- AXL INHIBITOR FORMULATIONS
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Formulations of Compound 1 or a pharmaceutically acceptable salt thereof are described. Also disclosed are capsules having a dry blended powder comprising Compound 1 or a pharmaceutically acceptable salt thereof. The Compound 1 or a pharmaceutically accep
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Paragraph 195-196
(2021/04/10)
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- Controlled synthesis of N, N-dimethylarylsulfonamide derivatives as nematicidal agents
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Gramine can be intelligently and efficiently supplied with N, N-dimethylamino group and then reacted with the corresponding sulfonyl chlorides to synthesize N, N-dimethylarylsulfonamides. We herein designed and controlled synthesis of N, N-dimethylarylsulfonamide derivatives, and first reported the results of the nematicidal activity of 15 title compounds 3a-o against Meloidogyne incongnita in vitro, respectively. Among all of the title derivatives, compounds 3a, 3c, 3k, and 3o exhibited potent nematicidal activity with median lethal concentration (LC50) values ranging from 0.22 to 0.26 mg/L. Most noteworthy, N, N-dimethyl-4-methoxyphenylsulfonamide (3c) and N, N-dimethyl-8-quinolinesulfonamide (3o) showed the best promising and pronounced nematicidal activity, with LC50 values of 0.2381 and 0.2259 mg/L, respectively.
- Chen, Gen-Qiang,Xia, Yan-Fei,Yang, Jin-Ming,Che, Zhi-Ping,Sun, Di,Li, Shen,Tian, Yue-E,Liu, Sheng-Ming,Jiang, Jia,Lin, Xiao-Min
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p. 1197 - 1206
(2019/12/03)
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- AXL KINASE INHIBITORS AND USE OF THE SAME
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Tartrate salts of the compound of structure (I), crystalline forms thereof, and therapeutic applications thereof for treating solid tumors (e.g., advanced solid tumor) or hematopoietic cancers. Also provided herein are methods for synthesizing the tartrat
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Page/Page column 162
(2019/10/29)
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- Preparation method of N,N-dimethylsulfamide derivatives
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The invention discloses a preparation method of N,N-dimethylsulfamide derivatives and belongs to the technical field of synthesis of medical compounds. The preparation method comprises the following steps: reacting gramine, a reactant with sulfonyl chloride groups and an alkaline substance with any one of solvents such as CH2Cl2, CH3COCH3 and CH3CN at a temperature of minus 15 DEG C to 80 DEG C for 24-48 hours so as to obtain the product, wherein the molar ratio of the gramine to the reactant to the alkaline substance is (1.0-2.0):(1.2-4.0):(1.5-6.0). The N,N-dimethylsulfamide derivatives can be simply and efficiently prepared withlow cost, and the yield is up to 70-98%.
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Paragraph 0101-0105; 0171
(2019/10/01)
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- INHIBITORS OF CYCLIN DEPENDNT KINASE 7 (CDK7)
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The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
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Paragraph 618
(2018/02/28)
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- Compound used as ALK (anaplastic lymphoma kinase) inhibitor and application thereof
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The invention discloses a compound shown in a formula I, and pharmaceutically acceptable salts, stereoisomers, solvates or predrugs. The symptoms are defined in claim requirements. The compound shownin the formula I has good inhibiting activity on ALK (anaplastic lymphoma kinase), and can be used for preparing medicines for adjusting the activity of the ALK activity or treating the ALK-related diseases, especially nonsmall-cell lung cancer drugs. (The formula I is shown in the attached figure.).
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Paragraph 0243; 0245; 0246; 0247
(2018/11/04)
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- POLYCYCLIC ANAPLASTIC LYMPHOMA KINASE INHIBITOR
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Provided is a polycyclic inhibitor of anaplastic lymphoma kinase as represented by Formula (I), or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R1, R2, R3, R4, and ring A are as defined in the description. The invention also relates to a method for preparing the compound, a pharmaceutical preparation and a pharmaceutical composition comprising the compound, and use of the compound, the pharmaceutically acceptable salt or stereoisomer thereof in manufacture of a medicament for the treatment and/or prevention of an anaplastic lymphoma kinase-mediated cancer or non-cancer related diseases.
