1-(DIALKYLAMINOALKYL)-5-(3-PHENYL-5-OXA-2,4-DIAZOL

专利名称：1-(DIALKYLAMINOALKYL)-5-(3-PHENYL-5-OXA-2,4-DIAZOLYL)-BIGUANIDES

发明人：ARON SAMUEL J,FR申请号：US28219472申请日：19720811公开号：US3808224A公开日：19740430

摘要：1351025 Oxadiazol - 5 - yl - biguanides J M D ARON-SAMUEL 18 Aug 1972 [20Aug 1971] 39234/71 Heading C2C Novel compounds (I) their quaternary ammoniumderivatives and acid addition salts in which R 1 , R 2 , R 3 , R 4 , R 5 are selected fromhydrogen, halo, alkyl, alkoxy, monohalo or polyhalo-alkyl or two adjacent groups mayform an alkylene-dioxy bridge and R is (a) NR 6 R 7 in which R 6 , R 7 are hydrogen, alkyl,allyl or a heterooyclic group optionally substituted by an alkyl group or together withthe N atom form a 5- or 6-membered heterocycle which may contain another

heteroatom and may be substituted by at least one group selected from alkyl, hydroxy,alkoxy phenyl, alkylphenyl and haloalkylphenyl or (b) n which R 8 is hydrogen or alkyl, Ais straight or branched chain alkylene and R 9 and R 10 are alkyl or together with the Natom form a 5-7 membered heterocycle which may be substituted by at least one alkylgroup and may contain another heteroatom, are prepared by reaction of a biguanide (II)with an oxadiazole derivative in which X is halogen or tri-halomethyl. Preferredcompounds include 1 - (3 - dibutylaminopropyl) - 5 - (3 - phenyl - 5 - oxadiazolyl)-biguanide, 1 - morpholino - 5 - (3 - phenyl - 5- oxadiazolyl) - biguanide, 1 - (5 -diethylamino- 2 - pentyl) - 5 - (3 - phenyl - 5 - oxadiazolyl)- biguanide, 1 - (3 -

dibutylaminopropyl)- 5 - (3- m - chlorophenyl - 5 - oxadiazolyl) - biguanide and 1 - [(4 -hydroxy - 4 - p - chlorophenyl)- piperidino] - 5 - (3 - phenyl - 5 - oxadiazolyl)- biguanide.Compounds (I) have anti-spasmodic properties, analgesic, anti-inflammatory andantimalarial action and form with a carrier a pharmaceutical preparation which may beadministered orally, parenterally or rectally.

申请人：ARON SAMUEL J,FR

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