Background:
Bortezomib is reversible inhibitor of proteasome proteins for mammalian cells. Bortezomib is proven to be
cytotoxic to a number of tumor cells by disrupting their normal homeostatic mechanism and thereby causing cell death.
Currently, Bortezomib is prescribed for patients with multiple myeloma and mantle cell lymphoma.
Objective:
This assessment highlights the overview of recent patents of Bortezomib. This review includes patents grouped
in sections like product patents, process patent, composition related patents as well as treatment methodology. Objective of
this article is to facilitate researchers with all existing patents at single place.
Methods:
Data were searched from various online databases. In which, paid databases include SciFinder®
and Orbit®
. Free
databases include Patentscope® (WIPO), Worldwide Espacenet®
(EPO), Google Patents and InPASS (Indian patent
database).
Results:
Several new processes and composition related patents of Bortezomib have been recently patented as its orangebook listed patents are going to soon expire during July 2022. Further, due to problem of oxidation during development and
long-term storage of Bortezomib formulation, a number of excipients are tried in these patents to stabilize the same.
However, there is still need for further development of improved formulation of Bortezomib with better characteristics.
Conclusion:
Extensive research have been carried out on various process for preparing Bortezomib and composition
thereof. This type of dynamic research will clear the path for many generic players in the United States which lead in
reduction of price of the composition and thereby enhancing global health care at cheaper prices.
Background:
mTORC1/ PI3K control multiple anabolic pathways, including protein
synthesis, ribosome production, lipogenesis, and nucleotide synthesis, are all important for cell and
tissue growth. Sapanisertib and Dactolisib inhibit PI3K/AKT/mTOR pathway, an important signaling
pathway for many cellular functions such as growth control, metabolism and translation initiation.
Methods:
Dactolisib contains quinolin-3-yl-2,3-dihydroimidazo[4,5-c]quinolin scaffold and Sapanisertib
contains benzo[d]oxazol-5-yl-1-ethyl-1H-pyrazolo[3,4-d]pyrimidinnucleous. From the reference
to both of drug novel series of 4-Amino-3-(isoquinolin-4-yl)-1H-pyrazolo[3,4-d]pyrimidin was
developed by molecular docking. In sillico analysis was done with SWISSADME online tools.
Results:
Among all the designed derivatives, compounds 6(-10.6 kcal/mol) , 12( -10.7 kcal/mol),
14( -10.2 kcal/mol), and 16(-10.2 kcal/mol) have a good binding affinity than others. Biological
activity was predicted by Molinspirationonline software tool showing that all compounds are active
on G- protein coupled receptor. In silico toxicity profile of designed compounds was performed
using the SWISSADME program, indicating that all the compounds follow the Lipinski
rule of five and do not penetrate Blood brain barrier.
Conclusion:
Series of pyrazolo[3,4-d]pyrimidin derivatives gives good binding affinity with pan-
PI3-Kinese/Mtor inhibitors. The present study provided a better understanding of the molecular
modeling requisite for maintaining and/or improving PI3K/mTOR inhibitors.
Background:
Pemetrexed is a folate analogue metabolic inhibitor for mammalian cells. Pemetrexed is
established to be toxic to several cancer cells by interfering with their new biosynthesis of nucleotides and thus causing
cell apoptosis. Presently, Pemetrexed is given to patients with non-small cell lung cancer (NSCLC).
Objective:
This review focuses on the recent patents of Pemetrexed. This assessment includes patents grouped in
segments like crystalline form patent, composition related patents, product patents, as well as a method of treatment. The
aim of this review is to simplify inventors with altogether existing patents at a single place.
Methods:
Data were searched from several available databases. In which, paid databases include Orbit® and SciFinder®.
Free databases include Worldwide Espacenet® (EPO), Patentscope® (WIPO), InPASS (Indian patent database) and Google
Patents.
Results:
Some new polymorph and composition related inventions of Pemetrexed have been recently patented as its
orange-book listed patents will soon expire in May 2022. Further, because of the problem of oxidation through the
development and continuing storage of Pemetrexed composition, several excipients are experimented within these patents
to stabilize the same. Nevertheless, there is a need for further development of an improved composition of Pemetrexed
with improved characteristics.
Conclusion:
Wide research has been conducted on different processes for preparing Pemetrexed and formulation thereof.
Such type of active research may clear the track for the generic companies in the United States which produces in the
reduction of the price of the formulation and hence, providing universal health care at economic prices.
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