Patents by Inventor George Joseph Cullinan

George Joseph Cullinan has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 6432983
    Abstract: The instant invention provides compound of formula I wherein: R1 is —H, —OH, —O(C1-C4 alkyl), —O—CO—(C1-C6 alkyl), —O—CO—O(C1-C6 alkyl), —O—CO—Ar in which Ar is optionally substituted phenyl, or —O—SO2—(C4-C6 alkyl); R2 is —H, —OH, —O(C1-C4 alkyl), —O—CO—(C1-C6 alkyl), —O—CO—O(C1-C6 alkyl), —O—CO—Ar in which Ar is optionally substituted phenyl, —O—SO2—(C4-C6 alkyl), —F, —Cl, or —Br; n is an integer from 5 to 8; R3 and R4 each are independently C1-C4 alkyl, or combine to form, with the nitrogen to which they are attached, piperidinyl, pyrrolidinyl, methylpyrrolidinyl, dimethylpyrrolidinyl, or hexamethyleneimino; or a pharmaceutically acceptable salt or solvate thereof, intermediates, pharmaceutical formulations, processes, and methods of use.
    Type: Grant
    Filed: June 30, 1997
    Date of Patent: August 13, 2002
    Assignee: Eli Lilly and Company
    Inventors: George Joseph Cullinan, Kennan Joseph Fahey
  • Patent number: 6432982
    Abstract: The invention provides novel benzothiophenes of the formula: wherein R1 is —H, —OH, —O(C1-C4 alkyl), —O—CO(C1-C6 alkyl), —OSO2(C4-C6 alkyl, or —OCOAr where Ar is optionally substituted phenyl; R2 is —H, —OH, —Cl, —Br, —O(C1-C4 alkyl), —OCO(C1-C6 alkyl), —OSO2(C4-C6 alkyl, or —OCOAr where Ar is optionally substituted phenyl; R3 is —H, —F, —Cl, —(C1-C4 alkyl), —CN, or —O(C1-C3 alkyl); R4 is —H, —F, —Cl, —(C1-C4 alkyl), —CN or —O(C1-C3 alkyl); R5 is —H, —F, —Cl, —(C1-C4 alkyl), or —O(C1-C3 alkyl); and R6 is —H, —F, —Cl, —(C1-C4 alkyl), or —O(C1-C3 alkyl); with the provisos that R3, R4, R5 and R6 can not all be hydrogen, and that when one of R3, R4, R5 or R6 is C1-C4 alkyl, no more than two of R3, R4, R5 and R6 can be hydrogen; Y is —CO—, —CHOH—, or &mda
    Type: Grant
    Filed: January 14, 1997
    Date of Patent: August 13, 2002
    Assignee: Eli Lilly and Company
    Inventors: George Joseph Cullinan, Kennan Joseph Fahey
  • Patent number: 6410565
    Abstract: The present invention relates to an &agr;1-adrenergic receptor antagonist of formula I or an N-oxide or pharmaceutical salt or solvate thereof; wherein A is a moiety selected from the group consisting of:
    Type: Grant
    Filed: June 22, 2001
    Date of Patent: June 25, 2002
    Assignee: Eli Lilly and Company
    Inventor: George Joseph Cullinan
  • Patent number: 6403615
    Abstract: This invention provides methods which are useful for the inhibition of the various medical conditions associated with estrogen deprivation syndrome including osteoporosis and hyperlipidemia utilizing compounds of formula I:
    Type: Grant
    Filed: September 29, 2000
    Date of Patent: June 11, 2002
    Assignee: Eli Lilly and Company
    Inventor: George Joseph Cullinan
  • Patent number: 6395769
    Abstract: This invention provides methods which are useful for the inhibition of the various medical conditions associated with estrogen deprivation syndrome including osteoporosis and hyperlipidemia utilizing compounds of formula I:
    Type: Grant
    Filed: May 12, 2000
    Date of Patent: May 28, 2002
    Assignee: Eli Lilly and Company
    Inventor: George Joseph Cullinan
  • Patent number: 6258826
    Abstract: Formulations and applications thereof are described which are useful for the inhibition of various medical conditions associated with estrogen deprivation syndrome including osteoporosis and hyperlipidemia utilizing compounds of structure I represented by the following structure in combination with compounds of formula II represented by the following structure where X, Y, R, R′, R6, R7 and R8 are as defined herein.
