- Hetero-aromatic compound and its use in medicine
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The invention provides a hetero-aromatic compound or a stereisomer, geometric isomer, tautomer, despinner, nitrogen oxide, hydrate, solvate, metabolite, metabolism precursor and pharmaceutically acceptable salt or prodrug thereof, which is used for treating proliferative diseases. The invention also discloses a pharmaceutical composition containing the compound and an application of the compound or pharmaceutical composition thereof in preparation of a medicine for treating proliferative diseases.
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Paragraph 0989; 1006-1007
(2019/07/04)
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- PYRIDO[1,2-a]PYRIMIDONE DERIVATIVES AS A mTOR/PI3K SUPPRESSOR
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The invention discloses pyrido[1,2-a]pyrimidone derivatives as a mTOR/PI3K suppressor; and in particular, this invention relates to a compound having the formula (I) structure or its pharmaceutically acceptable salts.
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Paragraph 0132; 0133
(2016/10/08)
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- A new strategy for the construction of α-amino acid esters via decarboxylation
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A new α-amino acid esters formation reaction has been developed via decarboxylation. The methodology is distinguished by its practical novelty in terms of the readily accessible starting materials, environmentally benign reaction conditions and waste streams, and wide substrate scope.
- Zhang, Jie,Jiang, Jiewen,Li, Yuling,Zhao, Yun,Wan, Xiaobing
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supporting information
p. 3222 - 3225
(2013/07/26)
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- POSITIVE RESIST COMPOSITION AND PATTERNING PROCESS
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A positive resist composition comprises (A) a resin component which becomes soluble in an alkaline developer under the action of an acid and (B) an acid generator. The resin (A) is a polymer comprising recurring units containing a non-leaving hydroxyl group represented by formula (1) wherein R1 is H, methyl or trifluoromethyl, X is a single bond or methylene, m is 1 or 2, and the hydroxyl group attaches to a secondary carbon atom. The composition is improved in resolution when processed by lithography.
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- Reaction of methyl diazoacetate with amines catalyzed by Ru 2(OAc)4Cl
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Reactions of primary and secondary amines with methyl diazoacetate in the presence of Ru2(OAc)4Cl gave the corresponding N-substituted glycine methyl esters in almost quantitative yield. Catalytic decomposition of methyl diazoacetate
- Maidanova,Bakeeva,Sultanova,Biglova,Dokichev
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experimental part
p. 1461 - 1465
(2011/03/17)
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- N-SUBSTITUTED PIPERIDINE AND PIPERAZINE DERIVATIVES
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This invention relates to compounds of the formula 1 wherein R1, R2, R7, R8, R9, U, V, Z, A, W, X, M, E, L, T and D are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system and other disorders.
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Page/Page column 92
(2010/02/12)
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- Novel tertiary (meth)acrylates having lactone structure, polymers, resist compositions and patterning process
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Novel tertiary (meth)acrylate compounds having a lactone structure are polymerizable into polymers having improved transparency, especially at the exposure wavelength of an excimer laser and dry etching resistance. Resist compositions comprising the polymers are sensitive to high-energy radiation, have a high resolution, and lend themselves to micropatterning with electron beams or deep-UV rays.
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- NK1 and NK3 antagonists
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The invention is to a compound exhibiting neurokinin inhibitory properties, a pharmaceutical composition comprising same and a method of treatment for neurokinin-mediated conditions.
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Page/Page column 27
(2010/02/14)
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- New indium-mediated reactions of enamines
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New reactions of enamines were observed with allyl bromide or methyl bromoacetate in the presence of indium powder in THF, yielding respectively homoallylamines and β-aminoesters.
- Bossard, Fabienne,Dambrin, Valery,Lintanf, Valeie,Beuchet, Pierre,Mosset, Paul
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p. 6055 - 6058
(2007/10/02)
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- Morpholinoalkyl ester prodrugs of diclofenac: Synthesis, in vitro and in vivo evaluation
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Morpholinoalkyl esters (HCl salts) of diclofenac (1) were synthesized and evaluated in vitro and in vivo for their potential use as prodrugs for oral delivery. Prodrugs were freely soluble in simulated gastric fluid (SGF) and pH 7.4 phosphate buffer and showed a minimum of a 2000-fold increase in solubility over the parent drug. All prodrugs were more lipophilic than 1 as indicated by n-octanol/pH 7.4 buffer partition coefficients, but less lipophilic than 1 in terms of n-octanol/SGF partition coefficients. Potentiometrically determined ionization constants (pK(a)s) were in the range of 7.52 to 8.40 at 25 °C. The chemical and enzymatic hydrolyses of prodrugs were evaluated in SGF/pH 7.4 phosphate buffer and rat plasma, respectively, at 37 °C. All prodrugs were quantitatively hydrolyzed to 1 by either chemical and/or enzymatic means. An increase in carbon chain length rendered the prodrugs more stable at pH 7.4, but less stable in SGF. In general, the esters were hydrolyzed rapidly in rat plasma at 37 °C, the half-lives of hydrolysis being in the range of 4.85 to 23.49 min. Based on in vitro results, prodrug 2 was chosen to evaluate solid-state stability, bioavailability, and in vivo ulcerogenicity. At elevated temperatures, the solid-state decomposition of 2 followed biphasic kinetics, with rapid decomposition occurring initially. The extent, but not the rate, of absorption was significantly greater in rats for prodrug 2 than 1 following single dose oral administration. Prodrug 2 was significantly less irritating to gastric mucosa than 1 following single and chronic oral administration in rats.
- Tammara,Narurkar,Crider,Khan
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p. 644 - 648
(2007/10/02)
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