Derivatives of substituted pyrazole, a means to control insect

 

(57) Abstract:

Describes new derivatives of substituted pyrazole of the General formula I, where R is defloratin or triptorelin; n is the number 0, 1, 2. They are well tolerated by plants and low toxicity to warm-blooded animals and are suitable for combating pests, such as insects, arachnids and nematodes. Also described means for controlling insects on the basis of the compounds of formula I. 2 C. p. F.-ly, 1 table.

The invention relates to new derivatives of pyrazole with biological activity, in particular to new derivatives of substituted pyrazole.

Known derivatives of substituted pyrazole, possessing biological activity, in particular 5-amino-3-cyano-1-(2,6 - dichloro-4-triptoreline)-4-triftormetilfullerenov, known under the trade name "Fipronil" (see application EP N 0 295 117 A1, C 07 D 231/44, A 01 N 43/56).

The objective of the invention is to expand the Arsenal of highly active derivatives of substituted pyrazole.

This task is solved proposed derivatives substituted pyrazole of the General formula I

< / BR>
where R is defloratin or triptorelin,

n is the number 0, 1, 2.

R>
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with a compound of General formula III

R-S-Hal

where R has the above value, a Hal means halogen,

if necessary in the presence of a diluent and if appropriate in the presence of auxiliary tools,

or

b) the compound of General formula IV

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where R has the above meaning,

subjected to interaction with the oxidizing agent, if necessary in the presence of a diluent and if appropriate in the presence of a catalyst.

In the case of method a) get the target product, in which n means 0, and in the case of method b) - target product, in which n denotes 1 or 2.

As a diluent for carrying out the method (a) can be used in inert organic solvents, in particular aliphatic, alicyclic or aromatic, if necessary, halogenated hydrocarbons, such as benzine, benzene, toluene, xylene, chlorobenzene, petroleum ether, hexane, cyclohexane, dichloromethane, chloroform, carbon tetrachloride, ethers, such as, for example, diethyl ether, dioxane, tetrahydrofuran or etilenglikolevye or diethyl esters, ketones, such as acetone or butanone, NITRILES, such as iparralde or triamide hexamethylphosphoric acid, esters, such as, for example, a complex of ethyl esters of acetic acid, sulfoxidov as dimethyl sulfoxide, or acids, such as acetic acid.

Method (a) can also be carried out in the presence of an auxiliary tool. You can use any conventional inorganic or organic bases, such as hydroxides of alkali metals, such as, for example, sodium hydroxide or potassium hydroxide, carbonates of alkali metals, such as, for example, sodium carbonate, potassium or sodium bicarbonate, and tertiary amines, such as, for example, triethylamine, N,N-dimethylaniline, pyridine, N,N - dimethylaminopyridine, diazabicyclo, Diisobutylene or databaseconnect.

In the process (a) the reaction temperature can be varied within a wide range. In General the reaction is carried out at temperatures between -20 and 120oC, preferably 0 and 50oC.

For implementing the method (a) mol derivatives of pyrazole of the formula II in General apply 1.0 to 2.5 mol, preferably 1.0 to 1.5 mol of sulphonylchloride formula III and, if necessary, 1.0 to 2.5 mol, preferably 1.0 to 1.5 mol AIDS. The implementation of the reaction, processing and isolation of the compounds of formula I politely, used for the oxidation of sulfur. In particular, a suitable peroxide, organic nagkalat, as, for example, peracetic acid, m-chloroperbenzoic acid, p-nitrofurantoina acid or oxygen.

As a diluent for implementing the method (b) can also be used inert organic solvents. Preferably use hydrocarbons, such as benzine, benzene, toluene, hexane or petroleum ether, chlorinated hydrocarbons, such as dichloromethane, 1,2-dichloroethane, chloroform, carbon tetrachloride or chlorobenzene, ethers, such as diethyl ether, dioxane or tetrahydrofuran, carboxylic acids, such as acetic acid or propionic acid, or dipolar aprotic solvents, such as acetonitrile, acetone, complex ethyl ester of acetic acid or dimethylformamide.

