Oxazolidinones Bearing Antimicrobial Activity Composition and Methods of Preparation
First Claim
Patent Images
1. An oxazolidinone compound of Formula I. wherein Q is X and Y may be same or different, represent, CH, CF, N;
- X′ and
Y′
may be same or different, represent, CH, CF, N, C—
OCH3, C—
CH2—
Ra;
wherein Ra is hydrogen, amino, halogen, hydroxyl, azido, carboxamido, NHCH2CONH2, N(CH2CONH2)2;
R2 and R2′
may be same or different, represent, hydrogen, methyl, hydroxyl, C1-C6 alkoxy or halogen;
R4 is selected from the group comprisinga) O—
R1,b) NRbRc;
wherein Rb is selected from hydrogen, C1-C6 alkylcarbonyl;
Rc is selected from hydrogen, C(O)OCH2OC(O)Rd or CH(CH3)OC(O)Re;
wherein Rd is hydrogen, C1-C6 alkyl, substituted C1-C6 alkyl with substitutents selected from amino or C1-C6 alkylamidoRe is selected from hydrogen, C1-C6 alkyl, substituted C1-C6 alkyl;
c) formamide;
d) carbamate;
e) thiocarbamate;
f) urea;
g) C1-C6 alkylamido;
h) C1-C6 haloalkylamido;
i) C1-C6 thioalkylamido;
j) substituted C1-C6 thioalkylamido, wherein the alkyl group is substituted with halo;
k) unsubstituted or substituted heteroaryl, wherein substituents of the heteroaryl to are selected from the group comprising C1-C6 alkyl, nitro, cyano, hydroxyl, halo, amino, C1-C6 alkylcarbonyl, C1-C6 alkoxycarbonyl, carboxy;
wherein R1 is selected from the group comprising hydrogen, C1-C6 alkylsulfonyl, C1-C6-alkylcarbonyl, —
P(O)(OM)2, wherein M is hydrogen, methyl, ethyl, t-butyl, phenyl or an alkali metal ion such as Li, Na, K;
or R1 is an amino acid residue derived from one of the 20 naturally occurring amino acids viz. alanine, arginine, asparagine, aspartic acid, cysteine, glutamine, glutamic acid, glycine, histidine, isoleucine, leucine, lysine, methionine, phenylalanine, proline, serine, threonine, tryptophan, tyrosine and valine, attached to the oxygen via carbonyl of the amino acid to form a ester linkage;
When Q is wherein n is 0, 1 or 2;
W represents 3-7 membered heterocyclyl bearing one or more heteroatom selected from N;
O, S, optionally substituted with one or more substitutents selected from the group comprising C1-C6 alkyl, C1-C6 alkylcarbonyl, C1-C6 alkoxycarbonyl, carboxamide, cyano, hydroxyl, amino, heterocyclyl, substituted heterocyclyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl or heteroaryl bearing one or more heteroatom selected from N, O S, optionally substituted with one or more substitutents selected from the group comprisingi. substituted or unsubstituted C1-C6 alkyl with substituents selected from the group hydroxyl, halo, nitro, cyano, aryl or heteroaryl;
ii. substituted or unsubstituted C2-C6 alkenyl with substituents selected from the group hydroxyl, halo, nitro, cyano, aryl or heteroaryl;
iii. C1-C6 alkylcarbonyl;
iv. C1-C6 alkoxycarbonyl;
v. C1-C6 alkoxycarbonylalkyl;
vi. C1-C6 alkylcarbonylalkyl;
vii. C1-C6 haloalkyl;
viii formyl;
ix. carboxy;
x. carboxamide;
xi. cyano;
xii. amino;
xiii nitro;
xiv. hydroxyl;
xv halo;
xvi. morpholinocarbonylalkyl;
xvii. hydroxyiminoalkyl;
xviii. alkylcarbonylaminoalkyl;
xix. alkoxyiminoalkyl;
xx. aralkyloxyiminoalkyl;
xxi. hydroiminoaminoalkyl;
xxii. aryl, substituted aryl, with substituents selected from C1-C6 alkyl, nitro, cyano, hydroxyl, halo, amino, heterocyclyl;
xxiii. substituted or unsubstituted heteroaryl, with substituents selected from C1-C6 alkyl, nitro, cyano, hydroxyl, halo, amino, heterocyclyl;
xxiv. substituted or unsubstituted heterocyclyl, with substituents selected from C1-C6 alkyl, C1-C6 alkylcarbonyl, aralkyl, nitro, cyano, hydroxyl, halo, amino;
xxv. C1-C6 alkylthio;
xxvi. C1-C6 alkylsulfanylalkyl;
xxvii. C1-C6 aralkylsulfanyl;
xxviii. C1-C6 alkylsulfonylmethyl;
xxix. C1-C6 alkylsulfonyloxy;
xxxi. —
(C1-C6 alkyl)-NRf—
(C1-C6 alkyl)-NRbRc;
wherein Rf is hydrogen, C1-C6 alkyl, substituted C1-C6 alkyl with substitutents selected from amino or C1-C6 alkylamido;
or W is heteroaryloxy group optionally substituted with one or more substitutents such as C1-C6 alkyl, C2-C6 alkenyl, C1-C6 alkylcarbonyl, C1-C6 alkoxycarbonyl, formyl, carboxy, carboxamide, cyano, amino, hydroxyiminoalkyl, alkoxyiminoalkyl, aralkyloxyiminoalkyl, hydroxyiminoaminoalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclyl, substituted heterocyclyl;
OR when Q is X′ and
Y′
are as defined above;
T is hydrogen or wherein R2 and R2′
are as defined above;
“
a”
is optional double bond;
R3 and R3′
may be same or different, represent, hydrogen, methyl, hydroxyl, C1-C6 alkoxy or halogen;
with the proviso that when T is hydrogen, R4 is not acetamido;
Z represents group selected from CH, NH, O, S, CH2, C(R6)R6′
, C═
O, NR7, C═
C(R8)R8′
, SO, SO2, S—
NH, S═
NC(O)CH3, S═
NC(O)NHCH3, S(O)═
NH, S(O)═
NCH3, S(O)NC(O)CH3, S(O)═
NC(O)NHCH3, S(O)═
NC(O)NHCH2CH2Cl, with proviso that when X is CH, Y is CF, one of X′
or Y′
or both X′
, Y′
are N, then Z is not NH. wherein R6 and R6′
may be same or different, represent, hydrogen, hydroxyl, amino, azido, C1-C6 alkoxy, C1-C6 alkylcarbonyloxy, C1-C6 alkylsulfonyloxy, heterocyclyl, substituted heterocyclyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, C1-C6 alkyl optionally substituted with one or more substituent selected from the group comprising azido, cyano, carboxamido, hydroxyl, C1-C6 alkyloxy, C1-C6 alkylcarbonyloxy, C1-C6 alkylcarbonyl or C2-C6 alkenyl optionally substituted with one or more azido, cyano, carboxamido or hydroxyl;
or R6 and R6′
are combined together to provide 3-7 member heterocyclyl bearing one or more heteroatom selected from N, O, S optionally substituted with substituent selected from group comprising C1-C6 alkyl, C2-C6 alkenyl, C1-C6 alkylcarbonyl, C1-C6 alkoxycarbonyl, formyl, carboxy, carboxamide, cyano, amino, hydroxyiminoalkyl, alkoxyiminoalkyl, aralkyloxyiminoalkyl, hydroxyiminoaminoalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclyl, substituted heterocyclyl;
R7 represents hydrogen, cyano, aralkyl, CO—
OCH2Ph, C1-C6-alkylcarbonyl, C1-C6 alkyl optionally substituted with one or more azido, cyano, heteroaryl, substituted heteroaryl, carboxamido or hydroxyl;
R8, R8′
may be same or different, represent, hydrogen, C1-C6 alkyl, C2-C6 alkenyl, cyano, amino, C1-C6 alkylcarbonyl, C1-C6 alkoxycarbonyl, cyano, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclyl, substituted heterocyclyl;
and isomers, polymorphs, N-oxides thereof or pharmaceutical acceptable salts thereof.
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Abstract
The present invention concerns recombinant DNA'"'"'s comprising cDNA of genomic RNA of a Salmonidae alphavirus preceded by a spacer sequence, under the control of a suitable promoter. Said recombinant DNA'"'"'s are useful for obtaining expression vectors, producing recombinant Salmonidae alphavirus, and for obtaining vaccines.
