Patents Represented by Attorney, Agent or Law Firm Robert D. Titus
  • Patent number: 7745438
    Abstract: The present invention provides BACE inhibitors of Formula (I); methods for their use and preparation, and intermediates useful for their preparation.
    Type: Grant
    Filed: September 20, 2005
    Date of Patent: June 29, 2010
    Assignee: Eli Lilly and Company
    Inventors: Howard Barff Broughton, Robert Dean Dally, Timothy Barrett Durham, Maria Rosario Gonzalez-Garcia, Patric James Hahn, Kenneth James Henry, Jr., Todd Jonathan Kohn, James Ray McCarthy, Timothy Alan Shepherd, Jon Andre Erickson, Ana Belen Bueno Melendo
  • Patent number: 7491716
    Abstract: The present invention provides kinase inhibitors of Formula I.
    Type: Grant
    Filed: March 4, 2003
    Date of Patent: February 17, 2009
    Assignee: Eli Lilly and Company
    Inventor: Thomas Albert Engler
  • Patent number: 7468365
    Abstract: The present invention provides crystalline (N)-((S)-2-hydroxy-3-methyl-butyryl)-1-(L-alaninyl)-(S)-1-amino-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepin-2-one, a crystalline anydrate and dihydrates thereof, compositions comprising (N)-((S)-2-hydroxy-3-methyl-butyryl)-1-(L-alaninyl)-(S)-1-amino-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepin-2-one, its crystalline anhydrate or dihydrate, and methods for using the same.
    Type: Grant
    Filed: January 11, 2006
    Date of Patent: December 23, 2008
    Assignees: Eli Lilly and Company, Elan
    Inventors: James Edmund Audia, Benjamin Alan Diseroad, Varghese John, Lee H. Latimer, Jeffrey Scott Nissen, Gregory Alan Stephenson, Eugene D. Thorsett, Jay S. Tung
  • Patent number: 7417064
    Abstract: There is provided a compound of formula (I) wherein A is selected from —O— and —S—; X is selected from C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1-C4 alkyl; Z is selected from H, OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl
    Type: Grant
    Filed: October 24, 2003
    Date of Patent: August 26, 2008
    Assignee: Eli Lilly and Company
    Inventors: Serge Louis Boulet, Sandra Ann Filla, Peter Thaddeus Gallagher, Kevin John Hudziak, Anette Margareta Johansson, Rushad E. Karanjawala, John Joseph Masters, Victor Giulio Matassa, Brian Michael Mathes, Richard Edmund Rathmell, Maria Ann Whatton, Chad Nolan Wolfe
  • Patent number: 7410982
    Abstract: There is provided a heretoaryloxy/thio 3-substituted propanamine compound of formula (I) wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C1-C4 alkyl and C1-C4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C1-C4 alkyl, and C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl —S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, and thienopyridyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro acetyl, —CF3, —SCF3 a
    Type: Grant
    Filed: October 24, 2003
    Date of Patent: August 12, 2008
    Assignee: Eli Lilly and Company
    Inventors: Serge Louis Boulet, Sandra Ann Filla, Peter Thaddeus Gallagher, Kevin John Hudziak, Anette Margareta Johansson, Rushad E. Karanjawala, John Joseph Masters, Brian Michael Mathes, Richard Edmund Rathmell, Maria Ann (nee Fagan) Whatton, Victor Matassa, Chad Nolan Wolfe
  • Patent number: 7410996
    Abstract: There is provided a compound of formula (I) wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C1-C4 alkyl and C1-C4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C1-C4 alkyl, and C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0,
    Type: Grant
    Filed: October 24, 2003
    Date of Patent: August 12, 2008
    Assignee: Eli Lilly and Company
    Inventors: Serge Louis Boulet, Sandra Ann Filla, Peter Thaddeus Gallagher, Kevin John Hudziak, Anette Margareta Johansson, Rushad E. Karanjawala, John Joseph Masters, Victor Giulio Matassa, Brian Michael Mathes, Richard Edmund Rathmell, Maria Ann Whatton, Chad Nolan Wolfe
  • Patent number: 7405305
    Abstract: The present invention provides kinase inhibitors of Formula (I)
    Type: Grant
    Filed: March 5, 2003
    Date of Patent: July 29, 2008
    Assignee: Eli Lilly and Company
