217488-49-8Relevant articles and documents
C10-ALKYLENE SUBSTITUTED 13-MEMBERED MACROLIDES AND USES THEREOF
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Paragraph 00322, (2020/06/10)
Provided are 13-membered macrolides for the treatment of infectious diseases. The 13-membered macrolides described herein are azaketolides. Also provided are methods for preparing the 13- membered macrolides, pharmaceutical compositions comprising the 13-membered macrolides, and methods of treating infectious diseases, and in particular, disease resulting from Gram negative bacteria using the disclosed macrolides. Formula (I)
QUINAZOLINE COMPOUND FOR EGFR INHIBITION
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Paragraph 0232-0233, (2019/11/21)
Disclosed is a novel quinazoline compound. Specifically, disclosed are a compound represented by the formula (I) and a pharmacologically acceptable salt.
Selective Synthesis of (+)-Dysoline
Coffin, Aaron,Ready, Joseph M.
supporting information, p. 648 - 651 (2019/01/26)
Dysoline, a novel chromone alkaloid isolated from Dysoxylum binectariferum, was reported to have selective cytotoxicity for HT1080 fibrosarcoma cells (IC50 of 0.21 μM). Given the scarcity of natural material, a concise synthesis of (+)-dysoline was developed, allowing for further biological evaluation. An enantioselective nucleophile-catalyzed aldol lactonization formed the piperidine ring with control of relative and absolute stereochemistry. Construction of the C6-chromone core with complete regioselectivity was achieved using a Danheiser benzannulation.
PYRAZOLO[1,5-A]PYRIMIDINE-5,7-DIAMINE COMPOUNDS AS CDK INHIBITORS AND THEIR THERAPEUTIC USE
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, (2015/09/28)
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain pyrazolo[1,5-a]pyrimidine-5,7- diamine compounds (referred to herein as "PPDA compounds") that, inter alia, inhibit (e.g., selectively inhibit) CDK (e.g., CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8, CDK9, CDK10, CDK11, CDK12, CDK13, etc.). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CDK; and to treat disorders including: disorders that are associated with CDK; disorders that result from an inappropriate activity of a cyclin-dependent kinase (CDK); disorders that are associated with CDK mutation; disorders that are associated with CDK overexpression; disorders that are associated with upstream pathway activation of CDK; disorders that are ameliorated by the inhibition of CDK; proliferative disorders; cancer; viral infections (including HIV); neurodegenerative disorders (including Alzheimer's disease and Parkinson's disease); ischaemia; renal diseases; and cardiovascular disorders (including atherosclerosis). Optionally, the treatment further comprises treatment (e.g., simultaneous or sequential treatment) with a further active agent which is, e.g., an aromatase inhibitor, an anti-estrogen, a Her2 blocker, a cytotoxic chemotherapeutic agent, etc.
Synthesis and in vitro antibacterial activity of quinolone/naphthyridone derivatives containing 3-alkoxyimino-4-(methyl)aminopiperidine scaffolds
Lv, Kai,Wu, Jinwei,Wang, Jian,Liu, Mingliang,Wei, Zengquan,Cao, Jue,Sun, Yexin,Guo, Huiyuan
, p. 1754 - 1759 (2013/04/10)
We report herein the synthesis of a series of 7-[3-alkoxyimino-4-(methyl) aminopiperidin-1-yl]quinolone/naphthyridone derivatives. In vitro antibacterial activity of these derivatives was evaluated against representative strains, and compared with ciprofl
Structure-based design and synthesis of macroheterocyclic peptidomimetic inhibitors of the aspartic protease β-site amyloid precursor protein cleaving enzyme (BACE)
Hanessian, Stephen,Yang, Gaoqiang,Rondeau, Jean-Michel,Neumann, Ulf,Betschart, Claudia,Tintelnot-Blomley, Marina
, p. 4544 - 4567 (2007/10/03)
Based on the X-ray cocrystal structure of the Tang-Ghosh heptapeptide inhibitor 1 (OM00-3), a series of macroheterocyclic analogues were designed and synthesized. Analogues containing dithia, dioxa, oxathia, and carbathia macrocycles were synthesized by m
Enzyme-catalyzed kinetic resolution of piperidine hydroxy esters
Solymar, Magdolna,Forro, Eniko,Fueloep, Ferenc
, p. 3281 - 3287 (2007/10/03)
Enantiomers of N-protected piperidine-based cis- and trans-4-hydroxy-3- carboxylates and cis-3-hydroxy-4-carboxylates were prepared through kinetic resolution utilizing lipase AK from Pseudomonas fluorescens and Candida antarctica lipase A. The highly enantioselective (E >200) kinetic resolution of (±)-ethyl cis-(±)-4 and trans-1-(tert-butoxycarbonyl)-4- hydroxypiperidine-3-carboxylate (±)-5 was achieved by Pseudomonas fluorescens lipase-catalyzed asymmetric acylation with vinyl acetate in diisopropyl ether at room temperature. Candida antarctica lipase A-catalyzed asymmetric acylation of (±)-ethyl cis-1-benzyl-3-hydroxypiperidine-4- carboxylate (±)-11 was performed with vinyl propanoate in diisopropyl ether at 3°C, with good enantioselectivity (E = 75).
