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ABSTRACTIntroduction: 1,2,3,4-Tetrahydroisoquinoline (THIQ) is one of the ‘privileged scaffolds’, commonly found in nature. Initially, this class of compounds was known for its neurotoxicity. Later on, 1-methyl-1,2,3,4-tetrahydroisoquinoline was proved as an endogeneous Parkinsonism-preventing agent in mammals. The fused THIQs have been studied for their role as anticancer antibiotics. The US FDA approval of the trabectedin for the treatment of soft tissue sarcomas, is a milestone in the anticancer drug discovery.Areas covered: This review covers the patents on various therapeutic activities of the THIQ derivatives in the years between 2010 and 2015. Patents were collected using a thorough search of Espacenet and WIPO databases. The therapeutic areas covered include cancer, malaria, central nervous system (CNS), cardiovascular, metabolic disorders, and so on. This also includes several patents on specific THIQs of clinical importance.Expert opinion: A large number of the THIQ derivatives have been synthesised for various therapeutic activities, with noticeable success in the area of drug discovery for cancer and CNS. They may also prove to be promising candidates for various infectious diseases, such as malaria, tuberculosis, HIV-infection, HSV-infection, leishmaniasis, etc. They can also be developed as novel class of drugs for various therapeutic activities with unique mechanism of action.

Introduction:Berberine, a protoberberine alkaloid, and its derivatives exhibit a wide spectrum of pharmacological activities. It has been used in traditional Chinese medicine and Ayurvedic medicine and current research evidences support its use for various therapeutic areas.Areas covered:This review covers the patents on therapeutic activities of berberine and its derivatives in the years between 2009 and 2012. An extensive search was done to collect the patent information using European Patent Office database and SciFinder. The therapeutic areas covered include cancer, inflammation, infectious diseases, cardiovascular, metabolic disorders, and miscellaneous areas such as polycystic ovary syndrome, allergic diseases, and so on.Expert opinion:Berberine along with its derivatives or in combination with other pharmaceutically active compounds or in the form of formulations has applications in various therapeutic areas such as cancer, inflammation, diabetes, depression, hypertension, and various infectious areas. Berberine has demonstrated wide physiological functions and has great potential to give a multipotent drug if some inherent problems on poor bioavailability and solubility are taken care of. Additionally, polyherbal formulations with berberine-containing plants as major ingredients can be successfully developed.