Compounds and compositions are disclosed in which a quaternized drug unit is linked to a targeting ligand unit from which a tertiary amine-containing drug is released at the targeted site of action. An exemplary composition of the invention is represented by the structure: wherein “Ligand” is a Ligand Unit from a targeting moiety, which selectively binds to a target moiety, wherein the targeting moiety is an antibody, a receptor ligand or transporter substrate and the target moiety is an antigen, receptor or transporter on hyper-proliferating cells, hyper-stimulated immune cells, or other abnormal or unwanted cells or on cells characteristic of the environment of these abnormal cells, D+ is the quaternized drug unit that is released upon processing of a cleavable unit of which Q1 or Q2 is comprised and wherein Lb, R’, J, V, Z1, Z2, Z3 and p are as disclosed in the specification. Methods for treating diseases characterized by the targeted abnormal cells, such as cancer or an autoimmune disease using the compounds and compositions of the invention are also disclosed.本發明揭示化合物及組合物,其中四級銨化藥物單元與靶向配位體單元連接,該靶向配位體單元在標的作用位點處釋放含三級胺之藥物。本發明之例示性組合物由以下結構表示:其中「配位體」為來自靶向部分之配位體單元,其選擇性地結合至目標部分,其中該靶向部分為抗體、受體配位體或轉運體受質且該目標部分為過度增殖性細胞、過度刺激之免疫細胞或其他異常或非所需細胞上或在此等異常細胞之環境所特有之細胞上的抗原、受體或轉運體,D+為在加工處理包含Q1或Q2之可裂解單元後釋放的四級銨化藥物單元;且其中Lb、R、J、V、Z1、Z2、Z3及p如本說明書中所揭示。本發明亦揭示用於使用本發明之化合物及組合物來治療其特徵在於標的異常細胞之疾病(諸如癌症或自體免疫疾病)的方法。
