Santacruzamate: Compositions, Analogs and Methods of Use: A Patent Evaluation of WO 2014/018913 (A2)

Background: Santacruzamate A (SCA) is a natural product isolated from a marine cyanobacterium. Activity test results revealed that SCA is a highly potent HDAC2 inhibitor with an IC50 value of 0.112 nM. The IC50 of SCA in inhibiting cancer cell proliferation is 28.3 μM and 1.3μM on HCT116 and HuT-78 cells, respectively. Objective: To develop HDAC inhibitors with improved activity, SCA analogs were synthesized for the structure-activity relationship (SAR) studies. Method: Various substituted groups were introduced into the zinc binging group, linker, and cap regions of SCA by various chemical synthetic methods. Result: Compared with SCA, the derivatives of SCA did not exhibit improved HDAC2 inhibitory activity. Nevertheless, several molecules such as III-32, III-33, IV-4b, and IV-11 showed improved activity in inhibiting cell proliferation on HCT116 and HuT-78 cells. Conclusion: Collectively, a potent HDAC2 inhibitor SCA was discovered as a lead compound for further development of selective HDAC inhibitors.

Therapeutic Potential, Synthesis, Patent evaluation and SAR studies of thieno[3,2-d]pyrimidine derivatives: Recent updates.

: Thieno[3,2-d]pyrimidine ring framework comprises a significant class of heterocyclics that serve as a promising platform showing different pharmacological activities. The interest in thieno[3,2-d]pyrimidine cores for pharmaceutical products makes this scaffold an exceptionally helpful building block for organic chemistry. This review presents current research on thieno[3,2-d]pyrimidines and elucidates their biological importance in anti-cancer, anti-infectious, anti-convulsant, anti-diabetic, CNS, and osteoporosis drug discoveries. Patents on the thieno[3,2-d]pyrimidines are also elaborated as a piece of useful information. Here we additionally focus on the synthesis of this vital ring and the discovery of new thieno[3,2-d]pyrimidines.

Scientific Production and Intellectual Property

In Brazil, Public Research Institutions (PRI) are agents that promote innovation and technological production. The role of these institutions in social and regional development is to provide scientific and technological production and make it available for productive arrangements. This study aims to relate the evaluation and valuation of patents with the processes of Technology Transfer in Public Research Institutions in Brazil. To justify the execution of the study, it is observed that it is necessary to improve the use of technologies created in PRI so that society can take advantage of the advances promoted in scientific research, and so that the distance between industry and academia is minimized. We researched 30 Public Research Institutions, in five variables collected on the platform of INPI (National Institute of Industrial Property), ESPACENET (European Patent Office) and BDTD (Brazilian Digital Library of Theses and Dissertations). In possession of the data, the Shapiro-Wilk test and the Spearman correlation coefficient were used used to analyze them. The R software was used to apply the statistical methods. For data discussion, the reports of FORMICT (Information Form on Intellectual Property Policy of Scientific and Technological Institutions) were analyzed to guide the arguments. The data did not show normality and have moderate and strong correlations, the significance of the correlations is strong or very strong. It is believed that the patent evaluation and valuation processes have space for improvement and thus can enhance the Transfer of Technologies of PRI.