materials are washed.

Process for the manufacture of sodium pantothenate

PROCEDURE FOR THE SYNTHESIS OF OMEGAAMINATED ACID DERIVATIVES (Machine-translation by Google Translate, not legally binding)

Compounds of the formula I < IMAGE > for use in treating epilepsy, depression, dyskinesias such as Parkinson's disease, muscular spasms of nervous origin, hypertension, hypotension, sleeping troubles, memory defects, and as anthelminthic and analgesic agents wherein R represents:- a linear or branched C2 to C12 alkyl radical a linear or branched C2 to C4 alkyl radical substituted by a phenyl or phenoxy nucleus which may be substituted by one or two linear or branched C1 to C4 alkyl radicals by one or two linear or branched C1 to C4 alkoxy radicals or by one or two halogen atoms a linear or branched C2 to C6 acyl radical substituted by a phenyl nucleus which may be substituted by one or two linear or branched C1 to C4 alkyl radicals by one or two linear or branched C1 to C4 alkoxy radicals or by one or two halogen atoms. R1 represents hydrogen, a linear or branched C2 to C11 acyl radical a linear or branched C2 to C6 acyl radical substituted by a phenyl nucleus which may be substituted by one or two linear or branched C1 to C4 alkyl radicals by one or two linear or branched C1 to C4 alkoxy radicals or by one or two atoms of halogen, such as fluorine, chlorine or bromine, R2 represents:- a hydroxyl group an alkoxy group R3O- in which R3 is a linear or branched C1 to C3 alkyl radical an amino group and n is 3, 4 or 5 or a pharmaceutically or veterinarily acceptable salt thereof.

Process for the prduction of 4-(trialkylammonium)- acetoacetarylides

Abstract of the Disclosure A process is disclosed for the production of 4-(trialkylammonium)-acetoacetarylides having the formula:

PROCESS FOR THE PREPARATION OF N-ACYLHYDROXYARYL GLYCINS.

New amino derivative and its preparation process

METHOD FOR OBTAINING ACYLIC XYLIDIDES

Quaternary ammonium compounds

N-acyl phenylalanine amides

THE ABOVE-CAPTIONED COMPOUNDS ARE USEFUL AS PHARMACOLOGICAL, E.G., ANTI-INFLAMMATORY, AGENTS. THEY ARE MANUFACTURED BY ACYLATING PHENYLALANINE TO PRODUCE THE NACYL DERIVATIVES, THEN REACTING THE LATTER INTERMEDIATES SUCCESSIVELY WIH AN ALKYL CHLOROFORMATE AND A PRIMARY AMINE TO YIELD THE DESIRED N-ACYL PHENYLALNINE AMIDES.

Process for the preparation of anesthetically active, basic substituted carboxamides

Patent FR2118985A1

Process for the preparation of carnitinamide

Process for the production of carnitine amide in the form of a chloride. The carnitine ethyl ester is obtained by reaction of 4-chloroacetoacetic acid ethyl ester with trimethyl amine and the subsequent hydrogenation is carried out with the help of a Pt/C catalyst. Such carnitine ethyl ester, without isolating it, is reacted with ammonia in an autoclave at -30 DEG to +10 DEG C. Everything is heated to 40 DEG to 80 DEG C. The mixture is stirred at such temperature at an ammoniac pressure of 8 to 24 atu. The product is filtered after cooling it to ambient temperature and counterbalancing the excess pressure. The product is then washed with alcohol and subsequently dried at 30 DEG to 50 DEG C. and at a pressure of 15 to 25 torr.

