Patents
Literature
Hiro is an intelligent assistant for R&D personnel, combined with Patent DNA, to facilitate innovative research.
Hiro

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

Therapeutic Agents Targeting the NCCA-ATP Channel and Methods of Use Thereof

The present invention is directed to therapeutic compositions targeting the NCCa-ATP channel of an astrocyte, neuron or capillary endothelial cell and methods of using same. More specifically, agonists and antagonists of the NCCa-ATP channel are contemplated. The therapeutic compositions are used to treat cancer, more specifically, a metastatic brain tumor, wherein a tumor-brain barrier is present. Such treatments are contemplated in combination with conventional anti-cancer therapies. Alternatively, the compositions are used to prevent cell death and to treat cerebral edema that result from ischemia, due to interruption of blood flow, to tissue trauma or to increased tissue pressure.
Owner:U S GOVERNMENT REPRESENTED BY THE DEPT OF VETERANS AFFAIRS

Pharmaceutical compositions containing a glycopeptide antibiotic and a cyclodextrin

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.
Owner:CUMBERLAND PHARM INC

Antibody drug conjugate and application thereof

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.
Owner:MABPLEX INT LTD

Stable polypeptide inhibitor targeting HDAC and application of stable polypeptide inhibitor

ActiveCN109912686AImprove enzyme activity inhibitory effectGood tumor suppressor effectPeptide/protein ingredientsPeptidesHigh dosesCell cycle
The invention provides a stable polypeptide inhibitor for targeting HDAC. The amino acid sequence structure of the stable polypeptide inhibitor is shown in specification. The invention also provides application of the stable polypeptide inhibitor targeting HDAC in preparation of a drug for inhibiting the enzymatic activity of HDAC family. The invention also provides application of the stable polypeptide inhibitor targeting HDAC in preparation of a drug for inhibiting tumor stem cells with high expression of HDAC1. The invention further provides application of the stable polypeptide inhibitor targeting HDAC in preparation of a drug for treating human ovarian teratoma or testicular embryonic carcinoma. Experiments of cell proliferation, apoptosis and cell cycle arrest prove that the polypeptide can effectively inhibit proliferation of the tumor stem cells, and the polypeptide has no obvious tissue damage or toxicity to mice at a high dose.
Owner:PEKING UNIV SHENZHEN GRADUATE SCHOOL

Combinations of anti-pd-l1 antibody and mek inhibitor and/or braf inhibitor

A novel combination comprising the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro- 4-iodo-phenylamino)6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3- d]pyrimidin-1 -yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, and / or a B-Raf inhibitor, particularly N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1 - dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, and an anti-PD-L1 antibody; pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and / or B-Raf and / or neutralizing or inhibiting the interaction between PD-L1 and its receptor, e.g. PD-1, is beneficial, eg. cancer.
Owner:NOVARTIS AG

Drug conjugate with multiple targeting ligands having cell endocytosis mediating function

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.
Owner:COHERENT BIOPHARMA (SUZHOU) LTD

Sulfonium salt-based stable HDAC-targeting polypeptide drug conjugate and application thereof

The invention relates to a sulfonium salt stable targeting HDAC polypeptide drug conjugate and application thereof, a sulfonium salt stable apoptosis-promoting polypeptide is coupled with an HDAC inhibitor to form a stable polypeptide HDAC inhibitor with tumor selective toxicity, the nonspecific toxicity of apoptosis polypeptide chemically stabilized by sulfonium salt is remarkably reduced, the stability of protease is higher, and the tumor selective toxicity of the apoptosis polypeptide is remarkably reduced. When a polypeptide drug conjugate is formed by coupling with an HDAC inhibitor, the polypeptide drug can significantly improve the selective toxicity to tumor cells, and has weak toxicity to normal cells. Cell proliferation, cell apoptosis and cell cycle arrest experiments prove that the polypeptide can effectively inhibit proliferation of malignant liver cancer, has relatively good biological safety and has a potential anti-tumor clinical application prospect.
Owner:XIEHE HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI & TECH UNIV

