Patents by Inventor Kyriacos C. Nicolaou

Kyriacos C. Nicolaou 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).

  • Patent number: 11584754
    Abstract: In one aspect, the present disclosure provides analogs of thailanstatin of the formula wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein.
    Type: Grant
    Filed: June 8, 2017
    Date of Patent: February 21, 2023
    Assignee: William Marsh Rice University
    Inventors: Kyriacos C. Nicolaou, Derek Rhoades, Soundarapandian M. Kumar, Manas R. Pattanayak, Manjunath Lamani
  • Patent number: 11465997
    Abstract: In one aspect, the present disclosure provides disorazole analogs of the formula: Formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided.
    Type: Grant
    Filed: June 21, 2018
    Date of Patent: October 11, 2022
    Assignee: William Marsh Rice University
    Inventors: Kyriacos C. Nicolaou, Gabriel Bellavance, Marek Buchman, Kiran Kumar Pulukuri, Stephan Rigol
  • Patent number: 11274124
    Abstract: In one aspect, the present disclosure provides tubulysin analogs of the formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided.
    Type: Grant
    Filed: November 28, 2018
    Date of Patent: March 15, 2022
    Assignee: William Marsh Rice University
    Inventors: Kyriacos C. Nicolaou, Rohan Diliprao Erande, Dionisios Vourloumis, Kiran Kumar Pulukuri, Stephan Rigol
  • Publication number: 20210238187
    Abstract: In one aspect, the present disclosure provides epothilone analogs of the formula: (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided.
    Type: Application
    Filed: April 11, 2018
    Publication date: August 5, 2021
    Applicant: WILLIAM MARSH RICE UNIVERSITY
    Inventors: Kyriacos C NICOLAOU, Derek RHOADES, Yangping WANG
  • Publication number: 20210230178
    Abstract: In one aspect, the present disclosure provides trioxacarcin analogs of the formula: wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein as well as dimers of the compounds described herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided.
    Type: Application
    Filed: August 16, 2018
    Publication date: July 29, 2021
    Applicant: William Marsh Rice University
    Inventors: Kyriacos C. NICOLAOU, Pengxi CHEN, Shugao ZHU, Quan CAI
  • Publication number: 20210188906
    Abstract: In one aspect, the present disclosure provides tubulysin analogs of the formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided.
    Type: Application
    Filed: November 28, 2018
    Publication date: June 24, 2021
    Applicant: William Marsh Rice University
    Inventors: Kyriacos C. NICOLAOU, Rohan Diliprao ERANDE, Dionisios VOURLOUMIS, Kiran Kumar PULUKURI, Stephan RIGOL
  • Publication number: 20210155616
    Abstract: In one aspect, the present disclosure provides disorazole analogs of the formula: Formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided.
    Type: Application
    Filed: June 21, 2018
    Publication date: May 27, 2021
    Applicant: WILLIAM MARSH RICE UNIVERSITY
    Inventors: Kyriacos C. NICOLAOU, Gabriel BELLAVANCE, Marek BUCHMAN, Kiran Kumar PULUKURI, Stephan RIGOL
  • Patent number: 10899773
    Abstract: In one aspect, the present invention provides novel derivatives of trioxacarin analogs of the formula (I) wherein the variables are as defined herein. The application also provides compositions, methods of treatment, and methods of synthesis thereof.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: January 26, 2021
    Assignee: William Marsh Rice University
    Inventors: Kyriacos C Nicolaou, Quan Cai
  • Patent number: 10889590
    Abstract: In one aspect, the present disclosure provides new analogs of uncialamycin. The present disclosure also provides novel synthetic pathways to obtaining uncialamycin and analogs thereof. Additionally, the present disclosure also describes methods of use of uncialamycin and analogs thereof. In another aspect, the present disclosure provides antibody-drug conjugates which may be used to treat cancer or another disease or disorder.
    Type: Grant
    Filed: March 18, 2019
    Date of Patent: January 12, 2021
    Assignees: William Marsh Rice University, The Scripps Research Institute, Bristol-Myers Squibb Company
    Inventors: Kyriacos C. Nicolaou, Min Lu, Debashis Mandal, Sanjeev Gangwar, Naidu S. Chowdari, Yam B. Poudel
  • Patent number: 10874646
    Abstract: In one aspect, the present disclosure provides epothilone analogs of the formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided.
    Type: Grant
    Filed: October 14, 2016
    Date of Patent: December 29, 2020
    Assignee: William Marsh Rice University
    Inventors: Kyriacos C Nicolaou, Derek Rhoades, Yanping Wang, Sotirios Totokotsopoulos
  • Patent number: 10870670
    Abstract: The invention relates to processes for preparing (S,S)-secoisolariciresinol diglucoside and (R,R)-secoisolariciresinol diglucoside and compositions comprising the same.
    Type: Grant
    Filed: July 23, 2018
    Date of Patent: December 22, 2020
    Assignees: THE SCRIPPS RESEARCH INSTITUTE, THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
    Inventors: Melpo Christofidou-Solomidou, Kyriacos C. Nicolaou, Roman A. Valiulin, Nicholas Simmons, Philipp M. Heretsch
  • Patent number: 10808007
    Abstract: In one aspect, the present disclosure provides tubulysin analogs of the formula (I) wherein R1, R2, R3, R4, X1, X2, X3, and A1 are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein.
