申请人:Whitby Research, Inc.
公开号:US05274003A1
公开(公告)日:1993-12-28
Optically active or racemic compounds are provided having the formula ##STR1## where R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H and OH with the provision that at least one of R.sub.2, R.sub.3 and R.sub.4 is H, that R.sub.2 and R.sub.4 are not both OH; X is oxygen; and R.sub.1 is selected from the group consisting of ##STR2## wherein Z is oxygen, nitrogen or sulfur, wherein Y is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido, halogen, hydrocarbyl and heteroatom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12 carbon atoms, and a is an integer of from zero to 3. These compounds are capable of binding selectivity of one or more dopamine D.sub.2 receptors, for instance, in humans. They are useful in treatment of disorders of the central nervous, cardiovascular, and endocrine systems, such as elevated intraocular pressure, schizophrenia and Parkinsonism, and for inducing anorexia and weight loss in humans and other mammals.
提供具有以下式子的旋光性或外消旋化合物:##
STR1## 其中R.sub.2、R.sub.3和R.sub.4分别选择自H和OH的组,但至少其中一个为H,且R.sub.2和R.sub.4不同时为OH;X为
氧;R.sub.1选择自下列组:##
STR2## 其中Z为
氧、
氮或
硫,Y选择自羟基、硝基、
氰基、
叠氮基、
氨基、
酰胺基、
羧酸胺基、三
氟甲基、
硫酸酯、磺
酰胺基、卤素、烃基和取代烃基基团,其中所述的杂原子选择自卤素、
氮、
氧、
硫和
磷的组,所述的烃基基团包含1至12个
碳原子,且a为0至3的整数。这些化合物能够选择性地结合一种或多种
多巴胺D.sub.2受体,例如在人体中。它们在治疗中枢神经、心血管和内分泌系统的疾病方面有用,例如高眼压、精神分裂症和帕
金森病,并可诱导人类和其他哺乳动物的厌食和减重。