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Citations
48 Claims
-
1. An oxazolidinone compound of Formula I.
wherein Q is X and Y may be same or different, represent, CH, CF, N; -
X′ and
Y′
may be same or different, represent,CH, CF, N, C—
OCH3, C—
CH2—
Ra;
wherein Ra is hydrogen, amino, halogen, hydroxyl, azido, carboxamido, NHCH2CONH2, N(CH2CONH2)2;R2 and R2′
may be same or different, represent, hydrogen, methyl, hydroxyl, C1-C6 alkoxy or halogen;R4 is selected from the group comprising a) O—
R1,b) NRbRc; wherein Rb is selected from hydrogen, C1-C6 alkylcarbonyl; Rc is selected from hydrogen, C(O)OCH2OC(O)Rd or CH(CH3)OC(O)Re; wherein Rd is hydrogen, C1-C6 alkyl, substituted C1-C6 alkyl with substitutents selected from amino or C1-C6 alkylamido Re is selected from hydrogen, C1-C6 alkyl, substituted C1-C6 alkyl; c) formamide; d) carbamate; e) thiocarbamate; f) urea; g) C1-C6 alkylamido; h) C1-C6 haloalkylamido; i) C1-C6 thioalkylamido; j) substituted C1-C6 thioalkylamido, wherein the alkyl group is substituted with halo; k) unsubstituted or substituted heteroaryl, wherein substituents of the heteroaryl to are selected from the group comprising C1-C6 alkyl, nitro, cyano, hydroxyl, halo, amino, C1-C6 alkylcarbonyl, C1-C6 alkoxycarbonyl, carboxy; wherein R1 is selected from the group comprising hydrogen, C1-C6 alkylsulfonyl, C1-C6-alkylcarbonyl, —
P(O)(OM)2, wherein M is hydrogen, methyl, ethyl, t-butyl, phenyl or an alkali metal ion such as Li, Na, K;or R1 is an amino acid residue derived from one of the 20 naturally occurring amino acids viz. alanine, arginine, asparagine, aspartic acid, cysteine, glutamine, glutamic acid, glycine, histidine, isoleucine, leucine, lysine, methionine, phenylalanine, proline, serine, threonine, tryptophan, tyrosine and valine, attached to the oxygen via carbonyl of the amino acid to form a ester linkage; When Q is wherein n is 0, 1 or 2; W represents 3-7 membered heterocyclyl bearing one or more heteroatom selected from N;
O, S, optionally substituted with one or more substitutents selected from the group comprising C1-C6 alkyl, C1-C6 alkylcarbonyl, C1-C6 alkoxycarbonyl, carboxamide, cyano, hydroxyl, amino, heterocyclyl, substituted heterocyclyl, aryl, substituted aryl, heteroaryl, substituted heteroarylor heteroaryl bearing one or more heteroatom selected from N, O S, optionally substituted with one or more substitutents selected from the group comprising i. substituted or unsubstituted C1-C6 alkyl with substituents selected from the group hydroxyl, halo, nitro, cyano, aryl or heteroaryl; ii. substituted or unsubstituted C2-C6 alkenyl with substituents selected from the group hydroxyl, halo, nitro, cyano, aryl or heteroaryl; iii. C1-C6 alkylcarbonyl; iv. C1-C6 alkoxycarbonyl; v. C1-C6 alkoxycarbonylalkyl; vi. C1-C6 alkylcarbonylalkyl; vii. C1-C6 haloalkyl; viii formyl; ix. carboxy; x. carboxamide; xi. cyano; xii. amino; xiii nitro; xiv. hydroxyl; xv halo; xvi. morpholinocarbonylalkyl; xvii. hydroxyiminoalkyl; xviii. alkylcarbonylaminoalkyl; xix. alkoxyiminoalkyl; xx. aralkyloxyiminoalkyl; xxi. hydroiminoaminoalkyl; xxii. aryl, substituted aryl, with substituents selected from C1-C6 alkyl, nitro, cyano, hydroxyl, halo, amino, heterocyclyl; xxiii. substituted or unsubstituted heteroaryl, with substituents selected from C1-C6 alkyl, nitro, cyano, hydroxyl, halo, amino, heterocyclyl; xxiv. substituted or unsubstituted heterocyclyl, with substituents selected from C1-C6 alkyl, C1-C6 alkylcarbonyl, aralkyl, nitro, cyano, hydroxyl, halo, amino; xxv. C1-C6 alkylthio; xxvi. C1-C6 alkylsulfanylalkyl; xxvii. C1-C6 aralkylsulfanyl; xxviii. C1-C6 alkylsulfonylmethyl; xxix. C1-C6 alkylsulfonyloxy; xxxi. —
(C1-C6 alkyl)-NRf—
(C1-C6 alkyl)-NRbRc;wherein Rf is hydrogen, C1-C6 alkyl, substituted C1-C6 alkyl with substitutents selected from amino or C1-C6 alkylamido; or W is heteroaryloxy group optionally substituted with one or more substitutents such as C1-C6 alkyl, C2-C6 alkenyl, C1-C6 alkylcarbonyl, C1-C6 alkoxycarbonyl, formyl, carboxy, carboxamide, cyano, amino, hydroxyiminoalkyl, alkoxyiminoalkyl, aralkyloxyiminoalkyl, hydroxyiminoaminoalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclyl, substituted heterocyclyl; OR when Q is X′ and
Y′
are as defined above;T is hydrogen or wherein R2 and R2′
are as defined above;“
a”
is optional double bond;R3 and R3′
may be same or different, represent, hydrogen, methyl, hydroxyl, C1-C6 alkoxy or halogen;with the proviso that when T is hydrogen, R4 is not acetamido; Z represents group selected from CH, NH, O, S, CH2, C(R6)R6′
, C═
O, NR7, C═
C(R8)R8′
, SO, SO2, S—
NH, S═
NC(O)CH3, S═
NC(O)NHCH3, S(O)═
NH, S(O)═
NCH3, S(O)NC(O)CH3, S(O)═
NC(O)NHCH3, S(O)═
NC(O)NHCH2CH2Cl,with proviso that when X is CH, Y is CF, one of X′
or Y′
or both X′
, Y′
are N, then Z is not NH.wherein R6 and R6′
may be same or different, represent, hydrogen, hydroxyl, amino, azido, C1-C6 alkoxy, C1-C6 alkylcarbonyloxy, C1-C6 alkylsulfonyloxy, heterocyclyl, substituted heterocyclyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, C1-C6 alkyl optionally substituted with one or more substituent selected from the group comprising azido, cyano, carboxamido, hydroxyl, C1-C6 alkyloxy, C1-C6 alkylcarbonyloxy, C1-C6 alkylcarbonyl orC2-C6 alkenyl optionally substituted with one or more azido, cyano, carboxamido or hydroxyl; or R6 and R6′
are combined together to provide 3-7 member heterocyclyl bearing one or more heteroatom selected from N, O, S optionally substituted with substituent selected from group comprising C1-C6 alkyl, C2-C6 alkenyl, C1-C6 alkylcarbonyl, C1-C6 alkoxycarbonyl, formyl, carboxy, carboxamide, cyano, amino, hydroxyiminoalkyl, alkoxyiminoalkyl, aralkyloxyiminoalkyl, hydroxyiminoaminoalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclyl, substituted heterocyclyl;R7 represents hydrogen, cyano, aralkyl, CO—
OCH2Ph, C1-C6-alkylcarbonyl, C1-C6 alkyl optionally substituted with one or more azido, cyano, heteroaryl, substituted heteroaryl, carboxamido or hydroxyl;R8, R8′
may be same or different, represent, hydrogen, C1-C6 alkyl, C2-C6 alkenyl, cyano, amino, C1-C6 alkylcarbonyl, C1-C6 alkoxycarbonyl, cyano, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclyl, substituted heterocyclyl;and isomers, polymorphs, N-oxides thereof or pharmaceutical acceptable salts thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 34, 38, 42, 46, 47, 48)
wherein n, R2, R2′
-
-
3. The compound of claim 2, wherein n is 0 or 1.
-
4. The compound of claim 2, wherein R2 and R2′
- are each independently hydrogen, methyl, hydroxyl, halogen.
