Thiazolyl-substituted carbocyclic 1,3-diones as agent for pest controlling

FIELD: organic chemistry, agriculture.

SUBSTANCE: Disclosed are compound of formula I wherein Het represents group of formula 2 (m = 0 or 1; X is hydrogen or C1-C12-alkyl or C1-C4-haloalkyl; Y is group of formula 3 and 4 wherein substitutes have meanings described in specification); A represents hydrogen, unsubstituted C1-C12-alkyl; C3-C8-cycloalkyl, or aryl; B represents hydrogen or C1-C6-alkyl; or A and B with carbon atom to which they are attached form saturated C3-C10-alkyl; A and Q1 together represent unsubstituted C3-C6-alkanediyl, wherein two non-adjacent carbon atoms optionally form further unsubstituted cycle; meanings of the rest substitutes are as described in specification.

EFFECT: new agents for controlling of agriculture pests.

4 cl, 28 ex

 

The text descriptions are presented in facsimile form.

1. The compounds of formula (I)

where Het means a group

m means the number 0 or 1,

X denotes hydrogen or alkyl with 1-6 carbon atoms,

Y represents the group

and

V1means halogen, alkyl with 1-12 carbon atoms or halogenated with 1-4 carbon atoms,

V2and V3mean hydrogen,

V1and V2means together with the carbon atom to which they relate, unsubstituted or substituted by alkyl with 1-4 carbon atoms or halogen 5 - or 6-membered cycle in which optionally one to two carbon atoms may be replaced by oxygen, sulfur or nitrogen,

A represents hydrogen, unsubstituted alkyl with 1-12 carbon atoms, cycloalkyl with 3-8 carbon atoms or aryl,

In the mean hydrogen or alkyl with 1-6 carbon atoms, a, b and the carbon atom to which they are bound represent a saturated cycloalkyl with 3-10 carbon atoms, in which optionally one ring link is replaced by oxygen,

And Q1together signify unsubstituted alcander with 3-6 carbon atoms, in which two carbon atoms that are not in close proximity to each other, form a, if necessary, further unsubstituted cycle

Q1denotes hydrogen, alkyl with 1-6 carbon atoms or phenyl, substituted by halogen,

Q2means hydrogen or alkyl with 1-4 carbon atoms,

Q3, Q4mean hydrogen,

Q1and Q2means together with the carbon atom to which they are connected, means cycloalkyl,

G denotes hydrogen or a group

,, or

where L denotes oxygen,

M stands for oxygen or sulphur,

R1means unsubstituted alkyl with 1-20 carbon atoms, or alkoxyalkyl with 1-8 carbon atoms in the CNS part and 1 to 8 carbon atoms in the alkyl part, or unsubstituted or substituted by a halogen cycloalkyl with 3-8 carbon atoms, or substituted with halogen phenyl or hetaryl,

R2means unsubstituted alkyl with 1-20 carbon atoms, phenyl or benzyl,

R3means unsubstituted alkyl with 1-8 carbon atoms, R6and R7means together with the nitrogen atom to which they relate, unsubstituted alkalinity radical of 3-6 carbon atoms, in which optionally one carbon atom is replaced by oxygen.

2. The compounds of formula (I) according to claim 1, in which

Het stands for a group,

m means the number 0 or 1,

X denotes hydrogen or alkyl with 1-4 carbon atoms,

Y stands for a group

V1means fluorine, chlorine, alkyl with 1-6 carbon atoms, or halogenated with 1-2 carbon atoms,

V2means hydrogen,

V1and V2together with the carbon atom to which they relate, signify unsubstituted or substituted by fluorine or stands 5 - or 6-membered cycle in which otonom, if necessary, one or two carbon atoms may be replaced by oxygen,

A represents hydrogen, unsubstituted alkyl with 1-8 carbon atoms, cycloalkyl with 5-6 carbon atoms or phenyl,

In the mean hydrogen or alkyl with 1-4 carbon atoms,

A, b and the carbon atom to which they are bound represent a saturated cycloalkyl with 5-6 carbon atoms, in which optionally one ring link replaced with oxygen, provided that in this case Q1only means hydrogen or alkyl with 1-4 carbon atoms,

And Q1together mean alcander with 3-4 carbon atoms,

Q1denotes hydrogen, alkyl with 1-4 carbon atoms or substituted by halogen phenyl,

Q2means hydrogen, methyl or ethyl,

Q3and Q4mean hydrogen,

Q1and Q2means together with the carbon atom to which they relate, cycloalkyl with 3-7 carbon atoms,