Method (b) can also be applied in the presence of an acid acceptor. You can use any commonly used organic and inorganic acid acceptors. Preferably used hydroxides, acetates or carbonates of alkaline or alkaline earth metals, such as, for example, calcium hydroxide, sodium hydroxide, acetate natho catalyst. You can use any commonly used for such okislenii sulfur catalysts are metal salts, such as, for example, ammonium molybdate and sodium tungstate.

In the process (b) the reaction temperature can be varied within a wide range. In General the reaction is carried out at temperatures between -20 and 70oC, preferably 0 and 50oC.

For implementing the method (b) 1 mol of substituted 1-arylpyrazole formula IV in General apply 0.8 to 1.2 mol, preferably equimolar amount of an oxidant, if you want to interrupt the oxidation of sulfur on stage sulfoxide. For oxidation to the sulfone 1 mol of substituted 1-arylpyrazole formula IV is used in a total of 1.8 to 3.0 mol, preferably 2 mol oxidant. The implementation of the reaction, processing and isolation of the compounds of formula I is carried out in the usual way.

Derivatives of substituted pyrazole of the General formula I exhibit high insecticidal activity, and therefore, they can be an active substance means to control insect, which is an additional object of the present invention.

The proposed product contains not only the active ingredient in an effective amount, but at maimer, in the form of a solution, emulsions, suspensions, powders, foams, pastes, granules, aerosols, impregnated with active substances of natural and synthetic substances, microcapsules in polymeric materials and membranes for seed, and also as a component of combustible mixtures, for example, cartridges, banks and spirals for fumigation and so on, as well as preparations for the extremely fine distribution of cold and warm mist.

These preparations are prepared by known methods, for example, by mixing the active substances with targeted supplements, such as, for example, liquid solvents, pressurized liquefied gases and/or solid carriers, if appropriate using surface-active substances, such as, for example, emulsifiers and/or dispersants and/or foam-forming means. If the solvent used water, it is also possible to use organic solvents as auxiliary solvents. As liquid solvents are mainly used fragrances, such as xylene, toluene, or alkylnaphthalenes, chlorinated fragrances or chlorinated aliphatic hydrocarbons, such as, for example, chlorobenzene, chloroethylene or mate the functions, alcohols, such as butanol or glycol and also their ethers and esters, ketones, such as acetone, methyl ethyl ketone, methyl isobutyl ketone or cyclohexanone, strongly polar solvents, such as, for example, dimethylformamide and dimethylsulfoxide, and water; liquefied gaseous diluents or carriers are such solvents and carriers, which at room temperature and atmospheric pressure are gaseous, such as, for example, aerosol precursor gases, as, for example, halogenated hydrocarbons, butane, propane, nitrogen and carbon dioxide; as solid carriers used, for example, natural rock flours, such as, for example, kaolin, alumina, talc, chalk, quartz, attapulgite, montmorillonite or diatomaceous earth, and synthetic rock flours, such as, for example, highly dispersed silicic acid, alumina and silicates; as solid carriers for the preparation of pellets used, for example, crushed and fractionated natural rocks such as calcite, marble, pumice, thick, dolomite, and also synthetic granules of inorganic and organic flours, and granules of organic material such, the ve emulsifiers and/or foaming means can be called, for example, non-ionic or anionic emulsifiers, such as, for example, a complex polyoxyethylenic a fatty acid ester, a simple polyoxyethylene ether of fatty alcohol series, for example, a simple alkylarylsulphonates ether, alkyl sulphonates, alkyl sulphates, arylsulfonate, and also protein hydrolysates; as dispersing agents include, for example, exhaust ligninolytic liquor and methylcellulose.

