Abstract

The present invention relates to a compound simultaneously having triple activities of thrombolysis, antithrombosis and free radical scavenging, as well as the preparation method, composition, and applications thereof. The compound is represented by the formula I shown below: The present invention relates to a compound simultaneously having triple activities of thrombolysis, antithrombosis and free radical scavenging, as well as the preparation method, composition, and applications thereof. The compound is represented by the formula I shown below: The present invention relates to a compound simultaneously having triple activities of thrombolysis, antithrombosis and free radical scavenging, as well as the preparation method, composition, and applications thereof. The compound is represented by the formula I shown below: wherein the definitions of T, Q, R1 and R2 are described herein. The compound of the present invention simultaneously has triple functions of thrombolysis, free radical scavenging and thrombus-targeting/antithrombosis. The present invention also relates to a pharmaceutical composition comprising the compound, and a preparation method and a nanostructure of the compound.

IPC Classes  ?

• C07K 5/097 - Tripeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp, e.g. thyroliberin, melanostatin
• C07D 217/00 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
• C07K 5/02 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof containing at least one abnormal peptide link
• C07K 5/11 - Tetrapeptides the side chain of the first amino acid containing more amino groups than carboxyl groups, or derivatives thereof, e.g. Lys, Arg
• C07K 5/078 - Dipeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp
• A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
• A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds

Abstract

The present invention relates to injectable, extended-release, pharmaceutical formulations comprising a nalbuphine ester prodrug homogenously dissolved in a solution comprising a pharmaceutically acceptable oil and an oil-miscible retaining solvent, as well as manufacturing processes and medical uses of the formulations. The invention further provides methods for adjusting the duration of action of the formulations by varying the ratio of the pharmaceutically acceptable oil and the oil-miscible retaining solvent.

IPC Classes  ?

• A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
• A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 9/00 - Medicinal preparations characterised by special physical form

Abstract

Disclosed herein are topical pharmaceutical compositions of Sebacoyl Dinalbuphine Ester (SDE) and methods of using such compositions for treating pruritus, pain, and inflammatory conditions.

IPC Classes  ?

• A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin

Abstract

Disclosed are fusion proteins, methods of making fusion proteins, and methods of using fusion proteins, wherein the fusion proteins comprise a functional single-domain antibody (sdAb) or a functional variant thereof and a cytosine deaminase (CD) protein or a functional variant thereof, optionally connected via a peptide linker. The fusion proteins of the disclosure also have CD activity. Also disclosed are pharmaceutical compositions or formulations comprising such fusion proteins and pharmaceutically acceptable excipients, as well as medical uses of these fusion proteins.

IPC Classes  ?

• C07K 14/725 - T-cell receptors
• A61P 35/00 - Antineoplastic agents
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
• C12N 9/78 - Hydrolases (3.) acting on carbon to nitrogen bonds other than peptide bonds (3.5)

Abstract

Disclosed are fusion proteins, methods of making fusion proteins, and methods of using fusion proteins, wherein the fusion proteins comprise a functional single-domain antibody (sdAb) or a functional variant thereof and a cytosine deaminase (CD) protein or a functional variant thereof, optionally connected via a peptide linker. The fusion proteins of the disclosure also have CD activity. Also disclosed are pharmaceutical compositions or formulations comprising such fusion proteins and pharmaceutically acceptable excipients, as well as medical uses of these fusion proteins.

IPC Classes  ?

• C07K 14/725 - T-cell receptors
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
• C12N 9/78 - Hydrolases (3.) acting on carbon to nitrogen bonds other than peptide bonds (3.5)
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to injectable, extended-release, pharmaceutical formulations comprising a nalbuphine ester prodrug homogenously dissolved in a solution comprising a pharmaceutically acceptable oil and an oil-miscible retaining solvent, as well as manufacturing processes and medical uses of the formulations. The invention further provides methods for adjusting the duration of action of the formulations by varying the ratio of the pharmaceutically acceptable oil and the oil-miscible retaining solvent.

IPC Classes  ?

• A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
• A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 9/00 - Medicinal preparations characterised by special physical form

Abstract

The present invention discloses a novel compound with effects of thrombolysis, free radical scavenging and thrombus-targeting, as well as a preparation method and use thereof. The compound is a ternary conjugate formed by conjugating a thrombolytic peptide, a free radical scavenger and a thrombus-targeting/antithrombotic peptide together via a linking arm. The present invention also discloses a pharmaceutical composition containing the compounds, wherein the compounds form a nanospherical structure.

IPC Classes  ?

• A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
• C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
• C07K 5/09 - Tripeptides the side chain of the first amino acid containing more amino groups than carboxyl groups, or derivatives thereof, e.g. Lys, Arg
• C07K 5/083 - Tripeptides the side chain of the first amino acid being acyclic, e.g. Gly, Ala
• A61K 38/06 - Tripeptides
• A61K 38/07 - Tetrapeptides
• A61K 47/69 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
• A61K 38/00 - Medicinal preparations containing peptides
• C07K 5/097 - Tripeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp, e.g. thyroliberin, melanostatin
• A61K 31/4164 - 1,3-Diazoles
• A61K 38/08 - Peptides having 5 to 11 amino acids
• A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound

Abstract

The present invention relates to a compound simultaneously having triple activities of thrombolysis, antithrombosis and free radical scavenging, as well as the preparation method, composition, and applications thereof. The compound is represented by the formula I shown below: 2 are described herein. The compound of the present invention simultaneously has triple functions of thrombolysis, free radical scavenging and thrombus-targeting/antithrombosis. The present invention also relates to a pharmaceutical composition comprising the compound, and a preparation method and a nanostructure of the compound.

