Quinolylpropylpiperidine derivatives, intermediates and...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C514S323000, C546S200000, C546S236000

Reexamination Certificate

active

10659164

ABSTRACT:
Quinolylpropylpiperidine derivatives of general formula (I) in which R1is hydrogen or fluorine, R2is carboxyl, carboxymethyl or hydroxymethyl, R3is alkyl substituted either with phenylthio optionally substituted with halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkyloxycarbonyl, cyano or amino, or with cycloalkylthio (3 to 7 members) optionally substituted with halogen or trifluoromethyl, or with heteroarylthio (5 to 6 members and 1 to 4 heteroatoms chosen from N, O and S), optionally substituted with halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkyloxycarbonyl, cyano or amino or R3is propargyl substituted by phenyl or heteroaryl as defined above and R4is alkyl, alkenyl-CH2— or alkynyl-CH2—, cycloalkyl or cycloalkylalkyl, in their various isomeric forms, separate or as mixtures, and also their salts, their preparation process and intermediates and the compositions containing them. These novel derivatives are potent antibacterial agents

REFERENCES:
patent: 1 253 741 (1971-11-01), None
patent: WO 00/43383 (2000-07-01), None
patent: WO 01/25227 (2001-04-01), None
patent: WO 02/40474 (2002-05-01), None
Grethe, Guenter et al, “Reinvestigation of the Classical Synthesis of Cinchona Alkaloids. I. A New Synthesis of Homomeroquinene and Quinotoxine,” Helvetica Chimica Acta, vol. 56(5), 1973, pp. 1485-1494.
G. Grethe, et al., “107.Synthesis of 9-epi-Quinine and 9-epi-Quinidine,” Helvetica Chimica Acta, 55 Fasc. 3 (1972) No. 107, pp. 1044-1047.
M. Rubtsov, “Synthesis of Racemic N-Acetylhomomeroquinene,” Zhurnal Obschei Khimii, vol. 30, No. 5 (J. Gen. Chem, USSR-English translation) (1960), pp. 1514-1522.

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