Patent DE-19843383-A1 (DE)
Title: New amino and imino substituted organo-phosphorus compounds useful in medicine against viral, bacterial, fungal and parasiticidal infections and as herbicides, plant fungicides and plant bactericides
Inventor: JOMAA HASSAN
IPC: C07F9/6506
Filed: 1998-09-22
Abstract: Amino and imino substituted organo-phosphinoyl, organo-phosphinic acid and organo-phosphonic acid derivatives are new. Pharmaceutical preparations containing compounds (I) and a broad range of other pharmaceutically active substances are also new.  The derivatives are compounds (I) and their salts, esters, amides and ester salts:  R3 and R4  = H; optionally substituted alkyl, hydroxyalkyl, alkenyl or alkynyl with up to 26C; optionally substituted aryl, acyl, aralkyl, cycloalkyl or heterocyclyl; halo; OX3; or OX4; X3 and X4  = H; optionally substituted alkyl, hydroxyalkyl, alkenyl or alkynyl with up to 26C; optionally substituted aryl, aralkyl, cycloalkyl or heterocyclyl; silyl; an organic or inorganic cation, especially a group Ia, IIa or IIIa metal, optionally substituted ammonium or an ammonium group derived from ethylenediamine or an amino acid;  B  = N(R1)(R2)-A-; or R1-N=A-;  A  = alkyleneamino, alkenyleneamino, hydroxyalkyleneamino, alkyleneimino, alkenyleneimino or hydroxyalkyleneimino in which the N atom bonds the P atom to N(R1)(R2) or to R1-N=;  R1 and R2  = H; optionally substituted alkyl, hydroxyalkyl, alkenyl, alkynyl, aryl, acyl, cycloalkyl, aralkyl or heterocyclyl; halo; OX1; or OX2;  X1 and X2  = H; or optionally substituted alkyl, hydroxyalkyl, alkenyl, alkynyl, aryl, acyl, cycloalkyl, aralkyl or heterocyclyl. Independent claims are also included for a pharmaceutical preparation containing a compound (I) and optionally:  (a) sulfadoxine, artemisinine, atovaquone, quinine, chloroquine, hydroxychloroquine, mefloquine, halofantrine, pyrimethamine, armesine, tetracycline, doxycycline, proguanil, metronidazole, praziquantil, niclosamide, mebendazole, pyrantel, tiabendazole, diethylcarbazine, piperazine, pyrivinium, metrifonate, oxamniquine, bithional or suramin; or  (b) penicillin, benzylpenicillin, phenoxypenicillins, isoxazolylpenicillins, aminopenicillins, ampicillin, amoxicillin, bacampicillin, carboxypenicillin, ticarcillin, temocillin, acylaminopenicillins, azlocillin, mezlocillin, piperacillin, apalcillin, mecillinam, cefoxitin, cefotetan, cefmetazole, latamofex, flomoxef, cefozidime, ceftazidime, cefpirome, cefepime, cefsulodin cefoperazone, loracarbef, cefprozil, cefixime, cefpodoxime proxetil, cefuroxime axetil, cefetamet, cefotiam hexetil, cefdinir, cefibuten, carbapenem, imipenem/cilastatin, meropenem, biapenem, aztreonam, clavulanic acid/amoxycillin, clavulanic acid/ticarcillin, sulbactam/ampicillin, tazobactam/piperacillin, oxytetracycline, rolitetracycline, minocycline, chloramphenicol, gentamycin, tobramycin, netilmycin, amikacin, spectionomyxin, erythromycin, clarithromycin, roxithromycin, azithromycin, dirithromycin, spiramycin, josamycin, lincosamide, clindamycin, fusidic acid, vancomycin, tecoplanin, fosfomycin, co-trimoxazole, trimethoprim, nitrofurantoin, nitrofurazone, norfloxacin, ciprofloxacin, ofloxacin, sparfloxacin, enoxacin, fleroxacin, pefloxacin, lomefloxacin, Bay Y3118, isoniazid, rifampicin, rifabutin, ethambutol, pyrazinamide, streptomycin, capreomycin, prothionamide, terizidone, dapsone, clofazimine, bacitracin, tyrothricin, neomycin, kanamycin, paromomycin, mupirocin, acyclovir, ganciclovir, azidothymidine, didanosine, zalcitabin, thiacytidine, stavudin, ribavirin, idoxuridine, trifluridine, foscarnet, amantadine, interferons, amphotericin B, nystatin, natamycin, miconazole, ketoconazole, itraconazole, fluconazole, UK-109,496, clotrimazole, econazole , isoconazole, oxiconazole, bifonazole, flucytosine, griseofulvin, ciclopiroxolamine, tolnaftate, naftifine, terbinafine, amorolfine, betulinic acid, quinidine, amodiaquine, acridine, benzonaphthyridine, mepacrine, pyronaridine, sulfadoxine, sulfalene, trimethoprim, primaquine, aminoquinolines, WR 238,605, dihydroartemisinin, 10b artemether, arteether, artesunate, atovaquone, melarsoprol, nifurtmox, stibogluconate sodium, pentamidine, clioquinol, ivermectin or embonate.