Abstract: A process for resolving amino protected racemic 3-amino-2-methylpropionic acid which comprises the steps of: (1) reacting said amino protected acid with a protected amino group with an enantiomer of a chiral amine to form diastereomeric salts; (2) recrystallizing the diastereomeric salts from ethyl acetate to separate the diastereomeric salts into crystal fractions; and (3) releasing the resolved acid from the diastereomeric salt by treating the diastereomeric salt with a basic solution is disclosed. A process for the preparation of the cryptophycin molecules is also disclosed.
Type:
Grant
Filed:
May 8, 2000
Date of Patent:
April 16, 2002
Assignee:
Eli Lilly and Company
Inventors:
James Abraham Aikins, Tony Yantao Zhang
Abstract: The present invention relates to a compound of formula (I): or a pharmaceutical acid addition salt thereof; which is useful for activating 5-HT1f receptors and inhibiting protein extravasation in a mammal.
Type:
Grant
Filed:
December 5, 2000
Date of Patent:
March 19, 2002
Assignee:
Eli Lilly and Company
Inventors:
Sandra Ann Filla, Daniel James Koch, Brian Michael Mathes, Vincent Patrick Rocco
Abstract: A packaging system for storing and dispensing individual doses of medication on prescribed days, the packaging system comprising a series of sheets adapted to fold over each other with doses of medication removably held thereon. A plurality of labels are held on at least one of the sheets, each label corresponding to one dose of medication, each of the labels being adapted to be removed from one of the sheets and applied to a calendar to thereby serve as a reminder of the day on which the corresponding individual dose of medication is to be taken. The packaging system may further comprise a sleeve with one open end, the open end and the sleeve engaging the sheets when in a folded state.
Abstract: The present invention provides novel 2-amino-1,2,3,4-tetrahydro-9H-carbazole-6-carboxamides and 3-amino-10H-cyclohepta[7,6-b]indole-7-carboxamides of Formula I:
where R1, R2, R3 and n are as described in the specification.
Abstract: This invention provides methods and 2-(azetidin-2-on-1-yl)acetic acid derivatives for the antagonism of the vasopressin V1a receptor.
Type:
Grant
Filed:
August 19, 1999
Date of Patent:
March 20, 2001
Assignee:
Eli Lilly and Company
Inventors:
Robert F Bruns, Jr., Robin DG Cooper, Bruce A Dressman, David C Hunden, Stephen W Kaldor, Gary A Koppel, John R Rizzo, Jeffrey J Skelton, Mitchell I Steinberg
Abstract: The power of citalopram, fluvoxamine and paroxetine to increase the availability of sarotonin, norepinephrine and dopamine, particularly serotonin, is augmented by administration in combination with a drug which is a serotonin 1A receptor antagonist.
Abstract: The present invention provides processes and intermediates of Formula I: ##STR1## where X and R are defined in the specification, for the preparation of 5-amino-3-(1-methylpiperidin-4-yl)pyrrolo-[3,2-b]pyridine.
Type:
Grant
Filed:
November 6, 1998
Date of Patent:
November 21, 2000
Assignee:
Eli Lilly and Company
Inventors:
Vincent Mancuso, Freddy Andre Napora, Uko Effiong Udodong, Daniel Edward Verral, II
Abstract: The invention relates to a method of treating psychosis, acute mania, mild anxiety states or depression in combination with psychotic episodes by administering to a patient a combination of an atypical antipsychotic and a serotonin reuptake inhibitor.
Type:
Grant
Filed:
September 23, 1997
Date of Patent:
November 14, 2000
Assignee:
Eli Lilly and Company
Inventors:
Franklin P. Bymaster, Kenneth W. Perry, Gary D. Tollefson
Abstract: This invention provides certain sulfonamide compounds, formulations, and a method for treating susceptible neoplasms in mammals using certain sulfonamide compounds.
Type:
Grant
Filed:
March 24, 1993
Date of Patent:
November 14, 2000
Assignee:
Eli Lilly and Company
Inventors:
Thomas A. Crowell, J. Jeffry Howbert, John S. Ward
Abstract: The present invention relates to a compound of formula I: ##STR1## or a pharmaceutical acid addition salt thereof; which are useful for activating 5-HT.sub.1F receptors and inhibiting neuronal protein extravasation in a mammal.
Type:
Grant
Filed:
June 16, 1999
Date of Patent:
October 17, 2000
Assignee:
Eli Lilly and Company
Inventors:
Joseph Herman Krushinski, Jr., John Mehnert Schaus
Abstract: This invention provides novel 5-HT.sub.1F agonists of Formula ##STR1## where X, R.sup.1, R.sup.2, and R.sup.3 are defined in the specification, which are useful for the treatment of migraine and associated disorders.
Type:
Grant
Filed:
October 12, 1999
Date of Patent:
October 3, 2000
Assignee:
Eli Lilly and Company
Inventors:
James E Fritz, Patric J Hahn, Stephen W Kaldor, Miles G Siegel, Yao-Chang Xu
Abstract: This invention provides 3-(bicyclic heteroaryl)-8-azabicyclo[3.2.1]oct-2-enes and 3-(bicyclic heteroaryl)-8-azabicyclo[3.2.1]octanes which are useful for the inhibition of serotonin reuptake in mammals.
Type:
Grant
Filed:
June 7, 1999
Date of Patent:
August 22, 2000
Assignee:
Eli Lilly and Company
Inventors:
James Edmund Audia, Stacey Leigh McDaniel, Jeffrey Scott Nissen