IPC classes for russian patent 3-amino-6-(1-aminoethyl)tetrahydropyrane derivatives (RU 2471795):
Another patents in same IPC classes:
Oxazolidine antibiotics / 2470022
Claimed invention relates to derivatives of antibiotics, which represent compounds of formula (I) ![]() and their pharmaceutically acceptable salts, where U, V, W, X, R 1, R 2, R 3, R 4, R 5, R 6, A, B, D, E, G, m and n are determined in description. Invention also relates to pharmaceutical composition, containing said compounds and their application for obtaining medication for prevention or treatment of bacterial infections.
Azaindoles useful as janus kinase inhibitors / 2453548
Invention relates to novel azaindole derivatives, having JAK-2 and JAK-3 kinase inhibiting activity, or pharmaceutically acceptable salts thereof. In formula (I): ![]() R 3 denotes H; X 1 denotes N or CR 4; R 2 denotes H, COOH, COOR' or CONHR'; R 4 denotes H, F, R, OH, OR', COR', COOH, COOR', CONH 2 or CN; or R 2 and R 4, taken together, form a benzene ring optionally substituted with 1-2 R 10; R' denotes C 1-3-alkyl or C 1-3-alkenyl, each optionally substituted 1-2 R 5; each R 5 is independently selected from CN, unsubstituted C 1-2alkyl, or two groups R 5 together with a carbon atom with which they are bonded form a cyclopropyl ring; each R 10 is independently selected from halogen, OCH 3 or OH; R 1 denotes ![]() or ![]() , R ” is H or denotes C 1-2alkyl, optionally substituted with 1-3 R 11; R 6 denotes C 1-4alkyl, optionally substituted with 1-5 R 12; values of radicals R 7 -R 9, ring A, R 11 -R 14. The invention also relates to a pharmaceutical composition containing said compounds and a method of treating or reducing severity of a pathological condition such as allergy, asthma, amyotrophic lateral sclerosis, multiocular sclerosis, graft rejection, rheumatoid arthritis, solid malignant tumour, haematologic malignant disease, leukaemia, lymphoma and myeloproliferative disorders.
Substituted imidazopyridine derivatives as melanocortin-4 receptor antagonists / 2451684
Present invention relates to substituted imidazopyridine derivatives of general formula ![]() (I) or enantiomers, diastereomers and tautomers and pharmaceutically acceptable salts thereof, in which A denotes -NH-, -CH 2-, -CH 2-CH 2- or a bond; X denotes phenyl, phenyl condensed with a saturated heterocyclic 5- or 6-member ring, where the heterocyclic ring can contain one or two heteroatoms selected from O and N, and where the heterocyclic ring can further be substituted with an oxo group, a 6-member saturated heterocyclyl containing O as a heteroatom, a 5-6-member heteroaryl containing 1 or 2 heteroatoms selected from N, O and S, and where each phenyl and heteroaryl is possibly substituted with 1 to 2 R 14 and/or 1 substitute R 4b and/or 1 substitute R 5; R 1 and R 2 are independently selected from the following groups: C 1-6-alkyl and C 1- 6-alkylene-C 3-7-cycloalkyl, and where each alkyl is possibly substituted with a OH group, or R 1 and R 2 together with the nitrogen atom with which they are bonded form a 5-6-member ring which is possibly substituted with one substitute selected from C 1-6-alkyl and O-C 1-6-alkyl; R 4b denotes C(O)NH 2, C(O)OH, C(O)NH-C 1- 6-alkyl, C(O)N-(C 1. 6-alkyl) 2, SO 2-C 1-6-alkyl, oxo group, and where the ring is at least partially saturated, NH 2, NH-C 1-6-alkyl, N-(C 1-6-alkyl) 2; R 5 denotes a 6-member heteroaryl containing N as a heteroatom; R 3 denotes -(CR 8R 9) n-T; R 8 and R 9 are independently selected from the following groups: H and C 1-6-alkyl; n equals 1, 2, 3, 4, 5 or 6; T denotes ![]() or NR 12R 13; R 10 denotes H, NH 2, OH, C 1-6-alkyl, possibly substituted with one OH, a halogen atom, NH(C 1-6-alkyl) or N(C 1-6-alkyl) 2; q equals 1 or 2; Y denotes CH 2, NR 11 or O; R 11 denotes H, or C 1-6-alkyl; R 12 and R 13 are independently selected from the following groups: H, C 1-6-alkyl, C 1-6-alkynyl, (CH 2) 0- 2-C 3-7-cycloalkyl, and C 1-6-alkylene-O- C 1-6-alkyl, where C 1-6-alkyl is possibly substituted with one halogen; R 14 denotes a halogen atom, CN, C 1-6-alkyl, possibly substituted with 1-3 substitutes selected from halogen atom, OH, O- C 1-6-alkyl, O-C(O)C 1-6-alkyl, O- C 1-6-alkyl, possibly substituted with one substitute selected from OH, O- C 1-6-alkyl, and O-C(O) C 1-6-alkyl, or OH. The invention also relates to a pharmaceutical composition based on the compound of formula (I).
