A61K31/787

CUCURBITURIL MOLECULAR CONTAINERS AND METHODS OF USING SAME
20210379099 · 2021-12-09 ·

Disclosed herein are water-soluble, cyclic cucurbit[n]uril, compositions containing the same, methods of preparation thereof, and uses thereof. These compounds are useful, for example, as sequestering agents for various agents, such as, for example, drugs of abuse.

AGENT TARGETING DOUBLE-MEMBRANE ORGANELLE DNA

The present invention provides a drug for a pathological condition including mitochondria-related disease by a conjugate of a double-membrane organelle DNA sequence recognizing compound and a double-membrane organelle localizable compound. The present invention provides a conjugate in which a double-membrane organelle localizable lipophilic cation is attached to linear PI polyamide that specifically binds to a double-membrane organelle DNA sequence, a linear PI polyamide-TPP conjugate targeting the mitochondrial DNA mutation or polymorphism, comprising the conjugate, and a pharmaceutical composition comprising the conjugate.

AGENT TARGETING DOUBLE-MEMBRANE ORGANELLE DNA

The present invention provides a drug for a pathological condition including mitochondria-related disease by a conjugate of a double-membrane organelle DNA sequence recognizing compound and a double-membrane organelle localizable compound. The present invention provides a conjugate in which a double-membrane organelle localizable lipophilic cation is attached to linear PI polyamide that specifically binds to a double-membrane organelle DNA sequence, a linear PI polyamide-TPP conjugate targeting the mitochondrial DNA mutation or polymorphism, comprising the conjugate, and a pharmaceutical composition comprising the conjugate.

Method for producing hyaluronidase conjugate with polyethylenepiperazine derivatives and the use of the conjugate produced

This disclosure relates to methods for obtaining immobilized enzyme preparations, in particular to a preparation and application of a novel active conjugate of an enzyme with a polymer carrier. Said conjugate possesses the properties of the known Longidaza® drug and inhibits hyperplasia of connective tissue, and presents anti-inflammatory action, and can be used for manufacturing stable, active and safe in use long-acting drugs in the form of a suppository, ointment, injection, cosmetic cream, and for making veterinary drugs. These methods include conjugation of hyaluronidase with a water-soluble copolymer using the carbodiimide or azide conjugation method. The conjugation is carried out with the use of a copolymer N-oxide 1,4-ethylene piperazine, (N carboxymethyl)-1,4-ethylene piperazine or its hydrazide, and 1,4-ethylene piperazine of general formula: ##STR00001## where n is from 40% to 90% of the total number of units; m is from 3% to 40% of the total number of units; and n+m+1=100%.

Method for producing hyaluronidase conjugate with polyethylenepiperazine derivatives and the use of the conjugate produced

This disclosure relates to methods for obtaining immobilized enzyme preparations, in particular to a preparation and application of a novel active conjugate of an enzyme with a polymer carrier. Said conjugate possesses the properties of the known Longidaza® drug and inhibits hyperplasia of connective tissue, and presents anti-inflammatory action, and can be used for manufacturing stable, active and safe in use long-acting drugs in the form of a suppository, ointment, injection, cosmetic cream, and for making veterinary drugs. These methods include conjugation of hyaluronidase with a water-soluble copolymer using the carbodiimide or azide conjugation method. The conjugation is carried out with the use of a copolymer N-oxide 1,4-ethylene piperazine, (N carboxymethyl)-1,4-ethylene piperazine or its hydrazide, and 1,4-ethylene piperazine of general formula: ##STR00001## where n is from 40% to 90% of the total number of units; m is from 3% to 40% of the total number of units; and n+m+1=100%.

METHODS FOR MODULATING CHEMOTHERAPEUTIC CYTOTOXICITY

Disclosed herein are methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a chemotherapeutic agent. Example disclosed methods reduce cardiotoxicity of a chemotherapeutic agent. Also disclosed are methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a chemotherapeutic agent. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the chemotherapeutic agent.

METHODS FOR MODULATING CHEMOTHERAPEUTIC CYTOTOXICITY

Disclosed herein are methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a chemotherapeutic agent. Example disclosed methods reduce cardiotoxicity of a chemotherapeutic agent. Also disclosed are methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a chemotherapeutic agent. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the chemotherapeutic agent.

ORAL RINSE COMPOSITIONS FOR ALLEVIATING XEROSTOMIA COMPRISING POLYETHYLENE GLYCOL DERIVATIVES
20230248759 · 2023-08-10 ·

An oral rinse composition for alleviating xerostomia includes a polyethylene glycol derivative as an active ingredient, which allows not only covalent bonding of the composition to the oral mucosa without irritation to increase the oral moisturizing capacity, but also allows easy manufacture, storage, use and packaging by having a granule formulation.

ORAL RINSE COMPOSITIONS FOR ALLEVIATING XEROSTOMIA COMPRISING POLYETHYLENE GLYCOL DERIVATIVES
20230248759 · 2023-08-10 ·

An oral rinse composition for alleviating xerostomia includes a polyethylene glycol derivative as an active ingredient, which allows not only covalent bonding of the composition to the oral mucosa without irritation to increase the oral moisturizing capacity, but also allows easy manufacture, storage, use and packaging by having a granule formulation.

COMPOUNDS FOR THE PREVENTION, TREATMENT AND DIAGNOSIS OF THROMBI

The present invention relates to compounds for medical use in the treatment or in the prevention or in the diagnosis of arterial or venous thromboembolism.