41489-76-3Relevant academic research and scientific papers
PYRROLOBENZODIAZEPINE DIMER PRECURSOR AND LIGAND-LINKER CONJUGATE COMPOUND THEREOF
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Paragraph 0136; 0137, (2020/02/18)
The present invention relates to a pyrrolobenzodiazepine dimer prodrug and a ligand-linker conjugate compound thereof, a composition containing these, and therapeutic use thereof particularly as an anticancer drug. The stability of the compounds themselves and the stability thereof in plasma are excellent and the compounds are advantageous in terms of manifestation of toxicity, and thus the compounds are industrially useful in that it is possible to target proliferative diseases such as cancer, to perform a specific treatment, to maximize the drug efficacy, and to minimize the occurrence of side effects.
Anti-tumor compound as well as preparation method and application thereof
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Paragraph 0062; 0063; 0064; 0065, (2019/01/21)
The invention belongs to the technical field of medicines and in particular relates to an anti-tumor compound as well as a preparation method and application thereof. The anti-tumor compound providedby the invention has a molecular structure shown as a fo
Thiosemicarbazone Dynamic Combinatorial Chemistry: Equilibrator-Induced Dynamic State, Formation of Complex Libraries, and a Supramolecular On/Off Switch
Larsen, Dennis,Jeppesen, Anne,Kleinlein, Claudia,Pittelkow, Michael
, p. 8580 - 8589 (2017/08/23)
Dynamic combinatorial libraries that equilibrate under thermodynamic control and can be trapped kinetically when desired are key to creating complex systems that can mimic dynamic biological systems, such as the biochemical system of life. A much-sought-after feature is the ability to turn off the dynamic exchange of the system, in order to investigate a transient state away from thermodynamic equilibrium, and then turn on the dynamic exchange again. We describe here the first use of thiosemicarbazone exchange to form dynamic combinatorial libraries. The libraries were found to require a nucleophilic catalyst, or equilibrator, in order to reach thermodynamic equilibrium. This equilibrator approach adds a supramolecular level of control over the dynamic system and allows the dynamic exchange to be turned off by addition of 18-crown-6, which binds the equilibrator in a nonnucleophilic complex. The dynamic exchange can be restarted by addition of potassium ions that competitively bind 18-crown-6, thus liberating the equilibrator. The highly complex thiosemicarbazone-based macrocyclic libraries contain both [2]catenanes and sequence isomers, which can be distinguished by HPLC-MS/MS.
Synthesis of salicylaldehydes from phenols via copper-mediated duff reaction
Fu, Xue-Wen,Pu, Wen-Chen,Zhang, Guo-Lin,Wang, Chun
, p. 8147 - 8158 (2015/02/19)
A copper-mediated Duff reaction for ortho-selective formylation of phenols has been developed. In the presence of copper species, significant improvements of yield and ortho-selectivity of the Duff formylation were achieved, which provides an easy access to salicylaldehydes from phenols.
1-PHENYL-2-PYRIDINYL ALKYL ALCOHOL DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS
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Paragraph 0632; 0633, (2014/06/23)
Compounds of formula (I) described herein are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and are useful for the prevention and/or treatment of an allergic disease state or a disease of the respiratory tract characterized by airway obstruction.
POLYMERIZABLE CHIRAL COMPOUND, POLYMERIZABLE LIQUID CRYSTAL COMPOUND, LIQUID CRYSTAL POLYMER AND OPTICALLY ANISOTROPIC BODY
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Paragraph 0258, (2013/03/26)
The present invention is to provide a novel polymerizable chiral compound (chiral agent) having high left-handed helical twisting power, a polymerizable liquid crystal composition comprising the polymerizable chiral compound and a polymerizable liquid crystal compound, a liquid crystal polymer, and an optically anisotropic body. The object was achieved by a left-handed-helix-inducing polymerizable chiral compound represented by the following formula (I), a polymerizable liquid crystal composition comprising the polymerizable chiral compound and a polymerizable liquid crystal compound, a liquid crystal polymer and an optically anisotropic body: wherein X represents the following formula (X-i) or (X-ii) wherein * represents a bond: wherein Y1 to Y6 are each one selected from the group consisting of —O—, —S—, —O—C(═O)—, —C(═O)—O— and so on; Yx is one selected from the group consisting of —C(═O)—, —O—C(═O)—, —CH═CH—C(═O)—, —CH2— and so on; Yz is one selected from the group consisting of —C(═O)—, —C(═O)—O—, —C(═O)—CH═CH— and so on; G1 and G2 are each a divalent aliphatic group which has 1 to 20 carbon atoms and which may have a substituent; Z1 and Z2 are each an alkenyl group which has 2 to 10 carbon atoms and which may be substituted by a halogen atom; Q1 to Q4 are each a hydrogen atom or an alkyl group which has 1 to 6 carbon atoms and which may have a substituent; A1 to A6 are each a divalent organic group having 1 to 30 carbon atoms; and a and b are each 0 or 1.
Studies on benzofuran-7-carboxamides as poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors
Lee, Sunkyung,Yi, Kyu Yang,Lee, Byung Ho,Oh, Kwang Seok
scheme or table, p. 1147 - 1153 (2012/07/14)
Benzofuran-7-carboxamide was identified as a novel scaffold of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor. A series of compounds with various 2-substituents including (tertiary amino)methyl moieties substituted with aryl ring and aryl groups containing tertiary amines, were synthesized and biologically evaluated to elucidate the structure-activity relationships and optimize the potency. 2-[4-(Pyrrolidin-1-ylmethyl)phenyl]-benzofuran-7- carboxamide (42) was the most potent as an IC50 value of 40 nM among those.
POLYMERIZABLE CHIRAL COMPOUND, POLYMERIZABLE LIQUID CRYSTALLINE COMPOSITION, LIQUID CRYSTALLINE POLYMER, AND OPTICAL ISOMER
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Page/Page column 22, (2011/06/26)
The present inventions to provide a novel polymerizable chiral compound (chiral agent) having high helical twisting power, a polymerizable liquid crystal composition comprising the polymerizable chiral compound and a polymerizable liquid crystal compound,
NOVEL COMPOUNDS
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Page/Page column 79, (2011/04/25)
The present invention discloses novel compounds inhibiting LRRK2 kinase activity, the preparation processes thereof, the compositions containing them, as well as the use in treating diseases characterized by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.
POLYMERIZABLE LIQUID CRYSTAL COMPOUND, POLYMERIZABLE LIQUID CRYSTAL COMPOSITION, LIQUID CRYSTALLINE POLYMER, AND OPTICALLY ANISOTROPIC MATERIAL
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Page/Page column 29, (2010/01/29)
A polymerizable liquid crystal compound shown by the following formula (I), a polymerizable liquid crystal composition that includes the polymerizable liquid crystal compound and a chiral compound polymerizable with the polymerizable liquid crystal compou