Beta-lactamase inhibitors / 2445314
Present application describes substituted bicyclic beta-lactams of formula I: ![]() which are class A and class C β-lactamase inhibitors wherein X, R 1 and R 2 are specified in the application, as well as a method for producing them. The compounds of formula I and their pharmaceutically acceptable salts are applicable for preparing a pharmaceutical composition and for producing a drug. The declared compounds are applicable for treating bacterial infections, optionally in a combination with a β-lactam antibiotic. Particularly, the compounds may be used with such β-lactam antibiotics, as e.g. imipenem, piperacillin or ceftazidime to control microorganisms resistant to β -lactam antibiotics due to the presence of β-lactamases.
Phosphoinositide-3-kinase inhibitors and pharmaceutical compositions containing said inhibitors / 2437888
Invention relates to compounds of formulae ![]() and ![]() including their stereoisomers, as well as pharmaceutically acceptable salt, where X denotes O or S; R 1 is selected from H, F, CI, Br, I, CN, -CR 14R 15-NR 16R 17, -CR 14R 15-NHR 10, -(CR 14R 15)NR 10R 11, -(CR 14R 15) nNR 12C(=Y)R 10, -(CR 14R 15) nNR 12S(O) 2R 10, -(CR 14R 15) mOR 10, -(CR 14R 15) nS(O) 2R 10, -C(OR 10)R 11R 14, -C(R 14)=CR 18R 19, -C(=Y)OR 10, -C(=Y)NR 10R 11, -C(=Y)NR 12OR 10, -C(=O)NR 12S(O) 2R 10, -C(=O)NR 12(CR 14R 15) mNR 10R 11, -NHR 12, -NR 12C(=Y)R 10, -S(O) 2R 10, -S(O) 2NR 10R 11, C 2-C 12 alkyl, C 2-C 8 alkenyl, C 2-C 8 alkynyl, C 3-C 4 carbocyclyl, piperidinyl, thiopyranyl, phenyl or C 5-C 6 heteroaryl; R 2 is selected from H, C 2-C 12 alkyl and thiazolyl; R 3 denotes a condensed bicyclic heteroaryl selected from indazole, indole, benzoimidazole, pyrrolopyridine, imidazopyridine and quinoline; R 10, R 11 and R 12 independently denote H, C 2-C 12 alkyl, C 3 carbocyclyl, heterocyclyl selected from pyrrolidine, morpholine and piperazine, phenyl or heteroaryl selected from pyrazole, pyridine, benzothiophene; or R 10 and R 11 together with a nitrogen atom with which they are bonded possibly form a saturated C 3-C 6 heterocyclic ring, possibly containing one additional ring atom selected from N or O, where said heterocyclic ring is possibly substituted with one or more groups independently selected from oxo, (CH 2) mOR 10, NR 10R 11, SO 2R 10, C(=O)R 10, NR 12S(O)R 11, C(=Y)NR 10R 11, C 1-C 12 alkyl and heterocyclyl selected from pyrrolidine; R 14 and R 15 are independently selected from H or C 1-C 12 alkyl; R 16 and R 17 independently denote H or phenyl; R 18 and R 19 together with a carbon atom with which they are bonded form a C 3-C 20 heterocyclic ring, where said alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, phenyl, heteroaryl, piperidinyl and condensed bicyclic heteroaryl possibly substituted with one or more groups independently selected from F, CI, Br, I, CF 3, -C(=Y)R 10, -C(=Y)OR 10, oxo, R 10, -C(=Y)NR 10R 11, -(CR 14R 15) nNR 10R 11, -NR 10R 11, -NR 12C(=Y)R 10, -NR 12C(=Y)NR 10R 11, -NR 12SO 2R 10, OR 10, SR 10, -S(O) 2R 10, -S(O) 2NR 10R 11, possibly substituted with carbocyclyl, selected from cyclopropyl, possibly substituted heterocyclyl selected from piperazine, possibly substituted with alkyl and alkylsulphonyl, pyrrolidine, morpholine, piperdine, possibly substituted CH 3, phenyl and possibly substituted heteroaryl selected from imidazole and triazole; Y denotes O; m equals 0, 1 or 2; n equals 1 and t equals 2. The invention also relates to a pharmaceutical composition which modulates lipid kinase activity, based on said compounds.
