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56results about How to "Reduces and avoids symptom and cause" patented technology

Stabilized polypeptides as regulators of rab gtpase function

The present invention provides inventive polypeptides comprising a C terminal RAB binding domain (RabBD) of RAB family interacting proteins (FIPs) stabilized by peptide stapling, and pharmaceutical compositions thereof. Also provided are methods for modulating RAB function comprising contacting an inventive stapled polypeptide with a RAB protein, and methods of treatment associated with modulation of RAB activity. The present invention also provides methods of making the inventive stapled polypeptides by ring closing metathesis of unstapled polypeptide precursors.
Owner:PRESIDENT & FELLOWS OF HARVARD COLLEGE

Bone marrow on x chromosome kinase (BMX) inhibitors and uses thereof

ActiveUS20150246913A1Amplify tyrosine kinase signalingDownstream signaling can be enhancedBiocideOrganic chemistryDiseaseTec kinase
The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the compounds of Formula (I) or (II), or compositions thereof, for treating or preventing a wide range of diseases (e.g., proliferative diseases (e.g., cancers, benign neoplasms, angiogenesis, inflammatory diseases, autoimmune diseases) and metabolic diseases (e.g., diabetes (e.g., type 2 diabetes, gestational diabetes)) in a subject. Treatment of a subject with a disease using a compound of Formula (I) or (II), or compositions thereof, may downregulate the expression and / or inhibit the activity of a kinase (e.g., a tyrosine kinase, such as a Tec kinase, in particular, bone marrow on X chromosome kinase (BMX)), and therefore, suppress tyrosine kinase singling in the subject.
Owner:DANA FARBER CANCER INST INC +1

Drug delivery polymer and uses thereof

Described herein are platinum-based brush-arm star polymers (Pt-BASPs), or a pharmaceutical composition thereof, for delivery of platinum-based agents, such as cisplatin. Also provided are methods and kits involving the Pt-BASPs, or a pharmaceutical composition thereof, for treating proliferative diseases such as cancers (e.g., lung cancer, head-and-neck cancer, esophagus cancer, stomach cancer, breast cancer, pancreas cancer, liver cancer, kidney cancer, or prostate cancer) in a subject.
Owner:MASSACHUSETTS INST OF TECH

Drug delivery polymers and uses thereof

Described herein are platinum-based brush-arm star polymers (Pt-BASPs), or a pharmaceutical composition thereof, for delivery of platinum-based agents, such as oxaliplatin. Also provided are methods and kits involving the Pt-BASPs, or a pharmaceutical composition thereof, for treating proliferative diseases such as cancers (e.g., lung cancer, head-and-neck cancer, esophagus cancer, stomach cancer, breast cancer, pancreas cancer, colorectal cancer, liver cancer, kidney cancer, or prostate cancer) in a subject.
Owner:MASSACHUSETTS INST OF TECH

Stabilized polypeptides as regulators of RAB GTPase function

The present invention provides inventive polypeptides comprising a C terminal RAB binding domain (RabBD) of RAB family interacting proteins (FIPs) stabilized by peptide stapling, and pharmaceutical compositions thereof. Also provided are methods for modulating RAB function comprising contacting an inventive stapled polypeptide with a RAB protein, and methods of treatment associated with modulation of RAB activity. The present invention also provides methods of making the inventive stapled polypeptides by ring closing metathesis of unstapled polypeptide precursors.
Owner:PRESIDENT & FELLOWS OF HARVARD COLLEGE

Drug delivery polymers and uses thereof

Described herein are platinum-based brush-arm star polymers (Pt-BASPs), or a pharmaceutical composition thereof, for delivery of platinum-based agents, such as oxaliplatin. Also provided are methods and kits involving the Pt-BASPs, or a pharmaceutical composition thereof, for treating proliferative diseases such as cancers (e.g., lung cancer, head-and-neck cancer, esophagus cancer, stomach cancer, breast cancer, pancreas cancer, colorectal cancer, liver cancer, kidney cancer, or prostate cancer) in a subject.
Owner:MASSACHUSETTS INST OF TECH

Brush-arm star polymer imaging agents and uses thereof

Disclosed are methods, compositions, reagents, systems, and kits to prepare nitroxide-functionalized brush-arm star polymer organic radical contrast agent (BASP-ORCA) as well as compositions and uses thereof. Various embodiments show that BASP-ORCA display unprecedented per-nitroxide and per-molecule transverse relaxivities for organic radical contrast agents, exceptional stability, high water solubility, low in vitro and in vivo toxicity, and long blood compartment half-life. These materials have the potential to be adopted for tumor imaging using clinical high-field 1H MRI techniques.
Owner:MASSACHUSETTS INST OF TECH +1

N-arylated analogues and uses thereof

ActiveUS20190373890A1Enhance therapeutic efficacyImproves overall therapyBiocideOrganic chemistryCystic fibrosis lungsPolymicrobial Infections
The present invention provides novel compounds of Formula (I′) and (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for killing a microorganism (e.g., bacteria, fungi, viruses, protozoa, or multicellular parasites), the prevention and / or treatment of infectious diseases (e.g., infections by microorganisms, bacterial infection, cystic fibrosis infection, foreign body infection, urinary tract infection (UTI), or infections leading to biofilms), controlling and / or eradicating biofilms (e.g., bacterial biofilms), preventing biofilm formation, sterilizing a surface, and / or eradicating persister cells (e.g., in a subject in need thereof or in a subject involving a biofilm).
Owner:UNIV OF FLORIDA RES FOUNDATION INC

