Patents Represented by Attorney, Agent or Law Firm Paul R. Darkes
  • Use of protein kinase C inhibitors to enhance the clinical efficacy of radiation therapy
    Patent number: 6288053
    Abstract: A method for treating neoplasms is disclosed, particularly using the &bgr;-isozyme selective PKC inhibitor, (S)-3,4-[N,N′-1,1′-((2″-ethoxy)-3′″(O)-4′″-(N,N -dimethylamino)butane)-bis-(3,3′-indolyl)]-1(H)-pyrrole-2,5-dione or one of its salts, such PKC inhibitors enhance the clinical efficacy of oncolytic agents and radiation therapy.
    Type: Grant
    Filed: November 17, 1998
    Date of Patent: September 11, 2001
    Assignee: Eli Lilly and Company
    Inventors: Michael R. Jirousek, Lawrence E. Stramm, Douglas Kirk Ways
  • Therapeutic treatment for VEGF related diseases
    Patent number: 6284751
    Abstract: A method for inhibiting VEGF stimulated endothelial cell growth, such as associated with neoplasia, and VEGF stimulated capillary permeability, such as associated with pulmonary edema are disclosed, particularly using the &bgr;-isozyme selective PKC inhibitor, (S)-3,4-[N,N′-1,1′-((2″-ethoxy)-3′″(O)-4′″-(N,N-dimethylamino)-butane)-bis-(3,3′-indolyl)]-1(H)-pyrrole-2,5-dionehydrochloridesalt.
    Type: Grant
    Filed: June 18, 1999
    Date of Patent: September 4, 2001
    Assignee: Eli Lilly and Company
    Inventors: Lloyd P. Aiello, Michael R. Jirousek, George L. King, Louis Vignati, Douglas Kirk Ways
  • Use of protein kinase C inhibitors to enhance the clinical efficacy of oncolytic agents and radiation therapy
    Patent number: 6232299
    Abstract: A method for treating neoplasms is disclosed, particularly using the &bgr;-isozyme selective PKC inhibitor, (S)-3,4-[N, N′-1,1′-((2″-ethoxy)-3′″-(O)-4′″-(N,N-dimethylamino)-butane)-bis-(3,3′-indolyl)]-1(H)-pyrrole-2,5-dione or one of its salts, such PKC inhibitors enhance the clinical efficacy of oncolytic agents and radiation therapy.
    Type: Grant
    Filed: April 30, 1997
    Date of Patent: May 15, 2001
    Assignee: Eli Lilly and Company
    Inventors: Michael R. Jirousek, Lawrence E. Stramm, Douglas Kirk Ways
  • Therapeutic treatment for renal dysfunction
    Patent number: 6225301
    Abstract: A method for treating renal dysfunctions is disclosed, particularly using the isozyme selective PKC inhibitor, (S)-3,4-[N, N′-1,1′-((2″-ethoxy)-3′″(O)-4′″-(N,N-dimethylamino)-butane)-bis-(3,3′-indolyl) ]-1(H)-pyrrole-2,5-dionehydrochloridesalt.
    Type: Grant
    Filed: February 22, 1999
    Date of Patent: May 1, 2001
    Assignees: Eli Lilly and Company
    Inventors: Douglas Kirk Ways, Richard Ernest Gilbert
  • Hypoglycemic and hypolipidemic compounds
    Patent number: 6194446
    Abstract: This invention provides compounds and their pharmaceutically-acceptable salts, pharmaceutical formulations of said compounds, and methods for treating hyperglycemia associated with non-insulin dependent diabetes and for treating hyperlipidemia.
    Type: Grant
    Filed: December 18, 1998
    Date of Patent: February 27, 2001
    Assignee: Eli Lilly and Company
    Inventors: Samuel James Dominianni, Margaret Mary Faul, Russell Dean Stucky, Leonard Larry Winneroski, Jr.
  • Synthesis of bisindolylmalimides
    Patent number: 6133452
    Abstract: The present invention provides for the reaction of optionally substituted indole-3-acetamides with optionally substituted methyl indole-3-glyoxyl reagent to prepare potent PKC inhibitors. The reaction is very efficient and robust macrocyclization methodology.
    Type: Grant
    Filed: January 21, 1999
    Date of Patent: October 17, 2000
    Assignee: Eli Lilly and Company
    Inventors: Margaret Mary Faul, Leonard Larry Winneroski, Jr.
