15 results about "Cathepsin K" patented technology

The present invention relates to a method for preparing controlled-release enzyme-loaded microspheres for preventing and treating skin photoaging and their application, belonging to the field of pharmaceutical engineering drug preparations. The present invention's preparation method produces controlled-release enzyme-loaded microspheres loaded with cathepsin D and cathepsin K, combining the advantages of microsphere controlled release with the therapeutic strategy of cathepsins. The resulting microspheres have the effect of preventing and treating skin photoaging, representing a major breakthrough in the research and development of specific drugs for preventing and treating photoaging and related skin lesions. The present invention can provide a new strategy for developing better small-molecule drugs for the prevention and treatment of photoaging and related skin diseases, and has important theoretical and practical value.

The present invention relates to a cathepsin K inhibitor comprising or consisting of Formula (I) (X1)(X2)(X3)(X4)(Y)(X5)(X6)(X7) Formula (I), wherein (X1) is the amino acid K; (X2) is an amino acid selected from R and W, and is preferably R; (X3) is an amino acid selected from R and W, and is preferably R; (X4) is the amino acid L; (X5) is an amino acid selected from Y, V and W, and is preferably V or Y, and is most preferably V; (X6) is an amino acid selected from I, M, L, W and R, and is preferably I, L or W; and is most preferably I; (X7) is an amino acid selected from H, W, A T, R; and is preferably H or R, and is most preferably R; and (Y) is a Michael acceptor. The present invention also relates to a cathepsin L inhibitor comprising or consisting of Formula (II) (X1)(X2)(X3)(X4)(Y)(X5)(X6)(X7) Formula (II), wherein (X1) is the amino acid K; (X2) is the amino acid R; (X3) is an amino acid selected from R, L and M, and is preferably L; (X4) is an amino acid selected from L, W, F and Y, and is preferably W; (X5) is an amino acid selected from V, H and R, and is preferably V; (X6) is an amino acid selected from M, L, I, W and R, and is preferably L; (X7) is an amino acid selected from W, A T, R; and is preferably W; and (Y) is a Michael acceptor.

The present invention relates to a cathepsin K inhibitor comprising or consisting of Formula (I) (X1)(X2)(X3)(X4)(Y)(X5)(X6)(X7) Formula (I), wherein (X1) is the amino acid K; (X2) is an amino acid selected from R and W, and is preferably R; (X3) is an amino acid selected from R and W, and is preferably R; (X4) is the amino acid L; (X5) is an amino acid selected from Y, V and W, and is preferably V or Y, and is most preferably V; (X6) is an amino acid selected from I, M, L, W and R, and is preferably I, L or W; and is most preferably I; (X7) is an amino acid selected from H, W, A T, R; and is preferably H or R, and is most preferably R; and (Y) is a Michael acceptor. The present invention also relates to a cathepsin L inhibitor comprising or consisting of Formula (II) (X1)(X2)(X3)(X4)(Y)(X5)(X6)(X7) Formula (II), wherein (X1) is the amino acid K; (X2) is the amino acid R; (X3) is an amino acid selected from R, L and M, and is preferably L; (X4) is an amino acid selected from L, W, F and Y, and is preferably W; (X5) is an amino acid selected from V, H and R, and is preferably V; (X6) is an amino acid selected from M, L, I, W and R, and is preferably L; (X7) is an amino acid selected from W, A T, R; and is preferably W; and (Y) is a Michael acceptor.

The present invention discloses an application and a kit for differential histoproteins and / or metabolites of pigmented villonodular synovitis; the differential histoproteins include at least one of the following proteins: TNFSF11, cathepsin K, and adhesion G protein-coupled receptor E5; the differential metabolites include at least one of the following products: 13-hydroxyperoxylinoleic acid and octadecadienoic acid; the present invention provides a new screening marker for pigmented villonodular synovitis (PVNS) through proteomics and metabolomics, which can achieve effective screening for pigmented villonodular synovitis; the obtained screening marker is used in a screening kit, which only needs synovial fluid as a test sample, can quickly perform screening and detection, and has the advantages of high efficiency and simple detection.

The invention relates to the related technical field of medical drugs, in particular to an anti-osteoporosis pill based on hydroxyapatite combined Erzhi pill and a preparation method thereof, the pill comprises a nano-hydroxyapatite carrier (Ca / P = 1.67: 1, and the particle size is 20-100nm), Erzhi pill active components (the compatibility of ligustrum lucidum ait total glycoside and eclipta ethyl acetate part is 1: 1) and pharmaceutical auxiliary materials, through ionic bond / hydrogen bond loading, the drug loading ratio is (5-20): 1. The preparation method comprises the following steps: synthesizing nano-hydroxyapatite by a hydrothermal method, extracting active components of Erzhi pills by using ethanol, adsorbing and carrying medicines by using a buffer solution with the pH value of 7.4, and tabletting and forming. According to the anti-osteoporosis pill based on the hydroxyapatite combined Erzhi pill and the preparation method of the anti-osteoporosis pill, the synergistic anti-osteoporosis effect is achieved by up-regulating bone morphogenetic genes (osterix, OCN), inhibiting osteoclast genes (c-Src, cathepsin K) and regulating an LCN2 / Sema3A pathway, the targeting property is high, the bioavailability is high, and the anti-osteoporosis pill is suitable for treating postmenopausal and senile osteoporosis.

