专利号:US-3968112-A 优先权日:1974-08-02 标 题:Synthesis of penniclavine and elymoclavine 发明人:KORNFELD EDMUND C; BACH NICHOLAS J 权利人:LILLY CO ELI 摘要:Synthesis of penniclavine and of elymoclavine, intermediates useful therein, and novel compounds producible therefrom.
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-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:EP-0354945-B1 优先权日:1988-01-13 标 题 :Process for the enhancement of enzyme activities and synthetic efficiency in microorganisms and higher plants 发明人:FIEDLER FRANZ; ZENK MEINHART H; GUNDLACH HEIDRUN; WEBER ALFRED; KENNECKE MARIO 权利人:SCHERING AG 摘要:In the process disclosed, the organisms are brought into contact witn inactivated elicitor-containing microorganisms, fragments of the latter, or excretions of elicitor-containing microorganisms. Only inactivated elicitor-containing bacteria, fragments of the latter, or excretions of elicitor-containing bacteria may be used to activate enzymes and promote synthesis in non-microbial organisms. The process can be used, for example, to promote synthesis in microorganisms or plants which produce pigments, antibiotics, alkaloids or phytoalexins or to activate enzymes in microorganisms capable of transforming steroids.
专利号:DE-1795023-C2 优先权日:1967-08-02 标 题 :Process for the production of 2-benzyloxy-2-isopropylmalonic acid diethyl ester and its use for the production of heterocycles for the total synthesis of reptide alkaloids of ergot
专利号:US-4082753-A 优先权日:1976-02-17 标题:Penniclavine acetonide 发明人:KORNFELD EDMUND C; BACH NICHOLAS J 权利人:LILLY CO ELI 摘要:Synthesis of penniclavine and of elymoclavine, intermediates useful therein, and novel compounds producible therefrom.
1: Cherewyk JE, Parker SE, Blakley BR, Al-Dissi AN. Sustained vascular contractile response induced by an R- and S-epimer of the ergot alkaloid ergocristine and attenuation by a noncompetitive antagonist. J Anim Sci. 2022 Sep 1;100(9):skac235. doi: 10.1093/jas/skac235. 2: Rudolph W, Remane D, Wissenbach DK, Peters FT. Comparative study on the metabolism of the ergot alkaloids ergocristine, ergocryptine, ergotamine, and ergovaline in equine and human S9 fractions and equine liver preparations. Xenobiotica. 2019 Oct;49(10):1149-1157. doi: 10.1080/00498254.2018.1542187. Epub 2019 Jan 9. 1117:127-135. doi: 10.1016/j.jchromb.2019.04.016. Epub 2019 Apr 5. 1(1):23-33. doi: 10.1111/j.1472-8206.1987.tb00542.x. 232(2):249-56. doi: 10.1007/BF00213784. 57(11):1313-6. doi: 10.1139/y79-195.
合成参考文献
摘要: 摘要: 摘要:Franke C et al; Chemosphere 29: 1501-14 (1994) 参考文献:10.1002/rcm.2648 摘要:Mohamed R, Gremaud E, Tabet JC, Guy PA. Mass spectral characterization of ergot alkaloids by electrospray ionization, hydrogen/deuterium exchange, and multiple stage mass spectrometry: Usefulness of precursor ion scan experiments. Rapid Commun Mass Spectrom. 2006;20(19):2787–99. doi: 10.1002/rcm.2648.