The preparations may also contain binders, such as, for example, carboxymethylcellulose, natural and synthetic powdered, granular or Latecoere polymers, such as, for example, gum Arabic, polyvinyl alcohol, polyvinyl acetate, and also natural phospholipids, such as, for example, Catalina and lecithins, and synthetic phospholipids. As further additives can be called mineral and vegetable oils.

In addition, they may contain dyes, for example, inorganic pigments such as, for example, iron oxide, titanium oxide, ferrocyanide, and organic dyestuffs, such as alizarin dyes, azo dyes and metallophthalocyanine dyes and food trace elements, such as, for example, salts of iron, manganese, Betpakdala 0.5 to 90 wt.%.

Offer active substances may exist in the form of trading drugs, as well as get them drugs in a mixture with other active substances, such as, for example, insecticides, baits, sterilizing agent, acaricides, nematicides, fungicides, plant growth regulators or herbicides.

In addition, the proposed active substance can be in the form of their trading drugs, as well as derived from them, ready to use drugs in a mixture with synergists. Synergists are compounds which increase the action of the active substances themselves are not as active.

The concentration of active substance in the preparations can vary within wide limits. It is usually 0,0000001 - 95 wt.%, preferably of 0.0001 and 1 wt.%.

The usual treatment is carried out, the relevant drugs.

The following examples explain the present invention.

If nothing else is specified, the mean percent weight%.

Example 1.

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2 g (0,005 mol) 5-amino-3-cyano-4-(2,2,2-triptoreline)-1-(2,6-dichloro-4-triptoreline)-pyrazole are dissolved in 10 ml of acetic acid and mixed with sodium tungstate, zatrucie hydrogen. Stirred for another 18 hours as the results of thin-layer chromatography, the mixture is still not completely reacted, add 6 g (0,052 mol) of 30% hydrogen peroxide solution and stirred for another 18 h at room temperature. Then the reaction mixture is diluted with about 100 ml of water and extracted with dichloromethane. The dichloromethane phase is dried over magnesium sulfate and evaporated in a rotary evaporator under vacuum. Get 1 g (47% of theory) of 5-amino - 3-cyano-4-(2,2,2-cryptonemiales)-1-(2,6-dichloro-4 - triptoreline)-pyrazole with a melting point of 157oC.

Analogously to example 1 and in accordance with the above data according to the methods (a) and (b) one can obtain the following target products of the formula I:

about

1. Derivatives of substituted pyrazole of the General formula I

< / BR>
where R is defloratin or triptastic;

n is the number 0, 1, 2.

2. Means for combating insects, containing the active substance based on a derivative of the substituted pyrazole and at least one carrier, characterized in that as a derivative of the substituted pyrazole it contains a compound of General formula I

< / BR>
where R is defloratin or triptorelin;

n is the number 0, 1 or 2,

in an effective amount.

 

Same patents:

The invention relates to new derivatives of 5-arylindole formula I, where R1matter referred to in the description, A, B, C, and D each represent a carbon or one of them represents a nitrogen; R2, R3, R4, R5each independently represents hydrogen, C1- C6-alkyl, phenyl, halogen, cyano,- (CH2)mNR14R15, -(CH2)mOR9, -(CH2)mNR14COR9, -(CH2)mNR14CONHR9, -CO2R9; R6represents hydrogen, -OR10; R7, R8, R14, R15each independently represents hydrogen, C1- C6-alkyl, (CH2)xOR11; R9represents hydrogen, C1- C6-alkyl, phenyl; R10is1- C10-alkyl; R11is1- C6-alkyl; n = 0,1 or 2; m = 0, 1, 2 or 3; x = 2 or 3; the dotted line indicates the optional single bond or their pharmaceutically acceptable salts