-
5. The compound of claim 4, wherein halogen is F.
-
6. The compound of claim 2, wherein W is heteroaryl or substituted heteroaryl, wherein substituents are as defined in claim 1.
-
7. The compound of claim 6, wherein heteroaryl is [1,2,3]-triazol, [1,2,4]-triazol, pyrrol, pyrazol, tetrazol, imidazol, [1,3,4]-oxadiazol, [1,2,4]-thiadiazol, [1,3,4]-thiadiazol, oxazol, isoxazol, thiazol, benzotriazol.
-
8. The compound of claim 6, wherein heteroaryl is [1,2,3]-triazol, [1,2,4]-triazol, pyrazol, tetrazol, [1,2,4]-thiadiazol, [1,3,4]-thiadiazol.
-
9. The compound of claim 6, wherein heteroaryl is [1,2,3]-triazol, tetrazol.
-
10. The compound of claim 2, wherein n is 0 or 1;
-
R2, R2′
each and independently is hydrogen, hydroxyl, fluorine;W is [1,2,3]-triazol or tetrazol;
R4 is as defined in claim 1.
-
-
11. The compound of claim 6, wherein the substituents of the heteroaryl are selected from the group comprising methyl, cyano, amino, ethoxycarbonyl, fluoro, difluoromethyl, formyl, [1,3]-dioxolan, hydroxymethyl, hydroxyethyl, carboxamido, carboxy, acetyl, methyl-oxiranyl, (E/Z)-2-cyano-vinyl, hydroxyimino-methyl, 1-methoxyimino-ethyl, 1-methoxyimino-methyl, 1-benzyloxyimino-methyl, hydroxyiminoamino-methyl, 4-N,N-dimethylaminoethylaminomethyl, phenyl, 4-nitrophenyl, 4-pyridinyl, 3-pyridinyl, morpholin-4-yl, diethylamino, piperazin-1-yl, methylsulfanylmethyl, methylsulfonylmethyl, benzylsulfanyl, thiophen-2-yl-methyl, morpholinocarbonylmethyl, 4-methylpiperazin-1-yl, 4-acetyl-piperazin-1-yl, 4-cyanopiperazin-1-yl, 4-benzylpiperazin-1-yl, ethoxycarbonylmethyl, acetylaminomethyl.
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12. The compound of claim 6, wherein substituted heteroaryl is selected from the group comprising 3-ethoxycarbonyl-imidazol, fluoro-4-(1H-[1,2,3]-triazol, 4-difluoromethyl-1H-[1,2,3]-triazol, 4-formyl-1H-[1,2,3]-triazol, 4-[1,3]-dioxolan-2-yl-1H-[1,2,3]-triazol, 4-ethoxycarbonyl-1H-[1,2,3]-triazol, 4-hydroxymethyl-1H-[1,2,3]-triazol, 4-cyano-1H-[1,2,3]-triazol, 4-carboxamido-1H-[1,2,3]-triazol, 4-hydroxycarbonyl-1H-[1,2,3]-triazol, 4-acetyl-H-[1,2,3]-triazol, 4-(1-hydroxyethyl)-1H-[1,2,3]-triazol, 4-(methyl-oxiranyl)-1H-[1,2,3]-triazol, 4-(2-hydroxyethyl)-1H-[1,2,3]-triazol, 4-((E/Z)-2-cyano-vinyl)-1H-[1,2,3]-triazol, 4-(hydroxyimino-methyl)-1H-[1,2,3]-triazol, 4-(1-methoxyimino-ethyl)-1H-[1,2,3]-triazol, 4-(1-methoxyimino-methyl)-1H-[1,2,3]-triazol, 4-(1-benzyloxyimino-methyl)-1H-[1,2,3]-triazol, 4-(hydroxyiminoamino-methyl)-[1,2,3]-triazol, 4-benzotriazol, 4-N,N-dimethylaminoethylaminomethyl)-1H-[1,2,3]-triazol, 1-methyl-1H-tetrazol, 2-methyl-2H-tetrazol, 5-methyl-tetrazol, 5-phenyl-tetrazol, 5-(4-nitrophenyl)-tetrazol, 5-(4-pyridinyl)-tetrazol, 5-(3-pyridinyl)-tetrazol, 5-(morpholin-4-yl)-tetrazol, 5-amino-tetrazol, 5-(diethylamino)-tetrazol, 5-(piperazin-1-yl)-tetrazol, 5-methylsulfanylmethyl-tetrazol, 5-methylsulfonylmethyl-tetrazol, 5-benzylsulfanyl-tetrazol, 5-(thiophen-2-yl-methyl)-tetrazol, 5-(morpholinocarbonylmethyl)-tetrazol, 5-(4-methylpiperazin-1-yl)-tetrazol, 5-(4-acetyl-piperazin-1-yl)-tetrazol, 5-(4-cyanopiperazin-1-yl)-tetrazol, 5-(4-benzylpiperazin-1-yl)-tetrazol, 5-ethoxycarbonylmethyl-tetrazol, 5-hydroxyethyl-tetrazol, 5-acetylaminomethyl-tetrazol, 5-methyl-[1,2,4]-oxadiazol, 5-phenyl-[1,2,4]-oxadiazol, 5-pyridin-3-yl-[1,2,4]-oxadiazol, 5-methyl-[1,3,4]-oxadiazol, 5-phenyl-[1,3,4]-oxadiazol, 5-amino-2H-[1,3,4]-thiadiazol, 5-amino-2H-[1,2,4]-thiadiazol.
-
13. The compound of claim 6, wherein substituents of the heteroaryl are selected from the group comprising methyl, cyano, amino, fluoro, difluoromethyl, formyl, hydroxyl methyl, carboxamide, acetyl, 1-methoxyimino-methyl, 4pyridinyl, 3-pyridinyl, diethylamino, methylsulfonylmethyl.
-
14. The compound of claim 2, wherein X and Y are each independently CH, or CF.
-
15. The compound of claim 2, wherein at least one of X and Y is CF.
-
16. The compound of claim 2, wherein R4 is C1-C6 alkylamido, C1-C6 haloalkylamido, C1-C6 thioalkylamido, substituted C1-C6 thioalkylamido, wherein the alkyl group is substituted with halo;
- carbamate, thiocarbamate, urea, unsubstituted or substituted heteroaryl, wherein substituents of the heteroaryl are selected from the group comprising C1-C6 alkyl, nitro, cyano, hydroxyl, halo, amino, C1-C6 alkylcarbonyl, C1-C6 alkoxycarbonyl, carboxy.
-
17. The compound of claim 2, wherein R4 is acetamide, difluoroacetamide, thioacetamide, difluoroacetamide, carbamate, thiocarbamate, urea, [1,2,3]-triazol, [1,2,4]-triazol.
-
18. The compound of claim 2, wherein R4 is acetamide, carbamate, [1,2,3]-triazol.
-
19. The compound of claim 10, wherein n, R2, R2′
- , W is as defined in claim 10, R4 is acetamide, carbamate, [1,2,3]-triazol;
X and Y are each independently CH, or CF.
- , W is as defined in claim 10, R4 is acetamide, carbamate, [1,2,3]-triazol;
-
20. The compound of claim 1, wherein X, Y, R4 are as defined in claim 1;
- and Q is
wherein X′
, Y′ and
T have the definition as provided in claim 1.
- and Q is
-
21. The compound of claim 20, wherein X′
- and Y′
are each independently CH, CF, N, C—
CH3.
- and Y′
-
22. The compound of claim 20, wherein X′
- and Y′
are each independently CH, CF, N, C—
CH3;
X, Y, R4 are as defined in claim 1;T is hydrogen or wherein R2, R2′
, R3, R3′
, Z, n, have definition as provided in claim 1, with proviso that when T is hydrogen, R4 is not acetamido.
- and Y′
-
23. The compound of claim 22, wherein Z is selected from the group comprising CH, NH, O, S, CH2, C(R6)R6′
- , C═
O, NR7, C═
C(R8)R8′
, SO, SO2, S═
NH, S═
NC(O)CH3, S═
NC(O)NHCH3, S(O)═
NH, S(O)═
NCH3, S(O)NC(O)CH3, S(O)═
NC(O)NHCH3, S(O)═
NC(O)NHCH2CH2Cl,with proviso that when X is CH, Y is CF, one of X′
or Y′
or both X′
, Y′
are N, then Z is not NH.
