Patent classifications
A61K47/545
AMHRII-BINDING ANTIBODY DRUG CONJUGATES AND THEIR USE THEREOF IN THE TREATMENT OF CANCERS
The present invention relates to an antibody drug conjugate (ADC) of general formula (I) (D-Lk.sub.1-C(O)-Lk.sub.2-C.sub.2H.sub.4—NH-Lk.sub.3).sub.n-Ab. A pharmaceutical composition comprising, in a pharmaceutically acceptable medium, the said ADC is also concerned by the present invention, as well as the use of this ADC or composition as a medicament, and in particular in the prevention and/or the treatment of an anti-Müllerian hormone type II receptor (AMHRII) expressing cancer in an individual.
COMPOSITIONS, DEVICES AND METHODS FOR INDUCING IMMUNE RESPONSES TO INFECTIOUS AGENTS
Described herein are implantable devices comprising cells engineered to express and secrete antigens of infectious agents. The devices are useful for inducing protective immune responses against infectious agents.
RAPAFUCIN DERIVATIVE COMPOUNDS AND METHODS OF USE THEREOF
The present disclosure provides macrocyclic compounds inspired by the immunophilin ligand family of natural products FK506 and rapamycin. The generation of a Rapafucin library of macrocyles that contain FK506 and rapamycin binding domains should have great potential as new leads for developing drugs to be used for treating diseases.
BASE-EDITING SYSTEMS
The present disclosure relates to base-editing systems including a fusion protein including a DNA-binding domain and a cytidine deaminase domain and a non-protein uracil-DNA glycosylase inhibitor, and methods of using the same. The DNA-binding domains of base-editing systems of the present disclosure include domains with a variety of target region possibilities, which increase the number and type of sequences that can be edited. The npUGIs of the base-editing systems of the present disclosure improve UDG inhibition (e.g., UDG inhibition is more complete) and are suitable for use in a wide range of organisms.
CROSS-LINKING COMPOUNDS AND METHODS OF USE THEREOF
Compounds of Formula IA, IB, II, III, IV, and/or V are described herein along with their methods of use. A compound of the present invention may cross-link under physiological conditions and/or in vivo.
Bifunctional Small Molecules to Target the Selective Degradation of Circulating Proteins
The present disclosure is directed to bifunctional small molecules which contain a circulating protein binding moiety (CPBM) linked through a linker group to a cellular receptor binding moiety (CRBM) which is a membrane receptor of degrading cell such as a hepatocyte or other degrading cell. In certain embodiments, the (CRBM) is a moiety which binds to asialoglycoprotein receptor (an asialoglycoprotein receptor binding moiety, or ASGPRBM) of a hepatocyte. In additional embodiments, the (CRBM) is a moiety which binds to a receptor of other cells which can degrade proteins, such as a LRP1, LDLR, FcγRI, FcRN, Transferrin or Macrophage Scavenger receptor.
Method for making a conjugate azole-based surface modified silicon dioxide nanoparticle
A combination therapy involving different therapeutic molecules can enhance and improve the therapeutic potentials. An effective therapeutic strategy conjugates silica (SiO.sub.2) nanoparticles with, e.g., 3-glycidyloxypropyl, trimethoxysilane and azoles, e.g., 1,2,4-triazole (Tri), 3-aminotriazole (ATri), 5-aminetetrazole (Atet), imidazole (Imi). These exemplary materials—classified as SiO.sub.2-3GPS-Tri (Conj. 1), SiO.sub.2-3GPS-Atri (Conj. 2), SiO.sub.2-3GPS-Atet (Conj. 3), SiO.sub.2-3GPS-Btri (Conj. 4), and SiO.sub.2-3GPS-Imi (Conj. 5)—can amplify targeting of therapeutics for human colorectal carcinoma cells (HCT-116), enhancing anti-cancer effects.
BIFUNCTIONAL COMPOUNDS FOR THE TREATMENT OF CANCER
The invention provides bifunctional compounds of formula (I) or a pharmaceutically acceptable salt thereof. Formula (I). The compounds cause the degradation of SMARCA2 via the targeted ubiquination of SMARCA2 protein and subsequent proteasomal degradation and are thus useful for the treatment of cancer. The targeting ligand is of formula (TL).
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HETEROBIFUNCTIONAL COMPOUNDS AS DEGRADERS OF HPK1
Disclosed are Hematopoietic Progenitor Kinase 1 (HPK1) degradation/disruption compounds including a HPK1 ligand, a degradation/disruption tag and a linker, and methods for use of such compounds in the treatment of HPK1-mediated diseases.
METHODS FOR ENHANCING IMMUNITY AND TUMOR TREATMENT
Provided are compositions, combinations, and methods and uses for treating a subject having a tumor, lesion or cancer. In some aspects, the methods and uses include administering a targeting molecule that binds PD-L1, conjugated with phthalocyanine dye, such as IR700. In some aspects, after administration of the conjugate, a target area is illuminated with a wavelength of light suitable for the activation of the conjugate. In some aspects, the illumination leads to the killing of PD-L1-expressing cells. The provided embodiments result in growth inhibition, volume reduction, and elimination of tumors, lesions or cancers, including metastatic tumor cells, invasive tumor cells, heterogeneous tumors and/or tumors that are not responsive to and/or resistant to other therapies. The disclosure also relates to compositions, combinations, methods and uses for enhancing immune responses, such as anti-tumor or anti-cancer immune responses, for responses against tumor growth and for effective treatment of tumors, lesions or cancers.