- Ultralow-Molecular-Weight Stimuli-Responsive and Multifunctional Supramolecular Gels Based on Monomers and Trimers of Hydrazides
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The simpler, the better. A series of simple, neutral and ultralow-molecular-weight (MW: 140–200) hydrazide-derived supramolecular gelators have been designed and synthesized in two straightforward steps. For non-conjugated cyclohexane-derived hydrazides, their monomers can self-assemble to form gels through intermolecular hydrogen bonds and dipole-dipole interactions. Significantly, conjugated phthalhydrazide can self-aggregate into planar and circular trimers through intermolecular hydrogen bonds and then self-assemble to form gels through intermolecular π–π stacking interactions. It is interesting that these simple gelators exhibit unusual properties, such as self-healing, multi-response fluorescence, and visual and selective recognition of chiral (R)/(S)-1,1′-binaphthalene-2,2′-diamine and S2? through much different times of gel re-formation and blue-green color change, respectively. These results underline the importance of supramolecular gels and extend the scope of supramolecular gelators.
- Wu, Dehua,Song, Jintong,Qu, Lang,Zhou, Weilan,Wang, Lei,Zhou, Xiangge,Xiang, Haifeng
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supporting information
p. 3370 - 3378
(2020/10/02)
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- NOVEL 5 OR 8-SUBSTITUTED IMIDAZO [1, 5-a] PYRIDINES AS INDOLEAMINE AND/OR TRYPTOPHANE 2, 3-DIOXYGENASES
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Disclosed herein are 5 or 8-substituted imidazo[l,5-a]pyridines and pharmaceutical compositions comprising at least one such 5 or 8-substituted imidazo[l,5-a]pyridines, processes for the preparation thereof, and the use thereof in therapy. Disclosed herein are certain 5 or 8- substituted imidazo[l,5-a]pyridines that can be useful for inhibiting indoleamine 2,3- dioxygenase and/or tryptophane 2,3-dioxygenase and for treating diseases or disorders mediated thereby.
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Paragraph 0542
(2016/10/31)
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- BENZAMIDE IMIDAZOPYRAZINE BTK INHIBITORS
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Provided are Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I, pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, or their use in therapy.
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Page/Page column 122
(2016/07/27)
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- Cis-Dichlorido(3,6,9-trithiabicyclo[9.3.1]pentadecane-κ2 S 3,S 6)palladium(II) acetonitrile 0.8-solvate
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In the title complex, [PdCl2(C12H22S 3)]·0.8CH3CN, a potentially tridentate thioether ligand coordinates in a cis-bidentate manner to yield a square-planar environment for the PdII cation [mean deviation of the Pd from the Cl2S2 plane = 0.0406 (7) A]. Each square-planar entity packs in an inverse face-to-face manner, giving pairs with plane-to-plane separations of 3.6225 (12) A off-set by 1.1263 (19) A, with a Pd...Pd separation of 3.8551 (8) A. A partial acetonitrile solvent molecule is present. The occupancy of this molecule was allowed to refine, and converged to 0.794 (10). The synthesis of the previously unreported 3,6,9-trithiabicyclo[9.3.1]pentadecane ligand is also outlined.
- Dawe, Louise Nicole,Penney, Lisa,Black, Daniel A.,Miller, David O.,Lucas, C. Robert
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p. 727 - 729
(2013/07/26)
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- BICARBOCYCLIC AND TRICARBOCYCLIC ETHYNYL DERIVATIVES AND USES OF SAME
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The present invention provides compounds of formula (1): where R1, R2, X. Y and n are as described herein, and pharmaceutical compositions, uses and methods comprising same.
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Page/Page column 23
(2013/03/28)
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- BICYCLO[3.2.1]OCTYL AMIDE DERIVATIVES AND USES OF SAME
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The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; pharmaceutical compositions and methods using the same.
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Page/Page column 24
(2012/07/13)
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- Pyridine derivatives
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Pyridine compounds of general formula: wherein —R1represents in which R11is hydrogen, C1-6alkyl, halogen, hydroxy, C1-12alkoxy, nitro, amino, C1-6alkylsulfonylamino, C1-6alkoxycarbonyl, C1-6alkylamino, di(C1-6alkyl)amino, C1-6alkanoylamino, phenyl C1-6alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2represents hydrogen or halogen; R3represents hydrogen, —CR31R32R33, or —NR34R35; R4is hydrogen, carbamoyl, CN, carboxyl, etc.; R5is amino, C1-6alkylamino, di C1-6alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.