Amines

The invention comprises esters of the general formula <FORM:0768770/IV(b)/1> wherein n is an integer from 1 to 6 inclusive and R is a tertiary amino radical, and acid addition and quaternary ammonium salts thereof; and their preparation by esterifying a 2,6 - dimethyl - 4 - carbomethoxybenzoyl halide with a tertiary alkanolamine, ammonolysing the so-formed tertiary aminoalkyl ester of 2,6-dimethyl-4-carbomethoxy-benzoic acid to give a tertiary aminoalkyl 2,6-dimethyl-4-carbamoylbenzoat and subjecting this to a Hofmann degredation to the corresponding amine. Tertiary alkanolamines which may be used include dialkylamino-, dicycloalkylamino-, alkylaralkylamino- and diaralkylamino-alkanols and heterocyclicamino-alkanols such as 1-pyrolidyl-, piperidino- and morpholino-alkanols and alkyl-substituted homologues thereof. The Hofmann degradation, which is generally effected by dissolving the amide in a very slight excess of cold aqueous alkali-metal hypohalite solution followed by rapid warming, is advantageously modified by carrying out the reaction in an alcoholic solution with subsequent hydrolysis of the intermediate so obtained. Salt forming acids referred to are hydrochloric, hydrobromic, sulphuric, acetic, lactic, tartaric, succinic, benzoic, salicylic and picric acids. Quaternary ammonium salt-forming compounds referred to include alkyl halides, aralkyl halides and alkyl esters of aryl sulphonic acids. Examples describe the preparation of (1) b -diethyl aminoethyl-2,6-dimethyl-4-aminobenzoate via the intermediates diethylaminoethyl 2,6 - dimethyl - 4 - carbomethoxybenzoate, b - diethylaminoethyl 2,6 - dimethyl-4 - carbamoyl benzoate and b - diethylaminoethyl 2,6 - dimethyl - 4 - carbomethoxyaminobenzoate, the latter being hydrolysed with aqueous sodium hydroxide to the required product, which is converted to its methochloride, ethochloride, benzyl chloride, monohydrochloride, dihydrochloride, monoacetate, benzoate, citrate and sulphate; (2) b - ...

Derivatives of omega-amino acids,the preparation and utilisation thereof,and the compositions containing these derivatives

Compounds of the formula I for use in treating epilepsy, depression, dyskinesias such as Parkinson's disease, muscular spasms of nervous origin, hypertension, hypotension, sleeping troubles, memory defects, and as anthelminthic and analgesic agents wherein R represents:- a linear or branched C2 to C12 alkyl radical a linear or branched C2 to C4 alkyl radical substituted by a phenyl or phenoxy nucleus which may be substituted by one or two linear or branched C1 to C4 alkyl radicals by one or two linear or branched C1 to C4 alkoxy radicals or by one or two halogen atoms a linear or branched C2 to C6 acyl radical substituted by a phenyl nucleus which may be substituted by one or two linear or branched C1 to C4 alkyl radicals by one or two linear or branched C1 to C4 alkoxy radicals or by one or two halogen atoms. R1 represents hydrogen, a linear or branched C2 to C11 acyl radical a linear or branched C2 to C6 acyl radical substituted by a phenyl nucleus which may be substituted by one or two linear or branched C1 to C4 alkyl radicals by one or two linear or branched C1 to C4 alkoxy radicals or by one or two atoms of halogen, such as fluorine, chlorine or bromine, R2 represents:- a hydroxyl group an alkoxy group R3O- in which R3 is a linear or branched C1 to C3 alkyl radical; an amino group; and n is 3, 4 or 5; or a pharmaceutically or veterinarily acceptable salt thereof.

PROCESS FOR THE PREPARATION OF AMINO-4 BUTYRAMIDE

1. A process for the preparation of 4-aminobutyramide characterized in that 4-nitrobutyramide is reduced by hydrogenation in the presence of a catalyst.

