4-溴-2-氟苯甲酸置于三甲基氯硅烷体系中,用 甲醇 用作溶剂,化学反应 12.0H,以52%的收率获得2-氟-4-溴苯甲酸甲酯 参考文献:Heterocyclic Compounds With Carboxyl Isostere Groups And Their Use For The Treatment Of Cardiovascular Diseases 标题:Heterocyclic Compounds With Carboxyl Isostere Groups And Their Use For The Treatment Of Cardiovascular Diseases 摘要:本申请涉及新颖的杂环化合物,它们的制备方法,它们用于治疗和/或预防疾病的用途,以及它们用于生产用于治疗和/或预防疾病的药物的用途,特别是用于治疗和/或预防心血管疾病.
专利号:US-2022073513-A1 优先权日:2018-12-29 标题:1h-pyrrolo[2,3-b]pyridine derivatives and related compounds as bcl-2 inhibitors for the treatment of neoplastic and autoimmune diseases 发明人:CHEN YI 权利人:NEWAVE PHARMACEUTICAL INC 摘要:The present invention relates to compounds of Formula (II) and more preferably to 1H-pyrrolo[2,3-b]pyridine derivatives of formula (III) and related compounds. The variables are defined in the claims. The compounds are BCL-2 inhibitors for treating neoplastic, autoimmune or neurodegenerative diseases. The present description discloses the synthesis of exemplary compounds as well as pharmacological data thereof (pages 61 to 72; examples 1 to 4; tables). An exemplary compound is e.g. 4-(4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl]piperazin-1-yl)-2-[methyl(1H-pyrrolo[2,3-b]pyridin-5-yl)phosphoroso]-N-[3-nitro-4-[(oxan-4-yl methyl)amino]benzenesulfonyl]benzamide (example 1).
专利号:US-2024400552-A1 优先权日:2016-11-11 标题 :Heterocyclic modulators of lipid synthesis 发明人:BUCKLEY DOUGLAS I; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S 权利人:SAGIMET BIOSCIENCES INC 摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by dysregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).
专利号:US-11622968-B2 优先权日:2011-03-08 标 题:Heterocyclic modulators of lipid synthesis 发明人:BUCKLEY DOUGLAS; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S 权利人:SAGIMET BIOSCIENCES INC 摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).
专利号:US-11034690-B2 优先权日:2016-11-11 标 题:Heterocyclic modulators of lipid synthesis 发明人:BUCKLEY DOUGLAS I; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S 权利人:SAGIMET BIOSCIENCES INC; SAGINIET BIOSCIENCES INC 摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).
专利号:US-9809591-B2 优先权日:2011-03-08 标题 :Heterocyclic modulators of lipid synthesis 发明人:OSLOB JOHAN D; MCDOWELL ROBERT S; JOHNSON RUSSELL; YANG HANBIAO; EVANCHIK MARC; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W 权利人:3-V BIOSCIENCES INC 摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders.
专利号:US-10995078-B2 优先权日:2013-03-13 标 题:Compounds and compositions for inhibition of FASN 发明人:BAIR KENNETH W; LANCIA JR DAVID R; LI HONGBIN; LOCH JAMES; LU WEI; MARTIN MATTHEW W; MILLAN DAVID S; SCHILLER SHAWN E R; TEBBE MARK J 权利人:FORMA THERAPEUTICS INC 摘要:The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:
参考文献:10.1055/s-0029-1219833 摘要:Kula P, Spadło A, Żurowska M, Dąbrowski R. Synthesis of New Chiral Smectic Mesogenes with 4-(2-Phenylethyl)biphenyl and 4-[2-(3-Fluorophenyl)ethyl]biphenyl Molecular Cores. Synlett. 2010 Apr 15;2010(09):1394–6. doi: 10.1055/s-0029-1219833.