44results about How to "Expanding Therapeutic Window" patented technology

Disclosed are pharmaceutical compositions containing a cyclodextrin and a therapeutically effective amount of a glycopeptide antibiotic or a salt thereof. Also disclosed are methods of treating a bacterial disease in a mammal by administering such pharmaceutical compositions.

According to the invention, one or more cysteine residues or cysteine derivative residues are used as a drug connection carrier; one or more drugs are coupled to limited connecting sites of the antibody at the same time, so that drugs with higher drug loading capacity are prepared or drugs with lower toxicity can be selected to prepare ADC products, and ADC products with larger treatment windows are obtained. Furthermore, since a plurality of drug molecules can be coupled at one connection site, the ADC product obtained by the method provided by the invention has better uniformity under the condition of preparing antibody drug conjugates with the same DAR value. The use amount of the antibody required in production can be greatly reduced, so that the production cost is effectively reduced.Compared with the antibody drug conjugate of which the same site can only be connected with one drug molecule, the antibody drug conjugate prepared by adopting the method disclosed by the invention still has the same inhibiting or killing effect on tumor cells under the condition that the total amount of the coupled drug molecules is greatly reduced.

The invention discloses a drug conjugate with multiple targeting ligands having a cell endocytosis mediating function. The drug conjugate consists of drug molecules and connexons coupled with the drug molecules; the drug conjugate at least comprises two or more ligands which can be specifically bound to cell surface receptors; the ligands at least include one first ligand which has the cell endocytosis mediating function; and at least one of the ligands and the first ligand are coupled and then are selectively coupled with the drug molecules or the connexons so as to form the drug couplet. The drug conjugate provided by the invention has the beneficial effects that by combining targeting and endocytosis structures, polypeptide, which is targeted by any ligands, is taken as a guiding part, so that the targeting scope of the like medicines is widened. The affinity and the targeting performance of the drug conjugate on diseased cells can be enhanced by virtue of the multiple targeting ligands, so that efficient toxin drugs such as MMAE can be carried, efficacy can be enhanced, a therapeutic window can be widened and side effects of the medicines can be avoided.

The invention discloses an aconitine injection for intrathecal injection and a preparation method thereof. Aconitine refers to a compound with a structural feature in the formula shown in the description, wherein R1-R18 represent H or OH or X or OX, the X comprises Me, Ac, Bzl, a para methoxyphenyl formyl group and an o-acetamido benzoyl group, but not limited to the groups. The dosage of the aconitine injection ranges from 0.02 mg to 20 mg per bottle, and the aconitine injection is used for treating pain; the preparation forms comprise the injection, a freeze-dried powder injection, a prefilled injection and the like which are delivered through injection; the dosage is decreased to about one-tenth of original dosage, the toxic and side effects are greatly reduced, and the safety window and the therapeutic index are increased, processing of an aconitine preparation is completed through a low-temperature technology at the temperature lower than 50 DEG C, impurities produced through high-temperature hydrolysis of the aconitine are avoided, and therefore qualified products can be produced in a batched mode.

The present invention discloses a targeting ligand-drug conjugate having a cell endocytosis mediating function. The targeting ligand-drug conjugate comprises a drug molecule and a linker coupled to the drug molecule, and is characterized by further comprising a molecule having a mediating effect and a ligand specifically bound to a cell surface receptor, wherein the ligand is a polypeptide or small molecule ligand, and the molecule can be coupled to the ligand, can be coupled to the drug molecule or linker to form the drug conjugate, or is respectively and separately coupled to one of the drug molecule and the linker to form the drug conjugate. According to the present invention, with the combination of the targeting and the endocytosis (transmembrane) structure, the any ligand targeting polypeptide can be adopted as the leader so as to broaden the targeting range of the drug; and with the conjugate, the stability of the drug during the in vivo circulation is ensured, and the drug toxicity is reduced.

The invention discloses an application of compound omeprazole in the preparation of information treatment drug, a preparation method of the compound omeprazole, and a prepared novel drug. The information treatment drug is characterized in that the drug is not contacted with a human body directly in the treatment, the substance ingredient of the drug cannot be consumed, only the drug information is used for physical treatment, and the chemical treatment effect can be achieved, a treatment window is enlarged by more than 1000 times, and the side effects of the chemical treatment are avoided. After the omeprazole is used as the information treatment drug, the contents of active ingredients are not changed, and the omeprazole can be used as the conventional preparation of the chemical treatment for secondary effective use.

The present invention describes the modification of polypeptides, more particularly channel proteins with a thiol reactive agent so as to introduce an azide group. The present invention further describes vesicles comprising channel proteins modified according to the invention, which upon reaction with a phosphine open up thereby releasing the content of the vesicles. The reagents, polypeptides and vesicles described in the present invention have in vivo and in vitro applications in both drug delivery and imaging.

The invention discloses an application of a glibenclamide compound in preparation of an information therapy medicament, a method for preparing the information therapy medicament, and a novel drug prepared with the method. The information therapy medicament is not in direct contact with a human body during treatment, the components of the medicament is not consumed, only medicament information is utilized for physical therapy, so that the chemical treatment effect can be achieved, the therapeutic window is enlarged by more than a thousand times, and the side effect of chemical treatment is avoided. After the glibenclamide is used as the information therapy medicament, the content of effective components of the glibenclamide is not changed, so that the glibenclamide can be used as a conventional preparation in chemical treatment for secondary effective use.

Multi-specific binding proteins that bind a tumor associated antigen, the NKG2D receptor, and CD 16 are described, as well as pharmaceutical compositions and therapeutic methods useful for the treatment of cancer.

The invention discloses application of an allopurinol compound in preparing an information treatment drug, a preparation method of the allopurinol compound and a novel drug prepared by the preparation method. During the treatment, the information treatment drug does not directly touch a human body, drug substance components are not consumed, chemotherapy effects can be achieved only by drug information physiotherapy, and the therapy window is enlarged more than one thousand times, and side effects of the chemotherapy are avoided. After allopurinol is used as the information treatment drug, the effective component content is not changed, and allopurinol can be used secondarily and effectively as a chemotherapy normal preparation.

The invention discloses application of ambroxol hydrochloride in the preparation of an information therapeutic drug, a preparation method of the ambroxol hydrochloride and a novel drug prepared by the preparation method. The information treatment drug is characterized in that the drug does not contact a human body directly in the treatment, any substance ingredient of the drug can not be consumed, only the drug information is utilized for physical treatment, but the chemical treatment effect can be achieved, a treatment window is enlarged by more than 1000 times, and the side effects of the chemical treatment are avoided. After the ambroxol hydrochloride is used as the information treatment drug, the contents of active ingredients are not changed, and the ambroxol hydrochloride can be used as the conventional preparation in the chemical treatment for secondary effective use.