Patents by Inventor Lester Lobo

Lester Lobo has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Process for the synthesis of cyclic heptapeptide
    Patent number: 8829157
    Abstract: The present invention relates to an improved process for the large scale synthesis of cyclic heptapeptide using Fmoc solid phase synthesis technique. The described process assembles the peptide on a solid support resin by coupling to one another by peptide bonds to obtain a peptide wherein the coupling of cysteine to the resin employs a combination of solvents to reduce cysteine racemization. The process described relates to the use of C1-C4 alcohols as total substitute to organic nitriles thus making the process cost effective, non-toxic and eco-friendly.
    Type: Grant
    Filed: January 17, 2011
    Date of Patent: September 9, 2014
    Assignee: USV, Ltd.
    Inventors: Divya Lal Saksena, Chandrakesan Muralidharan, Lester Lobo, Digamber Shripati Pawar, Nikhil Umesh Mohe, Radhakishnan Venkatasubramanian Tarur
  • Process for synthesis of cyclic octapeptide
    Patent number: 8377891
    Abstract: This invention relates a process for preparing octreotide and derivatives thereof. The starting material, Cys(Trt)-2-Chlorotrityl resin is coupled with various amino acids to obtain a protected heptapeptide of formula (2): Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-2-Chlorotrityl resin. The linear protected peptide of formula (2) is cleaved from the support using TFA5TIS and water to yield linear protected peptide of formula (3) Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-OH Linear protected heptapeptide of formula (3) is deprotected to yield heptapeptide of formula (6): D-Phe-Cys-Phe-D-Tip-Lys-Thr-Cys-OH; which is cyclized using hydrogen peroxide and to the cyclic peptide of formula (7) D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-OH; threoninol is coupled at C terminal to yield octreotide.
    Type: Grant
    Filed: May 4, 2009
    Date of Patent: February 19, 2013
    Assignee: USV, Ltd.
    Inventors: Divya Lal Saksena, Digamber Shripati Pawar, Nikhil Umesh Mohe, Nilesh Dagdu Patil, Chandrakesan Muralidharan, Lester Lobo, Radhakrishnan Venkatasubramanian Tarur
  • Process for Synthesis of Cyclic Octapeptide
    Publication number: 20120035117
    Abstract: This invention relates a process for preparing octreotide and derivatives thereof. The starting material, Cys(Trt)-2-Chlorotrityl resin is coupled with various amino acids to obtain a protected heptapeptide of formula (2): Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-2-Chlorotrityl resin. The linear protected peptide of formula (2) is cleaved from the support using TFA5TIS and water to yield linear protected peptide of formula (3) Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-OH Linear protected heptapeptide of formula (3) is deprotected to yield heptapeptide of formula (6): D-Phe-Cys-Phe-D-Tip-Lys-Thr-Cys-OH; which is cyclized using hydrogen peroxide and to the cyclic peptide of formula (7) D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-OH; threoninol is coupled at C terminal to yield octreotide.
    Type: Application
    Filed: May 4, 2009
    Publication date: February 9, 2012
    Inventors: Divya Lal Saksena, Digamber Shripati Pawar, Nikhil Umesh Mohe, Nilesh Dagdu Patil, Chandrakesan Muralidharan, Lester Lobo, Radhakrishnan Venkatasubramanian Tarur
  • Process for the Synthesis of Cyclic Heptapeptide
    Publication number: 20110118437
    Abstract: The present invention relates to an improved process for the large scale synthesis of cyclic heptapeptide using Fmoc solid phase synthesis technique. The described process assembles the peptide on a solid support resin by coupling to one another by peptide bonds to obtain a peptide wherein the coupling of cysteine to the resin employs a combination of solvents to reduce cysteine racemization. The process described relates to the use of C1-C4 alcohols as total substitute to organic nitriles thus making the process cost effective, non-toxic and eco-friendly.
    Type: Application
    Filed: January 17, 2011
    Publication date: May 19, 2011
    Inventors: DIVYA LAL SAKSENA, Chandrakesan Muralidharan, Lester Lobo, Digamber Shripati Pawar, NIKHIL UMESH MOHE, Radhakishnan Venkatasubramania Tarur