    Type: Grant
    Filed: February 25, 2016
    Date of Patent: October 20, 2020
    Assignee: William Marsh Rice University
    Inventors: Kyriacos C. Nicolaou, Dionisios Vourloumis, Jun Yin, Rohan Erande, Debashis Mandal, Phillipp Klahn
  • Patent number: 10590158
    Abstract: In one aspect, the present disclosure provides shishijimicin analogs of the formula: wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, antibody drug conjugates of the compounds are also provided.
    Type: Grant
    Filed: June 29, 2016
    Date of Patent: March 17, 2020
    Assignee: WILLIAM MARSH RICE UNIVERSITY
    Inventors: Kyriacos C. Nicolaou, Ruofan Li, Zhaoyong Lu, Te-ik Sohn, James Woods, Emmanouil N. Pitsinos
  • Publication number: 20200024283
    Abstract: In one aspect, the present disclosure provides analogs of thailanstatin of the formula wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein.
    Type: Application
    Filed: June 8, 2017
    Publication date: January 23, 2020
    Applicant: WILLIAM MARSH RICE UNIVERSITY
    Inventors: Kyriacos C. NICOLAOU, Derek RHOADES, Soundarapandian M. KUMAR, Manas R. PATTANAYAK, Manjunath LAMANI
  • Publication number: 20190382412
    Abstract: In one aspect, the present disclosure provides new analogs of uncialamycin. The present disclosure also provides novel synthetic pathways to obtaining uncialamycin and analogs thereof. Additionally, the present disclosure also describes methods of use of uncialamycin and analogs thereof. In another aspect, the present disclosure provides antibody-drug conjugates which may be used to treat cancer or another disease or disorder.
    Type: Application
    Filed: March 18, 2019
    Publication date: December 19, 2019
    Applicants: WILLIAM MARSH RICE UNIVERSITY, BRISTOL-MYERS SQUIBB COMPANY, THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Kyriacos C. Nicolaou, Min LU, Debashis MANDAL, Sanjeev GANGWAR, Naidu S. CHOWDARI, Yam B. POUDEL
  • Patent number: 10233192
    Abstract: In one aspect, the present disclosure provides new analogs of uncialamycin. The present disclosure also provides novel synthetic pathways to obtaining uncialamycin and analogs thereof. Additionally, the present disclosure also describes methods of use of uncialamycin and analogs thereof. In another aspect, the present disclosure provides antibody-drug conjugates which may be used to treat cancer or another disease or disorder.
    Type: Grant
    Filed: August 15, 2017
    Date of Patent: March 19, 2019
    Assignees: WILLIAM MARSH RICE UNIVERSITY, THE SCRIPPS RESEARCH INSTITUTE, BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Kyriacos C. Nicolaou, Min Lu, Debashis Mandal, Sanjeev Gangwar, Naidu S. Chowdari, Yam B. Poudel
  • Publication number: 20190062363
    Abstract: The invention relates to processes for preparing (S,S)-secoisolariciresinol diglucoside and (R,R)-secoisolariciresinol diglucoside and compositions comprising the same.
    Type: Application
    Filed: July 23, 2018
    Publication date: February 28, 2019
    Applicants: The Trustees of the University of Pennsylvania, The Scripps Research Institute
    Inventors: Melpo CHRISTOFIDOU-SOLOMIDOU, Kyriacos C. Nicolaou, Roman A. Valiulin, Nicholas Simmons, Philipp M. Heretsch
  • Publication number: 20190023717
    Abstract: In one aspect, the present invention provides novel derivatives of trioxacarin analogs of the formula (I) wherein the variables are as defined herein. The application also provides compositions, methods of treatment, and methods of synthesis thereof.
    Type: Application
    Filed: December 18, 2015
    Publication date: January 24, 2019
    Applicant: WILLIAM MARSH RICE UNIVERSITY
    Inventors: Kyriacos C NICOLAOU, Quan CAI
  • Publication number: 20190022069
    Abstract: In one aspect, the present disclosure provides epothilone analogs of the formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided.
    Type: Application
    Filed: October 14, 2016
    Publication date: January 24, 2019
    Applicant: WILLIAM MARSH RICE UNIVERSITY
    Inventors: Kyriacos C NICOLAOU, Derek RHOADES, Yanping WANG, Sotirios TOTOKOTSOPOULOS
  • Publication number: 20180327439
    Abstract: In one aspect, the present disclosure provides shishijimicin analogs of the formula: wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, antibody drug conjugates of the compounds are also provided.
    Type: Application
    Filed: June 29, 2016
    Publication date: November 15, 2018
    Applicant: WILLIAM MARSH RICE UNIVERSITY
    Inventors: Kyriacos C. NICOLAOU, Ruofan LI, Zhaoyong LU, Te-ik SOHN, James WOODS, Emmanouil N. PITSINOS