Compounds of Formula (I) are estrogen receptor alpha modulators, where the variables in Formula (I) are described in the disclosure. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions that are estrogen receptor alpha dependent and/or estrogen receptor alpha mediated, including conditions characterized by excessive cellular proliferation, such as breast cancer.

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Compounds of Formula (I) are estrogen receptor alpha modulators, where the variables in Formula (I) are described in the disclosure. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions that are estrogen receptor alpha dependent and/or estrogen receptor alpha mediated, including conditions characterized by excessive cellular proliferation, such as breast cancer.

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The present disclosure provides a method of improvement, preservation, prophylaxis, or inhibition-of-deterioration of a healthspan parameter of a mammalian subject. In exemplary embodiments, the method comprises administering to the subject a composition that comprises an insulin-like growth factor-1 receptor (IGF-1 R) inhibitor, wherein the composition is administered in an amount effective to improve, provide prophylaxis for, or inhibit-the-deterioration of the healthspan parameter.

The present disclosure provides a method of improvement, preservation, prophylaxis, or inhibition-of-deterioration of a healthspan parameter of a mammalian subject. In exemplary embodiments, the method comprises administering to the subject a composition that comprises an insulin-like growth factor-1 receptor (IGF-1 R) inhibitor, wherein the composition is administered in an amount effective to improve, provide prophylaxis for, or inhibit-the-deterioration of the healthspan parameter.

Embodiments are directed to a secnidazole formulations and the use of a secnidazole formulation for the treatment of bacterial vaginosis (BV).

Method of treating a sexually transmitted infection in a subject in need thereof involving administering to the subject a therapeutically effective amount of secnidazole in a microgranule formulation, wherein the microgranule formulation comprises a plurality of microgranules having a volume-weighted particle size distribution within a microgranule population, wherein the volume-weighted particle size distribution as measured from a representative sample of the microgranule population comprises (a) 10% of the microgranule population having a volume-weighted particle size about no less than 470 micrometers; (b) 50% of the microgranule population having a volume-weighted particle size between about no less than 640 micrometers and about no more than 810 micrometers; (c) 90% of the microgranule population having a volume-weighted particle size about no more than 1170 micrometers; or (d) a combination thereof, which can include some or all of (a) through (c) above. Pharmaceutical compositions and uses thereof are included herein.

The present invention relates to a process for the preparation of a compound of formula (I) said process comprising the steps of: a) reacting a compound of formula (II), with an acylating or a silylating agent to produce a compound of formula (III), wherein P.sup.1 and P.sup.2 are each independently a protecting group selected from R.sup.2—Si—R.sup.3R.sup.4, or R.sup.1CO—, wherein R.sup.1 is a group selected from C.sub.1-6alkyl or C.sub.3-6cycloalkyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C.sub.1-4alkyl; R.sup.2, R.sup.3 and R.sup.4 are each independently a group selected from C.sub.1-6alkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C.sub.1-4alkyl; b) reacting the compound of formula (III) in the presence of palladium acetate or a derivative thereof to produce compound of formula (IV); and c) reacting the compound of formula (IV) with a reducing agent to produce compound of formula (I). ##STR00001##

Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula I structure:

##STR00001## and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

The present invention relates to a process for the preparation of a compound of formula (I) comprising the steps of a) reacting a compound of formula (II) with a silylating or an acylating agent to produce compound of formula (III), wherein P.sup.1 is a protecting group selected from R.sup.2—Si—R.sup.3R.sup.4 or R.sup.1CO—, R.sup.1 is a group selected from C.sub.1-6alkyl or C.sub.3-6cycloalkyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C.sub.1-4alkyl; R.sup.2, R.sup.3 and R.sup.4 are each independently a group selected from C.sub.1-6alkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C.sub.1-4alkyl; b) halogenation or sulfinylation of the compound of formula (III) to produce a compound of formula (IV); wherein X is halo, or —O—SO—R.sup.5, and R.sup.5 is a group selected from C.sub.6-10aryl or heteroaryl, each group being optionally substituted by one or more substituents independently selected from chloro or C.sub.1-4alkyl; c) dehalogenation or desulfinylation of the compound of formula (IV) to produce compound of formula (V); and d) reacting the compound of formula (V) with a reducing agent to produce compound of formula (I). ##STR00001##

The present invention relates to a use of D-chiro-inositol, pinitol, or analog compounds thereof for preventing or treating female menopausal symptoms. The active ingredient compound of the present invention has an effect of increasing the activity of female hormones by increasing the blood concentration of 17β-estradiol and lowering the blood concentration of sex hormone-binding globulin. Therefore, the active ingredient compound of the present invention can be developed as a drug or a nutraceutical for preventing, alleviating or treating female menopausal symptoms. The active ingredient of the present invention is derived from a natural product, and thus, unlike an agonist of female sex hormones or chemically synthesized sex hormones, has very few side effects when applied to the human body.