24 results about "Cathelicidins" patented technology

The present invention is directed to cathepsin inhibitor conjugates, precursors and compositions comprising thereof. Further, methods of use such as for the treatment and prevention of a disorder associated with abnormal cathepsin activity in a subject in need thereof are also provided.

The present invention provides a compound of formula (X) or a pharmaceutically acceptable salt thereof, an isotopic variant thereof, a tautomer thereof, a stereoisomer thereof, an ester thereof, a polymorph thereof, or a hydrate thereof. The present invention further provides a preparation method for the compound, a pharmaceutical composition comprising same, and use thereof for treating and / or preventing diseases related to the inhibition of cathepsin C.

The present invention relates to novel use of a cathepsin L inhibitor Z-Phe-Tyr-CHO (C26H26N2O5), wherein the cathepsin L inhibitor Z-Phe-Tyr-CHO inhibits cancer progression and cachexia and muscle damage that are caused by cancer, and thus can be effectively used for preventing, ameliorating or treating cachexia and muscle loss, while having anticancer activity.

This invention relates to compounds that are useful as inhibitors, in particular as inhibitors of Cathepsin K (CatK), and to a method of inhibiting cathepsin activity, comprising administering a compound or formulation comprising a compound according to the invention.

A pyrimidine-2,4-diamine compound and a preparation method and application thereof are provided. The pyrimidine-2,4-diamine compound of the present disclosure can be used in the research of biological or pharmacological phenomena and cathepsin C-involved signal pathway transduction and the evaluation of novel cathepsin C inhibitors. The pyrimidine-2,4-diamine compound is subjected to the screening of anti-cathepsin C activity in vitro and in vivo and proved to have strong inhibitory activity on cathepsin C. The pyrimidine-2,4-diamine compound is subjected to the screening of anti-NSP activity in vivo and proved to have strong inhibitory activity on NSP. The pyrimidine-2,4-diamine compound is subjected to the screening of anti-inflammatory activity in vivo and proved to have an effective therapeutic effect on inflammatory disease models. Meanwhile, the pyrimidine-2,4-diamine compound shows low toxicity and exhibits good application prospect.

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.

A class of ketoamide-based compounds, in particular, a ketoarnide-based compound as represented by general formula A is provided. The ketoamide compound may be used as a 2019 novel coronavirus (2019-nCov) 3 CL protease inhibitor and / or human cathepsin L inhibitor, and / or may be used in the preparation of a medicament for treating and / or preventing and relieving respiratory tract infection, pneumonia and other related diseases caused by 2019 novel coronavirus infection. Pharmaceutical compositions of the class of compounds, pharmaceutical salts, enantiomeric forms, diastereoisomers and racemic compounds thereof in the preparation of a medicament for treating and / or preventing and relieving respiratory tract infections and other related diseases caused by the 2019 novel coronavirus infection are also provided.

The invention discloses an application of a cathepsin D inhibitor in preparation of a medicine for preventing or treating osteoarthritis, and an application of the cathepsin D inhibitor in preparation of a medicine for inhibiting degradation of type II collagen and / or articular cartilage. The invention relates to an application of a cathepsin D inhibitor in preparation of drugs for inhibiting expression of cathepsin D in bone joints. In the application, the cathepsin D can effectively relieve tissue lesions of osteoarthritis.

The present disclosure provides a plurality of compounds. The compounds can inhibit cathepsin L (CatL). Compositions comprising at least one of these compounds are also provided. Methods for treating or preventing one or more CatL-associated diseases in a subject are also provided. The method may include administering the composition to the subject.

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.

Disclosed in the present invention are a polymorph of a benzo[c]chroman compound, a preparation method therefor and use thereof. The present invention particularly provides a polymorph of a compound represented by formula I, a preparation method therefor and use thereof. The compound represented by formula I is used as a cathepsin C inhibitor, and a crystalline form of the compound and a pharmaceutical composition comprising the crystalline form can be used for treating asthma, obstructive pulmonary diseases, bronchiectasis, ANCA-related vasculitis, psoriasis, α1-antitrypsin deficiency, lupus nephritis, diabetes, inflammatory bowel diseases, rheumatic arthritis, rhinosinusitis, hidradenitis suppurativa or cancers.

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 anti- body-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.

