110 results about "Prolyl Hydroxylases" patented technology

The invention described herein relates to certain bicyclic heteroaromatic N-substituted glycine derivatives of formula (I)which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

The invention described herein relates to certain bicyclic heteroaromatic N-substituted glycine derivatives of formula (I)which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

The invention described herein relates to certain pyrimidinedione N-substituted glycine derivatives of formula (I)which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

The crystal structure of ligand-bound EGLN1 catalytic domain of prolyl hydroxylase is disclosed. These coordinates are useful in computer aided drug design for identifying compounds that regulate EGLN1 prolyl hydroxylase and thereby regulate HIF-regulated disorders.

The present invention relates to substituted 4-hydroxypyrimidine-5-carboxamides useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.

The invention relates to an oral nutrition composition for beautifying skin, which contains collagen, hyaluronicacid and vitamin C, wherein the collagen is active small molecule peptide with the molecular weight of 2000-6000Dalton, the hyaluronicacid is sodium salt, zinc salt and kali salt, and the vitamin C is natural or synthesized. The invention overcomes the defects that the collagen can not be absorbed by a human body or hydrolyzed into amino acid because the molecular weight is too big, and most of the collagen loses the beautifying efficacy and the like. Hydroxyproline in collagen peptide is promoted to generate by using the vitamin C through active prolyl hydroxylases, the collagen forms big molecule collagen required by beautifying the skin by crosslinked with the hydroxyproline, the hyaluronicacid is also a better nutrient absorption promoting agent except for special water-holding function and is matched with the vitamin C and the collagen for use, which can achieve more ideal effect of promoting the hyaluronicacid to be absorbed.

The invention described herein relates to certain pyridazinedione N-substituted glycine derivatives of formula (I)which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

The invention discloses a method for producing CIS-4-hydroxyproline. The method comprises the steps of obtaining a recombinant strain by constructing an overexpression prolyl hydroxylase gene Ecp4H in a host bacteria cell and inhibiting expressions of a prolyl hydroxylase gene putA during degradation pathway of proline and succinate dehydrogenase genes sucA and sucB, an isocitrate lyase gene aceA and an isocitrate kinase gene aceK during degradation pathway of alpha-ketoglutaric acid by utilizing a CRISPR-Cas9 technology, and conducting whole-cell transformation and production on the CIS -4- hydroxyproline after conducting fermentation and cultivation on the recombinant strain. The method for the CIS -4- hydroxyproline is simple in cultivation mode and high in strain vigor and product yield.

The present invention provides a triazolopyridine compound having a prolyl hydroxylase inhibitory action and an erythropoietin production-inducing ability. The present invention relates to a compound represented by the following formula [I]:wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof, as well as a prolyl hydroxylase inhibitor or erythropoietin production-inducing agent containing the compound. The compound of the present invention shows a prolyl hydroxylase inhibitory action and an erythropoietin production-inducing ability and is useful as a prophylactic or therapeutic agent for various diseases and pathologies (disorders) caused by decreased production of erythropoietin.

The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I), (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

The invention discloses a gene segment provided with coded and highly-active trans-4-hydroxyl-L-prolyl hydroxylase and an application thereof. Gene codons of trans-4-hydroxyl-L-prolyl hydroxylase (GenBank ID: BAA 20094.1) in Dactylosporangiumsp. RH1 are optimized to obtain a p4hyd gene; the optimized p4hyd gene is truncated to obtain a P4Hyd1-257 gene; recombinant plasmids including pET-M-3C-P4Hyd and pET-M-3C-P4Hyd1-257 are built respectively, prokaryotic expression is performed through escherichia coli, and trans-4-hydroxyl-L-proline is produced in a conversion manner by utilizing thalli as an enzyme source. An experimental result shows that L-proline is taken as a substrate, compared with pET-M-3C-P4Hyd, the highest conversion rate of trans-4-hydroxyl-L-proline generated by pET-M-3C-P4Hyd1-257 in the conversion manner is increased from 91.4% to 97.4%, the conversion time is shortened from 80 hours to 60 hours, so that the conversion rate is improved remarkably, and the conversion time is shortened remarkably. The gene segment provided with coded and highly-active trans-4-hydroxyl-L-prolyl hydroxylase and the application thereof can be used for producing L-proline by a bioconversion method, and have better industrial application prospect.