- , C═
-
24. The compound of claim 22, wherein Z is selected from the group S, SO, SO2;
-
X′ and
Y′
are each independently CH, CF, N, C—
CH3;X, Y, are each independently CH or CF; R4 is as defined in claim 1; R2, R2′
, R3, R3′
, are each independently selected from hydrogen, methyl, hydroxyl, fluorine.
-
-
25. The compound of claim 22, wherein R4 is acetamido, [1,2,3]-triazol, methyl carbamate, t-butyl carbamate, OR1 wherein R1 is hydrogen, P(O)(OM)2, wherein M is hydrogen, Na, methyl, ethyl, t-butyl, phenyl;
- or R1 is an amino acid residue derived from one of the 20 naturally occurring amino acids viz. alanine, arginine, asparagine, aspartic acid, cysteine, glutamine, glutamic acid, glycine, histidine, isoleucine, leucine, lysine, methionine, phenylalanine, proline, serine, threonine, tryptophan, tyrosine and valine, attached to the oxygen via carbonyl of amino acid to form an ester linkage.
-
26. The compound of claim 25, wherein amino acid is L-alanine and L-valine.
-
27. The compound of claim 22, wherein at least one of the X, Y is CF and at least one of X′
- , Y′
is CF.
- , Y′
-
28. The compound of claim 22, wherein at least one of the X, Y is CF and at least one of X′
- , Y′
is N.
- , Y′
-
29. The compound of claim 22, wherein X, is CH, Y is CF, X′
- is N and Y′
is C—
CH3.
- is N and Y′
-
30. The compound of claim 24, wherein Z, X, Y, X′
- , Y′
, R2, R2′
, R3, R3′
are as defined in claim 24, R4 is selected from the group comprising acetamido, [1,2,3]-triazol, methyl carbamate, t-butyl carbamate, OR1, wherein R1 is as defined in claim 25.
- , Y′
-
34. Pharmaceutical composition comprising a compound according to claim 1 and an excipient, diluent, solvent or a carrier.
-
38. A method for treating a disease caused by a microbial infection in a human or animal comprising administering an effective amount of a compound according to claim 1, to the human or animal in need thereof.
-
42. A method for preventing a disease caused by a microbial infection in a human or animal comprising administering an effective amount of a compound according to claim 1, to the human or animal at risk of being infected.
-
46. The animal in claim 38-45 is selected from mammal, fish, bird.
-
47. The microbial infection in claims 38-45 are central nervous system infections, external ear infections, infections of the middle ear, such as acute otitis media, infections of the cranial sinuses, eye infections, infections of the oral cavity, such as infections of the teeth, guns and mucosa, upper respiratory tract infections, lower respiratory tract infections, genitourinary infections, gastrointestinal infections, gynecological infections, mastitis, septicemia, bone and joint infections, skin and skin structure infections, bacterial endocarditis, burns, antibacterial prophylaxis of surgery, and antibacterial prophylaxis in immunosuppressed patients, such as patients receiving cancer chemotherapy, or organ transplant patients, osteomyelitis, endocarditis and diabetic foot.
-
48. The method of preparation of a compound according to claim 1.
-
31. A compound or a pharmaceutically acceptable salt thereof which is
(S)— - N-{3-[4-(4-(2-Cyanoaziridin-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;
(S)—
N-{3-[4-(4-pyrrol-1-yl-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[3,5-Difluoro-4-(4-pyrrol-1-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(1H-imidazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4 (2H-[1,2,3]-triazol-2-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(2H-[1,2,3]-triazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(1H-[1,2,3]-triazol-1-yl)-3-fluoropiperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(2H-[1,2,3]-triazol-2-yl)-3-fluoropiperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(1H-[1,2,3]-triazol-1-yl)-3-fluoropiperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(2H-[1,2,3]-triazol-2-yl)-3-fluoropiperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(1H-[1,2,4]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-([1,2,3,4]-tetrazol-5-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-([1,2,3,4]-tetrazol-5-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(1H-[1,2,3,4]-tetrazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(1H-[1,2,3,4]-tetrazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(1H-[1,2,3,4]-tetrazol-1-yl)-3-hydroxypiperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide and isomer thereof;(S)—
N-{3-[4-(4-(1H-[1,2,3,4]-tetrazol-1-yl)-3-hydroxypiperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(1H-[1,2,3,4]-tetrazol-1-yl)-3-fluoropiperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-formyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-formyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylrmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-formyl-1H-[1,2,3]-triazol-1-yl)-3-fluoropiperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-[4-(4-(4-formyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-5-(1-1-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; (S)—
N-{3-[4-(4-(4-difluoromethyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-difluoromethyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-[1,3]-Dioxolan-2-yl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-5-(1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one;(S)—
N-{3-[4-(4-(4-ethoxycarbonyl-1H-[1,2,3]-triazol-1-yl)-methyl-piperidin-1-yl)-3-fluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-ethoxycarbonyl-1H-[1,2,3]-triazol-1-yl)-methyl-piperidin-1-yl)-3-fluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-ethoxycarbonyl-1H-[1,2,3]-triazol-1-yl)-3-fluoropiperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-ethoxycarbonyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-[4-(4-(4-ethoxycarbonyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-5-(1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; (R)-{3-[4-(4-(4-ethoxycarbonyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-5-(1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; (S)—
N-{3-[4-(4-(4-hydroxymethyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-hydroxymethyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-hydroxymethyl-1H-[1,2,3]-triazol-1-yl)-3-fluoropiperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-hydroxymethyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-[4-(4-(4-hydroxymethyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-5-(1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; (R)-{3-[4-(4-(4-hydroxymethyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-5-(1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; (S)—
N-{3-[4-(4-((4-hydroxymethyl)-[1,2,3]-triazol-1-yl-methyl)-piperidin-1-yl)-3-fluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-cyano-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-carboxamido-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-[4-(4-(4-carboxamido-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-5-(1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; (S)—
N-{3-[4-(4-(4-carboxamido-1H-[1,2,3]-triazol-1-yl)-methyl-piperidin-1-yl)-3-fluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-carboxamido-1H-[1,2,3],-triazol-1-yl)-methyl-piperidin-1-yl)-3-fluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-hydroxycarbonyl-1H-[1,2,3]-triazol-1-yl)-methyl-piperidin-1-yl)-3-fluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-hydroxycarbonyl-1H-[1,2,3]-triazol-1-yl)-methyl-piperidin-1-yl)-3-fluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-acetyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-acetyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-[4-(4-(4-acetyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-5-(1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; (S)—
N-{3-[4-(4-(4-acetyl-1H-[1,2,3]-trizol-1-ylmethyl)-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-(1-hydroxyethyl)-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-(1-hydroxyethyl)-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-[4-(4-(4-(2-hydroxyethyl)-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-5-(1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; (S)—