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Paragraph 0144; 0145
(2018/02/06)
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- Of tetracyclic Anaplastic lymphoma kinase inhibitors (by machine translation)
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The invention belongs to the field of medical technology, in particular to general formula (I) as shown in of tetracyclic Anaplastic lymphoma kinase inhibitor, its pharmaceutically acceptable salt or a stereoisomer thereof, wherein R 1, R 2, R 3, R 4, R 5 and A link like defined in the specification. The invention also relates to methods of preparing such compounds, pharmaceutical preparations comprising these compounds and pharmaceutical composition, the compound and, its pharmaceutically acceptable salts or stereoisomers thereof, in the preparation of the treatment and/or prevention of Anaplastic lymphoma kinase-mediated cancer diseases related to the application of the medicament. (by machine translation)
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Paragraph 0258; 0259; 0260
(2016/10/08)
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- COMPOUNDS AND METHODS FOR INDUCING CHONDROGENESIS
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Described herein are compounds and compositions for the amelioration of arthritis or joint injuries by inducing mesenchymal stem cells into chondrocytes.
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Paragraph 0764; 0765
(2014/09/29)
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- PYRAZOLES USEFUL IN THE TREATMENT OF INFLAMMATION
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There is provided compounds of formula (I), wherein R1, R2, X1, X2 and n have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a lipoxygenase (e.g. 15-lipoxygenase) is desired and/or required, and particularly in the treatment of inflammation.
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Page/Page column 47
(2008/06/13)
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- ARYLGLYCINE DERIVATIVES FOR USE AS GLYCINE TRANSPORT INHIBITORS
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The present invention relates to compounds of Formula (I) and salts solvates and hydrates thereof. The invention further relates to pharmaceutical compositions containing said compounds and methods of treating neurological and neuropsychistric disorders using said compounds.
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Page 101; 102
(2010/02/06)
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- N-(phenylsulfonyl)picolinamide derivatives, process for producing the same, and herbicide
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A herbicide containing as the active ingredient an N-(henylsulfonyl)picolinamide derivative represented by general formula (I) wherein X reprcsents a halogeno, a C1-4 alkyl, a C1-4 haloalkyl, a C1-4 alkoxy, a C1-4 haloalkoxy, a (C1-4 alkoxy)carbonyl, a [di(C1-4 alkyl)amino]sulfonyl, an [N—(C1-4 alkyl)-N—(C1-4 alkoxy)amino]sulfonyl, a (C1-4 alkylamino)sulfonyl, a C1-4 alkylthio, a C1-4 alkylsulfinyl, a C1-4 alkylsulfonyl, or nitro; n is an integer of 0 to 5; Y represets a halogeno, a C1-4 alkyl, a C1-4 haloalkyl, a C1-4 alkoxy, C1-4 haloalkoxy, a C1-4 alkylthio, a C1-4 haloalkylthio, amino, a C1-4 alkylamino, a di(C1-4 alkyl)amino, a (C1-4 alkoxy) C1-4 alkyl, a (C1-4 alkylthio) C1-4 alkyl, or nitro; and m is an integer of 0 to 4. This active ingredient is synthesized by condensing a substituted picolinic acid with a substituted benzenesulfonamide under dehydration, or by reacting the phenyl ester of a substituted picolinic acid with a substituted benzenesulfonamide in the presence of a basic compound.
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- Azo coupling of o- and p-(dialkylaminosulfonyl)benzene-diazonium salts with 7-acetylamino-4-hydroxynaphthalene-2-sulfonic acid in citrate-phosphate buffer solution
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Dependences of the partial rate constants for azo coupling of o-(dialkylaminosulfonyl)benzene-diazonium salts with 7-acetylamino-4-hydroxynaphthalene-2-sulfonic acid (N-Acetyl-I-acid) on the fraction of the dianionic form of the latter indicate considerable steric hindrances to the second stage of the reaction. Ionization of the hydroxy group of N-acetyl-I-acid gives rise to additional electrostatic repulsion at the stage of formation of the σ complex, which reduces the rate of azo coupling at the 3-position of orthanilic acid.
- Kornev,Zheltov
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p. 962 - 968
(2007/10/03)
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- N.M.R. Spectroscopic and X-Ray Crystallographic Studies on some o-NO2 Substituted Aromatic Sulphur Amides
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Solid state 13C c.p.-m.a.s. and solution 13C, 15N, 14N, and 17O n.m.r. spectra have been measured for N,N-dimethyl-o-nitrobenzenesulphenamide, o-nitrobenzenesulphenamide, and N,N-dimethyl-o-nitrobenzenesulphonamide.The 13C c.p.-m.a.s. n.m.r. resonance sig
- Ruostesuo, Pirkko,Haekkinen, Anna-Maija,Kivekaes, Raikko,Sundberg, Markku R.
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p. 1397 - 1404
(2007/10/02)
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