CAS: 147460-41-1; 2-Bromo-5-Fluorophenol

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CAS号348-57-2 2,4-二氟溴苯 | CAS号147460-43-3 2-溴-5-氟硫代苯甲醚 | CAS号450-88-4 2-溴-5-氟苯甲醚 | CAS号199287-75-7 1-bromo-4-fluor... | CAS号954235-83-7 1-溴-2-(二氟甲氧基)-4-氟苯 | CAS号202857-88-3 2-(苄氧基)-1-溴-4-氟苯 | CAS号72216-35-4 3-(苄氧基)氟苯 | CAS号162269-78-5 1-溴-4-氟-2-(甲氧基甲氧基)苯 | CAS号191014-55-8 4-氟-2-甲氧基苯甲腈 | CAS号253429-31-1 4-氟-7-溴苯并呋喃 | CAS号7509-00-4 3-fluorobenzo[c...

2-溴-5-氟苯甲醚置于三溴化硼体系中,用 二氯甲烷 用作溶剂,化学反应生成2-溴-5-氟苯酚
参考文献:鉴定4-(4-硝基-2-苯乙氧基苯基)吡啶是发现人和大鼠11β-羟化酶抑制剂的有前途的新线索
标题:鉴定4-(4-硝基-2-苯乙氧基苯基)吡啶是发现人和大鼠11β-羟化酶抑制剂的有前途的新线索
摘要:11日的抑制β羟化酶是用于治疗库欣综合征,特别是复发和亚临床病例有希望的策略.为在大鼠中获得概念验证,已努力确定抑制人和大鼠cyp11B1的新型先导化合物.对h Cyp11B1,H Cyp11B2和h Cyp19(化合物iv)的强效混杂抑制剂的修饰表现出中度的r Cyp11B1抑制作用,导致化合物8作为一种新的有前途的先导化合物.与起始点iv相比,对人和大鼠cyp11B1的抑制效力均获得了显着改善(ic 50值分别为2和163 Nm)以及在h Cyp19上的选择性(ic 50 = 1900 Nm).因此,就抑制人和大鼠cyp11B1而言,化合物8的效力比甲吡酮高约7倍和28倍,并且相对于h Cyp11B2表现出相当的选择性(sf为3.5对4.9).随着对该新的先导化合物8的进一步优化,预期将发现具有令人满意的概况的候选药物.
Doi:10.1016/j.Ejmech.2015.04.013

专利信息

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人：MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.

专利号:US-2009318476-A1
优先权日:2006-08-09
标 题 :Azacycloalkane Derivatives as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase
发明人：RAMTOHUL YEEMAM K
权利人:MERCK FROSST CANADA LTD
摘要:Azacycloalkane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis. Formula (I).

专利号:US-2010004245-A1
优先权日:2006-10-20
标 题:Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：OBALLA RENATA M; DESCHENES DENIS; GAGNON MARC; LEBLANC YVES; POWELL DAVID; RAMTOHUL YEEMAN K
权利人:MERCK FROSST CANADA LTD
摘要:Azacycloalkane derivatives of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.

专利号:US-2009099200-A1
优先权日:2005-06-09
标题 :Azacyclohexane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：LI CHUN SING; RAMTOHUL YEEMAN K; HUANG ZHENG; LACHANCE NICOLAS
权利人:LI CHUN SING; RAMTOHUL YEEMAN K; HUANG ZHENG; LACHANCE NICOLAS
摘要:Azacyclohexane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.

专利号:US-2010120784-A1
优先权日:2007-04-20
标题 :Novel heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：LACHANCE NICOLAS; LI CHUN SING; LECLERC JEAN-PHILPPE; RAMTOHUL YEEMAN K
权利人:LACHANCE NICOLAS; LI CHUN SING; LECLERC JEAN-PHILPPE; RAMTOHUL YEEMAN K
摘要:Heteroaromatic compounds of structural formula (I) or a pharmaceutically acceptable salt thereof, wherein W is a substituted heteroaryl, X and Y are each independently a bond, —O—, —S—, —S(O)—, —S(O) 2 —, —NR 6 —, —C(O)—, —C(CH 3 )(OH)— or —C(CH 3 )â•?CH—, u (I) is an integer from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis, obesity, Type 2 diabetes, insulin resistance, hyperglycemia, Metabolic Syndrome, neurological disease, cancer, and liver steatosis

专利号:US-8063224-B2
优先权日:2006-12-01
标 题 :Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：LACHANCE NICOLAS; LI CHUN SING; LECLERC JEAN-PHILIPPE; RAMTOHUL YEEMAN K
权利人:LACHANCE NICOLAS; LI CHUN SING; LECLERC JEAN-PHILIPPE; RAMTOHUL YEEMAN K; MERCK CANADA INC
摘要:Azacycloalkane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.