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- Method for hydrogenating benzene polycarboxylic acids or derivatives thereof by using a catalyst containing macropores
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A process for hydrogenating a benzenepolycarboxylic acid or a derivative thereof or a mixture of two or more thereof by bringing the benzenepolycarboxylic acid or the derivative thereof or the mixture of two or more thereof into contact with a hydrogen-containing gas is carried out in the presence of a catalyst which comprises as active metal at least one metal of transition group VIII of the Periodic Table alone or together with at least one metal of transition group I or VII of the periodic table applied to a support which contains macropores with the proviso that if dimethyl terephthalate is hydrogenated, the hydrogenation using a catalyst which comprises as active metal ruthenium either alone or together with at least one metal of transition group I, VII or VIII of the Periodic Table applied to a support, where the support has a mean pore diameter of at least 50 nm and a BET surface area of at most 30 m2/g and the amount of the active metal is from 0.01 to 30% by weight, based on the total weight of the catalyst, and the ratio of the surface areas of the active metal and the catalyst support is less than 0.05, and/or a catalyst which comprises as active metal ruthenium either alone or together with at least one metal of transition group I, VII or VIII of the Periodic Table in an amount of from 0.01 to 30% by weight, based on the total weight of the catalyst, applied to a support, where from 10 to 50% of the pore volume of the support is formed by macropores having a pore diameter in the range from 50 nm to 10,000 nm and from 50 to 90% of the pore volume of the support is formed by mesopores having a pore diameter in the range from 2 to 50 nm, where the sum of the pore volumes adds up to 100%, is excluded, and novel hydrogenation products, obtainable by hydrogenating benzenepolycarboxylic acid (derivatives) as well as their use as plasticizers in plastics.
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- Preparation of [2.2]-para-, meta-, and orf/ro-cyclophanes containing a 1, 3-cyclohexano group
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[2.2]-para-, ineta-, and o/7/w-CycIophanes containing a 1, 3-cyclohexane ring bridged with two carbons were prepared through a coupling reaction to form dithiacyclophane, followed by oxidation to yield the sulfone and then pyrolysis.
- Lin, Shaw-Tao,Yang, Fu-May,Liang, David W.
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p. 1725 - 1729
(2007/10/03)
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- Thiazolidinone compounds and composition for angina pectoris comprising the compounds as an active ingredient
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A thiazolidinone compound represented by general formula (I) or a pharmacoligically acceptable salt thereof, STR1 wherein W represents sulfur or oxygen and X represents --N(R1)--, or alternatively X represents sulfur or oxygen and W represents --N(R1)--, and R1 represents hydrogen, alkyl or substituted alkyl; R2 and R3 are the same or different from each other, and each represents hydrogen, alkyl, substituted alkyl, aryl, or 5- or 6-membered heteroaryl; R4 represents hydrogen, alkyl or substituted C1 -C4 alkyl; R5 represents substituted cycloalkyl which may contain nitrogen, provided the substituents include --B--ONO2 (wherein B represents a single bond or alkylene) as the indispensable member and alkyl groups as optional members; and A represents a single bond or alkylene, has an excellent anti-anginal effect and thus is useful as an angina pectoris remedy or preventive.
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- Bridgehead Carbocations: Solvolysis of a Series of 5-Substituted Bicycloheptyl Bromides. Nucleophilic Solvent Assistance to Ionization of 1-Bromobicycloheptane
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The synthesis of a range of 5-substituted bicycloheptyl bromides for solvolytic studies is described.It is found that the substituent has a profound effect on the rate of solvolysis of the system and acts principally in accordance with the magnitude of its inductive/field constant ?I.The most spectacular example of the effect of the substituent is provided by the COOMe group which leads to a retardation in the rate of methanolysis by a factor of 6.5E5.While a linear relationship in the plot of log k and ?I is generally obeyed, as expected for a mechanism mediated by the bicycloheptyl bridgehead cation, two of the bromides, 1-bromobicycloheptane and its 5-methoxy derivative, show deviant behaviour and react more rapidly than predicted on the basis of the Hammett plot.Evidence is presented to show that the enhanced rate of the parent is the result of nucleophilic assistance by the solvent.Anchimeric assistance in the solvolysis of 5-methoxybicycloheptyl bromide is attributed to the powerful p-donor property of the methoxy substituent which stabilizes the transition state in a unique concerted ring-opening and ionization step.
- Della, Ernest W.,Elsey, Gordon M.