The invention described herein relates to certain bicyclic heteroaromatic N-substituted glycine derivatives of formula (I)which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

The invention relates to the field of medicinal chemistry, in particular to a triazopyridine formylglycine compound (I). The compound has high prolyl hydroxylase inhibition activity, and can stabilizeintracellular hypoxia inducing factors, increase generation and secretion of erythropoietin and promote erythropoiesis. The invention also relates to a preparation method of the compound, a medicinalcomposition containing the compound or a pharmaceutically acceptable salt thereof, as well as application of the compound or the pharmaceutically acceptable salt thereof to preparation of medicines for inhibiting prolyl hydroxylase or preparation of medicines for promoting generation of the erythropoietin.

The present invention relates to spiroindalone compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.

The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond expressed / synthetic to the modulation of PHD2 gene expression and / or activity, and / or modulate a beta-catenin gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including small nucleic acid molecules, such as short inter-fering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsR-NA), micro-RNA (miRNA), and short hair-pin RNA (shRNA) molecules that are capa-ble of mediating or that mediate RNA inter-ference (RNAi) against PHD2 gene expres-sion.

The present invention relates to spiroazaindole compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.

The invention described herein relates to certain quinoxaline-5-carboxamide derivatives of formula (I)which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

The invention discloses a high-efficiency conversion method for producing trans-4-hydroxy-L-proline by a bioconversion technology. The high-efficiency conversion method comprises a high-activity self-induced expression method of L-prolyl hydroxylase in recombinant engineered escherichia coli, types and concentrations of assistants used in an L-proline-to-trans-4-hydroxy-L-proline efficient conversion system, and conversion conditions of the conversion system. The high-efficiency conversion method provides an important scientific basis for establishing bioconversion-based industrial production of trans-4-hydroxy-L-proline.

The present invention relates to naphthyridine compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.

The invention described herein relates to certain pyrimidinedione N-substituted glycine derivatives of formula (I)which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

The invention provides a recombinant humanized III-type collagen. The recombinant humanized III-type collagen has a triple helix structure, and has an amino acid sequence reducing a humanized III-typecollagen alpha-1 chain and including 1068 amino acids. The invention further provides a preparation method of the recombinant humanized III-type collagen, wherein the prolyl hydroxylase of PBCV-1 includes 209 amino acids, and the base sequence is optimized according to the codons of saccharomyces cerevisiae. Compared with the prior art, the preparation method has the advantages that the triple helix is formed in vitro from collagen chains by utilizing the prolyl hydroxylase; and the saccharomyces cerevisiae expression system adopted by the invention is applicable to large-scale amplificationwithout endotoxin or later removal, the preparation cost is low, and the protein expression quantity is further improved. The recombinant humanized III-type collagen is excellent in stability, the amino acid composition of the recombinant humanized III-type collagen is almost completely the same as that of the alpha-1 chain of a natural collagen, and no immunological rejection can be generated when the recombinant humanized III-type collagen is applied to a human body. The recombinant humanized III-type collagen is good in biocompatibility and can be widely applied to surgical treatment and cosmetic medical industry.

The invention provides prolyl hydroxylase and application thereof. The prolyl hydroxylase comprises (a) a protein with an amino acid sequence as shown by SEQ ID NO: 2; (b) a protein with the amino acid sequence as shown by the SEQ ID NO: 2 being mutated through one or more amino acids, and prolyl hydroxylase activity; or (c) a protein with mutation of one or more amino acids in the (b), prolyl hydroxylase activity, and at least 78 percent of homology with the amino acid sequence of the protein in the (b). Due to the protein with the amino acid sequence as shown by the SEQ ID NO: 2 and a mutant obtained through improving the protein by utilizing a gene engineering means, the prolyl hydroxylase provided by the invention has higher catalysis specifity compared with existing prolyl hydroxylase, or the catalytic activity is remarkably improved.

The present invention relates to naphthyridine compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.

The invention discloses a new dual inhibitor for prolyl hydroxylase and histone deacetylase shown as formula I, a preparation method and an application thereof. The new dual inhibitor is capable of selectively promoting the level of hypoxia-inducible factor -2alpha(HIF-2alpha) by simultaneously inhibiting activities of prolyl hydroxylase (PHD) and histone deacetylase (HDAC) and is expected to become a new radiation protection drug.

The invention described herein relates to certain pyridazinedione N-substituted glycine derivatives of formula (I)which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

The present invention relates to Tetrahydrofuropyridones compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.

The invention described herein relates to certain bicyclic heteroaromatic N-substituted glycine derivatives of formula (I)which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.