Patents by Inventor Gregory S. Welmaker

Gregory S. Welmaker 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: 11014876
    Abstract: Cancer is a disease for which there remains a great unmet medical need, and therefore the discovery and development of new antineoplastic agents is critically important. The present invention relates in part to new therapeutic compounds with antineoplastic activity. Provided herein are polyamine sulfonamides such as compounds of Formula (I), or pharmaceutically acceptable salts thereof, which may be used in the treatment and/or prevention of diseases such as cancer. Also provided herein are pharmaceutical compositions and kits comprising the inventive compounds. Furthermore, the present invention provides methods of treating and/or preventing diseases (e.g., cancer) using compounds of Formula (I), or pharmaceutically acceptable salts thereof or pharmaceutical compositions thereof. Other methods provided include methods for inducing apoptosis of a cell, as well as methods for inhibiting alpha-enolase enzymatic activity in vivo and in vitro.
    Type: Grant
    Filed: November 4, 2016
    Date of Patent: May 25, 2021
    Assignees: University of Florida Research Foundation, Inc., Torrey Pines Institute for Molecular Studies
    Inventors: Christopher R. Cogle, Amy M. Meacham, Peter P. Sayeski, Marcello A. Giulianotti, Richard A. Houghten, Gregory S. Welmaker
  • Publication number: 20200179361
    Abstract: The present disclosure provides compositions including a ?4?2 nAChR antagonist, pharmaceutical compositions including a ?4?2 nAChR antagonist, methods of making the compositions or pharmaceutical compositions, methods of treatment of a condition (e.g., nicotine addiction) or disease, methods of treatment using compositions or pharmaceutical compositions, and the like. Embodiments of the present disclosure can be used to reduce nicotine cravings and treat nicotine addiction. The compositions have selective affinity for the ?4?2 receptor, which appears to be involved in nicotine dependence.
    Type: Application
    Filed: May 21, 2018
    Publication date: June 11, 2020
    Inventors: Marcello GIULIANOTTI, Lawrence TOLL, Gregory S. WELMAKER, Jinhua WU, Yongping YU
  • Publication number: 20180297942
    Abstract: Cancer is a disease for which there remains a great unmet medical need, and therefore the discovery and development of new antineoplastic agents is critically important. The present invention relates in part to new therapeutic compounds with antineoplastic activity. Provided herein are polyamine sulfonamides such as compounds of Formula (I), or pharmaceutically acceptable salts thereof, which may be used in the treatment and/or prevention of diseases such as cancer. Also provided herein are pharmaceutical compositions and kits comprising the inventive compounds. Furthermore, the present invention provides methods of treating and/or preventing diseases (e.g., cancer) using compounds of Formula (I), or pharmaceutically acceptable salts thereof or pharmaceutical compositions thereof. Other methods provided include methods for inducing apoptosis of a cell, as well as methods for inhibiting alpha-enolase enzymatic activity in vivo and in vitro.
    Type: Application
    Filed: November 4, 2016
    Publication date: October 18, 2018
    Applicants: University of Florida Research Foundation, Inc., Torrey Pines Institute for Molecular Studies
    Inventors: Christopher R. Cogle, Amy M. Meacham, Peter P. Sayeski, Marcello A. Giulianotti, Richard A. Houghten, Gregory S. Welmaker
  • Patent number: 7973044
    Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: July 5, 2011
    Assignees: Elan Pharmaceuticals, Inc., Wyeth
    Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
  • Patent number: 7968547
    Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Grant
    Filed: December 14, 2009
    Date of Patent: June 28, 2011
    Assignees: Elan Pharmaceuticals, Inc., Wyeth
    Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis
  • Patent number: 7745454
    Abstract: Disclosed are certain alpha amino acid compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Grant
    Filed: September 7, 2004
    Date of Patent: June 29, 2010
    Assignees: Elan Pharmaceuticals, Inc., Wyeth
    Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Farouz, Christopher M. Semko, Ying-Zi Xu
  • Publication number: 20100160341
    Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Application
    Filed: December 22, 2009
    Publication date: June 24, 2010
    Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
  • Publication number: 20100160343
    Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Application
    Filed: December 14, 2009
    Publication date: June 24, 2010
    Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
  • Patent number: 7662831
    Abstract: The present invention is directed to compounds of Formula I: that are potassium channel modulators and pharmaceutical compositions thereof. The present invention is further directed to methods of treatment using the compounds and pharmaceutical compositions of the invention. The present invention is still further directed to synthetic processes for producing the compounds of the invention.
    Type: Grant
    Filed: July 26, 2007
    Date of Patent: February 16, 2010
    Assignee: Wyeth LLC
    Inventors: Matthew A. Wilson, Gregory S. Welmaker, Eugene J. Trybulski, John A. Butera, Ronald L. Magolda
  • Patent number: 7601856
    Abstract: The present invention is directed to compounds of Formula I: that are potassium channel modulators and pharmaceutical compositions thereof. The present invention is further directed to methods of treatment using the compounds and pharmaceutical compositions of the invention. The present invention is still further directed to synthetic processes for producing the compounds of the invention.
