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US 2008/0269221 A1Published application
Antibacterial agents
AssigneeNovartis Vaccines and Diagnostics, Inc.
InventorsNiels H. Andersen, Jason Bowman, Alice Erwin, Eric Harwood, Toni Kline, Khisimuzi Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
Life of this patent
Estimating the term…
Abstract
Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
Claims48
A compound according to the formula IA:
- or a stereoisomer, pharmaceutically acceptable salt, ester, or prodrug thereof,
- wherein
- D is absent or selected from the group consisting of
- (1) substituted or unsubstituted C3-C8-cycloalkyl;
- (2) substituted or unsubstituted aryl;
- (3) substituted or unsubstituted heterocyclyl;
- and
- (4) substituted or unsubstituted heteroaryl;
- Y is selected from the group consisting of
- (1) substituted or unsubstituted C3-C8-cycloalkyl;
- (2) substituted heterocyclyl;
- and
- (3) substituted heteroaryl;
- R4 is H or substituted or unsubstituted C1-C6-alkyl;
- A is selected from the group consisting of
- (1) —C(R1a, R2a)OR3a;
- and
- (2) —C(R1a, R2a)N(R4a, R5a);
- wherein R1a, R2a, R3a, R4a, and R5a are independently selected from the group consisting of
- (1) H;
- and
- (2) substituted and unsubstituted C1-C6-alkyl.
19 more elements
A compound according to the formula IB:
- or a stereoisomer, pharmaceutically acceptable salt, ester, or prodrug thereof,
- wherein
- D is absent or selected from the group consisting of
- (1) substituted or unsubstituted C3-C8-cycloalkyl;
- (2) substituted or unsubstituted aryl;
- (3) substituted or unsubstituted heterocyclyl;
- and
- (4) substituted or unsubstituted heteroaryl;
- G is —C≡C—C≡C—;
- Y is selected from the group consisting of
- (1) substituted or unsubstituted C3-C8-cycloalkyl;
- (2) substituted or unsubstituted aryl;
- (3) substituted or unsubstituted heterocyclyl;
- and
- (4) substituted or unsubstituted heteroaryl;
- R4 is H or substituted or unsubstituted C1-C6-alkyl;
- A is —C(R1a, R2a)N(R4a, R5a);
- wherein R1a, R2a, R4a, and R5a are independently selected from the group consisting of
- (1) H;
- and
- (2) substituted and unsubstituted C1-C6-alkyl.
18 more elements
A compound according to Formula VIII:
- or stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof, wherein
- E is absent or selected from the group consisting of
- (1) H,
- (2) substituted or unsubstituted C1-C6-alkyl,
- (3) substituted or unsubstituted aryl,
- (4) substituted or unsubstituted heterocyclyl, and
- (5) substituted or unsubstituted heteroaryl,
- or E and R3L, together with the atoms to which they are attached form a substituted or unsubstituted heterocyclic ring, having from 5 to 10 ring atoms,
- wherein 1-4 ring atoms of the heterocyclic ring system are selected from N, O and S;
- R1L, R3L are independently selected from the group consisting of
- (1) H,
- (2) substituted or unsubstituted C1-C6-alkyl,
- (3) C1-C6-alkyl substituted with aryl,
- (4) C1-C6-alkyl substituted with heterocyclyl, and
- (5) C1-C6-alkyl substituted with heteroaryl,
- or R1L and R3L, together with the atoms to which they are attached form a substituted or unsubstituted heterocyclic ring, having from 5 to 7 ring atoms, wherein 1-2 ring atoms of the heterocyclic ring system are selected from N, O and S.
13 more elements
A compound according to the formula IA:
- or a stereoisomer, pharmaceutically acceptable salt, ester, or prodrug thereof,
- wherein
- D is absent or selected from the group consisting of
- (1) substituted or unsubstituted C3-C8-cycloalkyl;
- (2) substituted or unsubstituted aryl;
- (3) substituted or unsubstituted heterocyclyl;
- and
- (4) substituted or unsubstituted heteroaryl;
- Y is selected from the group consisting of
- (1) substituted or unsubstituted aryl;
- (2) substituted or unsubstituted heterocyclyl;
- and
- (3) substituted or unsubstituted heteroaryl;
- R4 is H or substituted or unsubstituted C1-C6-alkyl;
- A is —C(R1a, R2a)N(R4a, R5a);
- wherein R1a, R2a, R4a, and R5a are independently selected from the group consisting of
- (1) H;
- and
- (2) substituted and unsubstituted C1-C6-alkyl.
16 more elements
A compound according to the formula IA:
- or a stereoisomer, pharmaceutically acceptable salt, ester, or prodrug thereof,
- wherein
- D is absent or selected from the group consisting of
- (1) substituted or unsubstituted C3-C8-cycloalkyl;
- (2) substituted or unsubstituted aryl;
- (3) substituted or unsubstituted heterocyclyl;
- and
- (4) substituted or unsubstituted heteroaryl;
- Y is an unsubstituted aryl;
- R4 is H or substituted or unsubstituted C1-C6-alkyl;
- and
- A is —CH2OH.
9 more elements
A compound according to the formula IA:
- or a stereoisomer, pharmaceutically acceptable salt, ester, or prodrug thereof,
- wherein
- D is absent or selected from the group consisting of
- (1) substituted or unsubstituted C3-C8-cycloalkyl;
- (2) substituted or unsubstituted aryl;
- (3) substituted or unsubstituted heterocyclyl;
- and
- (4) substituted or unsubstituted heteroaryl;
- Y is selected from the group consisting of
- (1) substituted or unsubstituted aryl;
- and
- (2) unsubstituted heterocyclyl;
- and
- (3) unsubstituted heteroaryl;
- R4 is H or substituted or unsubstituted C1-C6-alkyl;
- and
- A is —CH(CH3)OH.
14 more elements
A compound according to the formula IA:
- or a stereoisomer, pharmaceutically acceptable salt, ester, or prodrug thereof,
- wherein
- D is selected from the group consisting of
- (1) substituted or unsubstituted C3-C8-cycloalkyl;
- (2) substituted or unsubstituted aryl;
- (3) substituted or unsubstituted heterocyclyl;
- and
- (4) substituted or unsubstituted heteroaryl;
- Y is selected from the group consisting of
- (1) substituted or unsubstituted C3-C8-cycloalkyl;
- (2) substituted or unsubstituted aryl;
- (3) substituted or unsubstituted heterocyclyl;
- and
- (4) substituted or unsubstituted heteroaryl;
- R4 is H or substituted or unsubstituted C1-C6-alkyl;
- A is selected from the group consisting of
- (1) —C(R1a, R2a)OR3a;
- and
- (2) —C(R1a, R2a)N(R4a, R5a);
- wherein R1a, R2a, R3a, R4a, and R5a are independently selected from the group consisting of
- (1) H;
- and
- (2) substituted and unsubstituted C1-C6-alkyl.
20 more elements
Dependencies are inferred from the claim text.