- Derivative containing nitrogen heterocyclic rings and application of derivative in retinal neovascularization diseases
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The invention discloses a derivative containing nitrogen heterocyclic rings and application of the derivative in retinal neovascularization diseases. The derivative has the biological structural formula shown in the description, wherein R1, R2, R3 and R4 are respectively and independently selected from -H or -CN. Under the same concentration of 5microg/mL, the growth inhibition ratios of the embodiment II, the embodiment III and the embodiment IV to HRCEC are superior to a monoclonal antibody drug Avastin. By injecting the compound into a vitreous body, the formation of pathologic new vesselscan be reduced, so that the derivative of the formula I or the salt of the derivative can be used for deeply researching and developing retinal neovascularization relevant diseases such as retinal vein occlusion, proliferative diabetic retinopathy, subretinal neovascular membrane, neovascular glaucoma, retinopathy of prematurity and proliferative vitreoretinopathy.
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Paragraph 0021-0024
(2018/12/02)
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- Nitrogen heterocycle containing derivatives and application thereof in retinal diseases
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The invention discloses nitrogen heterocycle containing derivatives and an application thereof in retinal diseases. The nitrogen heterocycle containing derivatives have a structural formula which is described in the specification. In the structural formula, R1, R2, R3 and R4 are independently selected from the group consisting of -H and -F. The nitrogen heterocycle containing derivatives providedby an embodiment 1, an embodiment 2, an embodiment 3 and an embodiment4 of the invention have an HRCEC proliferation inhibition rate superior to the HRCEC proliferation inhibition rate of a monoclonalantibody medicine namely Avastin at the same concentration of 5 [mu]g/mL. According to the invention, after intravitreal injection administration, a compound provided by the invention can reduce pathological neovascularization; thus, the nitrogen heterocycle containing derivatives with a formula I or salts thereof provided by the invention are proved to be able to be used for in-depth research and development for treatment of retinal neovascularization related diseases, such as retinal vein occlusion, proliferative diabetic retinopathy, subretinal neovascular membrane, neovascular glaucoma, retinopathy of prematurity, proliferative vitreoretinopathy, etc.
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Paragraph 0022; 0023; 0024
(2019/01/07)
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- BiCl3: A versatile catalyst for the tetrahydropyranylation and depyranylation of 1°,2°,3°, allylic, benzylic alcohols, and symmetric diols
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Bismuth trichloride as mild reagent, has been found to be a worthful catalyst for tetrahydropyranylation of 1°,2°,3°, allylic, benzylic alcohols, and symmetric di-ols. At room temperature the reagent THP(3,4-dihydro-2H-pyran) was successfully employed as pyranylating agent in presence of BiCl3catalyst without the use of a solvent and the yields of the products were found to be 90-96%. Further, the depyranylation of alcohols was achieved in quantitative yield by simple addition of MeOH using the same catalyst. The developed method was showed good chemo-selectivity in symmetrical diols for mono THP protection.
- Vijaya Durga,Balamurali Krishna,Baby Ramana,Santha Kumari,Vijay,Hari Babu
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p. 1030 - 1034
(2017/05/26)
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- Multi-gram synthesis of a porphyrazine platform for cellular translocation, conjugation to Doxorubicin, and cellular uptake
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We report the synthesis of the near infrared (NIR) fluorescent porphyrazine (Pz) 285, with pendant hydroxyl groups, as a non-toxic platform for delivery of conjugated chemotherapeutic agents to tumor cells. Conjugation of Pz 285 to Doxorubicin via an acid
- Trivedi, Evan R.,Blumenfeld, Carl M.,Wielgos, Todd,Pokropinski, Sharon,Dande, Prasad,Hai, Ton T.,Barrett, Anthony G.M.,Hoffman, Brian M.
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supporting information
p. 5475 - 5478
(2013/01/13)
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- AI(OTf)3 - A highly efficient catalyst for the tetrahydropyranylation of alcohols under solvent-free conditions
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A simple and highly efficient method has been developed for the tetrahydropyranylation of alcohols by their reaction with 3,4-dihydro-2H-pyran (DHP) using a catalytic amount (0.01-1 mol%) of aluminium triflate under solvent-free conditions. The effect of various factors like temperature, amount of the catalyst, and molar ratio of substrates on the reaction conditions has also been studied. The comparative study of tetrahydropyranylation of benzyl alcohol using various catalysts including some reported ones shows the efficiency of this catalyst.
- Kamal, Ahmed,Naseer A Khan,Srikanth,Srinivasa Reddy
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scheme or table
p. 1099 - 1104
(2009/03/11)
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- Phosphorus pentoxide as an efficient catalyst for the tetrahydropyranylation of alcohols under solvent-free conditions
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A facile and efficient method for the preparation of tetrahydropyranyl ethers from alcohols is improved in solvent-free media. These reactions are catalyzed by P2O5 and afford various tetrahydropyranyl ethers in shorter reaction time, with good to excellent yields (75-95%) at room temperature. This method is also compatible with substrates containing acid-sensitive functional groups.