Novel compounds and use thereof / 2437887
Invention relates to compounds of formula ![]() where R 1 is selected from H, F, CI, Br, CF 3, C 1-C 6 alkoxy and OH; R 2 is selected from H and C 1-C 6 alkyl; n equals 1-5; m equals 0 or 1; and Y is selected from CH 2, NR 3, (NR 3R 4) +X -, O and S; R 3 and R 4 are independently selected from H and C 1-C 4 alkyl; and X - is selected from pharmaceutically acceptable anions. The invention also relates to a method of producing said compound and to an antiviral pharmaceutical composition based on said compound of formula (I).
Novel heterocyclic compound or salt thereof and intermediate compound thereof / 2434868
Described is a compound of general formula: ![]() [1], where R 1 denotes an optionally substituted C 2-C 12 alkyl, aryl or heterocyclic group which can be a mono- or bicyclic 5-11-member radical, where the heteroatoms can be nitrogen, oxygen or sulphur; X 1 denotes C 2-C 4 an alkylene group; X 2 denotes a bond; X 3 denotes a group of general formula NR 3 or CR 4R 5NR 3 (where R 3 denotes a hydrogen atom, optionally substituted lower alkyl group or imino-protective group) and R 4 and R 5 are identical or different, and each denotes a hydrogen atom or a lower alkyl group or bond; X 4 denotes a lower alkylene or lower alkenylene or lower alkynylene group, which can be substituted with one or more oxo groups or a bond; X 5 denotes a sulphur atom or bond; Y 1 denotes an optionally substituted divalent 4-, 5- or 6-member alicyclic hydrocarbon residue or an optionally subsituted divalent 5- or 6-member alicyclic amine residue, where the heteroatoms can be nitrogen or oxygen; Z 1, Z 2, Z 3, Z 4, Z 5 and Z 6 are identical or different, and each denotes a nitrogen atom or a group of general formula CR 7 (where R 7 denotes a hydrogen atom, a halogen atom, a hydroxyl group, a cyano group, an optionally substituted amino group, or an amino group substituted with one or more C 1-6 alkyl groups, a lower alkyl group, a cycloalkyl, a lower alkoxy group or a monocyclic 5-member heterocyclic group which can be substituted with one or more halogen atoms, where the heteroatoms can be nitrogen, acid or sulphur or a group of general formula Q 1CO 2R 10 (where R 10 denotes a carboxyl-protective group and Q 1 denotes a lower alkenylene group), provided that at least one of Z 3, Z 4, Z 5 and Z 6 denotes a nitrogen atom, or salt thereof. The invention also describes an antimicrobial agent based on said compound.
Method of producing diamine derivative / 2464271
Method is realised by mixing a compound of formula (B) with p-toluenesulphonic acid or a monohydrate of toluenesulphonic acid in less than 1 molar equivalent with respect to the compound of formula (B), in a solvent while heating. An additional amount of p-toluenesulphonic acid or monohydrate of p-toluenesulphonic acid is then added to the mixed solution while cooling in such an amount that their total molar equivalent with p-toluenesulphonic acid or monohydrate of p-toluenesulphonic acid at the mixing step is equal to 1 molar equivalent or more with respect to the compound of formula (B). At the last step, the obtained solution is crystallised to separate a compound of formula ![]() (A).
