Abstract: An ORL-1 receptor antagonist of the formula: its uses, and methods for its preparation are described.
Type:
Grant
Filed:
November 10, 2010
Date of Patent:
July 31, 2012
Assignee:
Eli Lilly and Company
Inventors:
Ana Belen Benito Collado, Nuria Diaz Buezo, Alma Maria Jimenez-Aguado, Celia Lafuente Blanco, Maria Angeles Martinez-Grau, Concepcion Pedregal-Tercero, Miguel Angel Toledo Escribano
Abstract: The present invention provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof. Also, the present invention provides a pharmaceutical composition comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof with a pharmaceutically acceptable diluent or carrier. The present invention further provides methods for treating abdominal aortic aneurysm, plaque instability, atherosclerosis, or autoimmune disorders such as rheumatoid arthritis, psoriasis, and lupus comprising administering a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable diluent or carrier.
Type:
Grant
Filed:
October 14, 2011
Date of Patent:
July 24, 2012
Assignee:
Eli Lilly and Company
Inventors:
Gary G. Deng, Konstantinos Gavardinas, Prabhakar Kondaji Jadhav, Euibong Jemes Kim, Matthew Allen Schiffler
Abstract: The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine, persistent pain, and anxiety: where A and B are each independently —C(H)? or —N?, provided that at least one of A and B is —N?, n is 1-3, m is 0-3, and R1-4 are as defined herein.
Type:
Grant
Filed:
May 7, 2008
Date of Patent:
June 19, 2012
Assignee:
Eli Lilly and Company
Inventors:
Valentina O. Badescu, Anne Marie Camp, Barry Peter Clark, Michael Philip Cohen, Sandra Ann Filla, Peter Thaddeus Gallagher, Sarah Lynne Hellman, Michael Philip Mazanetz, Marta Maria Pineiro-Nunez, John Mehnert Schaus, Patrick Gianpietro Spinazze, Maria Ann Whatton
Abstract: A serotonin and norepinephrine reuptake inhibitor of the formula: its uses, and methods for its preparation are described.
Type:
Grant
Filed:
April 6, 2010
Date of Patent:
May 8, 2012
Assignee:
Eli Lilly and Company
Inventors:
Nicolas Jacques Francois Dreyfus, Sandra Ann Filla, Anette Margareta Johansson, Thierry J. Masquelin, Jikesh Arvind Shah, Eric George Tromiczak, Magnus Wilhelm Walter
Abstract: Compounds and pharmaceutical compositions comprising compounds of the Formula as CB1 receptor inverse agonists useful for reducing body weight in mammals, treating cognitive impairment associated with schizophrenia, and mitigating treatment emergent weight gain observed during treatment with antipsychotics.
Type:
Grant
Filed:
October 22, 2007
Date of Patent:
May 1, 2012
Assignee:
Eli Lilly and Company
Inventors:
David Scott Coffey, Jingdan Hu, Stacy Jo Keding, Joseph Herman Krushinski, Jr., John Mehnert Schaus, David Edward Tupper
Abstract: The present invention relates to compounds of Formula (I), pharmaceutical compositions thereof, and the use of such compounds as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric and neuroendocrine disorders, neurological diseases, and metabolic syndrome.
Type:
Grant
Filed:
September 13, 2007
Date of Patent:
February 7, 2012
Assignee:
Eli Lilly and Company
Inventors:
Zhaogen Chen, Shaojuan Jia, James Lee Toth
Abstract: Methods for using TRL V6 as a biomarker for the modulation of triglyceride and/or lipoprotein metabolism in a mammal induced by a weight loss pharmaceutical agent. The biomarker may be used for determining if an individual patient will likely respond favorably to a given weight loss pharmaceutical agent.
Abstract: The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine: where A is —C(H)? or —N?; m is 0, 1 or 2; R1 is optionally substituted phenyl, optionally substituted pyrazol-4-yl; optionally substituted imidazolyl, optionally substituted pyridyl, or thienyl; R2 is hydrogen or methyl; and R3 and R4 are as defined herein.
