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| | United States Patent Application: 0020037828 |
 | | Numerous phosphodiesterase inhibitors have previously been described in the literature for a variety of therapeutic uses, including treatment of obstructive lung disease, allergies, hypertension, angina, congestive heart failure and depression (see, e.g., Goodman and Gilman's The Pharmacological Basis of Therapeutic Ninth Edition, Chapter 34). | | | A pharmaceutical formulation for treating premature ejaculation and adapted for transmucosal drug administration, comprising a therapeutically effective amount of a phosphodiesterase inhibitor and a carrier suitable for transmucosal drug delivery buccally, sublingually, intranasally, rectally, or by inhalation. | | | Another form of transmucosal drug delivery is "urethral" or "transurethral" delivery, referring to delivery of the drug into the urethra such that the drug contacts and passes through the wall of the urethra. |
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http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO2&Sect2=HITOFF&u=/netahtml/PTO/search-adv.html&r=1&f=G&l=50&d=PG01&p=1&S1=20020037828&OS=20020037828&RS=20020037828
(12472 words)
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| | Pulmonary Responses to Selective Phosphodiesterase-5 and Phosphodiesterase-3 Inhibitors -- Matot and Gozal 125 (2): 644 ... |
| | McMahon, TJ, Ignarro, LJ, Kadowitz, PJ Influence of zaprinast on vascular tone and vasodilator responses in the cat pulmonary vascular bed. | | | Thusu, KG, Morin, FC, Russell, JA, et al The cGMP phosphodiesterase inhibitor zaprinast enhances the effect of nitric oxide. | | | Pulmonary Responses to Selective Phosphodiesterase-5 and Phosphodiesterase-3 Inhibitors -- Matot and Gozal 125 (2): 644 -- Chest |
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http://www.chestjournal.org/cgi/content/full/125/2/644
(3032 words)
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| | Potent Medicine: Science News Online, Aug. 20, 2005 |
| | He and his fellow investigators made an animal model of heart failure by surgically constricting the main artery leading out of a mouse's heart. | | | Their findings, the researchers say, suggest that sildenafil can relieve at least one cause of fetal-growth restriction. | | | But for such conditions, he says, "we don't have enough clinical evidence [to] safely start prescribing." |
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http://www.sciencenews.org/articles/20050820/bob9.asp
(2227 words)
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| | Phosphodiesterase-4 Inhibitor Found Promising for COPD - CME Teaching Brief - MedPage Today |
| | The class of phosphodiesterase-4 inhibitors "shows promise as a new therapeutic strategy," Dr. Rabe and colleagues concluded. | | | Roflumilast, on the other hand, was well tolerated, the researchers said. | | | The most common side effect that the researchers thought was likely to be related to the study drug was mild to moderate diarrhea. |
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http://www.medpagetoday.com/Pulmonary/SmokingCOPD/tb1/1527
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| | Patent 6,627,632 |
| | Suitable nonspecific phosphodiesterase inhibitors include IBMX, theophylline, dyphylline theobromine, aminophylline, pentoxifylline, papaverine, caffeine and other methyl xanthine and non-xanthine derivatives (Goodman and Gilman's "The Pharmacological Basis of Therapeutics" The McGraw-Hill Companies, 1996). | | | We found that theophylline relaxed the rat IAS when instilled into the distal anal canal. | | | Inhibitors of phosphodiesterases (PDE), are agents which can block the breakdown of cAMP and cGMP in the tissue. |
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http://www.pharmcast.com/Patents/Yr2003/Sept2003/093003/6627632_Anorectal093003.htm
(8478 words)
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| | Bronchodilator Effect of Inhaled Olprinone, a Phosphodiesterase 3 Inhibitor, in Asthmatic Patients -- MYOU et al. 160 ... |
| | Third Department of Internal Medicine and Laboratory of Medicine, Kanazawa University School of Medicine, Kanazawa, Japan; and Central Laboratory, Kanazawa University Hospital, Kanazawa, Japan | | | Bronchodilator Effect of Inhaled Olprinone, a Phosphodiesterase 3 Inhibitor, in Asthmatic Patients | | | the usefulness of inhaled PDE3 inhibitors in the treatment of |
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http://ajrccm.atsjournals.org/cgi/content/abstract/160/3/817