The invention relates to new derivatives of 3(2H)-pyridazinone General formula I, where R1is hydrogen, phenyl, methyl, substituted CH3O or CH3SO2NH, C2-C4-alkyl, substituted R8R9N; C3-C5alkenyl, substituted phenyl, which is optionally substituted by halogen, one of A and B is hydrogen and the other a group of formula II, where R2and R3is independently hydrogen, C1-C4-alkyl or together with the adjacent group-N(CH2)nN - form pieperazinove or homopiperazine ring; R4is hydrogen or C1-C4-alkyl, R5, R6and R7is hydrogen, C1-C4-alkoxy, CH3SO2NH, X is a simple valence bond, an oxygen atom or the group-CH= CH-, m = 0-1, n = 2-3; R8and R9- independently C1-C4-alkyl, or together with the nitrogen atom to which they are attached, form morpholino - or 4-R10- piperazinone, where R10- C1-C4-alkyl, substituted phenoxypropane, or C3-C5alkenyl, substituted phenyl group, or an acid additive salts, which possess antiarrhythmic activity, pharmaceutical compositions containing an effective amount of the compounds in the mixture

The invention relates to substituted derivative asalaam, which is an effective anti-Helicobacter tools that can be used as monotherapy for eradication of Helicobacter pylori and related species

The invention relates to crystals containing water of crystallization (hereinafter referred to as hydrated form or simply hydrate), and the crystals without water of crystallization (hereinafter referred to as the anhydrous form or simply anhydrous), to a method for selective receipt of these crystals and, in addition, to pharmaceutical preparations containing such crystalline form

The invention relates to new chemical substances possessing valuable properties, in particular nitrogen-containing cyclic derivative of General formula

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where X is carbinieri, unsubstituted or substituted at the nitrogen atom by alkyl, aryl, heteroaryl or cyano, carbonyl, thiocarbonyl, sulfonyl, 1-nitroethene-2,2-diyl or 1,1-dicyano-Eten-2,2-diyl,

Y is unsubstituted or substituted Rcor Rdor Rcand Rdnonbranched alkylen or albaniles with 2 to 4 carbon atoms, which may optionally be substituted by one or two alkyl groups and in which one or two methylene groups can be replaced by a carbonyl, 1,2-cycloalkyl with 5 to 7 carbon atoms, unsubstituted or substituted Rcor Rdor Rcand Rd, 1,2 - cycloalkenyl with 5 to 7 carbon atoms, unsubstituted or substituted Rcor Rdor Rcand Rd, 1,2-Allen, 1,2-phenylene, in which one or two methine groups are replaced by nitrogen atom or one or two groups-CH=CH - replaced by a group-CO-NH - or a methine group substituted by nitrogen atom and one group-CH= CH - replaced by a group-CO-NH-, and above heterocycles or substituted Rcor Rd,

the first of the residues Ra- Rdmeans A group-B-, in which A group of the formula

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or

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where pentostatin can be monogamist the remainder R25mono - or Disaese the remainder R26or monogamist the remainder R25and additionally monogamist the remainder R26and the substituents R25and R26that may be the same or different and have the meanings stated below, in one bancoestado 1 - 3 methine group may be replaced by a nitrogen atom or a group-CH= CH - may be replaced by a group-CO-NR1or one methine group may be replaced by nitrogen atom and one group-CH=CH - may be replaced by a group-CO-NR1-, where R1means a hydrogen atom or alkyl,

G1and G4- bond or methylene which may be mono - or Disaese the alkyl, aryl or heteroaryl, and the substituents may be the same or different,

G2- bond or methylene, substituted residues R7and R8,

G3communication, methyl nitrogen atom or Metin, unsubstituted or substituted by alkyl, aryl or heteroaryl,

R2is a hydrogen atom, alkyl, aryl or heteroaryl or hydroxyl or alkoxyl if at least one of the groups G2and G3doesn't mean the relationship,

R3is a hydrogen atom, alkyl, aryl or heteroaryl or R3together with R2form an oxygen atom, if at least one of the groups G2and G3doesn't mean the relationship,