Pyrrolo- and thiazolopyridine compounds (versions) and based pharmaceutical composition / 2461557
Invention describes the pyrrolo- and thiazolopyridinium compounds and their pharmaceutically acceptable salts covered by general structural formula I: ![]() wherein the values A, B, R 1, R 2, R 3, R 4, R 5, R 6, R 7 and R 8 are those as presented in cl.1, and a pharmaceutical composition based on the given compound for inhibition of hypoxia-inducible factor (HIF) hydroxylase activity.
Glucokinase activators / 2457207
Invention relates to compounds of formula I ![]() , and pharmaceutically acceptable salts thereof, where L denotes O, S, or CH 2; Y denotes N or CH; Z denotes CR 3; G denotes CH; R 1 denotes a heteroaryl ring of formula ![]() , where D 1 denotes S, O; D 2 denotes N or CR 12; D 3 denotes CR 12; R 2 denotes (C 6-C 10)-aryl; 5-9-member mono- or bicyclic heteroaryl with 1 or 2 heteroatoms independently selected from N or S; a saturated or partially saturated (C 3-C 7)-cycloalkyl; or a saturated 5-6-member heteocyclyl with 1 heteroatom selected from N, where said aryl, heteroaryl, cycloalkyl and heterocyclyl are optionally substituted with one or two groups independently selected from (C 1-C 6)-alkyl, F, Cl, Br, CF 3, CN, NO 2, OR 6, C(-O)R 6, C(=O)OR 6, C(=O)NR 6R 7, saturated 6-member heterocyclyl with 2 heteroatoms independently selected from N or O, and S(O) 2R 6, and where said alkyl is optionally substituted with one -OR 8 group; R 3 denotes H; (C 1-C 6)-alkyl; (C 2-C 6)-alkenyl; Cl; Br; OR 6; SR 6; phenyl; or a 6-member heteroaryl with 1 heteroatom selected from N, where said alkyl and alkenyl are optionally substituted with one group selected from C(=O)OR 8, -OR 8, -NR 8R 9; or a saturated 6-member heterocyclyl with 1 heteroatom selected from N or O.
Benzotriazole uv-absorbers, having absorption spectrum shifted towards long-wave side, and use thereof / 2455305
Described are novel benzotriazole UV-absorbers, having absorption spectrum shifted towards the long-wave side with considerable absorption in the region up to 410-420 nm, having general formulae (a)-(k) (structural formula and values of radicals are given in the description), composition which is stabilised with respect to UV radiation and containing novel UV-absorbers, and use of the novel compounds as UV light stabilisers for organic materials.
Hiv-inhibiting 5-(hydroxymethylene- and aminomethylene)substituted pyrimidines / 2452737
Invention relates to novel substituted pyrimidine derivatives, having HIV replication inhibiting properties, or pharmaceutically acceptable salts thereof. In formula (1): ![]() R 1 denotes hydrogen; R 2 and R 3 independently denote hydrogen; R 7 and R 8 denote C 1-6alkyl; R 4 denotes cyano; R 9 denotes C 1-6alkyl optionally substituted with cyano, C 2-6alkenyl substituted with cyano, C 2-6alkynyl optionally substituted with cyano; R 5 denotes C 1-6alkyl optionally substituted with Ar or Het; C 2-6alkenyl optionally substituted with Ar or Het; C 2-6alkynyl optionally substituted with Ar or Het; C 3-7cycloalkyl; Ar; Het; R 6 denotes H, Het; Y denotes -OR 11, -NR 12R 13; R 11 denotes hydrogen or C 1-6alkyl optionally substituted with hydroxy, C 1-6alkoxy or pyridyl; R 12 denotes hydrogen or C 1-6alkyl; R 13 denotes hydrogen or C 1-6alkyl; or R 12 and R 13 together with a nitrogen atom, which is substituted by said two substitutes, form a morpholinyl; imidazolyl; X denotes -NR 1-; Het denotes 5- or 6-member completely saturated ring, where one or two ring members are heteroatoms, each independently selected from nitrogen and sulphur, and where the rest of the ring members are carbon atoms; and where any member of the heterocycle with a nitrogen heteroatom can optionally be substituted with C 1-6alkyl; where the 5- or 6-member ring can optionally be annelated with a benzene or thiophene ring; each aryl independently denotes phenyl or phenyl substituted with one substitute selected from C 1-6alkoxy.