- Eshghi, Hossein,Shafieyoon, Parvaneh
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p. 2149 - 2152
(2007/10/03)
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- Network single ion conductors based on comb-branched polyepoxide ethers and lithium bis(allylmalonato)borate
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The synthesis of network single ion conductors to obtain single ion conductors with high ambient temperature conductivity and mechanical strength is discussed. The single ion conductors were based on comb-branched polyepoxide ethers and lithium (Li) bis(allylmelonato)borate. The single ion conductors possessed good mechanical strength due to the formation of network structure and the Li/Li symmetric cell cycling showed no concentration polymerization. The results show that the backbone structure of the polyepoxides contributes to the total ionic conductivity and it increases with the increasing side chain length.
- Sun, Xiao-Guang,Kerr, John B.,Reeder, Craig L.,Liu, Gao,Han, Yongbong
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p. 5133 - 5135
(2007/10/03)
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- Oligonucleotide analogs with an amino acid or a modified amino alcohol residue
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The present invention provides various novel oligonucleotide analogs having one or more properties that make the subject compounds superior to conventional oligonucleotides for use in procedures employing oligonucleotides. The compounds of the invention are oligonucleotide analogs in which the furanose ring of a naturally occurring nucleic acid is replaced with an amino acid or a modified amino alcohol residue. Some embodiments of the novel compounds of the invention are particularly useful for the antisense control of gene expression. The compounds of the invention may also be used as nucleic acid hybridization probes or as primers. Another aspect of the invention is to provide monomeric precursors of the oligonucleotide analogs of the invention. These monomeric precursors may be used to synthesize the subject polynucleotide analogs. Another aspect of the invention is to provide formulations of the subject polynucleotide analogs that are designed for the treatment or prevention of disease conditions. Yet another aspect of the invention is to provide methods for treating or preventing diseases, particularly viral infections and cell growth disorders. The subject disease treatment methods comprise the step of administering an effective amount of the subject polynucleotide analogs for use as antisense inhibitors.
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- Lithium tetrafluoroborate-in acetonitrile (LTAN) catalyzed Ferrier rearrangement - Facile synthesis of alkyl 2,3-unsaturated glycopyranosides?
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Treatment of 3,4-dihydro-2H-pyran 1 with various alcohols 2 - 10 furnished the tetrahydropyranyl ethers 11 - 19 in the presence of lithium tetrafluoroborate in acetonitrile (LTAN).
- Babu, B. Sobhana,Balasubramanian
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p. 1261 - 1262
(2007/10/03)
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- Mild and efficient tetrahydropyranylation of alcohols-catalysis by lithium perchlorate in diethyl ether
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Treatment of 3,4-dihydro-2H-pyran 1 with various alcohols 2 - 10 furnished the tetrahydropyranyl ethers 11 - 19 in the presence of 5M lithium perchlorate in diethyl ether (5M LPDE), which is essentially a neutral medium.
- Babu, Boga Sobhana,Balasubramanian, Kalpattu Kuppuswamy
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p. 9287 - 9288
(2007/10/03)
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- Envirocat EPZG as a new heterogenous catalyst for the solvent-free tetrahydropyranylation of alcohols and phenols
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Envirocat EPZG was used as a solid supported acid catalyst for tetrahydropyranylation of alcohols and phenols in the absence of a solvent. This new method is rapid, efficient and convenient giving the corresponding products in high yields and purity.
- Bandgar,Jagtap,Aghade,Wadgaonkar
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p. 2211 - 2215
(2007/10/02)
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- Intramolecularly alkylated Costa complexes: New models for coenzyme B12 with a cobalt-to-ligand carbon bridge
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The synthesis of Costa-type B12 models 1 with a carbon bridge between the equatorial ligand and cobalt has been accomplished by condensation of butanedione monoxime and 2-(ω-functionalized)alkyl-1,3-diaminopropanes 8 followed by complexation with Co(II), introduction of a leaving group and intramolecular alkylation via Co(I) intermediates. The solution structure of intramolecularly alkylated Costa complexes with a bridge of two (1a) or of three (1b) methylene groups was investigated by NMR spectroscopy and compared with that of propyl(iodo) Costa complex 13.
- Van Arkel, Bert,Van Der Baan, Juul L.,Balt, Sijbe,Bickelhaupt, Friedrich,De Bolster, Martinus W. G.,Klumpp, Gerhard W.
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p. 4161 - 4172
(2007/10/02)
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- Neutral Ligands with Surfactant-Type Structure - Synthesis, Complexation, and Ion Transfer
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New lipophilic neutral ligands which combine crown ether and podand characteristics with structural features of surfactants (cf. formulas 1-12, 16-26) were synthesized.Their complexation behaviour was studied, their solid-to-liquid and liquid-to-liquid phase transfer properties as well as their efficiency in ion transport across a liquid model membrane.Crystalline stoichiometric complexes of the cycles 2a-4a and of 3e with NaSCN, Ba(SCN)2, and BaI2 can be isolated.Among the noncyclic representatives a crystalline complex is obtained only from 11 with BaI2.The ligand 8d behaves in aqueous solution as a typical surfactant showing micelle formation and cloud point.
- Weber, Edwin
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p. 770 - 801
(2007/10/02)
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