The present disclosure provides anti-CD19 antibody drug conjugates (ADCs), including compositions and methods of using such ADCs.

The present disclosure provides human tumor necrosis factor alpha antibody glucocorticoid receptor agonist conjugates and methods of using the conjugates for the treatment of autoimmune and inflammatory diseases.

Provided herein are glucocorticoid receptor agonist immunoconjugates, glucocorticoid receptor agonists, and methods of using the same, e.g., to treat autoimmune or inflammatory diseases.

Described herein protein steroid conjugates that are useful, for example, for the target-specific delivery of glucocorticoids (GCs) to cells.

The present invention discloses a process for the preparation of pregnadiene derivatives having formula I, their stereoisomer and intermediate thereof. Formula I wherein each substituent is independently, R.sub.1 and R.sub.2 is hydrogen or C.sub.1-C.sub.8 straight, branched alkyl chain, saturated or unsaturated cycloalkyl; R.sub.3 is hydrogen or wherein R.sub.5 represents C.sub.1-C.sub.8 straight, branched alkyl chain or cycloalkyl; R.sub.4 is hydrogen or halogen; R.sub.6 is hydrogen or halogen;

##STR00001##

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).

A drug conjugate of a glucocorticoid receptor agonist, and an application thereof in medicine. Specifically, the present invention relates to an antibody-drug conjugate as represented by formula (I): Ab-(L-D)k (I), wherein Ab is an antibody or an antigen-binding fragment thereof, L is a linker covalently linking Ab to D, k is 1 to 20, and D is as represented by formula (II-A) or (II-B). The groups in the formulas are as defined in the description. The antibody-drug conjugate can effectively treat autoimmune diseases.

##STR00001##

The invention provides a novel, general, and facile strategy for the creation of small molecules with high structural and stereochemical complexity. Aspects of the methods include ring system distortion reactions that are systematically applied to rapidly convert readily available natural products to structurally complex compounds with diverse molecular architectures. Through evaluation of chemical properties including fraction of sp.sup.3 carbons, ClogP, and the number of stereogenic centers, these compounds are shown to be significantly more complex and diverse than those in standard screening collections. This approach is demonstrated with natural products (gibberellic acid, adrenosterone, and quinine) from three different structural classes, and methods are described for the application of this strategy to any suitable natural product.

The invention relates to a drug conjugate including a drug and a plant steroid. The drug conjugate may target the drug for intestinal cell delivery, and thus may be used to treat diseases, including intestinal diseases, or to affect intestinal metabolism. The invention therefore also relates to treating intestinal diseases and affecting intestinal metabolism with the drug conjugate.

The present invention discloses a process for the preparation of 16, 17-acetals of pregnane derivatives having formula I ##STR00001##
wherein each substituent is independently selected from; R.sub.1 is H or CH.sub.3; R.sub.2 is C.sub.1-C.sub.6 linear or branched alkyl, alkynyl group or cycloalkyl group; aryl or heteroaryl group; or R.sub.1 and R.sub.2 combine to form saturated, unsaturated C.sub.3-C.sub.6 cyclic or heterocyclic ring; R.sub.3 and R.sub.4 are same or different and each independently represents H or halogen; R.sub.5 is OH or OCOR wherein R represents H or C.sub.1-C.sub.6 linear, branched or cyclic alkyl group that may be substituted.