Patent classifications
A61P7/02
ARYL AMINOPYRIMIDINES AS DUAL MERTK AND TYRO3 INHIBITORS AND METHODS THEREOF
Aminopyrimidine containing compounds that inhibit both Mer tyrosine kinase (MerTK) activity and Tyro3 kinase activity are disclosed herein. Additionally disclosed are methods of synthesis and use of the aminopyrimidine containing compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents.
COMPOSITIONS AND METHODS OF TREATING THROMBOSIS
A method of inhibiting hypercoagulation and/or thrombosis in a subject having or at risk of hypercoagulation or thrombosis includes administering to the subject an amount of a composition effective to inhibit MRP-8/14 and/or MRP-14 binding to platelet CD36 and inhibit hypercoagulation and/or thrombosis in the subject.
PEG-LIPID
A PEG-lipid is produced by mixing a cation-PEG-lipid comprising at least one amino group with a sulfated glycosaminoglycan comprising at least one carbonyl group to form a Schiff base intermediate. A reducing agent is added to the Schiff base intermediate to form a sulfated glycosaminoglycan-PEG-lipid. The sulfated glycosaminoglycan-PEG-lipid can be used to biological tissue against thromboinflammation. Coating of biological tissue with the sulfated glycosaminoglycan-PEG-lipid can be done in a single step process and does not cause any significant cell aggregation.
PEG-LIPID
A PEG-lipid is produced by mixing a cation-PEG-lipid comprising at least one amino group with a sulfated glycosaminoglycan comprising at least one carbonyl group to form a Schiff base intermediate. A reducing agent is added to the Schiff base intermediate to form a sulfated glycosaminoglycan-PEG-lipid. The sulfated glycosaminoglycan-PEG-lipid can be used to biological tissue against thromboinflammation. Coating of biological tissue with the sulfated glycosaminoglycan-PEG-lipid can be done in a single step process and does not cause any significant cell aggregation.
Drug composition and coating
According to the invention there is provided inter alia a medical device for delivering a paclitaxel to a tissue, the device the device having a coating layer applied to a surface of the device, the coating layer comprising components i), ii) and iii), wherein component i) is a therapeutic agent which is paclitaxel; and component ii) is urea or a pharmaceutically acceptable salt thereof, or a urea derivative or a pharmaceutically acceptable salt thereof; and component iii) is succinic acid, glutaric acid or caffeine, or a pharmaceutically acceptable salt of any one thereof.
Materials and methods for producing blood products
Provided herein are materials and methods for the preparation of blood products. In one aspect, provided herein is a composition including platelets or platelet derivatives and an aqueous medium, wherein the aqueous medium has a protein concentration less than 50% of the protein concentration of donor apheresis plasma.
Methods of inhibiting MASP-2-dependent complement activation in a subject suffering from catastrophic antiphospholipid syndrome
In one aspect, the invention provides methods of inhibiting the effects of MASP-2-dependent complement activation in a living subject suffering from, or at risk for developing a thrombotic microangiopathy (TMA). The methods comprise the step of administering, to a subject in need thereof, an amount of a MASP-2 inhibitory agent effective to inhibit MASP-2-dependent complement activation. In some embodiments, the MASP-2 inhibitory agent inhibits cellular injury associated with MASP-2-mediated alternative complement pathway activation, while leaving the classical (C1q-dependent) pathway component of the immune system intact.
Synthetic peptides, pharmaceutical compositions comprising the same, and uses thereof in treating thromboembolism-related diseases
Disclosed herein is a biomolecule comprising a synthetic peptide for targeting thrombus, a pharmaceutical composition comprising the same, and uses thereof in the treatment of thromboembolism-related diseases. According to embodiments of the present disclosure, the synthetic peptide having the amino acid sequence of SEQ ID NO: 1, 2, or 3 exhibits a binding affinity and specificity to thrombus. Thus, the synthetic peptide may serve as a targeting element for delivering a therapeutic agent (e.g., an anticoagulant agent or a thrombolytic agent) to the thrombus thereby improving the therapeutic safety and efficacy of the therapeutic agent.
Treatment of hypercoagulopathy in Cushing's syndrome by administration of glucocorticoid receptor modulators
Novel methods for preventing, reducing the risk of development of, and for treating hypercoagulopathy in Cushing's syndrome patients with elevated risk of developing hypercoagulopathy are disclosed. The methods are further useful to prevent, to reduce the risk of developing, and to treat deep vein thrombosis (DVT), pulmonary embolism (PE), and venous thromboembolism (VTE); and to treat inflammatory states. The methods include: administering heteroaryl-ketone fused azadecalin glucocorticoid receptor modulator (HKGRM) to a Cushing's syndrome patient at risk of developing hypercoagulopathy, thereby treating hypercoagulopathy. Methods of preventing, reducing risk of developing, and of treating DVT, PR, or VTE in a Cushing's syndrome patient comprise administering a HKGRM to the patient. Methods of unmasking and subsequently reducing an inflammatory state comprise administering an effective amount of a HKGRM to a Cushing's syndrome patient, effective first to increase inflammatory symptoms and then to subsequently decrease said inflammatory symptoms in the patient.
Phenyl Amino Pyrimidine Compounds and Uses Thereof
The present invention relates to phenyl amino pyrimidine compounds which are inhibitors of protein kinases including JAK kinases. In particular the compounds are selective for JAK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.