N-{3-[4-(4-(4-(2-methyl-oxiranyl)-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-[4-(4-(4-(2-dimethyl-oxiranyl)-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-5-(1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; (S)—
N-{3-[4-(4-((4-((E/Z)-2-cyano-vinyl)-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-hydroxyimino-methyl)-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(1-methoxyimino-ethyl)-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-(1-methoxyimino-ethyl)-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-[4-(4-(4-(1-methoxyimino-ethyl)-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-5-(1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; (R)-{3-[4-(4-(4-(1-methoxyimino-ethyl)-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-5-(1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; (S)—
N-{3-[4-(4-(1-methoxyimino-methyl)-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(1-methoxyimino-methyl)-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(1-benzyloxyimino-methyl)-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-hydroxyiminoamino-methyl)-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-N,N-dimethylaminoethylaminomethyl)-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(2H-benzotriazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(1H-benzotriazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-Benzotriazol-2-yl-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-Benzotriazol-1-yl-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-(1H-[1,2,3,4]-tetrazol-1-ylmethyl)-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(2H-[1,2,3,4]-tetrazol-2-ylmethyl)-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(1H-imidazol-1-ylmethyl)-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-[4-(4-(1H-[1,2,3]-triazol-1-yl)-3-fluoropiperidin-1-yl)-3-fluorophenyl]-5-(1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; (R)-{3-[4-(4-(1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-5-(1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; (R)-{3-[4-(4-(1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-5-(1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; (R)-{3-[4-(4-(1H-[1,2,3]-triazol-1-yl)-3-fluoropiperidin-1-yl)-3,5-difluorophenyl]-5-(1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; (S)—
N-{3-[4-(4-([1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-thioacetamide;(S)—
N-{3-[4-(4-(5-methyl-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-methyl-1H-[1,2,3,4]-tetrazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-methyl-1H-[1,2,3,4]-tetrazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-methyl-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(2-methyl-2H-tetrazol-5-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(1-methyl-1H-tetrazol-5-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(2-methyl-2H-tetrazol-5-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(1-methyl-1H-tetrazol-5-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-[4-(4-(2-methyl-2H-tetrazol-5-yl)-piperidin-1-yl)-3-fluorophenyl]-5-(1H-[1,2,3]-triazol-1ylmethyl)}-oxazolidin-2-one; (R)-{3-[4-(4-(1-methyl-1H-tetrazol-5-yl)-piperidin-1-yl)-3-fluorophenyl]-5-(1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; (S)—
N-{3-[4-(4-(1-methyl)-1H-tetrazol-5-ylmethyl-piperidin-1-yl)-3,5-difluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(2-methyl)-2H-tetrazol-5-ylmethyl-piperidin-1-yl)-3,5-difluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(1-methyl-1H-tetrazol-5-ylmethyl)-piperidin-1-yl)-3-fluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(2-methyl-2H-tetrazol-5-ylmethyl)-piperidin-1-yl)-3-fluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-methylsulfanylmethyl-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-methylsulfanylmethyl-1H-[1,2,3,4]-tetrazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-methylsulfanylmethyl-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-methylsulfanylmethyl-1H-[1,2,3,4]-tetrazol-1-yl)-piperidin-1-yl)-3,5-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-benzylsulfanyl-1H-[1,2,3,4]-tetrazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(benzylsulfanyl)-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(benzylsulfanyl)-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(benzylsulfanyl)-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-methylsulfonylmethyl-1H-[1,2,3,4]-tetrazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-methylsulfonylmethyl-1H-[1,2,3,4]-tetrazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(thiophen-2-yl-methyl)-1H-[1,2,3,4]-tetrazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(thiophen-2-yl-methyl)-1H-[1,2,3,4]-tetrazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(thiophen-2-yl-methyl)-1H-[1,2,3,4]-tetrazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(thiophen-2-yl-methyl)-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(morpholinocarbonylmethyl)-1H-[1,2,3,4]-tetrazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(morpholinocarbonylmethyl)-1H-[1,2,3,4]-tetrazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(morpholin-4-yl)-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(morpholin-4-yl)-2H-[1,2,3,4]-tetrazol-2-yl}-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl)-acetamide;(S)—
N-{3-[4-(4-(5-phenyl-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-phenyl-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(4-nitrophenyl)-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(4-nitrophenyl)-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(4-pyridinyl)-1H-[1,2,3,4]-tetrazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(3-pyridinyl)-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(4-pyridinyl)-1H-[1,2,3,4]-tetrazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(3-pyridinyl)-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-amino-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-amino-2H-[1,2,3,4]-tetrazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(diethylamino)-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(piperazin-1-yl)-2H-[1,2,3,4],-tetrazol-2-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(piperazin-1-yl)-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(5-(4-methylpiperazin-1-yl)-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(4-methylpiperazin-1-yl)-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(4-acetyl-piperazin-1-yl)-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(4-acetyl-piperazin-1-yl)-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(4-cyanopiperazin-1-yl)-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(4-cyanopiperazin-1-yl)-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(4-benzylpiperazin-1-yl)-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-(4-benzylpiperazin-1-yl)-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-1H-tetrazol-5-ylmethyl-piperidin-1-yl)-3-fluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-1H-tetrazol-5-ylmethyl-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-([1,2,3]-triazol-1-yl-methyl)-piperidin-1-yl)-3-fluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-[4-(4-(1H-[1,2,3,4]-tetrazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-5-(1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; (R)-{3-[4-(4-(2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3-fluorophenyl]-5-(1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; (S)-{3-[4-(4-([1,2,3,4]-tetrazol-5-yl)-piperidin-1-yl)-3-fluorophenyl]-5-(1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; (S)—
N-{3-[4-(4-(5-methyl-[1,2,4]-oxadiazol-3-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-methyl-[1,2,4]-oxadiazol-3-ylmethyl)-piperidin-1-yl)-3-fluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-methyl-[1,2,4]-oxadiazol-3-ylmethyl)-piperidin-1-yl)-3,5-difluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-phenyl-[1,2,4]-oxadiazol-3-ylmethyl)-piperidin-1-yl)-3-fluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-phenyl-[1,2,4]-oxadiazol-3-ylmethyl)-piperidin-1-yl)-3,5-difluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-((5-pyridin-3-yl)-[1,2,4]-oxadiazol-3-ylmethyl)-piperidin-1-yl)-3-fluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-methyl-[1,3,4]-oxadiazol-2-ylmethyl)-piperidin-1-yl)-3-fluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-phenyl-[1,3,4]-oxadiazol-2-ylmethyl)-piperidin-1-yl)-3-fluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-Amino-2H-[1,3,4]-thiadiazol-2-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-Amino-[1,3,4]-thiadiazol-2-yl)-piperidin-1-yl)-3,5-difluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-Amino-[1,3,4]-thiadiazol-2-ylmethyl)-piperidin-1-yl)-3,5-difluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(3-ethoxycarbonyl-imidazol-1-yl)-methyl-piperidin-1-yl)-3-fluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[3,5-Difluoro-4-(4-2H-tetrazol-2-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-carbamic acid methyl ester;(S)—
