CAS: 171599-83-0; 5-(2-Ethoxy-5-((4-Methylpiperazin-1-yl)Sulfonyl)Phenyl)-1-Methyl-3-Propyl-1H-Pyrazolo[4,3-D]Pyrimidin-7(4H)-One 2-Hydroxypropane-1,2,3-Tricarboxylate

该化合物是一种血管抑制剂,它通过有选择地抑制五型磷化酶(PDE5)酶活动,有效治疗勃起功能障碍,从而增加循环guanosine 单磷酸酯(cGMP)水平,促进肌肉平稳放松,改善血液流向阴茎,促进性...

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citric acid sildenafil 4-[(2-ethoxybenzoyl)amino]-1-methyl-3-propyl-1H-pyrazole-5-carboxamide 1-methyl-4-nitro-3-propyl-1H-pyrazole-5-carboxamide

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    专利信息


    专利号:US-10173993-B2
    优先权日:2015-12-09
    标题 :Process for the synthesis of sulfones and sulfonamides
    发明人:VON WOLFF NIKLAS; CHAR JOËLLE; CANTAT THIBAULT
    权利人:COMMISSARIAT ENERGIE ATOMIQUE
    摘要:A one pot single step process is described for the synthesis of a compound, including a labeled compound, containing a sulfonyl functional group comprising the step of mixing together a silane, an SO 2 source, an electrophilic compound, an activating compound and optionally a metal catalyst. A process for producing tracers from a labeled sulfonyl containing compound prepared by the described process is also included.

    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:WO-2016147205-A1
    优先权日:2015-03-13
    标题 :Novel substituted 3-spirophosphoryl pyrazole-2-oxindoles as anti-infectives and process for the synthesis thereof
    发明人:SURYAVANSHI GURUNATH MALLAPPA; SHELKE ANIL MARUTI
    权利人:COUNCIL SCIENT IND RES
    摘要:The present invention relates to novel substituted 3-spirophosphoryl, pyrazole-2-oxindoles of Formula (I) and its pharmaceutically acceptable salts, esters, ethers, isomers, stereoisomers, positional isomers and pplymorphs. The present invention further relates to one pot, one step process for the synthesis of spirophosphoiyl pyrazole oxindoles of Formula (I) with yield in the range of 70-85%.

    专利号:US-2004137081-A1
    优先权日:2003-01-13
    标题 :Attaining sexual wellness and health of the sexual vascular system with proanthocyanidins
    发明人:ROHDEWALD PETER; FERRARI VICTOR
    摘要:Sexual wellness or sexual fitness is enhanced over time by administrating on a daily basis a source of proanthocyanidins and a source of arginine. Both sources may be blended into a composition or taken separately from a kit. The source of arginine may be a salt or peptide of L-arginine and aspartic acid such as arginine aspartate. The proanthocyanidins stimulate an endothelial NO-synthase enzyme, which serves as a catalyst for synthesis of the nitric oxide from a substration that is the source of the arginine. A sufficient amount of the nitric oxide is released over time to enhance sexual wellness or sexual fitness. In case of low levels of androgenic hormones in both sexes, the combination may contain as a further ingredient a sex hormone or a sex hormone precursor or a sex hormone stimulant or a sex hormone bioavailability enhancer.

    专利号:US-2005171030-A1
    优先权日:2000-05-26
    标题:Relieving symptoms of erectile dysfunction and attaining sexual wellness and health of the sexual vascular system with proanthocyanidins
    发明人:ROHDEWALD PETER; FERRARI VICTOR
    摘要:Sexual wellness or sexual fitness is enhanced over time by administrating on a daily basis a source of proanthocyanidins and a source of arginine. Both sources may be blended into a composition or taken separately from a kit. The source of arginine may be a salt or peptide of L-arginine and aspartic acid such as arginine aspartate. The proanthocyanidins stimulate an endothelial NO-synthase enzyme, which serves as a catalyst for synthesis of the nitric oxide from a substration that is the source of the arginine. A sufficient amount of the nitric oxide is released over time to enhance sexual wellness or sexual fitness. In case of low levels of androgenic hormones in both sexes, the combination may contain as a further ingredient a sex hormone or a sex hormone precursor or a sex hormone stimulant or a sex hormone bioavailability enhancer.

