The invention relates to processes for preparing 17-alkynyl-7-hydroxy-steroids, such as 17-Ethynyl-10R,13S-dimethyl 2,3,4,7,8R,9S, 10,11,12,13,14S,15,16,17-hexadecahydro-1H-cyclopenta[a]phenanthrene-3R,7R,17S-triol (also referred to as 17-ethynyl-androst-5-ene-3, 7, 17-triol), that are essentially free of process impurities having binding activity at nuclear estrogen receptors.

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, betulinic acid derivaties that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: ##STR00001##
These compounds are useful for the treatment of HIV and AIDS.

Anti-inflammatory and antiallergic compounds of the glucocorticosteroid series, according to formula (I) according to formula (I) defined herein are useful for treating diseases of the respiratory tract characterized by airway obstruction.

The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic agent such as fluticasone or triamcinolone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, meibomian gland dysfunction or skin inflammation or a respiratory disease (e.g., asthma).

It is intended to provide a novel terpenoid derivative that exhibits anti-inflammatory action and a cytoprotective action by activating the Keap1/Nrf2/ARE signaling pathway. The present invention provides terpenoid derivative A represented by the following formula (I):

##STR00001##

The present invention relates to a steroid compound and a conjugate thereof, and specifically relates to a compound and a conjugate thereof, or a tautomer, a mesomer, a racemate, an enantiomer and a diastereoisomer thereof, or a mixture form thereof, or a pharmaceutically acceptable salt thereof; and a method for preparing the compound and the conjugate thereof and the use thereof.

Described herein protein drug conjugates and compositions thereof that are useful, for example, for the target-specific delivery of drugs to cells. By administering these compounds, compositions, and conjugates as described herein to specific target cells, side-effects due to non-specific binding phenomena, for example, to non-target cells are reduced. In certain embodiments, compounds, compositions, and conjugates are provided, which include hydrophilic residues in linker-payloads and protein conjugates thereof.

The present invention provides a compound of Formula I: ##STR00001## wherein R.sup.1 is H, halogen, C1-C3 alkyl, or C1-C3 alkoxy; R.sup.2 is H or halogen; and X is O, OCH.sub.2, or CH.sub.2, or a pharmaceutically acceptable salt thereof, wherein the compound of Formula I, or pharmaceutically acceptable salt thereof is useful for treating autoimmune and inflammatory diseases, such as atopic dermatitis, rheumatoid arthritis, and lupus nephritis.

A drug on the basis of 7,19-epoxy steroids, comprising a compound of the general formula (I)

##STR00001## or a physiologically acceptable salt thereof, wherein R.sup.1=H; methyl, aryl-CH.sub.2, R.sup.xC(O) or R.sup.xOC(O), or R.sup.1O is dispensed with if there is a double bond between 4-5, W.sup.1, W.sup.2, independently of each other, represent H, OH, CHR.sup.2OH, CHR.sup.2R.sup.x, CR.sup.2R.sup.xOH or W.sup.1 and W.sup.2 together represent O, R.sup.2=saturated or unsaturated, optionally branched alkyl groups with 4 to 9 C atoms, wherein these alkyl groups can also have a cyclopropane or cyclobutane substructure; R.sup.3=methyl or ethyl, X.sup.1, X.sup.2 independently of each other represent R.sup.x or OR.sup.5, or together represent O, NOR.sup.4; Y.sup.1, Y.sup.2 independently of each other represent R.sup.x or OR.sup.5, or together represent O, NOR.sup.4; or X.sup.1 and Y.sup.1 together form a double bond or an epoxy group; Z.sup.1, Z.sup.2 independently of each other represent R.sup.x or OR.sup.5, or together represent O, NOR.sup.4, CH.sub.2; R.sup.4 independently of each other represent H, alkyl or aryl; and R.sup.5 independently of each other represent H; alkyl, aryl-CH.sub.2, R.sup.xC(O) or R.sup.xOC(O), SO.sub.3H, SO.sub.3CH.sub.3, PO(OH).sub.2 or glycosyl; with each R.sup.x independently of each other representing H, saturated or unsaturated, optionally branched alkyl groups, saturated or unsaturated, optionally branched substituted alkyl, aryl, heteroaryl, PEG, SO.sub.3H, PO(OH).sub.2, or glycosyl; and wherein up to 3 hydrogens can be substituted by fluorine.

Chemical entities that are novel compounds, pharmaceutical compositions and methods of treatment of cancer are described.