CAS: 131-03-3; (1S,2S,4As,13Bs,14As)-Methyl 2-Hydroxy-1,2,3,4,4A,5,7,8,13,13B,14,14A-Dodecahydroindolo[2',3':3,4]Pyrido[1,2-B]Isoquinoline-1-Carboxylate

上下游产品

tert-butylatepotassium tert-butylate benzene alloyohimbine rauwolscine hydr°Chloride Yohimbine

📜(4As,13Bs,14As)-1-(1,3-Dithian-2-Ylidene)-3,4,4A,5,7,8,13,13B,14,14Adecahydroindolo[2',3':3,4]Pyrido[1,2-B]Isoquinolin-2(1H)-One置于samarium Diiodide,对甲苯磺酸体系中,用 四氢呋喃,甲醇,二氯甲烷,水 用作溶剂,化学反应 24.17H,反应生成1H-1-苯氮杂卓-1-乙酸,3-氨基-2,3,4,5-四氢-A-甲基-2-羰基-
参考文献:一种用于合成育亨宾生物碱的简明对映选择性方法
标题:一种用于合成育亨宾生物碱的简明对映选择性方法
摘要:我们报告了育亨宾生物碱 (-)-Rauwolscine 和 (-)-Alloyohimbane 的简明,对映选择性合成.关键转化涉及高度对映选择性和非对映选择性 Nhc 催化的二聚化和酰胺化/n-酰基胺离子环化序列,以在两次操作中提供五个必需环中的四个和五个立体中心中的三个.该路线还提供了从常见中间体获得育亨宾生物碱核心立体三联体的所有四种非对映体排列的有效途径.这种平台方法与从卡宾催化反应中获取两种对映异构体的能力相结合,是一种强大的策略,可以为未来的生物医学研究生产各种复杂的生物碱和相关结构.
Doi:10.1021/jacs.9B12319

专利信息

专利号:US-6469065-B1
优先权日:1996-02-02
标 题:Nitrosated and nitrosylated α-adrenergic receptor antagonist, compositions and methods of use
发明人：GARVEY DAVID S; SCHROEDER JOSEPH D; DE TEJADA INIGO SAENEZ; GASTON RICKY D; SHELEKHIN TATIANA E; WANG TIANSHENG
权利人:NITROMED INC
摘要:The present invention describes novel nitrosated and/or nitrosylated α-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated α-adrenergic receptor antagonist, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are a substrate for nitric oxide synthase, and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one α-adrenergic receptor antagonist, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing benign prostatic hyperplasia, hypertension, congestive heart failure, variant (Printzmetal) angina, glaucoma, neurodegenerative disorders, vasospastic diseases, cognitive disorders, urge incontinence, or overactive bladder, and for reversing the state of anesthesia.

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-2005187222-A1
优先权日:1996-02-02
标题:Nitrosated and nitrosylated alpha-adrenergic receptor antagonist compounds
发明人：GARVEY DAVID S; DE TEJADA INIGO S; GASTON RICKY D; KHANAPURE SUBHASH P; SHELEKHIN TATIANA E; WANG TIANSHENG
权利人:NITROMED INC
摘要:The present invention describes novel nitrosated and/or nitrosylated α-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated α-adrenergic receptor antagonist, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are a substrate for nitric oxide synthase, and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one α-adrenergic receptor antagonist, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing benign prostatic hyperplasia, hypertension, congestive heart failure, variant (Printzmetal) angina, glaucoma, neurodegenerative disorders, vasospastic diseases, cognitive disorders, urge incontinence, or overactive bladder, and for reversing the state of anesthesia.

专利号:US-2014134283-A1
优先权日:2012-11-15
标 题:Compositions and Methods for Affecting Mental State and Body Composition
发明人：GEISSLER JACOBO EDWARD; ZHOU JIANG; JIANG YANG; ZHOU LI
权利人:USPLABS LLC
摘要:The invention discloses compositions, including nutritional products and dietary supplements, comprising aegeline, which is a compound that occurs naturally in the Bael plant. The invention also describes methods comprising the administration of aegeline to mammals. The methods result in increased mental stamina, focus, and energy level, improved mood, increased thermogenesis, increased libido, and anabolic effects and increased strength output and/or muscle mass. These effects can improve cognition, influence body composition, promote weight loss, and/or promote fitness and well-being. A novel method for the synthesis of aegeline is also provided.

专利号:US-9403755-B2
优先权日:2013-01-18
标 题:Isometheptene isomer
发明人：LEDERMAN SETH; DAUGHERTY BRUCE; GERSHELL LELAND J; RIDEOUT DARRYL; KAWASAKI ANDREW
权利人:TONIX PHARMACEUTICALS INC; TONIX PHARMA HOLDINGS LTD (BERMUDA)
摘要:The invention relates to a purified Isometheptene compound comprising the structure according to Formula (I), n nor a hydrochloride, or a pharmaceutically acceptable addition salt thereof. In particular, the disclosure relates to the synthesis, purification and characterization of an Isometheptene isomer mucate crystal 2, wherein the Isometheptene isomer 2 is stereochemically characterized as (R)-enantiomer, respectively. The Isometheptene (R)-enantiomer activity indicates a selective centrally acting selective ligand for Imidazoline subtype 1 (I1) receptor sites; and more specifically, the disclosure provides an antihypertensive composition for treatment of migraine and other neurovascular or neurogenic pain from abdominal distress. (R)-Isometheptene enantiomer or isomer 2 may be an anti-hypertensive agent with lower side effects than the racemate form. Therefore (R)-Isometheptene is believed to be effective against episodic tension-type headaches (ETTH). The (R)-Isometheptene enantiomer or isomer 2 is believed to effectively lower blood pressure, used alone or together with other headache ameliorating drugs. Methods of synthesis and treatment are described. Regarding (R)-Isometheptene crystals data of X-ray crystallography are presented.

专利号:US-6620815-B1
优先权日:1997-06-18
标题:Oxazolidinones and uses thereof
发明人：LAGU BHARAT; DHAR T G MURALI; NAGARATHNAM DHANAPALAN; JEON YOON T; MARZABADI MOHAMMAD R; WONG WAI C; GLUCHOWSKI CHARLES
权利人:SYNAPTIC PHARMA CORP
摘要:This invention is directed to oxazolidinone compounds which are selective antagonists for human α 1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the α 1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.