A compound selected from N-[(S)-1-((3aS,6S,6aS)-6-fluoro-3-oxo-hexahydro-furo[3,2-b]pyrrole-4-carbonyl)-3-methyl-butyl]-4-[2-(4-methyl-piperazin-1-yl)-thiazol-4-yl]-benzamide, N-[(S)-1-((3aS,6S,6aS)-6-Fluoro-3,3-dihydroxy-hexahydro-furo[3,2-b]pyrrole-4-carbonyl)-3-methyl-butyl]-4-[2-(4-methyl-piperazin-1-yl)-thiazol-4-yl]-benzamide, mixtures thereof, and pharmaceutically acceptable salts thereof has utility in the treatment of a disorder mediated by cathepsin K in companion non-human animals, especially periodontal disease and / or a tooth resorption.

The invention relates to the technical field of biological medicines, and discloses a pharmaceutical composition, a preparation method and application thereof, and a medicine for promoting wound healing. The pharmaceutical composition comprises a cathepsin K inhibitor and an exosome. Through combined use of the cathepsin K inhibitor and the exosome, especially the exosome derived from mesenchymal stem cells, the defects of an existing diabetes wound treatment method are overcome, collagen degradation is reduced, and collagen deposition is promoted; angiogenesis is enhanced, and wound blood supply is improved; the cell survival rate is improved; energy metabolism is recovered, and cell functions are enhanced. Moreover, the purposes of repairing and healing wounds more efficiently can be achieved on the premise that the dosage is smaller, the production cost is reduced, and the treatment feasibility and clinical popularization value are improved.

The instant disclosure describes an injectable composition comprising a Cathepsin K blocking amount of a polydisperse preparation of collagen macropeptides with an average molecular weight between about 10 and about 100 kDa and an acceptable sterile injection vehicle. Methods of treating arthritis and methods of manufacturing injectable composition are also disclosed.

The invention provides a cathepsin K (CTSK) responsive polypeptide derivative and application thereof. The CTSK responsive polypeptide derivative provided by the invention has the following structure: Ar-L1-dipeptide linker-hydrophobic membrane permeation sequence-CTSK response sequence-bone targeting sequence, and can be self-assembled to form bone targeting nanoparticles. According to the CTSK responsive polypeptide derivative and the bone targeting nanoparticles obtained from the CTSK responsive polypeptide derivative disclosed by the invention, the combination of osteoclast and apoptotic body mediated bone regeneration is specifically eliminated by utilizing self-assembly triggered by CTSK, so that bone balance is recovered, and physiological bone remodeling is not destroyed.

The invention relates to the technical field of biological medicines, in particular to application of cathepsin K (CTSK) or a coding gene thereof serving as a target to preparation of an ARDS diagnosis product or treatment product or preparation of an ARDS related pulmonary fibrosis diagnosis product or treatment product. The invention discloses that the CTSK level in serum or pulmonary alveolar lavage fluid can be used for accurately evaluating whether ARDS or ARDS-related pulmonary fibrosis occurs or not and the degree of pulmonary alveolar-capillary membrane injury; aRDS caused by different factors can be used as a biomarker; compared with existing evaluation indexes, the CTSK has higher response speed and higher sensitivity to ARDS or ARDS-related pulmonary fibrosis, is beneficial to early diagnosis and prognosis evaluation of acute lung injury, and has good market transformation prospects.

The instant disclosure describes an injectable composition comprising a Cathepsin K blocking amount of a polydisperse preparation of collagen macropeptides with an average molecular weight between about 10 and about 100 kDa and an acceptable sterile injection vehicle. Methods of treating arthritis and methods of manufacturing injectable composition are also disclosed.

The invention discloses a macrophage targeting probe, a preparation method and application, the probe is based on blood platelets coupled with a CD41 antibody, and the surfaces of the blood platelets are further modified with phospholipid compounds coupled with a cathepsin substrate peptide fragment-fluorophore structure. The probe has the advantages of good macrophage targeting property, low immunogenicity and capability of crossing a biological membrane barrier. Meanwhile, the cathepsin substrate peptide fragment-fluorophore structure in the probe can generate fluorescence only after being cut by cathepsin K in the macrophage, real-time fluorescence tracking imaging of the functional state and position of the macrophage can be effectively achieved, and then early diagnosis of diseases and guidance of disease treatment are achieved.

The present invention relates to a cathepsin K inhibitor having the structure as shown in formula (0) and / or formula (II), wherein cyanopyrimidine or a keto group as an electrophilic group is a key group to exert a good inhibitory effect on cathepsin K. Further provided are a preparation method therefor and use thereof. The provided cathepsin K inhibitor has a relatively high inhibitory effect and selectivity, and is expected to be used for treating diseases including thyroid diseases, cardiovascular diseases, bone diseases and gum diseases.

Provided herein are methods of diagnosing, monitoring and treating a disease or disorder using cathepsin K as a biomarker. The disease or disorder may be an inflammatory disease, an autoimmune disease, or sepsis. Also, provided herein are compositions for treating the disease or disorder diagnosed by the described methods.

A compound selected from N-[(S)-1-((3aS,6S,6aS)-6-fluoro-3-oxo-hexahydro-furo[3,2-b]pyrrole-4-carbonyl)-3-methyl-butyl]-4-[2-(4-methyl-piperazin-1-yl)-thiazol-4-yl]-benzamide, N-[(S)-1-((3aS,6S,6aS)-6-Fluoro-3,3-dihydroxy-hexahydro-furo[3,2-b]pyrrole-4-carbonyl)-3-methyl-butyl]-4-[2-(4-methyl-piperazin-1-yl)-thiazol-4-yl]-benzamide, mixtures thereof, and pharmaceutically acceptable salts thereof has utility in the treatment of a disorder mediated by cathepsin K in companion non-human animals, especially periodontal disease and / or a tooth resorption.