R4and R14is a hydrogen atom, cycloalkyl with 3 to 7 carbon atoms, cycloalkyl with 3 to 7 carbon atoms in cycloalkyl parts, alkyl with 1 to 8 carbon atoms, alkenyl with 3 to 8 carbon atoms, which may not be linked to the nitrogen atom through the vinyl group, hydroxyalkyl, alkoxyalkyl, aminoalkyl, acylaminoalkyl, dialkylaminoalkyl, cianelli, carboxyethyl, alkoxycarbonylmethyl, aminocarbonylmethyl, N-alkylaminocarbonyl, N,N-dialkylaminoalkyl, arylalkyl, heteroallyl, alkoxycarbonyl, allmediascotland, formyl, acetyl, TRIFLUOROACETYL, allyloxycarbonyl, amidino or R11CO-0-(R12CR13)-O-CO-, where R11is alkyl with 1 to 8 carbon atoms, cycloalkyl with 5 to 7 carbon atoms, aryl or arylalkyl, R12is a hydrogen atom, alkyl, cycloalkyl with sweetlenny alkylen 2 - 4 carbon atoms or methylene, if G2doesn't mean the relationship,

R5is a hydrogen atom, alkyl, aryl or heteroaryl or hydroxyl or alkoxyl, if G1no means of communication, or R4together with R5mean an additional bond, if G1means of communication,

R6is a hydrogen atom, alkyl, aryl or heteroaryl or a chlorine atom, a hydroxyl, methoxyl, amino, alkylamino or dialkylamino, if G1means linking and R4together with R5mean an additional bond, or R6together with R5mean oxygen atom, if G1doesn't mean the relationship,

R7is a hydrogen atom, alkyl, aryl or heteroaryl,

R8is a hydrogen atom, alkyl, aryl or heteroaryl or R8together with R4mean the unbranched alkylene with 2 to 5 carbon atoms,

R9is a hydrogen atom, alkyl, aryl or heteroaryl or hydroxyl or alkoxyl, if G2doesn't mean the relationship,

R10is a hydrogen atom, alkyl, aryl or heteroaryl or R10together with R4mean the unbranched alkylene with 2 to 4 carbon atoms,

R15is a hydrogen atom or chlorine, alkyl, aryl, heteroaryl, hydroxyl, methoxyl, amino, alkylamino or dialkylamino,

R16- foelkel 1 8 carbon atoms, alkenyl with 3 to 8 carbon atoms, which may not be linked to the nitrogen atom through the vinyl group, hydroxyalkyl, alkoxyalkyl, aminoalkyl, acylaminoalkyl, dialkylaminoalkyl, cianelli, carboxyethyl, alkoxycarbonylmethyl, aminocarbonylmethyl, N-alkylaminocarbonyl, N,N-dialkylaminoalkyl or arylalkyl,

R17is a hydrogen atom or alkyl, or R16together with R17mean an additional bond, if G4means of communication,

R18is a hydrogen atom, alkyl or fluorine atom, chlorine or bromine, hydroxyl, methoxyl, amino, alkylamino or dialkylamino, if G4means linking and R16and R17together denote an additional bond,

n is the number 1 or 2,

In - line, alkylen, albaniles, Allen, peridinin, pyrimidinyl, personalen or pyridazinyl, in which one or two groups-CH=N - can be replaced by a group-CO-NH - and one of the nitrogen atoms may be associated with the remainder of A connection instead of a hydrogen atom, and these heterocyclic groups may be optionally substituted by one or two alkyl groups, cycloalkyl with 4 to 7 carbon atoms, unsubstituted or substituted by one or two alkyl groups, unsubstituted or RC="http://www.fips.ru/fullimg2/rupat3/19993/003.dwl/2126002-6t.gif" ALIGN="ABSMIDDLE">replaced by a nitrogen atom, and, in addition, in the above mentioned 5 - to 7-membered rings, one adjacent to the nitrogen atom of the methylene group may be replaced by carbonyl, the second of the residues Ra- Rdmeans a group of the formula