3,7-dithia-1,5-diazabicyclo[3,3,0]octane - fungicidally active agent / 2448971
Invention relates to novel agents for controlling plant fungal diseases, specifically 3,7-dithia-1,5-diazabicyclo[3,3,0]octane ![]() as an agent against Bipolaris sorokiniana, Aspergillus fumigates, Aspergillus niger, synthesis of which takes place in a single step using readily available reactants in contrast to multi-step synthesis of existing agents used for controlling fungal diseases of plants and materials.
Novel heteroaryl-substituted benzothiazoles / 2448106
Invention relates to a novel heteroaryl-substituted derivative of benzothiazole - 2-[6-(methylamino)pyridin-3-yl]-1,3-benzothiazol-6-ol ![]() where one or more atoms may be a detectable isotope, in form of a free base or pharmaceutically acceptable salt thereof, capable of binding with amyloid deposits, to pharmaceutical compositions based on the radioactive-labelled disclosed compound, to use of the detectable isotope-labelled disclosed compound for determining amyloid deposits, as well as use of the disclosed compound in producing a medicinal agent for preventing and/or treating Alzheimer's disease and familial Alzheimer's disease. The present invention also relates to a novel intermediate compound for producing the disclosed heteroaryl-substituted benzothiazole derivative ![]()
Production and use of substituted dihydro- and tetrahydrooxazolo-pyrimidinones / 2470937
Invention relates to novel 2-substituted-2,3-dihydrooxazolo[3,2-a]pyrimidin-7-ones and 2-substituted-2,3,5,6-tetrahydrooxazolo[3,2-a]pyrimidin-7-ones of formula (I): ![]() where p, n, X, Y, R 1, R 2, R 3, R 4, R 5, R 6, R 7 and R 8 are described in the description. These compounds are modulators of metabotropic glutamate receptors (mGluR), particularly the mGluR2 receptor. Compounds in the present invention are therefore suitable for use as pharmaceutical agents, especially in treating and(or) preventing various disorders of the central nervous system (CNS), including, among others, acute and chronic neurodegenerative disorders, psychosis, convulsions, anxiety, depression, migraine, pain, sleep disorder and emesis.
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FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to new antibacterial compounds of formula I
wherein R1 represents halogen or alkoxy group; each U and W represents N; V represents CH, and R2 represents H or F, or each U and V represents CH; W represents N, and R2 represents H or F, or U represents N; V represents CH; W represents CH or CRa, and R2 represents H, or also when W represents CH, may represent F; Ra represents CH2OH or alkoxycarbonyl; A represents group CH=CH-B, a binuclear heterocyclic system D, phenyl group which is mono-substituted in the position 4 by C1-4 alkyl group, or phenyl group which is di-substituted in positions 3 and 4 wherein each of two substitutes is optionally specified in a group consisting of C1-4 alkyl and halogen; B represents mono- or di-substituted phenyl group wherein each substitute is a halogen atom; D represents group ![]()
wherein Z represents CH or N, and Q represents O or S; or to salts of such compounds.
EFFECT: compounds are used for treating bacterial infections.
13 cl, 2 tbl, 25 ex
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1. The compound of the formula I

where R1represents a halogen or alkoxygroup;
U and W each represent N, V represents CH and R2represents H or F, or
U and V each represent CH, W pre is is a N and R 2represents H or F, or
U represents N, V represents CH, W represents CH or CRaand R2represents H or, when W represents CH, can represent F;
Rarepresents CH2HE or alkoxycarbonyl;
And represents the group CH=CH -, binuclear heterocyclic system D, a phenyl group which is mono-substituted in position 4
With1-4alkyl group, or phenyl group which is di-substituted in positions 3 and 4, where each of the two substituents independently from each other selected from the group including1-4alkyl and halogen;
Represents a mono - or di-substituted phenyl group, where
each Deputy is a halogen atom;
D is a group of
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where Z represents CH or N, and
Q represents O or S;
or a salt of such compounds.
