Abstract:
PROBLEM TO BE SOLVED: To provide a substituted 2,5-diamino-3-hydroxyhexane useful for producing HIV protease inhibitors, and to provide a method for producing the compound. SOLUTION: The substituted 2,5-diamino-3-hydroxyhexane useful for producing HIV protease inhibitors is represented by general formula I. COPYRIGHT: (C)2006,JPO&NCIPI
Abstract:
Disclosed herein is a process for the preparation of erythromycin derivatives, or pharmaceutically acceptable salts thereof, which contain an optionally substituted propargyl group at the 6-O-position.
Abstract:
A process for the preparation of a compound having formula (a) wherein R1, R2, R3, R4, and R5 are defined, from an enamine by chain expansion and ring closure followed by additional derivatization, treatment with a 3-alkoxyl-acryloyl compound, another ring closure, and converting a hydroxyl group to a leaving group.
Abstract:
A process for the preparation of a compound having the formula: wherein R1, R2, R3, R4, and R5 are defined, from an enamine by chain expansion and ring closure followed by additional derivatization, treatment with a 3-alkoxyl-acryloyl compound, another ring closure, and converting a hydroxyl group to a leaving group.
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.
Abstract:
Disclosed herein is a process for the preparation of erythromycin derivative s, or pharmaceutically acceptable salts thereof, which contain an optionally substituted propargyl group at the 6-O- position.
Abstract:
Processes are disclosed which are useful for the preparation of a substantially pure compound of formula (3), wherein R6 and R7 are each hydrogen or R6 and R7 are independently selected from (i), wherein Ra and Rb are independently selected from hydrogen, loweralkyl and phenyl and Rc, Rd and Re are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and (ii) wherein the naphthyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy, and halo; or R6 is as defined above and R7 is R7aOC (O)- wherein R7a is loweralkyl or benzyl; or R6 and R7 taken together with the nitrogen atom to which they are bonded are (a) or (b), wherein Rf, Rg, Rh and Ri are independently selected from hydrogen, loweralkyl, alkoxy, halogen, and trifluoromethyl and R8 is hydrogen or -C(O)R'' wherein R'' is loweralkyl, alkoxy, benzyloxy or phenyl wherein the phenyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or an acid addition salt thereof.
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