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-5094782-A 优先权日:1990-12-24 标 题:Synthesis of capsacin derivatives and their use as an analgesic drug and vessel dilation drug 发明人:CHEN ING-JUN; YEH JWU-LAI 权利人:NAT SCIENCE COUNCIL REPUBLIC CHINA 摘要:Nonanoyl vanillylamide succinate was synthesized from synthetic capsaicin (nonanoyl vanillylamide) and succinic anhydride. The antinociceptive and cardiovascular effects of nonanoyl vanillylamide and its derivatives were investigated. We found that nonanoyl vanillylamide and nonanoyl vanillylamide succinate strongly inhibited the writhing response, led to the vascular smooth muscle relaxation, produces bradycardia and a fall of blood pressure. The potency of nonanoyl vanillylamide succinate was found to be slight greater than that of nonanoyl vanillylamide, when compared with the same molar dose/kg of their administrations.
专利号:US-4158005-A 优先权日:1975-02-10 标题:Intermediates useful in the synthesis of optically active m-acyloxy-α-[(methylamino)methyl]benzyl alcohols 发明人:BODOR NICOLAE S; YUAN SUN-SHINE 权利人:INTERX RESEARCH CORP 摘要:Optically and therapeutically active compounds of the formula: ##STR1## wherein R represents a member selected from the group consisting of a straight or branched alkyl group of from one to twenty carbon atoms (C 1 -C 5 being preferred), an ethoxycarbonyl group, a benzyloxycarbonyl group, a phenyl group, an ##STR2## WHEREIN R is as defined above and R 3 is a member selected from the group consisting of a hydrogen atom, a methyl group and a phenyl group, and a 2-, 3-, or 4-pyridyl group, or the HX salts thereof, wherein X represents a pharmaceutically acceptable acid addition salt anion, are prepared optically active m-hydroxy-α-[methylamino)methyl]benzyl alcohol (phenylephrine). n The compounds prepared by the process of this invention find therapeutic application to warm-blooded animals (e.g., humans) in the management of asthma, nasal congestion and as decongestants, vasoconstrictors, mydriatic agents, and anti-glaucomatous agents in the practice of ophthalmology. n Upon administration, these compounds will enzymatically 'cleave,' thus releasing optically active phenylephrine (m-hydroxy-α-[(methylamino)methyl]benzyl alcohol, the therapeutically active moiety thereof.
专利号:US-4028368-A 优先权日:1975-02-10 标 题:Novel intermediates useful in the synthesis of optically active m-acyloxy-α-[(methylamino)methyl]benzyl alcohols 发明人:BODOR NICOLAE S; YUAN SUN-SHINE 权利人:INTERX RESEARCH CORP 摘要:Optically and therapeutically active compounds of the formula: ##STR1## wherein R represents a member selected from the group consisting of a straight or branched alkyl group of from one to twenty carbon atoms (C 1 -C 5 being preferred), an ethoxycarbonyl group, a benzyloxycarbonyl group, a phenyl group, an ##STR2## group, wherein R is as defined above and R 3 is a member selected from the group consisting of a hydrogen atom, a methyl group and a phenyl group, and a 2-, 3-, or 4-pyridyl group, or the HX salts thereof, wherein X represents a pharmaceutically acceptable acid addition salt anion, are prepared using optically active m-hydroxy-α-[(methylamino)methyl]benzyl alcohol (phenylephrine).
专利号:US-4174450-A 优先权日:1975-02-10 标 题:Intermediates useful in the preparation of optically and therapeutically active-m-acyloxy-(methyl-amino) methyl benzyl alcohols 发明人:BODOR NICOLAE S; YUAN SUN-SHINE 权利人:INTERX RESEARCH CORP 摘要:This invention deals with chemical intermediates having the formula ##STR1## wherein R 1 and R 2 together with the carbon atom to which they are attached form a single hetero atom member selected from the group consisting of a five-to seven-membered heterocycle containing one hetero-N-atom and a N-substituted five-to seven-membered heterocycle containing an hetero-N-atom whose substituent is C 1 -C 2 alkyl. These compounds are useful in the synthesis of compounds having a variety of uses as pharmaceuticals.
专利号:US-8617854-B2 优先权日:2008-09-17 标题 :Method for producing L-phenylephrine using an alcohol dehydrogenase of Aromatoleum aromaticum EBN1 (Azoarcus sp. EBN1) 发明人:BREUER MICHAEL; PLETSCH ANDREAS; HAUER BERNHARD; SIEGEL WOLFGANG 权利人:BREUER MICHAEL; PLETSCH ANDREAS; HAUER BERNHARD; SIEGEL WOLFGANG; BASF SE 摘要:The present invention relates to a multi-stage process for producing substituted, optically active alcohols, comprising an enzyme-catalyzed synthesis step, in particular a synthesis step which is catalyzed by an alcohol dehydrogenase. The inventive method is particularly suitable for producing phenylephrine, i.e. 3-[(1R)-1-hydroxy-2-methylamino-ethyl]-phenol.
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