专利号:WO-2015109451-A1 优先权日:2014-01-22 标 题 :Synthesis of compounds containing 8-oxa-3-azabicyclo (3.2.1)octane ring 发明人:LI PENG; DECAMPO FLORYAN; SHI FENG; CUI XINJIANG; YUAN HANGKONG 权利人:RHODIA OPERATIONS; LANZHOU INSTITUTION OF CHEMICAL PHYSICS CHINESE ACADEMY OF SCIENCE 摘要:The present invention mainly pertains to catalytic processes for the direct amination of 2, -bis(hydroxymethyl) tetrahydrofuran to obtain compounds containing the 8-oxa-3-azabicyclo (3.2.1) octane ring, in the presence of: a homogenous catalyst which is a complex comprising at least one element selected from the group consisting of Iridium or Ruthenium and at least one donor ligand, or a heterogeneous catalyst comprising at least one Group 8-11 transition metal element and one poor metal element in the p-block of the period table.
专利号:US-11766432-B2 优先权日:2018-07-27 标题 :Cleavable conjugates of catechol compounds and water-soluble polymers and methods of treatment using the same 发明人:BENTLEY MICHAEL; FANG ZHIHAO; WEIMER REBECCA; VIEGAS TACEY; MOREADITH RANDALL 权利人:SERINA THERAPEUTICS INC 摘要:Described are conjugates comprising a water-soluble polymer linked to a compound comprising a catechol moiety via a cleavable linkage, wherein the cleavable linkage is formed between the water-soluble polymer and a first phenolic hydroxyl group of the catechol moiety and a second phenolic hydroxyl group of the catechol moiety is linked to a blocking group wherein the rate of hydrolytic release of the compound comprising the catechol moiety is controlled, at least in part, through structure or design of the blocking group on the second phenolic hydroxyl group of the catechol moiety. Therefore, the rate of hydrolytic release of the compound comprising the catechol moiety can be tuned through structural design of the group on the second phenolic hydroxyl group of the catechol moiety. Compounds used in the synthesis of the described conjugates and methods of using the described conjugate and other compounds in the treatment of dopamine-responsive disorders are also described.
专利号:US-2011319644-A1 优先权日:2006-11-02 标 题:Process for production of 1-hydroxy-19-norcyclovitamin d derivative and intermediate for the production 发明人:TOYODA ASAKO; NAGAI HAZUKI; KONUKI KANAME; TSUCHIDA TOSHIO 权利人:TOYODA ASAKO; NAGAI HAZUKI; KONUKI KANAME; TSUCHIDA TOSHIO 摘要:A cyclovitamin D derivative produced from 25-hydroxyvitamin D is reacted with osmium tetraoxide or a permanganic acid salt to produce a 10,19-diolcyclovitamin D derivative. The 10,19-diolcyclovitamin D derivative is reacted with a perhalogenic acid salt or lead tetraacetate to produce a 10-oxocyclovitamin D derivative. A 1-hydroxycyclovitamin D derivative is produced from the 10-oxocyclovitamin D derivative via a cyclovitamin D derivative and a 1,10-olefincyclovitamin D derivative. The 1-hydrocyclovitamin D derivative is subjected to solvolysis, thereby producing a 1-hydroxy-19-norviatmin D derivative. Thus provided are a novel process for production of 1-hydroxy-19-norcyclovitamin D derivative that is utilizable as an intermediate in the synthesis of 1-hydroxy-19-norvitamin D derivative which is useful as a pharmaceutical agent; and an intermediate for the production.
专利号:US-6989401-B2 优先权日:2000-07-19 标题:Sulfonic acid derivatives of hydroxamic acids and their use as medicinal products 发明人:MAEDA KAZUHIRO; SONDA SHUJI; TAKEMOTO TADAHIRO; GOTO TOMOKAZU; KOBAYASHI FUJIO; KAJII MASAHIKO; KOMORITA NARUYASU; HIRAYAMA FUMIHIRO 权利人:MITSUBISHI PHARMA CORP 摘要:The present invention relates to a novel sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable salt thereof. More particularly, the present invention relates to a sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable salt thereof, which is useful as an inhibitor of lipopolysaccharides (LPS). In addition, the present invention relates to a novel intermediate compound useful for the synthesis of this sulfonic acid derivative of hydroxamic acid.
专利号:US-8158362-B2 优先权日:2005-03-30 标题:Methods of diagnosing susceptibility to myocardial infarction and screening for an LTA4H haplotype 发明人:HELGADOTTIR ANNA; HAKONARSON HAKON; GULCHER JEFFREY R; GURNEY MARK E 权利人:HELGADOTTIR ANNA; HAKONARSON HAKON; GULCHER JEFFREY R; GURNEY MARK E; DECODE GENETICS EHF 摘要:Polymorphisms in the FLAP and LTA4H gene are shown by genetic association analysis to be susceptibility markers for myocardial infarction (MI) and ACS, as well as stroke and PAOD. Pathway targeting for treatment and diagnostic applications in identifying those who are at risk of developing MI, ACS, stroke or PAOD, in particular are described. The invention also provides methods of prophylaxis therapy for MI in human subjects having a race including black African ancestry by administering to the subject a composition comprising a therapeutically effective amount of MI therapeutic agent that inhibits leukotriene synthesis in vivo. The invention also provides for compositions comprising a leukotriene synthesis inhibitor and a statin and methods of using these compositions to reduce C-reactive protein in a human subject at risk of MI, ACS, stroke and/or PAOD.
专利号:US-2010216863-A1 优先权日:2004-01-30 标 题 :Susceptibility Gene for Myocardial Infarction, Stroke, and PAOD; Methods of Treatment 发明人:HELGADOTTIR ANNA; HAKONARSON HAKON; GULCHER JEFFREY R; GURNEY MARK E 权利人:DECODE GENETICS EHF 摘要:Polymorphisms in the FLAP and LTA4H gene are shown by genetic association analysis to be susceptibility markers for myocardial infarction (MI) and ACS, as well as stroke and PAOD. Pathway targeting for treatment and diagnostic applications in identifying those who are at risk of developing MI, ACS, stroke or PAOD, in particular are described. The invention also provides methods of prophylaxis therapy for MI in human subjects having a race including black African ancestry by administering to the subject a composition comprising a therapeutically effective amount of MI therapeutic agent that inhibits leukotriene synthesis in vivo. The invention also provides for compositions comprising a leukotriene synthesis inhibitor and a statin and methods of using these compositions to reduce C-reactive protein in a human subject at risk of MI, ACS, stroke and/or PAOD.