Abstract: This invention comprises methods of inducing or maintaining sphincter continence, or inhibiting or alleviating incontinence, in a mammal comprising administration of a compound of the formulae I or II:
wherein Z is a moiety selected from the group of:
wherein: R1 is selected from H, OH or the C1-C12 esters or C1-C12 alkyl ethers thereof, benzyloxy, or halogens; or C1-C4 halogenated ethers including trifluoromethyl ether and trichloromethyl ether; R2, R3, R4, R5, and R6 are H, OH or C1-C12 esters or C1-C12 alkyl ethers thereof, halogens, or C1-C4 halogenated ethers, cyano, C1-C6 alkyl, or trifluoromethyl, with the proviso that, when R1 is H, R2 is not OH; Y is the moiety:
R7 and R8 are alkyl or concatenated together to form an optionally substituted, nitrogen-containing ring; or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
June 29, 2001
Date of Patent:
September 24, 2002
Assignee:
Wyeth
Inventors:
Simon Nicholas Jenkins, Christopher Paul Miller
Abstract: This invention provides a method of contraception which comprises administering to a female of child beating age for a combination of a progestin at a daily dosage of 40-500 &mgr;g trimegestone, 250 &mgr;g-4 mg dienogest, or 250 &mgr;g-4 mg drospirenone, and an estrogen at a daily dosage equivalent in estrogenic activity to 10-20 &mgr;g ethinyl estradiol for 23-25 days beginning on day 1 of the menstrual cycle, and wherein the same dosage of the progestin and estrogen combination is administered in each of the 23-25 days.
Abstract: This invention provides compounds of Formula I having the structure
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 12, 2001
Date of Patent:
September 17, 2002
Assignee:
Wyeth
Inventors:
Mark Anthony Ashwell, William Ronald Solvibile, Dominick Anthony Quagliato, Albert John Molinari
Abstract: This invention provides substituted 4-phenyl, 4-pyridin-2-yl and and 4-pyridin-3-yl substituted indole, benzothiophene and benzofuran compounds: of the formula:
or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
Type:
Grant
Filed:
January 19, 2001
Date of Patent:
September 3, 2002
Assignee:
Wyeth
Inventors:
Jay E. Wrobel, Arlene J. Dietrich, Madelene M. Antane
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 ethers of 7-desmethylrapamycin which are useful in inducing immunosuppression and in the treatment of transplantation rejection, autoimmune diseases, solid tumors, fungal infections, and vascular disease.
Abstract: This invention provide pegylated hydroxyesters of rapamycin which are useful in inducing immunosuppression and in the treatment of transplantation rejection, autoimmune diseases, solid tumors, fungal infections, and vascular disease.
Abstract: This invention provides novel bicyclic compounds of Formula (I):
wherein u, v, m, Y, G, A—B, R1, R1a, R2, R4, R5, R5a, and R5b are defined in the specification which compounds exhibit activity as inhibitors of bone resorption and compounds of Formula (II)
wherein u, v, m, Y, G, D, A—B, R1, R1a, R2, R3, R4, R5, R5a, and R5b are defined in the specification which compounds exhibit activity as inhibitors of bone resorption.
Type:
Grant
Filed:
July 20, 2000
Date of Patent:
August 6, 2002
Assignee:
Wyeth
Inventors:
Arie Zask, Diane Barbara Hauze, Kenneth Lewis Kees, Richard Dale Coghlan, John Yardley
Abstract: This invention provides 1-oxorapamycins, which are useful in inducing immunosuppression, as a neurotrophic agent, and in the treatment of transplantation rejection, autoimmune diseases, solid tumors, fungal infections, and vascular disease.
Abstract: This invention provides hydroxyesters of 7-desmethylrapamycin which are useful in inducing immunosuppression and in the treatment of transplantation rejection, autoimmune diseases, solid tumors, fungal infections, and vascular disease.
Abstract: This invention provides a method of providing progestational therapy to a mammal in need thereof which comprises administering a progestationally effective amount of a pharmaceutically acceptable salt of 5&agr;-pregnan-3&bgr;-ol-20-one 3-sulfate ester to said mammal.