F - E - D-,

where D is alkylene with 1 to 6 carbon atoms in which one methylene group may be replaced by oxygen atom or sulfur, sulfinil, sulfonium or the group-NR19-, where R19means a hydrogen atom, alkyl, alkylaryl, alkylsulfonyl, arylcarbamoyl or arylsulfonyl, or in which one ethylene group may be replaced by a group-CO-NR20- or-NR20-CO-, where R20means a hydrogen atom or alkyl, albaniles with 2 to 6 carbon atoms, Allen, peridinin, pyrimidinyl, personalen or pyridazinyl, in which one or two groups-CH=N - can be replaced by a group-CO-NH - and one of the nitrogen atoms, together with the hydrogen atom may also be linked with the rest of E, if the latter does not mean the connection or not connected via a heteroatom or a carbonyl with the rest of D, and these heterocyclic groups may be optionally substituted by one or two alkyl groups, indaniel, naftilan, 1,2,3,4-tetrahydronaphthalen or benzoguanamine, in which one of the be substituted by one or two alkyl groups, and the aromatic ring may be substituted by fluorine atom, chlorine, bromine or iodine, alkyl, trifluoromethyl, hydroxyl, alkoxyl, alkylsulfanyl, alkylsulfonyl, alkylsulfonyl or cyano, cycloalkyl with 4 to 7 carbon atoms, unsubstituted or substituted by one or two alkyl groups, unsubstituted or substituted by one or two alkyl groups cycloalkyl with 5 to 7 carbon atoms, in which one groupreplaced by a nitrogen atom, and, in addition, in the above mentioned 5 - to 7-membered rings, one adjacent to the nitrogen atom of the methylene group may be replaced by carbonyl, unsubstituted or substituted by one or two alkyl groups piperazinyl in which one adjacent to the nitrogen atom of the methylene group may be replaced by a carbonyl, or alkilenkarbonatov with the total number of carbon atoms 2-6, if E is a cyclic aminogroup, and a carbonyl linked to a nitrogen atom of a cyclic aminogroup group E, or a link, if E does not mean the relationship,

E - communication, alkylene with 1 to 6 carbon atoms which may be substituted by one or two alkyl groups with 1 to 8 carbon atoms, alkenyl or quinil with 2 to 4 carbon atoms, hydroxyl, is POI with the total number of carbon atoms of 2 10, the group HNR21- or N-alkyl-NR21-, where R21means alkylsulphonyl or alkylsulfonyl with 1 to 8 carbon atoms in the alkyl part, allyloxycarbonyl with the total number of carbon atoms 2 and 5 cycloalkylcarbonyl or cycloalkylcarbonyl with 5 to 7 carbon atoms in cycloalkyl part, arylalkylamines, arylalkylamines, arylethoxysilanes, arylcarbamoyl or arylsulfonyl, albaniles with 2 to 6 carbon atoms, Allen, peridinin, pyrimidinyl, personalen or pyridazinyl, unsubstituted or substituted by one or two alkyl groups, unsubstituted or substituted by one or two alkyl groups cycloalkyl with 5 to 7 carbon atoms, in which one groupreplaced by a nitrogen atom linked to the carbon atom of the residue D, cycloalkyl with 4 to 7 carbon atoms in cycloalkanones part, unsubstituted or substituted by one or two alkyl groups with 1 to 8 carbon atoms, alkenyl or quinil with 2 to 4 carbon atoms, hydroxyl, amino, aryl, heteroaryl, alkoxyl or alkylamino with 1 to 8 carbon atoms, dialkylamino with the total number of carbon atoms of 2 to 10, a group HNR21- or N-alkyl-NR21-, where R2119-, -NR20-CO - or-CO-NR20-, where R19and R20have the above meanings, with alkylene may be optionally substituted by one or two alkyl groups with 1 to 8 carbon atoms, alkenyl or quinil with 2 to 4 carbon atoms, hydroxyl, amino, aryl, heteroaryl, alkoxyl or alkylamino with 1 to 8 carbon atoms, dialkylamino with the total number of carbon atoms of 2 to 10, group-HNR21- or N-alkyl-NR21where R21have the above significance, with an additional heteroatom substituent heteroatom is separated from the remainder of W by at least two carbon atoms, if D does not mean the relationship,

