101 results about "Dipeptidyl peptidase" patented technology

Provided herein are compounds of formulae (I) - (IX), or pharmaceutically acceptable salts or deuterated forms thereof as defined herein. Also provided herein are pharmaceutical compositions comprising a compound of formula (I) - (IX) or pharmaceutically acceptable salt or deuterated form thereof, and methods of using a compound of formula (I) - (IX) or pharmaceutically acceptable salt or deuterated form thereof, e.g., in the treatment of a disease that is treatable by administration of a DPP1 inhibitor.

The invention belongs to the technical field of probiotics, and particularly relates to fermented lactobacillus mucus BM01 with an effect of relaxing bowel and application of the fermented lactobacillus mucus BM01. A new fermented lactobacillus mucus BM01 strain is separated from excrement of a healthy infant in Guangzhou city, Guangdong province, a zebra fish constipation model is constructed through loperamide hydrochloride, and research finds that the strain can remarkably promote intestinal tract movement, increase the content of in-vivo serotonin and inhibit the enzyme activity of dipeptidyl peptidase-4, so that the constipation of the zebra fish can be inhibited, the constipation of the zebra fish can be inhibited, and the constipation of the zebra fish can be inhibited. Therefore, the bowel relaxing effect is achieved. It is indicated that the BM01 strain can play the bowel relaxing effect through multiple mechanisms, has significant application value, can be used for research and development of drugs for treating constipation, irritable bowel syndrome and other intestinal diseases or development of health care products with the bowel relaxing effect, and can also be used as a feed additive to improve animal intestinal health and reduce disease risks. The culture benefit is improved.

Provided herein are compounds of formula (I), or pharmaceutically acceptable salts or deuterated forms thereof, wherein ring R1, R2, and L are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of formula (I) or pharmaceutically acceptable salt or deuterated form thereof, and methods of using a compound of formula (I) or pharmaceutically acceptable salt or deuterated form thereof, e.g., in the treatment of a disease that is treatable by administration of a DPP1 inhibitor.

The invention provides a rehmannia fermented extract, a composition as well as a preparation method and application of the rehmannia fermented extract and the composition, and belongs to the technical field of biological medicines. According to the invention, raw dark green tea and rehmannia are fermented by using a single strain of eurotium cristatum to respectively obtain a raw dark green tea fermentation extract and a rehmannia fermentation extract. Experiments prove that the two extracts have a relatively good inhibition effect on dipeptidyl peptidase-4 when being independently used; furthermore, the two extracts are combined, and animal experiments prove that the composition has relatively good inhibitory activity on intestinal tract and excrement dipeptidyl peptidase-4 and also has a hypoglycemic effect.

The invention discloses a polypeptide with DPP-IV (dipeptidyl peptidase-IV) inhibitory activity and application of the polypeptide. Pure peptides APFP and MPFP are obtained through a solid-phase synthesis method, the DPP-IV inhibition IC50 values of the pure peptides APFP and MPFP are measured to be 153.08 mu M and 296.50 mu M respectively, and the DPP-IV inhibition activity of the pure peptides APFP and MPFP is higher than that of partial fragments in the sequences of the pure peptides APFP and MPFP. The peptide fragments APFP and MPFP disclosed by the invention have relatively strong DPP-IV inhibitory activity, can be used for preparing hypoglycemic drugs or foods, and have wide application prospects in industrial application.

The invention relates to the technical field of plant extracts, and provides a plant extract composition with synergistic hypoglycemic activity and application thereof, and the plant extract composition comprises a mulberry leaf extract, a white kidney bean extract and bitter gourd powder in a mass ratio of 8: (1-24): (1-64). By optimizing the mass ratio of the mulberry leaf extract, the white kidney bean extract and the bitter gourd powder, the blood sugar reducing effect of the plant extract taking the mulberry leaf extract, the white kidney bean extract and the bitter gourd powder as main raw materials is remarkably superior to that of a plant extract in the prior art. Meanwhile, the plant extract composition also has the effects of synergistically reducing the number of neutrophils around nerves, improving peripheral neuroinflammation, synergistically enhancing the fluorescence intensity of the peripheral nerves, improving peripheral nerve injury and inhibiting the enzymatic activity of a bacterium source dipeptidyl peptidase-4.

