Patent classifications
C07K5/0215
CAMPTOTHECINE ANTIBODY-DRUG CONJUGATES AND METHODS OF USE THEREOF
The present disclosure provides antibody-drug conjugate (ADC) structures, which include a camptothecine or a camptothecine derivative linked to a polypeptide (e.g., an antibody) through a linker. The disclosure also encompasses compounds and methods for production of such conjugates, as well as methods of using the conjugates.
1,2,4-oxadiazole compounds as inhibitors of CD47 signalling
The present invention relates to compounds of formula (I), compositions, methods and uses involving the said formula (I) that inhibit CD47 signaling pathway. The present invention also relates to methods of making such compounds and their uses for the treatment of diseases or disorders mediated by CD47.
Macrocyclic compounds as proteasome inhibitors
The compounds of the present invention are represented by the following compounds having Formula I and Formula (I′): where the substituents R.sup.1, R.sup.2, R.sup.2′, R.sup.3, R.sup.4, R.sup.5, R′, R″, X, Y, and Z are as defined herein and where the substituents R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R′, R″, X, Y, and Z are as defined herein. These compounds are used in the treatment of bacterial infections, parasite infections, fungal infections, cancer, immunologic disorders, autoimmune disorders, neurodegenerative diseases and disorders, inflammatory disorders, or muscular dystrophy or for providing immunosuppression for transplanted organs or tissues. ##STR00001##
SPECIFICALLY-SHAPED CRYSTAL OF COMPOUND AND METHOD FOR PRODUCING SAME
The present invention provides a method for obtaining a specifically-shaped crystal (specifically, spherocrystal) of a compound with good reproducibility. This method for producing a specifically-shaped crystal (specifically spherocrystal) of a compound comprises: (1) a step for preparing a supersaturated solution of a compound having a degree of supersaturation equal to or higher than a critical degree of supersaturation; and (2) a step for precipitating a specifically-shaped crystal (specifically spherocrystal) of a compound from the supersaturated solution.
THERAPEUTIC COMPOUNDS AND METHODS
Disclosed herein are compounds of formula I: (I) or pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, and R.sup.3 may any of the values defined herein, as well as compositions comprising such compounds. Also disclosed are methods for treating diseases including neurodegenerative disorders such as Parkinson's Disease and Alzheimer's Disease.
##STR00001##
PEPTIDOMIMETIC INHIBITORS OF THE WDR5-MLL INTERACTION
The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.5a and R.sup.5b are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a condition, disease, or disorder responsive to inhibition of the WDR5 interaction with its binding partners including, but not limited to, the WDR5-MLL protein-protein interaction.
##STR00001##
Sulfoxyalkyl organonitro and related compounds and pharmaceutical compounds for use in medicine
The invention provides sulfoxyalkyl organonitro and related compounds, compositions containing such compounds, and methods for using such compounds and compositions to treat medical disorders, such as a neurodegenerative disorder, autoimmune disease, infection, or cancer in a patient. Exemplary sulfoxyalkyl organonitro compounds described herein include ((2-(3,3-dinitroaze-tidin-1-yl)-2-oxoethyl)sulfinyl)-D-alanine and variants thereof.
1,2,4-Oxadiazole Compounds as Inhibitors of CD47 Signalling Pathways
The present invention relates to compounds of formula (I), compositions, methods and uses involving the said formula (I) that inhibit CD47 signaling pathway. The present invention also relates to methods of making such compounds and their uses for the treatment of diseases or disorders mediated by CD47.
IMAGING AGENT
##STR00001##
The invention relates to platinum and rhenium complexes of formula (I) that may be used as imaging agents. In particular, the invention relates to imaging agents, for example imaging agents for use in the imaging of peroxisomes. Certain embodiments of the invention relate to compounds per se. Other embodiments relate to a process for the preparation of compounds and to the use of compounds as imaging agents. (Formula (I))
PSMA Imaging Agents
Compounds for targeting and agents for imaging, prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.