744209-63-0

Usage

Uses

Used in Neurodegenerative Disease Research:
1H-Pyrrolo[2,3-b]pyridine, 4-chloro-1-(phenylsulfonyl)is used as a research tool for studying the role of TSPO in neurodegenerative diseases. Its interaction with the TSPO protein helps in understanding the underlying mechanisms of these diseases and exploring potential therapeutic interventions.
Used in Cancer Research:
In the field of oncology, 1H-Pyrrolo[2,3-b]pyridine, 4-chloro-1-(phenylsulfonyl)is used as a ligand to investigate the involvement of TSPO in cancer progression. Its modulation of TSPO activity may offer new avenues for cancer treatment by targeting specific pathways related to tumor growth and metastasis.
Used in Psychiatric Disorder Research:
1H-Pyrrolo[2,3-b]pyridine, 4-chloro-1-(phenylsulfonyl)is utilized as a research compound in psychiatric studies to explore the connection between TSPO and various psychiatric disorders. Its ability to modulate TSPO activity could lead to the development of new treatments for conditions such as depression, anxiety, and schizophrenia.
Used in Drug Discovery:
In the pharmaceutical industry, 1H-Pyrrolo[2,3-b]pyridine, 4-chloro-1-(phenylsulfonyl)is used as a tool compound in drug discovery research. It aids in the identification and development of novel TSPO-targeted drugs with potential applications in various therapeutic areas, including neurodegenerative diseases, cancer, and psychiatric disorders.

InChI:InChI=1/C14H11ClN2O2S/c1-10-2-4-11(5-3-10)20(18,19)17-9-7-12-13(15)6-8-16-14(12)17/h2-9H,1H3

Upstream product

• 98-09-9 benzenesulfonyl chloride 
• 55052-28-3 4-chloro-7-azaindole 
• 271-63-6 7-Azaindole 
• 1245649-52-8 1-(benzenesulfonyl)-4-chloro-5-nitro-1H-pyrrolo[2,3-b]pyridine 

Downstream Products

• 940948-30-1 4-chloro-2-iodo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine 
• 55052-28-3 4-chloro-7-azaindole 
• 1315495-69-2 4-(5-nitro-1-phenylsulfonyl-1H-pyrrolo[2,3-b]pyridine-4-ylamino)-4-methylpiperdine-1-carboxylic acid tert-butyl ester 
• 1315495-70-5 4-(5-amino-1-phenylsulfonyl-1H-pyrrolo[2,3-b]pyridine-4-ylamino)-4-methyl-piperdine-1-carboxylic acid tert-butyl ester 
• 1315495-71-6 4-[6-phenylsulfonyl-4-(imidazo[4,5-d]pyrrolo[2,3-b]-pyridin-1(6H)-yl)]-4-methyl-piperidine-1-carboxylic acid tert-butyl ester 
• 1315484-14-0 1-[1-(phenylmethyl)-piperidin-4-yl]-1,6-dihydro-imidazo-[4,5-d]pyrrolo[2,3-b]pyridine 
• 1315497-67-6 4-(6-phenylsulfonyl-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl))-cyclohexanone 
• 1315484-23-1 [4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridine-1(6H)-yl)-piperidin-1-yl]phenylmethanone 

Relevant academic research and scientific papers

ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors

Rho kinase (ROCK) inhibitors are potential therapeutic agents for the treatment of a variety of disorders including hypertension, glaucoma and erectile dysfunction. Here we disclose a series of potent and selective ROCK inhibitors based on a substituted 7-azaindole scaffold. Substitution of the 3-position of 7-azaindole led to compounds such as 37, which possess excellent ROCK inhibitory potency and high selectivity against the closely related kinase PKA.

