158 results about "Enzyme Inhibitor Agent" patented technology

The invention provides compositions and methods for treating diseases associated with expression of BCMA. The invention also relates to a method of administering a BCMA-targeting agent which is an anti-BCMA antibody molecule or a recombinant non-antibody protein that binds to BCMA, and a gamma secretase inhibitor.

This invention discloses a compound of formula I, or a pharmaceutically acceptable salt, stereoisomer, ester, prodrug, or solvate thereof. Experimental results show that the compound provided by this invention exhibits high inhibitory activity against PAK4 kinase and PAK I / II selectivity, good liver microsomal stability, and rat PK pharmacokinetic properties, especially with low hERG cardiotoxicity risk, representing a significant improvement over prior art compounds.

This invention provides the application of CTH inhibitors and / or xCT inhibitors in the preparation of drugs for inhibiting mammalian embryo implantation, relating to the field of pharmaceutical technology. This invention verifies the efficacy of cystathionine-γ-lyase (CTH) inhibitors and / or solute carrier family 7 member 11 (xCT) inhibitors in inhibiting mammalian embryo implantation. The results show that xCT inhibitors and / or CTH inhibitors can significantly inhibit the proliferation of luteinized granulosa cells and progesterone secretion in mouse models. Furthermore, in vivo injection of xCT inhibitors and / or CTH inhibitors into mouse models not only significantly inhibits ovulation and the maturation rate of released oocytes, but also significantly reduces the formation of functional corpus luteum and embryo implantation. Therefore, this application provides new ideas and methods for the development of contraceptive drugs.

The application discloses application of a BLM helicase inhibitor in treating myocardial hypertrophy. The application firstly finds that the BLM helicase inhibitor ML216 can significantly inhibit cardiac hypertrophy and myocardial cell fibrosis, thereby providing a new drug for treating myocardial cell hypertrophy diseases in the field, and providing practical experimental evidence and scientific basis for treating myocardial cell hypertrophy diseases, and having a good application prospect in treating myocardial hypertrophy and / or cardiac hypertrophy.

The present disclosure is directed, in part, to compounds, or pharmaceutically acceptable salts thereof, for modulating the activity of Cytochrome BD oxidase, or a mutant thereof. The disclosure also provides pharmaceutically acceptable compositions comprising compounds of the present disclosure and methods of using said compositions in the treatment of various diseases and disorders related to Cytochrome BD oxidase. Formula (I) and (II).

Disclosed herein are methods for increasing sensitivity of a cancer cell to alternating electric fields by administering an AKT inhibitor, a mammalian target of rapamycin (mTOR) inhibitor, a Phosphatidylinositol 3-Kinase (PI3K) inhibitor, and / or a Glycogen synthase kinase 3β (GSK3β) inhibitor. Disclosed are methods of increasing treatment efficacy comprising applying alternating electric fields to a target site of the subject for a period of time, the alternating electric fields having a frequency and field strength, wherein the target site comprises one or more cancer cells, and administering a therapeutically effective amount of one or more of an mTOR inhibitor, AKT inhibitor, PI3K inhibitor, or GSK3β inhibitor to the subject. Disclosed are methods of reducing viability of cancer cells using alternating electric fields for a period of time, the alternating electric fields having a frequency and field strength in combination with either an mTOR inhibitor, AKT inhibitor, PI3K inhibitor, or GSK3β inhibitor and / or a composition or compound that increases cyclin D1. Disclosed are methods of increasing apoptosis of a cancer cell comprising exposing the cancer cell to alternating electric fields for a period of time, the alternating electric fields having a frequency and field strength; and exposing the cancer cell to a PI3K inhibitor.

A hypoxia inducible factor prolyl hydroxy lase inhibitor (PHD inhibitor) for use in the treatment of blood cancer.

Described herein, inter alia, are GTPase inhibitors and uses thereof.

This invention relates to compounds of formula (I) and methods of treatment using the compounds. The compounds of the invention can be used in combination with antibacterial agents to treat bacterial infections. More specifically, the compounds of formula (I) can be used in combination with a class of antibacterial agents known as carbapenems. The novel compounds of the present invention are enzyme inhibitors and more particularly are metallo-β-lactamase inhibitors.

