Compounds of structural formula (I): ##STR1## are squalene synthestase inhibitors useful in inhibiting the biosynthesis of cholesterol in the treatment of hypercholesterolemia and related disorders.
This invention is directed to a continuous fluorescence assay of Ras farnesyl:protein transferase. This assay can be used to screen for inhibitors of farnesyl:protein transferase. The assay may also be modified to screen for inhibitors of other protein transferases.
The present invention provides an excellent squalene synthesizing enzyme inhibitor. Specifically, it provides a compound (I) represented by the following formula, a salt thereof or a hydrate of them. ##STR1## In which R.sup.1 represents (1) hydrogen atom or (2) hydroxyl group; HAr represents an aromatic heterocycle which may be substituted with 1 to 3 groups; Ar represents an optionally substituted aromatic ring; W represents a chain represented by (1) --CH.sub.2 --CH.sub.2 -- which may be substituted, (2) --CH.dbd.CH-- which may be substituted, (3) --C.ident.C--, (4) --NH--CO--, (5) --CO--NH--, (6) --NH--CH.sub.2 --, (7) --CH.sub.2 --NH--, (8) --CH.sub.2 --CO--, (9) --CO--CH.sub.2 --, (10) --NH--S(O).sub.l --, (11) --S(O).sub.l --NH--, (12) --CH.sub.2 --S(O)-- or (13) --S(O).sub.l --CH.sub.2 -- (l denotes 0, 1 or 2); and X represents a chain represented by (1) a single bond, (2) an optionally substituted C.sub.1-6 alkylene chain, (3) an optionally substituted C.sub.2-6 alkenylene chain, (4) an optionally substituted C.sub.2-6 alkynylene chain, (5) a formula --Q-- (wherein Q represents oxygen atom, sulfur atom, CO or N(R.sup.2) (wherein R.sup.2 represents a C.sub.1-6 alkyl group or a C.sub.1-6 alkoxy group)), (6) --NH--CO--, (7) --CO--NH--, (8) --NH--CH.sub.2 --, (9) --CH.sub.2 --NH--, (10) --CH.sub.2 --CO--, (11) --CO--CH.sub.2 --, (12) --NH--S(O).sub.m --, (13) --S(O).sub.m --NH--, (14) --CH.sub.2 --S(O).sub.m --, (15) --S(O).sub.m --CH.sub.2 -- (wherein m denotes 0, 1 or 2) or (16) --(CH.sub.2).sub.n --O-- (wherein n denotes an integer from 1 to 6).
An apparatus for converting an optical wave having a relatively smaller cross section into an optical wave having a relatively larger cross section which may be manufactured in a monolithically integrated fashion in a simple way. In this apparatus, a wave-guiding, rib-shaped taper having an end for coupling the optical wave with a small cross section into the taper is fashioned on a rib of a rib waveguide which guides the optical wave. An optical wave having a larger cross section is fashioned thereon in a longitudinal direction of the rib. The infeed end of the taper and the taper itself has a smaller breadth in comparison to the breadth of the rib of the rib waveguide. Proceeding from this end, the taper broadens and decreasingly tapers in thickness in the longitudinal direction of the rib waveguide.
This invention relates to a class of novel aliphatic amino bis-aryl compounds containing at least four carbon atoms and an amino group either substituted thereon or incorporated therein and is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
This invention relates to a class of novel polycyclic compounds containing a cycloalkyl ring having substituted thereon a primary amine and which is further linked or bridged to two mono- and/or bicyclic rings and which reduces levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.