# US 2023/0054099 A1 · Role Of Novel Carbazole Linked 1, 2, 3- Triazole Analogs in Alleviating Methylglyoxal-Mediated Late Diabetic Vascular Complications

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- Number: US 2023/0054099 A1
- Document ID: US20230054099A1
- Status: Published application
- Kind: A1
- Application number: 17/408,006
- Filed: 2021-08-20
- Published: 2023-02-23
- Earliest claimed: 2021-08-20
- Inventors: Humera Jahan; Mohammad Iqbal Choudhary; Nimra Naz Siddiqui; Fatima Z. Basha; Shazia Iqbal
- Web page: https://patentgrep.com/patent/US20230054099A1

## CPC

- A61K 31/4196: 1,2,4-Triazoles
- A61K 31/403: condensed with carbocyclic rings, e.g. carbazole
- A61K 31/4439: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465)
- A61P 9/12: Antihypertensives
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present intervention identifies the antiglycating inhibitors from a series of carbazole-linked 1,2,3 triazole derivatives through in vitro MGO-mediated glycating BSA model. Derivatives 12, and 13 established a remarkable antiglycation activity at the receptor level in human monocytes. These compounds were found non-toxic, and possess the potential to halt AGE-RAGE/ROS- mediated NF- kB-dependent COX-2, and its proinflammatory product, PGE2, production in monocytes. Hence, carbazole-linked 1,2,3 triazole derivatives provide treatment modalities to delay or prevent the onset of late diabetic micro- and macro-vascular complications in diabetic patients.

## Claims

### Claim 1

A method for reducing the development of diabetes-associated late vascular impairment diabetic atherogenesis progression comprising administration to humans and animals an effective dose of a carbazole-linked 1,2,3-triazole compounds, in combination with inert pharmaceutical ingredients.

### Claim 2 (depends on 1)

The method of claim 1, wherein the carbazole-linked 1,2,3-triazole compounds are 2-(4-((9H-Carbazole-9-yl)methyl)-1H-1,2,3-triazole-1-yl)-1-(4-nitrophenyl)ethan-1-one and 9-((1-(2-(2-Methyl-5-nitro-1 H-imidazol-1 -yl)ethyl)-1 H1 ,2,3-triazol-4-yl)methyl)-9H-carbazole.

### Claim 3 (depends on 1)

The method of claim 1, wherein the diabetes-associated late vascular impairment and diabetic atherogenesis progression comprise AGEs formation, pro-inflammatory biomarkers, further comprising COX-2 and its associated PGE2 formation.