Patents by Inventor Timothy A. Grese

Timothy A. Grese 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).

  • Publication number: 20080090860
    Abstract: The present invention is directed to compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof: The invention is also directed to pharmaceutical compositions, methods of use and methods of making compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof.
    Type: Application
    Filed: August 23, 2007
    Publication date: April 17, 2008
    Inventors: Kevin Gardinier, Douglas Gernert, Timothy Grese, David Neel, Christopher Mapes, Pierre-Yves Michellys, Marcus Boehm
  • Patent number: 7348359
    Abstract: The present invention is directed to compounds represented by Structural Formula (I) and pharmaceutically acceptable salts, solvates and hydrates thereof: (I). The invention is also directed to pharmaceutical compositions, methods of use and methods of making compounds represented by Structural Formula (I) and pharmaceutically acceptable salts, solvates and hydrates thereof.
    Type: Grant
    Filed: March 14, 2002
    Date of Patent: March 25, 2008
    Assignees: Eli Lilly and Company, Ligand Pharmaceuticals
    Inventors: Kevin M. Gardinier, Douglas L. Gernert, Timothy A. Grese, David A. Neel, Christopher M. Mapes, Pierre-Yves Michellys, Marcus F. Boehm
  • Publication number: 20060235222
    Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrier, diluent, or excipient, and methods for treating physiological disorders, particularly congestive heart disease, comprising administering to a patient in thereof an effective amount of a compound of Formula I.
    Type: Application
    Filed: January 20, 2004
    Publication date: October 19, 2006
    Applicant: ELI LILLY AND COMPANY
    Inventors: Michael Bell, Konstantinos Gavardinas, Douglas Gernert, Timothy Grese, Prabhakar Jadhav, Peter Lander, Mitchell Steinberg
  • Publication number: 20060063759
    Abstract: The present invention relates to methods of treating pathological disorders susceptible to steroid hormone nuclear receptor modulation comprising administering to a patient in need thereof an effective amount of a compound of the formula (I): or a pharmaceutically acceptable salt thereof. In addition, the present invention provides novel pharmaceutical compounds of Formula (I), including the pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions which comprise as an active ingredient a compound of Formula (I).
    Type: Application
    Filed: June 13, 2003
    Publication date: March 23, 2006
    Inventors: Michael Coghlan, Jonathan Green, Timothy Grese, Prabhakar Kondaji, Doanald Matthews, Mitchell Steinberg, Kevin Fales, Michael Bell
  • Publication number: 20050054712
    Abstract: he present invention relates to methods of treating pathological disorders susceptible to steroid hormone nuclear receptor modulation, particularly congestive heart failure, comprising administering to a patient in need thereof an effective amount of a compound of the formula: I or a pharmaceutically acceptable salt thereof. In addition, the present invention provides novel pharmaceutical compounds of Formula I, including the pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions which comprise as an active ingredient a compound of Formula I.
    Type: Application
    Filed: March 11, 2003
    Publication date: March 10, 2005
    Inventors: Timothy Grese, Prabhakar Jadhav, David Neel, Mitchell Steinberg, Peter Lander
  • Patent number: 6861530
    Abstract: This invention relates to substituted piperidine derivatives having at least one six-membered ring substituent. The piperidine derivatives exhibit antitumor activity and are useful as pharmaceuticals such as an antitumor agent.
    Type: Grant
    Filed: July 6, 2001
    Date of Patent: March 1, 2005
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Shinji Nara, Rieko Nakatsu, Yutaka Kanda, Shiro Akinaga, Mitsunobu Hara, Jun Eishima, Timothy A. Grese, Douglas L. Gernert
  • Publication number: 20040167160
    Abstract: The present invention is directed to compounds represented by Structural Formula (I) and pharmaceutically acceptable salts, solvates and hydrates thereof: (I). The invention is also directed to pharmaceutical compositions, methods of use and methods of making compounds represented by Structural Formula (I) and pharmaceutically acceptable salts, solvates and hydrates thereof.
