Patents Represented by Attorney, Agent or Law Firm James J. Sales
  • Patent number: 5451590
    Abstract: A method of inhibiting sexual precocity comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
    Type: Grant
    Filed: December 21, 1993
    Date of Patent: September 19, 1995
    Assignee: Eli Lilly & Co.
    Inventor: Jeffrey A. Dodge
  • Patent number: 5447941
    Abstract: A method of inhibiting pulmonary hypertensive disease comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
    Type: Grant
    Filed: December 21, 1993
    Date of Patent: September 5, 1995
    Assignee: Eli Lilly and Company
    Inventor: Steven H. Zuckerman
  • Patent number: 5446053
    Abstract: A method of inhibiting dysfunctional uterine bleeding comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethylenemino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
    Type: Grant
    Filed: December 21, 1993
    Date of Patent: August 29, 1995
    Assignee: Eli Lilly and Company
    Inventor: Patrick Keohane
  • Patent number: 5446061
    Abstract: A method of lowering serum cholesterol levels, comprising administering an effective amount of a compound having the formula ##STR1## wherein: R.sup.1 and R.sup.2 are, independently, --H, --OH, halo, --OC.sub.1 -C.sub.17 alkyl, --OC.sub.3 -C.sub.6 cycloalkyl, --O(CO)C.sub.1 -C.sub.17 alkyl, --O(CO) aryl, --O(CO)O aryl, or --OSO.sub.2 -(n-butyl or n-pentyl);R.sup.3 is ##STR2## and R.sup.4 is --H, methyl, ethyl, propyl, ethenyl or ethynyl; or a pharmaceutically acceptable salt or solvate thereof, to an animal in need of lower cholesterol levels.
    Type: Grant
    Filed: November 5, 1993
    Date of Patent: August 29, 1995
    Assignee: Eli Lilly and Company
    Inventors: Henry U. Bryant, Timothy A. Grese
  • Patent number: 5441964
    Abstract: A method of inhibiting bone loss comprising administering to a human in need of treatment an effective amount of a substituted benzothiophene.
    Type: Grant
    Filed: October 15, 1993
    Date of Patent: August 15, 1995
    Assignee: Eli Lilly and Company
    Inventors: Henry U. Bryant, Timothy A. Grese
  • Patent number: 5441947
    Abstract: Wortmannin and certain of its analogs are inhibitors of restinosis.
    Type: Grant
    Filed: August 25, 1993
    Date of Patent: August 15, 1995
    Assignee: Eli Lilly and Company
    Inventors: Jeffrey A. Dodge, Masahiko Sato
  • Patent number: 5441966
    Abstract: A method of inhibiting Turner's Syndrome comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
    Type: Grant
    Filed: December 21, 1993
    Date of Patent: August 15, 1995
    Assignee: Eli Lilly and Company
    Inventor: Jeffrey A. Dodge
  • Patent number: 5441965
    Abstract: A method of inhibiting thrombin and its attending diseases and conditions comprising administering to a human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidino, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
    Type: Grant
    Filed: December 21, 1993
    Date of Patent: August 15, 1995
    Assignee: Eli Lilly and Company
    Inventors: Daniel J. Sall, Gerald F. Smith
  • Patent number: 5439923
    Abstract: A method of inhibiting acne or seborrhea comprising administering to a human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
    Type: Grant
    Filed: December 21, 1993
    Date of Patent: August 8, 1995
    Assignee: Eli Lilly and Company
    Inventor: George J. Cullinan
  • Patent number: 5439931
    Abstract: A method of increasing libido in post-menopausal women comprising administering to a female human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, -CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneimino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
    Type: Grant
    Filed: December 21, 1993
    Date of Patent: August 8, 1995
    Assignee: Eli Lilly and Company
    Inventor: James J. Sales
  • Patent number: 5436258
    Abstract: The administration of a xanthine oxidase inhibitor is effective for the treatment or prevention of the excessive resorption of bone in conditions such as osteoporosis and the like.
    Type: Grant
    Filed: September 9, 1992
    Date of Patent: July 25, 1995
    Assignees: Eli Lilly and Company, London Hospital Medical College, St. George's Hospital Medical School
    Inventors: David R. Blake, Jill A. Panetta, Mone Zaidi
  • Patent number: 5434259
    Abstract: Provided is a process for isolating cefaclor from an acylation reaction mixture by adding anthraquinone-1,5-disulfonic acid to the mixture. The acid highly selectively precipitates with cefaclor so that isolation and recovery is streamlined.
