Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein, R1 is hydrogen, alkyl of 1–6 carbon atoms, benzyl, alkylcarbonyl of 2–7 carbon atoms, or benzoyl; X is R2 is hydrogen, alkyl of 1–6 carbon atoms, benzyl, alkylcarbonyl of 2–7 carbon atoms, or benzoyl; R3 is hydrogen, alkyl of 1–6 carbon atoms, hydroxy, or alkoxy of 1–6 carbon atoms; a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable salt of a sulfate ester of the hydroxyl group at the 3- or 17-position when R1 or R2 is hydrogen, or a glucuronide of the hydroxyl group at the 3- or 17-position when R1 or R2 is hydrogen.
Type:
Grant
Filed:
January 21, 2003
Date of Patent:
June 26, 2007
Assignee:
Wyeth
Inventors:
Heather A. Harris, James C. Keith, Jr., Leo M. Albert, Galina Vid, Sreenivasulu Megati, Christopher P. Miller
Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein R1, R2, R2a, R3, R3a, and R4, and X as defined in the specification, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
May 17, 2004
Date of Patent:
December 12, 2006
Assignee:
Wyeth
Inventors:
Michael S Malamas, Robert E McDevitt, Iwan Gunawan, Eric S Manas, Michael D Collini, Heather A Harris, James C Keith, Jr., Leo M Albert, Cecil Richard Lyttle
Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein R1, R2, R2a, R3, R3a, and R4, and X as defined in the specification, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
August 19, 2004
Date of Patent:
October 31, 2006
Assignee:
Wyeth
Inventors:
Michael S. Malamas, Robert E. McDevitt, Iwan Gunawan, Eric S. Manas, Michael D. Collini
Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10, are as defined in the specification, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
March 18, 2004
Date of Patent:
June 27, 2006
Assignee:
Wyeth
Inventors:
Richard E. Mewshaw, Richard J. Edsall, Cuijian Yang, Heather A. Harris, James C. Keith, Jr., Leo M. Albert, Eric S. Manas
Abstract: This invention provides the use of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) in the treatment or inhibition of hepatic fibrosis and hepatic cirrhosis.
Type:
Grant
Filed:
January 29, 2004
Date of Patent:
June 13, 2006
Assignee:
Wyeth
Inventors:
Brenda Cooperstone, Robert Clare, George Stanley
Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein R, R?, A, A?, X, Y, and Y are as defined in the specification, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
April 21, 2004
Date of Patent:
April 4, 2006
Assignee:
Wyeth
Inventors:
Christopher P. Miller, Michael D. Collini, David H. Kaufman, Robert L. Morris, Robert R. Singhaus, Jr., John W. Ullrich, Heather A. Harris, James C. Keith, Jr., Leo M. Albert, Rayomand J. Unwalla
Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10, are as defined in the specification, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
December 11, 2002
Date of Patent:
July 5, 2005
Assignee:
Wyeth
Inventors:
Richard E. Mewshaw, Richard J. Edsall, Cuijian Yang, Heather A. Harris, James C. Keith, Jr., Leo M. Albert, Eric S. Manas
Abstract: This invention provides estrogen receptor modulators of formula I, having the structure R1, R2, and R3 are as defined in the specification, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
December 11, 2002
Date of Patent:
June 7, 2005
Assignee:
Wyeth
Inventors:
Robert E. McDevitt, Folake O. Adebi, Heather A. Harris, James C. Keith, Jr., Leo M. Albert
Abstract: The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below:
which are useful in lowering cholesterol levels.
Type:
Grant
Filed:
November 24, 2003
Date of Patent:
December 28, 2004
Assignee:
Wyeth
Inventors:
Chris P. Miller, Michael D. Collini, Bach D. Tran, Arthur A. Santilli
Abstract: This invention provides estrogen receptor modulators of formula I, having the structure
wherein,
R1, R2, R3, X, and Y are as defined in the specification, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
January 10, 2003
Date of Patent:
December 28, 2004
Assignee:
Wyeth
Inventors:
Richard D. Coghlan, William F. Fobare, Heather A. Harris, James C. Keith, Jr., Leo M. Albert
Abstract: This invention provides 3&bgr;-hydroxy-5,7,9-estratriene-17-one and a pharmaceutically acceptable salt of its 3-sulfate ester, which is useful as an estrogen.
