Office | CNIPA |
Document type: | Patent |
Inventor(s): | Ricardo José Nunes; Alessandra Mascarello; Rosendo Augusto Yunes; Taisa Regina Stumpf; Paulo Cesar Leal; José Andres Yunes; Carolina Pereira De Souza Melo; Rafael Renatino Canevarolo; Louise Domeneghini Chiaradia; André Bortolini Silveira; Anqelo Brunelli Albertoni Laranjeira |
Applicant: | Alessandra Mascarello; André Bortolini Silveira; Carolina Pereira de Souza Melo; José Andres Yunes; Louise Domeneghini Chiaradia; Paulo Cesar Leal; Rafael Renatino Canevarolo; Ricardo José Nunes; Rosendo Augusto Yunes; Taisa Regina Stumpf; Universidade Federal de Santa Catarina (UFSC) |
Year: | 2012 |
Application Number: | CN 201280063518 |
IPC: | A61K 31/166 A61K 31/381 A61K 31/4164 A61P 35/02 C07C 251/86 C07D 233/54 C07D 271/107 C07D 333/02 |
The present invention relates to acyl-hydrazone compounds, in particular 3,4,5-trimethoxyphenyl-hydrazide derivatives, oxadiazole analogs and other similar compounds thereof, and to their use in the treatment of diseases associated with cell proliferation Drug use in various diseases such as leukemia, including acute lymphoblastic leukemia (ALL), tumors and inflammation. An acyl-hydrazone having similar activity to the compound used as a standard in the experiment (colchicine) has been obtained. The greater selectivity of the compounds according to the invention is an important feature associated with less side effects compared to drugs currently used in clinical therapy. Synthetic acyl-hydrazones, more particularly compounds 02 and 07, exhibited significant anti-leukemic activity, suggesting that 02 and 07 may be useful in the treatment of leukemia, especially acute lymphoblastic leukemia (ALL), tumors and diseases such as inflammatory Drug prototypes or drug candidates for other proliferative diseases. In addition to selectivity studies in healthy human lymphocytes, the mechanism of action of the most active compounds was determined by testing using DNA microarrays followed by chip indication.
FAPESP's process: | 09/04167-1 - Metabolomics of methotrexate resistance in acute lymphoblastic leukemia |
Grantee: | Rafael Renatino Canevarolo |
Principal Investigator: | José Andrés Yunes |
Institution: | Centro Infantil de Investigações Hematológicas Dr Domingos A Boldrini (CIB) |
Support Opportunities: | Scholarships in Brazil - Master |
FAPESP's process: | 12/11952-0 - Methotrexate resistance is directly associated with glutathione concentration in acute lymphoblastic leukemia cell lines |
Grantee: | Rafael Renatino Canevarolo |
Principal Investigator: | José Andrés Yunes |
Institution: | Centro Infantil de Investigações Hematológicas Dr Domingos A Boldrini (CIB) |
Support Opportunities: | Scholarships in Brazil - Doctorate |
FAPESP's process: | 08/02106-2 - IGFBP7 role in chemotherapy resistance of Pediatric Acute Lymphoblastic Leukemia |
Grantee: | Angelo Brunelli Albertoni Laranjeira |
Principal Investigator: | José Andrés Yunes |
Institution: | Centro Infantil de Investigações Hematológicas Dr Domingos A Boldrini (CIB) |
Support Opportunities: | Scholarships in Brazil - Doctorate |
FAPESP's process: | 12/03039-2 - IGFBP7 and insulin/IGFs in Childhood Acute Lymphoblastic Leukemia chemoresistance |
Grantee: | Angelo Brunelli Albertoni Laranjeira |
Principal Investigator: | José Andrés Yunes |
Institution: | Centro Infantil de Investigações Hematológicas Dr Domingos A Boldrini (CIB) |
Support Opportunities: | Scholarships in Brazil - Post-Doctoral |
FAPESP's process: | 14/08247-8 - Preclinical studies of novel inhibitors of DNA methyltransferase in acute leukemia |
Grantee: | Nathalia Moreno Cury |
Principal Investigator: | José Andrés Yunes |
Institution: | Centro Infantil de Investigações Hematológicas Dr Domingos A Boldrini (CIB) |
Support Opportunities: | Scholarships in Brazil - Doctorate |