2. The compound of formula I according to claim 1, where, if U represents N and V represents CH, then W represents CRaand R2represents H;
or a salt of such compounds.
3. The compound of formula I according to claim 1, which is also a compound of the formula ICE

where R1represents a halogen or1-4alkoxygroup;
U and W each is th is a N, V represents CH and R2represents H or F, or
U and V each represent CH, W represents N and R2represents H or F, or
U represents N, V represents CH, W represents CH or CRaand R2represents H or, when W represents CH, can represent F;
Rarepresents CH2HE or C1-4alkoxycarbonyl;
And represents the group CH=CH -, binuclear heterocyclic system D, a phenyl group which is mono-substituted in position 4
C1-4alkyl group, or phenyl group which is disubstituted in positions 3 and 4, where each of the two substituents independently from each other selected from the group including1-4alkyl and halogen;
Represents a di-substituted phenyl group, in which each Deputy is a fluorine atom;
D is a group of
,
where Z represents CH or N, and
Q represents O or S;
or a salt of such compounds.
4. The compound of formula I according to claim 3, where, if U represents N and V represents CH, then W represents CRaand R2represents H;
or a salt of such compounds.
5. The compound of formula I according to claim 1, where R1represents a C1-4/sub> alkoxygroup;
or a salt of such compounds.
6. The compound of formula I according to claim 1, where a represents the group CH=CH -;
or a salt of such compounds.
7. The compound of formula I according to claim 1, where a represents a binuclear heterocyclic system D;
or a salt of such compounds.
8. The compound of formula I according to claim 1, where a represents a phenyl group which is mono-substituted in position 4 With1-4alkyl group, or phenyl group which is disubstituted in positions 3 and 4, where each of the two substituents independently from each other selected from the group including1-4alkyl and halogen;
or a salt of such compounds.
9. The compound of formula I according to claim 1, which is selected from the following compounds:
{(3R,6S)-6-[(1R)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-yl}-[3-(E)-(2,5-differenl)allyl]amine;
{(3R,6S)-6-[(1S)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-yl}-[3-(E)-(2,5-differenl)allyl]amine;
{(3R,6S)-6-[(1R)-1-amino-2-(6-ftorhinolon-4-yl)ethyl]tetrahydropyran-3-yl}-[(E)-3-(2,5-differenl)allyl]amine;
{(3R,6S)-6-[(1S)-1-amino-2-(6-ftorhinolon-4-yl)ethyl]tetrahydropyran-3-yl}-[(E)-3-(2,5-differenl)allyl]amine;
6-({(3R,6S)-6-[(1R)-1-amino-2-(6-methoxyquinoline-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]thiazin-3-one;
6-({(3R,6S)-6-[(1S)-1-amino-2-(6-methoxyquinoline-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4 is-pyrido[3,2-b][1,4]thiazin-3-one;
{(3R,6S)-6-[(1R)-1-amino-2-(6-methoxyquinoline-4-yl)ethyl]tetrahydropyran-3-yl}-[3-(E)-(2,5-differenl)allyl]amine;
{(3R,6S)-6-[(1S)-1-amino-2-(6-methoxyquinoline-4-yl)ethyl]tetrahydropyran-3-yl}-[3-(E)-(2,5-differenl)allyl]amine;
6-({(3R,6S)-6-[(1R)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]thiazin-3-one;
6-({(3R,6S)-6-[(1S)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]thiazin-3-one;
