- ARYL HETEROCYCLIC COMPOUNDS AS KV1.3 POTASSIUM SHAKER CHANNEL BLOCKERS
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A compound of Formula (I), or a pharmaceutically-acceptable salt thereof, is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.
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Paragraph 0467-0468
(2021/04/17)
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- Preparation process of 3,5-dichloro-2-iodoanisole
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The invention relates to a preparation process of 3,5-dichloro-2-iodoanisole. The preparation process comprises the following steps: sequentially adding 3,5-dichlorophenol and an organic solvent into a container, adding alkali at low temperature, carrying out uniform stirring, then recovering the temperature of a system to room temperature, performing stirring and reacting for quantitative time, slowly adding iodine at low temperature, gradually recovering to room temperature, conducting stirring overnight, quenching a reaction with acid, adding ethyl acetate for extraction, combining organic layers to obtain an intermediate product 3,5-dichloro-2-iodophenol, sequentially adding 3,5-dichloro-2-iodophenol, alkali and an organic solvent into the container, adding a methylation reagent, carrying out stirring for a reaction overnight under the condition of nitrogen protection, pouring reaction liquid into ice water, adding an organic solvent for extraction, and finally combining organic layers to obtain the final product 3, 5-dichloro-2-iodoanisole. The method is mild in reaction conditions, low in raw material price and free of dangerous goods, and has great advantages when being put into large-batch production.
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Paragraph 0034-0040; 0046-0052; 0058-0064
(2021/11/06)
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- NLRP3 INFLAMMASOME INHIBITORS
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The present invention relates to novel pyridazin-3-yl phenol compounds of Formula (I): wherein R1, R2, R3, R4, R5 and Z are defined herein, which inhibit NOD-like receptor protein 3 (NLRP3) inflammaso
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Paragraph 0713-0714
(2020/12/04)
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- Regioselective iodination of chlorinated aromatic compounds using silver salts
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The iodination of chlorinated aromatic compounds using Ag 2SO4/I2, AgSbF6/I2, AgBF4/I2, and AgPF6/I2 offers access to iodoarenes that are valuable intermediates in organic synthesis. Specifically, iodination of phenols, anisoles, and anilines with a 3,5-dichloro substitution pattern preferentially yielded the ortho, para, and para iodinated product, respectively. In the case of chlorobenzene and 3-chlorotoluene, AgSbF6/I2, AgBF4/I2, and AgPF 6/I2, but not Ag2SO4/I2, selectively introduced the iodine in para position to the chlorine substituent.
- Joshi, Sudhir N.,Vyas, Sandhya M.,Wu, Huimin,Duffel, Michael W.,Parkin, Sean,Lehmler, Hans-Joachim
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scheme or table
p. 7461 - 7469
(2011/10/10)
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- BENZODIAZEPINE COMPOUNDS USEFUL FOR THE TREATMENT OF HEPATITIS C
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The invention concerns benzodiazepine derivatives of Formula (I): wherein X, L1, L2, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment or prophylaxis of hepatitis C virus infection.
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Page/Page column 40
(2011/12/14)
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- Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1h- pyrazol-1-yl)ethoxy]-6-methylphenyl}-n-(2,2-difluoropropyl)-5, 7-dihydro-6h-pyrrolo[3,4-d]pyrimidine-6-carboxamide
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Figure Presented. A novel class of heat shock protein 90 (Hsp90) inhibitors was discovered by high-throughput screening and was subsequently optimized using a combination of structure-based design, parallel synthesis, and the application of medicinal chemistry principles. Through this process, the biochemical and cell-based potency of the original HTS lead were substantially improved along with the corresponding metabolic stability properties. These efforts culminated with the identification of a development candidate (compound 42) which displayed desired PK/PD relationships, significant efficacy in a melanoma A2058 xenograft tumor model, and attractive DMPK profiles.
- Zehnder, Luke,Bennett, Michael,Meng, Jerry,Huang, Buwen,Ninkovic, Sacha,Wang, Fen,Braganza, John,Tatlock, John,Jewell, Tanya,Zhou, Joe Zhongxiang,Burke, Ben,Wang, Jeff,Maegley, Karen,Mehta, Pramod P.,Yin, Min-Jean,Gajiwala, Ketan S.,Hickey, Michael J.,Yamazaki, Shinji,Smith, Evan,Kang, Ping,Sistla, Anand,Dovalsantos, Elena,Gehring, Michael R.,Kania, Robert,Wythes, Martin,Kung, Pei-Pei
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supporting information; experimental part
p. 3368 - 3385
(2011/06/27)
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- BENZODIAZEPINE DERIVATIVES FOR TREATING HEPATITIS C INFECTION
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The invention concerns benzodiazepine derivatives of Formula (I) wherein W, X, L1, L2, L3, R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment or prophylaxis of hepatitis C virus infection.
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Page/Page column 45
(2011/04/14)
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- BENZODIAZEPINE COMPOUNDS USEFUL FOR THE TREATMENT OF HEPATITIS C
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The invention concerns benzodiazepine derivatives of Formula (I) wherein A, X, L1, L2, R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment or prophylaxis of hepatitis C virus infection.
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Page/Page column 52
(2011/12/14)
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- 2-AMINO PYRIMIDINE COMPOUNDS AS POTENT HSP-90 INHIBITORS
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The present invention is directed to compounds of formula (I), or pharmaceutically acceptable salts thereof, their synthesis, and their use as HSP-90 inhibitors.
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Page/Page column 20
(2010/03/04)
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- S1P RECEPTORS MODULATORS
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The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.
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Page/Page column 54
(2010/04/30)
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- 2-AMINO PYRIDINE COMPOUNDS
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The present invention is directed to 2-aminopyrimidine compounds and pharmaceutically acceptable salts thereof, their synthesis and their use as HSP-90 inhibitors.
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Page/Page column 50
(2008/12/05)
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- 2-AMIN0-5, 7-DIHYDR0-6H- PYRROLO [3, 4-D] PYRIMIDINE DERIVATIVES AS HSP-90 INHIBITORS FOR TREATING CANCER
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The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, their synthesis, and their use as HSP-90 inhibitors.
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Page/Page column 76
(2008/12/08)
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