The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention. For example, orexin receptor-modulatory compounds of the present invention can be used in treatment of an eating disorder, obesity, alcoholism or an alcohol-related disorder, drug abuse or addiction including addiction to cocaine, opiates, amphetamines, or nicotine, a sleep disorder, a cognitive dysfunction in a psychiatric or neurologic disorder, depression, anxiety, post-traumatic stress disorder, seasonal affective disorder, an eating disorder, panic disorder, schizophrenia, Alzheimer’s disease, Parkinson’s disease, Huntington’s chorea, headache, migraine, pain, gastrointestinal diseases, epilepsy, inflammations, immune-related diseases, endocrine-related diseases, cancer, hypertension, behavior disorder, mood disorder, manic depression, dementia, sex disorder, psychosexual disorder, or renal disease.本發明係關於調節食慾素受體(例如OX1或OX2或二者)之生物活性之化合物;包含本發明化合物之醫藥組合物及組合;治療患者之其中在醫學上適合調節食慾素受體之不良狀況的方法;及製備本發明化合物之方法。舉例而言,本發明之食慾素受體調節性化合物可用於治療飲食障礙、肥胖症、酒精中毒或酒精相關病症、藥物濫用或成癮(包括對可卡因(cocaine)、鴉片劑、安非他命(amphetamine)或尼古丁(nicotine)成癮)、睡眠障礙、精神病或神經病症中之認知功能障礙、抑鬱症、焦慮、創傷後壓力症候群、季節性情感障礙、飲食障礙、恐慌症、精神分裂症、阿茲海默氏病(Alzheimer’s disease)、帕金森氏病(Parkinson’s disease)、亨汀頓氏舞蹈症(Huntington’s chorea)、頭痛、偏頭痛、疼痛、胃腸疾病、癲癇、發炎、免疫相關疾病、內分泌相關疾病、癌症、高血壓、行為障礙、情緒障礙、躁狂性抑鬱症、失智症、性病症、性心理障礙或腎病。