Type:
Grant
Filed:
January 21, 2003
Date of Patent:
November 16, 2004
Assignee:
Wyeth
Inventors:
Syed M. Shah, Panolil Raveendranath, Michael Z. Kagan
Abstract: This invention provides estrogen receptor modulators of formula I, having the structure
wherein
R1, R2, R2a, R3, R3a, and R4, and X as defined in the specification, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
December 4, 2002
Date of Patent:
September 21, 2004
Assignee:
Wyeth
Inventors:
Michael S. Malamas, Robert E. McDevitt, Iwan Gunawan, Eric S. Manas, Michael D. Collini
Abstract: The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below:
which are useful in providing hormone replacement therapy.
Type:
Grant
Filed:
July 10, 2003
Date of Patent:
September 7, 2004
Assignee:
Wyeth
Inventors:
Chris P. Miller, Michael D. Collini, Bach D. Tran, Arthur A. Santilli
Abstract: This invention provides estrogen receptor modulators of formula I, having the structure
wherein
R, R′, A, A′, X, Y, and Y are as defined in the specification, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
December 16, 2002
Date of Patent:
August 10, 2004
Assignee:
Wyeth
Inventors:
Christopher P. Miller, Michael D. Collini, David H. Kaufman, Robert L. Morris, Robert R. Singhaus, Jr., John W. Ullrich, Heather A. Harris, James C. Keith, Jr., Leo M. Albert, Rayomand J. Unwalla
Abstract: This invention provides compounds of Formula I having the structure
wherein R1, R2, R3, R4, W, X, and Y are as defined hereinbefore or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
Abstract: This invention provides estrogen receptor modulators of formula I, having the structure
wherein
R1, R2, R3, R4 R5, R6, and R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
December 11, 2002
Date of Patent:
April 20, 2004
Assignee:
Wyeth
Inventors:
Richard E. Mewshaw, Richard J. Edsall, Stephen T. Cohn, Heather A. Harris, James C. Keith, Jr., Leo M. Albert
Abstract: This invention provides a pharmaceutically acceptable salt of 5&agr;-pregn-16-en-3&bgr;-ol-20-one 3-sulfate ester, which is useful as a progestational agent.
Type:
Grant
Filed:
November 1, 1999
Date of Patent:
March 30, 2004
Assignee:
Wyeth
Inventors:
Reinhold H. W. Bender, Mahdi B. Fawzi, Horace Fletcher, III, George O. Morton, Syed M. Shah, Xuejun Tang
Abstract: This invention provides estrogenic agents having the formula
wherein
A and B are each, independently,
R is SO3−X+;
X+ is alkali metal, alkaline earth metal, ammonium, alkylammonium containing 1-6 carbon atoms, or dialkylammonium containing 1-6 carbon atoms in each alkyl group, or trialkylammonium containing 1-6 carbon atoms in each alkyl group;
with the proviso that at least one of A or B is
Type:
Grant
Filed:
June 5, 2002
Date of Patent:
February 17, 2004
Assignee:
Wyeth
Inventors:
Michael Z. Kagan, Panolil Raveendranath, Syed M. Shah, Michael W. Winkley
Abstract: This invention provides a method of treating or inhibiting cardiovascular, cerebral vascular, or peripheral vascular disease in a mammal in need thereof, which comprises providing said mammal with an effective amount of a rapamycin.
Type:
Grant
Filed:
December 6, 2002
Date of Patent:
December 30, 2003
Assignee:
Wyeth
Inventors:
Neal I. Azrolan, Steven J. Adelman, Surendra N. Sehgal