Reagents for assaying central local acetylcholinesterase activity
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, (2008/06/13)
The present invention relates to N-alkylpiperidine derivatives represented by general formula (1) or (2); wherein R1represents optionally fluorinated lower alkyl; R2represents lower alkyl; and R3represents alkenyl substituted at the 1-position with hydroxy, lower alkoxy, lower alkoxyalkyloxy, lower alkoxyalkyloxyalkyloxy, or lower alkanoyloxy and substituted at the end with radioactive iodine, or alkenyloxymethyl substituted at the end with a radioactive iodine reagent containing the same for assaying central local AchE activity; a method for assaying the central local AchE activity; and labeled precursors of the above compounds. After easily passing through the blood-brain barrier, these compounds are hydrolyzed specifically by AchE in the brain into alcohols, which are then captured by the brain. In contrast, alcohols formed outside the brain do not migrate into the brain. The compounds of the invention emit γ-rays at an appropriate energy level. These characteristics make the compounds highly useful as tracers for SPECT in assaying the central AchE activity.
Synthesis of N-methyl-3-acetoxy-4-(1-hydroxy-3-[123I]iodoprop-2-enyl) piperidine, a novel acetylcholine analog
Ueda,Irie,Fukushi,Ikota,Namba,Shinotoh,Iyo,Tanada,Maeda,Takatoku,Yomoda,Nagatsuka
, p. S762-S764 (2007/10/03)
Lipophilic acetylcholine analogs (N-methylpiperidine derivatives) have been used to map central acetylcholinesterase (AchE) activity in animals and humans. In the former meeting, we reported synthesis of an analog with 4-acetoxy group and side chain at 3-position labeled with iodine-123 (MHIP4A) which showed moderate metabolic clearance. Now, we have synthesized another analog with higher metabolic clearance, namely, N-methyl-3-acetoxy-4-(1-hydroxy-3-[123I]iodoprop-2-enyl)piperidine (HIP3C3A). Eight isomers of HIP3C3A were isolated by diastereomeric and enantiomeric separation with silica gel chromatography and chiralcel HPLC. Tributylstannyl precursors were used for iodination with peracetic acid as an oxidizing agent. The iodination could be carried out quite easily yielding 50-60%. Of the isomers, one isomer showed extremely high metabolic clearance (4.19 mL/min/g with 84% specificity) and another isomer was hydrolyzed by AchE moderately (0.36 mL/min/g with 95% specificity) in rat cerebral cortical homogenate.
A study of baker's yeast reduction of piperidone-carboxylates
Willert, Marianne,Bols, Mikael
, p. 461 - 468 (2007/10/03)
The stereoselective baker's yeast reduction of various N-protected piperidone-carboxylic acids have been studied, and the enantioselectivity was found to be widely dependent on whether fermenting or non-fermenting conditions were employed. Thus reaction o