The invention belongs to the technical field of biology, and particularly relates to animal bifidobacterium subsp. Lactis FMBL B24304AHDM and application thereof.The animal bifidobacterium subsp. Lactis FMBL B24304AHDM is preserved in the China Center for Type Culture Collection on November 18, 2024, the preservation number is CCTCC NO: M 20242505, and the animal bifidobacterium subsp. Lactis FMBL B24304AHDM has the good inhibition capacity on pathogenic bacteria and has the high scavenging capacity on DPPH and ABTS free radicals; the compound has the effect of inhibiting the activity of alpha-glucosidase, alpha-amylase and dipeptidyl peptidase IV, and the oral glucose tolerance and insulin tolerance of T2DM mice can be remarkably reduced; the composition of intestinal microbiome is obviously improved, the abundance and variety of effective microbial communities in the intestinal tract are improved, and the relative abundance of pathogenic bacteria is reduced, so that the disorder of short-chain fatty acids of T2DM mice is improved, and the application prospect is wide.

Provided herein are compounds of formulae (I)-(IX), or pharmaceutically acceptable salts or deuterated forms thereof as defined herein. Also provided herein are pharmaceutical compositions comprising a compound of formula (I)-(IX) or pharmaceutically acceptable salt or deuterated form thereof, and methods of using a compound of formula (I)-(IX) or pharmaceutically acceptable salt or deuterated form thereof, e.g., in the treatment of a disease that is treatable by administration of a DPP1 inhibitor.

Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts or deuterated forms thereof, wherein R1, R2, R3, R4, L, n, m, Ra, Rb, Rc, and Rd are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt or deuterated form thereof, and methods of using a compound of Formula (I) or pharmaceutically acceptable salt or deuterated form thereof, e.g., in the treatment of a disease that is treatable by administration of a DPP1 inhibitor.

The invention belongs to the technical field of medicines, and particularly provides a novel application of a theaflavin compound in preparation of a product for inhibiting dipeptidyl peptidase-4 (DPP-4), and the theaflavin compound is one or more of theaflavin-3-gallate (TF2A), theaflavin-3 '-digallate (TF3) and theaflavin (TF). The research systematically proves that TF2A, TF3 and TF have new application of inhibiting DPP-4 for the first time: in-vitro enzymology and fluorescence experiments show that theaflavin can inhibit DPP-4 and interact with DPP-4, and molecular docking further shows possible binding configuration and key action sites of theaflavin. In vivo, the activity of DPP-4 in serum and different tissues of high-fat diet mice can be reduced, serum glucagon-like peptide-1 (GLP-1) can be up-regulated, and glycometabolism and inflammatory phenotype can be improved. Therefore, the theaflavin compound disclosed by the invention can be applied to preparation of products for inhibiting DPP-4, and has a good development prospect.

The invention discloses a micromolecular bioluminescent probe capable of being used for monitoring in vivo / in vitro dipeptidyl peptidase IV in real time and a preparation method and application thereof.The probe is marked as DPP4-PD, during preparation, N-[t-butyloxycarbonyl] glycyl-L-proline and 6-amino-2-benzothiazole formonitrile serve as starting materials and then react with L-cysteine hydrochloric acid, and finally Boc is removed. The synthesis raw materials are easy to obtain, operation is simple, and popularization is easy. The micromolecular bioluminescence probe provided by the invention can specifically respond to DPP4 enzyme in vivo / in vitro in real time; and the probe has the remarkable advantages of high selectivity, high sensitivity, high stability, high biological safety, high signal-to-noise ratio (S / N) and the like during imaging, and has wide application prospects in the fields of pathological research, efficacy evaluation and new drug research and development.

Disclosed are a crystal of the compound (S)—N—((S)-1-cyano-2-(2-fluoro-4-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)phenyl)ethyl)-1,4-oxazacycloheptane-2-carboxamide salt or a salt thereof, a preparation method therefor, and the uses thereof in pharmaceutical compositions and in medicine.

The invention discloses a polypeptide as well as preparation and application thereof, and belongs to the technical field of active peptides. According to the present invention, three active peptides are prepared from walnut meal protein, the amino acid sequences of the three polypeptides are respectively Leuu-Pro-Gln-Phe (LPQF), Leuu-Pro-Ser-Phe (LPSF) or Vla-Pro-Phe-Pro (VPFP), and the detection results show that the three polypeptides have inhibition activity on dipeptidyl peptidase-IV (DPP-IV), such that the three polypeptides can be used for preparing the blood sugar reducing drug.

