CAS: 96125-53-0; Clentiazem

上下游产品

(+)-(2S,3S)-Cis-8-Chloro-5-<2-(Dimethylamino)Ethyl>-2,3-Dihydro-3-Hydroxy-2-(4-Methoxyphenyl)-1,5-Benzothiazepin-4(5H)-One 96125-25-6
(+)-(2S,3S)-8-Chloro-2,3-Dihydro-3-Hydroxy-2-(4-Methoxyphenyl)-1,5-Benzothioazepin-4(5H)-One 96142-63-1

📜(+)-(2S,3S)-8-Chloro-2,3-Dihydro-3-Hydroxy-2-(4-Methoxyphenyl)-1,5-Benzothioazepin-4(5H)-One置于4-二甲氨基吡啶,Potassium Carbonate体系中,用 N,N-二甲基甲酰胺,甲苯 作为反应溶剂,化学反应 4.0H,反应生成 克仑硫卓
参考文献:芳基 α-氯 β-酮酯的生物催化动态还原动力学拆分:地尔硫卓,克林硫卓和西拉硫卓的发散立体控制合成
标题:芳基 α-氯 β-酮酯的生物催化动态还原动力学拆分:地尔硫卓,克林硫卓和西拉硫卓的发散立体控制合成
摘要:对芳基 α-氯 β-酮酯进行酮还原酶 (Kred) 催化的动态还原动力学拆分 (Dyrkr) 的首次系统研究,并在 74-98% 的分离产率,以及中等至优异的非对映选择性(高达 >99 : 1 Dr)和非常好至优异的对映选择性(大部分 >99% Ee).lfsdr1 催化完全还原 10 克规模的 100 G L-1底物6B是通过连续补料分批策略实现的,在破纪录的时空产量 96 G L-1 D-1. 地尔硫卓,克林特西姆和西拉硫卓的八步合成以 32-45% 的总收率完成,具有这种多功能的生物催化还原反应以及高效,绿色的流动氯化反应.
DOI:10.1039/d2Cc03102G

专利信息

专利号:US-2008287407-A1
优先权日:2003-12-10
标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
发明人：GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

专利号:US-7708989-B2
优先权日:1999-10-29
标题 :Methods of treating vascular diseases characterized by nitric oxide insufficiency
发明人：LOSCALZO JOSEPH; VITA JOSEPH A; LOBERG MICHAEL D; WORCEL MANUEL
权利人:NITROMED INC
摘要:The invention provides methods of treating and/or preventing vascular diseases characterized by nitric oxide insufficiency by administering a therapeutically effective amount of at least one nitrosated angiotensin-converting enzyme inhibitor, nitrosated beta-adrenergic blocker, nitrosated cholesterol reducer, nitrosated calcium channel blocker, nitrosated endothelin antagonist, nitrosated angiotensin II receptor antagonist, nitrosated renin inhibitor, and optionally at least one compound used to treat cardiovascular diseases and/or at least one antioxidant, or a pharmaceutically acceptable salt thereof, and/or at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof. The compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase may preferably be isosorbide dinitrate and/or isosorbide mononitrate. The vascular diseases characterized by nitric oxide insufficiency include a cardiovascular disease and a disease resulting from oxidative stress.

专利号:US-7384976-B2
优先权日:2001-05-02
标 题:Nebivolol and its metabolites in combination with nitric oxide donors, compositions and methods of use
发明人：GARVEY DAVID S
权利人:NITROMED INC
摘要:The invention describes novel compositions comprising nebivolol and/or at least one metabolite of nebivolol and at least one nitric oxide donor, and, optionally, at least one antioxidant or a pharmaceutically acceptable salt thereof, and/or at least one compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof, and/or at least one nitrosated compound used to treat cardiovascular diseases. The compounds and compositions of the invention can also be bound to a matrix. The nitric oxide donor is a compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and may preferably be isosorbide dinitrate and/or isosorbide mononitrate. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof. The invention also provides methods for treating and/or preventing vascular diseases characterized by nitric oxide insufficiency; and for treating and/or preventing Raynaud's syndrome; and for treating and/or preventing cardiovascular diseases or disorders.

专利号:US-2008214827-A1
优先权日:2004-02-03
标 题:Synthesis of Cyanoimino-Benzoimidazoles
发明人：GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
权利人:EURO CELTIQUE SA
摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

专利号:EP-0415384-B1
优先权日:1989-08-31
标题 :Heterogeneous synthesis of azepinones from esters
发明人：MARTIN DANIEL E
权利人:HOECHST MARION ROUSSEL INC
摘要:An amino-acid ester compound can be cyclized into a cyclic amido-carbonyl compound by contacting the amino-acid ester compound in a liquid medium with a heterogeneous acidic ion-exchange substance. For example, 2-hydroxy-3-(2-aminophenylthio)-3-(4-methoxyphenyl)propionic acid, methyl ester, threo form, can be cyclized in an aqueous mixture into cis-2-(4-methoxyphenyl)-3-hydroxy-2,3-dihydro-1,5-benzothiazepin-4(5H) -one by employing a sulfonated polystyrene-divinylbenzene ion-exchange resin in its acid form, e.g., Dowex 50X4-400, at yields exceeding 85 percent of theory, and the product can be used to make diltiazem hydrochloride.

专利号:US-7235237-B2
优先权日:1999-10-29
标 题 :Methods of treating vascular diseases characterized by nitric oxide insufficiency
发明人：LOSCALZO JOSEPH; VITA JOSEPH A; LOBERG MICHAEL D; WORCEL MANUEL
权利人:NITROMED INC
摘要:The present invention provides methods of treating or preventing vascular diseases caused by nitric oxide (NO) insufficiency. The methods encompass administering a composition comprising an antioxidant, a compound to treat cardiovascular diseases, a nitrosated compound, a compound that donates, transfers or relases NO, or is a NO synthase substrate, or endogenously stimulates NO synthesis, or stimulates levels of endothelium derived relaxing factor. In the said composition, a hydralazine compound may be an antioxidant, isosorbide mono-or dinitrate may be the compound to donate, transfer, release, or stimulate endogenous NO synthesis. The isorsorbide may also elevate endogenous levels of endotherlium-derived relaxing factor, or be a NO synthase substrate and angiotensin enzyme inhibitor may be nitrosated compound. Disclosed in the invention is also a method to treat, or prevent Renaud's syndrome by administering a therapeutically effective amount of an antioxidant, a NO donor, a nitrosated compound and novel sustained-release formulations (e.g. a transdermal patch).