CAS: 47141-42-4; Levobunolol

上下游产品

5-Hydroxy-1-tetralone tert-butylaminetert-butylamine epichlorohydrin

📜(Rs)-5-(3-Chloro-2-Hydroxypropoxy)-3,4-Dihydronaphthalen-1(2H)-One置于acrylic Resin-Immobilized Lipase From Candida Antarctica L4777,三乙胺体系中,用 乙醇,环己烷 作为反应溶剂,化学反应 48.0H,反应生成 左布诺洛尔
参考文献:脂肪酶介导的 (Rs)-,(R)-和 (S)-布布洛尔的新化学酶合成
标题:脂肪酶介导的 (Rs)-,(R)-和 (S)-布布洛尔的新化学酶合成
摘要:β-肾上腺素能受体阻断剂是一类重要的药物分子.本研究报告了 (Rs)-,(R)-和 (S)-布诺洛尔(一种有效的 β-肾上腺素受体阻滞剂)的新化学和化学酶合成工艺.在化学酶法中,利用cal L4777脂肪酶进行对映选择性动力学拆分,从相应的外消旋醇合成对映体纯(R)-醇和(S)-酯.此后,将相应的(R)-醇和脱酰基化的(S)-酯用叔丁胺处理,分别产生(S)-和(R)-布布洛尔.化学方法中,以环氧氯丙烷(Rs-,R-,S-)为起始原料,分别以(Rs)-,(S)-,(R)-缩水甘油醚为中间体,合成对映体(Rs)-,(R)-和(S)-布洛尔.比较两种方法,发现化学酶法更有效,对映体过量达 98%,产率 35%.
DOI:10.1002/chir.23627

专利信息

专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人：GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-10421873-B2
优先权日:2015-05-25
标 题 :Method for in-site synthesis of transparent conductive coating of poly(3,4-ethylenedioxythiophene)/nano silver
发明人：LI JIANXIONG; MA YAXIAO; LIU ANHUA
权利人:UNIV SOUTH CHINA TECH
摘要:A method for in-site synthesis of transparent conductive coating of poly(3,4-ethylenedioxythiophene)/nano silver hybrid on transparent substrate is provided. Transparent substrate with oxidant coating containing silver salt is immersed into 3,4-ethylenedioxythiophene (EDOT) solution. The oxidant turns EDOT monomer to poly(3,4-ethylenedioxythiophene) (PEDOT) coating on the transparent substrate; meanwhile, the silver salt itself is reduced to nano silver by the EDOT monomer, resulting in a nano silver-doped PEDOT coating. Thereby, a transparent conductive film made of PEDOT/nano silver coating on transparent substrate is obtained. The transparent conductive film with PEDOT/nano silver coating prepared in the present invention possesses the advantages of high electrical conductivity, optical transparency and environmental stability.

专利号:US-2003050305-A1
优先权日:2000-05-22
标题:Thromboxane inhibitors, compositions and methods of use
发明人：TEJADA INIGO SAENZ DE
摘要:The present invention describes methods for treating or preventing sexual dysfunctions in males and females, and for enhancing sexual responses in males and females by administering a therapeutically effective amount of at least one thromboxane inhibitor, and, optionally, 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 vasoactive agent. The male or female may preferably be diabetic. The present invention also provides novel compositions comprising at least one thromboxane inhibitor, 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, optionally, at least one therapeutic agent, such as, vasoactive agents, nonsteroidal antiinflanmmatory compounds (NSAIDs), selective cyclooxygenase-2 (COX-2) inhibitors, anticoagulants, angiotensin converting enzymes (ACE) inhibitors, angiotensin II receptor antagonists, renin inhibitors, and mixtures thereof. The present invention also provides methods for treating or preventing ischemic heart disorders, myocardial infarction, angina pectoris, stroke, migraine, cerebral hemorrhage, cardiac fatalities, transient ischaemic attacks, complications following organ transplants, coronary artery bypasses, angioplasty, endarterectomy, atherosclerosis, pulmonary embolism, bronchial asthma, bronchitis, pneumonia, circulatory shock of various organs, nephritis, graft rejection, cancerous metastases, pregnancy-induced hypertension, preeclampsia, eclampsia, thrombotic and thromboembolic disorders, intrauterine growth, gastrointestinal disorders, renal diseases and disorders, disorders resulting from elevated uric acid levels and dysmenorrhea, and for inhibiting platelet aggregation or platelet adhesion or relaxing smooth muscles.

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:EP-0286447-B1
优先权日:1987-04-09
标题 :Method and agents relating to prophylactic treatment of autoimmune diseases
摘要:Autoimmune diseases are the result of an immune response directed against a self antigen. Susceptibility to an autoimmune disease is conferred by antigen encoded within an allele of the MHC. A potentially susceptible individual is protected from developing the autoimmune disease by an antigen encoded within a second allele of the MHC. Individuals who have the allele for susceptibility, and lack the allele for protection are highly susceptible to manifestation of the autoimmune disease. The present invention provides a method for prophylactically treating individuals who are highly susceptible to an autoimmune disease. In the method, the individuals are tolerized by administration of a protective antigen encoded within the protective allele. As part of the invention, the sequences encoding the protective antigen(s), as well as the antigen(s) conferred susceptibility, are elucidated. The elucidation of these sequences allows for the synthesis of the antigens conferring these traits. These antigens may be used pharmacologically; in addition, they may be used to raise monoclonal antibodies. Monoclonal antibodies to these antigens are useful in diagnosis of susceptibility, and in elucidating the mechanisms by which antigens control the manifestation of the autoimmune disease. In addition, the sequence data allows the synthesis of nucleotide probes which are useful in diagnosis of susceptibility to the autoimmune disease.