Patents Represented by Attorney MaCharri R. Vorndran-Jones
  • Patent number: 7259175
    Abstract: The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts thereof, Formula I: wherein: (a) R5 is selected from the group consisting of (C1-C6) alkyl, (C1-C6) alkenyl, substituted aryl(C0-C4)alkyl, substituted aryloxy(C0-C4)alkyl, substituted arylthio(C0-C4)alkyl, unsubstituted aryl(C0-C4)alkyl, unsubstituted aryloxy(C0-C4)alkyl, and unsubstituted arylthio(C0-C4)alkyl; (b) T1 is C or N; (c) Q is selected from the group consisting of O, a single bond, O(CH2)q and C; (d) q is 1 or 2; (e) W is selected from the group consisting of O, S, (CH2)rN(R20)(CH2)k, NHSO2, C(O)N(R20)(CH2)r, (CH2)rN(R20)C(O), and SO2; (f) X is CmH2m; (g) m is 0, 1 or 2; (h) A is an functional group selected from the group consisting of carboxyl, C1-C3 alkylnitrile, carboxamide, and (CH2)n COOR19; and (i) R19 is selected from the group consisting of hydrogen, optionally substituted C1-C4alkyl and optionally substituted arylmethyl
    Type: Grant
    Filed: February 13, 2003
    Date of Patent: August 21, 2007
    Assignee: Eli Lilly and Company
    Inventors: Scott Eugene Conner, Nathan Bryan Mantlo, Guoxin Zhu
  • Patent number: 6686365
    Abstract: The present invention provides a pharmaceutical composition comprising pemetrexed; at least one antioxidant selected from the group consisting of monothioglycerol, L-cysteine, and thioglycolic acid; and a pharmaceutically acceptable excipient. The pharmaceutical formulation is suitable for liquid parenteral administration.
    Type: Grant
    Filed: October 4, 2002
    Date of Patent: February 3, 2004
    Assignee: Eli Lilly and Company
    Inventors: Bernd Ulrich Riebesehl, Jens Kemken
  • Patent number: 6187798
    Abstract: The present invention provides aza-bicyclo[2.2.1]heptane compounds which are useful for modulating a muscarinic receptor.
    Type: Grant
    Filed: June 1, 1999
    Date of Patent: February 13, 2001
    Assignee: Eli Lilly and Company
    Inventors: Leander Merritt, Lone Jeppesen, John S. Ward
  • Patent number: 6071900
    Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.
    Type: Grant
    Filed: March 22, 1999
    Date of Patent: June 6, 2000
    Assignee: Eli Lilly and Company
    Inventors: Leander Merritt, John S. Ward
  • Patent number: 6043258
    Abstract: This invention relates to the use of xanomeline for the treatment of Disruptive Behavior Disorder and Attention Deficit Hyperactivity Disorder.
    Type: Grant
    Filed: December 16, 1998
    Date of Patent: March 28, 2000
    Assignee: Eli Lilly and Company
    Inventors: Franklin P Bymaster, Harlan E Shannon
  • Patent number: 6030966
    Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.
    Type: Grant
    Filed: July 28, 1999
    Date of Patent: February 29, 2000
    Assignee: Eli Lilly and Company
    Inventors: Leander Merritt, John S. Ward
  • Patent number: 5821371
    Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: October 13, 1998
    Assignee: Eli Lilly and Comany
    Inventors: Charles A. Alt, Leander Merritt, Gary A. Rhodes, Roger L. Robey, Eldon E. Van Meter, John S. Ward, Charles H. Mitch
  • Patent number: 5736544
    Abstract: The present invention provides methods for binding a 5-HT.sub.2B receptor in mammals using both known and novel compounds. Further, the invention provides a method for treating or preventing 5-HT.sub.2B related conditions. Finally, the invention provides an article of manufacture.
    Type: Grant
    Filed: March 25, 1996
    Date of Patent: April 7, 1998
    Assignee: Eli Lilly and Company
    Inventors: James E. Audia, Marlene L. Cohen, Jaswant S. Gidda, David L. G. Nelson
  • Patent number: 5629317
    Abstract: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: May 13, 1997
    Assignee: Eli Lilly and Company
    Inventors: James E. Audia, Stephen R. Baker, Jesus E. Carrera, Carlos L. Peteira, Concepcion P. Tercero
  • Patent number: 5580900
    Abstract: A compound of the formula: ##STR1## in which each R.sup.1 to R.sup.4 group is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxy-carbonyl, halo, hydroxy, nitro, cyano, trihalomethyl or optionally substituted phenyl, each R.sup.5 to R.sup.16 group is hydrogen or C.sub.1-4 alkyl, each Z', Z", Z'" and Z"" group is an alkylene radical, and X and Y are each --(CH.sub.2).sub.n -- or --(CH.sub.2).sub.m --A--(CH.sub.2).sub.p -- where A is --CH.dbd.CH--, optionally substituted phenylene or optionally substituted naphthalenyl, n is 2 to 10, and m and p are each 1 or 2, salts thereof, and intermediates for the production thereof.
    Type: Grant
    Filed: November 30, 1994
    Date of Patent: December 3, 1996
    Assignee: Lilly Industries Limited
    Inventors: Barry P. Clark, John R. Harris
  • Patent number: 5576435
    Abstract: The present invention provides novel intermediates which are useful for the preparation of excitatory amino acid receptor antagonists. Further provided is a process to enatioselectively prepare hydroisoquinoline compounds with central nervous system activity.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: November 19, 1996
    Assignee: Eli Lilly and Company
    Inventors: Anita Melikian-Badalian, Paul L. Ornstein
  • Patent number: 5574028
    Abstract: The present invention provides a method for treating anxiety in a human in need thereof, comprising administering to the human an antianxiety amount of a muscarinic agonist compound of the general formula ##STR1## wherein Z is a 5-membered heterocyclic ring as defined in the disclosure.
