Abstract: The present invention provides an imidazo[4,5-c]quinolin-2-one compound, or a pharmaceutically acceptable salt thereof, that inhibits both PI3K and mTOR and, therefore, is useful in the treatment of cancer.
Type:
Application
Filed:
January 11, 2012
Publication date:
July 19, 2012
Applicant:
ELI LILLY AND COMPANY
Inventors:
David Anthony Barda, Mary Margaret Mader
Abstract: Disclosed is a method of preparing a GLP-1 compound that is soluble in aqueous solution at pH 7.4 from a GLP-1 compound that is substantially insoluble in aqueous solution at pH 7.4. The insoluble GLP-1 compound is dissolved in aqueous base or in aqueous acid to form a GLP-1 solution. The GLP-1 solution is then neutralized to a pH at which substantially no amino acid racemization of the GLP-1 compounds occurs, after which the soluble GLP-1 compound is isolated from the neutralized solution.
Type:
Grant
Filed:
September 1, 2009
Date of Patent:
July 17, 2012
Assignee:
Eli Lilly and Company
Inventors:
Walter Francis Prouty, Jr., Joseph Vincent Rinella, Jr.
Abstract: The present invention provides formulation parameters and manufacturing conditions for stable pharmaceutical compositions comprising N-{4-(2,2-dimethyl-propionyl)-(5R)-5-[(2-ethylamino-ethanesulfonylamino)-methyl]-5-phenyl-4,5-dihydro-[1,3,4]thiadiazol-2-yl}-2,2-dimethyl-propionamide that minimize undesirable chiral conversion to the less active S enantiomeric form.
Type:
Grant
Filed:
July 7, 2008
Date of Patent:
July 17, 2012
Assignees:
Eli Lilly and Company, Kyowa Hakko Kirin Co., Ltd.
Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.
Type:
Grant
Filed:
June 23, 2011
Date of Patent:
July 10, 2012
Assignee:
Eli Lilly and Company
Inventors:
Robert Dean Dally, Jeffrey Alan Dodge, Scott Alan Frank, Ronald Jay Hinklin, Timothy Alan Shepherd, Owen Brendan Wallace
Abstract: A medication and needle module (20) for an injection device. The module (20) includes a housing (22) including a first portion (39) and a second portion (38) detachably connected together, the second housing portion having a periphery complementarily shaped with a cavity (154) in the injection device (150) to be loadable therein, a primary container (120) within the first housing portion and including a medication filled reservoir (124), a secondary container (70) within the second housing portion and including a medication tillable reservoir, a needle cassette (60) rotatably mounted within the second housing portion and including a plurality of delivery needles (64), and a transfer needle assembly (100) within the housing. The detachability of the second housing portion from the first housing portion permits the second housing portion with the secondary container and the needle cassette to be loaded as a unit independently of the first housing portion into the injection device cavity for use.
Type:
Grant
Filed:
May 9, 2007
Date of Patent:
July 10, 2012
Assignee:
Eli Lilly and Company
Inventors:
Andrew Christopher Burroughs, Rodney Hal Monson, Volker Roos
Abstract: Provided are monoclonal antibodies, antigen-binding fragments thereof, and combinations of the foregoing, that bind to, and inhibit the activity of, c-Met, and that are effective in treating cancers and other diseases, disorders, or conditions where pathogenesis is mediated by c-Met.
Type:
Grant
Filed:
November 18, 2009
Date of Patent:
July 10, 2012
Assignee:
Eli Lilly and Company
Inventors:
Julian Davies, Ling Liu, Jirong Lu, Peter Edward Vaillancourt, Mark Andrew Wortinger, Wei Zeng
Abstract: This invention relates to synthetic excitatory amino acid prodrugs and processes for their preparation. The invention further relates to methods of using, and pharmaceutical compositions comprising, the compounds for the treatment of neurological disorders and psychiatric disorders.
Type:
Application
Filed:
March 13, 2012
Publication date:
July 5, 2012
Applicant:
ELI LILLY AND COMPANY
Inventors:
Eric David Moher, James Allen Monn, Concepcion Pedregal-Tercero, Jaime Gonzalo Blanco-Urgoiti, Ivan Collado Cano
Abstract: The present invention provides compounds of the formula below or pharmaceutical salts thereof, wherein R1, R2 and R3 are as described herein; methods of treating osteoarthritis using the compounds; and a process for preparing the compounds.
