Patents Assigned to Eli Lilly & Company
  • Cyclization for preparing antifolate compounds
    Patent number: 5969136
    Abstract: This invention provides a process for preparing a compound of formula III ##STR1## wherein R.sup.1 is bromo, iodo or COOR.sup.2 ;R.sup.2 is H, C.sub.1 -C.sub.4 alkyl, phenyl which may be substituted or benzyl; andA is a 5- or 6-membered aromatic residue which may contain up to three hetero atoms and which may optionally be substituted with one or two groups selected from the group consisting of halo, hydroxy, C.sub.1 -C.sub.4 alkyl, and C.sub.1 -C.sub.4 alkoxy; or a salt thereof, which comprises(a) reacting a compound of formula I ##STR2## wherein R is C.sub.1 -C.sub.4 alkyl or phenyl which may be substituted; andR.sup.1, R.sup.2, and A are as defined above;or a salt thereof, with a sulfurization agent;(b) cyclizing the reaction product from step (a) with guanidine; and(c) optionally salifying the reaction product from step (b).
    Type: Grant
    Filed: July 23, 1993
    Date of Patent: October 19, 1999
    Assignee: Eli Lilly and Company
    Inventors: Charles J. Barnett, Thomas M. Wilson
  • Benzothiophene compounds, intermediates, compositions and methods
    Patent number: 5969142
    Abstract: The present invention provides compounds and processes for the preparation of compounds of formula I ##STR1## wherein R.sup.1a is --H or --OR.sup.7a in which R.sup.7a is --H or a hydroxy protecting group;R.sup.2a is --H, halo, or --OR.sup.8a in which R.sup.8a is --H or a hydroxy protecting group;R.sup.
    Type: Grant
    Filed: June 18, 1997
    Date of Patent: October 19, 1999
    Assignee: Eli Lilly and Company
    Inventors: Alan David Palkowitz, Kenneth Jeff Thrasher
  • Process for the synthesis of benzothiophenes
    Patent number: 5969157
    Abstract: The instant invention provides improved processes for preparing benzothiophenes utilizing methanesulfonic acid.
    Type: Grant
    Filed: November 18, 1997
    Date of Patent: October 19, 1999
    Assignee: Eli Lilly and Company
    Inventor: Jeffrey Thomas Vicenzi
  • Cyclic peptide antifungal agents
    Patent number: 5965525
    Abstract: Provided are compounds of the formula (1): ##STR1## wherein R' is hydrogen, methyl or NH.sub.2 C(O)CH.sub.2 --;R" and R'" are independently methyl or hydrogen;R and R.sup.y are independently hydroxy or hydrogen;R.sub.1 is hydroxy, hydrogen, or hydroxysulfonyloxy;R.sub.7 is hydroxy, hydrogen, hydroxysulfonyloxy or phosphonooxy;R.sub.2 is a novel acyl side chain. Also provided are novel formulations, methods of inhibiting fungal and parasitic activity, and a process for preparing dideoxy (R=H) forms of the compounds.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: October 12, 1999
    Assignee: Eli Lilly and Company
    Inventors: Frederick J. Burkhardt, Manuel Debono, Jeffrey S. Nissen, William W. Turner, Jr.
  • Pulsatile delivery of leptin receptor ligands
    Patent number: 5965521
    Abstract: This invention provides a method for optimizing the administration of leptin receptor ligands to a mammal in need of such treatment. More specifically, this invention provides an improved method of delivering leptin receptor ligands to a mammal in need of such treatment comprising pulsatile or peak delivery of leptin receptor ligands to treat obesity and related conditions, including hyperglucocorticoidinemia, fertility or delayed puberty, and/or growth hormone deficiencies.
    Type: Grant
    Filed: February 25, 1997
    Date of Patent: October 12, 1999
    Assignee: Eli Lilly Company
    Inventors: Thomas W. Stephens, Mark L. Heiman, Jose F. Caro
  • Benzothiophene compounds, and uses and formulations thereof
    Patent number: 5962698
    Abstract: Novel benzothiophenes, and intermediates thereof, and the uses and formulations thereof, are provided by the present invention.
