The invention relates to tetrahydroisoquinoline derivatives of the Formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of a hydrogen and a hydroxyl group. These derivatives are useful in tocology (obstetrics). Administration of the inventive compounds induces relaxation of uterine muscles, a property that is particularly useful in cases of second trimester miscarriage, premature birth up to the 37th or 38th week of pregnancy, and during delivery. The compounds are especially useful from the onset of labor up to delivery of the newborn's head, a period which is often accompanied or complicated by frequent, violent, uncoordinated contractions of the uterus. The compounds are also useful in obstetric and gynecological operations, such as a hysterectomy, surgery for acute placental insufficiency, etc.
The invention concerns a method for treating pain and/or CNS disorders characterized in that the method uses a compound which acts selectively as an antagonist of gamma aminobutyric acid (GABA) at GABA autoreceptors relative to GABA.sub.A receptors.
The invention provides .beta..sub.3 -adrenoreceptor agonists, pharmaceutical compositions comprising .beta..sub.3 -adrenoreceptor agonist compounds, and methods of using such compounds for stimulating, regulating or modulating metabolism of fats in adipose tissue in animals.
The invention provides .beta..sub.3-adrenoreceptor agonists, pharmaceutical compositions comprising .beta..sub.3-adrenoreceptor agonist compounds, and methods of using such compounds for stimulating, regulating or modulating metabolism of fats in adipose tissue in animals.
The invention provides compounds of formula: ##STR1## wherein R.sub.1 is --NHS(O).sub.m R, wherein R is alkyl, substituted alkyl, alkoxy, substituted alkoxy, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycle, or substituted heterocycle; X is independently selected from the group consisting of halo, alkyl, substituted alkyl, alkoxy, substituted alkoxy, hydroxy, nitro, amino, and substituted amino; R.sub.2 is benzyl or benzyl substituted with one or more substituents selected from the group consisting of halo, CF.sub.3, hydroxy, nitro, alkoxy, substituted alkoxy, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycle, substituted heterocycle, amino, and substituted amino of formula --NHR' or --NR'R', wherein each R' is alkyl, substituted alkyl, --C(O)Y, --C(O)NHY, or --C(O)SY, wherein Y is alkyl or substituted alkyl; R.sub.3 is H or alkyl; n is 0-3; m is 1-2; p is 1-4; the sum of n and p is 1-4; and pharmaceutically acceptable salts thereof.
The invention provides compounds useful as .beta..sub.3 -adrenorecptor agonists and pharmaceutical compositions comprising such compounds. The invention further includes a method for stimulating, regulating, and modulating metabolism in fats of adipose tissue in mammals by administering an effective amount of a compound of the invention.