  • Hypoglycemic and hypolipidemic compounds
    Patent number: 6121282
    Abstract: This invention provides 1,2,3,4-tetrahydroisoquinoline compounds and their pharmaceuticallyacceptable salts, pharmaceutical formulations of said compounds, and methods for treating hyperglycemia associated with non-insulin dependent diabetes and for treating hyperlipidemia.
    Type: Grant
    Filed: December 18, 1998
    Date of Patent: September 19, 2000
    Assignee: Eli Lilly and Company
    Inventors: Samuel James Dominianni, William Harlan Gritton
  • Protein kinase C inhibitor
    Patent number: 6117861
    Abstract: This invention provides novel bis-indolylmaleimide macrocycle derivatives of the formula: ##STR1## and solvates thereof. The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.
    Type: Grant
    Filed: December 7, 1999
    Date of Patent: September 12, 2000
    Assignee: Eli Lilly and Company
    Inventors: Gary Lowell Engel, Nagy Alphonse Farid, Margaret Mary Faul, Michael Robert Jirousek, Lori Ann Richardson, Leonard Larry Winneroski, Jr.
  • Therapeutic treatment for VEGF related ocular diseases
    Patent number: 6114320
    Abstract: A method for inhibiting VEGF stimulated endothelial cell growth, such as associated with macular degeneration, and VEGF stimulated capillary permeability, such as associated with macular edema are disclosed, particularly using the isozyme selective PKC inhibitor, (S)-3,4-[N,N'-1,1'-((2"-ethoxy)-3'"(O)-4'"-(N,N-dimethylamino)-butane)-bis -(3,3'-indoly 1)]-1(H)-pyrrole-2,5-dionehydrochloridesalt.
    Type: Grant
    Filed: April 30, 1997
    Date of Patent: September 5, 2000
    Assignees: Eli Lilly and Company, Joslin Diabetes Center
    Inventors: Lloyd P. Aiello, Michael R. Jirousek, George L. King, Louis Vignati, Douglas Kirk Ways
  • Therapeutic treatment for HIV infection
    Patent number: 6107327
    Abstract: A method for treating HIV infection is disclosed, particularly using the isozyme selective PKC inhibitor, (S)-3,4-[N, N'-1,1'-((2"-ethoxy)-3'"(O)-4'"-(N,N-dimethylamino)-butane)-bis-(3,3'-indo lyl)]-1(H)-pyrrole-2,5-dione or its acid salt.
    Type: Grant
    Filed: August 26, 1997
    Date of Patent: August 22, 2000
    Assignee: Eli Lilly and Company
    Inventors: Michael R. Jirousek, Douglas Kirk Ways, Lawrence E. Stramm
  • Therapeutic treatment for autoimmune diseases
    Patent number: 6103713
    Abstract: Methods for inhibiting activation and/or proliferation of T cells and B cells and for treating autoimmune diseases and/or disease manifestations are disclosed, particularly using the isozyme selective PKC inhibitor, (S)-3,4-[N, N'-1,1'-((2"-ethoxy)-3'"(O)-4'"-(N,N-dimethylamino)-butane)-bis-(3,3'-indo ly 1)]-1(H)-pyrrole-2,5-dione and its pharmaceutically acceptable salts.
    Type: Grant
    Filed: February 22, 1999
    Date of Patent: August 15, 2000
    Assignee: Eli Lilly and Company
    Inventors: Douglas Kirk Ways, Daniel Wierda
  • Therapeutic treatment for asthma
    Patent number: 6103712
    Abstract: A method for treating asthma and disease conditions associated therewith is disclosed, particularly using the isozyme selective PKC inhibitor, (S)-3,4-[N,N'-1,1'-((2"-ethoxy)-3'"-(O)-4'"-(N,N-dimethylamino)-butane)-bi s-(3,3'-indoly1)]-1 (H)-pyrrole-2,5-dione and its pharmaceutically acceptable salts.
    Type: Grant
    Filed: February 22, 1999
    Date of Patent: August 15, 2000
    Assignee: Eli Lilly and Company
    Inventor: Douglas Kirk Ways
  • Therapeutic treatment for skin disorders
    Patent number: 6093740
    Abstract: A method for reducing or inhibiting vascular permeability especially the increased vascular permeability associated with VPF/VEGF, and dermal edema exhibited with bullous phemigoid, erythema multiforme, dermatitis herpetiformis, contact dermatitis/delayed hypersensitivity is disclosed, particularly using the .beta.-isozyme selective PKC inhibitor, (S)-3,4-[N,N'-1,1'-((2"-ethoxy)-3'"(O)-4'"-(N,N-dimethylamino)-butane)-bis -(3,3'-indolyl)]-1(H)-pyrrole-2,5-dione and its pharmaceutically acceptable salts.