    Type: Grant
    Filed: June 3, 1998
    Date of Patent: October 5, 1999
    Assignee: Eli Lilly and Company
    Inventors: David Thompson Berg, George Joseph Cullinan, Brian William Grinnell, Mark Alan Richardson
  • Methods of treating or ameliorating the symptoms of common cold or allergic rhinitis with serotonin 5-HT.sub.1F
    Patent number: 5962473
    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-HT.sub.1F agonist.
    Type: Grant
    Filed: August 5, 1997
    Date of Patent: October 5, 1999
    Assignee: Eli Lilly and Company
    Inventors: Kirk Willis Johnson, Lee Alan Phebus
  • Methods for lowering serum cholesterol and inhibiting smooth muscle cell proliferation, restenosis, endometriosis, and uterine fibroid disease
    Patent number: 5962497
    Abstract: The present invention provides novel methods of lowering serum cholesterol and inhibiting smoother muscle cell proliferation, particularly restenosis, in humans, and inhibiting uterine fibroid disease and endometriosis in women comprising administering to a human/woman in need of treatment an effective amount of a compound of formula I ##STR1## wherein R is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halo, or trifluoromethyl;R.sup.1 and R.sup.2 each are the same or different C.sub.1 -C.sub.6 alkyl group;n is an integer from 2 to 6; andR.sup.3 and R.sup.4 each are independently C.sub.1 -C.sub.4 alkyl, or combine to form a substituent selected from the group consisting of pyrrolidino, morpholino, piperidino, piperazino, 4-(C.sub.1 -C.sub.6 alkyl)piperazino, and 4-phenyl-piperazino; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 30, 1998
    Date of Patent: October 5, 1999
    Assignee: Eli Lilly and Company
    Inventors: Henry U. Bryant, Jeffrey A. Dodge
  • 5-substituted-3-(1,2,3,6-tetrahydropyridin-4-yl)-and 3-(piperidin-4-yl)-1h-indoles: 5-HT.sub.1F agonists
    Patent number: 5962474
    Abstract: This invention provides novel 5-HT.sub.1F agonists of Formula I ##STR1## where A--B, R,R.sup.1 and X are as defined in the specification, which are useful for the treatment of migraine and associated disorders.
    Type: Grant
    Filed: November 24, 1997
    Date of Patent: October 5, 1999
    Assignee: Eli Lilly and Company
    Inventors: James Edmund Audia, Bruce Anthony Dressman, James Joseph Droste, James Erwin Fritz, Stephen Warren Kaldor, Daniel James Koch, Joseph Herman Krushinski, Jr., Jeffrey Scott Nissen, Vincent Patrick Rocco, John Mehnert Schaus, Dennis Charles Thompson
  • Substituted benzo(B)thiophene compounds having activity as selective estrogen receptor modulators
    Patent number: 5962475
    Abstract: The present invention provides compounds with nitrogen, sulfur or carbon linked basic side chains of formula ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen, halo, hydroxy, alkoxy, alkylcarbonyloxy, alkoxycarbonyl, alkoxycarbonyloxy, arylcarbonyloxy, aryloxycarbonyloxy, or alkylsulfonyloxy; O--SO.sub.2 --(C.sub.4 -C.sub.6 alkyl), chloro, fluoro, or bromo; W is CHOH, C(O), or CH.sub.2 ; Y is --CH.sub.2 --, --NH--, --NMe--, --S--, --SO.sub.2 --; and R.sup.3 and R.sup.4 are independently hydrogen, alkyl, alkylcarbonyl, alkylamino-carbonyl, or arylcarbonyl, or together with the nitrogen to which they are attached form 1-pyrrolidinyl, 1-piperidinyl, or a 5- or 6-membered imide or cyclic amide ring.
    Type: Grant
    Filed: October 23, 1997
    Date of Patent: October 5, 1999
    Assignee: Eli Lilly and Company
    Inventors: Christopher Randall Schmid, James Patrick Sluka, Kristin Sue Marron
  • 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
  • Benzo?b!thiophene compounds, intermediates, formulations, and methods
    Patent number: 5958969
    Abstract: This invention relates to the field of pharmaceutical and organic chemistry and provides benzothiophene compounds, intermediates, formulations, and methods.