Process for the preparation of 4-aminobutyric acid amide hydrochloride

Process for the preparation of anesthetically active N-alkylaminocarboxylic acid anilides

PROCESS FOR THE ELABORATION OF 4-AMINOBUTIRICA AMIDE CHLORHYDRATE

N-(3, 4-dihydroxy-beta-phenethyl) amides of amino-acids - - which are renal vasodilators and hypertensives

Title amides of formula (I): (where R is H, lower alkyl, hydroxymethyl, hydroxybenzyl, 2-hydroxyethyl, mercaptomethyl, methylmercaptoethyl, 3-indolylmethyl, 2-carboxyethyl, 3-guanidinopropyl, 4-aminobutyl or 5-imidazolylmentyl) and their acceptable acid addition salts, which can be used for treating renal hypertension and shock, may be prepd. by reacting 3,4-dibenzyloxy-beta-phenethylamine with HOOC-CHR-NH-COOCH2C6H5 and hydrogenating the resulting N-carbobenzoxy cpd. in the presence of methanol and acid.

Process for the preparation of N-benzoyl-L- (D- or DL) -glutamic acid-l-amides

A process for the manufacture of carboxylic acid amides of quaternary ammonium compounds

547,057. Amides of crotonic acid betaine compounds. ROCHE PRODUCTS, Ltd., BERGEL, F., COHEN, A., and HINDLEY, N. C. Dec. 10, 1940, No. 6578/42. Divided out of 546,596. [Class 2 (iii)] Amides of crotonic acid betaine compounds and quarternary ammonium compounds of similar constitution are prepared by reacting an acid chloride of the general formulawith ammonia, an amine, or an α - amino acid alkyl ester. In the formula R, R<SP>1</SP> and R<SP>11</SP> are identical or different alkyl, aryl, or arakyl groups, X is halogen and n is 1 or.2. In place of the above acid chloride there may be used as starting material a corresponding simple ester. In examples (1) crotonic acid betaine chloride is treated with methyl alcohol in the presence of dry hydrogen chloride and the ester so produced treated with concentrated liquid ammonia to give the quarternary chloride of crotonic acid betaine amide. (2) crotonic acid betaine chloride is converted into the acid chloride and treated with concentrated aqueous ammonia to give the corresponding amide which is purified by its reineckate. (3) The acid chloride of crotonic acid betaine chloride is mixed with dry powdered silica to form a granular solid which is gradually added to an ether solution of the ethyl ester of glycine to give a betaine-peptide of the formula- Specifications 546,596 and 546,613 are referred to.

DERIVATIVES OF OMEGA-AMINO ACIDS, THE PREPARATION AND USE THEREOF AND PREPARATIONS CONTAINING THESE DERIVATIVES.

Process for the production of therapeutically active amides of N benzoylglutamic acid

Process for preparing 4-amino-butyric acid amide hydrochloride

PROCEDURE FOR THE PREPARATION OF DL-FENIL-GLYCINAMIDE

PROCEDURE FOR PREPARING SUBSTITUTED DERIVATIVES OF 2-AMINO ACETAMIDE.

Compounds are provided of the following general structure: <CHEM> wherein B is hydrogen, lower alkyl (C1-C4) or methoxycarbonyl; R1 is hydrogen or methyl and where W and Q are independently selected from phenyl or 4-fluorophenyl. They are useful for providing sedative and antiepileptic activity.

PROCESS FOR THE PRODUCTION OF SODIUM PANTOTHENATE.

Procedure for the preparation of substitute hydrazine compounds (Machine-translation by Google Translate, not legally binding)

Process for the preparation of substituted hydrazine compounds, of the general formula ** (See formula) ** wherein R1 represents hydrogen or aminosubstituted acyl, and n is an integer value of 2 to 3, and its salts, characterized in that it comprises the reaction of a hydrazine of the general formula ** (See formula) ** wherein R1 has the same meaning as before and the hydrogen atoms of the hydrazinic portion can be replaced by protecting groups, or a salt thereof, with a carbonyl compound of the formula ** (See formula) ** wherein R2 represents hydroxy or hydroxy etherified with an alkyl portion dissociable by hydrogenolysis and n has the same meaning as before, followed by the hydrogenation of the hydrazone thus formed, after which, if necessary, the protective groups are dissociated from the hydrazinic compound thus formed, and finally, if desired, acylation and/or conversion into a salt. (Machine-translation by Google Translate, not legally binding)

