Claims
- 1. A method of treating hypertension in a warm-blooded animal in need of such treatment comprising administering to the animal in an amount effective to lower the animal's blood pressure a compound of the formula: ##STR79## or a pharmaceutically suitable salt thereof, wherein A is a carbon-carbon single bond, CO, O, NHCO, or OCH.sub.2 ;
- R.sup.1 is alkyl of 2 to 6 carbon atoms, alkenyl or alkynyl of 3 to 6 carbon atoms, or (CH.sub.2).sub.n OR.sup.4 provided that when R.sup.1 is (CH.sub.2).sub.n OR.sup.4 then R.sup.2 is H, alkyl of 2 to 6 carbon atoms, or alkenyl or alkynyl of 3 to 6 carbon atoms;
- R.sup.2 is H, alkyl of 2 to 6 carbon atoms, alkenyl or alkynyl of 3 to 6 carbon atoms; --(CH.sub.2).sub.n OR.sup.4 ; --(CH.sub.2m COR.sup.6 ; --(CH.sub.2).sub.n OCOR.sup.4 ; --(CH.sub.2).sub.n S(O) R.sup.4 ; --(CH.dbd.CH(CH.sub.2).sub.m CR.sup.4 HOR.sup.12 ; --CH.dbd.CH(CH.sub.2).sub.m COR.sup.6 ; --(CH.sub.2).sub.n NHCOOR.sup.11 ; --(CH.sub.2).sub.n NHSO.sub.2 R.sup.11 ; --(CH.sub.2).sub.n F; or ##STR80## R.sup.3 is CO.sub.2 H, --NHSO.sub.2 CF.sub.3 ; or ##STR81## R.sup.4 is H or alkyl of 1-4 carbon atoms; R.sup.5 is H, halogen, NO.sub.2, methoxy, or alkyl of 1 to 4 carbon atoms;
- R.sup.6 is H, alkyl of 1 to 6 carbon atoms; cycloalkyl of 3 to 6 carbon atoms, (CH.sub.2).sub.m C.sub.6 H.sub.5, OR.sup.7 or NR.sup.8 R.sup.9 ;
- R.sup.7 is H, alkyl of 1 to 5 carbon atoms; cycloalkyl of 3 to 6 carbon atoms; phenyl or benzyl;
- R.sup.8 and R.sup.9 are independently H, alkyl of 1 to 4 carbon atoms, phenyl, or benzyl; or NR.sup.8 R.sup.9 taken together form a ring of the formula: ##STR82## O is NR.sup.10, O or CH.sub.2 ; R.sup.10 is H, alkyl of 1 to 4 carbon atoms or phenyl;
- R.sup.11 is alkyl of 1 to 6 carbon atoms or perfluoroalkyl of 1 to 6 carbon atoms or (CH.sub.2).sub.p C.sub.6 H.sub.5 ;
- R.sup.12 is H, alkyl of 1 to 4 carbon atoms, or acyl of 1 to 4 carbon atoms;
- m is 0 to 6;
- n is 1 to 6;
- p is 0 to 3;
- r is 0 to 1;
- t is 0 to 2.
- 2. The method of treatment of claim 1 wherein for the formula:
- A is a carbon-carbon single bond or NHCO;
- R.sup.1 is alkyl, alkenyl or alkynyl, each of 3 to 5 carbon atoms;
- R.sup.2 is H, alkyl, alkenyl or alkynyl, each of 3 to 5 carbon atoms;
- --(CH.sub.2).sub.n OR.sup.4 ; --(CH.sub.2).sub.m COR.sup.6 ; --(CH.sub.2).sub.n OCOR.sup.4 ;
- --CH.dbd.CH(CH.sub.2).sub.m CR.sup.4 HOR.sup.12 ; --CH.dbd.CH(CH.sub.2).sub.m COR.sup.6 ;
- --(CH.sub.2).sub.n NHCOOR.sup.11 ; --(CH.sub.2).sub.n NHSO.sub.2 R.sup.11 ; --(CH.sub.2).sub.n F; or ##STR83## R.sup.4 is H or CH.sub.3 ; R.sup.5 is H;
- R.sup.6 is H, alkyl of 1 to 6 carbon atoms; OR.sup.7 or NR.sup.8 R.sup.9 ;
- R.sup.7 is alkyl of 1 to 5 carbon atoms;
- R.sup.8 and R.sup.9 are independently H or alkyl of 1 to 4 carbon atoms; or NR.sup.8 R.sup.9 taken together form a ring of the formula: ##STR84## R.sup.11 is alkyl of 1 to 4 carbon atoms, CF.sub.3 or phenyl; m is 0 to 3;
- n is 1 to 3;
- or a pharmaceutically suitable salt thereof.
- 3. The method of treatment of claim 2 wherein,
- A is a carbon-carbon single bond;
- R.sup.1 is alkyl or alkenyl of 3 to 5 carbon atoms;
- R.sup.2 is alkyl or alkenyl of 3 to 5 carbon atoms; --CH.sub.2 OR.sup.4 ; --COR.sup.6 ; --CH.sub.2 COR.sup.6 ; --CH.sub.2 OCOR.sup.4 ; or --CH.sub.2 NHCOOR.sup.11 ;
- R.sup.6 is H, alkyl of 1 to 4 carbon atoms or OH; or a pharmaceutically suitable salt thereof.
- 4. The method of treatment of claim 3 wherein the compound is 5-butyl-1-[(2'-carboxybiphenyl-4-yl)methyl]-1,2,3-triazole, or a pharmaceutically suitable salt thereof.
CROSS-REFERENCE TO RELATED APPLICATIONS
This is a division of application Ser. No. 07/279,193, filed Dec. 6, 1988, now U.S. Pat. No. 5,015,651, which is a continuation-in-part of U.S. application Ser. No. 07/141,669, filed Jan. 7,1988, now abandoned.
US Referenced Citations (12)
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EPX |
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Non-Patent Literature Citations (3)
Entry |
Biagi et al., "1-(4-Substituted-benzyl)-1,2,3-triazoles, etc" CA 104 : 122573a (1986). |
Pals, et al., Cir. Res., 29, 673 (1971). |
Streeten & Anderson, Handbook of Hypertension, vol. 5, Clinical Pharmacology of Antihypertensive Drugs, A. E. Doyle (Ed.) Elsevier Sci. Publ. BV., p. 246 (1984). |
Divisions (1)
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Number |
Date |
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Parent |
279193 |
Dec 1988 |
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Continuation in Parts (1)
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141669 |
Jan 1988 |
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