G denotes hydrogen or a group

,,or

where L denotes oxygen,

M stands for oxygen or sulphur,

R1means unsubstituted alkyl with 1-16 carbon atoms, alkoxyalkyl with 1-4 carbon atoms in the CNS part and 1-2 carbon atoms in al the safe side, unsubstituted or one - to twice substituted by fluorine, chlorine, cycloalkyl with 3-6 carbon atoms, phenyl, one to twice substituted by residues from the group comprising fluorine, chlorine, bromine, pyridyl or thienyl, once substituted residues from the group comprising fluorine, chlorine, bromine,

R2means unsubstituted alkyl with 1-16 carbon atoms, phenyl or benzyl,

R3means unsubstituted alkyl with 1-4 carbon atoms,

R6and R7means together with the nitrogen atom to which they relate, unsubstituted alkalinity radical with 5-6 carbon atoms, in which optionally one methylene group is replaced by oxygen.

3. The compounds of formula (I) according to claim 1, in which

Het stands for a group

m means the number 0 or 1,

X means hydrogen, methyl, ethyl, N.-propyl or isopropyl,

Y stands for a group

V1means hydrogen, fluorine, chlorine, bromine, methyl, ethyl, N.-propyl, isopropyl, N.-butyl, isobutyl, trebuil or trifluoromethyl,

V2means hydrogen,

A represents hydrogen, methyl, ethyl, N.-propyl, isopropyl, N.-butyl, isobutyl, tertbutyl, phenyl or cyclohexyl,

In the mean hydrogen, methyl or ethyl,

A, b and the carbon atom to which they are bound represent a saturated is cloaker with 5-6 carbon atoms, in which optionally one ring link replaced with oxygen, provided that in this case Q1only means hydrogen,

And Q1together signify unsubstituted alcander with 3-4 carbon atoms,

Q1means hydrogen, methyl, ethyl, N.-propyl, isopropyl or 4-chlorophenyl,

Q2means hydrogen, methyl or ethyl,

Q3and Q4mean hydrogen,

Q1and Q2means together with the carbon atom to which they are bound, a saturated cycloalkyl with 5-6 carbon atoms, provided that in this case And only means hydrogen,

G denotes hydrogen or a group

,,or

where L denotes oxygen, and

M stands for oxygen or sulphur,

R1means unsubstituted alkyl with 1-8 carbon atoms, alkoxyalkyl with 1-2 carbon atoms in the CNS part and 1-2 carbon atoms in the alkyl part, cyclopropyl or cyclohexyl, unsubstituted or once substituted by residues from the group comprising fluorine, chlorine, phenyl, once substituted by a residue from the group comprising fluorine, chlorine, bromine, thienyl or pyridyl, once substituted residues from the group comprising fluorine, chlorine and bromine,

R2Osnach the em alkyl with 1-8 carbon atoms, phenyl or benzyl,

R3means methyl or ethyl,

R6and R7means together with the nitrogen atom to which they relate, alkalinity radical with 5 carbon atoms, in which optionally one methylene group is replaced by oxygen.

4. The compounds of formula (I) according to claim 1, in which

Het stands for a group,

m means the number 0 or 1,

X means hydrogen, methyl or ethyl,

Y stands for a group

V1means hydrogen, chlorine, methyl, ethyl, N.-propyl, isopropyl, N.-butyl, isobutyl, tertbutyl, trifluoromethyl,

A represents hydrogen, methyl, ethyl, N.-propyl, isopropyl, N.-butyl, isobutyl, phenyl or cyclohexyl,

In the mean hydrogen, methyl or ethyl,

A, b and the carbon atom to which they are bound represent a saturated cycloalkyl with 5-6 carbon atoms, in which optionally one ring link replaced with oxygen, provided that in this case Q1only means hydrogen,

And Q1together mean alcander with 3-4 carbon atoms,

Q1means hydrogen, methyl, ethyl, N.-propyl, isopropyl or 4-chlorophenyl,

Q2means hydrogen, methyl or ethyl,

Q3means hydrogen,

Q4means hydrogen,

Q1very lovely and q 2means together with the carbon atom to which they are bound, a saturated cycloalkyl with 5-6 carbon atoms,

provided that in this case And only means hydrogen,

G denotes hydrogen or a group

,,or

where L denotes oxygen, and

M stands for oxygen or sulphur,

R1means alkyl with 1-8 carbon atoms, alkoxyalkyl with 1-2 carbon atoms in the CNS part and 1-2 carbon atoms in the alkyl part, or unsubstituted or substituted once by chlorine cyclopropyl, once substituted by chlorine, phenyl or substituted once by chlorine pyridyl,

R2means alkyl with 1-8 carbon atoms, phenyl or benzyl,

R3means methyl or ethyl,

R6and R7means together with the nitrogen atom to which they relate, alkalinity radical with 5 carbon atoms, in which optionally one methylene group is replaced by oxygen.