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p. 967 - 986
(2007/10/02)
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- 1,2-Bridged Cyclopropenes
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The dehalogenations of 1,5-dihalobicyc1o[3.1.0]hexanes and 1,6-dihalobicyclo[4.1.0]heptanes have been studied in solution and in the gas phase. The solution reactions led to the formation of bicyclo[3.1.0]hex-1(5)-ene and bicyclo-[4.1.0]hept-1(6)-ene, res
- Wiberg, Kenneth B.,Artis, Dean R.,Bonneville
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p. 7969 - 7979
(2007/10/02)
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- Remote Enzyme-Coupled Amine Release
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A remote enzyme-coupled amine release system has been developed in which biochemical and chemical "demasking" processes are sequentially linked via an enforced 1,3-diaxial disposition.Thus, pig liver esterase hydrolyzes an ester to an acid, and the acid promotes a fast intramolecular cleavage of an amide to an amine.The sequence has potential pharmacokinetic relevance because it allows enzyme-specific discharge of amine-based drugs following their trans-membrane journey as uncharged amides.
- Menger, F. M.,Ladika, M.
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p. 3006 - 3007
(2007/10/02)
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- Reaction of Aliphatic Dicarboxylic Acids with Acyl Chlorides in the Presence of Aluminum Chloride
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The treatment of succinic acid with lauroyl or stearoyl chloride gave the five-membered β-diketone (II) substituted with a long chain at the α-position, together with a trimer (III) of the acyl chloride.Bicyclononane-2,4-dione (VI) substituted with a methyl or ethyl group at the C3-position was prepared from cyclohexane-1,3-dicarboxylic acid (V) and propionyl or butyryl chloride, respectively.D-Camphoric acid afforded an unexpected product, 4-acyl-2,2,3-trimethyl-3-cyclopentenecarboxylic acid (IX), on reaction with acyl chloride.Although acetyl chloride gave no product on treatment with succinic acid, it afforded 3-acetylbicyclooctane-2,4-dione (XI), 3-acetylbicyclononane-2,4-dione (VId), and 2-acetylcyclohexane-1,3-dione (XII) on reaction with the corresponding dicarboxylic acids.Keywords - β-diketone; cyclic β-diketone; bicyclic β-diketone; dicarboxylic acid; aluminum chloride; acyl chloride; bicycloalkane-2,4-dione
- Matoba, Katsuhide,Tachi, Masashi,Itooka, Toshiyuki,Yamazaki, Takao
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p. 2007 - 2012
(2007/10/02)
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- Synthesis of Bridgehead-Bridgehead Substituted Bicycloalkanes
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A convenient synthetic route to several bicycloalkanes bearing substitution at both bridgehead positions is described.The two-step procedure, which involves alkylation of the monoenolates of readily available cyclohexane diesters with 1,2-dihaloethane followed by a base-inducted cyclization of the derived haloethylated product, was successfully applied to the synthesis of dimethyl bicyclooctane-1,4-dicarboxylate, dimethyl bicycloheptane-1,4-dicarboxylate and dimethyl bicyclooctane-1,5-dicarboxylate.Additionally, it was found that the two latter diesters could be obtained in quite acceptable yields in a one-pot procedure through their corresponding cyclohexyl bisenolate precursors.
- Della, Ernest W.,Tsanaktsidis, John
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p. 1705 - 1718
(2007/10/02)
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- Regioselectivity in cycloaddition reactions on solid phases
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A 1percent crosslinked divinylbenzene-styrene copolymer, incorporating benzyl acrylate groups, reacted in normal Diels-Alder reactions with E-1-phenyl-1,3-butadiene or methyl E-2,4-pentadienoate to give their respective polymer-bound benzyl cyclohexenecarboxylates.Polymer-bound benzyl propiolate and polymer-bound benzyl phenylpropiolate reacted with benzonitrile oxide in a typical 1,3-dipolar addition reaction to give their respective polymer-bound isoxazoles.Cleavage of the polymer-bound Diels-Alder adducts and the polymer-bound 1,3-dipolar addition adduct derived from polymer-bound benzyl propiolate gave mixtures of ortho and meta regiomers similar to those produced in analogous reactions in solution.Cleavage of the polymer-bound 1,3-dipolar addition adduct, derived from polymer-bound benzyl phenylpropiolate, followed by esterification, gave a solitary adduct, 4-carbomethoxy-3,5-diphenylisoxazole, but an analogous solution 1,3-dipolar addition yielded a 1:1 ratio of the two possible regiomers.
- Yedidia, Varda,Leznoff, Clifford C.
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p. 1144 - 1150
(2007/10/02)
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