- Magnetic Field Dependent Reaction Yields from Radical Ion Pairs Linked by a Partially Rigid Aliphatic Chain
-
The electron donor-acceptor compound pyrene-(CH2)3-cyclohexane-(CH2)3-dimethylaniline, abbreviated as Py3(C6)3DMA, has been investigated.Photoinduced electron transfer leads to the singlet radical ion pair Py-3(C6)3DMA+.An extraordinary large and distinct magnetic field effect is observed in the yield of the locally excited triplet state of the pyrene moiety, the recombination product of the triplet radical ion pair.The half-width of the "J-resonance" maximum in the magnetic field dependent triplet yield curve is just 66 G, corresponding to 7.7*10-7 eV or 6.2*10-3 cm-1.This is due to the influence of the rigid trans-cyclohexane part in the aliphatic chain, which leads to a reduced intramolecular mobility and to a narrow probability distribution of the radical ion pair distance, as predicted by Monte-Carlo computer simulations.The magnetic field dependence of the triplet generation is further transmitted to secondary reactions like triplet-triplet annihilation, thus leading to a magnetic field dependent delayed fluorescence and to a delayed excimer fluorescence.
- Werner, Udo,Kuehnle, Wolfgang,Staerk, Hubert
-
-
Read Online
- Discovery of Hydroxyamidine Derivatives as Highly Potent, Selective Indoleamine-2,3-dioxygenase 1 Inhibitors
-
In this study, a series of novel hydroxyamidine derivatives were identified as potent and selective IDO1 inhibitors by structure-based drug design. Among them, compounds 13-15 and 18 exhibited favorable enzymatic and cellular activities. Compound 18 showed improved bioavailability in mouse, rat, and dog (F% = 44%, 58.8%, 102.1%, respectively). With reasonable in vivo pharmacokinetic properties, compound 18 was further evaluated in a transgenic MC38 xenograft mouse model. The combination of compound 18 with PD-1 monoclonal antibody showed a synergistic antitumor effect. These data indicated that compound 18 as a potential cancer immunotherapy agent should warrant further investigation.
- Jin, Fangfang,Hu, Qiyue,Fei, Hongbo,Lv, Hejun,Wang, Shenglan,Gui, Bin,Zhang, Junzhen,Tu, Wangyang,Zhang, Yun,Zhang, Lei,Wan, Hong,Zhang, Limin,Hu, Bin,Yang, Fanglong,Bai, Chang,He, Feng,Zhang, Lianshan,Tao, Weikang
-
supporting information
p. 195 - 201
(2021/02/06)
-
- BIS-BENZIMIDAZOLE COMPOUNDS AND METHODS OF USING SAME
-
Provided herein are compounds and methods for modulating abnormal repeat expansions of gene sequences. More particularly, provided are inhibitors of RNA and the uses of such inhibitors in regulating nucleotide repeat expansions, e.g., to treat Myotonic Dystrophy Type 1 (DM1 ), Myotonic Dystrophy Type 2 (DM2), Fuchs dystrophy, Huntington Disease, Amyotrophic Lateral Sclerosis, or Frontotemporal Dementia.
- -
-
Paragraph 00752-00754
(2019/06/05)
-
- Preparation method of trans-1,4-cyclohexane dicarboxylic acid monomethyl ester
-
The invention discloses a preparation method of trans-1,4-cyclohexanedicarboxylic acid monomethyl ester. The preparation method comprises the following steps of using cis and trans mixed type dimethyl1,4-cyclohexanedicarboxylate with better solvent property in organic solvents as the raw material, performing isomerization reaction under the catalyzing action of an organic alkaline catalyst, and performing high-selectivity monoester hydrolyzing under the action of inorganic alkaline, so as to obtain the trans-1,4-cyclohexanedicarboxylic acid monomethyl ester. Compared with the prior art, the preparation method has the advantages that (1) the used raw material has good dissolvability in the organic solvent, such as methyl alcohol; (2) by adopting the optimized catalyst, the activating energy of the isomerization reaction is reduced, the isomerization time is shortened, the reaction energy consumption is decreased, the cost is reduced, and the optimized catalyst is suitable for industrialized production; (3) the hydrolyzing of diester is effectively reduced, the amount of diacid byproducts is reduced to be 2% or lower, and the product purity is improved; (4) a small amount of unreacted raw material is sent into an organic phase via an extracting procedure, and is separated from the product at high efficiency, so that the purity of the product is further improved.
- -
-
Paragraph 0027-0041
(2018/07/06)
-
- Polymerizable compound, composition, polymer, an optically anisotropic material, an organic EL element and a liquid crystal display element
-
An object of the invention is to provide polymerizable compounds having excellent optical characteristics and suited as materials for optically anisotropic articles, compositions containing the polymerizable compounds, polymers obtained by polymerizing th
- -
-
Paragraph 0133; 0134
(2016/10/10)
-
- TRICYCLIC PYRROLOPYRIDINE COMPOUND, AND JAK INHIBITOR
-
To provide a novel tricyclic pyrrolopyridine compound having a JAK inhibitory activity and useful for prevention, treatment and/or improvement of particularly autoimmune diseases, inflammatory diseases and allergic diseases. A novel tricyclic pyrrolopyridine compound represented by the formula (I), a tautomer or pharmaceutically acceptable salt of the compound or a solvate thereof: wherein the respective substituents are defined in detail in the specification, and R1 is a C1-6 alkyl group or the like, R2 is a hydrogen atom or the like, R3 is a hydrogen atom or the like, the ring A is C3-11 cycloalkane or the like, L1 is a C1-6 alkylene group or the like, and R4 is NRaRb or the like.
