1314705-19-5Relevant articles and documents
Optimization of the Everolimus Intermediate Preparation Process: Impurity Identification Followed by One-Pot Transformation to the Desired Product
Shestakov, Aleksandr N.,Supurgibekov, Murat B.,Shpakova, Elena A.,Sharkov, Dmitrii E.
, p. 222 - 233 (2022/01/20)
An investigation of the everolimus intermediate PG-EVR preparation process resulted in the identification of three impurities PG-D,E,F constantly formed as byproducts in large amounts. Their structures were reliably established based on two-dimensional (2
RAPAMYCIN ANALOGS AND USES THEREOF
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Paragraph 00520-00521, (2020/01/08)
The present invention provides compounds, compositions thereof, and methods of using the same.
Substituted Oxopyridine Derivatives and Use Thereof in the Treatment of Cardiovascular Disorders
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Paragraph 1652-1654, (2016/05/02)
The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.
RAFAMYCIN ANALOGS AND METHODS FOR MAKING SAME
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Paragraph 0084, (2015/02/25)
A semi-synthetic rapamycin analog with a triazole moiety or a pharmaceutically acceptable salt or prodrug thereof, is a broad-spectrum cytostatic agent and a mTOR inhibitor, and is useful in the treatment of various cancers, or tumors in organs such as kidney, liver, breast, head and neck, lung, prostate, and restenosis in coronary arteries, peripheral arteries, and arteries in the brain, immune and autoimmune diseases. Also disclosed are fungal growth-, restenosis-, post-transplant tissue rejection- and immune- and autoimmune disease-inhibiting compositions and a method of inhibiting cancer, fungal growth, restenosois, post-transplant tissue rejection, and immune and autoimmune disease in a mammal. One particular preferred application of such triazole-moiety containing rapamycin analog is in treating renal carcinoma, lung cancer, colon cancer, and breast cancers wherein potency of the drug, its half-life, tissue distribution properties, and its pharmacokinetic properties including bioavailability through oral and intravenous routes are essential to the clinical outcomes.
SUBSTITUTED OXOPYRIDINE DERIVATIVES AND USE THEREOF IN THE TREATMENT OF CARDIOVASCULAR DISORDERS
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Paragraph 2414-2417, (2016/10/07)
The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.
RAFAMYCIN ANALOGS AND METHODS FOR MAKING SAME
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Paragraph 48, (2014/06/23)
A semi-synthetic rapamycin analog with a triazole moiety or a pharmaceutically acceptable salt or prodrug thereof, is a broad-spectrum cytostatic agent and a m TOR inhibitor, and is useful in the treatment of various cancers, or tumors in organs such as kidney, liver, breast, head and neck, lung, prostate, and restenosis in coronary arteries, peripheral arteries, and arteries in the brain, immune and autoimmune diseases. Also disclosed are fungal growth-, restenosis-, post- transplant tissue rejection- and immune- and autoimmune disease- inhibiting compositions and a method of inhibiting cancer, fungal growth, restenosois, post-transplant tissue rejection, and immune and autoimmune disease in a mammal. One particular preferred application of such triazole-moiety containing rapamycin analog is in treating renal carcinoma, lung cancer, colon cancer, and breast cancers wherein potency of the drug, its half-life, tissue distribution properties, and its pharmacokinetic properties including bioavailability through oral and intravenous routes are essential to the clinical outcomes.
ALKYLATION WITH AN ALKYL FLUOROALKYL SULFONATE
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Page/Page column 22; 23; 24; 25; 26; 28; 29, (2015/01/07)
The present invention discloses a process for preparing a chemical compound comprising reacting a nucleophile with an alkyl fluoroalkyi sulfonate in the presence of a base of formula NR1 R2R3, wherein R1 and R2 are independently 2-methylpropyl or isopropyl and R3 is - CH(R4)(R5), wherein R4 and R5 are identical or different alkyls that are optionally connected to form a ring. The invention also relates to a process for preparing an alkyl fluoroalkyi sulfonate. The invention further relates to a use of the base in a chemical reaction comprising an alkyl fluoroalkyi sulfonate. The process and uses are suitable for preparing chemical compounds, reactants or intermediates thereof, and in particular for preparing API or reactants, like for example everolimus or reactants for its preparation.
Tritium labelling of RAD001 - A new rapamycin derivative
Moenius,Andres,Acemoglu,Kohler,Schnelli,Zueger
, p. 113 - 120 (2007/10/03)
RAD001 2, a new immunosuppressant, was labelled in its hydroxyethyl side chain as well as in the rapamycin skeleton using carrier-free lithium triethylborotritide and tributyltin tritide (TBTT), respectively. The tritium labelling of the rapamycin moiety followed Curran's strategy of intramolecular hydrogen transfer. Our studies demonstrated that base-free TBTT is essential for a successful reaction.
