- Total syntheses of N-boc-protected 3′-deoxy-4′-azathymidine and 4′-azauridine
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Novel modified nucleosides 4, 11, ent-11, and 17, wherein the furanose ring oxygen is replaced by nitrogen, have been synthesized by reacting azasugars 3, 10, ent-10, and 15 with silylated uracil or thymine bases.
- Rassu, Gloria,Pinna, Luigi,Spanu, Pietro,Ulgheri, Fausta,Casiraghi, Giovanni
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- INHIBITORS OF APOL1 AND METHODS OF USING SAME
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The disclosure provides at least one entity chosen from compounds of formula (I), solid state forms of the same, compositions comprising the same, and methods of using the same, including use in treating focal segmental glomerulosclerosis (FSGS) and/or non-diabetic kidney disease (NDKD).
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- NOVEL FUNCTIONALIZED LACTAMS AS MODULATORS OF THE 5-HYDROXYTRYPTAMINE RECEPTOR 7 AND THEIR METHOD OF USE
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Pharmaceutical compositions of the invention comprise functionalized lactam derivatives of formula (I) having a disease-modifying action in the treatment of diseases associated with dysregulation of 5- hydroxytryptamine receptor 7 activity. A is selected
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Paragraph 01106
(2019/11/28)
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- Discovery of an 8-aza-5-thiaProstaglandin E1 analog as a highly selective EP4 receptor agonist
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For the purpose of discovering an orally available EP4 subtype-selective agonist, a series of 8-aza prostaglandin E1 (PGE1) analogs were synthesized and evaluated for their affinity for PGE2 receptor subtypes. Additionally
- Kambe, Tohru,Maruyama, Toru,Naganawa, Atsushi,Asada, Masaki,Seki, Akiteru,Maruyama, Takayuki,Nakai, Hisao,Toda, Masaaki
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experimental part
p. 1494 - 1508
(2012/01/13)
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- Asymmetric synthesis of ceramide sphingolipid based on (2S,3S,4S)-3,4- dihydroxy-5-(hydroxymethyl)pyrrolidine lactam
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A facile approach to the versatile chiral building block 2 was developed based on glutamic acid, whereby a new method for asymmetric synthesis of sex pheromone 1 was explored from cheap glutamic acid.
- Huang, Wen-Feng,Li, Qian-Ru,Chao, Lu-Men,Lei, Xin-Sheng,Wei, Bang-Guo
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body text
p. 4317 - 4319
(2010/09/20)
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- BLOOD FLOW PROMOTERS FOR CAUDA EQUINA TISSUES
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It is intended to provide highly safe and efficacious blood flow promoters for cauda equina tissues. Among prostaglandin-like compounds having a weak hypotensive effect, compounds having an effect of promoting the blood flow in cauda equina tissues (excluding limaprost) are useful as highly safe blood flow promoters for cauda equina tissues and , therefore, are efficacious in preventing and/or treating lumbar pain, lower limb pain, lower limb palsy, intermittent claudication, vesicorectal failure, hypogonadism, etc. caused by cauda equina injuries.
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Page/Page column 26
(2010/11/23)
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- Expeditious syntheses of sugar-modified nucleosides and collections thereof exploiting furan-, pyrrole-, and thiophene-based siloxy dienes
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A series of individual sugar-modified pyrimidine nucleosides including enantiomerically enriched 2',3'-dideoxynucleosides 14a-c (α and β anomers of L- and D-series), 2',3'-dideoxy-4'-thionucleosides 21a-c (α and β anomers of L- and D-series), and 2',3'-dideoxy-4'-azanucleosides 28a-c (β anomers of L- and D-series) were synthesized, with uniform chemistry and high stereochemical efficiency, exploiting a triad of versatile heterocyclic siloxy dienes, namely, 2-(tert-butyldimethylsiloxy)furan (TBSOF), 2-(tert- butyldimethylsiloxy)thiophene (TBSOT), and N-(tert-butoxycarbonyl)-2-(tert- butyldimethylsiloxy)pyrrole (TBSOP). The synthetic procedure advantageously used both enantiomers of glyceraldehyde acetonide (D-1 and L-1) as sources of chirality and as synthetic equivalents of the formyl cation. The outlined chemistry also allowed for the rapid assemblage of a 30-member collection of racemic nucleosides (D,L-L) as well as one 15-member ensemble of chiral analogues (L-L), along with some related sublibraries.
- Rassu, Gloria,Zanardi, Franca,Battistini, Lucia,Gaetani, Enrico,Casiraghi, Giovanni
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p. 168 - 180
(2007/10/03)
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- An expeditious and practical synthetic process for phytosphingosine and tetrahydroxy-LCB from D-glutamic acid
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For the asymmetric synthesis of phytosphingosine and 2-amino-1,3,4,5-tetrahydroxyoctadecene, the long chain base (LCB) part of novel cerebrosides, a simple and short synthetic route is described featuring the elabortion of the functionalized homochiral lactam derived from D-glutamic acid as a common structural unit.
- Yoda, Hidemi,Oguchi, Tetsuhiro,Takabe, Kunihiko
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p. 2113 - 2116
(2007/10/03)
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- 12. Approaches to the Synthesis of Cytochalasans; Part 9: A Versatile Concept Leading To All Structural Types of Cytochalasans
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Starting from D-glutamic acid (5), the bicyclic compounds 4a and 4b were synthesized via 17 (Schemes 1 and 2).The reaction leading to 4g and 4h with LiCuPh2 was not successful.But treatment of the N-protected model lactams 19, 21, and 22 with Li2Cu(CN)Ph2 gave the amino ketones 24, 26, and 26, respectively (Scheme 3).The desired compound 23 was obtained from 20.Conversion of the unprotected lactams 28, 31, and 32 gave the phenyl derivative 34 in excellent yields.Ester 35 was transformed to the α-amino-γ-oxo-acid derivative 36.This conversion opens a novel access to this type of compounds.
- Ackermann, Jean,Matthes, Michael,Tamm, Christoph
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p. 122 - 132
(2007/10/02)
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