(280 words)
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| | CHEST: Phosphodiesterase Inhibitor Attenuation of Fibroblast Chemotaxis Depends on Endogenous Prostaglandin Production ... |
| | Abbreviation: [PDE.sub.4] = phosphodiesterase 4 (CHEST 2001; 120:14S-15S) | | | The current study, therefore, demonstrates that the [PDE.sub.4] inhibitor Ariflo is dependent, at least in part, on endogenous cyclooxygenase activity and, presumably, prostaglandin production in order to exert its inhibitory effect on fibroblast chemotaxis. | | | Fibroblasts are the major source of extracellular connective tissue matrix, and the recruitment and activation of these cells are thought to play an important role in wound healing and in the development of fibrosis. |
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http://www.findarticles.com/p/articles/mi_m0984/is_1_120/ai_76994116
(542 words)
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| | HFS: Phosphodiesterase Inhibition Allows Successful Titration Of Beta Blockade In Heart Failure Patients |
| | Four of 15 had expired while taking the phosphodiesterase inhibitor. | | | Though preliminary, the results suggest support with phosphodiesterase inhibitors can ease the titration of patients with advanced heart failure to beta blockade, including patients who fail initial titration, she concluded. | | | Intermittent IV administration of a phosphodiesterase inhibitor allowed successful titration of beta blockade in 73 percent of these patients, Dr. Lawless explained. |
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http://www.docguide.com/dg.nsf/PrintPrint/20E9A8703831BC9B85256AC600491E45
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| | SB 207499 (Ariflo), a Second Generation Phosphodiesterase 4 Inhibitor, Reduces Tumor Necrosis Factor alpha and ... |
| | Deletion of phosphodiesterase 4D in mice shortens {alpha}2-adrenoceptor-mediated anesthesia, a behavioral correlate of emesis | | | Phosphodiesterase 4 inhibitors reduce human dendritic cell inflammatory cytokine production and Th1-polarizing capacity | | | The ability of the second generation phosphodiesterase 4 inhibitor SB 207499 (Ariflo), [c-4-cyano-4-(3-cyclopentyloxy-4-methoxyphenyl)-r-l-cyclohexane |
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http://jpet.aspetjournals.org/cgi/content/abstract/287/2/705
(635 words)
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| | Datamonitor - Altana considers divesting pharma business - Expert Opinion |
| | Datamonitor infectious diseases analyst Lisette Oversteegen weighs up the situation. | | | The growth of Altana's pharmaceuticals arm has been powered by strong sales of its proton pump inhibitor, Pantozol/Protonix (pantoprazole), which generated $1.5 billion in sales in 2004. | | | However, this product is entering the mature sales growth phase, a factor which has contributed to the low 2003-04 growth of 6.5% recorded by the company's pharma arm overall. |
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http://www.datamonitor.com/industries/news/article/?pid=B7616A75-125C-4B90-85FF-AC7936B78CD7&type=ExpertView
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| | [No title] |
| | The PKC inhibitor, staurosporine, antagonized mitogenesis stimulated by ATP. | | | The effects of the kinase inhibitor staurosporine on mitogenesis in NIH/3T3 fibroblasts were characterized. |
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http://www.cs.brandeis.edu/~marc/medstract/inhibitors/inhibitor1.html
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| | Rolipram, a specific type IV phosphodiesterase inhibitor, is a potent inhibitor of HIV-1 replication. |
| | CONCLUSION: Rolipram is a potent inhibitor HIV-1 replication and therefore deserves further investigation as a potential therapeutic agent in the treatment of HIV-1-infected patients. | | | Pentoxifylline is a non-specific phosphodiesterase inhibitor that blocks TNF-alpha synthesis and HIV-1 replication in vitro and has been shown in preliminary clinical studies to decrease viral replication in HIV-1-infected patients. | | | The state of the art may have changed since the publication date. |
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http://www.aegis.com/aidsline/1996/mar/M9630250.html
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| | Effects of amrinone, a phosphodiesterase inhibitor, on right ventricular/arterial coupling immediately after cardiac ... |
