Abstract: A method of introducing a second stereogenic center into a tetrahydro-?-carboline have two stereogenic centers using a modified Pictet-Spengler reaction is disclosed. The method provides a desired cis- or trans-isomer in high yield and purity, and in short processes times.
Type:
Grant
Filed:
July 14, 2003
Date of Patent:
June 23, 2009
Assignee:
Lilly ICOS LLC
Inventors:
Mark W. Orme, Michael J. Martinelli, Christopher W. Doecke, Joseph M. Pawlak, Erik C. Chelius
Abstract: Compounds of formula (I) in which R1=C1-6 alkyl, optionally halosubstituted; R2=H, C1-4 alkyl, optionally halosubstituted or replaced by halogen; R3=C2-4 alkyl, optionally halosubstituted; R4=SO2NR5R&, CO2R7 or halogen, C2-4 alkenyl; optionally substituted with NR5R6, SONR5R6, CONR5R6, CO2R7 or halogen, C2-4 alkanoyl, optionally substituted with NR5R6, SONR5R6, CONR5R6, CO2R7 or halogen; R5 and R6=independently H or C1-4 alkyl, or, together with the N atom to which they are attached, a pyrrolidino, piperidino, morpholino, 4-(NR8)-1-piperazinyl or 1-imidazolyl ring optionally substituted with one or two C1-4 alkyl groups; R7=H, C1-4 alkyl, optionally fluorosubstituted, and R8=H,C1-3 alkyl or hydroxyalkyl with 1-4 C atoms, or the pharmaceutically acceptable salts thereof are useful for the chemotherapeutic treatment of neuropathies.
Abstract: A method of treating symptoms of benign prostatic hypertrophy and a method of treating lower urinary tract symptoms, are disclosed. The method includes administering to a mammal about 1 to about 20 milligrams of an agent that inhibits cyclic guanosine 3,5-monophosphate specific phosphodiesterase type 5.
Type:
Application
Filed:
October 10, 2006
Publication date:
April 26, 2007
Applicant:
LILLY ICOS LLC
Inventors:
Bela Denes, Kenneth Ferguson, John Whitaker
Abstract: Formulations containing a PDE5 inhibitor, a water-soluble diluent, a lubricant, a hydrophilic binder, a disintegrant, and optional microcrystalline cellulose and/or a wetting agent, and their use in treating sexual dysfunction, are disclosed.
Type:
Grant
Filed:
April 26, 2000
Date of Patent:
February 27, 2007
Assignee:
Lilly Icos LLC.
Inventors:
Peter L. Oren, Neil R. Anderson, Martha A. Kral
Abstract: Compounds of general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents as inhibitors of phosphodiesterase 5 cardiovascular disorders
Type:
Grant
Filed:
April 2, 2002
Date of Patent:
October 3, 2006
Assignee:
Lilly Icos LLC
Inventors:
Jason S. Sawyer, Mark W. Orme, James D. Copp
Abstract: The present invention relates to highly selective phosphodieterase (PDE) enzyme inhibitors and to their use in pharmaceutical articles of manufacture. In particular, the present invention relates to potent inhibitors of cyclic guanosine 3?,5?-monophosphate specific phosphodiesterase type 5 (PDE5) that when incorporated into a pharmaceutical product at about 1 to about 20 mg unit dosage are useful for the treatment of sexual dysfunction.
Type:
Grant
Filed:
April 26, 2000
Date of Patent:
September 13, 2005
Assignee:
Lilly ICOS LLC.
Inventors:
William Ernest Pullman, John Steven Whitaker