808756-71-0

Usage

Uses

Used in Pharmaceutical Industry:
N-[(1R)-5-(1,1-Dimethylethyl)-2,3-dihydro-1H-inden-1-yl]-N'-1H-indazol-4-ylurea is used as a therapeutic agent for neuropsychiatric disorders due to its ability to selectively inhibit PDE10A, thereby modulating cAMP levels which are implicated in the pathophysiology of these conditions.
Used in Schizophrenia Treatment:
BI8622 is used as a potential treatment for schizophrenia, leveraging its PDE10A inhibitory properties to address the underlying biochemical imbalances associated with this mental disorder.
Used in Huntington's Disease Management:
N-[(1R)-5-(1,1-Dimethylethyl)-2,3-dihydro-1H-inden-1-yl]-N'-1H-indazol-4-ylurea is also being explored for its use in managing Huntington's disease, where it may help alleviate symptoms by modulating the cAMP signaling pathway, which is implicated in the progression of the disease.
Clinical Trials:
N-[(1R)-5-(1,1-Dimethylethyl)-2,3-dihydro-1H-inden-1-yl]-N'-1H-indazol-4-ylurea is currently under evaluation in clinical trials to assess its efficacy and safety in treating the aforementioned neuropsychiatric conditions, marking a significant step in the development of novel therapeutics for these challenging disorders.

InChI:InChI=1/C21H24N4O/c1-21(2,3)14-8-9-15-13(11-14)7-10-18(15)24-20(26)23-17-5-4-6-19-16(17)12-22-25-19/h4-6,8-9,11-12,18H,7,10H2,1-3H3,(H,22,25)(H2,23,24,26)/t18-/m1/s1

Upstream product

• 935680-90-3 5-tert-butyl-2,3-dihydro-1H-inden-1-ylamine 
• 4600-86-6 5-(tert-butyl)-2,3-dihydro-1H-inden-1-one 
• 735330-50-4 4-(2,5-dioxopyrrolidin-1-yl-oxycarbonylamino)indazole-1-carboxylic acid methyl ester 
• 934593-36-9 (1R)-5-tert-butyl-indan-1-ylamine tosylate 
• 28547-33-3 1-(4-(tert-butyl)phenyl)-3-chloropropan-1-one 
• 253185-03-4 tert-butylbenzene 
• 808756-69-6 methyl 4-[({[(1R)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]amino}carbonyl)amino]-1H-indazole-1-carboxylate 
• 952734-48-4 (R)-1-(2-benzyl-2H-indazol-4-yl)-3-(5-tert-butyl-2,3-dihydro-1H-indan-1-yl)urea 

Relevant academic research and scientific papers

Identification of (R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H- indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management

Vanilloid receptor TRPV1 is a cation channel that can be activated by a wide range of noxious stimuli, including capsaicin, acid, and heat. Blockade of TRPV1 activation by selective antagonists is under investigation by several pharmaceutical companies in an effort to identify novel agents for pain management. Here we report that replacement of substituted benzyl groups by an indan rigid moiety in a previously described N-indazole-N′-benzyl urea series led to a number of TRPV1 antagonists with significantly increased in vitro potency and enhanced drug-like properties. Extensive evaluation of pharmacological, pharmacokinetic, and toxicological properties of synthesized analogs resulted in identification of (R)-7 (ABT-102). Both the analgesic activity and drug-like properties of (R)-7 support its advancement into clinical pain trials.

Development of a large scale asymmetric synthesis of vanilloid receptor (TRPV1) antagonist ABT-102

A highly efficient asymmetric synthesis of TRPV1 antagonist ABT-102 was developed and successfully demonstrated on a multi-kilogram scale. This process incorporates a new asymmetric synthesis of (R)-tert-butylaminoindan, which is based on a chiral auxiliary induced diastereoselective reduction of its iminoindan precursor.

Prodrugs of compounds that inhibit TRPV1 receptor

Compounds of formula (I) wherein A, R1, R2, and R3 are defined in the specification, and which are useful as therapeutic compounds particularly for treating disorders or conditions associated with inflammation, pain, bladd

Process for the Preparation of Indazolyl Ureas that Inhibit Vanilloid Subtype1 (VR1) Receptors

The present invention relates to a process of preparing indazolyl ureas that are useful as antagonists of the vanilloid receptor subtype 1 (VR1).

Fused compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor

Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence, or bladder overactivity.