F - carbonyl, substituted by hydroxyl, alkoxyl with 1 to 8 carbon atoms, arialcategory or group R22O-, where R22means cycloalkyl with 4 to 8 carbon atoms and cycloalkyl with 3 to 8 carbon atoms in cycloalkyl part, in which cycloalkyl part may be substituted by alkyl, alkoxyl or dialkylamino, or alkyl and 1 to 3 methyl groups, with one methylene group in the 4 - to 8-membered cycloalkyl part may be replaced by oxygen atom or alkylaminocarbonyl, benzocyclobutene the PA R23CO-O-CHR24-O-CO-, where R23means alkyl or alkoxy with 1 to 8 carbon atoms, cycloalkyl with 5 to 7 carbon atoms, cycloalkyl with 5 to 7 carbon atoms in cycloalkyl parts, aryl, aryloxy, arylalkyl or Allakaket and R24is a hydrogen atom or alkyl,

the shortest distance between the residue of F and located at a maximum distance from the rest F the nitrogen atom of the group A-B - is at least 11 links,

the third of the residues Ra- Rdmeans a hydrogen atom, alkyl, perfluoroalkyl, alkoxy, alkylsulfanyl, alkylsulfonyl, alkylsulfonyl, amino, alkylamino, dialkylamino, aryl, heteroaryl or arylalkyl,

the fourth of the residue Ra- Rdmeans a hydrogen atom, alkyl or aryl, and if nothing else is mentioned,

under the above term "aryl" is to be understood phenyl, which can be monogamist the remainder R25mono-, di - or triamese the remainder R26or monogamist the remainder R25and additionally mono - or Disaese the remainder R26and the substituents may be the same or different, R25means cyano, carboxyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminoalkyl, alkoxycarbonyl, alkylboron, the Mino, alkylamino, dialkylamino, alkylcarboxylic, phenylalkylamine, phenylcarbonylamino, alkylsulfonyl, phenylalkylamine, phenylcarbonylamino, N-alkyl-alkylcarboxylic, N-alkyl-phenylalaninamide, N-alkyl-phenylcarbonylamino, N-alkyl-alkylsulfonyl, N-alkyl-phenylalaninamide, N-alkyl-phenylcarbonylamino, aminosulfonyl, alkylaminocarbonyl or dialkylaminoalkyl, R26- alkyl, hydroxyl or alkoxy, fluorine atom, chlorine, bromine or iodine, and two residue R26if they are linked to adjacent carbon atoms, may also be alkylene with 3 to 6 carbon atoms, 1,3-butadiene-1,4-deelen or methylendioxy group

under the above term "Allen" should be understood phenylene, which can be monogamist the remainder R25mono - or Disaese the remainder R26or monogamist the remainder R25and additionally monogamist the remainder R26and the substituents may be the same or different and have the above values,

under the above term "heteroaryl" should read 5-membered heteroaromatic ring containing one atom of oxygen, sulfur or nitrogen, one atom of nitrogen and one atom of oxygen, sulfur is certain heteroaromatic ring, in which one or two of the groups-CH= N - can be replaced by a group-CO-NR20where R20has the above value, the heteroaromatic ring can be substituted by one or two alkyl groups or by a fluorine atom, chlorine, bromine or iodine, hydroxyl or alkoxyl in the carbon skeleton,

and, if nothing else is mentioned, the above alkyl, alkylene or CNS groups can contain 1 to 4 carbon atoms and each of the carbon atoms in the above alkilinity and cycloalkenes groups associated at least one heteroatom,

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