Our planet is supposed to host 11.213 billion people by the end of the year 2100. Such demographic explosion poses serious problems for human life quality and security. Generally, the term “seaweed” is conventionally used to designate multicellular marine algae. In the last three decades, and due to the high diversity of their metabolites, seaweeds are used in medicine to treat gall stones, stomach ailments, eczema, cancer, renal disorders, scabies, psoriasis, asthma, arteriosclerosis, heart disease, lung diseases, ulcers, etc. Compounds like carotenoid, polysaccharides, fatty acids, glycoproteins, haloforms, halogenated alkanes, alkenes, alcohols, aldehydes, hydroquinones, ketones, phlorotannins, pigments, lectins, alkaloids, terpenoids, sterols and some heterocyclic and phenolic compounds are among the most important seaweed substances that receive attention from pharmaceutical companies for use in drug development, or from scientists in the field of medical research. The potential pharmaceutical, medicinal and investigatory applications of these compounds in antibiotic, antiviral, anticancer, antioxidants, anti-inflammatory, anticoagulants, and antidiabetic production are discussed in this chapter.