The invention provides a special culture medium for prostate cancer organoid and a culture method thereof, and belongs to the technical field of biological medicines. The special culture medium for the prostatic cancer organoid is composed of a basic culture medium and a culture additive, and the basic culture medium does not contain exogenously added Noggin recombinant protein and R-spondin recombinant protein. The culture additive is prepared from a basic fibroblast growth factor, a keratinocyte growth factor, a fibroblast growth factor 10, insulin, a p38MAPK signal channel inhibitor, an insulin-like growth factor 1, B27, nicotinamide, N-acetylcysteine, hydrocortisone, a ROCK kinase inhibitor, retinoic acid, interleukin 6, prostaglandin E2, a eriocin and androgen. According to the special culture medium for the prostatic cancer organoid, the culture success rate is increased while the cost is reduced.

This disclosure relates to a single pharmaceutical composition comprising a therapeutically effective or prophylactically effective amount of both minoxidil, or a similar antihypertensive vasodilator, and a 5-alpha reductase inhibitor (in some embodiments, the 5-alpha reductase inhibitor is finasteride) for treating or preventing hair loss in a subject. This disclosure also relates to a pharmaceutical package comprising a pharmaceutical composition for oral administration of a therapeutically effective or prophylactically effective amount of minoxidil, or a similar antihypertensive vasodilator, and a pharmaceutical composition for oral administration comprising a therapeutically effective or prophylactically effective amount of a 5-alpha reductase inhibitor (in some embodiments, the 5-alpha reductase inhibitor is finasteride) for treating or preventing hair loss in a subject. The disclosure further provides methods of treating or preventing hair loss in a subject using the disclosed compositions and packages.

The application discloses a composition containing a peripheral vasodilator and a 5alpha-reductase inhibitor, effectively solves the transdermal inhibition of the peripheral vasodilator on the 5alpha-reductase inhibitor by adding a specific penetration enhancer, improves the transdermal rate of the active ingredients in the pharmaceutical composition by proportion adjustment, greatly improves the synergistic effect of local combined medication, avoids the side effects brought by oral 5alpha-reductase inhibitor, and improves the safety of the medicine.

The invention belongs to the field of medicinal chemistry, and relates to carbonyl fused heterocyclic derivatives used as ubiquitin-specific protease inhibitors, in particular to a compound shown in the formula (I), an isomer thereof or pharmaceutically acceptable salt thereof.

This invention relates to the synthesis of compounds that can be used to treat bacterial infections in combination with other antibacterial agents, and more specifically in combination with a class of antibacterial agents known as carbapenems. The compounds resulting from the novel methods of the present invention are enzyme inhibitors and more particularly are metallo-β-lactamase inhibitors.

Telomerase inhibitor compounds are provided. Some compounds contain a lactone or lactam group covalently bonded to a phenyl ring, which is itself bonded to a pyrazole group. In other examples, a sulfonamide-containing moiety is covalently bonded to a phenyl ring, which is itself bonded to a pyrazole group. In some embodiments, the telomerase inhibitor compounds have an amide moiety and a vinyl sulfonamide group bonded to an aromatic group. In other examples, the inhibitor compounds have an isothiazolidine 1,1-dioxide core bonded to a phenyl group. Aspects of the present invention also include pharmaceutical compositions containing the telomerase inhibitor compounds of the present invention, as well as methods for treating telomerase-related diseases or conditions.

The invention discloses a temperature-sensitive gel preparation containing a glutaminase inhibitor as well as a preparation method and application of the temperature-sensitive gel preparation, and belongs to the technical field of biological medicines. The temperature-sensitive gel preparation comprises outer-layer gel and inner-layer gel, the inner-layer gel is coated with the outer-layer gel, the outer-layer gel accounts for 40-75% of the total mass of the temperature-sensitive gel preparation, and the inner-layer gel accounts for 25-60% of the total mass of the temperature-sensitive gel preparation; the outer-layer gel is prepared from the following raw materials: an outer-layer gel matrix, a glutaminase inhibitor, a photosensitizer and a stabilizer; the raw materials of the inner-layer gel comprise an inner-layer gel matrix and an immune checkpoint inhibitor. According to the temperature-sensitive gel preparation, through photo-thermal control, the glutaminase inhibitor is firstly released to relieve the immunosuppression state, then the immune checkpoint inhibitor is released to kill tumors, and the glutaminase inhibitor and the immune checkpoint inhibitor act synergistically, so that efficient anti-tumor immunotherapy is achieved.