    Type: Grant
    Filed: February 5, 1993
    Date of Patent: July 18, 1995
    Assignee: Eli Lilly and Company
    Inventor: John P. Gardner
  • Patent number: 5434166
    Abstract: A method of inhibiting demyelinating or dysmyelinating diseases or their symptoms comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
    Type: Grant
    Filed: August 22, 1994
    Date of Patent: July 18, 1995
    Assignee: Eli Lilly and Company
    Inventor: Andrew L. Glasebrook
  • Patent number: 5424203
    Abstract: A method for selectively deactivating catalase while retaining D-amino acid oxidase activity is disclosed. The catalase and the oxidase are both present in whole cells or a cell-free extract. The method comprises combining the whole cells or the cell-free extract with a basic solution at a pH between about 11 and about 12 for a time of about 1 hour and 45 minutes to about 2 hours. The catalase activity is eliminated and the oxidase activity is uneffected. This results in the production of a solution which contains the oxidase and which has no catalase activity. The pH of the solution containing the oxidase is then lowered to provide a D-amino acid oxidase capable of enzymatic oxidation of cephalosporin C to glutaryl-7-ACA in high yields. The whole cells and cell-free extract are preferrably from Triginopsis variablilis.
    Type: Grant
    Filed: March 11, 1994
    Date of Patent: June 13, 1995
    Assignee: Eli Lilly and Company
    Inventor: Jeffrey T. Vicenzi
  • Patent number: 5420349
    Abstract: A group of 2-amino-3-aroyl-benzo[.beta.]thiophenes are prepared by preparing an .alpha.-hydroxy thioacetamide by silyl mediated condensation of an aldehyde with an anion of dialkylamino thioformamide, cyclizing the .alpha.-hydroxy thioamide, and subsequently acylating the benzo[.beta.]thiophene to yield the 2-amino-3-aryl derivative. These compounds may be treated with suitable phenyl Grignard reagents, and after deprotection, yield 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[.beta .]thiophene.
    Type: Grant
    Filed: June 10, 1994
    Date of Patent: May 30, 1995
    Assignee: Eli Lilly and Company
    Inventor: Alexander G. Godfrey
  • Patent number: 5418252
    Abstract: A method of inhibiting cartilage degradation comprising administering to a human or other mammal in need of treatment an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidino and piperidino, a pharmaceutically acceptable salt or solvate thereof.
    Type: Grant
    Filed: October 15, 1993
    Date of Patent: May 23, 1995
    Assignee: Eli Lilly and Company
    Inventor: Daniel C. Williams
  • Patent number: 5412094
    Abstract: The invention provides complexes of the formula: ##STR1## wherein X is chloro, hydrogen, vinyl, or --CH.sub.3,Z is O;is 0-5;Y is phenyl or 1,4-cyclohexadien-1-yl;R.sub.1 and R.sub.2 are hydrogen or hydroxy, with the proviso that R.sub.1 and R.sub.2 are not both hydrogen andR.sub.3 is --COO.sup.-, --COO(C.sub.1 -C.sub.4 alkyl), --NO.sub.2 or ##STR2## wherein R.sub.4 is C.sub.1 -C.sub.4 alkyl.
    Type: Grant
    Filed: June 28, 1993
    Date of Patent: May 2, 1995
    Assignee: Eli Lilly and Company
    Inventors: Jane G. Amos, Joseph M. Indelicato, Carol E. Pasini, Susan M. Reutzel
  • Patent number: 5407947
    Abstract: A method of inhibiting bone loss comprising administering to an animal an effective amount of a compound having the formula ##STR1## wherein: R.sup.1 and R.sup.2 are, independently, --H, --OH, halo, --OC.sub.1 -C.sub.17 alkyl, --OC.sub.3 -C.sub.6 cycloalkyl, --O(CO)C.sub.1 -C.sub.17 alkyl, --O(CO) aryl, --O(CO)O aryl, or --OSO.sub.2 -(n-butyl or n-pentyl);R.sup.3 is ##STR2## R.sup.4 is --H, methyl, ethyl, propyl, ethenyl or ethynyl; or a pharmaceutically acceptable salt or solvate thereof.
    Type: Grant
    Filed: November 5, 1993
    Date of Patent: April 18, 1995
    Assignee: Eli Lilly and Company
    Inventors: Henry U. Bryant, Timothy A. Grese
  • Patent number: 5399686
    Abstract: The invention is directed to the crystalline isopropyl alcohol solvate of loracarbef, and also is directed to a process for the preparation of the crystalline monohydrate form of the compound of formula (I) ##STR1## which includes exposing the crystalline isopropyl solvate form of the compound of formula (I) to a temperature of between about 50.degree. and 90.degree. C. and a relative humidity of between about 60 to about 100%.
    Type: Grant
    Filed: June 4, 1993
    Date of Patent: March 21, 1995
    Assignee: Eli Lilly and Company
    Inventors: William C. Henning, Michael E. O'Dea
  • Patent number: 5393882
    Abstract: A method for preparing 2-amino-.beta.-lactams which are substituted by readily-removed protecting groups is provided. According to this invention, an acyl-2-amino-.beta.-lactam is further acylated with a different acyl group and is subsequently treated with base to provide a protected 2-amino .beta.-lactam with a more desirable protecting group.
    Type: Grant
    Filed: February 24, 1993
    Date of Patent: February 28, 1995
    Assignee: Eli Lilly and Company
    Inventors: Larry C. Blaszczak, John E. Munroe, Douglas O. Spry