3-DIMENSIONAL PHARMACEUTICALS (DDDP) Message Board

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Biotech / Medical : 3-DIMENSIONAL PHARMACEUTICALS (DDDP)

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To: keokalani'nui who wrote (78)	6/28/2002 9:08:49 PM
From: scaram(o)uche	Read Replies (1) of 146

Thanks for finding that. I'm not a big fan of blockers of viral adhesion, but......... SUMMARY OF THE INVENTION [0038] The present invention is directed to novel tetrahydroisoquinoline-3- -carboxylic acid alkoxyguanidine compounds having Formula I (below). Also provided is a process for preparing compounds of Formula I. The novel compounds of the present invention exhibit inhibition of .alpha..sub.v.beta..sub.3 and .alpha..sub.v.beta..sub.5 integrin receptor binding. Also provided is a method of treating .alpha..sub.v.beta..sub.3 integrin- and .alpha..sub.v.beta..sub.5 integrin-mediated pathological conditions such as tumor growth, metastasis, osteoporosis, restenosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis in a mammal in need of such treatment comprising administering to said mammal an effective amount of a compound of Formula I. Further provided is a pharmaceutical composition comprising a compound of Formula I and one or more pharmaceutically acceptable carriers or diluents. appft.uspto.gov:8080/netacgi/nph-Parser?Sect1=PTO2&Sect2=HITOFF&p=1&u=/netahtml/PTO/search-bool.html&r=6&f=G&l=50&co1=AND&d=PG01&s1='3-Dimensional+Pharmaceuticals'&OS="3-Dimensional+Pharmaceuticals"&RS="3-Dimensional+Pharmaceuticals" and here's the description from the last 10-K..... Antagonists of alpha/v/beta/3/ and alpha/v/beta/5/ Integrins: The integrin adhesion proteins alpha/v/beta/3/ and alpha/v/beta/5/ are essential mediators of the adhesion of cells in tumor angiogenesis (the process by which tumors develop blood vessels), atherosclerosis, restenosis and osteoporosis. We have applied DiscoverWorks to the discovery of potent and selective small molecule antagonists of alpha/v/beta/3/ and alpha/v/beta/5/ and discovered several independent lead series of compounds. Our research has focused on finding selective antagonists which are equipotent at alpha/v/beta/3/ and alpha/v/beta/5/ integrins, thereby inhibiting cell adhesion or attachment as well as the migration of endothelial cells to form blood vessels in tumors. Our lead compounds have been shown to inhibit cellular processes that require functioning of alpha/v/beta/3/ and alpha/v/beta/5/ integrins. They are not cytotoxic and are being evaluated in several different in-vivo models for efficacy and pharmacokinetics. So, remember to buy DDDP hand over fist if they advance a candidate to clinical testing and if MEDI reports a decrease in viral titers in HIV-positive patients with RA? ;-)

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