 

Same patents:

FIELD: organic chemistry, organic synthesis, chemical technology.

SUBSTANCE: invention describes a method for synthesis of di-[(6-benzyl-4,2,6-thiadiazolidine-2-yl)methyl]sulfide of the general formula (1): . Method involves interaction of formaldehyde aqueous solution saturated with hydrogen sulfide with benzyl hydrazine in the mole ratio benzyl hydrazine : formaldehyde : hydrogen sulfide = 1:3:2, respectively, at temperature 0°C and stirring the mixture for 3 h. Invention provides preparing the end product with high regioselectivity.

EFFECT: improved method of synthesis.

1 cl, 1 ex

FIELD: synthesis of biologically active compounds.

SUBSTANCE: invention provides 1,5-benzothiazepines of general formula I (formulae presented below), in which Rv and Rw are independently selected from hydrogen and C1-C5-alkyl; one of Rx and Ry represents hydrogen or C1-C6-alkyl and the other hydroxy or C1-C6-alkoxy; Rz is selected from halogen, nitro, cyano, hydroxy, amino, carboxy, carbamoyl, mercapto, sulfamoyl, C1-C6-alkyl, and other residues indicated in claim 1 of invention; v is a number from 0 to 5; one of R4 and R5 represents group of general formula IA; R3 and R6 and the second from R4 and R5 are independently selected from hydrogen, halogen, nitro, cyano, hydroxy, amino, carboxy, carbamoyl, mercapto, sulfamoyl, C1-C6-alkyl, and other residues indicated in claim 1; R3 and R6 and the second from R4 and R5 being optionally substituted by one or several R16 groups at their carbon atoms; D represents -O-, -N(Ra)-, -S(O)b- or -CH(Ra)-, wherein Ra is hydrogen or C1-C6-alkyl; and b=0-2; ring A represents aryl or heteroaryl and is optionally substituted by one or several substituents selected from R17; R7 represents hydrogen, C1-C4-alkyl, carbocyclyl, or heterocyclyl and is optionally substituted by one or several substituents selected from R18; R8 represents hydrogen or C1-C4-alkyl; R9 represents hydrogen or C1-C4-alkyl; R10 represents hydrogen or C1-C4-alkyl, carbocyclyl, or heterocyclyl and is optionally substituted by one or several substituents selected from R19; R11 represents carboxy, sulfo, sulfino, phosphono, tetrazolyl, -P(O)(ORc)(ORd), -P(O)(OH)(ORc), -P(O)(OH)(Rd), or -(O)(ORc)(Rd), wherein Rc and Rd are independently selected from C1-C6-alkyl; or R11 represents group of general formula IB, in which X is -N(Rq)-, N(Rq)C(O)-, -O-, or -S(O)a, wherein a=0-2; and Rq is hydrogen or C1-C4-alkyl; R12 represents hydrogen or C1-C4-alkyl; R13 and R14 are independently selected from hydrogen, C1-C4-alkyl, carbocyclyl, heterocyclyl, or R23, of which C1-C4-alkyl, carbocyclyl, heterocyclyl, or R23 can be optionally independently substituted by one or several substituents selected from R20; R15 represents carboxy, sulfo, sulfino, phosphono, tetrazolyl, -P(O)(ORe)(ORf), -P(O)(OH)(ORe), -P(O)(OH)(Re), or -P(O)(ORe)(Rf), wherein Re and Rf are independently