221877-56-1

Upstream product

• 288-94-8 1H-tetrazole 
• 146903-47-1 C₅₈H₈₅NO₁₅S 
• 53123-88-9 sirolimus 

Relevant academic research and scientific papers

Rapamycin analogs with reduced systemic exposure

The synthesis and biological activities of rapamycin (I) analogs modified at the C-40 position are reported. Emphasis placed on compounds that potentially have an improved safety profile on account of their shorter in vivo half-life when compared with rap

MEDICAL DEVICES CONTAINING RAPAMYCIN ANALOGS

A medical device comprises a supporting structure capable of containing or supporting a pharmaceutically acceptable carrier or excipient, which carrier or excipient may contain one or more therapeutic agents or substances, with the carrier preferably including a coating on the surface thereof, and the coating containing the therapeutic substances, such as, for example, drugs. Supporting structures for the medical devices that are suitable for use in this invention include, but are not limited to, coronary stents, peripheral stents, catheters, arterio-venous grafts, by-pass grafts, and drug delivery balloons used in the vasculature. Drugs that are suitable for use in this invention include, but are not limited to drugs of Formula (I). The drugs of Formula (I) can be used in combination with another drug including those selected from anti-proliferative agents, anti-platelet agents, anti-inflammatory agents, anti-thrombotic agents, cytotoxic drugs, agents that inhibit cytokine or chemokine binding, cell de-differentiation inhibitors, anti-lipaedemic agents, matrix metalloproteinase inhibitors, cytostatic drugs, or combinations of these drugs.

CRYSTALLINE FORMS OF RAPAMYCIN ANALOGS

A rapamycin analog composition includes a crystalline form of a rapamycin analog. The crystal can be a hydrate, dehydrate, solvate, or desolvate. The rapamycin analog can have a structure of Formula (I), which is optionally a prodrug, salt, derivative, or

CASCADE SYSTEM

A method of purifying an active pharmaceutical ingredient sufficient for administration into a human subject can include: obtaining a reaction product composition having the active pharmaceutical ingredient and impurities, wherein said active pharmaceutical ingredient is rapamycin or a rapamycin analog; introducing the reaction product composition into a first column of a chromatography system; directing a first portion of a first elutant from the first column to waste, said first portion having more impurity than active pharmaceutical ingredient; directing a second portion of the first elutant from the first column into a second column, said second portion having more active pharmaceutical ingredient than impurity; collecting factions of a second elutant from the second column that include the active pharmaceutical ingredient; and concentrating the said collected fractions to obtain a purity of the active pharmaceutical ingredient greater than 98% and with less than or about 0.95% being first and second major impurities.

One pot synthesis of tetrazole derivatives of sirolimus

A single-step, one-pot process to obtain zotarolimus and other rapamycin derivatives on large scale is presented, which improves currently available synthesis schemes. In one embodiment, dried rapamycin is dissolved in isopropylacetate (IPAc). The solutio

Combination of rapamycin and its tetrazole isomers and epimers, methods of making and using the same

Epimers and isomers of tetrazole-containing rapamycin analogs are immunomodulatory agents and are useful in the treatment of restenosis and immune and autoimmune diseases. Also disclosed are cancer-, fungal growth-, restenosis-, post- transplant tissue re

TETRAZOLE-CONTAINING RAPAMYCIN ANALOGS WITH SHORTENED HALF-LIVES

A compound having formula (I) or a pharmaceutically acceptable salt or prodrug thereof, is an immunomodulatory agent and is useful in the treatment of restenosis and immune and autoimmune diseases. Also disclosed are cancer-, fungal growth-, restenosis-,