CAS: 19404-18-3; 5-Chloro-3-Methylbenzo[b]Thiophene

上下游产品

CAS号25784-83-2 (4-氯苯基硫)丙-2-酮 | CAS号106-54-7 4-氯苯硫酚 | CAS号71-43-2 苯 | CAS号78-95-5 氯丙酮 | CAS号1198-51-2 3-溴甲基-5-氯苯并噻吩 | CAS号16296-68-7 5-氯苯并[b]噻吩-3-甲醛

(4-氯苯基硫)丙-2-酮置于polyphosphoric Acid体系中,化学反应生成5-氯-3-甲基苯并噻吩
参考文献:一系列新型2-(苯硫基)苯并[b]噻吩作为选择性mt 2受体配体的制备及药理学评价
标题:一系列新型2-(苯硫基)苯并[b]噻吩作为选择性mt 2受体配体的制备及药理学评价
摘要:合成了一系列的n-(2-(5-氟-2-(4-氟苯硫基)苯并[b]噻吩-3-基)乙基)乙酰胺,并评估了其对褪黑激素受体的结合亲和力和内在活性.通过对在cho细胞中表达的克隆人mt 1和mt 2受体的结合研究,确定了每种化合物对褪黑激素受体的亲和力.在[ 35 S]Gtpγs结合试验中测定了最有趣的化合物的激动剂和拮抗剂的效价.新衍生物8-14显示了轻微的,为mt高选择性(4之间和220)2受体.选择性最高的化合物n-(2-(5-氟-2-(4-氟苯硫基)苯并[b]噻吩-3-基)乙基)丁-3-烯酰胺(14),一个mt 2配体具有亲和力的mt 2类似于受体褪黑激素的作用和相对于mt 1受体的220倍的优先选择,起部分激动剂的作用.另外,N-(2-(5-氟-2-(4-氟苯硫基)苯并[b]噻吩-3-基)乙基)丙酰胺(9),一种具有非常好选择性比的纳摩尔mt 2配体(mt 1 / Mt 2 = 5
Doi:10.1016/j.Ejmech.2011.02.044

专利信息

专利号:WO-9958474-A9
优先权日:1998-05-12
标 题 :Generation of combinatorial libraries of compounds corresponding to virtual libraries of compounds
发明人：GRIFFEY RICHARD; SWAYZE ERIC
权利人:ISIS PHARMACEUTICALS INC; GRIFFEY RICHARD; SWAYZE ERIC
摘要:The present invention provides methods for the generation of virtual libraries of compounds and using these libraries to build combinatorial libraries. The virtual compounds are generated in silico. The present invention encompasses methods for tracking the addition of fragments, use of reagents, and transformations performed. Further, methods for interfacing the information necessary to generate libraries of compounds with instrumentation that conducts the actual synthesis of the compounds are provided.

专利号:EP-1491540-B1
优先权日:2001-03-30
标题 :Intermediates useful for the synthesis of pyridazinone aldose reductase inhibitors

专利号:ES-2274369-T3
优先权日:2001-03-30
标 题:USEFUL INTERMEDIATES FOR SYNTHESIS OF PIRIDAZINONAS INHIBIDORAS OF ALDOSA REDUCTASA.

专利号:US-2006211603-A1
优先权日:2004-08-18
标 题:Ramoplanin derivatives possessing antibacterial activity
发明人：RAJU BORE G; CIABATTI ROMEO; MAFFIOLI SONIA I; SINGH UPINDER; ROMANO GABRIELLA; MICHELUCCI ELENA; TISENI PAOLO S; CANDIANI GIANPAOLO; KIM BUM; O'DOWD HARDWIN
权利人:VICURON PHARM INC
摘要:Novel ramoplanin derivatives are disclosed. These ramoplanin derivatives exhibit antibacterial activity. As the compounds of the subject invention exhibit potent activities against gram positive bacteria, they are useful antimicrobial agents. Methods of synthesis and of use of the compounds are also disclosed.

专利号:US-2009137557-A1
优先权日:2005-11-22
标题 :Calcilytic Compounds
发明人：KU THOMAS WEN FU; LIN HONG; LUENGO JUAN I; MARQUIS JR ROBERT W; RAMANJULU JOSHI M; TROUT ROBERT; YAMASHITA DENNIS S
权利人:KU THOMAS WEN FU; LIN HONG; LUENGO JUAN I; MARQUIS JR ROBERT W; RAMANJULU JOSHI M; TROUT ROBERT; YAMASHITA DENNIS S
摘要:Novel calcilytic compounds, pharmaceutical compositions, methods of synthesis and methods of using them are provided.

专利号:EP-1465880-B1
优先权日:2001-11-28
标题 :5-sulphanyl-4h-1,2,4-triazole derivatives and their use to treat disorders associated with somatostatine
发明人：GALCERA CONTOUR MARIE-ODILE; SIDHU ALBAN; ROUBERT PIERRE; THURIEAU CHRISTOPHE
权利人:IPSEN PHARMA
摘要:The invention concerns novel 5-sulphanyl-4H-1,2,4-triazole derivatives of formula (I), wherein: R1, R2 and R3 represent variable groups and the methods for preparing them by liquid-phase parallel synthesis processes. Said product exhibit good affinity for certain sub-types of somatostatin receptors; they are particularly useful for treating pathological conditions or diseases wherein one (or more) somatostatin receptors is (are) involved. The invention also concerns pharmaceutical compositions containing said products and their use for preparing a medicine.