    Inventors: Pamela Ann Albaugh, Jochen Ammenn, Timothy Paul Burkholder, Joshua Ryan Clayton, Scott Eugene Conner, Brian Eugene Cunningham, Thomas Albert Engler, Kelly Wayne Furness, James Robert Henry, Sushant Malhotra, Mark Joseph Tebbe, Guoxin Zhu, YiHong Li, Brian Raymond Berridge, Charles Edward Ruegg, John Morris Sullivan
  • Patent number: 7390801
    Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: May 12, 2006
    Date of Patent: June 24, 2008
    Assignees: Athena Neurosciences, Inc., Eli Lilly and Company
    Inventors: Eugene D. Thorsett, Michael A. Pleiss, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Bruce A. Dressman, James J. Droste, Steven S. Henry, Russell D. Stucky, Warren J. Porter
  • Patent number: 7384934
    Abstract: Described herein are compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, S, and O; Alk is (C1-4) alkylene or hydroxy substituted (C1-4) alkylene; X is oxygen or sulfur; R1 is hydrogen, (C1-6) fluroalkyl, (C3-6) cycloalkyl, or (C1-4) alkyl, wherein the (C1-4) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCH2CH2OH, or —CN; R2 is H, halogen, (C1-6) fluoroalkyl, (C1-6) cycloalkyl, OR4, SR4, NO2, CN, COR4, C(O)OR4, CONR5R6, NR5R6, SO2NR5R6, NR5COR4, NR5SO2R4, optionally substituted aromatic, or (C1-6) alkyl, wherein (C1-6) alkyl is unsubstituted or substituted with a hydroxy group; R3 is hydrogen (C1-6) fluoroalkyl, (C2-6) alkenyl, Ar, (C1-4)alkyl-Ar, or (C1-4) alkyl wherein (C1-4) alkyly is unsubstituted or substituted with a phenyl; R4 is hydrogen, (C1-6) alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionally
    Type: Grant
    Filed: July 28, 2003
    Date of Patent: June 10, 2008
    Assignee: Eli Lilly and Company
    Inventors: Thomas Daniel Aicher, Zhaogen Chen, Yvan LeHuerou, Fionna Mitchell Martin, Marta Maria Pineiro-Nunez, Vincent Patrick Rocco, Kevin Michael Ruley, John Mehnert Schaus, Patrick Gianpietro Spinazze, David Edward Tupper
  • Patent number: 7294623
    Abstract: A compound of formula (I) (I) wherein R is H; Ar is an aromatic group selected from phenyl; X is a phenyl group; R? is H or C1-C4 alkyl; each R1 is independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereof
    Type: Grant
    Filed: August 18, 2003
    Date of Patent: November 13, 2007
    Assignee: Eli Lilly and Company
    Inventors: Barry Peter Clark, Peter Thaddeus Gallagher, Helen Louise Haughton
  • Patent number: 7214673
    Abstract: Described herein are antipyschotic compounds of formula (I) wherein, A is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, O, and S; Alk is (C1-4) alkylene optionally substituted with OH, methoxy, ethoxy, or F; Ar is optionally substituted phenyl, naphthyl, monocyclic heteroaromatic, or bicyclic heteroaromatic; R1 is hydrogen or (C1-4) alkyl optionally substituted with OH, OR3, or OCH2CH2OH, wherein R3 is (C1-2) alkyl; R2 is H, (C1-6) alkyl, halogen, fluorinated (C1-6) alkyl, OR4, SR4, NO2, CN, COR4, CONR5R6, SO2NR5R6, NR5R6, NR5COR4, NR5SO2R4, or optionally substituted phenyl, wherein R4 is hydrogen, (C1-6) alkyl, fluorinated (C1-6) alkyl, or optionally substituted phenyl, R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionally substituted phenyl; Z is one or two substituents independently selected from hydrogen, halogen, (C1-6) alkyl, fluorinated (C1-6) alkyl, OR7, SR7, NO2, CN, COR7, CONR8R9, SO2NR8R9, NR8SO2R
    Type: Grant
    Filed: March 17, 2003
    Date of Patent: May 8, 2007
    Assignee: Eli Lilly and Company
    Inventors: Thomas Daniel Aicher, Zhaogen Chen, Joseph Herman Krushinski, Jr., Yvan Le Huerou, Marta Maria Pineiro-Nunez, Kevin Michael Ruley, John Mehnert Schaus, Dennis Charles Thompson, David Edward Tupper, Ying Chen, Margaret Mary Faul, Vincent Patrick Rocco
  • Patent number: 7153847
    Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: December 12, 2003
    Date of Patent: December 26, 2006
    Assignees: Athena Neurosciences, Inc., Eli Lilly and Company
    Inventors: Jing Wu, Jay S. Tung, Jeffrey S. Nissen, R. Jeffrey Neitz, James A. Audia, Thomas E. Mabry
  • Patent number: 6951854
    Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: September 29, 2004
    Date of Patent: October 4, 2005
    Assignees: Athena Neurosciences, Inc., Eli Lilly and Company
    Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
  • Patent number: 6683114
    Abstract: Norepinephrine reuptake inhibitors are used to treat psoriasis.
