24results about "Dipeptides" patented technology

The present disclosure provides protein degradation targeting chimeras comprising (i) a benzo[c][l,2,5]thiadiazolyl-based targeting ligand capable of binding to toxic peptides and / or protein aggregates (e.g., alpha-synuclein fibrils, amyloid plaques, and / or tau protein tangles) in brain tissue for degradation; (ii) a ubiquitin ligase recruiting ligand; and (iii) a linker between (i) and (ii). These protein degradation targeting chimeras are useful, for example, in the treatment of neurodegenerative disorders such as Parkinson’s disease (PD), multiple system atrophy (MSA), and Lewy body dementia.

The present invention provides a composition and method for increasing muscle mass, preventing muscle atrophy, and promoting muscle growth. [Solution] In certain aspects, the disclosed composition comprises dileucine and leucine and pharmaceutically acceptable salts thereof. In certain aspects, the disclosed composition is administered to subjects in need to increase muscle mass, prevent muscle atrophy, and / or promote muscle growth.

The present invention provides a RAS inhibitor that selectively binds to or selectively inhibits Ras(ON). [Solution] A compound having the structure of formula Ia, or a pharmaceutically acceptable salt thereof. JPEG2026090276000524.jpg80170

Disclosed is an antibody-drug conjugate that binds to human oncology targets.The antibody-drug conjugate comprises an antibody or its antigen-binding fragment that is covalently linked to two anti-neoplastic drug payloads through a dual linker, where at least one of the anti-neoplastic drug payloads is a BH3 mimetic.The disclosure further relates to a method and composition for use in treating cancer by administering the antibody-drug conjugate provided herein.Also disclosed is a linker-drug conjugate that comprises at least one BH3 mimetic and a method for making it.

The invention relates to a method for producing a compound of general formula I, wherein E is silicon or germanium, by reacting a compound of general formula IIa and / or a compound of general formula IIb with a compound of general formula III RR'E(NR 3 R 4 )2 (III), where E is silicon or germanium.

The present disclosure provides therapeutic agents comprising VLA-4 (α4β1) and α4β? inhibitors as defined herein. Methods of using the therapeutic agents are also provided. The present disclosure further provides combinations of VLA-4 inhibitors with one or more agents that interact with one or more chemokine receptors, and methods of using the same. In some embodiments, the disclosed combinations can be used in methods of mobilizing hematopoietic stem cells. In some embodiments, the disclosed methods can be used in the treatment of conditions that require collection of hematopoietic stem cells for transfusion or in chemotherapy. The present disclosure further provides methods of treating a patient comprising administering an agent that interacts with a chemokine, such as G-CSF, plerixafor, BL-8040 (motixafortide), or Crop and a VLA-4 inhibitor.

The present invention provides compositions for the prevention, improvement, or treatment of obesity and diabetes. [Solution] A therapeutic composition is provided that contains zinc gluconate and cyclo-hispro (CHP) as active ingredients.

The present invention provides a linker, an antibody-drug conjugate, and a method for preparing the same. The drug linker of the present invention has good solubility, can significantly improve the water solubility of existing low-molecular-weight compounds, and improves the stability and uniformity of the conjugate after coupling with an antibody.

To provide compounds and compositions including such compounds useful for imaging and / or treatment of a glioma, a breast cancer, an adrenal cortical cancer, a cervical carcinoma, a vulvar carcinoma, an endometrial carcinoma, a primary ovarian carcinoma, a metastatic ovarian carcinoma, a prostate cancer, and the like.SOLUTION: A compound of a formula (I) is provided. In the formula, ABD is an antigen-binding domain; W1 is -C(O)-, -(CH2)n-, or the like; and one of R1, R2 and R3 is a group comprising an albumin-binding moiety.SELECTED DRAWING: Figure 1

