CAS: 1858276-04-6; ((1R,2S,4R)-4-((5-(4-((R)-7-Chloro-1,2,3,4-Tetrahydroisoquinolin-1-yl)-5-Methylthiophene-2-Carbonyl)Pyrimidin-4-yl)Amino)-2-Hydroxycyclopentyl)Methyl Sulfamate

📜5-甲基-2-噻吩甲醛置于吡啶,盐酸,正丁基锂,磷酸,三溴化磷,Potassium Carbonate,对甲苯磺酸,溶剂黄146体系中,用 四氢呋喃,N-甲基吡咯烷酮,正己烷,二氯甲烷,水,N,N-二甲基甲酰胺,甲苯,乙腈 用作溶剂,化学反应 43.92H,反应生成[(1R,2S,4R)-4-[[5-[[5-[4-((1R)-7-氯-1,2,3,4-四氢异喹啉-1-基)-5-甲基噻吩-2-基]羰基]嘧啶-4-基]氨基]-2-羟基环戊基]甲基磺酸甲酯
参考文献: Heteroaryl Compounds Useful As Inhibitors Of Sumo Activating Enzyme[fr] Composés Hétéroaryle Utiles En Tant Qu'Inhibiteurs De L'Enzyme D'Activation Sumo
标题: Heteroaryl Compounds Useful As Inhibitors Of Sumo Activating Enzyme[fr] Composés Hétéroaryle Utiles En Tant Qu'Inhibiteurs De L'Enzyme D'Activation Sumo
摘要:公开了公式(I)的化合物或其药物可接受的盐; 其中y,Ra,Ra',Rb,Rc,X1,X2,X3,Rd,Z1和z2具有本文所述的值,并且星号位置表示的立体化学配置指示绝对立体化学. 根据本公开的化学实体可用作sumo激活酶(sae)的抑制剂. 进一步提供了包含本公开化合物的药物组合物以及使用该组合物治疗增殖性,炎症性,心血管和神经退行性疾病或病症的方法.

专利信息

专利号:US-6133409-A
优先权日:1996-12-19
标 题:Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and αβ-unsaturated carboxylic acid and aldehyde compounds
发明人：SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F
权利人:AVENTIS PHARM PROD INC
摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and alpha , beta -unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.

专利号:US-3959322-A
优先权日:1960-09-22
标 题:Synthesis of 13-alkyl-gon-4-ones
发明人：HUGHES GORDON ALAN; SMITH HERCHEL
权利人:SMITH HERCHEL
摘要:The preparation of 13-methylgon-4-enes and novel 13-polycarbonalkylgon-4-enes by a new total synthesis is described. 13-Alkylgon-4-enes having progestational, anabolic and androgenic activities are prepared by forming a tetracylic gonane structure unsaturated in the 1,3,5(10),9(11) and 14-positions, selectively reducing in the B- and C-rings, and converting the aromatic A-ring compounds so-produced to gon-4-enes by Birch reduction and hydrolysis.

专利号:WO-2011106929-A1
优先权日:2010-03-02
标题:Inhibitors of hepatitis c virus ns5b polymerase
发明人：MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO
权利人:MERCK SHARP & DOHME; ANGELETTI P IST RICHERCHE BIO; MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO
摘要:Compounds of formula I that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infection and for inhibiting HCV viral replication and /or viral production in a cell-based system.

专利号:US-6229055-B1
优先权日:1996-04-12
标题 :Synthesis of fluorinated xanthene derivatives
发明人：KLAUBERT DIETER H; GEE KYLE R
权利人:MOLECULAR PROBES INC
摘要:Facile syntheses for fluorinated resorcinol and aminophenol derivatives are provided that yield isomer-free products in good yield. These novel methods use generally available precursors and standard laboratory reagents and equipment to reproducibly produce these synthetically useful reagents in relatively large quantities. The resulting fluorinated resorcinols and aniinophenols possess utility in the preparation of fluorinated fluorescein and rhodol dyes.

专利号:US-7897762-B2
优先权日:2006-09-14
标 题:Kinase inhibitors useful for the treatment of proliferative diseases
发明人：FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C
权利人:DECIPHERA PHARMACEUTICALS LLC
摘要:The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.

专利号:US-8188113-B2
优先权日:2006-09-14
标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
发明人：FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C
权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC
摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.