CAS: 137-58-6; Lidocaine

上下游产品

CAS号109-89-7 二乙胺 | CAS号1131-01-7 2,6-二甲基氯代乙酰苯胺 | CAS号87-62-7 2,6-二甲基苯胺 | CAS号109366-65-6 2-(Diethylamino... | CAS号2903-45-9 利多卡因N-氧化物 | CAS号39942-41-1 4-Hydroxylid°Caine | CAS号34604-55-2 3'-hydroxy Lid°Caine | CAS号7728-40-7 去乙基利多卡因 | CAS号18865-38-8 甘氨酸二甲基苯胺 | CAS号34604-56-3 3-Hydroxy-N-des... | CAS号39942-49-9 3-Nitro Lid°Caine | CAS号1044658-01-6 3-Bromo Lid°Caine

2-(N-Ethylacetamido)2',6'-Dimethylacetanilide置于硼烷四氢呋喃络合物体系中,用 四氢呋喃 用作溶剂,以176 Mg的收率获得利多卡因
参考文献:1,3,5-三嗪酮类药物在ugi反应中作为福尔马胺替代品
标题:1,3,5-三嗪酮类药物在ugi反应中作为福尔马胺替代品
摘要:1,3,5-三嗪酮被用作ugi反应中易于操作,稳定的福尔马胺替代物,用于快速组装具有多样性的三种多样性的甘氨酰胺衍生物,收率接近定量.该方案适用于利多卡因和几种不对称取代的二酮哌嗪的一锅两步合成法.
Doi:10.1002/ejoc.202000569

专利信息

专利号:US-2017348280-A1
优先权日:2016-06-06
标题 :Counteracting the inhibition of collagen synthesis by select calcium and sodium channel blockers using ascorbic acid and ascorbyl palmitate
发明人：RATH MATTHIAS W; NIEDZWIECKI ALEKSANDRA; IVANOV VADIM O; IVANOVA SVETLANA V
权利人:RATH MATTHIAS W; NIEDZWIECKI ALEKSANDRA; IVANOV VADIM O; IVANOVA SVETLANA V
摘要:A therapeutic use of ascorbyl palmitate, ascorbic acid and/or derivatives thereof to reverse or counter the adverse effects of channel blockers in the medical management of cardiovascular disease in a subject is presented. Effects of select Na- and Ca-channel blockers on collagen synthesis and deposition were evaluated in cultured human dermal fibroblasts and aortic smooth muscle cells by immunoassay. Ca and Na-channel blockers inhibited the synthesis of collagen type I and collagen type IV, the basic molecules of vascular wall stability. The inhibitory effects of the calcium and sodium channel blockers on collagen synthesis was reversed by introducing ascorbic acid and/or ascorbyl palmitate. It can be concluded that calcium and sodium channel blockers have a direct inhibitory effect on collagen synthesis, favoring the instability of the vascular wall and the progression of cardiovascular disease, an effect that is mitigated by treatment with, ascorbyl palmitate, ascorbic acid and or derivatives thereof.

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-12129222-B2
优先权日:2016-08-11
标题:Production of bitter principle derivatives
发明人：WYRWA RALF; RODE CLAUDIA; SEEMANN THOMAS; MEINEL LORENZ; RITZER JENNIFER; SCHNABELRAUCH MATTHIAS
权利人:UNIV WUERZBURG J MAXIMILIANS; JULIUS MAXIMILIANS UNIV
摘要:It is an object of the present invention to introduce carboxylic acid-functionalities suitable for coupling into the denatonium structure by means of simple synthesis, namely the synthesis of bitter principle derivatives based on the denatonium structure according to formula 1:For example, according to the invention, lidocaine derivatives may be reacted with carboxylated benzyl halogenides. The carboxylated denatonium derivatives of the present invention are especially applied in medicine, biology, medical engineering as well as cosmetics, the pharmaceutical, chemical, and foodstuff industry.

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-6436997-B1
优先权日:1998-06-01
标题 :Endogenous nitric oxide synthesis under conditions of low oxygen tension
发明人：DE TEJADA INIGO SAENZ
权利人:NITROMED INC
摘要:The present invention provides methods of promoting synthesis of nitric oxide or endothelium-derived relaxing factor (EDRF) in hypoxic mammalian tissues by administering at least one N-hydroxyguanidine compound that is a substrate of nitric oxide synthase, and, optionally, one or more vasoactive agents and/or thromboxane A2 receptor antagonists. The present invention also provides methods of promoting vasorelaxation and treating sexual dysfunctions in patients by administering at least one N-hydroxyguanidine compound that is a substrate for nitric oxide synthase, and, optionally, at least one vasoactive agent and/or thromboxane A2 receptor antagonist. The present invention also provides methods for treating clinical conditions resulting from hypoxic conditions such as pulmonary disease, cardiovascular disorders, circulatory hypoxia, specific organ hypoxia, localized hypoxia, edema, central nervous system disorders, memory loss, or arterial disease. The present invention also provides methods for treating clinical conditions resulting from an abnormally high level of arginase activity, such as, heart disease, systemic hypertension, pulmonary hypertension, sexual dysfunction, autoimmune disease, chronic renal failure and cerebral vasospasm. The present invention also provides methods for treating clinical conditions associated with a deficient nitric oxide pathway by administering at least one N-hydroxyguanidine compound and, optionally, one or more vasoactive agents and/or thromboxane A2 receptor antagonists. The present invention also provides pharmaceutical compositions comprising at least one N-hydroxyguanidine compound, and, optionally, one or more vasoactive agents and/or thromboxane A2 receptor antagonists.

专利号:US-6693122-B2
优先权日:1999-05-12
标题:Nitrosated and nitrosylated potassium channel activators, compositions and methods of use
发明人：GARVEY DAVID S; SAENZ DE TEJADA INIGO
权利人:NITROMED INC
摘要:The present invention describes novel nitrosated and/or nitrosylated potassium channel activators, and novel compositions comprising at least one nitrosated and/or nitrosylated potassium channel activator, 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 present invention also provides novel compositions comprising at least one potassium channel activator, 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 vasoactive agent. 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 cardiovascular disorders, cerebrovascular disorders, hypertension, asthma, baldness, urinary incontinence, epilepsy, sleep disorders, gastrointestinal disorders, migraines, irritable bowel syndrome and sensitive skin.