IPC Classes  ?

• A61K 38/06 - Tripeptides
• A61K 38/07 - Tetrapeptides
• C07D 217/00 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
• C07K 5/097 - Tripeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp, e.g. thyroliberin, melanostatin
• C07K 5/02 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof containing at least one abnormal peptide link
• C07K 5/11 - Tetrapeptides the side chain of the first amino acid containing more amino groups than carboxyl groups, or derivatives thereof, e.g. Lys, Arg
• C07K 5/078 - Dipeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp
• A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
• A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
• A61K 38/00 - Medicinal preparations containing peptides

Abstract

The present invention relates to injectable, extended-release, pharmaceutical formulations comprising a nalbuphine ester prodrug homogenously dissolved in a solution comprising a pharmaceutically acceptable oil and an oil-miscible retaining solvent, as well as manufacturing processes and medical uses of the formulations. The invention further provides methods for adjusting the duration of action of the formulations by varying the ratio of the pharmaceutically acceptable oil and the oil-miscible retaining solvent.

IPC Classes  ?

• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
• A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters

Abstract

The present invention relates to injectable, extended-release, pharmaceutical formulations comprising a nalbuphine ester prodrug homogenously dissolved in a solution comprising a pharmaceutically acceptable oil and an oil-miscible retaining solvent, as well as manufacturing processes and medical uses of the formulations. The invention further provides methods for adjusting the duration of action of the formulations by varying the ratio of the pharmaceutically acceptable oil and the oil-miscible retaining solvent.

IPC Classes  ?

• A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
• A61K 9/08 - Solutions
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
• A61P 25/04 - Centrally acting analgesics, e.g. opioids

Abstract

The present invention relates to injectable, extended-release, pharmaceutical formulations comprising a nalbuphine ester prodrug homogenously dissolved in a solution comprising a pharmaceutically acceptable oil and an oil-miscible retaining solvent, as well as manufacturing processes and medical uses of the formulations. The invention further provides methods for adjusting the duration of action of the formulations by varying the ratio of the pharmaceutically acceptable oil and the oil-miscible retaining solvent.

IPC Classes  ?

• A61K 31/485 - Morphinan derivatives, e.g. morphine, codeine
• A61K 9/08 - Solutions
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
• A61P 25/04 - Centrally acting analgesics, e.g. opioids

Abstract

The present invention relates to a compound simultaneously having triple activities of thrombolysis, antithrombosis and free radical scavenging, as well as the preparation method, composition, and applications thereof. The compound is represented by the formula I shown below: 2 are described herein. The compound of the present invention simultaneously has triple functions of thrombolysis, free radical scavenging and thrombus-targeting/antithrombosis. The present invention also relates to a pharmaceutical composition comprising the compound, and a preparation method and a nanostructure of the compound.

IPC Classes  ?

• A61K 38/06 - Tripeptides
• A61K 38/07 - Tetrapeptides
• C07D 217/00 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
• C07K 5/097 - Tripeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp, e.g. thyroliberin, melanostatin
• C07K 5/02 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof containing at least one abnormal peptide link
• C07K 5/11 - Tetrapeptides the side chain of the first amino acid containing more amino groups than carboxyl groups, or derivatives thereof, e.g. Lys, Arg
• C07K 5/078 - Dipeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp
• A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
• A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
• A61K 38/00 - Medicinal preparations containing peptides

Abstract

Provided in the present invention are new compounds having the triple activities of thrombolysis, antithrombotic and radical scavenging as represented by general formula (I), wherein T is a connecting arm having at least two groups for connection use, Q is a peptide having a thrombolysis activity, and R1 and R2 are C1-4alkyl, wherein R1 and R2 can be the same or different. Also provided in the present invention are the preparation method and use of the compound, and a pharmaceutical composition containing the compounds.

IPC Classes  ?

• C07K 5/117 - Tetrapeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp
• A61K 38/07 - Tetrapeptides
• A61P 7/02 - Antithrombotic agentsAnticoagulantsPlatelet aggregation inhibitors
• A61P 39/06 - Free radical scavengers or antioxidants

Abstract

The present invention relates to a compound simultaneously having triple activities of thrombolysis, antithrombosis and free radical scavenging, as well as the preparation method, composition, and applications thereof. The compound is represented by the formula l shown below: wherein the definitions of T, Q, Ri and R2 are described herein.The compound of the present invention simultaneously has triple functions of thrombolysis, free radical scavenging and thrombus-targeting/antithrombosis. The present invention also relates to a pharmaceutical composition comprising the compound, and a preparation method and a nanostrutucre of the compound.

IPC Classes  ?

• C07K 5/117 - Tetrapeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp
• A61K 38/07 - Tetrapeptides
• A61P 7/02 - Antithrombotic agentsAnticoagulantsPlatelet aggregation inhibitors
• A61P 39/06 - Free radical scavengers or antioxidants

Abstract

Disclosed are a novel compound with effects of thrombolysis, free radical scavenging and thrombus-targeting as well as a preparation method and a use thereof. The compound is a ternary conjugate formed by combining a thrombolytic peptide, a free radical scavenger with a thrombus-targeted/antithrombotic peptide together via a linking arm. Also disclosed is a pharmaceutical composition containing the compound, the compound being formed with a nanometer spherical structure.

IPC Classes  ?

• C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
• C07K 1/06 - General processes for the preparation of peptides using protecting groups or activating agents
• A61K 38/08 - Peptides having 5 to 11 amino acids
• A61P 7/02 - Antithrombotic agentsAnticoagulantsPlatelet aggregation inhibitors
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 39/06 - Free radical scavengers or antioxidants