Type:
Application
Filed:
December 16, 2011
Publication date:
June 21, 2012
Applicant:
ELI LILLY AND COMPANY
Inventors:
Steven Lee Kuklish, Matthew Allen Schiffler, Jeremy Schulenburg York
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: The present invention provides AKT inhibitors of the formula: Formula I The present invention also provides pharmaceutical compositions comprising compounds of Formula I, uses of compounds of Formula I and method of using compounds of Formula I.
Type:
Application
Filed:
October 20, 2010
Publication date:
June 14, 2012
Applicant:
ELI LILLY AND COMPANY
Inventors:
Douglas Wade Beight, Timothy Paul Burkholder, Joshua Ryan Clayton, MariJean Eggen, Kenneth James Henry, JR., Deidre Michelle Johns, Saravanan Parthasarathy, Huaxing Pei, Mark Edward Rempala, Jason Scott Sawyer
Abstract: A cartridge with injection needles for an injection device. The cartridge includes a plurality of injection needle assemblies, each including a hub, mounted to be shiftable in cavities of a needle assembly support. A hub ledge having a drive member engageable push surface projects within a gap between a first hub portion and a second hub portion. Driving engagement of the push surface by an injection device drive member shifts the needle assembly from a retracted position to an injection position, during which shifting the second hub portion moves relative to the first hub portion. A pull surface on the second hub portion is engagable with the drive member for lifting the needle assembly from the injection position.
Abstract: The present invention relates to the compound of the formula: to pharmaceutical compositions comprising the compound of Formula (I); and to methods for treating or preventing hypogonadism, osteoporosis, osteopenia, sarcopenia, cachexia, muscle atrophy, sexual dysfunction or erectile dysfunction, comprising administering to a patient in need thereof an effective amount of the compound of Formula (I).
Abstract: Provided are monoclonal antibodies and antigen-binding fragments thereof that bind to, and inhibit the activity of human FPN1, and which are effective in maintaining or increasing the transport of iron out of mammalian cells and/or maintaining or increasing the level of serum iron, reticulocyte count, red blood cell count, hemoglobin, and/or hematocrit in a subject in vivo.
Type:
Grant
Filed:
December 1, 2009
Date of Patent:
May 22, 2012
Assignee:
Eli Lilly and Company
Inventors:
Donmienne Doen Mun Leung, Peng Luan, Joseph Vincent Manetta, Ying Tang, Derrick Ryan Witcher
Abstract: The invention provides GLP-1 compounds coupled to two polyethylene glycol molecule or derivative thereof, resulting in a biologically active peptide with an extended half-life and a slower clearance when compared to that of unPEGylated peptide. These PEGylated GLP-1 compounds and compositions are useful in treating conditions or disorders benefited by lowering blood glucose, decreasing food intake, decreasing gastric or intestinal emptying, increasing beta (?) cell population, or decreasing gastric or intestinal motility.
Type:
Grant
Filed:
May 11, 2006
Date of Patent:
May 22, 2012
Assignee:
Eli Lilly and Company
Inventors:
Wolfgang Glaesner, John Philip Mayer, Rohn Lee Millican, Jr., Andrew Mark Vick, Lianshan Zhang
Abstract: The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have histamine—H3 receptor antagonist or inverse agonist activity, as well as methods and intermediates for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.
Type:
Grant
Filed:
March 28, 2006
Date of Patent:
May 15, 2012
Assignee:
Eli Lilly and Company
Inventors:
Philip Arthur Hipskind, Takako Takakuwa, Cynthia Darshini Jesudason, Robert Alan Gadski, William Joseph Hornback, Richard Todd Pickard, Lisa Selsam Beavers
Abstract: Human monoclonal antibodies that specifically bind to TNFSF13b polypeptides are disclosed. These antibodies have high affinity for hTNFSF13b (e.g., KD=10?8 M or less), a slow off rate for TNFSF13b dissociation (e.g., Koff=10?3 sec?1 or less) and neutralize TNFSF13b activity in vitro and in vivo. The antibodies of the invention are useful in one embodiment for inhibiting TNFSF13b activity in a human subject suffering from a disorder in which hTNFSF13b activity is detrimental. Nucleic acids encoding the antibodies of the present invention, as well as, vectors and host cells for expressing them are also encompassed by the invention.