The present disclosure provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The provided compounds may be kinase (e.g., Janus kinase (JAK), e.g., Janus kinase 2 (JAK2)) inhibitors. Also provided are pharmaceutical compositions and kits including the provided compounds. Further provided are methods of using the provided compounds, pharmaceutical compositions, and kits (e.g., for treating a disease (e.g., proliferative disease) in a subject in need thereof).

This invention discloses the application of the plasmin inhibitor NKI10 in the preparation of drugs for preventing and treating excessive inflammatory responses, belonging to the field of biomedical technology. The amino acid sequence of the plasmin inhibitor NKI10 disclosed in this invention is shown in any one of SEQ ID NO. 1 to 10. The plasmin inhibitor NKI10 can significantly inhibit the production of IL-6, IL-1β, and TNF-α in animal and cellular inflammation models. Since the plasmin inhibitor NKI10 can inhibit excessive inflammatory responses, it can be prepared for use as a drug for preventing and treating excessive inflammatory responses.

This invention belongs to the field of pharmaceutical chemical synthesis technology, specifically a method for preparing the CSF-1R kinase inhibitor Vimseltinib (DCC-3014). The synthetic method of this invention involves the following reaction steps: 6-halo-2-methylpyridin-3-ol (1) is reacted with boric acid or a borate ester compound (5) via a Suzuki coupling reaction to obtain the key intermediate compound 2. This intermediate compound 2 is then reacted with 2,4-dihalopyridine (6) under alkaline conditions to obtain compound 3. Finally, this compound 3 is reacted with boric acid or a borate ester compound (7a-7b) to obtain the target compound Vimseltinib (DCC-3014) (4).

This invention provides the use of β-glucuronidase in the preparation of an antidote for the prevention and / or treatment of zearalenone poisoning, and an antidote for the prevention and / or treatment of zearalenone poisoning, belonging to the field of feed additives. This invention, for the first time from the perspective of in vivo exposure control in animals, proposes a method to reduce the overall ZEN exposure level by inhibiting the activity of intestinal bacterial β-glucuronidase. The technical path is clear and highly operable. This is achieved through in vivo toxicokinetic parameters (AUC, C...). max Changes in (and / or MRT) objectively reflect a reduction in ZEN exposure levels in vivo, and the technical effects are quantifiable and verifiable. The β-glucuronidase inhibitors used in this invention are widely available, particularly suitable for the field of feed additives, and have promising application prospects.

The invention provides a nucleic acid protective agent and a preparation method and application thereof, the nucleic acid protective agent comprises a nucleic acid stabilizing main reagent, an RNA enzyme inhibitor and an antioxidant, the nucleic acid stabilizing main reagent comprises maltodextrin, xylitol and hydroxypropyl-beta-cyclodextrin; the RNA enzyme inhibitor comprises cyclopentanol and tetrahydrofurfuryl alcohol; the antioxidant comprises sodium thiosulfate, sodium pyrophosphate and ascorbic acid. According to the nucleic acid protective agent provided by the invention, free nucleic acid substances including DNA and RNA can be preserved for 2 weeks under the condition of 37 DEG C, preserved for 6 months under the condition of 2-8 DEG C and preserved for 15 months under the condition of-20 DEG C, and the degradation rate is less than 10%.

The invention provides a benzylimidazole glutamine cyclase inhibitor as well as a preparation method and application thereof, and belongs to the field of medical chemistry. The compound as shown in the formula I is prepared, the compound has good inhibitory activity on glutamine cyclase, and the half inhibitory concentration of most compounds reaches the nanomole level; the compound has a wide application prospect in preparation of drugs for treating Alzheimer's disease, depression, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, tumor, synovial membrane disease, gout, acute / chronic enteritis, rheumatoid arthritis or inflammatory diseases, and lays a material basis for research and development of related drugs.