The present disclosure relates to a use of Lacticaseibacillus rhamnosus FMBL L23004 CNN in the preparation of a medicament for preventing or treating diabetes mellitus. The Lacticaseibacillus rhamnosus FMBL L23004 CNN was deposited with the China Center for Type Culture Collection (CCTCC) on 26 Jun. 2023 under the accession number CCTCC NO: M 20231099. The Lacticaseibacillus rhamnosus FMBL L23004 CNN strain has the effect of inhibiting the activity of α-glucosidase, α-amylase, and dipeptidyl peptidase IV. Administration of the strain can significantly lower oral glucose tolerance and insulin tolerance in Type 2 Diabetes Mellitus (T2DM) mice, reduce abnormal postprandial blood glucose fluctuations, decrease fasting blood glucose levels, lower fasting insulin levels, reduce blood lipid levels, and alleviate insulin resistance. The strain significantly improves the composition of the gut microbiome, increases the abundance and diversity of beneficial gut bacteria, and reduces the relative abundance of pathogenic bacteria.

This invention is applied in the field of medicine, namely in endocrinology, and can be used in the treatment of type 1 diabetes. The invention proposes a combination containing a dipeptidyl peptidase 4 (DPP-4) inhibitor, a proton pump inhibitor (PP1), and γ-aminobutyric acid or γ-aminobutyric acid receptor agonist. This unique combination and dosage of drugs leads to the regeneration (recovery) of pancreatic β-cells, which occurs with a dramatic reduction in insulin requirements up to a total cessation of insulin in some individuals and is intended for the treatment of type 1 diabetes mellitus.

Provided is a nitrile derivative compound represented by formula (I), its stereoisomers, deuterated compounds, cocrystals, solvates or pharmaceutically acceptable salts, with each group as defined in the specification. The compound has dipeptidyl peptidase 1 inhibitory activity and can be used for preparing drugs for treating diseases including airway obstructive diseases, bronchodilation, cystic fibrosis, asthma, emphysema and chronic obstructive pulmonary disease, etc.

The application belongs to the technical field of biotechnology, and particularly relates to application of albumin polypeptide gel beads in a product for treating or preventing sarcopenia. Egg white protein is used as raw material to extract protein, and albumin dipeptide-based peptidase-IV inhibitory peptide is prepared through a biological enzymolysis method. Bioinformatics analysis is used to screen out the inhibitory peptide TPYMFP, and the IC50 value of the inhibitory peptide TPYMFP for dipeptide-based peptidase-IV reaches 3.12 ± 0.49 mmol / L. Further, the optimal preparation conditions of sodium alginate SA and carboxymethyl chitosan CMCS-based gel beads CMCS / SA / TPYMFP are explored. When the SA concentration is 1.5% (w / v), the CMCS concentration is 0.5% (w / v), and the CaCl2 concentration is 1% (w / v), the polypeptide encapsulation rate is increased to 98.26% ± 0.25%. It is verified that the albumin polypeptide gel beads have good pH response characteristics, and efficient protection and intestinal target delivery of the sarcopenia inhibitory peptide are realized. The albumin polypeptide gel beads are applied to preparation of a product for treating or preventing sarcopenia, or in preparation of a related product for increasing muscle mass and strength.

Compositions comprising satiety peptides (e.g., PYY, PYY(3-36), GLP-1, oxyntomodulin, and cholecystokinin) and DPP-IV inhibitors and methods of treating metabolic diseases with such compositions are provided.

The invention discloses hypoglycemic peptide sheep milk powder and a preparation method thereof, and belongs to the technical field of enzyme engineering. According to the preparation method, sheep milk is taken as a raw material, the inhibition rates of different proteases on dipeptidyl peptidase IV (DPP-IV) are compared after the sheep milk is subjected to enzymolysis by different proteases, the optimal compound protease is obtained, then the hypoglycemic peptide sheep milk is obtained through hydrolysis of the compound protease, the hypoglycemic peptide sheep milk has DPP-IV inhibition activity, and the sheep milk powder with the hypoglycemic activity is further obtained through spray drying. The DPP-IV inhibition rate is 69.44% + / -2.66%-87.45% + / -1.25%, and the compound can be used for assisting in reducing blood sugar of consumers and reducing the dosage of hypoglycemic peptides so as to reduce side effects. The hypoglycemic peptides in the enzymolysis sheep milk are separated, purified and identified through ultrafiltration, preparative chromatography and HPLC-MS / MS, 12 hypoglycemic peptides from sheep milk protein are obtained, and theoretical and technical supports are provided for development of hypoglycemic assisting dairy products.