selected from C1-C6-alkyl; or R15 represents group of general formula IC, in which R24 is selected from hydrogen and C1-C4-alkyl; R24 is selected from hydrogen, C1-C4-alkyl carbocyclyl, heterocyclyl, and R27, of which C1-C4-alkyl, carbocyclyl, heterocyclyl, or R27 can be optionally independently substituted by one or several substituents selected from R28; R26 is selected from carboxy, sulfo, sulfino, phosphono, tetrazolyl, -P(O)(ORg)(ORh), -P(O)(OH)(ORg), -P(O)(OH)(Rg), or -P(O)(ORg)(Rh), wherein Rg and Rg are independently selected from C1-C6-alkyl; p=1-3; wherein meanings for R13 can be the same or different; q=0-1; r=0-3; wherein meanings for R14 can be the same or different; m=0-2; wherein meanings for R10 can be the same or different; n=1-3; wherein meanings for R7 can be the same or different; z=0-3; wherein meanings for R25 can be the same or different; R16, R17, and R18 are independently selected from halogen, nitro, cyano, hydroxy, carbamoyl, mercapto, sulfamoyl, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkynyl, C1-C4-alkoxy, C1-C4-alkanoyl, C1-C4-alkanoyloxy, N-(C1-C4-alkyl)amino, N,N-(di-C1-C4-alkyl)amino, C1-C4-alkyl-S(O)a (wherein a=0-2), C1-C4-alkoxycarbonyl, N-(C1-C4-alkyl)sulfamoyl, and N,N-(di-C1-C4-alkyl)sulfamoyl; wherein R16, R17, and R18 can be optionally independently substituted by one or several of R21 at their carbon atoms; R19, R20, R23, R27, and R28 are independently selected from halogen, nitro, cyano, hydroxy, carbamoyl, mercapto, sulfamoyl, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkynyl, C1-C4-alkoxy, C1-C4-alkanoyl, C1-C4-alkanoyloxy, N-(C1-C4-alkyl)amino, N.N-(di-C1-C4-alkyl)amino, C1-C4-alkanoylamino, N-(C1-C4-alkyl)carbamoyl, N,N-(di-C1-C4-alkyl)carbamoyl, C1-C4-alkyl-S(O)a (wherein a=0-2), C1-C4-alkoxycarbonyl, N-(C1-C4-alkyl)sulfamoyl, N,N-(di-C1-C4-alkyl)sulfamoyl, carbocyclyl, heterocyclyl, sulfo, sulfino, amidino, phosphono, -P(O)(ORa)(ORb), -P(O)(OH)(ORa), -P(O)(OH)(Ra), or -P(O)(ORa)(Rb), wherein Ra and Rb are independently selected from C1-C6-alkyl and wherein R19, R20, R23, R27, and R28 can be optionally independently substituted by one or several of R22 at their carbon atoms; R21 and R22 are independently selected from halogen, hydroxy, cyano, carbamoyl, mercapto, sulfamoyl, trifluoromethyl, trifluoromethoxy, methyl, ethyl, methoxy, ethoxy, vinyl, allyl, ethynyl, methoxycarbonyl, formyl, acetyl, formamido, acetylamino, acetoxy, methylamino, dimethylamino, N-methylcarbamoyl, N,N-dimethylcarbamoyl, methylthio, methylsulfinyl, mesyl, N-methylsulfamoyl, N,N-dimethylsulfamoyl; or pharmaceutically acceptable salt thereof, solvate, or salt solvate. Described are also method for preparing compounds of formula I, pharmaceutical compositions based on compounds I, and a method for achieving inhibiting effect relative to interscapular brown adipose tissue (IBAT), and intermediates. (I), (IA), (IB), (IC).