    Type: Application
    Filed: January 16, 2004
    Publication date: August 26, 2004
    Inventors: Kevin M. Gardinier, Douglas J. Gernert, Timothy A. Grese, David A. Neel, Christopher M. Mapes, Pierre-Yves Michellys, Marcus F. Boehm
  • Publication number: 20020137770
    Abstract: This invention relates to piperidine derivatives having antitumor activity and useful as pharmaceuticals such as an antitumor agent.
    Type: Application
    Filed: July 6, 2001
    Publication date: September 26, 2002
    Inventors: Shinji Nara, Rieko Nakatsu, Yutaka Kanda, Shiro Akinaga, Mitsunobu Hara, Jun Eishima, Timothy A. Grese, Douglas L. Gernert
  • Patent number: 6417198
    Abstract: A method of inhibiting one or more CNS disorders in a post-menopausal woman comprising administering to a female human in need of treatment an effective amount of a compound having the formula wherein R1 and R3 are independently hydrogen, wherein Ar is optionally substituted phenyl; R2 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: July 9, 2002
    Assignee: Eli Lilly and Company
    Inventors: Henry U. Bryant, Andrew L. Glasebrook, Timothy A. Grese, David L. Phillips
  • Patent number: 5663184
    Abstract: A method of inhibiting one or more CNS disorders in a post-menopausal woman 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, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: September 2, 1997
    Assignee: Eli Lilly and Company
    Inventors: Henry U. Bryant, Andrew L. Glasebrook, Timothy A. Grese, David L. Phillips
  • Patent number: 5637598
    Abstract: The instant invention provides methods for inhibiting bone loss comprising adminstering to a mammal in need of treatment a compound as provided in formula I.
    Type: Grant
    Filed: May 2, 1995
    Date of Patent: June 10, 1997
    Assignee: Eli Lilly and Company
    Inventor: Timothy A. Grese
  • Patent number: 5556876
    Abstract: A method of lowering serum cholesterol levels comprising administering to a human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R is hydrogen; hydroxy; C.sub.1 -C.sub.6 alkoxy; a group of the formula --O--C(O)--R.sup.a, wherein R.sup.a is hydrogen, C.sub.1 -C.sub.6 alkyl optionally substituted with amino, halo, carbonyl, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.1 -C.sub.7 alkanoyloxy, carbamoyl and/or aryl; or R.sup.a is C.sub.1 -C.sub.6 alkenyl optionally substituted with aryl; or R.sup.a is a C.sub.3 -C.sub.7 cycloalkyl; or R.sup.a is aryl optionally substituted with hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, and/or halo; or R.sup.a is --O-aryl;or R is a group of the formula --O--C(O)R.sup.c --O--(C.sub.1 -C.sub.6 alkyl) wherein R.sup.c is a bond or C.sub.1 -C.sub.6 alkanediyl;R.sup.1 is halo, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.7 alkyl substituted with C.sub.1 -C.sub.6 alkyl, substituted or unsubstituted C.sub.3 -C.sub.
    Type: Grant
    Filed: August 15, 1995
    Date of Patent: September 17, 1996
    Assignee: Eli Lilly and Company
    Inventors: Henry U. Bryant, Timothy A. Grese
  • Patent number: 5552433
    Abstract: A method of lowering serum cholesterol levels is disclosed comprising administering to a human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R is herein defined; R.sup.1 is halo, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.7 alkyl substituted with C.sub.1 -C.sub.6 alkyl, substituted or unsubstituted C.sub.3 -C.sub.7 cycloalkyl, or substituted or unsubstituted C.sub.3 -C.sub.7 cycloalkenyl;R.sup.2 is O or CH.sub.2 ;R.sup.3 is CH.sub.2 or (CH.sub.2).sub.2 ;R.sup.4 is ##STR2## CH.sub.2, or a bond; and R.sup.5 is amino, or a pharmaceutically acceptable salt or solvate thereof.
