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 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, 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: 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, 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 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 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
Abstract: This invention comprises methods of inducing or maintaining sphincter continence, or inhibiting or alleviating incontinence, in a mammal comprising administration of 2-(4-Hydroxy phenyl)-3-methyl-1-(4-(2-piperidin-1-yl-ethoxy)-benzyl-1H-indol-5-ol
Type:
Grant
Filed:
March 1, 2002
Date of Patent:
October 21, 2003
Assignee:
Wyeth
Inventors:
Simon Nicholas Jenkins, Timothy Michael Argentieri
Abstract: This invention provides compounds of Formula I having the structure
wherein,
U, V, W, X, and Y are as defined hereinbefore,
or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.
Type:
Grant
Filed:
July 2, 2002
Date of Patent:
August 12, 2003
Assignee:
Wyeth
Inventors:
Mark Anthony Ashwell, William Ronald Solvibile, Dominick Anthony Quagliato, Albert John Molinari
Abstract: This invention provides estrogen receptor modulators of formula I, having the structure
wherein
X, Y1, Y2, Y3, Y4, Z1, Z2, Z3, and Z4 are as defined in the specification, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
May 15, 2002
Date of Patent:
July 8, 2003
Assignee:
Wyeth
Inventors:
Christopher P. Miller, Michael D. Collini, Heather A. Harris, James C. Keith, Jr.
Abstract: The present invention relates to new formulations containing one or more estrogens and 2-Phenyl-1-[4-(amino-1-yl-alk-1-ynyl)-benzyl]-1H-indol-5-ol compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structure below:
and related methods of treatment for providing tissue selective estrogenic activity while minimizing undesirable side effects of estrogen treatment or therapy, such as excessive estrogenic uterine stimulation.
Type:
Grant
Filed:
May 6, 1999
Date of Patent:
June 24, 2003
Assignee:
Wyeth
Inventors:
James Harrison Pickar, Barry Samuel Komm
Abstract: This invention provides compounds of Formula I having the structure
wherein:
A, X, Y, Z, R1, R2, R3, R4, R5, and R6 are as defined hereinbefore or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.
Abstract: This invention provides estrogen receptor modulators of formula 1, having the structure
wherein
X, Y1, Y2, Y3, Y4, Z1, Z2, Z3, and Z4 are as defined in the specification, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
April 15, 2002
Date of Patent:
May 6, 2003
Assignee:
Wyeth
Inventors:
Christopher P. Miller, Michael D. Collini, Heather A. Harris, James C. Keith, Jr.
Abstract: This invention provides tissue selective estrogens of formula I having the structure
wherein:
R1 and R2 are independently, hydrogen, alkyl chain of 1-6 carbon atoms, benzyl, acyl of 2-7 carbon atoms, benzoyl,
X is hydrogen, alkyl of 1-6 carbon atoms, CN, halogen, trifluoromethyl, or thioalkyl of 1-6 carbon atoms;
n=1-3;
with the proviso that at least one of R1 or R2 are not hydrogen, alkyl chain of 1-6 carbon atoms, benzyl, acyl of 2-7 carbon atoms, or benzoyl;
or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
March 1, 2002
Date of Patent:
March 25, 2003
Assignee:
Wyeth
Inventors:
Chris P. Miller, Michael D. Collini, Bach D. Tran, Anita Wai-Yin Chan, Arkadiy Z. Rubezhov