EFFECT: expanded synthetic possibilities in the 1,5-benzothiazepine series.

36 cl, 121 ex

FIELD: organic chemistry, medicine, biology.

SUBSTANCE: invention relates to novel derivatives of thiazole that are strong antagonists, agonists or partial agonists of cannabinoid CB1 receptors. Compounds show the general formula (I): wherein R and R1-R4 have values given in the invention claim. Also, invention relates to using compounds of the formula (I) or their stereoisomers for preparing a pharmaceutical composition. Also, invention relates to intermediate compounds of the formula (V): wherein R2 and R8 have values given in the invention claim.

EFFECT: valuable medicinal and biological properties of compounds.

5 cl, 1 tbl, 7 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of phenoxy-N-[4-(1,1-dioxoisothiazolidin-2-yl)-valeramide and describes compounds of the formula (I): wherein E represents phenyl or isoquinoline each of that is monosubstituted with group R1 wherein R1 represents -CN, amidino-group, halogen atom, -NH2, -CH2NH2 or compound of the formula: W represents -OCHAr', -OCHA, -NHCHAr', -NHCHA, -NHCOOCHAr', -NHCONHCHAr' or piperidine-1,2-diyl; Ar' represents unsubstituted phenyl or mono- or disubstituted phenyl, Hal, A or -CF3; A represents alkyl with 1, 2, 3, 4, 5, 6 or 7 C-atoms; X represents -CONH; Y represents Ar-diyl; T represents group -(CH2)3; Ar represents unsubstituted phenyl or mono- or disubstituted phenyl, Hal, A or -CF3; Hal represents fluorine (F), chlorine (Cl), bromine (Br) or iodine (J) atoms. These compounds are the coagulation factor Xa inhibitors. Also, invention relates to a method for synthesis of compounds of the formula (I), a medicinal agent containing these compounds and using compounds of the formula (I) for preparing a drug used in treatment of thrombosis, myocardium infarction, arteriosclerosis, inflammation, apoplexy, stenocardia, restenosis after plastic surgery in vessels, intermittent lameness, migraine, tumors, tumor diseases and/or tumor metastasis and a kit (set). Also, invention relates to intermediate compounds of the formula (I-1): wherein R1 represents -NO2 or -NH2; R represents methyl, chlorine atom or trifluoromethyl and their salts. Invention provides synthesis of novel compounds possessing valuable biological properties.

EFFECT: valuable medicinal properties of compounds.

9 cl, 1 tbl, 14 ex

FIELD: organic chemistry, herbicides.

SUBSTANCE: invention describes substituted benzoylpyrazoles of the general formula (I): wherein Q means oxygen atom (O); R1 means alkyl with 1-6 carbon atoms; R2 means hydrogen atom; R3 and R4 mean independently of one another hydrogen atom, halogen atom, alkyl with 1-4 carbon atoms substituted with halogen atom; R5 means hydrogen atom, alkyl with 1-6 carbon atoms; Y means hydrogen atom; Z means alkoxyamino-group with 1-6 carbon atoms, alkylamino-group with 1-6 carbon atoms, substituted alkoxy-group with 1-4 carbon atoms, N-alkylalkoxyamino-group with 1-4 carbon atoms, phenyl substituted with halogen atom, monocyclic heterocyclyl, heterocyclylamino-group, group -N=(heterocyclyl) chosen from the group: furyl, tetrahydrofurylmethylamino-group, isoxazolyl, dihydroisoxazolyl (isoxazolinyl), tetrahydroisoxazolyl (isoxazolidinyl), tetrahydro-(2H)-1,2-oxazine-2-yl, dihydrothiazolyl (thiazolinyl), oxadiazolylamino-, thiadiazolylamino-group, piperidinyl, piperidinylamino-group, 2-oxo-1,3-diazacyclohexyl, morpholinyl, morpholinylamino-group, respectively, and substituted if necessary with alkyl with 1-4 carbon atoms, halogenalkyl with 1-4 carbon atoms, cycloalkyl with 3-6 carbon atoms involving their all possible tautomeric forms and possible salts. Also, invention describes a herbicide agent based in proposed compounds. Proposed compounds possess herbicide activity.

EFFECT: valuable properties of compounds and agent.

4 cl, 5 tbl, 77 ex

FIELD: chemistry of heterocyclic compounds, medicine, pharmacy.

SUBSTANCE: invention relates to novel heterocyclic compounds of the general formula (I): wherein R1 represents hydrogen atom or (C1-C6)-alkyl; R2 represents hydrogen atom, -CO-R3 wherein R3 represents (C2-C6)-alkyl substituted optionally with halogen atom, -CO-C(R4)=C(R4)-R5 wherein R4 represents hydrogen atom or (C1-C4)-alkyl; R5 represents (C1-C8)-alkyl, (C2-C8)-alkenyl and others; Y represents compound of the formula: wherein R7 represents hydrogen atom or (C1-C4)-alkyl; R8 represents (C5-C8)-alkyl, (C4-C8)-cycloalkyl and others; X represents oxygen atom or sulfur atom and others. Also, invention relates to pharmaceutically acceptable salts of these compounds. Compounds of the formula (I) possess hypoglycemic and/or hypolipidemic activity and can be used in medicine in treatment of diabetes mellitus, hyperlipidemia, hyperglycemia, diseases caused by resistance to insulin and other diseases.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

