179002-82-5

Upstream product

• 19438-10-9 methyl 3-hydroxybenzoate 
• 26690-80-2 2-(N-tert-butoxycarbonylamino)ethanol 
• 2446-83-5 diisopropyl (E)-azodicarboxylate 
• 108-95-2 phenol 
• 39684-80-5 2-(tert-butoxycarbonylamino)ethyl bromide 
• 534-17-8 caesium carbonate 

Downstream Products

• 153938-41-1 methyl 3-(2-aminoethoxy)benzoate 

Relevant academic research and scientific papers

An Aldehyde Responsive, Cleavable Linker for Glucose Responsive Insulins

A glucose responsive insulin (GRI) that responds to changes in blood glucose concentrations has remained an elusive goal. Here we describe the development of glucose cleavable linkers based on hydrazone and thiazolidine structures. We developed linkers with low levels of spontaneous hydrolysis but increased level of hydrolysis with rising concentrations of glucose, which demonstrated their glucose responsiveness in vitro. Lipidated hydrazones and thiazolidines were conjugated to the LysB29 side-chain of HI by pH-controlled acylations providing GRIs with glucose responsiveness confirmed in vitro for thiazolidines. Clamp studies showed increased glucose infusion at hyperglycemic conditions for one GRI indicative of a true glucose response. The glucose responsive cleavable linker in these GRIs allow changes in glucose levels to drive the release of active insulin from a circulating depot. We have demonstrated an unprecedented, chemically responsive linker concept for biopharmaceuticals.

GLUCOSE-SENSITIVE PEPTIDE HORMONES

The present invention relates to a conjugate of the formula P-L-I, wherein P is a peptide hormone effecting the metabolism of carbohydrates in vivo, L is a hydrolysable linker molecule consisting of Lp and Lj, and I is a molecule capable of inhibiting the effect of the peptide hormone P on the metabolism of carbohydrates in vivo. Under in vivo conditions, the conjugate is the major compound. When the concentration of glucose increases in v/vo,the concentration of the peptide hormone effecting the metabolism of carbohydrates in vivo also increases.

PYRIDAZINONES AS PARP7 INHIBITORS

The present invention relates to pyridazinones and related compounds which are inhibitors of PARP7 and are useful in the treatment of cancer.

NOVEL MONOTHIOL MUCOLYTIC AGENTS

Provided are mucolytic agents represented by formula (la)-(ld) where the structural variables Rl, R2, R5 and R6 are as defined herein. Also provided are a variety of methods of treatment which take advantage of the mucolytic properties of the compounds re

AMINE DERIVATIVE COMPOUNDS FOR TREATING OPHTHALMIC DISEASES AND DISORDERS

Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.

Chemical compounds

The invention provides compounds of formula (I): as modulators of chemokine and H1 receptor activity. The compounds are especially useful in the treatment of asthma and rhinitis.

Aromatic compounds containing basic and acidic termini useful as fibrinogen receptor antagonists

This invention relates to novel compounds containing basic and acidic termini, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.