Disclosed are polymorphs of benzo[c]chromane compounds, and preparation methods and uses thereof, and specifically provided are polymorphs of a compound shown in formula I, and preparation methods and uses thereof. The compound shown in formula I is a cathepsin C inhibitor, and the crystal form and the pharmaceutical composition containing the crystal form can be used for treating asthma, obstructive pulmonary disease, bronchiectasis, ANCA-associated vasculitis, psoriasis, alpha 1-antitrypsin deficiency, lupus nephritis, diabetes, inflammatory bowel disease, rheumatoid arthritis, sinusitis, hidradenitis suppurativa or cancer.

Provided herein are compositions comprising an endoplasmic reticulum / sarcoplasmic reticulum calcium channel inhibitor and a gap junction inhibitor for use in a variety of methods, such as methods for treating or preventing necrosis, methods for treating or preventing cell death, methods for treating or preventing tissue damage, methods for treating or preventing tissue damage, methods for treating or preventing tissue damage, and methods for treating or preventing tissue damage. Or a method for treating or preventing organ injury. The composition can also include a plasma membrane calcium channel inhibitor and / or a calcium chelating agent. Also provided are compositions comprising a calpain inhibitor and a cathepsin inhibitor for use in a variety of methods. Also provided are compositions comprising a calcium chelating agent, preferably used in a variety of methods at relatively high doses.

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.

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 anti- body-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.

A pharmaceutically acceptable salt of a benzo[c]chroman compound and a polymorphic form and use of the pharmaceutically acceptable salt. The pharmaceutically acceptable salt is selected from hydrochloride, methanesulfonate, phosphate, L-tartrate, maleate, p-toluenesulfonate, sulfate, fumarate, succinate, citrate, malate, and hydrobromide. The pharmaceutically acceptable salt and the polymorphic form thereof improve the bioavailability and the stability, and as a cathepsin C inhibitor, can be used for treating asthma, obstructive pulmonary disease, bronchiectasis, ANCA-associated vasculitis, psoriasis, α1-antitrypsin deficiency, lupus nephritis, diabetes, inflammatory bowel disease, rheumatoid arthritis, sinusitis, hidradenitis suppurativa, or cancer.

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.

Disclosed herein are compounds. The compounds are capable of inhibiting Cathepsin L (CatL). Also disclosed herein are compositions comprising at least one of the compounds. Also provided herein are methods of treating or preventing one or more CatL-related diseases. The methods can comprise administering the compositions to a subject.

The present invention discloses a polymorph of a benzo[c]chroman compound, a method for producing the same, and use thereof. In particular, the present invention provides a polymorph of a compound represented by formula I: a method for producing the same, and use thereof, of the compound represented by JPEG2025518342000022.jpg55127. The compound represented by formula I is used as a cathepsin C inhibitor, and the crystalline form of the compound and the pharmaceutical composition containing the crystalline form can be used for the treatment of asthma, obstructive pulmonary disease, bronchiectasis, ANCA-associated vasculitis, psoriasis, α1-antitrypsin deficiency, lupus nephritis, diabetes, inflammatory bowel disease, rheumatoid arthritis, rhinosinusitis, hidradenitis suppurativa, or cancer.

In the present invention, it has been confirmed that cathepsin L (CTSL) is a dual-action target capable of simultaneously inhibiting tumor progression and CD8⁺ T cell-mediated muscle wasting. That is, pharmacological inhibition of CTSL not only alleviated muscle wasting induced by anti-PD-L1, but also further inhibited tumor growth through down-regulation of BNIP3. As a result, the present invention demonstrates that CTSL acts as a dual-action target that enhances anticancer efficacy while alleviating muscle-specific irAEs, which suggests a new strategic approach that can overcome the clinical limitations of ICIs and improve therapeutic efficacy.

The present invention relates to novel use of a cathepsin L inhibitor Z-Phe-Tyr-CHO (C26H26N2O5), wherein the cathepsin L inhibitor Z-Phe-Tyr-CHO inhibits cancer progression and cachexia and muscle damage that are caused by cancer, and thus can be effectively used for preventing, ameliorating or treating cachexia and muscle loss, while having anticancer activity.

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.

Provided herein is a plurality of the compounds. The compounds are capable of inhibiting Cathepsin L (CatL). A composition including at least one of these compounds is also provided. A method for treating or preventing one or more CatL-related diseases in a subject is further provided. The method may include administering the composition to the subject.