28 cl, 3 tbl, 131 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel substituted derivatives of 4-phenyltetrahydroisoquinoline of the general formula (I): wherein R1, R2, R3 and R4 mean independently of one another hydrogen (H), fluorine (F), chloride (Cl), bromine (Br) atoms, CaH2a+1 wherein one or more atoms H are substituted with F, -NR11R12 or -SOj-R15 wherein a = 1-8; R11 and R12 mean independently of one another H, CeH2e+1 or CrrH2rr-1 wherein e = 1-4; rr = 3, 4, or in common with nitrogen atom to which they are bound form a cycle chosen from group consisting of pyrrolidinyl, piperidinyl, N-methylpiperazinyl, piperazinyl or morpholine; j = 1 or 2; R15 means CkH2k+1 wherein k = 1-8; R5 means CpH2p+1 or CssH2ss-1; p = 1-8; ss = 3-8; R6 means H; R7, R8 and R9 mean independently of one another mean -SOwR23, -NR32COR30, NR32CSR30, -NR32SObbR30, H, F, Cl, Br, -OH, -NH2, CeeH2ee+1, -NR40R41, -CONR40R41 or -COOR42 wherein w = 0, 1 or 2; bb = 2 or 3; R23 means NR25R26 wherein R25 and R26 mean independently of one another H or CzH2z+1, CzzH2zz-1 wherein z = 1-8; zz = 3-8 wherein in CzH2z+1 and CzzH2zz-1 one or more H atoms are substituted with fluorine atom and one or more CH2-groups are substituted with -C(=O) or NR27 wherein R27 means H or CaaH2aa+1 wherein aa = 1-4; or R25 and R26 in common with nitrogen atom to which they are bound form 5-, 6- or 7-membered cycle; R30 means H, CccH2cc+1, CyyH2yy-1, pyrrolydinyl, piperidinyl wherein in their cycles CH2-group can be substituted with oxygen atom (O) or -NR33; R32 and R33 mean independently of one another H or ChH2h+1 wherein cc = 1-8; yy = 3-8; h = 1-8 wherein in the group ChH2h+1 one or more hydrogen atoms are substituted with fluorine atom, and in the groups CccH2cc+1 and CyyH2yy-1 one or more hydrogen atoms can be substituted with fluorine atom, and CH2-group can be substituted with O or -NR31 wherein NR31 means H, methyl, ethyl, acetyl or -SO2CH3; or R30 means 6-membered heteroaryl with 1-4 nitrogen atoms, 0 or 1, S-atoms or 0, or 1 O-atom that represents unsubstituted or substituted with up to three substitutes chosen from group consisting of F, Cl, Br, J, CooH2oo+1 wherein one or more hydrogen atoms can be substituted with fluorine atom, -NO2 or -NR70R71 wherein oo = 1-8; R70 and R71 mean independently of one another H, CuuH2uu+1 or -COR72 wherein uu = 1-8; R72 means H, CvvH2vv+1 wherein vv = 1-8; ee = 1-8; R40 and R41 mean independently of one another H, CttH2tt+1 or -C(NH)NH2 wherein tt = 1-8 and wherein in the group CttH2tt+1 one or more CH2-groups can be substituted with NR44 wherein R44 means CggH2gg+1 wherein gg = 1-8; R42 means H or ChhH2hh+1 wherein hh = 1-8 being, however, two substitutes from group R7, R8 and R9 can't mean -OH simultaneously, and at least one residue from R7, R8 and R9 must be chosen from group consisting of -CONR40R41, -OvSOwR23, -NR32COR30, -NR32CSR30 and -NR32SObbR30. Also, invention relates to using above given compounds for preparing a medicinal agent. Also, invention considers a medicinal agent representing inhibitor of sodium-proton exchange of subtype III (NHE3) based on proposed compounds. Invention provides synthesis of novel compounds, a medicinal agent based on thereof for aims of treatment of such diseases as nervous system ischemia, insult and brain edema, in treatment of snore, shock, impaired respiratory impulse, as purgative agents, as agents against extoparasites, for prophylaxis of gall stones formation, as anti-atherosclerotic agents, agents against diabetes mellitus later complications, cancer diseases, fibrous diseases, endothelial dysfunction, hypertrophies and hyperplasia of organs and others.

EFFECT: valuable medicinal properties of compounds and medicinal agents.

21 cl, 15 tbl, 221 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention proposes novel derivatives of thiazole that able for effective binding and activating PPARα and/or PPARγ simultaneously and, respectively, combine antiglycemic effect caused by activation of PPARγ with anti-dyslipidemic effect caused by activation of PPARα. Also, the claim describes compounds of the formula (I): wherein substitutes from R1 to R10 as well as X and Y are determined in the description and invention claim, and their pharmaceutically acceptable salts and esters also. Also, the proposed invention describes pharmaceutical compositions possessing antagonistic activity with respect to PPARα and/or PPARγ comprising compound of the formula (I) as an active component and pharmaceutically acceptable carrier and/or additive. Except for, the invention proposes claimed compounds as therapeutically active substances for treatment and/or prophylaxis of diseases mediated by agonists of PPARα and/or PPARγ, such as diabetes mellitus, non-insulin dependent diabetes mellitus, elevated blood pressure, increased level of lipids and cholesterol, atherosclerotic diseases, metabolic syndrome, endothelial dysfunction, procoagulant state, dyslipidemia, ovary polycystic syndrome, inflammatory or proliferative diseases.