The invention relates to the field of protein, in particular to a milk-derived peptide APPSPIGVF with antihypertensive activity as well as a preparation method and application of the milk-derived peptide APPSPIGVF, and the amino acid sequence of the milk-derived peptide APPSPIGVF is Ala-Pro-Pro-Ser-Pro-Ile-Gly-Val-Phe. An angiotensin converting enzyme activity inhibition experiment, an alpha-amylase activity inhibition experiment and a dipeptidyl peptidase-4 activity inhibition experiment prove that the milk-derived peptide APPSPIGVF has very good functions of resisting hypertension and reducing blood sugar. The milk-derived peptide APPSPIGVF disclosed by the invention has an anti-hypertension capability, and can be used for remarkably inhibiting the activity of alpha-amylase and dipeptidyl peptidase-4, improving the capability of resisting chronic diseases such as hypertension and hyperglycemia of an organism, reducing the morbidity of the organism and improving the quality of life; the method has very important significance for developing food, health care products and medicines with the functions of resisting hypertension and reducing blood sugar.

The present invention relates to the dipeptidyl-peptidase I (DPPI or Cathepsin C) inhibitor of formula (I), which is useful in the prevention and / or treatment of bronchiectasis with certain underlying aetiologies, in the prevention and / or treatment of anti-neutrophil cytoplasmic antibody-associated vasculitis or hidradenitis suppurativa using therapeutically efficacious dosages and to polymorphs of Compound (I) as well as to pharmaceutical compositions comprising Compound (I) and its polymorphs.

This invention provides a fermented extract of Rehmannia glutinosa, a composition thereof, its preparation method, and its application, belonging to the field of biomedical technology. This invention obtains fermented extracts of black tea and Rehmannia glutinosa by fermenting black tea and Rehmannia glutinosa with a single strain of *Aspergillus cristatus*. Experiments have verified that both extracts, used alone, have good inhibitory effects on dipeptidyl peptidase-4. Further, combining the two extracts and verifying through animal experiments, shows that they have good inhibitory activity against dipeptidyl peptidase-4 in the intestine and feces, while also exhibiting a hypoglycemic effect.

Disclosed are a crystal of the compound (S)-N-((S)-1-cyano-2-(2-fluoro-4-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)phenyl)ethyl)-1,4-oxazacycloheptane-2-carboxamide salt or a salt thereof, a preparation method therefor, and the uses thereof in pharmaceutical compositions and in medicine.

The invention relates to the technical field of biological medicines, in particular to application of dipeptidyl peptidase 3 (DPP3) as a treatment target of septicopyemia-induced myocardial injury. The invention discloses a key action mechanism of dipeptidyl peptidase 3 (DPP3) in septicopyemia induced myocardial injury, and provides a novel septicopyemia cardiomyopathy intervention strategy taking DPP3 as a target spot based on the key action mechanism. A theoretical basis and an experimental basis are provided for developing early diagnosis tools and targeted therapy drugs for septicopyemia-induced cardiomyopathy, and remarkable clinical application value and significance are achieved.

Disclosed is a nitrile derivative compound represented by formula (I), a stereoisomer, a deuterated product, a co-crystal, a solvate or a pharmaceutically acceptable salt thereof, wherein each group is as defined in the description. The compound has dipeptidyl peptidase 1 inhibitory activity and can be used to prepare a drug for treating diseases including obstructive airway diseases, bronchiectasis, cystic fibrosis, asthma, emphysema, and chronic obstructive pulmonary diseases.

The invention relates to new compounds of the general Formula (I), which are Dipeptidyl peptidase 9 (DPP9) enzyme inhibitors. The present invention further relates to specific compounds based on Formula (I) that binds to an E3 ligase and to DPP9 and induce proteolysis of DPP9. The invention also relates to specific DPP9 binding compounds comprising a probe moiety, according to formula (I). The present invention further relates to pharmaceutical compositions and their use thereof.

The present disclosure relates to certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof),that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and / or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

To find out a novel component having dipeptidyl peptidase-IV inhibitory activity, and provide a dipeptidyl peptidase-IV inhibitor, a hyperglycemia inhibitor and an anti-diabetic agent.SOLUTION: Tetrapeptide Ile-Pro-Ala-Gly and tripeptide Val-Ala-Tyr included in hydrolysate of almond-derived protein has dipeptidyl peptidase-IV inhibitory activity, and can be used as a dipeptidyl peptidase-IV inhibitor, a hyperglycemia inhibitor and an anti-diabetic agent.SELECTED DRAWING: None

The present invention relates to a novel adamantyl derivative or a pharmaceutically acceptable salt thereof, and a use thereof. The adamantyl derivative may be a dipeptidyl peptidase-4 (DPP4) inhibito

The present invention is directed to a compound of structural formula I as inhibitor of the dipeptidyl peptidase-IV enzyme and which is useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising the compound and their use in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.