- -
-
Paragraph 0171; 0172
(2016/01/01)
-
- HETEROCYCLIC COMPOUNDS AS DGAT1 INHIBITORS
-
The present invention relates to heterocyclic compounds of formula 1, in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, solvates, polymorphs, prodrugs, carboxylic acid isosteres and N-oxides. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.
- -
-
-
- NITROGENOUS FUSED BICYCLIC COMPOUND
-
A novel nitrogenous fused bicyclic compound represented by the following general formula [1] or a pharmacologically acceptable salt of the compound. They have excellent SK channel blocking activity and are useful as a medicine. [I] (In the formula, R 0 represents hydrogen, halogeno, etc.; R 1 represents a group represented by the formula (a) or (b); A represents a group represented by the formula (X) or (Y); D 1 , D 2 and D 3 each represents N or CH; R 2 represents halogeno or optionally halogenated lower alkyl, etc.; R 3 represents hydrogen or lower alkyl; and Q represents lower alkylene.)
- -
-
Page/Page column 55
(2010/11/26)
-
- FUSED FURAN COMPOUND
-
The present invention provides a condensed furan compound of the formula (I): wherein Ring X is benzene, pyridine, or the like; Y is an optionally substituted amino, an optionally substituted cycloalkyl, an optionally substituted aryl, an optionally substituted saturated heterocyclic group, an optionally substituted unsaturated heterocyclic group; A is a single bond, lower alkylene, lower alkenylidene, lower alkenylene or an oxygen atom; R3 is hydrogen or the like; and , R4 is hydrogen, or the like, or pharmaceutically acceptable salts thereof, which is useful as a medicament, particularly, as an activated blood coagulation factor X inhibitor.
- -
-
Page/Page column 116
(2008/06/13)
-
- Design, Synthesis, and Biological Evaluation of Substituted 2-Cyclohexyl-4-phenyl-1H-imidazoles: Potent and Selective Neuropeptide Y Y5-Receptor Antagonists
-
Antagonizing the robust stimulation of food intake by neuropeptide Y represents a new potential therapeutic approach for the treatment of obesity. Earlier pharmacological studies have pointed to the Y1 and Y5 receptors as the most likely mediators of the
- Blum, Charles A.,Zheng, Xiaozhang,De Lombaert, Stéphane
-
p. 2318 - 2325
(2007/10/03)
-
- SUBSTITUTED 2-CYCLOHEXYL-4-PHENYL-1H-IMIDAZOLE DERIVATIVES
-
Substituted 2-cyclohexyl-4-phenyl-1H-imidazole derivatives capable of modulating NPY5 receptor activity, are provided. Such compounds may be used to modulate NPY binding to NPY5 receptors in vivo or in vitro, and are particularly useful in the treatment o
- -
-
-
- Separation of cis/trans-cyclohexanecarboxylates by enzymatic hydrolysis: Preference for diequatorial isomers
-
4-Substituted cis/trans-cyclohexanecarboxylates have been separated into the isomers by enzymatic hydrolysis with lipase from Candida rugosa with very good selectivity. The enzyme preferentially recognizes diequatorial conformations. Copyright (C) 1996 Elsevier Science Ltd.
- Koenigsberger, Kurt,Luna, Hector,Prasad, Kapa,Repic, Oljan,Blacklock, Thomas J.
-
p. 9029 - 9032
(2007/10/03)
-
- SELECTIVE MONOMETHYL ESTERIFICATION OF DICARBOXYLIC ACIDS BY USE OF MONOCARBOXYLATE CHEMISORPTION ON ALUMINA.
-
The application of alumina as a solid support affords a new procedure for selective reactions. Although it is difficult to obtain monoesters in the esterification of dicarboxylic acids by conventional methods, dicarboxylic acids adsorbed on alumina selectively form the monoesters. Terephthalic acid (1), isophthalic acid, cis- and trans-1,4-cyclohexanedicarboxylic acids, and aliphatic dicarboxylic acids give the corresponding monomethyl esters quantitatively with diazomethane. On the basis of these results, the authors suggest that dicarboxylic acids are adsorbed on alumina through one of their carboxyl groups, and the carboxyl group not adsorbed on the alumina is esterified selectively. Selective monomethyl esterification of phthalic acid is not successful on alumina, probably as a consequence of the close proximity of the two carboxyl groups and the forced orientation of the second group when one is adsorbed.
- Ogawa,Chihara,Taya
-
p. 1365 - 1369
(2007/10/02)
-