    Type: Grant
    Filed: September 1, 1999
    Date of Patent: July 10, 2001
    Assignee: Eli Lilly and Company
    Inventors: George Joseph Cullinan, Brian Stephen Muehl, Kenneth Jeff Thrasher
  • Patent number: 6156786
    Abstract: This invention provides methods which are useful for the inhibition of the various medical conditions associated with estrogen deprivation syndrome including osteoporosis and hyperlipidemia utilizing compounds of formula I: ##STR1##
    Type: Grant
    Filed: November 4, 1998
    Date of Patent: December 5, 2000
    Assignee: Eli Lilly and Company
    Inventor: George Joseph Cullinan
  • Patent number: 6147092
    Abstract: The invention provides novel benzothiophenes of the formula (I): ##STR1## wherein R.sub.1 is N-pyrrolidinyl or N-piperidinyl; R.sub.2 and R.sub.3 are independently hydrogen,--CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), --CO--(C.sub.10 -C.sub.22 alkynyl),or --CO--(CH.sub.2).sub.n COR.sub.4 ; provided R.sub.2 and R.sub.3 are not both dodecanoyl, and one of R.sub.2 or R.sub.3 is not hydrogenR.sub.4 is -3-cholesteryl or --O(CH.sub.2).sub.2 (OR.sub.5)CH.sub.2 OR.sub.6 ;R.sub.5 and R.sub.6 are independently hydrogen, --CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), or --CO--(C.sub.10 -C.sub.22 alkynyl); provided one of R.sub.5 or R.sub.6 is not hydrogen;n is 0-4; and pharmaceutically acceptable salts and solvates thereof.
    Type: Grant
    Filed: April 19, 1999
    Date of Patent: November 14, 2000
    Assignee: Eli Lilly and Company
    Inventors: George Joseph Cullinan, Raymond Francis Kauffman
  • Patent number: 6121293
    Abstract: The invention provides benzothiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia, and estrogen-dependent cancer.
    Type: Grant
    Filed: June 29, 1998
    Date of Patent: September 19, 2000
    Assignee: Eli Lilly and Company
    Inventors: George Joseph Cullinan, Brian Stephen Muehl
  • Patent number: 6113876
    Abstract: A method of increasing sphincter competence 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, hexamethyleneimino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.Also encompassed by the invention is a method of inhibiting urinary or fecal incontinence, or gastroesophageal disease or its symptoms, which includes administering to a human in need thereof an effective amount of a compound of formula 1.
    Type: Grant
    Filed: January 7, 1997
    Date of Patent: September 5, 2000
    Assignee: Eli Lilly and Company
    Inventor: George Joseph Cullinan
  • Patent number: 6107346
    Abstract: The present application relates to a series of compounds, and pharmaceutical formulations thereof, of the formula ##STR1## which provide a method of inhibiting hyperlipidemia, especially hypercholesterolemia, and the pathological sequelae thereof, in mammals, including humans.
