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US Patent 6069145 - Piperazinonephenyloxazolidinone derivatives and their use as antibacterial agents

US Patent Issued on May 30, 2000
Estimated Patent Expiration Date: Icon_subject July 27, 2018Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
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Abstract

The invention concerns a compound of formula (I) wherein: R1 is of the formula --NHC(=O)(1-4C)alkyl, --NHS(O)n (1-4C)alkyl wherein n is 0, 1 or 2 or R1 is hydroxy; R2 and R3 are independently hydrogen or fluoro; R4 is hydrogen, methyl, ethyl or oxo; R5 is hydrogen, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or of the formula R6 (CH2)m -- wherein either m is 1-4 and R6 is, for example, trifluoromethyl, difluoromethyl, fluoromethyl, (1-4C)alkoxy, (1-4C)alkyl S(O)p -- wherein p is 0, 1 or 2, (1-6C)alkanoyloxy, di-(N-(1-4C)alkyl)amino, N-((1-4C)alkyl)(1-4C)alkanoylamino, cyano, carboxy, (1-4C)alkoxycarbonyl, carbamoyl, di-(N-(1-4C)alkyl)carbamoyl, N-((1-4C)alkyl)(1-4C)alkanesulphonamido, N1 -((1-4C)alkyl)-di-(N3 -(1-4C)alkyl)ureido, or of the formula --OC(=O)NR7 (R8) or --N(R9)SO2 NR7 (R8) wherein R7 and R8 are independently hydrogen or (1-4C)alkyl and R9 is (1-4C)alkyl; or m is 2-4 and R6 is, for example, hydroxy, (1-4C)alkanoylamino, amino, (1-4C)alkylamino, (1-4C)alkanesulphonamido, ureido, di-(N3 -(1-4C)alkyl)ureido or of the formula --NHSO2 NR7 (R8); and pharmaceutically-acceptable salts thereof; processes for their preparation; pharmaceutical compositions containing them and their use as antibacterial agents.

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Inventor

Assignee

Application

No. 117337 filed on 07/27/1998

US Classes:

514/254.02, The additional five-membered hetero ring also has chalcogen as a ring member544/3691,3-oxazole ring or 1,3-thiazole ring (including hydrogenated)

Field of Search

544/369, 1,3-oxazole ring or 1,3-thiazole ring (including hydrogenated)544/252Ring nitrogen is shared by two of the cyclos

Examiners

Primary: Bernhardt, Emily

Attorney, Agent or Firm

US Patent References

4346102, 3H-Dihydrofuranone-2 derivatives and pharmaceutical use thereof
Issued on: 08/24/1982
Inventor: Langlois ,   et al.
4705799, Aminomethyl oxooxazolidinyl benzenes useful as antibacterial agents
Issued on: 11/10/1987
Inventor: Gregory
5164510, 5'Indolinyl-5ଲ-amidomethyloxazolidin-2-ones
Issued on: 11/17/1992
Inventor: Brickner
5182403, Substituted 3(5'indazolyl) oxazolidin-2-ones
Issued on: 01/26/1993
Inventor: Brickner
5231188, Tricyclic [6.5.51]-fused oxazolidinone antibacterial agents
Issued on: 07/27/1993
Inventor: Brickner
5523403, Tropone-substituted phenyloxazolidinone antibacterial agents
Issued on: 06/04/1996
Inventor: Barbachyn
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Issued on: 06/25/1996
Inventor: Habich, et al.
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Issued on: 07/29/1997
Inventor: Brickner, et al.
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Inventor: Riedl, et al.
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Issued on: 10/27/1998
Inventor: Riedl, et al.
58614132-oxo- and 2-thio-1,2-dihydroquinolinyl-oxazolidinones
Issued on: 01/19/1999
Inventor: Habich, et al.

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International Classes

A61K 031/495
C07D 413/10

Foreign Application Priority Data

1996-01-27 GB

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