- Preparation of diaza dioxa dithia crown p-tert-butylcalix[4]arene by S-alkylation reactions: Use of metallo-calix[4]arene complexes as reaction templates
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New nickel-thiolato-calix[4]arene complexes were produced by mean of metal-template synthesis employing S-alkylation of a nickel thiolato complex with a dichloroethyl-or a dibromoethylcalix[4]arene derivative. Demetallation of a nickel-thiolato-calix[4]arene complex resulted in a p-tert-butylcalix[4]arene derivative containing two N-, two O-and two S-donors.
- Tomapatanaget, Boosayarat,Pulpoka, Buncha,Tuntulani, Thawatchai
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Read Online
- LOX INHIBITORS
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The disclosure relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, Formula (I) as defined herein. Compounds according to Formula I are pharmacologically effective as lysyl oxidase (LOX) inhibitors and are believed to be useful in the treatment of, for instance, cancer.
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Paragraph 00379-00382; 00398
(2020/06/05)
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- ALKYNYL-SUBSTITUTED HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF
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The present invention relates to an alkynyl-substituted heterocyclic compound acting as an FGFR inhibitor, a preparation method therefor and a medical use thereof. In particular, the present invention relates to a compound as shown in general formula (I) and a pharmaceutically acceptable salt thereof; a pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof; a method for treating and/or preventing FGFR-associated diseases, particularly tumors, by using the compound or a pharmaceutically acceptable salt thereof; and a preparation method for the compound or a pharmaceutically acceptable salt thereof. The present invention also relates to the use of the compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof in the preparation of a drug for treating and/or preventing FGFR-associated diseases, particularly tumors, wherein the definition of each substituent group in general formula (I) is the same as that in the description.
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Paragraph 0327; 0328; 0329
(2019/07/23)
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- Alkynyl-substituted heterocyclic compound, preparation method therefor and medical use therefor for effectively treating and/or preventing FGFR-related diseases such as tumors
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The present invention relates to an alkynyl-substituted heterocyclic compound serving as an FGFR inhibitor, a preparation method therefor and a medical use therefor. In particular, the present invention relates to a compound represented by the general formula (I) and its pharmaceutically acceptable salt, a pharmaceutical composition including the compound or its pharmaceutically acceptable salt, a method for treating and/or preventing FGFR-related diseases, particularly tumors, by using the compound or its pharmaceutically acceptable salt, and a preparation method of the compound or its pharmaceutically acceptable salt. The present invention also relates to an use of the compound or its pharmaceutically acceptable salt, or an pharmaceutical composition including the compound or its pharmaceutically acceptable salt in the preparation of a drug for treating and/or preventing FGFR-related diseases, particularly tumors, wherein the definition of each substituent in the general formula (I) is the same as that in the specification.
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Page/Page column 89-90
(2020/02/18)
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- SUBSTITUTED AZASPIRO(4.5)DECANE DERIVATIVES
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The invention relates to substituted spirocyclic cyclohexane derivatives which have an affinity for the μ opioid receptor and/or the ORL1 receptor, processes for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.
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Page/Page column 86
(2016/02/10)
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- Synthesis, radiolabeling and evaluation of novel amine guanidine derivatives as potential positron emission tomography tracers for the ion channel of the N-methyl-d-aspartate receptor
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The N-Methyl-d-Aspartate receptor (NMDAR) is involved in many neurological and psychiatric disorders including Alzheimer's disease and schizophrenia. The aim of this study was to develop a positron emission tomography (PET) ligand to assess the bio-availa
- Klein, Pieter J.,Chomet, Marion,Metaxas, Athanasios,Christiaans, Johannes A.M.,Kooijman, Esther,Schuit, Robert C.,Lammertsma, Adriaan A.,Van Berckel, Bart N.M.,Windhorst, Albert D.
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p. 143 - 160
(2016/05/09)
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- Synthesis and Preclinical Evaluation of Three Novel Fluorine-18 Labeled Radiopharmaceuticals for P-Glycoprotein PET Imaging at the Blood-Brain Barrier
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P-Glycoprotein (P-gp), along with other transporter proteins at the blood-brain barrier (BBB), limits the entry of many pharmaceuticals into the brain. Altered P-gp function has been found in several neurological diseases. To study the P-gp function, many positron emission tomography (PET) radiopharmaceuticals have been developed. Most P-gp radiopharmaceuticals are labeled with carbon-11, while labeling with fluorine-18 would increase their applicability due to longer half-life. Here we present the synthesis and in vivo evaluation of three novel fluorine-18 labeled radiopharmaceuticals: 4-((6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)methyl)-2-(4-fluorophenyl)oxazole (1a), 2-biphenyl-4-yl-2-fluoroethoxy-6,7-dimethoxy-1,2,3,4-tetrahydro-isoquinoline (2), and 5-(1-(2-fluoroethoxy))-[3-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-propyl]-5,6,7,8-tetrahydronaphthalen (3). Compounds were characterized as P-gp substrates in vitro, and Mdr1a/b(-/-)Bcrp1(-/-) and wild-type mice were used to assess the substrate potential in vivo. Comparison was made to (R)-[11C]verapamil, which is currently the most frequently used P-gp substrate. Compound [18F]3 was performing the best out of the new radiopharmaceuticals; it had 2-fold higher brain uptake in the Mdr1a/b(-/-)Bcrp1(-/-) mice compared to wild-type and was metabolically quite stable. In the plasma, 69% of the parent compound was intact after 45 min and 96% in the brain. Selectivity of [18F]3 to P-gp was tested by comparing the uptake in Mdr1a/b(-/-) mice to uptake in Mdr1a/b(-/-)Bcrp1(-/-) mice, which was statistically not significantly different. Hence, [18F]3 was found to be selective for P-gp and is a promising new radiopharmaceutical for P-gp PET imaging at the BBB. (Chemical Equation).