    Type: Grant
    Filed: July 26, 2007
    Date of Patent: October 13, 2009
    Assignee: Wyeth
    Inventors: Gregory S. Welmaker, Matthew A. Wilson, Geraldine McFarlane, Joan E. Sabalski, John A. Butera, Eugene J. Trybulski, David R. Herbst
  • Publication number: 20080182850
    Abstract: Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Application
    Filed: October 16, 2007
    Publication date: July 31, 2008
    Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu, Frank Stappenbeck
  • Patent number: 7378529
    Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Grant
    Filed: January 10, 2005
    Date of Patent: May 27, 2008
    Assignee: Wyeth
    Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
  • Patent number: 7351839
    Abstract: This invention provides processes for preparing compounds formula: wherein R is H, alkyl, acyl, aryl, aroyl or —C(O)R?; R? is alkyl or aryl; R1, R2, R4 and R5 are H, —OH, alkyl, cycloalkyl, alkoxy, halogen, fluorinated alkyl or alkoxy, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, acyl, aryl or aroyl; R3 is H, alkyl, cycloalkyl, alkoxy, fluorinated alkyl, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, aryl, or aroyl; or a pharmaceutically acceptable salt thereof, as well as novel compounds useful in the synthesis of these compounds.
    Type: Grant
    Filed: November 21, 2006
    Date of Patent: April 1, 2008
    Assignee: Wyeth
    Inventors: Gregory S. Welmaker, Joan E. Sabalski, Michael D. Smith
  • Publication number: 20080027090
    Abstract: The present invention is directed to compounds of Formula I: that are potassium channel modulators and pharmaceutical compositions thereof. The present invention is further directed to methods of treatment using the compounds and pharmaceutical compositions of the invention. The present invention is still further directed to synthetic processes for producing the compounds of the invention.
    Type: Application
    Filed: July 26, 2007
    Publication date: January 31, 2008
    Applicant: WYETH
    Inventors: Matthew A. WILSON, Gregory S. WELMAKER, Eugene J. Trybulski, John A. BUTERA, Ronald L. MAGOLDA
  • Publication number: 20080027049
    Abstract: The present invention is directed to compounds of Formula I: that are potassium channel modulators and pharmaceutical compositions thereof. The present invention is further directed to methods of treatment using the compounds and pharmaceutical compositions of the invention. The present invention is still further directed to synthetic processes for producing the compounds of the invention.
    Type: Application
    Filed: July 26, 2007
    Publication date: January 31, 2008
    Applicant: WYETH
    Inventors: Gregory S. WELMAKER, Matthew A. WILSON, Geraldine R. McFARLANE, Joan E. SABALSKI, John A. BUTERA, Eugene J. Trybulski, David R. HERBST
  • Patent number: 7291645
    Abstract: Disclosed are a series of phenylalanine derivatives, to compositions containing them, to processes for their preparation, and to their use in medicine.
    Type: Grant
    Filed: December 12, 2003
    Date of Patent: November 6, 2007
    Assignees: Elan Pharmaceuticals, Inc., Wyeth
    Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
  • Patent number: 7271163
    Abstract: This invention provides compounds of the formulae: wherein: R1 is hydrogen, —C(O)CH3 or alkyl of 1-6 carbon atoms; R2 and R3 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl, alkoxy of 1-6 carbon atoms, —CH2OH, fluoroalkyl, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, aryl, or aroyl; R4 and R5 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, fluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R6 and R7 are each independently hydrogen, C1-C6 alkyl or cycloalkyl; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions containing these
    Type: Grant
    Filed: July 23, 2004
    Date of Patent: September 18, 2007
    Assignee: Wyeth
    Inventors: Annmarie L. Sabb, Robert L. Vogel, James A. Nelson, Sharon J. Rosenzweig-Lipson, Gregory S. Welmaker, Joan E. Sabalski
  • Patent number: 7223762
    Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Grant
    Filed: April 14, 2005
    Date of Patent: May 29, 2007
    Assignees: Elan Pharmaceuticals, Inc., Wyeth
    Inventors: Andrei W. Konradi, Michael A. Pliess, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher M. Semko, Ying-Zi Xu
  • Patent number: 7141563
    Abstract: This invention provides processes for preparing compounds formula: wherein R is H, alkyl, acyl, aryl, aroyl or —C(O)R?; R? is alkyl or aryl; R1, R2, R4 and R5 are H, —OH, alkyl, cycloalkyl, alkoxy, halogen, fluorinated alkyl or alkoxy, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, acyl, aryl or aroyl; R3 is H, alkyl, cycloalkyl, alkoxy, fluorinated alkyl, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, aryl, or aroyl; or a pharmaceutically acceptable salt thereof, as well as novel compounds useful in the synthesis of these compounds.
    Type: Grant
    Filed: November 2, 2001
    Date of Patent: November 28, 2006
    Assignee: Wyeth
    Inventors: Gregory S. Welmaker, Joan E. Sabalski, Michael D. Smith
  • Patent number: 7015216
    Abstract: Disclosed are a series of heteroaryl-?-alanine derivatives, compositions containing them, processes for their preparation and their use in medicine.
    Type: Grant
    Filed: July 19, 2001
    Date of Patent: March 21, 2006
    Assignees: Elan Pharmaceuticals, Inc., Wyeth
    Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu