- Design, synthesis, and biological evaluation of pyridineamide derivatives containing a 1,2,3-triazole fragment as type II c-Met Inhibitors
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A series of 4-(pyridin-4-yloxy)benzamide derivatives containing a 1,2,3-triazole fragment were designed, synthesized, and their inhibitory activity against A549, HeLa, and MCF-7 cancer cell lines was evaluated. Most compounds exhibited moderate to potent antitumor activity against the three cell lines. Among them, the promising compound B26 showed stronger inhibitory activity than Golvatinib, with IC50 values of 3.22, 4.33, and 5.82 μM against A549, HeLa, and MCF-7 cell lines, respectively. The structure-activity relationships (SARs) demonstrated that the modification of the terminal benzene ring with a single electron-withdrawing substituent (fluorine atom) and the introduction of a pyridine amide chain with a strong hydrophilic group (morpholine) to the hinge region greatly improved the antitumor activity. Meanwhile, the optimal compound B26 showed potent biological activity in some pharmacological experiments in vitro, such as cell morphology study, dose-dependent test, kinase activity assay, and cell cycle experiment. Finally, the molecular docking simulation was performed to further explore the binding mode of compound B26 with c-Met.
- Xiong, Hehua,Cheng, Jianxin,Zhang, Jianqing,Zhang, Qian,Xiao, Zhen,Zhang, Han,Tang, Qidong,Zheng, Pengwu
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- Picolinamide compound containing triazole or quinolinone structure and application of picolinamide compound
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The invention provides a picolinamide compound containing a triazole or quinolinone structure and application of the picolinamide compound. According to a technical scheme in the invention, extensiveresearch is conducted on the picolinamide compound, and
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- Design, synthesis and biological evaluation of 4-(pyridin-4-yloxy)benzamide derivatives bearing a 5-methylpyridazin-3(2H)-one fragment
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A series of 4-(pyridin-4-yloxy)benzamide derivatives bearing a 5-methylpyridazin-3(2H)-one fragment were designed, synthesized, and evaluated for their biological activity. Most compounds showed effective inhibitory activity against cancer cell lines of A
- Duan, Yongli,Tang, Qidong,Xiong, Hehua,Zhang, Han,Zhang, Jianqing,Zhang, Qian,Zheng, Pengwu
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- Preparation and application of 2-pyridine carboxamide compound
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The invention relates to a 2-pyridine carboxamide derivative as shown in a formula I, and pharmaceutically acceptable salt, hydrate, solvate and prodrug thereof. Substituents R1, R2, X and Y have themeanings given in the description. The invention further relates to a compound in the general formula I, and the compound has the strong inhibition effect on FLT-3; the invention further relates to the applications of the compound, and the pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof to preparation of drugs for treating diseases caused by abnormal high expression of FLT-3kinase, especially the applications to preparation of drugs for treating and/or preventing cancers.
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- DIPHENYL DERIVATIVES AND USES THEREOF
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The present disclosure provides a compound of formula (I): or a pharmaceutically acceptable salt thereof, and its therapeutic uses for activating a growth factor pathway, promoting wound healing, promoting tissue repair, and treating hearing loss, skeletal muscle loss, organ degeneration, tissue damage, neurodegeneration, and muscular atrophy. The disclosure further provides pharmaceutical compositions and combinations. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.
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Paragraph 1241
(2019/03/30)
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- RAF-DEGRADING CONJUGATE COMPOUNDS
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The present disclosure provides, inter alia, RAF-Degrading Conjugate Compounds that are useful in the treatment of cancer and other RAF related diseases. Also provided are, pharmaceutical compositions, methods of treatment, and kits comprising a RAF- Degrading Conjugate Compound.
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Paragraph 0209; 0211
(2018/11/22)
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- Synthesis method of 2-pyridylaldehyde derivative
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The invention relates to the field of medical intermediates, in particular to a synthesis method of 2-pyridylaldehyde derivative. A synthesis path shown in the formula 1 is adopted, wherein X can be Cl or Br or CF3. Cheap starting raw materials are adopted, the use of hazardous materials which have large toxicity and are easily explosive is avoided, the cost of the product is greatly lowered, popularization and industrialized production are facilitated, and the synthesis method has the advantages of being low in cost, easy to operate, high in yield, easy to industrialize and the like. The formula 1 is shown in the description.
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Paragraph 0067-0071; 0084-0086
(2018/09/28)
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- SUBSTITUTED PYRIDINE COMPOUNDS AS CRAC MODULATORS
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The present invention relates to compounds described herein Formula (I) and pharmaceutical acceptable salts thereof, which modulate the activity of calcium release- activated calcium (CRAC) channel. The invention also describes the compounds of Formula (I)and pharmaceutical compositions containing such compounds thereof for treating, managing, and/or lessening the severity of diseases, disorders, syndromes or conditions associated with the modulation of calcium release-activated calcium (CRAC) channel.
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Page/Page column 48
(2013/11/19)
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- Use of Metal Complex Compounds as Oxidation Catalysts
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The present invention relates to the use, as oxidation catalysts, of metal complex compounds having tetradentate ligands of formula (2) wherein all substitutents have the meanings as defined in Claim 1. The present invention relates also to formulations comprising such metal complex compounds, to novel metal complex compounds and to novel ligands.
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- PYRIDINE OR PYRIMIDINE DERIVATIVE HAVING EXCELLENT CELL GROWTH INHIBITION EFFECT AND EXCELLENT ANTI-TUMOR EFFECT ON CELL STRAIN HAVING AMPLIFICATION OF HGFR GENE
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A pyridine or pyrimidine derivative represented by the formula (I) has an excellent HGFR inhibitory activity and exhibits strong cell proliferation inhibitory effect and anti-tumor effect against cancer cell lines with amplified HGFR gene. wherein R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents -CH=, nitrogen.
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Page/Page column 41
(2009/12/05)
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- AZETIDINES AND CYCLOBUTANES AS HISTAMINE H3 RECEPTOR ANTAGONISTS
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The invention relates to compounds of formula (I) wherein R, R0, R1, m, n and X1 to X4 have the meaning as cited in the description and the claims. Said compounds are useful as Histamine H3 receptor antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
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Page/Page column 77-78
(2010/01/29)
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- NOVEL PYRIDINE DERIVATIVE AND PYRIMIDINE DERIVATIVE (3)
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A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity and cancer metastasis inhibitory activity. [R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents -CH=, nitrogen or the like.]
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Page/Page column 43
(2008/06/13)
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- Use of metal complex compounds as catalysts for oxidation using molecular oxygen or air
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Use, as a catalyst for oxidation reactions using molecular oxygen and/or air, of at least one metal complex compound of formula (1) wherein Me is manganese, titanium, iron, cobalt, nickel or copper, X is a coordinating or bridging radical, n and m are each independently of the other an integer having a value of from 1 to 8, p is an integer having a value of from 0 to 32, z is the charge of the metal complex, Y is a counter-ion, q=z/(charge of Y), and L is a ligand of formula (2) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are each independently of the others hydrogen; unsubstituted or substituted C1-C18alkyl or aryl; cyano; halogen; nitro; —COOR12 or —SO3R12 wherein R12 is in each case hydrogen, a cation or unsubstituted or substituted C1-C18alkyl or aryl; —SR13, —SO2R13 or —OR13 wherein R13 is in each case hydrogen or unsubstituted or substituted C1-C18alkyl or aryl; —NR14R15; —(C1-C6alkylene)-NR14R15; —N(+)R14R15R16; —(C1-C6alkylene)-N(+)R14R15R16; —N(R13)—(C1-C6alkylene)-NR14R15; —N[(C1-C6alkylene)-NR14R15]2; —N(R13)—(C1-C6alkylene)-N(+)R14R15R16; —N[(C1-C6alkylene)-N(+)R14R15R16]2; —N(R13)—N—R14R15 or —N(R13)N″R14R15R16, wherein R13 is as defined above and R14, R15 and R16 are each independently of the other(s) hydrogen or unsubstituted or substituted C1-C18alkyl or aryl, or R14 and R15, together with the nitrogen atom linking them, form an unsubstituted or substituted 5-, 6- or 7-membered ring which may contain further hetero atoms. [in-line-formulae][LnMemXp]zYq??(1) [/in-line-formulae]
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Page/Page column 19
(2010/02/15)
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- IL-12 MODULATORY COMPOUNDS
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The invention relates to heterocyclic compounds, compositions including the compounds and methods of using and methods of making thereof. The compounds (and compositions) are useful, inter alia, in modulating IL-12 production and processes mediated by IL-
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Page/Page column 179
(2010/11/30)
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- Identification of chemokine receptor CCR4 antagonist
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The present study reports the identification and hits to leads optimization of chemokine receptor CCR4 antagonists. Compound 12 is a high affinity, non-cytotoxic antagonist of CCR4 that blocks the functional activity mediated by the receptor.
- Purandare, Ashok V.,Gao, Aiming,Wan, Honghe,Somerville, John,Burke, Christine,Seachord, Carrie,Vaccaro, Wayne,Wityak, John,Poss, Michael A.
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p. 2669 - 2672
(2007/10/03)
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