Process for the preparation of 2-methyl-6-carbalkoxy-n-alkylamino-acylanilides

Improvements in or relating to diquaternary compounds

The invention comprises compounds of the general formula (C6H5)2CH-(CH2)m-X-(CH2)n\t -+N1-(CH2)2-+N22A-in which X represents the grouping-NHCO-or -CONHCH2-; m is either zero or an integer from one to three and n is an integer from one to five, providing that the sum (m + n) does not exceed six; +N1 is a quaternary nitrogen atom carrying two alkyl groups which are methyl or ethyl groups; +N2 is a quaternary nitrogen atom carrying at least one methyl or ethyl group and either carrying two further alkyl groups which are methyl or ethyl groups or forming part of a pyrrolidino, piperidino or morpholino ring; and A- is an anion of an inorganic or organic acid which may be for example, halide or alkyl sulphate. The compounds may be prepared by treating a diamine (C6H5)2CH-(CH2)m-X-(CH2) n-N3-(CH2)2-N4 wherein N3 is a secondary or tertiary nitrogen atom, and N4 is a primary, secondary tertiary or quaternary nitrogen atom, with a quaternising agent such as an alkyl halide or a dialkyl sulphate, the substituents provided by the said agent, together with any substituents or N3 and N4, being such as will give the desired substitution in the compound of the invention. The diamines used as starting materials are prepared by (a) (wherein X is -NHCO-) reacting a primary amine (C6H5)2CH-(CH2)m -NH2 with a diamino-ester, ROOC-(CH2)n-N3-(CH2)2-N4 where R is a lower alkyl group and (b) (wherein X is -CONHCH2-) reacting an ester (C6H5)2CH-(CH2)m-COOR with a triamine H2N-(CH2)n + 1-N3-(CH2)2 -N4. N-Methyl-N-2-piperidinoethylaminoacetate is prepared from ethyl bromoacetate and N-methyl-N-2-piperidinoethylamine. N1-(2-Diethylaminoethyl)-N1-methylethylene-diamine is prepared by reacting chloroacetonitrile with diethylaminoethylmethylamine to form N-(2-diethylamino-ethyl)-N-methylaminoacetonitrile which is hydrogenated. N1 - (2-Piperidoethyl)-N1-methyltrimethylenediamine is prepared by reacting acrylonitrile with N-methyl-N-(2-piperidinoethyl)amine to form b -(N-methyl-N-2- ...

METHOD FOR PREPARING DL-PHENYLGYLCINAMIDE

METHOD FOR PRODUCING CARNITINAMIDE.

Process for the production of carnitine amide in the form of a chloride. The carnitine ethyl ester is obtained by reaction of 4-chloroacetoacetic acid ethyl ester with trimethyl amine and the subsequent hydrogenation is carried out with the help of a Pt/C catalyst. Such carnitine ethyl ester, without isolating it, is reacted with ammonia in an autoclave at -30 DEG to +10 DEG C. Everything is heated to 40 DEG to 80 DEG C. The mixture is stirred at such temperature at an ammoniac pressure of 8 to 24 atu. The product is filtered after cooling it to ambient temperature and counterbalancing the excess pressure. The product is then washed with alcohol and subsequently dried at 30 DEG to 50 DEG C. and at a pressure of 15 to 25 torr.

2 - aminoacetamide derivatives

Compounds are provided of the following general structure: <CHEM> wherein B is hydrogen, lower alkyl (C1-C4) or methoxycarbonyl; R1 is hydrogen or methyl and where W and Q are independently selected from phenyl or 4-fluorophenyl. They are useful for providing sedative and antiepileptic activity.

Process for the preparation of aminoacetic anilides

2-AMINOACETAMIDE DERIVATIVES.

