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diethyl cyclopropane-1,1-dicarboxylate 1,1-cyclopropanedimethanol diacetate cyclopropane-1,1-dicarboxylic acid methylidenecyclobutane 1,1-bis(bromomethyl)cyclopropane 1,1-bis-benzenesulfonyloxymethyl-cyclopropane 1‐(hydroxymethyl)cyclopropane‐1‐carboxylic acid 5,7-dioxa-6-thia-spiro[2.5]°Ctane 6-oxide 合成工艺路线路线简述
- 合成目标产物 1,1-Bis(Hydroxymethyl)Cyclopropane 主要起始原料 Diethyl 1,1-Cyclopropanedicarboxylate And Water
- (文献来源)合成步骤主要原料 Diethyl 1,1-Cyclopropanedicarboxylate 和 Water
1,1-环丙基二羧酸置于lithium Aluminium Tetrahydride体系中,用 四氢呋喃 用作溶剂,化学反应 4.0H,反应生成1,1-环丙烷二甲醇
参考文献:的结构-活性关系研究β氧化作用抗性基于吲哚-5-氧代6,8,11,14二十碳四烯酸(5-氧代ete)受体拮抗剂
标题:的结构-活性关系研究β氧化作用抗性基于吲哚-5-氧代6,8,11,14二十碳四烯酸(5-氧代ete)受体拮抗剂
摘要:5-Oxo-6,8,11,14-二十碳四烯酸(5-Oxo-Ete)由5 S-羟基-6,8,11,14-二十碳四烯酸(5-Hete)通过5-脂氧合酶( 5-Lo)途径在与氧化应激相关的条件下.5-Oxo-Ete是重要的促炎介质,它通过选择性的g蛋白偶联受体oxe受体(oxe-R)刺激嗜酸性粒细胞的迁移.以前,我们设计并合成了5-Oxo-Ete的结构模拟物,例如1使用吲哚支架.在目前的工作中,我们在该部分的c-3处添加了各种取代基,以阻断5-氧代戊酸酯侧链的潜在β-氧化,并研究了所得新型β-抗氧化拮抗剂的结构-活性关系.环丙基和环丁基取代基在该位置具有非常好的耐受性,但作为高活性3 S-甲基化合物的效力较低.3-烷基取代基似乎可以影响含有关键的酮基和羧基的5-氧戊酸侧链的构象,从而影响与oxe-受体的相互作用.
Doi:10.1016/j.Bmcl.2017.08.034
专利信息
专利号:US-9718807-B2
优先权日:2012-06-05
标 题 :Synthesis of antiviral compound
发明人:SCOTT ROBERT WILLIAM; VITALE JUSTIN PHILIP; MATTHEWS KENNETH STANLEY; TERESK MARTIN GERALD; FORMELLA ALEXANDRA; EVANS JARED WAYNE
权利人:GILEAD PHARMASSET LLC
摘要:The present disclosure provides processes for the preparation of a compound of formula I: n nwhich is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula I.
专利号:US-8022235-B2
优先权日:2007-06-01
标 题 :Compositions of phospholipid ether boronic acids and esters and methods for their synthesis and use
发明人:PINCHUK ANATOLY; WEICHERT JAMEY P; LONGINO MARC
权利人:CELLECTAR INC
摘要:The present invention discloses boronic acids and esters of phospholipid ether analogs and methods for their synthesis and use. The boronic acids and esters of phospholipid ether analogs described herein can be used in treating cancer and in particular can be used in conjunction with radiation therapy, such as external beam radiation therapy and neutron capture therapy to specifically target and kill cancer cells.
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:CA-2875508-C
优先权日:2012-06-05
标 题:Synthesis of hepatitis c antiviral fluorenyl-benzimidazole derivatives compounds
专利号:US-8633182-B2
优先权日:2012-05-30
标题:Indanyloxyphenylcyclopropanecarboxylic acids
发明人:HAMPRECHT DIETER; FRATTINI SARA; LINGARD IAIN; PETERS STEFAN
权利人:HAMPRECHT DIETER; FRATTINI SARA; LINGARD IAIN; PETERS STEFAN; BOEHRINGER INGELHEIM INT
摘要:The present invention relates to compounds of general formula I, n nwherein the groups R 1 , R 2 , R 3 , m and n are defined as in claim 1 , which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
专利号:US-11780834-B2
优先权日:2018-06-21
标题:Solid forms of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3- yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol and processes for preparing fused tricyclic compounds comprising a substituted phenyl or pyridinyl moiety, including methods of their use
发明人:CHUNG CHEOL KEUN; XU JIE; IDING HANS; CLAGG KYLE; DALZIEL MICHAEL; FETTES ALEC; GOSSELIN FRANCIS; LIM NGIAP-KIE; MCCLORY ANDREW; ZHANG HAIMING; CHAKRAVARTY PAROMA; NAGAPUDI KARTHIK; ROBINSON SARAH
权利人:HOFFMANN LA ROCHE; GENENTECH INC
摘要:Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.