    Type: Grant
    Filed: April 9, 1998
    Date of Patent: July 25, 2000
    Assignee: Eli Lilly and Company
    Inventors: Michael Robert Jirousek, Lawrence E. Stramm, Louis Vignati, Douglas Kirk Ways
  • Therapeutic treatment for sexual dysfunctions
    Patent number: 6093709
    Abstract: A method for treating sexual dysfunctions is disclosed, particularly using the isozyme selective PKC inhibitor, (S)-3,4-[N,N'-1,1'-((2"-ethoxy)-3'"(O)-4'"-(N,N-dimethylamino)-butane)-bis -(3,3'-indoly1)]-1(H)-pyrrole-2,5-dione, particularly its hydrochloride, or mesylate salt.
    Type: Grant
    Filed: August 19, 1997
    Date of Patent: July 25, 2000
    Assignee: Eli Lilly and Company
    Inventors: Michael R. Jirousek, Douglas Kirk Ways, Lawrence E. Stramm
  • Process for preparing substituted acrylamides by reaction of propiolamides and aromatic rings
    Patent number: 6069247
    Abstract: The present invention relates to a process for preparing acrylamides; wherein, a propiolamide is reacted with an activated aromatic ring to yield a wide variety of acrylamides.
    Type: Grant
    Filed: October 5, 1998
    Date of Patent: May 30, 2000
    Assignee: Eli Lilly and Company
    Inventors: Lynne Ann Hay, David Mitchell
  • Process for preparing bis-indoly macrocycles
    Patent number: 6057440
    Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## wherein R.sub.1, R.sub.2, X, W, and Y are as defined in the specification. The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.
    Type: Grant
    Filed: November 14, 1997
    Date of Patent: May 2, 2000
    Assignee: Eli Lilly and Company
    Inventors: William F. Heath, Jr., Michael R. Jirousek, John H. McDonald, III, Christopher J. Rito
  • Protein kinase C inhibitor
    Patent number: 6015807
    Abstract: This invention provides novel bis-indolylmaleimide macrocycle derivatives of the formula: and solvates thereof. The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.
    Type: Grant
    Filed: November 7, 1997
    Date of Patent: January 18, 2000
    Assignee: Eli Lilly and Company
    Inventors: Gary Lowell Engel, Nagy Alphonse Farid, Margaret Mary Faul, Michael Robert Jirousek, Lori Ann Richardson, Leonard Larry Winneroski, Jr.
  • Synthesis of bisindolylmaleimides
    Patent number: 5990319
    Abstract: The present invention provides for the reaction of optionally substituted indole-3-acetamides with optionally substituted methyl indole-3-glyoxyl reagent to prepare potent PKC inhibitors. The reaction is a very efficient and robust macrocyclization methodology.
    Type: Grant
    Filed: August 22, 1997
    Date of Patent: November 23, 1999
    Assignee: Eli Lilly and Company
    Inventors: Margaret Mary Faul, Leonard Larry Winneroski, Jr.
  • Therapetutic treatment for human T cell lymphotrophic virus type 1 infection
    Patent number: 5962446
    Abstract: A method for treating human T cell lymphotrophic virus type 1 infection using an isozyme selective PKC inhibitor, particularly using the isozyme selective PKC inhibitor, (S)-3,4-?N,N'-1,1'-((2"-ethoxy)-3'"(O)-4'"-(N,N-dimethylamino)-butane)-bis -(3,3'-indolyl)!-1(H)-pyrrole-2,5-dione hydrochloride salt.
    Type: Grant
    Filed: August 26, 1997
    Date of Patent: October 5, 1999
    Assignee: Eli Lilly and Company
    Inventors: Michael R. Jirousek, Douglas Kirk Ways, Lawrence E. Stramm
  • Synthesis of bisindolylmaleimides
    Patent number: 5948907
    Abstract: The present invention provides for the reaction of optionally substituted indole-3-acetamides with optionally substituted methyl indole-3-glyoxyl reagent to prepare potent PKC inhibitors.
    Type: Grant
    Filed: May 19, 1998
    Date of Patent: September 7, 1999
    Assignee: Eli Lilly and Company
    Inventors: Margaret Mary Faul, Leonard Larry Winneroski, Jr.