| 摘要 |
<p>The instant invention provides disubstituted tetrazoles that antagonizes the effect of leukotrienes C4, D4 and E4 in selected tissues. The disubstituted tetrazoles are used in pharmaceutical formulations and methods of treatment of conditions caused by excessive amounts of leukotrienes C4, D4 or E4 or any combination thereof, and have the formula: <CHEM> wherein: R1 is C1 to C3 alkyl; R2 is C1 to C6 alkyl or C3 to C6 alkenyl; R3 is a hydrogen atom, chloro, bromo, nitro, or a group of the formula -NRaRb wherein Ra and Rb are the same or different and are a hydrogen atom, C1 to C4 alkyl, phenyl, benzyl, or C1 to C4 acyl; R4 and R5 are the same or different and are a hydrogen atom or C1 to C3 alkyl; W is from one to six; Z is O, S or a group of the formula -NRe , (wherein Re is a hydrogen atom, C1 to C4 alkyl, C1 to C4 acyl, phenyl, or benzyl); n is 0 to 6; Rc and Rd are the same or different and are hydrogen, hydroxy, halo or an ether group of the formula -O-(C1 to C6 alkyl); [Tet] is a disubstituted 1H- or 2H-tetrazolyl ring of the formula <CHEM> wherein: L is 1) C1 to C10 alkylidene; or 2) a group of the formula <CHEM> wherein y is 1 to 3 (and the phenyl ring is bonded to A); A is 1) 5-(tetrazolyl); 2) carboxy; 3) -NRfRg,wherein Rf and Rg are the same or different and are a hydrogen atom, C1 to C4 alkyl, phenyl, benzyl or C1 to C4 acyl; or 4) a group of the formula <CHEM> wherein q is 0, 1 or 2 and Rh is C1 to C4 alkyl, phenyl or benzyl; or a pharmaceutically-acceptable salt thereof.</p> |