The problem that the present invention aims to solve is to provide a heterobifunctional compound containing a target protein binding site and an E3 ubiquitin ligase binding site, as well as related methods of use. [Solution] The present invention relates to a bifunctional compound used as a regulator of Carsten Ras sarcoma protein (KRas or KRAS). In particular, the hetero-bifunctional compound of the present invention contains a site that binds to von Hippel-Lindau E3 ubiquitin ligase at one end and a site that binds to KRas at the other end, so that the target protein is positioned near the ubiquitin ligase, resulting in the degradation (and inhibition) of the target protein. The hetero-bifunctional compound of the present invention exhibits a broad range of pharmacological activity related to the degradation / inhibition of the target protein. Diseases or disorders resulting from abnormal control of the target protein can be treated or prevented with the compounds and compositions of the present invention.

A technique useful in the field of agri-horticulture such as a technique for preventing pest damage to plants is provided. Pest damage to plants is prevented by using various glutamic acid derivatives.

The present invention relates to a ketoamide compound, a method for preparing the same, a pharmaceutical composition, and uses thereof. Specifically, the ketoamide compound is represented by Formula A, its racemate, enantiomer, diastereomer, or mixture thereof, or its pharmaceutically active metabolite, or a pharmaceutically acceptable salt, solvate, or prodrug thereof. The ketoamide compound effectively inhibits coronavirus or Ebola virus, thereby preventing or treating coronavirus-related or Ebola virus-related diseases. Formula A: [Formula 1]

To solve a problem in which, coupling of BSH and an intracellular transport peptide can be performed by once synthesis by modifying the intracellular transport peptide by a maleimide group, in a prior art, however, there is a possibility of generation of chiral carbon on a coupling point when the maleimide group is used and generation of a racemic body.SOLUTION: The invention is configured so that, by coupling BSH and an intracellular transport peptide by a methylene carbonyl linker (-C-C(O)-), generation of a racemic body can be suppressed and a boron compound which can be safely administered to a human body can be acquired.SELECTED DRAWING: Figure 1

To provide compounds and radiolabeled compounds that can achieve both improved accumulation in target tissues and reduced accumulation in non-target tissues, particularly in the kidneys. [Solution] The compound of the present invention, when viewed macroscopically in terms of its chemical structure, has a chelate moiety located at the center of the structure, with an atomic group including an albumin binding moiety bonded to one side of the chelate moiety, and an atomic group including a target molecule binding moiety bonded to the other side of the chelate moiety. The chelate moiety may preferably be DOTA or a derivative thereof. The target molecule binding moiety may preferably have a structure that binds to a target molecule expressed in cancer tissue. The present invention also provides a radiolabeled compound in which the compound is coordinated to a radioactive metal ion.

To provide cannabinoid prodrug compounds that enable site-specific delivery to an area of interest.SOLUTION: A prodrug compound of cannabidiol (CBD), pharmaceutical compositions thereof and methods of use thereof in patients in need are provided. In at least some embodiments, the prodrug compounds of the present invention target a member of the soluble carrier 15 (SLC15) peptide transport family, including the PEPT1 (Peptide transporter 1) transporter system and enhances the uptake of the cannabinoid by at least 2 folds, 3 folds, 4 folds or preferably at least 5 folds higher than the degree if the cannabinoid was being delivered in its natural form.SELECTED DRAWING: Figure 2

The present invention provides a triazine compound having protein kinase inhibitory activity, and a pharmaceutical composition containing the compound for the prevention, mitigation, or treatment of cancer. [Solution] The present invention provides a 2,7-substituted pyrrolo[2,1-f][1,2,4]triazine compound, a pharmaceutically acceptable salt thereof, and a pharmaceutical composition for the prevention, mitigation, or treatment of diseases induced by abnormal cell growth containing this compound as an active ingredient. The 2,7-substituted pyrrolo[2,1-f][1,2,4]triazine cyclized compound exhibits excellent inhibitory effects on various protein kinases involved in growth factor signaling, and is therefore useful as a preventive, mitigating, or therapeutic agent for abnormal cell growth diseases induced by these protein kinases.