Bone marrow on x chromosome kinase (BMX) inhibitors and uses thereof

InactiveUS20190112305A1Enhanced signalEnhance signaling downstreamOrganic chemistryAntineoplastic agentsDiseaseTec kinase
The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the compounds of Formula (I) or (II), or compositions thereof, for treating or preventing a wide range of diseases (e.g., proliferative diseases (e.g., cancers, benign neoplasms, angiogenesis, inflammatory diseases, autoimmune diseases) and metabolic diseases (e.g., diabetes (e.g., type 2 diabetes, gestational diabetes)) in a subject. Treatment of a subject with a disease using a compound of Formula (I) or (II), or compositions thereof, may downregulate the expression and / or inhibit the activity of a kinase (e.g., a tyrosine kinase, such as a Tec kinase, in particular, bone marrow on X chromosome kinase (BMX)), and therefore, suppress tyrosine kinase singling in the subject.
Owner:BETH ISRAEL DEACONESS MEDICAL CENT INC +1

Diphosphate mimetics and uses thereof

The present invention provides compounds of Formulae (I)-(V), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. In one aspect, compounds of the present invention are useful as glycosyltransferase inhibitors, in particular, O-linked N-acetylglucosamine (O-GlcNAc) transferase (OGT) inhibitors. In another aspect, compounds of the present invention are useful as kinase inhibitors, in particular, PLK1 inhibitors, GSK3P inhibitors, or MAPKAPK2 inhibitors. The present invention further provides methods of using the inventive compounds, e.g., as biological probes to study the inhibition of OGT and / or kinase activity and as therapeutics, e.g., for the treatment of OGT-associated and / or kinase-associated conditions.
Owner:PRESIDENT & FELLOWS OF HARVARD COLLEGE

Compounds for treating infectious diseases

The present invention provides compounds of Formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting fungal or parasitic growth. The compounds are useful as inhibitors of glycosylphosphatidylinositol (GPI)-anchor biosynthesis, in particular, as inhibitors of fungal Gwt1 activity. The present invention further provides methods of using the compounds described herein for treating fungal or parasitic infections. The compounds can also be used as biological probes to study the effects of inhibiting Gwt1 activity.
Owner:WHITEHEAD INST FOR BIOMEDICAL RES +1

Enterobactin conjugates and uses thereof

The present invention provides novel enterobactin-cargo conjugates, such as compounds of Formula (I), and salts thereof, where X is the cargo and may be an antibiotic, a fluorophore, or biotin. The present invention also provides complexes, compositions, kits, and methods that involve the compounds of Formula (I) and are useful in delivering a cargo to a bacterium, treating a bacterial infection, cystic fibrosis, and / or inflammatory bowel disease in a subject, preventing a bacterial infection, cystic fibrosis, and / or inflammatory bowel disease in a subject, inhibiting the growth of or killing a bacterium, or determining the concentration of a bacterium in a biological sample. In certain embodiments, the bacterium is a Gram-negative bacterium.
Owner:MASSACHUSETTS INST OF TECH

Phenylsulfonamido-benzofuran derivatives and uses thereof in the treatment of proliferative diseases

Described herein are phenylsulfonamido-benzofuran derivatives, and pharmaceutically acceptable salts thereof. Also provided are pharmaceutical compositions, methods, uses, and kits involving compounds of Formulae (I), (II), (III), (IV), (V), or (VI) for treating and / or preventing proliferative diseases (e.g. cancers, inflammatory diseases, and autoimmune diseases) in a subject. The compounds and pharmaceutical compositions as described herein inhibit at least one protein of the BCL-2 family in a biological sample or subject to treat and / or prevent a proliferative disease. In certain embodiments, compounds described herein are selective inhibitors of MCL-1, a BCL-2 family member protein.
Owner:MEMORIAL SLOAN KETTERING CANCER CENT

N-arylated analogues and uses thereof

The present invention provides novel compounds of Formula (I′) and (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for killing a microorganism (e.g., bacteria, fungi, viruses, protozoa, or multicellular parasites), the prevention and / or treatment of infectious diseases (e.g., infections by microorganisms, bacterial infection, cystic fibrosis infection, foreign body infection, urinary tract infection (UTI), or infections leading to biofilms), controlling and / or eradicating biofilms (e.g., bacterial biofilms), preventing biofilm formation, sterilizing a surface, and / or eradicating persister cells (e.g., in a subject in need thereof or in a subject involving a biofilm).
Owner:UNIV OF FLORIDA RES FOUNDATION INC

Methods for treating polycystic kidney disease and polycystic liver disease

The present invention provides compounds of Formula (I) or (II), which are thought to be able to inhibit mTOR (mammalian target of rapamycin) signaling pathway, induce UPR (unfolded protein response), and / or perturb mitochondrial function of a cyst cell (e.g., a cyst cell causing polycystic kidney disease (PKD, e.g., autosomal dominant PKD (ADPKD) or autosomal recessive PKD (ARPKD)) or polycystic liver disease (PLD, e.g., autosomal dominant PLD (ADPLD) or autosomal recessive PLD (ARPLD)). The invention also provides pharmaceutical compositions, kits, and methods involving the compounds described herein for use in treating PKD or PLD, inhibiting the growth of a cyst cell, and / or killing a cyst cell.
Owner:YALE UNIV +1
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