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US 6,093,744 AGranted
N-acyl sulfamic acid esters useful as hypocholesterolemic agents
AssigneeWarner-Lambert Company
InventorsHelen Tsenwhei Lee, Joseph Armand Picard, William Howard Roark, Bruce David Roth, Drago Robert Sliskovic
Life of this patent
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Abstract
The instant invention is new compounds of Formula I ##STR1## their use as cerebrovascular agents in diseases such as stroke, peripheral vascular disease, restenosis, and as agents for regulating plasma cholesterol concentrations, for treating hypercholesterolemia and atherosclerosis, and for lowering the serum or plasma level of Lp(a). A pharmaceutical composition is also claimed.
Claims16
A compound of formula ##STR4## or a pharmaceutically acceptable salt thereof wherein:
- R.sup.1 is hydrogen, alkyl, or alkoxy;
- R.sup.2 to R.sup.5 are alkyl, alkoxy, or unsubstituted or substituted phenyl;
- R.sup.6 is --CN,
- --(CH.sub.2).sub.0-1 --NR.sup.7 R.sup.8,
- --O--(CH.sub.2).sub.1-10 --Z wherein Z is --NR.sup.9 R.sup.10, OR.sup.1, or CO.sub.2 R.sup.1,
- --OC(.dbd.O)R.sup.11,
- --SR.sup.11,
- --SCN,
- --S(CH.sub.2).sub.1-10 Z,
- --S(O).sub.1-2 R.sup.12 wherein R.sup.12 is hydroxy, alkoxy, alkyl, (CH.sub.2).sub.1-10 Z or NR.sup.7 R.sup.8,
- --C(.dbd.O)XR.sup.11,
- --CH.sub.2 --R.sup.13 wherein R.sup.13 is (CH.sub.2).sub.0-5 --Y--(CH.sub.2).sub.0-5 Z, or
- wherein R.sup.7 and R.sup.8 are each independently selected from:
- --hydrogen, at least one of R.sup.7 and R.sup.8 is other than hydrogen,
- --(CH.sub.2).sub.1-10 Z wherein Z is as above and R.sup.9 and R.sup.10 are each independently selected from hydrogen, alkyl, and unsubstituted or substituted phenyl, or
- R.sup.9 and R.sup.10 are taken together with the nitrogen to which they are attached to form a ring selected from:
- --(CH.sub.2).sub.2 --O--(CH.sub.2).sub.2,
- --(CH.sub.2).sub.2 --S--(CH.sub.2).sub.2,
- --(CH.sub.2).sub.2 --CR.sup.14 R.sup.15 --(CH.sub.2).sub.1-2, and
- --(CH.sub.2).sub.2 --NR.sup.16 --(CH.sub.2).sub.2, wherein
- R.sup.14, R.sup.15, and R.sup.16 are each independently selected from hydrogen, alkyl, and unsubstituted or substituted phenyl;
- --C(.dbd.Q)XR.sup.11 wherein X is a bond or NH wherein Q is O or S,
- R.sup.11 is hydrogen, alkyl, unsubstituted or substituted phenyl,
- --(CH.sub.2).sub.0-5 --Y--(CH.sub.2).sub.0-5 Z wherein Z is as defined above and Y is phenyl or a bond;
- --C(.dbd.O)CR.sup.17 R.sup.18 Z;
- --C(.dbd.O)NRCR.sup.17 R.sup.18 Z wherein R.sup.17 and R.sup.18 are each independently hydogen, alkyl, phenyl, substituted phenyl, or the side chain of a naturally occurring amino acid;
- --S(O).sub.1-2 R.sup.19 wherein R.sup.19 is alkyl, unsubstituted or substituted phenyl, naphthyl, or a heteroaromatic ring, or NR.sup.9 R.sup.10 or
- R.sup.7 and R.sup.8 are taken together with the nitrogen to which they are attached to form a ring:
- --(CH.sub.2).sub.2 --O--(CH.sub.2).sub.2 --,
- --(CH.sub.2).sub.2 --S--(CH.sub.2).sub.2 --,
- --(CH.sub.2).sub.2 --CR.sup.14 R.sup.15 --(CH.sub.2).sub.1-2 --,
- --(CH.sub.2).sub.2 --NR.sup.16 --(CH.sub.2).sub.2 -- wherein R.sup.14, R.sup.15, and R.sup.16 are as above.
29 more elements
Dependencies are inferred from the claim text.