Abstract: This invention provides a pharmaceutically acceptable salt of 3&bgr;-hydroxy-5(10)-estrene-17-one 3-sulfate ester and a pharmaceutically acceptable salt of 3&agr;-hydroxy-5(10)-estrene-17-one 3-sulfate ester, which are useful as an estrogens.

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

Abstract: This invention provides the use of a combination of CCI-779 and EKB-569 in the treatment of neoplasms.

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.

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.

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: 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.

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.

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.

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.

Abstract: This invention provides compounds of Formula I having the structure wherein, R1, R2, R3, R4, R5, T, T1, T2, and X 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.

Abstract: This invention provides a method of treating or inhibiting an estrogen receptor positive carcinoma in a mammal in need thereof, which comprises providing said mammal with an effective amount of a combination of a rapamycin and an antiestrogen.

Abstract: This invention comprises methods of treatment, prevention, inhibition or alleviation of the problems associated with excessive intraocular pressure 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, 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.

Abstract: This invention provides compounds of Formula I having the structure wherein A, B, Z, R and R1 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.

Abstract: This invention provides a method of contraception which comprises administering to a female of child bearing age for 23-25 consecutive days, a first phase 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 3-8 days beginning on day 1 of the menstrual cycle, wherein the same dosage of the progestin and estrogen combination is administered in each of the 3-8 days, a second phase combination of a progeslin 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 4-15 days beginning on the day immediately following the last day of administration of the first phase combination, wherein the same dosage of the progestin and estrogen combination is administered in each of

Abstract: The present invention relates to new formulations containing one or more estrogens and 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below:

Abstract: This invention comprises methods of treating cardiovascular disorders and lowering blood LDL levels comprising administration of a statin 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 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, A, X, Y, Z, W, 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, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.

Abstract: This invention provides compounds of Formula I having the structure wherein R1, R2, R3, R4, R5, R6, Y, Z, m, n, and 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.

Abstract: This invention provides estra-5(10),7-dien-3&bgr;-ol-17-one or a pharmaceutically acceptable salt of its 3-sulfate ester, estra-5(10),7-dien-3&bgr;-ol-17-one 3-glucuronide or a pharmaceutically acceptable salt thereof, estra-5(10),7-dien-3&agr;-ol-17-one or a pharmaceutically acceptable salt of its 3-sulfate ester, estra-5(10),7-dien-3&bgr;-ol-17-one 3-glucuronide or a pharmaceutically acceptable salt thereof, estra-5(10),7-dien-3&bgr;-ol-17-one 3-alkali metal salt, and estra-5(10),7-dien-3&agr;-ol-17-one 3-alkali metal salt which are useful as estrogenic agents.