    Type: Grant
    Filed: August 4, 1998
    Date of Patent: August 22, 2000
    Assignee: Eli Lilly and Company
    Inventor: George Joseph Cullinan
  • Patent number: 6096781
    Abstract: This invention provides methods which are useful for the inhibition of the various medical conditions associated with estrogen deprivation syndrome including osteoporosis and hyperlipidemia utilizing compounds of formula I: ##STR1##
    Type: Grant
    Filed: November 4, 1998
    Date of Patent: August 1, 2000
    Assignee: Eli Lilly and Company
    Inventor: George Joseph Cullinan
  • Patent number: 6096764
    Abstract: A method of inhibiting detrimental side-effects of GnRH or GnRH agonist administration in a mammal which comprises the administration to a mannal in need thereof of an effective amount of a compound of formula I ##STR1## wherein R.sup.1 and R.sup.3 are, independently, --H, --CH.sub.3, --CO(C.sub.1 -C.sub.6 alkyl), or --COAr, where Ar is optionally substituted phenyl;R.sup.3 is selected from the group consisting of pyrrolidine, piperidine, and hexamethyleneimino; ora pharmaceutically acceptable salt or solvate thereof.
    Type: Grant
    Filed: August 14, 1998
    Date of Patent: August 1, 2000
    Assignee: Eli Lilly and Company
    Inventors: Henry Uhlman Bryant, George Joseph Cullinan, Jeffrey Alan Dodge
  • Patent number: 6087378
    Abstract: Formulations and applications thereof are described which are useful for the inhibition of various medical conditions associated with estrogen deprivation syndrome including osteoporosis and hyperlipidemia utilizing compounds represented by the following structure where X is a halogen.
    Type: Grant
    Filed: September 1, 1999
    Date of Patent: July 11, 2000
    Assignee: Eli Lilly and Company
    Inventors: George Joseph Cullinan, Brian Stephen Muehl, Kenneth Jeff Thrasher
  • Patent number: 5985865
    Abstract: A method of increasing gastroesophageal sphincter competence 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 pyrrolidino, hexamethyleneimino, and piperidino; or a pharmaceutically acceptable salt or solvate thereof.
    Type: Grant
    Filed: April 20, 1998
    Date of Patent: November 16, 1999
    Assignee: Eli Lilly and Company
    Inventor: George Joseph Cullinan
  • Patent number: 5980938
    Abstract: The present invention provides methods of inhibiting PAI-1 using benzopyrans.
    Type: Grant
    Filed: June 25, 1997
    Date of Patent: November 9, 1999
    Assignee: Eli Lilly and Company
    Inventors: David Thompson Berg, George Joseph Cullinan, Brian William Grinnell, Mark Alan Richardson
  • Patent number: 5981570
    Abstract: The invention provides benzothiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, cardiovascular-related pathological conditions, including hyperlipidemia.
    Type: Grant
    Filed: September 22, 1997
    Date of Patent: November 9, 1999
    Assignee: Eli Lilly and Company
    Inventors: Henry Uhlman Bryant, George Joseph Cullinan, Jeffrey Alan Dodge
  • 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
  • Patent number: 5952350
    Abstract: The invention provides a compound of formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical compositions containing a compound of formula I, and methods of using a compound of formula I for inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia, and estrogen dependent cancer.
    Type: Grant
    Filed: October 23, 1997
    Date of Patent: September 14, 1999
    Assignee: Eli Lilly and Company
    Inventors: George Joseph Cullinan, Brian Stephen Muehl
  • Patent number: 5948795
    Abstract: Novel benzothiophenes, ##STR1## wherein R.sub.1, R.sub.2, and R.sub.3 are independently --OH, --OCO(C.sub.1 -C.sub.6 alkyl), --O(CO)O(C.sub.1 -C.sub.6 alkyl), --OCO--Ar, where Ar is phenyl or substituted phenyl, or --O(CO)O--phenyl; and R.sub.4 is N-pyrrolidinyl, N-piperidinyl, or N-hexamethyleneimino, and intermediates thereof, and the uses and formulations thereof, are provided by the present invention.
    Type: Grant
    Filed: June 25, 1997
    Date of Patent: September 7, 1999
    Assignee: Eli Lilly and Company
    Inventors: David Thompson Berg, George Joseph Cullinan, Brian William Grinnell, Mark Alan Richardson