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US 7,732,612 B2Granted
7-amino alkylidenyl-heterocyclic quinolones and naphthyridones
AssigneeJanssen Pharmaceutica NV
InventorsEugene B. Grant, Mark J. Macielag, Steven David Paget, Michele Ann Weidner-Wells, Xiaoqing Xu, Xiaodong Xu
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Abstract
The present invention relates to compounds having a structure according to Formula I wherein n, m, z, R, R2, R3, R4, R5, R6, A, E, X, Y, a and b are as defined above; or an optical isomer, diastereomer or enantiomer thereof; a pharmaceutically acceptable salt, hydrate, or prodrug thereof.
Claims12
A compound having a structure according to Formula I:
- wherein:
- n is an integer from 1 to 3;
- m is an integer from 1 to 3;
- z is an integer from 0 to 3;
- R is selected from hydrogen, hydroxy, and alkoxy;
- R2 is hydrogen;
- R3 and R4 are independently selected from hydrogen, halogen, amino, hydroxy, alkoxy, alkylthio, alkyl, alkenyl and alkynyl;
- R5 is selected from hydrogen, hydroxy, halogen, alkyl, aryl, alkoxy, cyano, CO2R13, and alkylthio;
- R6 is independently selected from alkyl, hydroxy, alkoxy, alkylthio, alkenyl, alkynyl, aryl, alkoxyimino, and halogen;
- or R5 and R6 join to form a 4- to 7-membered carbocyclic ring wherein each carbon atom of the ring can be optionally substituted with R12, wherein R12 is selected from the group consisting of halogen, amino, hydroxy, alkoxy, alkylthio, alkyl, alkenyl, alkynyl, oxo, alkoxyimino and hydroxyimino;
- R13 is hydrogen, alkyl, aryl, or a carboxylic acid protecting group;
- E is selected from the group consisting of:
- wherein,
- q is an integer from 1 to 3;
- R7 and R8 are each independently selected from hydrogen and alkyl, or R7 and R8 join to form a 3 to 6 membered carbocyclic ring, or either of R7 or R8 can be joined independently to either of R9 or R10 to form a heterocyclic ring containing the nitrogen atom to which R9 or R10 are bonded, wherein
- R9 and R10 are each independently selected from hydrogen, alkyl, arylalkyl, acyl, alkoxycarbonyl, or sulfonyl, or alternatively R9 and R10 join to form a heterocyclic ring containing the nitrogen atom to which they are bonded;
- wherein,
- q is as defined above;
- R7 and R8 are each independently selected from hydrogen and alkyl, or R7 and R8 join to form a 3- to 6-membered carbocyclic ring, and R9 is selected from hydrogen, alkyl, acyl, alkoxycarbonyl, or sulfonyl;
- and
- 3) alkenyl;
- A is C(R11), wherein R11 is selected from hydrogen, alkyl, halogen, hydroxy, alkoxy, alkylthio, and cyano;
- X is C, a is a double bond and b is a single bond;
- and
- Y is N(R1), wherein R1 is selected from C3 to C6 cycloalkyl, C4 to C6 heterocycloalkyl, alkyl, alkene, a 6-membered aryl and a 6-membered heteroaryl;
- or an optical isomer, diastereomer or enantiomer thereof;
- or a pharmaceutically acceptable salt, thereof.
24 more elements
Dependencies are inferred from the claim text.