Type:
Grant
Filed:
August 19, 2008
Date of Patent:
November 1, 2011
Assignee:
Eli Lilly and Company
Inventors:
Michael Philip Cohen, Sarah Lynne Hellman, Sean Patrick Hollinshead, Sandra Ann Filla, Michael Wade Tidwell
Abstract: The present invention relates to compounds of Formula (I), pharmaceutical compositions thereof, and use thereof as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric and neuroendocrine disorders, neurological diseases, and metabolic syndrome.
Type:
Grant
Filed:
September 17, 2007
Date of Patent:
October 4, 2011
Assignee:
Eli Lilly and Company
Inventors:
Zhaogen Chen, Chafiq Hamdouchi Hamdouchi, Erik James Hembre, Philip Arthur Hipskind, Jason Kenneth Myers, Takako Takakuwa, James Lee Toth
Abstract: The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT2C receptor agonists for the treatment of 5-HT2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: where: R6 is —C?C—R10, —O—R12, —S—R14, or —NR24R25; and other substituents are as defined in the specification.
Type:
Grant
Filed:
February 18, 2005
Date of Patent:
September 20, 2011
Assignee:
Eli Lilly and Company
Inventors:
John Gordon Allen, Karin Briner, Michael Philip Cohen, Christopher Stanley Galka, Sarah Lynne Hellman, Maria Angeles Martinez-Grau, Matthew Robert Reinhard, Michael John Rodriguez, Roger Ryan Rothhaar, Michael Wade Tidwell, Frantz Victor, Andrew Caerwyn Williams, Deyi Zhang, Michael Philip Mazanetz
Abstract: Compound and pharmaceutical compositions comprising the compounds of the Formula or a pharmaceutically acceptable salt thereof, as a CB1 receptor inverse agonist, useful for reducing body weight in mammals, treating cognitive impairment associated with schizophrenia, and mitigating treatment emergent weight gain observed during treatment with antipsychotics.
Abstract: The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula (I) as selective 5-HT2C receptor agonists for the treatment of 5-HT2c associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: R6 D R?N—R?R* where R6 is —(CrC3)alkyl-S—(C0-C3)alkyl-R10, —(C1-C3)alkyl-NR11R12, —(CrC3)alkyl-O—R13. and other substituents are as defined in the specification.
Type:
Grant
Filed:
September 1, 2006
Date of Patent:
August 9, 2011
Assignee:
Eli Lilly and Company
Inventors:
John Gordon Allen, Karin Briner, Christopher Stanley Galka, Richard Charles Hoying, Maria Angeles Martinez-Grau, Julie Miyashiro, Natalia Pokrovskaia, Matthew Robert Reinhard
Abstract: The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT2C receptor agonists for the treatment of 5-HT2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: Formula (I) where: R6 is selected from the group consisting of (a, b, c, d, e) and other substituents are as defined in the specification.
Type:
Grant
Filed:
September 1, 2006
Date of Patent:
July 19, 2011
Assignee:
Eli Lilly and Company
Inventors:
Karin Briner, Anne Marie Camp, Alan Cornell, Michael Philip Mazanetz, Roger Ryan Rothhaar, Frantz Victor, Andrew Caerwyn Williams, Deyi Zhang
Abstract: The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine: where A is —C(H)? or —N? and R1-7 are as defined herein.
Type:
Grant
Filed:
September 30, 2008
Date of Patent:
March 22, 2011
Assignee:
Eli Lilly and Company
Inventors:
Valentina O Badescu, Sandra Ann Filla, Peter Thaddeus Gallagher, Maria Ann Whatton
Abstract: This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor. An example of a compound of formula (I) is (a).
Type:
Grant
Filed:
November 10, 2005
Date of Patent:
April 20, 2010
Assignee:
Eli Lilly and Company
Inventors:
Ankush Baburao Argade, Theodore Goodson, Jr., David Kent Herron, Sajan Joseph, Salvatore Donato Lepore, Angela Lynn Marquart, John Joseph Masters, David Mendel, Leander Merritt, Andrew Michael Ratz, Gerald Floyd Smith, Anne Louise Tebbe, Michael Robert Wiley, Ying Kwong Yee