- ALPHAvBETA1 INTEGRIN ANTAGONISTS
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The present disclosure provides pharmaceutical agents, including those of the formula: (I) wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods of using the pharmaceutical agents are also provided. The compounds may be used for the inhibition or antagonism of integrins ανβ1 and/or α5β1. In some embodiments, the compounds provided herein exhibit reduced inhibitory or antagonistic activity of integrins ανβ3, ανβ5, ανβ6, ανβ8, and/or αIIbβ3.
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- Non-peptidic αvβ3 antagonists containing indol-1-yl propionic acids
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We describe the synthesis and structure/activity relationship of RGD mimetics that are potent inhibitors of the integrin αvβ 3. Indol-1-yl propionic acids containing a variety of basic moieties at the 5-position, as well as substitutions alpha and beta to the carboxy terminus were synthesized and evaluated. Novel compounds with improved potency have been identified.
- Leonard, Kristi,Pan, Wenxi,Anaclerio, Beth,Gushue, Joan M.,Guo, Zihong,DesJarlais, Renee L.,Chaikin, Marge A.,Lattanze, Jennifer,Crysler, Carl,Manthey, Carl L.,Tomczuk, Bruce E.,Marugan, Juan Jose
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p. 2679 - 2684
(2007/10/03)
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- Substituted indoles and their use as integrin antagonists
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The present invention relates to novel substituted indole compounds that are antagonists of alpha V (αv) integrins, for example αvβ3 and αvβ5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by αvβ3 and αvβ5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, D, X, W, a, m, n, i, j, k and v are defined herein.
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