Penicillin derivatives and process for preparation of the same

Details Penicillin derivatives and process for preparation of the same Penicillin derivatives and process for preparation of the same

A - Human Necessities

61

K

167/187

A61K 31/43 (2006.01)

Patent

CA 1224151

ABSTRACT OF THE DISCLOSURE A pharmaceutical composition useful for treating bacterial infections in mammals which comprises (A) a .beta.- lactam antibiotic and (B) a compound of the formula Image (I) wherein R1 is hydrogen or trialkylsilyl; R2 is hydrogen, trialkylsilyl or COOR2' wherein R2' is hydrogen, C1-18 alkyl, C2-7 alkoxymethyl, C3-8 alkylcarbonyloxymethyl, C4-9 alkylcarbonyloxyethyl, (C5-7 cycloalkyl)carbonyloxymethyl, C9-14 benzylcarbonyloxyalkyl, C3-8 alkoxycarbonylmethyl C4-9 alkoxycarbonylethyl, phthalidyl, crotonolacton-4-yl, .gamma.- butyrolacton-4-yl, halogenated C1-6 alkyl substituted with 1 to 3 halogen atoms, C1-6 alkoxy- or nitro-substituted or unsubstituted benzyl, benzhydryl, tetrahydropyranyl, di- methylaninoethyl, dimethylchlorosilyl, trichlorosilyl, (5- substituted C1-6 alkyl or phenyl or unsubstituted-2-oxo-1, 3-dioxoden-4-yl)methyl, C8-13 benzoyloxyalkyl or group for forming a pharmaceutically acceptable salt; and R3 has the same meaning as above R2', the weight ratio of (A)/(B) being 0.1 to 10, said .beta. -lactam antibiotics being selected from the group consiting of penicillins such as ampicillin, amoxicillin, hetacillin, ciclaciIlin, mecillinam, carbeni- cillin, sulbenicillin, ticarcillin, piperacillin, apalcil- lin, methicillin, mezocillin, bacampicillin, carindacillin, talampicillin, carfecillin and pivmecillinam; cephalosporins such as cephaloridine, cephalothin, cephapirin, cephace- trile, cefazolin, cephalexin, cefradine, cefotiam, cefaman- dole, cefuroxime, cefoxitin, cefmetazole, cefsulodin, cefo- perazone, cefotaxime, ceftizoxime, cefmenoxime, latamoxef, cefaclor, cefroxadine, cefatrizine, cefadroxil and cephalo- glycin; and pharmaceutically acceptable salts thereof.

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