775331-26-5Relevant articles and documents
INSULIN CONJUGATES
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Paragraph 0611; 0612-0614, (2020/07/05)
The present invention relates to a conjugate comprising a sulfonamide of formula (I) and an active pharmaceutical ingredient such as an insulin analog comprising at least one mutation relative to the parent insulin, wherein the insulin analog comprises a mutation at position B16 which is substituted with a hydrophobic amino acid and/or a mutation at position B25 which is substituted with a hydrophobic amino acid. The present invention further relates to a sulfonamide of formula (A). Moreover, the present invention relates to an insulin analog comprising at least one mutation relative to the parent insulin.
Novel valdecoxib derivatives by ruthenium?II)-promoted 1, 3-dipolar cycloaddition of nitrile oxides with alkynes - Synthesis and COX-2 inhibition activity
Roscales, Silvia,Bechmann, Nicole,Holger Weiss, Daniel,K?ckerling, Martin,Pietzsch, Jens,Kniess, Torsten
supporting information, p. 534 - 544 (2018/03/28)
Novel valdecoxib-based cyclooxygenase-2 inhibitors were synthesized in one step via 1, 3-dipolar cycloaddition of nitrile oxides with a series of eleven aryl alkynes, six of them described for the first time. Application of Ru?II)-catalysis leads preferab
RAFAMYCIN ANALOGS AND METHODS FOR MAKING SAME
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Paragraph 72, (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.