    Type: Grant
    Filed: August 7, 2002
    Date of Patent: January 27, 2004
    Assignee: Eli Lilly and Company
    Inventor: Holly Read Thomasson
  • Patent number: 6610680
    Abstract: This invention provides substituted 2-(azetidinon-1-yl) acetic acid derivatives of Formula II for the antagonism of the vasopressin V1a receptor.
    Type: Grant
    Filed: December 20, 2002
    Date of Patent: August 26, 2003
    Assignee: Eli Lilly and Company
    Inventors: Robert F Bruns, Jr., Robin D G Cooper, Bruce A Dressman, David C Hunden, Stephen W Kaldor, Gary A Koppel, John R Rizzo, Jeffrey J Skelton, Mitchell I Steinberg
  • Patent number: 6541668
    Abstract: The present invention provides processes for the preparation of 3-aryloxy-3-arylpropylamines and intermediates thereof using an nucleophilic aromatic displacement in 1,3-dimethyl-2-imidazolidinone or N-methylpyrrolidinone.
    Type: Grant
    Filed: September 12, 2001
    Date of Patent: April 1, 2003
    Assignee: Eli Lilly and Company
    Inventors: Douglas Patton Kjell, Kurt Thomas Lorenz
  • Patent number: 6521611
    Abstract: This invention provides methods and 2-(azetidin-2-on-1-yl) acetic acid derivatives of Formula I for the antagonism of the vasopressin V1a receptor.
    Type: Grant
    Filed: December 8, 2000
    Date of Patent: February 18, 2003
    Assignee: Eli Lilly and Company
    Inventors: Robert F Bruns, Jr., Robin D G Cooper, Bruce A Dressman, David C Hunden, Stephen W Kaldor, Gary A Koppel, John R Rizzo, Jeffrey J Skelton, Mitchell I Steinberg
  • Patent number: 6380201
    Abstract: This invention provides methods for the treatment or amelioration of the symptoms of the common cold or allergic rhinitis which comprises administering to a mammal in need thereof a serotonin 5-HT1F agonist.
    Type: Grant
    Filed: March 4, 1999
    Date of Patent: April 30, 2002
    Assignee: Eli Lilly and Company
    Inventors: Kirk Willis Johnson, Lee Alan Phebus
  • Patent number: 6376230
    Abstract: This invention provides processes for preparing intermediates useful for the preparation of cryptophycin compounds.
    Type: Grant
    Filed: October 8, 1999
    Date of Patent: April 23, 2002
    Assignee: Eli Lilly and Company
    Inventors: James Abraham Aikins, Barbara Shreve Briggs, Tony Yantao Zhang, Milton Joseph Zmijewski, Jr.
  • Patent number: RE39030
    Abstract: A superior enteric formulation of the antidepressant drug, fluoxetine, is in the form of enteric pellets of which the enteric layer comprises hydroxypropylmethylcellulose acetate succinate.
    Type: Grant
    Filed: January 28, 2002
    Date of Patent: March 21, 2006
    Assignee: Eli Lilly and Company
    Inventors: Neil Robert Anderson, Roger Garrick Harrison, Daniel Frederick Lynch, Peter Lloyd Oren