Abstract: This invention encompasses methods for the inhibition of Alzheimer's Disease comprising administering to a human in need thereof an effective amount of a compound of Formula I ##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, hexamethylenemino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.The present invention also provides methods of increasing TGF-.beta. expression in the brain, comprising administering to a human in need thereof an effective amount of a compound of formula 1.The present invention also provides methods of inhibiting the .beta.-amyloid peptide mediated neurotoxicity or inflammatory response associated with Alzheimer's Disease (AD) comprising administering to a human in need thereof an effective amount of a compound of formula 1.

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: 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: The administration of a xanthine oxidase inhibitor is effective for the treatment or prevention of the excessive resorption of bone in conditions such as osteoporosis and the like.

Abstract: A method of increasing macrophage function 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.Also encompassed by the invention is a method of treating immunocompromissed individuals comprising administering a compound of formula 1.

Abstract: The present invention provides methods of inhibiting bone loss in mammals via the administration to a mammal in need of such treatment an effective amount of a compound from a series of benzoquinolin-3-ones. Such compounds also are sequentially or concurrently coadministered with a bone antiresorptive agent or a bone anabolic agent.

Abstract: A method of inhibiting musculoaponeurotic fibromatoses comprising administering to a mammal 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, hexamethyleneimino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.

Abstract: A method of inhibiting one or more CNS disorders in a post-menopausal woman 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: The present invention provides a method of inhibiting hormone-dependent breast carcinoma in a mammal comprising administering to said mammal in need of treatment an effective amount of a first component which is a compound of formula I ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl);R.sup.2 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl);n is 2 or 3; andR.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;or a pharmaceutically acceptable salt thereof, and an effective amount of a second component which is a compound of formula II ##STR2## wherein either R.sup.4 is H or a lower alkyl radical and R.sup.5 is a lower alkyl radical, or R.sup.4 and R.sup.

Abstract: This invention encompasses methods for the inhibition of Alzheimer's Disease comprising administering to a human in need thereof an effective amount of a compound of Formula I ##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, hexamethylenemino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.The present invention also provides methods of increasing TGF-.beta. expression in the brain, comprising administering to a human in need thereof an effective amount of a compound of formula 1.The present invention also provides methods of inhibiting the .beta.-amyloid peptide mediated neurotoxicity or inflammatory response associated with Alzheimer's Disease (AD) comprising administering to a human in need thereof an effective amount of a compound of formula 1.

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, hydoxyl, 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: 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 bone loss or resorption, or lowering serum cholesterol, comprising administering to a human in need thereof a compound having the formula ##STR1## or a pharmaceutically acceptable salt or solvate thereof, in a low dosage amount. Also encompased by the invention is a a pharmaceutical formulation in unit dosage form comprising, per unit dosage, a low dosage amount.

Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 3-benzyl-benzofurans which are .alpha.-substituted with ether, thioether amino, cyano or halo that are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.

Abstract: Methods of inhibiting vascular smooth muscle cell migration comprising administering to a human or other mammal in need of treatment an effective amount of a compound having the formula ##STR1## wherein R.sub.1 and R.sub.3 are independently hydrogen, ##STR2## wherein Ar is optionally substituted phenyl; R.sub.2 is pyrrolidino, hexamethyleneimino, or piperidino; and pharmaceutically acceptable salts and solvates thereof.

Abstract: The invention provides compounds of the formula: ##STR1## wherein the variables are hereinbelow described; and salts thereof. Also, pharmaceutical formulations and methods for treating bacterial infections in man or other animals using the above compounds are disclosed.

Abstract: A method of inhibiting bone loss or resorption, or lowering serum cholesterol, comprising administering to a human in need thereof a compound having the formula ##STR1## or a pharmaceutically acceptable salt or solvate thereof, in a low dosage amount. Also encompased by the invention is a pharmaceutical formulation in unit dosage form comprising, per unit dosage, a low dosage amount.

Abstract: A method of inhibiting angiogenesis is disclosed 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 and piperidino; or a pharmaceutically acceptable salt of solvate thereof.

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.