6-({(3R,6S)-6-[(1R)-l-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]oxazin-3-one;
6-({(3R,6S)-6-[(1S)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]oxazin-3-one;
methyl ester of 8-[(2R)-2-amino-2-{5-[(E)-3-(2,5-differenl)allylamino]tetrahydropyran-2-yl}ethyl]-2-methoxyaniline-5-carboxylic acid;
methyl ester of 8-[(2S)-2-amino-2-{5-[(E)-3-(2,5-differenl)allylamino]tetrahydropyran-2-yl}ethyl]-2-methoxyaniline-5-carboxylic acid;
8-((S)-2-amino-2-{(2S,5R)-5-[(E)-3-(2,5-differenl)allylamino]tetrahydropyran-2-yl}ethyl)-2-methoxyaniline-5-yl] methanol;
[8-((R)-2-amino-2-{(2S,5R)-5-[(E)-3-(2,5-differenl)allylamino]tetrahydropyran-2-yl}ethyl)-2-methoxyaniline-5-yl]methanol;
6-({(3R,6S)-6-[(1R)-1-amino-2-(3-fluoro-6-methoxyquinoline-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]thiazin-3-one;
6-({(3R,6S)-6-[(1S)-1-amino-2-(3-fluoro-6-methoxyquinoline-4-yl)ethyl]tetrahydropyran-3-the laminitis}methyl)-4H-pyrido[3,2-b][1,4]thiazin-3-one;
6-({(3R,6S)-6-[(1R)-1-amino-2-(3-fluoro-6-methoxyquinoline-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4-pyrido[3,2-b][1,4]oxazin-3-one;
6-({(3R,6S)-6-[(1S)-1-amino-2-(3-fluoro-6-methoxyquinoline-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]oxazin-3-one;
6-({(3R,6S)-6-[(1R)-1-amino-2-(3-fluoro-6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]thiazin-3-one;
6-({(3R,6S)-6-[(1S)-1-amino-2-(3-fluoro-6-methoxy[l,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]thiazin-3-one;
6-({(3R,6S)-6-[(1S)-1-amino-2-(3-fluoro-6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]oxazin-3-one;
6-({(3R,6S)-6-[(1S)-1-amino-2-(3-fluoro-6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]oxazin-3-one;
{(3R,6S)-6-[(1S)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-yl}-(4-active compounds)amine;
{(3R,6S)-6-[(1S)-1-amino-2-(6-methoxyquinoline-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-benzo[1,4]oxazin-3-one;
6-({(3R,6S)-6-[(1S)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]oxazin-3-one;
6-({(3R,6S)-6-[(1S)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-yl}-(3-fluoro-4-methylbenzyl)amine;
{(3R,6S)-6-[(1S)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-benzo[1,4]oxazin-3-one;
6-({(3S,6R)-6-[(1R)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}IU who yl)-4H-pyrido[3,2-b][1,4]thiazin-3-one;
6-({(3S,6R)-6-[(1S)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]thiazin-3-one;
6-({(3S,6R)-6-[(1R)-1-amino-2-(7-fluoro-2-methoxyquinoline-8-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]oxazin-3-one;
6-({(3R,6S)-6-[(1S)-1-amino-2-(7-fluoro-2-methoxyquinoline-8-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]oxazin-3-one;
6-({(3R,6S)-6-[(1R)-1-amino-2-(7-fluoro-2-methoxyquinoline-8-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]thiazin-3-one;
6-({(3R,6S)-6-[(1S)-1-amino-2-(7-fluoro-2-methoxyquinoline-8-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]thiazin-3-one;
6-({(3R,6S)-6-[(1R)-1-amino-2-(3-fluoro-6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-benzo[1,4]oxazin-3-one;
6-({(3R,6S)-6-[(1S)-1-amino-2-(3-fluoro-6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-benzo[1,4]oxazin-3-one;
or a salt of such compounds.