    Type: Grant
    Filed: September 3, 1997
    Date of Patent: September 28, 1999
    Assignee: Eli Lilly and Company
    Inventors: Henry Uhlman Bryant, Michael John Martin, Ken Matsumoto
  • Process for preparing 3-substituted indazoles
    Patent number: 5959121
    Abstract: The invention provides a method of preparing compounds of formula I and VIII: ##STR1## which are useful intermediates to compounds that are used as antagonists and partial agonists for the serotonin receptor 5-HT.sub.4.
    Type: Grant
    Filed: December 14, 1998
    Date of Patent: September 28, 1999
    Assignee: Eli Lilly and Company
    Inventor: Thomas Michael Wilson
  • Benzofluorene compounds, intermediates, compositions, and methods
    Patent number: 5958917
    Abstract: The present invention provides compounds of formula I ##STR1## wherein R.sub.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.6 alkyl), --OCOO(C.sub.1 -C.sub.6 alkyl), --OCOAr, --OCOOAr, or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);R.sub.2 is --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.6 alkyl), --OCOO(C.sub.1 -C.sub.6 alkyl), --OCOAr, --OCOOAr, or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);R.sub.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; andn is 2 or 3;or a pharmaceutically acceptable salt or solvate thereof.
    Type: Grant
    Filed: September 24, 1997
    Date of Patent: September 28, 1999
    Assignee: Eli Lilly and Company
    Inventors: Thomas Alan Crowell, Charles David Jones, Henry Uhlman Bryant
  • Potentiation of serotonin response
    Patent number: 5958429
    Abstract: The availability of serotonin, norepinephrine and dopamine in the brain is increased by administering a serotonin reuptake inhibitor with a serotonin 1A antagonist and L-tryptophan or 5-hydroxy-L-tryptophan.
    Type: Grant
    Filed: July 28, 1998
    Date of Patent: September 28, 1999
    Assignee: Eli Lilly and Company
    Inventor: David T Wong
  • Excitatory amino acid receptor modulators
    Patent number: 5958960
    Abstract: Compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are as defined in the specification, and non-toxic metabolically labile ester and amides thereof are useful as modulators of metabotropic glutamate receptor function.
    Type: Grant
    Filed: May 13, 1998
    Date of Patent: September 28, 1999
    Assignee: Eli Lilly and Company
    Inventors: Steven Marc Massey, James Allen Monn, Matthew John Valli
  • Dihydronaphthalene and naphthalene compounds, intermediates, formulations, and methods
    Patent number: 5958916
    Abstract: The instant invention provides dihydronaphthalene and naphthalene compounds, intermediates, formulations, and methods for use in the treatment of bone loss or bone resorption.
    Type: Grant
    Filed: August 26, 1997
    Date of Patent: September 28, 1999
    Assignee: Eli Lilly and Company
    Inventors: Henry Uhlman Bryant, Thomas Alan Crowell, Charles David Jones
  • Method for treating depression with olanzapine
    Patent number: 5958921
    Abstract: This invention relates to the use of the antipsychotic drug olanzapine for the treatment of depression, including depressive signs and symptoms and Major Depression.
    Type: Grant
    Filed: June 18, 1998
    Date of Patent: September 28, 1999
    Assignee: Eli Lilly and Company
    Inventor: Gary D Tollefson
  • Streptococcus pneumoniae gene sequence FtsY
    Patent number: 5958730
    Abstract: The invention provides isolated nucleic acid compounds encoding FtsY of Streptococcus pneumoniae. Also provided are vectors and transformed host cells for expressing the encoded protein, and a method for identifying compounds that bind and/or inhibit said protein.
    Type: Grant
    Filed: December 8, 1997
    Date of Patent: September 28, 1999
    Assignee: Eli Lilly and Company
    Inventors: Paul Luther Skatrud, Robert Brown Peery, Q May Wang, Paul Robert Rosteck, Jr., Michele Louise Young Bellido
  • Naphthofluorene compounds, intermediates, compositions, and methods
    Patent number: 5959103
    Abstract: The invention provides naphthofluorene compounds, intermediates, formulations, processes, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, cardiovascular-related pathological conditions, including hyperlipidemia, and estrogen-dependent cancer.
    Type: Grant
    Filed: September 30, 1998
    Date of Patent: September 28, 1999
    Assignee: Eli Lilly and Company
    Inventors: Henry Uhlman Bryant, Jeffrey Alan Dodge, Charles Willis Lugar, III