C07J71/0031

ANTI-CD19 ANTIBODY DRUG CONJUGATES

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

ANTI-CD19 ANTIBODY DRUG CONJUGATES

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

ANTI-CD19 ANTIBODY DRUG CONJUGATES

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

Timosaponin compounds

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.

Glucocorticoid receptor agonists

Provided herein are compounds that are glucocorticoid receptor agonists useful for the treatment of autoimmune and inflammatory diseases, processes for preparing these compounds, and pharmaceutical compositions comprising these compounds.

NOVEL STEROID PAYLOADS, STEROID LINKERS, ADCs CONTAINING AND USE THEREOF

The invention provides novel glucocorticosteroids, glucocorticosteroid-linkers and antibody drug conjugates (ADC's) comprising an antibody or antibody fragment which binds to an antigen expressed on immune cells, optionally an antigen expressed on human immune cells. In some instances the ADCs comprise an anti-human VISTA (V-region Immunoglobulin-containing Suppressor of T cell Activation (1)) antibody or anti-VISTA antigen-binding antibody fragment which binds to VISTA expressing cells at physiologic pH having a short serum half-life (24-72 or 24-48 or 12-24 hours or less in a human VISTA knock-in rodent or ((1-3.5 days or less in a human or non-human primate). In some instances these ADCs have a rapid onset of action and are potent for prolonged duration as they are very effectively internalized by immune cells in large amounts where they are cleaved releasing large amounts of active steroid payload. The invention also relates to the use of such ADCs and novel steroids for the treatment of autoimmune, allergic and inflammatory conditions. The invention further relates to methods for reducing the adverse side effects and/or enhancing the efficacy of glucocorticoid receptor agonists by using such ADCs to selectively deliver these anti-inflammatory agents to target immune cells, such as monocytes, neutrophils, B cells, T cells, Tregs, cosinophils, NK cells, macrophages, myeloid cells, et al., and particularly myeloid cells, thereby reducing potential toxicity to non-target cells.

Anti-Inflammatory Compound and Use Thereof

Provided are an anti-inflammatory compound and use thereof. Specifically, provided are the compound or a tautomer, a mesomer, a racemate, an enantiomer and a diastereoisomer thereof, or a mixture form thereof, or a pharmaceutically acceptable salt thereof. Further provided are a method for preparing the compound and use thereof.

Montelukast esters and pharmaceutical compositions containing the same

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.

Steroids and protein-conjugates thereof

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

Glucocorticoid receptor agonists

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, CC, 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.