Compounds are provided of the following general structure: <CHEM> wherein B is hydrogen, lower alkyl (C1-C4) or methoxycarbonyl; R1 is hydrogen or methyl and where W and Q are independently selected from phenyl or 4-fluorophenyl. They are useful for providing sedative and antiepileptic activity.

Derivatives of w-amino acids, the preparation and utilisation thereof; and the compositions containing these derivatives

ABSTRACT Derivatives of .omega.-amino acids of general formula : I also racemic or non-racemic mixtures thereof, optically pure isomers thereof and salts of these compounds formed with pharmaceutically utilisable acids, bases and metals, wherein R represents a linear or branched alkyl radical C2-C12, a linear or branched alkyl radical C2-C4 substituted by a phenyl or phenoxy nucleus which may be itself substituted, a linear or branched acyl radical C2-C6 substituted by a phenyl nucleus which may be itself substituted; R1 represents hydrogen, a linear or branched acyl radical C2-C11, a linear or branched acyl radical C2-C6 substituted by a phenyl nucleus which may be itself substituted; R2 is an amino group, and n is equal to 3, 4 or 5. Such derivatives can be used in the treatment of neurological, psychic or cardiovascular problems, and as anthelminthic and analgesic agents.

Derivatives of omega-amino acids,the preparation and utilisation thereof,and the compositions containing these derivatives

PROCESS FOR PREPARING 4-AMINOBUTTERAUMEAMIDE HYDROCHLORIDE

Acyl xylidide local anaesthetics

The 2-alkyl-2-alkylamino-2'',6''-acetoxylidide compounds are useful as long lasting local anaesthetics.

Patent NO135934C

Acenaphthene derivatives

Manufacture of 44aminobutyric acid amide hydrochloride

Process for the preparation of dl carnitinamide chloride

1. Process for the preparation of D,L-carnitinamide chloride (I) see diagramm : EP0166901,P3,F1 characterized in that, in a first reaction stage, 2,3-epoxypropyltrimethylammonium chloride is reacted in aqueous solution with 0.8 to 2.0 equivalents of hydrocyanic acid at a pH above 7 and not above 11 and at a temperature between 20 and 100 degrees C, and the resulting nitrile is, without intermediate isolation and without addition of base, treated in the reaction solution with 1.5 to 5 equivalents of aqueous hydrogen peroxide at a temperature between 30 and 100 degrees C, and the reaction product is isolated in a manner known per se.

ª -amino-ª -hydroxy carboxylic acid amides and process for preparing them

The invention comprises alpha-amino-beta-hydroxy-butyric acid amides substituted on the amido nitrogen atom by an aliphatic hydrocarbon radical R which is attached to the nitrogen atom by a tertiary carbon atom, and acid-addition salts thereof; and the preparation thereof by treating a compound of the formula CH3COCH2CONHR (prepared from diketene and the amines NH2R) with nitrous acid or reacting it with an aryl diazonium salt, and reducing the product. The products of the reaction with nitrous acid are a -isonitroso derivatives of the keto-amides of the above formula, and they may be reduced in stages, first by reduction with for example, nascent-hydrogen to a compound of the formula CH3COCH(NH2)CONHR and then to the required product with, for example, sodium or aluminium amalgam and an alcohol and sodium borohydride or by catalytic hydrogenation or electrolytically. Before this final reduction, the intermediate amine is desirably acylated to give a compound of the formula CH3COCH(NHAc) CONHR (wherein Ac is an acylating group such as an acetyl, propionyl, benzoyl or phenylacetyl group) which on reduction gives a compound of the formula CH3CH(OH) CH(NHAc)CONHR from which the required final product is obtained by hydrolysis. The products of the reaction with an aryl diazonium salt are a -arylazo derivatives of the keto-amide starting materials, which may then be reduced in stages by the same methods as are employed for the isonitroso compounds. Alternatively the reduction process of the invention may be effected in one stage, by catalytic hydrogenation, or electrolytically, or with nascent hydrogen or sodium borohydride. Detailed examples are given, one product being isolated in two isomeric forms. The amides of the invention, which have analgesic properties, may be incorporated in pharmaceutical compositions with the aid of suitable carriers. Specifications 816,225 and 828,694 are referred to.

