| 词条 | Pimagedine |
| 释义 |
|Verifiedfields = changed |Watchedfields = changed |verifiedrevid = 403348066 |ImageFileL1 = Aminoguanidin.svg |ImageFileL1_Ref = {{chemboximage|correct|??}} |ImageNameL1 = Skeletal formula of a pimagedine |ImageFileR1 = Aminoguanidine sf.png |ImageFileR1_Ref = {{chemboximage|correct|??}} |ImageNameR1 = Spacefill model of a pimagedine |IUPACName = 2-Aminoguanidine |OtherNames = {{Unbulleted list|Aminoguanidine|Guanyl hydrazine|Hydrazinecarboximidamide|Imino semicarbazide|Monoaminoguanidine}} |Section1 = {{Chembox Identifiers |IUPHAR_ligand = 5135 |CASNo = 79-17-4 |CASNo_Ref = {{cascite|correct|CAS}} |PubChem = 2146 |ChemSpiderID = 2061 |ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} |UNII = SCQ4EZQ113 |UNII_Ref = {{fdacite|changed|FDA}} |ChEMBL = 225304 |ChEMBL_Ref = {{ebicite|correct|EBI}} |KEGG = D05479 |SMILES = NC(N)N=N |StdInChI = 1S/CH6N4/c2-1(3)5-4/h1,4H,2-3H2 |StdInChI_Ref = {{stdinchicite|changed|chemspider}} |StdInChIKey = DRCHNMARIZRTKI-UHFFFAOYSA-N |StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} }} |Section2 = {{Chembox Properties |C=1 | H=6 | N=4 |LogP = −1.475 |Density = 1.72 g/ml |MolarMass = 74.085 g/mol |BoilingPtC = 261 }} |Section3 = {{Chembox Related |OtherCompounds = Guanidine}} }} Pimagedine, also known as aminoguanidine, is an investigational drug for the treatment of diabetic nephropathy that is no longer under development as a drug.[1] Pimagedine is a diamine oxidase and nitric oxide synthase inhibitor. It acts to reduce levels of advanced glycation end products (AGEs) through interacting with 3-deoxyglucosone. Development as a potential drugPimagedine was under development as a drug for kidney diseases by the pharmaceutical company Alteon (now known Synvista Therapeutics Inc.) that was founded in 1986.[2] In 1987, Alteon acquired a license to intellectual property relating to AGE inhibition from Rockefeller University.[3] In 1989, Alteon and Marion Merrell Dow Inc (MMD) entered into a joint development program for pimagedine.[4] In 1992, Alteon licensed a patent from Rockefeller University relating to the use of pimagedine to inhibit AGE formation.[3] In 1995, Hoechst AG (now sanofi-aventis) acquired MMD and subsequently terminated its agreement with Alteon, which led Alteon to stop of all clinical trials due to lack of funds, which caused some controversy.[4] In 1997, Alteon and Genentech announced a collaboration agreement under which Genentech would fund development of pimagedine and would have the rights to sell the drug if it would be approved.[5] In March 1998, Alteon announced that it had been advised that it should discontinue its Phase III trial of pimagedine in non-insulin-dependent (type II) diabetes patients with overt nephropathy, after the trial's external safety monitoring committee found an increased risk of side effects in the treatment group.[6] In November 1998, Alteon announced that its Phase III trial for pimagedine as a treatment for end stage renal disease had failed to prove efficacy, which led Carl Gordon, a leading biotech analyst, to say: "It looks like pimagedine is probably finished."[7] In February, 1999, Genentech ended its collaboration with Alteon to develop pimagedine.[8] In April 1999 Alteon announced that it would cease development of pimagedine as a treatment for end stage renal disease but might consider continuing development in type 1 diabetic patients with overt nephropathy or progressive kidney disease.[9] Alteon's 2000, 2001, 2002 annual reports indicated that it was not running any clinical trials on pimagedine but was seeking co-development partners.[10][11][12] Alteon's 2003 and subsequent annual reports did not mention that Alteon was seeking partners for pimagenine,[13] which indicated that efforts to interest other companies and investors had failed and which signaled that commercial efforts to develop pimagedine as a drug were indeed finished. References1. ^{{cite journal|journal=Expert Opinion on Investigational Drugs|volume=11|issue=4|pages=565–574|doi=10.1517/13543784.11.4.565|title=Pimagedine: a novel therapy for diabetic nephropathy|author=W Kline Bolton, Emaad Abdel-Rahman|pmid=11922864|year=2002}} {{Nitric oxide signaling}}{{Monoamine metabolism modulators}}{{Hydrazines}}2. ^Synvista Therapeutics Inc. Biocentury. Retrieved August 17, 2017. 3. ^1 {{cite web|title=Alteon 10-K For the fiscal year ended December 31, 1996|url=https://www.sec.gov/Archives/edgar/data/878903/0000893220-97-000614.txt|publisher=Alteon via SEC Edgar|date=March 27, 1997}} 4. ^1 {{cite journal|url=http://www.thelancet.com/journals/lancet/article/PIIS0140-6736(97)26029-0/fulltext|author=Harry Keen|author2=JH Fukker|author3=G Menzinger|title=Early closure of European Pimagedine trial|journal=The Lancet|publisher=PlumX Metrics|volume=350|issue=9072|pages=214–215|date=July 19, 1997|doi=10.1016/S0140-6736(97)26029-0}} 5. ^{{cite news|url=http://articles.latimes.com/1998/jan/03/business/fi-4444 | work=Los Angeles Times|author=Barbara Marsh|title=Biotech's New Watchword: Partnership|date=January 3, 1998|accessdate=August 17, 2017}} 6. ^{{cite web|url=http://www.thepharmaletter.com/file/19466/alteon-may-drop-pimagedine-in-niddm.html|title=Alteon May Drop Pimagedine In NIDDM|publisher=The Pharma Letter|date=March 19, 1998|accessdate=August 17, 2017}} 7. ^{{cite news|url=http://www.sddt.com/News/article.cfm?SourceCode=19981116faq|title=Alteon Shares Plummet On Poor Pimagedine Test Results|publisher=San Diego Source|date=November 16, 1998|accessdate=August 17, 2017}} 8. ^http://business.globe24h.com/sec/001/06/060000/0000060271.shtml {{Dead link|date=August 2017}} 9. ^{{cite web|url=http://www.thepharmaletter.com/file/71571/alteons-pimagedine-fails-primary-endpoint.html|title=Alteon's pimagedine fails primary endpoint|publisher=The Pharma Letter|date=April 12, 1999|accessdate=August 17, 2017}} 10. ^https://www.sec.gov/Archives/edgar/data/878903/0000893220-00-000381.txt 11. ^https://www.sec.gov/Archives/edgar/data/878903/000089322001000240/0000893220-01-000240.txt 12. ^https://www.sec.gov/Archives/edgar/data/878903/000089322002000222/0000893220-02-000222.txt 13. ^https://www.sec.gov/Archives/edgar/data/878903/000089322003000272/0000893220-03-000272.txt 2 : Guanidines|Hydrazines |
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