N-{3-[3,5-Difluoro-4-(4-1H-tetrazol-1-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-carbamic acid methyl ester;(S)—
N-{3-[3,5-Difluoro-4-(4-[1,2,3]-thiazol-1-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-carbamic acid methyl ester;(S)—
N-{3-[3-fluoro-4-(4-2H-tetrazol-2-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-carbamic acid methyl ester;(S)—
N-{3-[3-fluoro-4-(4-1H-tetrazol-1-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-carbamic acid methyl ester;(S)—
N-{3-[4-(4-2H-[1,2,3]-triazol-2-yl-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-carbamic acid methyl ester;(S)—
N-{3-[3,5-Difluoro-4-(4-[1,2,3]triazol-2-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-2,2-difluoro-acetamide;(S)—
N-{3-[3,5-Difluoro-4-(4-[1,2,3]-triazol-1-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-2,2-difluoro-acetamide;(S)—
N-{3-[3,5-Difluoro-4-(4-[1,2,3,4]-tetrazol-2-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-2,2-difluoro-acetamide;(S)—
N-{3-[3,5-Difluoro-4-(4-[1,2,3,4]-triazol-1-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-2,2-difluoro-acetamide;(S)—
N-{3-[3,5-Difluoro-4-(4-2H-tetrazole-2-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-2,2-dichloro-acetamide;(S)—
N-{3-[3-fluoro-4-(4-2H-tetrazol-2-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-carbamic acid ethyl ester;(S)—
N-{3-[3,5-Difluoro-4-(4-1H-tetrazole-1-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-2,2-difluoro-thioacetamide;(S)—
N-{3-[3,5-Difluoro-4-(4-1H-tetrazole-1-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-cyclopropane carboxamide;(S)—
N-{3-[3,5-Difluoro-4-(4-[1,2,3]-triazol-1-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-propionamide;(S)—
N-{3-[3,5-Difluoro-4-(4-[1,2,3]-triazol-2-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-propionamide;(S)—
N-{3-[3,5-Difluoro-4-(4-2H-tetrazol-2-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-propionamide;(S)—
N-{3-[3,5-Difluoro-4-(4-1H-tetrazol-1-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-propionamide;(S)N-{3-[3-Fluoro-4-(4-2H-tetrazol-2-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-propionamide; (S)N-{3-[3-Fluoro-4-(4-1H-tetrazol-1-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-propionamide; (S)—
N-{3-[3,5-Difluoro-4-(4-[1,2,3]-triazol-2-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-propionamide;(S)—
N-{3-[3,5-Difluoro-4-(4-[1,2,3]-triazol-1-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-propionamide;(S)—
N-{3-[3,5-Difluoro-4-(4-(5-methyl-tetrazol-2-yl)-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-propionamide;(S)—
N-{3-[3,5-Difluoro-4-(4-(5-methyl-tetrazol-1-yl)-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-propionamide;(S)—
N-{3-[3,5-Difluoro-4-(4-(4-methyl-5-thioxo-4,5-dihydro-tetrazol-1-yl)-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[3,5-Difluoro-4-(4-(4-methyl-5-thioxo-4,5-dihydro-[1,2,4]triazol-1-yl)-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[3-fluoro-4-(4-(4-methyl-5-thioxo-4,5-dihydro-[1,2,4]triazol-1-yl)-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(isoxazol-3-yloxymethyl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-([1,2,3]-triazol-1-yl)-methyl-piperidin-1-yl)-3-fluoro-phenyl]-5-(isoxazol-3-yloxymethyl)}-oxazolidin-2-one;(R)-{3-[4-(4-((4-hydroxymethyl)-[1,2,3]-triazol-1-yl)-methyl-piperidin-1-yl)-3-fluoro-phenyl]-5-(isoxazol-3-yloxymethyl)}-oxazolidin-2-one; cis-(R)-{3-[4-(4-(5-ethoxycarbonyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-5-(5-ethoxycarbonyl-1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; cis-(R)-{3-[4-(4-(5-ethoxycarbonyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluoro-phenyl]-5-(4-ethoxycarbonyl-1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; trans-(R)-{3-[4-(4-(5-ethoxycarbonyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluoro-phenyl]-5-(5-ethoxycarbonyl-1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; trans-(R)-{3-[4-(4-(5-ethoxycarbonyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluoro-phenyl]-5-(4-ethoxycarbonyl-1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; trans-(R)-{3-[4-(4-(5-hydroxymethyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluoro-phenyl]-5-(4-hydroxymethyl-1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; trans-(R)-{3-[4-(4-(5-hydroxymethyl-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluoro-phenyl]-5-(5-hydroxymethyl-1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; trans-(R)-{3-[4-(4-(5-cyano-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluoro-phenyl]-5-(5-cyano-1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; trans-(R)-{3-[4-(4-(5-cyano-1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluoro-phenyl]-5-(4-cyano-1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; (3R,5S)—
N-{3-[4-(Fluoro-4-(1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3-fluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-[4-(4-(5-ethoxycarbonylmethyl-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-5-(1H-[1,2,3]-triazol-1-ylmethyl)}-oxazolidin-2-one; (S)—
N-{3-[4-(4-(5-hydroxyethyl-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(5-acetylaminomethyl-2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-(4-phenyl-3-fluorophenyl)-5-1H-1,2,3-triazol-1-ylmethyl}-oxazolidin-2-one; (R)-{3-(4-phenyl-3-fluorophenyl)-5-1H-1,2,4-triazol-1-ylmethyl}-oxazolidin-2-one; (R)-{3-(4-phenyl-3-fluorophenyl)-5-1H-1,2,3-triazol-2-ylmethyl}-oxazolidin-2-one; (R)-{3-[4-(4-(piperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-methanesulfonate; (S)—
N-{3-[4-(4-(piperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)-{3-[4-(4-(piperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-5-imidazol-1-ylmethyl}-oxazolidin-2-one; (R)-{3-[4-(4-(piperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-5-1H-1,2,3-triazol-1-ylmethyl}-oxazolidin-2-one; (R)-{3-[4-(4-(piperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-5-1H-1,2,3-triazol-2-ylmethyl}-oxazolidin-2-one; (R)-{3-[4-(4-(piperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-5-1H-1,2,3,4-tetrazol-1-ylmethyl}-oxazolidin-2-one; (S)—
N-{3-[4-(4-(4,4-dimethoxypiperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-[4-(4-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-methanesulfonate; (S)—
N-{3-[4-(4-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-[4-(4-(4-oxo-piperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-methanesulfonate; (S)—
N-{3-[4-(4-(4-oxo-piperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-[4-(4-(4-hydroxy-piperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-methanesulfonate; (S)—
N-{3-[4-(4-(4-hydroxy-piperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(4-hydroxy-piperidin-1-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-[4-(4-(4-methanesulfonyloxy-piperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-methanesulfonate; (S)—
N-{3-[4-(4-(4-methanesulfonyloxy-piperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(4-methanesulfonyloxy-piperidin-1-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-cyanomethylidene-piperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-[4-(4-(4-cyanomethylidene-piperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-5-(1H-1,2,3-triazol-1-yl)-methyl}-oxazolidin-2-one; (R)-{3-[4-(4-(4-cyanomethylidene-piperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-5-(1H-tetrazol-1-yl)methyl}-oxazolidin-2-one; (S)—
N-{3-[4-(4-(4-cyanomethyl-3,4-dehydropiperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-cyanomethyl-piperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-hydroxy-4-hydroxymethyl-piperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-azidomethyl-4-hydroxy-piperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(4-(1H-1,2,3-triazol-1-yl)-piperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide and isomer thereof;(S)—