Discovery of imidazopyrrolopyridines derivatives as novel and selective inhibitors of JAK2

Herein, we describe the design, synthesis, and structure?activity relationships of a series of imidazopyrrolopyridines derivatives that selectively inhibit Janus kinase 2 (JAK2). These screening cascades revealed that 6k was a preferred compound, with IC50 values of 10 nM for JAK2. Moreover, 6k was a selective JAK2 inhibitor with 19-fold, >30-fold and >30-fold selectivity over JAK1, JAK3 and TYK2 respectively. In cytokine-stimulated cell-based assays, 6k exhibited a higher JAK2 selectivity over JAK1 isoforms. Indeed, at a dose of 20 mg/kg compound 6k, pSTAT3 and pSTAT5 expression was reduced to levels comparable to those of control animals untreated with GM-CSF. Additionally, 6k showed a relatively good bioavailability (F = 38%), a suitable half-life time (T1/2 = 1.9 h), a satisfactory metabolic stability, suggesting that 6k might be a promising inhibitor of JAK2 for further development research for the treatment of MPNs.

Design and synthesis of 7-azaindole derivatives and their antitumor and analgesic activities

To develop effective anti-tumor and analgesic drugs, a series of novel 7-azaindole derivatives were designed and synthesized through a four-step reaction. 18 target compounds were obtained and characterized through Nuclear Magnetic Resonance and High Resolution Mass Spectrometry. Their anti-proliferative activities and analgesic effect were evaluated. When the 1-position was a methylsulfonyl group and the 5-position was a nitro group, compound 4f demonstrated the best activity. Furthermore, there was a dramatic difference between the IC50 values of compound 4f in tumor and in healthy cell line. The IC50 values of compound 4f in MCF7 breast cancer cell line was 5.781 μmol/L and 8.077 μmol/L in HepG2 hepatoma carcinoma cell line, but more than 100 μmol/L in HL7702 liver cell line. Preliminary results showed that compounds 3a, 3g and 4i had significant analgesic effects in mice, which were stronger than aspirin. These compounds have good prospects for new drug development.

SUBSTITUTED PYRROLOPYRIDINES AS INHIBITORS OF ACTIVIN RECEPTOR-LIKE KINASE

Described herein are compounds that inhibit ALK2 and its mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.

A new synthetic process of the pyrrole compounds and the use of the anti-tumor effect (by machine translation)

The present invention discloses a new synthetic process of the pyrrole compounds and the use of the anti-tumor effect, and in particular relates to compounds 1 - benzenesulfonyl - 4 - chloro - 5 - nitro - 1 H - pyrrolo [2, 3 - b] pyridine, hydrate and its salt of new synthetic process and the use of the anti-tumor effect, this synthesis process takes 1 H - pyrrolo [2, 3 - b] pyridine as the starting material, after chloro-, prepared by acylation reaction such as 1 - benzenesulfonyl - 4 - chloro - 5 - nitro - 1 H - pyrrolo [2, 3 - b] pyridine, hydrate and its salt, provides a simple operation, high yield of the new process, the preparation method is simple, mild reaction conditions, at the same time the compound anti-tumor activity is prominent, little toxicity to normal cell, is favorable to its anti-tumor field widely popularized. (by machine translation)

POLYCYCLIC TLR7/8 ANTAGONISTS AND USE THEREOF IN THE TREATMENT OF IMMUNE DISORDERS

The present invention relates to compounds of Formula (I) and pharmaceutically acceptable compositions thereof, useful as toll-like receptor 7/8 (TLR7/8) antagonists. In Formula (I), Ring A is aryl or heteroaryl; Ring B is aryl or heteroary; and X is C(R4)2, O, NR4, S, S(R4), or S(R4)2.

METHOXY-SUBSTITUTED PYRROLOPYRIDINE MODULATORS OF RORC2 AND METHODS OF USE THEREOF

The present invention provides methoxy-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating RORγ activity and/or reducing the amount of IL- 17 in a subject, and methods of treating various medical disorders using such pyrrolopyridines and pharmaceutical compositions thereof.

RORC2 INHIBITORS AND METHODS OF USE THEREOF

The present invention provides compounds, pharmaceutical compositions, methods of inhibiting RORγ activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such compounds and pharmaceutical compositions.

Aminosulfonylmethylcyclohexanes as JAK inhibitors

The invention relates to a compound of formula wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful as therapeutic agent for organ transplants, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, Type I diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, inflammatory bowel diseases, Crohn's disease, Alzheimer's disease, leukemia, osteoarthritis, control of pruritus, chronic respiratory disease or keratoconjunctivitis in mammals.

THIAZOLECARBOXAMIDES AND PYRIDINECARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS

The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.