    Type: Grant
    Filed: October 31, 1994
    Date of Patent: November 12, 1996
    Assignee: Eli Lilly and Company
    Inventors: Neil C. Bodick, Franklin P. Bymaster, Walter W. Offen, Harlan E. Shannon
  • Patent number: 5574158
    Abstract: A compound of the formula: ##STR1## in which each R.sup.1 to R.sup.4 group is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxy-carbonyl, halo, hydroxy, nitro, cyano, trihalomethyl or optionally substituted phenyl, each R.sup.5 to R.sup.16 group is hydrogen or C.sub.1-4 alkyl, each Z', Z", Z'" and Z"" group is an alkylene radical, and X and Y are each --(CH.sub.2).sub.n -- or --(CH.sub.2).sub.m --A--(CH.sub.2).sub.p -- where A is --CH.dbd.CH--, optionally substituted phenylene or optionally substituted naphthalenyl, n is 2 to 10, and m and p are each 1 or 2, salts thereof, and intermediates for the production thereof.
    Type: Grant
    Filed: February 20, 1996
    Date of Patent: November 12, 1996
    Assignee: Lilly Industries Limited
    Inventors: Barry P. Clark, John R. Harris
  • Patent number: 5574029
    Abstract: The present invention provides a method for treating anxiety in a human in need thereof, comprising administering an antianxiety amount of a muscarinic agonist compound of the general formula ##STR1## wherein X R.sup.43, R.sup.44, R.sup.45 and R.sup.46 are defined in the disclosure.
    Type: Grant
    Filed: May 23, 1995
    Date of Patent: November 12, 1996
    Assignee: Eli Lilly and Company
    Inventors: Neil C. Bodick, Franklin P. Bymaster, Walter W. Offen, Harlan E. Shannon
  • Patent number: 5574169
    Abstract: The present invention provides an enantiomerically selective process and intermediates for preparing certain 4,5-disubstituted pyrazolidinones and intermediates which are useful for treating diseases of the central nervous system.
    Type: Grant
    Filed: February 16, 1995
    Date of Patent: November 12, 1996
    Assignee: Eli Lilly and Company
    Inventors: William B. Blanchard, Thomas C. Britton, David L. Varie
  • Patent number: 5574053
    Abstract: The present invention provides a method for treating anxiety in humans using a compound of the formula ##STR1## as described in the specification which modulates a muscarinic receptor.
    Type: Grant
    Filed: May 23, 1995
    Date of Patent: November 12, 1996
    Assignee: Eli Lilly and Company
    Inventors: Neil C. Bodick, Franklin P. Bymaster, Walter W. Offen, Harlan E. Shannon
  • Patent number: 5399565
    Abstract: Novel substituted pyrazolidinones have been found to exhibit significant binding to cholecystokinin (CCK) receptors and gastrin receptors in the brain and/or peripheral sites such as the pancreas, stomach, and ileum. The pyrazolidinones are CCK and gastrin receptor antagonists and find therapeutic application in the treatment of gastrointestinal disorders, central nervous system disorders and for appetite regulation in warm-blood vertebrates. Pharmaceutical formulations for such indications are described.
    Type: Grant
    Filed: November 12, 1993
    Date of Patent: March 21, 1995
    Assignee: Eli Lilly and Company
    Inventors: Beverley Greenwood, David R. Helton, J. Jeffry Howbert, Steven J. Mitan, Kurt Rasmussen
  • Patent number: 5399708
    Abstract: The present invention provides an enantiomerically selective process and intermediates for preparing certain 4,5-disubstituted pyrazolidinones and intermediates which are useful for treating diseases of the central nervous system.
    Type: Grant
    Filed: November 12, 1993
    Date of Patent: March 21, 1995
    Assignee: Eli Lilly and Company
    Inventors: William B. Blanchard, Thomas C. Britton, David L. Varie
  • Patent number: 5338735
    Abstract: Compounds of the formula: ##STR1## in which each R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R.sup.2 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl, R.sup.3 and R.sup.4 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or C.sub.6-9 cycloalkyl optionally substituted by 1 to 4 C.sub.1-4 alkyl groups, R.sup.5 is optionally substituted phenyl, tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C.sub.6-10 cycloalkyl optionally substituted with 1 to 4 C.sub.1-4 alkyl groups or a phenyl group, or C.sub.4-9 heterosubstituted cycloalkyl optionally substituted with 1 to 4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof.The compounds are indicated for use in the treatment of disorders of the central nervous system.
    Type: Grant
    Filed: August 12, 1993
    Date of Patent: August 16, 1994
    Assignee: Lilly Industries Limited
    Inventors: John Fairhurst, David E. Tupper
  • Patent number: 5334725
    Abstract: The present invention provides a novel process for preparing a 2-(aminomethyl)-4-thiazolemethanol. The compounds produced by the process of the present invention are useful for synthesizing anti-ulcer compounds such as Nizatidine.
    Type: Grant
    Filed: June 14, 1993
    Date of Patent: August 2, 1994
    Assignee: Eli Lilly and Company
    Inventor: Kenneth P. Moder