N-{3-[4-(4-(4-(1H-1,2,3,4-tetrazol-1-yl)-piperidin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide and isomer thereof;(S)—
N-{3-[4-(6-(4-Oxopiperidin-1-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(4-Hydroxy-4-methoxymethylpiperidin-1-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(4-Hydroxy-4-acetyloxymethylpiperidin-1-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-[4-(4-(piperazin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-5-1H-1,2,3-triazol-1-ylmethyl}-oxazolidin-2-one; (R)-{3-[4-(4-(piperazin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-5-1H-1,2,3,4-tetrazol-1-ylmethyl}-oxazolidin-2-one; (R)-{3-[4-(4-(piperazin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-methanesulfonate hydrochloride; (R)-{3-[4-(4-(piperazin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-5-(1,2,3-triazol-1-yl)methyl}-oxazolidin-2-one hydrochloride; (S)-{3-[4-(4-(4-hydroxymethylcarbonyl-piperazin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide; (R)-{3-[4-(4-(4-(2-nitrofuran-5-yl-methyl)-piperazin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-methanesulfonate; (S)—
N-{3-[4-(4-(4-(2-nitrofuran-5-yl-methyl)-piperazin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-[4-(4-(4-benzyloxycarbonyl-piperazin-1-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-methanesulfonate; (S)-{3-[4-(4-benzyloxycarbonyl-piperazin-1-yl-3-fluorophenyl)-3-fluorophenyl]-5-1H-1,2,3-triazol-1-ylmethyl}-oxazolidin-2-one; (S)—
N-{3-[4-(4-benzyloxycarbonyl-piperazin-1-yl-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(1-oxa-6-azaspiro[2.5]oct-6-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(morpholin-1-yl)-phenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(thiomorpholin-4-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-methanesulfonate;(S)—
N-{3-[4-(6-(thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-[4-(6-(Thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-methansulphonate; (S)—
N-{3-[4-(6-(Thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-formamide;(S)—
N-{3-[4-(6-(Thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-propionamide;(S)-{3-[4-(6-(thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-carbamic acid methyl ester; (S)-{3-[4-(6-thiomorpholin-4-yl-pyridin-3-yl)-3-fluorophenyl]-5-1,2,3-triazol-1-ylmethyl}-oxazolidin-2-one; (S)—
N-{3-[6-(6-(Thiomorpholin-4-yl)-pyridin-3-yl)-pyridin-3-yl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[6-(4-(Thiomorpholin-4-yl)-3-fluorophenyl)-pyridin-3-yl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(Thiomorpholin-4-yl)-pyridin-3-yl)-phenyl]-2-oxo-oxazolidin-5-yl methyl}-acetamide;(S)—
N-{3-[4-(2-(Thiomorpholin-4-yl)-pyrimidin-5-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-carbamic acid methyl ester;(S)—
N-{3-[4-(2-(Thiomorpholin-4-yl)-pyrimidin-5-yl)-3-fluorophenyl]-5-hydroxymethyl}-oxazolidin-2-one;(S)—
N-{3-[4-(2-(Thiomorpholin-4-yl)-pyrimidin-5-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(2-(Thiomorpholin-4-yl)-pyrimidin-5-yl)-3-fluorophenyl]-5-1,2,3-triazol-1-ylmethyl}-oxazolidin-2-one;(S)—
N-{3-[4-(6-(Thiomorpholin-4-yl)-3-methylpyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-carbamic acid methyl ester;(S)—
N-{3-[4-(6-(Thiomorpholin-4-yl)-3-methylpyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(Thiomorpholin-4-yl)-3-methylpyridin-3-yl)-3-fluorophenyl]-5-hydroxymethyl}-oxazolidin-2-one;(S)—
N-{3-[4-(6-(Thiomorpholin-4-yl)-3-methylpyridin-3-yl)-3-fluorophenyl]-5-1,2,3-triazol-1-ylmethyl}-oxazolidin-2-one;(S)—
N-{3-[4-(2-(S-Oxo-thiomorpholin-4-yl)-pyridin-5-yl)-3-fluorophenyl]-5-hydroxymethyl}-oxazolidin-2-one;(S)—
N-{3-[4-(4-(S-oxo-thiomorpholin-4-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[6-[6-(S-oxo-thiomorpholin-4-yl)-pyridin-3-yl]-pyridin-3-yl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(S-oxo-thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-{3-[4-(6-(S-Oxo-thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-methansulphonate; (S)—
N-{3-[4-(6-(S-Oxo-thiomorpholin-4-yl)-pyridin-3-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(2-(S-Oxo-thiomorpholin-4-yl)-pyrimidin-5-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-carbamic acid methyl ester;(S)—
N-{3-[4-(2-(S-Oxo-thiomorpholin-4-yl)-pyrimidin-5-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(2-(S-Oxo-thiomorpholin-4-yl)-pyrimidin-5-yl)-3-fluorophenyl]-5-1,2,3-triazol-1-ylmethyl}-oxazolidin-2-one;(S)—
N-{3-[4-(6-(S-Oxo-thiomorpholin-4-yl)-pyrimidin-5-yl)-3-fluorophenyl]-5-hydroxymethyl}-oxazolidin-2-one;(S)—
N-{3-[4-(6-(S-Oxo-thiomorpholin-4-yl)-3-methylpyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-carbamic acid methyl ester;(S)—
N-{3-[4-(6-(S-Oxo-thiomorpholin-4-yl)-3-methylpyridin-3-yl)-3-fluorophenyl]-5-1,2,3-triazol-1-ylmethyl}-oxazolidin-2-one;(S)—
N-{3-[4-(6-(S-Oxo-thiomorpholin-4-yl)-3-methylpyridin-3-yl)-3-fluorophenyl]-5-hydroxymethyl}-oxazolidin-2-one;(S)—
N-{3-[4-(6-(S-Oxo-thiomorpholin-4-yl)-3-methylpyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(S-oxo-3-fluoro-thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(S,S-dioxo-thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(S,S-dioxo-thiomorpholin-4-yl)-pyridin-3-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(S,S-dioxo-3-methyl-thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl)]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(S,S-dioxo-thiomorpholin-4-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[6-[6-(S,S-dioxo-thiomorpholin-4-yl)-pyridin-3-yl]-pyridin-3-yl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[6-(4-(S,S-dioxo-thiomorpholin-4-yl)-3-fluorophenyl)-pyridin-3-yl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-3-{4-[6-(S,S-dioxo-thiomorpholin-4-yl)-pyridin-3-yl]-3-fluorophenyl}-5-hydroxymethyl-oxazolidin-2-one; (2S,5R)-2-Amino-propionic acid 3-{4-[6-(S,S-dioxo-thiomorpholin-4-yl)-pyridin-3-yl]-3-fluoro-phenyl}-2-oxo-oxazolidin-5-ylmethyl ester; (2S,5R)-2-Amino-propionic acid 3-{4-[6-(S,S-dioxo-thiomorpholin-4-yl)-pyridin-3-yl]-3-fluoro-phenyl}-2-oxo-oxazolidin-5-ylmethyl ester methanesulfonic acid salt; (2S,5R)-2-Amino-3-methyl-butyric acid 3-{4-[6-(S,S-dioxo-thiomorpholin-4-yl)-pyridin-3-yl]-3-fluoro-phenyl}-2-oxo-oxazolidin-5-ylmethyl ester; (2S,5R)-2-Amino-3-methyl-butyric acid 3-{4-[6-(S,S-dioxo-thiomorpholin-4-yl)-pyridin-3-yl]-3-fluoro-phenyl}-2-oxo-oxazolidin-5-ylmethyl ester methane sulfonic acid salt; (R)-Acetic acid 3-{4-[6-(S,S-dioxo-thiomorpholin-4-yl)-pyridin-3-yl]-3-fluoro-phenyl}-2-oxo-oxazolidin-5-ylmethyl ester; (S)—
N-{3-[4-(6-(S,S-Dioxo-thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-formamide;(R)-{3-[4-(6-(S,S-Dioxo-thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-methansulphonate; (S)—
N-{3-[4-(6-(S,S-Dioxo-thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-propionamide;(S)—
N-{3-[4-(6-(S,S-Dioxo-thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-carbamic acid methyl ester;N-Acetyl-(R)—
N-{3-4-{2-(S,S-Dioxo-thiomorpholin-4-yl)-pyridyl-5-yl-3-fluorophenyl-1-yl-]}-2-oxo-oxazolidin-5-ylmethyl}-aminocarbonyl-oxymethyl acetate;(S)—
N-{3-[4-(6-(S,S-Dioxo-thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-5-1,2,3-triazol-1-ylmethyl}-oxazolidin-2-one;(S)—
N-{3-[4-(6-(S,S-Dioxo-thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-urea;(S)—
N-{3-[4-(6-(S,S-Dioxo-thiomorpholin-4-yl)-pyridin-3-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[6-(6-(S,S-Dioxo-thiomorpholin-4-yl)-pyridin-3-yl)-pyridin-3-yl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(2-(S,S-Dioxo-thiomorpholin-4-yl)-pyrimidin-5-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-carbamic acid methyl ester;(S)—
N-{3-[4-(2-(S,S-Dioxo-thiomorpholin-4-yl)-pyrimidin-5-yl)-3-fluorophenyl]-5-hydroxymethyl}-oxazolidin-2-one;(S)—
N-{3-[4-(2-(S,S-Dioxo-thiomorpholin-4-yl)-pyrimidin-5-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(2-(S,S-Dioxo-thiomorpholin-4-yl)-pyrimidin-5-yl)-3-fluorophenyl]-5-1,2,3-triazol-1-ylmethyl}-oxazolidin-2-one;(S)—
N-{3-[4-(6-(S,S-Dioxo-thiomorpholin-4-yl)-3-methylpyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-carbamic acid methyl ester;(S)—