- Savolainen, Heli,Cantore, Mariangela,Colabufo, Nicola A.,Elsinga, Philip H.,Windhorst, Albert D.,Luurtsema, Gert
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p. 2265 - 2275
(2015/07/15)
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- 6,7-DIOXYALKYLTETRAHYDROISOQUINOLINE COMPOUNDS
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The present invention relates to a 6,7-dioxyalkyltetrahydroisoquinoline compound, or a salt or solvate thereof according to formula I: (formula I), (I) wherein R represents hydrogen or a fluorinated alkyl group, and R2 and R3 independently represents hydrogen or an alkyl group.
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Page/Page column 10; 11
(2016/08/03)
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- PROCESS FOR PREPARING FLUORINE-CONTAINING ALKOXYALKANE
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A process for preparing a fluorine-containing alkoxyalkane represented by the general formula (1) R1—O—R2—O—R3 where at least one of R1, R2 and R3 contains one or more fluorine atoms. An alcohol with the highest acidity selected from the group consisting of the compounds represented by the general formula (2) R1—OH, the general formula (3) R3—O—R2—OH, the general formula (4) R1—O—R2—OH, and the general formula (5) R3—OH is reacted with at least one selected from the group consisting of the compounds represented by the general formula (6) Lg-R2—O—R3, the general formula (7) Lg-R1, the general formula (8) Lg-R3, and the general formula (9) Lg-R2—O—R1 where Lg represents an anionic leaving group in the presence of a basic compound.
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Page/Page column 8
(2009/01/20)
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- Smiles-type free radical rearrangement of aromatic sulfonates and sulfonamides: Syntheses of arylethanols and arylethylamines
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Smiles-type free radical rearrangements of arenesulfonates and arenesulfonamides are exploited for synthetic purposes. 4-Substituted benzenesulfonates cause Smiles-type rearrangement only when substituted by an electron withdrawing group. Therefore, ipso-sttack by an alkyl radical on arenesulfonates takes place in an electrophilic manner. Arenesulfonamides rearrange only when the amide nitrogen is substituted by an alkoxycarbonyl group, due to the electron withdrawing nature of this group. Sulfonates and the N-ethoxycarbonylsulfonamide derivatives of naphthalene, quinoline, and thiophene cause more rearrangement and show synthetic utility. Aromatic amino acid analogues were synthesized by Smiles-type rearrangement with moderate yields. The radical Smiles-type rearrangement of sulfonate and sulfonamide derivatives can be a useful synthetic route when we understand the electronic character of these reactions.
- Tada, Masaru,Shijima, Hiroyasu,Nakamura, Masaharu
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p. 2499 - 2505
(2007/10/03)
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- Bifunctionalization of α,ω-Sulphonamides via Kinetically Controlled Reaction of α,ω-Bis(N-nitrososulphonamides)
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α,ω-Bis(N-nitrososulphonamides) in hot benzene were converted into α,ω-disulphonates and bifunctional α-sulphonate-ω-sulphonamides, in good yields, by intramolecular N-nitrososulphonamide-sulphonate rearrangement.
- Iwata, Masaaki,Kuzuhara, Hiroyoshi
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p. 918 - 919
(2007/10/02)
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- PARTICIPATION OF SULFONATE IONS IN THE ELECTROPHILIC ADDITION OF HALOGENS TO OLEFINS
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The reactions of ethylene, 1-heptene, cyclohexene, and styrene with chlorine and bromine in methylene chloride and chloroform in the presence of tetrabutylammonium p-toluenesulfonate and tetrabutylammonium methanesulfonate were investigated.In all cases the 2-halogenoalkyl esters of the sulfonic acids were obtained with comparable yields in addition to the 1,2-dihalides.The addition of chlorine and bromine to cyclohexene and also of bromine to 1-heptene in acetic acid in the presence of lithium p-nitrobenzenesulfonate leads to 2-halogenoalkyl esters of the sulfonicacids and acetic acid in addition to the 1,2-dihalides.These data indicate concurrent combination of the sulfonate anions at the concluding stage of AdE reactions.The mechanistic aspects and consequences of this effect are discussed.
- Zefirov, N. S.,Koz'min, A. S.,Dan'kov, Yu. V.,Zhdankin, V. V.,Kirin, V. N.
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p. 205 - 213
(2007/10/02)
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