152918-49-5

Upstream product

• 94838-55-8 tert-butyl (4-aminobenzyl)carbamate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 103658-75-9 4-amino-3-iodo-N-benzylamine hydrochloride 
• 33348-34-4 4-amino-3-iodobenzonitrile 
• 94838-58-1 tert-butyl 4-nitrobenzylcarbamate 
• 18600-42-5 4-nitrobenzylamine hydrochloride 
• 873-74-5 4-Aminobenzonitrile 
• 106941-22-4 4-amino-3-iodobenzylamine 

Downstream Products

• 911124-01-1 (4-amino-3-vinylbenzyl)carbamic acid t-butyl ester 
• 1241911-54-5 tert-butyl 4-azido-3-iodobenzylcarbamate 
• 1470058-10-6 C₁₆H₂₂N₂O₃ 
• 1470058-09-3 O-tert-butyl-4-amino-3-(4-N,N'-bis-tert-butoxycarbonylguanidinobut-1-yne-1-yl)benzylcarbamate 
• 1470058-05-9 O-tert-butyl-3-iodo-4-(4-methylphenylsulfonylamido)benzylcarbamate 
• 1470058-07-1 5-(O-tert-butoxycarbonyl)aminomethyl-2-(2-N,N'-bis-tert-butoxycarbonylguanidinoethyl)-1-N-(4-methylphenylsulfonyl)indole 
• 1470058-06-0 5-(O-tert-butoxycarbonyl)aminomethyl-2-(2-hydroxyethyl)-1-N-(4-methylphenylsulfonyl)indole 
• 459449-88-8 (E)-3-[4-(tert-butoxycarbonylamino-methyl)-2-iodo-phenylamino]-but-2-enoic acid benzyl ester 
• 911124-97-5 tert-butyl 3-iodo-4-(methylsulfonamido)benzylcarbamate 

Relevant academic research and scientific papers

Oxidative Approach Enables Efficient Access to Cyclic Azobenzenes

Azobenzenes are versatile photoswitches that have found widespread use in a variety of fields, ranging from photopharmacology to the material sciences. In addition to regular azobenzenes, the cyclic diazocines have recently emerged. Although diazocines have fascinating conformational and photophysical properties, their use has been limited by their synthetic accessibility. Herein, we present a general, high-yielding protocol that relies on the oxidative cyclization of dianilines. In combination with a modular substrate synthesis, it allows for rapid access to diversely functionalized diazocines on gram scales. Our work systematically explores substituent effects on the photoisomerization and thermal relaxation of diazocines. It will enable their incorporation into a wide variety of functional molecules, unlocking the full potential of these emerging photoswitches. The method can be applied to the synthesis of a new cyclic azobenzene with a nine-membered central ring and distinct properties.

In silico design, synthesis, and screening of novel deoxyhypusine synthase inhibitors targeting HIV-1 replication

The human enzyme deoxyhypusine synthase (DHS) is an important host cell factor that participates in the post-translational hypusine modification of eukaryotic initiation factor 5A (eIF-5A). Hypusine-modified eIF-5A plays a role in a number of diseases, in

NOVEL BRONCHODILATING DIAZAHETEROARYLS

The invention relates to novel compounds having the general formula (I), and which compounds are useful to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma.

NOVEL BRONCHODILATING DIAZAHETEROARYLS

The invention relates to novel compounds having the general formula (I), and which compounds are useful to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma.

Synthesis and structural optimization of multiple H-bonding region of diarylalkyl (thio)amides as novel TRPV1 antagonists

Structural optimization of multiple H-bonding region and structure-activity relationship of diarylalkyl amides/thioamides as novel TRPV1 antagonists are described. In particular, we identified amide 34o and thioamides 35o and 35r, of which antagonistic activities were highly enhanced by an incorporation of cyano or vinyl-substituent to the multiple H-bonding region. They exhibited potent 45Ca2+ uptake inhibitions in rat DRG neuron with IC50s of 25, 32 and 28 nM, respectively.

Novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor antagonist; and a pharmaceutical composition containing the same

This present invention relates to compounds of formula (I), in which R3 represents C2-C5 alkenyl or C2-C5 alkynyl and the other variables are as defined in the claims, isomers thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonists; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating pain, inflammatory disease of the joints, urinary bladder hypersensitivity including urinary incontinence, stomach duodenal ulcer, irritable bowel syndrome, inflammatory bowel disease, neurotic/allergic/inflammatory skin disease, psoriasis, asthma, chronic obstructive pulmonary disease, pruritus or prurigo.

NOVEL COMPOUNDS, ISOMER THEREOF, OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF AS VANILLOID RECEPTOR ANTAGONIST; AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receotor 1; VR1; TRPV1 )antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, and heart disease.

Novel potent antagonists of transient receptor potential channel, vanilloid subfamily member 1: Structure-activity relationship of 1,3-diarylalkyl thioureas possessing new vanilloid equivalents

Recently, 1,3-diarylalkyl thioureas have merged as one of the promising nonvanilloid TRPV1 antagonists possessing excellent therapeutic potential in pain regulation. In this paper, the full structure-activity relationship for TRPV1 antagonism of a novel series of 1,3-diarylalky thioureas is reported. Exploration of the structure-activity relationship, by systemically modulating three essential pharmacophoric regions, led to six examples of 1,3-dibenzyl thioureas, which exhibit Ca2+ uptake inhibition in rat DRG neuron with IC50 between 10 and 100 nM.

Functionalized heterocycles as modulators of chemokine receptor function and methods of use therefor

Disclosed are novel compounds having the formula or a physiologically acceptable salt, amide, ester or prodrug thereof. The compounds can be used to modulate (antagonize, agonize) chemokine receptor function. Also disclosed is a method for treating a patient having an inflammatory disease and/or viral infection comprising administering an effective amount of a compound of Formula I. In particular embodiments, the invention is a method for treating a patient infected with HIV.