N-{3-[4-(6-(S,S-Dioxo-thiomorpholin-4-yl)-3-methylpyridin-3-yl)-3-fluorophenyl]-5-hydroxymethyl}-oxazolidin-2-one;(S)—
N-{3-[4-(6-(S,S-Dioxo-thiomorpholin-4-yl)-3-methylpyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(S,S-Dioxo-thiomorpholin-4-yl)-3-methylpyridin-3-yl)-3-fluorophenyl]-5-1,2,3-triazol-1-ylmethyl}-oxazolidin-2-one;(S)—
N-{3-[4-(6-(S,S-Dioxo-3-methyl-thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-difluoroacetamide;(S)—
N-{3-[4-(6-(S-Oxo-S—
(N-methylimino)-thiomorpholin-4-yl)-pyridyl-3-yl)-3-fluorophenyl-1-yl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(S-Oxo-S—
(N-methylimino)-thiomorpholin-4-yl)-pyridin-3-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(S-Oxo-S—
(N-acetylimino)-thiomorpholin-4-yl)-pyridyl-3-yl)-3-fluorophenyl-1-yl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(S-Oxo-S-(1-chloroethylurido)-thiomorpholin-4-yl)-pyridyl-3-yl)-3-fluorophenyl-1-yl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(S-Oxo-S-imino-thiomorpholin-4-yl)-pyridyl-3-yl)-3-fluorophenyl-1-yl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(1,4-Dioxa-8-azaspiro[4.5]dec-8-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(S-Oxo-3,3-dichloro-thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-Phosphoric acid {3-[4-(6-(S,S-dioxo-thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}ester disodium salt; Phosphoric acid mono (R)—
N-{3-{4-{2-(thiomorpholin-4-yl)-pyrimidin-5-yl}-3-fluorophenyl]}-2-oxo-oxazolidin-5-ylmethyl}ester;Phosphoric acid mono (R)—
N-{3-{4-(2-(S-oxo-thiomorpholin-4-yl)-pyrimidin-5-yl}-3-fluorophenyl]}-2-oxo-oxazolidin-5-ylmethyl}ester;Phosphoric acid mono (R)—
N-{3-{4-{2-(S,S-dioxo-thiomorpholin-4-yl)-pyrimidin-5-yl}-3-fluorophenyl]}-2-oxo-oxazolidin-5-ylmethyl}-ester;(R)-Phosphoric acid mono {3-[4-(6-(S,S-dioxo-thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}ester; Phosphoric acid mono (R)—
N-{3-{4-{2-(S,S-Dioxo thiomorpholin-4-yl)-pyrimidin-5-yl}-3-fluorophenyl]}-2-oxo-oxazolidin-5-ylmethyl}-ester disodium salt;(R)-Phosphoric acid mono {3-[4-(6-(thiomorpholin-4-yl)-3-methylpyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}ester; (R)-Phosphoric acid mono {3-[4-(6-(S-oxo-thiomorpholin-4-yl)-3-methylpyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}ester; (R)-Phosphoric acid mono {3-[4-(6-(S,S-dioxo-thiomorpholin-4-yl)-3-methylpyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}ester; (R)-Phosphoric acid mono {3-[4-(6-(S-oxo-thiomorpholin-4-yl)-3-methylpyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}ester disodium salt; (5S)—
N-[3-(3′
-Chloromethyl-2-fluoro-biphenyl-4-yl)-2-oxo-oxazolidin-5-ylmethyl]-acetamide;(5S)—
N-[3-(2-Fluoro-3′
-fluoromethyl-biphenyl-4-yl)-2-oxo-oxazolidin-5-ylmethyl]-acetamide;(5S)—
N-[3-(2-Fluoro-3′
-azidomethyl-biphenyl-4-yl)-2-oxo-oxazolidin-5-ylmethyl]-acetamide;(5S)—
N-[3-(3′
-Aminomethyl-2-fluoro-biphenyl-4-yl)-2-oxo-oxazolidin-5-ylmethyl]-acetamide;(5S)-2-({4′
-[5-(Acetylamino-methyl)-2-oxo-oxazolidin-3-yl]-2′
-fluoro-biphenyl-3-ylmethyl}-amino)-acetamide;(5S)-2-({4′
-[5-(Acetylamino-methyl)-2-oxo-oxazolidin-3-yl]-2′
-fluoro-biphenyl-3-ylmethyl}-carbamoylmethyl-amino)-acetamide;(5S)—
N-{3-[4-(4-Azido-piperidin-1-yl)-3,5-difluoro-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(5S)-{3-[2-Fluoro-1,1′
-biphenyl-3′
-methoxy-4-yl]-2-oxo-oxazolidin-5yl-methyl}-acetamide;(5S)-{3-[(2-Fluoro-1,1′
-biphenyl-3′
-yl)methanol]-2-oxo-oxazolidin-5yl-methyl}-acetamide;(5S)-{3-[(3,5-Difluoro-4-[6-(4-thiomorpholin-1,1-dioxide-4-yl)-3-pyridinyl]phenyl]-2-oxo-oxazolidin-5yl-methyl}-acetamide; - View Dependent Claims (35, 39, 43)
- N-{3-[4-(4-(2-Cyanoaziridin-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;
-
32. A compound or a pharmaceutically acceptable salt thereof which is
(S)— - N-{3-[4-(4-(1H-[1,2,3,4]-tetrazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;
(S)—
N-{3-[4-(4-(2H-[1,2,3,4]-tetrazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4 (1H-[1,2,3,4]-tetrazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide(S)—
N-{3-[4-(4-(1H-[1,2,3]-triazol-1-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[3,5-difluoro-4-(4-2H-tetrazol-2-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-propionamide;(S)—
N-{3-[3,5-difluoro-4-(4-1H-tetrazol-1-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-propionamide;(S)—
N-{3-[4-(4-(2H-benzotriazol-2-yl)-piperidin-1-yl)-3,5-difluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[3,5-difluoro-4-(4-[1,2,3]-triazol-1-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-carbamic acid methyl ester;(S)—
N-{3-[3-fluoro-4-(4-2H-tetrazol-2-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylrmethyl}-carbamic acid methyl ester;(S)—
N-{3-[3-fluoro-4-(4-1H-tetrazol-1-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-carbamic acid methyl ester;(S)—
N-{3-[3,5-difluoro-4-(4-(4-methyl-5-thioxo-4,5-dihydro-tetrazol-1-yl)-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[3,5-difluoro-4-(4-[1,2,3]-triazol-1-yl-piperidin-1-yl)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-2,2-difluoro-acetamide;- View Dependent Claims (36, 40, 44)
- N-{3-[4-(4-(1H-[1,2,3,4]-tetrazol-1-yl)-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;
-
33. A compound or a pharmaceutically acceptable salt thereof which is
(S)— - N-{3-[4-(4-(thiomorpholin-4-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;
(S)—
N-{3-[4-(4-(S-oxo-thiomorpholin-4-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(4-(S,S-dioxo-thiomorpholin-4-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazobidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(S-oxo-thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(S,S-dioxo-thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(6-(S,S-dioxo-3-methyl-thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(R)-3-{4-[6-(S,S-Dioxo-thiomorpholin-4-yl)-pyridin-3-yl]-3-fluorophenyl}-5-hydroxymethyl-oxazolidin-2-one; (R)-Phosphoric acid mono {3-[4-(6-(S,S-dioxo-thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}ester; (R)-Phosphoric acid {3-[4-(6-(S,S-dioxo-thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}ester disodium salt; (2S,5R)-2-Amino-propionic acid 3-{4-[6-(S,S-dioxo-thiomorpholin-4-yl)-pyridin-3-yl]-3-fluoro-phenyl}-2-oxo-oxazolidin-5-ylmethyl ester; (2S,5R)-2-Amino-propionic acid 3-{4-[6-(S,S-dioxo-thiomorpholin-4-yl)-pyridin-3-yl]-3-fluoro-phenyl}-2-oxo-oxazolidin-5-ylmethyl ester methanesulphonic acid salt; (2S,5R)-2-Amino-3-methyl-butyric acid 3-{4-[6-(S,S-dioxo-thiomorpholin-4-yl)-pyridin-3-yl]-3-fluoro-phenyl}-2-oxo-oxazolidin-5-ylmethyl ester; (2S,5R)-2-Amino-3-methyl-butyric acid 3-{4-[6-(S,S-dioxo-thiomorpholin-4-yl)-pyridin-3-yl]-3-fluoro-phenyl}-2-oxo-oxazolidin-5-ylmethyl ester methanesulphonic acid salt; (2S,5R)-Acetic acid 3-{4-[6-(S,S-dioxo-thiomorpholin-4-yl)-pyridin-3-yl]-3-fluoro-phenyl}-2-oxo-oxazolidin-5-ylmethyl ester; (S)—
N-{3-[4-(6-(Thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-formamide,(S)—
N-{3-[4-(6-(S,S-Dioxo-thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-formamide;(S)-{3-[4-(6-(thiomorpholin-4-yl)-pyridin-3-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-carbamic acid methyl ester; (S)—
N-{3-[4-(2-(S,S-Dioxo-thiomorpholin-4-yl)-pyridin-5-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-carbamic acid methyl ester;(S)—
N-{3-[4-(2-(S,S-Dioxo-thiomorpholin-4-yl)-3-methylpyridin-5-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-carbamic acid methyl ester;(S)—
N-{3-[4-(2-(S,S-Dioxo-thiomorpholin-4-yl)-3-methylpyridin-5-yl)-3-fluorophenyl]-5-hydroxymethyl}-oxazolidin-2-one;(R)-Phosphoric acid mono {3-[4-(2-(S,S-dioxo-thiomorpholin-4-yl)-3-methylpyridin-5-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}ester; (R)-Phosphoric acid mono {3-[4-(2-(S-oxo-thiomorpholin-4-yl)-3-methylpyridin-5-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}ester disodium salt; (S)—
N-{3-[4-(2-(S,S-Dioxo-thiomorpholin-4-yl)-3-methylpyridin-5-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;(S)—
N-{3-[4-(2-(S,S-Dioxo-thiomorpholin-4-yl)-3-methylpyridin-5-yl)-3-fluorophenyl]-5-1,2,3-triazol-1-ylmethyl}-oxazolidin-2-one;- View Dependent Claims (37, 41, 45)
- N-{3-[4-(4-(thiomorpholin-4-yl)-3-fluorophenyl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide;
Specification