Abstract: The present invention provides aqueous inclusion complexes of certain known benzothiophene compounds, particularly Raloxifene, and water soluble cyclodextrins. Also provided are pharmaceutical compositions of such inclusion complexes, and methods of using these complexes for inhibiting bone loss and reducing serum cholesterol in mammals.

Abstract: A method of inhibiting atrophy of the skin or vagina comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is oprionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.

Abstract: The present invention relates to compounds of the formula ##STR1## where X is a bond or --CH2--;R.sup.2 is pyrrolidino;R is OH, --OSO.sub.2 --(CH.sub.2).sub.n --CH.sub.3 or ##STR2## R.sup.1 is hydrogen, OH, fluoro, chloro, --OSO.sub.2 --(CH.sub.2).sub.n --CH.sub.3 or ##STR3## each R.sup.3 is independently C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, unsubstituted or substituted phenyl where the substituent is fluoro, chloro, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy;each n is independently 3, 4 or 5; and pharmaceutically acceptable salts and solvates thereof; provided that at least one of R and R.sup.1 is ##STR4## The invention also relates to methods of use of the compounds of formula I and pharmaceutical compositions which comprise compounds of formula I.

Abstract: The present invention provides a method for minimizing the bone loss effect of a compound of formula II ##STR1## or a pharmaceutically acceptable salt thereof, wherein said formula II compound is administered to a mammal in need of treatment, comprising concurrently or sequentially administering to said mammal an effective amount of a compound of formula I ##STR2##

Abstract: The present invention relates to sulfonate and carbamate derivatives of 3-aroylbenzo[b]thiophenes, pharmaceutical formulations containing these compounds and methods of using such compounds for inhibiting the loss of bone, lowering serum cholesterol levels and therapeutically treating hormone dependent mammalian breast and uterine carcinoma.

Abstract: This invention discloses methods of using certain aryl-benzo[b]thiophene and benzo[b]furan compounds to block or inhibit cannabinoid receptors in mammals. It also discloses novel compounds which are antagonists of the cannabinoid receptors and also discloses pharmaceutical formulations which contain the compounds as an active ingredient.

Abstract: A method of inhibiting breast disorders administering to a human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3 ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.

Abstract: This invention provides a new method for treating osteoporosis comprising administering:1) a compound of formula I ##STR1## wherein R and R.sup.1, independently, are hydrogen, hydroxyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 acyloxy, C.sub.1 -C.sub.6 alkoxy-C.sub.2 -C.sub.6 -acyloxy, R.sup.2 -substituted aryloxy, R.sup.2 -substituted aroyloxy, R.sup.3 -substituted carbonyloxy or halo;R.sup.2 is C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 -alkoxy, hydrogen or halo; andR.sup.3 is C.sub.1 -C.sub.6 -alkoxy or aryloxy;n is 2, 3 or 4; andp is 4, 5 or 6;or a pharmaceutically acceptable salt or solvate thereof; together with2) a progestin selected from medroxyprogesterone, norethindrone or norethynodrel, or a pharmaceutically acceptable salt thereof; in amounts such that the combination retains or increases bone density.

Abstract: A method of inhibiting hirsutism or alopecia in women comprising administering to a female human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.

Abstract: A method of inhibiting imperfect tissue repair or a physiological condition due at least in part thereto comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.

Abstract: The present invention provides a method for treating hyperglycemia in mammals by administering an antiestrogen compound and pharmaceutically acceptable salts and solvates thereof.

Abstract: The present invention provides a compound of formula I ##STR1## wherein R.sub.1 is hydrogen, a hydroxy protecting group, or methyl;R.sub.2 and R.sub.3 are independently C.sub.1 -C.sub.6 alkyl, or R.sub.2 and R.sub.3, together with the nitrogen to which they are attached, form a heterocycle selected from the group consisting of pyrrolidino, hexamethyleneimino, morpholino, and piperidino;Z is bromo, chloro, fluoro, hydroxy, a protected hydroxy, or hydrogen; and pharmaceutically acceptable salts and solvates thereof.The present invention further provides pharmaceutical compositions containing compounds of formula I, optionally containing estrogen or progestin, and the use of such compounds alone, or in combination with estrogen or progestin, for alleviating the symptoms of post-menopausal syndrome, particularly osteoporosis, cardiovascular related pathological conditions, and estrogen-dependent cancer.

Abstract: A method of inhibiting scarring comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt or solvate thereof.

Abstract: A method of inhibiting bone prosthesis degeneration comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.

Abstract: The present invention provides a method for inhibiting bone loss comprising administering to a human in need of treatment an effective amount of vanadyl sulfate, or a pharmaceutically acceptable solvate or hydrate thereof, and pharmaceutical compositions thereof.

Abstract: The present invention provides a method for inhibiting bone loss comprising administering to a human in need of treatment an effective amount of a compound of formula I ##STR1## wherein each R is the same or different --H, --C.sub.1 -C.sub.6 alkyl, --CH.sub.2 OH, or --CH.sub.2 O(C.sub.1 -C.sub.6) alkyl; andeach R.sup.1 is the same or different --H, --C.sub.1 -C.sub.6 alkyl, --CH.sub.2 OH, or --CH.sub.2 O(C.sub.1 -C.sub.6)alkyl;or a pharmaceutically acceptable solvate or hydrate thereof, and pharmaceutical compositions thereof.

Abstract: The current invention provides methods and pharmaceutical formulations that are useful for inhibiting the loss of bone. These methods and formulations can be used without the associated adverse effects of estrogen therapy, and thus serve as an effective and acceptable treatment for osteoporosis.

Abstract: A method of inhibiting vasomotor symptoms and attending psychological disturbances surrounding post-menopausal syndrome comprising administering to a female human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.

Abstract: Provided are compounds of the formula II ##STR1## wherein R.sub.6 and R.sub.7 are independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.5 is naphthyl, substituted nephthyl, or phenyl substituted one to three times with C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkyl, phenyl, or hydroxy; with the proviso that if the phenyl is substituted once with hydroxy, it must be further be substituted once or twice with C.sub.1 -C.sub.6 alkoxy, C.sub.l -C.sub.6 alkyl, phenyl or hydroxy, and pharmaceutically acceptable salts thereof.

Abstract: A method of inhibiting 5-lipoxygenase comprising administering to a mammal in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.3 is hydrogen, or a group of the formula ##STR2## wherein R.sub.4 phenyl, substituted phenyl, naphthyl or substituted naphthyl, with the proviso that when R.sub.1 and R.sub.2 are both C.sub.1 -C.sub.6 alkyl, R.sub.3 is not hydrogen; and pharmaceutically acceptable salts thereof.