Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Use of neutrophil elastase inhibitors in lung diseases

An anti-trypsin, lung disease technology, applied in the field of chronic lung disease, can solve problems affecting the quality of life of patients

Pending Publication Date: 2022-07-15
PH PHARMA CO LTD
View PDF5 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These drugs must be administered by intravenous infusion, usually once a week, which can be uncomfortable at the least and seriously affect the patient's quality of life

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Use of neutrophil elastase inhibitors in lung diseases
  • Use of neutrophil elastase inhibitors in lung diseases
  • Use of neutrophil elastase inhibitors in lung diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] Example 1. Preparation of tablets.

[0078] Compound 1(4S)-4-[4-cyano-2-(methylsulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluoromethyl) yl)phenyl]-1,2,3,4-tetrahydropyrimidine-5-carbonitrile is formulated into tablets for oral use. These tablets are manufactured using standard pharmaceutical processing techniques. All inactive pharmaceutical ingredients in the following examples meet the requirements of the United States Pharmacopoeia (USP), National Formulary (NF), European Pharmacopoeia (Ph. Eur.) and / or Japanese Pharmacopoeia (Ph. Jap.) as indicated, And tested and released according to the monograph for each ingredient specified in the indicated standard. Batch sizes vary depending on the amount required for a specific clinical purpose. The following two examples show the qualitative / quantitative composition of exemplary doses and are for illustrative purposes. It should be understood that additional dose sizes and batch sizes are contemplated by the present i...

Embodiment 2

[0095] Example 2. Phase 1 clinical study of compound 1 in healthy patients

[0096] Study description. Phase 1, single-center, randomized, double-blind, placebo-controlled, single-ascending-dose study designed to evaluate the safety, tolerability, and pharmacokinetics (PK) of Compound 1 in healthy subjects. Good Clinical Practice (GCP), ethical principles derived from the Declaration of Helsinki and all other applicable laws, rules and regulations.

[0097] Within each dose cohort, subjects were randomized in a 3:1 ratio (6 active agents and 2 placebo) to receive Compound 1 or placebo. Following screening, subjects received a single dose of study drug and were monitored during the clinical phase and outpatient follow-up. Subjects were confined to the study site on study days -2 to 7 for the collection of PK and safety assessments. After leaving the study site on study day 7, subjects returned to the study site on study days 14, 21, 28 and 35.

[0098] result. A total of...

Embodiment 3

[0101] Example 3. Phase 2 clinical study of compound 1 in patients with AATD

[0102] Study description . This study is a Phase 2, multicenter, double-blind, randomized (1:1), placebo-controlled, proof-of-concept study to evaluate compound 1 administered daily for 12 weeks in patients with confirmed AATD (α-1ZZ Safety and tolerability in patients with genotype [Pi*ZZ]) or alpha-1 null phenotype [Pi* null phenotype], AAT level <11 μM (0.5g / L)) and AATD-related emphysema properties and effects on pharmacodynamic markers. Trials were conducted in accordance with Good Clinical Practice (GCP), ethical principles derived from the Declaration of Helsinki and all other applicable laws, rules and regulations. Eligible patients will be enrolled and randomized in a 1:1 ratio (1 active agent and 1 placebo) within 30 days of screening to receive Compound 1 at 20 mg per day or 10 mg per day or matching placebo per day for 84 days (12 weeks). Compound 1 will be provided as immediate re...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
melting pointaaaaaaaaaa
Login to View More

Abstract

The present invention relates to a method for treating chronic lung disease, in particular alpha-1 antitrypsin deficiency or emphysema caused by alpha-1 antitrypsin deficiency, with a neutrophil elastase inhibitor. The invention also relates to a pharmaceutical composition comprising a neutrophil elastase inhibitor.

Description

[0001] CROSS-REFERENCE TO RELATED APPLICATIONS [0002] This application claims priority to US Provisional Patent Application No. 62 / 890,774, filed August 23, 2019, the contents of which are incorporated herein by reference in their entirety. technical field [0003] The present invention relates to methods for chronic lung disease, in particular for the treatment of alpha-1 antitrypsin deficiency or emphysema caused by alpha-1 antitrypsin deficiency, with neutrophil elastase inhibitors. The present invention also relates to a pharmaceutical composition comprising a neutrophil elastase inhibitor. Background technique [0004] Alpha-1 antitrypsin deficiency (AATD) is an autosomal recessive disorder associated with emphysema and (less frequently) cirrhosis (Crystal, R.G., The Lancet, 2017, Vol. 5, http: https: / / dx.doi.org / 10.1016 / S2213-2600(16)30434-9). The disorder is caused by mutations in the SERPINA1 gene, which encodes the protease inhibitor alpha-1 antitrypsin (AAT or ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5415A61K31/575A61K31/713
CPCA61P11/00A61P1/16A61K31/513A61K9/2054
Inventor S·萨亚尔许颢宁
Owner PH PHARMA CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com