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:
September 11, 2000
Date of Patent:
April 30, 2002
Assignee:
American Home Products Corporation
Inventors:
Chris P. Miller, Michael D. Collini, Bach D. Tran, Anita Wai-Yin Chan, Arkadiy Z. Rubezhov
Abstract: The present invention provides compounds of the formula:
wherein R1, R2, R3, R4, X, n Y and Z, are as defined in the specification, or a pharmaceutically acceptable salt thereof, as well as pharmaceutical formulations and methods of treating or preventing disease states or syndromes which are caused or associated with an estrogen deficiency or an excess of estrogen utilizing these compounds.
Type:
Grant
Filed:
February 25, 2000
Date of Patent:
April 30, 2002
Assignee:
American Home Products Corporation
Inventors:
Marci C. Koko, John W. Ullrich, Arthur A. Santilli
Abstract: This invention comprises methods of inducing or maintaining sphincter continence, or inhibiting or alleviating incontinence, in a mammal comprising administration of ([1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol.
Type:
Grant
Filed:
June 29, 2001
Date of Patent:
April 23, 2002
Assignee:
American Home Products Corporation
Inventors:
Simon Nicholas Jenkins, Timothy Michael Argentieri
Abstract: This invention comprises methods of depression, anxiety, generalized anxiety disorder (GAD), hot flush, post partum depression, premenstrual syndrome, obesity, obsessive compulsive disorder, post-traumatic stress disorder, social phobia, disruptive behavior disorders, impulse control disorders, borderline personality disorder, chronic fatigue disorder, premature ejaculation, pain, attention deficit disorders, with and without hyperactivity, Gilles de la Tourette syndrome, bulimia nervosa, or Shy Drager Syndrome comprising administration of a selective serotonin reuptake inhibitor and compound of the formulae I or II:
wherein Z is a moiety selected from the group of:
wherein:
R1 is selected from H, OH or the C1-C12 esters or C1-C12 alkyl ethers thereof, benzyloxy, or halogen; or C1-C4 halogenated ethers including trifluoromethyl ether and trichloromethyl ether; R2, R3, R4, R5, and R6 are H, OH or C1-C12 esters or C1-C12 alkyl ethers thereof, halogens, or C1-C4 halogenated e
Abstract: This invention provides compounds of the formula
wherein R1, R2, R3, R4, R5, R6, R7, X, n and Y, are as defined in the specification, or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods utilizing the compounds for treating or preventing disease states or syndromes which are caused or associated with an estrogen deficiency or an excess of estrogen utilizing these compounds.
Abstract: This invention comprises methods of treating treatment or prevention of diseases associated with an excess of neuropeptide Y comprising administration of a compound of the formulae I or II:
wherein Z is a moiety selected from the group of:
wherein: R1 is selected from H, OH or the C1-C12 esters or C1-C12 alkyl ethers thereof, benzyloxy, or halogen; or C1-C4 halogenated ethers including trifluoromethyl ether and trichloromethyl ether; R2, R3, R4, R5, and R6 are H, OH or C1-C12 esters or C1-C12 alkyl ethers thereof, halogens, or C1-C4 halogenated ethers, cyano, C1-C6 alkyl, or trifluoromethyl, with the proviso that, when R1 is H, R2 is not OH; Y is the moiety:
R7 and R8 are alkyl or concatenated together to form an optionally substituted, nitrogen-containing ring; or a pharmaceutically acceptable salt thereof.
Abstract: This invention provides compounds of formula I having the structure
wherein R1, Ar, Ar′, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof, which are useful as contraceptive agents.
Type:
Grant
Filed:
March 24, 2000
Date of Patent:
March 12, 2002
Assignee:
American Home Products Corporation
Inventors:
Jay E. Wrobel, John F. Rogers, Daniel M. Green, Wenling Kao, James W. Jetter
Abstract: This invention provides estrogens and antiestrogens of formula I having the structure
wherein X, Y, Z, and R are as defined hereinbefore in the specification, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
October 13, 1998
Date of Patent:
March 12, 2002
Assignee:
American Home Products Corporation
Inventors:
Chris P. Miller, Ivo Jirkovsky, Bach Dinh Tran
Abstract: This invention provides novel water soluble pegylated esters of rapamycin, having the general structure:
wherein n is an integer from about 5 to about 450, as well as pharmaceutical compositions containing these compounds and methods for their use as immunosuppressive, anti-inflammatory, antifungal, antiproliferative and antitumor agents.
Type:
Grant
Filed:
August 16, 2000
Date of Patent:
December 18, 2001
Assignee:
American Home Products Corporation
Inventors:
Tianmin Zhu, Syed M. Shah, Richard W. Saunders