SUBSTITUTED THIAZOLES AND PHARMACEUTICAL COMPOSITIONS

    公开(公告)号:NZ232369A

    公开(公告)日:1992-01-29

    申请号:NZ23236990

    申请日:1990-02-05

    Applicant: ABBOTT LAB

    Abstract: A composition for the inhibition of lipoxygenase enzymes comprising a pharmaceutically acceptable carrier and a compound of the formula: I wherein R1 and R2 are independently selected from the group consisting of alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, arylalkenyl, reduced heteroaryl, and reduced heteroarylalkyl and substituted derivatives thereof having one or more substituents independently selected from the group consisting of halogen, alkyl, halosubstituted alkyl, aryl, arylalkyl, reduced heteroaryl, arylalkoxy, cyano, nitro, COR4, SO2R4, NR5R6, OR6, COCX1X2NR6R7, CON(OH)R6, NR6COR4, CR5(NH2)CO2R5, NHCX1X2CO2R5, N(OH)CONR5R6, N(OH)COR4, NHCONR5R6, C(NOH)NHOH and CONHNR5R6; R3 is selected from the group consisting of hydrogen, a pharmaceutically acceptable salt, COR4, COCX1X2NR6R7, CR8R9OR10, CH2CR8(OR10)CH2OR11 and SiR12R13R14; R4 is selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced heteroaryl, reduced heteroarylalkyl, OR5, NHCX1X2CO2R5 and NR6R7; R5 is selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, reduced heteroaryl, and reduced heteroarylalkyl; R6 and R7 are independently selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, reduced heteroaryl, reduced heteroarylalkyl and (CH2)nOR5 where n is 2-4 and R5 is as defined above; R8, R9, R10 and R11 are independently selected from the group consisting of hydrogen, alkyl, aryl, arylalkyl and (CH2)nOR5 or at least two of R8, R9, R10 and R11 together form a ring system containing 5-10 atoms wherein said ring system is carbocyclic, heterocyclic or reduced heterocyclic and R5 and n are as defined above; R12, R13 and R14 are independently selected from the group consisting of alkyl and aryl; and X1 and X2 are independently selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, aryl, and arylalkyl; and the acid addition salts thereof.

    Process for preparation of 4-H-4-oxo-quinolizine-3-carboxylic acid derivatives

    公开(公告)号:NZ336876A

    公开(公告)日:2000-12-22

    申请号:NZ33687698

    申请日:1998-02-06

    Applicant: ABBOTT LAB

    Abstract: Substituted pyrazole-3-yl benzazoles of formula (I) and salts thereof wherein: R1 is H, alkyl or alkyl halide; R2 is CN, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, alkylsulphinyl, haloalkylsulphinyl, alkylsulphonyl, or haloalkylsulphonyl; R3 is H, CN, NO2, halogen, alkyl or haloalkyl; R4 is H, halogen; R5 is H, CN, halogen, alkyl, haloalkyl, alkoxy or haloalkoxy; Z is N=C(XR6)O or N=C(XR6)S, bonded to alpha by the nitrogen, oxygen or sulphur; X is a chemical bond, oxygen, sulphur, S(O), SO2, NH or N(R7); R6 and R7 are alkyl, haloalkyl, cyanoalkyl, hydroxyalkyl, alkenyl, cyanoalkenyl, haloalkenyl, alkinyl, cyanoalkinyl, haloalkinyl, alkoxyalkyl, haloalkoxyalkyl, alkenyloxyalkyl, alkinyloxyalkyl, cycloalkyloxyalkyl, aminoalkyl, alkylaminoalkyl, di(alkyl)aminoalkyl, alkylthioalkyl, haloalkylthioalkyl, alkenylthio alkyl, alkinylthioalkyl, alkylsulphinylalkyl, haloalkylsulphinylalkyl, alkenylsulphinylalkyl, alkinylsulphinylalkyl, alkylsulphonylalkyl, haloalkylsulphonylalkyl, alkenylsulphonylalkyl, alkinylsulphonylalkyl, hydroxycarbonylalkyl, alkoxycarbonylalkyl, which can carry a CN or alkoxycarbonyl group, alkylthiocarbonylalkyl, aminocarbonylalkyl, alkylaminocarbonylalkyl, di(alkyl)aminocarbonylalkyl, dialkylphosphonylalkyl, alkoxyiminoalkyl, alkenyloxyiminoalkyl, optionally substituted cycloalkyl, cycloalkylalkyl, phenyl, phenylalkyl, 3 to 7member heterocyclic or heterocyclylalkyl, wherein each cycloalkyl ring and each heterocyclyl ring contain a CO or CS ring member; if X is a chemical bond, O, S, NH or N(R7), R6 also being alkylcarbonyl, haloalkylcarbonyl, alkoxycarbonyl, alkylsulphonyl or haloalkylsulphonyl; if X is a chemical bond, R6 additionally designating CN, SH, NH2, halogen, CH2CH(halogen)R8, CH=CHR8 or CH=C(halogen)R8, or R6 plus R7 designating an optionally substituted 1,3propylene, tetramethylene, pentamethylene or ethylene oxyethylene chain R8 is COOH, alkoxycarbonyl, alkylthiocarbonyl, CONH2, alkylaminocarbonyl, dialkylaminocarbonyl or dialkylphosphonyl. These substances are useful as herbicides and for the desiccation and/or defoliation of plants

Patent Agency Ranking