EFFECT: valuable medicinal properties of compounds.

27 cl, 140 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of benzothiazole of the general formula (I): and their pharmaceutically acceptable acid-additive salts used as ligands of adenosine receptors and to a medicinal agent based on thereof. In compound of the general formula (I) R means phenyl, pyridine-2-yl, -C(O)-O-(lower)-alkyl, -C(O)-(lower)-alkyl, -C(O)-morpholinyl, -C(O)-NR'2, -(CH2)n-NR'2 or -(CH2)n-O-(lower)-alkyl; R' means hydrogen atom or (lower)-alkyl. Compounds can be used in treatment and prophylaxis of diseases mediated by adenosine receptors A2A and A1, for example, in Alzheimer's disease, some depressive states, toxicomania, Parkinson's disease.

EFFECT: valuable medicinal properties of compounds.

15 cl, 3 sch, 6 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of nicotine- or isonicotine-benzothiazole of general formulas (IA) and (IB) their pharmaceutically acceptable acid-additive salts and a medicinal agent based on thereof. In compounds of general formula (IA) and (IB) R1 means phenyl, piperidine-1-yl or morpholine; A means -O-; R means -(CH2)n-N(R'')-C(O)-lower alkyl, -(CH2)n-O-lower alkyl, -(CH2)n-O-(CH2)n-O-lower alkyl, lower alkyl, -(CH2)n-morpholinyl, -(CH2)n-phenyl, -(CH2)n-N(R''), -(CH2)n-pyridinyl, -(CH2)n-CF3, -(CH2)n-2-oxopyrrolidinyl or (C4-C6)-cycloalkyl; R'' mean(s) independently of one another hydrogen atom or lower alkyl; n= 1 or 2; A means -N(R')-; R means lower alkyl, (C4-C6)-cycloalkyl, -(CH2)n-O-lower alkyl, -(CH2)n-pyridinyl, -(CH2)n-piperidinyl, -(CH2)n-phenyl, -(CH2)n-N(R'')-C(O)-lower alkyl, -(CH2)n-morpholinyl or -(CH2)n-N(R'')2; R' and R'' mean independently of one another hydrogen atom or lower alkyl; n = 1 or 2; or A means -CH2-; R means -N(R'')-(CH2)m-O-lower alkyl, -N(R'')2, S-lower alkyl, or R means azethidinyl, pyrrolidinyl or piperidinyl that are substituted optionally with hydroxy-group or lower alkoxy-group; or R means morpholinyl, -N(R'')-(CH2)m-(C4-C6)-cycloalkyl, -N(R'')-(CH2)m-C(O)-O-lower alkyl, -O-(CH2)m-O-lower alkyl or alkoxy-group; R'' mean(s) independently of one another hydrogen atom or lower alkyl; m = 1, 2 or 3; or A means -S-; R means lower alkyl, or A-R mean in common piperazinyl substituted with alkyl, -C(O)-lower alkyl or oxo-group, or group A-R means piperidinyl substituted with lower alkoxy-group or hydroxy-group, or group A-R means morpholinyl substituted with lower alkyl, or group A-R means (C4-C6)-cycloalkyl, azethidine-1-yl optionally substituted with hydroxy-group or lower alkoxy-group, or group A-R means thiomorpholinyl-1,1-dioxo-group, tetrahydropyrane or 2-oxa-5-azabicyclo[2.2.1]hept-5-yl. Proposed compounds can be used in treatment of diseases mediated by adenosine A2A-receptors, for example, Alzheimer disease, some depressive states, toxicomania and Parkinson's disease.

EFFECT: valuable medicinal properties of compounds and agent.