Aconitine injection for intrathecal injection and preparation method thereof

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.
Owner:云南扬软生物科技有限公司

Method for developing intelligent cancer drug

The invention discloses a method for developing an intelligent cancer drug, which belongs to the field of biomedicine and is a method for developing the intelligent cancer drug. According to the scheme, the drug is specifically activated in tumor tissues through design modification, so that systemic toxic diseases of the drug are reduced to widen the treatment window of the drug; tissue specificity is utilized to improve the targeting property of the drug, so that the induced differentiation capability of differentiated drugs on tumor cells is improved, or the toxicity of anticancer drugs on cancer cells is improved; and a liposome is taken as a drug carrier, so that the drug has the advantages of maintaining the drug activity, enhancing the drug solubility, reducing the effect on normal tissues and the like. The technology can be applicable to auxiliary targeted treatment of multiple cancers, and has a wide application prospect.
Owner:上海英南智能技术发展有限公司

Targeting ligand-drug conjugate having cell endocytosis mediating function

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.
Owner:COHERENT BIOPHARMA (SUZHOU) LTD

Application of compound omeprazole in preparation of information treatment drug, preparation method of compound omeprazole, and prepared novel drug

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.
Owner:北京中卫神农慢性病医学研究院有限公司

Azide modified proteins

ActiveUS20110064667A1Modify structural/functional propertyEasy to controlBiocideTissue cultureThiolVesicle/vacuole
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.
Owner:KONINKLIJKE PHILIPS ELECTRONICS NV

Bispecific anti pd1-anti tim3 antibodies

The disclosure provides means and methods for interfering with Programmed Cell Death 1 protein (PD-1) and T-cell immunoglobulin and mucin-domain containing-3 (TIM-3) mediated inhibition in a PD-1 and / or TIM-3 positive cell. A method may comprise contacting said cell with an antibody or a functional part, derivative and / or analogue thereof that comprises a variable domain that can bind to an extracellular part of PD-1 and a variable domain that can bind to an extracellular part of TIM-3, thereby inhibiting PD-1 and / or TIM-3 mediated activity in said cell. The invention also provides antibodies or variants thereof that comprises a variable domain that can bind to an extracellular part of PD-1 and a variable domain that can bind to an extracellular part of TIM-3.
Owner:MERUS NV

Antibody protac conjugates

An immunoconjugate having the Formula Ab-[L1-(A-L2-B)m]n, wherein: (a) Ab is an antibody or a binding fragment thereof; (b) L1 and L2 are each independently a linker, wherein L1 and L2 are the same ordifferent and wherein L1 links to L2; (c) A is a target-protein ligand / binder; (d) B is a ubiquitin ligase ligand / binder, and (e) n and m are independently integers from 1 to 8. The target protein includes kinase, G protein-coupled receptors, transcription factor, phosphatases, and RAS superfamily members.
Owner:DEV CENT FOR BIOTECHNOLOGY

Application of glibenclamide compound in preparation of information therapy medicament, method for preparing information therapy medicament, and novel drug prepared with method

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.
Owner:北京中卫神农慢性病医学研究院有限公司

Nanoparticle with effect-enhancing and toxicity-reducing effect on synergistic and attenuating effects on annonaceous acetogenins drugs, and preparation method and application thereof

ActiveCN109223769AImprove the anti-tumor effect in vivoBreak through narrow bottleneck problemsOrganic active ingredientsPharmaceutical non-active ingredientsAdjuvantNanoparticle
The invention provides a nanoparticle with effect-enhancing and toxicity-reducing effect on synergistic and attenuating effects on annonaceous acetogenins drugs, and belongs to the field of pharmaceutical preparations. The present invention uses poloxamer P188, Poloxamer P407, Poloxamer P124, one or more of poloxamer P237 and poloxamer P338 are adjuvants, By limiting the kinds and dosage of excipients, the problems of insoluble and difficult administration of annonolactone are solved, and more importantly, the anti-tumor effect in vivo is improved, at the same time, it has better safety, breaks through the bottleneck problem of narrow window of treatment of annonolactone, and provides a feasible solution for clinical application.
Owner:INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI

Application of desloratadine compound in preparing information medicine, preparation method and prepared novel drug

The invention discloses application of a desloratadine compound in preparing an information medicine, a preparation method of the information medicine by the desloratadine compound and a novel drug prepared by the preparation method. During the treatment, the information medicine does not directly touch a human body, drug substance components are not consumed, chemotherapy effects can be achieved only by utilizing drug information physiotherapy, and the therapy window is enlarged by more than one thousand times, and side effects of the chemotherapy are avoided. After desloratadine is used as the information treatment drug, the effective component content is not changed, and desloratadine can be used secondarily and effectively as a chemotherapy normal preparation.
Owner:北京中卫神农慢性病医学研究院有限公司

Application of allopurinol compound in preparing information treatment drug, preparation method and prepared novel drug

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.
Owner:北京中卫神农慢性病医学研究院有限公司

Application and preparation method of ambroxol hydrochloride in preparation of information therapeutic drug and novel drug prepared by preparation method

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.
Owner:北京中卫神农慢性病医学研究院有限公司

Application of composition Xiaoke pills in preparation of information intervention agent, preparation method of information intervention body and product

The invention relates to application of composition Xiaoke pills to preparation of an information intervention agent, a preparation method of an information intervention body and a product . The composition Xiaoke pills achieve an intervention effect by performing the reaction on Xiaoke pill information and a human body information receptor and adopting a Xiaoke pill information physical method without being used as a plant chemical treatment medicament. Therefore, after the Xiaoke pills are used as the information intervention body, the Xiaoke pill material is not consumed for the information intervention, so that the quality of the Xiaoke pills is not influenced and the Xiaoke pills also can be effectively reused as a plant chemical treatment conventional preparation.
Owner:北京中卫神农慢性病医学研究院有限公司

Application and preparation method of compound madopar to preparation of information therapeutic medicine and novel medicine prepared from compound madopar

The invention discloses an application and a preparation method of a compound madopar to preparation of an information therapeutic medicine and a novel medicine prepared from the compound madopar. The information therapeutic medicine is indirect with a human body during therapy, so that material components of the information therapeutic medicine cannot be consumed, a chemical treatment effect can be achieved by only using medicine information physical therapy; and a therapy window of the information therapeutic medicine is enlarged by above thousands, and thus side effects of chemical therapy are avoided. After the madopar is used as the information therapeutic medicine, contents of effective components are not changed, and the information therapeutic medicine can be used as a chemical therapeutic conventional preparation to be secondarily and effectively used.
Owner:北京中卫神农慢性病医学研究院有限公司

Prodrug compound of dithiocarbamic acid metal complex as well as preparation method and application of prodrug compound

The invention discloses a prodrug compound of a dithiocarbamic acid metal complex as well as a preparation method and application of the prodrug compound. According to the prodrug compound disclosed by the invention, dithiocarbamic acid and metal ions can be carried in a single small molecule at the same time, and the dithiocarbamic acid and the metal ions are kept in an inert state; under specific conditions, the dithiocarbamic acid prototype is triggered and released, the metal chelating function of the dithiocarbamic acid prototype is recovered, and the dithiocarbamic acid prototype and metal ions carried in molecules are subjected to intramolecular metal coordination reaction to form the dithiocarbamic acid metal complex with biological activity. The prodrug compound disclosed by the invention can realize selective in-situ activation of a metal complex, and has a good application prospect in tumor prevention and treatment and diseases related to abnormal metal ion metabolism; meanwhile, a feasible thought and a feasible method are provided for the prodrug design of the metal coordination type drug.
Owner:SUN YAT SEN UNIV +1
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products