    专利号:US-6565851-B2
    优先权日:2000-05-26
    标题:Relieving symptoms of erectile dysfunction with proanthocyanidins
    发明人:ROHDEWALD PETER; FERRARI VICTOR
    权利人:HORPHAG RES LTD
    摘要:Use of proanthocyanidins as an active ingredient of a stimulator as a source of arginine and a source of nitric oxide in the treatment of erectile dysfunction. The active ingredient stimulates the endothelial NO-synthase enzyme, which acts as a catalyst for the synthesis of nitric oxide from its substrate L-arginine or its salts. The nitric oxide in turn activates theguanylyl cyclase, which leads to an increased development of cyclic guanosine monophosphate, which causes relaxation of smooth muscles. Blood vessel diameter may increase. The stimulator may also have Sildenafil or enzymes that inhibit an enzyme phosphodiesterase type5 from reducing an amount of the cyclic guanosine monophosphate. The substrate may be amino acid L-arginine, arginine salts or a dipeptide of arginine and aspartic acid.
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    主要参考文献


    1: Barzani HAH, Anwar Omer R, Salih Barzani KI, Jawhar ZH, Sulaiman SH. A Critical Review of Analytical Methods for Sildenafil and Its Metabolites. Crit Rev Anal Chem. 2026 Jan
    4:1-35. doi: 10.1080/10408347.2025.2611097. Epub ahead of print. 13(9):2274. doi: 10.3390/biomedicines13092274.
    3: Zhuo ML, Xu JL, Zhang W, Rao GW, Zheng Q. Efficacy of sildenafil combined with statins in treating pulmonary hypertension secondary to chronic obstructive pulmonary disease. Pathol Res Pract. 2025 Sep;273:156097. doi: 10.1016/j.prp.2025.156097. Epub 2025 Jul 20. 317(1):642. doi: 10.1007/s00403-025-04152-8. 17(3):726-739. doi: 10.18632/aging.206222. Epub 2025 Mar 17.

    合成参考文献


    参考文献:10.1007/s10549-010-0765-7
    摘要:Di X, Gennings C, Bear HD, Graham LJ, Sheth CM, White KL, Gewirtz DA. Influence of the phosphodiesterase-5 inhibitor, sildenafil, on sensitivity to chemotherapy in breast tumor cells. Breast Cancer Research and Treatment. 2010 Feb 13;124(2):349–60. doi: 10.1007/s10549-010-0765-7.
    参考文献:10.3109/09638280903511594
    摘要:Pace G, Del Rosso A, Vicentini C. Penile rehabilitation therapy following radical prostatectomy. Disabil Rehabil. 2010;32(14):1204–8. doi: 10.3109/09638280903511594.
    参考文献:10.1556/oh.2010.28800
    摘要:Kopa Z, Romics I. [Therapy of erectile dysfunction]. Orv Hetil. 2010 Feb 27;151(9):354–7. doi: 10.1556/oh.2010.28800.
    参考文献:10.1007/s00213-005-0232-z
    摘要:Devan BD, Bowker JL, Duffy KB, Bharati IS, Jimenez M, Sierra-Mercado D, Nelson CM, Spangler EL, Ingram DK. Phosphodiesterase inhibition by sildenafil citrate attenuates a maze learning impairment in rats induced by nitric oxide synthase inhibition. Psychopharmacology (Berl). 2006 Jan;183(4):439–45. doi: 10.1007/s00213-005-0232-z.
    参考文献:10.1161/circulationaha.111.038885
    摘要:Waxman AB. Pulmonary hypertension in heart failure with preserved ejection fraction: a target for therapy Circulation. 2011 Jul 12;124(2):133–5. doi: 10.1161/circulationaha.111.038885.
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