37 cl, 10 sch, 109 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to compounds of the formula: or wherein x means 1, 2, 3 or 4; m means 1 or 2; n means 1 or 2; Q represents carbon atom (C) or nitrogen atom (N); A represents oxygen atom (O) or sulfur atom (S); R1 represents lower alkyl; X represents -CH; R2 represents hydrogen (H) or halogen atom; R2a, R2b and R2c can be similar or different and they are chosen from hydrogen atom (H), alkyl, alkoxy-group or halogen atom; R3 represents aryloxycarbonyl or alkoxyaryloxycarbonyl; Y represents -CO2R4 wherein R4 represents hydrogen atom (H) or alkyl, and including all their stereoisomers, their prodrugs as esters and their pharmaceutically acceptable salts. These compounds are useful antidiabetic and hypolipidemic agents and agents used against obesity also.

EFFECT: valuable medicinal properties of compounds.

29 cl, 12 tbl, 587 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new compounds of the following formulae:

and , and to a pharmaceutical composition possessing the PPAR-ligand binding activity and comprising the indicated compound, and a pharmaceutically acceptable vehicle. Also, invention relates to a method for treatment of patient suffering with physiological disorder that can be modulated with the compound possessing the PPAR-ligand binding activity. Method involves administration to the patient the pharmaceutically effective dose of indicated compound or its pharmaceutically acceptable salt.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

10 cl, 1 tbl, 104 ex

The invention relates to a method for producing 4-methyl-5-formyl-thiazol by oxidation of 4-methyl-5-(2-hydroxyethyl)-thiazole using an aqueous solution of chromium oxide or inorganic bichromate in the presence of sulfuric acid and the oxidation is carried out in a two-phase system water-organic solvent, at a temperature of 20-50C., the organic solvent used diethyl ether, benzene, chloroform, and methylene chloride

The invention relates to a method for producing 5-[4-[[3-methyl-4-oxo-3,4-dihydroquinazolin-2-yl] methoxy] benzyl] thiazolidin-2,4-dione of formula (1), including the restoration of the compounds of formula (2'), where R is a (C1-C4)alkyl group, with the use of Raney Nickel or magnesium and, optionally, re-esterification using sulfuric acid in the temperature range from 0 to 60oWith obtaining the compounds of formula (3'), which is subjected to hydrolysis to obtain the acid of formula (4), the condensation of the acid of formula (4) with N-methyl-anthranilamide formula (7) without any pre-activation of the acid to obtain the compounds of formula (1), which is optionally transformed into a pharmaceutically acceptable salt

The invention relates to new derivatives oksiminoalkil acid of the formula (I), where R1is oxazolyl, optionally substituted with 1-2 substituents selected from lower alkyl, phenyl, teinila, furil; thiazolyl, optionally substituted with 1-2 substituents selected from lower alkyl, phenyl; unsubstituted chinoline and so on; X represents a bond or the group-NR6- where R6represents hydrogen or C1-4alkyl; n represents an integer from 1 to 3; Y represents an oxygen atom or the group-NR7- where R7is hydrogen; ring a represents a benzene ring, optionally substituted by one or two1-4alkoxy; p is an integer from 1 to 3; R2represents phenyl, optionally substituted lower alkyl, halogen, and so on; unsubstituted furyl; unsubstituted pyridyl; pyridinyl-1-oxide; q is an integer from 0 to 6; m represents 0 or 1; R3represents a hydroxy-group, lower alkoxy or-NR9R10where R9and R10represent identical or different groups selected from hydrogen, lower alkyl and lower alkylsulfonyl; R4and R5represent identical or different groups selected from hydrogen or

The invention relates to new thiazole derivative of the formula I, where R1denotes a group of formula (a), (b), (C), R2denotes a group of formula (d), where Het represents a five - or six-membered heterocyclic group which is substituted by9and in the loop which, in addition to the nitrogen atom, can optionally contain an oxygen atom, R3denotes hydrogen, alkyl, cycloalkyl, phenyl, R4denotes hydrogen, phenyl, R5- R8independently of one another denotes hydrogen, R9denotes a group of formula (e) and (f), R10denotes phenyl, a-i denotes 0 or a positive integer, i.e

The invention relates to compounds of dehalogenation, insecticide/acaricidal agents containing these compounds as active ingredients and intermediates for their production

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new compounds of the following formulae:

and , and to a pharmaceutical composition possessing the PPAR-ligand binding activity and comprising the indicated compound, and a pharmaceutically acceptable vehicle. Also, invention relates to a method for treatment of patient suffering with physiological disorder that can be modulated with the compound possessing the PPAR-ligand binding activity. Method involves administration to the patient the pharmaceutically effective dose of indicated compound or its pharmaceutically acceptable salt.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

10 cl, 1 tbl, 104 ex

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