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Pub. No.:    WO/1997/010223    International Application No.:    PCT/US1996/014135
Publication Date: 20.03.1997 International Filing Date: 09.09.1996
Chapter 2 Demand Filed:    03.04.1997    
C07D 263/20 (2006.01), C07D 413/10 (2006.01), C07D 413/12 (2006.01), C07D 417/10 (2006.01), C07D 491/08 (2006.01), C07D 491/10 (2006.01), C07D 495/08 (2006.01)
Applicants: PHARMACIA & UPJOHN COMPANY [US/US]; 301 Henrietta Street, Kalamazoo, MI 49001 (US) (For All Designated States Except US).
GADWOOD, Robert, C. [US/US]; (US) (For US Only).
KAMDAR, Bharat, V. [US/US]; (US) (For US Only)
Inventors: GADWOOD, Robert, C.; (US).
KAMDAR, Bharat, V.; (US)
Agent: GAMMILL, Martha, A.; Pharmacia & Upjohn Company, Intellectual Property Legal Services, 301 Henrietta Street, Kalamazoo, MI 49001 (US).
PERRY, Robert, Edward; Gill Jennings & Every, Broadgate House, 7 Eldon Street, London EC2M 7LH (GB)
Priority Data:
60/003,838 15.09.1995 US
Abstract: front page image
(EN)The present invention provides for aminoaryl oxazolidinone N-oxide compounds of formula (I), wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines $i(in vivo), making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as $i(Bacteroides spp.) and $i(Clostridia spp.) species, and acid-fast organisms such as $i(Mycobacterium tuberculosis), $i(Mycobacterium avium) and $i(Mycobacterium spp.), and in organisms such as $i(Mycoplasma spp.).
(FR)Composés d'aminoaryle oxazolidinone N-oxyde de formule (I) dans laquelle les variables sont telles que définies dans le descriptif. Ces composés sont excessivement solubles dans l'eau, ce qui les rend très utiles pour préparer des compositions pharmaceutiques avec lesdits composés. Ils sont également rapidement retransformés en amines $i(in vivo), ceci permettant de les utiliser comme promédicaments des amines. Ils sont efficaces contre un certain nombre de pathogènes s'attaquant à l'homme et aux animaux, y compris les bactéries aérobies à gram positif telles que les entérocoques, les streptocoques et les staphylocoques polyrésistants ainsi que les organismes anaérobies tels que les espèces $i(Bacteroides spp.) et $i(Clostridia spp.), et les organismes acido-résistants tels que $i(Mycobactérium tuberculosis), $i(Mycobactérium avium) et $i(Mycobactérium spp.) et dans des organismes tels que $i(Mycoplasma spp.).
Designated States: AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CZ, DE, DK, EE, ES, FI, GB, GE, HU, IL, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, TJ, TM, TR, TT, UA, UG, US, UZ, VN.
African Regional Intellectual Property Organization (KE, LS, MW, SD, SZ, UG)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)