    Type: Grant
    Filed: August 15, 1995
    Date of Patent: September 3, 1996
    Assignee: Eli Lilly and Company
    Inventors: Henry U. Bryant, Timothy A. Grese
  • Patent number: 5521172
    Abstract: A method of lowering serum cholesterol levels comprising administering to a human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R is as herein defined;R.sup.1 is halo, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.7 alkyl substituted with C.sub.1 -C.sub.6 alkyl, substituted or unsubstituted C.sub.3 -C.sub.7 cycloalkyl, or substituted or unsubstituted C.sub.3 -C.sub.7 cycloalkenyl;R.sup.2 is O or CH.sub.2 ;R.sup.3 is CH.sub.2 or (CH.sub.2).sub.2 ;R.sup.4 is ##STR2## CH.sub.2, or a bond; and R.sup.5 is an N-heterocyclic ring, other than pyrrolidin or piperidino, which optionally has another hetero atom selected from N, O, or S in said ring; or a pharmaceutically acceptable salt or solvate thereof.
    Type: Grant
    Filed: August 15, 1995
    Date of Patent: May 28, 1996
    Assignee: Eli Lilly and Company
    Inventors: Henry U. Bryant, Timothy A. Grese
  • Patent number: 5494929
    Abstract: A method of inhibiting effects of growth hormone 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 accepatable salt of solvate thereof.
    Type: Grant
    Filed: January 12, 1995
    Date of Patent: February 27, 1996
    Assignee: Eli Lilly and Company
    Inventor: Timothy A. Grese
  • Patent number: 5482950
    Abstract: A method of lowering serum cholesterol levels comprising administering to a human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R is hydrogen; hydroxy; C.sub.1 -C.sub.6 alkoxy; a group of the formula --O--C(O)--R.sup.a, wherein R.sup.a is hydrogen, optionally substituted C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkenyl optionally substituted with aryl, C.sub.3 -C.sub.7 cycloalkyl, optionally substituted aryl or R.sup.a is optionally substituted --O--aryl,or R is a group of the formula --O--SO.sub.2 --R.sup.b wherein R.sup.b may be C.sub.1 -C.sub.6 alkyl or optionally substituted aryl;or R is carbamoyloxy wherein the nitrogen may be substituted once or twice with C.sub.1 -C.sub.6 alkyl;or R is a group of the formula --O--C(O)R.sup.c --O--(C.sub.1 -C.sub.6 alkyl) wherein R.sup.c is a bond or C.sub.1 -C.sub.6 alkanediyl;R.sup.1 is halo, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.7 alkyl substituted with C.sub.1 -C.sub.6 alkyl, substituted or unsubstituted C.sub.3 -C.sub.
    Type: Grant
    Filed: October 15, 1993
    Date of Patent: January 9, 1996
    Assignee: Eli Lilly and Company
    Inventors: Henry U. Bryant, Timothy A. Grese
  • Patent number: 5480904
    Abstract: A method of inhibiting uterine fibrosis comprising administering to a human in need of treatment an effective amount of a benzothiophene compound.
    Type: Grant
    Filed: October 28, 1993
    Date of Patent: January 2, 1996
    Assignee: Eli Lilly and Company
    Inventors: Henry U. Bryant, Timothy A. Grese
  • 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: 5446071
    Abstract: The present invention provides methods for lowering serum cholesterol comprising administering to a mammal in need of treatment a serum cholesterol lowering amount of a compound of formula I or formula II ##STR1## wherein L is --CON< or --N<; andthe dotted line in the B-ring is an optional bond; or a pharmaceutically acceptable salt thereof; and ##STR2## wherein Q is a moiety having the formula ##STR3## L is --CON< or --N<; B is --O--, --S--, --CH.sub.2 -phenyl-O--, -phenyl-O--, or -benzyl-O--;G is a moiety which together with L forms a substituted or unsubstituted heterocyclic ring having at least one nitrogen atom or is selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower alkynyl, (C.sub.3 -C.sub.7)cycloalkyl, halo(lower)alkyl, cyano(lower)alkyl, carboxy(lower)alkyl, (lower)alkoxycarbonyl(lower)alkyl, (C.sub.6 -C.sub.10)aryl, (C.sub.7 -C.sub.11)aryl akyl, di(lower)alkylamino(lower)alkyl, and fluoro-substituted analogs of the foregoing;Z is --O--, --S--, --CH.sub.
    Type: Grant
    Filed: November 18, 1994
    Date of Patent: August 29, 1995
    Assignee: Eli Lilly and Company
    Inventor: 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