10. The connection according to claim 9, which is selected from the following compounds:
{(3R,6S)-6-[(1R)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-yl}-[3-(E)-(2,5-differenl)allyl]amine;
{(3R,6S)-6-[(1S)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-yl}-[3-(E)-(2,5-differenl)allyl]amine;
{(3R,6S)-6-[(1R)-1-amino-2-(6-ftorhinolon-4-yl)ethyl]tetrahydropyran-3-yl}-[(E)-3-(2,5-differenl)allyl]amine;
{(3R,6S)-6-[(1S)-1-amino-2-(6-ftorhinolon-4-yl)ethyl]tetrahydropyran-3-yl}-[(E)-3-(2,5-differenl)allyl]amine;
6-({(3R,6S)-6-(1R)-1-amino-2-(6-methoxyquinoline-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]thiazin-3-one;
6-({(3R,6S)-6-[(1S)-1-amino-2-(6-methoxyquinoline-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]thiazin-3-one;
{(3R,6S)-6-[(1R)-1-amino-2-(6-methoxyquinoline-4-yl)ethyl]tetrahydropyran-3-yl}-[3-(E)-(2,5-differenl)allyl]amine;
{(3R,6S)-6-[(1S)-1-amino-2-(6-methoxyquinoline-4-yl)ethyl]tetrahydropyran-3-yl}-[3-(E)-(2,5-differenl)allyl]amine;
6-({(3S,6R)-6-[(1R)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]thiazin-3-one;
6-({(3R,6S)-6-[(1S)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]thiazin-3-one;
6-({(3R,6S)-6-[(1R)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]oxazin-3-one;
6-({(3R,6S)-6-[(1S)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]oxazin-3-one;
methyl ester of 8-[(2R)-2-amino-2-{5-[(E)-3-(2,5-differenl)allylamino]tetrahydropyran-2-yl}ethyl]-2-methoxyaniline-5-carboxylic acid;
methyl ester of 8-[(2S)-2-amino-2-{5-[(E)-3-(2,5-differenl)allylamino]tetrahydropyran-2-yl}ethyl]-2-methoxyaniline-5-carboxylic acid;
8-((S)-2-amino-2-{(2S,5R)-5-[(E)-3-(2,5-differenl)allylamino]tetrahydropyran-2-yl}ethyl)-2-methoxyaniline-5-yl]methanol;
[8-((R)-2-amino-2-{(2S,5R)-5-[(E)-3-(2,5-differenl)allylamino]tetrahydropyran-2-yl}ethyl)-2-methoxyaniline-5-yl]methanol;
6-({(3R,6S)-6-[(1R)-1-amino-2-(3-fluoro-6-methoxyquinoline-4-yl)ethyl]tetrahydropyran-3-ylamine is}methyl)-4H-pyrido[3,2-b][1,4]thiazin-3-one;
6-({(3R,6S)-6-[(1S)-1-amino-2-(3-fluoro-6-methoxyquinoline-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]thiazin-3-one;
6-({(3R,6S)-6-[(1R)-1-amino-2-(3-fluoro-6-methoxyquinoline-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]oxazin-3-one;
6-({(3R,6S)-6-[(1S)-1-amino-2-(3-fluoro-6-methoxyquinoline-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]oxazin-3-one;
6-({(3R,6S)-6-[(1R)-1-amino-2-(3-fluoro-6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]thiazin-3-one;
6-({(3R,6S)-6-[(1S)-1-amino-2-(3-fluoro-6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]thiazin-3-one;
6-({(3R,6S)-6-[(1R)-1-amino-2-(3-fluoro-6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]oxazin-3-one;
6-({(3R,6S)-6-[(1S)-1-amino-2-(3-fluoro-6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]oxazin-3-one;
{(3R,6S)-6-[(1S)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-yl}-(4-active compounds)amine;
{(3R,6S)-6-[(1S)-1-amino-2-(6-methoxyquinoline-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-benzo[1,4]oxazin-3-one;
6-({(3R,6S)-6-[(1S)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]oxazin-3-one;
6-({(3S,6R)-6-[(1R)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-yl}-(3-fluoro-4-methylbenzyl)amine;
{(3R,6S)-6-[(1S)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-silts what about the}methyl)-4H-benzo[1,4]oxazin-3-one;
6-({(3S,6R)-6-[(1R)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]thiazin-3-one and
6-({(3S,6R)-6-[(1S)-1-amino-2-(6-methoxy[1,5]naphthiridine-4-yl)ethyl]tetrahydropyran-3-ylamino}methyl)-4H-pyrido[3,2-b][1,4]thiazin-3-one
or a salt of such compounds.
11. The compound of formula I according to one of claims 1 to 10 or its pharmaceutically acceptable salt as a medicine for the prevention or treatment of bacterial infections.
12. The use of the compounds of formula I according to one of claims 1 to 10 or its pharmaceutically acceptable salt to obtain drugs for prevention or treatment of bacterial infections.
13. The compound of formula I according to one of claims 1 to 10 or its pharmaceutically acceptable salt for the prevention or treatment of bacterial infections.
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