Basic substituted carboxylic acid amides and process for the preparation of these acid amides

Fatty acid amides and derivatives thereof

PROCEDURE FOR THE PREPARATION OF 4-AMINOBUTYRICAL AMIDA CHLORHYDRATE

Acyl xylidide local anaesthetics

Process for the preparation of diphenylamides

METHOD OF PREPARING 4-AMINOBUTYRAMIDE

Process for the preparation of new racemic or optically active 2-alkyl-2-dialkylaminoacet-2 ', 6'-xylidides and their salts

Improvements relating to the preparation of dialkyl aminoacetyl anilides

Aminoacetyl anilides of the general formula <FORM:0746552/IV(a)/1> in which R1 is hydrogen or a methyl group and R2 and R3 are alkyl groups of not more than 3 carbon atoms are made by the reaction of 2:6-dimethyl or 2:4:6-trimethyl aniline with an aminoacetic acid of the formula HO.CO.CH2.NR2R3 in the presence of a dehydrating agent such as phosphorus pentoxide, phosphorus oxychloride or phosphorus pentachloride. The products are used as an sthetics. In examples: (1) and (2) diethylaminoacetic acid hydrochloride is heated with 2:6-xylidine, phosphorus oxychloride is added and the mixture is kept at 100 DEG C. for 5 hours to give diethylaminoacetyl-2:6-xylidide and (3) diethylaminoacetic acid is reacted with 2:6-xylidine in the presence of phosphorus pentoxide to give the product of (1). Similar methods may be used to prepare the corresponding dimethyl-, methyl-propyl-, methyl - ethyl - and ethyl - propyl - aminoacetyl xylidides and the dimethyl- and diethylaminoacetyl mesidides.

NOVEL PROCESS FOR THE PRODUCTION OF 4-AMINOBUTYRAMIDE OR GABAMIDE HYDROCHLORIDE

L'INVENTION CONCERNE UN NOUVEAU PROCEDE DE FABRICATION DE CHLORHYDRATE DE 4-AMINOBUTYRAMIDE, A PARTIR DE CHLORHYDRATE DE 4-AMINOBUTYRONITRILE PAR HYDROLYSE DE CE DERNIER EN MILIEU AQUEUX CHLORHYDRIQUE; CE QUI PERMET D'ISOLER LE CHLORHYDRATE DE 4-AMINOBUTYRAMIDE, OU GABAMIDE DANS DE BONNES CONDITIONS DE PURETE ET DE RENDEMENT. CE PRODUIT PRESENTE UN INTERET EN TANT QUE TEL, PAR SES PROPRIETES PSYCHOTROPES, ET EN TANT QU'INTERMEDIAIRE DE SYNTHESE, DE NOUVELLES MOLECULES AYANT DES PROPRIETES GABAMIMETIQUES. THE INVENTION CONCERNS A NEW PROCESS FOR MANUFACTURING 4-AMINOBUTYRAMIDE HYDROCHLORIDE, FROM 4-AMINOBUTYRONITRILE HYDROLYSIS BY HYDROLYSIS OF THE LATTER IN A HYDROCHLORIC WATER MEDIUM; WHICH ALLOWS TO ISOLATE 4-AMINOBUTYRAMIDE HYDROCHLORIDE, OR GABAMIDE IN GOOD CONDITIONS OF PURITY AND PERFORMANCE. THIS PRODUCT IS OF INTEREST AS SUCH, BY ITS PSYCHOTROPIC PROPERTIES, AND AS AN INTERMEDIATE IN SYNTHESIS, OF NEW MOLECULES HAVING GABAMIMETIC PROPERTIES.

Process for the preparation of dialkylaminoacylanilides with local anesthetics

Process for the production of camphor derivatives