Supercharge Your Innovation With Domain-Expert AI Agents!

Il-8 inihibitors for use in the treatment of some urological disorders

1. The technology of IL-8 and inhibitors, which is applied in the direction of urinary system diseases, diseases, bone diseases, etc., can solve the problems of lack of impact information, no specific effect, etc.

Inactive Publication Date: 2019-06-25
DOMPE FARM SPA
View PDF6 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The aforementioned literature teaches that IC / PBS is associated with the presence of multiple inflammatory mediators, including IL-8, in the patient's urine or serum, but does not provide any teaching on the specific role of each of these mediators in disease onset and progression
Furthermore, the literature lacks any information on the effect of inhibition of the identified potential markers on the onset and / or progression of urologic disease

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
  • Il-8 inihibitors for use in the treatment of some urological disorders
  • Il-8 inihibitors for use in the treatment of some urological disorders
  • Il-8 inihibitors for use in the treatment of some urological disorders

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0037] According to a preferred embodiment, said 2-phenyl-propionic acid derivative is a compound of formula (I):

[0038]

[0039] in,

[0040] R1 is hydrogen;

[0041] X is OH;

[0042] R2 is hydrogen or straight chain C 1 -C 4 alkyl;

[0043] Y is a heteroatom selected from S, O and N;

[0044] Z is selected from straight chain or branched chain C 1 -C 4 Alkyl, straight chain or branched C 1 -C 4 Alkoxy, halo C 1 -C 3 Alkyl and halo C 1 -C 3 alkoxy.

[0045] Preferably, Z is CF 3 .

[0046] More preferably, the compound of formula (I) has a phenylpropyl chiral carbon atom in S configuration.

[0047] Particularly preferred compounds of formula (I) according to the invention are selected from: (R,S)-2-(4-{[4-(trifluoromethyl)-1,3-thiazol-2-yl]amino}benzene yl)propionic acid or (2S)-2-(4-{[4-(trifluoromethyl)-1,3-thiazol-2-yl]amino}phenyl)propionic acid and its pharmaceutically acceptable salts , preferably its sodium salt. According to the present inven...

Embodiment 1

[0083] Characterization of compound 1 in an in vitro inflammation model of prostatitis

[0084] To characterize compound 1 in an in vitro inflammatory prostatitis model, normal human prostate cells RWPE-1 (ATCC, Lot No. 61840713) were contacted with activated macrophages; thus inducing an inflammatory microenvironment to enhance the release of reactive oxygen and nitrogen species produced (Debelec-Butuner et al., Mol. Carcinogen. 2014, 53:85–97).

[0085] Human U-937 monocytes (ATCC, Lot No. 61795631 ) seeded at 50.000 cells / ml were differentiated with phorbol acetate (16 mM) for 16 hours. To stimulate cytokine production, lipopolysaccharide (LPS) (10 ng / ml for 24 hours) was added and conditioned medium (CM) was collected.

[0086] After 24 hours of culture, RWPE-1 cells were treated with compound 1 (0.1, 1 and 10 μM) and then exposed to CM from activated U-937. After 3 h, reactive oxygen species (ROS) and reactive nitrogen species (RNS) were quantitatively measured by 2′,7′...

Embodiment 2

[0089] Effect of Oral Compound 1 in Experimental Autoimmune Chronic Prostatitis (EACP)

[0090] Experimental autoimmune chronic prostatitis (EACP) can be easily generated in rats by specific immunization with homogenate of syngeneic rat prostate. As already described, pelvic pain arises due to a strong inflammatory response (Zhang et al., Scand J Immunol 2011, 73:546-553; Zhang et al., Prostate 2012, 72:90-99; Wang et al., Int Urol Nephrol 2015 , 47:307-316; Rudick et al., Am J Physiol Regul Integr Comp Physiol 2008, 294: R1268-1275).

[0091] A total of 36 Lewis male rats (250-270 g) from Charles River, Italy were used in this study according to the regulations of the Animal Ethics Committee (IACUC n.631).

[0092] Rats were maintained under standard laboratory conditions on a 12:12 light / dark cycle with free access to food pellets and tap water.

[0093] Initially, each animal was immunized with 2 mg homologous prostatin diluted in saline, emulsified with 2 mg / ml H37a myco...

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

No PUM Login to View More

Abstract

The present invention relates to IL-8 inhibitor compounds for use in the treatment of chronic prostatitis / chronic pelvic pain syndrome (CP / CPPS) and benign prostatic hyperplasia.

Description

technical field [0001] The present invention relates to IL-8 inhibitor compounds useful in the treatment of chronic prostatitis / chronic pelvic pain syndrome (CP / CPPS) and benign prostatic hyperplasia. Background technique [0002] Prostatitis is inflammation of the prostate gland, the walnut-sized gland located just below the bladder in men. The prostate secretes a fluid that, together with sperm, makes semen. There are different types of prostatitis, one of which is chronic prostatitis / chronic pelvic pain syndrome (CP / CPPS). This is the most common type. Young and middle-aged men are more likely to develop CP / CPPS, but it can occur at any age. CP / CPPS can be classified as inflammatory or noninflammatory based on the presence or absence of leukocytes in prostatic secretions, urine, or semen. In inflammatory cases, urine, semen, and fluid secreted by the prostate contain infection-fighting cells, but these fluids are free of bacteria. [0003] Chronic prostatitis / chronic...

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): A61K31/255A61K31/421A61K31/427A61P13/08
CPCA61K31/255A61K31/421A61K31/427A61P13/08A61P15/00A61P19/00A61P43/00A61K31/425A61K45/06A61K31/4168A61K31/426
Inventor M·阿莱格雷蒂A·阿拉米尼M·C·切斯塔G·比安基尼L·布兰多利尼
Owner DOMPE FARM SPA
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

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

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com