| | Yoshie Ochiai, MD Shigeki Morita, MD Yoshihisa Tanoue, MD Yoshito Kawachi, MD Ryuji Tominaga, MD Hisataka Yasui, MD From the Department of Cardiovascular Surgery, Faculty of Medicine, Kyushu University, Fukuoka, Japan. | | | Effects of amrinone, a phosphodiesterase inhibitor, on right ventricular/arterial coupling immediately after cardiac operations -- Ochiai et al. | | | Effects of amrinone, a phosphodiesterase inhibitor, on right ventricular/arterial coupling immediately after cardiac operations |
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http://jtcs.ctsnetjournals.org/cgi/content/abstract/116/1/139
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| | The Effect of Rolipram, a Type IV Phosphodiesterase Inhibitor, on Pseudomonas aeruginosa Infection of Respiratory ... |
| | Clinical studies on the effects of selective PDE inhibitors | | | Brunnee, T., Engelstatter, R., Steinijans, V. and Kunkel, G.: Bronchodilatory effects of inhaled zardaverine, a phosphodiesterase III and IV inhibitor, in patients with asthma. | | | The Effect of Rolipram, a Type IV Phosphodiesterase Inhibitor, on Pseudomonas aeruginosa Infection of Respiratory Mucosa -- Dowling et al. |
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http://www.jpet.org/cgi/content/full/282/3/1565
(4128 words)
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| | phosphodiesterase inhibitor |
| | any substance or agent which suppresses, prevents or opposes the actions or biosynthesis of phosphodiesterases. |
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http://crisp.cit.nih.gov/Thesaurus/00006261.htm
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| | Phosphodiester bonds - Wikipedia, the free encyclopedia |
| | In biological systems, the phosphodiester bond between two ribonucleotides can be broken by alkaline hydrolysis because of the free 2' hydroxyl group. | | | Phosphodiester bonds can be catalyzed by the action of phosphodiesterases which play an important role in repairing DNA sequences. | | | When a single phosphate or two phosphates known as pyrophosphates break away and catalyze the reaction, the phosphodiester bond is formed. |
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http://en.wikipedia.org/wiki/Phosphodiesterase
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| | PJ Online News: Phosphodiesterase inhibitor improves asthma symptoms |
| | Roflumilast, a novel phosphodiesterase 4 inhibitor, is as efficacious as inhaled beclometasone dipropionate in treating asthma, according to data presented at the American Thoracic Society conference. | | | Conference summaries 24 May 31 May 7 June 14 June |
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http://www.pharmj.com/Editorial/20030614/news/asthma.html
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| | Stocks That Make You Breathe Easier [Fool.com: Commentary] July 18, 2005 |
| | But for an investor looking to get in early on emerging new therapies, it's tough to call a winner. | | | Perhaps one of the most interesting companies to watch in this space is Rigel (Nasdaq: RIGL), which is in phase 2 development of its Syk kinase inhibitor R112. | | | The company kept rights to R112 for allergic rhinitis, however, although Pfizer has an option to license that compound on different terms at a later date. |
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http://www.fool.com/news/commentary/2005/commentary05071803.htm?ref=foolwatch
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| | Farmacy Query |
| | PM57:A133: Schussler, M., Fricke, U., Nikolov, N., and Holzl, J. Comparison of the Flavonoids Occurring in Crataegus species and Inhibition of 3',5'-Cyclic Adenosine Monophosphate Phosphodiesterase. | | | TCM10:41: Shin, C. G., Strayer, J. M., Wani, M., Snapka, R. Rapid Evaluation of Topoisomerase Inhibitors: Caffeine Inhibition of Topoisomerases in vivo. |
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http://ww.rain-tree.com/db/Paullinia-cupana-phytochem.htm
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| | Calbiochem: 524714: Phosphodiesterase V Inhibitor II |
| | Second Messengers » Phosphodiesterase Products » Phosphodiesterase Inhibitors | | | -carboline-hydantoin compound that acts as a potent and highly selective phosphodiesterase V inhibitor (IC = 5 nM for bovine aorta PDE V; IC m | | | Calbiochem: 524714: Phosphodiesterase V Inhibitor II Tech Resources |
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http://www.emdbiosciences.com/product/524714
(153 words)
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