The present invention provides a compound of Formula I: ##STR00001##
wherein R is H or ##STR00002##
R.sup.1 is H, halogen, C1-C3 alkyl, C3-C6 cycloalkyl, C1-C3 alkoxy, C2-C3 alkenyl, OCF.sub.3, ##STR00003##
R.sup.2 is H, halogen, C1-C3 alkyl, C1-C3 alkoxy, or C2-C4 alkenyl;
R.sup.3 is NH.sub.2, or CH.sub.2NH.sub.2; and
X is O, OCH.sub.2, OCH.sub.2CH.sub.2, OCH(CH.sub.3), CH.sub.2O, SCH.sub.2, CH.sub.2S, CH.sub.2, NHCH.sub.2, CH.sub.2NH, N(CH.sub.3)CH.sub.2, CH.sub.2CH.sub.2, C≡C, or a bond, wherein X is connected to phenyl ring A at the ortho or the meta position, 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 and rheumatoid arthritis.

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.

The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic gent 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 dysfuntion or skin inflammation or a respiratory disease (e.g., asthma).

This invention provides a method of synthesizing new active compounds for pharmaceutical uses including cancer treatment, wherein the cancers comprise breast, leukocytic, liver, ovarian, bladder, prostatic, skin, bone, brain, leukemia, lung, colon, CNS, melanoma, renal, cervical, esophageal, testicular, splenic, kidney, lymphatic, pancreatic, stomach and thyroid cancers. This invention provides compounds and compositions for up regulating levels of biomarker of Death Receptors including DR1, DR4 and DR5 or alike thereof, for the treatment of cancer and inhibition of cancer cell growth in a subject, and up regulating levels of biomarker of said Death Receptors in cells for the inhibition of cell growth. This invention is an anti-adhesion therapy which uses the compound as a mediator or inhibitor of adhesion proteins and angiopoietins, inhibiting excess adhesion and cell attachment. It modulates angiogenesis. The compounds are also used as mediators of cell adhesion receptor, cell circulating, cell moving and inflammatory diseases.

The present invention pertains to pharmaceutical chemical field, and relates to a sterol derivative as well as preparation method and uses thereof. Specifically, the present invention relates to a compound of Formula I, or a pharmaceutically acceptable salt, ester or ether thereof, wherein, R.sub.1 is selected from the group consisting of —OH, ═O(carbonyl), H, and C.sub.1-C.sub.3 alkyl; R.sub.2 is selected from the group consisting of —OH, H, and C.sub.1-C.sub.3 alkyl; R.sub.3 is selected from the group consisting of —OH, ═O, H, and C.sub.1-C.sub.3 alkyl; R.sub.4 is selected from the group consisting of —OH, H, and C.sub.1-C.sub.3 alkyl; and none, one, two, three or four of R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are —OH. The compound of the present invention can inhibit HMG-CoA reductase, tumor cells and lipase effectively, and is a potential drug for reducing blood-fat, antitumors, or for losing weight.

##STR00001##

Provided herein are timosaponin compounds of Formula I, II, III, I′, II′ and III′, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are uses of said timosaponin compounds for preparing medicament for the treatment of diseases associated with beta-amyloid in hosts or subjects in need thereof.

The present specification discloses tripartite androgen receptor eliminators (AREs), pharmaceutical compositions and medicaments comprising such AREs, methods and uses for such AREs and compositions and medicaments, and methods and uses for AREs and compositions and medicaments for treating an androgen receptor signaling-mediated condition, disease or disorder.

The present invention relates to esters of Montelukast with corticosteroids, preferably with des-ciclesonide, triamcinolone, budesonide or flunisolide, pharmaceutical compositions containing the same and the use thereof in the treatment of several respiratory tract diseases, especially asthma, chronic obstructive pulmonary disease (COPD) and allergic rhinitis. The invention further relates to the process for preparing said esters.

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.

3,4-thiazolo steroids are provided herein. Also provided herein are methods of making and using the same for the inhibition of cell proliferation or the killing of cells.