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).
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Publication number: 20080090860Abstract: 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: ApplicationFiled: August 23, 2007Publication date: April 17, 2008Inventors: Kevin Gardinier, Douglas Gernert, Timothy Grese, David Neel, Christopher Mapes, Pierre-Yves Michellys, Marcus Boehm
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Patent number: 7348359Abstract: 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: GrantFiled: March 14, 2002Date of Patent: March 25, 2008Assignees: Eli Lilly and Company, Ligand PharmaceuticalsInventors: Kevin M. Gardinier, Douglas L. Gernert, Timothy A. Grese, David A. Neel, Christopher M. Mapes, Pierre-Yves Michellys, Marcus F. Boehm
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Publication number: 20060235222Abstract: 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: ApplicationFiled: January 20, 2004Publication date: October 19, 2006Applicant: ELI LILLY AND COMPANYInventors: Michael Bell, Konstantinos Gavardinas, Douglas Gernert, Timothy Grese, Prabhakar Jadhav, Peter Lander, Mitchell Steinberg
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Publication number: 20060063759Abstract: 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: ApplicationFiled: June 13, 2003Publication date: March 23, 2006Inventors: Michael Coghlan, Jonathan Green, Timothy Grese, Prabhakar Kondaji, Doanald Matthews, Mitchell Steinberg, Kevin Fales, Michael Bell
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Publication number: 20050054712Abstract: 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: ApplicationFiled: March 11, 2003Publication date: March 10, 2005Inventors: Timothy Grese, Prabhakar Jadhav, David Neel, Mitchell Steinberg, Peter Lander
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Patent number: 6861530Abstract: 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: GrantFiled: July 6, 2001Date of Patent: March 1, 2005Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Shinji Nara, Rieko Nakatsu, Yutaka Kanda, Shiro Akinaga, Mitsunobu Hara, Jun Eishima, Timothy A. Grese, Douglas L. Gernert
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Publication number: 20040167160Abstract: 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: ApplicationFiled: January 16, 2004Publication date: August 26, 2004Inventors: Kevin M. Gardinier, Douglas J. Gernert, Timothy A. Grese, David A. Neel, Christopher M. Mapes, Pierre-Yves Michellys, Marcus F. Boehm
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Publication number: 20020137770Abstract: This invention relates to piperidine derivatives having antitumor activity and useful as pharmaceuticals such as an antitumor agent.Type: ApplicationFiled: July 6, 2001Publication date: September 26, 2002Inventors: Shinji Nara, Rieko Nakatsu, Yutaka Kanda, Shiro Akinaga, Mitsunobu Hara, Jun Eishima, Timothy A. Grese, Douglas L. Gernert
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Patent number: 6417198Abstract: 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: GrantFiled: December 21, 1993Date of Patent: July 9, 2002Assignee: Eli Lilly and CompanyInventors: Henry U. Bryant, Andrew L. Glasebrook, Timothy A. Grese, David L. Phillips
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Patent number: 5663184Abstract: 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: GrantFiled: April 28, 1995Date of Patent: September 2, 1997Assignee: Eli Lilly and CompanyInventors: Henry U. Bryant, Andrew L. Glasebrook, Timothy A. Grese, David L. Phillips
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Patent number: 5637598Abstract: 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: GrantFiled: May 2, 1995Date of Patent: June 10, 1997Assignee: Eli Lilly and CompanyInventor: Timothy A. Grese
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Patent number: 5556876Abstract: 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: GrantFiled: August 15, 1995Date of Patent: September 17, 1996Assignee: Eli Lilly and CompanyInventors: Henry U. Bryant, Timothy A. Grese
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Patent number: 5552433Abstract: 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: GrantFiled: August 15, 1995Date of Patent: September 3, 1996Assignee: Eli Lilly and CompanyInventors: Henry U. Bryant, Timothy A. Grese
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Patent number: 5521172Abstract: 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: GrantFiled: August 15, 1995Date of Patent: May 28, 1996Assignee: Eli Lilly and CompanyInventors: Henry U. Bryant, Timothy A. Grese
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Patent number: 5494929Abstract: 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: GrantFiled: January 12, 1995Date of Patent: February 27, 1996Assignee: Eli Lilly and CompanyInventor: Timothy A. Grese
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Patent number: 5482950Abstract: 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: GrantFiled: October 15, 1993Date of Patent: January 9, 1996Assignee: Eli Lilly and CompanyInventors: Henry U. Bryant, Timothy A. Grese
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Patent number: 5480904Abstract: A method of inhibiting uterine fibrosis comprising administering to a human in need of treatment an effective amount of a benzothiophene compound.Type: GrantFiled: October 28, 1993Date of Patent: January 2, 1996Assignee: Eli Lilly and CompanyInventors: Henry U. Bryant, Timothy A. Grese
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Patent number: 5446071Abstract: 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: GrantFiled: November 18, 1994Date of Patent: August 29, 1995Assignee: Eli Lilly and CompanyInventor: Timothy A. Grese
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Patent number: 5446061Abstract: 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: GrantFiled: November 5, 1993Date of Patent: August 29, 1995Assignee: Eli Lilly and CompanyInventors: Henry U. Bryant, Timothy A. Grese
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Patent number: 5441964Abstract: A method of inhibiting bone loss comprising administering to a human in need of treatment an effective amount of a substituted benzothiophene.Type: GrantFiled: October 15, 1993Date of Patent: August 15, 1995Assignee: Eli Lilly and CompanyInventors: Henry U. Bryant, Timothy A. Grese