Compounds of Formula (A-I) or stereoisomers or pharmaceutically acceptable salts thereof as glutamine cyclase inhibitors, processes for their preparation, pharmaceutical compositions containing the compounds of Formula (A-I) or stereoisomers or pharmaceutically acceptable salts thereof, and the Formula (A-I) The invention relates to a use of a compound or a stereoisomer thereof or a pharmaceutically acceptable salt thereof in the prevention or treatment of QPCT and / or QPCTL mediated diseases or conditions including neurodegenerative diseases.

The invention belongs to the technical field of biological medicine, and particularly relates to an alpha-amylase inhibitory active peptide and application thereof.The alpha-amylase inhibitory active peptide is separated from free peptide of smelly mandarin fish, and the amino acid sequence of the alpha-amylase inhibitory active peptide is shown as any one of Leuu-Pro-Lys-Leu-Arg-Val-Lys-Val; val-Glu-Lys-Ser-Lys-Val-Tyr is selected from the group consisting of Glu-Lys-Ser- Glu-Val-Ile-Glu-Leu-Asp-Trp-Arg is selected from the group consisting of Glu-Val-Ile-Glu- The active peptide has good alpha-amylase inhibitory activity, and can be applied to preparation of an alpha-amylase inhibitor, a hypoglycemic drug or a drug for preventing or treating hyperglycemia-related diseases.

The application provides a kinase inhibitor leading compound, a virtual screening method thereof and application of the kinase inhibitor leading compound in preparation of branched-chain alpha-keto acid dehydrogenase kinase inhibitors and / or drugs for treating diseases mediated by branched-chain alpha-keto acid dehydrogenase kinase. The virtual screening method provided by the application combines various virtual screening platforms to screen a large-scale compound library, improves the true positive rate of screening results, reduces the number of compounds needing experimental screening, and saves screening time and cost. In addition, the compounds I-III screened out with good binding affinity to BCKDK can be used in researches on targeting BCKDK to treat major diseases such as obesity, insulin resistance, maple syrup urine disease, neurological dysfunction, liver cancer, colorectal cancer and tumor cachexia.

This invention relates to the field of pharmaceutical technology, specifically to ubiquitin-specific protease 1 inhibitor compounds, pharmaceutically acceptable salts, esters, deuterated derivatives or stereoisomers thereof, pharmaceutical compositions and formulations containing said compounds, pharmaceutically acceptable salts, esters, deuterated derivatives or stereoisomers thereof, methods for preparing said compounds, pharmaceutically acceptable salts, esters, deuterated derivatives or stereoisomers thereof, and the use of said compounds, pharmaceutically acceptable salts, esters, deuterated derivatives or stereoisomers thereof in the preparation of medicaments for the treatment and / or prevention of USP1-mediated diseases and related diseases.

The present invention relates to a urease inhibitor composition, which can be used in agricultural and pharmaceutical sectors. The composition comprises a urease inhibitor, specifically dihydrolevoglucosenone, and can include co-solvents, plant extracts, living microorganisms or extracts thereof.

The present invention concerns antibody-conjugate having general structure (2):wherein AB is an antibody capable of targeting Trop-2-expressing tumours and D is selected from the group consisting of taxanes, anthracyclines, camptothecins, epothilones, mytomycins, combretastatins, vinca alkaloids, maytansinoids, enediynes such as calicheamicins, duocarmycins, tubulysins, amatoxins, bleomycins, dolastatins and auristatins, pyrrolobenzodiazepine dimers, indolinobenzodiazepine dimers, radioisotopes, therapeutic proteins and peptides (or fragments thereof), kinase inhibitors, MEK inhibitors, KSP inhibitors, and analogues or prodrugs thereof. These antibody-conjugates exhibit an improved therapeutic index. The invention further concerns a process for preparing the antibody-conjugate according to the invention, a method for targeting Trop-2-expressing cells, medical uses of the antibody-conjugates according to the invention.